pharmacopeia
GET
/api/v1/drug/diltiazem
2D structure
[(2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] acetate
SMILES CC(=O)O[C@@H]1[C@@H](SC2=CC=CC=C2N(C1=O)CCN(C)C)C3=CC=C(C=C3)OC
InChIKey HSUGRBWQSSZJOP-RTWAWAEBSA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: Calcium Channel Antagonists; Cytochrome P450 3A4 Inhibitors; L-Calcium Channel Receptor Antagonists.

Calcium ChannelCytochrome P450 3A4L-Calcium Channel Receptor

Indications

Sourced from openFDA
  • Diltiazem hydrochloride extended-release capsules are indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive medications.ICD-10: I10

Contraindications

Sourced from openFDA
  • Diltiazem hydrochloride is contraindicated in (1) patients with sick sinus syndrome except in the presence of a functioning ventricular pacemaker, (2) patients with second- or third-degree AV block except in the presence of a functioning ventricular pacemaker, (3) patients with hypotension (less than 90 mm Hg systolic), (4) patients who have demonstrated hypersensitivity to the drug, and (5) patients with acute myocardial infarction and pulmonary congestion documented by x-ray on admission.contraindicated

Dosage & administration

Sourced from openFDA

Patients controlled on diltiazem alone or in combination with other medications may be switched to diltiazem hydrochloride extended-release capsules, USP at the nearest equivalent total daily dose. Higher doses of diltiazem hydrochloride extended-release capsules, USP may be needed in some patients. Monitor patients closely. Subsequent titration to higher or lower doses may be necessary. There is limited general clinical experience with doses above 360 mg, but doses to 540 mg have been studied in clinical trials. The incidence of side effects increases as the dose increases with first-degree AV block, dizziness, and sinus bradycardia bearing the strongest relationship to dose. Hypertension : Adjust dosage to individual patient needs. When used as monotherapy, reasonable starting doses are 180 to 240 mg once daily, although some patients may respond to lower doses. Maximum antihypertensive effect is usually observed by 14 days of chronic therapy; therefore, schedule dosage adjustments accordingly. The usual dosage range studied in clinical trials was 240 to 360 mg once daily. Individual patients may respond to higher doses of up to 480 mg once daily. Angina : Dosages for the treatment of angina should be adjusted to each patient's needs, starting with a dose of 120 or 180 mg once daily. Individual patients may respond to higher doses of up to 480 mg once daily. When necessary, titration may be carried out over a 7- to 14-day period.

Warnings & precautions

Sourced from openFDA

Cardiac Conduction : Diltiazem hydrochloride prolongs 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 (13 of 3290 patients or 0.40%). 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 (see ADVERSE REACTIONS ). 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). An acute study of oral diltiazem in patients with impaired ventricular function (ejection fraction 24% ± 6%) showed improvement in indices of ventricular function without significant decrease in contractile function (dP/dt). Worsening of congestive heart failure has been reported in patients with preexisting impairment of ventricular function. Experience with the use of diltiazem hydrochloride in combination with beta-blockers in patients with impaired ventricular function is limited. Caution should be exercised when using this combination.

Adverse reactions

Sourced from openFDA

Serious adverse reactions have been rare in studies carried out to date, but it should be recognized that patients with impaired ventricular function and cardiac conduction abnormalities have usually been excluded from these studies. The following table presents the most common adverse reactions reported in placebo-controlled angina and hypertension trials in patients receiving diltiazem hydrochloride extended-release capsules up to 360 mg with rates in placebo patients shown for comparison. In addition, the following events were reported infrequently (less than 1%) in angina or hypertension trials: Cardiovascular: Congestive heart failure, palpitations, syncope, ventricular extrasystoles. Nervous System: Abnormal dreams, amnesia, depression, gait abnormality, hallucinations, insomnia, nervousness, paresthesia, personality change, somnolence, tinnitus, tremor. G astrointestinal: Anorexia, constipation, diarrhea, dry mouth, dysgeusia, dyspepsia, mild elevations of SGOT, SGPT, LDH, and alkaline phosphatase (see WARNINGS, Acute Hepatic Injury ), thirst, vomiting, weight increase. Dermatological: Petechiae, photosensitivity, pruritus, urticaria. Other: Amblyopia, CPK increase, dyspnea, epistaxis, eye irritation, hyperglycemia, hyperuricemia, impotence, muscle cramps, nasal congestion, nocturia, osteoarticular pain, polyuria, sexual difficulties.

Use in specific populations

Sourced from openFDA

Pregnancy Reproduction studies have been conducted in mice, rats, and rabbits. Administration of doses ranging from five to ten times greater (on a mg/kg basis) than the daily recommended therapeutic dose has resulted in embryo and fetal lethality. These doses, in some studies, have been reported to cause skeletal abnormalities. In the perinatal/postnatal studies, there was an increased incidence of stillbirths at doses of 20 times the human dose or greater. There are no well-controlled studies in pregnant women; therefore, use diltiazem hydrochloride in pregnant women only if the potential benefit justifies the potential risk to the fetus.

Overdosage

Sourced from openFDA

The oral LD 50 s in mice and rats range from 415 to 740 mg/kg and from 560 to 810 mg/kg, respectively. The intravenous LD 50 s in these species were 60 and 38 mg/kg, respectively. The oral LD 50 in dogs is considered to be in excess of 50 mg/kg, while lethality was seen in monkeys at 360 mg/kg. The toxic dose in man is not known. Because of its extensive metabolism, blood levels after a standard dose of diltiazem can vary over tenfold, limiting the usefulness of blood levels in overdose cases. There have been reports of diltiazem overdose in amounts ranging from <1 g to 18 g. Of cases with known outcome, most patients recovered and in cases with a fatal outcome, the majority involved multiple drug ingestion. Events observed following diltiazem overdose included bradycardia, hypotension, heart block, and cardiac failure. Most reports of overdose described some supportive medical measure and/or drug treatment. Bradycardia frequently responded favorably to atropine, as did heart block, although cardiac pacing was also frequently utilized to treat heart block.

Approval history

Sourced from openFDA
  • Nov 5, 1982NDANDA018602Bausch
  • Dec 27, 1991NDANDA020062Bausch
  • Nov 5, 1992ANDAANDA074093Chartwell Molecules
  • May 31, 1995ANDAANDA074185Teva
  • Sep 11, 1995NDANDA020401Bausch
  • Feb 28, 1996ANDAANDA074617Sagent
  • Feb 6, 2003NDANDA021392Bausch
  • Feb 21, 2025NDANDA218038Hq Spclt Pharma

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
34,042 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Dyspnoea3,2469.5%
  2. 2Fatigue2,6767.9%
  3. 3Nausea2,4107.1%
  4. 4Pain2,3917.0%
  5. 5Dizziness2,1336.3%
  6. 6Diarrhoea2,0726.1%
  7. 7Drug Ineffective2,0286.0%
  8. 8Headache1,9855.8%
  9. 9Fall1,9605.8%
  10. 10Atrial Fibrillation1,7645.2%
  11. 11Asthenia1,7175.0%
  12. 12Pneumonia1,6134.7%
  13. 13Arthralgia1,5724.6%
  14. 14Hypotension1,4994.4%
  15. 15Pain In Extremity1,4664.3%

Literature

View JSON

Recent PubMed references pinned to Diltiazem as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 135 ClinicalTrials.gov registrations naming Diltiazem as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Diltiazem work?
Mechanism-of-action classes: Calcium Channel Antagonists; Cytochrome P450 3A4 Inhibitors; L-Calcium Channel Receptor Antagonists.
What is Diltiazem used for?
According to FDA labeling, Diltiazem carries indications including: Diltiazem hydrochloride extended-release capsules are indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive medications.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Diltiazem?
Diltiazem is classified as Benzothiazepine derivatives, Muscle relaxants, Calcium Channel Blocker, Calcium Channel Antagonists, Cytochrome P450 3A4 Inhibitors, L-Calcium Channel Receptor Antagonists, Coronary Arterial Vasodilation, Decreased Blood Pressure, Negative Chronotropy.
What are the brand names for Diltiazem?
Diltiazem is marketed under brand names including Cardizem, Cartia, Dilt, Diltzac, Matzim, Taztia, Tiadylt, Tiazac.
What are the contraindications for Diltiazem?
Diltiazem labeling lists contraindications including: Diltiazem hydrochloride is contraindicated in (1) patients with sick sinus syndrome except in the presence of a functioning ventricular pacemaker, (2) patients with second- or third-degree AV block except in the presence of a functioning ventricular pacemaker, (3) patients with hypotension (less than 90 mm Hg systolic), (4) patients who have demonstrated hypersensitivity to the drug, and (5) patients with acute myocardial infarction and pulmonary congestion documented by x-ray on admission.. Always consult the full prescribing information and a clinician.
Note. Data for diltiazem is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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