Androgenic Drugs 3) 17α-methyltestosterone

➔ addition of methyl group

- Androgenic Medications: ➔ 1:1 ratio (have similar androgenic and anabolic effect)
➔ Replacement therapy for decreased endogenous testosterone ➔ Longer duration of action
(Hypogonadism) ➔ Not safe & not commonly used
- Anabolic Medications: ➔ S/E: hepatotoxicity and reduces HDL level
➔ Muscle wasting
➔ Osteoporosis ❖ Orally active testosterones

The drugs 1) Fluoxymesterone

➔ 1:2 ratio
❖ Orally inactive testosterones ➔ Hypogonadism
1) Exogenous Testosterone ➔ Breast cancer
➔ Treatment for hypogonadism • Decreasing the levels of estrogen (anti-estrogenic
➔ 1:1 ratio (have similar androgenic and anabolic effect) effect)
➔ used as transdermal patch or gel
2) Oxandrolone
2) Testosterone Esters ➔ 1:30 ratio
➔ adding an ester group, ➔ Hypogonadism
➔ 1:1 ratio (have similar androgenic and anabolic effect) ➔ Muscle wasting
➔ Treatment for hypogonadism ➔ Osteoporosis
➔ given as IM injections
➔ Longer duration of action 3) Danazol
➔ Examples: ➔ Androgenic effect
• Testosterone cypionate (5-7 days) ➔ Anti-estrogenic effect, Thus treat:
• Testosterone enanthate (4-5 days) • Endometriosis
• Fibrocystic breast disease

4) Dehydroepiandrosterone (DHEA):
➔ Claim that it has anti-aging and anti-inflammatory effects (not
very true.)
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 Anti-androgens • Premature closure of the ductus arteriosus →
Oligohydramnios
▪ Interfere with binding between androgens and their receptors ➔ C/I:
▪ MOA: • Ulcerations & bleeding tendency
- Inhibition of 5α-reductase • Low amniotic fluid around the baby
➔ ↓ DHT thus ↓ its effects
- Androgen Receptor Inhibitors: 2) Calcium Channels Blockers
The drugs: ➔ Example: Nifedipine
➔ Oral administration
1) Finasteride (Propecia) ➔ Very effective, DOA: 7 days
➔ 5α-reductase inhibitor ➔ less adverse effects if compared to the β2 agonists.
➔ Given orally ➔ First line:
➔ Treatment of benign prostatic hyperplasia • More than 32 weeks
➔ Treatment of alopecia • 32 weeks & less & Indomethacin is C/I
2) Flutamide ➔ Second line:
➔ Androgen receptor blockers • 32 weeks & less & Indomethacin isn’t effective
➔ Treatment of prostate cancer ➔ S/E: Patients with CVS problems will experience reflux.

Modulators of uterine motility 3) β2-Agonists.

➔ Example: Ritodrine & Terbutaline
Tocolytic Therapy ➔ Not used as first line therapy
▪ ↓ Uterine contractility, for: ➔ Used as second line therapy after nifedipine
➔ Prevent premature labor OR Delay of labor. ➔ Oral and injectable
➔ S/E: tachycardia, hyperglycemia, fluid retention.
1) Prostaglandin Synthesis Inhibitors ➔ Very effective, DOA: 2 to 7 days
➔ Example: Indomethacin
➔ Orally & rectally 4) Nitrates
➔ Very effective, DOA: 2-7 days ➔ Transdermal patches
➔ Used in pregnancy less than 32 weeks after that will cause: ➔ DOA: 2 days, least effective.

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 5) Oxytocin Blockers 2) Misoprostol
➔ Example: Atosiban ➔ PG E Analogues
➔ Expensive and found in injectable forms ➔ Oral & vaginal tablets
➔ Has similar effect to β2 agonists ➔ Used during 2nd trimester pregnancy, (Used if baby is died)
➔ Not used as first line therapy • Cause Cervical Ripening (softening to the cervix)
➔ Used as second line therapy after nifedipine ➔ S/E: GI upset
➔ S/E: intrauterine growth retardation 3) Mifepristone
6) Magnesium Sulfate ➔ Progesterone Receptor Blockers
➔ Reduce the influx of calcium ➔ Used for:
➔ Rarely used, serious S/E • Terminating pregnancy during early pregnancy
➔ Serious adverse effects - In range of 70-77 days of pregnancy, (illegal)
• Cardiac arrest ➔ 3-office-visits protocol
• NMJ block • 1st visit: administer Mifepristone.
• Respiratory distress • 2nd & 3rd visits: Misoprostol.
• Affects the fetus ➔ S/E: hemorrhage & infection.
Stimulant Therapy Estrogen-Based Therapeutics
▪ Stimulate the contractility of uterus, for: ▪ Hormone replacement therapy:
➔ Labor Induction & Postpartum Uterine Atony - Post-menopausal hormone therapy
➔ ↓ Postpartum Hemorrhage. ➔ When symptoms are annoying
1) Pitocin ➔ Lowest dose and the shortest period
➔ Oxytocin Analogues ➔ Estrogen combined with progesterone
➔ Injectable. • To ↓ risk of endometrial cancer
➔ First line therapy in hospitals. - Patients with estrogen deficiency
• Better effect during late pregnancy: ➔ Estrogen combined with progesterone
➔ S/E: • To ↓ risk of endometrial cancer
• Uterine Hypertonicity (higher doses → ruptures) ▪ Contraception:
• Water Intoxication, due to prolonged use. - Exogenous estrogen will reduce the level of Estrogen
• Fetal/neonatal complications ➔ No ovulation

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The drugs:
▪ S/E: Endometrial hyperplasia and malignancies.
❖ Naturally occurring estrogens
- Estradiol
➔ Metabolized by liver & excreted by bile & urine & low DOA Raloxifene
❖ Synthetic estrogen analogs: ▪ No effect in endometrium.
▪ In breast tissues:
- Ethinyl estradiol & Mestranol & Estradiol valerate
➔ Act as antagonists on estrogen receptors
➔ Metabolized by liver & excreted by bile & urine
➔ Used for:
➔ More duration of action.
• Treatment of breast cancer
S/E: • Prophylaxis for susceptible people

▪ In bone:
- Increase the risk of endometrial and breast cancers ➔ Act as agonist on estrogen receptors:
❖ Selective Estrogen Receptor Modulators ➔ Decreased bone resorption & Increased bone density
➔ Decreased vertebral fractures
- Agonists & Antagonist effects depending on the tissues ➔ Prevention & treatment of post-menopausal
Tamoxifen osteoporosis
▪ S/E:
▪ Orally ➔ Increased risk of deep vein thrombosis
▪ In breast tissues: ➔ Pulmonary embolism
➔ Act as antagonists on estrogen receptors ➔ Retinal vein thrombosis
➔ Used for:
• Treatment of breast cancer
• Prophylaxis for susceptible people Progesterone -Based Therapeutics
❖ Naturally occurring progestogens
▪ In endometrial tissues
➔ Act as agonist on estrogen receptor - Progesterone
➔ Should use for short period. ➔ Metabolized by liver & excreted by bile & urine & low DOA.

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❖ Synthetic progestogens analogs:
▪ Progestin-only pills (Mini pills)
- Norgestrel, Levonorgestrel
- Less effective than combination
➔ 19-nortestosterone derivatives
- Indications:
➔ More duration of action compared to natural
➔ Female intolerant to estrogen
➔ S/E: acne & increase hair growth
➔ Breast-feeding female
➔ Smokers
- Medroxyprogesterone
▪ Injectable progestin
➔ Oral tablets:
- Medroxyprogesterone
• For HRT: half-life: 30 days
- S/E:
➔ Injectable:
➔ Weight gain
• Contraceptive: half-life: 40-50 days ➔ Amenorrhea
Contraceptive medications ➔ Delayed fertility
➔ Bone loss and osteoporosis:
▪ Combination oral contraceptives: - Should not be continued for more than 2 years
- Monophasic combination pills
➔ Constant dose of estrogen & progesterone ▪ Vaginal ring
- Triphasic oral contraceptive - MOA:
➔ Variable dose of hormones to mimic natural female cycle ➔ Via negative feedback:
- MOA: • Reduce the release of LH and FSH → prevent ovulation
➔ Via negative feedback: - Very effective as oral contraceptives
• Reduce the release of LH and FSH → prevent ovulation
➔ Progesterone increase: ▪ Emergency Contraceptives
• Thickening of cervical mucus → Block sperm entrance. - Should be taken within 72 hours after intercourse

▪ Transdermal patch
- Less effective in obese females
- Increase chance of S/E.
➔ Thromboembolism

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