Diltiazem

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

It can also decrease myocardial contractility, decrease the AV conduction velocity and the number of myocardial contractions. 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 CVD diseases:

• Ischemic heart disease , including angina pectoris;
• increased blood pressure (monotherapy or combination with other antihypertensive drugs);
• SVT;
• hypertension of the lungs .
• It can be used to prevent the development of coronary spasm during the procedure of coronary artery bypass grafting or when performing coronary angiography.

Used in combined treatment:

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

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

Release form

The release of the therapeutic substance is realized in the form of 60 mg tablets, 30 pieces inside the 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. Reduces the ventricular rate in people with an increased ventricular rate, in which atrial flutter and atrial fibrillation are noted. [2]

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

Pharmacokinetics

After oral administration, the drug is almost completely absorbed inside the gastrointestinal tract. Participates in intensive metabolic processes during the 1st intrahepatic passage. The bioavailability level is approximately 40%. Plasma readings are variable.

Protein synthesis - approximately 80%. Diltiazem is secreted in mother's milk. Intrahepatic metabolic processes proceed with the help of the P450 hemoprotein enzyme system. The metabolic component desacetyldyltiazem has 25-50% of the effect of the unchanged element.

The term of 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 in the urine. With dialysis, excretion of the substance is poor.

Dosing and administration

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

You can take no more than 0.36 g of the substance per day. You need to take the tablets on an empty stomach, swallowing whole and drinking it with plain water.

With long-term use and obtaining a long-term positive drug effect, the portion can be reduced to a minimum.

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

• Application for children

It is forbidden to appoint persons under the age of 18.

Use Diltiazem during pregnancy

Diltiazem should not be used during pregnancy.

If you need to take the drug during hepatitis B, you should refuse to breastfeed.

Contraindications

Among the contraindications:

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

It is forbidden to use with β-blockers. It should be used with caution when stabilizing the heart rate in people with hemodynamic disorders.

Side effects Diltiazem

The main side symptoms:

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

Overdose

In case of Diltiazem poisoning, there is a decrease in blood pressure, intracardiac block, bradycardia and heart failure.

It is required to perform gastric lavage and take enterosorbents. In addition, hemoperfusion and plasmapheresis are performed. Calcium substances are introduced as an antidote in / in the way, and isoproterenol, atropine, dobutamine or dopamine are also used. Forced diuresis can be performed.

If there is a severe form of AV block, 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 the progression of bradycardia.

The drug is able to increase serum digoxin values (by 20-60%).

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

The drug reduces the blood counts of diazepam.

Drugs that block the action of H2-terminations (for example, cimetidine) can increase serum values of diltiazem.

Storage conditions

Diltiazem must be stored at temperatures not exceeding 25 ° C.

Shelf life

Diltiazem can be used for 24 months from the date of manufacture of the drug.

Analogs

The analogs of the drug are the substances Blokaltsin, Dilren, Aldisem with Dilcardia, Tiakem with Dilcem and Cardil. In addition, Diakordin, Cortiazem and Silden are on the list.