PLAQUENIL- hydroxychloroquine sulfate tablet
Concordia Pharmaceuticals Inc.
DESCRIPTION
PLAQUENIL� (hydroxychloroquine sulfate) is a white or practically white, crystalline powder, freely soluble in water; practically insoluble in alcohol, chloroform, and in ether. The chemical name for hydroxychloroquine sulfate is 2-[[4-[(7-Chloro-4-quinolyl)amino]pentyl]ethylamino] ethanol sulfate (1:1).
he molecular weight of hydroxychloroquine sulfate is 433.95, and molecular formula is C18 H26 ClN3 O.H2 SO4 .
PLAQUENIL (hydroxychloroquine sulfate) tablets contain 200 mg hydroxychloroquine sulfate, equivalent to 155 mg base, and are for oral administration.
Inactive Ingredients: Dibasic calcium phosphate USP, hypromellose USP, magnesium stearate NF, polyethylene glycol 400 NF, polysorbate 80 NF, corn starch, titanium dioxide USP, carnauba wax NF, shellac NF, black iron oxide NF.
CLINICAL PHARMACOLOGY
Pharmacokinetics: Following a single 200 mg oral dose of PLAQUENIL to healthy male volunteers, the mean peak blood concentration of hydroxychloroquine was 129.6 ng/mL, reached in 3.26 hours with a half-life of 537 hours (22.4 days). In the same study, the plasma peak concentration was 50.3 ng/mL reached in 3.74 hours with a half-life of 2963 hours (123.5 days). Urine hydroxychloroquine levels were still detectable after 3 months with approximately 10% of the dose excreted was parent drug. Results following a single dose of a 200 mg tablet versus i.v. infusion (155 mg), demonstrated a half-life of about 40 days and a large volume of distribution. Peak blood concentrations of metabolites were observed at the same time as peak levels of hydroxycholoquine. The mean fraction of the dose absorbed was 0.74. After administration of single 155 mg and 310 mg intravenous doses, peak blood concentrations ranged from 1161 ng/mL to 2436 ng/mL (mean 1918 ng/mL) following the 155 mg infusion and 6 months following the 310 mg infusion. Pharmacokinetic parameters were not significantly different over the therapeutic dose range of 155 mg and 310 mg indicating linear kinetics.
INDICATIONS AND USAGE
Malaria
PLAQUENIL is indicated for the treatment of uncomplicated malaria due to P. falciparum, P. malariae, P. ovale, and P. vivax.
PLAQUENIL is indicated for the prophylaxis of malaria in geographic areas where chloroquine resistance is not reported.
Lupus Erythematosus
PLAQUENIL is indicated for the treatment of chronic discoid lupus erythematosus and systemic lupus erythematosus in adults.
Rheumatoid Arthritis
PLAQUENIL is indicated for the treatment of acute and chronic rheumatoid arthritis in adults.
DOSAGE AND ADMINISTRATION
One PLAQUENIL tablet contains 200 mg of hydroxychloroquine sulfate, which is equivalent to 155 mg base.
Take PLAQUENIL with a meal or a glass of milk.
