|
Diltiazem
resources
|
|
|
|
|
|
DRUG INFO
Diltiazem
Drug Name:
Diltiazem
Indication: For the treatment of Hypertension
Pharmacology: Diltiazem, a benzothiazepine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Diltiazem is similar to other peripheral vasodilators. Diltiazem inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Mechanism Of Action: Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, dilitiazem, like verapamil, inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue.
Drug Category: Vasodilator Agents; Cardiovascular Agents; Antihypertensive Agents; Calcium-channel blocking agents; ATC:C08DB01
Brand Names/Synonyms: Acalix; Anoheal; Adizem; Altiazem; Anginyl; Angizem; Apo-Diltiaz; Britiazim; Bruzem; Calcicard; Cardizem; Cardizem CD; Cardizem SR; Cardizen LA; Cartia XT; Citizem; Cormax; Deltazen; Dilacor; Dilacor-XR; Diladel; Dilcontin; Dilpral; Dilrene; Dilt-cd; Dilta-Hexal; Diltia; Dilticard; Dilzem; Dilzen; Endrydil; Herbesser; Incoril AP; Masdil; Novo-Diltazem; Nu-Diltiaz; Syn-Diltiazem; Tiazac Tildiem; d-cis-Diltiazem
Dosage Forms: SOLUTION
Absorption: Diltiazem is well absorbed from the gastrointestinal tract but undergoes substantial hepatic first-pass effect.
Interactions: Interactions for Diltiazem:
Due to the potential for additive effects, caution and careful titration are warranted in patients receiving diltiazem hydrochloride concomitantly with other agents known to affect cardiac contractility and/or conduction. Pharmacologic studies indicate that there may be additive effects in prolonging AV conduction when using beta-blockers or digitalis concomitantly with Tiazac. As with all drugs, care should be exercised when treating patients with multiple medications. Diltiazem is both a substrate and an inhibitor of the cytochrome P-450 3A4 enzyme system. Other drugs that are specific substrates, inhibitors, or inducers of the enzyme system may have a significant impact on the efficacy and side effect profile of diltiazem. Patients taking other drugs that are substrates of CYP450 3A4, especially patients with renal and/or hepatic impairment, may require dosage adjustment when starting or stopping concomitantly administered diltiazem in order to maintain optimum therapeutic blood levels.
Beta Blockers
Controlled and uncontrolled domestic studies suggest that concomitant use of diltiazem hydrochloride and beta-blockers is usually well tolerated, but available data are not sufficient to predict the effects of concomitant treatment in patients with left ventricular dysfunction or cardiac conduction abnormalities. Administration of diltiazem hydrochloride concomitantly with propranolol in five normal volunteers resulted in increased propranolol levels in all subjects and bioavailability of propranolol was increased approximately 50%. In vitro, propranolol appears to be displaced from its binding sites by diltiazem. If combination therapy is initiated or withdrawn in conjunction with propranolol, an adjustment in the propranolol dose may be warranted.
Cimetidine
A study in six healthy volunteers has shown a significant increase in peak diltiazem plasma levels (58%) and AUC (53%) after a 1-week course of cimetidine 1200 mg/day and a single dose of diltiazem 60mg. Ranitidine produced smaller, nonsignificant increases. The effect may be mediated by cimetidine's known inhibition of hepatic cytochrome P-450, the enzyme system responsible for the first-pass metabolism of diltiazem. Patients currently receiving diltiazem therapy should be carefully monitored for a change in pharmacological effect when initiating and discontinuing therapy with cimetidine. An adjustment in the diltiazem dose may be warranted.
Digitalis
Administration of diltiazem hydrochloride with digoxin in 24 healthy male subjects increased plasma digoxin concentrations approximately 20%. Another investigator found no increase in digoxin levels in 12 patients with coronary artery disease. Since there have been conflicting results regarding the effect of digoxin levels, it is recommended that digoxin levels be monitored when initiating, adjusting, and discontinuing diltiazem hydrochloride therapy to avoid possible over- or under-digitalization.
Anesthetics
The depression of cardiac contractility, conductivity, and automaticity as well as the vascular dilation associated with anesthetics may be potentiated by calcium channel blockers. When used concomitantly, anesthetics and calcium channel blockers should be titrated carefully.
Cyclosporine
A pharmacokinetic interaction between diltiazem and cyclosporine has been observed during studies involving renal and cardiac transplant patients. In renal and cardiac transplant recipients, a reduction of cyclosporine dose ranging from 15% to 48% was necessary to maintain cyclosporine trough concentrations similar to those seen prior to the addition of diltiazem. If these agents are to be administered concurrently, cyclosporine concentrations should be monitored, especially when diltiazem therapy is initiated, adjusted, or discontinued.
The effect of cyclosporine on diltiazem plasma concentrations has not been evaluated.
Carbamazepine
Concomitant administration of diltiazem with carbamazepine has been reported to result in elevated serum levels of carbamazepine (40% to 72% increase), resulting in toxicity in some cases. Patients receiving these drugs concurrently should be monitored for a potential drug interaction.
Benzodiazepines
Studies showed that diltiazem increased the AUC of midazolam and triazolam by 3-4 fold and the Cmax by 2-fold, compared to placebo. The elimination half life of midazolam and triazolam also increased (1.5-2.5 fold) during coadministration with diltiazem. These pharmacokinetic effects seen during diltiazem coadministration can result in increased clinical effects (e.g., prolonged sodation)of both midazolam and triazolam.
Lovastatin
In a ten-subject study, coadministration of diltiazem (120 mg bid) with lovastatin resulted in a 3-4 times increase in mean lovastatin AUC and Cmax vs. lovastatin alone; no change in pravastatin AUC and Cmax was observed during diltiazem coadministration. Diltiazem plasma levels were not significantly affected by lovastatin or pravastatin.
Rifampin
Coadministration of rifampin with diltiazem lowered the diltiazem plasma concentrations to undetectable levels. Coadministration of diltiazem with rifampin or any known CYP3A4 inducer should be avoided when possible, and alternative therapy considered.
Chemical IUPAC Name: [2-(2-dimethylaminoethyl)-5-(4-methoxyphenyl)-3-oxo-6-thia-2-azabicyclo[5.4.0]undeca-7,9,11-trien-4-yl]ethanoate
Chemical Formula: C22H26N2O4S
Half Life: 3.0 - 4.5 hours
Drug Type: Approved Drug
# Accession No: APRD00473
CAS Registry Number: 42399-41-7
|
|
|
|
|
|
Diltiazem News
(When available)
When Abroad, Beware of Drug Name Confusion Feb 8, 2006
...confusion can be harmful was made evident recently by the case of a Michigan man who was traveling in Serbia when he ran out of Dilacor (diltiazem), which he ... - Diabetes Self Management
KV Pharmaceutical Reports Record Revenues for Fiscal 2006 Third ... Feb 7, 2006
We are also currently waiting approvals for Diltiazem (Tiazac(R) - Biovail/Forest) and Levothyroxine (Levoxyl(R) - King), which we expect to receive this ... - PR Newswire (press release),
FDA: Drug Name Confusion Makes Imports Dangerous Jan 16, 2006
The case involved a patient traveling in Serbia who ran out of his prescription for Dilacor XR (diltiazem extended release), which is used to treat high blood ... - Forbes
FDA Cautions Consumers Against Filling US Prescriptions Abroad Jan 11, 2006
...an active ingredient different from the product in the US ISMP described a patient who traveled to Serbia and ran out of Dilacor XR (diltiazem extended release ... - PharmaLive.com (press release),
Big, muscular heart can lead to big trouble — even death Jan 24, 2006
Many medicines are used to assist these hearts in pumping with greater ease — beta blockers, verapamil and diltiazem are examples. ... - SouthCoastToday.com,
Elan meldt financiële resultaten vierde kwartaal en hele jaar ... Jan 31, 2006
4.5 45.4 8.7 7.8 Verelan(TM) 27.8 34.7 2.7 3.2 Skelaxin(TM) 12.2 17.9 3.5 2.7 Ritalin(TM) 11.8 13.8 4.9 4.3 Avinza(TM) 15.8 13.4 4.1 5.8 Diltiazem(TM) 19.3 ... - Netherlands Corporate News (persbericht),
Patients' Genes Can Be Bad Medicine Jan 12, 2006
These drugs included the antidepressant fluoxetine, the beta blocker metoprolol, the high blood pressure drug diltiazem and the anticoagulant warfarin. ... - Forbes
Genes’ influence on common drugs may affect health-care quality ... Jan 9, 2006
Among these drugs are fluoxetine (Prozac™), metoprolol (a beta-blocker), diltiazem (used to treat high blood pressure), and warfarin (an anticoagulant). ... - innovations report,
Here we go, down the hole, chasing a Part D drug plan Jan 14, 2006
Newsday, But a 30-day supply of most brand-name maintenance drugs (such as Celebrex, Paxil, Lipitor, Cardizem and Pravachol) for which there are no generics, carries co ...
US warns of brand errors in imported drugs Jan 12, 2006
International Herald Tribune, The agency's notice cited the example of a patient who ran out of Dilacor XR, a blood-pressure medicine, while traveling in Serbia. ...
FDA Cautions Consumers Against Filling US Prescriptions Abroad Jan 11, 2006
PharmaLive.com (press release), ...an active ingredient different from the product in the US ISMP described a patient who traveled to Serbia and ran out of Dilacor XR (diltiazem extended release ...
US warns of brand errors in imported drugs Jan 12, 2006
International Herald Tribune, The agency's notice cited the example of a patient who ran out of Dilacor XR, a blood-pressure medicine, while traveling in Serbia. ...
FDA Cautions Consumers Against Filling US Prescriptions Abroad Jan 11, 2006
PharmaLive.com (press release), US but contained an active ingredient different from the product in the US ISMP described a patient who traveled to Serbia and ran out of Dilacor XR (diltiazem ...
Sosei, HRA, and Sandoz/Hexal Australia to Conclude Sublicensing ... Dec 21, 2005
Japan Corporate News (press release), Sosei has announced that it and French pharmaceutical Laboratoire HRA Pharma (HRA) have entered into a sublicensing agreement with Sandoz/Hexal Australia, a ...
Novartis May Bid for Serono Jan 10, 2006
Red Herring, It also snapped up two generic drugmakers, Hexal and Eon Labs, in 2005 for a total of $8.5 billion (see Novartis Divests to Get Eon). ...
Novartis, the Great Consolidator Jan 10, 2006
TheStreet.com And they should get an idea how the generic drug company acquisitons -- Germany's Hexal and the US's Eon Labs -- helped Novartis close out 2005. ...
Benefit cheat caught Dec 15, 2005
News Shopper, She was arrested following an anonymous tip-off to Lewisham Council and her home in Hexal Road, Catford, was raided by police in April last year. ...
Novartis confirms eyeing Berna Biotech counter bid UPDATE Dec 18, 2005
Forbes It recently announced an agreed 5.1 bln usd acquisition of the 58 pct it did not already own in Chiron, it bought generics makers Hexal and Eon Labs for some 8 ...
Novartis May Counter Crucell Offer for Berna Biotech (Update2) Dec 18, 2005
Bloomberg The Chiron acquisition was Novartis' third major purchase this year, coming after the buy of German generic-drug maker Hexal AG and its US affiliate Eon Labs ...
Burrill's Biotech Outlook for 2006 ...and a Look Back at 2005 Dec 22, 2005
Canada NewsWire (press release), Some examples: Big pharma/pharma: Teva/Ivax $7.4 billion Novartis/Hexal $7.3 billion Solvay/Fournier $1.7 billion Big pharma/biotech: Novartis/Chiron $5.1 ...
|
|
|
