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Pharmacology > Non-Opioid Analgesics/ Anti-inflammatories Exam 4 > Flashcards

Non-Opioid Analgesics/ Anti-inflammatories Exam 4 Flashcards

1
Q

What is the mechanism of action of aspirin?

A

1) Inhibit cyclooxygenase so prostaglandins cannot be formed
2) Sensitize pain receptors to substances such as bradykinin
3) MORE effective if given before painful stimuli is experienced

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2
Q

What is the mechanism of action of Acetaminophen (Tylenol) - miscellaneous analgesic (not NSAID)

A

1) works on COX 3 in the CNS
2) NOT an anti inflammatory

3) Does not:
● inhibit platelet aggregation
● irritate the GI tract
● cause bronchoconstriction

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3
Q

What is the mechanism of action of NSAIDS (non-steroidal anti-inflammatory drugs) - true analgesics?

A

1) INHIBIT prostaglandin synthesis

2) INHIBIT cyclooxygenase so that prostaglandins are not formed
● Non-selective: COX-1 & COX-2
● Selective: COX-2

3) INHIBIT cytoprotective PG as well as PG associated w/ inflammation

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4
Q

What is the clinical indications for use for aspirin?

A

1) fever
2) salicylate for analgesia
3) throbbing pain (due to inflammation)

  • – Most effective if given before painful stimuli are experienced
  • Aspirin is more effective against throbbing
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5
Q

What is the clinical indications for use for acetaminophen?

A 
•	Inhibitor of COX 3 = acts more upon CNS COX  than peripheral COX
•	Acts centrally
•	Does not:
o	inhibit platelet aggregation
o	irritate the GI tract
o	cause bronchoconstriction
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6
Q

What is the clinical indications for use for NSAIDS?

A

1) Dental: pain, fever, inflammation

2) Medical: osteoarthritis, rheumatoid arthritis, gouty arthritis, fever, dysmenorrhea, pain

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7
Q

What is the clinical indications for use for acetaminophen ?

A

– (Remember that acetaminophen and aspirin are):

1) Equally efficacious (reduces same degree of pain)
2) Equally potent (same dose in mg needed for effect)
3) Acetaminophen is LESS useful clinically, because it is not anti-inflammatory ***

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8
Q

What is the clinical indications for use for NSAIDS?

A

1) Dental: pain, fever, inflammation

2) Medical: osteoarthritis, rheumatoid arthritis, gouty arthritis, fever, dysmenorrhea, pain

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9
Q

What are the clinical effects of aspirin (Analgesic) ?

A

1) relieves mild to moderate pain

2) NOT potent enough to relieve more intense pain

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10
Q

What are the clinical effects of aspirin (Antipyretic) ?

A

1) fever reduction
2) inhibition of prostaglandin synthesis in hypothalamus
3) induces peripheral vasodilation and sweating

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11
Q

What are the clinical effects of aspirin (Anti-inflammatory) ?

A

1) DECREASED prostaglandins causes decreased capillary permeability = decreased erythema & swelling of inflamed area
2) Important b/c almost all dental pain is inflammatory

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12
Q

What are the clinical effects of aspirin (Uricosuric) ?

A

1) Large/high doses (3+ g/day) = excretion of uric acid in urine
2) Used to tx gout (b/c of uric acid retention)

3) Low doses (< 1g/day): uric acid retention
- take probenecid (Benemid) to excrete uric acid
- aspirin can antagonize these effects = drug interaction

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13
Q

What are the clinical effects of aspirin (Antiplatelet) ?

A

1) Irreversible for life of platelet (7 to 10 days)

2) Inhibits cyclooxygenase which inhibits to formation of thromboxane A2
○	A2 normally causes vasoconstriction and platelet aggregation = facilitates clotting 
○	aspirin REDUCED risks for clots (heart attack) & stroke at low doses (81 mg)
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14
Q

What are the clinical effects of Acetaminophen?

A

1) equally potent to aspirin
2) equally efficacious as aspirin
3) used less clinically b/c it’s NOT an anti-inflammatory
4) No effect on uric acid
5) No anticoagulant effects
6) Yes analgesic
7) Yes antipyretic

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15
Q

What are the clinical effects of NSAIDS?

A

1) Reversible effects on blood platelets
• Effect lasts only as long as the drug is in bloodstream
• Need to discontinue NSAIDS before surgery is based on half-life:
- Ibuprofen = 1 day
- Naproxen = 4 days
-Discontinue 4 to 5 half-lives prior to dental surgery
(Check individual drugs to determine half-life & length of time for discontinuation)

2) Aspirin (a salicylate) causes irreversible effects on platelets: discontinue 7-10 days prior to dental surgery

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16
Q

Identify and discuss common adverse events associated with aspirin (GI)

A

GI: dyspepsia, nausea, vomiting, gastric bleeding

1) Gastric irritation and inhibition of cytoprotective prostaglandins (mucus in stomach)
2) Stimulation of chemoreceptor trigger zone in the CNS (nausea/vomiting)
3) Exacerbates pre-existing ulcers, gastritis, hiatal hernia, reflux disease

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17
Q

Identify and discuss common adverse events associated with aspirin (Bleeding)

A

1) irreversible effects on platelets
2) reduces platelet adhesiveness/aggregation by interfering with ADP release causing prolonged bleeding
3) inhibits production of prothrombin causing hypoprothrombinemia
4) GI bleeding (often painless)

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18
Q

Identify and discuss common adverse events associated with aspirin (Reye’s syndrome)

A

1) aspirin is contraindicated in children/adolescents with viral infections (ex: flu, chickenpox)
2) children can OD b/c loss of water with diarrhea and vomiting
3) Reye’s syndrome can manifest with fluid in brain (encephalitis) and hepatotoxicity
4) Use acetaminophen (Tylenol) instead

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19
Q

Identify and discuss common adverse events associated with aspirin (Salicylism)

A

● confusion, tinnitus, dizziness, nausea, vomiting, headache, dimness of vision, hyperthermia
● High doses: hyperventilation, respiratory alkalosis, renal loss of bicarbonate → respiratory and metabolic acidosis
● death from aspirin is usually acidosis and electrolyte imbalance (6-10 grams in adults)

20
Q

Identify and discuss common adverse events associated with aspirin (Hypersensitivity/Allergy)

A

1) TRUE allergy: rash, wheezing, urticaria (hives), angioneurotic edema, anaphylaxis
○ if allergic then will have cross-sensitivity to other NSAIDS
○ allergic reactions look like asthma attacks

2) not a true allergy: stomach problems
3) asthmatics are more likely to have hypersensitivity reaction = contraindicated

4) Hypersensitivity triad:
○ Aspirin hypersensitivity
○ Asthma
○ Nasal polyps

21
Q

Identify and discuss common adverse events associated with aspirin (Aspirin burn)

A

1) when aspirin is applied directly to oral mucosa, ester in water splits to acetic acid and salicylic acid
2) causes oral ulcerations

22
Q

Identify and discuss common adverse events associated with Acetaminophen

A

1) Hepatotoxic

2) Contraindicated in patients w/:
● Liver disease or dysfunction
● Patients treated w/ drugs that are dependent on liver function
● alcoholism (3+ drinks/day)
● patients on Warfarin (Coumadin) = enhanced anticoagulation

3) Increased risk of bleeding (increased INR)

23
Q

Identify and discuss common adverse events associated with NSAIDS

A

1) Reversible effects on blood platelets
2) Increase risk of MI, stroke
3) Hypertension

4) Compromised renal function
● nephrotoxicity w/ excessive or chronic use
● contraindicated in pts w/ advanced renal disease
● more susceptible in elderly

24
Q

Identify and discuss common adverse events associated with (GI)

A

GI: Ulcerations, irritation, bleeding, perforation

1) INCREASED risk w/ taking alcohol
2) Use caution if smoker, elderly, debilitated, pts with history of ulcers, concurrent aspirin therapy or warfarin (Coumadin)

25
Q

Identify and discuss common adverse events associated with ( CNS)

A

CNS: sedation, dizziness, confusion, mental depression, headache, vertigo, convulsions, blurred vision, tinnitus

1) No addition, tolerance or withdrawal
2) Caution when operating heavy machinery or driving

26
Q

Identify and discuss common adverse events associated with (Hypersensitivity/reactions)

A

■ Skin reactions
■ Do not use if pts have aspirin allergy, asthma, or who has rhinitis/itching/bronchospasm (cross-sensitivity)
■ Use w/ caution if decreased hepatic fxn
● rare = liver reactions, fulminating hepatitis

■ Hypersensitivity: hives, itching, angioneurotic edema, chills, fever, Steven-Johnson syndrome, exfoliative dermatitis, bronchospasm (wheezing), anaphylaxis

● Cross sensitivity if pt is allergic to aspirin or other NSAIDS

27
Q

Identify and discuss common adverse events associated with (Kidney damage)

A

Kidney damage:

1) INHIBITING prostaglandin shuts down renal blood flow
2) renal necrosis
3) short term usage has little risk
4) increased risk of UTI, cystitis

28
Q

What is the dosing of NSAIDS as it relates to analgesic versus anti-inflammatory effects?

A

1) Anti-inflammatory = only seen after 3500 mg aspirin per day (used for arthritis management)
- It is difficult to take this dose chronically, it will lead to GI ulceration & bleeding

2) Analgesic = dosing used for pain control is not enough for anti-inflammatory effects
- Greater the dose, the more likely that you will experience adverse effects

29
Q

What is the dose for optimal analgesia and chronic inflammatory pain regarding Ibuprofen (Motrin)?

A

1) Optimal analgesia (ceiling effect for dental pain) = 400 mg

2) Chronic inflammatory pain: 400-800 mg, 4x day, not exceeding 3200 mg
● less dosage for pts with kidney disease, GI ulcers
● takes days to weeks to reach anti-inflammatory effects from gradual reduction in prostaglandin synthesis

30
Q

What is the dose for optimal analgesia and inflammatory pain regarding Naproxen (Aleve, Anaprox, Naprosyn) ?

A

1) Analgesia: 1 hour onset, up to 7 hours

2) Inflammatory dosing: less than 12 hours, peaks after 2 weeks

31
Q

What are non-selective NSAIDS?

A

Non-selective NSAIDS: BLOCKS COX 1 & 2

1) Most NSAIDS used today
2) COX-1 (Functional Form)
3) Normal function:
- maintains renal blood flow, body temp, BP, HR, reproduction
- regulates amount of stomach acid produced

4) When taking aspirin/NSAIDS
- blocks formation of both cytoprotective prostaglandins and prostaglandins associated with inflammation
- Decreases production of protective stomach mucus → f GI ulceration & bleeding

5) COX-2 (Inducible form)
- Produced during trauma & need inflammatory response for healing
- No effect on stomach

32
Q

What are Selective NSAIDS?

A

1) BLOCKS COX-2 only !

2) Ex: celecoxib (Celebrex) for arthritis pain
○ Acetaminophen (Tylenol) blocks COX-3 therefore is not categorized

33
Q

Write a sample prescription for ibuprofen for the management of dental pain

A

○ Rx: 400 mg tablets
○ Disp: 16 tablets
○ Take 1-2 tablets by mouth 3-4 times per day as needed for pain. Do not exceed 8 tables within 24 hours
(Max analgesic efficacy is at 400 mg )

○ Children: 4 - 10 mg/kg/dose every 6-8 hours (max 4 doses per day)
○ Adults: 200 - 400 mg/dose every 4-6 hours for max daily dose of 1200 mg unless otherwise directed

34
Q

Discuss the relative potencies of different NSAIDS (piroxicam (Feldene)) and how potency relates to dosing

A

1) piroxicam (Feldene) = longest acting of all NSAIDS *
- 10 mg 2 times per day
- Long half life = 45-50 hours

35
Q

Discuss the relative potencies of different NSAIDS (flurbiprofen (ANSAID)* and how potency relates to dosing

A

1) flurbiprofen (ANSAID)*
- 100 mg every 12 hours
- Onset of action = 1-2 hours
- Half life = 5.7 hours

36
Q

Discuss the relative potencies of different NSAIDS (ketorolac (Toradol)* and how potency relates to dosing

A

ketorolac (Toradol)* =
-Used for up to 5 days for severe acute pain requiring analgesia at opioid level

-Taken primarily by injection; causes renal damage

37
Q

Discuss the relative potencies of different NSAIDS (diflunisal (Dolobid)* and how potency relates to dosing

A

o “super aspirin” = No greater efficacy than aspirin
o Onset = 1 hour
o Duration = 8-12 hours
o Long half-life = 8-12 hours
o RX: Dolobid 500 mg tablets
o Disp: 16 tablets
o Sig: Take 2 tablets initially, then 1 tablet every 8-12 hours as needed for pain

38
Q

What are the common drug interactions associated with aspirin?

A

Aspirin = separate dosing intervals w/ NSAIDS to avoid attenuation of anti-platelet effects of aspirin

1) Alcohol: increases risk of GI bleeding associated w/ aspirin & NSAIDS

2) Antihypertensive medications (diuretics, Beta blockers, ACE inhibitors)
■ aspirin & NSAIDS may decrease effectiveness
■ monitor BP w/ NSAIDS to pts taking BP meds

3) Methotrexate & ibuprofen/aspirin
■ tx: autoimmune diseases and cancer
■ ibuprofen inhibits breakdown of methotrexate = toxicity
■ can’t give aspiring = displaces MTX & interferes w/ clearance, increasing serum concentrations & causing toxicity (bone marrow depression)

39
Q

What are the common drug interactions associated with NSAIDs?

A

NSAIDS = taking multiple NSAIDS together can give an additive toxic effect

1) Lithium = used for bipolar disorder
■ NSAIDS blocks excretion of lithium

2) Aspirin & NSAIDS decrease effectiveness of many common antihypertensive medications = monitor BP if giving NSAIDS to patients taking BP meds
- Diuretics
- Beta blockers
- ACE inhibitors

3) Contraindications/Caution w/ NSAIDS:
■ asthma
■ CV or kidney disease
■ stomach ulcer, ulcerative colitis
■ coagulopathies
■ previous hypersensitivity to aspirin or other NSAIDS
■ geriatric pts = more prone to adverse hepatic or renal adverse events

40
Q

What are the prescribing considerations for aspirin, acetaminophen and NSAIDS in patients with asthma, kidney or liver dysfunction?

A

1) Allergy: manifests as bronchial reaction
■ DON’T t use if pts has aspirin allergy, asthma, or who has rhinitis/itching/bronchospasm

2) chronic gastritis: inc. chance for GI ulceration and bleeding
3) gout: interacts w/ probenecid
4) contraindicated in pts with advanced renal disease
5) With decreased hepatic function, use w/ caution, if has liver disease or takes medications that depends on liver functions

41
Q

What are the prescribing considerations for aspirin, acetaminophen and NSAIDS in patients with pregnant patients?

A

3rd trimester of pregnancy (Category C/D):
1) Can prolong labor: dec. prostaglandins responsible for uterine contractions

2) Increases risk of bleeding complications
3) Risk of premature closing of ductus arterioles in fetus causing pulmonary vasculature abnormalities & pulmonary hypertension in newborns
4) LOW dose may have positive effects
5) Not been shown to be teratogenic

42
Q

What are the effects of aspirin on platelet function?

A

Aspirin: Irreversible effects on blood platelets

■ REDUCES platelet adhesiveness/aggregation by interfering w/ ADP release causing prolonged bleeding

■ INHIBITS production of prothrombin causing hypoprothrombinemia

■ GI bleeding (often painless)

43
Q

What are the effects of NSAIDS on platelet function?

A

NSAIDS: Reversible effects on blood platelets
■ if need to discontinue prior to surgery, count back 4 to 5 half-lives

■ FDA states that “ibuprofen can interfere with the antiplatelet effect of low-dose aspirin (81 mg), potentially rendering aspirin less effective when used for cardioprotection and stroke prevention.”

■ FDA recommends for patients who use immediate release aspirin (not enteric coated) & take a single dose or chronic doses of ibuprofen 400 mg, dose ibuprofen at least 30 minutes or longer after aspirin ingestion or more than 8 hours before aspirin ingestion to avoid attenuation of aspirin’s effect

■ Occasional use of ibuprofen or other NSAIDS pose little risk for attenuation of anti-platelet effects of low-dose aspirin

44
Q

Acetaminophen has ________ affect on platelet function

A

NO EFFECT

45
Q

What are the dental practice management considerations related to the platelet effects caused by aspirin and NSAIDS?

A

1) DON’T need to discontinue aspirin prior to dental tx if on LOW dose therapy (81 mg/day)
2) 1 single dose of aspirin exerts an effect for a minimum of 4 days

3) For highly invasive surgeries must weigh risk to pt vs bleeding risk
■ Ex: pts w/ cardiac stents are on aspirin & anti platelet drug (Plavix) → discontinue Plavix but not aspirin before surgery

4) If need to discontinue NSAIDS prior to surgery time is based on ½ life (count back 4-5 half lives)
■ Ibuprofen = 1 day
■ naproxen = 4 days

Pharmacology (13 decks)

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