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

Corn starch 107.2 mg, talc purified 10.0 mg, gelatin 5.0 mg, stearic acid 1.0 mg, methylparaben 0.5 mg, propylparaben 0.05 mg, sodium metabisulphite 0.25 mg.

Description:Round flat cylindrical tablets of white color with a risk on one side and bevel.

Pharmacotherapeutic group:Anti-tuberculosis drug

ATX: & nbsp

J.04.A.K.01 Pyrazinamide

Pharmacodynamics:Pyrazinamide - anti-tuberculosis drug of the II series. It acts on intracellularly located Mycobacterium tuberculosis. Has a bacteriostatic or bactericidal effect depending on the concentration and sensitivity of the microorganism. More active on tuberculostatic activity than aminosalicylic acid, although inferior to isoniazid, streptomycin, rifampicin. It acts on Mycobacterium tuberculosis, resistant to other anti-tuberculosis drugs of the II series. The drug penetrates well into the centers of tuberculous lesion. Its activity does not decrease in the acidic environment of caseous masses, and therefore it is often prescribed for caseous lymphadenitis, tuberculomas and caseous-pneumonic processes.

Pharmacokinetics:Pyrazinamide well absorbed from the gastrointestinal tract. After oral administration at a dose of 500 mg, the maximum concentration of pyrazinamide in blood plasma is 9-12 μg / ml and is achieved within 2 hours, 7 μg / ml after 8 hours and 2 μg / ml after 24 hours. Pyrazinamide penetrates into tissues and body fluids, including the liver, lungs, brain, cerebrospinal fluid. Connection with blood plasma proteins - 10-20%. Metabolised in the liver,where the active metabolite (pyrazinic acid) is first formed, which then becomes an inactive metabolite - 5-hydroxypyrazinic acid. The half-life is 8-9 hours in patients whose liver and kidney function are not impaired. It is excreted by the kidneys in unchanged form - 3%, in the form of pyrazinic acid - 33%, in the form of other metabolites - 36%. Removed during hemodialysis.

Indications:It is used for the treatment of tuberculosis (as part of a combination therapy).

Contraindications:

- Hypersensitivity to pyrazinamide, other components of the drug;

- liver disease;

- gout;

- Hyperuricemia;

- pregnancy, the period of breastfeeding;

- Children's age up to 3 years (for this dosage form).

Pregnancy and lactation:The use of the drug during pregnancy and during breastfeeding is contraindicated.

Dosing and Administration:

The drug is used inside during or after a meal, once a day, preferably at breakfast with a little water.

Adults appoint 25-30 mg / kg body weight, which corresponds to patients with body weight less than 50 kg - 1.5 g and for patients with a body weight of more than 50 kg - 2 g.

The maximum daily dose is 2.5 g.

In case of unsatisfactory portability pyrazinamide appoint 2-3 reception.

In elderly and elderly people, the drug should be administered every other day at a daily dose of 15 mg / kg body weight.

Children older than 3 years are prescribed 15-20 mg / kg once a day (maximum dose of 1.5 g per day).

Pyrazinamide is used in combination with aminoglycosides (streptomycin or kanamycin in a dose of 15 mg / kg), isoniazid (10 mg / kg), rifampicin (10 mg / kg).

The course of treatment is 3 months or more. The duration of the course of treatment depends on the nature and form of the disease, the effectiveness and tolerability of the drug.

Side effects:

From the digestive system: nausea, vomiting, diarrhea, "metallic" taste in the mouth, abnormal liver function (anorexia, pain in the right upper quadrant, hepatomegaly, jaundice, yellow atrophy of the liver); exacerbation of peptic ulcer, epigastric pain.

From the central nervous system: dizziness, headache, sleep disturbances, increased excitability, depression, hallucinations, convulsions, confusion.

On the part of the organs of hematopoiesis and the system of hemostasis: thrombocytopenia, sideroblastic anemia, erythrocyte vacuolization, porphyria, hypercoagulation, splenomegaly.

From the genitourinary and urinary system: dysuria, interstitial nephritis.

From the musculoskeletal system: arthralgia, myalgia.

Allergic reactions: skin rash, hives.

Other: hyperthermia, fever, weakness, hyperuricemia, exacerbation of gout, increased serum iron concentration, photosensitivity, acne, hypoglycemia (in patients with diabetes mellitus).

Overdose:

Symptoms: nausea, vomiting, abdominal pain, impaired liver function, increased severity of side effects from the central nervous system, acute pulmonary edema, respiratory disorders, hyperglycemia, metabolic ketoacidosis.

Treatment: symptomatic; gastric lavage, Activated carbon, forced diuresis.

Interaction:

Pyrazinamide is combined with other anti-tuberculosis drugs. In particular, with chronic destructive forms it is recommended to combine it with rifampicin (pronounced effect) or ethambutol (better tolerability). Strengthens the effects of other anti-tuberculosis drugs, incl. fluoroquinolones. The likelihood of developing a hepatotoxic effect of the drug is increased when combined withrifampicin.

Possible development of hypoglycemia in patients with diabetes mellitus.

With simultaneous application with probenecid, a decrease in excretion and, consequently, an increase in the toxic reactions of pyrazinamide is possible.

Weakens the effect of anti-gouty drugs.

Special instructions:

There is evidence of a delay in the body under the influence of pyrazinamide uric acid, and there may be pain in the joints. It is necessary to monitor the activity of hepatic transaminases and the concentration of uric acid in the blood regularly (at least once a month).

With prolonged use may have toxic effects on the liver. If liver function is impaired, pyrazinamide should be discontinued.

It is not recommended to use ethanol while using the drug.

During treatment it is necessary to avoid sunlight and artificial UV irradiation to avoid the development of photosensitization.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets 500 mg.

Packaging:10 tablets are placed in PVC / AL blisters or AL / AL aluminum foil strips. For 2 or 10 blisters or strips, together with the instructions for use are placed in a cardboard box.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N016308 / 01

Date of registration:17.06.2005 / 06.02.2014

Expiration Date:Unlimited

The owner of the registration certificate:FARMGID CJSCFARMGID CJSC Russia

Manufacturer: & nbsp

Laika Labs Limited India

Information update date: & nbsp07.04.2018

Illustrated instructions

Instructions

Linamide (Lynamide)