Raneksa

Ранекса Drug photo

The description is actual on 10.03.2016

  • Latin name: Ranexa
  • ATH code: C01EB18
  • Active ingredient: Ranolazin (Ranolazine)
  • Producer: DSM Pharmaceuticals Inc. (USA)

Structure

In 1 tablet of a ranolazin of 500 or 1000 mg and excipients.

Release form

Tablets of the prolonged action in a film cover of 500 mg and 1000 mg.

Pharmacological action

Anti-anginal.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

The effective anti-anginal and anti-ischemic remedy which is authentically reducing quantity of attacks of stenocardia. The mechanism of action is unique that distinguishes this drug from other anti-anginal means. In the conditions of ischemia the overload of muscle cells of heart is noted by calcium ions that breaks relaxation of a myocardium in a diastole and reduces filling of coronary arteries, causing stenocardia attacks. Ranolazin inhibits late current of ions of sodium in cardiomyocytes, and decrease in intracellular sodium attracts reduction of intracellular calcium. Decrease in excess of calcium in a cell leads to relaxation of a myocardium, decrease in diastolic tension of ventricles, improvement of a coronary blood-groove in general and in an ischemia zone, in particular. Thus, the vicious circle of ischemia is broken off.

At treatment of development of tolerance does not occur, and after sharp cancellation the frequency of attacks does not increase. Considerably portability of loadings at patients improves. There is a clear dependence "dose effect": the dose is higher, the anti-anginal effect is higher. On an ECG lengthening of an interval of QTc, decrease in height of a tooth of T, reduction of frequency of developing of arrhythmias is noted. At all these effects insignificant decrease in ChSS and decrease in the systolic ABP is observed.

Pharmacokinetics

At intake of Cmax in blood is defined by 2 — 6 h. Equilibrium concentration is reached in 3 days of administration of drug 2 times a day. Bioavailability makes 35-50%. About 63% of active ingredient contact blood proteins. Is exposed to a metabolism in a liver with participation of isoenzymes of CYP3A4 and CYP2D6. It is allocated with kidneys and through intestines. Period about 7 hours. At HSN increase of concentration by 1,3 times is noted. At elderly persons strengthening of effect of drug is possible. At a renal failure of AUC the ranolazina is 1,7-2 times higher, than at healthy.

Indications to use

Treatment of stable stenocardia.

Contraindications

  • renal failure of average and heavy degree;
  • use with itrakonazoly, pozakonazoly, Ketokonazoly, klaritromitsiny, nefazodony, telitromitsiny, the being powerful inhibitors of CYP3A4 enzyme;
  • use with antiarrhytmic drugs of a class I A and III;
  • age till 18 flyings;
  • feeding by a breast;
  • pregnancy;
  • hereditary lactose intolerance;
  • hypersensitivity.

With care Raneks's drug is used at persons 75 years, weighing less than 60 kg, when lengthening an interval of QT, HSN III-IV of a functional class, at simultaneous use with diltiazem, erythromycin, flukonazoly, rifampicin, phenobarbital, Phenytoinum, carbamazepine and drugs of the St. John's Wort which is made a hole are more senior than insufficiency of an isoenzyme of CYP2D6.

Side effects

Often met side reactions:

Infrequently and seldom met side reactions:

  • loss of appetite or its total absence, dehydration;
  • abdominal pain, meteorism, dryness mucous a mouth, pain in a stomach, an erosive duodenitis;
  • sleeplessness, alarm, hallucinations;
  • block, drowsiness, syncope, tremor;
  • amnesia, lacks of coordination and gait, loss of consciousness, change of sense of smell;
  • sight illegibility, various visual frustration;
  • vertigo, sonitus, decrease in hearing;
  • the expressed decrease in the ABP, cold snap of extremities;
  • short wind, cough;
  • skin itch, rash, small tortoiseshell, allergic dermatitis;
  • extremity pain, weakness in muscles and spasms, swelling of joints;
  • dysuria, ischuria, hamaturia;
  • peripheral hypostases;
  • increase of activity "hepatic" transtaminaz, concentration of creatinine and urea.

Raneksa, application instruction (Way and dosage)

Raneks's pill are taken inside is not dependent on meal. Tablets should not be chewed, crushed or broken. An initial dose of Raneks of 500 mg 2 times a day. If necessary in 2 weeks the dose increases to 1000 mg twice a day that the MS a dose is.

At emergence of dizziness or nausea the dose decreases to 500 mg again. Use of drug is stopped if by-effects do not disappear.

To patients with HSN III-IV FC, a renal and liver failure, to persons is more senior 75 and weighing less than 50 kg careful selection of a dose is carried out.

Overdose

Overdose is shown by dizziness, nausea, doubling in eyes, block, a faint. Symptoms accrue at increase in a dose. The gastric lavage, use of sorbents, symptomatic therapy is carried out.

Interaction

Use with CYP3A4 isoenzyme inhibitors significantly increases concentration of a ranolazin that attracts strengthening of dozozavisimy side reactions therefore appointment along with powerful inhibitors of an isoenzyme about which it was stated above, contraindicated. It is necessary to remember that grapefruit juice — powerful inhibitor of an isoenzyme CYP3A4.

Inhibitors of an isoenzyme of average force (diltiazem, erythromycin, flukonazol) cause increase of Css value of drug by 1,5-2,5 times therefore Raneks dose decline is necessary. Inductors of activity of an isoenzyme, on the contrary, lead to decrease in efficiency.

The dose of drug decreases at use with Cyclosporine and Verapamil which increase its concentration in blood.

As ranolazin weak inhibitor of an isoenzyme CYP2D6, its reception increases concentration and strengthens action of a metoprolol, propafenon, flekainid, tricyclic antidepressants and neuroleptics.

At use with digoxin its concentration by 1,5 times increases.

Reception of a ranolazin in high doses increases concentration of a simvastatin. Cases of a rabdomioliz at use of these drugs are registered. The lovastatin requires also restriction of a dose.
Ranolazin causes increase in concentration in blood of a takrolimus, sirolimus, cyclosporine, an everolimus.

Medicinal the means extending an interval of QT and applied along with ranolaziny (terfenadin, mizolastin, astemizol, quinidine, procaineamide, Disopyramidum, Imipraminum, amitriptyline, doksepin), cause risk of ventricular arrhythmias.

Terms of sale

According to the recipe.

Storage conditions

Temperature of storage is up to 25 °C.

Period of validity

4 years.

Raneksa's analogs

There are no structural analogs. Have similar action: verapamil, diltiazem, nifedipine, anaprilin, metoprolol, Talinololum.

About Raneks

Ranolazin is used in the combined treatment of ischemic heart disease patients and renders additional anti-ischemic and anti-anginal effect. So, reduction of frequency of attacks, increase in duration of an exercise stress at addition of 1000 mg a day Raneks at patients who accepted only amlodipin is noted. As a result of treatment the dose of an amlodipin was reduced. Also patients note reduction of frequency of attacks and a dose decline of nitroglycerine after reception of this drug within 6 weeks. At some patients against treatment attacks of ventricular and supraventricular tachycardia decreased.

Ranolazin did not exert considerable impact on ChSS and arterial pressure and did not cause the expressed side effects if it was applied independently in the form of monotherapy. And at appointment together with β-adrenoblockers or BKK not expressed headaches and dizzinesses, weakness were observed.

Zdravzona

  • Traneksam of 250 mg No. 30 tabletkiobninsky HFK
  • Traneksam 50mg/ml 5 ml No. 10 of amp. Moscow endocrine plant of federal state unitary enterprise
  • Traneksam of 250 mg No. 10 tabletkiobninsky HFK
  • Traneksam of 500 mg No. 10 tabletkiobninsky HFK
  • Raneksa of 1000 mg No. 60 tabletkimenarini A.

Drugstore of IFC

  • Traneksam tbl p / about 250 mg No. 10 **, Nizhpharm / Obninsk chemical-farm.kompaniya Zaorossiya
  • Raneksa tbl pro-longum. p / about 500 mg No. 60, Menarini Industriegermaniya
  • Traneksam tbl p / about 250 mg No. 30 **, Nizhpharm / Obninsk chemical-farm.kompaniya Zaorossiya
  • Raneksa tbl pro-longum. p / about 1000 mg No. 60, Menarini Industriegermaniya
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Apteka24

  • Traneksam30

BIOSPHERE

  • Raneksa of 500 mg No. 60 tabl.p.p.o.menarini-Von Heyden GmbH (Germany)
  • Raneksa of 1000 mg No. 60 tabl.p.p.o.menarini-Von Heyden GmbH (Germany)
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Section: Cardiological Cardiovascular
in more detail

Education: Graduated from Sverdlovsk medical school (1968 - 1971) as "Paramedic". Graduated from the Donetsk medical institute (1975 - 1981) as "An epidemiologist, a hygienist". Passed postgraduate study in the Central scientific research institute of epidemiology Moscow (1986 - 1989). An academic degree – the candidate of medical sciences (degree is awarded in 1989, protection – the Central scientific research institute of epidemiology Moscow). Numerous advanced training courses are studied in epidemiology and infectious diseases.

Experience: Work as the manager of department of disinfection and sterilization of 1981 - 1992. Work as the manager of department of especially dangerous infections of 1992 - 2010. Teaching activity at Medical institute 2010 - 2013.

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