Diltiazem

Diltiazem is a drug with antihypertensive, antianginal and antiarrhythmic properties; its active ingredient is diltiazem. The drug can block the activity of Ca channels, suppress the formation of action potential, and also uncouple the activity of "excitation-contraction".

It can also reduce myocardial contractility, decrease the speed of AV conduction and the number of myocardial contractions. It significantly increases the duration of the sinus cycle and restores sinus rhythm during tachycardia. [ 1 ]

Indications Diltiazem

It is used in the treatment of the following cardiovascular diseases:

• IHD, including angina pectoris;
• elevated blood pressure (monotherapy or combination with other antihypertensive medications);
• SVT;
• pulmonary hypertension.
• It can be used to prevent the development of coronary spasm during coronary artery bypass grafting or during coronary angiography.

Used in combination treatment:

• after myocardial infarction (if there are contraindications to the use of β-blockers);
• diabetic form of nephropathy;
• in case of ventricular flutter and fibrillation, as well as to eliminate paroxysms of atrial fibrillation.

It is prescribed in transplantology, after kidney transplantation, to prevent the development of transplant failure, and also when performing immunosuppressive treatment.

Release form

The therapeutic substance is released in the form of tablets of 60 mg, 30 pieces per box.

Pharmacodynamics

Diltiazem is able to relax the smooth muscles of the coronary vessels, acting in concentrations that do not lead to a negative inotropic effect. It reduces the ventricular rate in people with an increased ventricular rate, in which atrial flutter and fibrillation are observed. [ 2 ]

The drug has a relaxing effect on vascular smooth muscle, which reduces systemic peripheral vascular resistance and attenuates the peripheral and renal effects of angiotensin-2. [ 3 ]

Pharmacokinetics

After oral administration, the drug is almost completely absorbed in the gastrointestinal tract. It participates in intensive metabolic processes during the first intrahepatic passage. The bioavailability level is approximately 40%. Plasma parameters are variable.

Protein synthesis – approximately 80%. Diltiazem is secreted in breast milk. Intrahepatic metabolic processes occur with the help of the enzyme system of hemoprotein P450. The metabolic component desacetyldiltiazem has 25-50% of the effect of the unchanged element.

The half-life of the drug is within 3-5 hours. It is excreted mainly in the form of decay products with urine and bile; about 2-4% is excreted unchanged with urine. Excretion of the substance is poor with dialysis.

Dosing and administration

Often the medication is taken in the amount of 1 tablet 2-3 times a day (taking into account the patient's reaction to Diltiazem and indications). If necessary, the dose can be increased to 2 tablets 2 times a day. Dosage changes can be made after at least 14 days.

You can take no more than 0.36 g of the substance per day. The tablets should be taken on an empty stomach, swallowed whole and washed down with plain water.

With prolonged use and obtaining a long-term positive medicinal effect, the dose can be reduced to a minimum.

When administered in combination with another antihypertensive drug, it may also be necessary to change the dosage of the latter.

• Application for children

Do not administer to persons under 18 years of age.

Use Diltiazem during pregnancy

Diltiazem should not be used during pregnancy.

If you need to take the drug during breastfeeding, you should stop breastfeeding.

Contraindications

Among the contraindications:

• severe intolerance to one of the components of the drug;
• cardiogenic shock;
• sinus type bradycardia;
• systolic left ventricular dysfunction (also in case of myocardial infarction);
• severe form of aortic stenosis;
• renal or hepatic dysfunction;
• SSSU.

It is prohibited to use with β-blockers. It is necessary to use with caution when stabilizing the heart rhythm in people suffering from hemodynamic disorders.

Side effects Diltiazem

Main side effects:

• temporary hypotension;
• conduction disturbance and bradycardia;
• tachycardia and decrease in cardiac output;
• eosinophilia, weakness, fainting, dizziness, tinnitus and cephalgia;
• potency disorders, peripheral edema, mood lability;
• hyperplasia in the area of the mucous gums and dyspepsia;
• hyperglycemia, hyperemia, and hyperthermia;
• signs of allergy (itching and epidermal rashes), erythema multiforme;
• polyuria or nocturia.

Overdose

In cases of poisoning with Diltiazem, a decrease in blood pressure, intracardiac block, bradycardia and heart failure are observed.

Gastric lavage and enterosorbents are required. In addition, hemoperfusion and plasmapheresis are performed. Calcium substances are administered intravenously as an antidote, and isoproterenol, atropine, dobutamine or dopamine are also used. Forced diuresis can be performed.

If severe AV block is observed, cardiac pacing should be performed.

Interactions with other drugs

The use of the drug together with substances that block β-adrenergic receptors can provoke AV conduction disorders and progression of bradycardia.

The drug is capable of increasing serum digoxin levels (by 20-60%).

Diltiazem enhances the antihypertensive activity of diuretics and other antihypertensive drugs, and potentiates the negative impact of fluorothane on the heart.

The drug reduces blood levels of diazepam.

H2-receptor blocking agents (eg, cimetidine) may increase serum diltiazem levels.

Storage conditions

Diltiazem should be stored at temperatures no higher than 25°C.

Shelf life

Diltiazem can be used for a period of 24 months from the date of manufacture of the medicinal product.

Analogues

The analogs of the drug are Blokaltsin, Dilren, Aldizem with Dilcardia, Tiakem with Dilcem and Cardil. In addition, the list includes Diacordin, Cortiazem and Zilden.