Pda2 Test 1 Set 2

Front 1

Structural nonspecific drugs act in what way? and 1 ex

Back 1

physical ways

antacids

Front 2

Structurally specific acting agents act how?

Back 2

with a specific receptor that initiates a specific biologic response or transduction of a signal

Front 3

Structurally specific acting agents are also called...

Back 3

ligands

Front 4

Receptors are usually located where? and composed of what? and are usually ____ for a certain ligand

Back 4

in/on a membrane

protein

stereospecific

Front 5

Which affinity is higher 1mcg or 1mg? and why

Back 5

1mcg, b/c takes only 1mcg to saturate receptor

Front 6

Potency?

Back 6

min amt. reqd to elicit response

Front 7

Efficacy?

Back 7

can we get a full response when ligand interacts w/ receptor

Front 8

A receptor is usually composed of _____ AA's

Back 8

3-4

Front 9

A biologic response is the result of...

Back 9

interaxn of drug w/ fxnal group of molecules

Front 10

____ forces must be involved in the drug-receptor complex

Back 10

weak forces

Front 11

Drug must have ____ to interact well w/ receptor

Back 11

high degree of structural specificity w/ complimentary groups

Front 12

Bonds used by ligands to interact w/ receptor (6) (and which is not weak?)

Back 12

1)hydrogen bonds
2)ionic bonds
3)van der waals
4)hydrophobic
5)dipole-dipole
6)covalent****

Front 13

3 types of ionic bonds (and what makes them ionic bonds)

Back 13

1)ionic
2)ion-dipole
3)reinforced ionic interaxns

require a charge

Front 14

What groups can form Hydrogen bonds (4) and why?

Back 14

-OH, -COOH, -NH2, =NH

b/c of excessive electrons on O and N

Front 15

___ bonds are seen in suicide interaxns

Back 15

covalent

Front 16

4 major types of steric factors influence pharmacological activity?

Back 16

2)geometric isomerism
1)optical isomerism
2)conformational isomerism
3)isosterism

Front 17

Constitutional isomer? (2)

Back 17

1)difference in connectivity
2)different physical properties

Front 18

Configurational isomer (3)

Back 18

1)differing in the spatial array of atoms
2)non-superimposable
3)usually contain a chiral carbon

Front 19

Conformational isomer? (2)

Back 19

1)differing in spatial array of atoms in a molecule of a given constitution and configuration
2)rotamers

Front 20

What determines which rotamer a receptor will accept?

Back 20

will accept one that is most stable w/ least amount of energy

Front 21

Enantiomers? (2)

Back 21

1)non-superimposable
2)mirror images

Front 22

Difference in biologic activity b/w optical isomers depends on....

Back 22

ability to react selectively at an asymmetric center in the biological system

Front 23

4 things to overcome before desired biologic response

Back 23

2)membrane selectivity
3)selective metabolism
4)non-specific receptors
5)desired response

Front 24

Ligand activity can be lost via...

Back 24

acting @ non-specific receptors

Front 25

Why do enantiomers differ in biologic response (4)

Back 25

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

Front 26

If asked on test which isomer has the majority of activity + or - which is usually right?

Back 26

-

Front 27

Problem with chiral compounds? and what must be done to drugs w/ chiral carbons?

Back 27

having more than 1 chiral carbon gives many isomers

the different isomers must be separated (chiral separation)

Front 28

B2 adrenergic receptor has how many domains and what are domains?

Back 28

7 domains

[]ed areas of AAs in membrane

Front 29

What 3 AAs form AS of B2 adrenergic receptor and use what kind of bonds?

Back 29

Serine 204, Serine 207, Aspartate 113

2 hydrogen bonds, 1 ionic bond

Front 30

Geometric isomer types (2)

Back 30

1)diasteriomers
2)cis/trans isomers

Front 31

Influence of geometric isomerism on pharmacological activity

Back 31

differences in interatomic distances of groups influences pharmacological activity at receptor

Front 32

Conformational isomerism and pharmacological activity (3)

Back 32

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

Front 33

Stay away from what when making a drug?

Back 33

drugs w/ a rotatable bond b/c it results in too many CONFORMATIONS

Front 34

Pharmacophore building from ___ is done....

Back 34

knowledge of the structure of the target (receptor)

Front 35

Will any compound with proper dimensions to have activity at an opoid receptor always be an opoid?

Back 35

NO

Front 36

Drug of know pharmacological profile is ID'd as the....

Back 36

lead compound

Front 37

Analogs of the lead compound are synthesized by....(2)

Back 37

1)modify structure to retain/reinforce the desirable effect while minimizing unwanted effects
2)use target analogs as pharmacological probes

Front 38

Molecular modifications of the "lead compound" can involve one or more of the follow strategies:(5)

Back 38

1)bioisosteric replacement
2)design of rigid analogs
3)homologation of alkyl chains
4)alteration of stereochemistry
5)alteration of interatomic distances

Front 39

Bioisosterism
a)derived from...
b)bioisosteric similarity of molecules is commonly assigned on basis of....
c)2 subdivision of bioisosterism

Back 39

a)certain physical properties of chemically different substances are similar
b)valence of electrons of an atom
c)classical bioisosteres, nonclassical bioisosteres

Front 40

Most common classical bioisosteres (2)

Back 40

1)F for H
2)OH for NH

Front 41

What happens to acid in the stomach via stimulated by...
a)PSNS
b)SNS

Back 41

a)increase in acid
b)decrease in acid

Front 42

Parietal Cell fxn and mechanism (2)

Back 42

1)puts acid into stomach using an H/K pump
2)does this when H2 histamine receptor is stimulated

Front 43

ECL Cell fxn and mechanism (3)

Back 43

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

Front 44

Decrease acid to the stomach via 2 mechanisms (2)

Back 44

1)inhibit H/K pump
2)block histamine H2 receptor

Front 45

____ goes from kidney to bladder

Back 45

ureters

Front 46

Urogenital system is controlled by...(2)

Back 46

1)smooth muscle
2)ANS

Front 47

Urinary bladder parts (4)

Back 47

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)

Front 48

Urinary bladder smooth muscle activations (2)

Back 48

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

Front 49

How is bladder sort of controlled voluntarily?

Back 49

Somatic muscles surround trigone and urethera to provide voluntary retention

Front 50

When happens to penis when stimulated by...
a)SNS
b)PSNS

Back 50

a)ejaculation
b)erection

Front 51

Penis parts fxns
a)seminal vesicle
b)vas deferens
c)prostatic capsule

Back 51

a)contains sperm
b)conveys sperm from testicles to seminal vesicle
c)pushes semen out

Front 52

Penis activations (2)

Back 52

1)alpha1 activation causes contraction of seminal vesicles, prosstatic capsule, vas deferens causing ejaculation

2)M3 receptor activation causes erection

Front 53

Which ANS mostly innervates vasculature (and exception)

Back 53

SNS (except in penis)

Front 54

Vascular smooth muscles activations (2)

Back 54

1)alpha1/2 vasoconstriction
2)B2 vasodilation

Front 55

What receptor domainates
a)blood vessels to liver and skeletal muscle
b)other blood vessels

Back 55

a)B2
b)alpha1

Front 56

M3 is found rarely on BLOOD VESSELS, what is its effect?

Back 56

VASODILATION

Front 57

Vasodilation process in blood vessel at M3 receptor (2)

Back 57

1)arginine to NO via NO synthase
2)NO and GTP to cGMP via guanyl cyclase

Front 58

Why will heart beat if pulled from chest?

Back 58

b/c SA node spontaneously depolarizes

Front 59

Receptor types found in heart and what dominates (2)

Back 59

M2****
B1

Front 60

Heart term definitions
a)inotropic
b)chronotropic
c)dromotropic

Back 60

a)contractile force
b)frequency of heart beat
c)conduction thru AV node

Front 61

Heart activation of M2 receptor results (3)

Back 61

1)decreased frequency of beating (negative chronotropic)
2)decrease in contractile force (negative inotropic)
3)delays conduction thru AV node (negative dromotropic)

Front 62

Heart activation of B1 receptor results (3)

Back 62

1)increased frequency of beating (positive chronotropic)
2)increase in contractile force (positive inotropic)
3)enhances conduction thru AV node (positive dromotropic)

Front 63

____ not nerves line the inside of the heart

Back 63

conducting fibers

Front 64

M3 stimulates what secretory glands? (3) via what NT?

Back 64

1)salivary
2)nasopharyngeal
3)sweat glands

ACh

Front 65

alpha1 stimulates what secretion?

Back 65

1)sparse amounts of think fluid from salivary gland

Front 66

B2 receptor stimulates what secretion? (2)

Back 66

1)amylase
2)insulin

Front 67

alpha2 receptor stimulates what secretion?

Back 67

inhibits insulin release

Front 68

Adenylate cyclase
a)activated by...(2)
b)mechanism (4)

Back 68

a)adrenaline, glucagon
b1)adenylate cyclase gets activated @ B3 receptor
b2)converts ATP to cAMP
b3)cAMP activates PKA
b4)PKA activates lipase

Front 69

Adipose tissue
a)receptor
b)fxn

Back 69

a)B3
b)mediates lipolysis

Front 70

Glycogenolysis
a)receptor
b)fxn
c)most evident where?

Back 70

a)B2
b)convert glycogen to glucose in all tissues
c)skeletal muscle, liver

Front 71

ACh effect on BP

Back 71

decrease

Front 72

Atropine is a....

Back 72

muscarinic antagonist

Front 73

LARGE ACh dose after atropine effect on BP

Back 73

reduction in BP followed by increase in BP; overshoot caused by SNS overcompensation

Front 74

Epinephrine after atropine effect on BP

Back 74

increase in BP

Front 75

phenoxybenzamine fxn

Back 75

block alpha receptors irreversible

Front 76

Epinephrine after atropine and phenoxybenzamine BP/HR effects

Back 76

incr heart rate

decr BP (get B effects b/c alpha is blocked) (EPINEPHRINE REVERSAL)

Front 77

Cholinomimetic drugs (5)

Back 77

1)methacholine
2)bethanechol
3)pilocarpine
4)nicotine
5)TMA

Front 78

Methacholine
a)metabolism (2)
b)site of axn
c)therapeutic use (2)

Back 78

a)not metabolized by pseudo cholinesterase; slowly metabolized by acetylcholinesterase
b)muscarinic agonist
c)diagnostic for bronchial asthma, peripheral vascular spasms

Front 79

Bethanechol
a)metabolism
b)site of axn
c)therapeutic uses (2)

Back 79

a)NOT susceptible to hydrolysis by acetylcholinesterase
b)muscarinic receptors in GI and urinary bladder
c)treat postoperative abdominal distension and postoperative urinary retention

Front 80

Pilocarpine
a)properties (3)
b)site of axn
c)therapeutic uses

Back 80

a)alkaloid, non-choline ester, tertiary amine
b)muscarinic receptors that can affect CNS by crossing BBB
c)glaucoma

Front 81

Why is ACh not used clinically? (2)

Back 81

1)massive metabolism
2)acts @ many sites in body

Front 82

Adverse effects of cholinomimetics? (6)

Back 82

1)salivation
2)diaphoresis (incr sweating)
3)intestinal cramping
4)hypotension
5)dyspnea (via bronchoconstriction)
6)spasm of accommodation

Front 83

Adverse effects of cholinomimetics: Hypotension can be caused at 2 sites...

Back 83

endothelial cell @ M3

SA node

Front 84

Narrow/closed angle glaucoma?
a)cause
b)can cause...
c)optical treatment

Back 84

a)blockage of drainage of aqueous humor (aqeous humor production is normal)
b)blindness due to pressure on optic nerve
c)remove iris

Front 85

Open angle glaucoma cause

Back 85

increased production of aqueous humor; drainage of it is normal

Front 86

Mechanism of pilocarpine's treatment of glaucoma? and what type of glaucoma

Back 86

cause miosis to facilitate drainage in narrow angle glaucoma

Front 87

3 contraindications of cholinomimetics

Back 87

1)bronchial asthma
2)gastrointestinal ulcer
3)hyperthyroidism

Front 88

Why are GI ulcer and hyperthyroidism contraindications of cholinomimetics?

Back 88

1)cholinomimetics incr acid and incr GI smooth muscle contractions
2)mimetics are bad w/ hyperthyroidism b/c these ppl have sensitive myocardiums

Front 89

Direct acting nicotinic cholinomimetics fxn?

Back 89

smoking cessation

Front 90

Reversible cholinesterase inhibitors? (2)

Back 90

1)physostigmine
2)neostigmine

Front 91

Reversible inhibitors of acetylcholinesterase act by...

Back 91

inhibiting destruction of ACh

Front 92

Physostigmine
a)mechanism
b)sites of axn
c)use
d)unique feature
e)drug category

Back 92

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

Front 93

Neostigmine
a)mechanism
b)sites of axn
c)use
d)difference from physostigmine
e)drug category

Back 93

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

Front 94

Edrophonium
a)category of drug
b)use
c)axns are...

Back 94

a)reversible ACHesterase inhibitor
b)diagnosis of myasthenia gravis
c)indirect, short

Front 95

General formula of IRReversible inhibitors of ACHesterase

Back 95

O
||
R-P-X
||
R

Front 96

IRReversible inhibitors of ACHesterase act by...and are...

Back 96

covalently phosphorylating esteratic site of cholinesterase

TOXIC

Front 97

IRReversible inhibitors of ACHesterase (2 and other are..)

Back 97

1)DFP
2)Echothiophate
3)nerve gases, pesticides

Front 98

DFP
a)sites of axn
b)therapeutic uses
c)drug class
d)warning
e)CNS activity?

Back 98

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

Front 99

Echothiophate
a)sites of axn
b)therapeutic uses
c)drug class
d)CNS activity?

Back 99

a)all PERIPHERAL
b)miotic for narrow glaucoma
c)IRReversible ACHesterase inhibitor
d)NO

Front 100

Adverse effects of IRReversible ACHesterase inhibitors (4)

Back 100

1)cholinergic overstimulation with paralysis of respiratory muscles
2)ganglionic blockade
3)cataracts
4)chronic neurotoxicity: weak leg, recovery slow