Pharmacology of Pain II Flashcards
Describe mechanism of Ibuprofen, diclofenac, ketoprofen [1]
COX-1 and COX-2 inhibition plus additional mechanisms
Celecoxib is a selective COX-2 inhibitor, but has a significant risk of what? [1]
significant risk of cardiovascular events
carbamazepine, sodium valproate, pregabalin are what type of drugs? [1]
Anti-convulsant drugs
Carbamazepine, sodium valproate, pregabalin treat what type of pain? [2]
Neuropathic pain; Trigeminal neuralgia
Name a tricyclic antidepressant that is used to treaet neuropathic and cancer pain [1]
Amitriptyline
Carbamazepine and sodium valproate act on what type of channels:
Ca2+
K+
Amines
Na+
NH3
Carbamazepine and sodium valproate act on what type of channels:
Ca2+
K+
Amines
Na+
NH3
Pregabalin acts on the α2δ subunit of what type of channels
Ca2+
K+
Amines
Na+
NH3
Pregabalin acts on the α2δ subunit of what type of channels
Ca2+
K+
Amines
Na+
NH3
Explain the mechanism of action of tricylic anti-depressants [2]
Tricylic antidepressants inhibit the reuptake of amines (dopamine, norepinephrine, adrenaline, noradrenaline histamine, and serotonin) and also block sodium and calcium channels
Name a drug used to treat migraines [1]
Describe its MoA [1]
Sumatriptan: vasoconstriction of cerebral arteries reducing inflammatory response and trigeminal activation
Pain management for complex pain types
Describe MoA of ketamine [1]
NMDA glutamate receptor antagonist
Pain management for complex pain types
Name two calcium channel ligands [2]
gabapentin, pregabalin [2]
Binds α2δ 1 and 2 in voltage gated calcium channels to reduce calcium currents
Pain management for complex pain types
What is the MoA of baclofen? [1]
What type of pathologies is it used to treat? [2]
GABA receptor agonists
It’s used to relieve muscle spasms, cramping or tightness caused by conditions such as MS, cerebral palsy
Pain management for complex pain types
Describe the MoA of tramadol & tapentadol [2]
Oopioid receptors AND amine reuptake inhibition
What are the first three firstline drug classes recommended for neuropathic pain? [3]
- SNRIs (duloxetine)
- tricyclic antidepressants (amitrypyline)
- calcium channel blockers (gabapentin, pregabalin)
Local anaesthetics
Name 3 examples [3]
MoA? [1]
lignocaine, bupivacaine, prilocaine (all end in -caine)
Block Na channels
Local anaesthetics
Mode of administration? [3]
Risks of systermic toxicity include? [3]
Mode of administration: surface, infiltration, epidural
Risk of systemic toxicity: hypotension, respiratory depression, bradycardia
General anaesthetics
Mode of administration? [2]
Mechanism of action? [2]
Mode of administration: inhalational or intravenous
Mechanism of action: activation of inhibitory receptors or inhibition of excitatory receptors
What do you need to remember with general anaesthetics? [1]
Most do not act as analgesics, instead they induce a loss of conciousness
Which drug acts as a general anaesthetic AND acts as an analgesic? [1]
ketamine
Name some inhaled anaesthetics [2] and IV anaesthetics [2]
Inhaled: [end with -ane]
Halothane
Enflurane
Isoflurane
Nitrous oxide
Intravenous anaesthetics:
Propofol
Thiopental
Etomidate
Ketamine
Midazolam
Define trigeminal neuralgia [1]
is sudden, severe facial pain. It’s often described as a sharp shooting pain or like having an electric shock in the jaw, teeth or gums
What is trigeminal neuralgia caused by? [1]
Compression, distortion or stretching of the nerve V
root fibres by a branch of the anterior or posterior inferior cerebellar artery
Treatment for trigeminal neuralgia? [5]
carbamazepine (sodium channel blocker): 1st line
baclofen (GABAB agonist): 1st line if unresponsive
phenytoin (sodium channel blocker)
valproate (sodium channel blocker and other targets)
clonazepam (benzodiazepine)
