week 5: Ch. 41 [Inflammation/Fever Pharm] Flashcards by Sasha K.

Inflammation is the response to agents that could:

damage tissue

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Acute VS chronic inflammation

–Acute =________ onset
▪Result of influx of _____________
▪Pain and edema result
▪Lasts ___________________

–Chronic = ________ onset
▪Caused by _________________________________________
▪Scar tissue can result
▪May last __________

–Acute = immediate onset
▪Result of influx of neutrophils
▪Pain and edema result
▪Lasts 1 to 2 weeks

–Chronic = slow onset
▪Caused by lymphocytes and macrophages
▪Scar tissue can result
▪May last years

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Both types of inflammation may have a febrile response:

–Body temperature over ______
–Pulse over ____ beats/minute
–Respirations greater than ____ breaths/min
–WBC count over __________/mm3

–Body temperature over 102°F
–Pulse over 90 beats/minute
–Respirations greater than 20 breaths/min
–WBC count over 12,000/mm3

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Inflammation is not a disease, it is a

symptom of an underlying disorder/cause

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To treat inflammation, the

underlying cause must be treated

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2 main goals of pharmacotherapy of inflammation:

–Prevent/decrease intensity of inflammation
response

–Reduce fever

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Nonspecific inflammations treated with:

–NSAIDs
–Corticosteroids

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Fever treated with :

antipyretics

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Three major classes of NSAIDs

–Salicylates
–Ibuprofen and ibuprofen-like agents
–Cyclooxygenase-2 (COX-2) inhibitors

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Salicylates

–Aspirin first-generation salicylate
▪Originally derived from_______________
▪Indications
–>Analgesic
–>Anti-inflammatory
–>Antipyretic
–>Suppression of platelet aggregation

–Aspirin first-generation salicylate
▪Originally derived from willow bark
▪Indications
–>Analgesic
–>Anti-inflammatory
–>Antipyretic
–>Suppression of platelet aggregation

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Salicylates–Mechanisms of actions

▪Prostaglandins are local hormones found in every tissue
▪Aspirin blocks the synthesis of prostaglandins by
inhibiting enzyme cyclooxygenase (COX)

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Aspirin [prototype drug]

–Therapeutic classification
–Pharmacologic classification

–Therapeutic classification
▪Nonnarcotic analgesic
▪Antipyretic
▪Antiplatelet

–Pharmacologic classification
▪Salicylate
▪NSAID

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Therapeutic effects and uses of Aspirin

▪Mild-moderate intensity _________,_____________, _________
▪Prevention of thromboembolic event
▪Stroke prophylaxis in patients with history of TIAs or persistent or paroxysmal atrial fibrillation
▪MI prophylaxis
▪Suspected coronary thrombosis
▪Off-label use to prevent ________________________________

▪Mild-moderate intensity pain, inflammation, fever
▪Prevention of thromboembolic event
▪Stroke prophylaxis in patients with history of TIAs
or persistent or paroxysmal atrial fibrillation
▪MI prophylaxis
▪Suspected coronary thrombosis
▪Off-label use to prevent colorectal cancer

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Mechanism of action of Aspirin

▪Reduces _________________ synthesis
▪_________body temperature
▪Causes centrally mediated peripheral vasodilation and __________

▪Reduces prostaglandin synthesis
▪Lowers body temperature
▪Causes centrally mediated peripheral vasodilation and sweating

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Adverse effects of Aspirin

– Serious adverse effects
▪Hypersensitivity reaction
▪GI bleeding
▪Thrombocytopenia
▪Hemolytic anemia
▪Occult bleeding
▪Nephrotoxic effects
▪Hepatotoxicity
▪Tinnitus and hearing loss with high doses

– Adverse effects
▪Stomach irritation
▪Heartburn
▪Nausea
▪Vomiting
▪Diarrhea
▪Stomach pain

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Contraindications/precautions with Aspirin

▪Hypersensitivity to any___________ (including in food)
▪“Aspirin triad”
▪Agranulocytosis
▪_______ trauma or increased intracranial pressure
▪History of _____ bleeding
▪Hypoprothrombinemia
▪Vitamin K deficiency
▪Heart failure (HF)
▪Flu or flulike illness in ______________________________
▪Pregnancy, especially in the ________ trimester

More precautions: patients with…
–Hypothyroidism
–Immunosuppression
–Asthma, gout, or anemia
–Chronic kidney disease (CKD)
–Hepatic impairment
–G6PD deficiency

▪Hypersensitivity to any salicylate (including in food)
▪“Aspirin triad”
▪Agranulocytosis
▪Head trauma or increased intracranial pressure
▪History of GI bleeding
▪Hypoprothrombinemia
▪Vitamin K deficiency
▪Heart failure (HF)
▪Flu or flulike illness in children or teens
▪Pregnancy, especially in the third trimester

More precautions: patients with…
–Hypothyroidism
–Immunosuppression
–Asthma, gout, or anemia
–Chronic kidney disease (CKD)
–Hepatic impairment
–G6PD deficiency

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Drug interactions with Aspirin

▪Other ________________ (additive effect)
▪Ammonium chloride and other acidifying agents
▪Anticoagulants, thrombolytics, or antiplatelet agents
▪Oral ______________ agents
▪______ alcoholic drinks per day
▪Corticosteroids
▪Methotrexate
▪Probenecid and sulfinpyrazone
▪_______blockers

▪Herbal/food
–Feverfew, garlic, ginger, horse chestnut, red clover
–Caffeine
–St. John’s wort

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▪Other salicylates (additive effect)
▪Ammonium chloride and other acidifying agents
▪Anticoagulants, thrombolytics, or antiplatelet agents
▪Oral antidiabetic agents
▪3+ alcoholic drinks per day
▪Corticosteroids
▪Methotrexate
▪Probenecid and sulfinpyrazone
▪Beta blockers

▪Herbal/food
–Feverfew, garlic, ginger, horse chestnut, red clover
–Caffeine
–St. John’s wort

Treatment for Aspirin overdose

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▪Emesis (vomiting), gastric lavage, and alkalinization of urine
▪Hemodialysis

Most common drugs for mild to moderate pain and inflammation:

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Ibuprofen-like drugs

Ibuprofen-like drugs all have same mechanism of action:

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inhibit COX

Most Ibuprofen-like drugs are weak acids > easily absorbed in :

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GI tract

*Prototype drug: Ibuprofen (Advil, Motrin, others)
–Therapeutic classification?
–Pharmacologic classification?

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–Therapeutic classification
▪Analgesic
▪Anti-inflammatory drug
▪Antipyretic

–Pharmacologic classification
▪NSAID

Therapeutic effects and uses of Ibuprofen

▪Relief of fever and mild to moderate pain associated with chronic symptomatic __________________________ and osteoarthritis

▪Myalgia, ______________, ________________ & dysmenorrhea

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▪Relief of fever and mild to moderate pain associated with chronic symptomatic rheumatoid
arthritis (RA )and osteoarthritis

▪Myalgia, headache, dental pain, & dysmenorrhea

Mechanism of action of Ibuprofen

▪Inhibits ____________________, which block __________________ synthesis and modulate T-cell function
▪Inhibits inflammatory cell chemotaxis
▪Decreases release of superoxide radicals
▪Increases scavenging of superoxide radicals at inflammatory sites

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▪Inhibits COX-1 and COX-2, which block prostaglandin synthesis and modulate T-cell function
▪Inhibits inflammatory cell chemotaxis
▪Decreases release of superoxide radicals
▪Increases scavenging of superoxide radicals at inflammatory sites

Ibuprofen adverse effects

▪Most common: GI related–Bleeding, anorexia, heartburn, N/V, Constipation or diarrhea ▪CNS effects: Dizziness, headache, drowsiness, tinnitus ▪Rare but serious: Peripheral edema, aplastic anemia, leukopenia and anaphylaxis ▪Chronic use may lead to: Polyuria, azotemia, cystitis, hematuria, & increased creatinine and blood urea nitrogen (BUN) levels

Black box warnings of Ibuprofen [Can be fatal]

▪Risk of serious and potentially fatal cardiovascular thrombotic events, MI, and stroke ▪Risk of serious GI adverse effects (bleeding, ulcer, and stomach or intestine perforation)

Contraindications/precautions with Ibuprofen ▪Allergy to aspirin or___________________ ▪Peptic Ulcer Disease (PUD) ▪________________ abnormalities ▪Perioperative pain related to coronary artery bypass graft (CABG) ▪Severe hepatic impairment ▪Hypertension (HTN) ▪History of GI bleeding ▪Diabetes mellitus ▪Impaired ______________________ function ▪Heart failure, serious HTN, or history of stroke/MI ▪Diminished respiratory function in children with asthma

▪Allergy to aspirin or other NSAIDs ▪Peptic Ulcer Disease (PUD) ▪Bleeding abnormalities ▪Perioperative pain related to coronary artery bypass graft (CABG) ▪Severe hepatic impairment ▪Hypertension (HTN) ▪History of GI bleeding ▪Diabetes mellitus ▪Impaired renal or hepatic function ▪Heart failure, serious HTN, or history of stroke/MI ▪Diminished respiratory function in children with asthma

Drug interactions with Ibuprofen ▪Oral anticoagulants and antiplatelet drugs can increase risk of______________ ▪May increase toxicity of digoxin, lithium, or methotrexate ▪Other NSAIDs, alcohol, or corticosteroids may cause serious adverse __________________ ▪Reduced antihypertensive action of diuretics, beta blockers, and angiotensin-converting enzyme (ACE) inhibitors ▪Herbal/food –Feverfew, garlic, ginger, ginkgo may increase risk of ____________

▪Oral anticoagulants and antiplatelet drugs can increase risk of bleeding ▪May increase toxicity of digoxin, lithium, or methotrexate ▪Other NSAIDs, alcohol, or corticosteroids may cause serious adverse GI events ▪Reduced antihypertensive action of diuretics, beta blockers, and angiotensin-converting enzyme (ACE) inhibitors ▪Herbal/food –Feverfew, garlic, ginger, ginkgo may increase risk of bleeding.

Treatment of Ibuprofen overdose

Administration of activated charcoal and nasogastric suction

Cyclooxygenase-2 inhibitors –Celecoxib (Celebrex) is second-generation NSAID –Blocks COX-2 without inhibiting COX-1 –Less GI bleeding and ulcer formation than with ibuprofen or aspirin –Limited use due to risk of MI and stroke –Therapeutic classification ? –Pharmacologic classification ?

–Therapeutic classification = Anti-inflammatory –Pharmacologic classification ▪COX-2 inhibitor ▪NSAID

Prototype drug: Celecoxib (Celebrex) Therapeutic effects and uses: ▪ ________________________________________________________________________ associated with RA, osteoarthritis, dysmenorrhea, dental procedures, headache, and ankylosing spondylitis ▪Prophylaxis of adenomas or colorectal polyps

▪Mild - moderate pain and inflammation associated with RA, osteoarthritis, dysmenorrhea, dental procedures, headache, and ankylosing spondylitis ▪Prophylaxis of adenomas or colorectal polyps

Celecoxib (Celebrex) mechanism of action ▪Selectively inhibits the enzyme _____ ▪Inhibits ____________ synthesis

▪Selectively inhibits the enzyme COX-2 ▪Inhibits prostaglandin synthesis

*Acetaminophen –Used to: [1] –Has no anti-inflammatory properties = Not an : [2] –Does not cause GI bleeding or ulcers –Often combined with opioid analgesics

1- relieve pain and to reduce fever 2- Not an NSAID

*Acetaminophen –Therapeutic classification ? –Pharmacologic classification ?

–Therapeutic classification ▪Nonopioid analgesic ▪Antipyretic –Pharmacologic classification ▪Para-aminophenol derivative

Acetaminophen (Tylenol) therapeutic effects/uses:

▪Mild to moderate pain ▪Osteoarthritis of the hip or knee ▪Dysmenorrhea ▪Dental procedures ▪Headache and myalgia ▪Fevers

Mechanism of action of Acetaminophen (Tylenol) ▪Inhibits ________ ▪May inhibit chemical _____________ of pain ▪Direct action on ______________ center of hypothalamus

▪Inhibits COX ▪May inhibit chemical mediators of pain ▪Direct action on heat-regulating center of hypothalamus

Acetaminophen (Tylenol) adverse effects – Adverse effects ▪At recommended doses, _______________________ ▪Acute ___________ failure – Serious adverse effects ▪Acute acetaminophen poisoning –Symptoms: anorexia, nausea, vomiting, dizziness, lethargy, diaphoresis, chills, epigastric/ abdominal pain, diarrhea ▪Chronic use can lead to: –Neutropenia –Pancytopenia –Leukopenia –Thrombocytopenic purpura –Hepatotoxicity in alcoholics –Chronic Kidney Disease (CKD) –Stevens–Johnson syndrome

– Adverse effects ▪At recommended doses,well tolerated ▪Acute hepatic failure – Serious adverse effects ▪Acute acetaminophen poisoning –Symptoms: anorexia, nausea, vomiting, dizziness, lethargy, diaphoresis, chills, epigastric/ abdominal pain, diarrhea ▪Chronic use can lead to: –Neutropenia –Pancytopenia –Leukopenia –Thrombocytopenic purpura –Hepatotoxicity in alcoholics –Chronic Kidney Disease (CKD) –Stevens–Johnson syndrome

Black box warning on Acetaminophen (Tylenol) ▪Potential to cause severe _______ injury ▪Serious _______________________ –Symptoms: angioedema, difficulty breathing, itching, or rash

▪Potential to cause severe liver injury ▪Serious allergic reactions –Symptoms: angioedema, difficulty breathing, itching, or rash

Contraindications/precautions with Acetaminophen (Tylenol) ▪Allergy to ______________ ▪Anemia ▪G6PD deficiency ▪___________ disease ▪Rheumatoid or osteoarthritis ▪Malnutrition ▪_______________ depression ▪Immunosuppression ▪CKD

▪Allergy to acetaminophen ▪Anemia ▪G6PD deficiency ▪Hepatic disease ▪Rheumatoid or osteoarthritis ▪Malnutrition ▪Bone marrow depression ▪Immunosuppression ▪CKD

Drug interactions with Acetaminophen (Tylenol) ▪Alcohol increases risk of ______________________ ▪Increase anticoagulant actions with warfarin ▪Can increase the risk of bone marrow suppression with zidovudine ▪Herbal/food –___________ enhances analgesic effects –Hepatotoxicity reported with echinacea

▪Alcohol increases risk of hepatotoxicity ▪Increase anticoagulant actions with warfarin ▪Can increase the risk of bone marrow suppression with zidovudine ▪Herbal/food –Caffeine enhances analgesic effects –Hepatotoxicity reported with echinacea

Treatment of Acetaminophen (Tylenol) overdose ▪Treat within __________ of ingestion ▪Three-bag method of acetylsteine (_______________)

▪Treat within 8 hours of ingestion ▪Three-bag method of acetylsteine (Acetadote)

week 5: Ch. 41 [Inflammation/Fever Pharm] Flashcards

(41 cards)