Amlotop, pills 5mg 30pcs

Composition

1 tablet contains:

Active ingredient:  

Amlodipine bezylate 6.93 mg (based on amlodipine 5 mg).

Auxiliary substances:  

Lactose monohydrate — 77.67 mg;

MCC — 11.6 mg;

Calcium stearate-1 mg;

Croscarmellose sodium (primellose) – 1.8 mg;

Colloidal silicon dioxide (aerosil) — 1 mg

Pharmacological action

A derivative of dihydropyridine-BCC of the second generation, has an antianginal and antihypertensive effect.

Binding to dihydropyridine receptors, it blocks calcium channels, reduces the transmembrane transfer of calcium ions into the cell (to a greater extent — into vascular smooth muscle cells than into cardiomyocytes).

The antianginal effect is caused by the expansion of coronary and peripheral arteries and arterioles: in angina pectoris, it reduces the severity of myocardial ischemia; by expanding peripheral arterioles, it reduces OPSS, reduces preload on the heart, and reduces the need for oxygen in the myocardium.

Dilating the main coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, increases oxygen supply to the myocardium (especially in vasospastic angina); prevents the development of coronary artery constriction (including caused by smoking).

In patients with angina pectoris, a single daily dose increases exercise time, slows down the development of angina pectoris and “ischemic” ST-segment depression, reduces the frequency of angina attacks and nitroglycerin consumption.

It has a long-term dose-dependent hypotensive effect.

The hypotensive effect is due to the direct vasodilating effect on vascular smooth muscles.

In arterial hypertension, a single dose provides a clinically significant reduction in blood pressure for 24 hours (in the patient’s “lying” and “standing” positions).

It does not cause a sharp decrease in blood pressure, reduced exercise tolerance, or left ventricular ejection fraction.

Reduces the degree of left ventricular myocardial hypertrophy, has anti-atherosclerotic and cardioprotective effects in CHD.

It does not affect the contractility and conduction of the myocardium, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases the glomerular filtration rate, and has a weak natriuretic effect.

In diabetic nephropathy, it does not increase the severity of microalbuminuria.

It has no adverse effects on the metabolism and blood plasma lipids.

The time of onset of the effect is 2-4 hours, the duration of the effect is 24 hours.

Indications

• Arterial hypertension (monotherapy or in combination with other antihypertensive agents).
• Tension angina, vasospastic angina (Prinzmetal angina).

Use during pregnancy and lactation

Contraindicated during pregnancy and lactation.

Contraindications

• Hypersensitivity to amlodipine and other dihydropyridine derivatives;
• severe hypotension;
• collapse, cardiogenic shock;
• pregnancy and lactation;
• age up to 18 years (efficacy and safety have not been established).

With caution: impaired liver function, sinus node weakness syndrome (severe bradycardia, tachycardia), decompensated chronic heart failure, mild or moderate arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after), diabetes mellitus, lipid profile disorders, elderly age.

Side effects

From the cardiovascular system:  palpitations, shortness of breath, marked decrease in blood pressure, fainting, vasculitis, edema (swelling of the ankles and feet), flushing of blood to the face, rarely — rhythm disorders (bradycardia, ventricular

tachycardia, atrial flutter), chest pain, orthostatic hypotension, very rarely — development or aggravation of heart failure, extrasystole, migraine.

From the central nervous system:  

headache, dizziness, fatigue, drowsiness, mood swings, seizures, rarely-loss of consciousness, hypesthesia, nervousness, paresthesia, tremor, vertigo, asthenia, malaise, insomnia, depression, unusual dreams, very rarely-ataxia, apathy, agitation, amnesia.

From the digestive system:  

nausea, vomiting, epigastric pain, rarely-increased levels of hepatic transaminases and jaundice (due to cholestasis), pancreatitis, dry mouth, flatulence, gum hyperplasia, constipation or diarrhea, very rarely — gastritis, increased appetite.

From the genitourinary system:  

rarely-pollakiuria, painful urination, nocturia, sexual dysfunction (including decreased potency); very rarely — dysuria, polyuria.

From the side of the skin:  

very rarely — xeroderma, alopecia, dermatitis, purpura, skin discoloration.

Allergic reactions:  

skin pruritus, rash (including erythematous, maculopapular rash, urticaria), angioedema.

From the musculoskeletal system:  

rarely-arthralgia, arthrosis, myalgia (with prolonged use); very rarely-myasthenia gravis.

Other services:  

rarely — gynecomastia, uricemia, increase/decrease of body weight, thrombocytopenia, leukopenia, hyperglycemia, blurred vision, double vision, conjunctivitis, eye pain, tinnitus, back pain, dyspnea, epistaxis, increased sweating, thirst;

very rarely — a cold clammy sweat, cough, rhinitis, parosmia, a violation of taste sensations, disturbance of accommodation, xerophthalmia.

Interaction

Inhibitors of microsomal oxidation increase the concentration of amlodipine in blood plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes reduce. The antihypertensive effect is weakened by nonsteroidal anti-inflammatory drugs, especially indomstacin (sodium retention and blockade of prostaglandin synthesis by the kidneys), alpha-adrenostimulants, estrogens (sodium retention), sympathomimetics. Thiazide and loop diuretics, beta-blockers, verapamil, ACE inhibitors, and nitrates enhance the antianginal and hypotensive effects. Amiodarone, quinidine, alpha-1-adrenoblockers, antipsychotic drugs (neuroleptics), and slow calcium channel blockers may enhance the antihypertensive effect. It does not affect the pharmacokinetic parameters of digoxin and warfarin. Cimetidine does not affect the pharmacokinetics of amlodipine. When combined with lithium preparations, it is possible to increase the manifestations of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Calcium supplements can reduce the effect of slow-acting calcium channel blockers. Procainamide, quinidine, and other drugs that cause prolongation of the QT interval increase the negative inotropic effect and may increase the risk of significant prolongation of the QT interval. Grapefruit juice may reduce the concentration of amlodipine in the blood plasma, but this decrease is so small that it does not significantly change the effect of amlodipine.

How to take, course of use and dosage

Inside, the initial dose for the treatment of arterial hypertension and angina pectoris is 5 mg of the drug 1 time per day. The maximum dose can be increased to 10 mg once a day. In patients with arterial hypertension, the maintenance dose may be 2.5-5 mg / day. For angina pectoris of tension and vasospastic angina pectoris — 5-10 mg per day, once. For the prevention of angina attacks — 10 mg / day. Thin patients, short patients, elderly patients, patients with impaired liver function as a hypotensive agent, amlodipine is prescribed at an initial dose of 2.5 mg, as an antianginal agent-5 mg. No dose adjustment is required when co-administered with thiazide diuretics, beta-blockers, and angiotensin converting enzyme (ACE) inhibitors. No dose adjustment is required in patients with renal insufficiency.

Overdose

Symptoms: marked decrease in blood pressure, tachycardia, excessive peripheral vasodilation. Treatment: gastric lavage, use of activated charcoal, maintenance of the cardiovascular system, monitoring of heart and lung function, elevated position of the extremities, monitoring of the volume of circulating blood and diuresis. To restore vascular tone – the use of vasoconstrictor drugs (in the absence of contraindications to their use); to eliminate the consequences of calcium channel blockade – intravenous use of calcium gluconate. Hemodialysis is not effective.

Purpose

Antihypertensive agents

Description

Tablets of white or almost white color are flat-cylindrical in shape with a chamfer and with a risk.

Functional features

After oral use, amlodipine is slowly absorbed from the gastrointestinal tract. The average absolute bioavailability is 64%, the maximum concentration in the blood serum is observed after 6-9 hours. The concentration of stable equilibrium is reached after 7 days of therapy. Food does not affect the absorption of amlodipine. The average volume of distribution is 21 l / kg of body weight, which indicates that most of the drug is in the tissues, and relatively less in the blood. Most of the drug in the blood (95%) binds to plasma proteins. Amlodipine undergoes slow but extensive metabolism (90%) in the liver with the formation of inactive metabolites, has a “first pass” effect through the liver. The metabolites do not have significant pharmacological activity.After a single oral dose, the half-life (T 1/2) varies from 31 to 48 hours, with repeated use of T 1/2 is approximately 45 hours. About 60% of the oral dose is excreted in the urine mainly in the form of metabolites,10% in unchanged form, and 20-25% in feces, as well as in breast milk. The total clearance of amlodipine is 0.116 ml / s / kg (7 ml / min / kg,0.42 l / h / kg). In elderly patients (over 65 years of age), the elimination of amlodipine is slowed (T 1/2 65 h) compared to young patients, but this difference is not clinically significant. In patients with hepatic insufficiency, T1/2 is expected to be prolonged, and with prolonged use, the accumulation of the drug in the body will be higher (T 1/2 to 60 hours). Renal failure does not significantly affect the kinetics of amlodipine. The drug penetrates the blood-brain barrier. It is not removed during hemodialysis.

Special instructions

During the treatment period, it is necessary to monitor body weight and sodium intake, prescribe an appropriate diet. It is necessary to maintain dental hygiene and frequent visits to the dentist (to prevent soreness, bleeding and gum hyperplasia). The dosage regimen for the elderly is the same as for patients of other age groups. When increasing the dose, careful monitoring of elderly patients is necessary. Despite the absence of a “slow” calcium channel blocker withdrawal syndrome, a gradual dose reduction is recommended before discontinuing treatment. Amlodipine does not affect plasma concentrations of K+, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and uric acid nitrogen. Effects on driving ability and mechanismamines There have been reports of effects of amlodipine on driving or working with mechanisms. However, some patients may experience drowsiness and dizziness primarily at the beginning of treatment. If they occur, the patient should take special precautions when driving a car and working with mechanisms.

Form of production

Tablets of 5 mg and 10 mg. 10 or 30 tablets in a contour cell pack made of PVC film and aluminum foil. 2 or 3 contour cell packs of 10 tablets or 1 contour cell pack of 30 tablets together with the instructions for use in a cardboard pack.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf

life is 3 years. Do not use later than the date indicated on the package.

Active ingredient

Amlodipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Angina, Hypertension