国: カナダ
言語: 英語
ソース: Health Canada
ATOVAQUONE
GLAXOSMITHKLINE INC
P01AX06
ATOVAQUONE
750MG
SUSPENSION
ATOVAQUONE 750MG
ORAL
210 ML
Prescription
MISCELLANEOUS ANTIPROTOZOALS
Active ingredient group (AIG) number: 0124073001; AHFS:
APPROVED
2001-08-07
_ _ _Page 1 of 38_ _ _ PRODUCT MONOGRAPH PR MEPRON ® Atovaquone Oral Suspension, USP 750 mg/5 mL ANTIPROTOZOAL AGENT GlaxoSmithKline Inc. 7333 Mississauga Road Mississauga, Ontario L5N 6L4 Date of Revision: July 26, 2016 SUBMISSION CONTROL NO: 188021 _©_ _2016 GlaxoSmithKline Inc., All Rights Reserved. _ _MEPRON is a registered trademark of Glaxo Group Limited, used under license by GlaxoSmithKline Inc. _ _ _ _ _ _ _ _Page 2 of 38_ _ _ PRODUCT MONOGRAPH PR MEPRON ® Atovaquone Oral Suspension, USP 750 mg/5 mL ANTIPROTOZOAL AGENT CLINICAL PHARMACOLOGY Atovaquone is a hydroxy-1,4-naphthoquinone, an analog of ubiquinone, with anti- pneumocystis activity. The mechanism of action against _Pneumocystis carinii_ has not been fully elucidated. The pharmacokinetics of atovaquone have been studied in healthy volunteers, HIV- infected adults with varying stages and manifestations of HIV infection and in immunocompromised children. The half-life of atovaquone is long (2 to 3 days) due to presumed enterohepatic cycling and eventual fecal elimination. There is no evidence that the drug is metabolized in man. Atovaquone is a highly lipophilic compound with a low aqueous solubility. It is extensively bound to plasma proteins (>99.9%). The bioavailability of atovaquone is highly dependent on formulation and diet. MEPRON ® (atovaquone) Oral Suspension, which has now replaced MEPRON ® (atovaquone) Tablets, has atovaquone particles significantly smaller than those in the tablet formulation, and provides an approximately two-fold increase in atovaquone bioavailability in the fasting or fed state compared to the tablet formulation studied under the same conditions. The bioavailability of MEPRON ® (atovaquone) Oral Suspension can be increased greatly when administered with meals. In healthy volunteers, a standard meal (23 g fat; 610 kCal) increased the bioavailability two to three-fold following 750 mg single doses of atovaquone suspension. The mean area under the atovaquone _ _ _Page 3 of 38_ plasma concentration-time curve (AUC) 完全なドキュメントを読む