uworld Flashcards
methimazole (use, MOA)
- hyperthyroid
- prevents organification of coupling of iodine in the thyroid
metoclopramide (MOA, use)
- dopamine antagonist
- prokinetic and antiemetic properties: increase gastric motility and prevent nausea/vomiting
misoprostol (what is it, what is it used for)
- prostaglandin E1 analogue
- used to prevent NSAID ulcers
Sulfonylureas (MOA, use (be specific), and who you should be careful with)
- close K+ channel in beta islet cells, membrane depolarizes, triggers insulin release via increased intracellular calcium
- only useful in T2DM, need some beta function to release endogenous insulin
- risk of hypoglycemia in renal failure patients
Sulfonylureas (1st gen (2) vs 2nd gen (3) and SE of each generation)
- 1st gen: tolbutamide, chorpropramide … disulfram-like
- 2nd gen: glyburide, glimepiride, glipizide … hypoglycemia
bupropion (MOA, one bad SE, two benefits of using as opposed to other antidepressants)
- unknown MOA (sorry), but results in increased norepi and DA
- SE: Sz in bulimic pts
- benefits: smoking cessation and no sexual SE
name 4 SSRIs
-fluoxetine, paroxetine, sertraline, citalopram
name 2 SNRIs
-venlafaxine, duloxetine
name 4 MAOIs (MAO takes pride in shanghai) also what is the general MOA of MAOI’s
- tranylcypromine, phenelzine, isocarboxazid, silegiline (MAO-B selective)
- increases levels of monoamine neurotransmitters (norepi, serotonin, DA) by decreasing breakdown within neurons
alpha-glucosidase inhibitors (name 2 and MOA)
- acarbose, miglitol
- inhibit alpha glucosidase in intestinal brush border, delays hydrolysis of sugar and therefor glucose absorption
- best at lowering post-prandial hyperglycemia
acarbose and miglitol are ….. (class) used to treat ….
- alpha glucosidase inhibitors
- T2DM
nimodipine (special Ca2+ channel blocker), why?
-tx for vasospasm that is a common complication (up to 50%) 4-12 days after subarachnoid hemorrhage
B-blockers can be used in thyrotoxicosis because…
- high levels of thyroid hormone up regulate insertion of B-receptors into membranes, increasing sensitivity to sympathetic outflow (block those receptors)
- B-blockers also inhibit T4 –> T3 conversion
pyrazinamide (what is it used for, what is its unique characteristic)?
- RIPE treatment of TB
- most active in acidic environment like inside lysosomes
antidote for digoxin toxicity?
-magnesium (also effective in tornadoes de pointes)
finasteride (MOA, tx for… bonus for another use that is primarily cosmetic, but arguably as detrimental)
- 5-alpha-reductase inhibitor (prevent conversion from T- DHT)
- tx: BPH, bonus for… baldness
anastrazole (MOA)
- aromatase inhibitor
- post-menopausal women with breast cancer (shooting from the hip here, but maybe also precocious puberty or CAH to prevent early fusion of long bones)
palivizumab (MOA)
-monoclonal antibody agains F-protein in RSV
fidaxomicin (tx for) bonus for alternative option
- recurrent c. diff
- fecal implant
dobutamine (primarily affects… (receptor type) and is used in…)
- Beta 1 receptors
- cardiac stress testing
ethosuximide (MOA)
- blocks T-type Ca2+ channels
- tx for absence sz
phenytoin (MOA)
-blocks Na+ channels and delays rate of recovery
adenosine (MOA) and antagonists (2)
- opens K+ channels in cardiac pacemaker cells, prolonging K+ release and hyper polarizing them (more negative)
- prevents Ca+ T-type channels from opening, decreasing initial inward current of Ca+ (also hyper polarizing)
- caffeine and theophylline
niacin, increases levels of… name 3 side effects
- increases HDL, can lower LDL a little bit (MOA: decreases synthesis of VLDL and inhibits lipolysis in adipose)
- red, flushed face (due to prostaglandin mediated vasodilation, can be prevented with co-administration of aspirin.
- hyperglycemia.
- hyperuricema (exacerbate gout).
dapsone (MOA… generally speaking, major use, 2 side effects (one in a specific population))
- kind of like a sulfa, inhibits folate synthesis
- tuberculoid leprosy
- agranulocytosis
- hemolytic anemia in G6PD
polyethylene glycol (class)
-osmotic diuretic
procainamide (class, use, SE)
- class 1A anti-arrythmic
- best for suppressing arrhythmias from places normally responsible for automaticity
- can prolong QT, susceptible to v-tach, SLE
transpeptidases (what is it? i don’t know, i don’t know.)
-penicillin binding protein that crosslinks peptidoglycan (target of penicillins and cephalosporins)
daptomycin (tx, MOA, can’t be used in…, SE)
- tx: for for s. aureus when nothing else is working (MRSA)
- creates pores in the membrane which allows ions to leak, depolarizing cell, preventing DNA/RNA synthesis, leading to cell death
- inactivated by surfactant, no can do pneumonia
- SE: myopathy, monitor creatine kinase, careful with statins
linezolid (tx, MOA, SE)
- MRSA
- binds to 23s portion of 50s ribosomal subunit, preventing formation of 70s ribosome
- thrombocytopenia and optic neuritis
name the class 3 anti-arrythmetics (4)
- AIDS
- amiodarone, ibutilide, dofetilide, soltalol
what is DRESS syndrome
- drug reaction with eosinophilia and systemic symptoms
- 2-8 wks after starting new drug (anticonvulsants are high risk), marked eosinophilia and impressive rash that can coalesce into giant single plaque, fever, facial edema
- thought to involve reactivation of herpes virus followed by massive t-cell rxn. self resolving after a few weeks off drug
succinylcholine (MOA, SE) *sorry, its a beast
- depolarizing skeletal muscle relaxant
- acts at nicotinic ACh receptors (stimulating), but not degraded, resulting in constant stimulation and no chance for repolarization
- SE: because nicotinic ACh receptors are at non-selective channels, not only does Na+ rush in, but K+ rushes out, prolonged use in susceptible pts (people with lots of K+ around (crush, burn injuries, demyelinating dz)) can be in big trouble for cardiac arrhythmia
baclofen (MOA)
- GABA-b agonist in spinal cord, causes muscle relaxation
- used for muscle spasm (low back pain)
buspirone (MOA, use, not good for…)
- selective agonist of 5HT-1
- anxiolytic, minimal to no hypnotic effects, used in generalized anxiety disorder (good for pts who had problems with benzos prior, little risk of abuse)
- not good for immediate (or as needed) use as it take a couple weeks to start working
name 2 alpa-glucosidase inhibitors and tell me what they do, what they are used for.
- acarbose and miglitol
- inhibit brush border alpha-glucosidases, delaying sugar hydrolysis and limiting glucose absorption
- best for decreasing postprandial hyperglycemia
one potential side effect of PPAR-gamma drugs (and way to tx SE)
- peripheral neuropathy
- give ACE-I or ARB
GLP-1 analogs (name 2, MOA, shortcoming)
- exenatide, liraglutide
- they promote insulin sensitivity, inhibit glucagon action and do so, ONLY when hyperglycemic (inactive in normal fasting range)
- unfortunately, rapidly degraded by DPP-4 (t1/2 of 2 min)
DPP-4 inhibitors (what is the suffix, and why are they given?)
- suffix: -liptin
- to prevent breakdown of GLP-1 analogues
SGLT2 inhibitors (name 2, MOA, SE)
- canagliflozin, dapagliflozin
- increase glucose excretion
- increased risk of UTI, hypotension
direct Xa inhibitors (name 2 and their use)
- rivaroxaban, apixaban
- tx and prophylaxis for DVT and PE
- SE: bleeding
argatroban (name other drug in this class, use) and bonus fun fact about where the drug comes from…
- bivalirudin
- direct thrombin inhibitor
- used instead of heparin for anticoag when pts get HIT (IgG against heparin bound to platelets (PF4 complex))
- derivative of anticoagulant used by leeches
cilostazol (name other drug in this class, MOA, use)
- dipyridamole
- phosphodiesterase III inhibitor, increases cAMP in platelets, preventing aggregation
- also acts as a direct arterial vasodilator
- used in peripheral artery disease and prevention of stroke/TIA
abciximab and tirofiban (MOA and use)
- bind GIIb/IIIa on activated platelets, preventing aggregation
- used in percutaneous transluminal coronary angioplasty
terbinafine (use, MOA)
- oral anti fungal used for tinea capitis
- squalene epoxidase inhibitor
unusual benign liver mass associated with use of 2 drugs….
- hepatic adenoma
- OCP and steroids
- can resolve if you discontinue meds
pralidoxime
-regenerates ACh Esterase by dephosphorylation (only used in cases of organophosphate poisoning in which the drug phosphorylates AChE)
phenoxybenzamine vs phentolamine (also class)
- non-selective alpha antagonists
- phenoxybenzamine is non-reversible, phentolamine, is
clomiphene (class, MOA, use)
- SERM
- prevents negative feedback inhibition of estrogen at hypothalamus, resulting in increased FSH and LH… ovulation
- PCOS who want to get pregnant, promote ovulation
rituximab (moa, use)
- monoclonal antibody that targets CD20 receptors on lymphocytes
- used for lymphomas with CD20 positive cells
infliximab (moa, use (3))
- monoclonal antibody against TNF-alpha
- RA, ankylosing spondylitis, chrons
demeclocine (MOA, use, SE)
- ADH antagonist
- SIADH
- member of tetracycline family, all of those apply here
class 1A anti-arrhythmics, name 3, level of use-dependence (relative to other class 1) and SE
- quinidine, procainamide, disopyramide
- intermediate (less than C, more than B)
- QT prolangation, TORSADES
drugs that can cause “coronary steal syndrome” (2)
- dypyridamole, adenosine
- in ischemic heart, collateral vessels are already maximally dilated trying to get perfusion to areas that are being blocked by atherosclerosis etc, giving these drugs which are selective coronary vasodilators, you dilate all of the coronary vessels including those not leading to ischemic tissue, effectively stealing blood away from areas that need it most
handy feature of scopolamine in adjunctive tx for myasthenia graves…
-MOA: anti-cholinergic action, selectively at muscarinic receptors… can decrease side effects of acetylcholinesterase inhibitors used in myasthenia graves without taking away their beneficial action on muscles at nicotinic receptors
pilocarpine and carbachol (MOA and use)
- cholinergic agonists, (mostly) specific for receptors in the eye, cause miosis, increases anterior chamber angle, allowing for aqueous humor to move
- glaucoma
bethanochol (MOA and use)
- cholinergic agonist, stimulates gastric and cystic motility
- postoperative ileus and atonic bladder
sulfasalazine (loose MOA and more importantly use)
- inhibits cytokine, prostaglandin and leukotriene production (anti-inflammatory properties)
- used in chrons and ibd
cyproheptadine (MOA, special use)
- 1st gen antihistamine, which is a 5-HT2 serotonin antagonist
- can be used for serotonin syndrome
methyldopa (first line use for)
-HTN in pregnancy
cladribine (MOA, use, resistant to…)
- synthetic purine analog (incorporated into DNA, causing breaks…)
- used in hairy cell leukemia (very effectively)
- resistant to adenosine deaminase
dopamine agonists (3)
-bormocriptine (ergot), pramipexole, ropinerole (non-ergot)
COMT inhibitors (2, and site of action for each)
- entacapone (inhibits peripheral methylation of levadopa)
- tolcapone (inhibits central and peripheral methylation)
5 major sites of action of TCAs (primary neurotransmitters, central receptor (1), peripheral receptors (3))
- inhibit serotonin and norepi reuptake
- inhibit histamine 1 receptors (sedation)
- fast Na+ channels in heart (arrhythmia)
- peripheral alpha-1 blockade (vasoD especially orthostatic)
- antimuscarinic effect (systemic… atropine like)
amifostine (MOA, use)
- free radical scavenger
- used to protect against nephrotox assoc with DNA alkylating agents and platinum containing agents
GnRH agonists (one name and one “-ending”
- leuprolide
- “-relin” ie. nafarelin
anastrazole (MOA)
-aromatase inhibitor
flutamide
-competitive inhibitor at testosterone and DHT receptors
glargine and detamir (how often)
-once daily
NPH (how often)
-twice daily
short acting insulin (3)
-aspart, lispro and glulisine
denosumab (MOA, use)
- monoclonal antibody against RANK on osteoclasts
- osteoporosis, given as subQ injection twice a year
nevirapine (class) (bonus for 2 others in that class)
- NNRTI (does not have to be activated by cellular kinases)
- efavirenz, delaverdine
efavirenz (class) (bonus for 2 others in that class)
- NNRTI (doesn’t have tone activated by cellular kinases)
- delaverdine, nevirapine
pentazocine (MOA, possible SE)
- partial mu agonist, partial mu antagonist
- can precipitate opioid withdrawal
aldesluekin (MOA and use)
- synthetic IL-2
- metastatic melanoma and renal cell carcinoma
amifostine (use)
- free-radical scavenger
- prevents nephrotox assoc with cisplatin (and other platinum containing agents) that use ROS
N-acetylcysteine (3 uses)
- acetaminophen tox
- mucolytic (CF)
- prevent nephrotox associated with IV-contrast
amantidine (MOA and use)
- binds to M2 protein and prevents viral uncoating (influenza, rotavirus)
- increases availability of endogenous dopa (parkinson)
finasteride vs. flutamide
- finasteride is a 5-alpha reductase inhibitor (BPH)
- flutamide is a competitive inhibitor of androgens (prostate cancer)
fexofenadine
- second gen anti-histamine
- not associated with anti-muscarinic, anti-serotonergic, anti-alpha adrenergic affects
fenoldopam (MOA, use)
- novel dopamine antagonist (selective for D1)
- arterial dilation, particularly at kidney
- able to simultaneously increase blood flow to kidney and lower BP with added benefit of diuresis and natriuresis
4 drugs that cause serotonin syndrome
- tramadol
- linezolid
- ondansetron (5-HT3 antagonist)
- triptans (5-HT1b/1d