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Definition
Ibuprofen, Naproxen, Indomethacin and Sulindac Inhibit conversion of arachadonic acid, irreversibly inhibiting the enzyme cyclooxygenase Analgesia (ceiling effect), anti inflame action (epigastric distress), platelet function Inhibit production of the mucous layer Use PPI to precent NSAID gastric ulcer Nephrotox, increased Na and H2O retention NSAIDs block ACE inhibitors, B Blockers, Increase Warfarin anticoag |
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COX 1 inhibitor (a little COX 2 also) Pain and platelet blocking CNS- tinnitus, HSN, Uric acid excretion, Resp depression, *Reye syndrome (not for use in kids), GI symptoms |
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MOA unkown. No effects on platelets or bleeding time Hepatic metabolism, conjugated with glucuronic acid and sulfuric acid Both conjugates are excreted by the kidneys N-acetylcysteine is an antidote for acetaminophen No GI problems or DIs |
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Antidote for opioid poisoning. Short DOA Get increase of NE release centrally with opioid WD |
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Analgesic gold standard Hepatic metabolism with glucuronic acid conjugation M6G is more potent than parent compound and undergoes enter-hepatic recycling. Half life is 2-3 hrs Mets can accum in renal dx H release: urticaria, pruritis, rare asthma exacerbation |
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Morphine prodrug, crosses the BBB faster, lipid soluble Rapidly met to MAM Can cause euphoria by altering DA in the ventral segmental pathway Anticholinergics can inc risk of constipation |
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Morphine, heroin, codeine, meperidine, Methadone, oxycodone, fentanyl |
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Low potency, used for antitussive uses CYP 2D6 inhib can abolish the effects of codeine High PO/IV ratio Used for visceral pain, cough with pain |
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Not used much due to seizures and renal acc |
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NMDA antagonist High PO/IV ratio |
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Used as patch, or lollipop Potency is 60 times more than morphine DOA is 20-30 min Resp ceiling at high doses |
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CNS actions include analgesia and sedation Parenteral, nasal spray for migraines |
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Stim opiod Rs, block reuptake of 5HT3 and NE Impaired renal funct results in decreased excretion of tramadol and its active met, M1. Dose Adj < 30 CrCL Seizures in renal impaired |
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Muscle Relaxants MOA PK AE DI |
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Definition
Cyclobenzaprine (TCAs, lots SEs) Baclofen (GABA inhibit NT, spasticity from MS) Diazepam (BZ blocks spinal polysynaptic pathways) Dantrolene (direct acting skeletal muscle relax, blocks ca release from SR) - to tx MH |
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Definition
inhibit the trigeminal nerve pathway Serotonin 1B, 1D, 1F Rs Not for pregnancy, lactation, ischemic disorders, CA vasospasm, uncontrolled HTN, liver kidney dx |
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Definition
Agonist at the 5HT 1B/1D R Burning at site, flushing, drowsiness, fatigue CI'd with CAD, HTN |
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Vasoconstriction Block release of vasoactive neuropeptides Interrupt pain signal tm |
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Definition
TCAs, B Blockers, Ca Ch blockers, anti-epileptic drugs |
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Definition
Mu1- supraspinal analgesia Mu2- resp depression, CV, GI, spinal analgesia, miosis, phys dependence Delta- spinal and supraspinal Kappa- spinal, sedation, dysmorphic effects, mitosis, resp depression |
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Meperidine, methadone, morphine, fentanyl |
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Definition
morphine, meperidine, fentanyl, methodone, buprenorphine |
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Definition
Morphine, meperidine, fentanyl, methadone, Buprenorphine |
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