Yes

Aminoquinoline (Antimalarial)

Suppression or chemoprophylaxis of malaria; treatment of uncomplicated or mild to moderate malaria; extraintestinal amebiasis

C

Retinal or visual field changes; patients with psoriasis; known hypersensitivity to chloroquine

Use with caution in patients with liver disease, G-6-PD deficiency, alcoholism or in conjunction with hepatotoxic drugs, psoriasis, porphyria may be exacerbated; retinopathy (irreversible) has occurred with long or high-dose therapy; discontinue drug if any abnormality in the visual field or if muscular weakness develops during treatment

>1%: Gastrointestinal: Nausea, diarrhea

<1%: Hypotension, EKG changes, fatigue, personality changes, headache, pruritus, hair bleaching, anorexia, vomiting, stomatitis, blood dyscrasias, retinopathy, blurred vision

Symptoms of overdose include headache, visual changes, cardiovascular collapse, seizures, abdominal cramps, vomiting, cyanosis, methemoglobinemia, leukopenia, respiratory and cardiac arrest

Following initial measures (immediate GI decontamination), treatment is supportive and symptomatic

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

Binds to and inhibits DNA and RNA polymerase; interferes with metabolism and hemoglobin utilization by parasites; inhibits prostaglandin effects; chloroquine concentrates within parasite acid vesicles and raises internal pH resulting in inhibition of parasite growth; may involve aggregates of ferriprotoporphyrin IX acting as chloroquine receptors causing membrane damage; may also interfere with nucleoprotein synthesis

Absorption: Oral: Rapid (~89%)

Distribution: Widely distributed in body tissues such as eyes, heart, kidneys, liver, and lungs where retention is prolonged; crosses the placenta; appears in breast milk

Metabolism: Partial hepatic metabolism occurs

Half-life: 3-5 days

Time to peak serum concentration: Within 1-2 hours

Elimination: ~70% excreted unchanged in urine; acidification of the urine increases elimination of drug; small amounts of drug may be present in urine months following discontinuation of therapy

Oral ( dosage expressed in terms of mg of base):

Children: Administer 5 mg base/kg/week on the same day each week (not to exceed 300 mg base/dose); begin 1-2 weeks prior to exposure; continue for 4-6 weeks after leaving endemic area; if suppressive therapy is not begun prior to exposure, double the initial loading dose to 10 mg base/kg and administer in 2 divided doses 6 hours apart, followed by the usual dosage regimen

Adults: 300 mg/week (base) on the same day each week; begin 1-2 weeks prior to exposure; continue for 4-6 weeks after leaving endemic area; if suppressive therapy is not begun prior to exposure, double the initial loading dose to 600 mg base and administer in 2 divided doses 6 hours apart, followed by the usual dosage regimen

Acute attack:

Oral:

Children: 10 mg/kg on day 1, followed by 5 mg/kg 6 hours later and 5 mg/kg on days 2 and 3

Adults: 600 mg on day 1, followed by 300 mg 6 hours later, followed by 300 mg on days 2 and 3

I.M. (as hydrochloride):

Children: 5 mg/kg, repeat in 6 hours

Adults: Initial: 160-200 mg, repeat in 6 hours if needed; maximum: 800 mg first 24 hours; begin oral dosage as soon as possible and continue for 3 days until 1.5 g has been given

Extraintestinal amebiasis:

Children: Oral: 10 mg/kg once daily for 2-3 weeks (up to 300 mg base/day)

Adults:

Oral: 600 mg base/day for 2 days followed by 300 mg base/day for at least 2-3 weeks

I.M., as hydrochloride: 160-200 mg/day for 10 days; resume oral therapy as soon as possible

Dosing adjustment in renal impairment: Cl_cr <10 mL/minute: Administer 50% of dose

Hemodialysis: Minimally removed by hemodialysis

May be administered with meals to decrease GI upset

Periodic CBC, examination for muscular weakness, and ophthalmologic examination in patients receiving prolonged therapy

May rarely cause fatigue or personality changes

May cause blood dyscrasias; 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. May turn urine black/brown (normal). You may experience 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.

Chloroquine phosphate tablets have also been mixed with chocolate syrup or enclosed in gelatin capsules to mask the bitter taste

Monitor periodic CBC, examination for muscular weakness and ophthalmologic examination in patients receiving prolonged therapy

Injection: 50 mg [40 mg base]/mL (5 mL)

Tablet: 250 mg [150 mg base]; 500 mg [300 mg base]

A 10 mg chloroquine base/mL suspension is made by pulverizing two Aralen® 500 mg phosphate = 300 mg base/tablet, levigating with sterile water, and adding by geometric proportion, a significant amount of the cherry syrup and levigating until a uniform mixture is obtained; qs ad to 60 mL with cherry syrup, stable for up to 4 weeks when stored in the refrigerator or at a temperature of 29°C

August C, Holzhausen H-J, Schmoldt A, et al, "Histological and Ultrastructural Findings in Chloroquine-Induced Cardiomyopathy," J Mol Med, 1995, 73(2):73-7.

Avina-Zubieta JA, Johnson ES, Suarez-Almazor ME, et al, "Incidence of Myopathy in Patients Treated With Antimalarials. A Report of Three Cases and a Review of the Literature," Br J Rheumatol, 1995, 34(2):166-70.

Clemmessy JL, Favier C, Borron SW, et al, "Hypokalemia Related to Acute Chloroquine Ingestion," Clin Toxicol, 1995, 33(5):514.

Demaziere J, Fourcade JM, and Busseuil CT, "The Hazards of Chloroquine Self Prescription in West Africa," J Toxicol Clin Toxicol, 1995, 33(4):369-70.

Drenou B, Guyader D, Turlin B, et al, "Treatment of Sideroblastic Anemia With Chloroquine," N Engl J Med, 1995, 332(9):614

Jaeger A, Sauder P, Kopferschmitt J, et al, "Clinical Features and Management of Poisoning Due to Antimalarial Drugs," Med Toxicol Adverse Drug Exp, 1987, 2(4):242-73.

Liu AC, "Hepatotoxic Reaction to Chloroquine Phosphate in a Patient With Previously Unrecognized Porphyria Cutanea Tarda," West J Med, 1995, 162(6):548-51.

Mirochnick M, Barnett E, Clarke DF, et al, "Stability of Chloroquine in an Extemporaneously Prepared Suspension Stored at Three Temperatures," Pediatr Infect Dis J, 1994, 13(9):827-8.

Mulhauser P, Allemann Y, and Regamey C, "Chloroquine and Nonconvulsive Status Epilepticus," Ann Intern Med, 1995, 123(1):76-7.

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

Rajah A, "The Use of Diazepam in Chloroquine Poisoning," Anaesthesia, 1990, 45(11):955-7.

Riou B, Barriot P, Rimailho A, et al, "Treatment of Severe Chloroquine Poisoning," N Engl J Med, 1988, 318(1):1-6.

Schröder S, August C, Pompecki R, et al, "Fatal Vacuolar Cardiomyopathy in Chronic Chloroquine Drug Treatment," Pathologe 1995, 16(1):81-4.

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

Wyler DJ, "Malaria Chemoprophylaxis for the Traveler," N Engl J Med, 1993, 329(1):31-7.

Wyler DJ, "Malaria: Overview and Update," Clin Infect Dis, 1993, 16(4):449-56.