Furazolidone (active ingredient: 3- (5-nitro-2-furanyl) methylene-amino-2- oxazolidinone ) is a drug with a pronounced antimicrobial effect, a derivative of nitrofurans . MAO inhibitor.
| Furazolidone | |
|---|---|
| Furazolidone | |
 | |
| Chemical compound | |
| IUPAC | 3 - [[(5-Nitro-2-furanyl) methylene] amino] -2-oxazolidinone |
| Gross formula | C 8 H 7 N 3 O 5 |
| Molar mass | 225.158 g / mol |
| CAS | |
| Pubchem | |
| Drugbank | |
| Classification | |
| ATH | |
| Dosage Forms | |
| granules for the preparation of suspensions for oral administration, tablets | |
| Mode of administration | |
| Oral-local | |
| Other names | |
| Furazolidone | |
Pharmacological action
Active against gram-positive and gram-negative microbes , Trichomonas spp. , Giardia lamblia . Most sensitive to furazolidone Shigella dysenteria spp. , Shigella flexneri spp. , Shigella boydii spp. , Shigella sonnei spp. , Salmonella typhi , Salmonella paratyphi . It has little effect on the causative agents of purulent and anaerobic infections. The resistance of microorganisms develops slowly. Inhibits MAO . Nitrofurans disrupt the cellular respiration of microorganisms, inhibit the tricarboxylic acid cycle (Krebs cycle) , and also inhibit other biochemical processes of microorganisms, resulting in the destruction of their membrane or cytoplasmic membrane . As a result of the action of nitrofurans, microorganisms secrete less toxins , and therefore it is possible to improve the general condition of the patient even before the pronounced suppression of the growth of microflora . Unlike many other antimicrobial drugs, they not only do not inhibit, but even activate the body's immune system (they increase the complement titer and the ability of leukocytes to phagocytose microorganisms).
Pharmacokinetics
Furazolidone is poorly absorbed in the gastrointestinal tract and acts in the intestine.
Indications
Dysentery , paratyphoid , giardiasis , salmonellosis , food toxicoinfections .
Contraindications
Hypersensitivity, end-stage chronic renal failure, pregnancy , lactation , child age (up to 1 year).
- With caution
Chronic renal failure , deficiency of glucose-6-phosphate dehydrogenase, liver and nervous system diseases , age less than 1 month - for local use.
Side Effects
Decreased appetite , including anorexia , nausea , vomiting , allergic reactions (skin rash, hyperemia and itching of the skin, angioedema ). With prolonged use increases the risk of kidney neoplasms. For this reason, is prohibited to use in the US and the EU.
Dosing regimen
Inside, after eating. With dysentery, paratyphoid and foodborne diseases - 100-150 mg 4 times a day (but not more than 800 mg), for 5-10 days. With giardiasis: adults - 100 mg 4 times a day, children - 10 mg / kg / day, distributing the daily dose in 3-4 doses. The highest single dose for adults is 200 mg; daily - 800 mg. Previously used: With trichomonad colpit - 100 mg 3-4 times a day for 3 days, and at the same time 5-6 g of powder containing furazolidone with milk sugar in the ratio of 1: 400-1: 500 are injected into the vagina , and intestine - candles containing 4-5 mg. The course of treatment is 7-14 days. With Trichomonas urethritis - inside, 100 mg 4 times a day for 3 days. For the treatment of burns and wound infections used topically, in the form of irrigation or wet-drying dressings with a solution of furazolidone (1: 25000).
Overdose
With the use of excessive doses of the drug in patients may develop toxic liver damage, including acute toxic hepatitis. In addition, the development of polyneuritis (neurotoxic effect) and the hematotoxic effect of furazolidone are possible. There is no specific antidote. With an overdose of the drug is indicated gastric lavage, taking enterosorbents and salt laxatives. If necessary, conduct activities to maintain water and electrolyte balance. It is also possible the appointment of antihistamines and vitamins of group B. In the case of severe overdose of the drug, as well as the use of excessive doses of the drug in patients suffering from renal dysfunction, hemodialysis is shown.
Symptoms
Acute toxic hepatitis , hematotoxicity , polyneuritis .
Treatment
The abolition of the drug, taking a large amount of fluid, symptomatic therapy, antihistamine drugs, B vitamins .
Interaction
Furazolidone in combination with ethanol can lead to the development of disulfiram-like reactions . Antidepressants , MAO inhibitors , ephedrine , amphetamine , phenylephrine , tyramine - a sharp increase in blood pressure is possible.
Special instructions
Increases blood pressure depression against chloramphenicol and ristomycin . Increases sensitivity to the action of ethanol and can be used to treat alcoholism . Drugs that alkalize urine reduce the effect, and acidifying drugs increase it. Aminoglycosides and tetracycline enhance antimicrobial properties. During treatment, the same precautions should be observed as with the use of MAO inhibitors . For the prevention of neuritis with prolonged use must be combined with vitamins of group B.