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  1. Acetaminophen
    • MECHANISM: Reversibly inhibits cyclooxygenase, mostly in CNS. Inactivated peripherally.
    • CLINICAL USE: Antipyretic, analgesic, but not anti-inflammatory. Used instead of aspirin to avoid Reye syndromein children with viral infection.
    • TOXICITY: Overdose produces hepatic necrosis; acetaminophen metabolite (NAPQI) depletes glutathione and forms toxic tissue byproducts in liver. N-acetylcysteine is antidote—regenerates glutathione
  2. montelukast and zafrilukast MOA
    • inhibits LTC4, LTD4, LTE4 
    • inc bronchial tone
  3. Zileuton MOA
    • inhibits Lipoxygenase 
    • dec Leukotrienes
  4. what is Epoprostenol
    • PGI2
    • dec Plateletaggregation
    • dec Vascular tone
  5. what is Alprostadil
    • PGE1
    • dec Vascular tone
  6. what is Dinoprostone
    • PGE2
    • inc Uterine tone
  7. what is Carboprost
    • PGF2
    • inc Uterine tone
  8. TXA2 action
    • inc Platelet aggregation
    • inc Vascular tone
  9. LTB4 action
    LTB4 is a neutrophil chemotactic agent
  10. PGI2 action
    PGI2 inhibits platelet aggregation and promotesvasodilation
  11. Aspirin MOA
    Irreversibly inhibits cyclooxygenase (both COX-1 and COX-2) via acetylation, which dic synthesis of TXA2 and prostaglandins.       inc bleeding time. No effect on PT, PTT. A type of NSAID.
  12. Celecoxib MOA
    Reversibly inhibits specifically the cyclooxygenase (COX) isoform 2, which is found in inflammatory cells and vascular endothelium and mediates inflammation and pain; spares COX-1, which helps maintain gastric mucosa. Thus, does not have the corrosive effects of otherNSAIDs on the GI lining. Spares platelet function as TXA2 production is dependent on COX-1.
  13. Celecoxib toxicity
     inc risk of thrombosis. Sulfa allergy.
  14. NSAIDs
    Ibuprofen, naproxen, indomethacin, ketorolac, diclofenac
    Reversibly inhibit cyclooxygenase (both COX-1 and COX-2). Block prostaglandin synthesis.
  15. NSAID toxicity
    Interstitial nephritis, gastric ulcer (prostaglandins protect gastric mucosa), renal ischemia(prostaglandins vasodilate afferent arteriole).
  16. Bisphosphonates
    Alendronate, other -dronates.
    Pyrophosphate analogs; bind hydroxyapatite in bone, inhibiting osteoclast activity
  17. Teriparatide MOA ans Use
    • Recombinant PTH analog given subcutaneously daily. inc osteoblastic activity.
    • use: Osteoporosis. Causes  bone growth compared to antiresorptive therapies (e.g., bisphosphonates).
  18. Chronic gout drugs (preventive)
    • Allopurinol
    • Febuxostat
    • pegloticase
    • probencid
  19. Acute gout drugs
    • NSAID
    • Glucocorticoids 
    • Colchicine
  20. about TNF-α inhibitors
    All TNF-α inhibitors predispose to infection, including reactivation of latent TB, since TNF is important in granuloma formation and stabilization.
  21. Etanercept
    • Fusion protein (receptor for TNF-α + IgG1 Fc),produced by recombinant DNA. Etanercept is a TNF decoy receptor.
    • use: Rheumatoid arthritis, psoriasis, ankylosingspondylitis
  22. Infliximab,adalimumab
    • Anti-TNF-α monoclonal antibody.
    • use: Inflammatory bowel disease, rheumatoid arthritis,ankylosing spondylitis, psoriasis
  23. Glaucoma drugs goal
    dec IOP via dec amount of aqueous humor (inhibit synthesis/secretion or inc drainage).
  24. Glaucoma drugs
    • 1-α-agonists: Epinephrine (α1), Brimonidine (α2)
    • 2-β-blockers:Timolol, betaxolol,carteolol
    • 3-Diuretics: Acetazolamide
    • 4-Cholinomimetics:  Direct(pilocarpine,carbachol) Indirect(physostigmine,echothiophate)
    • 5-Prostaglandin: Latanoprost (PGF2α)
  25. Epinephrine (α1)
    Brimonidine (α2)
    Mydriasis (α1); do not use in closed-angle glaucoma Blurry vision, ocular hyperemia, foreign bodysensation, ocular allergic reactions, ocularpruritus
  26. Cholinomimetics
    Miosis and cyclospasm (contraction of ciliary muscle)
  27. Prostaglandin
    Darkens color of iris (browning)
  28. Opioid analgesics
    Morphine, fentanyl, codeine, loperamide, methadone, meperidine, dextromethorphan, diphenoxylate, pentazocine.
  29. Opioid analgesics
    Act as agonists at opioid receptors (μ = morphine, δ = enkephalin, κ = dynorphin) to modulate synaptic transmission—open K+ channels, close Ca2+ channels --> dec Ž  synaptic transmission. Inhibit release of ACh, norepinephrine, 5-HT, glutamate, substance P.
  30. dextromethorphan use
    cough suppression
  31. loperamide, diphenoxylate
  32. maintenance programs for heroin addicts what do u do?
    methadone, buprenorphine +naloxone
  33. in opioid tx Tolerance does not develop to
    miosis and constipation
  34. Butorphanol moa
    κ-opioid receptor agonist and μ-opioid receptor partial agonist; produces analgesia
  35. Butorphanol Use
    Severe pain (e.g., migraine, labor). Causes less respiratory depression than full opioid agonists.
  36. Butorphanol toxicity
    Can cause opioid withdrawal symptoms if patient is also taking full opioid agonist (competition for opioid receptors). Overdose not easily reversed with naloxone.
  37. Tramadol
    Very weak opioid agonist; also inhibits 5-HT and NE reuptake (works on multiple neurotransmitters—“tram it all” in with tramadol).
  38. Tramadol toxicity
    Similar to opioids. Decreases seizure threshold. Serotonin syndrome. 
  39. tx for ABSENCE seizure
    • fist line tx  Ethosuximide
    • Valporic acid 
    • Lamotrigine
  40. tx for simple and complex partial (focal) seizure
    • All drugs including Tiagabine and Vigabatrin except Ethosuximide.
    • Carbamazepine fist line tx
  41. tx for status epilepticus
    • Benzodiazepines (diazepam,lorazepam)1st line for acute
    • Phenytoin 1st line for prophylaxis.
  42. first line tx for tonic clonic seizure
    • Phenytoin
    • Carbamazepine
    • Valproic acid
  43. Ethosuximide
    Blocks thalamic T-type Ca2+ channels
  44. Benzodiazepines(diazepam,lorazepam) 
     INC GABAA action

    Also for eclampsia seizures (1st line is MgSO4)
  45. Phenytoin MOA
    INC Na+ channel inactivation;zero-order kinetics
  46. Carbamazepine MOA AND NOTE
    Na+ channel inactivation

    • 1st line for trigeminalneuralgia
  47. Valproic acid MOA AND NOTE
    INC Na+ channel inactivation, INC GABA concentrationby inhibiting GABA transaminase

    • Also used for myoclonicseizures, bipolardisorder
  48. Gabapentin MOA AND NOTE
    Primarily inhibits high voltage-activated Ca2+channels; designed as GABA analog

    Also used for peripheral neuropathy, postherpetic neuralgia
  49. Phenobarbital MOA
    INC  GABAA action

    1st line in neonates
  50. Topiramate MOA AND NOTE
    Blocks Na+ channels, INC GABA action

    Also used for migraine prevention
  51. Lamotrigine MOA
    Blocks voltage-gated Na+channels
  52. Levetiracetam MOA
    Unknown; may modulateGABA and glutamaterelease
  53. Tiagabine MOA
    INC GABA by inhibitingreuptake
  54. Vigabatrin MOA
    INC GABA by irreversibly inhibiting GABA transaminase
  55. Ethosuximide SE
    GI, fatigue, headache, urticaria,Stevens-Johnson syndrome.

    EFGHIJ—Ethosuximide causesFatigue, GI distress, Headache,Itching, and Stevens-Johnsonsyndrome
  56. Benzodiazepines(diazepam,lorazepam) 
    Sedation, tolerance, dependence,respiratory depression
  57. Phenytoin
    Nystagmus, diplopia, ataxia,sedation, gingival hyperplasia,hirsutism, peripheral neuropathy,megaloblastic anemia,teratogenesis (fetal hydantoinsyndrome), SLE-like syndrome,induction of cytochrome P-450,lymphadenopathy, Stevens-Johnson syndrome, osteopenia
  58. Carbamazepine
    Diplopia, ataxia, blood dyscrasias(agranulocytosis, aplastic anemia),liver toxicity, teratogenesis,induction of cytochrome P-450,SIADH, Stevens-Johnsonsyndrome
  59. Valproic acid SE
    GI, distress, rare but fatal hepatotoxicity (measure LFTs),neural tube defects (e.g., spinabifida), tremor, weight gain,contraindicated in pregnancy
  60. Gabapentin
    Sedation, ataxia
  61. Phenobarbital SE
    Sedation, tolerance, dependence,induction of cytochrome P-450,cardiorespiratory depression
  62. Topiramate SE
    Sedation, mental dulling, kidneystones, weight loss
  63. Lamotrigine SE
    Stevens-Johnson syndrome (must be titrated slowly)
Card Set
MSK, neuro from 444-446, 494-496
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