Ethionamide (Aethionamidum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Other synthetic antibacterial agents

Included in the formulation
  • Miobid-250
    pills inwards 
    Panacea Biotech Co., Ltd.     India
  • Ethid
    pills inwards 
    Lupine Co., Ltd.     India
  • Ethomide
    pills inwards 
    McLeodz Pharmaceuticals Co., Ltd.     India
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    J.04.A.D   Derivatives of thiourea

    J.04.A.D.03   Ethionamide

    Pharmacodynamics:

    Second-line anti-tuberculosis drug. The mechanism of action is not exactly known. Apparently, ethionamide suppresses the synthesis of proteins of mycobacteria. Has a bacteriostatic effect on Mycobacterium tuberculosis.

    Strengthens phagocytosis in the focus of tuberculous inflammation, which contributes to its resorption. During the treatment, the tuberculostatic activity of ethionamide is reduced.

    Pharmacokinetics:

    After oral administration ethionamide quickly absorbed from the digestive tract. At a dose of 250 mg, the maximum concentration in blood plasma is achieved after 2 hours and is about 2 μg / ml. Widely distributed in tissues and body fluids. Penetrates through the placental barrier, through intact cerebral membranes. In cerebrospinal fluid is determined in concentrations equivalent to serum.

    It is subject to intensive metabolism, probably in the liver with the formation of an active sulfoxide metabolite and inactive metabolites. Less than 1% is excreted in the urine unchanged.

    Indications:
    • Tuberculosis of the lung (in case of intolerance or inefficiency of other anti-tuberculosis drugs).
    • Leprosy.
    • MAS infection.
    ICD-10

    I.A15-A19.A15   Tuberculosis of respiratory organs, confirmed bacteriologically and histologically

    I.A30-A49.A30   Leprosy [Hansen's disease]

    I.A30-A49.A31.0   Pulmonary infection caused by Mycobacterium

    Contraindications:

    Hypersensitivity, including isoniazid, pyrazinamide, nicotinic acid and other similar in chemical structure, acute gastritis, peptic ulcer and duodenal ulcer, ulcerative colitis, cirrhosis and other liver diseases in the phase of exacerbation, chronic alcoholism, renal insufficiency, age up to 14 years.

    Carefully:

    Diabetes mellitus, epilepsy, liver disease without exacerbation (the risk of hepatotoxicity increases). Use with caution ethionamide with depression and other mental illnesses.

    Pregnancy and lactation:

    Contraindicated in pregnancy. Ethionamide passes through the placenta. Experimental animal studies (rabbits, rats) demonstrated teratogenic effects when using doses,exceeding those recommended for humans.

    It is recommended to give up breastfeeding for the duration of treatment (it is not known whether it penetrates ethionamide in breast milk).

    Dosing and Administration:

    Inside 30 minutes after eating, washed down with milk or orange juice. Adults: 250 mg 3-4 times a day; the maximum daily dose is 1.0 g; patients older than 60 years with a body weight of less than 50 kg - 250 mg 2 times a day. Children over 14 years of age: daily dose - at a rate of 10-20 mg / kg per day, but not more than 750 mg per day. The duration of the course of treatment is 1-2 years.

    Side effects:

    From the side nervous system and sense organs: neurological and mental disorders - headache, paresthesia, convulsions, decreased concentration, confusion, drowsiness or insomnia, weakness, depression, hallucinations, agitation, psychosis, peripheral neuritis, optic neuritis.

    From the side organs of the digestive tract: anorexia, metallic taste in the mouth, stomatitis, hypersalivation, belch with a rotten smell, nausea, vomiting, epigastric pain, diarrhea, flatulence, liver function disorder (hepatotoxicity up to hepatitis).

    From the side cardiovascular system and blood (hematopoiesis, hemostasis): tachycardia, orthostatic hypotension, impaired hematopoiesis (thrombocytopenia).

    Allergic reactions: skin rash, hives, exfoliative dermatitis.

    Other: gynecomastia, dysmenorrhea, impotence, hypothyroidism, episodes of hypoglycemia in diabetic patients, hypovitaminosis B6, weight loss, arthralgia, photosensitivity.

    Overdose:

    Symptoms: hepatitis or jaundice, peripheral neuritis, mental disorders, goitre or hypothyroidism, hypoglycemia, skin rashes and optic neuritis.

    Treatment: symptomatic.

    Interaction:

    With the simultaneous use of ethionamide and oral hypoglycemic drugs, hypoglycemic action of the latter is enhanced.

    With the simultaneous use of ethionamide and cycloserine, the risk of neurotoxic side effects increases (especially in patients who have a history of neurological or psychiatric disorders).

    Special instructions:

    It is necessary to avoid simultaneous administration of drugs that have a hepatotoxic effect.

    Before the use of ethionamide and every 2-4 weeks of treatment, it is necessary to monitor the activity of liver transaminases. In the case of combined use with pyrazinamide, more frequent monitoring of liver function is required.

    Before the start of therapy should be investigated in vitro the sensitivity of a newly isolated culture Mycobacterium tuberculosis to the ethionamide.

    Ethionamide is used only in combination with other anti-tuberculosis drugs. It is inappropriate to use ethionamide in combination with protionamide, as in mycobacteria tuberculosis there is a cross-resistance to these drugs.

    During the reception, ethionamide is administered pyridoxine to prevent the development of peripheral neuritis.

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