ANALGESICS - OPOIDS 1 Flashcards
Analgesics may be broadly classified to two?
Opioids
Non-opioids
The opioids may be classified according to their source to
Natural opioates
Semi synthetics
Synthetics
Endogenous alkaloids
Give :
1) 2 Natural opioates
2) 5 semi synthetic opioids
3) 5 synthetic opioids
4) 3 classes of the endogenous opioid
1) Morphine and Codeine
2) Buprenorphine , Hydromorphone , Hydrocodone , Oxycodone , Oxymorphone
3) Fentanyl , Meperidine , Methadone , Tapentadol , Tramadol
4) Endogenous opioids - Endorphins , Dynorphins and Pentapeptide enkephalins
Opioids can be classified according to their chemical structure into
1) Phenanthrenes
2) Benzmorphans
3) Phenylpiperidines
4) Diphenylheptanes
5) Phenylpropylamines
BP3D
Giev examples of phenanthrenes
(All the natural and semi synthetic opioids )
Levorphanol
Nalbuphine
Butorphanol
Naloxone
Give a Diphenyl heptane
Methadone
Give 2 Phenylpropylamines
Tramadol and Tapentadol
Give 4 Phenylpiperidines
Fentanyl
Meperidine
Alfentanil
Sufentanil
Give an example of a Benzmorphan
Pentazocine
Codeine and Oxycodone are what type of agonists
Moderate
Give two types of opioids antagonists
Naloxone and Naltrexone
Give three mixed agonist antagonist opioids
NBP
Nalbuphine
Butorphanol
Pentazocine
Buprenophine is termed as
A partial agonist antagonist
All the three opioids receptors are what kind
GPCRs
Give the three types of opioid receptors
Mu , kappa and delta
All opioid receptors are which kind of GPCRs
Gi
The opioid receptors have two main MOA , Explain
1) Activation of opioid receptors decreases the Calcium influx in response to an action potential thus reduce excitatory neurotransmitter release of glutamate , Ach , NE , Seratonin from presynaptic neuron
2) Activation of the opioid receptors increases potassium efflux and decreases the response of postsynaptic neurons to excitatory neurotransmitter release
Majority of the opioid analgesics act on which receptor
Mu
Give
1) 4 strong phenanthrene agonists
2) 4 mild to moderate phenanthrene agonists
3) Opioid antagonists
Strong phenanthrene agonists
1) Morphine
2) Hydromorphone
3) Heroin
4) Oxymorphone
Mild to moderate
1) Codeine
2) hydrocodone
3) Dihydrocodeine
4) Oxycodone
Antagonists - Naloxone , Naltrecone and Nalmefene
Codeine is also known as
Methylmorphine