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GI drugs > pain management > Flashcards

pain management Flashcards

1
Q

what is codeine

A

opiate receptor agonist

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2
Q

what is codeine converted to

A

morphine

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3
Q

describe the production of cAMP

A

opiate receptors are coupled with G-protein receptors, which activate adenylate cyclase and the production of cAMP

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4
Q

how does codein reduce the cAMP

A

inhibiting adenylate cyclase

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5
Q

what does codeine reducing cAMP do

A

stops release of the nociceptive neurotransmitters

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6
Q

nociceptive neurotransmitters names

A

substance P, GABA, dopamine, acetylcholine and noradrenaline

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7
Q

nociceptive hormones

A

vasopressin, somatostatin, insulin and glucagon

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8
Q

codeine and calcium channels explain

A

close N-type voltage-operated calcium channels and open calcium-dependent inwardly rectifying potassium channels

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9
Q

what does codeines affect on calcium channels do the the cell

A

hyperpolarise

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10
Q

what does codeine causing hyperpolarisation mean

A

reduced neuronal excitability

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11
Q

tramadol is what antagonist

A

OP3-receptor agonists

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12
Q

how does tramadol work

A

binds μ-opioid receptors and weak inhibition of reuptake of norepinephrine and serotonin in the CNS

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13
Q

diamorphine class

A

mu-opioid agonist

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14
Q

dimorphine reduces the production of what

A

endogenous opioids

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15
Q

why is diamorphine converted

A

converted into morphine to cross BBB

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16
Q

side effect of mrophine

A

respiratory depression

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17
Q

why do you get respiratory depression with morphine

A

reduction in the responsiveness of the brain stem to CO2

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18
Q

what does morphine inhibit

A

GABA inhibitory interneurons

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19
Q

what is fentanyl

A

opioid analgesic

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20
Q

what are opiod receptors coupled with

A

G-protein receptors

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21
Q

fentanyl decreases

A

intracellular cAMP

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22
Q

codein strong or weak opiod

A

weak

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23
Q

what are mu receptors couples with

A

G protein

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24
Q

codein action

A

weak agonist

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25
Q

codein closes which channels

A

N-type voltage-dependent calcium channels

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26
Q

codein opens which channels

A

calcium-dependent inwardly rectifying potassium channels

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27
Q

over all aim of codeine

A

Membrane hyperpolarisation, preventing release of substance P and glutamte, blocking the pain signal and reducing neuronal excitability

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28
Q

uses of codeine

A

cough suppression
pain
diarrhoea

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29
Q

important adverse affects of codeine

A

Respiratory depression
Hypotension
Paralytic ileus

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30
Q

what to avoid taking with codeine

A

alcohol

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31
Q

codeine at work

A

dont operate heavy machinery if drowsy

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32
Q

morphine target

A

G-protein coupled opioid ‘mu’ receptors

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33
Q

morphine action

A

full agonist

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34
Q

morphine uses

A

diarrhoea
cough in terminal
pain

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35
Q

how to reverse morphine overdose

A

naloxone

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36
Q

paracetamol class

A

analgesics, antipyretics

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37
Q

paracetamol target

A

COX 3

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38
Q

how does paracetamol stop pain

A

Inhibit synthesis of prostaglandins from arachidonic acid

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39
Q

how is paracetamol an antipyretic

A

inhibits the hypothalamic heat-regulation center

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40
Q

uses of paracetamol

A

pain

pyrexia

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41
Q

important side effects of paracetamol

A

blood disorder

hepatotosicity

42
Q

blood disorders you can get with paracetamol

A

thrombocytopenia, leucopenia, neutropenia

43
Q

what to do in paracetamol overdose

A

give N-acetyl-cysteine

44
Q

is paracetamol an NSAID

A

nah

45
Q

when can you not use NSAIDs where you might need paracetamol

A

peptic ulcer

46
Q

ibuprofen target

A

cox 1 and 2

47
Q

what does ibuprofen stop the conversion of

A

arachidonic acid to prostaglandins and thromboxanes

48
Q

what are thromboxanes responsible for

A

vasodilatation, oedema

49
Q

why are selective cox 2 useful

A

lower chance of GI ulcer

50
Q

e.g. of cox 2 selective

A

celecoxib, etoricoxib

51
Q

what are the negatives of the coxibs

A

thrombotic events

52
Q

important NSAID side effects

A

Gastric irritation, ulceration and bleeding
Compromised renal blood flow, renal impairment
Increased cardiovascular risk
Bronchospasm

53
Q

why cant you take NSAIDs with warfarin

A

enhances anticoagulation

54
Q

why cant you take NSAIDs with lithium

A

increased risk of lithium toxicity

55
Q

why cant you take NSAIDs with antidepressants

A

increased risk of bleeding

56
Q

what is ibuprofen

A

reversible inhibitor of the COX enzyme

57
Q

what part of the body does ibuprofen act on to control fever

A

hypothalamus

58
Q

Amitriptyline drug class

A

TCA

59
Q

Amitriptyline target

A

Noradrenaline and serotonin reuptake transporters on the pre-synaptic neuronal membrane

60
Q

Amitriptyline action

A

inhibitor

61
Q

what does amitriptyline prevent

A

Prevent re-uptake and subsequent degradation of the monoamine neurotransmitters serotonin and noradrenaline from the synaptic cleft

62
Q

Amitriptyline overall effect

A

Prolonged presence of serotonin and noradrenaline in the synaptic cleft leads to prolonged neuronal activity

63
Q

Amitriptyline uses

A

Depression
Neuralgia
Migrane prophylaxis (unlicensed)

64
Q

Amitriptyline use in children

A

Nocturnal enuresis in children

65
Q

common side effects of amitriptyline

A

Antimuscarinic effects
CNS side effects e.g. anxiety, dizziness, agitation, confusion
Weight gain

66
Q

Amitriptyline bad side effects

A

toxic in overdose

hyponatraemia

67
Q

why cant you take amitriptyline with MAOI

A

risk of hypertensive crisis and hyperthermia

68
Q

antimuscarinic side effects of amitriptyline

A

dry mouth, blurred vision, constipation, urinary retention

69
Q

why cant you take amitriptyline with antiepileptics

A

seizure threshold lowered

70
Q

why cant you take amitriptyline with anti-arrhythmics

A

increased risk of ventricular arrhythmias

71
Q

what is amitriptyline essentially

A

Noradrenaline/5HT reuptake inhibitor

Amitriptyline, is a sedating antidepressant, and so can ai

72
Q

what part of anxiety can amitriptyline help with specifically

A

sleep as it is a sedative

73
Q

Carbamazepine class

A

Antiepileptics

74
Q

carbamazepine class

A

Voltage-gated sodium channels

75
Q

carbamazepine and channels

A

Slows recovery of the voltage-gated sodium channels, opens potassium channels

76
Q

carbamazepine and GABA

A

promotes GABA release

77
Q

carbamazepine effect of the channels disruption

A

reduces excitability/blocks excitation of neurones that are firing repeatedly

78
Q

carbamazepine uses

A

Epilepsy
Trigeminal neuralgia
Prophylaxis of bipolar disorder

79
Q

carbamazepine common side effects

A

Ataxia
Hyponatraemia
drowsy

80
Q

carbamazepine important side effects

A

Cardiac condution disturbances
Leucopenia - bone marrow failure
Stevens-Johnson syndrome

81
Q

who to avoid giving carbamazepine in

A

people susceptible to angle-closure glaucoma
patients with AV conduction abnormalities
history of bone marrow depression
acute porphyria

82
Q

why not to use carbamazepine with warfarin

A

reduced anticoagulation

83
Q

why not to use carbamazepine with Antipsychotics

A

impaired anticonvulsant effect

84
Q

carbamazepine and women

A

use contraceptive

85
Q

what is carbamazapine

A

anticonvulsants - inhibits sodium channels

86
Q

pregabalin drug class

A

Antiepileptics

87
Q

pregabalin is an analogue of what

A

GABA

88
Q

pregabalin binds to

A

alpha2-delta protein

89
Q

what is pregabalin

A

an auxiliary subunit of the voltage-gated calcium channels

90
Q

pregabalin uses

A

Partial seizures
Neuropathic pain
Generalised anxiety disorders

91
Q

common side effects of pregabalin

A

Weight gain

Visual disturbances

92
Q

pregabalin important side effects

A

Hypertension

Leucopenia

93
Q

why cant you take pregabalin and opiates

A

CNS depression

94
Q

why cant you take pregabalin and antacids

A

reduced bioavailability of gabapentin

95
Q

what is alpha2-delta protein

A

auxiliary subunit of the voltage-gated calcium channels

96
Q

Capsaicin used as

A

topical analgesic

97
Q

Capsaicin treats

A

neuropathic pain

98
Q

Capsaicin receptor and action

A

TRPV1 receptor agonist

99
Q

Capsaicin aim

A

to reduce the amount of substance P associated with inflammation

100
Q

where do you find TRPV1 receptor agonist

A

A-delta and mostly C fibers

GI drugs (11 decks)

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