Pharma 7.2 Narcotic analgesics Flashcards Preview

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Flashcards in Pharma 7.2 Narcotic analgesics Deck (12)
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What are the 3 major groups of endogenous opioids?

Enkephalins, endorphins, dynorphins


What are the 3 classes of opioid receptor? Where are they found? Which receptor causes the majority of therapeutic effects?

MOP (Mu) - spuraspinally. Causes majority of effects.

KOP (Kappa) - spinally.

DOP (delta) - widely distributed


How do opioid receptors exert their effects?

GPCRs that increase outward flux of K, decrease influx of Ca by inhibiting ion channels, reduce cAMP synthesis that indirectly reduces influx of calcium.

All results in reduction of calcium conc which results in decreaesd release of neurotransmitter at synapse.


Name the opioids that can be considered agonists

morphine, codein, methadone


Name the opioids that can be considered partial agonists



Name the opioids that can be considered agonist/antagonist

nalbuphine - antagonist at MOP, partial agonist at KOP, and agonist at DOP.


Name the opioids that can be considered antagonist

naloxone. Used to treat OD.


Why is diamorphine much more effective than morphine?

Diamorphine is lipid soluble and therefore crosses BBB before breaking down. Also diffuses through tissues locally much more quickly.

Morphine is hydrophilic


What is the bioavailability, protein bound percentage, and half life of methadone?

Bio - 90%

Protein bound - 90%

half life - 15-30 hrs.


What ADRs are associated with opioids?

Resp depression, euphoria, constipation (mu receptors in gut inhibit motility), hypotension, vomiting, coma,


What other things can opioids be used to treat?

diarrhoea, heroin addiction, following an MI (vasodilatory and bronchodilatory effects), antitussive.