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Plaquenil

Pronunciation

Generic Name: Hydroxychloroquine Sulfate
Class: Antimalarials
VA Class: AP101
CAS Number: 747-36-4

Introduction

Antimalarial; 4-aminoquinoline derivative.a

Uses for Plaquenil

Malaria

Prevention (prophylaxis) of malaria caused by Plasmodium malariae, P. ovale, P. vivax, or susceptible strains of P. falciparum.105 109 CDC and others recommend chloroquine for prevention of malaria caused by Plasmodium susceptible to 4-aminoquinoline derivatives;105 110 hydroxychloroquine is as effective and may be better tolerated105 and may be used when chloroquine is unavailable.105 110

Treatment of uncomplicated malaria caused by P. malariae, P. ovale, P. vivax, or susceptible strains of P. falciparum.109 110

Active only against the asexual erythrocytic forms of Plasmodium (not exoerythrocytic stages) and cannot prevent delayed primary attacks or relapse of P. ovale or P. vivax malaria or provide a radical cure; primaquine usually also indicated to eradicate hypnozoites and prevent relapse in patients exposed to or being treated for P. ovale or P. vivax malaria.105 109

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Detailed recommendations regarding prevention of malaria available from CDC 24 hours a day from the voice information service (877-394-8747), fax information service (888-232-3299), or Internet at .105

Assistance with diagnosis or treatment of malaria available from CDC Malaria Epidemiology Branch by contacting CDC Malaria Hotline at 770-488-7788 from 8:00 a.m. to 4:30 p.m. Eastern Standard Time or CDC Emergency Operation Center at 770-488-7100 after hours, on weekends, and holidays.118

Rheumatoid Arthritis

Treatment of rheumatoid arthritis in patients whose symptoms progress despite an adequate regimen of nonsteroidal anti-inflammatory agents (NSAIAs).103 104 109

One of several disease-modifying antirheumatic drugs (DMARDs) that can be used when DMARD therapy is appropriate.103 104 If used for prolonged periods in treatment of rheumatoid arthritis, the risk of severe and sometimes irreversible toxicity should be considered.109 (See Cautions.)

Lupus Erythematosus

Treatment of discoid lupus erythematosus and systemic lupus erythematosus.109 Used as an adjunct to corticosteroids and/or other appropriate therapy.a

If used for prolonged periods in treatment of lupus erythematosus, the risk of serious and sometimes irreversible toxicity should be considered. (See Cautions.)

Q Fever

Treatment of Q fever endocarditis caused by Coxiella burnetii; used in conjunction with doxycycline.111 112 113

CDC recommends a 2- to 3-week regimen of doxycycline for treatment of acute Q fever, a 1-year regimen of doxycycline and hydroxychloroquine for treatment of acute Q fever in patients with preexisting valvular heart disease (to prevent progression of acute disease to endocarditis), and a 1.5- to 3-year regimen of doxycycline and hydroxychloroquine for treatment of chronic Q fever.113

Porphyria Cutanea Tarda and Polymorphous Light Eruptions

Has been used in treatment of porphyria cutanea tarda.115 116 117 (See Patients with Psoriasis or Porphyria under Cautions.)

Has been effective in some cases when used in the treatment of polymorphous light eruptions.

Plaquenil Dosage and Administration

Administration

Oral Administration

Administer orally.109

When used in treatment of rheumatoid arthritis, administer with a meal or a glass of milk.109

Dosage

Available as hydroxychloroquine sulfate; dosage usually expressed as hydroxychloroquine.109

Each 200 mg of hydroxychloroquine sulfate is equivalent to 155 mg of hydroxychloroquine.109

Pediatric Patients

Malaria
Prevention of Malaria in Areas Without Chloroquine-resistant Plasmodium
Oral

5 mg/kg (6.5 mg/kg of hydroxychloroquine sulfate) once weekly on the same day each week.105 109

Initiate prophylaxis 1–2 weeks prior to entering a malarious area and continue for 4 weeks after leaving the area.105 114 CDC states it may be advisable to initiate prophylaxis 3–4 weeks prior to travel to ensure that the drug or combination of drugs (in individuals receiving other drugs) is well tolerated and to allow ample time if a switch to another antimalarial agent is required.105

If not initiated prior to entering a malarious area, manufacturer recommends a loading dose of 10 mg/kg (13 mg/kg of hydroxychloroquine sulfate) given in 2 equally divided doses 6 hours apart followed by the usual dosage.109

Treatment of Uncomplicated Chloroquine-susceptible Malaria
Oral

An initial dose of 10 mg/kg (13 mg/kg of hydroxychloroquine sulfate) followed by 5-mg/kg doses (6.5 mg/kg of hydroxychloroquine sulfate) given at 6, 24, and 48 hours after the initial dose.109

Adults

Malaria
Prevention of Malaria in Areas Without Chloroquine-resistant Plasmodium
Oral

310 mg (400 mg of hydroxychloroquine sulfate) once weekly on the same day each week.105 109

Initiate prophylaxis 1–2 weeks prior to entering a malarious area and continue for 4 weeks after leaving the area.105 114 CDC states it may be advisable to initiate prophylaxis 3–4 weeks prior to travel to ensure that the drug or combination of drugs (in individuals receiving other drugs) is well tolerated and to allow ample time if a switch to another antimalarial agent is required.105

If not initiated prior to entering a malarious area, the manufacturer recommends a loading dose of 620 mg (800 mg of hydroxychloroquine sulfate) followed by the usual dosage regimen.109

Treatment of Uncomplicated Chloroquine-susceptible Malaria
Oral

An initial dose of 620 mg (800 mg of hydroxychloroquine sulfate) followed by 310-mg doses (400 mg of hydroxychloroquine sulfate) given 6–8 hours, 24, and 48 hours after the initial dose.109 This represents a total hydroxychloroquine dose of 1.55 g (2 g of hydroxychloroquine sulfate) in 3 days.109 Alternatively, adults may receive a single 620-mg dose (800 mg of hydroxychloroquine sulfate).109

Rheumatoid Arthritis
Oral

Initiate treatment with 310–465 mg (400–600 mg of hydroxychloroquine sulfate) daily.109 If adverse effects occur, dosage may be temporarily reduced; after 5–10 days, increase dosage gradually until an optimum response occurs without recurrence of adverse effects.109

A response may not occur until after 4–12 weeks and several months of therapy may be required to attain optimum response.109 When a good response is obtained, decrease dosage by 50% and continue treatment with a maintenance dosage of 155–310 mg (200–400 mg of hydroxychloroquine sulfate) daily.109

If relapse occurs after hydroxychloroquine is discontinued, the drug can be reinitiated or continued on an intermittent schedule if there is no evidence of adverse ocular effects.109

If objective improvement of rheumatoid arthritis (e.g., reduced joint swelling, increased mobility) does not occur within 6 months, hydroxychloroquine should be discontinued.109

Lupus Erythematosus
Oral

310 mg (400 mg of hydroxychloroquine sulfate) once or twice daily for several weeks or months depending on response of the patient.109 For prolonged maintenance therapy, 155–310 mg (200–400 mg of hydroxychloroquine sulfate) daily may be adequate.109

Q Fever
Acute Q Fever in Patients with Preexisting Valvular Heart Disease
Oral

CDC recommends 465 mg (600 mg of hydroxychloroquine sulfate) daily in conjunction with oral doxycycline (200 mg daily) for 1 year.113 Adjust hydroxychloroquine dosage to maintain plasma hydroxychloroquine concentrations at 1 ± 0.2 mcg/mL.113

Chronic Q Fever
Oral

CDC recommends 465 mg (600 mg of hydroxychloroquine sulfate) daily in conjunction with oral doxycycline (200 mg daily) for 1.5–3 years.113

Prescribing Limits

Pediatric Patients

Malaria
Prevention of Malaria in Areas Without Chloroquine-resistant Plasmodium
Oral

Maximum of 310 mg (400 mg of hydroxychloroquine sulfate) daily, regardless of weight.105

Cautions for Plaquenil

Contraindications

  • Hypersensitivity to 4-aminoquinoline derivatives.109

  • Retinal or visual field changes attributable to 4-aminoquinoline derivatives or to any other etiology.109

  • Long-term use in children.109

Warnings/Precautions

Warnings

Chloroquine-resistant Plasmodium

Hydroxychloroquine is not effective against chloroquine-resistant P. falciparum.105 109 For prevention of malaria, use only in individuals traveling to malarious areas where chloroquine-resistant P. falciparum malaria has not been reported.105

For prevention or treatment of malaria, consider that chloroquine-resistant P. falciparum have been reported in all areas where malaria occurs, except the Dominican Republic, Haiti, Mexico and Central America west of the former Panama Canal zone, Paraguay, northern Argentina, Egypt, most of the Middle East (chloroquine resistance has been reported in Iran, Oman, Saudi Arabia, and Yemen), and most of China (chloroquine resistance has been reported in Hainin and Yunnan provinces).105 110 114

Ocular Effects

Dose-related retinopathy reported, which may progress even after the drug is discontinued.109 Irreversible retinal damage has occurred in some patients who received long-term or high-dosage 4-aminoquinoline therapy for treatment of discoid and systemic lupus erythematosus or rheumatoid arthritis.109

Whenever long-term therapy is contemplated, perform initial (base line) and periodic (every 3 months) ophthalmologic examinations, including visual acuity, slit-lamp, funduscopic, and visual field tests.109

Discontinue drug immediately and closely observe patient for possible progression if there is any indication of abnormalities in visual acuity or visual field, abnormalities in the retinal macular area (such as pigmentary changes or loss of foveal reflex), or if any other visual symptoms (e.g., light flashes and streaks) occur which are not fully explainable by difficulties of accommodation or corneal opacities.109

Neuromuscular Effects

Skeletal muscle palsies or skeletal muscle myopathy or neuromyopathy reported.109 May lead to progressive weakness and atrophy of proximal muscle groups and may be associated with mild sensory changes, depression of tendon reflexes, and abnormal nerve conduction.109

Patients receiving prolonged therapy should be questioned and examined periodically for evidence of muscular weakness; knee and ankle reflexes should be tested.109

Discontinue hydroxychloroquine if muscular weakness occurs.109

Patients with Psoriasis or Porphyria

May exacerbate psoriasis and precipitate a severe attack in patients with the disease.109 Use in psoriasis patients only if potential benefits outweigh risks.109

May exacerbate porphyria.109 Use in patients with porphyria only if potential benefits outweigh risks.109

General Precautions

Dermatologic Effects

Dermatologic reactions may occur; use with caution in patients with tendency for dermatitis.109

Hematologic Effects

Aplastic anemia, agranulocytosis, leukopenia, thrombocytopenia (hemolysis in patients with G-6-PD deficiency) reported rarely.109

Periodically monitor CBCs in patients receiving prolonged treatment.109 Consider discontinuing hydroxychloroquine if any severe blood disorder occurs which is not attributable to the disease being treated.109

Use with caution in patients with G-6-PD deficiency.109

Specific Populations

Pregnancy

Category C.b

Avoid use during pregnancy unless the clinician determines that the benefits of prevention or treatment of malaria outweigh the risks.109 Chloroquine has been used for prophylaxis and treatment of malaria in pregnant women without evidence of adverse effects on the fetus,105 110 and CDC states that the benefits of chloroquine or hydroxychloroquine prophylaxis in pregnant women exposed to malaria outweigh potential risks to the fetus.105 110

Lactation

Distributed into milk.102 Amount of drug present in human milk does not appear to be harmful to nursing infants, but is insufficient to provide adequate protection against malaria in these infants.105 When chemoprophylaxis is necessary in such infants, they should receive recommended dosages of the appropriate antimalarial agent(s).105

Pediatric Use

Pediatric patients are especially sensitive to 4-aminoquinoline derivatives.109 Fatalities have been reported following accidental ingestion of relatively small doses.109

Prolonged therapy with hydroxychloroquine is contraindicated in children; safe use of the drug for treatment of juvenile arthritis has not been established.109

Hepatic Impairment

Hydroxychloroquine may concentrate in the liver;a use with caution in patients with hepatic disease or alcoholism and in patients receiving other hepatotoxic drugs.109

Common Adverse Effects

Ocular effects; skeletal muscle myopathy or neuromyopathy; GI effects (anorexia, diarrhea, nausea, abdominal cramps, vomiting); CNS effects (headache, dizziness); dermatologic effects.109

Plaquenil Pharmacokinetics

Distribution

Extent

Distributed into milk.102

Elimination

Metabolism

Partially metabolized; the major metabolites are desethylhydroxychloroquine and desethylchloroquine.100 Bisdesethylchloroquine, a carboxylic acid derivative, also is formed in small amounts.100

Elimination Route

Hydroxychloroquine and its metabolites are slowly excreted by the kidneys.100

Stability

Storage

Oral

Tablets

Room temperature ≤30°C in tight, light-resistant container.109

Actions and Spectrum

  • A blood schizonticidal agent active against asexual erythrocytic forms of most strains of Plasmodium malariae, P. ovale, P. vivax, and many strains of P. falciparum.a Not active against preerythrocytic or exoerythrocytic forms of plasmodia.a Gametocidal for P. malariae and P. vivax, but has no direct activity against the gametocytes of P. falciparum.a

  • Chloroquine-resistant P. falciparum also are resistant to hydroxychloroquine109 and may be cross-resistant to pyrimethamine or quinine.a

  • Has anti-inflammatory activity; mechanism(s) of action in the treatment of rheumatoid arthritis and lupus erythematosus has not been determined.a

Advice to Patients

  • Importance of keeping hydroxychloroquine out of reach of children since they are especially sensitive to 4-aminoquinoline derivatives.109

  • Necessity of taking protective measures to reduce contact with mosquitoes (protective clothing, insect repellents, mosquito nets, remaining in air-conditioned or well-screened areas).105 110

  • Possibility of contracting malaria during travel, regardless of prophylactic regimen used.105 110

  • Importance of seeking medical attention as soon as possible if febrile illness develops during or after return from a malaria-endemic area and of informing clinician of possible malaria exposure.105 110

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

  • Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed.109

  • Importance of advising patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Hydroxychloroquine Sulfate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets, film-coated

155 mg (of hydroxychloroquine)*

Plaquenil

Sanofi-Synthelabo

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Hydroxychloroquine Sulfate 200MG Tablets (WATSON LABS): 60/$35.99 or 180/$88.99

Plaquenil 200MG Tablets (SANOFI-AVENTIS U.S.): 60/$182.99 or 180/$529.96

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions August 1, 2005. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

Only references cited for selected revisions after 1984 are available electronically.

100. McChesney EW. Animal toxicity and pharmacokinetics of hydroxychloroquine sulfate. Am J Med. 1983; 75(Suppl. 1A):11-8. [IDIS 174380] [PubMed 6408923]

101. Janssen NM, Genta MS. The effects of immunosuppressive and anti-inflammatory medications on fertility, pregnancy, and lactation. Arch Inter Med. 2000; 160:610-9.

102. American Academy of Pediatrics Committee on Drugs. Transfer of drugs and other chemicals into human milk. Pediatrics. 1989; 84:924-36. [IDIS 260411] [PubMed 2677964]

103. American College of Rheumatology Subcommittee on Rheumatoid Arthritis Guidelines. Guidelines for the management of rheumatoid arthritis: 2002 update. Arthritis Rheum. 2002; 46:328-46. [IDIS 476480] [PubMed 11840435]

104. Anon. Drugs for rheumatoid arthritis. Med Lett Drugs Ther. 2000; 42:57-64. [PubMed 10887424]

105. Centers for Disease Control and Prevention. Health information for international travel, 2003–2004. Atlanta, GA: US Department of Health and Human Services; 2003:13-39,99-116,136,138,175-7,227,231-5,240-2,249-50. Updates available from CDC website ().

106. Clark P, Casas E, Tugwell P et al. Hydroxychloroquine compared with placebo in rheumatoid arthritis: a randomized controlled trial. Ann Intern Med. 1993; 119:1067-71. [IDIS 322560] [PubMed 8239224]

107. Harris ED Jr. Hydroxychloroquine is safe and probably useful in rheumatoid arthritis. Ann Intern Med. 1993; 119:1146-7. [IDIS 322565] [PubMed 8239236]

108. Makin AJ, Wendon J, Fitt S. Fulminant hepatic failure secondary to hydroxychloroquine. Gut. 1994; 35:569-70. [IDIS 330037] [PubMed 8175002]

109. Sanofi-Synthelabo. Plaquenil (hydroxychloroquine sulfate) prescribing information. New York, NY; 2002 Apr.

110. Anon. Drugs for parasitic infections. Med Lett Drugs Ther. Aug 2004. From the Medical Letter website (). Accessed 2005 Feb 2.

111. Raoult D, Houpikian P, Dupont HT et al. Treatment of Q fever endocarditis: comparison of 2 regimens containing doxycycline and ofloxacin or hydrochloroquine. Arch Intern Med. 1999; 159:167-73. [IDIS 418047] [PubMed 9927100]

112. Lupoglazoff JM, Brouqui P, Magnier S et al. Q fever tricuspid valve endocarditis. Arch Dis Child. 1997; 77:448-9. [IDIS 398559] [PubMed 9487972]

113. Centers for Disease Control and Prevention. Q fever—California, Georgia, Pennsylvania, and Tennessee, 2000-2001. MMWR Morb Mortal Wkly Rep. 2002; 51:924-5. [PubMed 12403408]

114. Anon. Advice for travelers. Med Lett Drugs Ther. 2004; 2:33-40.

115. Bruce AJ, Ahmed I. Childhood-onset porphyria cutanea tarda: successful therapy with low-dose hydroxychloroquine (Plaquenil). J Am Acad Dermatol. 1998; 38(5 pt 2):810-3. [IDIS 406218] [PubMed 9591792]

116. Wallace DJ. The use of chloroquine and hydroxychloroquine for non-infectious conditions other than rheumatoid arthritis or lupus: a critical review. Lupus. 1996; 5(Suppl 1):S59-64.

117. Petersen CS, Thomsen K. High-dose hydroxychloroquine treatment of porphyria cutanea tarda. J Am Acad Dermatol. 1992; 26:614-9. [PubMed 1597548]

118. Centers for Disease Control and Prevention. CDC treatment guidelines: Treatment of malaria (guidelines for clinicians). 2004 Jun 28. From the CDC website. Accessed 2004 Oct 25.

a. AHFS Drug Information 2004. McEvoy GK, ed. hydroxychloroquine Sulfate. Bethesda, MD: American Society of Health-System Pharmacists; 2004:827-8.

b. Briggs GG, Freeman RK, Yaffe SJ. Drugs in pregnancy and lactation. 6th ed. Philadelphia; PA: Lippincott Wiliams & Wilkins; 2002:671-4.

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