Pharmacology Flashcards
drug of choice = DOC
inhibitors of ACh synthesis, storage, release
hemicholinium-3, vesamicol, botulinum toxin
inhibitors of ACh degradation (AChE inhibitors)
edrophonium, neostigmine, pyridostigmine, ambenonium, physostigmine
diisopropyl flurophosphate
tacrine, donepezil, rivastigmine, galantamine
muscarinic receptor AGONISTS
methacholine (asthma challenge test)
carbachol, bethanechol, cevimeline, pilocarpine
nicotinic receptor AGONISTS
succinylcholine
muscarinic recept ANTAGONISTS
atropine
scopolamine
pirenzepine, methscopolamine, glycopyrrolate
ipratropium, tiotropium
oxybutynin, propantheline, terodiline, tolterodine, fesoterodine, trospium, darifenacin, solifenacin
nicotinic recept ANTAGONISTS
pancuronium, tubocurarine, vecuronium, rocuronium, mivacurium
trimethaphan, mecamylamine
sodium channel inhibitors (antiepileptics)
phenytoin
carbamezepine
lamotrigine
lacosamide
Ca channel inhibitors (antiepileptics)
ethosuxamide, valproic acid (inhib T-type Ca channel)
gabapentin, pregabalin (inhib HVA Ca channel)
GABA channel potentiators (antiepileptics)
Benzos (diazepam, lorazepam, midazolam, clonazepam) [increase amount of Cl influx]
barbiturates (phenobarbital) [increase duration of Cl influx]
vigabatrin (irrev inhibit GABA transaminase)
glutamate recept inhibitors (antiepileptics)
felbamate
rufinamide
other antiepileptic drugs under investigation
tiagabine
topiramate
levetiracetam
zonisamide
drug of choice for focal seizures
carbamazepine
drug of choice for idiopathic generalized seizures (and mixed seizures)
valproic acid
drugs of choice for absence seizures
ethosuxamide > valproic acid > lamotrigine > clonazepam
glucocorticoid receptor AGONISTS
prednisone (preggos), prednisolone, methylprednisolone, dexamethasone (fetal), hydrocortisone (replacement therapy)
fluticasone, beclomethasone, flunisolide, triamcinolone, budesonide [inhaled]
GC recept ANTAGONISTS
mifepristone (for ectopic ACTH synd)
Inhibitors of GC synthesis
mitotane (DDT) aminoglutethimide metyrapone (dx of hypo-pit-adrenal axis) trilostane ketoconazole (inhib P450 enzymes)
Minerocorticoid receptor AGONISTS
fludrocortisone
MC recept ANTAGONISTS
spironolactone
eplerenone
Adrenal sex steroid
Dehydroepiandrosterone (DHEA)
inhibitor of fungal nucleic acid synthesis
flucytosine
inhibitor of fungal MITOSIS
griseofulvin
inhibitors of squalene epoxidase
terbafine, naftinfine (allylamines)
butenafine (benzylamines)
inhibitors of 14-alpha sterol demethylase
Imidazoles:
ketoconazole
butoconazole, clotrimazole, econazole, miconazole, oxiconazole, sertaconazole, sulconazole [topical]
Triazoles:
fluconazole, itraconazole (inhibit P450)
posaconazole, terconazole, voriconazole
inhibitors of fungal membrane stability: polyenes
amophotericin B
nystatin
inhibitors of fungal wall synthesis: echinocandins
caspofungin, micafungin, anidulafungin
tx of acute cryptococcal meningitis in HIV-positive patient
flucytosine + amphotericin B
tx of fungal inf of hair, skin, nails
griseofulvin
drug of choice for tx of candidiasis and cryptococcal meningitis
fluconazole
drug of choice for tx of invasive aspergillosis
voriconazole
only triazole whose absorption NOT affected by gastric acid
fluconazole
drug of choice for vulvovaginal candidiasis
terconazole
prophylaxis tx of invasive fungal infection
posaconazole
tx of mucocutaneous candidiasis
nystatin
tx of esophageal candidiasis
caspofungin, (micafungin, anidulafungin)
inhib of viral attachment/entry (and mechanism)
maraviroc (only blocks CCR5, not CXCR4)
enfuvirtide (T-20) [inhib gp41-med fusion by binding HR1]
inhibitors of viral uncoating
block M2 channel proton
amantidine (also for Parkinson’s)
rimantidine
Antiherpesvirus nucleoside and nucleotide analogues (plus dz/tox if applicable)
phosphorylated by viral kinases:
acyclovir, valacylovir (HSV, VZV)
pencicyclovir, famcicyclovir (HSV, VZV - shingles)
ganciclovir, valganciclovir (CMV) (neutropenia)
phosphorylated by cellular kinase:
cidofovir - must be coadmin w/ probenicid (CMV retinitis in those w/ HIV) (NEPHROtox)
vidarabine, idoxuridine, trifluridine (HSV keratitis)
anti-HIV and -HBV nucleoside/nucleotide analogues/SE
zidovudine (AZT) stavudine (d4T) zalcitabine (ddC) Lamivudine (3TC) - [HBV] emtricitabine (FTC) - 1x daily didanosine (ddl) Abacivir ^^all these ass. w/ neutropenia, anemia
tenofovir (HIV) (hepatotoxicity)
adefovir (HBV) (renal toxicity)
entecavir (HBV) (dose adjust in pts w/ mod renal insuff)
nonnucleoside DNA polymerase inhibitors/SE
foscarnet (renal impairment = dose-limiting)
NNRTIs/SE
efavirenz (1x daily), nevirapine, delavirdine, etravirine [rash!!]
inhib of viral integration - inhib HIV INTEGRASE!
raltegravir
inhib of viral integration - inhib HIV PROTEASE!/SE
saquinavir, ritonavir, amprenavir, fosamprenavir, indinavir, nelfinavir, lopinavir, atazanavir, tipranavir, darunavir
SE = fat distrib and metabolic abnormalities
inhibitors of viral release
inhib neuraminidase!! - Flu A, B
zanamivir
oseltamivir (prophylaxis/tx)
antiviral drugs w/ UNKNOWN mech of action (+ dz)
fomivirsen (2nd line CMV retinitis)
Ribavirin (RSV, HCV w/ IFN-alpha)
docosanol (HSV) - lacks cytotoxicity
antiviral drugs that modulate immune system
IFN-alpha
IFN-beta (tx of MS)
Imiquimod (w/ TLR-7 + 8 to boost innate immunity)
alpha1 receptor functions
Gq
increase vasc SM contraction (vasoconstriction) –> increases systolic/diastolic BP –> reflex bradycardia (DECREASED HR)
increase pupillary dilator muscle contraction (mydriasis - dilation)
increase intestinal and bladder sphincter muscle contraction
alpha2 receptor functions
Gi decrease sympathetic outflow (inhib NE release) decrease insulin release decrease lipolysis increase platelet aggregation
beta1 receptor functions
Gs increase heart rate increase contractility and conductance increase renin release increase lipolysis
beta2 receptor functions
Gs vasodilation (decrease diastolic BP) bronchodilation increase HR increase contractility increase lipolysis increase insulin release decrease uterine tone (tocolysis) ciliary muscle relaxation increase aqueous humor production
M1 receptor functions
Gq
CNS, enteric NS
M2 receptor functions
Gi
decrease HR and contractility of atria at SA node (bradycardia)
M3 receptor functions
Gq
increase exocrine gland secretions (lacrimal, gastric gland, bronchial secretions, etc.)
increase gut peristalsis
increase bladder contraction
bronchoconstriction (increase airflow resistance)
increase pupillary sphincter muscle contraction (miosis)
ciliary muscle contraction (accomodation)
D1 receptor functions
Gs
relaxes renal vasc SM
D2 receptor functions
Gi
modulates transmitter release (esp in brain)
H1 receptor functions
Gq increase nasal and bronchial mucus prod (allergy symptoms) contraction of bronchioles pruritus pain
H2 receptor functions
Gs
increase gastric acid secretion
V1 receptor functions
Gq
increase vasc SM contraction
V2 receptor functions
Gs
increase water permeability and reabsorption in collecting tubules of kidney
CCB used on vasc SM
amlodipine, nifedipine
first line therapy for HTN in preg
hydralazine w/ methyldopa
can cause cyanide toxicity (releases cyanide)
nitroprusside
drugs of choice in pts w/ CAD and CHF w/ HTN
cardioselective beta blockers
A BEAM of beta-1 blockers
DOC in pts w/ isolated systolic HTN
CCB + thiazide diuretics (in non-diabetics)
ACE inhib or ARB (diabetics)
CCB used on heart
verapamil
partial beta agonists contraindicated in angina
pindolol, acebutolol
decrease GI absorption of statins
bile acid resins (cholestyramine, colestipol, colesevelam)
class IA antiarrhythmics
quinidine, procainamide, disopyramide
increases AP duration, ERP, QT interval
“the Queen Proclaims Diso’s Pyramid”
class IB antiarrhythmics
lidocaine, mexiletine, tocainide; (phenytoin can also fall into this class)
decreases AP duration
BEST POST-MI!! + in digitalis-induced arrhythmias
class IC antiarrhythmics
flecainide, propaferone
no change in AP duration
last-ditch drug
class II antiarrhythmics
metoprolol, propanolol, esmolol, atenolol, timolol
class III antiarrhythmics
amiodarone, ibutilde, dofetilide, sotalol
“AIDS”
class IV antiarrhythmics
verapamil, diltiazem
“other” antiarrhythmics
adenosine, Mg
does not presdisp to Torsades de Pointes even though prolongs QT interval
amiodarone (half life > 80 days)
DOC in dx/abolishing paroxysmal SVT
adenosine
effects blocked by theophylline and caffeine
adenosine
DM tx: no risk of hypoglycemia
metformin, pioglitazone, rosiglitazone, acarbose, miglitol, voglibose
sulfa drugs
probenecid furosemide acetazolamide celecoxib thiazides sulfonamide AB sulfasalazine sulfonylureas
“Sulfa Pills Frequently Cause Terrible Acute Symptoms”
pts w/ sulfa allergies –> fever, UTI, pruritic rash, Stevens-Johnson synd, hemolytic anemia, thrombocytopenia, agranulocytosis, urticaria (hives)
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
dantrolene
DOC for Pneumocystis jirovecii, Toxoplasma gondii, Nocardia, Stenotrophomonas meltophilia
TMP-SMX
Vd =
amount of drug in body/plasma drug concentration
half life =
0.7 x Vd / CL
loading dose =
Css x Vd/F (F=1 for IV dose)
maintenance dose =
Css x CL/F
reduces pain by decreasing levels of substance P in PNS
capsaicin
DOC for type II DM
metformin
P450 inducers
Momma Bear Steals Phen-phen and Refuses Greasy Carbs Chronically
modafinil barbiturates St.John's wort phenytoin rifampin griseofulvin carbamezapine chronic alcohol use
P450 inhibitors
MAGIC RACKS in GQ
macrolides amiodarone grapefruit juice isoniazid cimetidine ritonavir acute alcohol abuse ciprofloxacin ketoconazole sulfonamides gemfibrozil quinidine
AB to avoid in preg
Sulfonamides - Kernicterus Aminoglycosides - otoxicity Fluoroquinolones - cartilage damage Clarithromycin - embryotoxic Tetracyclines - discolored teeth, inhibition of bone growth Ribavirin (antiviral) - teratogenic Griseofulvin (antifungal) - teratogenic Chloramphenicol - "gray baby"
“SAFe Children Take Really Good Care”
DOC for DVT and pulmonary thromboembolism
warfarin
DOC for Legionella
erythromycin
DOC for Treponema
penicillin
DOC for Mycoplasma
erythromycin or tetracyclines
drug infused at constant rate achieves steady state in?
4-5 half-lives
DOC for hairy cell leukemia
cladribine (adenosine analog that is resistant to adenosine deaminase)
best agent to increase HDL levels?
niacin
best tx for high LDL
statins + ezetimibe
best agent for hypertriglyceridemia
fibrates
SE = increases TG levels
cholestyramine, colestipol, colesevelam
bile acid resins
MOA of cromolyn
prevents mast cell degranulation
cromolyn used for?
PROPHYLAXIS of asthma, allergies, aspirin HST
anti-TB drug most effective in acidic environments + most useful against INTRAcellular organisms
pyrazinamide
pyrazinamide most effective against?
M.tuberculosis engulfed by macrophages
what is needed to convert INH to active metabolite?
KatG (bacterial catalase-peroxidase)
solo prophylaxis against TB?
INH
meningococcal prophylaxis and chemoprophylaxis in contacts of children w/ H.influenzae type B?
rifampin
toxicity = blurry yellow vision (think Van Gogh)
digoxin
thiazide diuretics cause what SE?
- hypokalemic metab alkalosis (bc increased aldost secretion)
- hyponatremia, hypomagenesemia
- sulfa allergy
hypergGlycemia hyperLipidemia hypercCalcemia hyperUricemia ("Hyper Girls Like Crushing Uppers")
mannitol (osmotic diuretic) can cause what SE?
hypernatremia, pulmonary edema
mannitol is CI in pts w/ what?
anuria, CHF
carbidopa decreases what SE of L-dopa?
nausea, vomiting
carbidopa increases what SE of L-dopa?
anxiety, agitation, insomnia, confusion, delusions, hallucinations
leucovorin is a?
tetrahydrofolate derivative that does NOT req activation by dihydrofolate before it can function as cofactor for thymidylate synthase
N5-formyl-tetrahydrofolate
drug whose chemo effects overcome by leucovorin
methotrexate
drug whose chemo effects potentiated by leucovorin
5-FU
bortezomib MOA and indications?
proteasome inhibitor
tx for multiple myeloma and Waldenstrom’s macroglobulinemia
tx for mod-severe allergic asthma?
omalizumab (anti-IgE Ab)
this drug has increased toxicity w/ allopurinol
azathioprine (6-MP, 6-TG)
bc both metab by xanthine oxidase
antimetabolite not S-phase specific
gemcitabine (pyramidine analog)
methotrexate inhibits
dihydrofolate reductase
5-FU complexes w/ ________ that inhibits _______?
w/ folic acid (THF)
inhibits thymidylate synthase
5-FU overdose rescue =
thymidine
malignant hyperthermia a SE of what drugs?
inhalation anesthetics (except N2O) succinylcholine
chronotropic effects
increase RATE of contraction (HR)
inotropic effects
increase FORCE of contraction
inhibits dihydropteroate SYNTHASE
sulfonamides
inhibits dihydrofolate REDUCTASE
trimethoprim, pyrimethamine, methotrexate
tx for mild UTI that is safe in pregnancy?
nitrofurantoin (p.267 DIT)
most common medication used for UTI prophylaxis
TMP-SMX
cisplatin toxicity/prophylactic tx used to reduce toxicity?
nephrotoxicity;
amifostine or chloride diuresis (bc cisplatin stays in nonreactive state when in higher chloride concentration)
1st line therapy in trigeminal neuralgia?
carbamazepine
1st line tx for acute gouty arthritis?
NSAIDs
also Glucocorticoids in pts for whom NSAIDs are CI (ex. elderly pts w/ renal failure)
uricosuric drugs + xanthine oxidae inhibitors (allopurinol) used for?
PROPHYLACTIC therapy for prevention of acute gouty attacks (used in pts w/ more than 3 episodes of acute gouty arthritis and those w/ macroscopic tophi)
why can’t allopurinol be used in acute gouty attacks?
can exacerbate acute arthritis!
antiarrhyhtmics that can cause Torsades de Pointes
quinidine procainamide disopyramide ibutilide dofetilide sotalol
drugs that prolong PR interval
verapamil
metoprolol
drugs that act on microtubules
vincristine/vinblastine griseofulvin mebendazole/albendazole/thiabendazole paclitaxel/docetaxel colchicine
DOC in cluster HA
inhaled 100% oxygen
competitive inhib do what to potency/efficacy?
DECREASE potency (increase Km)
noncompetitive inhib do what to potency/efficacy?
DECREASE efficacy (decrease Vmax)
the lower the Km
the higher the potency
the higher the Vmax
the higher the efficacy
high efficacy drugs classes?
analgesic
antibiotics
antihistamines
decongestants
highly potent drug classes?
chemotherapeutic
antiHTN
antilipid
drug w/ low therapeutic index
digoxin
lithium
theophylline
warfarin
phase I drug metabolism?
reduction
oxidation
hydrolysis
can result in still active metabolite (can be more toxic)
uses CYP450!!
phase II drug metabolism?
conjugation: glucuronidation, acetylation, sulfation)
renally excreted
tx of OD of beta-blockers in arrhythmias
glucagon
1st gen cephalosporins
cefazolin
cephalexin
“PEcK”
2nd gen cephalosporins
cefoxitin
cefaclor
cefprozil
cefuroxime
“HENS PEcK”
3rd gen cephalosporins
ceftriaxone
cefotaxime
cefdinir
ceftazidime
4th gen cephalosporins
cefapime
ceftriaxone treats what?
meningitis and gonorrhea
excreted in bile and long acting
ceftazidime treats what?
Pseudomonas
3rd gen cephalosporins cover what?
serious gram neg bacteria
also S.pneumo!!
cefepime treats what?
Pseudomonas and gram +
aztreonam binds to?
PBP3
drug that inhibits ribonucleotide reductase
hydroxyurea
drug that inhibits dihydrofolate reductase
trimethoprim
methotrexate
drug that inhibits thymidylate synthase
5-FU
drug that inhibits IMP dehydrogenase
mycophenolate
drug that inhibits PRPP amidotransferase
6-MP
drug aiding in dx of Prinzmetal’s variant angina
ergonovine
low potency typical antipsychs
chlorpromazine
thioridazine
high potency typical antipsychs
trifluperazine
fluphenazine
haloperidol
drugs used to tx Tourette’s synd
fluphenazine, pimozide (high potency antipsychs)
tetrabenazine (help degrade dopamine)
typical antipsychs block what receptor?
D2 receptors (which increases cAMP)
clozapine acts on what receptors?
D4
DOC for tx of psychosis induced by Parkinson meds
quietapine
specific sympt of chlorpromazine
corneal deposits
specific sympt of thioridazine
retinal deposits
lithium MOA?
inhib IP3 (phosphoinositol cascade)
buspirone facts?
stim 5-HT1A receptors
no addiction, tolerance or sedation!
no interaction w/ alcohol
takes 1-2 wks to take effect
SSRIs
fluoxetine
paroxetine
sertraline
citalopram
SNRIs
venlafaxine
duloxetine (greater effect on NE)
SNRI MOA
inhib serotonin and NE reuptake
tx for fibromyalgia?
milnacipran or amitriptyline
can tx diabetic periph neuropathy
duloxetine
indication for imipramine
bedwetting
indication for clomipramine
OCD
which TCA has most anticholinergic SE?
3rd gen (amitriptyline)
use nortryptilline in elderly to decrease confusion, hallucination SE
which TCA is less sedating; but increases ________?
desipramine
increases seizure threshold
TCA MOA
block reuptake of NE and serotonin
TCAs
amitriptyine, nortriptyline
imipramine, desipramine, clomipramine
doxepin
amoxapine
MAOIs
tranylcypromine
phenelzine
isocarboxazid
selegiline
selegiline inhibits what selectively?
MAO-B - used for dopamine (Parkinson’s)
MAOI MOA/use
increased levels of NE, serotonin and dopamine by inhibiting MAO
can be used to tx atypical depression
ingestion of tyramine w/ MAOIs causes?
Hypertensive crisis
bupropion MOA + benefit
inhib NE and dopamine reuptake w/ greater effect on dopamine
no sexual SE!
mirtazapine MOA
alpha2-antag (increases release of NE and serotonin)
also potent 5-HT2 and 5-HT3 recept antag
trazodone MOA/use/SE
inhibit serotonin reuptake
used primarily for insomnia
SE = priapism
demeclocycline is used in
SIADH bc ADH antagonist
Na-channel binding strength for Class I antiarrhythmics
IC > IA > IB
IC = increased incidence of use dependence
class II antiarrhythmics MOA
decrease cAMP, Ca
decreases slope of phase 4 (slows HR)
increases PR interval
metoprolol can cause what SE
dyslipidemia
class II antiarrhythmics OD tx
glucagon
beta-blocker that can exacerbate prinzmetal’s angina
propanolol
used in tx of WPW
procainamide
amiodarone
class III antiarrhythmics MOA
increases AP, ERP, QT interval
works on phase 3!!
class I antiarrhythmics MOA (as a class!)
decreases slope of phase 0
class IV antiarrhythmics MOA
decrease depolarization of latter part of phase IV
decreases depolarization of phase 0 –> increases ERP
decreases SA/AV nodal activity
increases PR
class IV antiarrhythmics CI in
pts w/ HF exacerbation
adenosine MOA
increases K+ out of cells –> hyperpolarization
decreases Ca
prolong PR interval
adenosine effects blocked by
theophylline (pts w/ COPD/asthma)
caffeine
drug CI in closed-angle glaucoma
epinephrine
baclofen MOA
GABAb agonist
H1 blockers - 1st gen
can cross BBB - sedation!
diphenydramine, dimenhydrinate, chlorpheniramine
H1 blockers - 2nd gen
can’t cross BBB
loratadine, fexofenadine, desloratadine, cetirizine
beta-2 agonists for prophylaxis of asthma
salmeterol
formoterol
theophylline characteristics
inhib PDE –> decreases cAMP hydrolysis –> brochodil
narrow therapeutic index: cardiotox, neurotox (seizures)
blocks action of adenosine
tx OD w/ beta-blockers
inhaled GC effects/use
inhib synth of cytokines (by inhib phospholipase A2)
inactivate NF-KB –> decreased TNF-alpha prod (bc it’s the TF that activates this cytokine)
1st line for CHRONIC asthma
montelukast, zafirlukast MOA/use
block leukotriene recept (D4 recept antagonists)
aspirin-induced asthma!!
also chronic asthma prophylaxis
zileuton MOA/use
5-LOX inhib (no leukotriene synth)
chronic asthma prophylaxis
omalizumab MOA/use
Monoclonal anti-IgE Ab
used in allergic asthma resistant to other tx
N-acetylcysteine in asthma/CF use:
mucolytic by cleaving disulfide bonds in mucus glycoproteins
also prevents contrast-induced nephropathy
how does dextromethorphan cause cough suppression
antag NMDA glutamate receptors
bosentan MOA/use
for pulmonary arterial HTN
competitively antag endothelin-1-receptors
pseudoephedrine, phenylephrine resp uses
constrict dilated arterioles in nasal mucosa (via alpha-agonist properties) –> reduce nasal congestion
open obstructed Eustachian tubes
pseudoephedrine –> also a stimulant
pseudoephedrine, phenylephrine resp SE
HTN, rebound nasal congestion if taken long term (all)
CNS stim/anxiety (pseudoephedrine)
tachyphylaxis - due to decreased NE from neg feedback causing vasodil + congestion (phenylephrine)
acetazolamide used in glaucoma by
blocking bicarb formation –> decreases formation of aqueous humor
acetazolamide SE
hyperchloremic metab acidosis, sulfa allergy, paresthesias
loop diuretics SE
Ototox Hypokalemia/hypocalcemia Dehydration Allergy (sulfa) Nephritis (acute) Gout
“OH DANG!”
2 classes of diuretics causing ACIDEMIA
- acetazolamide
- K+-sparing (hyperkalemia causing –> H/K exchange in plasma)
2 classes of diuretics causing ALKALEMIA
loop and thiazides
- vol contraction (bicarb reabsorb –> Cl- secreted)
- K+ loss
- low K+ states (H exchanged for Na, instead of K exchanged)
increased aldosterone can have what effect on heart
cardiac remodeling –> can worsen LV dysfunct in HF pts
ACE inhib 2 unique clinical applications
diabetic renal disease
used Post-MI + in CHF pts (to prevent unfav heart remodeling as a result of chronic HTN)
ACE inhib SE
"CATCHH" Cough (dry!!) Angioedema Teratogen Creatinine increase (bc of decreased GFR --> decreased FF) Hyperkalemia Hypotension
methotrexate indications/SE
cancers ectopic preg hydatidiform mole RA psoriasis
SE: myelosuppression (reversed w/ leucovorin), macrovesicular fatty change in liver, mucositis, teratogen
cyclophosphamide MOA/SE
covalently X-link DNA @ guanine N-7
bioactivated by liver
SE - hemorrhagic cystitis prevented w/ mesna (thiol groups bind acrolein)
used against brain tumors
nitrosureas (carmustine, other -mustines, streptozocin)
cross BBB –> CNS!!! (therefore, CNS toxicity also)
busulfan
used in CML
used to ablate pt bone marrow before BMT
SE = pulm fibrosis, hyperpigmentation!
vinca alkaloids bind?
beta-tubulin in M phase + block polymerization of microtubules
vincristine SE
neurotox (periph neuritis)
vinblastine SE
bone marrow suppression
“vinblastine BLASTS bone”
paclitaxel MOA/indications
MOA - HYPERSTABILIZE polymerized microtubules –> can’t break down spindles
**ANAPHASE can’t occur
used for: ovarian/breast carcinomas
cisplatin SE
nephrotox (acute tubular injury; prevent w/ amifostine)
acoustic nerve damage
Chloride diuresis
etoposide, teniposide MOA
inhib topo II
hydroxyurea MOA/use
inhib ribonucleotide reductase
used in melanoma, sickle cell
irinotecan, topotecan MOA
inhib topo I
trastuzumab aka …
herceptin
Mab against HER2 (c-erbB2)
SE = cardiotox
bevacizumab
Mab against VEGF –> inhib angiogenesis
vemurafenib
inhib B-raf kinase w/ V600E mut
for metastatic melanoma
cimetidine SE
inhib CYP450
antiandrogenic effects
crosses BBB (confusion, dizziness, HA)
decreases renal excretion of creatinine (also seen w/ ranitidine)
sucralfate req?
acidic environment to polymerize
misoprostol indications
NSAID-induced PUD maintains PDA induces labor (ripens cervix)
octreotide (somatostatin analog) indications
acute variceal bleeds
acromegaly
VIPoma
carcinoid tumors
hypercalcemia can stim what?
G-cells to produce gastrin
terbutaline
Beta2-agonist used to reduce premature uterine contractions
tx HTN in pt w/ renal dz?
clonidine
methyldopa
these are alpha2-agonists
give to pts on MAOIs who eat tyramine containing food
phentolamine
vascular alpha receptors are mostly what type
1B
tamsulosin blocks
alpha-1A, 1D receptors on prostate + does not reduce blood pressure as much
beta agonists do what to BP?
DECREASE (bc of beta2 effect)
drug class used cautiously in diabetics
beta-blockers (can mask hypoglycemia); use beta1-blockers instead!
beta-blockers effects:
1) decrease O2 consumpt (by decreasing HR, contractility)
2) reduce mortality in MI
3) decrease AV conduction (metoprolol, esmolol)
4) decrease CO
5) decrease renin secretion
6) slow progression of HF in CHF (but make sure not to decrease HR too much!!)
7) decrease aqueous humor secretion (timolol)
tx for pts w/ HTN and bradycardia
partial beta blockers!
pindolol, acebutolol
non-selective beta blockers w/ alpha1-blocking ability too:
labetalol
carvedilol
hydroxychloroquine
tx for SLE
SE = permanent retinal damage, myopathies
direct cholinergic agonists
bethanechol
carbachol
pilocarpine
methacholine
AChE inhibitors
neostigmine physostigmine pyridostigmine donepezil edrophonium echothiophate diisopropyl flurophosphate
stim alpha1, 2 + beta1, 2
epinephrine
stim alpha1, 2 + SOME beta1
epinephrine
beta agonist (beta1 = beta2)
isoproterenol
beta1-agonist
dobutamine
alpha-agonist (alpha1 > alpha2)
phenylephrine
beta2-agonist for premature contractions
ritodrine
ephedrine MOA
releases stored catechol
-used for nasal decongest, urinary incontinence
alpha2-agonists
clonidine
methyldopa
alpha-blockers
phenoxybenzamine
phentolamine
alpha2-blocker
mirtazapine
tx of opioid withdrawal
methadone, buprenorphine
suboxone (a combo of naloxone + buprenorphine; harder to abuse)
neonatal opioid withdrawal - diluted tincture of opium solution
tx cocaine OD
benzos
haloperidol
NEVER BETA BLOCKERS!!
tx nicotine withdrawal (meds)
bupropion
varenicline
tx for PCP, LSD
benzos
tx for heroin addiction
methadone (long-acting oral opiate)
naloxone + buprenorphine = partial agonist; oral naloxone not easily abused
tx for delirium tremens w/ alcohol withdrawal
long-acting benzos preferred (unless pt has liver disease –> use short-acting benzos)
tx for anxiety
SSRI, SNRI, buspirone
tx for ADHD
methylphenidate, amphetamines
tx for bipolar disorder
Lithium
valproic acid, carbamazepine
atypical antipsych
tx for bulimia
SSRIs (fluoxetine esp)
tx for depression
SSRI, SNRI, TCA, buspirone
mirtazapine (esp w/ insomnia)
tx for OCD
SSRI, clomipramine
tx for panic disorder
SSRI, venlafaxine, benzos
tx for PTSD
SSRI
tx for schizophrenia
antipsych
tx for social phobias
SSRIs
tx for Tourette’s synd
antipsych
tx for drug-induced Parkinsonism
benztropine
trihexyphenidyl
ziprasidone SE
prolong QT interval
lithium excretion
exclusively by kidney; most reabsorbed @ PCT following Na reabsorption
cyclosporine SE
nephrotox (by vasoconstriction of aff + eff arterioles), HTN, hyperlipidemia, hyperglycemia
drug used in lupus nephritis
azathioprine
alemtuzumab
anti-CD52 humanized Mab for tx of CLL
beta2 > beta1 agonist
terbutaline
probenecid actions
inhib reabsorpt of uric acid @ PCT
inhib secretion of penicillin
TZD w/ increased risk of bladder cancer
pioglitazone
adiponectin does what?
is released by activation of PPAR-gamma (site of action of TZDs)
decreases insulin resistance
TZDs metabolized where?
liver
sitagliptan use req monitoring of what drug?
digoxin
drugs w/ anticholinergic properties
-ANTIHISTAMINES (H1 BLOCKERS)
chlorpheniramine, cyproheptadine, diphenhydramine, hydroxyzine
-ANTIDEPRESSANTS
amoxapine, amitriptyline, clomipramine, desipramine,
doxepin, nortriptyline, paroxetine, imipramine, protriptyline
-CARDIOVASCULAR MEDICATIONS
furosemide, digoxin, nifedipine, disopyramide
-Antidiarrheal Medications
diphenoxylate, atropine
-Antispasmodic Medications
belladonna, clidinium, chlordiazepoxide, dicyclomine, hyoscyamine, propantheline
-Antiulcer Medications
cimetidine, ranitidine
-ANTIPARKINSON MEDICATIONS
amantadine, benztropine, biperiden, trihexyphenidyl
-MUSCLE RELAXANTS
cyclobenzaprine, dantrolene, orphenadrine
-ANTIVERTIGO MEDICATIONS
meclizine, scopolamine
-ANTIPSYCHOTIC MEDICATIONS
chlorpromazine, clozapine, olanzapine, thioridazine
-URINARY INCONTINENCE
oxybutynin, probantheline, solifenacin, tolterodine, trospium
-PHENOTHIAZINE ANTIEMETICS
prochlorperazine, promethazine
DOC for myoclonic seizures
vaproic acid
DOC for simple/complex partial seizures
carbamazepine