Names and pronunciation
H (hye-drox-ee-klor′oh-kwin) Apo-Hydroxyguine , Plaquenil
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Drug reference
H (hye-drox-ee-klor′oh-kwin) Apo-Hydroxyguine , Plaquenil
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Func. class.: Antimalarial, antirheu- matic (DMARDs)
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Chem. class.: 4-Aminoquinoline derivative
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ACTION: Impairs complement-depen- dent antigen–antibody reactions
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USES: Malaria caused by susceptible strains of Plasmodium vivax, P. malar- iae, P. ovale, P. falciparum (some strains); SLE, rheumatoid arthritis
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Unlabeled uses: Lupus nephritis polymor- phous-light eruptions
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CONTRAINDICATIONS: Hyper- sensitivity to this product or chloroquine; retinal field changes Precautions: Pregnancy, breastfeeding, blood dyscrasias, severe GI disease, neu- rologic disease, alcoholism, hepatic dis- ease, G6PD deficiency, psoriasis, eczema, children, ocular disease
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SIDE EFFECTS CNS: Headache, fatigue, irritability, sei- zures, bad dreams, dizziness, confusion, psychosis, anxiety, suicidal ideation CV: HF, Torsades de pointes, QT prolonga- tion, asystole with syncope EENT: Blurred vision, corneal changes, tinnitus, vertigo, nystagmus, corneal deposits GI: Nausea, vomiting, anorexia, diar- rhea, cramps HEMA: Thrombocytopenia, agranulocyto- sis, leukopenia, aplastic anemia INTEG: Pruritus, exfoliative dermatitis, alopecia, Stevens-Johnson syndrome, photosensitivity, DRESS, rash, pruritus
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INTERACTIONS Increase: digoxin, methotrexate levels Increase: antibody titer—rabies vaccine Decrease: hydroxychloroquine action— magnesium or aluminum compounds Decrease: effect of—live virus vaccines, botulinum toxoids
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TREATMENT OF OVERDOSE: Induce vomiting; gastric lavage; adminis- ter barbiturate (ultrashort acting), vaso- pressor, ammonium chloride; tracheos- tomy may be necessary
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DOSAGE AND ROUTES Malaria • Adult: PO Suppression or preven- tion: 400 mg/wk, begin 2 wk before travel to endemic area, continue 4 wk after returning; treatment: 800 mg, then 400 mg after 6-8 hr, then 400 mg/day on 2nd and 3rd day, total dose 2 g • Child: PO Suppression or preven- tion: 6.4 mg/kg (5 mg/kg base) weekly, begin 1-2 wk before travel to endemic area, continue 4 wk after returning; treatment: 10 mg/kg, 6.4 mg/kg (5 mg/ kg base) at 6, 18, 24 hr after 1st dose Lupus erythematosus • Adult: PO 200-400 mg (310 mg base) daily or divided twice daily; length de- pends on patient response; maintenance: 200-400 mg/day • Child (unlabeled): PO 5 mg/kg/day, max 400 mg/day; long-term therapy is contraindicated Rheumatoid arthritis • Adult: PO 400-600 mg daily or di- vided twice daily for 4-12 wk, then 200- 400 mg/day after good response
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Available forms: Tabs 200 mg
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Administer: PO route • Tabs may be crushed and mixed with food, fluids • With food or milk; at same time each day to maintain product level • Store in tight, light-resistant container at room temperature; keep inj in cool environment
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Assess: • SLE, malaria symptoms: before treat- ment and daily • Rheumatoid arthritis: pain, swelling, ROM, temperature of joints; for de- creased reflexes: knee, ankle • Ophthalmic exam at baseline for reti- nal toxicity then annually after 5 yr of use, or annually in those with increased risk factors • Hepatic studies weekly: AST, ALT, biliru- bin if patient receiving long-term treat- ment • Blood dyscrasias: blood studies: CBC, platelets; WBC, RBC, platelets may be decreased; if severe, product should be discontinued; assess for malaise, fever, bruising, bleeding (rare) • ECG during therapy: watch for depres- sion of T waves, widening of QRS complex • Allergic reactions: pruritus, rash, urti- caria • Ototoxicity (tinnitus, vertigo, change in hearing); audiometric testing should be done before, after treatment • Toxicity: blurring vision, difficulty fo- cusing, headache, dizziness, knee, ankle reflexes; product should be discontinued immediately • Pregnancy/breastfeeding: increased rate of birth defects in the literature; CDC recommends this product for pregnant women with malaria or may be used in those with lupus; cautious use in breastfeeding
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Evaluate: • Therapeutic response: decreased symptoms of malaria, SLE, rheumatoid arthritis
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To use sunglasses in bright sunlight to decrease photophobia; to wear protec- tive clothing (photosensitivity) • That urine may turn rust or brown; that skin may become blue-black • To report hearing, visual problems, fever, fatigue, bruising, bleeding, which may indicate blood dyscrasias RA: To report to provider if there is no change in condition, may need several months for results Malaria prevention • Discuss how to prevent mosquitoes in the environment • Not to use with alcohol
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PHARMACOKINETICS Peak 3 hr; half-life 32-50 days; metabo- lized in liver; excreted in urine, feces, breast milk; crosses placenta, protein binding 45%
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• Child: PO Suppression or preven- tion: 6.4 mg/kg (5 mg/kg base) weekly, begin 1-2 wk before travel to endemic area, continue 4 wk after returning; treatment: 10 mg/kg, 6.4 mg/kg (5 mg/ kg base) at 6, 18, 24 hr after 1st dose Lupus erythematosus
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• Child (unlabeled): PO 5 mg/kg/day, max 400 mg/day; long-term therapy is contraindicated Rheumatoid arthritis
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