Ethionamide

2- ethyl pyridine -4- carbothioamide

J04AD03

Yellow crystalline powder or small, yellow crystals

Tuberculostatic

Practically insoluble in water, soluble in methanol, sparingly soluble in ethanol

Attention

1320 mg · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

Ethionamide is an antibiotic that is structurally one of the thionamides. It is used to treat multidrug-resistant tuberculosis bacteria. It is a drug of second choice, the application is only in combination with other anti-tuberculosis drug, as it quickly comes to resistance in administered alone. Ethionamide is led by the World Health Organization as an essential drug.

Pharmacodynamics

Mechanism of Action

The mechanism of action is not fully understood, ethionamide appears as a bacteriostatic agent in the synthesis of mycolic acids to inhibit component of the bacterial wall. When used alone rapidly develop resistance, which is also a full cross-resistance to protionamide (also on the group of thionamides ) arises.

Side effects

Common side effects are gastrointestinal symptoms ( diarrhea, abdominal pain, salivation, nausea, vomiting, anorexia ) that occur dose-dependent. Occasionally, allergic reactions, nerve damage, reversible hepatitis, gynecomastia, menstrual disorders, joint pain, decreased leukocytes, or underactive thyroid (hypothyroidism).

Pharmacokinetics

The bioavailability after oral administration as a tablet is 100 %, but may be limited by disturbances of the digestive function that may occur as a side effect. The distribution is carried out rapidly, the substance overcoming the blood- brain barrier. The reduction is carried out by the liver into active sulfoxide metabolites and other non- active metabolites.

Contraindications

Ethionamide has been shown in animal models has demonstrated teratogenic ( teratogenic ) effects and should not be used in pregnancy and lactation. Other contraindications include porphyria and severe liver disease. Renal insufficiency, however, has little effect on the degradation of active ingredient.

Trade names

Trecator (USA and others), Ethatyl, Ethide, Eton, Etyomid, Myobid ( more international product name, not available in D. )