METRONIDAZOL 250

Keep out of reach of children.

Read the directions carefully before use.

For prescription only.

QUALITATIVE AND QUANTITATIVE COMPOSITION:

Metronidazole .............................. 250 mg

Excipients q.s............................... 1 tablet

(Tabioca starch, lactose monohydrate, talc, magnesium stearate, povidone K30)

PHARMACEUTICAL FORM: Tablet.

Product description: A round, white to ivory-white, plain on one side, a break line on other side, intact edges.

THERAPEUTIC INDICATIONS:

For the treatment of infections of Trichomonas vaginalis, Entamoeba histolytica (acute intestinal form and liver abscess form), Dientamoeba fragilis in children, Giardia lamblia and Dracunculus medinensis.

For the treatment of severe infections caused by susceptible anaerobic bacteria e.g. intra-abdominal infections, gynecologic infections, skin and skin structure infections, CNS infections, septicemia, and endocarditis.

For the treatment of acute necrotizing ulcerative gingivitis, dental gingivitis, active Crohn’s disease in colon and rectum, ulcerative gastroduodenitis due to Helicobacter pylori (combination with some other drugs).

DOSAGE & ADMINISTRATION:

Treatment of protozoa infections:

Trichomoniasis: A single dose of 2 g or 1 tablet x 3 times daily for 7 days. Sexual partners should be treated concomitantly.

Amoebiasis: The therapy should be 5 - 10 days.

Adults: oral dose of 500 - 750 mg (2 - 3 tablets) x 3 times daily.

Children: oral dose of 35 mg - 40 mg/ kg body-weight/ day, in 3 divided doses

Giardiasis:

Adults: oral dose of 250 mg (1 tablet) x 3 times daily for 5 - 7 days or 2 g as a single dose daily for 3 days.

Children: oral dose of 15 mg/ kg body-weight/ day, in 3 divided doses, for 5 - 10 days.

Treatment of most anaerobic bacterial infections:

Colitis due to antibiotics: oral dose of 500 mg (2 tablets) x 3 - 4 times daily.

Ulcerative gastroduodenitis due to H. pylori: oral dose of 500 mg (2 tablets) x 3 times daily.

Or as directed by the physician.

CONTRAINDICATIONS:

Known hypersensitivity to metronidazole or other nitro-imidazole derivatives.

SPECIAL WARNINGS AND PRECAUTIONS FOR USE:

Metronidazole appears to inhibit alcohol dehydrogenase and other alcohol oxidizing enzymes; therefore, it is unadvisable to take alcohol during treatment.

Blood formula should be monitored in case of long-term treatment.

Excipient:

Lactose monohydrate: Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

USE IN PREGNANCY AND LACTATION:

The drug should not be used in the first trimester of pregnancy. It is advised to stop breast-feeding while taking metronidazole.

EFFECTS ON ABILITY TO DRIVE AND USE MACHINES:

Cautions should be taken when driving vehicles, operating machinery, working at height, and other cases.

INTERACTIONS:

Metronidazole has been reported to potentiate the effect of anticoagulant (warfarin) and nondepolarizing muscle relaxants (vecuronium).

Disulfiram-like reaction may occur if alcohol is consumed during and following metronidazole therapy.

Patients receiving phenobarbital metabolise metronidazole at a much greater rate than normally.

Metronidazole therapy has been associated with elevation of serum lithium.

UNDESIRABLE EFFECTS:

The adverse reactions reported in patients treated with metronidazole have been nausea, vomiting, anorexia, colic, diarrhea, unpleasant metallic taste (all these symptoms will disappear after discontinuation of treatment).

Light leukopenia.

Rarely: headache, skin rash, pruritus, darkened urine.

OVERDOSE:

Single oral doses of metronidazole up to 15 g, have been reported. Symptoms reported include nausea, vomiting, and ataxia.  Neurotoxic effects, including seizures and peripheral neuropathy, have been reported after 5 to 7 days of doses of 6 to 10.4 g every other day. Treatment: There is no specific antidote for metronidazole overdose; therefore, management of the patient should consist of symptomatic and supportive therapy.

PHARMACODYNAMIC PROPERTIES:

ATC code: J01XD01

Metronidazole is a 5-nitroimidazole derivative with broad-spectrum activity against protozoa e.g. amoeba, Giardia, and anaerobic bacteria. In the parasite, the 5-nitro group is reduced to get intermediate substances being toxic to cells. These substances are linked to spiral structure of DNA to break these fibers, and finally kill the cells.

Metronidazole is very effective in treatment of protozoa infections e.g. Entamoeba histolytica, Giardia lamblia, and Trichomonas vaginalis. Metronidazole is bactericidal against Bacteriodes, Fusobacterium, and other obligately anaerobic bacteria, but inactive against aerobic bacteria.

PHARMACOKINETIC PROPERTIES:

Metronidazole is rapidly and completely absorbed after oral administration. Approximately 10 - 20% of metronidazole bound to plasma protein. Metronidazole is widely distributed into most body tissues and fluids, including saliva and breast milk. Concentrations of metronidazole also is attained in cerebrospinal fluid. Metronidazole is metabolized in the liver to hydroxy- and acid-form metabolites; so dosage should be reduced in patient with hepatic impairment to avoid accumulation. A part of metronidazole is excreted in urine as a glucuronide. The metabolites still have somewhat their pharmaceutical effects.

PRESENTATIONS: Box of 10 blisters x 10 tablets.        

SHELF-LIFE: 24 months from the manufacturing date.

STORAGE CONDITIONS: Store in dry places, not exceeding 30⁰C, protect from light.

SPECIFICATIONS: Vietnamese Pharmacopoeia.