Vascopin

Vascopin is a blocking agent for slow Ca channels, a derivative of dihydropyridine.

Indications of the vaskopina

It is used to treat elevated blood pressure (and as a means of monotherapy, and in combination with other antihypertensive drugs). It is also used in the stable or variant form of angina pectoris (for monotherapy or simultaneously with other antianginal drugs).

Release form

Release in tablets of 5 mg. Inside the blister is 10 pieces. In the package there are 4 blister plates.

Pharmacodynamics

The drug is synthesized with dihydropyridine endings and blocks slow Ca channels. In addition, it inhibits the transmembrane movement of calcium into the region of the cells of the smooth cardiac muscle, as well as the vessels (mainly moves inside the cells of the vascular smooth muscle, and not inside the cardiomyocytes).

Has antianginal, and in addition to hypotensive properties.

The hypotensive effect of amlodipine is provided by its direct relaxing effect on the relatively smooth vascular musculature.

Antianginal effects are due to vasodilatation of arterioles having a peripheral type, as a result of which the OPSS decreases. It should be noted that the rate of heart rate remains almost unchanged, which makes it possible to reduce the consumption of energy expended, as well as the oxygen demand of the myocardium. In addition, the expansion of arteries that have a peripheral or coronary type, and with it arterioles (inside normal and also ischemic areas of the myocardium), as a result of which the amount of oxygen entering the myocardium increases in people with angina of a variant type. The drug prevents the emergence of coronarospasm, provoked by smoking.

People with high blood pressure receiving a single daily dose of drugs provides a reduction in pressure in the period of 24 hours in the positions lying and standing. Slow and gradual onset of the Vasconia's effect allows avoiding a sharp drop in blood pressure.

For people with angina, the use of a single daily dosage of amlodipine increases the duration of exercise, and also delays the occurrence of a new attack of angina with depression of the ST-type segment during exercise. Also, the medicine reduces the incidence of angina attacks and the intake of nitroglycerin.

Individuals with SSS pathologies (including coronary atherosclerosis, in which one vessel is affected, as well as stenosis of the 3+ arteries and narrowing of the carotid arteries) who have suffered myocardial infarction or PTCA in the coronary artery, and in addition to having stenocardia, thickening in the carotid CMY. 

In addition, it significantly reduces the rate of death due to cardiovascular disease, stroke with myocardial infarction, as well as coronary artery thrombosis with coronary artery bypass graft. Together with this, it helps to reduce the number of hospitalizations due to unstable angina and progression of CHF, and also reduces the number of procedures for restoring coronary circulation.

The drug does not increase the risk of death or the occurrence of complications that cause death in people with CHF (3-4 functional stage of NYHA) in treatment with diuretics, digoxin, and ACE inhibitors.

In individuals with CHF (grade 3-4 functional grade according to NYHA), which is of non-ischemic origin, the use of Vasconia can cause pulmonary edema.

The drug does not have a negative effect on metabolism, as well as the level of plasma lipids.

Pharmacokinetics

At oral intake of medicinal doses, the amlodipine substance is rapidly absorbed. Eating with food does not affect the absorption of the substance. The peak reaches 6-12 hours after ingestion. The absolute bioavailability is 64-80%. The distribution volume is about 21 l / kg. The synthesis with plasma protein is approximately 97.5%.

Amlodipine is able to pass through the BBB. The equilibrium plasma index is observed after 7-8 days of regular drug use.

Biotransformation occurs inside the liver, resulting in the formation of inactive decay products. The half-life of plasma is approximately 35-50 hours (with the use of the drug once per day). The total clearance is 0.43 l / h / kg.

About 10% of the unchanged active ingredient, and with it 60% of the decay products are excreted in the urine.

The half-life of people with CHF, as well as liver failure is prolonged to 56-60 hours.

In persons with kidney failure, a similar figure rises to 60 hours. The change in the plasma level of amlodipine does not correlate with the degree of functional renal impairment.

The period required for the substance to reach the peak plasma value in the elderly does not practically change in comparison with the younger age. It should be noted that in elderly people with CHF there is a tendency to decrease the level of clearance of the active component, which increases the AUC and half-life (up to 65 hours).

Dosing and administration

When eliminating angina and reducing the elevated blood pressure, the average initial dosage is 5 mg once a day. If there is such a need, it can be increased to a maximum of 10 mg.

Vaskopin should be taken orally - once a day, washing the pill with water (about 100 ml).

In the case of a combination with ACE inhibitors, thiazide diuretics and β-adrenergic blockers, dosage adjustment is not necessary.

Use of the vaskopina during pregnancy

There is no information on the safety of use of VASKINNA by pregnant or lactating women, which is why it is only allowed to take it during this period if the benefit for a woman is higher than the likelihood of a complication of a fetus or baby.

There is no information about the excretion of amlodipine together with the mother's milk, so that during the treatment the drug is required to refuse breastfeeding.

Contraindications

Among the contraindications: hypersensitivity to dihydropyridines, as well as reduced blood pressure in severe form.

Side effects of the vaskopina

Use of the medicine can lead to the development of such side effects:

• manifestations from the CCC: often there are puffiness of the peripheral type (on the feet with ankles) and palpitations. Orthostatic collapse, vasculitis develops more rarely and excessive blood pressure lowering is observed. Cardiac insufficiency develops and worsens occasionally. Individual disorders of the heart rhythm (this includes ventricular tachycardia, atrial fibrillation, as well as bradycardia), chest pain and myocardial infarction with migraine;
• reactions from the musculature and bones: in some cases there are pains in the back and muscle cramps, myalgia or asthenia develops. Myasthenia gravis occasionally occurs;
• disorders from the PNS and CNS: often there are flushes of blood to the face and a sense of heat, and in addition increased fatigue, headaches, a feeling of drowsiness and dizziness. Less often there is insomnia, a sense of anxiety, malaise, nervousness and depression. In addition, asthenia, hyperhidrosis, paresthesia with hypoesthesia, tremor, emotional lability and peripheral neuropathy develops. There are also strange dreams and fainting. Occasionally, there is apathy, but also a feeling of excitement and convulsions. Single amnesia or ataxia develops;
• disorders of the digestive function: often there are pains in the peritoneum and nausea. Less often there is swelling, constipation with vomiting, as well as diarrhea, dyspepsia, thirst and dryness of oral mucous membranes. Occasionally, there is an increase in appetite or gingival hyperplasia. There is a pancreatitis with gastritis, jaundice (mostly of the cholestatic type), hyperbilirubinemia and hepatitis, as well as an increase in the activity of liver transaminases;
• reaction of the hematopoietic system: there is a single thrombocyto- or leukopenia, as well as purpura of thrombocytopenic type;
• violations of metabolic processes: single appears hyperglycemia;
• manifestations from the respiratory organs: in some cases, there may be a runny nose and dyspnoea. There is a cough;
• disorders of the urinary function: sometimes there is an increase in urination or pain during this process, and in addition impotence or nocturia develops. There is polyuria or dysuria;
• manifestations of allergies: in some cases there are rashes on the skin and itching. Single hives, Quincke edema, and also erythema multiforme appear;
• others: there may be an ear ring, eye pain, conjunctivitis, chills and nosebleeds. In addition, alopecia, diplopia, gynecomastia and xerophthalmia develop. Also there are disorders of accommodation, vision or taste buds and there is a decrease or weight gain. Occasionally, dermatitis occurs. There is a disorder of skin pigmentation and xerodermia with parosmia, as well as cold sweat attacks.

Overdose

Signs of an overdose: a marked drop in the level of blood pressure with a possible subsequent appearance of tachycardia of the reflex type, as well as excessive peripheral vasodilation (there is a risk of persistent and strongly pronounced decrease in blood pressure, possibly further development of shock or death).

To eliminate the disorders, activated charcoal is assigned (especially during the first 2 hours after poisoning), and then gastric lavage (sometimes). Also, the victim should be placed so that his limbs have an elevated position, and constantly support the work of the CAS, monitor pulmonary and cardiac functions, and in addition for diuresis and BCC.

To restore vascular tone, as well as indicators of blood pressure (in the absence of contraindications), it is allowed to use vasoconstrictive drugs. In addition, an intravenous injection of calcium gluconate is performed. Since most of the amlodipine is synthesized with whey protein, the hemodialysis procedure will be ineffective.

Interactions with other drugs

In the case of combined use of the drug with cimetidine, there is no change in the pharmacokinetic parameters of amlodipine.

The simultaneous administration of Vascochin and NSAIDs (especially indomethacin) does not lead to the development of significant interactions.

When combined with loop or thiazide diuretics, as well as with ACE inhibitors, nitrates and verpamil with β-adrenoblockers, potentiation of antihypertensive and antianginal properties of Ca channel blockers can be observed. Their antihypertensive effect can be enhanced and when combined with neuroleptics and α-blockers.

Amlodipine does not affect the indices of synthesis with a plasma protein of substances such as indomethacin with phenytoin and digoxin with warfarin (in vitro).

One-time use of magnesium or aluminum-containing antacid drugs has little effect on the pharmacokinetic properties of amlodipine.

A single dose of sildenafil in the amount of 100 mg by persons with an essential form of hypertension does not provoke changes in the pharmacokinetic parameters of amlodipine. When re-ingesting 10 mg of the drug in combination with the use of 80 mg of atorvastatin, no significant changes in the pharmacokinetics of the latter occur.

The combined use of drugs with digoxin in volunteers does not change the clearance in the kidneys, and with it the serum values of digoxin.

One-time and repeated use Vasconia in a dosage of 10 mg does not significantly affect the pharmacokinetic properties of ethyl alcohol.

Amlodipine does not affect the changes in the indices of PTW, which are caused by the substance warfarin.

The pharmacokinetics of the drug cyclosporine varies little under the action of amlodipine.

The combination of a single dose of grapefruit juice (240 ml) together with Vasconin (10 mg) does not significantly affect the pharmacokinetics of the latter.

[1], [2]

Storage conditions

Vaskopin must be kept in a dark place under conditions of a maximum temperature of + 25 ° C.

[3]

Shelf life

Vascopin can be used in the period of 4 years from the date of release of the drug.