VALO'S ARCHIVE

Abstract

Opioids attach to receptors in the brain. Normally these opioids are the endogenous variety that are created naturally in the body. Once attached, they send signals to the brain of the "opioid effect" which blocks pain, slows breathing, and has a general calming and anti-depressing effect. The body cannot produce enough natural opioids to stop severe or chronic pain nor can it produce enough to cause an overdose. opioids can activate receptors because their chemical structure mimics that of a natural neurotransmitter. This similarity in structure "fools" receptors and allows the drugs to lock onto and activate the nerve cells. Although these drugs mimic brain chemicals, they don't activate nerve cells in the same way as a natural neurotransmitter, and they lead to abnormal messages being transmitted through the network. Opioids target the brain's reward system by flooding the circuit with dopamine. Dopamine is a neurotransmitter present in regions o...

Dr Mahesh Trivedi, Dr Shafee Shaikh, Specialist Registrars Dr Carl Gwinnutt, Consultant Department of Anaesthesia, Hope Hospital, Salford M6 8HD, UK. E mail: mptrivedi85@yahoo.com   PHARMACOKINETICS OF OPIOID AGONISTS There is substantial variability (3-5 fold) in the clinical response to opioids due to their pharmacokinetics and pharmacodynamics. Pharmacokinetic properties of the opioids commonly used in anaesthesia are displayed in table 3. Table 3: Pharmacokinetics of commonly used opioids Morphine Pethidine Fentanyl Alfentanil Remifentanil pKa 8.0 8.5 8.4 6.5 7.1 Unionised at pH 7.4 (%) 23 5 9 90 68 Plasma protein bound (%) 30 40 84 90 70 Terminal half life (hrs) 3 4 3.5 1.6 0.06 Clearance (ml/min/kg) 15-30 8-18 0.8-1.0 4-9 30-40 Volume of distribution (L/kg) 3-5 3-5 3-5 0.4-1.0 0.2-0.3 Relative lipid solubility 1 28 580 90 50 Opioids are weak bases (pKa 6.5-...

Pharmacology of Opioids Dr Mahesh Trivedi, Dr Shafee Shaikh, Specialist Registrars Dr Carl Gwinnutt, Consultant Department of Anaesthesia, Hope Hospital, Salford M6 8HD, UK. E mail: mptrivedi85@yahoo.com Before reading the tutorial try answering the following: What is an opioid and how do they work? How can opioid analgesics be classified? What are the adverse effects of opioids? Why is it useful to know the lipid solubility of an opioid? How does ionisation of opioids (at plasma pH) affects their onset of action. What are opioid antagonists, their uses and adverse effects? DEFINITIONS Opium : A mixture of alkaloids from the poppy plant- Papaver Somniferum. Opioid : Any naturally occurring, semi-synthetic or synthetic compounds that bind specifically to opioid receptors (see below) and share the properties of one or more of the naturally occurring endogenous opioids. Opiate : Any naturally occurring opioid derived from opium (eg morphine). Narcotic : ...