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Analgesics

Analgesics. Major Types. Nonnarcotic NSAIDS Acetaminophen Narcotic Opiates. Nonnarcotics : NSAIDS. “non-steroidal anti-inflammatory drugs” Work as analgesics, antipyretics, and anti-inflammatory agents. Different Types Salicylates : Aspirin

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Analgesics

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  1. Analgesics

  2. Major Types • Nonnarcotic • NSAIDS • Acetaminophen • Narcotic • Opiates

  3. Nonnarcotics: NSAIDS • “non-steroidal anti-inflammatory drugs” • Work as analgesics, antipyretics, and anti-inflammatory agents

  4. Different Types • Salicylates: Aspirin • Propiotic acid derivatives: Ibuprofen, Naproxen • Enolic acid derivatives (Oxicams): Piroxicam, Meloxicam • Acetic acid derivatives: Indomethacin, Diclofenac • Fenamic acid derivatives: Mefenamic Acid, Meclofenamic Acid • Selective COX-2 inhibitors: Celecoxib, Etoricoxib

  5. Pharmacodynamics • Blocks prostaglandin synthesis by nonselective inhibition of cyclooxgenase (COX-1 and COX-2) • For ASA and PAD: decrease PMN migration to site of inflammation • Pharmacokinetics • absorbed by the GI tract, metabolized in the liver, excreted in the urine • Highly protein bound • For ASA and PAD: more able to penetrate joint fluid • Varying half-lives and peaks: ibuprofen: 1 to 2 hours (half-life, 2 hours) ; naproxen: 2 to 4 hours (half-life, 14 hours); ketorprofen: 1 to 2 hours (half-life, 2 hours)

  6. Adverse Effects • GI iritation – less in COX II inhibitors • Renal Insufficiency – by decreasing prostaglandin-induced afferent arteriole vasodilation • Adverse Drug Reactions - hypersensitivity (particularly aspirin)

  7. Nonnarcotics: Acetaminophen • Analgesic and antipyretic qualities • Less protein bound • More even distributed in body fluids • Adverse effects include hepatic necrosis at very high doses, nephropathy secondary to renal papillary necrosis from deposition of p-aminophenol (from chronic use)

  8. Nonnarcotics: Dosage • Usual dosage

  9. Narcotics: Opiates • More potent analgesics for severe pain • Act largely on the CNS and GI tract • Analgesia is from decreased perception of pain, increased pain tolerance

  10. Different Types • Weak Opioid: Codeine, Tramadol • Strong opioids: buprenorphine, fentanyl, hydromorphone, methadone, morphine, Oxycodone

  11. Pharmacodynamics • Opioids bind to different opioid receptors in the CNS blocking pain signals and perception • Pharmacokinetics • Cleared by the liver • Side effects • Sedation, ventilatory depression, GI effects (constipation, nausea, vomiting), CVS effects (hypotension, vasodilation)

  12. Narcotics: Dosage

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