Verapamil

When ATH:
C08DA01

Characteristic.

Derivative fenilalkilamina. Verapamil hydrochloride - a white crystalline powder. Soluble in water, xloroforme, methanol.

Pharmacological action.
Antianginalnoe, gipotenzivnoe, antiarrhythmic.

Application.

Paroxysmal supraventricular tachycardia (except WPW-syndrome), sinus tachycardia, Atrial premature beats, fibrilloflutter, angina (incl. Princmetala, voltage, postinfarctnaya), arterial hypertension, hypertensive crisis, idiopathic hypertrophic stenosis subaortalnыy, gipertroficheskaya cardiomyopathy.

Contraindications.

Hypersensitivity, severe hypotension, cardiogenic shock, AV блокада II и III степени, myocardial infarction (acute or recent history and complexity of the phenomenon of bradycardia, gipotenzii, left ventricular failure), Chronic heart failure stage III, WPW-syndrome, sick sinus syndrome (if not implanted pacemaker), sinoatrialynaya blockade, syndrome morgagni-Adams-Stokes, digitalisnaya intoxication, severe aortic stenosis, pregnancy, lactation.

Restrictions apply.

AV block I degrees, Chronic heart failure stage I or II, vыrazhennaya bradycardia (less 50 u. / min), mild or moderate hypotension, vыrazhennaya myopathy (Duchenne syndrome), abnormal liver function or kidney, ventricular tachycardia with a wide QRS complex (for I / O reference).

Pregnancy and breast-feeding.

Contraindicated in pregnancy.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

At the time of treatment should stop breastfeeding.

Side effects.

Cardio-vascular system and blood (hematopoiesis, hemostasis): gipotenziya, bradycardia (sinus), AV ʙlokada, heart failure.

From the nervous system and sensory organs: headache, dizziness, nervousness, lethargy, drowsiness, weakness, fatiguability, paresthesia.

From the digestive tract: nausea, dyspepsia, constipation; rarely giperplazia gums, increase in liver transaminases, Alkaline phosphatase.

Allergic reactions: skin rash, hives, itching; rarely, angioneurotic edema, Syndrome Stevens - Johnson.

Other: facial flushing, bronchospasm (at / in the introduction), peripheral edema, very rarely ginekomastia, increased secretion of prolactin (individual cases).

Cooperation.

Increases plasma levels of digoxin, cyclosporine, teofillina, karʙamazepina, reduces-lithium. It weakens the antibacterial activity of rifampicin, deprimiruyuschie effect of phenobarbital, reduces the clearance of metoprolol and propranolol, enhances the effect of muscle relaxants. Rifampicin, sulfinpirazon, phenobarbital, calcium salt, Vitamin D-weakening effect. Increase the hypotensive effect of antihypertensive drugs (Diuretic, vasodilators), tricyclic and tetracyclic antidepressants and antipsychotics: antianginalny-nitrates. Beta-blockers, antiarrhythmics class IA, cardiac glycosides, inhalation anesthetics, X-ray contrast agents potentiate (mutually) a depressing effect on the automatism of sinoatrial node, AV conduction and myocardial contractility. If you are applying with acetylsalicylic acid Verapamil-strengthening existing bleeding. Cimetidine increases the plasma verapamil.

Overdose.

Symptoms: hypotension, bradycardia, OF блокада, cardiogenic shock, coma, asistolija.

Treatment: as a specific antidote used calcium gluconate (10-20 Ml 10% solution / in); bradycardia and AV blockade atropine, isoprenaline or orciprenaline; hypotension-plazmozameŝaûŝie solutions, Dopamine, norepinephrine; on the signs of heart failure-dobutamin.

Dosing and Administration.

Inside, during or immediately after a meal, drinking plenty of fluids.

Angina -for 80-120 mg 3 once a day, against the background of liver function abnormalities, in old age — on 40 mg 3 once a day.

Arrhythmias — in case of chronic atrial fibrillation on therapy of cardiac glycosides-240-320 mg/day 2-3 reception; for the prophylaxis of paroxysmal supraventricular tachycardia-240-480 mg/day 2-3 reception.

Hypertension - By 80 mg 3 once a day, if necessary - up 360 mg / day; patients older or small-to 40 mg 3 once a day; Children up to 6 years — 40-60 mg/day, 6-14 years-80-360 mg/day in 3-4 reception. In the form of dosage forms prolonged action when hypertension is on 180-240 mg/day once in the morning; the lack of effectiveness, increase the dose as follows:: 240 mg in the morning, then 180 mg in the morning + 180 mg in the evening (perhaps 240 mg in the morning + 120 mg in the evening) and further on 240 mg 2 times a day at intervals of 12 no, elderly patients or small growth 120 mg; If there is no adequate effect after dose 120 mg successive increase to 180, 240, 360 and 480 mg once in the morning.

When angina and arrhythmia -in the form retard forms 120-240 mg 2 times a day at intervals of 12 no. The tablets of 200 mg: by 1 Table. 1-2 Times a day, or 2 Table. 1 once a day.

Dosage form 24-hour controlled release (Only fully taken into) — for hypertension on 180 mg once at night; If necessary dose increase to consistently 240 mg at night, 360 mg (2 Table. by 180 mg) at night and then 480 mg (2 Table. by 240 mg) for the night.

In / in slowly: adults initial dose of 5-10 mg (for not less than 2 m), with little effect possible re-introduction of 30 min dose 10 mg. Children up 1 year under the control of ECG in the dose of 0.1-0.2 µg/kg (usually a single dose of 0.75-2 mg), for not less than 2 m, children 1-15 years in a dose of 0.1-0.3 mg/kg for at least 2 m (typically, a single dose is not more than 2-5 mg). In hypertensive crisis is 5-10 mg in/in slowly.

Precautions.

Be wary appoint patients with hypertrophic cardiomyopathy complicated by obstruction of the left ventricle, high-pressure pulmonary capillary wedge, paroxysmal nocturnal dyspnea or orthopnea, dysfunction of the sinoatrial node. When administered to patients with severe hepatic impairment and neuromuscular transmission (myopathy Dyushenna) require constant medical supervision and, perhaps, dose reduction. Be wary of during the drivers of vehicles and people, skills relate to the high concentration of attention (decreases the rate of reaction), is recommended that the use of alcohol.

Cautions.

The injectable form is incompatible with albumin, injectable formulations of amphotericin B, gidralazina, sulfamethoxazole, trimethoprim and may precipitate in a solution with a pH above 6,0.

Cooperation

Active substanceDescription of interaction
AkarʙozaFMR: antagonizm. Against the background of the effect of verapamil attenuated; the combined appointment requires constant monitoring of blood glucose concentrations.
Atenolol + XlortalidonFMR. Against the backdrop of intensified verapamil chrono, ino- and dromotropic effects.
Atrakuriya besilateFMR: synergism. Against the background of verapamil increases and prolonged muscle relaxation.
Acetylsalicylic acidFMR: synergism. Against the background of verapamil increases hypocoagulation activity and enhanced existing bleeding.
BumetanidFMR: synergism. May exacerbate (mutually) hypotensive effect.
ValsartanFMR: synergism. Strengthens (mutually) hypotensive effect.
Vekuroniya bromideFMR: synergism. Against the background of verapamil increases and prolonged muscle relaxation.
HalothaneFMR: synergism. It enhances the inhibition of the functions of the cardiovascular system (growing hypotension and oppression AV conduction).
Gidroxlorotiazid + CaptoprilFMR. Strengthen (mutually) hypotensive effect.
DigoxinFKV. FMR. On the background due to the decrease in clearance of verapamil and / or volume of distribution of concentration in the blood increases the risk of toxicity.
DiltiazemFMR: synergism. Strengthens (mutually) effects.
DoxorubicinAccording to experimental data, amid verapamil increases the initial peak concentration in the heart with increasing frequency and severity of the degenerative changes in the myocardium, accompanied by a shortened term survival.
IndomethacinFMR: antagonizm. It weakens the hypotensive effect by inhibiting PG kidney, circulatory deterioration in them with sodium and water retention.
Candesartan cïleksetïlFMR: synergism. Strengthens (mutually) hypotensive effect.
CarbamazepineFKV. FMR. Against the background of verapamil may increase the concentration, that leads to several side effects (diplopia, headache, ataxia or dizziness).
KlonidinFMR: synergism. Strengthens (mutually) hypotensive effect.
KolekaltsiferolFMR. It weakens the hypotensive effect.
Lithium carbonateWhen combined with the appointment of possible increase in the level of lithium in the tissues and strengthening of its neurotoxic effects.
LozartanFMR: synergism. Strengthens (mutually) hypotensive effect.
MetoprololFKV. Strengthens (mutually) hypotensive effect. Against the background of reduced clearance of verapamil.
MinoksidilFMR: synergism. Strengthens (mutually) hypotensive effect.
NadololFMR: synergism. Strengthens (mutually) hypotensive effect and increases the likelihood of violations of automaticity, conduction and myocardial contractility, increased negative impact on the heart rate (tyazhelaya bradycardia), AV conduction (until total blockade) and / or cardiac contractility.
NicotineFKV. FMR: antagonizm. By accelerating the biotransformation, It reduces the concentration in the blood and reduces the severity of anti-anginal, hypotensive and anti-arrhythmic effects.
OctreotideChanges effect; a joint application may require dose adjustment of verapamil.
PerindoprilFMR: synergism. Strengthens (mutually) hypotensive effect.
PrazosinFMR: synergism. Strengthens (mutually) hypotensive effect.
PramipexoleFKV. Against the background of verapamil, compete for the transport system, secreted into the tubules cations, reduced clearance (about 20%).
PropranololFMR: synergism. Strengthens (mutually) effect and may increase the negative effect on the heart rate, AV conduction and / or cardiac contractility, causing severe bradycardia, OF блокаду (up to complete). Against the background of reduced clearance of verapamil.
RamiprilFMR: synergism. Strengthens (mutually) hypotensive effect.
RifampicinFKV. FMR. Reduces bioavailability (It increases the loss of "first pass" through the liver), accelerates biotransformation (induces the activity of microsomal enzymes), lowers blood concentration, reduces the severity of antianginal, hypotensive and anti-arrhythmic effects.
Rokuroniya bromideFMR: synergism. Against the background of verapamil increases and prolonged muscle relaxation.
SpiraprilFMR: synergism. Strengthens (mutually) hypotensive effect.
TheophyllineFKV. Against the background of verapamil (reduces the activity of cytochrome P450) increased plasma levels and the risk of toxicity.
TrandolaprilFMR: synergism. Strengthens (mutually) hypotensive effect.
FelodipineFMR: synergism. Strengthens (mutually) effects.
PhenobarbitalFKV. Accelerates biotransformation, may increase the clearance and reduce the effects of.
FurosemidFMR: synergism. Strengthens (mutually) hypotensive effect.
QuinidineFKV. Against the background of verapamil (It inhibits the cytochrome P450) increasing concentration in the tissues and the risk of toxic effects.
XlortalidonFMR: synergism. Strengthens (mutually) hypotensive effect.
CyclosporineAgainst the background of verapamil (reduces the activity of cytochrome P450) increasing concentration in the tissues and increases the risk of toxic effects.
EnalaprilatFMR: synergism. Strengthens (mutually) hypotensive effect.
EprosartanFMR: synergism. Strengthens (mutually) hypotensive effect.
EthanolAgainst the background of verapamil, reducing the rate of failure, increased plasma concentration, at the time of treatment should abandon spirits.

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