First Aid - Pharm 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 ___
(-)1/K_m
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
5 weak acid drugs
treat overdose of weak acid with ___
phenobarbital MTX TCAs aspirin bicarbonate
weak base drug
__a__
treat overdose wtih _b__
a. amphetamine
b. 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
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 major functions
inc. vascular smooth muscle contraction
inc. pupillary dilator muscle contraction (mydriasis)
increase intestinal and bladder sphincter muscle contraction
alpha_1 adrenergic receptor type
G_qPCR
alpha_2 major function
decrease sympathetic outflow
decrease insulin release
decrease lipolysis
increase platelet aggregation
alpha_2 adrenergic receptor type
G_iPCR
beta 1 adrenergic major functions
increase heart rate
increase contractility
increase renin release
increase lipolysis
beta_1 adrenergic receptor type
G_sPCR
beta_2 adrenergic major functions
vasodilation bronchodilation increase contractility increase HR increase insulin release increase lipolysis ciliary muscle relaxation increase aqueous humor production decrease uterine tone
beta_2 adrenergic recetor type
GsPCR
M1 muscarinic receptor is ___
M2 muscarinic receptor is ___
M3 muscarinic receptor is ___
G_qPCR
G_iPCR
G_qPCR
M1 major functions
CNS, ENS
M2 major functions
decrease HR and contractility of atria
M3 major functions
increase exocrine gland secretion
increase gut peristalsis
increase bladder contraction
bronchocontriction
increase pupillary sphincter muscle contraction (miosis)
ciliary muscle contraction (accomodation)
D1Rs: receptor type and
major functions
G_sPCR
renal vascular smooth muscle relaxation
D2Rs: receptor type and
major functions
G_iPCR
neurotransmitter modulation
H1Rs: receptor type and
major functions
G_qPCR nasal and bronchial mucus secretion vascular permeability bronchoconstriction itching pain
H2Rs: receptor type and
major functions
G_sPCR
gastric acid secretion
ADH V1Rs: receptor type and major functions
G_qPCR
vasoconstriction
ADH V2Rs: receptor type and major functions
G_sPCR
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 agonists: cholinomimetics
bethanechol, carbachol, pilocarpine, methacholine
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 agaonists (cholinomimetics)
neostigmine, pyridostigmine, physostigmine, donepezil, rivastigmins, galantamine
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
CNS penetrations of
a. pyridostigmine
b. physiostigmine
c. echothiophate
a. low
b. high
c. low
what indirect agonist do you use for alzheimer’s?
donepezil, rivastigmine, galantamine
cholinesterase inhibitor poisoning
DUMBBELSS: Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation of skeletal and CNS Lacrimation Sweating Salivation
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)
E effects which receptor
beta > alpha (with alpha at higher doses)
E is indicated for ___ (4)
anaphylaxis
open angle glaucoma
asthma
hypoTN
NE effects which receptor
alpha_1 > alpha_2 > beta_1
NE is indicated for ___
hypoTN (*decreases renal perfusion)
isoproterenol effects which receptor
beta_1 = beta_2
isoproterenol is indicated for ___
evaluation of tachyarrhythmias
DA effects which receptor
D1 = D2 > beta > alpha
DA is indicated for ___ (3)
shock
heart failure
unstable bradycardia
DA’s effects on the heart
+ inotrope
+ chronotrope
at high doses
dobutamine effects which receptor
beta_1 > beta_2 > alpha
dobutamine is indicated for ___ (3)
heart failure
cardiac stress testing
dobutamine’s effects on the heart
inotropic > chronotropic
phenylephrine effects which receptor
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
alpha_2 agonists are indicated for ___ with ___
HTN
renal disease
clonidine toxicity symptoms
CNS depression, bradycardia, hypotension, respiratory depression, small pupil size
alpha-methyl dopa toxicity symptoms
direct coombs + hemolytic anemia, SLE-like syndrome
2 non-selective alpha blockers
___ is reversible blocker
phenoxybenzamine
phentolamine
phentolamine
phenoxybenzamine use:
HTN
prevention in heochromocytoma
phenoxybenzamine toxicity:
orthostatic hypotension, reflex tachycardia
phentolamine use:
MAO inhibitor patients who ate too much tyramine
alpha_1 selective blockers end in ___
zosin
alpha_1 blockers are indicated for
HTN
urinary retention from BPH
PTSD
3 alpha_1 SEs
1st dose orthostatic hypoHTN
dizziness
headache
alpha_2 selective blocker
mirtazapine
mirtazapine is indicated for ___
depression
3 mirtazapine SEs
sedation
hyperlipidemia
hyperphagia
beta blockers effects
decrease heart rate and contractility decrease MI mortality decrease AV conduction velocity in SVT decrease cardiac output and renin secretion decrease progression of CHF decrease aqueous humor
2 beta blockers for SVT
propranolol
esmolol
sexual SE of beta blocker
impotence
acebutolol is ___-selective beta blocker
beta_1
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
metoprolol is ___-selective beta blocker
beta_1
nadolol is ___-selective beta blocker
non
pindolol is ___-selective beta blocker
non
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
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
tx for beta blocker toxicity
glucagon
tx for digitalis toxicity (5)
stop digitalis normalize K+ lidocaine anti-dig Fab Mg2+
tx for Fe toxicity
desferoxamine
tx for Pb toxicity (4)
CaEDTA
dimercaprol
succimer
penicillamine
tx for As/Au/Pb toxicity (4)
dimercaprol
succimer
penicillamine
CaEDTA
tx for Cu 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)
ethanol
dialysis
fomepizole
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
tx for warfarin toxicity (2)
vitamin K
FFP
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
2 drugs causing coronary vasospasm
cocaine
sumatriptan
4 drugs causing flushing
vancomycin
adenosine
niacin
CCBs
3 drugs which cause torsades
class Ia antiarrhythmics class III antiarrhythmics cisapride
6 drugs which cause agranulocytosis
clozapine carbamazepine colchicine dapsone PTU methimazole
5 drugs which cause aplastic anemia
chloramphenicol benzene NSAIDs PTU methimazole
drug causing direct coombs positive hemolytic anemia
alpha methyldopa
drug causing gray baby syndrome
chloramphenicol
drugs causing hemolysis in context of G6PD deficiency
INH sulfonamides primaquine aspirin ibuprofen nitrofurantoin
drugs causing megaloblastic anemia
pheyntoin
MTX
sulfa
drug causing cough
ACEI
3 drugs causing pulmonary fibrosis
bleomycin
amiodarone
busulfan
drug causing acute cholestatic hepatitis
macrolide
4 drugs causing hepatic necrosis
halothane
VPA
acetaminophen
amanita phalloides
drug causing hepatitis
INH
2 drugs causing pseudomembranous colitis
clindamycin
ampicillin
6 drugs causing gynecomastia
spironolactone digitalis cimetidine alcohol ketoconazole estrogens
2 drugs causing hot flashes
tamoxifen
clomiphene
2 drugs causing hypothyroidism
Li
amiodarone
2 drugs causing gout
furosemide
thiazides
3 drugs causing photosensitivity
sulfonamides
amiodarone
tetracycline
8 drugs causing Stevens-Johnson syndrome
carbamazepine ethosuximide lamotrigine phenobarbital phenytoin sulfa penicillin allopurinol
4 drugs causing SLE-like syndrome
hydralazine
INH
procainamide
phenytoin
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
2 drugs causing hemorrhagic cystitis
prevent this by giving ___
CTX
ifosfamide
mesna
2 drugs which cause cinchonism
quinidine
quinine
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
2 drugs causing DI
Li
demeclocycline
4 drugs causing PD-like syndrome
haloperidol
chlorpromazine
metoclopramide
reserpine
3 drugs causing seizures
buproprion
imipinem/cilastatin
INH
drugs causing tardive dyskinesia
antipsychotics
4 drugs causing disulfiram-like reaction
metronidazole
cephalosporins (some)
procarbazine
1st generation sulfonylureas
disulfiram-like reaction means
mechanism is ___
feeling bad after EtOH
acetaldehyde dehydrogenase inhibition
drug causing nephrotoxicity + neurotoxicity
polymixins
4 drugs causing nephrotoxicity + ototoxicity
aminoglycosides
vancomycin
loop diuretics
cisplatin
9 CYP450 inducers
quinidine barbiturates st. john's wort phenytoin rifampin griseofulvin carbamazepine chronic alcholism
CYP450 inhibitors
INH sulfonamides cimetidine erythromycin grapefruit
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)
HA
thrombocytopenia
agranulocytosis