Pharmacology Flashcards
tamoxifen uses
breast cancer, menopausal women
tamoxifen moa
competitive inhibition of endogenous estrogen binding to target tissue. estrogen-responsive gene expression altered, prevents cell activation and proliferation
administration of tamoxifen
oral
side effects of tamoxifen
hot flush
risk of endometrial cancer
vte
tamoxifen metabolism
liver cyp3a4 (affected by grapefruit)
cyp2d6 (cough and cold meds can affect)
tamoxifen toxicity
neurotoxicity (tremor, dizziness)
pembrolizumab moa
pd1 blocker, binds to pd1 of T cell and prevents cancer cell from binding, preventing inhibition of T cell activation
pembrolizumab uses
inhibits cancer metastasis
pembrolizumab se
infusion related se
ND
joint pain
LT immune related inflamx on lung
pembrolizumab ci
corticosteroids
imunosuppressants
pregnant
hypersensitivity to other ab therapy
leuprorelin moa
analogue, inhibition of pituitary GnRH release, reduces androgen production in testes, androgen-sensitive prostate cancer cells undergo apoptosis
leuprorelin monitoring
first few weeks of therapy: PSA
after 4 weeks of therapy: LH, FSH, TTS
leuprorelin administration
SC or IM at 1,2,3 mths interval
leuprorelin se
infusion pain
flushes
headache
gi disturbances
libido loss
leuprolide ci
hypersensitivity to gnrh agonists
heart disease
risk for osteoporosis
bicalutamide moa
androgen receptor antagonist, impairs cell proliferation and triggers apoptosis in cancer cells
bicalutamide administration
oral
bicalutamide se
gynaecomastia
fatigue
sexual dysfunction
gi
biaclutamide metab
liver
tamoxifen uses
breast cancer, menopausal women
tamoxifen uses
breast cancer, menopausal women
metformin uses
t2dm
obese pt
metformin moa
inhibits gluconeogenesis in liver, upregulate protein kinase, increasing glucose uptake into tissues
metformin se
anorexia
gi disturbances
vit b12 deficiency
metformin excretion
urine (avoid patients with renal insufficiency)
glipizide moa
SU bind to SU receptor proteins and inhibits Katp channel mediated K+ efflux, triggering clacium dependent exocytosis of insulin granules from pancreatic B cells.
glipizide metab
liver
glipizide ae
hypogly, weight gain
sitagliptin moa
dpp4i, prolongs action of endogenous incretins
sitagliptin ae
gi disturbances
flu-like symptoms
skin reactions
careful in patients with pancreatitis
liraglutide uses
weight loss in obese patients
reduced risk of cvs complications
liraglutide moa
glp receptor agonist, upregulates cAMP and PKA, leads to increased insulin secretion and decreased glucagon release
liraglutide distribution
extended action due to long half life
empagliflozin moa
inhibits sglt2, decreased reabsorption of glucose and renal threshold for glucose. increased urinary glucose excretion
empagliflozin ae
uti
increased urination
diabetic ketoacidosis
carbimazole moa
reduce thyroid hormone synthesis by inhibiting thyroid peroxidase which is needed to give precursor of T3 and T4.
carbimazole uses
hyperthyroidism. before surgery
carbimazole ae
rash
joint pain
jaundice
nausea
agranulcytosis (rare)
carbimazole metab
cyp450, fmo (LIVER)
levothyroxine uses
restore levels of T4
levothyroxine moa
synthetic t4, body uses it to be converted to active T3 via deiodinase
levothyroxine admin instruction
30-60 minutes before breakfast / 4 hours after dinner
- Iron supplements / antacids / milk: at least 2 hours apart
affected by antacids, ppi
levothyroxine ae (overcompensation leading to hyperthy)
anorexia
anxiety
diarrhoea
hair loss
levothyroxine ci (signs of anxiety)
cardiac dysfunction
seizures
levothyroxine monitoring
serum tsh first 6-8 weeks
tamsulosin moa
reversible alpha 1 adrenoceptor blocker, prevents vasoconstriction induced by catecholamines that lead to contraction of internal sphincter of bladder, allowing urine to flow
does tamsulosin have effect on blood pressure?
no. great selectivity for a1A (blood vessels in prostate)
tamsulosin ae
abnormal ejaculation
back pain
tamsulosin metab
liver (cyp)
tamsulosin ci
concurrent usage of a1 antagonists
finasteride moa
competitively inhibits 5a reductase, prevents conversion of TTS to DHT, reduces prostate size growth
finasteride monitoring
PSA levels, take up to 6 months
finasteride ae
libido loss
finasteride metab
liver
finasteride ci
women/children
pregnant
sildenafil moa
pde5i in penis, increase cGMP causing SM relaxation and increased blood flow to corposa cavernosa -> erection
sildenafil metab
liver
sildenafil ci
cardiac pt on GTN (VD effect potentiated)
sildenafil ae
dizziness
priaprism (LT)
blur vision (LT)
headache
flushing
ethinyl estradiol moa
estrogen receptor agonist, inhibits FSH release and suppress development of ovarian follicle
endometrium made unsuitable for implantation
ethinyl estradiol metab
liver
enterohepatic circulation
ethinyl estradiol ae
breast tenderness
headache
bloating
weight gain
ethinyl estradiol LT ae
VTE
MI
ethinyl estradiol CI
- hx of thrombosis
- advanced diabetes with CVS
- uncontrolled HTN
- breastfeeding (<21d postpartum)
- breast cancer women
norethindrone moa
synthetic progestogen, inhibits LH release and prevents ovulation
endometrium unsuitable for implantation
norethindrone ae
headache
dizziness
weight gain
bloating
amenorrhea
spotting