Mifepristone

Drug #486

Mifepristone is a synthetic progesterone antagonist, related to norethindrone. Chemically Mifepristone is identified as (11ß,17ß)-11-[ 4-(dimethylaminoamino) phenyl ]-17-hydroxy-17-(1-propynyl) estra-4, 9-dien-3-one. Mifepristone is used orally for termination of pregnancy up to 9 weeks gestation.it should be used only in centres licensed under the abortion act. If abortion is not complete after 36-48 hrs, treatment with gemeprost should be given surgical abortionmay be used if drug treatment fails.

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Primary Characteristics

It is of Synthetic origin and belongs to Norethisterone.

It belongs to Progesterone antagonist pharmacological group on the basis of mechanism of action and also classified in Abortifacients pharmacological group.

Molecular Weight: 429.6 · pK_a: 3.7 · Solubility in Water: poorly · Solubility in Alcohol: 1 in 20 · Non-proprietary name: Mifepristone.

Pharmacokinetics

Absorption: Mifepristone has an oral bioavailability is 70%.

Distribution: Mifepristone has a plasma protein binding is 98 %.

Elimination: it is metabolised via Hepatic, plasma half-life is 18hr, renal excretion is 9 %.

Indications

Mifepristone is primarily indicated in conditions like Abortion, Contraception, Cushing's syndrome, Hypothyroid coma, Induction of labour, Menstruation disorders, Muscle spasm of varied aeitology, Routine management of the 3rd stage of labour, Severe nausea and vomiting (prevention), Softening and dilatation of cervix before mechanical cervical dilatation, Termination of pregnancy of 13-24 weeks gestation.

Contraindications

None recorded.

Dosage

Mifepristone's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
600 mg	600 mg	—		Up to 49 days for termination of pregnancy.
12 mg/kg	12 mg/kg	—	PO	Once
Paediatric Dosage (20kg)
0 – 0	—	—	—	Not Recommended under 12 Yrs Paeds
Neonatal Dosage (3kg)
0 – 0	—	—		Not recommended in this age group

Drug Interactions

Unknown1 interaction

3 interactions

Moderate1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Mifepristone in overdosage may give rise to further complications which include Hypotension , Hypotension , Hypersensitivity reactions .

Mifepristone is known to cause more or less tolerable side effects which are usually transient. These include Chills, Dizziness, Fever, GI craps, Headache, Heavy bleeding, Malaise, Urtercaria.

Warnings / Precautions

Mifepristone should not be given to patients with chronic adrenal failure, haemorrhagic disorders or those receiving anticoagulants or long term corticosteroid therapy, impaired liver or kidney function. It should be used with caution in patients with chronic obstructive air way disease, asthma or cardiovascular disease. It is not recommended to use during pregnancy.

Interference in Pathology

Mifepristone may interfere in the diagnosis of SGPT level disturbance. , Hematocrit Value , Changes in alkaline phosphatase activity.

Available Brands

None recorded.

Storage Conditions

Mifepristone should be stored Tab.

Drug Classification

1.18.3.1 — Hormonal contraceptives