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Alice M. Jenh, Pharm.D. and Paul A. Pham Pharm.D.
05-18-2011
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Available formulations in Zambia: oral tablet: 20 mg artemether/120 mg lumefantrine (adult formulation); 10 mg artemether/60 mg lumefantrine(pediatric formulation)
- Preferred treatment for uncomplicated P. falciparum malaria.
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LPV/r increased lumefantrine AUC by 193%, but co-administration was well tolerated.
- Artemether serum concentrations may also be increased with PI co-administration.
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Rifampicin, EFV, and NVP may decrease artemether and lumefantrine serum concentrations. Monitor closely for anti-malarial activity with co-administration. Artemether with lumefantrine may need to be increased.
- Should be administered with food containing at least 1.3 g of fat.
Zambia Information Author: Alice M. Jenh, Pharm.D. and Paul A. Pham Pharm.D.
- Falciparum malaria, uncomplicated disease in geographic areas of known chloroquine resistance.
- Not approved for patients with severe or complicated P. falciparum malaria.
- Not approved for the prevention of malaria.
- No data in complicated falciparum malaria
- Vivax malaria: Limited efficacy observed in one Thai study: rapid parasite clearance observed with 4-dose regimen, relapse was common, suggesting minimal activity against the hypnozoite stage of P. vivax (Karbwang et al, 2000).
brand
name
| generic
| Mfg
| brand
forms
| cost*
|
| Coartem | artemether / lumefantrine | Novartis Pharmaceuticals Corp. | Oral
tab
20 mg (artemether)/120 mg (lumefantrine) | $3.63 |
*Prices represent cost per unit specified and are representative of "Average Wholesale Price" (AWP).
AWP Prices were obtained and gathered by Lakshmi Vasist Pharm D using the Red Book, manufacturer's
information, and the McKesson database.
^Dosage is indicated in mg unless otherwise noted.
- Fixed-dose 20mg artemether/120mg lumefantrine tablet formulation: 4-dose regimen over 48 hours is now considered inferior; 6-dose regimen over 3 or 5 days is superior and recommended (van Vugt et al, 1999).
- Uncomplicated Falciparum malaria; adults (>35 kg): 6-dose regimen over 3 days (4 tablets/dose at 0, 8, 24, 36, 48, and 60 hours)
- Weight-based dosing: artemether-lumefantrine 1 tab stat, then 8 hours later, followed by 1 tab bid x 2 days (total course=6 tabs for 5kg to <15kg); Artemether-lumefantrine 2 tab stat, then 8 hours later, followed by 2 tab bid x 2 days (total course=12 tabs for 15 kg to <25kg); Artemether-lumefantrine 3 tab stat, then 8 hours later, followed by 3 tab bid x 2 days (total course=18 tabs for 25 kg to <35kg); Artemether-lumefantrine 4 tab stat, then 8 hours later, followed by 4 tab bid x 2 days (total course=24 tabs for 35kg to <65kg); >65kg limited experience, but consider Artemether-lumefantrine 4 tab stat, then 8 hours later, followed by 4 tab bid x 2 days with close monitoring
- Should be administered with food containing at least 1.3 g of fat.
- Tablet may be crushed and disolved in 5-10ml of water.
Usual dose
Limited data. Usual dose likely.
Limited data . Usual dose likely.
No data. On days of dialysis, dose post-HD.
No data.
No data. Not recommended in the treatment of severe malaria.
- Generally well tolerated with only 1.1% discontinuation ratedue to adverse drug reactions.
- Rash, pruritis
- Nausea and vomiting (generally within 1 hour of 1st dose), abdominal pain, anorexia, and diarrhea
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Anemia
- Myalgias
- Dizziness, headache, asthenia, insomnia
- Cough
- Hemolytic anemia
- Increased QTc interval (maximum mean change 7.5 msec), modest ST-elevations. Avoid in patients with baseline QTc prolongation.
- Nystagmus, abnormal gait, paresthesias, tremor
Both artemether and lumefantrine are CYP450 3A4 substrates. Inhibitors and inducers of CYP3A4 may affect artemether's and lumefantrine's serum concentrations. Artemether may induce CYP3A4/5. CYP2D6 may be inhibited.
- Aurothioglucose: Increased risk of blood dyscrasias. Avoid aurothioglucose co-administration.
- Halofantrine: may increase risk of QTc prolongation. Avoid halofantrine co-administration.
- Manufacturer recommends against the co-administration of artemether/lumefantrine with the following drugs that may prolong QTc: antiarrhythmics, such as amiodarone, disopyramide, flecainide, procainamide, sotalol, and quinidine; antibacterials, such as macrolides and quinolones; antidepressants (imipramine, amitriptyline, clomipramine); antifungals such as imidazoles and triazoles; terfenadine; other antimalarials; antipsychotic drugs (droperidol, pimozide and ziprasidone); . However, there is no evidence that co-administration with these drugs would be harmful. (WHO guidelines for the treatment of malaria. 2006.)
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Rifampicin, efavirenz,,nevirapine, phenobarbital, phenytoin, and carbamazepine, may decrease artemether and lumefantrine serum concentrations. Monitor closely for anti-malarial activity with co-administration.
- HIV-protease inhibitors may increase artemether and lumefantrine serum concentrations. Consider EKG monitoring for QTc prolongation.
- Grapefruit juice: may increase artemether and lumefantrine serum concentrations. Avoid
- Oral contraceptive: may reduce the effectiveness of hormonal contraceptives. Use an additional barrier form of contraception.
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Plasmodium falciparum (Chloroquine-resistant)
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Plasmodium vivax (requires additional treatment with other antimalarial agents to eradicate hypnozoites forms that may remain dormant in the liver)
- Artemisinin-based combination therapy (ACT) is currently the WHO recommended treatment of choice for the treatment of uncomplicated falciparum malaria: based on the level of resistance, in Africa, artemether-lumefantrine and artesunate + amodiaquine are the ACTs of choice; Amodiaquine + sulfadoxine-pyrimethamine may be considered as an interim option in situations where ACTs cannot be made available. Fixed artemether/lumefantrine is not indicated in the treatment of complicated falciparum malaria or Plasmodium vivax malaria.
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