Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Metabolism

A

Ph 1 Red/ox/hydrol
Cyt p450

Inducers
Rifampicin

Inhib
Cimitideine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Excretion

A

Change urinary ph

Sod bic - aspirin increase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is Cytp450

A 
Family protein in Sm ER heaptocytes
Mediate Red/Ox
Isoform enzyme
7  most improtant in metab
CYP3A4 - most
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Induce cyp450

A 
Barbiturates
Phenytoin
Carbamazepine
griseofulvin
rifampicin

Chronic alcohol

Polycyclic hrdyocarb - tobacco . meats
Brocolli - 1 form

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Summation

A

Action drugs additive

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Synergism

A

Combined action 2 drugs greater than summation

Sulphonamide & Trimethoprim

Bacteristitc alone
together bactericidal

clonidie & opiate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Potentiation

A

1 drugh increases effect of other

NDMR - from Mag

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Isobolgram

A

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

Draw from pg158

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Affinity

A

How avidly a drug binds to receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Intrinsic activity

A

‘efficacy’

Magnitude of effect drug produces after bound to receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Potency

A

Measure quanitiy drug needed to produce max effect

Large dose - not potent - small dose - max effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Agonist

A

Signifcant affinity for receptor & full intrinsic activity

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Inverse agonist

A

Significant affinity & intrisnce activty - opposit effect to endog agonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
Curve drug lower potenc
right shift in curve - max reponse save - height identical (higher conc reqd to prod response)
26
Right shjift of curve
Competive antag gven - higher conc reqired
27
Curve w/ non competitive antagonist
Move ro right max reponse recued - increase dose will not overcome
28
Parttial agonist -
no shift - impossible elicit max response heigh samller = pg 163
29
Dose ratio
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
Isomerism
Chemical compound same molecular formuale & weight but diff structural arrangement Diff phys / chem prop
31
Sreuctural isomers
Identical chemical formulae - diff arrangement bond -= diff structure wide range between sim effect to diff Chain Position Dynamic - tautomerism
32
Stereoisomers
Same atoms & same bond structure Diff 3d config Optical geomeric
33
chain isomers
Carbon chain alter - fnctiongroup same | butane & isobtene examples
34
Position isomers
Same structure - function group different Isoflurane + enflurane
35
Dynamic structural isomer
'tautomerism' Molecule exist two diff form depend physical environment midaz ion @ ph4 Change structure - at phys pH - lipid soluble - 7 ember uni ring
36
Geometric isomers
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
Optical isomers
mirror image that are not superimposable at least 1 chiral centre
38
What is a chiral centre
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
Optical stereoisomers
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
Nming steroeoisomer
Atom lower number - oserver other thre lie on plane - number identifiy - descend clockwise - rectus anti clockcwise - sinister - S
41
Racemic mix
Equal prop of different enationmers Volatile (not sevo) Equal prop of two enant - 1 may ber reponsi side effect other confer activity
42
Enatiopure
Only one enantiomer S - better PK ^ PD than R S bupiv, ropib, ketamine - side effect profile better
43
Diastereoismers
>1 chiral centre - mutliple steroisomer - not mirror images there not enatiomers Trac - 4 chiral
44
Physiolog enantiomers
Signle isomers - enzyme produce 1 conform Carbo dextrorotary rotate to right gluc d gluc - dextrose
45
Non-competitive antagonists How Can be reversed w/ increasing the conc Give some examples x3
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
Examples of competitive antagonists
Granisetron and prazosin are competitive antagonists at 5-HT3 and alpha-1 receptors respectively.
47
Drugs affected by NAT
``` 1 Isoniazid 2 Hydralazine 3 Procainamide 4 Sulfasalazine 5 Dapsone ```
48
High Vd drugs vd thio trac midaz
alter tissue and plasma prot bind Propofol flecanide digoxin fentanyl low thio 2.5l kg trac .15l midaz 1.5
49
Heparin + atIII what type bond
ionic | pentansachh atract basic arginine on antiIII
50
edrophonium - type bond where
hydrogen bond by hydroxyl group at esteratic site on achease
51
Albumin binds
Predom acidic and neutral | some basic
52
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
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
A1 A2 B1-B3 D1 D2
A1 Gq A2 Gi B1-B3 D1 Gs D2 Gi

Pharmacology (15 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions