Verapamil pills prolonged coated 240mg №20

Active ingredient

Active substance

Verapamil hydrochloride 240 mg.

Excipients

Magnesium stearate, microcrystalline cellulose, lactose monohydrate, sodium alginate, hydroxypropylmethylcellulose 4000 cp (hypromellose), hydroxypropylmethylcellulose 5 cP (hypromellose).

Shell composition

Opadry blue OY-L-30944 (hydroxypropylmethylcellulose 6 cP (hypromellose), titanium dioxide (E 171), talc, macrogol 400, indigo-carmine dye (E 132), ferric oxide black (E 172), ferric oxide yellow (E 172 )).

In the blister of 10 tablets. In packing 2 blisters.

Indications

• Arterial hypertension.
• Prevention of angina attacks (including Prinzmetal stenocardia).
• Prevention of supraventricular tachycardia.

Pharmacokinetics

Suction

When ingested, about 90-92% of Verapamil is absorbed in the gastrointestinal tract, however, bioavailability is low and is approximately 20% due to intensive metabolism during the "first pass" through the liver.

The concentration of verapamil in the blood plasma increases gradually. Maximum plasma concentrations are 81.34 ng / ml T _max averages 4.75 hours.

Relatively high therapeutic plasma concentrations (51.6 ng / ml) are detected after 24 hours after ingestion. About 90% of the drug is bound to plasma proteins.

Distribution

The half-life of a single dose is an average of 2.8-7.4 hours; when taking repeated doses - 4.5-12 hours. The elimination half-life from plasma in the elderly is increasing.

found in breast milk.

Metabolism

Metabolized by the “first pass” through the liver. 12 metabolites detected. The main metabolite is norverapamil, which has pharmacological activity, other metabolites are mostly inactive.

Removal

About 70% of the dose of the drug is excreted in the urine, and about 16% or more is excreted in the feces within five days when the drug is taken orally. About 3-4% is excreted unchanged.

Clinical Pharmacology

Verapamil is one of the main drugs of the “slow” Calcium channel blocker group.

It has antiarrhythmic, antianginal and antihypertensive activity.

The drug reduces myocardial oxygen demand by reducing myocardial contractility and reducing heart rate.

Causes dilatation of the coronary vessels of the heart and increases coronary blood flow; reduces the tone of the smooth muscles of the peripheral arteries and the total peripheral vascular resistance.

Verapamil significantly slows down the atrioventricular (AV) conduction, suppresses the automatism of the sinus node, which allows the use of the drug for the treatment of supraventricular arrhythmias.

Verapamil is the drug of choice for treating angina pectoris of vasospastic genesis (Prinzmetal stenocardia).

It has an effect on exertional angina, as well as in the treatment of angina pectoris with supraventricular rhythm disturbances.

Pregnanacy and breastfeeding

Contraindicated in pregnancy and lactation.

Contraindications

• Hypersensitivity to the drug.
• Severe bradycardia.
• Cardiogenic shock.
• Sinoatrial blockade.
• Atrioventricular block II and III.
• Sick sinus syndrome (bradycardia-tachycardia syndrome).
• Sinoatrial blockade.
• Severe arterial hypotension.
• Wolff-Parkinson-White syndrome.
• Acute phase of complicated myocardial infarction (with symptoms of bradycardia, severe hypotension, left ventricular failure).
• Age up to 18 years (efficacy and safety have not been established).
• Pregnancy.
• Lactation period.

Carefully:

• Atrioventricular block I degree.
• Chronic heart failure.
• Hypotension (systolic blood pressure less than 90 mm Hg).
• Atrial fibrillation / flutter with Wolf-Parkinson-White syndrome (risk of ventricular tachycardia).
• Liver dysfunction.

Adverse Effects

Since the cardiovascular system

Sinus bradycardia, sinoatrial block, asystole, AV blockade I, II and III degrees, bradyarrhythmic form of atrial fibrillation, development or aggravation of symptoms of heart failure, lowering blood pressure, palpitations, tachycardia.

From the side of the central nervous system

Rarely - Dizziness, drowsiness, lethargy, headache, fatigue, irritability, tremor, erythromelalgia or Paresthesia.

From the digestive tract

Constipation, nausea, vomiting, intestinal obstruction, pain, or a feeling of abdominal discomfort.

Laboratory values

Increased activity of "liver" enzymes, alkaline phosphatase, an increase in the level of prolactin.

Allergic reactions

Exanthema, urticaria, angioedema, Stevens-Johnson syndrome.

Other

Tides, peripheral edema.

Very rarely - Myalgia and arthralgia.

It was reported about cases of galactorrhea and impotence, gynecomastia, gum hyperplasia.

Interaction

With the simultaneous appointment of the drug Verapamil

Carbamazzin, increases the effect of the latter and increases the risk of toxic lesions of the nervous system.

The prescription of verapamil to patients who receive lithium for a long time increases the risk of a neurotoxic effect of lithium drugs.

Simultaneous use with rifampicin or phenobarbital reduces the effectiveness of verapamil.

Cimetidine enhances the action of verapamil.

Combined use with other antihypertensive drugs, diuretics, vasodilators leads to mutual enhancement of their action.

The combination with beta-blockers can lead to an increase in the negative inotropic effect, an increase in the risk of AV conduction disturbances and bradycardia.

While taking the drug Verapamil and Digoxin, theophylline, cyclosporine or quinidine, it is possible to increase the blood concentration of the above drugs during therapy with Verapamil.

Lipid-lowering drugs: Atorvastatin (an increase in serum levels of atorvastatin), lovastatin (an increase in serum levels of lovastatin), Simvastatin (an increase of AUC about 2.6 times and a maximum concentration of about 4.6 times simvastatin). Patients receiving verapamil, treatment with HMG-CoA reductase inhibitors should begin with the lowest possible doses, which gradually increase. If it is necessary to prescribe verapamil to patients already receiving HMG-CoA reductase inhibitors, their dose should be reconsidered according to the concentration of cholesterol in the blood serum.

Fluvastatin, pravastatin and Rosuvastatin are not metabolized by the action of CYP3A4 isoenzymes, therefore their interaction with verapamil is less likely.

With almotriptan, an increase in AUC by approximately 20% and a maximum concentration of almotriptan by approximately 24%.

Grapefruit juice - an increase in AUC and maximum concentration of verapamil.

St. John's wort - decreases the AUC of verapamil with a corresponding decrease in the maximum concentration.

Doxirubicin - reduces the half-life of doxirubicin. (approximately 27%) and maximum concentration (approximately 38%). In patients with advanced neoplasms, verapamil does not affect the level or clearance of doxirubicin. In patients with small cell lung cancer, verapamil reduces the half-life and the maximum concentration of doxirubicin.

Hypoglycemic agents (glyburide) - an increase in the maximum concentration of glyburide (approximately 28%), AUC (approximately 26%).

Aspirin (acetylsalicylic acid) - increase bleeding.

Overdosage

Symptoms: marked reduction in blood pressure (in some cases to levels that cannot be measured), shock, loss of consciousness, AV I, II degree block, often in the form of Wenckebach periods with or without a sliding rhythm, complete AV block with complete atrioventricular dissociation, sliding rhythm, cardiac arrest, sinus bradycardia, sinus node arrest, heart failure, asystole, sinoatrial block.

Treatment: with early detection (it must be borne in mind that the active substance is released and absorbed in the intestine within 48 hours after taking the drug inside) - gastric lavage is recommended in all cases, if at least 12 hours have passed since taking the drug, and also later terms with reduced GI motility (lack of intestinal noise during auscultation). The treatment is symptomatic and depends on the clinical picture of the overdose. Calcium is a specific antidote: 10-30 ml of 10% solution of Calcium gluconate is administered as an intravenous injection (2.25-4.5 mmol), if necessary, re-administered or as a slow drip infusion (for example, 5 mmol / hour). In the case of atrioventricular block II or III, sinus bradycardia, cardiac arrest: atropine, isoprenaline, ortsiprenalin or stimulation of the heart. In case of arterial hypotension: dopamine, dobutamine, norepinephrine (norepinephrine). Hemodialysis is not effective.

Dosage and administration

To accept during food or right after food, washing down with a small amount of water. Tablets do not chew. Doses of the drug are selected individually.

Arterial hypertension

In patients with arterial hypertension, the dose of the drug varies from 240 mg to 360 mg. In the case of patients who show a slow reduction in blood pressure, treatment should be started with a long-acting Ug pill in the morning.

The maximum daily dose of 360 mp The increase in the daily dose to 480 mg should be carried out only in the hospital.

Usually, prolonged-acting verapamil is prescribed in an average daily dose of 240 mg (1 tablet) 1 time a day in the morning, if necessary 240 mg in the morning and 120 mg (½ tablet) in the evening at 12-hour intervals. Lower initial doses of 120 mg are prescribed to patients with impaired liver and kidney function, elderly patients.

Prevention of angina attacks

At the beginning of treatment, the drug is prescribed at 120 mg with a dose rate of 1-2 times per day with an interval of 12 hours. The maximum daily dose of 240 mg.

Prevention of supraventricular tachyarrhythmias

The average single dose is 120 mg with a frequency rate of 1-2 times a day.

In patients with impaired liver function

The effect of verapamil increases and becomes longer (as a result of a slower metabolism of the drug, which depends on the severity of liver dysfunction). In such cases, you should set the dose carefully and start treatment with lower doses of verapamil, using verapamil in other dosage forms (40 mg tablets).

Precautionary measures

Influence on ability to drive and work with mechanisms

Depending on the individual response to treatment, the patient's ability to drive or work with mechanisms may be reduced, which is especially important at the beginning of therapy.

Storage conditions

Store in a dark place at a temperature of 15-25 ° C.