Diltiazem
Diltiazem: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Diltiazem
ATX code: C08DB01
Active ingredient: diltiazem (diltiazem)
Manufacturer: Teva Pharmaceutical Industries (Israel), Alkaloid AD (Republic of Macedonia), Lannacher Heilmittel (Austria), S. O. Rompharm Company SRL (Romania)
Description and photo update: 2019-16-08
Prices in pharmacies: from 62 rubles.
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Diltiazem is a drug with antiarrhythmic, hypotensive and antianginal effects.
Release form and composition
Diltiazem is available in the following dosage forms:
- Tablets (10 pcs. In blister strip packs, 3 packs in a cardboard box);
- Sustained-release tablets (30 pcs. In dark glass bottles, 1 bottle in a cardboard box).
The composition of 1 tablet and 1 prolonged-release tablet contains the active substance: diltiazem (in the form of hydrochloride) - 60 or 90 mg (respectively).
Pharmacological properties
Pharmacodynamics
Diltiazem is a benzothiazepine derivative that is a slow calcium channel blocker. The substance reduces the intracellular concentration of calcium ions in the cells that form the smooth muscles of blood vessels and cardiomyocytes, promotes the expansion of peripheral and coronary arterioles and arteries, reduces the total peripheral vascular resistance, weakens the tone of smooth muscles, intensifies renal, cerebral and coronary blood flow, reduces the frequency of …
The antiarrhythmic effect of the drug is associated with the obstruction of the transport of ionized calcium in cardiac tissues, which causes an increase in the effective refractory period and prolongation of the time spent in the atrioventricular node. This effect is clinically significant in patients with sick sinus syndrome and elderly patients in whom calcium channel blockade can suppress the generation of impulses in the sinus node and provoke sinoatrial blockade. At the same time, intraventricular conduction or normal atrial action potential remains unchanged (diltiazem usually does not affect normal sinus rhythm), however, with a decrease in the amplitude of atrial contraction, the conduction rate and depolarization rate decrease. Sometimes there is a reduction in the anterograde effective refractory period in additional bypass conduction bundles.
The antianginal effect is associated with the expansion of peripheral vessels and a decrease in systemic blood pressure (afterload state), as a result of which the tension of the myocardial wall and its need for oxygen supply decreases. When taken into the body in concentrations that do not provoke a negative inotropic effect, diltiazem causes relaxation of the smooth muscles of the coronary vessels and dilatation of both small and large arteries.
The antihypertensive effect is manifested in the form of a decrease in the total peripheral vascular resistance and dilatation of resistive vessels. The degree of decrease in blood pressure is directly proportional to its initial value (in normotonic patients, the drug has a minimal effect on blood pressure). After taking diltiazem, blood pressure decreases in both the sitting and lying positions. The use of the drug rarely leads to reflex tachycardia and postural arterial hypotension. With diltiazem treatment, the maximum heart rate during exercise remains unchanged or slightly decreases. During long-term therapy, the activity of the renin-angiotensin-aldosterone system does not increase, and there is no hypercatecholaminemia. Diltiazem provides a decrease in the renal and peripheral effects of angiotensin II and improves diastolic relaxation of the myocardium in patients with hypertrophic cardiomyopathy, ischemic heart disease, arterial hypertension, and also inhibits platelet aggregation.
The drug is characterized by a minimal effect on the smooth muscles of the gastrointestinal tract. During a long course of treatment (from 8 months), addiction to diltiazem does not develop. The substance does not change the lipid profile of the blood and can lead to regression of left ventricular hypertrophy in patients with arterial hypertension.
The hypotensive effect of the drug reaches its maximum severity within 2 weeks.
Pharmacokinetics
When taken orally, diltiazem is rapidly and almost completely absorbed from the gastrointestinal tract. Absorption completeness reaches 90% of the dose taken. The maximum level in blood plasma was recorded 4–6 hours after administration. In individual patients, the values of concentrations in blood plasma differ significantly.
Diltiazem binds to blood plasma proteins by about 70-80%. Its volume of distribution in the body is approximately 5.3 l / kg of body weight. Also, the substance is determined in breast milk.
Diltiazem is extensively metabolized in the liver through demethylation and deacetylation with the participation of isoenzymes CYP3A7, CYP3A5 and CYP3A4. In this case, the pharmacologically active metabolite deacetyldyltiazem is formed, which is contained in the blood plasma in concentrations that are 5-10 times lower than the corresponding indicators of diltiazem. The metabolite exhibits 2–4 times less activity than the active substance itself. Diltiazem exhibits therapeutic effect at concentrations of 20-40 ng / ml. The bioavailability of the drug is 40% and is associated with the effect of the first passage through the liver.
The drug is excreted from the body through the intestines with bile (about 65% of the dose taken) and, to a lesser extent, with urine (35% of the dose taken). The half-life of plasma elimination varies from 3.2 to 6.6 hours. With long-term treatment, the pharmacokinetic parameters of diltiazem remain unchanged. The substance does not show any tendency to cumulate or induce its own metabolism.
In patients with renal dysfunction and angina pectoris, the pharmacokinetics of diltiazem remain similar to those in healthy patients. In patients with hepatic insufficiency, an elongation of the half-life and an increase in bioavailability are observed. In elderly patients, clearance of diltiazem may decrease. The substance is not excreted by peritoneal dialysis and hemodialysis.
Indications for use
Indications for Diltiazem:
- Arterial hypertension;
- Attacks of angina pectoris, including Prinzmetal's angina (prevention);
- Supraventricular arrhythmias, including paroxysmal supraventricular tachycardia, atrial flutter and atrial fibrillation, extrasystole (prevention).
Contraindications
- Functional disorders of the kidneys and liver;
- Severe bradycardia;
- AV block II-III degree (except for patients with a pacemaker);
- Cardiogenic shock;
- Sick sinus syndrome;
- Atrial fibrillation in Laun-Ganogh-Levin and Wolff-Parkinson-White syndrome;
- Arterial hypotension;
- Myocardial infarction, accompanied by congestion in the lungs;
- Chronic heart failure II B-III stage;
- Hemodynamically significant aortic stenosis;
- Acute heart failure
- Pregnancy and lactation;
- Hypersensitivity to drug components.
During the use of Diltiazem, according to indications, care should be taken in patients prone to arterial hypotension, children (due to the lack of clinical data on the safety and efficacy of the drug in this age group), elderly patients, as well as with ventricular tachycardia with an expansion of the ORS complex, AV blockade of the I degree, intraventricular conduction disorders, chronic heart failure, myocardial infarction with left ventricular failure, hepatic and renal failure.
Instructions for use of Diltiazem: method and dosage
The tablets should be taken orally, swallowed whole and washed down with a liquid.
The drug is taken 3 times a day at 60 mg or 2 times a day at 90 mg. The optimal dosage for Diltiazem is 180-360 mg per day. Under the supervision of a physician in a hospital setting, it is possible to increase the daily dose to 480 mg.
Side effects
During therapy, the following disorders may develop:
- Cardiovascular system: asymptomatic decrease in blood pressure; rarely - arrhythmia (including fibrillation and flutter of the ventricles), angina pectoris, AV block II-III st. up to asystole, bradycardia (less than 50 beats per minute) or tachycardia, worsening or development of heart failure; when using Diltiazem in high doses - bradycardia, angina pectoris, AV blockade, worsening of chronic heart failure, a marked decrease in blood pressure;
- Nervous system and sensory organs: fainting, depression, headache, drowsiness, dizziness, asthenia, increased fatigue, sleep disturbances, anxiety, extrapyramidal disorders (difficulty in swallowing, mask-like face, ataxia, shuffling gait, trembling of fingers and hands, leg stiffness or hands); when using Diltiazem in high doses - tremor, paresthesia, visual impairment (transient loss of vision);
- Hematopoietic system: rarely - agranulocytosis, thrombocytopenia;
- Digestive system: vomiting, increased appetite, dry mouth, nausea, diarrhea or constipation, gingival hyperplasia (soreness, bleeding, swelling), increased activity of hepatic transaminases.
Overdose
Overdose symptoms are: asystole, bradycardia, cardiogenic shock, a marked decrease in blood pressure, turning into collapse, heart failure, atrioventricular conduction disorders. As an urgent measure when taking high doses of the drug, gastric lavage, intake of activated charcoal, and symptomatic therapy, if necessary, are recommended.
In case of atrioventricular blockade of II and III degrees, intravenous administration of atropine is prescribed in a dose of 0.6–1 mg. If the patient's body responds to treatment in an unsatisfactory manner, administration of isoprenaline is allowed. If arterial hypotension occurs, you should increase fluid intake and prescribe vasoconstrictor drugs. In case of heart failure, diuretics, drugs with a positive inotropic effect and symptomatic treatment are recommended.
special instructions
Before starting the use of Diltiazem, as well as in cases of development of uncharacteristic symptoms, you should consult a doctor.
Influence on the ability to drive vehicles and complex mechanisms
At the moment, it has not been proven that taking diltiazem in therapeutic doses affects the physical and mental activity of the patient. Patients with high sensitivity may (in particular, at the beginning of the course of drug treatment) experience an excessive decrease in blood pressure, dizziness and a temporary deterioration in the ability to drive vehicles.
Application during pregnancy and lactation
According to the instructions, Diltiazem is contraindicated in pregnant and lactating women, since clinical studies have confirmed its teratogenic effect.
Drug interactions
Potentially dangerous are combinations of Diltiazem with quinidine and other class Ia antiarrhythmic drugs, beta-blockers, cardiac glycosides (due to the risk of developing excessive bradycardia, slowing AV conduction, decreasing myocardial contractility).
With the simultaneous use of Diltiazem with certain drugs, undesirable effects may occur:
- Procainamide, quinidine and other drugs that cause prolongation of the QT interval: increased risk of significant QT prolongation;
- Thiazide diuretics and other drugs that lower blood pressure, drugs for inhalation anesthesia (hydrocarbon derivatives): increasing the hypotensive effect of diltiazem;
- Propranolol: an increase in its bioavailability is possible;
- Diazepam, phenobarbital, rifampicin: decrease in the concentration of diltiazem in the blood;
- Cyclosporine, theophylline, carbamazepine, quinidine, valproic acid and digoxin: an increase in their concentration in the blood (dose reduction may be required);
- Cimetidine: an increase in the concentration of diltiazem in the blood;
- Indomethacin and other non-steroidal anti-inflammatory drugs, estrogens and glucocorticosteroids, as well as sympathomimetic drugs: reducing the hypotensive effect;
- Lithium preparations: it is possible to increase the neurotoxic effect of diltiazem (with the development of vomiting, nausea, ataxia, diarrhea, trembling and / or tinnitus);
- General anesthetics: increased cardiodepressant action.
Perhaps the simultaneous appointment of Diltiazem with nitrates, including prolonged forms.
Analogs
Diltiazem analogs are: Aldizem, Diltiazem Lannacher, Diakordin 60, Diakordin 90 Retard, Diakordin 12 Retard, Cardil.
Terms and conditions of storage
Keep out of reach of children at temperatures up to 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Diltiazem
Reviews of Diltiazem confirm its effectiveness when used in patients with angina pectoris, ischemic heart disease, hypertension, and various arrhythmias. However, there are unfavorable opinions about the drug associated with its side effects (for example, patients complain of headaches).
Diltiazem price in pharmacies
The approximate price of Diltiazem in the form of tablets for a package containing 30 pieces is 63-117 rubles (dosage 60 mg) or 79-135 rubles (dosage 90 mg). You can buy 90 mg prolonged-release tablets for about 106-139 rubles.
Diltiazem: prices in online pharmacies
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Drug name Price Pharmacy |
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Diltiazem 60 mg tablets 30 pcs. RUB 62 Buy |
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Diltiazem Lannacher 90 mg film-coated tablets of prolonged action 20 pcs. 113 RUB Buy |
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Diltiazem 90 mg prolonged release tablets 30 pcs. 129 RUB Buy |
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Diltiazem 60mg tablets 30 pcs. 130 RUB Buy |
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Diltiazem Lannacher tablets p.p. prolonged action 90mg 20 pcs. 143 r Buy |
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Diltiazem retard 180 mg capsules 30 pcs. 143 r Buy |
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Diltiazem prolonged action tablets 90mg 30 pcs. 146 r Buy |
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Diltiazem Lannacher 180 mg film-coated tablets of prolonged action 30 pcs. 234 r Buy |
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Diltiazem Retard 180mg capsules 30 pcs. 251 RUB Buy |
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Diltiazem Lannacher tablets p.p. prolonged action 180mg 30 pcs. 279 r Buy |
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
