Clinical Information
Gen. Code and Des.
16424 diltiazem HCl INTRAVEN VIAL 5 MG/ML
GCN and Des.
2641 diltiazem HCl INTRAVEN VIAL 5 MG/ML
Strength
25MG
Dose Form
VIAL (ML)
Product Category
RX Pharmaceuticals
Fine Line Class
850085008510 All Rx Products
DEA Class
NC
OMP Family
AHFS Class
24289200 CALCIUM-CHANNEL BLOCKING AGENTS, MISC.
24081292 CALCIUM-CHANNEL BLOCK.AGT,MISC(HYPOTEN)
24280000 CALCIUM-CHANNEL BLOCKING AGENTS
24081200 CALCIUM-CHANNEL BLOCKING AGENTS(HYPOTEN)
24129200 VASODILATING AGENTS, MISCELLANEOUS
24040424 CLASS IV ANTIARRHYTHMICS
Active Ingredients
711 diltiazem HCl 33286225
Inactive Ingredients
2332 sodium citrate 68042
2599 sorbitol 50704
DILTIAZEM HYDROCHLORIDE- diltiazem hydrochloride tablet, film coated
Mylan Pharmaceuticals Inc.
DESCRIPTION
Diltiazem hydrochloride is a calcium ion cellular influx inhibitor (slow channel blocker or calcium antagonist). Chemically, diltiazem hydrochloride is 1,5-Benzothiazepin-4(5H)one, 3-(acetyloxy)-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl), monohydrochloride, (+)-cis-
Diltiazem hydrochloride, USP is a white to off-white crystalline powder with a bitter taste. It is soluble in water, methanol, and chloroform. It has a molecular weight of 450.99. Each tablet, for oral administration, contains 30 mg, 60 mg, 90 mg, or 120 mg diltiazem hydrochloride. In addition, each tablet contains the following inactive ingredients: ethylcellulose, hypromellose, lactose monohydrate, magnesium stearate, maltodextrin, polyethylene glycol, and sodium lauryl sulfate.
For oral administration.
CLINICAL PHARMACOLOGY
The therapeutic benefits achieved with diltiazem hydrochloride tablets are believed to be related to its ability to inhibit the influx of calcium ions during membrane depolarization of cardiac and vascular smooth muscle.
Mechanisms of Action
Although precise mechanisms of its antianginal actions are still being delineated, diltiazem is believed to act in the following ways:
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Angina Due to Coronary Artery Spasm: Diltiazem hydrochloride tablets have been shown to be a potent dilator of coronary arteries both epicardial and subendocardial. Spontaneous and ergonovine-induced coronary artery spasms are inhibited by diltiazem.
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Exertional Angina: Diltiazem hydrochloride tablets have been shown to produce increases in exercise tolerance, probably due to its ability to reduce myocardial oxygen demand. This is accomplished via reductions in heart rate and systemic blood pressure at submaximal and maximal exercise workloads.
In animal models, diltiazem interferes with the slow inward (depolarizing) current in excitable tissue. It causes excitation-contraction uncoupling in various myocardial tissues without changes in the configuration of the action potential. Diltiazem produces relaxation of coronary vascular smooth muscle and dilation of both large and small coronary arteries at drug levels which cause little or no negative inotropic effect. The resultant increases in coronary blood flow (epicardial and subendocardial) occur in ischemic and nonischemic models and are accompanied by dose-dependent decreases in systemic blood pressure and decreases in peripheral resistance.
INDICATIONS AND USAGE
Diltiazem hydrochloride tablets are indicated for the management of chronic stable angina and angina due to coronary artery spasm.
CONTRAINDICATIONS
Diltiazem hydrochloride tablets are contraindicated in:
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Patients with sick sinus syndrome except in the presence of a functioning ventricular pacemaker
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Patients with second- or third-degree AV block except in the presence of a functioning ventricular pacemaker
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Patients with hypotension (less than 90 mm Hg systolic)
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Patients who have demonstrated hypersensitivity to the drug
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Patients with acute myocardial infarction and pulmonary congestion documented by X-ray on admission
WARNINGS
1. Cardiac Conduction
Diltiazem hydrochloride tablets prolong AV node refractory periods without significantly prolonging sinus node recovery time, except in patients with sick sinus syndrome. This effect may rarely result in abnormally slow heart rates (particularly in patients with sick sinus syndrome) or second- or third-degree AV block (six of 1,243 patients for 0.48%). Concomitant use of diltiazem with beta-blockers or digitalis may result in additive effects on cardiac conduction. A patient with Prinzmetal's angina developed periods of asystole (2 to 5 seconds) after a single dose of 60 mg of diltiazem hydrochloride tablets (see ADVERSE REACTIONS).
2. Congestive Heart Failure
Although diltiazem has a negative inotropic effect in isolated animal tissue preparations, hemodynamic studies in humans with normal ventricular function have not shown a reduction in cardiac index nor consistent negative effects on contractility (dP/dt). Experience with the use of diltiazem hydrochloride tablets alone or in combination with beta-blockers in patients with impaired ventricular function is very limited. Caution should be exercised when using the drug in such patients.
3. Hypotension
Decreases in blood pressure associated with diltiazem hydrochloride tablets therapy may occasionally result in symptomatic hypotension.
4. Acute Hepatic Injury
In rare instances, significant elevations in enzymes such as alkaline phosphatase, LDH, SGOT, SGPT, and other phenomena consistent with acute hepatic injury have been noted. These reactions have been reversible upon discontinuation of drug therapy. The relationship to diltiazem hydrochloride tablets is uncertain in most cases, but probable in some
DOSAGE AND ADMINISTRATION
Exertional Angina Pectoris Due to Atherosclerotic Coronary Artery Disease or Angina Pectoris at Rest Due to Coronary Artery Spasm
Dosage must be adjusted to each patient's needs. Starting with 30 mg four times daily, before meals and at bedtime, dosage should be increased gradually (given in divided doses three or four times daily) at 1- to 2-day intervals until optimum response is obtained. Although individual patients may respond to any dosage level, the average optimum dosage range appears to be 180 mg/day to 360 mg/day. There are no available data concerning dosage requirements in patients with impaired renal or hepatic function. If the drug must be used in such patients, titration should be carried out with particular caution.
Concomitant Use with Other Cardiovascular Agents
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Sublingual NTG may be taken as required to abort acute anginal attacks during diltiazem hydrochloride tablets therapy.
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Prophylactic Nitrate Therapy. Diltiazem hydrochloride tablets may be safely coadministered with short- and long-acting nitrates, but there have been no controlled studies to evaluate the antianginal effectiveness of this combination.
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Beta-Blockers. (See WARNINGS and PRECAUTIONS).
Swallow diltiazem hydrochloride tablets whole; do not split, crush, or chew the tablets.
