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13 Cards in this Set
- Front
- Back
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2 classes of analgesic agents , examples and how they differ |
Opiods eg morphine Moderate to severe pain Does not reduce inflammation Non-opiod Mild to moderate pain Reduce inflammation |
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Classes of opiod analgesics and ex |
1. Natural opiods eg morphine 2. Semi synthetics of morphine eg hydromorphone, oxymorphone 3. Syntheitic eg methadone |
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Groups of opiod compounds |
1. Agonists - pain relief eg morphine and codeine 2. Mixed agonist/antagonists - weak relief of pain and and reversal of opiod intoxication eg Pentazocine 3. Antagonists - reverse opiod intoxication eg Naloxone |
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Types of opiod receptors |
Mu, kappa , delta 7 G linked glycoproteins distributed along brain , spinal coed and digestive tract |
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How do G protein coupled receptors work? |
1. - Ca2+ channels 2. Open K+ channels 3. Decrease cAMP action = Blockage of neurotransmitter release Net hyperpolarization of neurones (More difficult to excite) |
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Endogenous opiod ligands ( Happy molecules ) |
Short opiod ligands, fnc as neurotransmitters realsed during excitement and exercise - endorphins - dynorphins - encaphalins |
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Pharmacokinetics of morphine |
- usually admin IV IM - high first pass metabolism - low bioavailability after oral admin - 6x dose of morphine oral to achieve IV effects (Overcome by chronic admin of the morphine - active metabolite) |
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Metabolism of morphine |
- glucuronic acid (morphine-6-glucuronide) |
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Effects of morphine on CNS |
- analgesia - sedation - euphoria - suppression of cough reflex - nausea and vomiting - resp depression - pupillary constriction (overdose) |
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Caution with adverse effects of morphine |
- v young and old px - px with resp disease ( asthma, bronchitis) - hypothyroidism - pregnancy - chronic liver disease - renal impairment |
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Side effects |
- nausea, vomiting , constipation - resp depression, hypotension, muscle rigidity |
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Acute opiod intoxication |
- direct resp depression and coma - Naloxone : counteract effects |
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Codeine (compare with morphine) |
- high oral effectiveness - less potent - less resp effects - used for mild pain and as a cough suppressant - usually combined with NSAIDs |
