Verapamil, pills 80mg, 20pcs

Composition

Active ingredient:

verapamil hydrochloride ( in terms of 100% substance) – 40 mg or 80 mg;

Auxiliary substances:

lactose monohydrate-26.12 mg / 52.24 mg,

potato starch-9.5 mg/19.0 mg,

talc-0.375 mg/0.75 mg,

calcium stearate-0.375 mg/0.75 mg,

povidone K 17-3.63 mg/7.26 mg;

Shell excipients:

Polysorbate-80 (tween-80) – 0,2 mg/0,4 mg, titanium dioxide – 0,614 mg/1,228 mg, hypromellose (hydroxypropyl methylcellulose) was 1.06 mg/2,12 mg, beeswax yellow – 0.002 mg/0.004 mg, liquid paraffin -0,12 mg/0,24 mg, tropeolin About -0,004 mg/0,008 mg.

Pharmacological action

Verapamil is one of the main drugs of the group of slow calcium channel blockers. It has antiarrhythmic, antianginal and antihypertensive activity. The drug reduces the need for oxygen in the myocardium by reducing the contractility of the myocardium and reducing the heart rate. Causes dilation of the coronary vessels of the heart and increases coronary blood flow; reduces smooth muscle tone of peripheral arteries and total peripheral vascular resistance. Verapamil significantly slows down atrioventricular conduction, inhibits the automatism of the sinus node, which allows the drug to be used for the treatment of supraventricular arrhythmias. Verapamil is the drug of choice for the treatment of vasospastic angina (Prinzmetal angina). It has an effect on angina pectoris of tension. The action of verapamil begins 1-2 hours after ingestion, the maximum effect develops in most cases after 48 hours. Pharmacokinetics: When taken orally, more than 90% of the dose is absorbed. Bioavailability – 10-20%. The maximum concentration of the drug in the blood plasma is reached 1-2 hours after oral use (80-400 mg / ml). Verapamil penetrates the blood-brain and placental barriers. It is metabolized during the “primary passage” through the liver. The main metabolites are norverapamil, N-dealkylnorverapamil. Accumulation of the drug and its metabolites in the body explains the increased effect of course treatment. The relationship with plasma and blood proteins is 90%, the half-life with a single dose is 2.8-7.4 hours; with repeated doses-4.5-12 hours. It is excreted in small amounts in unchanged form (3-4%), the rest – in the form of metabolites (70%) by the kidneys, about 25% – with bile. The secretion in breast milk is low.

Indications

-Arterial hypertension. – Ischemic heart disease, including chronic stable angina (classical tension angina); unstable angina; angina caused by vasospasm (Prinzmetal angina). – Paroxysmal supraventricular tachycardia. – Atrial fibrillation / flutter accompanied by tachyarrhythmia (with the exception of Wolf-Parkinson-White and Laun-Ganong-Levin syndrome).

Contraindications

Hypersensitivity to the components of the drug, severe bradycardia (less than 50 beats/min), chronic heart failure in the decompensation stage, hypotension (below 100/60 mm Hg in men and 95/60 mm Hg in women), cardiogenic shock (except caused by arrhythmia), sinoatrial block, atrioventricular block II and III degrees (excluding patients with an artificial pacemaker); acute myocardial infarction complicated by bradycardia, severe hypotension and left ventricular insufficiency, sinus node weakness syndrome (except in patients with artificial pacemaker), aortic stenosis, Wolf-Parkinson-White syndrome, Morgagni-Adams-Stokes syndrome, concomitant use of beta-blockers (intravenous); Lown – Ganong-Levin syndrome, concomitant use of colchicine, lactose intolerance, lactase deficiency, glucose-galactose malabsorption, pregnancy, lactation, age up to 18 years. With caution: With caution, the drug is prescribed to patients with grade I atrioventricular block, severe liver and kidney function disorders, in the elderly, with bradycardia, hypertrophic obstructive cardiomyopathy, with diseases related to neuromuscular transmission (myasthenia gravis, Lambert-Eaton syndrome, Duchenne muscular dystrophy).

Side effects

From the cardiovascular system: AV block of I, II, III degrees, sinus node arrest, peripheral edema, tachycardia, sinus bradycardia, heart failure, marked decrease in blood pressure, “flushes” of blood to the skin of the face, palpitation sensation. From the gastrointestinal tract: nausea, vomiting, abdominal pain and discomfort, intestinal obstruction, constipation, diarrhea, gum hyperplasia, increased appetite; transient increase in “liver” transaminases and alkaline phosphatase in blood plasma;From the central nervous system: dizziness, tinnitus, headache, fainting, anxiety, lethargy, fatigue, asthenia, drowsiness, depression, extrapyramidal disorders, parasthesia, tremor. Allergic reactions: pruritus, urticaria, skin rash, erythema multiforme (including Stevens-Johnson syndrome), angioedema. Other: weight gain, agranulocytosis, gynecomastia, hyperprolactinemia, galactorrhea, arthritis, pulmonary edema, asymptomatic thrombocytopenia, purpura, peripheral edema, alopecia, muscle weakness, myalgia, arthralgia, erectile dysfunction.

Interaction

When used concomitantly with carbamazepine in patients with persistent partial epilepsy due to inhibition of carbamazepine metabolism in the liver, verapamil increases its effect (risk of side effects from the central nervous system, such as diplopia, headache, ataxia and dizziness).

When used concomitantly, verapamil inhibits cyclosporine metabolism in the liver, which leads to a decrease in its excretion and an increase in its concentration in blood plasma. This is accompanied by an increase in the immunosuppressive effect.

When used concomitantly, verapamil increases the concentration of theophylline (due to a decrease in clearance).

When verapamil is co-administered with quinidine, the concentration of quinidine in the blood plasma increases (the risk of a pronounced decrease in blood pressure, especially in patients with hypertrophic obstructive cardiomyopathy).

When used concomitantly, verapamil increases the concentration of ethanol in the blood plasma and prolongs its effect.

Since verapamil inhibits the surZa 4 isoenzyme, which is involved in the metabolism of atorvastatin, lovastatin and simvastatin, drug interactions may occur due to increased statin plasma concentrations (rhabdomyolysis).

When used concomitantly, verapamil increases the plasma concentrations of almotriptan and glibenclamide.

When used concomitantly, verapamil increases the plasma concentrations of sirolimus and tacrolimus.

When used concomitantly, verapamil increases the concentration of cardiac glycosides (requires careful monitoring and reducing the dose of glycosides). When used concomitantly, verapamil increases the concentration of metoprolol and propranolol in patients with angina pectoris.

When used concomitantly, verapamil increases the plasma concentration of colchicine (a substrate for the surZa isoenzyme and p-glycoprotein).

When verapamil is co-administered with doxorubicin, the concentration of doxorubicin in the blood plasma increases and its effectiveness increases.

Concomitant use of verapamil with imipramine increases the concentration of imipramine in blood plasma (risk of undesirable changes due to the additive inhibitory effect of verapamil and imipramine on AV conduction). It does not affect the concentration of the active metabolite, desipramine.

Verapamil increases the concentration of prazosin and terazosin when used simultaneously (risk of severe hypotension).

With simultaneous use of verapamil with buspirone or midazolam, their concentration in blood plasma increases (the risk of increased side effects). surZa 4 inhibitors (including erythromycin, human immunodeficiency virus protease inhibitors), telithromycin increase plasma concentrations of verapamil.

Grapefruit juice increases plasma concentrations of the r-and s-isomers of verapamil.

Cimetidine either does not change or reduces the clearance of verapamil (possibly increasing the effects of verapamil).

Rifampicin can significantly reduce the bioavailability (up to 92%), as well as the concentration of verapamil in blood plasma, which leads to a decrease in its clinical effectiveness.

Phenobarbital increases the clearance of verapamil by 5 times.

Sulfinpyrazone increases the clearance of verapamil by approximately 3 times and reduces bioavailability by up to 60%.

St. John’s wort preparations reduce the concentration of the r – and s-isomer of verapamil in blood plasma.

Concomitant use of verapamil with inhaled anesthetics increases the risk of developing bradycardia, atrioventricular block, and heart failure. The combination of verapamil with beta-blockers can lead to an increase in the negative inotropic effect, an increased risk of atrioventricular conduction disorders, and bradycardia (the use of verapamil and beta-blockers should be carried out at intervals of several hours).

Prazosin and other alpha-blockers, as well as other antihypertensive drugs (angiotensin-converting enzyme inhibitors, vasodilators, diuretics, beta-blockers) enhance the antihypertensive effect of verapamil.

With simultaneous use of verapamil with disopyramide and flecainide, severe hypotension and collapse, up to a fatal outcome, are possible. The risk of developing severe drug interactions is associated with increased negative inotropic effects.Disopyramide and flecainide should not be administered for 48 hours before or 24 hours after verapamil, as Verapamil increases the risk of neurotoxic effects of lithium preparations.

Verapamil enhances the effect of peripheral muscle relaxants (may require a change in the dosage regimen).

With simultaneous use of verapamil with acetylsalicylic acid, cases of increased bleeding time have been described.

How to take, course of use and dosage

Verapamil is taken orally during or after a meal with a small amount of water. The dosage regimen and duration of treatment are set individually depending on the patient’s condition, severity, features of the course of the disease and the effectiveness of therapy. For the prevention of angina attacks, arrhythmias and in the treatment of arterial hypertension, the drug is prescribed in an initial dose of 40-80 mg 3-4 times a day. If necessary, increase the single dose to 120-160 mg. The maximum daily dose of the drug is 480 mg. With long-term treatment, the daily dose of 480 mg should not be exceeded. In the maximum dose, the drug should be taken only in a hospital. In patients with severe hepatic impairment, the elimination of verapamil from the body is slow, so it is advisable to start treatment with minimal doses. The daily dose of the drug should not exceed 120 mg.

Overdose

Symptoms: sinus bradycardia leading to high-grade atrioventricular block, sometimes asystole, marked decrease in blood pressure, heart failure, shock, sinus node arrest, hyperglycemia, stupor, and metabolic acidosis. Treatment for early detection-gastric lavage, taking activated charcoal, setting up an artificial pacemaker; for rhythm and conduction disorders-intravenous use of isoprenaline, norepinephrine, atropine,10-20 ml of 10% calcium gluconate solution, artificial pacemaker; intravenous infusion of plasma-substituting solutions. Hemodialysis is not effective.

Special instructions

If blood pressure increases in patients with hypertrophic obstructive cardiomyopathy, alpha-adrenostimulants (phenylephrine) are prescribed; isoprenaline should not be used. Before starting therapy for heart failure, it is necessary to achieve a state of compensation. During treatment, it is necessary to monitor the function of the cardiovascular and respiratory systems, the concentration of glucose and blood electrolytes, the volume of circulating blood and the amount of urine released. It is not recommended to stop treatment suddenly” on ” the drug can not be canceled abruptly, it is recommended to gradually reduce the dose until the drug is completely discontinued. When taking the drug, it is necessary to monitor renal function in patients with impaired renal function. Influence on the ability to drive vehicles and mechanisms:After taking verapamil, individual reactions (drowsiness, dizziness) are possible, affecting the ability to perform work that requires high concentration of attention and the speed of psychomotor reactions. Use with caution when working for drivers of vehicles and people whose profession is associated with increased concentration of attention (reduced reaction speed).

Storage conditions

In a dry place, protected from light and out of reach of children, at a temperature not exceeding 25 °C.

Shelf

life is 3 years.

Active ingredient

Verapamil

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension, Arrhythmia