Pharm - Rami Pt 2 Flashcards
bisphosphonates uses
osteoporosis,
paget disease,
hypercalcemic bone metastasis
side effect of bisphosphonates
osteonecrosis of jaw (rare)
paget disease (osteitis deformans) first sign and hallmark
first sign: increased ALP,
hallmark: ivory vertebra
cushing’s syndrome
increased cortisol levels
cushing’s disease
increased cortisol levels due to overactive ACTH
dexamethasone suppression test
increases cortisol which should cause negative feedback
in cushing’s disease negative feedback will not happen so cortisol levels will remain high
colchicine MOA
induces microtubular polymerization by binding tubulin,
decreased migration of leukocytes (less inflammatory response)
colchicine use
acute gout attacks (also use NSAIDs like indomethacin or naproxen)
colchicine side effect
diarrhea
probenecid MOA
decreases reabsorption of uric acid in PCT by blocking active transport of uric acid
probenecid use
prevention of further gouty attacks (prophylaxis)
probenecid side effect
inhibition of renal excretion of penicillin and NSAIDs
allopurinol use
prevention of further gouty attacks (prophylaxis)
allopurinol MOA
inhibits xanthine oxidase (stops conversion of xanthine to uric acid)
allopurinol side effects
hypersensitivity reaction,
decreased metabolism of 6-mercaptopurine and azathioprine
orlistat MOA
inhibits lipase (decreased intestinal fat absorption), anti-obesity drug
orlistat side effects
steatorrhea
fecal incontinence,
decreased absorption of fat soluble vitamins
sibutramine MOA
serotonin, NE, and dopamine reuptake inhibitor,
anti-obesity drug
sibutramine side effect
sexual dysfunction
fen-phen (phentermine) MOA
increased catecholamine release in brain
anti-obesity drug
fen-phen (phentermine) side effects
increased risk of valvular disease and pulmonary hypertension,
withdrawn from market
flutamide MOA
competitive antagonist at androgen receptor,
decreases growth effects of testosterone on prostate
flutamide use
prostate cancer treatment
flutamide needs to always be given with what other drug and why?
leuprolide,
counteract increase LH levels caused by lower testosterone
flutamide side effects
gynecomastia,
LFTs
finasteride MOA
inhibits 5 alpha reductase (inhibits conversion of testosterone to DHT which stimulates prostate gland growth)
finasteride uses
BPH,
prostate cancer,
early male pattern baldness
finasteride side effects
decreased libido,
erectile dysfunction
leuprolide (naferelin and goserelin) MOA
GnRH agonist
eventual desensitization and downregulation of GnRH leads to decreased LH and decreased testosterone
leuprolide side effects
impotence,
hot flashes
leuprolide uses
metastatic prostate cancer,
leiomyomas,
infertility (given in pulsatile fashion)
danazol MOA
agonist at androgen and progesterone receptors,
decreased LH and FSH secretion
increases levels of C1 esterase inhibitor
danazol uses
endometriosis,
hereditary angioedema
danazol side effects
androgenic side effects in women (masculinization, hirsutism, acne)
clomiphene MOA
partial agonist at estrogen receptors in the pituitary gland,
decreases normal feedback inhibition
increases LH and FSH secretion
clomiphene use
infertility in patients with ovulatory dysfunction (polycystic ovary syndrome)
clomiphene side effects
hot flashes, abdominal discomfort, multiple pregnancies (10%)
anastrazole MOA
inhibits aromatase (decreases conversion of androgens to estrogens), results in decreased estradiol levels
anastrazole side effects
osteoporosis,
increased CV events,
hyperlipidemia
tamoxifen MOA
competitive estrogen receptor antagonist;
minimizes growth effect of estrogen
tamoxifen most effective in
postmenopausal women
tamoxifen side effects
increased risk of endometrial cancer,
increased risk of thromboembolism,
hot flashes
raloxifene MOA
like tamoxifen but mixed estrogen agonist/antagonist effects
raloxifene uses
treats osteoporosis and reduces risk of breast cancer without increased risk of endometrial cancer
breast cancer drugs
anastrazole,
tamoxifen,
raloxifene
oral contraceptive pills
made of a mix of synthetic estrogens and progestins
progestins
decrease GnRH release,
decrease FSH and LH levels,
inhibit follicular development and absence of ovulation
oral contraceptive pill side effect
increased risk of thromboembolism especially in women > 35
emergency contraception
high doses of synthetic progestins (up to 72 hours)
mifepristone MOA
competitive antagonist of progesterone receptor;
abortifacient at high doses
octreotide MOA
synthetic analog of somatostatin hormone;
inhibits release of many hormones
octreotide uses
treats many endocrine disorders (zollinger ellison syndrome, carcinoid syndrome, acromegaly)
oxytocin MOA/uses
made by posterior pituitary,
stimulates uterine contraction to induce labor,
stimulates breast milk let down,
controls post partum uterine hemorrhage
vasopressin released from
posterior pituitary
V1 receptor (vasopressin)
vasoconstriction
V2 receptor (vasopressin)
increase permeability to water in collecting ducts
V3 receptor (vasopressin)
increase factor 8 activity
vasopressin uses
central diabetes insipidus,
septic shock,
cardiac arrest
vasopressin side effect
hyponatremia
omeprazole (-prazole) MOA
proton pump inhibitor,
irreversibly inhibits H/K pump on parietal cells
ranitidine MOA
H2 receptor blocker,
reversibly blocks binding of histamine to H2 receptor on parietal cells
ranitidine uses
GERD, PUD
ranitidine side effect
gynecomastia
antacids MOA
weak bases acting to reduce acidity
antacids use
GERD
side effects of antacids
AlOH - constipation,
MgOH - diarrhea,
calcium carbonate - hypercalcemia, milk-alkali syndrome,
sodium bicarbonate - flatulence, metabolic alkalosis
ondansetron MOA
blocks 5-HT3 receptors present in chemoreceptor trigger zone in brainstem (part of vomiting reflex pathway)
promethazine MOA
blocks H1 receptor,
decreases GI motility
promethazine side effets
blurry vision, dry mouth (histaminergic block)
metoclopramide MOA
blocks D2 dopamine receptors present in chemoreceptor trigger zone in medulla (part of vomiting reflex pathway)
metoclopramide uses
treats diabetic gastroparesis (stimulates intestinal motility),
anti-emetic
anti-emetics
metoclopramide,
ondansetron,
promethazine
think: “get an anti-emetic or we’ll need a MOP”
ursodiol MOA
decreases incidence of cholesterol gallstones by:
- inhibits HMG-CoA reductase
- decreasing intestinal reabsorption of cholesterol
- inhibits secretion of cholesterol into bile
ursodiol uses
primary biliary cirrhosis,
cholesterol gallstones
sulfasalazine MOA
metabolized by bacteria in colon to sulfapyridine and 5-ASA,
5-ASA –> anti inflammatory
sulfasalazine uses
inflammatory bowel disease,
RA/juvenile arthritis
anti-diarrheals
diphenoxylate,
loperamide
anti-diarrheal MOA
bind opioid receptors in intestine leading to inhibition of ACh release,
decreases gut peristalsis
anthracyclines
doxorubicin,
daunorubicin,
idarubicin
anthracyclines MOA
block DNA and RNA synthesis,
produce oxygen free radicals,
disrupt fluid and ion transport,
DAMAGE DNA
use of doxorubicin
solid tumors and hematologic malignancies (leukemia, lymphoma, myeloma)
think: “DEOXYRIBOSEin” to remember you’re damaging DNA
daunorubicin uses
acute leukemia (AML, ALL, CML) neuroblastoma
think: “does in daun on you at ALL?”
idarubicin use
AML
side effects of anthracyclines
cardiac toxicity,
give dexrazoxane to decrease free radicals (less damage to myocytes)
ages for ALL, CLL, AML, CML
ALL - child,
CLL - over 60,
AML - 65,
CML - 45-85
dactinomycin MOA
antibiotic derived antineoplastic agent,
inhibits DNA dependent RNA polymerase,
only antineoplastic agent that interferes with RNA synthesis
dactinomycin uses
wilms tumor,
ewing sarcoma,
used with methotrexate to treat, gestational choriocarcinoma
dactinomycin side effects
bone marrow suppression,
“radiation recall” - patients with previous radiation may have skin abnormalities
similar drug to dactinomycin used to treat testicular cancers and Paget disease of bone?
plicamycin
bleomycin MOA
triggers formation of oxygen free radicals
DAMAGES DNA
bleomycin use
testicular tumors
bleomycin side effects
pulmonary fibrosis,
anaphylaxis,
bone marrow suppression is rare
think: “patients on bleo have trouble blowing air”
MOA of all alkylating agents
damage DNA by cross linking DNA strands
busulfan use
CML (philadelphia chromosome)
think: “take the bus to Philly (CML)”
busulfan side effects
pulmonary fibrosis,
adrenal insufficiency,
hyperpigmentation,
seizures
nitrosoureas (carmustine, streptozocin) uses
brain tumors (glioblastoma) - one of the few agents that cross the BBB streptozocin also used for insulinomas
nitrosoureas side effects
nephrotoxocity,
pulmonary fibrosis
cisplatin and carboplatin use
GU tumors
carboplatin and cisplatin side effects
nephrotoxicity (give amifostine to scavenge free radicals),
ototoxicity,
neurotoxicity
cyclophosphamide uses
treats solid and hematologic malignancies
also suppresses B and T cell function (along with cross linking DNA) - used as immunosuppressive drug to treat RA, SLE, Wegener granulomatosis, nephrotic syndrome
cyclophosphamide side effects
hemorrhagic cystitis (accumulation of metabolite acrolein in urine), bone marrow suppression
mechlorethamine use
part of MOPP - treats hodgkin lymphoma
procarbazine uses
part of MOPP,
hodgkin lymphoma,
brain tumors
patients should avoid what when taking procarbazine?
tyramine,
metabolite of procarbazine inhibits MAO
MOPP protocol
mechlorethamine,
vincristine (oncovin),
procarbazine,
prednisone
methotrexate MOA
inhibits dihydrofolate reductase (transforms folic acid to active form FH4 - precursor for thymidylate formation)
decreased DNA synthesis