Ethionamide
When ATH:
J04AD03
Characteristic.
Tioamid, isonicotinic acid derivative. TB drugs II series. Yellow crystalline powder with low or moderate smell of sulfur. Not hygroscopic. Practically insoluble in water and air; it is soluble in ethyl and methyl alcohol, propylene glycol; soluble in acetone, dichloroethane; freely soluble in pyridine. Molecular weight 166,25.
Pharmacological action.
Antiphthisic.
Application.
Tuberculosis (pulmonary and extrapulmonary, in case of intolerance or ineffectiveness of anti-TB drugs I series, incl. in the complex therapy tuberkulostaticheskoy).
Contraindications.
Hypersensitivity, incl. isoniazid, pirazinamidu, nicotinic acid and other similar chemical structure PM, acute gastritis, gastric ulcer and duodenal ulcer, yazvennыy colitis, cirrhosis and other liver diseases in the acute phase, Saint Martin's evil, renal failure, Age to 14 years.
Restrictions apply.
Diabetes, epilepsy, liver disease is worsening (It increases the risk of hepatotoxicity).
Pregnancy and breast-feeding.
Contraindicated in pregnancy. Ethionamide passes through the placenta. In experimental animal studies (Rabbits, rats) shown teratogenic effects at doses, exceeding the recommended human.
At the time of treatment is recommended not to breastfeed (unknown, whether ethionamide gets into breast milk).
Side effects.
From the nervous system and sensory organs: neurological and mental disorders - headache, paraesthesia, convulsions, poor concentration, confusion, drowsiness or insomnia, weakness, depression, hallucinations, excitation, psychosis, peripheral neuritis, optic neuritis.
From the digestive tract: anorexia, metallic taste in mouth, stomatitis, hyperptyalism, burp with rotten smell, nausea, vomiting, epigastric pain, diarrhea, flatulence, abnormal liver function (hepatotoxicity up to the development of hepatitis).
Cardio-vascular system and blood (hematopoiesis, hemostasis): tachycardia, orthostatic hypotension, hemodyscrasia (thrombocytopenia).
Allergic reactions: skin rash, hives, exfoliative dermatitis.
Other: gynecomastia, dysmenorrhoea, impotence, gipotireoidizm, episodes of hypoglycemia in patients with diabetes, hypovitaminosis B6, weight loss, arthralgia, photosensitivity.
Cooperation.
When used in conjunction with other anti means shown synergy in relation to the main action. Together with the admission cycloserine increases the risk of neurotoxic effects, in particular convulsions (especially in patients, having a history of neurological disease), with isoniazid, rifampicin and pyrazinamide - risk of hepatotoxicity. It enhances the toxic effect of alcohol.
Dosing and Administration.
Inside, through 30 min after meal, drinking milk or orange juice. Adults: by 250 mg 3-4 times a day; The maximum daily dose - 1,0 g; older patients 60 years, birth weight less than 50 kg - for 250 mg 2 once a day. Children over 14 years: daily dose - calculation of 10-20 mg / kg / day, but not more 750 mg / day. Duration of treatment: 1–2 years.
Precautions.
Before treatment is necessary to study the gastrointestinal tract and liver function, and determination of the sensitivity of the selected strains of mycobacteria. During treatment should be every 2-4 weeks to monitor the level of activity of hepatic transaminases, conduct eye examination, patients with diabetes — regularly to determine the level of glycemia.
In a joint application with pyrazinamide need more frequent monitoring of liver function. The combined use of prothionamide impractical because of the cross-resistance of Mycobacterium tuberculosis to these drugs. Avoid concurrent use with PM, possessing hepatotoxic.
To prevent side effects ethionamide be combined with nicotinamide (by 0,1 g 2-3 times per day) and vitamin B6 (1-2 ML 5% solution / m).
At the time of treatment should refrain from drinking alcohol. Be wary of the drivers of vehicles and people, activities which require high concentration of attention.
