Veratard 180

Verardard 180 is a selective antagonist of the Ca element, predominantly affecting heart function.

Indications Veratarda 180

It is used in cases of increased blood pressure, as well as to prevent angina pectoris attacks and paroxysmal supraventricular tachycardia.

Release form

The release of the medication occurs in capsules, in the amount of 10 pieces inside a packing pack. The box contains 3 or 5 such packs.

Pharmacodynamics

Verapamil is a derivative of the element phenylalkylamine, selectively blocks Ca channels. It has antianginal, antihypertensive, antiarrhythmic and antiischemic activity.

The therapeutic effect of the drug develops by blocking the Ca2 + channels, as well as suppressing the transmembrane transport of Ca2 + ions (mainly inside the smooth muscle cells of the myocardium with the vessels).

In the case of myocardial ischemia, the drug eliminates the imbalance between oxygen demand and the supply of the heart, and in addition reduces myocardial contractility and has a vasodilating effect. The weakening of the peripheral arterial tone leads to a decrease in blood pressure and overall peripheral vascular resistance.

Verapamil inhibits sinoatrial as well as AV conduction; has anti-arrhythmic effect.

Pharmacokinetics

After taking the drug inside the verapamil is gradually subjected to release, thereby maintaining its constant level inside the blood. It takes 5-7 hours to get plasma Cmax values. The process of release of the substance is carried out almost linearly, for 8-12 hours.

Subjected to the 1st intrahepatic passage, resulting in the formation of several metabolic products. The main metabolic product is the substance norverapamil, which has a weaker antihypertensive effect than the unchanged active element of drugs. Intlasma protein synthesis is 90%. 

Due to the effect of the 1st hepatic passage, the values of drug bioavailability after 1 single dose are 30%, and the half-life is approximately 7 hours. After repeated use of drugs, the average half-life is up to 12 hours - due to saturation of the enzyme hepatic systems and an increase in the plasma level of verapamil.

The excretion of the drug is largely carried out with the urine (70%) in the form of metabolic products, and another part is excreted in the feces.

Dosing and administration

The dosage can be selected only by a medical specialist, separately for each patient. At the initial stage of therapy, Verardard 180 is used in the amount of the 1st capsule, 1 time per day, in the morning. Increasing the portion is allowed after 14 days of taking the drug. Raising occurs to 0.36 g per day (taking the 1st capsule in the morning, as well as in the evening, the interval between uses is approximately 12 hours). Exceeding the allowable portion is allowed only for a very short period and under careful medical supervision.

The use of therapeutic forms of the drug with a slow release rate together with food increases the time it takes to reach peak values of verapamil with norverapamil inside the blood plasma, but their level of bioavailability remains the same. Because of this, the medicine is allowed to be used with food, before it and after it. Capsules do not chew and do not dissolve; swallow, squeezed with plain water.

Use Veratarda 180 during pregnancy

To use the drug during pregnancy (especially on the 1st and 3rd trimesters), and besides lactation is allowed only in situations where the probability of helping a woman is more expected than the negative impact on the fetus or baby.

Contraindications

Among the contraindications:

• the presence of hypersensitivity against verapamil;
• acute CH;
• pronounced degree of bradycardia (heart rate values are <50 beats / minute);
• SSSU;
• having 2nd or 3rd degree AV block;
• WPW syndrome;
• decreased blood pressure (systolic blood pressure below 90 mm Hg);
• CHF;
• having a pronounced degree of disorder in the liver.

Side effects Veratarda 180

The use of the drug may cause the following side effects:

• lesions associated with the cardiovascular system: sinus bradycardia, sinoatrial or AV blockade, reddening of the skin on the face, asystole, a decrease in blood pressure, and in addition CH and atrial fibrillation, which has a bradyarrhythmic character;
• dysfunction of the NA: paresthesia, dizziness, feeling of nervousness, lethargy or fatigue, as well as headaches;
• disorders of the gastrointestinal tract: nausea, atonic secretion and heartburn;
• other signs: allergy symptoms (rash or itching), transient increases in alkaline phosphatase or liver transaminases, arthralgia with myalgia and swelling in the ankle zone.

[1]

Overdose

Drug intoxication leads to AV blockade, severe bradycardia, HF, asystole, cardiogenic shock, and in addition to sinoatrial blockade and a decrease in blood pressure.

To eliminate these disorders, gastric lavage is carried out (during the passage of a segment less than 12 hours from the moment of taking the drug). It can also be performed later if there is weakened intestinal motility (during auscultation intestinal noise does not occur). In addition, symptomatic procedures are performed.

As an antidote, it is allowed to inject 10-20% calcium gluconate intravenously (in the amount of 2.25-4.5 mmol). If necessary, such an injection is allowed to be repeated or perform an additional infusion procedure through an IV line (speed is 5 mmol / hour). Correction arising hemodynamic disorders. Hemodialysis does not work.

Interactions with other drugs

Drug combination with the component amiodarone is prohibited - it increases the risk of heart failure.

The use together with carbamazepine potentiates the activity of the latter, because its metabolic processes are inhibited. As a result, negative symptoms develop in the form of NA intoxication.

The combination of the drug with long-lasting lithium drugs can increase the body's sensitivity to lithium and, in addition, provoke NS poisoning.

Taking it along with rifampicin causes a weakening of the antibacterial properties of this drug.

When combined with phenobarbital, a weakening of the depriving effect of this element is noted.

When combined with cimetidine, the pharmacological properties of Veratarda 180 are potentiated.

When used together with the inhalation form of anesthetics, β-blockers, antiarrhythmic drugs Іa subtype and SG, mutual potentiation of the suppressive effect on the myocardial-related conductivity is observed along with contractility, AV-conductivity, and also the automatism of the sinus angle.

Administration together with imipramine-type antidepressants, baclofen or antipsychotics can lead to potentiation of the antihypertensive activity of the drug.

Use in combination with nitrates of organic type is considered rational, because with it the antihypertensive and antianginal effects are summed up, and the reflex tachycardia developing under the action of nitrates is weakened.

Combining with theophylline, digoxin, and quinidine or cyclosporine increases the plasma performance of these funds.

Taking it with other hypotensive drugs (diuretic thiazide drugs, vasodilators and ACE inhibitors) leads to a mutual potentiation of antihypertensive activity.

Introduction to combination with drugs that actively undergo protein synthesis within the blood plasma (such as warfarin, tolbutamide, diazoxide, aminazine, prazosin with phenytoin, and besides non-selective monoamine inhibitors (reverse neuronal seizure), phenylbutazone with propranolol and furosemide), causes an increase in the level of the free fraction of such drugs, as a result of which a correction of the portion sizes is necessary.

Use with macrolides significantly increases the risk of ventricular fibrillation.

[2], [3]

Storage conditions

Verardard 180 must be kept in a dark and dry place, closed to small children. Temperature marks - not higher than 25 ° C.

Shelf life

Verardard 180 is allowed to use for a 24-month period from the date of release of the pharmaceutical agent.

Application for children

Appointment of Veratarda 180 in pediatrics is prohibited (persons under 14 years of age).

Analogs

Analogues of the drug are drugs Verapamil, Lekoptin and Verohalide with Isoptin.