MEFLOQUINE HYDROCHLORIDE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

MEFLOQUINE HYDROCHLORIDE (UNII: 5Y9L3636O3) (MEFLOQUINE - UNII:TML814419R)

Available from:

Physicians Total Care, Inc.

INN (International Name):

MEFLOQUINE HYDROCHLORIDE

Composition:

MEFLOQUINE HYDROCHLORIDE 250 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Mefloquine hydrochloride tablets are indicated for the treatment of mild to moderate acute malaria caused by mefloquine-susceptible strains of P. falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax . There are insufficient clinical data to document the effect of mefloquine in malaria caused by P. ovale or P. malariae . Mefloquine hydrochloride tablets are indicated for the prophylaxis of P. falciparum and P. vivax malaria infections, including prophylaxis of chloroquine-resistant strains of P. falciparum . Use of mefloquine hydrochloride tablets is contraindicated in patients with a known hypersensitivity to mefloquine or related compounds (eg, quinine and quinidine) or to any of the excipients contained in the formulation. Mefloquine hydrochloride tablets should not be prescribed for prophylaxis in patients with active depression, a recent history of depression, generalized anxiety disorder, psychosis, or schizophrenia or other major psychiatric disorders,

Product summary:

Mefloquine Hydrochloride tablets 250 mg are round, white to off white tablets, scored, debossed GP 118 on one side and plain on the reverse side, and are supplied as follows: NDC 54868-5434-0 bottles of 6 tablets NDC 54868-5434-1 bottles of 8 tablets Store at 20°-25°C (68°-77°F) (see USP Controlled Room Temperature).

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

MEFLOQUINE HYDROCHLORIDE - MEFLOQUINE HYDROCHLORIDE TABLET
PHYSICIANS TOTAL CARE, INC.
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DESCRIPTION
Mefloquine hydrochloride is an antimalarial agent available as 250 mg
tablets of mefloquine
hydrochloride (equivalent to 228.0 mg of the free base) for oral
administration.
Mefloquine hydrochloride is a 4-quinolinemethanol derivative with the
specific chemical name of (R*,
S*)-(±)-α-2-piperidinyl-2,8-bis
(trifluoromethyl)-4-quinolinemethanol hydrochloride. It is a 2-aryl
substituted chemical structural analog of quinine. The drug is a white
to almost white crystalline
compound, slightly soluble in water.
Mefloquine hydrochloride has a calculated molecular weight of 414.78
and the following structural
formula:
The inactive ingredients are crospovidone, lactose monohydrate,
low-substituted hydroxypropyl
cellulose, magnesium stearate, microcrystalline cellulose,
pregelatinized starch and talc.
CLINICAL PHARMACOLOGY
PharmacokineticsAbsorption
The absolute oral bioavailability of mefloquine has not been
determined since an intravenous
formulation is not available. The bioavailability of the tablet
formation compared with an oral solution
was over 85%. The presence of food significantly enhances the rate and
extent of absorption, leading to
about a 40% increase in bioavailability. In healthy volunteers, plasma
concentrations peak 6 to 24 hours
(median, about 17 hours) after a single dose of mefloquine. In a
similar group of volunteers, maximum
plasma concentrations in mcg/L are roughly equivalent to the dose in
milligrams (for example, a single
1000 mg dose produces a maximum concentration of about 1000 mcg/L). In
healthy volunteers, a dose
of 250 mg once weekly produces maximum steady-state plasma
concentrations of 1000 to 2000 mcg/L,
which are reached after 7 to 10 weeks.
Distribution
In healthy adults, the apparent volume of distribution is
approximately 20 L/kg, indicating extensive
tissue distribution. Mefloquine may accumulate in parasitized
erythrocytes. Experiments conducted _in_
_vitro_ with human bl