B / 16 : Progestins And Antiprogestins Flashcards
What is a natural progestin?
Progesterone
Why are synthetic progestins better?
Better oral bioavailability
Function of progestins
- Induce secretory changes in endometrium + breast proliferation
- Maintenance of pregnancy
- Metabolic effects (carbohydrate metabolism, stimulate fat deposition)
Side effects of progestins (5)
- Increased risk of breast cancer
- Decreased HDL
- Impairment of glucose tolerance
- Elevation of BP
- Headache
What are the pharmacologically used progesterones? (6)
- Medroxy[progesterone]-acetate
- Cyproterone-acetate
- Drospirenone
- Norethisterone
- Levonorgestrel
- Desogestrel
Medroxyprogesterone-acetate, drospirenone, cryproterone acetate
- MOA
- Effect
- Indication
- ROA
- Synthetic progesterone
- Thicken cervical mucus, inhibition of ovulation
- For hormonal contraception, hormone replacement, treatment of estrogen-dependant tumors
- Oral
In what ways can progesterone analogs be used in hormone replacement therapy?
Primary hypogonadism, postmenopausal therapy
Norethisterone
- MOA
- Effect
- Indication
- Synthetic progesterone
- Androgen / anabolic action
- Inhibit implantation, does not support pregnancy
Levonorgestrel, Desogestrel
- MOA
- Indication
- SE
- Synthetic progesterone
- Contraceptive progestin
- Increased risk of venous thromboembolism
What are the anti-progestins?
- Mifepristone
- Ulipristal acetate (morning after pill)
(Think of a priest with his falily/mif and his hair looks very oily/uli and his wife is pregnant)
Mifepristone
- MOA
- Effect
- Indication
- SE
- ROA
- Progestin and glucocorticoid receptor antagonist
- No more progesterone to maintain pregnancy
- For medical abortion with misoprostol
- Vomiting, abdominal pain
- Oral
Ulipristal acetate
- MOA
- Effect
- Indication
- SE
- ROA
- Selective progestin receptor antagonist
- Inhibits progesterone maintaining pregnancy
- Emergency contraceptive (within 5 days)
- Headache, tiredness, GI disturbances
- Oral
(-acetate : something to do with progestins)
What are the forms the combination agents can be used in?
Monophasic / biphasic / triphasic
MOA of estrogen + progesterone combinations
- Selective inhibition of pituitary function : no LH surge -> inhibition of ovulation
- Changes in the cervical mucosa, endometrium, motility and secretion of the tubes
Other uses for contraceptives (6)
- Treatment of acne
- Hirsutism
- Dysmenorrhea
- Endometriosis
- Prevent estrogen deficiency in hypogonadism
- Reduce cysts and cancers
