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AB 1st Year Principles > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

what is pharmacodynamics?

A

what a drug does to the body

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2
Q

what is pharmacokinetics?

A

what the body does to a drug

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3
Q

What do agonists do?

A

bind to a receptor to produce a cellular response

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4
Q

what do agonists possess?

A

affinity and efficacy

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5
Q

what do antagonists do?

A

bind to receptors and block activation by agonists

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6
Q

what do antagonists possess?

A

affinity

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7
Q

four processes that occur in drug disposition?

A

absorption
distribution
metabolism
excretion

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8
Q

what form of drug readily diffuses?

A

unionised forms

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9
Q

what is oral availability?

A

the fraction of drug that reaches the systemic circulation after oral ingestion

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10
Q

what is systemic availability?

A

this is the fraction that reaches the systemic circulation after absorption (IV drugs have 100% systemic availability)

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11
Q

factors affecting drug absorption?

A

solubility
chemical stability
lipid to water partition coefficient
degree of ionisation

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12
Q

factors affecting GI absorption?

A 
GI motility 
pH
blood flow
physicochemical interactions 
transporters present in membranes
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13
Q

when is Css (steady state concentration) reached?

A

after 5 half lives

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14
Q

what is steady state?

A

when drug administration is equal to drug elimination

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15
Q

what is a loading dose and when is it given?

A

a loading dose is an initial higher dose of a drug, given at the start of treatment so it decreases the time taken to reach steady state

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16
Q

what three reaction types occur in Phase 1 drug metabolism?

A

oxidation
reduction
hydrolysis

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17
Q

what does Phase 1 drug metabolism aim to do?

A

make the drug more polar and add a chemically reactive group, so conjugation (phase 2) can occur

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18
Q

what family of proteins mediate Phase 1 drug metabolism?

A

cytochrome P450 Monooxygenases

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19
Q

what happens in the monooxygenase P450 cycle?

A

drug (RH) enters and joins with P450
drug combines with one O of Oxygen, to produce ROH
other oxygen combines with H+ to form H20

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20
Q

what does Phase 2 drug metabolism aim to do ?

A

add an endogenous product, which is called conjugation, and inactivate the drug

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21
Q

what is glucoronidation?

A

transfer of glucoronic acid to the substrate

22
Q

what drugs can be excreted by glomerular filtration?

A

unbound drugs

23
Q

what facilitates tubular secretion?

A

organic anion transporter (against electrochemical)

organic cation transporter (with electrochem)

24
Q

in tubular secretion, what influences drug excretion?

A

concentration (pH) of urine

25
Q

what pH of urine favours excretion of acids/bases?

A

alkaline favours excretion of acids

acidic favours excretion of bases

26
Q

direction of Na concentration and electrochemical gradient

A

IN

IN

27
Q

direction of K concentration and electrochemical gradient

A

OUT

IN

28
Q

what is the equilibrium potential for EK?

A
  • 100mV
29
Q

what is the equilibrium potential for ENa?

A

+60mV

30
Q

positive feedback is shown by what channels?

A

sodium

31
Q

negative feedback is shown by what channels?

A

potassium

32
Q

what causes the refractory period?

A

Na+ channels enter a non conducting state when maintained depolarisation occurs

33
Q

where is sympathetic outflow from and what is it called?

A

T1-L2, thoracolumbar

34
Q

where is parasympathetic outflow from and what is it called?

A

CN 3, 7, 9 and 10

craniosacral

35
Q

in sympathetic, what are the two neurotransmitters and the receptors they work on?

A

acetylcholine (cholinergic)

Noradrenaline (adrenergic)

36
Q

in parasympathetic, what is the neurotransmitters and the receptors it works on?

A

acetylcholine (cholinergic)

37
Q

what type of channels are activated in effector cells, in the sympathetic? what activates them?

A

g protein coupled adrenoreceptors, noradrenaline

38
Q

what type of channels are activated in effector cells, in the parasympathetic? what activates them?

A

g protein coupled muscarinic acetylcholine receptors, acetylcholine

39
Q

in g protein coupled receptors, what does the receptor consist of?

A

7 transmembrane spans, joined by 3 extracellular and 3 intracellular loops

40
Q

in g protein coupled receptors, what does the g protein consist of?

A

alpha, beta and gamma subunits

a guanine nucleotide binding site for GTP/GDP

41
Q

how do g protein coupled receptors work?

A
  • alpha subunit binds to GDP
  • agonist binds to the receptor, causing the g protein to also
  • GDP->GTP in the guanine nucleotide binding subunit
  • g protein dissociated to alpha and beta/gamma subunits, with the alpha combining to the effector (with GTP attached)
  • this modifies the effector

TO INACTIVATE..

  • alpha subunit catalyses GTP->GDP +Pi, so the signal is turned off
  • g protein detaches from the effector and reassembles
42
Q

steps of cholinergic transmission and degradation

A
  • choline is uptaken
  • ACh is synthesised, via CAT, which is then stored in vesicles
  • depolarisation via an AP occurs
  • Ca2+ influx, causing release of ACh
  • ACh acts on receptors to cause a cellular response

degradation of ACh

  • ACh -> choline and acetate by AChE
  • choline is re uptaken and reused
43
Q

what receptors does ACh act on?

A

nicotinic ACh receptors (ligand gated ion channels)

g protein couples muscarinic ACh receptors

44
Q

3 types of g protein couples muscarinic ACh receptors and their effects

A

M1 Gq - stimulation of phospholipase C, causes increased acid secretion in the stomach

M2 Gi - inhibits adenylyl cyclase, decreases HR

M3 Gq - stimulation of phospholipase C, relaxes vascular smooth muscle and increases saliva production

45
Q

steps of noradrenergic transmission and degradation

A
  • synthesis of NA and storage in vesicles
  • depolarisation via an AP
  • Ca2+ influx, which causes release of NA
  • activation of G protein couples adrenoreceptors
  • reuptake of NA
46
Q

in presynaptic, what happens to NA?

A

U1 uptakes it

metabolised to MAO

47
Q

in postsynaptic, what happens to NA?

A

U2 uptakes it

metabolised to COMT

48
Q

4 types of G protein coupled adrenoreceptors and their effects

A

beta 1 Gs - stimulates adenylyl cyclase, increases HR and force

beta 2 Gs - stimulates adenylyl cyclase, relaxes bronchial and vascular smooth muscle

alpha 1 Gq - stimulates phospholipase C, contracts vascular smooth muscle

alpha 2 Gi - inhibits adenylyl cyclase, inhibits NA release

49
Q

what do presynaptic autoreceptors do?

A

act as a negative feedback system
increased neurotransmitter in the synaptic cleft is sensed by autoreceptors
they halt Ca2+ influx into the cell

50
Q

effects of agonist and antagonist on function of presynaptic autoreceptors?

A

agonist decrease release by autoreceptor (more neurotransmitter)
antagonist increase release by autoreceptor (less neurotransmitter)

AB 1st Year Principles (8 decks)

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