Etionamida

Etionamida Uses, Dosage, Side Effects, Food Interaction and all others data.

A second-line antitubercular agent that inhibits mycolic acid synthesis. It also may be used for treatment of leprosy. (From Smith and Reynard, Textbook of Pharmacology, 1992, p868)

Ethinamate is bacteriostatic against M. tuberculosis. In a study examining ethionamide resistance, ethionamide administered orally initially decreased the number of culturable Mycobacterium tuberculosis organisms from the lungs of H37Rv infected mice. Drug resistance developed with continued ethionamide monotherapy, but did not occur when mice received ethionamide in combination with streptomycin or isoniazid.

Trade Name Etionamida
Availability Prescription only
Generic Ethionamide
Ethionamide Other Names Ethinamide, Ethionamide, Ethionamidum, Ethioniamide, Ethylisothiamide, Ethyonomide, Etionamid, Etionamida, Etionamide, Etioniamid
Related Drugs ciprofloxacin, levofloxacin, Levaquin, rifampin
Type
Formula C8H10N2S
Weight Average: 166.243
Monoisotopic: 166.05646902
Protein binding

Approximately 30% bound to proteins.

Groups Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Etionamida
Etionamida

Uses

Etionamida is a second line antitubercular agent used to treat tuberculosis when other treatments have failed.

For use in the treatment of pulmonary and extrapulmonary tuberculosis when other antitubercular drugs have failed.

Etionamida is also used to associated treatment for these conditions: Active Tuberculosis

How Etionamida works

Etionamida may be bacteriostatic or bactericidal in action, depending on the concentration of the drug attained at the site of infection and the susceptibility of the infecting organism. Etionamida, like prothionamide and pyrazinamide, is a nicotinic acid derivative related to isoniazid. It is thought that ethionamide undergoes intracellular modification and acts in a similar fashion to isoniazid. Isoniazid inhibits the synthesis of mycoloic acids, an essential component of the bacterial cell wall. Specifically isoniazid inhibits InhA, the enoyl reductase from Mycobacterium tuberculosis, by forming a covalent adduct with the NAD cofactor. It is the INH-NAD adduct that acts as a slow, tight-binding competitive inhibitor of InhA.

Toxicity

Symptoms of overdose include convulsions, nausea, and vomiting.

Food Interaction

  • Take with or without food. Taking Etionamida with food may reduce gastrointestinal upset.

Etionamida Alcohol interaction

[Major] GENERALLY AVOID:

The concomitant use of protionamide with alcohol may enhance the central nervous system exciting effect of protionamide.

The mechanism is not known.

Excessive use of alcohol with another thiocarbamide derivative ethionamide, has been reported to precipitate a psychotic reaction.

In addition, alcohol tolerance is reported to be reduced during protionamide treatment.

Consumption of alcohol during protionamide treatment should be avoided.

The manufacturer of ethionamide also advises that excess alcohol consumption should be avoided during ethionamide therapy (US).

Volume of Distribution

  • 93.5 L [healthy volunteers]

Elimination Route

Essentially completely absorbed following oral administration and not subjected to any appreciable first pass metabolism. Bioavailability approximately 100%.

Half Life

2 to 3 hours

Elimination Route

Less than 1% of the oral dose is excreted as ethionamide in urine. Etionamida is extensively metabolized to active and inactive metabolites.

Innovators Monograph

You find simplified version here Etionamida

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http://classyfire.wishartlab.com/tax_nodes/C0000278
http://classyfire.wishartlab.com/tax_nodes/C0004150
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:4885
http://www.hmdb.ca/metabolites/HMDB0014747
http://www.genome.jp/dbget-bin/www_bget?drug:D00591
http://www.genome.jp/dbget-bin/www_bget?cpd:C07665
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2761171
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506077
https://www.chemspider.com/Chemical-Structure.2041901.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50239976
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=4127
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=4885
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1441
https://zinc.docking.org/substances/ZINC000003872520
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP001141
http://www.pharmgkb.org/drug/PA164768738
http://www.rxlist.com/cgi/generic2/ethionamide.htm
https://www.drugs.com/cdi/ethionamide.html
https://en.wikipedia.org/wiki/Ethionamide
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