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Opioids
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NSAIDs
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Paracetamol
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Opiod = poppy
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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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Respi depression
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↓ sensitive to pCO2, pCO2↑, dilatation derebral vessel, ↑ intracranial pressure
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Euphoria
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Cough supression
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Sedation
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Miosis
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Feature drug abuse & opioid poisoning, Antidote: iv naloxone
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Histamine release
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Hypotension, bradycardia
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Smooth muscle effect (GIT, bladder, uterus
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↑ GIT tone -> Constipation, ↓ uterine tone → prolong labor
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Cross BBB (Liphophilic: morphine < fentanyl, methadone, heroin)
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Cross placenta
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Poor oral bioavailability
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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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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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1. CNS depression
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2. Respi depression
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3. Pupil constriction
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