Names and pronunciation
(klor′oh-kwin)
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Individual generic drug information
Extracted information for chloroquine only.
(klor′oh-kwin)
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Func. class.: Antimalarial, antipro- tozoal
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Chem. class.: Synthetic 4- amino-quinoline derivative
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ACTION: Inhibits parasite replica- tion, transcription of DNA to RNA by forming complexes with DNA of parasite
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USES: Malaria of Plasmodium vivax, P. malariae, P. ovale, P. falciparum (some strains); amebiasis
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Unlabeled uses: Discoid lupus erythe- matosus, polymorphous light eruption, rheumatoid arthritis, ulcerative colitis
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Extracted information for chloroquine only.
CONTRAINDICATIONS: Hyper- sensitivity, retinal field changes Precautions: Pregnancy, breastfeeding, children, blood dyscrasias, severe GI/ neurologic/cardiac disease, alcoholism, C hepatic disease, G6PD deficiency, pso- riasis, eczema, seizures, preexisting audi- tory damage, torsades de pointes, infection
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SIDE EFFECTS CNS: Headache, stimulation, fatigue, seizures, psychosis, hallucinations, insomnia CV: Hypotension, heart block, asystole with syncope, ECG changes, cardiomyopathy EENT: Blurred vision, corneal changes, retinal changes, difficulty focusing, tin- nitus, vertigo, deafness, photophobia, corneal edema GI: Nausea, vomiting, anorexia, diar- rhea, cramps HEMA: Thrombocytopenia, agranulocyto- sis, hemolytic anemia, leukopenia INTEG: Pruritus, pigmentary changes, skin eruptions, lichen-planus–like erup- tions, eczema, exfoliative dermatitis
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INTERACTIONS • Reduced oral clearance and metabo- lism of chloroquine, cimetidine Increase: QT prolongation, torsades de pointes—class IA, III antidysrhythmics Increase: effects—2D6 inhibitors (amio- darone, chlorpheniramine, FLUoxetine, haloperidol, ritonavir, PARoxetine, terbina fine, ticlopidine); CYP3A4 inhibitors (diltiaZEM, verapamil, itraconazole, keto conazole, erythromycin, doxycycline, clarithromycin) Decrease: action of chloroquine—mag- nesium, aluminum compounds, kaolin; do not use concurrently Decrease: effects of ampicillin, rabies vaccine (ID) Drug/Lab Test Decrease: HB, platelets, WBC
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TREATMENT OF OVERDOSE: • Administer barbiturate (ultra-short- acting), vasopressor; tracheostomy may be necessary
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Extracted information for chloroquine only.
DOSAGE AND 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) daily × 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 first dose, then 8.3 mg (5-mg base)/kg, max 300-mg base 24 hr after first dose, then 8.3 mg (5-mg base)/kg, max 300-mg base 36 hr after first dose Malaria prophylaxis (in areas with chloroquine-sensitive P. falciparum) • Adult: PO 500 mg (300-mg base) weekly on same day of each wk starting 2 wk prior to travel and for 8 wk after leaving Extraintestinal amebiasis • Adult: PO 1 g (600-mg base) daily × 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) daily × 2-3 wk
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Available forms: Tablets 250 mg (150-mg base), 500 mg (300-mg base) phosphate
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Administer: • Product in mg or base; they are different PO route • Prior to or after meals at same time each day to maintain product level • Store in tight, light-resistant container at room temperature; keep injection in cool environment
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Extracted information for chloroquine only.
Assess: • Infection: resistance is common; not to be used for P. falciparum acquired in areas of resistance or where prophylaxis has failed • Ophthalmic test if long-term treatment or dosage of >150 mg/day, baseline and periodically • Screen for G6PD deficiency; identify risk of hemolysis • Blood studies: LFTs; CBC, as blood dyscrasias occur, stop if severe dyscra- sias occur; monitor for malaise, fever, bruising, bleeding (rare) • ECG during therapy; watch for depres- sion of T waves, widening of QRS complex in those with QT prolongation • Allergic reactions: pruritus, rash, urti- caria • For ototoxicity (tinnitus, vertigo, change in hearing); audiometric testing should be done prior to, after treatment • For toxicity: blurring vision; difficulty focusing; headache; dizziness; decreased knee, ankle reflexes; seizures, CV col- lapse; product should be discontinued immediately and IV fluids given
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Evaluate: • Therapeutic response: decreased symptoms of infection
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To take with meals or immediately af- ter meals • To use sunglasses in bright sunlight to decrease photophobia • That urine may turn rust or brown color • To report hearing, visual problems; fe- ver, fatigue, bruising, bleeding (may indi- cate blood dyscrasias) • To keep away from pets, children; overdose is fatal • Pregnancy/breastfeeding: to avoid use in pregnancy unless suppression of malaria is needed and benefits outweigh fetal risk; do not use in breastfeeding
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Extracted information for chloroquine only.
PHARMACOKINETICS Metabolized in liver; excreted in urine, feces, breast milk; crosses placenta PO: Peak 1-3 hr, half-life 3-5 days
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Filter the extracted dose blocks for this individual drug.
Acute malaria attacks
• 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 first dose, then 8.3 mg (5-mg base)/kg, max 300-mg base 24 hr after first dose, then 8.3 mg (5-mg base)/kg, max 300-mg base 36 hr after first dose Malaria prophylaxis (in areas with chloroquine-sensitive P. falciparum)
Candidate age grouping · source page 271
Acute malaria attacks
• Child (unlabeled): PO 16.6 mg (10- mg base)/kg (max 300-mg base) daily × 2-3 wk
Candidate age grouping · source page 271