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Diltiazem: Effects, Dosage & Side Effects

Diltiazem is a calcium channel blocker used to treat heart rhythm disorders, high blood pressure, and angina pectoris.

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Things worth knowing about "Diltiazem"

Diltiazem is a calcium channel blocker used to treat heart rhythm disorders, high blood pressure, and angina pectoris.

What is Diltiazem?

Diltiazem is a prescription medication belonging to the class of calcium channel blockers (also called calcium antagonists). It is classified within the benzothiazepine subgroup and is widely used in cardiology and internal medicine. Diltiazem affects the electrical activity of the heart and the tone of blood vessel walls, thereby reducing blood pressure and heart rate.

Indications

Diltiazem is used for a variety of cardiovascular conditions:

High blood pressure (arterial hypertension): Diltiazem relaxes blood vessels, reducing blood pressure.
Angina pectoris: It relieves chest pain caused by reduced blood flow to the heart.
Heart rhythm disorders (arrhythmias): Particularly for atrial fibrillation and atrial flutter, diltiazem is used to control heart rate.
Coronary artery disease: Diltiazem improves blood flow through the coronary arteries.

Mechanism of Action

Diltiazem blocks voltage-gated L-type calcium channels in cardiac muscle cells and in the smooth muscle cells of blood vessel walls. Calcium plays a critical role in muscle contraction. By blocking these channels, less calcium enters the cells, which produces the following effects:

Relaxation of blood vessel walls (vasodilation) → reduction in blood pressure
Slowing of the heart rate (negative chronotropic effect)
Reduction of electrical conduction speed in the heart (negative dromotropic effect)
Reduction of heart muscle contraction strength (negative inotropic effect)

Dosage and Forms

Diltiazem is available in several formulations:

Tablets and capsules (extended-release forms): For long-term management of hypertension and angina. Typical daily doses range from 120 mg to 360 mg, taken in 1 to 3 divided doses.
Intravenous injection: For acute arrhythmias in a hospital setting under medical supervision.

The exact dosage depends on the medical condition, the general health of the patient, and any other medications being taken. Dosage should not be changed without consulting a physician.

Side Effects

Like all medications, diltiazem can cause side effects. Common side effects include:

Headache and dizziness
Fatigue and general weakness
Fluid retention (edema), especially around the ankles
Facial flushing and a feeling of warmth
Slow heartbeat (bradycardia)
Gastrointestinal complaints such as nausea or constipation

Rare but serious side effects include severe slowing of the heart rate, heart block, or a significant drop in blood pressure. Medical attention should be sought immediately if any of these occur.

Contraindications and Interactions

Diltiazem must not be used in cases of:

Severe heart block (second- or third-degree AV block without a pacemaker)
Sick sinus syndrome (without a pacemaker)
Severe heart failure
Pregnancy and breastfeeding (consult a physician)

Important drug interactions exist with:

Beta-blockers: increased risk of bradycardia or heart block
Digoxin: diltiazem increases digoxin blood levels
Simvastatin and other statins: elevated statin levels are possible
Ciclosporin: elevated ciclosporin levels are possible
CYP3A4 inhibitors and inducers: diltiazem is metabolized via the CYP3A4 enzyme in the liver

Usage Notes

Diltiazem should be taken regularly at the same time each day to maintain a consistent blood level of the medication. Extended-release tablets or capsules should generally not be crushed or chewed. Patients should not discontinue therapy on their own, as this may lead to a rebound effect with a rise in blood pressure.

References

European Medicines Agency (EMA) - Diltiazem product information, current version. Available at: www.ema.europa.eu
Fuster, V. et al. - Hurst's The Heart. 14th edition. McGraw-Hill Education, 2017.
Opie, L.H. & Gersh, B.J. - Drugs for the Heart. 8th edition. Elsevier Saunders, 2013.

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