Opioid analgesia

Pregunta	Respuesta
Heroin	M agonist 3 ester groups, easily x BBB but has decreased receptor binding
Review	endogenous opioid peptides
Supraspinal sites of action	PAG RVM (Midline raphe nuclie)
Sites of action	Peripheral sensory nerves Spinal cord (dorsal horn) Supra spinal sites (activation of descending inhibitory pathways)
Consequences of MR +	inhibition of neuronal firing (increased potassium conductance) Decreased transmitter release (inhibition of Voltage gated Ca2+ ch) Dis inhibition
Therapeutic uses of opioids	Pain relief Severe diarrhoea Cough suppression
Problems with opioids as analgesics	Side effects Break through pain Neuropathic pains
Amytryptyline	Antidepressant Severe pain
Gabapentine	Anti-epileptic Severe pain
Carbamazepine	anti-epileptic Severe pain
Naloxone	M, d, K opioid antagonist
Tramadol	Weak M agonist
Pentacozine	M/K agonist
Codeine	MeO group -> decreases effectiveness
K (KOPr)	Therapeutic effect: Analgesia Abuse: Dysphoria/hallucinations Side effects: Diuresis
Morphine	M agonist
Miosis	+ CN3 PSNS
Nausea	+ of CTZ in brain stem
Respiratory depression	Decreased brain sensitivity to PaCO2
Euphoria and drowsiness	Disinhibition in the VTA --> increased DA in the Nucleus Accumbens
Psychological dependence	Compulsive drug seeking behavior
Physical dependence	Withdrawal syndrome of physical signs and symptoms
Which G proteins are opiod receptors coupled to?	Gi/Go beta-gamma/ alpha subunits mediate the effects of analgesia and physical dependence
Physical dependence	(-) AC
Analgesia	+ of GIRK -> -ve inside cell, - pain info (-) voltage gated ca2+ channels
M (MOPr)	Therapeutic effect: Analgesia Abuse: Euphoria (due to inhibition of gabaergic inhibitory interneuron) Side effect: Respiratory depression + constipation
d (DOPr)	Therapeutic effect: Analgesia Side effect: Antidepressant + proconvulsant

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	Creado por Bhavi Mistry hace más de 13 años