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PHAL211 > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

Efficacy

A

Ability of drug to drive a reactions response to full effect. Measured by Emax.

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2
Q

Potency

A

EC50 - concentration of drug required to produce a response

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3
Q

Affinity

A

Kd - strength of drug binding to receptor (action is longer plus higher chance of binding)

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4
Q

Orthosteric site

A

Where agonist binds

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5
Q

Endogenous ligand

A

what the ligand normally binds to

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6
Q

Agonist

A

has affinity and efficacy. Drug binds to receptor and produces a response (like endogenous ligand)

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7
Q

Partial agonist

A

binds (has affinity) but doesn’t fully activate to maximal efficacy, even at 100% occupancy (acts as antagonist)

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8
Q

Full agonist

A

Will produce full effect (at lower capacity)

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9
Q

Receptor reserve

A

irreversible antagonist act as a reversible due to not 100% binding having 100% efficacy

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10
Q

Inverse agonist

A

has negative efficacy, reduces basal activity “turns receptor off”

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11
Q

Constitutive activity

A

basal activity

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12
Q

Antagonist

A

binds to ligand but has no effect (efficacy)

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13
Q

Competitive orthosteric antagonist

A

binds reversible to orthosteric site but has no efficacy

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14
Q

Irreversible antagonist

A

reduces the maximal response of agonist by covalent bonds

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15
Q

Allosteric modulator

A

binds to a different place on receptor to the endogenous ligand and modifies response to orthosteric ligand (affinity or efficacy)

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16
Q

Allosteric vs orthosteric

A

selective, natural signalling pattern, no ceiling effect

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17
Q

Surmountable

A

action of agonist can be restored

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18
Q

Two state model

A

RR, agonist (towards R), inverse (towards R), antagonist (no change)

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19
Q

Therapeutic index

A

lethal dose 50/ED50

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20
Q

cAMP

A

PKA, ATP->ADP, Ca2+, fat and glycogen metabolism, release energy, lipolysis, decrease synthesis

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21
Q

G protein receptor kinase (GPRK) -> phosphorylation

A

= desensitisation, Arestin - binds to c terminal, blocks binding lead to invagination = tolerance

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22
Q

Nerve terminal drug targets (10)

A

Precursor transporter, neurotransmitter formation enzyme, vesicle storage, Na+ (action potential) ion channel, Ca2+ ion channel, vesicular fusion (enzymes), post synaptic receptor, pre synaptic receptor, off signal enzyme, neurotransmitter uptake transporter

23
Q

Ion channel

A

protein creates pore across cell membrane. Can be blocked or modulated.

24
Q

Ligand gated ion channel

A

receptor/protein that drug binds to. Receptor pore increases permeability.

25
Q

Voltage gated ion channel

A

response to change in membrane potential

26
Q

Carrier molecules/transporters

A

move ions/molecules across membranes. Can be normal transport, inhibited, false substrate.

27
Q

Enzymes

A

biological catalysts. inhibitor, false substrate or prodrug. (non-competitive/competitive)

28
Q

GPCR

A

G protein coupled receptors. (guanine nucleotide binding protein). 7 transmembrane domains, single polypeptide. intracellular c terminal. alpha, beta and gamma. binding -> GTP (alpha) -> dissociates

29
Q

Family A GPCR

A

ligand binds in transmembrane bundle (small molecule/peptide)

30
Q

Family B GPCR

A

binding in exterior N terminal (peptide hormones)

31
Q

Family C GPCR

A

large N terminals, folding pocket

32
Q

Adhesion family GPCR

A

chops off N terminal and binds ligand

33
Q

Frizzled family GPCR

A

extracellular N terminal, intracellular C terminal

34
Q

Gs

A

activates adenylate cyclase, increase cAMP

35
Q

Gi

A

inhibits adenylate cyclase, decreases cAMP

36
Q

Gq

A

activates PLC -> PIP2 -> DAG (->PKC) and IP3 (->Ca2+)

37
Q

Kinase linked/cytokine receptor

A

extracellular domain, intracellular transmembrane domain, tyrosine kinase domain. dimerisation -> autophosphorylation -> phosphorylate SH2 domains -> signalling cascade (growth hormones, cytokines, hormones)

38
Q

Kinase linked categories

A

tyrosine kinase, serine/threonine, cytokine

39
Q

Nuclear/steroid hormone receptor

A

N terminal, AF1, DNA BD, HR, LBD, C terminal, AF2. regulate CYP.

40
Q

Type one nuclear receptor

A

Steroid nuclear receptor. cytoplasm, homodimers, endocrine. Binding -> conformation change -> nucleus.

41
Q

Type two nuclear receptor

A

metabolite receptor. nucleus, heterodimers, lipids. nucleus -> binding ->conformation -> gene transcription

42
Q

Allosteric binding example

A

Benzodiazepine binding to GABAa to increase efficacy (Cl transport)

43
Q

Antagonists example

A

Propranolol (beta blocker), antihistamine

44
Q

Irreversible antagonist example

A

Novichok (Poison) - irreversible AChE inhibitor, parasympathetic then sympathetic

45
Q

Partial agonist example

A

Buprenorphine, replacement therapy for opioids

46
Q

Na+ channel inhibitor example

A

Lignocaine = local anaesthetic

47
Q

Nicotinic ion channel antagonist

A

Nicotine, pancuronium - muscle relaxant

48
Q

Prodrug

A

L-dopa - prodrug for dopamine = alzheimers (+carbidopa to inhibit metabolism in body)

49
Q

False substrate example

A

Methyl dopa - creates methyl noradrenaline a2 agonist

50
Q

Inhibits p-gp (p-glycoprotein)

A

Verapamil = increase bioavailability of drug/xenobiotics

51
Q

activates insulin receptor orthosteric site as Kinase linked receptor drug

A

Insulin

52
Q

RTK inhibition of multiple kinase linked receptors

A

Lapatinib

53
Q

Class one nuclear receptor drugs

A

Cortisol (glucocorticoid receptor), estrogen

54
Q

Class two nuclear receptor drugs

A

PPAR, cholesterol

PHAL211 (5 decks)

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