Amlodipine-ALSI, pills 5mg, 30pcs

Composition

One tablet contains:

as an active ingredient:

amlodipine bezylate — 6.9 mg, which corresponds to 5 mg of amlodipine;

excipients:  

lactose monohydrate-85.7 mg,

povidone-3.2 mg,

crospovidone-3.2 mg,

calcium stearate-1.0 mg

Pharmacological action

Dihydropyridine derivative-a blocker of” slow ” calcium channels (BMCC) 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 in vascular smooth muscle cells than in 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 total peripheral vascular resistance( OPSS), reduces preload on the heart, and reduces the need for myocardial oxygen.

Dilates 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 spasm (including caused by smoking). In patients with stable angina, a single daily dose increases exercise tolerance, slows down the development of angina and “ischemic” ST-segment depression, reduces the frequency of angina attacks and consumption of nitroglycerin and other nitrates.

It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to the direct vasodilating effect on vascular smooth muscles. In patients with arterial hypertension, a single dose provides a clinically significant reduction in blood pressure (BP) for 24 hours (in the patient’s “lying” and “standing” positions). Orthostatic hypotension with the appointment of amlodipine is quite rare. It does not cause a decrease in exercise tolerance, left ventricular ejection fraction.

Reduces the degree of left ventricular myocardial hypertrophy, has anti-atherosclerotic and cardioprotective effects in coronary heart disease (CHD). It does not affect the contractility and conduction of the myocardium, does not cause a reflex increase in heart rate (HR), 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 does not have any adverse effect on the metabolism and concentration of plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes mellitus and gout.

A significant decrease in blood pressure is observed after 6-10 hours, the duration of the effect is 24 hours. With long-term therapy, the maximum decrease in blood pressure occurs 6-12 hours after oral use of amlodipine. If amlodipine is discontinued after prolonged treatment, an effective reduction in blood pressure is maintained for 48 hours after the last dose. Then the blood pressure values gradually return to the initial level within 5-6 days.

Indications

• Arterial hypertension (monotherapy or in combination with other antihypertensive agents).
• Stable exertional angina and vasospastic angina (Prinzmetal angina) (monotherapy or in combination with other antihypertensive agents).

Recommendations for use

Inside, the initial dose for the treatment of arterial hypertension and angina pectoris is 5 mg of the drug once a day. The maximum daily dose is 10 mg once.

With arterial hypertension, the maintenance dose may be 2.5-5 mg (1/2 tablet of 5 mg – 1 tablet of 5 mg) per 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.

Patients with impaired liver function as a hypotensive agent, Amlodipine is prescribed with caution, at an initial dose of 2.5 mg (1/2 tablet of 5 mg), as an antianginal agent-5 mg.

In elderly patients, T_{1/2 may increase}Amlodipine and decrease creatinine clearance (CC). No dose changes are required, but patients should be monitored more closely.

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.

Contraindications

• Hypersensitivity to amlodipine, a derivative of dihydropyridine and other components of the drug;
• severe hypotension (systolic BP less than 90 mm Hg. St. )
• collapse, cardiogenic shock,
• unstable angina (with the exception of prinzmetals angina);
• clinically significant aortic stenosis;
• pregnancy and lactation;
• age to 18 years (effectiveness and safety have not been studied);
• lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Use with caution in: hepatic impairment, sinus node weakness syndrome (SSSS) (severe bradycardia, tachycardia), chronic heart failure of non-ischemic etiology of NYHA functional class III-IV, arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy (HOCMP), acute myocardial infarction (and within 1 month after myocardial infarction), in old age.

Side effects

World Health Organization (WHO)classification of the incidence of side effects:

very often >1/10>

often from > 1/100 to >< 1/10

sometimes from > 1/1000 to >< 1/100

rarely from >1/10000 to >< 1/1000

very rarely from

From the cardiovascular system: often-palpitations, peripheral edema (swelling of the ankles and feet), “flushes” of blood to the skin of the face; sometimes-excessive decrease in blood pressure; very rarely-syncope, shortness of breath, vasculitis, orthostatic hypotension, development or aggravation of heart failure, cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, chest pain.

From the central and peripheral nervous system: often-headache, dizziness, increased fatigue, drowsiness; sometimes-asthenia, general malaise, hypesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, mood lability, unusual dreams, nervousness, depression, anxiety, very rarely – migraine, increased sweating, apathy.

From the digestive system: often-nausea, abdominal pain; sometimes-vomiting, constipation or diarrhea, flatulence, dyspepsia, anorexia, dry mouth, thirst; rarely-gum hyperplasia, increased appetite; very rarely-pancreatitis, gastritis, jaundice (due to cholestasis), hyperbilirubinemia, increased activity of “liver” transaminases, hepatitis.

From the side of hematopoietic organs:  very rarely – thrombocytopenic purpura, leukopenia, thrombocytopenia.

From the genitourinary system: sometimes-frequent urination, painful urination, nocturia, impotence, very rarely-dysuria, polyuria, gynecomastia.

Respiratory system disorders:  sometimes – shortness of breath, rhinitis, very rarely-cough.

From the skin: rarely-dermatitis, very rarely-alopecia, xeroderma, “cold” sweat, skin pigmentation disorder.

Allergic reactions: pruritus of the skin, rash (including erythematous, maculopapular rash, urticaria), angioedema, erythema multiforme.

From the musculoskeletal system:  sometimes-muscle cramps, myalgia, arthralgia, back pain, osteoarthritis, rarely-myasthenia gravis.

Other services:  sometimes-tinnitus, diplopia, accommodation disorders, xerophthalmia, conjunctivitis, eye pain, chills, nosebleeds, very rarely-parosmia, hyperglycemia.

Interaction

Amlodipine can be safely used for the treatment of hypertension together with thiazide diuretics, alpha-blockers, beta-blockers or ACE inhibitors. In patients with stable angina, the drug can be combined with other antianginal agents, for example, with prolonged-acting nitrates, beta-blockers or short-acting nitrates.

Amlodipine can be used concomitantly with nonsteroidal anti-inflammatory drugs (NSAIDs) (especially indomethacin), antibacterial agents and hypoglycemic agents for oral use.

It is possible to enhance the antianginal and hypotensive effects of BMCC when combined with thiazide and loop diuretics, verapamil, ACE inhibitors, beta-blockers and nitrates, as well as to enhance their hypotensive effect when combined with alpha-1-blockers, neuroleptics.

Although no negative inotropic effects have usually been observed in studies of amlodipine, however, some BMCs may increase the severity of the negative inotropic effects of antiarrhythmic agents that cause prolongation of the QT interval (for example, amiodarone and quinidine).

A single dose of 100 mg of sildenafil in patients with essential hypertension does not affect the pharmacokinetics of amlodipine.

Repeated use of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin.

Ethanol (beverages containing alcohol): amlodipine with a single and repeated use in a dose of 10 mg does not affect the pharmacokinetics of ethanol.

Antiviral agents (ritonavir) increases plasma concentrations of BMCC, including amlodipine.

Neuroleptics and isoflurane-increase the hypotensive effect of dihydropyridine derivatives.

Calcium supplements may reduce the effect of BMCC.

When amlodipine is co-administered with lithium preparations, it is possible to increase the manifestation of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

Amlodipine does not alter the pharmacokinetics of cyclosporine.

It does not affect the serum concentration of digoxin and its renal clearance.

It does not significantly affect the effect of warfarin (prothrombin time).

Cimetidine does not affect the pharmacokinetics of amlodipine.

In vitro studies, amlodipine did not affect the binding of digoxin, phenytoin, warfarin, and Indometacin to blood proteins.

Grapefruit juice: concomitant single oral use of 240 mg grapefruit juice and 10 mg amlodipine is not accompanied by a significant change in the pharmacokinetics of amlodipine.

Overdose

Symptoms: excessive peripheral vasodilation with a pronounced and possibly prolonged decrease in blood pressure, collapse, shock.

Treatment: gastric lavage, use of activated charcoal, maintenance of the cardiovascular system, monitoring of heart and lung function indicators, elevated, above head level, position of the lower extremities, control of the volume of circulating blood and diuresis. To restore vascular tone – the use of vasoconstrictors (in the absence of contraindications to their use); in order to eliminate the consequences of calcium channel blockade – intravenous use of calcium gluconate. Hemodialysis is ineffective.

Description

Tablets are white or white with a cream tint, flat-cylindrical with a risk and chamfer.

Functional features

After oral use, amlodipine is slowly absorbed from the gastrointestinal tract (GI). The average absolute bioavailability is 64%, the maximum concentration (Cmax) in the blood serum is observed after 6-9 hours. Steady-state serum concentrations (Sss) are reached after 7-8 days of therapy. Food intake 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 active metabolism in the liver in the absence of a significant “first pass” effect. 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 by the kidneys mainly in the form of metabolites,10% – unchanged, and 20-25% – through the intestines, as well as with 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 hours) compared to young patients, but this difference is not clinically significant. Prolongation of T_1/2 in patients with hepatic insufficiency suggests that with prolonged use, the accumulation of the drug in the body will be higher (T_1/2-up 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 treatment with Amlodipine, it is necessary to monitor body weight and sodium intake, and prescribe an appropriate diet. It is necessary to maintain dental hygiene and follow up with a dentist (to prevent soreness, bleeding and gum hyperplasia).

Patients with low body weight, short stature, and severe hepatic impairment may require a lower dose.

In elderly patients, T_1/2 and drug clearance may be prolonged. No dose changes are required for elderly patients; if the dose is increased, more careful monitoring of patients is necessary.

If liver function is impaired, the T_1/2 of the drug may also be prolonged. Therefore, Amlodipine should be administered with caution in such patients.

Despite the fact that discontinuation of Amlodipine is not accompanied by the development of a “withdrawal” syndrome, it is advisable to stop treatment by gradually reducing the dose of the drug.

The efficacy and safety of the drug in hypertensive crisis has not been established.

Influence on the ability to drive a car and other complex mechanisms: No effects of Amlodipine on driving or working with machinery have been reported. However, some patients may experience drowsiness and dizziness, especially at the beginning of treatment. If they occur, the patient should take special precautions when driving a car and working with complex mechanisms.

Storage conditions

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

Keep out of reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Amlodipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Angina, Hypertension