No

Aminoquinoline (Antimalarial)

Suppresses and treats acute attacks of malaria; treatment of systemic lupus erythematosus and rheumatoid arthritis

C

Retinal or visual field changes attributable to 4-aminoquinolines; hypersensitivity to hydroxychloroquine, 4-aminoquinoline derivatives, or any component

Use with caution in patients with hepatic disease, G-6-PD deficiency, psoriasis, and porphyria; long-term use in children is not recommended; perform baseline and periodic (6 months) ophthalmologic examinations; test periodically for muscle weakness

>10%:

Central nervous system: Headache

Dermatologic: Itching

Gastrointestinal: Diarrhea, loss of appetite, nausea, stomach cramps, vomiting

Ocular: Ciliary muscle dysfunction

1% to 10%:

Central nervous system: Dizziness, lightheadedness, nervousness, restlessness

Dermatologic: Bleaching of hair, rash, discoloration of skin (black-blue)

Ocular: Ocular toxicity, keratopathy, retinopathy

<1%: Emotional changes, seizures, agranulocytosis, aplastic anemia, neutropenia, thrombocytopenia, neuromyopathy, ototoxicity

Symptoms of overdose include headache, drowsiness, visual changes, cardiovascular collapse, and seizures followed by respiratory and cardiac arrest

Treatment is symptomatic; activated charcoal will bind the drug following GI decontamination; urinary alkalinization will enhance renal elimination

Chloroquine and other 4-aminoquinolones may be decreased due to GI binding with kaolin or magnesium trisilicate

Increased effect: Cimetidine increases levels of chloroquine and probably other 4-aminoquinolones

Interferes with digestive vacuole function within sensitive malarial parasites by increasing the pH and interfering with lysosomal degradation of hemoglobin; inhibits locomotion of neutrophils and chemotaxis of eosinophils; impairs complement-dependent antigen-antibody reactions

Onset of effect: In rheumatic disease, may require 4-6 weeks to respond (maximum after several months)

Absorption: Oral: Complete

Protein binding: 55%

Metabolism: In the liver

Half-life: 32-50 days

Elimination: Metabolites and unchanged drug slowly excreted in urine, may be enhanced by urinary acidification

Note: Hydroxychloroquine sulfate 200 mg is equivalent to 155 mg hydroxychloroquine base and 250 mg chloroquine phosphate. Oral:

Chemoprophylaxis of malaria: 5 mg/kg (base) once weekly; should not exceed the recommended adult dose; begin 2 weeks before exposure; continue for 4-6 weeks after leaving endemic area; if suppressive therapy is not begun prior to the exposure, double the initial dose and give in 2 doses, 6 hours apart

Acute attack: 10 mg/kg (base) initial dose; followed by 5 mg/kg at 6, 24, and 48 hours

JRA or SLE: 3-5 mg/kg/day divided 1-2 times/day; avoid exceeding 7 mg/kg/day

Adults:

Chemoprophylaxis of malaria: 310 mg base weekly on same day each week; begin 2 weeks before exposure; continue for 4-6 weeks after leaving endemic area; if suppressive therapy is not begun prior to the exposure, double the initial dose and give in 2 doses, 6 hours apart

Acute attack: 620 mg first dose day 1; 310 mg in 6 hours day 1; 310 mg in 1 dose day 2; and 310 mg in 1 dose on day 3

Rheumatoid arthritis: 310-465 mg/day to start taken with food or milk; increase dose until optimum response level is reached; usually after 4-12 weeks dose should be reduced by 1/2 and a maintenance dose of 155-310 mg/day given

Lupus erythematosus: 310 mg every day or twice daily for several weeks depending on response; 155-310 mg/day for prolonged maintenance therapy

May be administered with food or milk

Ophthalmologic exam, CBC

May cause dizziness or nervousness

May rarely cause agranulocytosis; use caution with clozapine and carbamazepine

No information available to require special precautions

No effects or complications reported

It is important to complete full course of therapy which may take up to 6 months for full effect. May be taken with meals to decrease GI upset and bitter aftertaste. Avoid alcohol. You should have regular ophthalmic exams (every 4-6 months) if using this medication over extended periods. You may experience skin discoloration (blue/black), hair bleaching, or skin rash. If you have psoriasis, you may experience exacerbation. You may experience dizziness, headache, nervousness, or lightheadedness (use caution when driving or engaging in tasks requiring alertness until response to drug is known); nausea, vomiting, or loss of appetite (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); or increased sensitivity to sunlight (wear dark glasses and protective clothing, use sunblock, and avoid direct exposure to sunlight). Report vision changes, rash or itching, persistent diarrhea or GI disturbances, change in hearing acuity or ringing in the ears, chest pain or palpitation, CNS changes, unusual fatigue, easy bruising or bleeding, or any other persistent adverse reactions. Pregnancy precautions: Inform prescriber if you are or intend to be pregnant.

Periodic blood counts and eye examinations are recommended when patient is on chronic therapy

Tablet, as sulfate: 200 mg [base 155 mg]

A 25 mg/mL hydroxychloroquine sulfate suspension is made by removing the coating off of fifteen 200 mg hydroxychloroquine sulfate tablets with a towel moistened with alcohol; tablets are ground to a fine powder and levigated to a paste with 15 mL of Ora-Plus® suspending agent; add an additional 45 mL of suspending agent and levigate until a uniform mixture is obtained; qs ad to 120 mL with sterile water for irrigation; a 30 day expiration date is recommended, although stability testing has not been performed

Bernstein HN, "Ocular Safety of Hydroxychloroquine," Ann Ophthalmol, 1991, 23(8):292-6.

Buchanan NM, Toubi E, Khamashta MA, et al, "The Safety of Hydroxychloroquine in Lupus Pregnancy: Experience in 27 Pregnancies," Br J Rheumatol, 1995, 34(Suppl 1):14.

"Drugs for Parasitic Infections," Med Lett Drugs Ther, 1993, 35(911):111-22.

Emery H, "Clinical Aspects of Systemic Lupus Erythematosus in Childhood," Pediatr Clin North Am, 1986, 33(5):1177-90.

Furst DE, "Rational Use of Disease-Modifying Antirheumatic Drugs," Drugs, 1990, 39(1):19-37.

Giannini EH and Cawkwell GD, "Drug Treatment in Children With Juvenile Rheumatoid Arthritis. Past, Present, and Future," Pediatr Clin North Am, 1995, 42(5):1099-125.

"Guidelines for the Management of Rheumatoid Arthritis. American College of Rheumatology Ad Hoc Committee on Clinical Guidelines," Arthritis Rheum, 1996, 39(5):713-22.

Hart LE and Tugwell P, "The Use of Disease-Modifying Antirheumatic Drugs in the Management of Rheumatoid Arthritis," Postgrad Med J, 1989, 65(770):905-12.

Kutz DC and Bridges AJ, "Bullous Rash and Brown Urine in a Systemic Lupus Erythematosus Patient Treated With Hydroxychloroquine," Arthritis Rheum, 1995, 38(3):440-3.

Levy M, Buskila D, Gladman DD, et al, "Pregnancy Outcome Following First Trimester Exposure to Chloroquine," Am J Perinatol, 1991, 8(3):174-8.

Panisko DM and Keystone JS, "Treatment of Malaria - 1990," Drugs, 1990, 39(2):160-89.

Seguin P, Camus C, Leroy JP, et al, "Respiratory Failure Associated With Hydroxychloroquine Neuromyopathy," Eur Neurol, 1995, 35(4):236-7.

Wang R, "Hydroxychloroquine Cardiotoxicity," Clin Toxicol, 1995, 33(5):548.

White NJ, "The Treatment of Malaria," N Engl J Med, 1996, 335(11):800-6.