Verapamil - instructions for use, dose, side effects, contraindications

Excipients: magnesium stearate - 4.50 mg, microcrystalline cellulose - 18.20 mg, lactose monohydrate - 5,30 mg, sodium alginate - 114,75 mg, hydroxypropylmethylcellulose 4000 cP (hypromellose) - 38.25 mg, hydroxypropyl methylcellulose 5 cP (hypromellose) - 9.00 mg.

Sheath: Fill blue OY-L-30944 - 7.00 mg [hydroxypropylmethylcellulose 6 cP (hypromellose) - 4.3750 mg, titanium dioxide (E 171) -1.4518 mg, talc 0.7000 mg, macrogol 400 0.4375 mg, indigo carmine dye (E 132) - 0.0210 mg, iron oxide black (E 172) - 0.0140 mg, iron oxide yellow (E 172) - 0.0007 mg].

Description:

Oblong, biconvex tablets, covered with a coat of grayish-blue color, with a risk on one side.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

ATX: & nbsp

C.08.D.A.01 Verapamil

C.08.D.A Phenylalkylamine derivatives

Pharmacodynamics:

Verapamil is one of the main drugs group of blockers of "slow" calcium channels. It has antiarrhythmic, anti-anginal and anti-hypertensive activity.

The drug reduces the need for myocardium in oxygen by reducing myocardial contractility and reducing the heart rate (heart rate). Causes the enlargement of the coronary vessels of the heart and increases coronary blood flow; reduces the tone of the smooth muscles of peripheral arteries and the general peripheral vascular resistance.

Verapamil significantly slows 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 the treatment of angina of vasospastic genesis (Prinzmetal angina). Has an effect in angina pectoris, as well as in the treatment of angina with supraventricular rhythm disorders.

Pharmacokinetics:

Suction: When taken orally about 90-92% verapamil is absorbed in the gastrointestinal tract, but the bioavailability is low and is approximately 20% because of the intensive metabolism at the "first passage" through the liver. The concentration of verapamil in the blood plasma increases gradually. The maximum concentration in the blood plasma is 81.34 ng / ml. T_m_Oh averaging 4.75 hours.Relatively "high therapeutic concentrations in blood plasma (51.6 ng / ml) are detected and 24 hours after ingestion. About 90% of the drug binds to plasma proteins.

Distribution: Half-life with a single dose is an average of 2.8 - 7.4 hours; when taking repeated doses - 4,5 -12 hours. The half-life of plasma from the blood of elderly people is increasing. Verapamil penetrates the placental barrier and is found in breast milk.

Metabolism: It is metabolized by the "first pass" through the liver. Twelve metabolites were found. The main metabolite is noravapamil, which has pharmacological activity, other metabolites are mostly inactive.

Excretion: About 70% of the accepted dose of the drug is excreted in the urine, and approximately 16% or more is excreted with feces for five days when the drug is administered orally. About 3 - 4% is excreted from the body in unchanged form.

Indications:

- arterial hypertension;

- prevention of angina attacks (including angina of Prinzmetal);

- prophylaxis of supraventricular tachycardias.

Contraindications:

Hypersensitivity to the components of the drug, pronounced bradycardia, cardiogenic shock, sinoatrial block, atrioventricular blockade of II and III degree, sinus node syndrome (bradycardia-tachycardia syndrome), sinoatrial blockade, severe arterial hypotension, Wolff-Parkinson-White syndrome, acute phase of complicated myocardial infarction (with bradycardia, severe arterial hypotension, left ventricular failure), age under 18 years (efficacy and safety not established), pregnant nce and lactation.

Carefully:Atrioventricular block of degree I, chronic cardiac insufficiency, arterial hypotension (systolic blood pressure less than 90 mm Hg), atrial fibrillation / flutter with Wolff-Parkinson-White syndrome (risk of ventricular tachycardia), impaired liver function.

Dosing and Administration:

Take with food or immediately after meals, washing down with a little water. Tablets are not chewed. Doses of the drug are selected individually.

Arterial hypertension

In patients with hypertension, the dose of the drug varies from 240 mg to 360 mg.In the case of patients who show a slow decrease in blood pressure, treatment should be started with ½ prolonged-action tablets, in the morning.

The maximum daily dose is 360 mg.

An increase in the daily dose to 480 mg should be performed only in the hospital.

Usually Faithpamil prolonged action is prescribed in an average daily dose of 240 mg (1 tablet) once a day in the morning, if necessary 240 mg in the morning and 120 mg (^½tablets) in the evening with an interval of 12 hours.

Lower initial doses of 120 mg are prescribed for patients with impaired liver and kidney function, elderly patients.

Prevention of angina attacks

At the beginning of treatment, the drug is prescribed for 120 mg with a frequency of 1-2 times a day at intervals of 12 hours. The maximum daily dose is 240 mg.

Prevention of supraventricular tachyarrhythmias

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

In patients with impaired liver function, the effect of verapamil is increased and becomes more prolonged (as a result of a slow metabolism drug, which depends on the severity of violations, liver function). In such cases, the dose should be adjusted cautiously and treatment should begin with lower doses of verapamil, using verapamil in other dosage forms (tablets of 40 mg).

Side effects:

From the side of the cardiovascular system: sinus bradycardia, sinoatrial block, asystole, AV blockade I, II and III degrees, the bradyarrhythmic form of atrial arrhythmia, the development or strengthening of symptoms of heart failure, lowering blood pressure, palpitation, tachycardia.

From the central nervous system: rarely - dizziness, drowsiness, inhibition, headache, fatigue, increased excitability, tremor, erythromelalgia or paresthesia.

From the digestive tract: constipation, nausea, vomiting, intestinal obstruction, pain or discomfort in the abdomen.

Laboratory indicators: an increase in the activity of "hepatic" enzymes, alkaline phosphatase, an increase in the level of prolactin.

Allergic reactions: exanthema, urticaria, angioedema, syndrome Stevens-Johnson.

Other: flushes, peripheral edema, very rarely - myalgia and arthralgia. There were reports of cases of galactorrhea and impotence, gynecomastia, gingival hyperplasia.

Overdose:

A marked decrease in blood pressure (in some cases to levels that can not be measured), shock, loss of consciousness, AV blockade I, II degree, often in the form of periods of Wenkebach with or without a slipping rhythm, complete AV blockade with complete atrioventricular dissociation, slipping rhythm, cardiac arrest, sinus bradycardia, stopping the sinus node, heart failure, asystole, sinoatrial blockade.

Giving help: at early detection (it should be borne in mind that active the substance is released and absorbed in the intestine within 48 hours after ingestion) - gastric lavage is recommended in all cases if at least 12 hours have passed since the time of taking the drug, as well as at a later time with reduced motility of the gastrointestinal tract (absence of intestinal noises during auscultation ).

Treatment is symptomatic and depends on the clinical picture of the overdose.

Calcium is a specific antidote: 10-30 ml of 10% calcium gluconate solution is injected as an intravenous injection (2.25-4.5 mmol), if necessary, re-injected or as a slow drop infusion (eg, 5 mmol / h).

In the case of atrioventricular block of II or III degree, sinus bradycardia, cardiac arrest: atropine, isoprenaline, orciprenaline or heart stimulation.

In the case of arterial hypotension: dopamine, dobutamine, norepinephrine (norepinephrine). Hemodialysis is not effective.

Interaction:

With the simultaneous administration of the drug Verapamil with carbamazepine, the effect of the latter increases and the risk of toxic lesions of the nervous system increases.

Appointment of verapamil patients receiving long-term preparations of lithium, increases the risk of neurotoxic effect of lithium preparations.

Simultaneous application with rifapicin or phenobarbital, leads to a decrease in the effectiveness of verapamil.

Cimetidine strengthens the action of Verapamil.

Combined application with other antihypertensive agents, diuretics, vasodilators leads to a mutual reinforcement of their action.

Combination with beta-blockers can lead to an increase in the negative inotropic effect, an increased risk of violations AV conduction, bradycardia.

With simultaneous reception of the drug Verapamil and digoxin, theophylline, cyclosporine or chiidine, it is possible to increase the concentration in the blood of the above drugs against the background of Verapamil therapy.

With lipid-lowering agents: atorvastatin (increased levels of atorvastatin in the blood serum), lovastatin (increased serum levels of lovastatin), simvastatin (increase AUC approximately 2.6 times and a maximum concentration of about 4.6 times simvastatin).

Patients receiving verapamil, treatment with HMG-CoA reductase inhibitors should be started with as low a dose as possible, which is gradually increased. If you want to assign verapamil patients already receiving inhibitors of HMG-CoA reductase, it is necessary to revise their doses, respectively serum cholesterol concentrations.

Fluvastatin, pravastatin and rosuvastatin Do not metabolize under the action of isoenzymes CYP3A4, so their interaction with verapamil is least likely.

FROM almotriptan - increase AUC approximately 20% and the maximum concentration of almotriptan by approximately 24%.

Grapefruit juice - increase AUC and maximum concentration of verapamil.

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

Doxorubicin - the half-life of doxorubicin decreases (by approximately 27%) and the maximumconcentration (approximately 38%).

In patients with progressive neoplasms verapamil does not affect the level or clearance of doxorubicin. In patients with small cell lung cancer verapamil reduces half-life and maximum concentration of doxorubicin. Hypoglycemic agents (glyburide) - increase in the maximum concentration of glyburide (by approximately 28%), AUC (approximately by 26%).

Aspirin (acetylsalicylic acid) increased bleeding.

Effect on the ability to drive transp. cf. and fur:

Depending on the individual response to the treatment, the patient's ability to driving a car or working with mechanisms can be reduced, which is especially important at the beginning of therapy.

Form release / dosage:Tablets of prolonged action coated with 240 mg.

Packaging:

10 tablets per blister are perforated from aluminum foil and PVC film.

2 blisters together with instructions for use in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of 15-25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N011991 / 03

Date of registration:23.05.2011

Expiration Date:Unlimited

The owner of the registration certificate:Alkaloid, JSCAlkaloid, JSC Macedonia

Manufacturer: & nbsp

Alkaloid AO The Republic of Macedonia

Information update date: & nbsp29.01.2017

Illustrated instructions

Instructions

Verapamil (Verapamil)