PHARMACOLOGY

Pharmacotherapeutic Group:Amoebicide/ Anti parasitic Agent

 Pharmacodynamic Properties:

Metronidazole:

Metronidazole exerts antimicrobial effects in an anaerobic environment. The 5 nitro group undergoes reductive transformation to an active intermediate which then exerts an inhibitory effect against DNA. The reduced metabolite also causes a loss of the helical structure of DNA with subsequent DNA strand breakage.

Pharmacokinetics:

Metronidazole is well absorbed with peak plasma concentrations occuring between one and two hours after administration. Less than 20% of circulating Metronidazole is bound to plasma proteins. The major route of elimination of Metronidazole and its metabolites is via urine.

Diloxanide furoate:

Diloxanide furoate is a luminal amoebicide acting principally in bowel lumen and is used in the treatment of intestinal amoebiasis. Diloxanide furoate is given alone in the treatment of asymptomatic cyst-passers and in conjunction with an amoebicide that acts in the tissues such as metronidazole in patients with invasive amoebiasis.

Pharmacokinetics:

Diloxanide furoate is hydrolized into diloxanide and furoic acid before being absorbed. Diloxanide is readily absorbed from gastrointestinal tract.

 INDICATIONS

Acute and chronic amoebiasis, dysentry, giardiasis

 DOSAGE & ADMINISTRATION

Adults: 1 tablet three times daily for 5 days.

Children:

Below 5 years: 5ml three times daily for 5 days

5 to 12 years: 10ml three times daily for 5 days.

The treatment may be extended depending the patient condition.

ADVERSE DRUG REACTIONS

Seizures, headache, dizziness, peripheral neuropathy, unpleasant metallic taste, furred tongue, gastrointestinal disturbances, rashes, urticaria, pruritus, raised liver enzymes values, flatulence, nausea

 PRECAUTIONS

Renal and hepatic impairment, avoid alcohol

 DRUG INTERACTIONS

Acute Psychosis with disulfiram, synergistic effect with other antimicrobials. Enhances action of coumarin anticoagulants. Blood levels increased by cimetidine. Effect reduced by phenobarbitone

 CONTRAINDICATIONS

Hypersensitivity, blood dyscrasias, active central nervous disease (CNS), serious neurological disease, seizure, hepatic failure, first trimester pregnancy, lactation.

PRESENTATION

METDIL: Each box contains 20 Blister of 10 Tablets per strip

METDIL SUSPENSION: Each bottle contains 50ml of suspension