Diltiazem detailed information

Diltiazem detailed information

Clinical data
Pregnancy category	D: (USA)
Routes of administration	Oral
ATC code	C08DB01 (WHO)
Pharmacokinetic data
Bioavailability	40%
Metabolism	Hepatic
Elimination half-life	3-4.5 hours
Excretion	Renal Biliary Lactic (in lactiferous females)
Identifiers
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
CAS Number	42399-41-7
PubChem CID	39186
DrugBank	APRD00473
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C22H26N2O4S
Molar mass	414.519 g/mol

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Diltiazem is a member of the group of drugs known as benzothiazepines, which are a class of calcium channel blockers, used in the treatment of hypertension, angina pectoris, and some types of arrhythmia. It is a class 3 anti-anginal drug, and a class IV antidysrhythmic. It incites very minimal reflex sympathetic changes.

Diltiazem is a potent vasodilator, increasing blood flow and variably decreasing the heart rate via strong depression of A-V node conduction. Its pharmacolgical activity is somewhat similar to verapamil.

Diltiazem is metabolized by and acts as an inhibitor of the CYP3A4 enzyme.

Diltiazem is relatively contraindicated in the presence of sick sinus syndrome, atrioventricular node conduction disturbances, bradycardia, impaired left ventricle function, peripheral artery occlusive disease, chronic obstructive pulmonary disease, and Prinzmetal's angina.

Brand names

• Cardizem
• Cartia XT
• Tiazac
• Tiazac XC
• Tiamate
• Tildiem in particular in Europe
• Adizem
• Viazem
• Dilatam
• Dilzem
• Angiozem
• Dilatem
• Dilcardia
• Diltelan
• Diltime
• Dyalec
• Filazem
• Tildiem
• Vasmulax
• Zandil
• Zemtrial

Therapeutic effects

Potent vasodilator of coronary vessels.

Vasodilator of peripheral vessels. This reduces peripheral resistance and afterload.

Negative inotropic effect. Diltiazem causes a modest decrease in contractility and reduces myocardium oxygen consumption.

Negative chronotropic effect. Diltiazem causes a modest lowering of heart rate. This effect is due to slowing of the SA node. It results in reduced myocardium oxygen consumption.

Negative dromotropic effect. By slowing conduction through the AV node, diltiazem increases the time needed for each beat. This results in reduced myocardium oxygen consumption.

Nontherapeutic effects and toxicities

• Reflex sympathetic response. Caused by the peripheral dilatation of vessels and the resulting drop in BP; the response works to counteract the inotropic, chronotropic and dromotropic effects of diltiazem.
• Hypotension
• Bradycardia
• Dizziness
• Flushing

Indications

Stable (exercise-induced) Angina. Diltiazem increases coronary blood flow and decreases myocardial oxygen consumption, secondary to decreased peripheral resistance, heart rate, and contractility.

Variant Angina. Diltiazem is effective due to its direct effects on coronary dilatation.

Unstable (preinfarction, crescendo) Angina. Diltiazem may be particularly effective if the underlying mechanism is vasospasm. Supraventricular tachycardias. Diltiazem appears to be as effective as verapamil in treating reentrant supraventricular tachycardia.

Atrial fibrillation or flutter.

Hypertension. Because of its vasodilatatory effects, diltiazem is useful for treating hypertension. Calcium channel blockers are well-tolerated, and especially effective in treating low-renin hypertension.

Contraindications and precautions

CHF. Patients with reduced ventricular function may not be able to counteract the inotropic and chronotropic effects of diltiazem, the result being an even higher compromise of function.

SA node or AV conduction disturbances. Use of diltiazem should be avoided in patients with SA or AV nodal abnormalities, because of its negative chronotropic and dromotropic effects Low blood pressure. Patients with systolic blood pressures below 90 mm Hg should not be treated with diltiazem.

Wolff-Parkinson-White syndrome. Diltiazem may paradoxically increase ventricular rate in patients with WPW syndrome because of accessory conduction pathways.

Drug interactions

Beta blockers

Intravenous diltiazem should never be used concurrently with a beta-blocker as AV node block may result.

Quinidine

Quinidine should not be used concurrently with calcium channel blockers because of reduced clearance of both drugs and potential pharmacodynamic effects at the SA and AV nodes.

Miscellaneous

Inhibition of hepatic enzymes. Diltiazem and verapamil inhibit hepatic cytochromes CYP3A4, CYP2C9 and CYP2D6, possibly resulting in drug interactions.

Potential future indications

Recent research has shown that diltiazem is able to reduce cocaine cravings in drug addicted rats.[2] This is believed to be due to the effects of calcium blockers on dopaminergic and glutamatergic signalling in the brain.

Diltiazem is also being used to aid in the treatment of anal fissures and hemhorroids. However, it is not taken orally. It is made into a cream form using either vaseline or Phlogel. Phlogel absorbs the diltiazem into the problem area better than the vaseline base. It has excellent success rates.

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