Dosing and uses of Aralen, Chloroquine phosphate (chloroquine)
Adult dosage forms and strengths
tablet
- 250mg
- 500mg
Malaria
Prevention: 500 mg (300 mg base) PO once/week
Non-chloroquine-resistant
- 1 g (600 mg base) PO, THEN
- 500 mg (300 mg base) PO 6-8 hours later, THEN
- 500 mg (300 mg base) PO at 24 hours & 48 hours after initial dose
Amebiasis, Extraintestinal
1 g (600 mg base) PO qDay for 2 days, THEn
500 mg (300 mg base) qDay for 14-21 days
Porphyria Cutanea Tarda (Off-label)
125-250 mg (75-150 mg base) PO twice weekly
Glioblastoma (Orphan)
Orphan designation for treatment of glioblastoma multiforme
Sponsor
- DualTpharma B.V.; Boschstraat 111-D01; 6211 A W Maastricht; Netherlands
Pediatric dosage forms and strengths
tablet
- 250mg
- 500mg
Malaria
Prophylaxis: 5 mg/kg PO q1Week
Treatment
- 1st dose: 10 mg/kg PO x1 dose
- 6 hours after 1st dose: 5 mg/kg PO qDay x2 days
Porphyria Cutanea Tarda (Off-label)
Dosing schedules not well established in children
Case reports describe dosage regimens that are effective yet tolerated, such as 12.5 mg PO twice weekly over 2 yr in a child aged 4-6 yr, and 100 mg PO twice weekly over 5 months in a child aged 12 yr; mg/kg dosing not reported
Aralen, Chloroquine phosphate (chloroquine) adverse (side) effects
Frequency not defined
Abnormal ECg
Prolonged QT intervaL
Amnesia
Pruritus
Diarrhea,
Loss of appetite
Nausea
Stomach cramps
Vomiting
Methemoglobinemia (rare)
Muscle weakness
Retinopathy
Warnings
Black box warnings
Physicians should completely familiarize themselves with the complete contents of the package insert before prescribing chloroquine phosphate
Contraindications
Hypersensitivity to chloroquine, 4-aminoquinolones
Psoriasis, porphyria, retinal or visual field changes
Cautions
For prevention, may use proguanil concomitantly
Chloroquine not effective in most areas; CDC recommends mefloquine or atovaquone/proguanil - check CDC traveler information for specific recommendations for region
Caution with G-6-PD deficiency
Monitor CBC periodically with prolonged therapy
Caution with history of auditory damage
Caution with hepatic disease, alcoholism, and coadministration with other hepatotoxic drugs
May provoke seizures in patients with history of epilepsy
Antacids and kaolin reduce chloroquine absorption; separate administration by at least 4 hr
Retinopathy/maculopathy, as well as macular degeneration reported; irreversible retinal damage has been observed in patients who have received long-term or high-dosage 4-aminoquinoline therapy
May exacerbate heart failure
Pregnancy and lactation
Pregnancy category: not available
Lactation: enters breast milk/not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Aralen, Chloroquine phosphate (chloroquine)
Mechanism of action
Active against erythrocytic forms of Plasmodium vivax & P. malariae and most strains of Plasmodium falciparum
Precise mechanism not known
Absorption
Bioavailability: ~89%
Peak plasma time: 1-2 hr
Distribution
Distributed widely in body tissues (eg, eyes, heart, kidneys, liver, lungs) where retention prolonged; crosses placenta; enters breast milk
Metabolism
Partially in liver
Elimination
Half-life: 3-5 days
Excretion: urine (~70% as unchanged drug); acidification of urine increases elimination
Small amounts may be present in urine months following discontinuation of therapy
