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100 Cards in this Set

  • Front
  • Back
Structural nonspecific drugs act in what way? and 1 ex
physical ways

antacids
Structurally specific acting agents act how?
with a specific receptor that initiates a specific biologic response or transduction of a signal
Structurally specific acting agents are also called...
ligands
Receptors are usually located where? and composed of what? and are usually ____ for a certain ligand
in/on a membrane

protein

stereospecific
Which affinity is higher 1mcg or 1mg? and why
1mcg, b/c takes only 1mcg to saturate receptor
Potency?
min amt. reqd to elicit response
Efficacy?
can we get a full response when ligand interacts w/ receptor
A receptor is usually composed of _____ AA's
3-4
A biologic response is the result of...
interaxn of drug w/ fxnal group of molecules
____ forces must be involved in the drug-receptor complex
weak forces
Drug must have ____ to interact well w/ receptor
high degree of structural specificity w/ complimentary groups
Bonds used by ligands to interact w/ receptor (6) (and which is not weak?)
1)hydrogen bonds
2)ionic bonds
3)van der waals
4)hydrophobic
5)dipole-dipole
6)covalent****
3 types of ionic bonds (and what makes them ionic bonds)
1)ionic
2)ion-dipole
3)reinforced ionic interaxns

require a charge
What groups can form Hydrogen bonds (4) and why?
-OH, -COOH, -NH2, =NH

b/c of excessive electrons on O and N
___ bonds are seen in suicide interaxns
covalent
4 major types of steric factors influence pharmacological activity?
2)geometric isomerism
1)optical isomerism
2)conformational isomerism
3)isosterism
Constitutional isomer? (2)
1)difference in connectivity
2)different physical properties
Configurational isomer (3)
1)differing in the spatial array of atoms
2)non-superimposable
3)usually contain a chiral carbon
Conformational isomer? (2)
1)differing in spatial array of atoms in a molecule of a given constitution and configuration
2)rotamers
What determines which rotamer a receptor will accept?
will accept one that is most stable w/ least amount of energy
Enantiomers? (2)
1)non-superimposable
2)mirror images
Difference in biologic activity b/w optical isomers depends on....
ability to react selectively at an asymmetric center in the biological system
4 things to overcome before desired biologic response
2)membrane selectivity
3)selective metabolism
4)non-specific receptors
5)desired response
Ligand activity can be lost via...
acting @ non-specific receptors
Why do enantiomers differ in biologic response (4)
1)difference in reactivity at the receptor site
2)selective metabolism of one isomer
3)selective adsorption by membranes
4)rxns at non-specific receptors, thus loss of activity
If asked on test which isomer has the majority of activity + or - which is usually right?
-
Problem with chiral compounds? and what must be done to drugs w/ chiral carbons?
having more than 1 chiral carbon gives many isomers

the different isomers must be separated (chiral separation)
B2 adrenergic receptor has how many domains and what are domains?
7 domains

[]ed areas of AAs in membrane
What 3 AAs form AS of B2 adrenergic receptor and use what kind of bonds?
Serine 204, Serine 207, Aspartate 113

2 hydrogen bonds, 1 ionic bond
Geometric isomer types (2)
1)diasteriomers
2)cis/trans isomers
Influence of geometric isomerism on pharmacological activity
differences in interatomic distances of groups influences pharmacological activity at receptor
Conformational isomerism and pharmacological activity (3)
1)have non-identical spatial arrangement b/c of rotation of atoms about a single bond
2)difficult to predict which conformation interacts w/ receptor best
3)pharmacophore that binds to the receptor maybe different than the preferred conformation in the crystalline state
Stay away from what when making a drug?
drugs w/ a rotatable bond b/c it results in too many CONFORMATIONS
Pharmacophore building from ___ is done....
knowledge of the structure of the target (receptor)
Will any compound with proper dimensions to have activity at an opoid receptor always be an opoid?
NO
Drug of know pharmacological profile is ID'd as the....
lead compound
Analogs of the lead compound are synthesized by....(2)
1)modify structure to retain/reinforce the desirable effect while minimizing unwanted effects
2)use target analogs as pharmacological probes
Molecular modifications of the "lead compound" can involve one or more of the follow strategies:(5)
1)bioisosteric replacement
2)design of rigid analogs
3)homologation of alkyl chains
4)alteration of stereochemistry
5)alteration of interatomic distances
Bioisosterism
a)derived from...
b)bioisosteric similarity of molecules is commonly assigned on basis of....
c)2 subdivision of bioisosterism
a)certain physical properties of chemically different substances are similar
b)valence of electrons of an atom
c)classical bioisosteres, nonclassical bioisosteres
Most common classical bioisosteres (2)
1)F for H
2)OH for NH
What happens to acid in the stomach via stimulated by...
a)PSNS
b)SNS
a)increase in acid
b)decrease in acid
Parietal Cell fxn and mechanism (2)
1)puts acid into stomach using an H/K pump
2)does this when H2 histamine receptor is stimulated
ECL Cell fxn and mechanism (3)
1)secretes histamine to activate parietal cell @ H2 receptor
2)is activated by neurocrine via ACh receptor
3)OR is activated by endocrine via Gastrin receptor
Decrease acid to the stomach via 2 mechanisms (2)
1)inhibit H/K pump
2)block histamine H2 receptor
____ goes from kidney to bladder
ureters
Urogenital system is controlled by...(2)
1)smooth muscle
2)ANS
Urinary bladder parts (4)
1)detrusor (which contracts to squeeze urine out of bladder)
2)trigone (sphincter muscle that allows urine out of bladder)
3)ureter (how urine gets in)
4)urethra (how urine gets out)
Urinary bladder smooth muscle activations (2)
1)M3 receptor activation causes contraction of detrusor and relaxation of trigone = micturation

2)B2 activation causes relaxation of detrusor and alpha1 activation causes contraction of trigone = retention
How is bladder sort of controlled voluntarily?
Somatic muscles surround trigone and urethera to provide voluntary retention
When happens to penis when stimulated by...
a)SNS
b)PSNS
a)ejaculation
b)erection
Penis parts fxns
a)seminal vesicle
b)vas deferens
c)prostatic capsule
a)contains sperm
b)conveys sperm from testicles to seminal vesicle
c)pushes semen out
Penis activations (2)
1)alpha1 activation causes contraction of seminal vesicles, prosstatic capsule, vas deferens causing ejaculation

2)M3 receptor activation causes erection
Which ANS mostly innervates vasculature (and exception)
SNS (except in penis)
Vascular smooth muscles activations (2)
1)alpha1/2 vasoconstriction
2)B2 vasodilation
What receptor domainates
a)blood vessels to liver and skeletal muscle
b)other blood vessels
a)B2
b)alpha1
M3 is found rarely on BLOOD VESSELS, what is its effect?
VASODILATION
Vasodilation process in blood vessel at M3 receptor (2)
1)arginine to NO via NO synthase
2)NO and GTP to cGMP via guanyl cyclase
Why will heart beat if pulled from chest?
b/c SA node spontaneously depolarizes
Receptor types found in heart and what dominates (2)
M2****
B1
Heart term definitions
a)inotropic
b)chronotropic
c)dromotropic
a)contractile force
b)frequency of heart beat
c)conduction thru AV node
Heart activation of M2 receptor results (3)
1)decreased frequency of beating (negative chronotropic)
2)decrease in contractile force (negative inotropic)
3)delays conduction thru AV node (negative dromotropic)
Heart activation of B1 receptor results (3)
1)increased frequency of beating (positive chronotropic)
2)increase in contractile force (positive inotropic)
3)enhances conduction thru AV node (positive dromotropic)
____ not nerves line the inside of the heart
conducting fibers
M3 stimulates what secretory glands? (3) via what NT?
1)salivary
2)nasopharyngeal
3)sweat glands

ACh
alpha1 stimulates what secretion?
1)sparse amounts of think fluid from salivary gland
B2 receptor stimulates what secretion? (2)
1)amylase
2)insulin
alpha2 receptor stimulates what secretion?
inhibits insulin release
Adenylate cyclase
a)activated by...(2)
b)mechanism (4)
a)adrenaline, glucagon
b1)adenylate cyclase gets activated @ B3 receptor
b2)converts ATP to cAMP
b3)cAMP activates PKA
b4)PKA activates lipase
Adipose tissue
a)receptor
b)fxn
a)B3
b)mediates lipolysis
Glycogenolysis
a)receptor
b)fxn
c)most evident where?
a)B2
b)convert glycogen to glucose in all tissues
c)skeletal muscle, liver
ACh effect on BP
decrease
Atropine is a....
muscarinic antagonist
LARGE ACh dose after atropine effect on BP
reduction in BP followed by increase in BP; overshoot caused by SNS overcompensation
Epinephrine after atropine effect on BP
increase in BP
phenoxybenzamine fxn
block alpha receptors irreversible
Epinephrine after atropine and phenoxybenzamine BP/HR effects
incr heart rate

decr BP (get B effects b/c alpha is blocked) (EPINEPHRINE REVERSAL)
Cholinomimetic drugs (5)
1)methacholine
2)bethanechol
3)pilocarpine
4)nicotine
5)TMA
Methacholine
a)metabolism (2)
b)site of axn
c)therapeutic use (2)
a)not metabolized by pseudo cholinesterase; slowly metabolized by acetylcholinesterase
b)muscarinic agonist
c)diagnostic for bronchial asthma, peripheral vascular spasms
Bethanechol
a)metabolism
b)site of axn
c)therapeutic uses (2)
a)NOT susceptible to hydrolysis by acetylcholinesterase
b)muscarinic receptors in GI and urinary bladder
c)treat postoperative abdominal distension and postoperative urinary retention
Pilocarpine
a)properties (3)
b)site of axn
c)therapeutic uses
a)alkaloid, non-choline ester, tertiary amine
b)muscarinic receptors that can affect CNS by crossing BBB
c)glaucoma
Why is ACh not used clinically? (2)
1)massive metabolism
2)acts @ many sites in body
Adverse effects of cholinomimetics? (6)
1)salivation
2)diaphoresis (incr sweating)
3)intestinal cramping
4)hypotension
5)dyspnea (via bronchoconstriction)
6)spasm of accommodation
Adverse effects of cholinomimetics: Hypotension can be caused at 2 sites...
endothelial cell @ M3

SA node
Narrow/closed angle glaucoma?
a)cause
b)can cause...
c)optical treatment
a)blockage of drainage of aqueous humor (aqeous humor production is normal)
b)blindness due to pressure on optic nerve
c)remove iris
Open angle glaucoma cause
increased production of aqueous humor; drainage of it is normal
Mechanism of pilocarpine's treatment of glaucoma? and what type of glaucoma
cause miosis to facilitate drainage in narrow angle glaucoma
3 contraindications of cholinomimetics
1)bronchial asthma
2)gastrointestinal ulcer
3)hyperthyroidism
Why are GI ulcer and hyperthyroidism contraindications of cholinomimetics?
1)cholinomimetics incr acid and incr GI smooth muscle contractions
2)mimetics are bad w/ hyperthyroidism b/c these ppl have sensitive myocardiums
Direct acting nicotinic cholinomimetics fxn?
smoking cessation
Reversible cholinesterase inhibitors? (2)
1)physostigmine
2)neostigmine
Reversible inhibitors of acetylcholinesterase act by...
inhibiting destruction of ACh
Physostigmine
a)mechanism
b)sites of axn
c)use
d)unique feature
e)drug category
a)slowly hydrolyzed substrate for AChesterase; so ties it up
b)all cholinergic synapses
c)miotic/glaucoma
d)can cross BBB b/c not a quaternary ammonium salt (CNS axns)
e)reversible inhibitors of ACHesterase
Neostigmine
a)mechanism
b)sites of axn
c)use
d)difference from physostigmine
e)drug category
a)slowly hydrolyzed substrate of AChesterase; so ties it up
b)indirect at all cholinergic synapses; direct @ neuromuscular jxn (somatic)
c)myasthenia gravis (muscle weakness) via facilitating nerve impulses
d)is a quaternary ammonium salt so NO CNS actions
e)reversible inhibitor of ACHesterase
Edrophonium
a)category of drug
b)use
c)axns are...
a)reversible ACHesterase inhibitor
b)diagnosis of myasthenia gravis
c)indirect, short
General formula of IRReversible inhibitors of ACHesterase
O
||
R-P-X
||
R
IRReversible inhibitors of ACHesterase act by...and are...
covalently phosphorylating esteratic site of cholinesterase

TOXIC
IRReversible inhibitors of ACHesterase (2 and other are..)
1)DFP
2)Echothiophate
3)nerve gases, pesticides
DFP
a)sites of axn
b)therapeutic uses
c)drug class
d)warning
e)CNS activity?
a)all cholinergic synapses (indirect only)
b)miotic/glaucoma
c)IRReversible inhibitors of ACHesterase
d)crosses skin easily and is toxic if it does
e)Yes
Echothiophate
a)sites of axn
b)therapeutic uses
c)drug class
d)CNS activity?
a)all PERIPHERAL
b)miotic for narrow glaucoma
c)IRReversible ACHesterase inhibitor
d)NO
Adverse effects of IRReversible ACHesterase inhibitors (4)
1)cholinergic overstimulation with paralysis of respiratory muscles
2)ganglionic blockade
3)cataracts
4)chronic neurotoxicity: weak leg, recovery slow