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Pronunciation |
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(hye
droks ee KLOR oh
kwin) |
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U.S. Brand
Names |
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Plaquenil® |
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Generic
Available |
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No |
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Synonyms |
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Hydroxychloroquine Sulfate |
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Pharmacological Index |
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Aminoquinoline (Antimalarial) |
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Use |
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Suppresses and treats acute attacks of malaria; treatment of systemic lupus
erythematosus and rheumatoid arthritis |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Retinal or visual field changes attributable to 4-aminoquinolines;
hypersensitivity to hydroxychloroquine, 4-aminoquinoline derivatives, or any
component |
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Warnings/Precautions |
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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 |
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Adverse
Reactions |
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>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 |
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Overdosage/Toxicology |
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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
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Drug
Interactions |
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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 |
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Mechanism of
Action |
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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 |
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Pharmacodynamics/Kinetics |
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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 |
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Usual Dosage |
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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
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Dietary
Considerations |
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May be administered with food or milk |
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Monitoring
Parameters |
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Ophthalmologic exam, CBC |
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Mental Health: Effects
on Mental Status |
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May cause dizziness or nervousness |
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Mental Health:
Effects on Psychiatric
Treatment |
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May rarely cause agranulocytosis; use caution with clozapine and
carbamazepine |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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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. |
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Nursing
Implications |
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Periodic blood counts and eye examinations are recommended when patient is on
chronic therapy |
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Dosage Forms |
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Tablet, as sulfate: 200 mg [base 155 mg] |
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Extemporaneous
Preparations |
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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
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References |
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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. |
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