Amlo Sandoz®

General characteristics. Structure:

Active ingredient: amlodipine.
1 tablet contains an amlodipin of 5 mg or 10 mg in the form of an amlodipin бесилат;
excipients: starch sodium (type A), calcium hydra phosphate anhydrous, cellulose microcrystallic, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Amlodipin is the antagonist of calcium ions (a blocker of slow calcium channels) who blocks receipt of calcium ions through membranes in cells of unstriated muscles of a myocardium and vessels. The mechanism of hypotensive action of an amlodipin is caused by the direct running-down influence on unstriated muscles of vessels. The nature of anti-anginal effect of an amlodipin is studied not enough, however it is possible to claim that drug reduces the general ischemic frustration in such two ways:
- Expands peripheral arterioles and thus reduces OPSS (a loading post). As ChSS practically does not change, decrease in load of heart leads to decrease in consumption of energy and need of a myocardium for oxygen;
- To expansion of the main coronary arteries and coronary arterioles both in not changed, and in ischemic zones of a myocardium. Such dilatation increases intake of oxygen to a myocardium at patients with vasospastic stenocardia (Prinze's stenocardia of metal or alternative stenocardia) and prevents development of coronary vasoconstriction.
At patients with arterial hypertension the single dose of an amlodipin provides clinically significant decrease in the ABP for 24 h in situation both lying, and standing. Thanks to the slow beginning of action амлодипин does not cause acute hypotension.
At patients with stenocardia амлодипин promotes increase in physical effeciency (extends time of performance of an exercise stress, development of an attack of stenocardia and time of a depression of a segment of ST for 1 mm at loadings detains), reduces the frequency of attacks of stenocardia and the need for nitroglycerine reception.
Hemodynamic researches and controlled clinical tests at patients with heart failure of the II-III functional class (on NYHA classification) showed what амлодипин does not cause deterioration in their state by such criteria as tolerance to an exercise stress, fraction of emission of a left ventricle and clinical symptomatology.
Pharmacokinetics. After intake in therapeutic doses амлодипин it is well soaked up, reaching the maximum concentration in blood in 6 - 12 hours. Absolute bioavailability reaches 64 - 80%. The volume of distribution makes about 20 l/kg. About 97,5% of an amlodipin contact proteins of a blood plasma. Meal does not influence absorption of an amlodipin.
Plasma elimination half-life of blood makes about 35 - 50 hours that allows to appoint drug once a day. Resistant equilibrium concentration of an amlodipin in a blood plasma is reached in 7 - 8 days of regular use.
Amlodipin is extensively transformed in a liver with formation of inactive metabolites. It is removed with urine of 10% of a dose - in not changed look, 60% - in the form of metabolites.
At patients of advanced age and patients with congestive heart failure the tendency to decrease in clearance of an amlodipin is noted that "concentration time" (AUC) and a drug elimination half-life leads to increase in the area under a curve.

Indications to use:

Essential arterial hypertension. Chronic forms of coronary heart disease (stable stenocardia, vasospastic stenocardia, including Prinze's stenocardia of metal).

Route of administration and doses:

At arterial hypertension and stenocardia the initial dose of an amlodipin makes 5 mg a day. Depending on individual reaction of the patient the dose can be increased to the maximum, equal 10 mg. At coronary heart disease the recommended dose of an amlodipin makes 5 - 10 mg of 1 times a day.
Amlodipin it is possible to appoint as means of monotherapy or in combination with other anti-anginal drugs for patients with stenocardia.

Features of use:

Use for treatment of patients with heart failure. At use of an amlodipin for treatment of patients with heart failure of the 3-4th centuries. (On NYHA classification) growth of frequency of cases of edematization of lungs was noted.
Use for patients with an abnormal liver function.
The elimination half-life of an amlodipin, as well as other antagonists of calcium, increases at patients with an abnormal liver function, however any recommendations concerning correction of doses of drug are not developed yet. For this reason to use drug at such patients follows with care.
Use for treatment of patients with a renal failure.
амлодипин apply to treatment of such patients in usual doses. Changes of concentration of an amlodipin in plasma do not correlate with degree of a renal failure. Amlodipin is not brought at dialysis therefore patients who are on a hemodialysis should appoint it with care.

Use for elderly patients.
It is recommended to appoint drug in usual doses, at increase in a dose it is necessary to be careful.

Ability to influence speed of response at control of motor transport or work with other mechanisms.
Before clarification of individual reaction to drug it is recommended to be careful at control of motor transport or work with mechanisms.

Side effects:

From cardiovascular system: the hypostases of shins (which are not connected with a delay in a liquid organism have high-quality character and, as a rule, decrease / disappear after dose adjustment of an amlodipin), a cardiopalmus, a hyperemia of the person and other parts of a body, a headache, dizziness, arterial hypotension. As well as at reception of other antagonists of calcium, single by-effects which cannot be separated from effects of the natural course of a basic disease are described: a myocardial infarction, arrhythmia (including bradycardia, ventricular tachycardia and atrial fibrillation), and also pain behind a breast.
From a digestive tract and a liver: nausea, an abdominal pain, it is rare - dyspepsia, discomfort in epigastric area, appetite loss, change of flavoring feelings,  diarrhea, a meteorism, vomiting, dryness in a mouth, a hyperplasia of gums, is very rare - increase in level of hepatic transaminases, a cholestasia, an abnormal liver function.
From a nervous system and sense bodys: a headache, fatigue, a sleep disorder (drowsiness), it is rare - paresthesias, sleeplessness, a depression, a vision disorder (including diplopias), conjunctivitis, a ring in ears, it is very rare - a tremor, peripheral neuropathy.
From system of a hemopoiesis: very seldom - an agranulocytosis, in isolated cases - anemia, a leukopenia, thrombocytopenia.
From an urinary system: slight increase of a daily urine and frequency of an urination.
Skin: rash, allergic reactions (rash, an itch, an erythema), it is rare - system reactions, dermatitis, an alopecia, change of coloring of skin.
From a musculoskeletal system: adynamy, spasms, mialgiya, arthralgia.
Other reactions: the increased perspiration, a gynecomastia, erectile dysfunction, nonspecific pains of various localization, a hyperglycemia, it is very rare - cough.
After drug withdrawal side reactions in most cases completely disappeared.

Interaction with other medicines:

Amlodipin is safe at use with thiazide diuretics, α-adreno blockers β-adreno blockers, APF inhibitors, nitrates of the prolonged action, nitroglycerine for sublingual, with non-steroidal anti-inflammatory drugs, antibiotics and peroral hypoglycemic means.
Results of the researches in vitro with use of a blood plasma of the person demonstrate what амлодипин does not influence linkng with proteins of such drugs as digoxin, Phenytoinum, warfarin and indometacin.
Influence of drugs on pharmacokinetics of an amlodipin. Combined use of an amlodipin and Cimetidinum does not change pharmacokinetics of an amlodipin.
Simultaneous use of 240 ml of grapefruit juice with a single peroral dose of an amlodipin of 10 mg did not change pharmacokinetics of an amlodipin.
Combined use of aluminum / magnesian antacids with a single dose of an amlodipin did not influence pharmacokinetics of an amlodipin.
The dose of a sildenafil of 100 mg at patients with essential arterial hypertension did not influence pharmacokinetics of an amlodipin. At the combined use of an amlodipin and sildenafil each of drugs independently from each other showed hypotensive effect.
Influence of an amlodipin on pharmacokinetics of other drugs. Combined repeated use of 10 mg of an amlodipin and 80 mg of an atorvastatin did not influence equilibrium pharmacokinetic parameters of an atorvastatin.
Simultaneous use of an amlodipin and digoxin for healthy volunteers does not change the level of the last in blood serum and its renal clearance.
Single and reusable doses of an amlodipin of 10 mg did not change ethanol pharmacokinetics.
Amlodipin practically does not influence pharmacokinetics of cyclosporine and does not change influence of warfarin on prothrombin modern times.

Contraindications:

Hypersensitivity to drugs of a dihydropyridinic row, to an amlodipin or to any component of drug. An acute myocardial infarction (up to 4 weeks from the beginning of a disease), cardiogenic shock, unstable stenocardia, the expressed aortal stenosis, arterial hypotension (the ABP less than 90 mm of mercury.). Period of pregnancy and feeding by a breast. Age up to 18 years.

Overdose:

Symptoms. The considerable overdose (> 100 mg) can lead to an excessive peripheral vazodilatation and probable reflex tachycardia. Cases of essential and possibly long system hypotension, including shock are described.
Treatment. Use of absorbent carbon for healthy volunteers directly or in 2 hours after reception of 10 mg of an amlodipin significantly reduced drug absorption. In certain cases there can be useful a gastric lavage.
Clinically significant arterial hypotension caused by overdose of an amlodipin demands holding the active actions directed to maintenance of functions of cardiovascular system including monitoring of indicators of cardiac performance and lungs, sublime position of extremities, control of volume of the circulating blood, and a diuresis. For recovery of a tone of vessels and arterial pressure there can be useful a use of vasoconstrictive drug if there are no contraindications for its appointment. For the purpose of elimination of effects of blockade of calcium channels there can be useful an intravenous administration of a gluconate of calcium. As амлодипин substantially contacts proteins, efficiency of dialysis is improbable.

Use during pregnancy or feeding by a breast.
Degree of safety of use of an amlodipin for women during pregnancy and feeding by a breast is not established therefore it is not recommended to be applied during this period.

Children.
Do not apply.

Storage conditions:

Period of validity 3 years. To store at a temperature not above 25 °C in original packaging. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 5 mg, No. 30

Tablets of 10 mg, No. 30