UNWANTED - KIT
COMPOSITION:
Each kit contains,
(A) One Mifepristone Tablets IP
Mifepristone IP. 200mg
(B)Four Misoprostol Tablets IP
Misoprostol IP. 200mcg
DOSAGE FORM:
For oral use-Mifepristone tablets
For vaginal use-Misoprostol tablets
DESCRIPTION:
The unwanted kit is a combi pack of 1 tablet of Mifepristone 200mg and 4 tablets of Misoprostol 200mcg. Mifepristone tablet is to be administered orally and Misoprostol is to be given vaginally for the medical termination of pregnancy up to 9 weeks. This kit has been developed in accordance with guidelines issued by the Royal College of Obstetricians and Gynecologists, UK. Mifepristone exhibits anti-progestational activity i.e by inhibiting the activity of progesterone, mifepristone results in termination of pregnancy. Mifepristone also shows anti -glucocorticoid and weak anti-androgenic activity. Misoprostol is synthetic prostaglandin E1 analogue. Misoprostol promotes softening of the cervix and contraction in the uterus and also inhibits gastric acid secretion in humans.
PHARMACOLOGY:
Pharmacodynamic
(A)Mifepristone
Mifepristone shows anti-progestational activity by competitive interaction with progesterone at progesterone-receptor sites. Based on studies with various oral doses in several animal species(mouse, rat, rabbit, and monkey), the compound inhibits the activity of endogenous or exogenous progesterone which results in termination of pregnancy. Doses of 1mg/kg or greater of mifepristone have been shown to antagonize the endometrial and myometrial effects of progesterone in women. During pregnancy, the compound sensitizes the myometrium to the contraction inducing the activity of prostaglandins mifepristone also exhibits anti glucocorticoid and weak antiandrogenic activity. Doses of 4.5mg/kg or greater in human beings resulted in a compensatory elevation of adrenocorticotropic hormone (ACTH) and cortisol. The antiandrogenic activity was observed in rats following repeated administration of dose from 10 to 100mg/kg.
(B)Misoprostol
Misoprostol causes myometrial contraction by interacting with specific receptors on myometrial cells which results in a change in calcium concentration, thereby initiating muscle contraction. Misoprostol interacts with prostaglandin receptors and causes the cervix to soften and the uterus to contract, ultimately resulting in the expulsion of the uterine contents.
Pharmacokinetics
(A) Mifepristone
(a)Absorption
Mifepristone is rapidly absorbed after oral administration of a single dose of 200mg, with a peak plasma concentration of 1.98mg/l occurring approximately 90 minutes after ingestion. The absolute bioavailability of a 20mg oral loss is 69%.
(b)Distribution
Approximately 98% of mifepristone in plasma protein is bound to both albumin and alpha 1-acid glycoprotein. Binding to the latter protein is saturable, and the drug displays nonlinear kinetics with respect to plasma concentration and clearance.
COMPOSITION:
Each kit contains,
(A) One Mifepristone Tablets IP
Mifepristone IP. 200mg
(B)Four Misoprostol Tablets IP
Misoprostol IP. 200mcg
DOSAGE FORM:
For oral use-Mifepristone tablets
For vaginal use-Misoprostol tablets
DESCRIPTION:
The unwanted kit is a combi pack of 1 tablet of Mifepristone 200mg and 4 tablets of Misoprostol 200mcg. Mifepristone tablet is to be administered orally and Misoprostol is to be given vaginally for the medical termination of pregnancy up to 9 weeks. This kit has been developed in accordance with guidelines issued by the Royal College of Obstetricians and Gynecologists, UK. Mifepristone exhibits anti-progestational activity i.e by inhibiting the activity of progesterone, mifepristone results in termination of pregnancy. Mifepristone also shows anti -glucocorticoid and weak anti-androgenic activity. Misoprostol is synthetic prostaglandin E1 analogue. Misoprostol promotes softening of the cervix and contraction in the uterus and also inhibits gastric acid secretion in humans.
PHARMACOLOGY:
Pharmacodynamic
(A)Mifepristone
Mifepristone shows anti-progestational activity by competitive interaction with progesterone at progesterone-receptor sites. Based on studies with various oral doses in several animal species(mouse, rat, rabbit, and monkey), the compound inhibits the activity of endogenous or exogenous progesterone which results in termination of pregnancy. Doses of 1mg/kg or greater of mifepristone have been shown to antagonize the endometrial and myometrial effects of progesterone in women. During pregnancy, the compound sensitizes the myometrium to the contraction inducing the activity of prostaglandins mifepristone also exhibits anti glucocorticoid and weak antiandrogenic activity. Doses of 4.5mg/kg or greater in human beings resulted in a compensatory elevation of adrenocorticotropic hormone (ACTH) and cortisol. The antiandrogenic activity was observed in rats following repeated administration of dose from 10 to 100mg/kg.
(B)Misoprostol
Misoprostol causes myometrial contraction by interacting with specific receptors on myometrial cells which results in a change in calcium concentration, thereby initiating muscle contraction. Misoprostol interacts with prostaglandin receptors and causes the cervix to soften and the uterus to contract, ultimately resulting in the expulsion of the uterine contents.
Pharmacokinetics
(A) Mifepristone
(a)Absorption
Mifepristone is rapidly absorbed after oral administration of a single dose of 200mg, with a peak plasma concentration of 1.98mg/l occurring approximately 90 minutes after ingestion. The absolute bioavailability of a 20mg oral loss is 69%.
(b)Distribution
Approximately 98% of mifepristone in plasma protein is bound to both albumin and alpha 1-acid glycoprotein. Binding to the latter protein is saturable, and the drug displays nonlinear kinetics with respect to plasma concentration and clearance.
(c) Metabolism
Mifepristone is metabolized in the liver to N-didesmethyl & N-monodesmethyl compounds. CYP450 3A4 is primarily responsible for the metabolism.
The three metabolites identified in humans are: (1) RU 42 633, most widely found in plasma, is the N monodmethylated metabolite; (2) RU 42 848, which result from the loss of two methyl groups from the 4-dimethylaminophenyl in position 11beta; (3) RU 42 698, which result from the terminal hydroxylation of the 17-propynyl chain.
(d) Excretion
The main route of elimination of mifepristone is faecal. By 11days after a 600mg dose of a titrated compound, 83% of the drug has been accounted for by the faeces and 9% by the urine, serum level is undetectable by 11 days.
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