Diltiazem - instructions, reviews, similar products
In this article, you can read the instructions for using the drug Diltiazem. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Diltiazem in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Diltiazem in the presence of existing structural analogues. Use to treat hypertension or reduce blood pressure and prevent attacks of angina in adults, children, as well as during pregnancy and lactation.
Diltiazem - selective calcium channel blocker of the 3rd class, benzothiazepine derivative. Has antianginal, hypotensive and antiarrhythmic action.Reduces myocardial contractility, slows AV-conduction, decreases heart rate, reduces myocardial oxygen demand, expands coronary arteries, increases coronary blood flow. Reduces the tone of smooth muscles of peripheral arteries and OPSS.
Reduces the intracellular content of calcium ions in cardiomyocytes and smooth muscle cells of blood vessels, lowers heart rate, may have a slight negative inotropic effect, increases coronary, cerebral and renal blood flow. In concentrations in which there is no negative inotropic effect, it causes the relaxation of the smooth muscles of the coronary vessels and the dilatation of both large and small arteries.
The antianginal effect is due to improved blood supply to the myocardium and a decrease in its oxygen demand as a result of decreased OPSS, systemic blood pressure (afterload), a decrease in myocardial tone and an increase in the diastolic left ventricular relaxation time.
The antiarrhythmic effect is due to the suppression of the transport of calcium ions in the heart tissues, which leads to an elongation of the effective refractory period and slowing of the AV node (in patients with sinus syndrome (SSS) syndrome, elderly people,in which the blockade of calcium channels can interfere with the generation of a pulse in the sinus node and cause a sinoatrial blockade). The normal atrial action potential or intraventricular conduction does not change (normal sinus rhythm is usually unaffected), but with a decrease in the amplitude of atrial contraction, the rate of depolarization and speed of conduction decrease. Anterograde effective refractory period in additional bypass beams of conduction may be shortened. When parenteral administration causes a rapid transition of paroxysmal supraventricular tachycardia (including associated with additional bypass beams of conduction) into the sinus rhythm, as well as temporary cessation of ventricular tachycardia during flutter or atrial fibrillation.
The hypotensive effect is due to dilatation of the resistive vessels and a decrease in the OPSS. The degree of decrease in blood pressure correlates with its baseline level (with fluctuations in blood pressure within the limits of normal values, a minimal effect on blood pressure is noted). Reduces blood pressure in both horizontal and vertical position. Rarely causes postural arterial hypotension and reflex tachycardia.Does not change or slightly reduces the maximum heart rate under the load. Long-term therapy does not lead to hyperkatecholamineemia, increased activity of RAAS. Reduces renal and peripheral effects of angiotensin 2. Promotes diastolic relaxation of the myocardium in hypertension, ischemic heart disease, hypertrophic obstructive cardiomyopathy, reduces platelet aggregation. It is able to cause regression of left ventricular hypertrophy in patients with arterial hypertension.
Slightly affects the smooth muscles of the gastrointestinal tract. During a long (8 months) therapy, tolerance does not develop. Does not affect the lipid profile of the blood.
The beginning and duration of action depends on the dosage form used.
Composition
Diltiazema hydrochloride + excipients.
Pharmacokinetics
After intake diltiazem almost completely absorbed from the digestive tract. It is subjected to intensive metabolism at the "first passage" through the liver. Bioavailability is about 40%. Concentration in plasma is variable. Binding to plasma proteins is about 80%. Diltiazem is excreted in breast milk. Intensively metabolized in the liver with the participation of the enzymatic system of cytochrome P450.One of the metabolites, desacetylldithiazel, has a 25-50% activity of unchanged substance. It is excreted mainly in the form of metabolites with bile and urine, approximately 2-4% is excreted in the urine unchanged. Diltiazem is poorly excreted in dialysis.
Indications
- prevention of angina attacks (including angina pectoris)
- arterial hypertension (pressure reduction)
- prevention of supraventricular arrhythmias (paroxysmal supraventricular tachycardia, atrial fibrillation, atrial flutter, extrasystole)
- relief of angina pectoris, prevention of coronary artery spasm during coronary angiography or aortocoronary bypass surgery, paroxysmal ventricular tachycardia, for arresting the frequent rhythm of the ventricles with flicker or atrial flutter (with the exception of WPW syndrome) for intravenous administration.
Forms of release
Tablets of 30 mg, 60 mg and 90 mg.
Tablets of prolonged action, coated with 90 mg and 180 mg (Diltiazem Lannacher).
Capsules of prolonged action of 90 mg, 120 mg and 180 mg (Diltiazem Retard).
The tablets of the prolonged action, covered with a cover of 120 mg and 240 mg (Diltiazem Teva).
Instructions for use and dosage
Pills
When administered orally, the initial dose is 60 mg 3 times a day or 90 mg 2 times a day. With insufficient effectiveness, the dose is increased to 180 mg twice a day. Prolonged forms are applied 1-2 times a day, depending on the dose.
The maximum daily intake for oral administration is 360 mg.
Ampoules
When administered intravenously, a single dose of 300 μg / kg.
For IV injections, the dose is 2.8-14 μg / kg / min. The maximum daily dose is 300 mg.
Retard tablets
Tablets should be taken orally, before meals, whole, not liquid and not crumbling, with a small amount of liquid.
The initial dose of the drug Diltiazem retard is 1 tablet of 90 mg 2 times a day. The average daily dose is 180-240 mg. Correction of the dosing regimen can be carried out only after 2 weeks.
The maximum dose is 360 mg per day (it is used only in a hospital).
Lannacher Tablets
The drug is prescribed in a daily dose of 180-360 mg, divided into 2 divided doses. When switching to long-term maintenance therapy, the dose of the drug can be reduced to 180 mg once a day (in the morning).
Tablets should be taken whole, not liquid and squeezed with a small amount of liquid.
Side effect
- dry mouth;
- nausea, vomiting;
- constipation;
- flatulence;
- heartburn;
- increased activity of hepatic transaminases;
- arterial hypotension;
- violation of AV-conduction;
- symptoms of heart failure;
- bradycardia;
- headache;
- dizziness;
- increased fatigue;
- sleep disorders;
- nervousness;
- skin rash;
- itching;
- exanthema;
- swelling of the lower extremities;
- hyperplasia of the gingival mucosa.
Contraindications
- severe bradycardia;
- syndrome of weakness of the sinus node (SSSU);
- cardiogenic shock;
- AV-blockade of 2 and 3 degrees (except for patients with a pacemaker);
- WPW syndrome;
- arterial hypotension;
- chronic heart failure 2B-3 stage;
- acute heart failure;
- severe liver dysfunction;
- severe renal dysfunction;
- pregnancy;
- lactation;
- children under the age of 18;
- hypersensitivity to benzothiazepine derivatives.
Application in pregnancy and lactation
Diltiazem is contraindicated in pregnancy and lactation (breastfeeding).
Use in children
The drug is not indicated for use in children and adolescents under the age of 18 years.
special instructions
With caution should prescribe the drug to patients prone to arterial hypotension, bradycardia, with violations of intraventricular conduction, elderly patients, patients with impaired liver and kidney function.
During the intake of the drug, alcohol should be avoided.
Impact on the ability to drive vehicles and manage mechanisms
The drug may affect the performance of work requiring rapidity of psychomotor reactions (control mechanisms, vehicles).
Drug Interactions
With the simultaneous administration of the drug Diltiazem with antihypertensive drugs, there is an increase in hypotensive effect.
With the simultaneous administration of Diltiazem and digoxin, an increase in the concentration of Digoxin in the blood is possible.
With the simultaneous administration of Diltiazem with antiarrhythmics, beta-adrenoblockers, cardiac glycosides, bradycardia, AV-conduction, and symptoms of heart failure may develop.
Cimetidine weakens the process of biotransformation of diltiazem in the liver, slows its excretion, increasing the duration of the drug Diltiazem.
With the simultaneous administration of the drug with carbamazepine, quinidine, cyclosporine and theophylline, it is possible to intensify the toxic effect of the latter due to the inhibitory effect of diltiazem on cytochrome P450.
Analogues of the drug Diltiazem
Structural analogs for the active substance:
- Altiazem PP;
- Blocalcin;
- Diacordin 120 Retard;
- Diacordin 60;
- Diacordin 90 Retard;
- Dilcardia;
- Diltazem SR;
- Diltiazem hydrochloride;
- Diltiazem Lannacher;
- Diltiazem retard;
- Diltiazem Teva;
- Dilren;
- Diltz;
- Silden;
- Cardil;
- Cortiazem;
- Teakem.
Analogues on the pharmacological group (calcium channel blockers):
- Adalate;
- Amlodipine;
- Amocardium of Sanovel;
- Ammonorm;
- Amrorus;
- Ancardard;
- Vylloset;
- Verapamil;
- Vertizine;
- Diltzer;
- Isoptin;
- Kalchek;
- K Dalnev;
- Ko Exforge;
- Corvadil;
- Cordaflex;
- Cordipine;
- Corinfar;
- Lercamen;
- Lercanidipine;
- Lomir;
- Niebelong;
- Nicardy;
- Nimotop;
- Nifedex;
- Nifedipine;
- Nifecard;
- Norvasc;
- Normodipine;
- Octidipine;
- Plandil;
- Posekor;
- Prestan;
- The Procurator;
- Stamlo;
- Stugeron;
- Tenox;
- Felodipine;
- Felotenz retard;
- Finoptin;
- Foridon;
- Cinnarizine;
- Cinnasan;
- Ecquard;
- Equator;
- Exforge;
- Enanorm.