Nervous System Pharmacology 💊 Flashcards
What type of pain is transmitted via myelinated Ad fibres?
Sharp, well-localised pain
What type of pain is transmitted via non-myelinated C fibres?
Dull, diffuse, burning pain
What are the actions of stimulating opioid receptors?
Hyperpolarisation by potassium efflux, inhibit transmitter release, inhibit adenylyl cyclise so reduce cAMP production
What are some side effects of morphine?
Respiratory depression, nausea and vomiting, constipation
What structure in the nervous system help modulate pain peripherally and centrally?
Peripherally- substantia gelatinosa
Centrally- peri aqueductal grey
What are some endogenous opioids?
Enkephalins, endorphins, dynorphins
What type of receptors are opioid receptors?
G-protein coupled receptors
What are two common mechanisms of opioid tolerance?
1- phosphorylation and uncoupling, 2- cAMP production
What is morphine’s bioavailability like orally?
Poor
Can morphine easily cross the blood-brain barrier?
No it struggles to cross BBB
What are the metabolites of morphine formed from glucoronidation in the liver, which exerts therapeutic effect?
M6G- exerts therapeutic effect
M3G
How is morphine excreted?
Renally
How does fentanyl’s bioavailability compare to morphine’s?
Fentanyls is much higher
Can fentanyl cross the blood-brain barrier?
Yes- high level of CNS crossing
How is fentanyl metabolised and excreted?
Hepatic metabolism via CYP3A4
Excreted renally
How does codeine get broken down?
Codeine gets broken down into morphine via CYP2D6 enzyme
Why would you not give codeine to children under 12?
Risk of respiratory distress which is worse in children
How is buprenorphine metabolised and excreted?
Hepatic metabolism via CYP3A4
Biliary excretion
How does buprenorphine’s affinity for opioid receptors compare to that of morphine’s?
Buprenorphine has much higher affinity
What are some side effects of buprenorphine?
Respiratory depression, low BP, dizziness, nausea
What is an example of a mixed agonist-antagonist (partial agonist) of opioid receptor?
Buprenorphine
What is an example of an opioid receptor antagonist?
Naloxone
What is naloxone’s bioavailability like orally?
Very low
What is the duration of action of naloxone?
30-60mins