Progesterone information from DrugsUpdate
P - Contraindicated in pregnancy
L - Caution when used during lactation
LI - Lab*
Progesterone also known as P4 (pregn-4-ene-3,20-dione) is a C-21 steroid hormone involved in the female menstrual cycle, pregnancy (supports gestation) and embryogenesis of humans and other species. Progesterone belongs to a class of hormones called progestogens, and is the major naturally occurring human progestogen.
Progesterone is commonly manufactured from the yam family, Dioscorea. Dioscorea produces large amounts of a steroid called diosgenin, which can be converted into progesterone in the laboratory.
Pharmacodynamics
Pharmacokinetics
Progesterone is the main hormone secreted by corpus luteum. It induces secretory changes in the endometrium, promotes mammary gland development, relaxes uterus, blocks follicular maturation and ovulation, and maintains pregnancy.
Absorption
Oral bioavailability is low.
Distribution
Highly bound to plasma proteins. Distributes into breast milk.
Metabolism
Hepatic; extensive 1st-pass effect.
Excretion
Via the urine (as sulfate and glucuronide conjugates).
Progesterone Indications / Progesterone Uses
Information Not Available
Progesterone Adverse Reactions / Progesterone Side Effects
GI disturbances, appetite/wt change, fluid retention, oedema, acne, skin rash, urticaria, depression, headache, fever, fatigue, breast changes, hirsutism, changes in libido, altered menstrual cycles or irregular menstrual bleeding (rare).
Precautions
Capsules: Progestins and estrogens should not be used for prevention of CV disease. The Women's Health Initiative study reported increased risks of MI, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women during 5 years of treatment with oral conjugated estrogens combined with medroxyprogesterone. In addition, increased risk of developing probable dementia was reported in postmenopausal women 65 years of age and older during 4 years of treatment with oral conjugated estrogens plus medroxyprogesterone. Although other doses of oral conjugated estrogens with medroxyprogesterone and other combinations and dosage forms of estrogens and progestins were not studied, in the absence of comparable data, these risks should be assumed to be similar. Because of these risks, prescribe estrogens with or without progestins at the lowest effective dose and for the shortest duration consistent with treatment goals and risks for the individual woman.
Special Precautions
Discontinue medications if there is sudden partial or complete loss of vision, proptosis or diplopia; migraine and embolic disorders; epilepsy, migraine, asthma, cardiac or renal dysfunction. History of depression, glucose tolerance and diabetic patients. May impair ability to drive or operate machinery. Avoid sudden withdrawal of progesterone; lactation.
Other Drug Interactions
Enhanced clearance with enzyme-inducing drugs eg, carbamazepine, griseofulvin, phenobarbital, phenytoin and rifampicin. Ketoconazole may increase serum levels of progesterone. May inhibit ciclosporin metabolism.
Other Interactions
Information Not Available
Dosage
Oral
Progestogen component of menopausal hormonal replacement therapy
Adult: 200 mg daily as a single daily dose at night for 12-14 days of each month.
Oral
Amenorrhoea
Adult: 400 mg daily for 10 days.
Oral
Dysfunctional uterine bleeding
Adult: 400 mg daily for 10 days.
Intramuscular
Dysfunctional uterine bleeding
Adult: 5-10 mg daily for 5-10 days until 2 days prior to expected onset of menstruation.
Intramuscular
Amenorrhoea
Adult: 5-10 mg daily for 5-10 days until 2 days prior to expected onset of menstruation.
Intramuscular
Recurrent miscarriage with progesterone deficiency
Adult: 25-100 mg twice weekly from the 15th day of pregnancy until 8-16 weeks. May increase to daily injection, if necessary.
Vaginal
Dysfunctional uterine bleeding
Adult: 45 mg every other day from the 15th-25th day of the cycle. May increase dose to 90 mg in non-responders.
Vaginal
Amenorrhoea
Adult: 45 mg every other day from the 15th-25th day of the cycle. May increase dose to 90 mg in non-responders.
Vaginal
Premenstrual syndrome
Adult: 200 mg daily, may increase to 400 mg bid. Treatment is usually started on days 12-14 of the cycle and continues until onset of menstruation. Same doses may also be given rectally.
Intrauterine
Contraception
Adult: Insert the device (containing 38 mg of progesterone) into the uterine cavity; efficacy can last up till 1 year.
Food(before/after)
Information Not Available
List of Contraindications
Progesterone and Pregnancy
Contraindicated in pregnancy
Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Progesterone and Lactation
Caution when used during lactation
Progesterone and Children
Safety and efficacy not established
Progesterone and Geriatic
Use with caution, usually starting at the low end of the dosage range, because of the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant diseases or other drug therapy.
Progesterone and Other Contraindications
Hypersensitivity; thrombophloebitis; cerebral apoplexy; severe hepatic impairment; undiagnosed vag bleeding, incomplete abortion, hormone-dependent carcinoma, as a diagnostic test for pregnancy; pregnancy. History or current high risk of arterial disease.
Storage
Information Not Available
Lab interference
Information Not Available
FOLLOW US:
