Pharmacology Flashcards
Where can analgesics act?
Site of injury- Decrease sensitisation by decreasing prostaglandins
Block nerve conduction- Block Na channels (lidocaine)
Block synapse transmission in dorsal horn
Activate inhibitory descending path
Ion channels upregulated in nerve damage
What are the rungs of the analgesic ladder?
NSAIDs/paracetamol
Weak opioid
Strong opioid
Give some examples of NSAIDs
Aspirin
Diclofenac
Ibruprofen
Give some examples of weak opioids
Codeine
Tramadol
Give some examples of strong opioids
Morphine
Oxycodone
Whats the difference between opiates and opioids?
Opiates- Substances from or structurally similar to opium.
Opioids- Anything acting on opioid receptors
What are endogenous opioids called?
Enkephalins
How does the body naturally modulate nociception?
Descending pathways from the brainstem (Supraspinal Antinociception)
Where does the Supraspinal Antinociception system arise?
Periaqueductal grey (midbrain)
Where does the supraspinal antinociception system ultimately project to?
Spinal cord
Where does the PAG project to?
Locus ceruleus (pons) Nucleus raphe magnus (medulla)
What activates the PAG?
Opioids and electrical input
What does activation of nucleus raphe magnus do?
Release 5-HT (serotonin) and enkephalins onto dorsal horn to modulate nociception.
What chemical can activate the NRM?
Opioids (morphine)
What does activation of the locus ceruleus do?
Release NA onto dorsal horn to modulate nociception.
What kind of receptors are opioid receptors?
GCPR
What kind of GCPR are opioid receptors?
Gi/o
What does activation of GCPR do?
Inhibit presynaptic VGCC channel opening (By SU. Block vesicle release).
Open postsynaptic K+ channels to hyperpol (By SU)
Inhibit adenylate cyclase (a SU. Needed for long term effects)
What are the three main categories of opioid receptor?
Mu- Main but lots of side effects
Delta
Kappa
What are some side effects of opioids?
Addiction Resp depression Constapation N+V Orthostatic hypotension Confusion Hallucinations
Name six key opioid R agonists
Mrorphine Diamorphine Codeine Fentanyl Tramadol Methadone
How can morphine be given?
IV
Oral
IM
Subcut