Drugs affecting reproductive system

Drugs related to female hormones

Estrogens Antiestrogens Progesterone and progestogens Antiprogestogens Female contraception drugs

Drug related to male hormones

Androgens Antiandrogens Anabolic steroids Male contraception drugs

Estrogens 1. Pharmacological effects

(1) Development of the female genital tract and of the female secondary sex characeteristics (!) Maintenance of both proliferative and secretory phases of the uterine endometrium (") #vulation$ (small doses) or (larger doses) (%) Development of the breast and lactescence (small doses) or (larger doses) (&) #ther actions$ decreasing postmenopausal disturbances in sleep inhibiting the reabsorption of bone increasing aldosterone and causing 'ater and (a) retention decreasing *D* and increasing +D* levels in plasma increasing factor ,,- .,,- ,/- / and coagulation

2. Clinical uses
(1) Postmenopausal syndrome$ Postmenpausal hormone replacement therapy (+01)$ prevention of osteoporosis2 3 Fractures of the spine- 'rist- and hips decrease by &43546 and spinal bone density increases by 7&6 in 'omen treated 'ith estrogen 'ithin " years of the onset of menopause and for &814 years thereafter treat vasomotor 9 :(; symptoms 3 hot flushes- vaginal dryness- urinary stress incontinence- chilly sensations- di<<iness- fatigueirritability- and s'eating prevention of cardiovascular disease 3lo'ers *D* -1=2 raises +D* levels 3endothelial vasodilatation properties - anti3inflammatory (!) Primary hypogonadism ()$ replacement

vaginal atrophy- hypoestrogenism (") Menstrual disorders amenorrhea - dysmenorrhea- and oligomenorrhea2 severe dysfunctional uterine bleeding (%) :ontraception (&) #thers$ suppress lactation after child birth advanced breast cancer (postmenopausal) and prostatic cancer 3hormone3sensitive or hormone3receptor3positive cancers 3hormone therapy- or anti3estrogen therapy (not to be confused 'ith hormone replacement therapy) acne neuroprotection

3. Adverse effects
(1) #ral administration$ nausea-vomiting- diarrhea (!) :ardiovascular effects$ ris> of venous thromboembolisis plasma triglycerides hypertension- edema (") #thers$ gallbladder disease ris> of breast and endometrial carcinoma

Clomifene ( ) (1) Effects (2) !ses

Partial agonist?antagonist for estrogen receptor

anovulatory infertility () menstrual disorders advance breast cancer functional amenorrhea () amenorrhea galactorrhea syndrome ()

(3) Adverse effects

Multiple ovulation 'ith multiple pregnancy () ovary tumefaction () ovarian carcinoma follo'ing multiple exposure

Progestogens 1. Pharmacological effects

(1) :onverting the uterine epithelium from the proliferative to the secretory phase (!) ,nhibiting *+ secretion and ovulation (") Development of galactophore

(%) 1hermoregulation$ increasing body temperature (&) Metabolism$ antagoni<ing aldosterone- inducing hepatic drug3metaboli<ing en<yme

2. Clinical uses
(1)Menstrual disorders secondary amenorrhage- exacerbated uterine bleeding- dysmenorrhea ( ) and premenstrual syndrome- etc artificially induce progestogen 'ithdra'al bleeding 3 (orethindrone acetate 3medroxyprogesterone acetate (!) :ancers megestrol acetate solid malignancy- especially gastric and pancreatic cancerimprove appetite and reduce 'asting used in combination 'ith dexamethasone effects ta>e several 'ee>s to become apparent- but are relatively long3lived compared to those of corticosteroids the only drugs to increase lean body mass (") #thers endometriosis ()- hormone replacement therapy (+01)- premature pregnancy ()- etc

3. Adverse effects
=, reactions edema virili<ation () acne hirsulism () 'eight gain etc

"ifepristone Clinical uses

1 Medical termination of intrauterine pregnancies of up to %@ days gestation " termination of pregnancies bet'een 1" and !% 'ee>s gestation softening and dilatation of the cervix prior to mechanical cervical dilatation for pregnancy termination in combination 'ith gemeprost % *abor induction in fetal death in utero & emergency contraceptive used in smaller doses (14 mg) ta>en after sex but before ovulationprevent ovulation and so prevent pregnancy

C. Contraceptive drugs #or female

(1) ,nhibition of ovulation (!) Prevention of fertili<ation (") ,nhibition of implantation (%) Ase of spermicides in the vagina

#or male
(1) Direct inhibition of spermatomatogenesis (!) ,ndirect inhibition of spermatomatogenesis ;teroid contraceptives for female

Estrogens $ progestogens 1. Pharmacological effects

(1) ,nhibition of ovulation (!) ,nhibition of implantation (") ,ncrease in viscidity of cervical mucus (%) #thers$ interfering uterus or oviducal motility

2. Clinical uses
(1) #ral$ short3acting contraceptives long3acting contraceptives postcoital () contraceptives (!) long3acting inBections (") ;lo'3releasing preparations (%) Multiphasic preparations

3. Adverse effects
(1) =, reactions (!) Menstrual disorders$ brea>through bleeding- amenorrhea (") ,ncreased coagulation$ venous thromboembolism (%) #thers$ edema- depression- 'eight gain- acne- hirsutism- etc

%. Drug interactions
+epatic en<yme inducers attenuate the effect of contraceptive drugs

Contraceptives for male &ossypol

1his compound destroys elements of the seminiferous epithelium ( ) but does not alter the endocrine function of the testis =, and hepatic reactions- hypopotassaemia- etc ;timulatants of uterus #xytocin Pituitrin Ergot al>aloid

Prostaglandins 0elaxants of uterus 0itodrine 1erbutaline ;albuterol Magnesiun sulfate

'(ytocin Pharmacological effects

Aterine contraction important for cervical dilation before birth and causes contractions during the second and third stages of labor assist the uterus in clotting the placental attachment point postpartum3 during the first fe' 'ee>s of lactation +o'ever- in >noc>out mice lac>ing the oxytocin receptor- reproductive behavior and parturition are normal

Clinical uses
;mall doses (!3& A)$ rhythmic contraction2 induction of labor *arge doses (&314 A)$ tonic contraction2 postpartum hemorrhage relatively safe 'hen used at recommended doses- and side effects are uncommon :autions in induction of labor

Ergot al)aloid Pharmacological effects

1 Aterine smooth muscle stimulation ;electively and determined by the functional state of the uterus ! .essel3contracting effect Directly contract artery and venous vessels Damage vascular endothelial cells at high dose *ead to dry gangrene of the extremities after long term use " C3receptor bloc>ing effect

0everse the DP3elevating effect of (A

!sed in
uterus bleeding postpartum hemorrhage migraine

Adverse effects
=, disturbances$ diarrhea- nausea- and vomiting prolonged vasospasm

Contraindications
obstructive vascular2 pregnancy

Prostaglandins
dinoprostoneP=E! dinoprostP=F! sulprostone carboprost

!sed in
Abortion$ combined 'ith mifepristone Facilitation of labor

Adverse effects
=, disturbances$ nausea- vomiting and abdominal pain

Contraindications

bronchial asthma2 glaucoma