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Arinate

Reals Pharmaceuticals Limited
Plot 1 Junaid Dosunmu Street,Central Business District, Alausa, P.0. Box 3560 Ikeja, Lagos, Nigeria.
Email: reals@realsgroup.com
Tel: + 234-1-774-1205
Fax: +234-1-263-0919
Website: http://realsgroup.com

Brand Name

Arinate

Manufacturer

Dafra Pharma nv/sa, Slachthuisstraat 30 Bus 7, 2300 Turnhout, Belgium

Therapeutic Class

Antimalarial drugs

Dosage Form, Composition & NAFDAC Registration Number (NRN)

Tablet (NRN: 04-7732): Each scored tablet contains: Artesunate 100 mg. Excipients: Lactose monohydrate, microcrystalline cellulose, croscaramellose, anhydrous colloidal silica, magnesium stearate.

Pack size: Box of 6 blister-packed tablets.

Tablet (NRN: 04-7884): Each scored tablet contains: Artesunate 50 mg. Excipients: Lactose monohydrate, microcrystalline cellulose, croscaramellose, anhydrous colloidal silica, magnesium stearate.

Pack size: Box with one blister of 6 tablets.

Pharmacology

Artesunate is a typical blood schizontocide, active against all forms of malaria. Artesunate has a peroxide bond releasing inside the parasite singlet oxygen as well as free radicals. Both exert a direct cytotoxic effect on the cells and the subcellular membranes. This forms the essential part of the mechanism of action of Artesunate and explains its rapid effect as well as its efficacy.

Pharmacokinetics: Following oral administration, Artesunate is rapidly absorbed and reaches Cmax within 45 to 90 minutes. The product is metabolised in the liver and by simple hydrolysis or by esterases in the plasma; it gives rise to dihydroartemisinin (DHA) which is also effective against malaria by the same mechanism of action.

Elimination half-life is approx. 1-2 hours and follows urinary and biliary excretion. Protein binding varies in accordance with the species being studied, but tends to be about 50% in man.

Indications

Arinate is indicated for the curative treatment of malaria caused by all forms of plasmodium including severe malaria caused by multiple drug resistant strains of P. falciparium.

In case of an infection caused by P. vivax, recrudescence is common. A combination treatment with Primaquine is recommended.

Contra-indications

Precautions/Warnings

Pregnancy: Use of the product is not recommended during the organogenesis period (first 3 months) except if, in the doctor’s opinion, the potential benefits justify the potential risks to mother and foetus, e.g. in case of complicated or cerebral malaria. No case of human embryotoxicity or teratogenicity has been reported.

Breast-feeding: Artesunate is not known to appear in the breast milk of lactating mothers, but the metabolite DHA may be found.

Interactions

There have been no reports of negative drug interactions to date. The activity of other anti-malarial drugs could be potentiated namely Mefloquine, Amodiaquine and the combinations of Sulfonamides/Pyrimethamine.

Adverse Effects

Undesirable effects are generally rare at the therapeutic dose. In rare cases, however, slight changes to haematological values have been observed, including a reduction of reticulocytes as well as slight increase in transaminases. These signs do not generally give rise to any noticeable clinical manisfestations.

In rare cases, a slight but transient reduction in sinus heart rhythm has been observed. No drug induced electrocardiographic changes have been seen and the QTc interval is not affected.

Abdominal cramps and mild diarrhoea have been reported at elevated doses.

Dosage & Administration

Arinate 100 mg: Adults: 2 tablets (200 mg) as a single starting dose on the first day followed by 1 tablet (100 mg) as a single dose over the next 4 subsequent days. Tablets may be broken or crushed for convenience sake.

Arinate 50 mg: Children: Between 3 and 4 mg/kg bodyweight as a single starting dose on the first day, followed by half the dose, as a single dose, over the next 4 subsequent days. Tablets may be broken or crushed for convenience sake.

Child's Body-weight

Dose (# of tablets)
Day-1 Day-2 Day-3 Day-4 Day-5
8-15 kg 1 ½ ½ ½ ½
16-23 kg ¾ ¾ ¾ ¾
24-30 kg 2 1 1 1 1

Note: In order to ensure complete recovery, the entire course of treatment must be taken. In severe or complicated malaria, it may be necessary to prolong treatment to e.g. for 7 days.

Storage/Handling Recommendations

The tablets should preferably be kept dry and stored at room temperature below 30oC. They should always be kept in their original container.

Review Date

2015-11-19 02:57:58