Antisthene - instructions for use, dose, side effects, contraindications

Excipients (core): lactose monohydrate (sugar milk) - 49.30 mg, mannitol - 10.70 mg, corn starch - 10.70 mg, povidone (polyvinylpyrrolidone) - 2.30 mg, silicon dioxide colloid -1.10 mg, magnesium stearate - 0 , 90 mg.

Excipients (shell): hypromellose - 2.40 mg, titanium dioxide - 0.70 mg, polysorbate - 80 - 0.70 mg, castor oil ordinary oil seeds (oil castor) 0.17 mg, macrogol 4000 - 0.40 mg, dye azorubin - 0.08 mg, tropeolin-O - 0.05 mg, talc 0.50 mg.

Description:Tablets are round, biconvex, covered with a film coat from red to dark red. On the cross-section, two layers are visible, the inner layer is white or white with a yellowish tinge.

Pharmacotherapeutic group:Antihypoxic agent

ATX: & nbsp

C.01.E.B Other drugs for the treatment of heart disease

C.01.E.B.15 Trimetazidine

Pharmacodynamics:

Has antihypoxic effect.

By directly affecting cardiomyocytes and neurons of the brain, the drug optimizes their metabolism and function. The cytoprotective effect is due to an increase in the energy potential, activation of oxidative decarboxylation and rationalization of oxygen consumption (enhancement of glycolysis and fat oxidation blockade).

Trimetazidine supports myocardial contractility, prevents a decrease in the intracellular content of adenosine triphosphate (ATP) and phosphocreatine.

AT conditions of acidosis normalizes the functioning of ion channels of membranes, prevents the accumulation of calcium and sodium ions in cardiomyocytes, normalizes the intracellularThe exact content of potassium ions.

Reduces intracellular acidosis and increased phosphate content, caused by myocardial ischemia and reperfusion. Prevents damage the action of free radicals, preserves the integrity of cell membranes, prevents the activation of neutrophils in the ischemia zone, increases the duration electric potential, reduces the yield of creatine phosphokinase (CK) from cells and severity of ischemic myocardial damage.

Trimetazidine reduces the incidence of angina attacks, reduces the need for nitrates, after 2 weeks of use increases exercise tolerance, and sharp fluctuations in blood pressure (BP) decrease. Reduces dizziness and noise in the ears of ischemic etiology. In vascular pathology, the eye restores the functional activity of the retina.

Pharmacokinetics:

After taking the drug inside trimetazidine quickly and almost completely absorbed in the gastrointestinal tract. Bioavailability is 90%.Eating does not affect the bioavailability of the drug. The maximum concentration (Cmax) (after a single oral intake of 60 mg of trimetazidine) was 99 ng / ml. Time to reach the maximum concentration (TCmah) in blood plasma - 2 hours. The volume of distribution is 5.6 l / kg. Connection with blood plasma proteins - 16%. Trimetazidine is excreted from the body mainly by the kidneys (about 60% - unchanged). The half-life (T1 / 2) in young healthy volunteers is about 4 hours. Kidney clearance trimetazidine directly correlates with the clearance of creatinine (CC), the hepatic clearance decreases with age. Easily penetrates through the histohematological barriers.

Indications:

Ischemic heart disease: prevention of attacks of stable angina (in complex therapy).

Cochleovestibular disorders of ischemic nature, such as dizziness, noise in the ears; hearing impairment.

Chorioretinal vascular disorders.

Contraindications:

- Hypersensitivity to any component of the drug;

- renal failure (CC less than 15 ml / min);

- pronounced violations of the liver function;

- age to 18 years (efficiency and safety not established).

Pregnancy and lactation:

Studies on animals have not revealed a teratogenic effect, however, due to the lack of clinical data, the use of the drug Antistene during pregnancy is not recommended.

It is not known whether trimetazidine with breast milk. If you need to use the drug during lactation, you should decide whether to stop breastfeeding.

In experimental studies, the teratogenic effect of trimetazidine has not been established.

Dosing and Administration:

Inside, during meals, take whole, without chewing, washing with water.

Antisthenes recommended to use 1 tablet (20 mg) 2-3 times a day (40-60 mg / day).

The course of treatment is recommended by a doctor.

Side effects:

The incidence of side effects is given in the following gradation: very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10000, <1/1000); very rarely (<1/10000), including individual messages.

From the digestive system

Often: abdominal pain, diarrhea, indigestion, nausea, vomiting.

Common violations

Often: asthenia.

From the central nervous system

Often: dizziness, headache.

Very rarely: extrapyramidal symptoms (tremor, rigidity, akinesia), reversible after drug withdrawal.

From the skin

Often: skin rash, itching, hives.

From the side of the cardiovascular system

Rarely: orthostatic hypotension, "hot flashes" of blood to the skin of the face.

Overdose:

At present, there is only limited information on overdose.

In case of an overdose, symptomatic therapy should be given.

Interaction:There is no information.

Special instructions:

Do not use to stop angina attacks!

The drug is not indicated for the initial course of therapy for unstable angina or myocardial infarction.

In the case of an attack of angina pectoris, the treatment should be reviewed and adapted. If you skip one or more doses of the drug, you can not take a higher dose to the next dose!

Effect on the ability to drive transp. cf. and fur:

Antistane slightly affects the ability to drive vehicles and perform work that requires an increased speed of psychomotor reactions.

Form release / dosage:Film coated tablets a shell of 20 mg.

Packaging:

For 10, 30 tablets in a contour cell pack of film polyvinylchloride and foil aluminum printed varnished.

By 10, 14, 20, 28, 30, 40, 50 or 100 tablets in cans of polymeric medicines.

One bank or 1, 2, 3, 4, 5, 6, 8 or 10 contour cell packs together with instructions for use placed in a cardboard box (pack).

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:P N003953 / 01

Date of registration:30.11.2009 / 10.01.2013

Expiration Date:Unlimited

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp06.09.2017

Illustrated instructions

Instructions

Antisthene (Antisten)