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