Combipack of Mifepristone Kuwait Tablets IP and Misoprostol Tablets IP abortion pills cytotec

Combipack of Mifepristone Kuwait Tablets IP and Misoprostol Tablets IP abortion pills cytotec

Mifepristone

Mifepristone exhibits anti-progestational activity resulting from competitive interaction with progesterone at progesterone-receptor sites. Mifepristone has been shown to antagonize the endometrial ial and myometrial effects of progesterone in women. During pregnancy, Mifepristone sensitizes the myometrium to the contraction-inducing activity of prostaglandins. All these result in termination of pregnancy

Misoprostol

Misoprostol is a synthetic prostaglandin Et derivative. Prostaglandin Et causes myometrial contractions by interacting with specific receptors on myometrial cells. This interaction results in a change in calcium concentration, thereby initiating muscle contraction. By Interacting with prostaglandin receptors, Misoprostol causes the cervix to soften and increases the amplitude and frequency of uterine contractions, resulting in the expulsion of the uterine contents.

PHARMACOKINETICS

Mifepristone

Absorption

Following oral administration of a single dose of 600 mg. Mifepristone is rapidly absorbed, with a peak plasma concentration of 1.98 mg/occurring approximately 90 minutes after ingestion. The absolute bloavailability of a 20 mg oral dose is 69%

Distribution

Mifepristone is 98% bound to plasma proteins, albumin andy-acid glycoprotein, Binding to the latter protein is saturable, and the drug displays nonlinear kinetics with respect to plasma concentration and clearance. Following a distribution phase, elimination of Mifepristone is slow at first (50% eliminated between 12 and 72 hours) and then becomes more rapid with a terminal elimination half-life of 18 hours.

Metabolism  Combipack of Mifepristone Kuwait Tablets IP and Misoprostol Tablets IP abortion pills cytotec

Combipack of Mifepristone Kuwait Tablets IP and Misoprostol Tablets IP abortion pills cytotec

Metabolism of Mifepristone is primarily via pathways involving N-demethylation and terminal hydroxylation of the 17-propynyl chain In vitro studies have shown that CYP450 3A4 is primarily responsible for the metabolism. The three major metabolites identified in humans an (1) RU 42 633, the most widely found in plasma, is the N-monodemethylated metabolite; (2) RU 42 848, which results from the loss of two methyl groups from the 4-dimethylaminophenyl in position 110; and (3) RU 42 698, which results from terminal hydroxylation of the 17-propynyl chain.

Excretion

By 11 days, after a 600 mg dose of titrated compound, 83% of the drug has been accounted for by the feces and 9% by the urine, Serum levels are undetectable by 11 days.

Special Populations

The effects of age, hepatic disease and renal disease on the safety, efficacy and pharmacokinetics of Mifepristone have not been Investigated.

Misoprostol

Misoprostol is extensively absorbed, and undergoes rapid Combipack of Mifepristone Kuwait Tablets IP and Misoprostol Tablets IP abortion pills cytotec

de-esterification to its free acid, which is responsible for its clinical activity and, unlike the parent compound, is detectable in plasma. The alpha side chain undergoes beta oxidation and the beta side chain undergoes omega oxidation followed by reduction of the ketone to give prostaglandin Fanalogs. The compound is a lipophilic methyl ester pro-drug and is readily metabolized to the free acid, which is the biologically active form. Following oral administration, the plasma Misoprostol levels increased rapidly, with a peak at 30 minutes, declined rapidly by 120 minutes, and remained low thereafter.Combipack of Mifepristone Kuwait Tablets IP and Misoprostol Tablets IP abortion pills cytotec

In contrast, after vaginal administration, the plasma concentration gradually in creased, reaching maximum levels after 70-80 minutes and slowly declined with detectable levels present after 6 hours. Vaginal Misoprostol was present in the circulation longer than oral Misoprostol and hence its duration of stimulation of the uterus exceeds that of oral Misoprostol Vaginal application of Misoprostol results in slower increases and iqwer peak plasma concentrations of Misoprostol acid Combipack of Mifepristone Kuwait Tablets IP and Misoprostol Tablets IP abortion pills cytotec