Analgesics
2011a(6)99a(10) Write a brief outline of the pharmacology of remifentanil
2009a(5)04a(4)01b(12)Outline the effects of an opioid injected in the intrathecal space
2006b(8)03b(5)00a(10)95b(12)Describe the pathogenesis and management of paracetamol toxicity
2006a(7)97b(15)Briefly outline the pharmacology of naloxone
2004b(4)Write short notes on tramadol
2002b(6)Write brief notes on tolerance and dependence in relation to opioid analgesics
2002a(12)Outline potential mechanisms of action of NSAIDs and potential adverse effects
2000a(15)Describe the effects of opioids on the respiratory system
1996a(11)Describe briefly the pharmacokinetics of pethidine
1999(10)remifentanil MoA: incr intra cellular ca and incr k influx. should it be Inc k efflux, and dec intracellular ca?
iza
July 6, 2010 at 6:58 pm
Iza, you are partially correct. Mu receptor activation reduce neuronal excitability by an increase in K conductance (resulting in cell hyperpolarisation), but also inhibits Ca entry leading to a decrease in intracellular Ca. Rang & Dale have a good summary of the cellular actions of opioids.
primarysaqs
July 6, 2010 at 7:27 pm
Amanda, Norpethidine is hydrolysed to norpethidinic acid, not pethidinic acid as in 1996a(11): Describe briefly the pharmacokinetics of pethidine. Cheers…
Damien
June 8, 2011 at 12:58 pm
Hi Damien
I disagree with your above comment as it has skipped a few steps.
Pethidine is actually metabolised by multiple pathways:
1. liver cytochrome oxidases to norpethidine (which is neurotoxic)
– Norpethidine is metabolised either to minor metabolites for excretion via kidneys, by liver carboxyesterase to norpethidinic acid (which is inactive), or conjugated directly for renal excretion
– Norpethidinic acid is conjugated with glucoronic acid for renal excretion
2. Liver carboxyesterase to pethidinic acid (which is inactive)
– Metabolised to either norpethidinic acid or directly conjugated for excretion by kidneys
3. Metabolised to minor metabolites which are excreted in urine
Regards,
AD
primarysaqs
June 16, 2011 at 2:32 pm
Amanda, Apologies for the brevity of my original post. I was certainly not trying to explain the entire metabolism pathway, just one minor aspect. To that end, what I have stated is the same as you have pointed out in pathway #1. That is, that norpethidine is hydrolysed (via caboxyesterase) to norpethidinic acid. I hope you agree that the correction is valid. Cheers, Damien…
Damien
June 17, 2011 at 3:37 pm