AntimalarialUS FDA Database Verified

chloroquine (Rx)

Generic: Chloroquine

Brand: Aralen

(klor'oh-kwin)

Pregnancy Category: C

Pharmacological Action

Inhibits parasite replications, transcription of DNA to RNA by forming complexes with DNA of parasite

Therapeutic outcome: Decreased symptoms of malaria, amebiasis

Uses

Malaria caused by Plasmodium vivax, Plasmodium malariae, Plasmodium ovale, Plasmodium falciparum (some strains), amebiasis

Contraindications

Hypersensitivity, retinal field changes

Precautions: Pregnancy C, breastfeeding, children, blood dyscrasias, severe GI disease, neurologic disease, alcoholism, hepatic disease, G6 PD deficiency, psoriasis, eczema, seizures, preexisting auditory damage, infection, torsades de pointes

BLACK BOX WARNING: Infection

Dosage & Routes

Acute malaria attacks

Adult: PO 1000 mg (600 mg base), then 500 mg (300 mg base) in 6-8 hr, then 500 mg (300 mg base) q day 3 2 days for a total of 2.5 g (1.5 g base) in 3 days Adult/adolescent of low body weight, child/infant: PO 16.5 mg (10 mg base)/kg, max 600 mg base, then 8.3 mg (5 mg base)/kg max 300 mg base, 6 hr after 1 st dose, then 8.3 mg (5 mg base)/kg, max 300 mg base 24 hr after 1 st dose, then 8.3 mg (5 mg base)/kg max 300 mg base 36 hr after 1 st dose Malaria prophylaxis (in areas with chloroquine–sensitive P. falciparum)

Adult: PO 500 mg (300 mg base) q wk on same day of each wk, starting 2 wk before travel and 8 wk after leaving Extraintestinal amebiais

Adult: PO 1 g (600 mg base) q day 3 2 days, then 500 mg (300 mg base) for ≥ 2-3 wk Child (unlabeled): PO 16.6 mg (10 mg base)/kg (max 300 mg base) q day 3 2-3 wk

Available forms: Tabs 250 mg (150 mg base), 500 mg (300 mg base) phosphate

Implementation - Give with meals to decrease GI symptoms; better to take on empty stomach 1 hr before or 2 hr after meals - Give antiemetic if vomiting occurs - Give after C&S is completed; monthly to detect resistance IM route - Give IM after aspirating to prevent inj into bloodstream - Store in tight, light-resistant container at room temp; keep inj in cool environment

Adverse Effects

CNS: Headache, stimulation, fatigue, seizure, psychosis, hallucinations, insomnia

CV: Hypotension, heart block, asystole with syncope, ECG changes, cardiomyopathy

EENT: Blurred vision, corneal changes, retinal changes, difficulty focusing, tinnitus, vertigo, deafness, photophobia, corneal edema

GI: Nausea, vomiting, anorexia, diarrhea, cramps

HEMA: Thrombocytopenia, agranulocytosis, hemolytic anemia, leukopenia

INTEG: Pruritus, pigmentary changes, skin eruptions, lichen planus–like eruptions, eczema, exfoliative dermatitis

Pharmacokinetics

Absorption: Well absorbed

Distribution: Widely

Metabolism: Liver

Excretion: Kidneys, feces

Half-life: 3-5 days

Pharmacodynamics

PO: Onset Rapid, Peak 1-3 hr, Duration 6-8 hr

IM: Onset Rapid, Peak 30 min, Duration Unknown

Interactions

Individual drugs Ampicillin, rabies vaccine (ID): decreased effects

Cimetidine: decreased oral clearance, metabolism

Kaolin: decreased absorption

Magnesium: decreased action of chloroquine

Drug classifications CYP2 D6 inhibitors (amiodarone, chlorpheniramine, FLUoxetine, haloperidol, ritonavir, PARoxetine, terbinafine, ticlopidine), CYP3 A4 inhibitors (clarithromycin, diltiazem, doxycycline, erythromycin, itraconazole, ketoconazole, verapamil): increased effects Antacids (aluminum): decreased absorption Class IA, III antidysrhythmics: increased QT prolongation, torsades de pointes

Drug/lab test

Decreased: Hgb, platelets, WBC

Nursing Considerations

Assessment

BLACK BOX WARNING: Assess for infection: resistance is common, not to be used for P. falciparum acquired in areas of resistance or where prophylaxis has failed - Monitor ECG, baseline and periodically during therapy; watch for depression of T waves, widening of QRS complex - Assess for allergic reactions: pruritus, rash, urticaria - Assess for ototoxicity: tinnitus, vertigo, change in hearing; audiometric testing should be done before, after treatment - Assess for blood dyscrasias: malaise, fever, bruising, bleeding (rare) - Assess mental status often: affect, mood, behavioral changes; psychosis may occur - Assess for toxicity: blurring vision, difficulty focusing, headache, dizziness, decreased knee and ankle reflexes, product should be discontinued immediately

Patient/family education - Advise patient that compliance with dosage schedule, duration is necessary - Instruct patient that scheduled appointments must be kept or relapse may occur - Caution patient to avoid alcohol while taking product - Instruct diabetic to use blood glucose monitor to obtain correct result - Teach patient to report weakness, fatigue, loss of appetite, nausea, vomiting, yellowing of skin or eyes, tingling/numbness of hands/feet - Advise patient that urine may turn rust brown color - Instruct patient to use sunglasses in bright sunlight to prevent photophobia - Keep away from pets, children; overdose is fatal

Evaluation

Positive therapeutic outcome: Decreased symptoms of malaria

Reference

Mosby's Drug Guide; Davis Drug Guide

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