48376
Description
Flashcards by Bhavi Mistry, updated more than 1 year ago
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Created by Bhavi Mistry
over 11 years ago
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| Question | Answer |
| 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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