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

1
Q

Inflammation is the response to agents that could:

A

damage tissue

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2
Q

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 __________

A

–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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3
Q

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

A

–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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4
Q

Inflammation is not a disease, it is a

A

symptom of an underlying disorder/cause

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5
Q

To treat inflammation, the

A

underlying cause must be treated

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6
Q

2 main goals of pharmacotherapy of inflammation:

A

–Prevent/decrease intensity of inflammation
response

–Reduce fever

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7
Q

Nonspecific inflammations treated with:

A

–NSAIDs
–Corticosteroids

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8
Q

Fever treated with :

A

antipyretics

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9
Q

Three major classes of NSAIDs

A

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

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10
Q

Salicylates

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

A

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

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11
Q

Salicylates–Mechanisms of actions

A

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

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12
Q

Aspirin [prototype drug]

–Therapeutic classification
–Pharmacologic classification

A

–Therapeutic classification
▪Nonnarcotic analgesic
▪Antipyretic
▪Antiplatelet

–Pharmacologic classification
▪Salicylate
▪NSAID

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13
Q

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 ________________________________

A

▪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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14
Q

Mechanism of action of Aspirin

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

A

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

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15
Q

Adverse effects of Aspirin

A

– 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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16
Q

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

A

▪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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17
Q

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

A

▪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

18
Q

Treatment for Aspirin overdose

A

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

19
Q

Most common drugs for mild to moderate pain and inflammation:

A

Ibuprofen-like drugs

20
Q

Ibuprofen-like drugs all have same mechanism of action:

A

inhibit COX

21
Q

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

A

GI tract

22
Q

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

A

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

–Pharmacologic classification
▪NSAID

23
Q

Therapeutic effects and uses of Ibuprofen

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

▪Myalgia, ______________, ________________ & dysmenorrhea

A

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

▪Myalgia, headache, dental pain, & dysmenorrhea

24
Q

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

A

▪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

25
Q

Ibuprofen adverse effects

A

▪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

26
Q

Black box warnings of Ibuprofen

[Can be fatal]

A

▪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)

27
Q

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

A

▪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

28
Q

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 ____________

A

▪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.

29
Q

Treatment of Ibuprofen overdose

A

Administration of activated charcoal and
nasogastric suction

30
Q

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 ?

A

–Therapeutic classification = Anti-inflammatory

–Pharmacologic classification
▪COX-2 inhibitor
▪NSAID

31
Q

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

A

▪Mild - moderate pain and inflammation associated with RA, osteoarthritis, dysmenorrhea, dental procedures, headache, and ankylosing spondylitis

▪Prophylaxis of adenomas or colorectal polyps

32
Q

Celecoxib (Celebrex) mechanism of action

▪Selectively inhibits the enzyme _____
▪Inhibits ____________ synthesis

A

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

33
Q

*Acetaminophen

–Used to: [1]
–Has no anti-inflammatory properties = Not an : [2]

–Does not cause GI bleeding or ulcers
–Often combined with opioid analgesics

A

1- relieve pain and to reduce fever

2- Not an NSAID

34
Q

*Acetaminophen

–Therapeutic classification ?
–Pharmacologic classification ?

A

–Therapeutic classification
▪Nonopioid analgesic
▪Antipyretic

–Pharmacologic classification
▪Para-aminophenol derivative

35
Q

Acetaminophen (Tylenol) therapeutic effects/uses:

A

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

36
Q

Mechanism of action of Acetaminophen (Tylenol)

▪Inhibits ________
▪May inhibit chemical _____________ of pain
▪Direct action on ______________ center of hypothalamus

A

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

37
Q

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

A

– 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

38
Q

Black box warning on Acetaminophen (Tylenol)

▪Potential to cause severe _______ injury

▪Serious _______________________
–Symptoms: angioedema, difficulty breathing, itching, or rash

A

▪Potential to cause severe liver injury

▪Serious allergic reactions
–Symptoms: angioedema, difficulty breathing, itching, or rash

39
Q

Contraindications/precautions with Acetaminophen (Tylenol)

▪Allergy to ______________
▪Anemia
▪G6PD deficiency
▪___________ disease
▪Rheumatoid or osteoarthritis
▪Malnutrition
▪_______________ depression
▪Immunosuppression
▪CKD

A

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

40
Q

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

A

▪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

41
Q

Treatment of Acetaminophen (Tylenol) overdose

▪Treat within __________ of ingestion
▪Three-bag method of acetylsteine (_______________)

A

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