Vaskopin

Vaskopin is a slow Ca channel blocker drug, a derivative of the substance dihydropyridine.

Indications Vaskopina

It is used to treat high blood pressure (both as a monotherapy and in combination with other antihypertensive drugs). It is also used for stable or variant angina (for monotherapy or simultaneously with other antianginal drugs).

Release form

Released in tablets of 5 mg. Inside a blister - 10 pieces. In a package - 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 area of smooth cardiac muscle cells, as well as vessels (mostly moves into vascular smooth muscle cells, and not into cardiomyocytes).

It has antianginal and, in addition, hypotensive properties.

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

The antianginal effect occurs due to vasodilation of arterioles of the peripheral type, as a result of which the total peripheral vascular resistance decreases. It should be noted that the heart rate indicator remains almost unchanged, which allows for a reduction in the consumption of expended energy, as well as the oxygen demand of the myocardium. In addition, arteries of the peripheral or coronary type are dilated, and along with this, arterioles (inside normal and ischemic areas of the myocardium), as a result of which the amount of oxygen entering the myocardium increases in people with variant angina. The drug prevents the occurrence of coronary spasm caused by smoking.

For people with high blood pressure, taking a single daily dose of the drug provides a decrease in pressure over a 24-hour period in lying and standing positions. The slow and gradual onset of Vaskopin's effect allows avoiding a sharp decrease in blood pressure.

For people with angina, taking a single daily dose of amlodipine increases the duration of exercise and also delays the onset of a new attack of angina with ST-segment depression during exercise. The drug also reduces the frequency of angina attacks and the use of nitroglycerin.

For people with cardiovascular pathologies (including coronary atherosclerosis, in which 1 vessel is affected, as well as stenosis of 3+ arteries and narrowing of the carotid arteries), who have had a myocardial infarction or PTCA in the coronary arteries, and who also have angina pectoris, taking Vaskopin will help prevent the appearance of thickening in the area of the carotid artery IMC.

In addition, it significantly reduces the incidence of death due to cardiovascular diseases, stroke with myocardial infarction, and coronary artery bypass grafting. At the same time, it helps to reduce the number of hospitalizations due to unstable angina and progression of CHF, and reduces the number of procedures to restore coronary circulation processes.

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

In individuals with CHF (NYHA functional grade 3-4) of non-ischemic origin, the use of Vascopin may cause pulmonary edema.

The drug does not have a negative effect on metabolism or plasma lipid levels.

Pharmacokinetics

When taken orally in medicinal doses, the substance amlodipine is rapidly absorbed. Taking it with food does not affect the absorption of the substance. The peak is reached 6-12 hours after taking it. The absolute bioavailability index is 64-80%. The distribution volume is about 21 l/kg. Synthesis with plasma protein is approximately 97.5%.

Amlodipine is able to pass through the blood-brain barrier. Equilibrium plasma level is observed after 7-8 days of regular use of the drug.

Biotransformation occurs in the liver, resulting in the formation of inactive decay products. The half-life from plasma is approximately 35-50 hours (with single daily administration). The total clearance rate is 0.43 l/hour/kg.

About 10% of the unchanged active ingredient, and along with this 60% of the breakdown products, are excreted in the urine.

The half-life in people with CHF and liver failure is extended to 56-60 hours.

In individuals with renal failure, the same indicator increases to 60 hours. Changes in plasma levels of amlodipine do not correlate with the degree of functional renal impairment.

The period required for the substance to reach peak plasma levels in an elderly person remains virtually unchanged compared to a younger age. It should be noted that elderly people with CHF tend to have a lower clearance rate of the active component, which increases the AUC and half-life (up to 65 hours).

Dosing and administration

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

Vaskopin must be taken orally - once a day, washing down the tablet with water (about 100 ml).

In case of combination with ACE inhibitors, thiazide diuretics and β-blockers, there is no need to change the dosage.

Use Vaskopina during pregnancy

There is no information on the safety of using Vaskopin by pregnant or breastfeeding women, which is why it is allowed to be taken during this period only in cases where the benefit to the woman is higher than the likelihood of the risk of complications in the fetus or infant.

There is no information on the excretion of amlodipine in breast milk, therefore, breastfeeding should be discontinued during treatment with the drug.

Contraindications

Contraindications include hypersensitivity to dihydropyridines, as well as severely reduced blood pressure.

Side effects Vaskopina

The use of the drug may lead to the development of the following side effects:

• manifestations from the cardiovascular system: peripheral edema (on the feet and ankles) and palpitations often occur. Orthostatic collapse, vasculitis and excessive decrease in blood pressure are less common. Heart failure occasionally develops and worsens. Heart rhythm disorders (including ventricular tachycardia, atrial fibrillation and bradycardia), chest pain and myocardial infarction with migraine are observed sporadically;
• reactions from muscles and bones: in some cases, back pain and muscle cramps appear, myalgia or asthenia develops. Rarely, myasthenia occurs;
• disorders of the central and central nervous system: flushes of the face and a feeling of heat often occur, as well as increased fatigue, headaches, a feeling of drowsiness and dizziness. Less common are insomnia, a feeling of anxiety, malaise, nervousness and depression. In addition, asthenia, hyperhidrosis, paresthesia with hypesthesia, tremor, emotional lability and peripheral neuropathy develop. Strange dreams and fainting also occur. Apathy is occasionally observed, as well as a feeling of excitement and convulsions. Amnesia or ataxia develops isolated cases;
• digestive disorders: abdominal pain and nausea are often observed. Less common are bloating, constipation with vomiting, as well as diarrhea, dyspeptic symptoms, thirst and dry mouth. Increased appetite or gingival hyperplasia are occasionally observed. Pancreatitis with gastritis, jaundice (mainly cholestatic type), hyperbilirubinemia and hepatitis occur sporadically, and the activity of liver transaminases increases;
• reactions of the hematopoietic system: thrombocytopenia or leukopenia, as well as thrombocytopenic purpura, are observed sporadically;
• metabolic disorders: hyperglycemia appears occasionally;
• manifestations from the respiratory system: in some cases, a runny nose and dyspnea may be observed. Cough occurs sporadically;
• urinary dysfunction: sometimes there is increased frequency of urination or pain during this process, and in addition, impotence or nocturia develops. Polyuria or dysuria occurs sporadically;
• manifestations of allergy: in some cases, skin rashes and itching may occur. Urticaria, Quincke's edema, and erythema multiforme may appear occasionally;
• Others: ringing of the ears, eye pain, conjunctivitis, chills and nosebleeds may occur. In addition, alopecia, diplopia, gynecomastia and xerophthalmia develop. Accommodation, vision or taste bud disorders also occur, and weight loss or gain is observed. Dermatitis occasionally occurs. Skin pigmentation disorders and xeroderma with parosmia, as well as cold sweat attacks, are observed sporadically.

Overdose

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

To eliminate disorders, activated carbon is prescribed (especially during the first 2 hours after poisoning), and then gastric lavage (sometimes). Also, the victim should be placed so that his limbs are elevated, and the work of the cardiovascular system should be constantly maintained, pulmonary and cardiac functions should be monitored, as well as diuresis and BCC.

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

Interactions with other drugs

In case of combined use of the drug with cimetidine, no changes in the pharmacokinetic parameters of amlodipine are observed.

The simultaneous use of Vaskopin 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 the antihypertensive and antianginal properties of Ca channel blockers may be observed. Their antihypertensive effect may also be enhanced when combined with neuroleptics and α-adrenoblockers.

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

A single dose of magnesium- or aluminum-containing antacid drugs has little effect on the pharmacokinetic properties of the substance amlodipine.

A single dose of 100 mg of sildenafil in patients with essential hypertension does not cause changes in the pharmacokinetic parameters of amlodipine. Repeated administration of 10 mg of the drug in combination with 80 mg of atorvastatin does not cause significant changes in the pharmacokinetics of the latter.

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

Single and repeated use of Vaskopin at a dosage of 10 mg does not significantly affect the pharmacokinetic properties of ethyl alcohol.

Amlodipine does not affect the changes in PT values caused by warfarin.

The pharmacokinetics of the drug cyclosporine are little changed by amlodipine.

The combination of a single dose of grapefruit juice (240 ml) with Vaskopin (10 mg) does not have a significant effect on the pharmacokinetics of the latter.

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Storage conditions

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

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Shelf life

Vaskopin can be used for a period of 4 years from the date of release of the drug.