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Oxamniquine

'Oxamniquine' is "an anthelmintic with schistosomicidal activity against Schistosoma mansoni, but not against other Schistosoma spp. Oxamniquine causes worms to shift from the mesenteric veins to the liver where the male worms are retained; the female worms return to the mesentery, but can no longer release eggs. (From Martidale, The Extra Pharmacopoeia, 31st ed, p121)" more...

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History

In 1979, Pfizer at Sandwich was presented with the Queen’s Award for Technological Achievement in recognition of the outstanding contribution made to tropical medicine by MANSIL™ (oxamniquine).

Pharmacokinetics

Peak plasma concentrations are achieved 1 to 3 hours after a dose and the plasma half-life is 1 to 2.5 hours.

It is extensively metabolised to inactive metabolites, principally the 6-carboxy derivative, which are excreted in the urine. About 70% of a dose of oxamniquine is excreted as the 6-carboxy metabolite within 12 hours of a dose; traces of the 2-carboxy metabolite have also been detected in the urine.

Mode of Action

Is a semisynthetic tetrahydroquinoline and possibly acts by DNA binding resulting in contraction and paralysis of the worms and eventual detachment from terminal venules in the mesentry and death.

Uses

For treatment of schistomiasis. According to one systematic review it is equally effective as praziquantel (for treating S. mansoni).

Contraindications and Precautions

Pregnancy

Side Effects

It is generally well tolerated following oral doses. Dizziness with or without drowsiness occurs in at least a third of patients, beginning up to 3 hours after a dose and usually lasting for up to 6 hours. Headache and gastrointestinal effects such as nausea, vomiting, and diarrhoea are also common.

Allergic-type reactions including urticaria, pruritic skin rashes, and fever may occur. Liver enzyme values have been raised transiently in some patients. Epileptiform convulsions have been reported, especially in patients with a history of convulsive disorders. Hallucinations and excitement have occurred rarely.

A reddish discoloration of urine, probably due to a metabolite of oxamniquine, has been reported.

Dosage

Oral, 15 mg per kg of body weight two times a day for one day.

Brandnames

Vansil; (Pfizer) 250 mg capsules, syrup 250 mg/5ml
Mansil; 250 mg Tablets

External References

AHFS Database

Read more at Wikipedia.org

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Immune humoral response to circulating antigens of Schistosoma mansoni in mice experimentally infected before and after ozamniquine treatment
From Revista do Instituto de Medicina Tropical de Sao Paulo, 3/1/01 by Garcia, Eliane Timoteo

The dynamics of the IgM and IgG antibody response to S. mansoni circulating antigens was studied in three groups of S. mansoni infected mice (60-80 cercariae/animal), before and after chemotherapy. Two groups were treated with oxamniquine (100 mg/kg) and the third one was kept with no treatment. One group without infection was followed as a negative control.

The IgG and IgM reactivity patterns against different antigenic structures on worm sections was studied by immunofluorescence test. The presence of IgM and IgG antibodies reacting to gut antigens started to be observed from the 21 week of infection peaking up between 8 and 12 weeks. In successfully treated animals no antibodies were detected at the end of the experiment. Some mice of the second treated group showed eggs in the fecal examination, after chemotherapy, but tendency to decay of antibody levels was also observed.

By the Elisa test, the IgG antibody levels to total worm antigens and IgM to TCA-soluble fraction showed tendency to decrease in the first treated group. In the animals of the second group, with S. mansoni eggs in the feces after treatment, a drop of IgM antibodies to TCA-soluble fraction was observed but not of IgG against total worm antigens.

The results of Immunoblotting showed an intense reactivity of the IgG antibodies against 31/32 adult worm fraction starting around the 6th week of infection; some mice showed negative results and for some decay after treatment was observed. The reactivity of the IgM antibodies, observed as a diffuse band against a fraction with high molecular weight, corresponding to the circulating anodic antigen (CAA), showed no tendency to decay in most of the treated animals.

Antibodies against S. mansoni gut antigens were observed in animals infected with other parasite species, mainly with Toxocara canis. This must be better investigated to understand the significance of the cross reactivities among the different helminth species, and evaluate the use of these tests that detect antibodies against gut associated circulating antigens as a diagnostic tool in schistosomiasis.

GARCIA, Eliane Timoteo - Dinamica da resposta imune humoral contra antigenos circulantes de Schistosoma mansoni no modelo experimental em camundongos pre c pos tratamento com oxamniquine. Sao Paulo, 2000. (Dissertacao de mestrado - Faculdade de Ciencias Farmaceuticas da Universidade de Sao Paulo)

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