NSAIDs



|NSAIDs |

|COX 1 Non-Specific Inhibitors |

| |Aspirin |Acetaminophen |Indomethacin |Ibuprofen, Naproxen, Ketaprofen |Ketorolac |

| |Acetylsalicylic Acid | |Indocin | |Toradol |

|moa |Irreversibly acetylate cyclooxygenase |Central inhibition of |MOST POTENT cyclooxygenase |Inhibits |No Vent. or CV Depression |

| |enzyme( |Prostaglandin Synthesis |enzyme inhibitor |Prostaglandin synthesis & | |

| |( release and synthesis of | | |Cyclooxygenase enzyme |Exhibits ceiling effect w/ repeated |

| |prostaglandins ( | | | |doses |

| |Anagesia | | | | |

| | | | | |Reversible Inhibition of Prostaglandins|

|pharm.kinetics |Rapidly Absorbed ( pH Dependent |Complete Oral absorption | | |Max Plasma Conc in 45-60min |

| | | | | | |

| |pH Dependent ( alkaline = slower onset |Conjugation and Hydroxylation in | | | |

| | |the Liver ( to an inactive | | |Protein Binding 99% |

| |Highly Ionized crosses BBB slowly |metabolite | | | |

| | | | | | |

| |High Protein Binding | | | | |

| |Food slows absorption | | | | |

|clearance |Hydrolyzed in liver to Salicylic Acid |Uricosuric = | | |Metabolized by the Liver by |

| | |Anti-gout Drugs | | |Gllucuronic Acid conjugation |

| |Salicylic Acid conjugates with Glycine | | | | |

| |( Salicyluric Acid produced |( elimination of Uric Acid in | | |E ½ x = 5 hours |

| | |Urine | | | |

| |Salicyluric Acid is excreted in urine | | | | |

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| |Alkaline urine favors excretion (85%) | | | | |

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| |E ½ x = 15 -20 min | | | | |

| |E ½ x = 2 -3 hrs (Salicylic Acid) | | | | |

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|Uses |325 - 650 mg Q 4-6 hr | |Arthritis |Arthritis |Good for: |

| |Analgesic | |Ankylosing spondylitis |Musculoskeletal complaints |Postoperative Pain management. |

| |Antipyretic | |Gouty arthritis | |Alone or Combined w/Opioids |

| |81 - 325 mg/day | |PDA | | |

| |Post MI | | | |DO NOT give to pts having Fusions |

| |CABG | | |Dysmenorrhea | |

| |Stroke | |Dysmenorrhea | | |

| |2.4 - 3.6 g/day Divided | | | | |

| |Anti-Inflammatory | | | | |

|effects |Analgesia: Relief of Low Intensity Pain|Analgesic effects |Analgesic effects |Analgesic effects |Analgesic effects (POTENT) |

| |(H/A, Arthritis) | | | | |

| | |Antipyretic effects |Antipyretic effects |Antipyretic effects |Anti-inflammatory effects (Moderate) |

| |Antipyretic: Prevents pyrogen induced | | | | |

| |release of prostaglandins in CNS | |Anti-inflammatory effects |Anti-inflammatory effects | |

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| |Antiplatelet: Prevention of Heart | | | | |

| |Attack and Stroke | | | | |

| | | | | | |

| |Effects last the length of a platelet | | | | |

| |(7-10 days)*** | | | | |

|SE - GI |GI intolerance most common side effect |No GI irritation |GI upset |GI upset |GI upset |

| |Decreases prostaglandin secretion which| | | |Nausea |

| |normally inhibits gastric acid | | | | |

| |secretion = ulceration | | | |Peripheral Edema |

| |Ulceration may lead to 3-8cc Blood Loss| | | |(just another SE) |

| |per day | | | | |

|Prolonged Bleeding |Long lasting functional deficit |No alteration in Platelet Function|Inhibits Platelet Aggregation |Reversible platelet inhibition (compared |Inhibits aggregation of platelets and |

|Time |detectable as prolonged bleeding time | | |to ASA) |platelet Thromboxane production |

| |Platelet Dysfunction reflects the | | | | |

| |inhibition of Thromboxane formation | | |24 -48 hrs after discontinuation |Reversible inhibition of PGEs |

| |Platelet Inhibition is irreversible | | | | |

| |lasting the life of a platelet about | | |Coumadin Dose Must be (’d |Increased Bleeding Time |

| |7-10/d | | | | |

| | | | | | |

| |Causes oozing during surgery | | | | |

| |Can give Platelets to correct b/c new | | | | |

| |platelets not affected by cascade | | | | |

|NSAIDs |

|COX 1 Non-Specific Inhibitors |

| |Aspirin |Acetaminophen |Indomethacin |Ibuprofen, Naproxen, |Ketorolac |

| |Acetylsalicylic Acid | |Indocin |Ketaprofen |Toradol |

|Hepatic effects |Reversible elevated Transaminase Enzymes |Overdose can cause Hepatic |Abnormal LFTs | | |

| | |Necrosis and Death | | | |

| |Aspirin should be avoided in severe Hepatic Dysfunction b/c they |Single dose of > 15g | | | |

| |already have clotting mechanism dysfunction | | | | |

| |( Salicylates may cause changes in function |Treatment( Acetylcysteine w/in | | | |

| | |1st 8h | | | |

|Renal effects |Unlike other Non-steroidals |Metabolites conc. in the | |Exacerbation of Renal Dys. |Reduce doses in |

| |Aspirin DOES NOT cause Renal Failure with chronic use |hypertonic renal papillae ( | |d/t (’d renal bld flow |Elderly patients and |

| | |papillary necrosis | |(inhibition of PGEs |Renal Dysfunction |

| | | | |responsible for that) | |

| | |Hallmark of analgesic induced | | | |

| | |nephropathy | | | |

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|Metabolic (’s |Decrease Lipogenesis ( Blocking incorporation of Free Fatty Acids | | | | |

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| |May cause hyperglycemia ( with large doses | | | | |

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| |Glycogen depletion ( in Liver and Skeletal Muscles | | | | |

|Uterus effects |( in Prostaglandins ( ( Uterine Tone = ( Labor & (Postpartum bleeding | | | | |

|Allergic Reactions |Rare even but can be life-threatening | |Allergic Reactions | |Asthma patients may have a |

| |Aspirin is more likely the cause than salicylic acid | | | |reaction to Toradol |

| |Cross reaction to all inhibitors of prostaglandin synthesis | | | | |

| |S/S: | | | | |

| |Vasomotor | | | | |

| |Laryngeal Edema | | | | |

| |Bronchospasm | | | | |

| |CV Collapse | | | | |

| | | | | | |

|Aspirin Induced Asthma|8 - 20% Incidence ( Can be life-threatening ( Occurs 1-3 hrs after | | | |Bronchospasm (SE) |

| |taking | | | |Avoid in Patients |

| |Higher Incidence in pts w/Triad of Symptoms -“Francis, Samter or ASA | | | |with-“Triad” |

| |Triad” | | | |ASA sensitivity |

| |1. Rhinosinusitis | | | |Nasal polyps |

| |2. Asthma | | | |Asthma |

| |3. Nasal Polyps | | | | |

| |Caused by release of Leukotrienes | | | | |

| |With this triad DO NOT give Aspirin or Toradol | | | | |

|misc. |Leukotriene Pathway remains Intact (goes down left side) |Useful alternative for those | |Stop |30mg of Toradol = |

| |No Interaction w/ Opiod Receptors |unable to take ASA | |ibuprofen 48hrs before |MSO4 10mg or |

| |Stop ASA 7 days before surgery | | |surgery |Meperidine 100mg |

|NSAIDs |

|Miscellaneous Anti-Arthritis Drugs (assoc. w/gout) |

| |Colchicine |Allopurinal |Probenecid and Sulfinpyrazone |

|moa |Alters fibrillar microtubules in granulocytes |Interferes with terminal step in Uric Acid synthesis |Uricosuric Drugs |

| |- inhibits migration | |Act directly on renal tubules |

| | |Readily absorbed and converted to ( Oxypurinol |Increase rate of excretion of Uric Acid and other Organic Acids |

| |Does NOT increase excretion of Uric Acid | |Help decrease serum Uric Acid levels |

| | | |Both inhibit renal tubular reabsorption of Uric Acid |

|Effects |Reduces inflammation associated with Gout | |Lack Anti-inflammatory activity |

| | | | |

| |Not an Analgesic | | |

|Uses |Good for Gout |Preferred Treatment for Gout |Controls hyperuricemia from Chemo drugs and diseases with accelerated |

| |Acute Attacks and | |destruction of erythrocytes |

| |Prophylaxis (primary use)*** | |Non-Acute Gout |

|Side Effects |GI Symptoms appear before Toxicity ( |Maculopapular Rash |Rash |

| |Hemorrhagic Gastroenteritis |Pruritus |Decreased renal tubular secretion of drugs ( Oral hypoglycemics |

| | |Fever | |

| |GI Symptoms |Myalgia | |

| |N/V |Nephritis | |

| |Diarrhea |Vasculitis | |

| | |Pronlong effects of Oral Anti-Coagulants | |

| |Enhances CNS depressants and Sympathomimetics | | |

| |Depresses Ventilation | | |

|misc | | |Highly protein bound 90 - 98% |

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