Veratard 180

General characteristics. Structure:

International and chemical names: verapamil; 5-[(3,4-dimetoksifenetit) - methylamine]-2-(3,4-dimetoksifenit) - 2-izopropilvaleronitrit a hydrochloride; main physical and chemical properties: the solid capsules with a lid of yellow color and the transparent colourless case containing pellets white with yellowish or color, white with a creamy shade; structure: 1 capsule contains verapamil of a hydrochloride 180 mg in the form of pellets with the prolonged release.

Pharmacological properties:

Pharmacodynamics. Verapamil belongs to derivatives of a fenilalkilamin. The selection blocker of calcium channels. Drug shows anti-hypertensive, anti-anginal, anti-ischemic and antiarrhytmic properties. The mechanism of pharmacological effect of drug consists in blockade ^{of Sa2 +} channels and oppression of transmembrane transfer of ions ^{of Sa2 +} is preferential in cells of unstriated muscles of vessels and a myocardium. At myocardium ischemia verapamil eliminates a disproportion between requirement and supply of heart with oxygen, reduces contractility of a myocardium, has the vasodilating effect. Reduction of a tone of peripheral arteries promotes decrease in the general peripheric resistance of vessels and arterial pressure. Verapamil oppresses sinuatrial and AV conductivity, possesses antiarrhytmic action.

Pharmacokinetics. At oral administration of drug active ingredient verapamil is gradually released from capsular weight at the expense of what constant concentration it in blood is maintained. Time of achievement of the maximum concentration in plasma – 5-7 hours. Release of drug happens almost linearly within 8-12 hours. It is metabolized at "the first passing" through a liver with formation of several metabolites. The main metabolite is norverapamit, having less expressed hypotensive activity, than not changed verapamil. Linkng with proteins of a blood plasma – 90%.
Owing to effect of "the first passing" through a liver bioavailability of drug at a single dose makes 30%, and an elimination half-life – about 7 hours. At multiple dose the elimination half-life averages 12 hours that is connected with saturation of fermental systems of a liver and increase in concentration of verapamil in a blood plasma. It is excreted generally with urine (70%) in the form of metabolites, partially – with a stake.

Indications to use:

Arterial hypertension, prevention of attacks of stenocardia, prevention of attacks of a supraventricular Bouveret's disease at patients is more senior than 14 years.

Route of administration and doses:

The dose is selected by the doctor individually. In an initiation of treatment drug Veratard 180 is appointed on 1 capsule once a day, in the morning. Increase in a dose should be carried out after 2 weeks of use of drug. The dose is increased to 360 mg/days (on 1 capsule in the morning and in the evening, with an interval about 12 hours between receptions). Exceeding of a dose is possible only for very short time and under careful control of the doctor. For children of 14-18 years the dosing mode – as for adults.
At reception of verapamil in dosage forms with slow release during food time of achievement of the maximum concentration of initial drug and its metabolite of a norverapamil in a blood plasma increases, however bioavailability does not change. Therefore verapamil can be accepted to, in time or after food, without chewing and not rassasyvy, washing down with a small amount of water.

Features of use:

With care appoint drug at abnormal liver functions, AV to blockade І degrees (in connection with a possibility of transition to a total block). Use of drug for treatment of pregnant women (especially in І and ІІІ trimesters) and the women nursing is shown only when the expected therapeutic effect for the patient exceeds a possible negative impact on a fruit or the child.
After Veratard's reception 180 individual reactions (drowsiness, dizzinesses) influencing ability to perform the work requiring special attention and speed of psychomotor reactions are possible.

Side effects:

From cardiovascular system: erubescence of the person, sinus bradycardia, AV blockade, sinuatrial blockade, arterial hypotension, asystolia, bradiaritmichesky form of a ciliary arrhythmia, heart failure.
From a nervous system: dizziness, block, headache, feeling of fatigue, nervousness, paresthesias.
From digestive tract: heartburn, nausea, locks of atonic character.
Others: allergic reactions (a skin itch, rashes), tranzitorny increase in hepatic transaminases, an alkaline phosphatase, mialgiya, arthralgia, hypostases in anklebones.

Interaction with other medicines:

Simultaneous use of Veratard 180
– with Amiodaronum is an inadmissible combination: there is a danger of a cardiac standstill;
– with carbamazepine strengthens effect of carbamazepine due to suppression of his metabolism and emergence of side effects in the form of toxic defeats of a nervous system;
– with lithium drugs: Veratard's use by 180 patients, is long accepting lithium drugs, can lead to increase in sensitivity of an organism to lithium and toxic defeat of a nervous system;
– with rifampicin leads to decrease in antibacterial activity of rifampicin;
– with phenobarbital leads to decrease in the depriving of bonuses activity of phenobarbital;
– with Cimetidinum strengthens Veratard's action 180;
– with β-adrenoblockers, means for an inhalation anesthesia, cardiac glycosides and antiarrhytmic drugs Іа a class: there is mutual strengthening of the oppressing influence on automatism of a sinus node, AV conductivity, contractility and conductivity of a myocardium;
– with Baclofenum, imipraminovy antidepressants, neuroleptics: strengthening of hypotensive effect of Veratard 180 is possible;
– with organic nitrates is a rational combination of drugs. There is summation of anti-anginal and hypotensive action, the reflex tachycardia caused by nitrates decreases;
– with digoxin, theophylline, cyclosporine, quinidine: there is an increase in their concentration in a blood plasma;
– with other anti-hypertensive means (with vazodilatator, thiazide diuretics, APF inhibitors): there is mutual strengthening of hypotensive action;
– with the drugs which are actively contacting proteins of a blood plasma (with aminazine, warfarin, diazoxide, non-selective inhibitors of the return neyronalny capture of monoamines, Prazozinum, propranolol, Tolbutamidum, phenylbutazone, Phenytoinum, furosemide): there is an increase in concentration of free fraction of one of drugs, and it demands dose adjustment;
– with macroleads: considerably the probability of development of fibrillation of ventricles increases.

Contraindications:

Hypersensitivity to verapamil. An acute heart failure, the expressed bradycardia (ChSS <50 beats/min), a sick sinus syndrome, AV blockade of IІ ІІ the I degrees, WPW syndrome, arterial hypotension (systolic pressure less than 90 mm of mercury.), chronic heart failure. The expressed abnormal liver function. Children's age up to 14 years.

Overdose:

The overdose of drug can cause the expressed bradycardia, AV blockade, arterial hypotension, heart failure, cardiogenic shock, an asystolia, sinuatrial blockade.
Treatment: the gastric lavage is recommended in all cases if from the moment of administration of drug there passed no more than 12 hours, and also in later terms at reduced motility of a GIT (lack of intestinal noise at auscultation). Symptomatic therapy. As a specific antidote there can be an intravenous administration of 10-20 ml of 10% of solution of a gluconate of calcium (2,25 - 4,5 mmol). If necessary introduction can be repeated or carried out additional drop infusion (with a speed of 5 mmol/h). Correction of hemodynamic disturbances. The hemodialysis is inefficient.

Storage conditions:

To store in dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C.
Period of validity – 2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 capsules in a blister strip packaging; on 3 or 5 planimetric packagings in a pack.