MedWorm: Diltiazem

  Assessment -Symptomatic treatment for muscle cramps -an evidence-based review

Bottom-line conclusion: Although likely effective (Level A), quinine derivatives should be avoided for routine use in the management of muscle cramps because of the potential of toxicity, but in select patients they can be considered for an individual therapeutic trial once potential side effects are taken into account. Vitamin B complex, Naftidrofuryl, and calcium channel blockers such as diltiazem are possibly effective and may be considered in the management of muscle cramps (Level C). Further studies are needed to identify agents that are effective and safe for the treatment of muscle cramps. (Source: Neurological Conditions Specialist Library)

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  DILTIAZEM HYDROCHLORIDE (Diltiazem) Tablet, Film Coated [Physicians Total Care, Inc.]

Updated Date: Mar 10, 2010 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  DILTIAZEM HYDROCHLORIDE (Diltiazem) Capsule, Extended Release [Physicians Total Care, Inc.]

Updated Date: Mar 9, 2010 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  DILTIAZEM HYDROCHLORIDEcapsule, Extended Release DILTIAZEM HYDROCHLORIDEcapsule, Extended Release [TEVA Pharmaceuticals USA Inc.]

Updated Date: Mar 5, 2010 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  TIAZAC EXTENDED RELEASE (Diltiazem Hydrochloride) Capsule, Extended Release [Forest Laboratories, Inc.]

Updated Date: Mar 4, 2010 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  [Local treatment of a chronic anal fissure with diltiazem vs. nitroglycerin. A comparative study.]

CONCLUSIONS: Smooth muscle relaxant drugs do not achieve a higher cure rate than the traditional measures used in CAF, but offer more symptomatic relief, providing an opportunity to avoid surgery. Topical diltiazem does not have the side effects of the nitroglycerin and is better accepted by patients. PMID: 20206340 [PubMed - as supplied by publisher] (Source: Cirugia eEspanola)

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  GoLYTELY? or NoGO? Let’s be real about whole bowel irrigation

4 out of 5 stars Whole Bowel Irrigation and the Hemodynamically Unstable Calcium Channel Blocker Overdose: Primum non Nocere. Cumpston KL et al.  J Emerg Med 2010;38:171-174. Abstract As even its proponents admit, whole bowel irrigation (WBI) with high-molecular-weight polyethylene glycol (PEG) has never been proven to improve clinical outcomes in toxicology patients.  Despite this, some physicians argue that the procedure is safe, and recommend that it be considered in cases involving toxins that do not bind well to charcoal, patients who have ingested sustained/delayed/extended-release products, or in body-packers. This important paper, from the Toxikon group in Chicago, reminds us that with WBI — as with just about everything else in medicine — there’s no free lunch....

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  Tildiem tablets 60mg (diltiazem) - Revised SPC

Source: eMC (electronic Medicines Compendium) Area: Other Library Updates > SPC Changes Revised SPC includes changes to: Section 4.5 (Interaction with other medicinal products and other forms of interaction) - added information regarding interactions with statins, benzodiazepines (midazolam, triazolam) and methylprednisolone. Section 4.8 (Undesirable Effects) - Further safety information regarding lichenoid keratosis, mood changes (depression) and thrombocytopenia due to diltiazem treatment has been added. (Source: NeLM - SPC Changes)

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  DILTIAZEM HYDROCHLORIDEcapsule, Extended Release [Forest Laboratories, Inc.]

Updated Date: Feb 24, 2010 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  V–Y advancement flap as first-line treatment for all chronic anal fissures

Conclusions  We have shown excellent rates of healing of chronic anal fissures treated with a V–Y advancement flap regardless of sphincter pressures, previous treatment and symptom chronicity. These results show the technique can be applied to all chronic fissures with success and used as a primary therapy. Content Type Journal ArticleCategory Original ArticleDOI 10.1007/s00384-010-0881-1Authors William Chambers, Frenchay Hospital Department of Colorectal Surgery Bristol UKRai Sajal, Frenchay Hospital Department of Colorectal Surgery Bristol UKAnthony Dixon, Frenchay Hospital Department of Colorectal Surgery Bristol UK Journal International Journal of Colorectal DiseaseOnline ISSN 1432-1262Print ISSN 0179-1958 (Source: International Journal of Colorectal Dis...

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  Assessment: Symptomatic treatment for muscle cramps (an evidence-based review): Report of the Therapeutics and Technology Assessment Subcommittee of the American Academy of Neurology

Background: A Food and Drug Administration advisory in 2006 warned against the off-label use of quinine sulfate and its derivatives in the treatment of muscle cramps. Physicians are faced with a difficult scenario in choosing a treatment regimen for patients with muscle cramps. This American Academy of Neurology assessment systematically reviews the available evidence on the symptomatic treatment of muscle cramps. Methods: A total of 563 potential articles were reviewed, of which 24 met the inclusion criteria of prospective trials evaluating the efficacy of a particular treatment on muscle cramps as a primary or secondary outcome. Results: There are Class I studies showing the efficacy of quinine derivatives for treatment of muscle cramps. However, the benefit is modest and there are adver...

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  Calcinosis cutis and Sjogren's syndrome.

We present a case of dystrophic calcinosis cutis, affecting the fingertip of a woman with a 10-year history of primary Sjögren's syndrome (SS). She has been receiving diltiazem as a treatment for the last 15 months, resulting in the partial resolution of the lesions. We emphasize the fact that the presence of calcinosis cutis has not been described previously in patients with SS, and that diltiazem has partially improved our patient's cutaneous lesions. PMID: 20156928 [PubMed - as supplied by publisher] (Source: Lupus)

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  Effects of Concomitant Therapy With Diltiazem on the Lipid Responses to Simvastatin in Chinese Subjects.

This study assessed the impact of this interaction on the lipid-lowering effects of simvastatin. Chinese patients with hypercholesterolemia were randomized to receive simvastatin 20 mg daily alone or together with diltiazem 60 mg 3 times daily for 4 weeks with a washout period of 4 weeks in an open-label, crossover study. Blood pressure, fasting serum lipid profile, and safety tests were determined at baseline and after each treatment period. Trough serum diltiazem was measured at the end of the 4-week combination treatment. In the 30 patients who completed the study, simvastatin treatment significantly reduced low-density lipoprotein cholesterol by mean (+/- standard error) 41.0% +/- 2.2% (P < .001), and the combination with diltiazem showed an additional reduction of 1.66% (95% confid...

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  Effects of Labetalol on Hemodynamic Parameters and Soluble Biomarkers of Inflammation in Acute Coronary Syndrome in Patients With Active Cocaine Use

In conclusion, labetalol appears to be safe in cocaine-associated ACS. Furthermore, labetalol provides a beneficial hemodynamic response and, in comparison to diltiazem, potentiates an anti-inflammatory vascular response in this setting. (Source: Journal of Cardiovascular Pharmacology and Therapeutics)

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  Screening for the effectiveness of conservative treatment in chronic anal fissure patients using anorectal manometry

Conclusions  The ratio resting/voluntary contraction pressure may be predictive of healing in CAF, thus allowing the selection of patients at high risk of failure of conservative treatment. Content Type Journal ArticleCategory Original ArticleDOI 10.1007/s00384-010-0885-xAuthors José Gil, “Virgen de la Arrixaca” University Hospital Department of General Surgery Murcia SpainJuan Luján, “Virgen de la Arrixaca” University Hospital Department of General Surgery Murcia SpainQuiteria Hernández, “Virgen de la Arrixaca” University Hospital Department of General Surgery Murcia SpainElena Gil, “Virgen de la Arrixaca” University Hospital Department of General Surgery Murcia SpainMiguel G. Salom, University of Murcia Department of Physiology, Faculty of Medicine ...

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  DILTIAZEM HYDROCHLORIDEcapsule, Extended Release [American Health Packaging]

Updated Date: Feb 2, 2010 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  Tildiem Retard 90,120mg / Tildiem LA 200, 300 (Diltiazem) - Revised SPC

Source: eMC (electronic Medicines Compendium) Area: Other Library Updates > SPC Changes Revised SPC includes changes to: Section 4.5 - Interaction with other medicinal products and other forms of interaction - added information regarding interactions with statins, benzodiazepines (midazolam, triazolam) and methylprednisolone. Section 4.8 - Undesirable Effects? - Further safety information regarding lichenoid keratosis, mood changes (depression) and thrombocytopenia due to diltiazem treatment has been added (Source: NeLM - SPC Changes)

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  Participation of l-type calcium channels in ethanol-induced behavioral stimulation and motor incoordination: effects of diltiazem and verapamil.

In conclusion, these data provide further evidence of the important involvement of L-type calcium channels in the behavioral effects produced by ethanol. PMID: 20122967 [PubMed - as supplied by publisher] (Source: Behavioural Brain Research)

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  Diltiazem: Acute generalised exanthematous pustulosis in an elderly patient: case report

(Source: Reactions)

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  Cartia XT (Diltiazem Hydrochloride Extended Release Capsules) - updated on RxList

Cartia XT (Diltiazem Hydrochloride Extended Release Capsules) drug description - FDA approved labeling for prescription drugs and medications at RxList (Source: RxList - New and Updated Drug Monographs)

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  DILTIAZEM HYDROCHLORIDE (Diltiazem) Capsule, Extended Release [Physicians Total Care, Inc.]

Updated Date: Jan 14, 2010 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  Physiologically-based mechanistic modelling to predict complex drug-drug interactions involving simultaneous competitive and time-dependent enzyme inhibition by parent compound and its metabolite in both liver and gut-the effect of diltiazem on the time-course of exposure to triazolam.

CONCLUSION: Prediction of mDDIs involving diltiazem requires consideration of both competitive and time-dependent inhibition in gut and liver by both diltiazem and MA, as well as the complex interplay between the two moieties with respect to mutual inhibition of parent compound and its metabolite. PMID: 20025966 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)

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  Diltiazem/mephenoxalone/paracetamol: AGEP treated with etanercept: case report

(Source: Reactions)

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  L-type calcium channel blockers reverse docetaxel and vincristine-induced multidrug resistance independent of ABCB1 expression in human lung cancer cell lines.

Authors: Chiu LY, Ko JL, Lee YJ, Yang TY, Tee YT, Sheu GT Multidrug resistance (MDR) of cancer cells to cytotoxic drugs significantly impedes chemotherapeutic treatment. The purpose of this study is to characterize docetaxel (DOC) or vincristine (VCR) selected A549 and H1299 non-small cell lung cancer (NSCLC) sublines that exhibit MDR phenotypes and followed by re-sensitization study. Although all drug resistant sublines showed cross-resistance to DOC, VCR, and doxorubicin (DXR), the expression of ATP-binding cassette (ABC) transporter B1 (ABCB1) gene was found to be strongly induced in DOC but not in VCR resistant A549 sublines by quantitative reverse transcription real-time polymerase chain reaction (qRT-PCR). In DOC and VCR resistant H1299 sublines, moderate expression of ABCB1 was ...

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  Sustained Release of a Water-Soluble Drug from Alginate Matrix Tablets Prepared by Wet Granulation Method.

This study revealed that proper selection of SAL/CG ratio is important to produce alginate matrix tablet by wet granulation method for sustained release of DTZ. PMID: 19911286 [PubMed - as supplied by publisher] (Source: AAPS PharmSciTech)

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  Health News of the Day

is a daily summary made from the selected links I post on Twitter. It is in a bullet points format with links to the original sources which include 350 RSS feeds that produce about 2,500 items per day:FDA Issues Warning for Diabetes Drug Byetta about possible kidney problems, including renal failure http://bit.ly/1UOjwB"Who are the sleepiest people in the US?" Source: Morbidity and Mortality Weekly Report http://bit.ly/4djMWPX-rays showed 78 different items of cutlery in a 52-year-old woman's stomach http://bit.ly/4iojkQMayo Clinic: 10 great health foods for eating well http://bit.ly/sGLgF"Hospitals with hospitalists have an easier time recruiting subspecialists" http://bit.ly/WapWE and http://bit.ly/G85PLSleep Changes with Aging http://bit.ly/4CPzGJWhat drug is best for initial treatment...

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  TIAZAC EXTENDED RELEASE (Diltiazem Hydrochloride) Capsule, Extended Release [Forest Laboratories, Inc.]

Updated Date: Nov 3, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  DILTIAZEM HYDROCHLORIDEcapsule, Extended Release [Ethex Corporation]

Updated Date: Nov 3, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  Curing of aqueous polymeric film coatings: importance of the coating level and type of plasticizer.

Authors: Yang QW, Flament MP, Siepmann F, Busignies V, Leclerc B, Herry C, Tchoreloff P, Siepmann J The aim of this study was to better understand the effects of the curing conditions on the resulting drug release patterns from pellets coated with aqueous polymer dispersions. Diltiazem HCl was used as model drug, ethylcellulose as polymer, triethyl citrate (TEC), dibutyl sebacate (DBS), and distilled acetylated monoglycerides (Myvacet) as plasticizers. Interestingly, the effects of the curing conditions strongly depended on the coating level and type of plasticizer: In the case of TEC, the drug release rate monotonically decreased with increasing harshness of the curing conditions (time, temperature and relative humidity), irrespective of the coating level. In contrast, in the case of ...

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  Coronary arterial spasm in single right coronary artery.

We presented a case of anomalous single-coronary artery detected incidentally during routine coronary angiography. A 32-year-old male Chinese patient presented with recurrent pre-syncope and six episodes of syncope. Coronary angiography and coronary-computed tomography (CT)-angiography performed by a dual-source computed tomography (DSCT) revealed that the patient had a single large right coronary artery. A moderately large branch originated from the proximal part of the single right coronary artery and extended to the left, passing the anterior to the pulmonary artery, and divided into the anterior descending artery branch and circumflex branch at the base of the left auricular appendage. The episodes of the syncope were suspected to be caused by coronary arterial spasm, so this patient w...

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  Sildenafil increases the force of right atrial contractions in vitro via the NO-guanylyl cyclase pathway involving beta-adrenoceptor linked mechanisms.

This study was undertaken to elucidate the effect of sildenafil on cardiac contractility and the underlying mechanisms. The experiments were conducted on spontaneously-beating right atria isolated from adult rats. The effect of sildenafil on the isometric contractions in vitro was examined in the absence or presence of antagonists. Sildenafil (0.001-10 microM) produced a concentration-dependent increase in the atrial force of contraction without altering the atrial rate, even up to 10 microM. A concentration as low as 0.001 microM produced a significant increase (16%) in force and the increase was about 50% at 10 microM. Pretreatment with methylene blue (a guanylyl cyclase inhibitor) or N-omega-nitro-L-arginine methyl ester (L-NAME, a nitric oxide synthase inhibitor) blocked the force chan...

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  Presence of cyclic nucleotide-gated channels in the rat urethra and their involvement in nerve-mediated nitrergic relaxation

We have addressed the distribution of cGMP-gated channels (CNG) in the rat urethra for the first time, as well as their putative role in mediating of the relaxation elicited by electrical field stimulation of nitrergic nerves. Functional studies have shown that specifically blocking CNG with l-cis-diltiazem leads to the rapid inhibition of urethral relaxation induced either by nitric oxide (NO) released by the nerves or by soluble guanylate cyclase activated with YC-1. By contrast, nerve-mediated noradrenergic contractions were only slowly and mildly reduced by l-cis-diltiazem. This effect was mimicked by lower concentrations of the d-diltiazem isomer, probably due to the nonspecific inhibition of voltage-dependent calcium channels. However, d-diltiazem did not affect relaxation responses....

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  Termination of idiopathic sustained monomorphic ventricular tachycardia by intravenous adenosine in a pregnant woman

A 34-year-old pregnant woman presented to the emergency department with the complaints of palpitations at 32 weeks gestation. The diagnosis of right ventricular outflow tract ventricular tachycardia (VT) was made. Intravenous 5 mg of metoprolol and 25 mg of diltiazem did not terminate the VT. Ten milligrams of adenosine were administered. Within 10 s of adenosine administration, sustained VT converted to repetitive monomorphic VT and within 30 s to normal sinus rhythm. The mother and the foetus tolerated the medications well. Non-stress test for the assessment of the foetal well-being was normal. (Source: Europace)

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  Inhibition of MDR1 activity and induction of apoptosis by analogues of nifedipine and diltiazem: an in vitro analysis

In conclusion, our results identify two new molecules structurally related to the calcium-channel blocker nifedipine, but characterized by a very low LTCC blockers activity, able to potentiate the antiproliferative and apoptotic activities of doxorubicin through an increase of its intracellular concentration likely caused by the inhibition of MDR1 function. Content Type Journal ArticleCategory PRECLINICAL STUDIESDOI 10.1007/s10637-009-9340-7Authors Maurizio Viale, S.C. Terapia Immunologica Istituto Nazionale per la Ricerca sul Cancro L.go R. Benzi 10 16132 Genova ItalyCinzia Cordazzo, Università degli Studi di Bologna Dipartimento di Chimica Organica “A. Mangini” Via San Giacomo 11 40126 Bologna ItalyDaniela de Totero, S.C. Terapia Immunologica Istituto Nazionale per la Ricerc...

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  Systemic sclerosis sine scleroderma and calcinosis cutis: report of a rare case

Abstract  Systemic sclerosis sine scleroderma is a rare form of limited cutaneous scleroderma. These patients manifest without cutaneous involvement, but do not differ in its clinical or laboratory features and prognosis from classical systemic sclerosis. In the absence of cutaneous signs/symptoms, its diagnosis is delayed leading to morbidity. The exact prevalence of dystrophic calcification in systemic sclerosis sine scleroderma, though a feature of systemic sclerosis, is not known. Development of dystrophic calcification further aggravates patient's woes. This paper describes systemic sclerosis sine scleroderma in a 17-year-old girl diagnosed initially as seronegative juvenile rheumatoid arthritis. She developed progressively increasing disk-like masses of calcinosis ove...

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  Stereoselective Behavior of the Functional Diltiazem Analogue 1-[(4-Chlorophenyl)sulfonyl]-2-(2-thienyl)pyrrolidine, a New L-Type Calcium Channel Blocker

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable). (Source: Journal of Medicinal Chemistry)

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  CARDIZEM (Diltiazem Hydrochloride) Tablet, Coated [BTA Pharmaceuticals]

Updated Date: Oct 14, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  Hyperoxia and prevention of adhesion formation: a laparoscopic mouse model for open surgery

Conclusions Hyperoxia-enhanced adhesions were prevented by hypothermia, dexamethasone, phospholipids, Hyalobarrier® gel, diltiazem, r-PA and AA. All effects were similar to those in the hypoxia-enhanced adhesion model, suggesting that the underlying mechanisms are similar. (Source: BJOG: An International Journal of Obstetrics and Gynaecology)

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  Hyperoxia and prevention of adhesion formation: a laparoscopic mouse model for open surgery.

Conclusions Hyperoxia-enhanced adhesions were prevented by hypothermia, dexamethasone, phospholipids, Hyalobarrier((R)) gel, diltiazem, r-PA and AA. All effects were similar to those in the hypoxia-enhanced adhesion model, suggesting that the underlying mechanisms are similar. PMID: 19832833 [PubMed - as supplied by publisher] (Source: BJOG : An International Journal of Obstetrics and Gynaecology)

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  DILTIAZEM HYDROCHLORIDEcapsule, Extended Release DILTIAZEM HYDROCHLORIDEcapsule, Extended Release [TEVA Pharmaceuticals USA Inc.]

Updated Date: Oct 5, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  Mitochondrial oxidative phosphorylation in hearts subjected to Ca2+ depletion and Ca2+ repletion.

Authors: Makazan Z, Saini-Chohan HK, Dhalla NS Repletion of Ca2+ in the Ca2+-depleted heart has been shown to produce cardiac dysfunction, myocardial cell damage, intracellular Ca2+ overload, and defects in sarcolemmal and sarcoplasmic reticulum function (Ca2+ paradox). Although these alterations in the Ca2+-paradox heart are associated with a depression in the high-energy phosphate stores, little information regarding changes in mitochondrial oxidative phosphorylation is available. Perfusion of rat hearts with Ca2+-free medium for 5 min followed by reperfusion with a medium containing 1.25 mmol/L Ca2+ for 10 min depressed mitochondrial state 3 respiration, respiratory control index, ADP/O ratio, and rate of oxidative phosphorylation without any change in state 4 respiration. These alt...

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  Ligands of Diltiazem Binding Site: An Overview of Some Chemotypes.

Authors: Budriesi R, Ioan P, Carosati E, Cruciani G, Zhorov BS, Chiarini A The diltiazem binding site of L-type calcium channels is the least characterized to date. In this paper, we present some of the available chemotypes that bind to the benzothiazepine binding site: natural compounds, compounds synthesized by varying the benzothiazepine scaffold, and compounds discovered by means of computational approaches. PMID: 19929811 [PubMed - as supplied by publisher] (Source: Mini Reviews in Medicinal Chemistry)

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  Limitation of infarct size with preconditioning and calcium antagonist (Diltiazem): Difference in99mTc-PYP uptake in the myocardium

Conclusions: These findings suggest that preconditioning does not alleviate stunning, but it improves cell injury in spite of high uptake of99mTc-PYP. Diltiazem protects from both stunning and cell injury, suggesting a different mechanism of myocardial protection from that of preconditioning. Content Type Journal ArticleCategory Original ArticleDOI 10.1007/BF03165393Authors Kazumi Okuda, Kyoto University Hospital Third Division, Department of Internal Medicine 54 Kawaracho, Shogoin, Sakyo-ku 606 Kyoto JapanRyuji Nohara, Kyoto University Hospital Third Division, Department of Internal Medicine 54 Kawaracho, Shogoin, Sakyo-ku 606 Kyoto JapanMotonari Ogino, Kyoto University Hospital Third Division, Department of Internal Medicine 54 Kawaracho, Shogoin, Sakyo-ku 606 Kyoto JapanNagara Ta...

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  CARDIZEM (Diltiazem Hydrochloride) Capsule [BTA Pharmaceuticals Inc.]

Updated Date: Sep 30, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  TIAZAC EXTENDED RELEASE (Diltiazem Hydrochloride) Capsule, Extended Release [Forest Laboratories, Inc.]

Updated Date: Sep 29, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  DILTIAZEM HYDROCHLORIDEcapsule, Extended Release [Forest Laboratories, Inc.]

Updated Date: Sep 29, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  [Diltiazem-induced acute generalized exanthemic pustulosis: a case.]

Authors: Fernández-Ruiz M, López-Medrano F, García-Ruiz F, Rodríguez-Peralto JL PMID: 19775556 [PubMed - in process] (Source: Actas Dermo-Sifiliograficas)

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  In vitro interaction studies of diltiazem with H2 receptor antagonists

Abstract  Diltiazem is a well-known cardiovascular drug that is used clinically for the treatment of angina pectoris and hypertension. H2-receptor antagonists are used to treat gastroesophageal reflux, gastric and duodenal ulceration. In vitro interaction studies of diltiazem with H2-receptor antagonists (cimetidine, ranitidine, and famotidine) were investigated by using spectrophotometric and RP-HPLC techniques. The availability of diltiazem was found to be influenced considerably in presence of H2-receptor antagonists. The effect of various dissolution mediums, simulating body environments with respect to pH on these interactions was examined to elucidate the mechanism of these interactions. Moreover, diltiazem-H2 receptor complexes were synthesized to confirm the interacti...

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  Treatment of new-onset atrial fibrillation in noncardiac intensive care unit patients: a systematic review of randomized controlled trials

Source: DARE Area: Evidence > Disease Focused Reviews CRD Summary: The authors found insufficient evidence to make recommendations about standard treatment of noncardiac critically ill patients with new-onset atrial fibrillation. Despite some concerns about the risk of language and publication bias, this was generally a well-conducted review and the authors' conclusions were likely to be reliable. [The included studies compared procainamide, flecainide, magnesium, amiodarone, verapamil, diltiazem and esmolol with each other. ] CRD Commentary: The review question was clearly stated and inclusion criteria were specified. Although the review focus was on patients with atrial fibrillation some patients with other atrial tachycardias were also included. Several relevant sources were searc...

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  Pharmacological inhibition of the hypertensive response to combretastatin A-4 phosphate in rats.

In this study, we examined the potential cardiac toxicity and hypertensive effects of CA4P, and defined the most effective pharmacological inhibition of CA4P-induced hypertension in rats. There was a significant, concentration dependent increase in mean arterial blood pressure with a maximum increase of about 60% of the baseline MAP at 30 mg/kg of CA4P compared to the saline control. However, there was no significant increase in the cardiac troponin I level after CA4P injection. Nitroglycerin and the calcium channel blocker diltiazem effectively blocked the hypertensive effects of CA4P while the beta blocker metoprolol was ineffective. Furthermore, sublingual nitroglycerin administration demonstrated an additional anti-hypertensive effect in a setting of a low dose diltiazem infusion (10 m...

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  Two different approaches for the prediction of In Vivo plasma concentration-time profile from In Vitro release data of once daily formulations of diltiazem hydrochloride.

Authors: Bendas ER The aim of this study was to employ two different mathematical approaches: first, a convolution approach using computer software; second, a mathematical calculation exploiting Wagner-Nelson calculation to predict in vivo plasma concentration - time profile from the in vitro release study for the once daily formulations of a model drug diltiazem hydrochloride. The once daily extended release tablets (120 mg) were prepared by the wet granulation technique. Ethanol or ethanolic solutions of ethylcellulose (N22), were used as granulating agents along with hydrophilic matrix polymers like hydroxypropyl methylcellulose (HPMC) (K 15M). The granules showed satisfactory flow properties, compressibility, moisture content and drug content. All the tablet formulations showed acc...

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  The effects of diuretics on intracellular ca dynamics of arteriole smooth muscles as revealed by laser confocal microscopy.

In this study, hydrochlorothiazide (100 microM) and furosemide (100 microM) had no effect on the [Ca(2+)](i) dynamics. However, when spironolactone (300 microM) was applied, the [Ca(2+)](i) of smooth muscles increased. The response was considerably inhibited under either extracellular Ca(2+)-free conditions, the presence of Gd(3+), or with a treatment of diltiazem. After the thapsigargin-induced depletion of internal Ca(2+) store, the spironolactone-induced [Ca(2+)](i) dynamics was slightly inhibited. Therefore, the spironolactone-induced dynamics of [Ca(2+)](i) can be caused by either a Ca(2+) influx from extracellular fluid or Ca(2+) mobilization from internal Ca(2+) store, with the former being dominant. As tetraethylammonium, an inhibitor of the K(+) channel, slightly inhibited the spi...

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  Rapid large artery remodeling following the administration and withdrawal of calcium channel blockers in spontaneously hypertensive rats.

Authors: Vaja V, Ochodnicky P, Krenek P, Klimas J, Bajuszova Z, Kyselovic J Chronic treatment with several antihypertensive agents, including calcium channel blockers, may interfere with remodeling of large arteries and increased arterial stiffness. We hypothesize that even a short, seven day administration of calcium channel blockers might alter an aortic remodeling in spontaneously hypertensive rat (SHR). Male SHR and normotensive WKY rats (n=14 each) were treated by either vehicle, vasculoselective calcium channel blocker nifedipine (1mg/kg/day) or cardiac/vascular calcium channel blockers diltiazem (5mg/kg/day) or verapamil (4mg/kg/day, n=6 for each treatment) subcutaneously twice daily for seven days. Additional SHR rats were randomized for termination 24, 72 or 120h (n=5 each) af...

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  Dog left ventricular midmyocardial myocytes for assessment of drug-induced delayed repolarization: short-term variability and proarrhythmic potential

Conclusions and implications: LVMMs provide a suitable preclinical model to assess the effects of new drugs on APD and also yield additional information about putative indicators of proarrhythmia that add value to an integrated QT/TdP risk assessment. Our findings support the concept that increased STV(APD) may predict drug-induced proarrhythmia. (Source: British Journal of Pharmacology)

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  Randomized comparison of vasodilator effects of iloprost versus diltiazem on flow and pathologic changes in radial arteries: mid-term angiographic control study of the comparison of vasodilators on radial artery vasospasm.

CONCLUSIONS: Our evaluation of the results revealed the superior efficacy of iloprost over diltiazem in preventing RA spasm in the early period, and the 2-year angiographic findings showed that the use of iloprost produced superior mid-term patency. PMID: 19683989 [PubMed - in process] (Source: The Heart Surgery Forum)

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  [Acute generalised exanthematosus pustulosis (AGEP) due to diltiazem - a case report.]

Authors: Barcik K, Protas-Drozd F, Weiss-Rostkowska W, Flis E, Placek W A case of a patient who developed acute generalised exanthemotosus pustulosis (AGEP) due to diltiazem therapy is presented. On the day of the admission to hospital skin changes were present on the whole body in the form of sterile spots of an erythema origin. The laboratory tests showed anaemia, leucocytosis, hypocalcaemia, increased liver enzymes and increased ESR. The skin changes were accompanied by high temperature and bad condition. On the basis of medical history, clinical picture and medical tests, AGEP was diagnosed. After the application of a general treatment with erythromycin and external preparations, the skin changes subsided completely. PMID: 19784887 [PubMed - in process] (Source: Kardiologia Pol...

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  Is cytochrome modulation the new frontier for decreasing the risk of cataract?

Conclusion:&lt;/b&gt; A delayed occurrence of cataract with diltiazem (CYP inhibitor) and an early onset of cataract with pioglitazone (CYP inducer) indicate that a cytochrome P450 mediated pathway may affect the initiation of cataract but not the maturation pattern. (Source: Indian Journal of Pharmacology)

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  Prognostic factors for the long-term survival in patients with vasospastic angina Analysis of effects of patients' characteristics and therapeutic drugs.

CONCLUSION: These results indicate that the morbidity of patients with vasospastic angina increased with older age, lower CI or HDL cholesterol, and presence of severe coronary artery stenosis, and that treatment with benidipine appeared to reduce cardiovascular events in patients with vasospastic angina. PMID: 19632515 [PubMed - in process] (Source: Journal of Cardiology)

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  [Best Evidence Topic reports] BET 4. INTRAVENOUS DILTIAZEM FOR THE CONTROL OF VENTRICULAR RATE FOR PATIENTS WITH RECENT ONSET ATRIAL FIBRILLATION AND LEFT VENTRICULAR FAILURE

(Source: Emergency Medicine Journal)

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  Amlodipine/diltiazem/nifedipine: Purpura and haemorrhage: 4 case reports

(Source: Reactions)

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  Amlodipine/diltiazem/nifedipine: Purpura and haemorrhage: 4 case reports.

Page: 5 (Source: Reactions Weekly)

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  Development of high performance liquid chromatography method for buspirone in rabbit serum: Application to pharmacokinetic study.

Authors: Gannu R, Yamsani SK, Palem CR, Yamsani VV, Kotagiri H, Yamsani MR A simple and sensitive high performance liquid chromatographic (HPLC) method for quantification of buspirone (BUSP) in rabbit serum was developed and validated. BUSP and internal standard (IS), diltiazem hydrochloride were extracted into dichloromethane and separated using an isocratic mobile phase, on a Kromasil C(8) column. The eluent was monitored by UV detector at 235 nm and at a flow rate of 1.0 mL min(-1). The linearity range of proposed method was 1-3000 ng mL(-1). The intra-day and inter-day coefficient of variation and percent error values of the assay method were less than 15% and mean recovery was more than 97 and 96% for BUSP and IS, respectively. The method was found to be precise, accurate, and spe...

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  Diltiazem: Allergic contact dermatitis: case report

(Source: Reactions)

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  Diltiazem/niacin: Insulin autoimmune syndrome (first report) in an elderly patient: case report

(Source: Reactions)

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  Diltiazem: Allergic contact dermatitis: case report.

Page: 13 (Source: Reactions Weekly)

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  Diltiazem/niacin: Insulin autoimmune syndrome (first report) in an elderly patient: case report.

Page: 13 (Source: Reactions Weekly)

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  DILTIAZEM HYDROCHLORIDEcapsule, Extended Release [Biovail Pharmaceuticals Inc]

Updated Date: Jun 30, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  Preservation and Modulation of Peritoneal Function. A Potential Role of Pyruvate and Betaine.

Conclusions: Efforts focused in improving the dialyzing capabilities of the peritoneal membrane by means of pharmacological manipulation, have not yet offered clinically relevant innovations. Conversely, interventions designed to preserve the peritoneum as a reusable dialyzing living membrane are more promising, especially those aimed at neutralizing oxidative and osmotic injury. PMID: 19494598 [PubMed - as supplied by publisher] (Source: Contributions to Nephrology)

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  Intravenous diltiazem is superior to intravenous amiodarone or digoxin for achieving ventricular rate control in patients with acute uncomplicated atrial fibrillation *.

Page: 2174DOI: 10.1097/CCM.0b013e3181a02f56Authors: Siu, Chung-Wah MBBS; Lau, Chu-Pak MD; Lee, Wai-Luen MBBS; Lam, Kwok-Fai PhD; Tse, Hung-Fat MD, PhD (Source: Critical Care Medicine)

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  Influence of diltiazem in combination with a sucrose-rich diet on gingival alterations in rats

The aim of this study was to evaluate the influence of diltiazem in combination with a sucrose-rich diet on gingival alterations in rats. One hundred and twenty male Holtzman rats were randomly assigned to 10 groups (n = 12), being 2 control groups treated with saline and 8 test groups treated with diltiazem in daily doses of 5, 25, 50 and 100 mg/kg during 40 or 60 days. Afterwards, the mandibles were removed for macroscopic, histologic and histometric analyses of the buccal gingiva of the mandibular right first molar. No macroscopic characteristic of gingival overgrowth was observed in any of the groups. The microscopic analysis showed characteristics of normality with inflammatory cells only adjacent to the crevicular epithelium in all groups for both periods. The histometric analysis sh...

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  Pacing Threshold Testing Induced Ventricular Fibrillation Following Acute Rate Control of Atrial Fibrillation

Conclusion: Pacemaker-induced VF is an extraordinarily rare complication of cardiac pacing. Alterations in ventricular repolarization with rapid slowing of the heart rate demonstrated by acute prolongation of QT intervals may play a role. This report should alert physicians to the possibility of QT prolongation and an increased risk of ventricular arrhythmias following acute rate control of AF. (J Cardiovasc Electrophysiol, Vol. pp. 1[ndash]3) (Source: Journal of Cardiovascular Electrophysiology)

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  Food restriction promotes downregulation of myocardial L-type Ca2+ channels.

Authors: De Tomasi LC, Bruno A, Sugizaki MM, Lima-Leopoldo AP, Nascimento AF, Júnior SA, Pinotti MF, Padovani CR, Leopoldo AS, Cicogna AC Food restriction (FR) has been shown to impair myocardial performance. However, the mechanisms behind these changes in myocardial function due to FR remain unknown. Since myocardial L-type Ca2+ channels may contribute to the cardiac dysfunction, we examined the influence of FR on L-type Ca2+ channels. Male 60-day-old Wistar rats were fed a control or a restricted diet (daily intake reduced to 50% of the amount of food consumed by the control group) for 90 days. Myocardial performance was evaluated in isolated left ventricular papillary muscles. The function of myocardial L-type Ca2+ channels was determined by using a pharmacological Ca2+ channel...

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  Production variables affecting characteristics of pellets in melt pelletization with wax combination in a laboratory scale spheronizer.

Authors: Biswal S, Sahoo J, Murthy PN, Giradkar RP, Das S, Avari JG The purpose of the study was to evaluate the suitability of laboratory scale spheronizer for the production of spherical pellets loaded with diltiazem hydrochloride by wax combination. The 1:1 combination of cetyl alcohol and hydrogenated castor oil, as low and high melting point waxes, were used. The various production variables affecting the different characteristics of pellets and the process efficiency were evaluated. Drug loaded pellets were evaluated for drug release in distilled water. Bowl temperature primarily affects the sphericity and adhesion of pellets to the bowl. Mass temperature has a pronounced effect on size, size distribution and sphericity of pellets. Wax concentration affects all characteristics of...

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  Contact sensitization to topical diltiazem

(Source: Contact Dermatitis)

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  Is cytochrome modulation the new frontier for decreasing the risk of cataract?

Conclusion:&lt;/b&gt; A delayed occurrence of cataract with diltiazem (CYP inhibitor) and an early onset of cataract with pioglitazone (CYP inducer) indicate that a cytochrome P450 mediated pathway may affect the initiation of cataract but not the maturation pattern. (Source: Indian Journal of Pharmacology)

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  Voltage-independent calcium channels mediate lipopolysaccharide-induced hyporeactivity to endothelin-1 in the rat aorta

The roles of intracellular calcium concentration ([Ca2+]i) and Ca2+ sensitization in lipopolysaccharide (LPS)-induced vascular smooth muscle (VSM) hyporesponsiveness are incompletely understood. To investigate these roles, contraction responses to endothelin-1 (ET-1) and 80 mM KCl; relaxation responses to nifedipine; the expression levels of mRNAs of ET-1 and its receptors (ETA or ETB); the expression levels of protein kinase C (PKC) and phosphorylation of Rho kinase (ROK), CPI-17, and myosin phosphatase target subunit-1 (MYPT1); and changes in aortic VSM cell [Ca2+]i were measured in LPS-treated aortic rings from male Wistar rats (250–300 g). LPS (10 µg/ml, 20 h) decreased contraction induced by ET-1 (0.3–100 nM) or 80 mM KCl. LPS-induced hypocontractility was not observ...

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  Acetylcholine induces Ca2+ signaling in chicken retinal pigmented epithelial cells during dedifferentiation

Retinal pigmented epithelial cells exchange their cellular phenotypes into lens cells and neurons, via depigmented and non-epithelial-shaped dedifferentiated intermediates. Because these dedifferentiated cells can either revert to pigmented epithelial cells or transdifferentiate into lens cells and/or neurons, they are recognized as candidates for lens and retinal cell regeneration. The purpose of the present study was to elucidate the signal transduction pathways between chicken retinal pigmented epithelial cells and their dedifferentiated intermediates. We monitored intracellular Ca2+ concentrations using Fluo-4-based Ca2+ optical imaging and focused on cellular responses to the neurotransmitter acetylcholine. Muscarinic Ca2+ mobilization was observed both in retinal pigmented epithelial...

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  Evaluation of changes in cardiac biomarker concentrations and enzyme activities in serum after short- and long-duration transcutaneous cardiac pacing in dogs.

CONCLUSIONS AND CLINICAL RELEVANCE: Results indicated that application of TCP for > 1 hour in dogs may cause myocardial and skeletal muscular injuries. Serum concentrations of creatine kinase-MB fraction and cardiac troponin I and activities of aspartate transaminase, creatine kinase, and lactate dehydrogenase should be more carefully monitored after TCP of > 1 hour's duration to evaluate potential myocardial damages. PMID: 19405898 [PubMed - indexed for MEDLINE] (Source: American Journal of Veterinary Research)

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  Pharmacological characteristics and clinical applications of k201.

Authors: Kaneko N, Matsuda R, Hata Y, Shimamoto K K201 is a 1,4-benzothiazepine derivative that is a promising new drug with a strong cardioprotective effect. We initially discovered K201 as an effective suppressant of sudden cardiac cell death due to calcium overload. K201 is a non-specific blocker of sodium, potassium and calcium channels, and its cardioprotective effect is more marked than those of nicorandil, prazosine, propranolol, verapamil and diltiazem. Recently, K201 has also been shown to have activities indicated for treatment of atrial fibrillation, ventricular fibrillation, heart failure and ischemic heart disease, including action as a multiple-channel blocker, inhibition of diastolic Ca(2+) release from the sarcoplasmic reticulum, suppression of spontaneous Ca(2+) sparks...

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  Potentiating effect of diltiazem on pentobarbital-induced hypnosis is augmented by serotonergic system: the TMN and VLPO as key elements in the pathway.

Authors: Zhao X, Cui XY, Wang LE, Zhang YH To investigate the mechanism by which L-type Ca+ channel blockers exerted potentiating effects on pentobarbital-induced hypnosis, the present study was undertaken to determine if the interaction of diltiazem and serotonergic system influences the architecture of pentobarbital sleep in rats and examined c-Fos expression in the ventrolateral preoptic nucleus (VLPO) and the tuberomammillary nucleus (TMN). The polysomnogram consisting of EEG and EMG was recorded for analyzing sleep architecture. The results showed that diltiazem (2.0 and 5.0 mg/kg, p.o.) increased both total pentobarbital sleep and slow wave sleep (SWS), but decreased rapid eye movement (REM) sleep. These effects were potentiated by 5-hydroxytryptophan (5-HTP), a precursor of sero...

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  L-type voltage-gated calcium channel is involved in the pathogenesis of acoustic injury in the cochlea.

Authors: Uemaetomari I, Tabuchi K, Nakamagoe M, Tanaka S, Murashita H, Hara A Excessive calcium entry into cells leads to cell death, and voltage-gated calcium channels (VGCCs) are responsible for the calcium entry in the central nervous system. VGCC blockers inhibit excessive calcium entry and protect the central nervous system against various types of injury. The purpose of the present study was to identify the type of calcium channels that is responsible for acoustic injury of the cochlea. The effects of L- and T-type VGCC blockers on acoustic injury were examined. Female ddY mice, at 8 weeks of age, were used in this study. The animals were subjected to a 4-kHz pure tone of 128-dB sound pressure level (SPL) for 4 hours through an open field system inside a sound-exposure box. A L-t...

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  L-Type Calcium Channel Blockers: From Diltiazem to 1,2,4-Oxadiazol-5-ones via Thiazinooxadiazol-3-one Derivatives

Journal of Medicinal Chemistry, Volume 52, Issue 8, Page 2352-2362, April 23, 2009. (Source: Journal of Medicinal Chemistry)

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  Dilacor XR (Diltiazem Hydrochloride Capsule, Extended Release) - new on RxList

Dilacor XR (Diltiazem Hydrochloride Capsule, Extended Release) drug description - FDA approved labeling for prescription drugs and medications at RxList (Source: RxList - New and Updated Drug Monographs)

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  Tiazac (Diltiazem Hcl) - updated on RxList

Tiazac (Diltiazem Hcl) drug description - FDA approved labeling for prescription drugs and medications at RxList (Source: RxList - New and Updated Drug Monographs)

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  Probable Amlodipine-Induced Angioedema (April).

CONCLUSIONS: Although few reports of CCB-induced angioedema exist, to our knowledge, this is the first reported case to suggest a link between angioedema and amlodipine therapy. Clinicians should consider amlodipine as a potential cause of angioedema. PMID: 19299323 [PubMed - as supplied by publisher] (Source: The Annals of Pharmacotherapy)

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  Voltage independent calcium channels mediate lipopolysaccharide-induced hyporeactivity to endothelin 1 in the rat aorta.

Authors: El-Awady MS, Smirnov SV, Watson ML The roles of intracellular calcium ([Ca(2+)]i) and Ca(2+) sensitization in lipopolysaccharide (LPS) induced vascular smooth muscle (VSM) hyporesponsiveness are incompletely understood. To investigate these roles, contraction responses to endothelin 1 (ET 1) and 80 mM KCl, relaxation responses to nifedipine, the expression levels of mRNAs of ET-1 and its receptors (ETA or ETB), the expression levels of protein kinase C (PKC) and phosphorylation of Rho kinase (ROKalpha), CPI-17 and MYPT1, and changes in aortic VSM cells [Ca(2+)]i were measured in LPS-treated aortic rings from male Wistar rats (250 300g). LPS (10 microg.ml(-1), 20 h) decreased contraction induced by ET 1 (0.3-100 nM) or 80 mM KCl. LPS induced hypocontractility was not observed i...

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  [Efficacy and safety of topical diltiazem 2 % in anal fissure.]

CONCLUSIONS: Despite not having found statistical differences between the analysed variables, treatment of anal fissures with 2 per cent diltiazem ointment has avoided surgery in nearly 50 % of patients, with few adverse effects. PMID: 19480795 [PubMed - in process] (Source: Farmacia Hospitalaria)

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  Influence of bupropion and calcium channel antagonists on the nicotine-induced memory-related response of mice in the elevated plus maze.

In this study, we investigated the effects of acute administration of nicotine on memory-related behavior in mice using the elevated plus maze test. In this test, the time necessary for mice to move from the open arm to the enclosed arm (i.e., transfer latency) was used as an index of memory. Our results revealed that nicotine (0.035 and 0.175 mg/kg, base, sc) shortened the transfer latency relative to the saline-treated group. Moreover, we investigated the effects of bupropion (10, 20 and 40 mg/kg, ip) and L-type voltage-dependent calcium channel antagonists (nimodipine, flunarizine, verapamil, diltiazem - 5, 10 and 20 mg/kg, ip) on memory-related behavior. At all tested doses, bupropion, did not significantly affect transfer latency. However, flunarizine and verapamil (both at 10 mg/kg) ...

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  Rhabdomyolysis Caused by a Potential Sitagliptin-Lovastatin Interaction

Pharmacotherapy 29(3): 352-356 Abstract A 75-year-old woman with diabetes mellitus, hypertension, and hyperlipidemia came to the emergency department with generalized and upper-extremity weakness; she had experienced a fall 2 months earlier. On admission, her drug therapy included lovastatin 40 mg/day, controlled-release diltiazem 240 mg/day, and glimepiride 1 mg/day. Nineteen days earlier, sitagliptin 100 mg/day had been started; it was discontinued 2 weeks later, and glimepiride was begun. A cardiology consultation performed on the day of admission determined that a markedly elevated creatine kinase-myocardial band isoenzyme level and borderline-high troponin I level were diagnostic of rhabdomyolysis secondary to statin use. Because the patient had been taking lovastatin for the past 12 ...

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  Comparison of internal sphincterotomy with topical diltiazem for post-hemorrhoidectomy pain relief: A prospective randomized trial

Conclusions: In patients undergoing hemorrhoidectomy, addition of surgical internal sphincterotomy results in lesser pain in the postoperative period as compared to those receiving topical application of Diltiazem. (Source: Journal of Postgraduate Medicine)

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  Acetylcholine induces Ca2+ signaling in chicken retinal pigmented epithelial cells during dedifferentiation.

Authors: Sekiguchi-Tonosaki M, Obata M, Haruki A, Himi T, Kosaka J Retinal pigmented epithelial cells exchange their cellular phenotypes into lens cells and neurons, via depigmented and non-epithelial shaped dedifferentiated intermediates. Because these dedifferentiated cells can either revert to pigmented epithelial cells or transdifferentiate into lens cells and/or neurons, they are recognized as candidates for lens and retinal cell regeneration. The purpose of the present study was to elucidate the signal transduction pathways between chicken retinal pigmented epithelial cells and their dedifferentiated intermediates. We monitored intracellular Ca(2+) concentrations using Fluo-4-based Ca(2+) optical imaging and focused on cellular responses to the neurotransmitter acetylcholine. Mus...

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  Differential Effects of Calcium-Channel Blockers on Vascular Endothelial Function in Patients With Coronary Spastic Angina.

Conclusions: Benidipine, but not diltiazem or verapamil, improves endothelial dysfunction beyond blood pressure lowering effects in patients with coronary vasospasm. Upregulation of the nitric oxide - cGMP system by benidipine may partly contribute to the improvement. The dihydropyridine class may be more beneficial for vascular endothelial function than the non-dihydropyridine classes of CCBs. PMID: 19225210 [PubMed - as supplied by publisher] (Source: Circulation Journal)

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  Extracting a needle from a haystack: reanalysis of whole genome data reveals a readily translatable finding.

Authors: Keers R, Farmer AE, Aitchison KJ There is significant unmet need for more effective treatments for bipolar disorder. The drug discovery process is becoming prohibitively expensive. Hence, biomarker clues to assist or shortcut this process are now widely sought. Using the publicly available data from the whole genome association study conducted by the Wellcome Trust Case Control Consortium, we sought to identify groups of genetic markers (single nucleotide polymorphisms) in which each marker was independently associated with bipolar disorder, with a less stringent threshold than that set by the original investigators (p1x10-4). We identified a group of markers occurring within the CACNA1C gene (encoding the alpha subunit of the calcium channel Cav1.2). We then ascertained that ...

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  Levosimendan does not improve survival time in a rat model of verapamil toxicity.

Conclusion: In this rat model, levosimendan as a solitary antidotal treatment for verapamil toxicity was not beneficial. PMID: 19191208 [PubMed - in process] (Source: Journal of Medical Toxicology)

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  Clinical benefits versus shortcomings of diltiazem once-daily in the chronotherapy of cardiovascular diseases

Expert Opinion on Pharmacotherapy , February 2009, Vol. 10, No. 3, Pages 485-491. (Source: Expert Opinion: Expert Opinion on Pharmacotherapy: Table of Contents)

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  Systematic electrocardioversion for atrial fibrillation and role of antiarrhythmic drugs: a substudy of the SAFE-T trial.

CONCLUSION: Amiodarone and sotalol facilitated successful electrocardioversion, which could be achieved in a stepwise fashion. Upon achievement of successful electrocardioversion, amiodarone is superior to placebo, and sotalol has a lesser effect. Antiarrhythmic drugs had no effect on the total number of energy step use in patients who had successful electrocardioversion. Calcium channel blockers had no influence on the success rate in achieving sinus rhythm. Successful electrocardioversion was associated with lower BMI and AF history < or =1 year. Lower energy use was associated with biphasic shocks, lower BMI, and AF duration < or =1 year. PMID: 19187902 [PubMed - in process] (Source: Heart Rhythm)

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  Effects of metoprolol and diltiazem on plasma homocysteine levels in patients with isolated coronary artery ectasia.

Authors: Demir M, Ozaydin M, Varol E, Doğan A, Altinbaş A PMID: 19196583 [PubMed - in process] (Source: Anadolu Kardiyol Der...)

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  Validation of cytochrome P450 time-dependent inhibition assays: a two-time point IC(50) shift approach facilitates k(inact) assay design.

Authors: Perloff ES, Mason AK, Dehal SS, Blanchard AP, Morgan L, Ho T, Dandeneau A, Crocker RM, Chandler CM, Boily N, Crespi CL, Stresser DM Recent guidance from the US Food and Drug Administration (USFDA) has advocated testing of time-dependent inhibition of cytochrome P450 (CYP), which can be addressed by performing IC(50) shift as well as K(I)/k(inact) determinations. Direct (IC(50), K(i)) and time-dependent inhibition (IC(50) shift, K(I)/k(inact)) assays were validated in human liver microsomes with liquid chromatography-tandem mass spectrometry (LC/MS/MS) analysis for the following enzyme/substrate/inhibitor combinations: CYP1A2/phenacetin/alpha-naphthoflavone/furafylline, CYP2C8/amodiaquine/montelukast/gemfibrozil-1-O-beta-glucuronide, CYP2C9/diclofenac/sulfaphenazole/tienilic ac...

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  Validation of cytochrome P450 time-dependent inhibition assays: a two-time point IC50 shift approach facilitates kinact assay design.

Authors: Perloff ES, Mason AK, Dehal SS, Blanchard AP, Morgan L, Ho T, Dandeneau A, Crocker RM, Chandler CM, Boily N, Crespi CL, Stresser DM 1. Recent guidance from the US Food and Drug Administration (USFDA) has advocated testing of time-dependent inhibition of cytochrome P450 (CYP), which can be addressed by performing IC(50) shift as well as K(I)/k(inact) determinations. 2. Direct (IC(50), K(i)) and time-dependent inhibition (IC(50) shift, K(I)/k(inact)) assays were validated in human liver microsomes with liquid chromatography-tandem mass spectrometry (LC/MS/MS) analysis for the following enzyme/substrate/inhibitor combinations: CYP1A2/phenacetin/alpha-naphthoflavone/furafylline, CYP2C8/amodiaquine/montelukast/gemfibrozil-1-O-beta-glucuronide, CYP2C9/diclofenac/sulfaphenazole/tieni...

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  The pharmacologic treatment of atrial fibrillation

Summary  The pharmacologic treatment of atrial fibrillation (AF) is aimed at controlling the ventricular response, restoring sinus rhythm, and preventing or delaying relapses. In the control of ventricular response, digitalis maintains a primary role when the arrhythmia is accompanied by heart failure. In ischemic, hypertensive, and degenerative (whose number is increasing at present) cardiopathies without evident ventricular dilatation, treatments with calcium antagonists (such as verapamil, gallopamil, or diltiazem) or beta-blocking agents must be preferred. In order to control the ventricular response in patients with chronic AF during physical activity, the association of digitalis with beta-blocking agents or calcium antagonists seems to provide satisfactory results. T...

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  Twenty-Four hour ambulatory blood pressure profile of a new slow-release formulation of diltiazem in mild to moderate hypertension

Summary  Twelve patients with mild to moderate essential hypertension were included in a double-blind, balanced, randomized placebo-controlled cross-over study to assess the efficacy and duration of action of a new slow-release formulation of diltiazem (300 mg) given once daily for 3 weeks. All office blood pressure measurements were done 24 hours after drug intake. In order to improve the accuracy of the trial, 24-hours non-invasive ambulatory blood pressure monitoring (Spacelabs 90207 system) were performed as well. Diltiazem significantly lowered supine and standing systolic and diastolic office blood pressure (by 16.9/12.7 mmHg and by 17.3/ 13.8 mmHg, respectively), without changing office heart rate. Diltiazem also significantly lowered ambulatory blood pressure measur...

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  Usefulness of diltiazem in the acute management of supraventricular tachyarrhythmias in the elderly

Summary  Acute management of supraventricular tachyarrhythmias is often difficult in elderly patients. Diltiazem was given intravenously (loading dose of 0.25 mg/kg over 2 minutes followed by a 4 mg/kg/24 hr infusion) in 37 elderly patients (mean age 70 years, range 60–91). Fifteen out of the 37 patients (41%) had left ventricular cardiac disease, 12 (32%) had cor pulmonale, and 10 (27%) had no obvious cardiac disease. Hemodynamic tolerance of the supraventricular tachyarrhythmia was poor in 12 patients. A good result was defined as a return to sinus rhythm after bolus or infusion, or as a slowing of the ventricular rate (VR) to less than 100 beats/min. Of the 23 patients in atrial fibrillation, about half reverted to sinus rhythm after diltiazem, and in most of the other...

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  diltiazem, Cardizem, Dilacor, Tiazac

Title: diltiazem, Cardizem, Dilacor, TiazacCategory: MedicationsCreated: 12/31/1997Last Editorial Review: 1/9/2009 (Source: MedicineNet Heart General)

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  Mesenteric lymph duct ligation prevents trauma/hemorrhage shock-induced cardiac contractile dysfunction

In conclusion, gut-derived factors carried in mesenteric lymph are responsible for acute T/HS-induced cardiac dysfunction. (Source: Journal of Applied Physiology)

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  CARTIA XT (Diltiazem Hydrochloride) Capsule [Watson Pharma, Inc.]

Updated Date: Jan 5, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  Role of Ca2+ mobilization and Ca2+ sensitization in 8-iso-PGF2α-induced contraction in airway smooth muscle

This study was designed to determine the intracellular mechanisms underlying the effects of oxidative stress on airway smooth muscle, focused on Ca2+ signalling pathways involved in the effect of 8-iso-PGF2[alpha]. Using simultaneous recording of isometric tension and F340/F380 (an indicator of intracellular concentrations of Ca2+, [Ca2+]i), we examined the correlation between tension and [Ca2+]i in response to 8-iso-PGF2[alpha] in the fura-2 loaded tracheal smooth muscle. Augmented tension and F340/F380 by 8-iso-PGF2[alpha] were attenuated by ICI-192605, an antagonist of thromboxane A2 receptors (TP receptors). Moreover, D609, an antagonist of phosphatidylcholine-specific phospholipase C, markedly reduced both the tension and F340/F380 induced by 8-iso-PGF2[alpha], whereas U73122, an anta...

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  Modulation of Human Peripheral Blood Mononuclear Cell Proliferative Response by Diltiazem: In Vitro Comparison in Younger versus Older Subjects.

Page: 87DOI: 10.2165/0002512-200926010-00007Authors: D'Ambrosio, Antonella 1; Giordani, Luciana 2; Colucci, Manuela 1; Vanacore, Nicola 3; Quintieri, Francesca 1 (Source: Drugs & Aging)

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  Modulation of Human Peripheral Blood Mononuclear Cell Proliferative Response by Diltiazem: In Vitro Comparison in Younger versus Older Subjects

(Source: Drugs)

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  Drug release mechanisms from ethylcellulose: PVA-PEG graft copolymer-coated pellets.

Authors: Muschert S, Siepmann F, Leclercq B, Carlin B, Siepmann J The aim of this study was to better understand the underlying drug release mechanisms from aqueous ethylcellulose-coated pellets containing different types of drugs and starter cores. Theophylline, paracetamol, metoprolol succinate, diltiazem HCl and metoprolol tartrate were used as model drugs exhibiting significantly different solubilities (e.g. 14, 19, 284, 662 and 800mg/mL at 37 degrees C in 0.1N HCl). The pellet core consisted of a drug matrix, drug-layered sugar bead or drug-layered microcrystalline cellulose (MCC) bead, generating different osmotic driving forces upon contact with aqueous media. Importantly, the addition of small amounts of poly(vinyl alcohol)-poly(ethylene glycol) graft copolymer (PVA-PEG graft c...

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  Arrhythmogenic actions of the Ca2+ channel agonist FPL-64716 in Langendorff-perfused murine hearts

The experiments explored the extent to which alterations in L-type Ca2+ channel-mediated Ca2+ entry triggers Ca2+-mediated arrhythmogenesis in Langendorff-perfused murine hearts through use of the specific L-type Ca2+ channel modulator FPL-64716 (FPL). Introduction of FPL (1 [mu]m) resulted in a gradual development (>10 min) of diastolic electrical events and alternans in spontaneously beating hearts from which monophasic action potentials were recorded. In regularly paced hearts, they additionally led to non-sustained and sustained ventricular tachycardia (nsVT and sVT). Programmed electrical stimulation (PES) resulted in nsVT and sVT after 5[ndash]10 and >10 min perfusion, respectively. Pretreatments with nifedipine, diltiazem and cyclopiazonic acid abolished arrhythmogenic tendency indu...

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  Inhibition of MDR1 Activity in Vitro by a Novel Class of Diltiazem Analogues: Toward New Candidates

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable). (Source: Journal of Medicinal Chemistry)

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  Microencapsulation by Spray Coagulation of Diltiazem HCl in Calcium Alginate-Coated Chitosan.

Authors: Tapia C, Montezuma V, Yazdani-Pedram M The aim of this work was to develop a procedure for encapsulation of diltiazem HCl by spray coagulation. Factors affecting the formulations such as the effect of NaCl on the solubility of diltiazem in alginate solution, surface tension, pH, viscosity of the coagulation medium, and the effect of drug load on drug release were studied. The drug load was increased substantially from 10 up to 320 mg/mL by adding 1.2% w/v NaCl in 1% w/v alginate solution. More stable microcapsules were obtained at pH 4.6 (acetate buffer) than at a pH 2.8 (lactic acid), and the microencapsulation process was favored by the type of chitosan that produced low turbidity and viscosity in the coagulation medium. A dose of 50 mg/mL of diltiazem HCl, 1.2% w/v NaCl, an...

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  Effect of diltiazem on kidney function during laparoscopic surgery

Conclusion  Continuous infusion of diltiazem 2 μg/kg/min prevented the decrease in CrCl during pneumoperitoneum without hemodynamic derangement. Although the decrease in CrCl was transient in patients with normal kidney function in this study, diltiazem may be used to prevent further kidney injury in those with elevated CrCl during laparoscopic surgery. Content Type Journal ArticleDOI 10.1007/s00464-008-0225-1Authors Ji Young Kim, Yonsei University College of Medicine Department of Anesthesiology and Pain Medicine, Anesthesia and Pain Research Institute Seoul KoreaKyung Cheon Lee, Gachon University of Medicine and Science Gil Medical Center Department of Anesthesiology and Pain Medicine 1198 Guwol-dong Namdong-gu Incheon 405-760 KoreaHong Soon Kim, Gachon University o...

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  Ion-channel blocker sensitivity of voltage-gated calcium-channel homologue Cch1 in Saccharomyces cerevisiae.

Authors: Teng J, Goto R, Iida K, Kojima I, Iida H The Cch1 protein of the yeast Saccharomyces cerevisiae is a homologue of the pore-forming alpha(1) subunit of mammalian voltage-gated Ca(2+) channels (VGCCs), and it constitutes a high-affinity Ca(2+)-influx system with the Mid1 protein in this organism. Here, we characterized the kinetic property of a putative Cch1-Mid1 Ca(2+) channel overexpressed in S. cerevisiae cells, and showed that the L-type VGCC blockers nifedipine and verapamil partially inhibited Cch1-Mid1 activity, but typical P/Q-, N-, R- and T-type VGCC blockers did not inhibit activity. In contrast, a third L-type VGCC blocker, diltiazem, increased Cch1-Mid1 activity. Diltiazem did not increase Ca(2+) uptake in the cch1Delta and mid1Delta single mutants and the cch1Delta ...

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  CARDIZEM LA (Diltiazem Hydrochloride) Tablet [Kos Pharmaceuticals, Inc.]

Updated Date: Nov 26, 2008 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  Microbial degradation of pharmaceuticals in estuarine and coastal seawater.

Authors: Benotti MJ, Brownawell BJ Microbial degradation rates were measured for 19 pharmaceuticals in estuarine and coastal surface water samples. Antipyrine, carbamazepine, cotinine, sulfamethoxazole, and trimethoprim were the most refractory (half-lives, t(1/2)=35 to >100 days), making them excellent candidates for wastewater tracers. Nicotine, acetaminophen, and fluoxetine were labile across all treatments (t(1/2)=0.68-11 days). Caffeine, diltiazem, and nifedipine were also and relatively labile in all but one of the treatments (t(1/2)=3.5-13 days). Microbial degradation of caffeine was further confirmed by production (14)CO(2). The fastest decay of non-refractory compounds was always observed in more sewage-affected Jamaica Bay waters. Degradation rates for the majority of thes...

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  A pilot comparative study of fissurectomy/diltiazem and fissurectomy/botulinum toxin in the treatment of chronic anal fissure

Conclusions  In this small pilot study fissurectomy combined with chemical sphincterotomy resulted in high short-term fissure healing rates. The study also suggested that fissurectomy followed by 8 weeks of topical DTC may be as good as fissurectomy with BTA injection in the treatment of CAF. A prospective study, adequately powered to determine the significance of differences is needed. Content Type Journal ArticleCategory Original ArticleDOI 10.1007/s10151-008-0444-4Authors J. D. Arthur, Arrowe Park Hospital Wirral Colorectal Unit Wirral, Merseyside UKC. A. Makin, Arrowe Park Hospital Wirral Colorectal Unit Wirral, Merseyside UKT. Y. El-Sayed, Arrowe Park Hospital Wirral Colorectal Unit Wirral, Merseyside UKC. J. Walsh, Arrowe Park Hospital Wirral Colorectal Unit Wirr...

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  Apparent seizure and atrial fibrillation associated with paliperidone.

CONCLUSION: A man taking paliperidone and multiple other drugs experienced atrial fibrillation and a possible seizure. Although these are known adverse effects of atypical antipsychotics, it is unusual to have both events occur concurrently and with low-to-average dosages, and these events have not been associated with paliperidone in published case reports. PMID: 18997140 [PubMed - in process] (Source: American Journal of Health-System Pharmacy : AJHP)

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  Prognostic effects of calcium channel blockers on cardiac events, stroke and end-stage renal disease in patients with angina pectoris. Retrospective comparative study of benidipine, diltiazem and nifedipine.

CONCLUSION: This study demonstrated that benidipine prevents the occurrence of cardiovascular events in patients with AP, suggesting that benidipine contributes to a favorable long-term prognosis of such patients. PMID: 18972872 [PubMed - in process] (Source: Arzneimittel-Forschung)

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  Calcium-Channel Blockers Reduce the Antiplatelet Effect of Clopidogrel

Conclusions Coadministration of CCBs is associated with decreased platelet inhibition by clopidogrel. (Source: Journal of the American College of Cardiology)

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  Effect of genetic polymorphisms of CYP3A5 and MDR1 on cyclosporine concentration during the early stage after renal transplantation in Chinese patients co-treated with diltiazem

Conclusion  This study demonstrated that the G2677T/A single nucleotide polymorphisms in MDR1 and MDR1 haplotypes C-G-C, T-G-T and T-T-C are associated with the CsA concentration during the very early post-transplant period in Chinese renal transplant patients co-treated with diltiazem. These polymorphisms may be useful for determining the appropriate initial dose of CsA after renal transplantation. Content Type Journal ArticleCategory PharmacogeneticsDOI 10.1007/s00228-008-0577-4Authors Yixi Wang, Sun Yat-sen University Institute of Clinical Pharmacology, School of Pharmaceutical Sciences Guangzhou Guangdong Province ChinaChangxi Wang, Sun Yat-sen University Department of Organ Transplant, The First Affiliated Hospital Guangzhou Guangdong Province ChinaJiali Li, Sun Y...

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  Diltiazem: Phototoxic eruption: case report

(Source: Reactions)

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  Diltiazem: Phototoxic eruption: case report.

Page: 14 (Source: Reactions Weekly)

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  Calcium-independent phospholipase A(2) mediates store-operated calcium entry in rat cerebellar granule cells.

Authors: Singaravelu K, Lohr C, Deitmer JW Store-operated Ca(2+) entry (SOCE) has been extensively studied in non-neuronal cells, such as glial cells and smooth muscle cells, in which Ca(2+)-independent phospholipase A(2) (iPLA(2)) has been shown to play a key role in the regulation of SOCE channels. In the present study, we have investigated the role of iPLA(2) for store-operated Ca(2+) entry in rat cerebellar granule neurons in acute brain slices using confocal Ca(2+) imaging. Depletion of Ca(2+) stores by cyclopiazonic acid (CPA) induced a Ca(2+) influx, which could be inhibited by SOCE channel blockers 2-aminoethoxy-diphenylborate (2-APB) and 3,5-bistrifluoromethyl pyrazole derivative (BTP2), but not by the voltage-operated Ca(2+) channel blocker diltiazem and by the Na+ channel bl...

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  Spatial and temporal analysis of pharmaceutical concentrations in the upper Tennessee River basin.

Authors: Conley JM, Symes SJ, Schorr MS, Richards SM The behavior of pharmaceutical compounds in aquatic ecosystems is not well defined. In order to determine spatial and temporal variations in concentrations of pharmaceuticals in the Tennessee River, water samples were collected from multiple points along the river and at the inflow of major tributaries. Sampling structure was designed to investigate trends between surface and subsurface samples, seasonal trends (winter, spring, summer, and fall), the direct influence of sewage treatment plants (upstream versus downstream), and the effect of downstream distance on pharmaceutical concentrations. All samples were quantified via solid phase extraction followed by liquid chromatography-tandem mass spectrometry (LC-MS/MS). This method yiel...

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  [2% diltiazem as initial treatment of chronic anal fissures.]

Authors: Bernal Sprekelsen JC, Lorente Fernández L, Landete Molina FJ, Morera Ocón F PMID: 18783683 [PubMed - in process] (Source: Cirugia eEspanola)

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  Discovery of Novel and Cardioselective Diltiazem-like Calcium Channel Blockers via Virtual Screening

Emanuele Carosati, Roberta Budriesi, Pierfranco Ioan, Maria P. Ugenti, Maria Frosini, Fabio Fusi, Gaetano Corda, Barbara Cosimelli, Domenico Spinelli, Alberto Chiarini, and Gabriele CrucianiWeb Release Date: Thu, 28 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800151n (Source: Journal of Medicinal Chemistry)

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  [Original articles] A comparative study on in vitro and in vivo effects of topical vasodilators in human internal mammary, radial artery and great saphenous vein

Conclusions: (1) Comparing with nicorandil, urapidil and diltiazem, nitroglycerin caused a significant relaxation in all three graft vessels tested. (2) Nitroglycerin, nicorandil and urapidil were more effective in preventing RA spasm than diltiazem. (Source: European Journal of Cardio-Thoracic Surgery)

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  Induction of P-glycoprotein expression and function in human intestinal epithelial cells (T84).

Authors: Haslam IS, Jones K, Coleman T, Simmons NL Intestinal induction of Pgp is known to limit the oral availability of certain drug compounds and give rise to detrimental drug-drug interactions. We have investigated the induction of P-glycoprotein (Pgp; MDR1) activity in a human intestinal epithelial cell line (T84) following pre-exposure to a panel of drug compounds, reported to be Pgp substrates, inhibitors or inducers. Human MDR1-transfected MDCKII epithelial monolayers were used to assess Pgp substrate interactions and inhibition of digoxin secretion by the selected drug compounds. The T84 cell line was used to assess induction of Pgp-mediated digoxin secretion following pre-exposure to the same compounds. Changes in gene expression (MDR1, MRP2, PXR and CAR) were determined by q...

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  Impaired GFR exacerbates microalbuminuria-associated CV risk

The level of cardiovascular risk associated with microalbuminuria in hypertensive patients rises as their glomerular filtration rate declines, show data from the Nordic Diltiazem Study. (Source: MedWire News - Hypertension)

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  Impaired GFR exacerbates microalbuminuria-associated CV risk

The level of cardiovascular risk associated with microalbuminuria in hypertensive patients rises as their glomerular filtration rate declines, show data from the Nordic Diltiazem Study. (Source: MedWire News - Cardiology)

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  Diltiazem/metoprolol: Ventricular fibrillation (first report) in a patient with Wolff-Parkinson-White syndrome: case report

(Source: Reactions)

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  Diltiazem/metoprolol: Ventricular fibrillation (first report) in a patient with Wolff-Parkinson-White syndrome: case report.

Page: 12 (Source: Reactions Weekly)

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  Effects of amiloride, benzamil, and alterations in extracellular Na+ on the rat afferent arteriole and its myogenic response

Recent studies have implicated epithelial Na+ channels (ENaC) in myogenic signaling. The present study was undertaken to determine if ENaC and/or Na+ entry are involved in the myogenic response of the rat afferent arteriole. Myogenic responses were assessed in the in vitro hydronephrotic kidney model. ENaC expression and membrane potential responses were evaluated with afferent arterioles isolated from normal rat kidneys. Our findings do not support a role of ENaC, in that ENaC channel blockers did not reduce myogenic responses and ENaC expression could not be demonstrated in this vessel. Reducing extracellular Na+ concentration ([Na+]o; 100 mmol/l) did not attenuate myogenic responses, and amiloride had no effect on membrane potential. Benzamil, an inhibitor of ENaC that also blocks Na+/C...

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  Preliminary investigation on the development of diltiazem resin complex loaded carboxymethyl xanthan beads.

The objective of this study was to develop a multiunit sustained release dosage form of diltiazem using a natural polymer from a completely aqueous environment. Diltiazem was complexed with resin and the resinate-loaded carboxymethyl xanthan (RCMX) beads were prepared by interacting sodium carboxymethyl xanthan (SCMX), a derivatized xanthan gum, with Al(+3) ions. The beads were evaluated for drug entrapment efficiency (DEE) and release characteristics in enzyme free simulated gastric fluid (SGF, HCl solution, pH 1.2) and simulated intestinal fluid (SIF, USP phosphate buffer solution, pH 6.8). Increase in gelation time from 5 to 20 min and AlCl(3) concentration from 1 to 3% decreased the DEE respectively from 95 to 79% and 88.5 to 84.6%. However, increase in gum concentration from 1.5 to 2....

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  Evaluation of Sterculia foetida gum as controlled release excipient.

Authors: Chivate AA, Poddar SS, Abdul S, Savant G The purpose of the research was to evaluate Sterculia foetida gum as a hydrophilic matrix polymer for controlled release preparation. For evaluation as a matrix polymer; characterization of Sterculia foetida gum was done. Viscosity, pH, scanning electronmicrographs were determined. Different formulation aspects considered were: gum concentration (10-40%), particle size (75-420 microm) and type of fillers and those for dissolution studies; pH, and stirring speed were considered. Tablets prepared with Sterculia foetida gum were compared with tablets prepared with Hydroxymethylcellulose K15M. The release rate profiles were evaluated through different kinetic equations: zero-order, first-order, Higuchi, Hixon-Crowell and Korsemeyer and Pepp...

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  Recent advances in the pharmacotherapy of chronic anal fissure: an update.

Authors: Medhi B, Rao RS, Prakash A, Prakash O, Kaman L, Pandhi P Surgical sphincterotomy reduces anal tone and sphincter spasm and promotes ulcer healing. Because the surgery is associated with the side effect of faecal incontinence, pharmacological agents to treat chronic anal fissure have been explored recently. Glyceryl trinitrate (GTN) ointment (0.2%) has an efficacy of up to 68% in healing chronic anal fissure, but it is associated with headache as the major and most common side effect. Though botulinum toxin injected into the anal sphincter healed over 80% of chronic anal fissures, it is more invasive and expensive than GTN therapy. Diltiazem ointment achieved healing of chronic anal fissure comparable to 0.2% GTN ointment but was associated with fewer side effects. Other drugs ...

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  Brain natriuretic peptide secretion in adult rat heart muscle cells: The role of calcium channels.

CONCLUSION: These results suggest that transmembrane calcium channels may have an important role in the regulation of BNP secretion. PMID: 18848688 [PubMed - as supplied by publisher] (Source: Archives of Cardiovascular Diseases)

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  Prevalence of adverse drug combinations in a large post-mortem toxicology database

Abstract  The prevalence of important adverse drug combinations was studied among the 37,367 cases included in the Finnish post-mortem toxicology database during 2000–2006. The new SFINX interaction database (Swedish, Finnish, INteraction X-referencing) was utilised to identify adverse drug combinations. Consequently, the 24 drugs chosen for the study generated 96 two-compound combinations possessing potentially severe interactions. The total number of hits for the combinations found in the post-mortem database was 267, which accounts for approximately 0.71% of all cases. The potential role of adverse drug interaction (ADI) in these cases was evaluated from the background information and death certificate. The possible ADI cases comprised 23% of all hits and 0.17% of all ...

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  Taztia Xt(Diltiazem Hydrochloride) Capsule, Extended Release [Watson Pharma, Inc.]

Updated Date: Jun 27, 2008 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  Extended release of a large amount of highly water-soluble diltiazem hydrochloride by utilizing counter polymer in polyethylene oxides (PEO)/polyethylene glycol (PEG) matrix tablets.

Authors: Kojima H, Yoshihara K, Sawada T, Kondo H, Sako K The purpose of this study was to evaluate the feasibility of using a counter polymer in polyethylene oxide (PEO)/polyethylene glycol (PEG) polymeric matrices for the sustained release of a large amount of highly water-soluble drug. PEO/PEG matrix tablets (CR-A) containing four drugs with different water solubilities were prepared to investigate the effect of drug solubility on the drug-release and diffusion properties of PEO/PEG matrices. Cross-linked carboxyvinyl polymer (CVP)/PEO/PEG matrix tablets (CR-B) containing a water-soluble drug, diltiazem hydrochloride (DTZ), were also prepared, and their in vitro characteristics were compared with those of CR-A. Their in vitro drug release properties were evaluated using a dissolutio...

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  Lessons learnt in the pharmacokinetic analysis of the effect of haemoperfusion for acute overdose with sustained-release diltiazem

Anaesthesia, Volume 63, Issue 7, Page 714-718, July 2008. SummaryThe effect of charcoal haemoperfusion on the pharmacokinetics of diltiazem is described in a patient with severe clinical toxicity following acute overdose. The patient presented within 3 h following acute ingestion of multiple medications ... (Source: Anaesthesia)

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  [The comparison between the efficiency of different anti-arrhythmic agents in preventing postoperative atrial fibrillation after open heart surgery.]

CONCLUSION: Any anti-arrhythmic agent started 7 days before the operation and continued for 10 days, may reduce the prevalence of postoperative AF, morbidity and duration of hospitalization. However, we found that sotalol and amiodarone were more effective than other anti-arrhythmic agents in our patient population. PMID: 18524727 [PubMed - as supplied by publisher] (Source: Anadolu Kardiyol Der...)

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  Alteration in prehospital drug concentration after thermal exposure.

CONCLUSION: A decrease in concentration was found to be statistically significant in 8 (35%) of 23 commonly carried emergency medical services pharmaceuticals. These results provide new information and perspective regarding stability of emergency drugs in the prehospital environment by evaluating a broad range of pharmaceuticals as well as by using thermal exposure points that have been documented in the United States. PMID: 18534286 [PubMed - in process] (Source: The American Journal of Emergency Medicine)

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  Precipitation of ventricular fibrillation by intravenous diltiazem and metoprolol in a young patient with occult Wolff-Parkinson-White syndrome.

We report the case of a young man who presented with a rapid, narrow-complex atrial fibrillation. A few hours after being administered intravenous metoprolol and diltiazem for rate control, he developed intermittent ventricular preexcitation on the electrocardiogram (ECG) and experienced ventricular fibrillation, from which he was successfully defibrillated. A subsequent electrocardiogram in sinus rhythm demonstrated previously unknown Wolff-Parkinson-White pattern. A left lateral accessory pathway was successfully ablated. Wolff-Parkinson-White syndrome should be included in the differential diagnosis when a young patient presents with atrial fibrillation, even if the ventricular complexes on the ECG are not preexcited. PMID: 18507555 [PubMed - indexed for MEDLINE] (Source: Pacing and...

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  Regulatory Role of Calcium Channel Blockers on Spontaneous Muscular Activity of Gastrothylax Crumenifer, A Rumen Amphistome

Major proportion of intracellular calcium (Ca2+) is achieved through opening of calcium channels present in the plasma membrane which play an important role in regulating neuromuscular coordination and release of neurotransmitters from nerve terminals. Blockade of these calcium channels adversely affect contractile process and release of neurotransmitters in majority of the neuromuscular preparations in vitro. In present study, the cumulative addition of verapamil (10-7-10-3 M) caused marked excitation in amplitude, baseline tension and frequency of spontaneous muscular activity of Gastrothylax crumenifer a rumen amphistome. Diltiazem (10-6-10-3 M) caused a significant and concentration-dependent increase in amplitude and frequency of spontaneous muscular activity of isometrically mounted ...

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  The Effects of Amiloride, Benzamil and Alterations in Extracellular Sodium on the Rat Afferent Arteriole and its Myogenic Response.

Authors: Wang X, Takeya K, Aaronson PI, Loutzenhiser K, Loutzenhiser RD Recent studies have implicated epithelial sodium channels (ENaC) in myogenic signaling. The present study was undertaken to determine if ENaC and/or Na(+ )entry are involved in the myogenic response of the rat afferent arteriole. Myogenic responses were assessed in the in vitro hydronephrotic kidney model. ENaC expression and membrane potential responses were evaluated with afferent arterioles isolated from normal rat kidneys. Our findings do not support a role of ENaC, in that ENaC channel blockers did not reduce myogenic responses and ENaC expression could not be demonstrated in this vessel. Reducing extracellular [Na(+)] ( [Na(+)]o; 100 mmol/L) did not attenuate myogenic responses and amiloride had no effect on ...

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  AGS: A Little Anticholinergic Burden Can Be Disabling

WASHINGTON -- Drugs not usually thought of as anticholinergics -- such as furosemide (Lasix) and diltiazem (Cardizem) -- could lead to functional impairment when taken in combination, researchers reported here. (Source: MedPage Today Primary Care)

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  Drugs Behave as Substrates, Inhibitors and Inducers of Human Cytochrome P450 3A4.

Authors: Zhou SF Human cytochrome P450 (CYP) 3A4 is the most abundant hepatic and intestinal phase I enzyme that metabolizes approximately 50% marketed drugs. The crystal structure of bound and unbound CYP3A4 has been recently constructed, and a small active site and a peripheral binding site are identified. A recent study indicates that CYP3A4 undergoes dramatic conformational changes upon binding to ketoconazole or erythromycin with a differential but substantial (>80%) increase in the active site volume, providing a structural basis for ligand promiscuity of CYP3A4. A number of important drugs have been identified as substrates, inducers and/or inhibitors of CYP3A4. The ability of drugs to act as inducers, inhibitors, or substrates for CYP3A is predictive of whether concurrent ad...

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  Oxyhemoglobin-Induced Expression of R-Type Ca2+ Channels in Cerebral Arteries.

CONCLUSIONS: These results demonstrate that oxyhemoglobin exposure for 5 days induces the expression of CaV 2.3 in cerebral arteries. We propose that oxyhemoglobin contributes to enhanced cerebral artery constriction after SAH via the emergence of R-type VDCCs. PMID: 18436877 [PubMed - as supplied by publisher] (Source: Stroke)

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