Pharmacology of Pain Flashcards

1
Q

Opioids

A

Diversity of opioid peptides- Enkephalins, dynorphins, beta-endorphin
Peptides derived from large molecular weight precursors
–> enkephalins from proenkephalin
Peptides are targets for peptidases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Endogenous opioid systems

A

Proopiomelanocortin-derived
Proenkephalin-derived
Prodynorphin-derived

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Opioid receptors

A
Mu- 1,2,3
Delta- 1,2
Kappa- 1,2,3
Nociceptin/orphanin
Opioid receptors are widespread
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Morphine MOA

A

Attaches to receptor in cell
Activation of potassium conductance and decreased calcium conductance
Ca2+ entry blocked
–> decreased excitability + decreased release of neurotransmitters

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Effects mediated by main opioid receptors

A
Analgesia
Resp. depression
Pupillary constriction
Reduced GI motility
Sedation
Euphoria
Dysphoria
Dependence
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Types of opioid

A
Codeine
Methadone
Morphine
Oxycodone
Tramadol
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Effects of opioids- CNS

A
Analgesia
Resp. depression
Drowsiness
Euphoria
Miosis
Nausea + vomiting
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Effects of opioids- CV system

A

Hypotension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Effects of opioids- GI

A

Delayed gastric emptying

Decreased biliary and pancreatic secretions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Other Effects of opioids

A

Urinary urgency

Itching

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Morphine

A

M6G active metabolite

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Heroin

A

High solubility compared to morphine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Dextromoramide

A

Active sublingually

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Meptazinol

A

Less resp. depression

Mu 1 receptor agonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Warnings of opioid use

A

Resp. depression
Toxicity
Accumulation of methadone
Accumulation of M6G if renal function impaired

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Opioid tolerance

A

Depends on genetic background + ethnicity

Can switch opioids when patients become tolerant to particular opioid drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Analgesic ladder

A
1= non-opioids + adjuvant drugs
2= moderate efficacy opioids, non-opioids and adjuvant drugs
3= high-efficacy opioids, non-opioids and adjuvant drugs
18
Q

Paracetamol

A
Reduced active oxidised form of COX2
Modulates endogenous cannabinoid system
Analgesic
Antipyretic
Little anti-inflammatory
19
Q

Aspirin

A

COX1 and COX2 inhibitor
Analgesic
Antipyretic
Anti-inflammatory

20
Q

Ibuprofen, diclofenac, ketoprofen

A

COX1 and COX2 inhibition

Analgesic and anti-inflammatory

21
Q

Rofecoxib

A

Selective COX2 inhibitor

22
Q

NSAID indications

A
RA
OA
Dysmenorrhea
Gout
Muscle spasm
23
Q

NSAID SE

A

Nausea

GI bleeding

24
Q

NSAID Combinations

A

Codeine/paracetamol

Dihydrocodeine/paracetamol

25
Q

Anticonvulsants

A

Cabamazepine, sodium valproate, pregabalin
Neuropathic pain
Trigeminal neuralgia

26
Q

Carbamazepine MOA

A

Acts on Na channels

27
Q

Na Valproate MOA

A

Acts on Na channels

28
Q

Pregabalin

A

Acts on alpha 2 delta subunit on Ca channels

29
Q

Tricyclic antidepressants

A
Inhibit reuptake of amines
Block Na and Ca channels
Amitriptyline
Neuropathic pain
Cancer pain
30
Q

Migraine pain

A

Triptans

Ergotamine derivatives

31
Q

Antidepressants

A

TCA

SSRI

32
Q

Anticonvulsants

A

Na channels

33
Q

Calcium channel ligands

A

Gabapentin
Pregabalin
Verapamil

34
Q

Vanilloid receptors

A

TRPV family ligands

Capsaicin

35
Q

NMDA glutamate receptors

A

Ketamine

Dextromethorphan

36
Q

GABA receptor agonists

A

Baclofen

37
Q

Local anaesthetics

A

Lignocaine, bupivacaine, prilocaine
Block Na channels
Surface, infiltration, epidural
Risk of systemic toxicity - hypotension, resp. depression, bradycardia

38
Q

Inhalational general anaesthetics

A
Halothane
NO
Xenon
Isoflurane
Enflurane
39
Q

IV general anaesthetics

A

Propofol
Thiopental
Ketamine

40
Q

Trigeminal neuralgia

A
Most common facial pain syndrome
Tic douloureux
Sudden, paroxysmal attacks of pain
Commonly unilateral
Cheekbone, nose, upper lip + teeth
41
Q

Trigeminal neuralgia cause

A

Compression
Distortion
Stretching of V nerve root fibres by branch of AICA or PICA

42
Q

Trigeminal neuralgia treatment

A

Carbamazepine
Baclofen
Valproate
Clonazepam