Buy Aralen Online

Chloroquine (chloroquine phosphate)

OTHER BRAND NAMES

Aralen (Discontinued)

THERAPEUTIC CLASS

Aminoquinoline

DEA CLASS

RX

INDICATIONS

Suppressive treatment and for acute attacks of malaria due to Plasmodium vivaxPlasmodium malariaePlasmodium ovale, and susceptible strains of Plasmodium falciparum. Treatment of extraintestinal amebiasis.

ADULT DOSAGE

Malaria

Suppression:
500mg (300mg base) on exactly the same day of each week

Failure to Begin Suppressive Therapy 2 Weeks Prior to Exposure:
Initial Loading Dose: 1g (600mg base) in two divided doses, 6 hrs apart

Continue suppressive therapy for 8 weeks after leaving endemic area

Treatment of Acute Attack:
1g (600mg base), followed by 500mg (300mg base) after 6-8 hrs, then 500mg (300mg base) qd for 2 consecutive days

Extraintestinal Amebiasis

1g (600mg base) qd for 2 days, followed by 500mg (300mg base) qd for at least 2-3 weeks

PEDIATRIC DOSAGE

Malaria

Suppression:
5 mg base/kg on exactly the same day of each week
Max Dose: 500mg (300mg base) (regardless of weight)

Failure to Begin Suppressive Therapy 2 Weeks Prior to Exposure:
Initial Loading Dose: 10mg base/kg in two divided doses, 6 hrs apart

Continue suppressive therapy for 8 weeks after leaving endemic area

Treatment of Acute Attack:
First Dose: 10mg base/kg
Max: 600mg base

Subsequent Doses: 5mg base/kg 6, 24, & 36 hrs after first dose
Max Dose: 300mg base

DOSING CONSIDERATIONS

Dose Reductions
Treatment of Acute Malaria Attack:
Adults of Low Body Weight:
First Dose: 10mg base/kg
Max: 600mg base

Subsequent Doses: 5mg base/kg 6, 24, & 36 hrs after first dose
Max Dose: 300mg base

ADMINISTRATION

Oral route

HOW SUPPLIED

Tab: 250mg* (250mg tab=150mg base), 500mg (500mg tab=300mg base) *scored

CONTRAINDICATIONS

Retinal/visual field changes.

WARNINGS/PRECAUTIONS

Does not prevent relapses in patients with vivax or malariae malaria because it is not effective against exoerythrocytic forms of the parasite, nor will it prevent vivax or malariae infection when administered as a prophylactic. Should not be used for treatment of P. falciparum infections acquired in areas of chloroquine resistance or malaria occurring in patients where chloroquine prophylaxis has failed. Irreversible retinal damage reported with long-term or high-dose therapy. Retinopathy has been reported to be dose-related. If there is any indication (past or present) of abnormality in the visual acuity, visual field, or retinal macular areas, or any visual symptoms (eg, light flashes, streaks) that are not fully explainable by difficulties of accommodation or corneal opacities, d/c therapy immediately and closely observe for possible progression; retinal changes (and visual disturbances) may progress even after cessation of therapy. Monitor patients on long-term therapy periodically for muscular weakness (eg, by testing knee and ankle reflexes); d/c if weakness occurs. May precipitate a severe attack of psoriasis and may exacerbate porphyria; avoid with psoriasis or porphyria unless the benefit outweighs the potential risk. Consider discontinuation if any severe blood disorder appears that is not attributable to the disease under treatment. Caution with G6PD deficiency, hepatic disease or alcoholism, and in elderly. Caution with preexisting auditory damage; in case of any defects in hearing, d/c therapy immediately and closely observe patient. Risk of provoking seizures. Avoid during pregnancy except in the suppression or treatment of malaria when the benefit outweighs the potential risk to the fetus.

ADVERSE REACTIONS

Nyctalopia, nerve-type deafness, tinnitus, skeletal muscle myopathy or neuromyopathy, anorexia, N/V, diarrhea, pleomorphic skin eruptions, skin and mucosal pigmentary changes, mild and transient headache, polyneuritis, neuropsychiatric changes.

DRUG INTERACTIONS

Caution with known hepatotoxic drugs. Antacids and kaolin may reduce absorption; space dosing by at least 4 hrs. Cimetidine may increase levels; avoid concomitant use. Significantly reduced bioavailability of ampicillin; space dosing by at least 2 hrs. After introduction of therapy, a sudden increase in cyclosporine level reported; closely monitor cyclosporine level and, if necessary, d/c chloroquine. Coadministration with mefloquine may increase the risk of convulsions. May reduce antibody response to primary immunization with intradermal human diploid-cell rabies vaccine when given in the dose recommended for malaria prophylaxis.

PREGNANCY AND LACTATION

Safety not known in pregnancy; not for use in nursing.

MECHANISM OF ACTION

Aminoquinoline; antimalarial and amebicidal. Effect is believed to result, at least in part from its interaction with DNA.

PHARMACOKINETICS

Absorption: Rapid and almost complete. Distribution: Plasma protein binding (approximately 55%). Found in breast milk. Metabolism: Degradation. Desethylchloroquine (major metabolite, has antimalarial properties). Elimination: Urine (unchanged [slightly >50%], desethylchloroquine [25%]), feces.

ASSESSMENT

Assess for retinal/visual field changes, psoriasis, porphyria, G6PD deficiency, hepatic disease, alcoholism, preexisting auditory damage, history of epilepsy, hypersensitivity to drug, pregnancy/nursing status, and possible drug interactions. Perform baseline ophthalmologic exams when prolonged therapy is contemplated.

MONITORING

Monitor for hearing defects, seizures, and other adverse reactions. Perform periodic ophthalmologic exams and CBCs during prolonged therapy. Monitor patients on long-term therapy periodically for muscular weakness.

PATIENT COUNSELING

Inform of the risks and benefits of therapy. Instruct to report any adverse reactions to physician. Advise to contact physician if pregnant, planning to become pregnant, or breastfeeding.

STORAGE

20-25°C (68-77°F).

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