Semlopin

General characteristics. Structure:

Active ingredient: S (-) amlodipine besylate; 1 tablet contains S (-) an amlodipina бесилат S (-) to an amlodipin of 2,5 mg or 5 mg is equivalent.

Excipients: cellulose microcrystallic, calcium hydrophosphate the dihydrate, iron oxide yellow (Е 172), silicon dioxide colloid anhydrous, sodium krokhmalglikolit, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Amlodipin is an antagonist of calcium ions (a blocker of slow calcium channels of cellular membranes) who blocks the movement of calcium ions in cells of unstriated muscles of a myocardium and vessels and, thus, provides direct influence on target cells. The Antianginalny effect of an amlodipin is reached, first, by expansion of peripheral arterioles thanks to what decrease in an afterload is reached. As heart rate at the same time practically does not change, decrease in an afterload on heart leads to reduction of an expenditure of energy and, respectively, oxygen requirement. Secondly, амлодипин directly expands coronary arteries both in intact, and in ischemic sites of a myocardium that increases access of oxygen to an ischemic myocardium at patients with vasospastic stenocardia (Printsmetal's stenocardia).
At patients with arterial hypertension single application of an amlodipin provides clinically meaning lowering of arterial pressure within 24 hours. Amlodipin acts gradually and, as a rule, does not render symptomatic hypotension. At patients with stenocardia single application of an amlodipin increases time of performance of an exercise stress, development of an attack of stenocardia and depression of a segment of ST during execution of an exercise stress detains, reduces the frequency of attacks of stenocardia and reduces need for nitroglycerine.
Amlodipin does not exert negative impact on a metabolism and lipidic composition of plasma, he can be applied at treatment of patients with a diabetes mellitus and gout.

Pharmacokinetics. After oral administration амлодипин it is quickly soaked up from the digestive channel and reaches the maximum concentration in plasma in 6–12 hours. Food does not influence absorption of an amlodipin. Bioavailability makes 64–80%. The volume of distribution makes about 21 l/kg. About 97,5% of an amlodipin contact proteins of plasma. Resistant equilibrium concentration in plasma is reached in 7–8 days of regular use. Amlodipin is transformed in a liver with formation of inactive metabolites, at the same time 10% of not changed substance and 60% of metabolites are removed with urine. The elimination half-life makes about 35-50 hours that allows to use drug of 1 times a day.

Indications to use:

Arterial hypertension (in the form of monotherapy or as a part of a combination therapy).
Coronary heart disease (stable stenocardia and vasospastic stenocardia (Printsmetal's stenocardia). Drug can be used as means of monotherapy and in a combination with other anti-anginal means.

Route of administration and doses:

The initial dose of drug Semlopin makes 5 mg of 1 times a day. Depending on clinical effect the dose can be increased to maximum – 10 mg of 1 times a day.
There is no need to reduce a dose for patients with a renal failure.
The recommended dose for patients of advanced age makes 5 mg of 1 times a day.
For patients of advanced age the initial dose makes 2,5 mg a day.
During treatment by drug it is necessary to control the level of arterial pressure daily.

Features of use:

It is necessary to use with care drug the patient with an abnormal liver function as the elimination half-life of an amlodipin at such patients increases. There is no need to change dosing at patients with a renal failure, change of concentration of an amlodipin in plasma does not correlate with degree of a renal failure. Amlodipin is not brought at a hemodialysis.

Ability to influence speed of response at control of motor transport or work with other mechanisms. Influence of an amlodipin on ability to manage motor transport and it is improbable to work with dangerous mechanisms. Nevertheless, when developing dizziness and drowsiness during use of drug it is necessary to refrain from management of transport and work with difficult mechanisms.

Use during pregnancy or feeding by a breast. Amlodipin do not apply during pregnancy, except cases of vital indications.
Drug is not used during feeding by a breast.

Children. Safety of use of an amlodipin for children is not proved. Drug is contraindicated for use for persons age up to 18 years.

Side effects:

Majority of side reactions weak or moderate. The headache, hypostases, drowsiness, nausea, a stomach ache, inflows, a heart consciousness and dizziness are most often observed. Hypostases, inflows, a heart consciousness and drowsiness most often occur at women.
- From cardiovascular system: arrhythmia (including ventricular tachycardia and atrial fibrillation), a myocardial infarction, bradycardia, a stethalgia, arterial hypotension, peripheral ischemia, a loss of consciousness, tachycardia, dizziness, postural hypotension, a vasculitis.
- From the central and peripheral system: giposteziya, peripheral neuropathy, paresthesia, tremor, dizziness.
- From the autonomic nervous system: dryness in a mouth, perspiration.
- From digestive tract: anorexia, lock, dyspepsia, dysphagy, diarrhea, meteorism, pancreatitis, vomiting, hyperplasia of gums, change of flavoring feelings.
- From a musculoskeletal system: arthralgia, arthrosis, muscular spasms, myalgia.
- Mental disturbances: sleeplessness, nervousness, depression, sleep disorder, depersonalization, alarming states, change of mood.
- From respiratory system: short wind, nasal bleeding, cough, rhinitis.
- From skin: Quincke's disease, multiformny erythema, rash, itch, erimatozny rash, makulopapulyarny rash, alopecia, skin discoloration.
- From sense bodys: vision disorder, conjunctivitis, diplopia, eye pain, sonitus.
- From kidneys and secretory system: frequent urination, urination disturbance, nocturia.
- Metabolic disturbances: hyperglycemia, thirst.
- From system of a hemopoiesis: leukopenia, purpura, thrombocytopenia.
- From an organism in general: allergic reactions, adynamy, dorsodynia, indisposition, pain, muscle tension, increase or degrowth of a body.
- Disturbances of reproductive system and mammary glands: impotence, gynecomastia.
- It was reported also about cases of jaundice and increase in levels of liver enzymes.
 

Interaction with other medicines:

Semlopin can be applied along with thiazide diuretics, blockers of β-adrenoceptors, nitrates of the prolonged action, sublingual nitroglycerine, non-steroidal anti-inflammatory drugs, antibiotics and peroral glucose-lowering drugs.
Amlodipin does not change concentration of digoxin in plasma and its renal clearance.
Simultaneous use of an amlodipin with Cimetidinum does not change pharmacokinetics of an amlodipin.
Simultaneous use of an amlodipin with warfarin does not change influence of warfarin on a prothrombin time.
Juice of grapefruit can increase concentration of an amlodipin in blood, nevertheless, this phenomenon is not followed by clinically meaning lowering of arterial pressure. Amlodipin does not change concentration of digoxin in plasma and its renal clearance.
Simultaneous use of an amlodipin with Cimetidinum does not change pharmacokinetics of an amlodipin.
Simultaneous use of an amlodipin with warfarin does not change influence of warfarin on a prothrombin time.
Juice of grapefruit can increase concentration of an amlodipin in blood, nevertheless, this phenomenon is not followed by clinically meaning lowering of arterial pressure.

Contraindications:

Hypersensitivity to an amlodipin and other components of drug or to other dihydropyridines. Heavy arterial hypotension, klinichno significant aortal stenosis. Period of pregnancy and feeding by a breast. Children's age up to 18 years.

Overdose:

At overdose development of an excessive peripheral vazodilatation with a lowering of arterial pressure and reflex tachycardia is possible. In case of clinically meaning arterial hypotension it is necessary to carry out the measures directed to support of function of cardiovascular system, including monitoring of function of heart and lungs, control of a diuresis and volume of the circulating blood.
Absorbent carbon (especially in the first 2 hours after overdose), a gastric lavage, infusional therapy by saline solutions is appointed; if at the same time arterial hypotension is not eliminated, vazopressor are appointed (in the absence of contraindications for their appointment). For elimination of excessive blockade of calcium channels intravenous administration of calcium of a gluconate is shown.
As амлодипин considerably contacts proteins of plasma, the hemodialysis is not effective.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 14 tablets in blisters; on 2 blisters in cardboard packaging.