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Year 2 Revision > Pharm revision 2 > Flashcards

Pharm revision 2 Flashcards

1
Q

two common features of GAs

A

loss of consciousness

suppression of reflex responses

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2
Q

Inhalation

A

NO
Diethyl ether
halothane
enflurane

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3
Q

IV GA

A

propofol

etomidate

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4
Q

GABAa units important in anaesthetics

A

Beta 3 = supression of reflex in IV
alpha 5 = amnesia in IV
alpha 1 = suppression of reflex inhalational

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5
Q

what other targets do inhalational GAs have

A

block NMDA type glutamate
neural nicotinic ACh receptors
TREK background leak potassium channels

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6
Q

2 parts of LA

A

aromatic and basic amine side chain

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7
Q

general characteristics of LA’s

A

do not influence resting membrane potential
selectively block small diameter and non-myelinated
weak bases

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8
Q

spinal vs epidural anaesthesia

A

spinal - sub arachnoid space

epidural = epidural space

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9
Q

lidocaine CNS effects

A

stimulation
restlessness
confusion
tremor

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10
Q

M1/M3 receptors are

A

Gq IP3 DAG linked

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11
Q

M2 receptors are

A

Gi cAMP linked

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12
Q

nAchR muscle vs ganglion

A

alpha alpha beta delta gamma

alpha x 2 beta x 3

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13
Q

pilocarpine and glaucoma

A

constriction of pupil leads to drainage via canals of schlemm

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14
Q

how do muscarinic agonists affect vasculature

A

vasc endothelial cells to make NO via M3

induces smooth muscle relaxation

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15
Q

what type of drug are bethanecol and pilocarpine

A

choline esters

alkaloids

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16
Q

pilocarpine and bethanecol side effects

A 
blurred vision
sweating
GI pain
hypotension
resp distress
bradycardia
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17
Q

cholinesterase inhibitors dosage effects

A

low dose = muscarinic inc
moderate = inc at all autonomic ganglia also
high = depolarising block at autonomic and NMJs

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18
Q

CNS effects of non polar anticholinesterases and eg

A

physostigmine

excitation but then unconsciousness, resp depression death

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19
Q

how to treat anticholinesterase poisioning when does it happen

A

organophosphate
atropine iv
pralidoxime iv

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20
Q

dual action of ganglion blocking drug and problem

A

ion channel and receptor blocker

use dependent

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21
Q

when is trimetaphan used

A

hypotension during surgery bc just blocks receptor

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22
Q

cns effects of atropine and hyoscine

A

mild restless and agitation

cns depression or paradoxical excitation

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23
Q

tropicamide moa and use

A

machr antag

mydriasis retina examination

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24
Q

machr antag and parkinsons

A

block M4 leads to dec inhibition of dopamine neurones

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25
Q

machr antag and asthma

A

ipratropium blocks bronchoconstriction

cant get into systemic bc ionised

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26
Q

side effects of first gen antipsychotics

A

EPS

chlorpromazine has anticholinergic more

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27
Q

clozapine

A 
5ht2a antag
resistant and negative
neutropenia
agrnaulocytosis 
myocarditis
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28
Q

quetiapine

A

H1 antag

less eps

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29
Q

aripiprazole

A

partial agonist d2 5ht1a

less side effects but no more efficacious

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30
Q

depression symptoms

A 
misery
low self esteem
loss of motivation
anhedonia
slowing of thought and action
loss of libido
loss of appetite
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31
Q

unipolar depression reactive vs endogenous

A

stressful life event non familial
unrelated to external stress
familial

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32
Q

TCAs MOA

A

neuronal monoamine re-uptake inhibitors

also affect on alpha 2 , muscarinic, histamin, serotonin

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33
Q

antidepressants delayed effects

A

beta

5ht2a

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34
Q

TCA PK

A

highly PPB

hepatic metabolism into active metabolites

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35
Q

TCA unwanted

A 
atropine like
postural hypotension
sedation due to h1
Acute toxicity = excitement delirum, coma resp depression
CVS dysrhythmias and VF
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36
Q

TCA interactions

A

aspirin, phenytoin, warfarin
Hepatic = neuroleptics and oral contracepetives due to competition
potentiation of CNS
antihypertensive

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37
Q

MAOi eg

A

phenelzine

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38
Q

MAOi unwanted

A 
atropine like but less than tca
postural hypo
sedation and seizures
weight gain
hepatotoxicity
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39
Q

MAOi interactions

A

tyramine
TCA = hypertensive
pethidine = hyperpyrexia, restlessness, coma, hypotension

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40
Q

Moclobemide

A

reversible MAO-A inhib with less drug interactions

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41
Q

SSRI interaction

A

TCA hepatic enzymes

interact with MAOis

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42
Q

SSRI unwanted

A

nausea diarrhoea insomnia loss of libido

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43
Q

Vanlafaxine

A

dose dependent reuptake inhib more ofr 5ht
2nd line for severe
SNRI

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44
Q

mirtazapine

A

alpha 2 antagonist
inc serotonin and na release
SSRI intolerant patients

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45
Q

thiopentone

A

barbiturate inducing anaesthetic

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46
Q

problems with barbiturates

A 
low safety
enzyme inducers
potentiate cns depressants
dependence
tolerance
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47
Q

3rd bdz

A

oxazepam

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48
Q

which short acting bdz can become long

A

oxazepam

49
Q

unwanted effects of bdz

A 
sedation confusion amnesia ataxia
potentiate cns depressants
less tolerance
dependence
free plasma conc inc
50
Q

zopiclone

A

short acting
acts at bdz receptors
minimal hangover but dependency problem

51
Q

what else can you give for anxiety

A

antidepressant ssri
antipsychotic quietiapine
propranalol
buspirone = 5ht1a agonist with fewer side effects

52
Q

type 1 and type 2 receptors

A

ionotropic

metabotropic

53
Q

type 2 receptor structure

A

1 subunit 7 transmembrane domains

54
Q

type 1 receptor structure

A

4/5 subunits with transmembrane alpha helices

55
Q

drug enzyme interactions

A

false transmitter
pro drug
enzyme inhibitor

56
Q

receptor reserve

A

not all receptors need to be stimulated to generate max response = sensitivity

57
Q

3 exceptions to target site rule

A

antacids
GAs reduce synaptic trasnmisison with interaction
osmotic purgatives

58
Q

2 eg of drugs that act on transport system

A

TCAs

cardiac glycosidess

59
Q

4 things that affect drug distribution

A

regional blood flow
extracellular binding
capillary permeability
localisation in tissue

60
Q

half life equation for first order kinetics

A

volume of distribution x log2 clearance

61
Q

4 ways cross lipid membrane

A

diffusion
aqueous pores
carrier molecules
pinocytosis

62
Q

reduction reactions where and why

A

GI tract

low oxygen bc reductases are bacterial enzymes

63
Q

n-oxidation

A

oxidation of nitrogen
dative covalent
amino oxide

64
Q

what does n-demethylation do

A

remove pharmacological activity

65
Q

Enzyme for n-oxidation

A

flavine containing mono oxygenase

66
Q

what molecule causes fish odour syndrome

A

trimethylamine

67
Q

p450 active site

A

porphyrin ring and ferric fe3+

68
Q

methylation effect on polarity

A

dec polarity

69
Q

where are p450 and FCMO

A

ER

70
Q

where is alcohol dehydrogenase

A

cytoplasm

71
Q

two types of reduction enzymes

A

esterases

amidases

72
Q

why is glutathion conjugation important

A

conjugated with electrophiles so they can be excreted

important so they do not cause DNA and protein damage

73
Q

glucoridination conj agent

A

UDPGA

74
Q

PAPS =

A

3 phosphoadenosine 5 phosphosulphate

75
Q

properties of sulphation

A

v polar and water soluble

76
Q

intermediate for methylation

A

s-adenosyl methionine

77
Q

what is glutathione

A

glycine
glutamine
cysteine

78
Q

oxidation cycle p450

A

nadph gives electron to make fe2+ from fe3+
oxygen binds and takes electron so you have unstable oxygen and fe3+
nadph another electron to make more unstable oxygen
drug becomes OH, oxygen + protons -> water

79
Q

N-demthylation

A

oxidation of methyl group in a nitrogen

makes formaldehyde HCHP

80
Q

o- demythylation

A

oxidative attack of p450 on methyl group attached to oxygen to make formaledehyfe HCHO

81
Q

adrenaline clinical uses

A 
asthma emergencies
acute bronchospasm 
cardiogenic shock
spinal anaesthesia
local
anaphylaxis
82
Q

adrenaline unwanted actions

A 
tachy
arrhythmias
cold extremeites
htn
pulmonary oedema cerebral haemmorhage
83
Q

phenylepinephrine pk

A

resistant to comt

84
Q

SS in glaucoma

A

alpha 2 dec humour formation
alpha 1 = vasoconstrcition
beta blockers = less b1 bicarb production needed to make aqueous humour

85
Q

isoprenaline

A 
beta agonist 
resistant to MAO and uptake 1 
cardiogenic shock 
acute HF
MI
86
Q

salbutamol pk

A

resistant to mao and comt

87
Q

salbutamol other use

A

threatened premature labour

88
Q

beta agonist side effects

A

reflex tachy
tremor
blood sugar dysregulation

89
Q

beta blocker uses

A

arrhythmias
hypertension
angina
glaucoma

90
Q

methyldopa

A

alpha methyl NA which competes with NA
not broken down
alpha 2 agonist

91
Q

angina types

A 
stable = pain on exertion
unstable = pain with less and less exertion
variable = occurs at rest caused by coronary
92
Q

ethosuximide

A

t-type calcium antagonists
reduces activity in thalamic neurones
absence

93
Q

levetiracetam

A

SV2a preventing glutamate release

myoclonic

94
Q

topoiramate

A

NMDA and Kainate

partial

95
Q

diazepam

A

inc gaba inhibtion

status epilepticus

96
Q

sodium valproate

A

inhibits gaba transaminase

inc gaba mediated inhibition

97
Q

what gives opioids their analgesia effects

A

tertiary nitrogen

98
Q

why is codeine a prodrug

A

no hydroxyl group at position 3 so cant bind

99
Q

opioids PK

A

weak base
absorbed in small intestine
ionised in blood

100
Q

morphine metabolism

A

morphine 6 glucuronide is a agonist too

less side effects

101
Q

codeine metabolism

A

2d6 slow but makes in into morphine

3a4 fast and deactivates

102
Q

what do opioids do centrally

A

hyperpolarisation
dec calcium in
dec AC

103
Q

where does nrpg affect

A

nrm

104
Q

where do opioids act in pain pathway

A

NRPG
PAG
Dorsal horn

105
Q

how do opioids have anti tussive

A

inc serotonin which depresses inspiratory neurones

inhibit cholinergic contraction of smooth muscle

106
Q

opioids and respiratory depression

A

prebotzinger complex

chemoreceptors

107
Q

opioids and nv

A

activate ctz

108
Q

opioid tolerance due to

A

tissue tolerance and receptor internalization

109
Q

opioid antagonists

A

naloxone

110
Q

why does opioids cause hypotension

A

histamine release

111
Q

Pathophys parkinsons

A

lewy bodies in cell bodies
neurites in acons
abnormally phosphorylated neurofilaments ubiquitin and alpha synuclein

112
Q

another dopa decarboxylase inhib

A

benserazide

113
Q

comt inhibitors

A

entacapone

tolcapone

114
Q

Dopamine receptor agonists for parkinsons

A

ergot = bromocriptine and pergolide
cardiac fibrosis
non-ergot = ropinirol = extended release and aptch
MAOb inhibi = selegiline reduces dosage l dopa required

115
Q

parkinsons ANS

A

olfactory
orthostatic hypotension
constipation

116
Q

parkinsons neuropsych

A

slee
memory
depression
irritabiility

117
Q

inflammation hypothesis

A

microglia inc release of inflammatory mediators and cytotoxic proteins
inc phagocytosis
dec neuroprotective

118
Q

3 anticholinesterases for alzheimers

A

donepezil = reversible
rivastigmine = pseudoreversible ache bche
transdermal patch
galantamine = reversible but also alpha 7 nachr

119
Q

nmda blockers

A

memantine use dependente

Year 2 Revision (22 decks)

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