Endo/Repro Drugs Flashcards
terbutaline
b2 agonist
- activate adenylel cyclase -> raise cAMP-> phosphorylatase-> MLCK blocking
tocolytic
-suppress uterine smooth muscle
IV or PO
Ritodrine
b2 agonist
-activate adenylel cyclase -> raise cAMP -> phosphorylatase-> MLCK blocking
tocolytic
- suppress uterine smooth muscle
Magnesium Sulfate
tocolytic
IV
Competes w/ Ca and relaxes Smooth Muscle
Prevent seizures
Atosibane
Ocytocin receptor ANTAGONIST
delays labor
Pitocin
Oxytocin synthetic
oxytocic
Gq
Uterine contractions, milk let down, ADH and vasoactive and high concentrations
NO oral
Dinoprostone
prostaglandin (E)- hyperalgesia
oxytocic
softening of cervix
uterine contrations
abortifacent - vaginal suppository
- hydratiform mole
Gs
Carboprost
prostaglandin (F)
oxytocic
Uterine contractions
abortifacent
- IM
Gq
misoprostol
prostaglandin(E)
oxytocic
Softening of the uterus
uterine contractions
Vaginal or Oral
used / progesterone antagonist - mifepristone
Gs
Ergonovine
ergot
oxytocic
contraction of the uterus(NOT USED)
and postpartum bleeding
alpha adrenergic, dopaminergic and 5HT2 receptors
Ergotamine
ergot
Contraction of blood vessels - more for migraine HA
Indomethacin
reduces oxytocin induced uterine contractions
oxytocin receptor
Gq protein -> phospholiase C -> increased Ca
Need Mg and Cholesterol allosteric
Goserelin
GnRH analogue
-flare of symptoms before down regulation of receptors
prostate and ER + cancer (pre menopause)
low testosterone problems…
Leuprolide
GnRH Analogue
-flare of symptoms (given w/ flutamide) before down regulation of receptors
prostate and ER + cancer (pre menopause)
Low testosterone problems…
Degarelix
GnRH competitive antagonist
NO surge, much faster
in prostate and assister repro use
Shorter duration of action -> cost and compliance
Class promotes histamine release -> hypotension and allergic rxns, rash
Dutasteride
5 alpha reductase inhibitor
Testosterone -> DHT blocked
Used for BPH and baldness, prostate CA prevention
teratogenic
finasteride
5 alpha reductase inhibitor
Testosterone -> DHT blocked
Used for BPH and baldness, prostate CA prevention
teratogenic
Aminoglutethimide
Aromatase inhibitor- nonsteriodal/reversible
cholesterol -> pregnenolone (higher up)
Can mimic Adrenal Insufficiency
-myelosuppression
Anastrozole
aromatase inhibitor - nonsteriodal/reversible
testosterone ->estradiol in ovary (pre meno)
androstenedione -> estrone in adipose (POSTmeno)
polyarthralgia
bone density
Better lipid?
letrozole
aromatase inhibitor -nonsteriodal/reversible
testosterone ->estradiol in ovary (pre meno)
androstenedione -> estrone in adipose (POSTmeno)
polyarthralgia
bone density
better lipid?
Bicultamide
Anti androgen receptor
ADT therapy - Prostate
- given to fight flare w/ GnRH agonists( still have high testosterone but no effect)
Inhibit ligand binding and translocation
Not used long term or alone
Flutamide
Anti androgen receptor
ADT therapy - prostate
-given to fight GnRH agonist flare (still have high testosterone but no effect)
Inhibit ligand biding and translocation
not used long term or alone
older more side effects - gynectomastia, liver function, Diarrha, N/V, low testosterone effects
Nilutamide
Anti androgen receptor
ADT therapy - prostate
-given to fight GnRH flare (still have high testosterone but no effect)
Inhibit ligand binding and translocation
not used long term or alone
Raloxifene
anti estrogen(SERM)
oral, peaks hrs
NO benefit after 5 yrs
Good for all 3 - breast antagonist, uterus antagonist, bone agonist
tamoxifen
anti estrogen(SERM)
oral, peaks hrs
no benefit after 5yrs
GO TO drug for ER +
prevention of invasive carcinoma
Good: Breast antagonist, bone agonist
Given w/ GnRH analogue - due to inhib negative feedback (higher estradiol w/out)
Bad: Uterus agonist - endometrial CA
Also stroke risk
toremifene
Anti estrogen(SERM)
oral, peaks hrs
no benefit after 5 yrs
Good: Breast antagonist
Bad: Uterus agonist
Fulvestrant
anti Estrogen (SERD)
IM, peaks 7 days
Cyp3A4 concern
Competitive antagonist in EVERY tissue - hard on bone…
back pain, HA, phayngitis, GI
FAC regiment (1st)
5 fluoruacil
-anti metabolit
Adriamycin -doxyrubicin
- anthracycaline
- cardiotoxicity and local necrosis
cyclophasphamide
- alkylating agent
- hemorrhagic cyst worries
CMF regiment (2nd)
Cyclophosphamide
Methotrexate
- switch out of doxyrubacin when toxicity met
5 fluoruracil
-antimetabolite
Traztuzumab
Ab against HER2 surface marker
Paclitaxel
binds to tubulin to enhance and stabilize spindle formation
