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pathopharm exam 3
|WHAT DO Cyclooxygenase Inhibitors DO? ASIDE FROM ASPIRIN= other NSAIDs, effects decline as soon as drug levels fall-REVERSIBLE
|SRR UsesSuppress inflammationRelieve painReduce fever
|ADR ARE? COX 1
|GBRI Adverse effects Gastric ulcerationBleedingRenal impairmenT( hypovolemia, hepatic cirrhosis, or heart failure)
|MECHANISIM OF ACTION?
|Inhibit cyclooxygenase (COX), the enzyme that converts arachidonic acid into prostanoids(prostaglandins and related compounds) Inhibition of COX-1 (“good COX”) Gastric ulceration Bleeding Renal impairment
|BENEFITS OF COX1 MEDIATE BENEFICIALS PROCESSES W/ADR
|Protection against myocardial infarction (MI) and stroke (secondary to reduced platelet aggregation
|BENEFITS OF COX 2 -AT SITE OF TISSUE INJURY MEDIATE HAMFUL PROCESSES
|SARP Suppression of inflammationAlleviation of pain and reduction of feverProtection against colorectal cancer ADR= Renal impairment • Promotion of MI and stroke (secondary to suppressing vasodilation)
|Classification of Cyclooxygenase Inhibitors
|Drugs with anti-inflammatory properties Nonsteroidal anti-inflammatory drugs (NSAIDs) •Aspirin, celecoxib, ibuprofen, and naproxen Drugs without anti-inflammatory propertiesAcetaminophen
|First-Generation NSAIDs ARE?
|Inhibit COX-1 and COX-2 treat inflammatory disorders (rheumatoid arthritis, osteoarthritis, bursitis) Alleviate mild to moderate pain Suppress fever Relieve dysmenorrhea Suppress inflammation but pose risk of serious harm
|Aspirin BAYER ONLY ONE THAT PROTECT A/G MI & STROKE
|Nonselective (COX 1&2) Analgesic, antipyretic, anti-inflammatory Suppression of platelet aggregation-LESS LIKELY TO CLOT •Protects in thrombotic disorders Dysmenorrhea Cancer prevention Prevention of Alzheimer’s disease
|ADR (ADVERSE REACTION)ARE? INFANTS AND CHILDREN=REYES SYNDROM IS LIKELY= FATTY LIVER, ENCEPHELAPATHY= FATALITY
|(GI) effects Bleeding Renal impairment Salicylism: HIGH T.EFFEC LEVEL Tinnitus (ringing in the ears),sweating, headache, and dizziness Reye’s syndrome<18OLD Pregnancy•Anemia, postpartum hemorrhage; may prolong labor Hypersensitivity reaction
|Anticoagulants: Warfarin and heparin Glucocorticoids AlcoholIbuprofen ACE inhibitors and ARBs Acute poisoning=KIDNEY Immediate threats to life: Respiratory depression, hyperthermia, dehydration, and acidosis. Treatment is largely supportive.
|Nonaspirin First-Generation NSAIDs
|Aspirin-like drugs w/ < GI, renal, and hemorrhagic effects than aspirin 20+ nonaspirin NSAIDs available Inhibit COX-1 and COX-2: Inhibition is reversible Principal USE: Rheumatoid arthritis and osteoarthritis Do not protect against MI and stroke
|1ST GEN. NSAID IBUPROFEN IS: Advil, Motrin]
|Inhibits cyclooxygenase and has anti-inflammatory, analgesic, and antipyretic actions Indications: Fever, mild to moderate pain, arthritisGenerally well toleratedLow incidence of adverse effects W/FOOD
|SAFETY ALERT: LACK OF PROTAGLANDING=PROTECT LINING IN STOMACH
|All first-generation NSAIDs are associated with an increased risk of GI bleedinG that can lead to hospitalization or death TAKE W/ FOOD Stevens-Johnson syndrome, a severe hypeRSTVTY reaction=SKIN blistering and mucous membranes= scarring, blindness
|effective as traditional NSAIDs in suppressing inflammation and pain lower risk for GI side effects Can impair renal function and cause hypertension and edema Increased risk of MI and stroke
|Celecoxib [Celebrex] IS: LAST LINE OF DEFENSE LIKE NAPROXEN-RELIEVE JOINT PAIN, STIFFNESS AND SWEALING
|COX-2 inhibitor HBP+EDMA < adverse effects than first-generation drugs Because of cardiovascular risks, last-choice drug for long-term management of pain OsteoarthritisRheumatoid arthritisAcute painDysmenorrheaFamilial adenomatous polyposis
|CELECOXIB ADR ARE?
|Dyspepsia Abdominal pain Renal impairment Sulfonamide allergy Cardiovascular impact (stroke, MI, and other serious events) Use in pregnancy DECREASE DIURETIC + ACE AND INCREASE LITHIUM+FLUCONAZOLE
|DRUG INTERACTIONS CONTRAINDICATED IN 3RD SEMESTER
|Warfarin May decrease diuretic effect of furosemide May decrease antihypertensive effect of ACE inhibitors May increase levels of lithiumCelecoxib levels may be increased by fluconazole
|Acetaminophen [Tylenol] IS: CHILDREN CAN TAKE+IBUPROFEN
|Analgesic, antipyretic Does not have any anti-inflammatory or antirheumatic actions Not associated with Reye’s syndrom- Inhibits prostaglandin synthesis in central nervous system
|Very few at normal doses Stevens-Johnson syndrome (SJS), acute generalized exanthematous pustulosis (AGEP), andtoxic epidermal necrolysis (TEN) Hepatotoxicity •With overdose or iN patients with liver failure 4000MG/DAY
|TYLENOL OVERDOSE? Absence of jaundice AFTER USING Acetylcysteine FOR AN OVERDOSE =IT IS EFFECTIVE
|Hepatic necrosis(DEATH LIVER TISSUE) •Signs and symptoms of hepatic failure, coma, death •Early symptoms: Nausea and vomiting, diarrhea, sweating, abdominal pain •Treatment 4 overdose: Acetylcysteine(Mucomyst) NOT DRUG W/TYLENOL TAKEN W/ THIS -ASTHMA
|Alcohol WarfarinP Vaccines -DECREASE EFFECT OF VACCINE+IMMUNE RESPONSE
|AHA Statement on COX Inhibitors
|Most COX inhibitors, especially COX-2 inhibitors, increase the risk for MI and stroke American Heart Association (AHA) recommends a stepped-care approach
|A patient is prescribed celecoxib [Celebrex] and warfarin [Coumadin]. The nurse should monitor the patient for what?
|Bleeding Celecoxib may increase the anticoagulant effects of warfarin; the risk of bleeding is increased.
|A patient drinks five to six alcoholic beverages per day and takes acetaminophen [Tylenol] for pain relief. The nurse should caution the patient to do what?
|Patients who drink three or more alcoholic beverages per day -should limit their acetaminophen dosage to less than 2000 mg/day to prevent hepatic injury.
|Nonaspirin NSAIDs differ from aspirin in all but which way?
|They are safe to use in children with chickenpox or influenza.
|COX IN STOMACH-PROSTAGLADINS 1&2 they act locally
|promotes synthesis of PGE2 and PGI2,= help protect the gastric mucosa. Three mechanisms are involved: reduced secretion of gastric acid, increased secretion of bicarbonate cytoprotective mucus, maintenance of submucosal blood flow.
|In platelets, COX promotes synthesis of TXA2,( prostacyclin, thromboxane A2) which stimulates platelet aggregation.
|In blood vessels, COX promote synthesis of prostacyclin, which causes vasodilation
|kidney= COX catalyzes synthesis of PGE2 and PGI2, which promote vasodilation and thereby maintain renal blood flow.
|In the brain, COX-derived prostaglandins mediate fever and contribute to perception of pain. I
|In the uterus, COX-derived prostaglandins help promote contractions at term.
|FACTORS INCREASING RISK OF ULCERATION(ASPIRIN)
|• Advanced age • A history of peptic ulcer disease • Previous intolerance to aspirin or other NSAIDs • Cigarette smoking • History of alcohol abuse (Alcohol intensifies the irritant effects of aspirin and should not be consumed.)
|Precautions and Contraindications(ASPIRIN) asthma, hay fever, chronic urticaria, nasal polyps. ASPIRIN WITHDRAWM 1 WEEK B4 SURGERY
|peptic ulcer disease, hemophilia, vitamin K deficiency, hypoprothrombinemia), hypersensitivity to aspirin NSAIDs. caution pregnant women + children W/ chickenpox or influenza. smokeR heart failure, hepatic cirrhosis, hypovolemia,
|MANAGING PAIN IN CARDIOVACSCULAR PATIENT 81MG/DAY TRY CELECOXIB LAST=GREATEST RISK
|1-nondrug measures. p.THERAPY. exer.,wt loss, +heat or cold PADS. 2-If don’t work,USE TYLENOL or aspirin, NO RISK. an opioid or tramadol can be tried, only short term. Step 3. If step 2 drugs are ineffective ,TRY nonselective NSAIDs:naproxen, ibup
|PRE-ASSESSMENT ADMISSION LIST OF ALLERGIES-NSAID INTOLERANCE MEDICALS CONDITIONS(AVOID PT W, PEPTIC ULCER -RECREATIONAL USE-ALCOHOL-SMOKING
|-SUPRESS INFLAMMATION,RELIEF PAIN, REDUCE FEVER TREAT ARTHRITIS, OSTEARTHRITIS PREVENT STROKE AND MI H.RISK-PT 2-CELECOXIB NOT W/ ALLERGIC TO SULFA, HYPERSENSITIVITY ASPIRIN NOT W/ <18, & CHICKEN AND INFLUENZA WATCH PT. ON ANTICOAGULANT PREGNANT-
|ORAL ALL NSAIDS IV IBUPROFEN RECTAL-ASPIRIN ADVISE-W/ FOOD, MILK,H20 <GI UPSET NOT CRUSH DISCRAD ASPIRIN IF SMELL LIKE VINEGAR
|MINIMIZING ADVERSE EFFETS
|-GI EFFECT(DYSPEPSIA, NAUSEA, ABDOMINAL PAIN) TAKE W/ SOMETHG ON STOMACH -DON'T WANT PT TOO LONG ONN IT-FIND NONDRUGS MEASURES TEST AND ELIMINATE H.PYLORI BEFORE LONG-TERM THERAPY
|ASPIRIN POISONING? and mechanical ventilation=respiration is severely depressed Absorption of aspirin can be reduced by gastric lavage and by giving activated charcoal. If necessary, hemodialysis or peritoneal dialysis can accelerate salicylate removaL
|External cooling (eg, sponging with tepid water), infusion of fluids (to correct dehydration and electrolyte loss), infusion of bicarbonate (to reverse acidosis and promote renal excretion of salicylates),
|DISCONTINUE ASPIRIN =
|High-dose aspirin should be discontinued 1 week before elective surgery (cholecystectomy, hysterectomy