Pharmacology of pain Flashcards
What receptors are typically found on a C-fibre terminal?
NMDA receptors
u-, delta-, kappa- opioid receptors
EP (Prostaglandin E) receptors
What receptors are typically found on a dorsal horn neurone?
Non-NMDA receptors
Neurokinin 1 receptors
NMDA receptors
u-, delta-, kappa- opioid receptors
What NT is involved with NMDA and non-NMDA receptors?
Glutamate
What are opioids? Give examples of opioid peptides.
Endogenous peptides/endorphins
Examples: enkephalins, dynorphins, beta - endorphin
Name the 3 endogenous opioid systems.
Pro-opiomelanocortin derived
Pro-enkephalin derived
Prodynorphin derived
(also the pronociceptive system - cholecystokinin)
Describe the MOA of morphine.
Morphine attaches to its receptor (receptor has G1 and AC subunits)
Attachment of morphine causes a decrease in cAMP
This blocks calcium ion entry
Attachment also causes activation of potassium conductance and decreased calcium conductance
Overall, this causes a decrease in intracellular calcium
A decrease in intracellular calcium resulting in reduced excitability and reduced release of neurotransmitter
Give examples of opioid drugs.
Morphine Pentazocine Pethidine Fentanyl Methadone Sufentanil
What are the effects of activating mu opioid receptors?
Analgesia respiratory depression pupillary constriction reduced gut motility sedation euphoria dependence
What are the effects of activating delta opioid receptors?
spinal analgesia
respiratory depression
reduced GI motility
What are the effects of activating kappa opioid receptors?
spinal + peripheral analgesia respiratory depression reduced GI motility sedation dysphoria potentially dependence
What potential side effects are there of opioid drugs?
hypotension delayed gastric emptying reduced biliary and pancreatic secretion urinary urgency itching
Describe the different steps in the analgesic ladder.
- non-opioids and adjuvant drugs
- moderate efficacy opioids, non-opioids and adjuvants
- high efficacy opioids, non-opioids and adjuvants
Which enzyme is rofecoxib a selective inhibitor for?
COX-2
What are the indications for NSAIDs?
Rheumatoid arthritis Osteoarthritis Dysmenorrhea Gout Muscle spasm
What two drugs are often used in combination with paracetamol?
Codeine
Dihydrocodeine