Type of analgesics
Opioids |
NSAIDs |
Paracetamol |
Opiod = poppy |
Opioids classification (Action on Rc)
Opioid Receptor
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3 types opioid Rc μ, κ, δ
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Type of Rc GPCR
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Action of opioids 1. Close voltage gated Ca2+ in presynaptic neuron (↓ NT release). 2. Open K+ channel in postsynaptip neuron (↓ response to NT)
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Functional effect associated with Rc μ -> Respi depress, euphoria
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κ -> Hallucination, dysphoria
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δ -> less analgesic effect
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Pharmacological effect
Respi depression |
↓ sensitive to pCO2, pCO2↑, dilatation derebral vessel, ↑ intracranial pressure |
Euphoria |
Cough supression |
Sedation |
Miosis |
Feature drug abuse & opioid poisoning, Antidote: iv naloxone |
Histamine release |
Hypotension, bradycardia |
Smooth muscle effect (GIT, bladder, uterus |
↑ GIT tone -> Constipation, ↓ uterine tone → prolong labor |
Pharmacokinetics
Cross BBB (Liphophilic: morphine < fentanyl, methadone, heroin) |
Cross placenta |
Poor oral bioavailability |
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Opioids agonist
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Heroin & Morphine Acute MI, pulm edema, cancer
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Fentanyl Anaesthesia, Extremely potent, transdermal patch
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Pethidine labor (x ↓ uterine force, ↓ respi effect neonates)
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Methadone relieve opioid dependence
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Codeine mild pain, AE: constipation
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Dextromethorphan antitussive, cns effect
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Tramadol safe in lactation, post operative pain
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Loperamide diarrhea, neuropathic pain
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Buprenorphine partial agonist on μ
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Pentazocine rarely use dt AE
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Opioid anatagonist
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Naloxone Rapid reversal, no tolerance, no withdrawal syndrome
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Naltrexone Longer DOA
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Nalrophine causing physical dependence
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Opioids poisoning: CLinical triad
1. CNS depression |
2. Respi depression |
3. Pupil constriction |
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