Coxerin Plus - instructions for use, dose, side effects, contraindications

Excipients: magnesium oxide heavy (40.0 mg), methacrylic acid and methyl methacrylate copolymer (1: 2) (37.0 mg), magnesium trisilicate (8.0 mg), crospovidone (26.0 mg), talc purified (11.5 mg), magnesium stearate (2.5 mg).

Shell composition: hypromellose (4.0 mg), ethylcellulose (1.0 mg), titanium dioxide (1.2 mg), talc purified (0.4 mg), diethyl phthalate (0.4 mg), propylene glycol (0.4 mg) .

Description:

Round, biconvex tablets, coated with a coat of white or almost white.

Pharmacotherapeutic group:Other antibiotics in combination

ATX: & nbsp

J.04.A.B.01 Cycloserine

A.11.H.A.02 Pyridoxine (vitamin B6)

Pharmacodynamics:

Combined drug, the components of which are cycloserine and pyridoxine hydrochloride.

Cycloserine, a broad-spectrum bactericidal antibiotic, inhibits the synthesis of the cell membrane of sensitive strains of Gram-positive and Gram-negative bacteria and Mycobacterium tuberculosis.

Pyridoxine hydrochloride reduces the intensity of adverse reactions of cycloserine from the side of the central nervous system.

Pharmacokinetics:

Cycloserin is rapidly absorbed from the gastrointestinal tract (GIT) after ingestion, creating detectable plasma levels within one hour. It is freely distributed to the fluids and tissues of the body.

Cycloserine penetrates the blood-brain barrier (BBB), the concentrations in the cerebrospinal fluid are about the same as in plasma. In patients with tuberculosis cycloserine is found in sputum, as well as in pleural and ascitic fluids, in bile, amniotic fluid and fetal blood, in breast milk, lung tissue and lymphoid tissue.

Cycloserin is excreted by the kidneys, in the urine it is detected in half an hour after taking the dose. About 66% of the dose is found unchanged in the urine within 24 hours. 10% is displayed within the next 48 hours. The intestine displays a small amount. About 35% is metabolized, but metabolites have not been identified to date.

The half-life (T_1/2) cycloserine fluctuates within 8-12 hours.

Pyridoxine hydrochloride is absorbed rapidly throughout the small intestine, a larger amount is absorbed in the jejunum. Metabolised in the liver with the formation of pharmacologically active metabolites (pyridoxal phosphate and pyridoxamine phosphate). Pyridoxal phosphate with plasma proteins binds to 90%. It penetrates well into all tissues; accumulates mainly in the liver, less - in the muscles and central nervous system (CNS). Penetrates through the placenta, is secreted with breast milk. T_1/2 - is 15-20 days. It is excreted by the kidneys, as well as during hemodialysis.

Indications:

Kokserin® plus is used as a part of the combination therapy of active pulmonary and extrapulmonary (including renal) tuberculosis in case of ineffectiveness of combined therapy with drugs of the first series.

Coxerin® plus is used in the combination of tuberculosis with acute infections of the urinary tract caused by sensitive strains of gram-positive and gram-negative bacteria, especially Klebsiella spp., Enterobacter erp., And Escherichia coli with ineffective essential drugs.

Contraindications:

Hypersensitivity to cycloserine, pyridoxine and other components of the drug;
epilepsy;
depression;
marked excitement or psychosis;
severe chronic renal failure (creatinine clearance less than 25 ml / min);
acute and chronic heart failure;
alcohol and drug abuse;
children under 3 years of age and / or with a body weight of less than 25 kg.

Carefully:Chronic renal failure (with creatinine clearance more than 25 ml / min).

Pregnancy and lactation:

The use is possible only on strict indications or at life-threatening conditions, with the doctor's confidence that the potential benefit of using the drug in pregnant women exceeds the possible harm to the fetus.

Application in the period of breastfeeding. Concentrations in human milk approach the concentrations found in blood plasma. If it is necessary to use the drug during the lactation period, breast-feeding should be stopped.

Dosing and Administration:

Calculation of the dose is given in terms of cycloserine.

Adults. At the rate of 12.5 mg / kg of body weight when taking the drug 2 to 3 times a day. The initial dose for adults is often 250 mg in 2 divided doses at 12-hour intervals during the first week.

The average daily dose is from 250 mg to 1.0 g per day, but should not exceed 1.0 g.

Children older than 3 years (and with a body weight of more than 25 kg): The usual initial dose is from 10 mg / kg of body weight per day in 1-2 divided doses. The daily dose should not exceed 750 mg.

The elderly. Patients older than 60 years, and also with a body weight of less than 50 kg - 250 mg twice a day.

Side effects:

From the central nervous system: cramps, drowsiness, headache, tremor, dysarthria, dizziness, confusion and disorientation (with loss of memory), psychoses (including suicidal attempts), changes in character, increased irritability, aggressiveness, peripheral paresis, hyperreflexia, paresthesia, large and small seizures of clonic convulsions, coma.

From the gastrointestinal tract: nausea, heartburn, diarrhea, exacerbation of the disease especially in elderly patients with concomitant liver diseases.

Allergic reactions: skin rash, itching.

Lab tests: sideroblastic and megaloblastic anemia, increased activity of hepatic aminotransferases, deficiency of cyanocobalamin and folic acid.

Overdose:

Symptoms (when taking more than 1.0 g and adults with impaired renal function): headache, dizziness, confusion, increased irritability, paresthesia, dysarthria, psychosis, peripheral paresis, convulsions and coma. From the side of the cardiovascular system - exacerbation of chronic heart failure when applied at a dose of 1.0 - 1.5 g per day (see the section "Contraindications").

Treatment: symptomatic. To reduce the absorption of cycloserine, it is more preferable to use Activated carbon, than gastric lavage and induction of vomiting. Cycloserine is output by hemodialysis.

Interaction:

Cycloserine promotes a decrease in resistance to isoniazid, streptomycin and PASC.

Ethionamide increases the risk of side effects of cycloserine from the side of the central nervous system, especially seizures.

Isoniazid increases the incidence of dizziness, drowsiness with cycloserine (a dose adjustment of both drugs may be required).

Ethanol increases the risk of developing epileptic seizures when cycloserine is used, especially in individuals with chronic alcoholism.

Special instructions:

Before starting treatment with Coxerin® Plus, culture M. tuberculosis determine its sensitivity to cycloserine.

In case of development against the background of treatment of allergic dermatitis or symptoms of CNS damage (cramps, psychosis, drowsiness, confusion, hyperreflexia, headache, dizziness, tremor, peripheral paresis, dysarthria), the drug should be discontinued.

During the treatment period it is necessary to monitor the parameters of electroencephalography (EEG), hematological parameters, kidney and liver function.

In the treatment of patients with reduced renal function, taking a daily dose of cycloserine more than 500 mg, weekly monitoring of urinalysis is necessary.

Patients who receive more than 500 mg of cycloserine per day should be under the direct supervision of a physician because of the possible development of central nervous system damage (for example, convulsions, agitation, tremor). For the prevention of adverse neurotoxic effects prescribe drugs benzodiazepine series (diazepam, phenazepam), nootropic drugs (piracetam, glutamic acid).

Alcohol and reception of cycloserine are incompatible.

Features of the drug at the first admission or when canceled:

The drug does not have the features of the action at the first reception or upon its cancellation.

Description of the actions of the medical worker and the patient if one or several doses of the drug are missed:

Under no circumstances should you yourself prematurely terminate or temporarily discontinue the course of treatment started or take the medication irregularly.

If you miss a dose, you should take the next dose of the drug at the set time, or if you agree with the doctor, take the next dose at a time when you remembered taking the drug, smoothly shifting the next time you take the drug, you should not take twice the dose of the drug.

Special precautions for the destruction of an unused medicinal product or a drug with an expired shelf life is not required.

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

It should refrain from managing transport or other technical means and practicing potentially hazardous activities requiring increased attention and rapid psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 250 mg + 25 mg.

Packaging:

4 tablets in strips of aluminum foil. For 1 or 15 strips are placed in a pack of cardboard along with instructions for use.

10 tablets into aluminum foil strips. For 10 strips are placed in a pack of cardboard along with instructions for use.

When packaged at a Russian enterprise (LLC Dobrolek, FGBNU "RNTS named after NN Blokhin" or ZAO "Rafarma"), 10 strips of 10 tablets are placed in a pack of cardboard together with instructions for use.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001783

Date of registration:20.09.2011 / 09.12.2014

Expiration Date:Unlimited

The owner of the registration certificate:McLeodz Pharmaceuticals Co., Ltd. McLeodz Pharmaceuticals Co., Ltd. India

Manufacturer: & nbsp

MACLEODS PHARMACEUTICALS, Ltd. India

Representation: & nbspAdvansd Trading, OOOAdvansd Trading, OOO

Information update date: & nbsp30.01.2018

Illustrated instructions

Instructions

Coxerin® Plus (Coxerin Plus)