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Pharmacology > 1.3 Interactions, Agonist & Isomerism > Flashcards

1.3 Interactions, Agonist & Isomerism Flashcards

1
Q

Absorprtion

A

ADME

Charcoal - toxic in pos

Prokinetic - alter GIT

muscarinic - inhib emptying - oppostie

Distrib - CO increase red speec absorb
BBloq - red co sux longer NMJ

COmpeter site - enzyme syst
Phenytoin w/ sulphonamide - displace pheny

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2
Q

Metabolism

A

Ph 1 Red/ox/hydrol
Cyt p450

Inducers
Rifampicin

Inhib
Cimitideine

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3
Q

Excretion

A

Change urinary ph

Sod bic - aspirin increase

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4
Q

PD interactions

A

2 drugs @ / near site action

Direct - same mechanism
Flumazenil rev BZD
Naloxone - opiod

Indeirect - differ
neostigmine - rev NDMR - achesterase inhib
More ach at clef -compete NDMR binding site
Adrenaline - inc cAMP by GpCR
Enox - PDEi - inc CAMP

Indirect increase cAMP improve contractiliy

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5
Q

What is Cytp450

A 
Family protein in Sm ER heaptocytes
Mediate Red/Ox
Isoform enzyme
7  most improtant in metab
CYP3A4 - most
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6
Q

Induce cyp450

A 
Barbiturates
Phenytoin
Carbamazepine
griseofulvin
rifampicin

Chronic alcohol

Polycyclic hrdyocarb - tobacco . meats
Brocolli - 1 form

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7
Q

Inhbi cyp450

A

Imdazole derive - keto con, itra omprea
cimetidine
etomidate -
all by bind w/ haem

Macolride
Most anti dipre
HIV protease inhib
cyclosporine
Amio

Grapefruit juice

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8
Q

Summation

A

Action drugs additive

Premed w/ bzf - then prop
Dose to achieve anaesethesia lower

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9
Q

Synergism

A

Combined action 2 drugs greater than summation

Sulphonamide & Trimethoprim

Bacteristitc alone
together bactericidal

clonidie & opiate

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10
Q

Potentiation

A

1 drugh increases effect of other

NDMR - from Mag

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11
Q

Isobolgram

A

Effeects 2 drugs
Interaction /2
Fract conc - repr x y

Draw from pg158

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12
Q

Affinity

A

How avidly a drug binds to receptor

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13
Q

Intrinsic activity

A

‘efficacy’

Magnitude of effect drug produces after bound to receptor

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14
Q

Potency

A

Measure quanitiy drug needed to produce max effect

Large dose - not potent - small dose - max effect

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15
Q

Compare potency two drugs

A

Compare EC50 or ED50

EC 50 - conc drug prod spec repsonse halfway base & max

ED50
Specific response in 50% population take

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16
Q

Agonist

A

Signifcant affinity for receptor & full intrinsic activity

Bind - receptor prod max response that capable
intrisnic activity of 1

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17
Q

Partial agonist

A

Significant affinity but only partial intrinsic activity
max response never mediate
Int act 0-1
Bupenonrphine at U rec

Can act as agonist or antag - dep sitatuion

Use alone - agonist
produce some response even if not max

Also if use along a low dose true agon

If use w/ high dose true agonist - competitive antagonist - compete for receptpr - prevent full occupancy & ergo max response

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18
Q

Inverse agonist

A

Significant affinity & intrisnce activty - opposit effect to endog agonist

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19
Q

Antagonist

Types

A

Signif affinity - no intrnisic activty
bind no response - 0

Reversible
compet or non compt

Rev comp antag compete same receprot - effect of antag overcome increase dose agonist
NDMR (nic rec NMJ) & bbloq 0 com adrenaline @ b

Rev non comp - prev activation throuhg distrortion of receptor not bind same site
Cannot overcome w/ inc conc
Kewatmine 0- glut at NMDA

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20
Q

Rev Comp Antag & Rev Non comp

A

Rev comp antag compete same receprot - effect of antag overcome increase dose agonist
NDMR (nic rec NMJ) & bbloq 0 com adrenaline @ b

Rev non comp - prev activation throuhg distrortion of receptor not bind same site
Cannot overcome w/ inc conc
Kewatmine 0- glut at NMDA

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21
Q

Irrev antagonist

A

Bind irreversibly to rec or distant site
prevent binding
The agonist dose will not overcome as it is irreversible

Pehnoxybenzamine
Alpha adreno to antagonise catetchol

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22
Q

Competitve antagonist + Inverse agonist

A

Inverse agonist - exert to physiolog effect Opposit to agonist - bind w/rec

Competiv antag - no direct effect own - stop endog agonist

23
Q

Dose reponse curve

A

Draw

Graph conc x & response Y
Hyoerbolic
Initially drug conc inc & rec occupancy increase
- response increases

Number receptor decrease - effect increase - sammler effect of response
slope flatten @ 100

ec - halfway ma & min

24
Q

Log dose reponse curve

A

Semi log plot
log scale - dose x & response on Y
Classic sigmod shape
Steep part - approx linear - asses relationshjip easeier ed50 on steep linear part

25
Q

Curve drug lower potenc

A

right shift in curve - max reponse save - height identical (higher conc reqd to prod response)

26
Q

Right shjift of curve

A

Competive antag gven - higher conc reqired

27
Q

Curve w/ non competitive antagonist

A

Move ro right max reponse recued - increase dose will not overcome

28
Q

Parttial agonist -

A

no shift - impossible elicit max response heigh samller = pg 163

29
Q

Dose ratio

A

Dose gaonist in inhbibot/ dose agonist in abense inhbitor

Extent right shift - response curve w/ compet antagonist

Factor which dose increase to pro max respomse

30
Q

Isomerism

A

Chemical compound same molecular formuale & weight but diff structural arrangement

Diff phys / chem prop

31
Q

Sreuctural isomers

A

Identical chemical formulae - diff arrangement bond -= diff structure

wide range between sim effect to diff

Chain
Position
Dynamic - tautomerism

32
Q

Stereoisomers

A

Same atoms & same bond structure

Diff 3d config

Optical
geomeric

33
Q

chain isomers

A

Carbon chain alter - fnctiongroup same

butane & isobtene examples

34
Q

Position isomers

A

Same structure - function group different
Isoflurane
+ enflurane

35
Q

Dynamic structural isomer

A

‘tautomerism’

Molecule exist two diff form depend physical environment

midaz ion @ ph4
Change structure - at phys pH - lipid soluble - 7 ember uni ring

36
Q

Geometric isomers

A

Geometric - same chem constit +covalent bond -

diff spatial arrangement
molecule -

2 dissim group attached to 2 atoms - linked bound bond or ring
same side of colane t- cis
Opposite side transe

mivacurium 3 geometric isomer
majority - tran tran
trans cis cis cis
trac 10 - cis trac on

37
Q

Optical isomers

A

mirror image that are not superimposable

at least 1 chiral centre

38
Q

What is a chiral centre

A

Central atom that surronded by 4 diff chem groups
Arranged around central atom

1 group certically other 3 point to vertices of a tetrahedon

2 possible arrangeent - which are mirror image and non superimp
Like hnds

39
Q

Optical stereoisomers

A

All optically active - rotate palne polarised light
1 isomer rotate

left - Laevorotray

right dextrorotatory

‘Enatiomers’

Same pharmacochem
BP
Density
colour

drug action depends on parhamochem - similar action

if action dep on bind to rec - confromation difference = mark difference in activtyy

40
Q

Nming steroeoisomer

A

Atom lower number - oserver
other thre lie on plane - number identifiy - descend clockwise - rectus

anti clockcwise - sinister - S

41
Q

Racemic mix

A

Equal prop of different enationmers

Volatile (not sevo)

Equal prop of two enant - 1 may ber reponsi side effect other confer activity

42
Q

Enatiopure

A

Only one enantiomer
S - better PK ^ PD than R

S bupiv, ropib, ketamine - side effect profile better

43
Q

Diastereoismers

A

> 1 chiral centre - mutliple steroisomer - not mirror images there not enatiomers

Trac - 4 chiral

44
Q

Physiolog enantiomers

A

Signle isomers - enzyme produce 1 conform

Carbo dextrorotary rotate to right
gluc d gluc - dextrose

45
Q

Non-competitive antagonists
How

Can be reversed w/ increasing the conc

Give some examples x3

A

do not bind to the same receptor as agonists but they reduce its effect in some other way.

Increasing the agonist concentration will not overcome the antagonist effect.

An irreversible competitive antagonist is a receptor antagonist that dissociates from receptors slowly, or not at all. This term is often used instead of non-competitive antagonist.

Phenoxybenzamine is a non-competitive antagonist at alpha receptors by the formation of covalent bonds (it is more active at alpha-1 than alpha-2 receptors).

Ketamine is a non-competitive antagonist at NMDA receptors.

Bupropion is a dopamine uptake inhibitor used for smoking cessation, which is a non-competitive inhibitor of muscle nicotinic acetylcholine receptors.

46
Q

Examples of competitive antagonists

A

Granisetron and prazosin are competitive antagonists at 5-HT3 and alpha-1 receptors respectively.

47
Q

Drugs affected by NAT

A 
1 Isoniazid
2 Hydralazine
3 Procainamide
4 Sulfasalazine
5 Dapsone
48
Q

High Vd drugs

vd thio
trac
midaz

A

alter tissue and plasma prot bind

Propofol
flecanide
digoxin
fentanyl

low
thio 2.5l kg
trac .15l
midaz 1.5

49
Q

Heparin + atIII what type bond

A

ionic

pentansachh atract basic arginine on antiIII

50
Q

edrophonium -

type bond

where

A

hydrogen bond by hydroxyl group at esteratic site on achease

51
Q

Albumin binds

A

Predom acidic and neutral

some basic

52
Q

Do all subunit of ligan gated channel cross membrane

whats the largest group

where does thyroxine bind

What about insulin
intra /excell what does it trigger

A

Yes
gaba eg

GPRO

Thyroxine bind intracell receptor

insulin excell receptor
- binding trigger phosphorylation - Tyrosine

cholera toxin - persistent activation of GPRO stim AC (GS)

53
Q

A1
A2

B1-B3 D1

D2

A

A1 Gq
A2 Gi

B1-B3
D1 Gs

D2 Gi

Pharmacology (15 decks)

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