Araqal

Araqal Uses, Dosage, Side Effects, Food Interaction and all others data.

A 4-aminoquinoquinoline compound with anti-inflammatory properties.

Amodiaquine, a 4-aminoquinoline similar to chloroquine in structure and activity, has been used as both an antimalarial and an anti-inflammatory agent for more than 40 years. Amodiaquine is at least as effective as chloroquine, and is effective against some chloroquine-resistant strains, although resistance to amodiaquine has been reported. The mode of action of amodiaquine has not yet been determined. 4-Aminoquinolines depress cardiac muscle, impair cardiac conductivity, and produce vasodilatation with resultant hypotension. They depress respiration and cause diplopia, dizziness and nausea.

Artesunate is a potent and rapidly-acting blood schizontocide derived from the leaves of the chinese herb, Armesia annua. The exact mode of action is not clear but clinical studies have confirmed the effectiveness of artesunate in P. vivax and falciparum malaria.

Artesunate is an artemisinin derivative that is metabolized to DHA, which generates free radicals to inhibit normal function of Plasmodium parasites. It has a short duration of action due to its short half life, and a moderate therapeutic index. Patients should be counselled regarding the risk of post treatment hemolytic anemia and hypersenstivity.

Araqal
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Araqal
Generic	Amodiaquine + Artesunate
Weight	67.5mg, 25mg, 135mg, 50mg, 270mg, 100mg
Type	Tablet
Therapeutic Class
Manufacturer	Hilton Pharma (pvt) Limited
Available Country	Pakistan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Amodiaquine is an antimalarial drug.

For treatment of acute malarial attacks in non-immune subjects.

Artesunate can quickly and reliably control the acute attack of malaria. It is suitable to salvage the patients with pernicious malaria and treat P. falciparum malaria and P. vivax malaria. It is effective against malaria caused by chloroquine resistant strain of plasmodium falciparum.

Araqal is also used to associated treatment for these conditions: Acute Uncomplicated Plasmodium Falciparum Malaria, Malaria, Cerebral, Severe Malaria

How Araqal works

The mechanism of plasmodicidal action of amodiaquine is not completely certain. Like other quinoline derivatives, it is thought to inhibit heme polymerase activity. This results in accumulation of free heme, which is toxic to the parasites. The drug binds the free heme preventing the parasite from converting it to a form less toxic. This drug-heme complex is toxic and disrupts membrane function.

Artesunate is metabolized to the active DHA. the endoperoxide bridge of DHA reacts with heme, generating free radicals which inhibit protein and nucleic acid synthesis of the Plasmodium parasites during all erythrocytic stages. Reactions with these free radicals can also lead to alkylation of parasitic proteins such as a calcium adenosine triphosphatase and EXP1, a glutathione S-transferase.

Dosage

Araqal dosage

Adult: 5 days treatment: on the 1st day 2 tablets twice and 2nd day onward 1 tablet twice daily for remaining 4 days

Children:

1-3 years: 5 days treatment: on the 1st day ½ tablet twice and 2nd day onward ¼ tablet twice daily for remaining 4 days
4-5 years: 5 days treatment: on the 1st day 1 tablet twice and 2nd day onward ½ tablet twice daily for remaining 4 days
6-12 years: 5 days treatment: on the 1st day ½ tablet twice, 2nd day 1 tablet twice and 3rd day onward ½ tablet twice daily for remaining 3 days

Prophylmcis: 100 mg tablet once a week, from 1 week before entering malarial areas, to 4 weeks after leaving the area.

Side Effects

Transient and reversible reticulocytopaenia, drug fever, rash, bradycardia, transient 1st-degree heart block and reversible elevation of serum transaminases.

Toxicity

LD₅₀ (mouse, intraperitoneal) 225 mg/kg, LD₅₀ (mouse, oral) 550 mg/kg. Symptoms of overdose include headache, drowsiness, visual disturbances, vomiting, hypokalaemia, cardiovascular collapse and cardiac and respiratory arrest. Hypotension, if not treated, may progress rapidly to shock. Electrocardiograms (ECG) may reveal atrial standstill, nodal rhythm, prolonged intraventricular conduction time, broadening of the QRS complex, and progressive bradycardia leading to ventricular fibrillation and/or arrest.

Data regarding overdoses of artesunate are rare. Patients experiencing an overdose may present with pancytopenia, melena, seizures, multiorgan failure, and death. Treat overdose with symptomatic and supportive measures.

Precaution

Hepatic or renal insufficiency; Pregnancy and lactation.

Interaction

Antimalarial potentiating action seen with mefloquine, primaquine and tetracycline. Additive effect with chloroquine. Antagonistic effect with pyrimethamine and sulphonamides.

Volume of Distribution

The volume of distribution of artesunate is 68.5L while the volume of distribution of DHA is 59.7L.

Elimination Route

Rapidly absorbed following oral administration.

The C_max of artesunate is 3.3µg/mL while the C_max of the active metabolite DHA is 3.1µg/mL. The AUC of artesunate is 0.7µg*h/mL while the AUC of DHA is 3.5µg*h/mL. After intravenous artesunate, DHA has a T_max of 0.5-15 minutes in adult patients and 21-64 minutes in pediatric patients. Intramuscular artesunate has a T_max of 8-12 minutes. Infants less than 6 months old will have a higher AUC due to an undeveloped UGT metabolic pathway.

Half Life

5.2 ± 1.7 (range 0.4 to 5.5) minutes

The elimination half life of artesunate is 0.3h with a range of 0.1-1.8h. The elimination half life of DHA is 1.3h with a range of 0.9-2.9h. Half life after intramuscular administration is 48 min in children and 41 min in adults.