Dilatrend - Instructions For The Use Of Tablets, Price, Analogs, Reviews

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Dilatrend

Dilatrend: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Drug interactions
14. 14. Analogs
15. 15. Terms and conditions of storage
16. 16. Terms of dispensing from pharmacies
17. 17. Reviews
18. 18. Price in pharmacies

Latin name: Dilatrend

ATX code: C07AG02

Active ingredient: Carvedilol

Manufacturer: F. Hoffmann-La Roche Ltd. (Switzerland)

Description and photo update: 18.10.2018

Dilatrend is a drug with vasodilating, antianginal, antioxidant, antihypertensive, antiproliferative effects.

Release form and composition

Dilatrend dosage form - tablets: round, thickness 2.2-2.6 mm, diameter 6.9-7.1 mm, somewhat marble, with a double-sided line engraved on both sides: on one side - "B" and "M"; 6.25 mg each - yellow, engraved on the other side "F" and "1"; 12.5 mg each - light brown, engraving on the other side "H" and "3"; 25 mg each - from white to pale yellowish-beige, engraving on the other side "D" and "5" (in blisters of 10 pcs., in a cardboard box 1, 3, 5 or 10 blisters).

Composition of 1 tablet:

• active substance: carvedilol - 6.25, 12.5 or 25 mg;
• additional components (6.25 / 12.5 / 25 mg): lactose monohydrate - 51.8 / 59.1 / 10 mg; anhydrous colloidal silicon dioxide - 2.5 / 3.75 / 4 mg; magnesium stearate - 1.5 / 1 / 1.5 mg; sucrose - 21.25 / 12.5 / 25 mg; povidone K25 - 1 / 0.5 / 1 mg; crospovidone - 15.5 / 10.5 / 15.5 mg; dye red iron oxide (E172) - 0 / 0.1 / 0 mg; dye yellow iron oxide (E172) - 0.2 / 0.3 / 0 mg.

Pharmacological properties

Pharmacodynamics

Carvedilol belongs to the blockers of α1-, β1- and β2-adrenergic receptors. It has antiproliferative (in relation to smooth muscle cells of the vessel walls) and organoprotective effect. It is an antioxidant that removes free oxygen radicals.

Carvedilol is a racemic mixture of S (-) and R (+) stereoisomers, each of which has the same antioxidant and α-adrenergic blocking properties. The beta-adrenergic blocking action is due to the levorotatory S (-) stereoisomer and is non-selective.

Carvedilol has no internal sympathomimetic activity and, like propranolol, has a membrane stabilizing effect. By reducing the release of renin, it lowers the activity of the renin-angiotensin-aldosterone system, and therefore, fluid retention characteristic of selective alpha-blockers is rarely observed.

Carvedilol lowers total peripheral vascular resistance by selectively blocking α1-adrenergic receptors. Does not adversely affect the lipid profile and maintains a normal low / high density lipoprotein ratio.

In arterial hypertension, carvedilol, due to the combined blockade of β- and α1-adrenergic receptors, lowers blood pressure (blood pressure). Not all restrictions that apply to traditional beta-blockers apply to carvedilol. A decrease in blood pressure does not occur with a simultaneous increase in the total peripheral vascular resistance, which is observed when taking non-selective beta-blockers. The heart rate (heart rate) decreases slightly. There is no violation of renal blood flow and renal function, changes in stroke volume of blood and a decrease in total peripheral vascular resistance, blood supply to organs and peripheral blood flow. Increased fatigue during physical exertion and cold extremities are noted in rare cases. The antihypertensive effect persists for a long time.

Carvedilol is not among the effective agents for the treatment of renovascular arterial hypertension, including chronic renal failure, as well as in patients who are on hemodialysis or have undergone a kidney transplant. Carvedilol leads to a gradual decrease in blood pressure on days with / without dialysis. Its antihypertensive effect is comparable to that of undisturbed renal function.

Carvedilol is better tolerated and more effective than slow calcium channel blockers. It helps reduce morbidity and mortality among patients with cardiomyopathy who are on dialysis.

In ischemic heart disease, carvedilol has a long-term antianginal and anti-ischemic effect. It significantly reduces the activity of the sympathoadrenal system and myocardial oxygen demand. It also reduces pre- and afterload.

In the treatment of chronic heart failure, carvedilol reduces the mortality rate and the number of hospitalizations, reduces the severity of symptoms and improves left ventricular function in non-ischemic / ischemic disease. Its effects are dose-dependent.

Pharmacokinetics

• absorption: carvedilol is rapidly absorbed after oral administration. Its maximum plasma concentration in the blood (C _max) is reached after about 1.5 hours (T _max) and is 21 mg / l. It is a substrate for a carrier protein that acts as a pump in the intestinal lumen, glycoprotein P;
• distribution: about 95% of carvedilol binds to blood plasma proteins (it has high lipophilicity). Its volume of distribution varies in the range of 1.5–2 l / kg;
• metabolism: biotransformation of carvedilol occurs by oxidation and conjugation to form a number of metabolites excreted in the bile. The existence of the intestinal-hepatic circulation of the initial substance is shown. The oxidative metabolism of carvedilol is stereoselective. Various cytochrome P450 isoenzymes (CYP2E1, CYP2D6, CYP2C9, CYP1A2, CYP3A4) may be involved in the process of hydroxylation and oxidation. The S-stereoisomer is metabolized mainly by the isoenzymes CYP2D6 and CYP2C9, the R-stereoisomer (to a greater extent) is CYP2D6;
• genetic polymorphism: the isoenzyme CYP2D6 plays an important role in the metabolism of the R- and S-stereoisomers of carvedilol. Plasma concentrations of R- and S-stereoisomers in the blood increase with low activity of the CYP2D6 isoenzyme (the genetic polymorphism of the CYP2D6 isoenzyme has a certain clinical significance);
• excretion: after a single dose of 50 mg, about 60% is secreted in the bile and excreted in the form of metabolites through the intestines for 11 days. About 16% in the form of carvedilol or its metabolites is excreted by the kidneys. Less than 2% of the substance is excreted unchanged by the kidneys. The plasma clearance of carvedilol reaches approximately 600 ml / min, the half-life is approximately 2.5 hours. The total clearance of the R-stereoisomer after oral administration is approximately 2 times less than that of the S-stereoisomer.

Indications for use

• ischemic heart disease, including therapy for unstable angina pectoris and painless myocardial ischemia;
• essential arterial hypertension (as monotherapy, or in combination with other antihypertensive drugs, in particular, with diuretics or slow calcium channel blockers);
• chronic heart failure of ischemic / non-ischemic genesis in mild, moderate and severe course in order to reduce the number of complications - mortality, hospitalization, as well as to improve well-being and slow the progression of the disease (in combination with diuretics, angiotensin-converting enzyme inhibitors, in some cases - with digitalis preparations).

Also, Dilatrend can be prescribed as an adjunct to standard therapy for patients who do not receive vasodilators, digitalis drugs or nitrates.

Contraindications

Absolute:

• cardiogenic shock;
• severe arterial hypotension (with systolic pressure <85 mm Hg);
• sick sinus syndrome;
• decompensated / acute chronic heart failure, the therapy of which requires intravenous administration of inotropic agents;
• functional liver disorders of clinical significance;
• AV block II – III degree (except for patients with an artificial pacemaker), severe bradycardia (<50 beats / min);
• burdened history of bronchospasm and bronchial asthma;
• age up to 18 years;
• period of breastfeeding;
• established individual intolerance to the components of the drug.

Relative (diseases / conditions in which the appointment of Dilatrend requires caution):

• psoriasis;
• thyrotoxicosis;
• chronic obstructive pulmonary disease;
• depression;
• AV block I degree;
• major surgery and general anesthesia;
• Prinzmetal's angina;
• peripheral vascular occlusive disease;
• pheochromocytoma;
• hypoglycemia;
• renal failure;
• myasthenia gravis;
• diabetes;
• pregnancy.

Dilatrend instructions for use: method and dosage

Dilatrend is taken orally with a sufficient amount of liquid.

Essential hypertension

The initial dose in the first 2 days of use is 12.5 mg once a day, then a single dose should be increased to 25 mg.

In the future, if necessary, with a break of at least 14 days, the dose can be increased, bringing it to the highest daily dose - 50 mg (in 1-2 doses).

Cardiac ischemia

The initial dose of Dilatrend in the first 2 days of use is 12.5 mg 2 times a day, then a single dose should be increased to 25 mg.

In the future, if necessary, with a break of at least 14 days, the dose can be increased, bringing it to the highest daily dose - 100 mg (in 2 divided doses).

Chronic heart failure

Dilatrend dose should be selected individually; therapy should be carried out under close medical supervision. Before taking the drug in patients receiving diuretics, digitalis drugs and angiotensin-converting enzyme inhibitors, their doses must be stabilized.

The recommended initial dose for 14 days is 3.125 mg 2 times a day. If Dilatrend is well tolerated, with interruptions of at least 14 days, a single dose is sequentially increased to 6.25 / 12.5 / 25 mg. The dose should be increased to the maximum at which good tolerance is maintained.

Maximum single doses (with a frequency of administration 2 times a day):

• all patients with severe disease, patients with mild / moderate disease weighing up to 85 kg - 25 mg;
• patients with mild / moderate severity weighing from 85 kg - 50 mg.

Before each dose increase in Dilatrend, the patient should be examined by a physician for a possible increase in symptoms of vasodilation / heart failure. With fluid retention or a transient increase in symptoms of heart failure, the dose of diuretics should be increased, although in some cases a decrease in the dose of Dilatrend or its temporary cancellation is required.

If drug treatment is interrupted for more than 1 week, its use should be resumed at a lower dose with a further gradual increase according to the above scheme. If therapy has been interrupted for longer than 14 days, Dilatrend should be resumed with a single dose of 3.125 mg.

Elimination of the symptom of vasodilation is possible by reducing the dose of diuretics. If symptoms persist, you can reduce the dose of the angiotensin-converting enzyme inhibitor, and then, if necessary, the dose of Dilatrend. Until the condition stabilizes, its dose should not be increased.

Side effects

Estimation of the incidence of adverse reactions:> 10% - very often; > 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01%, including isolated messages - very rare.

Chronic heart failure

• cardiovascular system: often - a marked decrease in blood pressure, postural hypotension, bradycardia, edema (including peripheral, generalized, depending on the position of the body, hypervolemia, edema of the perineum / lower extremities, fluid retention); infrequently - syncope (including pre-syncope), heart failure and atrioventricular block (during the dose increase period);
• central nervous system: very often - headache, dizziness (as a rule, disorders are of a mild nature, most often develop at the beginning of therapy), depression, asthenia (including increased fatigue);
• hematopoietic system: rarely - thrombocytopenia; very rarely - leukopenia;
• digestive system: often - diarrhea, nausea, vomiting;
• metabolism: often - weight gain, hypercholesterolemia; in the presence of diabetes mellitus - hypoglycemia / hyperglycemia, decompensation of carbohydrate metabolism;
• others: often - visual impairment; rarely - renal failure and impaired renal function with diffuse vasculitis / renal dysfunction.

Arterial hypertension, ischemic heart disease

The nature of side effects from the cardiovascular system during long-term therapy of coronary heart disease and treatment of arterial hypertension is similar to that of heart failure, only they occur with a slightly lower frequency.

Possible violations:

• cardiovascular system: often - postural hypotension, bradycardia, syncope, especially at the beginning of the use of Dilatrend; infrequently - peripheral circulatory disorders (Raynaud's syndrome, cold extremities, exacerbation of intermittent claudication syndrome), AV block, peripheral edema, symptoms of heart failure, angina pectoris;
• central nervous system: often - headache, dizziness and general weakness (as a rule, they are mild, most often develop at the beginning of therapy); infrequently - sleep disturbances, low mood, paresthesia;
• digestive system: often - dyspeptic disorders (including nausea, abdominal pain, diarrhea); infrequently - vomiting, constipation;
• respiratory organs: often - bronchospasm and shortness of breath (if there is a predisposition); rarely - nasal congestion;
• laboratory parameters: very rarely - increased activity of hepatic transaminases (alanine aminotransferase, gamma-glutamyl transferase, aspartate aminotransferase), leukopenia, thrombocytopenia;
• skin: infrequently - skin reactions (dermatitis, allergic rash, itching, urticaria;
• others: often - pain in the limbs, irritation of the eyes; decreased tear production; infrequently - decreased potency, visual impairment; rarely - urination disorders, dry mouth; very rarely - allergic skin reactions (rash, exanthema, itching, urticaria), bronchospasm, flu-like syndrome, exacerbation of psoriatic eruptions, nasal congestion, sneezing, shortness of breath (if there is a predisposition).

During the use of Dilatrend, the possibility of manifestation of latent diabetes mellitus, inhibition of the contrainsular system or decompensation of existing diabetes mellitus is not excluded.

Overdose

The main symptoms of Dilatrend overdose: bradycardia, marked decrease in blood pressure, heart failure, cardiac arrest, cardiogenic shock.

It is also possible to develop respiratory disorders, bronchospasm, vomiting, generalized seizures and confusion.

During therapy, in addition to general measures, it is also necessary to monitor and correct vital signs, if necessary, in the intensive care unit.

The patient should be laid on his back (with raised legs), after which the following measures can be taken (depending on the indications):

• atropine intravenously, 0.5–2 mg - with severe bradycardia;
• glucagon intravenously in a stream at 1-10 mg, then in the form of a long-term infusion of 2-5 mg per hour - in order to maintain cardiovascular activity;
• sympathomimetics (isoprenaline, dobutamine, orciprenaline or epinephrine) in different doses (depending on the therapeutic efficacy and weight). If it is necessary to administer drugs with a positive inotropic effect, phosphodiesterase inhibitors are prescribed. If arterial hypotension dominates in the clinical picture of overdose, norepinephrine is administered under continuous monitoring of blood circulation parameters;
• an artificial pacemaker - with bradycardia resistant to therapy;
• aminophylline intravenously, beta-adrenomimetics in the form of an aerosol (in cases of ineffectiveness, intravenous administration is possible) - with bronchospasm;
• clonazepam, diazepam intravenously slowly - with convulsions.

Severe overdose of Dilatrend with shock symptomatology can occur with lengthening of the half-life of carvedilol and elimination of the drug from the depot; therefore, maintenance therapy should be carried out for a rather long time. The duration of detoxification / maintenance therapy is determined by the severity of the overdose. It should not be interrupted until the patient has stabilized.

special instructions

During the dose selection period, patients with chronic heart failure may experience fluid retention or an increase in symptoms of heart failure. In such cases, an increase in the dose of diuretics is required. Do not increase the dose of Dilatrend until the condition stabilizes. Sometimes it may be necessary to reduce its dose or temporarily cancel it. Such episodes do not interfere with further correct dose selection. Combined use with cardiac glycosides should be carried out with caution (due to the likelihood of an excessive slowdown in AV conduction).

With chronic heart failure and low blood pressure (with systolic blood pressure <100 mm Hg), coronary heart disease and diffuse vascular changes and / or renal failure, a reversible deterioration in renal function may occur (dose adjustment is possible).

For patients with chronic obstructive pulmonary disease (including bronchospastic syndrome) who do not receive oral / inhaled anti-asthma drugs, Dilatrend should be prescribed only in cases where the expected benefit outweighs the potential risk. When the initial signs of bronchospasm appear, the dose of the drug should be reduced.

In patients with diabetes mellitus, Dilatrend can mask / reduce the symptoms of hypoglycemia (in particular, tachycardia). With heart failure and diabetes mellitus, therapy may be accompanied by decompensation of carbohydrate metabolism.

The drug can aggravate the symptoms of arterial insufficiency (should be taken into account in the presence of peripheral vascular diseases), reduce the severity of symptoms of thyrotoxicosis.

Due to the likelihood of the summation of the negative effects of anesthetics and Dilatrend, the drug should be used with caution in patients who undergo surgery under general anesthesia.

During the period of therapy, bradycardia may develop, in cases of diagnosing a heart rate below 55 beats / min, the daily dose is reduced.

In the presence of anamnestic data on severe hypersensitivity reactions, as well as in patients undergoing a course of desensitization, Dilatrend should be prescribed with caution (due to the likelihood of increased sensitivity to allergens and the severity of anaphylactic reactions).

Patients with a history of the onset / exacerbation of psoriasis when using beta-blockers, Dilatrend can be prescribed only after a careful assessment of the benefit / risk ratio.

During the period of treatment, the amount of tear fluid may decrease, which must be taken into account by patients using contact lenses.

The drug is intended for long-term use. Its cancellation should be carried out gradually with a dose reduction at intervals of 7 days (especially important for patients with ischemic heart disease).

If a pheochromocytoma is suspected, Dilatrend should be administered with caution (the safety profile in this group has not been studied).

The color of the tablets may change when stored in the light.

The use of ethanol during the treatment period should be excluded.

Influence on the ability to drive vehicles and complex mechanisms

According to the instructions, Dilatrend should be administered with caution to patients whose work is associated with the need to have quick psychomotor reactions. The likelihood of individual reactions to the use of the drug should be taken into account - the development of dizziness, general weakness, especially at the beginning of therapy, when adjusting the dose and while using it with alcohol.

Application during pregnancy and lactation

There is no sufficient experience of using Dilatrend in pregnant women.

Carvedilol reduces placental blood flow, which can cause fetal death and premature birth. In addition, the fetus and the newborn may develop adverse reactions (in particular, hypoglycemia and bradycardia, complications from the lungs and heart). Animal studies have not revealed teratogenicity.

It is contraindicated to use Dilatrend during pregnancy unless the expected benefit is greater than the possible harm.

It has been established that carvedilol and its metabolites in animals pass into breast milk. There is no data on the excretion of Dilatrend with human milk, therefore its use during breastfeeding is contraindicated.

Pediatric use

Due to the lack of data confirming the safety / efficacy of Dilatrend, its use is contraindicated in this group of patients.

With impaired renal function

In patients with renal impairment, Dilatrend should be used with caution.

No dose adjustment is required for severe renal impairment.

For violations of liver function

In the presence of clinically significant violations of hepatic function, the drug is contraindicated.

Drug interactions

With the combined use of Dilatrend with certain drugs / substances, the following effects may develop:

• inhibitors / inducers of hepatic metabolism: rifampicin - a significant decrease in the concentration of carvedilol; cimetidine - an increase in the area under the concentration-time curve at a constant C _max (caution is required, but the likelihood of developing any clinically significant interactions is small);
• insulin or oral hypoglycemic drugs: increasing their hypoglycemic effect; symptoms of hypoglycemia, especially tachycardia, may subside / mask (regular monitoring of blood glucose is recommended);
• digoxin: an increase in its concentration; slowing down of atrioventricular conduction (at the beginning of the use of Dilatrend, when selecting its dose or canceling therapy, it is recommended to regularly monitor the plasma concentration of digoxin);
• drugs that lower the content of catecholamines, including reserpine, monoamine oxidase inhibitors: the occurrence of severe bradycardia / arterial hypotension (the combination requires caution);
• clonidine: potentiation of antihypertensive and heart rate-slowing effects; when canceling, dilatrend should be canceled first, after which clonidine should be canceled with a gradual dose reduction;
• cyclosporine (for chronic vascular graft rejection after kidney transplantation): a moderate increase in the average minimum concentrations of cyclosporine (requires careful monitoring of its concentration and, if necessary, dose adjustment);
• verapamil, diltiazem and other drugs with antiarrhythmic action, including amiodarone, propranolol: an increase in the likelihood of atrioventricular conduction disorders;
• drugs with antihypertensive action (for example, α1-blockers) or drugs that have a hypotensive effect as a side effect: enhancement of their action;
• blockers of slow calcium channels, including verapamil, diltiazem: there is information about individual cases of conduction disturbances, rarely - in combination with violations of hemodynamic parameters (therapy should be carried out under the control of blood pressure and ECG);
• α1-adrenergic receptor agonists, including phenylephrine: preventing an increase in blood pressure;
• some drugs for general anesthesia: synergistic negative inotropic effect.

Analogs

Dilatrend analogues are: Carvedigamma, Carvedilol, Carvenal, Acridilol, Vedicardol, Bagodilol, Talliton and others.

Terms and conditions of storage

Store in a place protected from light (in closed packages) at temperatures up to 25 ° C. Keep out of the reach of children.

Expiry date (depending on the dosage of the tablets):

• 6.25 mg - 3 years;
• 12.5 mg - 4 years;
• 25 mg - 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Dilatrend

The drug has a fairly high cost among analogues.

There are few reviews about Dilatrend that testify to its effectiveness.

Dilatrend price in pharmacies

Dilatrend's price for a package containing 30 tablets is: 6.25 mg - about 450 rubles, 12.5 mg - on average from 530 to 600 rubles, 25 mg - in the range of 670-710 rubles.

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!