P2 PHARAMCOLOGY Flashcards
Main androgens in the body are
Testosterone & Dihydrotestosterone
Sources of androgens
- Testes
- Adrenal glands
- Prostate cancer cells
a surgical castration that is the Least expensive & simplest form of androgen deprivation therapy
Orchiectomy
route & frequency of administration of LHRH agonist
Injected every month or by SC mini-
osmotic pump implant once a year
First injection of LHRH agonists initially increases testosterone levels before reaching very low levels , this is known as
flare phenomenon
what conditions the flare phenomenon may worsen
- bone pain
- pain / paralysis
- urinary difficulty
how to avoid the flare phenomenon
by giving anti-androgens during initial weeks
Examples of LHRH agonists
leuprolide, goserelin, triptorelin
Continuous (non-pulsatile) administration effects of LHRH agonists results in
- Reduced LH & FSH secretion
- ovarian suppression
Intermittent(pulsatile) administration effects of LHRH agonists results in
-Increased LH & FSH secretion
- Controlled ovarian stimulation for ovulation induction in ART
the inhibition of FSH & LH release by sustained non-pulsatile results in
hypogonadotropic hypogonadism
Examples of LHRH antagonist
Degarelix, Relugolix
MOA of LHRH antagonist
- Competitive antagonist of GnRH receptors
- Inhibit secretion of FSH & LH
route & frequency of administration of LHRH antagonist
a monthly SC injection
ADR of LHRH antagonist
pain , redness & swelling at the injection site
Mention at least 3 ADR of Androgen deprivation therapy
- anemia , fatigue
- reduced libido , impotence
- testicular & penile atrophy
- hot flashes , breast tenderness & gynecmastia
- weight gain
- dyslipidemia
- osteoporosis , fractures
what drug is given to lower adrenal androgens
Abiraterone
MOA of Abiraterone
block the enzyme CYP17
which anti-fungal drug block the production of androgens in adrenal glands
Ketoconazole
MOA of Androgen Receptor Antagonists
Block androgen receptors in prostate
examples of Androgen Receptor Antagonists
Flutamide, bicalutamide, enzalutamide, apalutamide
drugs used initially to prevent tumor flare
Flutamide; bicalutamide, enzalutamide, apalutamide
(androgen receptor antagonists )
ADRs OF estrogens that caused them not be used anymore
thromboembolism & gynecomastia
drug that is given by IV for multi-drug resistant organisms causing UTI
Colistin
Colistin ADR
Nephrotoxic and neurotoxic