Gestagens

Definition
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Female sex hormones that serve to create and maintain a pregnancy.

Pharmacodynamics (Effect)
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Inhibition of estrogen-induced endometrial proliferation, cycle regulation in dysfunctional bleeding and cycle abnormalities.

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Indication
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Moderate forms of acne vulgaris, hirsutism, female alopecia androgenetica, oral contraception (see Table 1).

Limited indication
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Z.n. apoplexy, Z.n. deep vein thrombosis, bladder mole, Z.n. intracerebral hemorrhage, endogenous depression, diabetes mellitus, epilepsy, Z.n. extrauterine pregnancy, Z.n. pemphigoid gestationis, heart failure, hypercholesterolemia, migraine, Z.n. myocardial infarction, renal failure, porphyria, Z.n. thromboembolism, thrombophlebitis.

Undesirable effects
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Weight gain, menstrual disorders, mastopathy, virilization, gastrointestinal disorders, cholestasis, icterus, acne, chloasma, alopecia, allergic reactions, thrombosis, blood pressure rise, depression, headaches, visual disturbances, hearing loss, myalgias, arthralgias.

Interactions
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See Table 2.

Contraindication
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Pregnancy (virilization of female fetuses), lactation, restrained miscarriage, unclear vaginal bleeding, severe acute or chronic pregnancy. liver disease.

Tables
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Brief overview of common progestogens

Active substance	Concentration [mg]	Application	Examples of ready-to-use preparations
Chlormadinone acetate	2	p.o.	Gestafortin Tbl.
Dydrogesterone	10	p.o.	Duphaston tbl.
Hydroxyprogesterone caproate	250	i.m.	Proluton Depot Amp.
Levonorgestrel	0,03	p.o.	Microlut
Levonorgestrel	0,052	p.o.	Mirena
Lynestrenol	5	p.o.	Orgametril tbl.
Medrogeston	5	p.o.	Prothil 5 mg tbl.
Medroxyprogesterone acetate	2,5/5/10	p.o.	Clinofem 2.5/5/10 tbl.
Medroxyprogesterone acetate	150	i.m.	Clinovir depot
Norethisterone acetate	1/5	p.o.	Norethisterone 1/5 mg
	5	p.o.	Primolut Nor 5 tbl.
	10	p.o.	Primolut Nor 10 tbl.
Norethisterone antate	200	i.m.	Noristerate
Progesterone	90	Gel	Crinone 8% vaginal gel
	100	p.o.	Utrogest Kps.
	10	Gel	Progestogel Gel

Major interactions of progestogens

Amoxicillin	Progestogen levels temporarily ↓ due to damage to intestinal flora
Ampicillin	Progestogen levels transient ↓ due to damage to intestinal flora
Barbiturates	Progestin degradation ↑, effect of low-dose progestins ↓
Butazones	Progestogen effect ↓
Carbamazepine	Effect of low-dose progestogens ↓
Insulin	Glucose tolerance disorder
Metformin	Glucose tolerance disorder
Phenytoin	Progestin degradation ↑
Rifampicin	Progestin depletion ↑
Sulfonylureas	Blood sugar lowering or ↓
Tetracyclines	Progestogen effect ↓ through damage to the intestinal flora