First Aid Pharmacology Flashcards
K_m reflects ___
substrate affinity for enzyme (inversely)
V_max is a function of ___
enzyme concentration
low ___ means high enzyme affinity
K_m
inhibitors are studied with graph of ___ vs. ___
this is aka ___ plot (2)
1/V
1/[S]
double reciprocal
Lineweaver-Burk
x intercept of double reciprocal plot is ___
NAME?
y intercept of double reciprocal plot is ___
1/V_max
K_m is the ___ at which V is ___
substrate concentration
V_max/2
competitive/noncompetitive inhibitors do not change V_max
competitive
competitive/noncompetitive inhibitors do not change K_m
noncompetitive
efficacy change means ___ of dose response curve
vertical shift
potency change means ___ of dose response curve
horizontal shift
competitive inhibitors change ___
potency
non-competitive inhibitors change ___
efficacy
V_d in terms of plasma drug concentration
V_d = (amount of drug in body)/(plasma concentration)
drugs with low V_d distribute in ___
drugs with medium V_d distribute in ___
drugs with high V_d distribute in ___
blood
ECF or TBW
tissues
low V_d means ___ L
4–8
clearance (CL) in terms of plasma drug concentration (C_p)
CL = (rate of drug elimination)/(C_p)
CL in terms of V_d
CL = V_d x K_e
t_1/2 in terms of V_d
t_1/2 = (0.7 x V_d)/CL
loading dose in terms of V_d
LD = (C_p x V_d)/F
where F is bioavailability
maintenance dose in terms of C_p
MD = (C_p x CL)/F
zero order kinetics means
constant elimination per unit time
3 drugs with zero order kinetics
phenytoin
ethanol
aspirin
first order kinetics means
constant fraction of drug eliminated per unit time
4 weak acid drugs
treat overdose of weak acid with ___
phenobarbital MTX TCAs aspirin bicarbonate
weak base drug___
treat weak base overdose with ___
amphetamine
ammonium chloride
phase I metabolism is done by ___
its products are active/inactive
3 phase I reactions
CYP450 active reduction oxidation hydrolysis
phase II metabolism products are active/inactive,
polar/nonpolar
3 phase II reactions
inactive very polar glucuronidation acetylation sulfation
geriatric patients lose phase ___ metabolism first
I
a partial agonist has higher/lower potency and
higher/lower efficacy
than full agonist.
higher OR lower OR same
lower
therapeutic index
TI = LD_50/ED_50
where LD_50 is median toxic dose,
ED_50 is median effective dose
the first synapse in a parasympathetic pathway is ___
nicotinic
the second synapse in a parasympathetic pathway is ___
muscarinic
the first synapse in a sympathetic pathway is ___
nicotinic
the second synapse in most sympathetic pathways is ___
2 exceptions are ___
noradrenergic
sweat gland
renal vascular smooth muscle
2nd synapse in sweat gland pathway is ___
muscarinic
2nd synapse in renal vascular smooth muscle pathway is ___
D1 dopaminergic
nicotinic receptor is ___tropic
muscarinic receptor is ___tropic
iono
metabo
nicotinic receptor is a ___-gated ___ channel
ligand
Na+/K+
alpha1 adrenergic effect on eye
dilator muscle contraction
alpha_1 adrenergic receptor type
G_qPLR
alpha_1 adrenergic affect on GIT
increased sphincter contraction
alpha_2 adrenergic receptor type
alpha 2 effect on metabolism
G_iPLR
decreased insulin release
beta_1 adrenergic receptor type
G_sPLR
beta_1 adrenergic affect on kidney
increased renin release
beta_1 adrenergic affect on metabolism
increased lipolysis
beta_2 adrenergic affect on vessels
vasodilation
both beta_1 and beta_2 affect the heart but ___ is stronger
only ___ affects the lungs, causing ___
beta_1
beta_2
bronchodilation
beta_2 adrenergic affect on metabolism (3)
increased lipolysis
increased glycogenolysis
increased insulin release
beta_2 adrenergic affect on eye
increased aqueous humor production
M1 muscarinic receptor is ___
M2 muscarinic receptor is ___
M3 muscarinic receptor is ___
G_qPLR
G_iPLR
G_qPLR
M2Rs are expressed by ___ and do ___
cardiomyocytes
negative inotropism and chronotropism
M3Rs do ___ to exocrine glands
increase secretion
M3Rs do ___ to GIT smooth muscle
increase peristalsis
M3Rs do ___ to lungs
bronchoconstriction
M3Rs do ___ (2) to eye
pupillary sphincter contraction (miosis)
ciliary muscle contraction (accomodation)
M3Rs do ___ to bladder
detrusor contraction
D1Rs are ___
they do ___
G_sPLR
renal vascular smooth muscle relaxation
D2Rs are ___
they do ___
G_iPLR
neurotransmitter modulation
histamine H1Rs are ___
G_qPLR
H1Rs do ___ (4)
RT mucus secretion
bronchoconstriction
itching
pain
histamine H2Rs are ___
they do ___
G_sPLR
gastric acid secretion
ADH V1Rs are ___
they do ___
G_qPLR
vasoconstriction
ADH V2Rs are ___
they do ___
G_sPLR
H2O reabsorption in collecting duct
Y is converted to ___ by ___.
this is blocked by ___, which works as a ___
DOPA
Y hydroxylase
metyrosine
antihypertensive
DOPA is converted to ___ by ___.
cofactor is ___
DA
DOPA decarboxylase (AAADC)
B6
DA is imported to vesicles by ___.
this is blocked by ___
VMAT (vesicular monoamine transporter)
reserpine
DA is converted to ___ by ___.
cofactor is ___
NE
DBH (DA beta hydroxylase)
vitamin C
In ___, NE is converted to ___ by ___, in the ___.
___ is required
adrenal medulla E PNMT (phenylethanolamine N-methyl transferase) cytoplasm SAM
After MAO-COMT in either order, DA becomes ___
HVA (homovanillic acid)
After MAO-COMT in either order, E becomes ___ and NE becomes ___
both become MHPG (methoxyhydroxyphenylglycol)
After COMT, E becomes ___ and NE becomes ___.
metanephrine
normetanephrine
adrenal pheochromocytomas make more ___ than ___, but other ones do the opposite
E
NE
catecholamine exocytosis is potentiated by ___ (2) and inhibited by ___
amphetamine
ephedrine
guanethidine
___ (3) blocks catecholamine reuptake
cocaine
amphetamine
TCAs
2 presynaptic receptors which inhibit catecholamine release
alpha_2
M2
1 presynaptic receptor which facilitates catecholamine release
AII (angiotensin)
rate limiting step of cholinergic neurotransmission is ___
this is inhibited by ___
Ch uptake
hemicholinium
ACh is synthesized by ___ from ___ and ___
choline acetyltransferase (ChAT)
choline
Ac CoA
uptake of ACh into vesicule is inhibited by ___
vesicular exocytosis is inhibited by ___
vesamicol
botulinum
direct cholinomimetic for GI motility
bethanechol
2 indications for bethanechol
ileus (post op, neurogenic)
urinary retention
b/c it activates bladder and bowel
2 direct cholinomimetics for glaucoma
pilocarpine
carbachol
pilocarpine causes contraction of ___ (2)
and secretion of ___ (3)
pupillary sphincter ciliary body saliva sweat tears
contraction of ___ helps open angle glaucoma
contraction of ___ helps closed angle glaucoma
ciliary body
sphincter pupillae
direct cholinomimetic for testing asthma
methacholine
indirect cholinomimetics are ___s
AChEI
indirect cholinomimetic for GI motility
neostigmine
neostigmine has high/low CNS penetration
low
4 neostigmine indications
ileus (post op, neurogenic)
urinary retention
MG
post op NMJ block reversal
cholinomimetic for MG dx
edrophonium
cholinomimetic for MG tx
pyridostigmine
2 indirect cholinomimetics for glaucoma
echothiophate
physiostigmine
pyridostigmine has high/low CNS penetration
physiostigmine has high/low CNS penetration
echothiophate has high/low CNS penetration
low
high
low
cholinergic intoxication causes CNS ___
and skeletal muscle ___
excitation
excitation
2 antidotes for cholinergic intoxication
atropine
pralidoxime
pralidoxime functions in cholinergic intoxication by ___
regenerating active ChE
antimuscarinic for eye
atropine
homatropine
tropicamide
atropine causes ___ (2)
mydriasis
cycloplegia
cycloplegia means ___
inability to accomodate
antimuscarinic for Parkinson’s disease
benztropine
antimuscarinic for motion sickness
scopolamine
2 antimuscarinic for asthma and COPD
ipratropium
tiotropium
2 antimuscarinics for bladder spasticity
oxybutynin
darifenacin
solifenacin
glycopyrrolate used for ___ (3)
reduce airway secretions
drooling
peptic ulcers
atropine effects
eye: pupil dilation, cycloplegia
respiratory: decreased secretions from airway
stomach: decreased acid secretion
gut: decreased motility
bladder: decreased urgency in cystitis
atropine toxicity
hot dry red blind (cycloplegia) mad (disoriented)
may cause acute angle-closure glaucoma, urinary retention (in BPH men or hyperthermic infants)
at low doses E agonizes ___
at higher doses it agonizes ___
beta_1
all adrenergic receptors
E is indicated for ___ (4)
anaphylaxis
open angle glaucoma
asthma
hypoTN
NE agonizes ___
alpha_1 > alpha_2 > beta_1
NE is indicated for ___
hypoTN (*decreases renal perfusion)
isoproterenol agonizes ___
beta_1 = beta_2
isoproterenol is indicated for ___
evaluation of tachyarrhythmias
DA agonizes ___
D1 = D2 > beta adrenergic > alpha adrenergic
DA is indicated for ___ (3)
shock
heart failure
unstable bradycardia
DA’s effects on the heart
+ inotrope
+ chronotrope
at high doses
dobutamine agonizes ___
beta_1 > beta_2 > alpha
dobutamine is indicated for ___ (3)
heart failure
cardiac stress testing
dobutamine’s effects on the heart
inotropic > chronotropic
phenylephrine agonizes ___
alpha_1 > alpha_2
phenylephrine is indicated for ___ (3)
pupil dilation
nasal decongestion
hypotension
5 beta_2-selective agonists
metaproterenol albuterol salmetrol terbutaline ritodrine
2 beta_2 agonists for acute asthma
metaproterenol
albuterol
beta_2 agonist for chronic asthma tx
salmetrol
2 tocolytic beta_2 agonist
terbutaline
ritodrine
3 indirect sympathomimetics
of these ___ (2) are secretagogues
amphetamine
ephedrine
cocaine
amphetamine
ephedrine
3 amphetamine indications
narcolepsy
obesity
ADD
3 ephedrine indications
nasal decongestion
urinary incontinence
hypoTN
what drug should you avoid prescribing in patients with cocaine intoxication?
beta blockers because of the unopposed alpha 1 activation leading to extreme hypertension
2 alpha_2 agonists
clonidine
alpha-methyldope
applications of clonidine
Hypertensive urgency, ADHD, severe pain, ethanol and opioid withdrawal
Toxicity of clonidine
CNS depression, bradycardia, hypotension, respiratory depression, small pupil size
applications of alpha-methyl dopa
hypertension in pregnancy
Toxicity of alpha-methyl dopa
direct Coombs+ hemolytic anemia, SLE like syndrome
2 non-selective alpha blockers
___ is reversible blocker
phenoxybenzamine
phentolamine
phentolamine
Phenoxybenzamine and phentolamine are (reversible/irreversible)?
phenoxybenzamine: irreversible; phentolamine: reversible
applications of phenoxybenzamine
pheo to prevent hypertensive crisis from too much catecholamines
toxicity of phenoxybenzamine
orthostatic hypotension, reflex tachycardia
applications of phenotolamine?
pts on MAO inhibitors that ate too much tyrosine
applications of a1 selective blockers
urinary Sxs of BPH, PTSD (prazosin), HTN (except tamsulosin)
Toxicity of a1 selective blockers
1st dose orthostatic hypoHTN
dizziness
H/A
alpha_1 selective blockers end in ___
zosin
alpha_2 selective blocker
mirtazapine
mirtazapine is indicated for ___
depression
3 mirtazapine SEs
sedation
increased cholesterol
increased appetite
what are the appliations of beta blockers?
angina pectoris, MI, SVT, HTN, CHF, Glaucoma
how do beta blockers effect angina pectoris?
decreases heart rate and contractility, resulting in decreased O2 consumption
which beta blockers decrease mortality in Mis?
metoprolol, carvedilol, bisoprolol
which beta blockers are used in SVT
metoprolol, esmolol
how do beta blockers effect SVT?
they decrease AV conduction velocity
how do beta blockers effect HTN?
decrease CO, decrease renin secretion by B1 block in JGA cells
How do beta blockers effect CHF?
slows progression
Which beta blocker effects glaucoma and how?
timolol by decreasing secretion of aqueous humor
what are the toxic effects of beta blockers?
impotence; CV adverse effects: bradycardia, AV block, CHF; CNS effects: seizures, sedation, sleep alterations; dyslipidemia (metoprolol), asthma or COPD exacerbation
acebutolol is ___-selective beta blocker
beta_1 (partial agonist)
atenolol is ___-selective beta blocker
beta_1
betaxolol is ___-selective beta blocker
beta_1
esmolol is ___-selective beta blocker
beta_1
labetalol is ___-selective beta blocker
non, also nonselective alpha
metoprolol is ___-selective beta blocker
beta_1
nadolol is ___-selective beta blocker
non
pindolol is ___-selective beta blocker
non (partial agonist)
propranolol is ___-selective beta blocker
non
timolol is ___-selective beta blocker
non
2 non-selectve alpha + beta blockers
carvedilol
labetalol
2 partial beta agonists
pindolol
acebutolol
what is nebivolol?
cardiac selective B1 adrenergic blockade with stimulation of beta 3 receptors leading to activation of NOS in vasculature
tx for acetaminophen poisoning
N-acetyl cysteine
tx for salicylate poisoning (2)
bicarbonate
dialysis
purpose of bicarbonate in salicylate poisoning
alkalinize urine
tx for amphetamine poisoning
ammonium chloride
purpose of ammonium chloride in amphetamine poisoning
acidify urine
tx for anticholinesterase poisoning (2)
atropine
pralidoxime
tx for antimuscarinic toxicity
physiostigmine salicylate and control HTN
tx for beta blocker toxicity
glucagon
tx for digitalis toxicity (5)
anti-dig Fab
tx for Fe toxicity
desferoxamine, deferasirox
tx for Pb toxicity (4)
CaEDTA
dimercaprol
succimer
penicillamine
tx for Hg/As/Au toxicity
dimercaprol (BAL), succimer
tx for Cu/As/Au toxicity
penicillamine
tx for CN- toxicity (3)
nitrite
hydroxocobalamin
thiosulfate
tx for methemoglobinemia (2)
methylene blue
vitamin C
tx for CO toxicity (2)
100% O2
hyperbaric O2
tx for MeOH/ethylene glycol toxicity (3)
fomepizole> ethanol
dialysis
tx for opioid toxicity
naloxone
tx for benzo toxicity
flumazenil
tx for TCA toxcity
bicarbonate
purpose of bicarbonate in TCA toxicity
alkalinize serum
tx for heparin toxicity
protamine sulfate
tx for warfarin toxicity (2)
vitamin K
plasma (if active bleeding)
tx for tPA/streptokinase toxicity
aminocaproic acid
tx for theophylline toxicity
beta blocker
Fe poisoning is particularly common with ___
kids
Fe is cytotoxic because of ___
membrane lipid peroxidation
acute Fe poisoning presents with ___
gastric bleeding
chronic Fe poisoning presents wtih ___ (2)
metabolic acidosis
GI obstruction 2’ to scarring
drugs causing atropine-like SEs
TCA
drugs causing coronary vasospasm
cocaine
sumatriptan, ergot alkaloids
drugs causing flushing
vancomycin
adenosine
niacin
Ca2+ channel blockers
drugs causing dilated cardiomyopathy
doxorubicin, daunorubicin
drugs which cause torsades
class Ia antiarrhythmics (quinidine) class III antiarrhythmics (sotalol) antiarrhythmics, macrolides, antipsychotics, TCAs
drugs which cause agranulocytosis
clozapine carbamazepine colchicine dapsone PTU methimazole
drugs which cause aplastic anemia
chloramphenicol , carbamazepine benzene NSAIDs PTU methimazole
drug causing direct coombs positive hemolytic anemia
alpha methyldopa, penicilin
drug causing gray baby syndrome
chloramphenicol
drugs causing hemolysis in context of G6PD deficiency
INH sulfonamides , dapsone primaquine aspirin ibuprofen nitrofurantoin
drugs causing megaloblastic anemia
pheyntoin
MTX
sulfa
drugs causing thrombocytopenia
heparin, cimetidine
thromboti complications
OCPs
drug causing cough
ACEI
drugs causing pulmonary fibrosis
bleomycin
, methotrexate
amiodarone
busulfan
drug causing acute cholestatic hepatitis, jaundice
macrolide - erythromycin
drugs causing diarrhea
metformin, erythromycin, colchicine, orlistat, acarbose
drugs causing hepatic necrosis
halothane
Valproic acid
acetaminophen
amanita phalloides
drugs causing pancreatitis
didanosine, corticosteroids, alcohol, valproic acid, azathioprine, diuretics (furosemide, HCTZ)
drug causing hepatitis
INH
drugs causing pseudomembranous colitis
clindamycin
ampicillin, cephalosporins
drugs causing gynecomastia
spironolactone digitalis cimetidine alcohol ketoconazole estrogens
drugs causing hot flashes
tamoxifen
clomiphene
drugs causing adrenocortical insufficiency
glucocorticoid withdrawal leads to HPA suppression
drugs causing hypothyroidism
Li
amiodarone, sulfonamides
drugs causing gout
furosemide
, cyclosporine
thiazides, pyrizinamide, niacin
drugs causing photosensitivity
sulfonamides
amiodarone
tetracycline, 5FU
drugs causing Stevens-Johnson syndrome
anti-epileptic drugs (carbamazepine ethosuximide lamotrigine phenobarbital phenytoin ) sulfa penicillin allopurinol
drugs causing SLE-like syndrome
Sulfa, hydralazine
INH
procainamide
phenytoin, etanercept
drugs causing teeth discoloration
tetracyclines
drugs causing fat redistribution
protease inhibitors, glucocorticoids
drugs causing gingival hyperplasia
phenytoin, verapamil, cyclosporine, nifedipine
drugs causing myopathy
fibrates, niacine, colchicine, hydroxychloroquine, interferon-alpha, penicillamine, statins, glucocorticoids
drugs causing osteoporosis
corticosteroids, heparin
drugs causing cinchonism
quinidine, quinine
drugs causing parkinson-like syndrome
antipsychotics, reserpine, metoclopramide
drugs causing seizures
INH, buproprion, imipenem/cilastatin, tramadol, enflurane, metoclopramide
drugs causing tardive dyskinesia
antipsychotics, metoclopramide
fluoroquinolones cause ___ (3) in kids
tendonitis
tendon rupture
cartilage damage
___ causes Fanconi’s syndrome
expired tetracycline
Fanconi’s syndrome is ___ wasting of ___ (4)
tubular bicarbonate AAs glucose uric acid
3 drugs causing interstitial nephritis
methicillin
NSAIDs
furosemide
drugs causing hemorrhagic cystitis
prevent this by giving ___
Cyclophosphamide
ifosfamide
mesna
cardiovascular aspects of cinchonism
flushing
arrhythmia
4 neurological sx of cinchonism
tinnitus/hearing loss
blurry vision
somnolence
confusion
2 cutaneous sx of cinchonism
flushing
rash
drugs causing DI
Li
demeclocycline
drugs causing disulfiram-like reaction
metronidazole
cephalosporins (some)
, griseofulvin
procarbazine
1st generation sulfonylureas
disulfiram-like reaction means
mechanism is ___
feeling bad after EtOH
acetaldehyde dehydrogenase inhibition
drug causing nephrotoxicity + neurotoxicity
polymixins
drugs causing nephrotoxicity + ototoxicity
aminoglycosides
vancomycin
loop diuretics
cisplatin
drugs causing antimuscarinic effects?
atropine, TCAs, H1 blockers, antipsychotics
CYP450 inducers
chronic alcoholism, modafinil, St. John’s wort, Phenytoin, Phenobarbital, nevirapine, rifampine, griseofulvin, carbamezepine
CYP450 substrates
antiepileptics, anti-depressants, antipsychotics, anesthetics, theophylline, warfarin, statins, OCPs
CYP450 inhibitors
acute alcohol abuse, gemfibrozil, ciprofloxacin, isoniazid, grapefruit juice, quinidine, amiodarone, ketoconazole, macrolides, sulfonamides, cimetidine, ritonavir
Sulfa drugs
probenacid, furoseide, acetazolamide, celecoxib, thiazides, sulfonamide antibiotics, sulfasalazine, sulfonylurea
3 drugs metabolized by alcohol dehydrogenase
ethylene glycol
MeOH
EtOH
ethylene glycol is metabolized by alcohol dehydrogenase to ___
effects are ___ (2)
oxalic acid
acidosis
nephrotoxicity
MeOH is metabolized by alcohol dehydrogenase to ___ (2)
effects are ___ (2)
formaldehyde
formic acid
acidosis
retinal damage
EtOH is metabolized by alcohol dehydrogenase to ___
effects are ___ (3)
acetaldehyde
nausea
vomiting
hypoTN
___ inhibits alcohol dehydrogenase
fomepizole
5 non-obvious sulfa drugs
celecoxib probenecid thiazides sulfonylurea sumatriptan
systemic part of sulfa allergic rxn
fever
cutaneous part of sulfa allergic rxn (3)
rash
urticaria (hives)
Stevens-Johnson
hematologic part of sulfa allergic rxn (3)
Hemolytic anemia
thrombocytopenia
agranulocytosis