Verapamil is a drug used in pathologies of a vascular nature and certain types of cardiac arrhythmias. By action on the body is one of the blockers of calcium channels. There are many analogues in Verapamil, all have a direction of closure of calcium channels.
The international classifier has the number 53-53-9.When using the drug, carefully study the instructions for use, since there are contraindications for certain categories of patients. So, let's consider the instructions for the use of the drug Verapamil, indications for use, its price, reviews, analogues.
Features of the preparation
Composition
The component composition of the verapamil tablets includes the main active ingredient - verapamil hydrochloride. The complete chemical name of the substance according to the IUPAC nomenclature is considered as a derivative of benzeneacetonitrile with several complex substituents and is represented in the hydrochloride form. The white matter powder has good solubility in water and organic solvents.
As auxiliary substances, stearic magnesium, butyl hydroxy anisole, gelatin, starch, calcium dihydrogen phosphate, titanium oxide, talc and a food cellulose derivative are included in Verapamil for better resorption of the tablet form and shaping.
Dosage forms
- Verapamil is produced in two dosage forms: tableted and injectable. Depending on the manufacturer of the drug and a number of other reasons, the minimum price for both tablets and ampoules is registered at 46 rubles per package( the manufacturer of ampoules is the pharmaceutical company Biosintez, the manufacturer of tablets is Ozone).
- The company "Alcaloid" delivers at a more expensive cost of Verapamil, but the assortment includes tablets of the drug at 40 mg and 80 mg and ampoules from 54 to 70 rubles.
- The highest cost of registered Verapamil retard tablets is 240 mg at 178 rubles.
Tablets are packed in blisters of 10 pieces. Tablets and ampoules are packed in carton boxes. Next, we consider the mechanism of action of verapamil.
Pharmacological action
Acting from the inside to the cell membrane, Verapamil covers the calcium channels and blocks the entry and exit of calcium ions through the membrane complex. The degree of polarization of the membrane plays a leading role in activating the closure of calcium channels. The less polarized the cell membrane, the greater the capacity of the active substance to block the channel. The sodium channels and one of the types of adrenoreceptors are dependent on Verapamil, but to a lesser extent than the channels of calcium.
- Verapamil reduces the frequency of contractions of the striated muscle tissue of the heart, reduces the rate of nerve impulses in the sinus-atrial and atrioventricular node, eliminates spasms of the peripheral arteries and arterioles, reduces the overall peripheral vascular resistance.
- Reduces the imbalance between the amount of oxygen required and consumed.
- Has a vasodilating property in relation to vessels, resulting in a reduction in systolic pressure.
- Reduces myocardial tension in the left ventricle, relieves spasms of the coronary arteries of the heart, preventing the development of angina pectoris.
- Headaches are reduced in case of impaired blood circulation in the vessels of the brain.
- The outflow of blood from the ventricles increases, the habituation and resistance of malignant tumor cells to the action of chemotherapeutic drugs decreases.
Pharmacokinetics
Verapamil is excreted by the digestive system( approximately a sixth), the main system for excretion of metabolites of the drug is urinary. The primary disintegration of the drug is carried out by the hepatic cells.
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The opinion of doctors. .. & gt; & gt;
Abuse of pregnant women of the drug causes intrauterine fatal outcome of the fetus. Verapamil easily penetrates through the hematomolar and hematoplanket barriers. Tests conducted on the effect of the drug on increasing the frequency of mutagenicity and tissue degeneration into malignant tumors showed a negative result.
Pharmacodynamics
Absorption of the active substance in the gastrointestinal tract is high, more than 90%.The amount of bioavailability varies from 20 to 35%.The drug effect of verapamil hydrochloride is combined with plasma proteins, the connection with which reaches more than 90%.
Intermediate product of Verapamil decomposition is noreapamil, which has activity of the active substance, but the pharmacological effect is 5 times weaker.
- The effect of the drug continues for 9 hours, for tablets and capsules with prolonged action - 1 day.
- Intravenous administration of the drug provides an effect for arrhythmia for 2 hours, with blood analysis after administration is stored in the plasma as a free substance for about 20 minutes.
- The half-life is 3-7.5 hours, repeated intake in conditions of saturation of the enzyme system of the liver is from 4 to 12 hours.
- Early disintegration after intravenous administration does not exceed 4.5 minutes. Late decay occurs in the interval of 2-5 hours.
Indications
Verapamil is indicated with:
- hypertension of pulmonary vessels;
- of arterial hypertension;
- by a sharp increase in systolic pressure( intravenous injection);
- of moderate degree of angina pectoris;
- supraventricular tachycardia;
- atrial fibrillation with rapid rhythm;
- atrial tachycardia.
In pregnancy, the possible risk of verapamil on the fetus should be evaluated. It is used in cases of exceeding the potential danger to the health of the mother. Breastfeeding is not recommended if the drug is started because of full penetration through the placenta. Children are allowed to use the drug in the dosage indicated by the pediatrician.
Contraindications
Verapamil is restricted to use in cases of:
- lactation period in women;
- childhood, if there is a choice of softer anti-anginal and antihypertensive drugs;
- during pregnancy;
- individual sensitivity to verapamil hydrochloride;
- acute phase of myocardial infarction;
- ventricular tachycardia;
- shock state of cardiogenic etiology;
- stenosis of the anterior aorta;
- all forms of heart failure;
- arterial hypotension;
- for the preliminary administration of a drug substance for blockade of β-adrenergic receptors;
- atrial fibrillation;
- of toxic myocardial dystrophy of medicinal origin;
- porphyrin disease;
- other cardiac abnormalities if the doctor finds them hazardous to use.
Instruction for use
Duration of the treatment period Verapamil is determined by the attending physician, taking into account the severity of the disease, the age of the patient, the effectiveness of the treatment, the features of the course of the disease. Capsules and tablets Verapamil should be taken with meals or after.
The drug is not allowed to use at a dose of more than 0.48 g per day. A single dose should not exceed 0.16 g. Usually, a doctor prescribes a dosage of 2 tablets 3 times a day( 40 mg tablet).Patients with hepatic pathologies can receive a dose that is 3 times lower than in patients with a relatively healthy liver.
Side effects of verapamil
The administration of the drug may be accompanied by swelling of the extremities of the extremities, redness of the skin and itching in patients prone to allergic reactions to chemicals. Individual patients experience rapid fatigue, headache, a low response rate to events, systolic hypotension, a decrease in the rhythm of heartbeats.
High doses of verapamil can provoke heart failure. There are cases of reactions from the gastrointestinal tract in the form of constipation, the urge to vomit.
Special instructions
During the reception of Verapamil, the patient needs medical supervision over the activity of the circulatory and respiratory systems, the concentration of ions and sugar in the blood plasma, the volume of diuresis and circulating blood.
Reviews
Reviews of doctors and patients with cardiovascular pathologies indicate a positive therapeutic effect if no side effects are detected. Verapamil to a number of patients, in their opinion, saves life after 80 years with discovered problems of heart rhythms.
Individual patients indicate the addiction of the organism to the active substance of the drug, as a result of which the therapeutic effect of taking the remedy is reduced. With increasing dosage, the symptoms of extrasystole and arrhythmia reduce the intensity of manifestation.
Analogues
Drugs with active substance verapamil hydrochloride number more than a half dozen. The most popular of them are Kaveril, Flamon, Isoptin, Verolhalid ER 240 and others.
Even more useful information about the drug Verapamil is contained in the video below: