Pharm revision 2 Flashcards
(119 cards)
1
Q
two common features of GAs
A
loss of consciousness
suppression of reflex responses
2
Q
Inhalation
A
NO
Diethyl ether
halothane
enflurane
3
Q
IV GA
A
propofol
etomidate
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
5
Q
what other targets do inhalational GAs have
A
block NMDA type glutamate
neural nicotinic ACh receptors
TREK background leak potassium channels
6
Q
2 parts of LA
A
aromatic and basic amine side chain
7
Q
general characteristics of LA’s
A
do not influence resting membrane potential
selectively block small diameter and non-myelinated
weak bases
8
Q
spinal vs epidural anaesthesia
A
spinal - sub arachnoid space
epidural = epidural space
9
Q
lidocaine CNS effects
A
stimulation
restlessness
confusion
tremor
10
Q
M1/M3 receptors are
A
Gq IP3 DAG linked
11
Q
M2 receptors are
A
Gi cAMP linked
12
Q
nAchR muscle vs ganglion
A
alpha alpha beta delta gamma
alpha x 2 beta x 3
13
Q
pilocarpine and glaucoma
A
constriction of pupil leads to drainage via canals of schlemm
14
Q
how do muscarinic agonists affect vasculature
A
vasc endothelial cells to make NO via M3
induces smooth muscle relaxation
15
Q
what type of drug are bethanecol and pilocarpine
A
choline esters
alkaloids
16
Q
pilocarpine and bethanecol side effects
A
blurred vision sweating GI pain hypotension resp distress bradycardia
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
18
Q
CNS effects of non polar anticholinesterases and eg
A
physostigmine
excitation but then unconsciousness, resp depression death
19
Q
how to treat anticholinesterase poisioning when does it happen
A
organophosphate
atropine iv
pralidoxime iv
20
Q
dual action of ganglion blocking drug and problem
A
ion channel and receptor blocker
use dependent
21
Q
when is trimetaphan used
A
hypotension during surgery bc just blocks receptor
22
Q
cns effects of atropine and hyoscine
A
mild restless and agitation
cns depression or paradoxical excitation
23
Q
tropicamide moa and use
A
machr antag
mydriasis retina examination
24
Q
machr antag and parkinsons
A
block M4 leads to dec inhibition of dopamine neurones
25
machr antag and asthma
ipratropium blocks bronchoconstriction
| cant get into systemic bc ionised
26
side effects of first gen antipsychotics
EPS
| chlorpromazine has anticholinergic more
27
clozapine
```
5ht2a antag
resistant and negative
neutropenia
agrnaulocytosis
myocarditis
```
28
quetiapine
H1 antag
| less eps
29
aripiprazole
partial agonist d2 5ht1a
| less side effects but no more efficacious
30
depression symptoms
```
misery
low self esteem
loss of motivation
anhedonia
slowing of thought and action
loss of libido
loss of appetite
```
31
unipolar depression reactive vs endogenous
stressful life event non familial
unrelated to external stress
familial
32
TCAs MOA
neuronal monoamine re-uptake inhibitors
| also affect on alpha 2 , muscarinic, histamin, serotonin
33
antidepressants delayed effects
beta
| 5ht2a
34
TCA PK
highly PPB
| hepatic metabolism into active metabolites
35
TCA unwanted
```
atropine like
postural hypotension
sedation due to h1
Acute toxicity = excitement delirum, coma resp depression
CVS dysrhythmias and VF
```
36
TCA interactions
aspirin, phenytoin, warfarin
Hepatic = neuroleptics and oral contracepetives due to competition
potentiation of CNS
antihypertensive
37
MAOi eg
phenelzine
38
MAOi unwanted
```
atropine like but less than tca
postural hypo
sedation and seizures
weight gain
hepatotoxicity
```
39
MAOi interactions
tyramine
TCA = hypertensive
pethidine = hyperpyrexia, restlessness, coma, hypotension
40
Moclobemide
reversible MAO-A inhib with less drug interactions
41
SSRI interaction
TCA hepatic enzymes
| interact with MAOis
42
SSRI unwanted
nausea diarrhoea insomnia loss of libido
43
Vanlafaxine
dose dependent reuptake inhib more ofr 5ht
2nd line for severe
SNRI
44
mirtazapine
alpha 2 antagonist
inc serotonin and na release
SSRI intolerant patients
45
thiopentone
barbiturate inducing anaesthetic
46
problems with barbiturates
```
low safety
enzyme inducers
potentiate cns depressants
dependence
tolerance
```
47
3rd bdz
oxazepam
48
which short acting bdz can become long
oxazepam
49
unwanted effects of bdz
```
sedation confusion amnesia ataxia
potentiate cns depressants
less tolerance
dependence
free plasma conc inc
```
50
zopiclone
short acting
acts at bdz receptors
minimal hangover but dependency problem
51
what else can you give for anxiety
antidepressant ssri
antipsychotic quietiapine
propranalol
buspirone = 5ht1a agonist with fewer side effects
52
type 1 and type 2 receptors
ionotropic
| metabotropic
53
type 2 receptor structure
1 subunit 7 transmembrane domains
54
type 1 receptor structure
4/5 subunits with transmembrane alpha helices
55
drug enzyme interactions
false transmitter
pro drug
enzyme inhibitor
56
receptor reserve
not all receptors need to be stimulated to generate max response = sensitivity
57
3 exceptions to target site rule
antacids
GAs reduce synaptic trasnmisison with interaction
osmotic purgatives
58
2 eg of drugs that act on transport system
TCAs
| cardiac glycosidess
59
4 things that affect drug distribution
regional blood flow
extracellular binding
capillary permeability
localisation in tissue
60
half life equation for first order kinetics
volume of distribution x log2 clearance
61
4 ways cross lipid membrane
diffusion
aqueous pores
carrier molecules
pinocytosis
62
reduction reactions where and why
GI tract
| low oxygen bc reductases are bacterial enzymes
63
n-oxidation
oxidation of nitrogen
dative covalent
amino oxide
64
what does n-demethylation do
remove pharmacological activity
65
Enzyme for n-oxidation
flavine containing mono oxygenase
66
what molecule causes fish odour syndrome
trimethylamine
67
p450 active site
porphyrin ring and ferric fe3+
68
methylation effect on polarity
dec polarity
69
where are p450 and FCMO
ER
70
where is alcohol dehydrogenase
cytoplasm
71
two types of reduction enzymes
esterases
| amidases
72
why is glutathion conjugation important
conjugated with electrophiles so they can be excreted
| important so they do not cause DNA and protein damage
73
glucoridination conj agent
UDPGA
74
PAPS =
3 phosphoadenosine 5 phosphosulphate
75
properties of sulphation
v polar and water soluble
76
intermediate for methylation
s-adenosyl methionine
77
what is glutathione
glycine
glutamine
cysteine
78
oxidation cycle p450
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
N-demthylation
oxidation of methyl group in a nitrogen
| makes formaldehyde HCHP
80
o- demythylation
oxidative attack of p450 on methyl group attached to oxygen to make formaledehyfe HCHO
81
adrenaline clinical uses
```
asthma emergencies
acute bronchospasm
cardiogenic shock
spinal anaesthesia
local
anaphylaxis
```
82
adrenaline unwanted actions
```
tachy
arrhythmias
cold extremeites
htn
pulmonary oedema cerebral haemmorhage
```
83
phenylepinephrine pk
resistant to comt
84
SS in glaucoma
alpha 2 dec humour formation
alpha 1 = vasoconstrcition
beta blockers = less b1 bicarb production needed to make aqueous humour
85
isoprenaline
```
beta agonist
resistant to MAO and uptake 1
cardiogenic shock
acute HF
MI
```
86
salbutamol pk
resistant to mao and comt
87
salbutamol other use
threatened premature labour
88
beta agonist side effects
reflex tachy
tremor
blood sugar dysregulation
89
beta blocker uses
arrhythmias
hypertension
angina
glaucoma
90
methyldopa
alpha methyl NA which competes with NA
not broken down
alpha 2 agonist
91
angina types
```
stable = pain on exertion
unstable = pain with less and less exertion
variable = occurs at rest caused by coronary
```
92
ethosuximide
t-type calcium antagonists
reduces activity in thalamic neurones
absence
93
levetiracetam
SV2a preventing glutamate release
| myoclonic
94
topoiramate
NMDA and Kainate
| partial
95
diazepam
inc gaba inhibtion
| status epilepticus
96
sodium valproate
inhibits gaba transaminase
| inc gaba mediated inhibition
97
what gives opioids their analgesia effects
tertiary nitrogen
98
why is codeine a prodrug
no hydroxyl group at position 3 so cant bind
99
opioids PK
weak base
absorbed in small intestine
ionised in blood
100
morphine metabolism
morphine 6 glucuronide is a agonist too
| less side effects
101
codeine metabolism
2d6 slow but makes in into morphine
| 3a4 fast and deactivates
102
what do opioids do centrally
hyperpolarisation
dec calcium in
dec AC
103
where does nrpg affect
nrm
104
where do opioids act in pain pathway
NRPG
PAG
Dorsal horn
105
how do opioids have anti tussive
inc serotonin which depresses inspiratory neurones
| inhibit cholinergic contraction of smooth muscle
106
opioids and respiratory depression
prebotzinger complex
| chemoreceptors
107
opioids and nv
activate ctz
108
opioid tolerance due to
tissue tolerance and receptor internalization
109
opioid antagonists
naloxone
110
why does opioids cause hypotension
histamine release
111
Pathophys parkinsons
lewy bodies in cell bodies
neurites in acons
abnormally phosphorylated neurofilaments ubiquitin and alpha synuclein
112
another dopa decarboxylase inhib
benserazide
113
comt inhibitors
entacapone
| tolcapone
114
Dopamine receptor agonists for parkinsons
ergot = bromocriptine and pergolide
cardiac fibrosis
non-ergot = ropinirol = extended release and aptch
MAOb inhibi = selegiline reduces dosage l dopa required
115
parkinsons ANS
olfactory
orthostatic hypotension
constipation
116
parkinsons neuropsych
slee
memory
depression
irritabiility
117
inflammation hypothesis
microglia inc release of inflammatory mediators and cytotoxic proteins
inc phagocytosis
dec neuroprotective
118
3 anticholinesterases for alzheimers
donepezil = reversible
rivastigmine = pseudoreversible ache bche
transdermal patch
galantamine = reversible but also alpha 7 nachr
119
nmda blockers
memantine use dependente
