Amlodipin Sandoz of 5 mg

General characteristics. Structure:

Active ingredients: Amlodipina безилат 6.934 mg. What corresponds to the maintenance of an amlodipin of 5 mg.

Excipients
Lactose anhydrous, cellulose microcrystallic, starch corn (dry), talc, silicon dioxide colloid anhydrous, magnesium stearate.

Pharmacological properties:

Blocker of slow calcium channels, derivative dihydropyridine. Has anti-hypertensive and anti-anginal effect. Contacting dihydropyridinic receptors, blocks calcium channels, reduces transmembrane transition of calcium ions to a cell (more in smooth muscle cells of vessels, than in cardiomyocytes).

Anti-anginal action is caused by expansion of coronary and peripheral arteries and arterioles: at stenocardia reduces expressiveness of ischemia of a myocardium; expanding peripheral arterioles, reduces OPSS, reduces preload of heart, reduces the need of a myocardium for oxygen . Expanding the main coronary arteries and arterioles in not changed and ischemic zones of a myocardium, increases intake of oxygen in a myocardium (especially at vasospastic stenocardia); prevents development of a konstriktion of coronary arteries (including caused by smoking). At patients with stenocardia the single daily dose increases time of performance of an exercise stress, slows down development of stenocardia and ischemic depression of a segment of ST, reduces the frequency of attacks of stenocardia and consumption of nitroglycerine .

Renders long-term dozozavisimy hypotensive effect. Hypotensive action is caused by direct vazodilatiruyushchy impact on unstriated muscles of vessels. At arterial hypertension the single dose provides clinically significant decrease in the ABP for 24 h (in position of the patient lying and standing). Does not cause sharp decrease in the ABP, decrease in tolerance to an exercise stress, fraction of emission of a left ventricle. Reduces degree of a hypertrophy of a myocardium of a left ventricle, has anti-atherosclerotic and cardiotyre-tread effect at an ischemic heart disease. Does not exert impact on contractility and conductivity of a myocardium, does not cause reflex increase in ChSS, slows down aggregation of thrombocytes , raises a glomerular filtration rate , possesses a weak natriuretic effect.

At a diabetic nephropathy does not increase expressiveness of a microalbuminuria. Does not exert adverse impact on a metabolism and lipids of a blood plasma .

Time of approach of effect - 2-4 h, duration of effect is 24 h.

Pharmacokinetics. Absorption
After intake амлодипин it is slowly absorbed from a GIT. Average absolute bioavailability makes 64%, C max in a blood plasma is observed through 6-9 p. C ss reached after 7 days of therapy. Meal does not influence absorption of an amlodipin.
 
Distribution
Average  makes V d 21 l/kg of body weight that indicates that the most part of drug is in fabrics, and rather smaller - in blood. The most part of the drug which is in blood (95%) contacts proteins of a blood plasma.

Gets through GEB.
 
Metabolism
Amlodipin is exposed to slow, but extensive metabolism (90%) in a liver with formation of inactive metabolites. Has effect of "the first passing" through a liver. Metabolites have no significant pharmacological activity.
 
Removal
After a single dose in T 1/2 varies from 31 to 48 h, at repeated purpose of T 1/2 makes about 45 h. About 60% of the dose accepted inside are removed with urine preferential in the form of metabolites, 10% - in not changed look, and 20-25% - with a stake, and also with breast milk. The general clearance of an amlodipin makes 0.116 ml / with/kg (7 ml/min., 0.42 l/h/kg).
 
Pharmacokinetics in special clinical cases
At patients of advanced age (65 years are more senior) removal of an amlodipin is slowed down (T 1/2 are 65 h) in comparison with young patients, however this difference has no clinical value.

At patients with a liver failure lengthening of T 1/2 is supposed , and at long appointment cumulation of drug in an organism will be higher (The t 1/2 increases up to 60 h).

The renal failure has no significant effect on kinetics of an amlodipin.

At a hemodialysis is not removed.

Indications to use:

- Arterial hypertension.
- Stable angina of exertion.
- Vasospastic stenocardia (Printsmetal's stenocardia).

Route of administration and doses:

Inside, irrespective of meal.
For treatment of arterial hypertension and prevention of attacks of an angina of exertion and vasospastic stenocardia 
The initial daily dose of Amlodipin makes 5 mg in 1 reception.

If necessary the dose can be increased to maximum - 10 mg/days once.
 
To patients with insignificant body weight or low growth, and also with the expressed liver failure
Smaller doses can be required.
 
To patients with a renal failure and to patients of advanced age 
Dose adjustment is not required.

Change of a dose at co-administration with thiazide diuretics is not required, to beta adrenoblockers and APF inhibitors.

Features of use:

It is optimum to use drug every day at the same time.

Despite the absence of at blockers of slow calcium channels of a withdrawal, before the termination of treatment gradual reduction of a dose is recommended.

Amlodipin it is possible to appoint in a combination with thiazide diuretics, alpha and beta adrenoblockers, APF inhibitors, nitrates of the prolonged action, sublingual nitroglycerine , NPVS, antibiotics, peroral hypoglycemic means.

Amlodipin does not exert adverse impact on a metabolism and lipids of a blood plasma therefore drug can be used at patients with bronchial asthma, a diabetes mellitus and gout.
Influence on ability to driving of motor transport and to control of mechanisms
Use of an amlodipin does not exert impact on ability to control of motor transport or other technical means, however because of possible excessive decrease in the ABP, delay of speed of response owing to development of dizziness, a headache, increased fatigue, etc. of side effects, it is necessary to show consideration for individual effect of drug at the beginning of a course of treatment and at change of the mode of dosing.

Side effects:

Classification of side effects at use of drug on occurrence frequency:
- Often (more than 1%).
- Seldom (from 0.1% to 1%).
- Very seldom (less than 0.01%).

From TsNS and peripheral nervous system
Often - a headache, dizziness, fatigue, drowsiness, lability of mood.

Seldom - an adynamy, faints, spasms, a peripheral neuropathy, the increased sweating, sleeplessness, a depression.

Very seldom - apathy, an ataxy, migraine.
 
From cardiovascular system
Often - heartbeat, an asthma, "inflows" of blood to the person, peripheral hypostases.

Seldom - thorax pains, excessive decrease in the ABP, orthostatic hypotension.

Very seldom - disturbances of a cordial rhythm (ventricular tachycardia , fibrillation of auricles ), a myocardial infarction, aggravation of heart failure.
 
From the alimentary system
Often - nausea, dryness in a mouth, an abdominal pain.

Seldom - dyspepsia, a lock, diarrhea, a hyperplasia of gums, pancreatitis.

Very seldom - gastritis, jaundice , increase in activity of hepatic transaminases.
 
From an urinary system
Seldom - a pollakiuria.
 
From a reproductive system
Seldom - disturbance of sexual function, a gynecomastia.
 
From a musculoskeletal system
Often - dorsodynias.

Seldom - a mialgiya, an arthralgia, muscular spasms.
 
Allergic reactions
Seldom - a skin itch, rash.

Very seldom - a mnogoformny erythema, a Quincke's disease.
 
Others
Seldom - a vision disorder, диспноэ, an alopecia.

Very seldom - a hyperglycemia, thrombocytopenia.

Interaction with other medicines:

Inhibitors of a microsomal oxidation can increase concentration of an amlodipin in plasma, strengthening risk of development of side effects, and inductors of microsomal enzymes of a liver - to reduce.

Unlike other blockers of slow calcium channels, clinically significant interaction with NPVS, especially with indometacin is not noted.

Thiazide and "loopback" diuretics, beta adrenoblockers, verapamil , APF inhibitors and nitrates strengthen anti-anginal or hypotensive effects.

Does not exert impact on pharmacokinetic parameters of digoxin and warfarin.

Cimetidinum does not influence pharmacokinetics of an amlodipin.

Drugs of calcium can reduce effect of blockers of slow calcium channels.

Antiviral means (ритонавир) increase plasma concentration of blockers of slow calcium channels.

Neuroleptics and изофлуран - strengthening of hypotensive action of derivatives of dihydropyridine.

Contraindications:

- The expressed arterial hypotension.
- Collapse.
- Cardiogenic shock.
- Unstable stenocardia (except for Printsmetal's stenocardia).
- Age up to 18 years (efficiency and safety are not established).
- A hereditary lactose intolerance , a galactosemia (lactose is a part of drug).
- Hypersensitivity to drug components.
- Hypersensitivity to other derivatives of dihydropyridine.

With care:
- Liver failure .
- Slight or moderate arterial hypotension.
- An acute myocardial infarction and within the first month after it.
- Stenosis of the mouth of an aorta.
- Chronic heart failure in a decompensation stage.
- SSSU.
- Hypertrophic subaortic stenosis.
- Advanced age.

Use at pregnancy and feeding by a breast

Safety of use at pregnancy and in the period of a lactation is not established therefore purpose of drug is possible only if the estimated advantage for mother exceeds potential risk for a fruit.

At purpose of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Overdose:

Symptoms: an excessive peripheral vazodilatation with clinically expressed decrease in the ABP with possible development of reflex tachycardia .
Treatment: purpose of absorbent carbon (in the first 2 h after overdose), a gastric lavage, sublime position of extremities, control of functions of warmly vascular and respiratory systems, OTsK and a diuresis, active maintenance of functions of cardiovascular system, is possible purpose of vasoconstrictive drugs for the purpose of recovery of a vascular tone and increase in the ABP, for elimination of effects of blockade of calcium channels - in/in introduction of a gluconate of Calcium . The hemodialysis is inefficient.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. Period of validity: 2 years. To store in places unavailable to children. Not to use after expiry date.

Issue conditions:

According to the recipe

Packaging:

In the blister of 10 tablets. In packaging 3 blisters.