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Criado por Bhavi Mistry
mais de 11 anos atrás
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Questão | Responda |
K (KOPr) | Therapeutic effect: Analgesia Abuse: Dysphoria/hallucinations Side effects: Diuresis |
d (DOPr) | Therapeutic effect: Analgesia Side effect: Antidepressant + proconvulsant |
M (MOPr) | Therapeutic effect: Analgesia Abuse: Euphoria (due to inhibition of gabaergic inhibitory interneuron) Side effect: Respiratory depression + constipation |
Analgesia | + of GIRK -> -ve inside cell, - pain info (-) voltage gated ca2+ channels |
Physical dependence | (-) AC |
Which G proteins are opiod receptors coupled to? | Gi/Go beta-gamma/ alpha subunits mediate the effects of analgesia and physical dependence |
Physical dependence | Withdrawal syndrome of physical signs and symptoms |
Psychological dependence | Compulsive drug seeking behavior |
Euphoria and drowsiness | Disinhibition in the VTA --> increased DA in the Nucleus Accumbens |
Respiratory depression | Decreased brain sensitivity to PaCO2 |
Nausea | + of CTZ in brain stem |
Miosis | + CN3 PSNS |
Morphine | M agonist |
Heroin | M agonist 3 ester groups, easily x BBB but has decreased receptor binding |
Codeine | MeO group -> decreases effectiveness |
Pentacozine | M/K agonist |
Tramadol | Weak M agonist |
Naloxone | M, d, K opioid antagonist |
Carbamazepine | anti-epileptic Severe pain |
Gabapentine | Anti-epileptic Severe pain |
Amytryptyline | Antidepressant Severe pain |
Problems with opioids as analgesics | Side effects Break through pain Neuropathic pains |
Therapeutic uses of opioids | Pain relief Severe diarrhoea Cough suppression |
Consequences of MR + | inhibition of neuronal firing (increased potassium conductance) Decreased transmitter release (inhibition of Voltage gated Ca2+ ch) Dis inhibition |
Sites of action | Peripheral sensory nerves Spinal cord (dorsal horn) Supra spinal sites (activation of descending inhibitory pathways) |
Supraspinal sites of action | PAG RVM (Midline raphe nuclie) |
Review | endogenous opioid peptides |
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