Mifepristone + Misoprostol Pharmacology

Mifepristone + Misoprostol

About Mifepristone + Misoprostol
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Mechanism of Action of Mifepristone + Misoprostol
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Pharmacokinets of Mifepristone + Misoprostol
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Onset of Action for Mifepristone + Misoprostol
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Duration of Action for Mifepristone + Misoprostol
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Half Life of Mifepristone + Misoprostol
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Side Effects of Mifepristone + Misoprostol
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Contra-indications of Mifepristone + Misoprostol
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Special Precautions while taking Mifepristone + Misoprostol
1.Any intrauterine device should be removed before treatment with mifepristone and misoprostol begins.
2.Pregnancy termination by surgery is recommended in cases when it fails to cause termination of intrauterine pregnancy.
3.Mifepristone may be administered by or under the supervision of a gynaecologist, able to assess the gestational age of an embryo and to diagnose ectopic pregnancies. The gynaecologist must also be able to provide surgical intervention in cases of incomplete abortion or severe bleeding, or have made plans to provide such care through others, and be able to assure the patient access to medical facilities equipped to provide blood transfusions and resuscitation, if necessary.
Pregnancy Related Information
N/A
Old Age Related Information
N/A
Breast Feeding Related Information
N/A
Children Related Information
N/A
Indications for Mifepristone + Misoprostol
Indicated for the medical termination of intrauterine pregnancy up to 63 days of gestation. For purposes of this treatment, pregnancy is dated from the first day of the last menstrual period in a presumed 28 days cycle with ovulation occurring at mid-cycle.
Interactions for Mifepristone + Misoprostol
N/A
Typical Dosage for Mifepristone + Misoprostol
The dosage is mifepristone 200 mg orally followed 1?3 days later by misoprostol 800 mcg
(4 tablets of 200 mcg) vaginally. The misoprostol may be administered by a clinician or
self-administered by the woman. For women at 49?63 days of gestation, if abortion has not occurred 4 hours after administration of misoprostol, a second dose of misoprostol 400 mcg
(2 tablets of 200 mcg) may be administered vaginally or orally (depending upon preference and amount of bleeding).
The patient should return for a follow-up visit approximately 14 days after the administration of mifepristone. This visit is very important to confirm by clinical examination or ultrasonographic scan that a complete termination of pregnancy has occurred.
Schedule of Mifepristone + Misoprostol
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Storage Requirements for Mifepristone + Misoprostol
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Effects of Missed Dosage of Mifepristone + Misoprostol
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Effects of Overdose of Mifepristone + Misoprostol
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Mifepristone

About Mifepristone
A synthetic steroid, Antiprogestin, Abortifacient,Antineoplastic Agent(Hormone Antagonist).
Mechanism of Action of Mifepristone
Mifepristone is a competitive progesterone receptor antagonist in the presence of Progestins. In the early stage of pregnancy Mifepristone blocks the uterine progesterone receptors and cause decidual breakdown. This leads to detachment of the blastocyst and decreases hCG production. This in turn decreases progesterone secretions from the corpus luteum and further augments decidual breakdown. These all results in increased uterine prostaglandin levels and sensitizes myometrium to contract. It also causes cervical softening and facilitates expulsion of the detached blastocyst
Mifepristone delay ovulation by its action on hypothalamus and pituitary rather than ovary and the mechanism is not known
Pharmacokinets of Mifepristone
Absorption: It is well absorbed after oral administration and its bioavailability is about 69%.
Distribution: It is widely distributed in protein bound from (94%) and also crosses the placenta.
Metabolism: It undergoes hepatic metabolism and forms 3 active compounds
Excretion: Mifepristone and its metabolites are excreted mainly through faeces and small amount in urine.
Onset of Action for Mifepristone
N/A
Duration of Action for Mifepristone
N/A
Half Life of Mifepristone
18 hours
Side Effects of Mifepristone
1.Dizziness
2.Headache
3.Diarrhea
4.Nausea
5.Vomiting
6.Back pain
7.Feeling tired
8.Hot flashes
9.Abdominal pain
10.Anorexia
11.Vginal bleeding
12.Bad-smelling vaginal discharge
13.Fainting
14.Irregular heartbeat
15.Palpitations
16.Chest pain
17.Fever
18.Redness, blistering, peeling or loosening of the skin, including inside the mouth
19.Skin rash
20.Uterine infections
Contra-indications of Mifepristone
1.Hypersensitivity to Mifepristone
2.Ectopic pregnancy
3.Adrenal failure
4.Patient on long term corticosteroid therapy
5.Haemorrhagic disorder
6.Concurrent anticoagulant therapy
7.Inherited porphyria
8.Hepatic impairment
9.Renal impairment
Special Precautions while taking Mifepristone
1.Asthma
2.Chronic obstructive pulmonary diseases
3.Cardiovascular diseases
4.Smoking
5.Alcoholism
6.Should be taken prior to and during surgical abortion to prevent rhesus immunisation.
Pregnancy Related Information
Contraindicated.
Old Age Related Information
Contraindicated
Breast Feeding Related Information
Contraindicated.
Children Related Information
Contraindicated
Indications for Mifepristone
1.Cervical ripening
2.Contraceptive pill
3.Termination of pregnancy
4.Induction of labour
Interactions for Mifepristone
Ketoconazole, itraconazole, erythromycin, and grape fruit may inhibit mifepristone metabolism.
Rifampicin, dexamethasone, phenytoin, phenobarbital, carbamazepine induce mifepristone`s metabolism.
Typical Dosage for Mifepristone
Adult:
1.Cervical ripening: 50 - 600mg to be taken 24 - 30 hour before surgery.
2.Postcoital contraception: 600mg as single dose within 3 days after intercourse.
3.Once a month contraceptive pill: 200mg as single dose on the second day after mid cycle.
4.Termination of pregnancy up to 49 days: 600 mg as single dose and after 2 days takes Misoprostol 400mcg as single dose.
5.Termination of pregnancy up to 63days: 600 mg as single dose and after 36 - 48 hours take Gemeprost vaginally.
6.Termination of pregnancy between 13 - 24 weeks of gestation: 600mg as single dose to be taken 36 - 48 hours before prostaglandin therapy
7.Induction of labour following intrauterine fetal death: 600mg / day for 2 days.
8.Softening and dilatation of cervix before surgical termination of pregnancy: 600 mg as single dose is given 36 - 48 hours before surgery.
Schedule of Mifepristone
N/A
Storage Requirements for Mifepristone
Store at 15 - 30 degree C. Protect from heat and light. Keep out of the reach of children
Effects of Missed Dosage of Mifepristone
For pregnancy termination: Does not apply
For other uses: Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Mifepristone
Give supportive measures and symptomatic treatment.

Misoprostol

About Misoprostol
A synthetic prostaglandin E1 (PGE1) analogue, Anti ulcer(antisecretory and protective),Abortifacient.
Mechanism of Action of Misoprostol
Misoprostol is a synthetic Prostaglandin E1 analog. It binds to the EP3 receptor on the basolateral membrane of the parietal cells and stimulates the inhibitory G protein (Gi) receptors. This will leads to decrease in intracellular cyclic AMP level and inhibits proton pump (H+K+ATPase) which exchange the extracellular K+ for intracellular H+ ion. By inhibiting the proton pump Misoprostol decreases gastric acid secretion. Misoprostol also binds to the EP3 receptor on the superficial epithelial cells of the lumen and stimulates the mucin and bicarbonate secretion and decreases nocturnal, basal and stimulated gastric acid secretion.
Pharmacokinets of Misoprostol
Absorption: Misoprostol is well absorbed after oral administration. Distribution: It is distributed in the body in protein bound form. Metabolism: Misoprostol is rapidly undergoes de-esterification and form active metabolite Misoprostol acid. Excretion: Metabolite is excreted mainly in the urine and small amount in the faeces.
Onset of Action for Misoprostol
30 minutes
Duration of Action for Misoprostol
3 hours
Half Life of Misoprostol
20 - 40 minutes
Side Effects of Misoprostol
1.Nausea
2.Vomiting
3.Diarrhoea
4.Abdominal pain
5.Headache
6.Dizziness
7.Dyspepsia
8.Flatulence
9.Constipation
10.Menorrhagia
11.Rashes
12.Dysmenorrhoea
Contra-indications of Misoprostol
1.Hypersensitivity to Misoprostol and other Prostaglandins
Special Precautions while taking Misoprostol
1.Cardiovascular disease
2.Cerebrovascular disease
3.Renal impairment


Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Contraindicated
NEONATES: contraindicated
Indications for Misoprostol
1.NSAID induced ulcer
2.Duodenal ulcer
3.Gastric ulcer
Interactions for Misoprostol
Analgesics: Increased risk of CNS toxicity with phenylbutazone.
Typical Dosage for Misoprostol
Adult: NSAID induced ulcer: 200mcg 4 times daily with meals and at bed time for atleast1 month and up to 2 month.
Duodenal ulcer, Gastric ulcer: 400 - 800 mcg/ day in 4 divided doses with meals and at bed time for 1 - 2 month.
Children: not recommended
Schedule of Misoprostol
N/A
Storage Requirements for Misoprostol
Store at 15 - 30 degree C in a tightly closed container. Protect from light.
Effects of Missed Dosage of Misoprostol
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Misoprostol
Give supportive measures and symptomatic treatment.

Home Delivery for Mifepristone + Misoprostol in Your City

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However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for mifepristone + misoprostol and other medicines and health products. Home delivery services for mifepristone + misoprostol may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

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Mifepristone + Misoprostol is a generic medicine name and there are several brands available for it. Some of the brands for mifepristone + misoprostol might be better known than mifepristone + misoprostol itself. If the pharmacy that's willing to deliver medicines to your home doesn't have mifepristone + misoprostol in stock, you can ask for one of the branded alternatives for mifepristone + misoprostol.