Term
| Therapeutic Indications of Progestins |
|
Definition
Contraception in females
Hormone replacement therapy (HRT)
Menstrual disorders
Dysmenorrhea (painful menstruation)
Endometriosis (functional endometrial tissue outside the uterus)
Endometrial carcinoma |
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|
Term
Antiprogestins:
Mifepristone (RU-486):
Mechanism: |
|
Definition
| High affinity for progesterone receptor competitive decrease of endogenous progesterone |
|
|
Term
Antiprogestins
Mifepristone (RU-486):
Indications |
|
Definition
Therapeutic abortion:
Alone: +/-70%
Combined with prostaglandins: +/- 95% |
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|
Term
|
Definition
Oral contraceptives (OCC)
Injections and implants
Transdermal patch |
|
|
Term
|
Definition
Combination of estrogen and progestin
Most popular |
|
|
Term
Types:
Monophasic
Bi- or triphasic |
|
Definition
Types:
Monophasic: fixed dose
Bi- or triphasic: variable dose |
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|
Term
|
Definition
|
|
Term
| How long are combineed OCCs taken for? |
|
Definition
| Combined OCC are taken daily for 21 days and stopped 7 days |
|
|
Term
| How long are minipills taken for? |
|
Definition
| Minipill is taken daily without break |
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|
Term
Mechanism of Action of OCC
Estrogen-progestin combinations: |
|
Definition
Suppress ovulation:
decrease GnRH from hypothalamus decrease FSH & LH from pituitary
Thicken cervical secretions (not optimal for sperm migration)
Inhibit implantation |
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|
Term
Mechanism of Action of OCC
Low-dose progestin: |
|
Definition
Thicken the cervical secretions (not optimal for sperm migration)
Inhibit implantation
variable suppression of ovulation by effect on FSH/LH |
|
|
Term
|
Definition
Salt and water retention edema
Hypertension
Vascular disorders:
Thromboebolic, coronary artery or cerebrovasular disease
Higher risk in smoker women above 35 years
Headache – migraine
Depression
Postpill amenorrhea |
|
|
Term
| Absolute contraindications of OCC |
|
Definition
Pregnancy
Breast feeding
Thromboebolic disease:
Coronary artery disease
Cerebrovasular disease
Breast/cervical cancer
Undiagnosed vaginal bleeding |
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|
Term
| Relative contraindications of OCC |
|
Definition
Hypertension
Impaired Liver Function
Migraine |
|
|
Term
|
Definition
Long acting progestins
Injections:
IM injection every 3 months
E.g., Medroxyprogesterone (provera) |
|
|
Term
|
Definition
Implants:
SC insertion of small capsules
Effective for 3 – 5 years
E.g., Levonorgestrel (norplant) |
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|
Term
| Hormone Replacement Therapy |
|
Definition
| Estrogen replacement in postmenopausal woman |
|
|
Term
| What has a lower dose of estrogen, contraceptives or HRT |
|
Definition
|
|
Term
| What can be added to HRT and why? |
|
Definition
| Progestins to reduce the risk of endometrial carcinoma. |
|
|
Term
| What can be added to HRT and why? |
|
Definition
| Progestins to reduce the risk of endometrial carcinoma. |
|
|
Term
|
Definition
Osteoporosis (decrease in bone mass)
Flushing, headaches and insomnia
Genital tract atrophy
Cardiovascular disease (improvement of lipid profile) |
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|
Term
| Name 4 natural (endogenous) androgens |
|
Definition
Testosterone
Dihydrotestosterone
Dehydroepiandrosterone (DHEA)
Androstenedione |
|
|
Term
| Name 3 types of synthetic androgens |
|
Definition
Methyltestosterone
Ethyloestrenol
Stanozolol |
|
|
Term
|
Definition
Regulate gene expression by activating a nuclear receptor
Development of primary & secondary male sex characters
Maturation of sperms
Anabolic effect:
some synthetic androgens (e.g., stanozolol) have more anabolic than androgenic activity |
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|
Term
Therapeutic Indications of Androgens
Hormone replacement: |
|
Definition
Hypogonadism in males
Hypopituitarism |
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|
Term
Therapeutic Indications of Androgens
Anemia refractory to treatment: |
|
Definition
| Androgens stimulate erythropoiesis |
|
|
Term
Therapeutic Indications of Androgens
Breast cancer (estrogen- or progestin-receptor positive): |
|
Definition
| Androgens may downgrade receptor expression |
|
|
Term
Therapeutic Indications of Androgens
Anabolic agents: |
|
Definition
Compensate for protein loss: e.g., after trauma, surgery or prolonged immobilization
Often abused by body builders and athletes |
|
|
Term
| What are teh 2 types of male hypogonadism? |
|
Definition
Primary: testicular failure
Secondary: hypothalamic-pituitary disease |
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|
Term
| Treatment and aim of male hypogonadism: |
|
Definition
Androgen replacement
Aim: Stimulate development of male secondary sex characters
Maintain muscle and bone mass |
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|
Term
| Regimen of androgen replacement for male hypogonadism: |
|
Definition
Oral: TDS
Transdermal patch: every 24 hours
IM injection: every 2-3 weeks
Subdermal implants: every 4-6 months |
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|
Term
Hyperandrogenemia:
In prepubertal male children: |
|
Definition
|
|
Term
Hyperandrogenemia
in females |
|
Definition
Virilization symptoms: hirsutism, acne, amenorrhea, clitoral enlargement and deepening of voice
During pregnancy: masculinization of external genitalia of infants |
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|
Term
Anti-androgens
Androgen suppressors (leuprolide acetate): |
|
Definition
Reduce testosterone to 10% of basal levels
Used to treat:
Prostatic carcinoma
Endometriosis |
|
|
Term
Anti-Androgens
Receptor inhibitors (cyproterone acetate): |
|
Definition
Used to treat:
Prostatic carcinoma
Hirsutism and virilization in women
Precocious puberty in boys |
|
|
Term
Male Oral Contraceptive:
Gossypol:
Actions: |
|
Definition
Derived from seeds of cotton plant
First used in China
Action:
Inhibition of sperm production |
|
|
Term
| Efficacy and adverse effects |
|
Definition
Efficacy is comparable to the female OCC
Adverse effects:
Irreversibility
Hypokalemia |
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|
