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Azmetrin Tablet

Agary Pharmaceutical Limited
Plot C39A, Amuwo Odofin Commercial Scheme, Along Alakoso Avenue, Amuwo Odofin, Lagos.
Email: agarypharm@gmail.com
Tel: 0809-275-6424, 0809-275-6425, 0808-745-4848.
Website: http://agarypharm.com/

Brand Name

Azmetrin Tablet

Manufacturer

Norris Medicines Limited,
plot No. 901/4-5, G.I.D.C. Estate Ankleshwar-393 002. (GUJ), India.

Therapeutic Class

Antimalarial drugs

Dosage Form, Composition & NAFDAC Registration Number (NRN)

Tablet (NRN:B4 4015): Artemether 20 mg, Lumefantrine 120 mg; yellow cross scored tablet.

Pack size: 4 x 6’s (in blisters)

Azmetrin   20   3

Pharmacology

PHARMACOLOGICAL PROPERTIES

Artemether is the most active derivative of the Artemisinin, a new class of anti-malarial drugs derived from Artemisinin. The latter compound is extracted from the plant Artemisia Annua and Artemether is prepared semi-synthetically.

PHARMACODYNAMIC PROPERTIES

Both components of Azmetrin have their own action site in the malaria parasite. The presence of the endoperoxide bridge in Artemether (generating singlet oxygen and free radicals: these are very cytotoxic to the plasmodia) appears to be essential for antimalarial activity. Morphological changes of the parasitic membranes induced by Artemether have been described, being the result of free- radical action.

Lumefantrine interferes most in the polymerization processes. Other in vitro test suggests that both cause a marked diminution of nucleic acid synthesis. Inhibition of protein synthesis as the basic mechanism of action is suggested in studies, which showed morphological changes in ribosomes as well as in the endoplasmic reticulum. Although Artemether acts essentially as a blood schizonticide, Azmetrin did clear gametocytes in comparative clinical trials.

PHARMACOKINETIC PROPERTIES

Orally administered Artemether is rapidly absorbed reaching therapeutic level within 60-90 minutes; Artemether is metabolized in the liver to the demethylated derivative dihydroartemisinin. (DHA).

The elimination is rapid, with a T½ of 2-4 hours. Dihydroartemisinin, being a potent antimalarial itself, has a T½ of about 2-4 hours. The degree of binding to plasma proteins varied markedly according to the species studied. The binding of Artemether with plasma protein in man is about 50%. Radioactivity distribution of Artemether is found to be equal between cells and plasma.

The absorption of lumefantrine is highly influenced by lipids and food intake (from 10% by fasting to 100% at normal diet). Therefore, patients should be encouraged to give the medication with some fatty food as soon as it can be tolerated. Lumefantrine is N-debutylated in human in liver microsomes.

This metabolite has 5 to 8 fold higher antiparasitic effects than Lumefantrine. Lumefantrine is found to be highly protein bound (95%). The elimination half-life in malaria patients will be 4 to 6 days. Lumefantrine and its metabolities are found in bile and faeces.

Indications

Azmetrin is indicated for the treatment of adults and children with acute, uncomplicated infections due to Plasmodium falciparum or mixed infection including P. falciparum and strains from multi-drug resistant areas.

Contra-indications

Azmetrin is contraindicated in:

• Hypersensitivity to artemether, lumefantrine or to any of the excipients of Azmetrin.

• Patients with severe malaria according to WHO definition.

• First trimester of pregnancy

• Patients with a family history of congenital prolongation of the QTc interval or sudden death or with any other clinical condition known to prolong the QTc interval such as patients with a history of symptomatic cardiac arrhythmias, with clinically relevant bradycardia or with severe cardiac disease.

• Patients with known disturbances of electrolyte imbalance e.g hypokalaemia or hypomagnesaemia. Patients taking any drug, which is metabolised by the cytochrome enzyme CYP206 (e.g flecainde, metorprolol, imipramine, amitriptyline, clomipramine)

• Patients taking drugs that are known to prolong the QTc interval such as antiarrhythmics of classes IA and III, neuoleptics, and antidepressive agents.

Precautions/Warnings

• Prolongation of the QT-interval. Azmetrin may prolong the QTc interval and increase the risk of cardiac arrhythmias.

• It is advisable to avoid the use of drugs during pregnancy. It must not be used in first Trimester of Pregnancy.

• Azmetrin should not be taken during breast-feeding. Due to long elimination half-life of Lumefantrine, it is recommended that breast-feeding should not start until at least one week after stopping an Artemether/Lumefantrine combination.

• Azmetrin should be taken with high-fat food or drinks such as milk. Patients should be encouraged to resume normal eating as soon as food can be tolerated since this improves absorption of artemether and Lumefantrine.

• In the event of vomiting within 1 hour of administration, a repeat dose should be taken.

Interactions

• It has interactions with other antimalarials, CYP450 3A4 inhibitors, Protease Inhibitor and anti-retroviral Drugs.

• Grapefruit juice inhibits the metabolism of some antimalarials , it is not advisable to drink grape juice while taking Azmetrin.

Adverse Effects

• Patients previously treated with antimalarials which can influence the ECG pattern e.g. Halofantrine and quinine, should be given a reasonable period of time before starting treatment with Azmetrin.

• Common side effects which may occur include: dizziness, anorexia, nausea, vomiting, diarrhea, coughing and rashes.

Dosage & Administration

Azmetrin-20 is designed for use in children and adults

Table: The dosage instructions for children and adults

Azemtrin-20

Patient weight/
Time interval

Day 1 Day 2 Day 3
0 Hour 8 hours after
the first dose
24 hours after
the first dose
12 hours after
the third dose
12 hours after
the fourth dose
12 hours after
the fifth dose
5 to ≤ 15 kg 1 tab. 1 tablet 1 tablet 1 tablet 1 tablet 1 tablet
15 to ≤ 25kg 2 tabs. 2 tablets 2 tablets 2 tablets 2 tablets 2 tablets
25 to ≤ 35kg 3 tabs. 3 tablets 3 tablets 3 tablets 3 tablets 3 tablets
35 Kg and above 4 tabs. 4 tablets 4 tablets 4 tablets 4 tablets 4 tablets

To increase absorption, Azmetrin should be taken with food or a milky drink (see section 5.2). If patients are unable to tolerate food, Azmetrin should be administered, but the systemic exposure may be reduced. Patients who vomit within 1 hour of taking the medication should repeat the dose. For administration to small children and infants, the dry syrup or dispersible tablets should be dissolved in water.

Renal or hepatic impairment

No dose adjustments are necessary in patients with renal or hepatic impairment. However, caution is advised when administering Azmetrin to patients with severe renal or hepatic problems.

Elderly

No special precautions or dosage adjustments are necessary in such patients.

Overdose

Experience of overdosage with artemether and lumefantrine is limited. In cases of suspected overdosage symptomatic and supportive therapy should be given as appropriate, which should include monitoring of ECG and serum electrolytes.

Storage/Handling Recommendations

Azmetrin-20 should be stored below 30°C away from light and humidity.

Azmetrin-20 should not be used after the date marked ”EXP Date“ on the pack.

Keep out of reach and sight of children.

Review Date

2017-08-26 05:32:21