products-page-bottom-left-box

Co-Arinate and Co-Arinate Junior

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

Co-Arinate and Co-Arinate Junior

Manufacturer

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

Therapeutic Class

Antimalarial drugs

Dosage Form, Composition & NAFDAC Registration Number (NRN)

Tablets (NRN:04-8132): Each containing 200 mg Artesunate. Excipients: Lactose monohydrate, microcrystalline cellulose, croscaramellose, anhydrous colloidal silica, magnesium stearate.

Each containing 500 mg Sulfamethoxypyrazine and 25 mg Pyrimethamine. Excipients: Cornstarch, microcrystalline cellulose, sodium starch glycolate, magnesium stearate and erythrosine sodium.

Pack SizeEach carton box contains 1 blister: Each blister contains 6 tablets

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

Each containing 250 mg Sulfamethoxypyrazine and 12.5 mg Pyrimethamine. Excipients: Cornstarch, microcrystalline cellulose, sodium starch glycolate, magnesium stearate and erythrosine sodium.

Pack SizeEach carton box contains 1 blister: Each blister contains 6 tablets

Pharmacology

Artesunate is a typical blood schizontocide, active against all forms of malaria.

Artesunate has a peroxide bond, which breaks up inside the parasite, forming singlet oxygen as free radicals. Both exert a direct cytotoxic effect on the cells and the subcellular membranes. In addition free radicals are formed and they in turn also exert a toxic action. This forms the essential part of the mechanism of action of Artesunate and explains its rapid effect as well as its efficacy.

Sulfamethoxypyrazine/Pyrimethamine interferes at two levels with the biosynthesis of folic acid essential for the growth and development of the malaria parasites. Sulfamethoxypyrazine/Pyrimethamine act as an antimalarial agent and has a long lasting effect [long elimination half life].

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.

Both the sulfamethoxypyrazine and the pyrimethamine from the combination tablet are well absorbed orally and are excreted mainly by the kidney. Following administration of a single tablet, Sulfamethopyrazine Cmax is achieved in 1.5-8 hours. The apparent half-life of elimination of sulfamethoxpyrazine will be around 65 hours, whereas pyrimethamine half-life ranged from 54 to148 hours. Sulfamethoxypyrazine is protein bound for 60%, pyrimethamine for 87%. Both drugs appear in breast milk of lactating mothers.

Indications

Co-Arinate is indicated for the curative treatment of malaria caused by all forms of plasmodium including severe malaria caused by multiple drug resistance 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

Since sulfamethoxypyrazine is excreted by the kidney, adequate fluid intake must be maintained in order to prevent crystalluria provoked by urinary excretion of sulfamethoxypyrazine and its metabolites.   

Patients taking this combination therapy should be warned that they should stop use of Sulfamethoxyphrazine/Pyrazine and seek medical attention immediately at the first appearance of any skin rash. An adequate diuresis should be maintained. Patients should also be warned that the appearance of arthralgia, pallor, purpura or jaundice could be early indications of serious disorders, which would require emergency treatment.

We have to take in consideration that Sulfamethoxyprazine/Pyrethamine, due to the presence of a sulphonamide, possibly can cause blood dyscrasis such as thrombocytopenia, purpura, leukopenia, neutropenia or seldom agranulocytosis, which are reversible when treatment ceases. Should any of these complications be suspected, specialized medical treatment in a hospital setting is required.

Special precautions should be taken in treating patients with condition predisposing to deficiency of folic acid. Patients should be warned not to administer this combination therapy to children less than 2 months of age because of inadequate development of the glucuronide-conjugating enzyme system.

Undesirable effects from Artesunate are generally rare at the therapeutic dose. In very rare cases, however, slight changes in haematology values have been seen, including a reduction in the number of reticulocytes as well as a slight increase in transaminases. These signs, however, do not generally give rise to any noticeable clinical manifestations. In rare cases, a slight, but transcient, reduction in sinus heart rhythm has been observed. Although no drug induced electrocardiographic changes have been seen and the QTc intervals is not affected.

Abdominal cramps and mild diarrhoea have been reported at elevated doses

Interactions

Adverse reactions which may increase in incidence and severity, when chloroquine is used together with Sulfamethoxyprazine/Pyrethamine, have been reported.

Sulfathoxyphrazine/Pyrethamine is compatible with quinine and with antibiotics. The same applies to Artesunate.

Antifolic acid drugs such as other sulfonamides or trimethoprim-sulfamethethoxazole combination should, however, not be used while the patient is receiving Sulfamethoxpyrazine/Pyrethamine for antimalaria treatment. Sulfamethoxypyrazine/Pyrimethamine has not been reported to interfere with anti-diabetic agents

No adverse drug interactions with Artesunate have been reported to date. The activity of other anti-malarial drugs may in fact, be potentiated by Artesunate.

Adverse Effects

Side effects caused by Artesunate are uncommon and restricted to a transient rise in transaminases; reduced reticulocyte count, and rare cases of dizziness have been reported. Artesunate does not affect the cardiovascular system but a slight slowing of sinus frequency has been noticed. No effects on wave or on QTc interval have been found.

Dosage & Administration

Co-Arinate: Adults (40-80 kg):

Day 1: 1 tablet (200 mg) Artesunate together with the 1 Sulfamethoxypyrazine/Pyrimethamine tablet.

Day 2: 1 tablet (200 mg) Artesunate together with the 1 Sulfamethoxypyrazine/Pyrimethamine tablet.

Day 3: 1 tablet (200 mg) Artesunate together with the 1 Sulfamethoxypyrazine/Pyrimethamine tablet.

 

Co-Arinate Junior: Adolescents and children (20-39 kg):

Day 1: Artesunate 4 mg/kg body weight as a single dose (1 tablet) together with 1 Sulfamethoxypyrazine/Pyrimethamine tablet.

Day 2: Artesunate 4 mg/kg body weight as a single dose (1 tablet) together with 1 Sulfamethoxypyrazine/Pyrimethamine tablet.

Day 3: Artesunate 4 mg/kg body weight as a single dose (1 tablet) together with 1 Sulfamethoxypyrazine/Pyrimethamine tablet.

Tablets may be broken or crushed for convenience. Do not exceed the recommended dose without seeking medical advice.

N.B.: In order to ensure complete recovery, the entire course of treatment must be taken.

Storage/Handling Recommendations

store in a cool dry place out of the reach of children.

Review Date

2016-02-16 08:11:46