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Analgesic drugs (Morphine (euphoria, sedation, sleep, Free hydroxl on…
Analgesic drugs
Morphine
euphoria, sedation, sleep
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Acute + chronic pain (slow-release tabs), less useful for neuopathic
3-4h half life, metabolized in liver
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GI upset + lowered activity, antitussive, hormonal (red. LH, incr. prolactin + ADH)
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(Syn.) Methadone series
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Tramadol: codeine analogue, short half life -> post-op
S/E's: nausea, sleepy, dizzy, sweaty
Meptamizol: High efficacy partial μ, shorter onset + duration., lacks euphoria
Oral, no tolerance, extensively metabolized
Methadone: 20-24h, μ agonist
TRPV1
Phophorylation by PKC + PLC (PIP2) sensitize -> hyperalgesia, allodynia
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4 subunits, 6-membrane spanning domains
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Non-competitive antagonists block aqueous pore (more active against over-activated), S/E hyperthermia
TRP fam respond to physical, protons, natural (capsaicin) + endovanillods, change in membrane potential, IC sig. cascades
Neuropathic pain
Anaesthetics: Ketamine: NDMA antagonist reduce central sensitization, inhibits NO production
Local anaesthetic Lidocaine blocks VGNaC, increases depolariation threshold -> reduced spontaneous discharge from damaged neurons (fibromyalgia)
Gabapentin (designed as mimetic) binds to alpa2-delta subunit to modulate VGCCs, 30% metab + rest excreted - OD
Anticonvulsants Carbamazepine, lamotrigine, phenytoin stabilize inactive Na channels
Antidepressants block NA and 5-HT uptake, enhances inhibition
NSAIDs
Paracetemol -> analgesic, antipyretic, antithrombotic, but lacks anti-inflammatory effects (brain COX-headaches)
Ulceration, GI bleeds (less so but cardiac for COX-2), renal toxicity
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Thebaine series
Buprenorphine: partial μ agonist, μ, κ antagonist, highly lipophillic 25-50x morphine, combined with naloxone
Benzamorphin series
Pentazocine: weak μ, strong κ (supraspinal agonism -> dysphoria + psychotic eff.), combined with naloxone
(Syn.) Pethidine series
Pethidine: fully syn. opiod, structurally diff to morphine, metabolic toxicity convulsions. Fentanyl 100x, Sufentanyl 500-100x