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PoD Test 3 > Antipyretics, Anti-inflammatory and analgesics > Flashcards

Antipyretics, Anti-inflammatory and analgesics Flashcards

1
Q

What are eicosanoids?

A

Members of a family of oxygenated products of polyunsaturated long-chain fatty acids

Prostaglandins, Thromboxanes, Leukotrienes

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2
Q

What is arachidonic acid?

A

Most abundant and important precursor of eicosanoids

Synthesized from linoleic acid

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3
Q

What is the form and function of COX-1?

A

Constitutive form found in endothelial cells, stomach and kidney

Housekeeping functions, increased stomach mucus

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4
Q

What is the form and function of COX-2?

A

Inducible by inflammation and cytokines

Immediate early response gene product in inflammatory/immune cells

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5
Q

What is the MoA of Prostanoids?

A

Paracrine/autocrine

Activate G proteins or PIP metabolism

Major affects are on smooth muscle: vascular, GI, airway, reproductive

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6
Q

What is the use and ADR of Misoprostol?

A

PGE1 analog

Adjunct to NSAID therapy to reduce ulcer formation

Inhibits gastric acid secretion

Contraindicated in pregnancy

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7
Q

What is the use of Latanoprost?

A

PGF2a analog

Ophthalmic preparation, used for open angle glaucoma

Increases aqueous humor outflow

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8
Q

What is the use of Alprostadil?

A

PGE1

Temporarily maintains patent ductus arteriousis in newborns until surgery can be done

Increases pulmonary blood flow, improving blood oxygenation

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9
Q

What does the lipoxygenase pathway produce?

A

Leukotrienes

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10
Q

What is the function of Leukotriene B4?

A

Chemotactic agents for PMNs

Can also produce hyperalgesia

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11
Q

What are the functions of the Cysteinyl Leukotrienes (LTC4, D4, and E4)?

A

Potent bronchoconstrictors

Increase vascular permeability

Components of slow reacting substance of anaphylaxis

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12
Q

What is CysLT1 and its function?

A

Eicosanoid receptor

Pulmonary inflammation and fibrotic response

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13
Q

What is the MoA for Afirlukast and Montelukast?

A

Competitive, reversible LTD4 (CysLT1) receptor antagonist

Inhibits LT mediate effects on bronchoconstriction and vascular permeability

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14
Q

What are the uses for Zafirlukast and Montelukast?

A

Prophylactic treatment for Asthma

Monte - 1yr or older

Zafir - 5yr or older

Allergic Rhinitis

Aspirin sensitivity induced asthma (montelukast only)

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15
Q

What is the dosage for Zafirlukast?

A

20mg BID

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16
Q

What is the dosage for Montelukast?

A

10mg for adults or 4mg for children QD

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17
Q

What are the ADRs and interactions of Zafirlukast?

A

Headache, pharyngitis, increased liver enzymes

Inhibits CYP3A4 and 2C9 (warfarin)

Must be taken 1-2 hrs prior to food

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18
Q

Whats the ADR for Montelukast?

A

Headacke

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19
Q

What is the MoA of Zileuton?

A

Inhibitor of 5-lipoxygenase

Inhibits synthesis of leukotrienes

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20
Q

What is the use for Zileuton?

A

Prophylaxis for asthma in adults/children over 12

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21
Q

What is the dosage for Zileuton?

A

400-800mg 2-4x daily

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22
Q

What are the drug interactions for zileuton?

A

Theophylline

Warfarin

Propranolol

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23
Q

What are the ADRs for Zileuton?

A

Contraindicated in liver disease

Ergot alkaloids contraindicated

Seldom used in USA due to safety

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24
Q

What is the MoA of NSAIDs?

A

Inhibits cycloxygenases

Non-selective

Aspirin - irreversible inhibitor

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25
Q

What are the common therapeutic actions of aspirin and NSAIDs?

A

Antipyretics - inhibit PG synthesis in the hypothalamus

Analgesics - reduction of mild to moderate pain associated with inflammation

Anti-inflammatory properties - inhibits localized PG synthesis

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26
Q

What are four common side effects associated with aspirin and tNSAIDs?

A

Increased risk of GI ulcers and pain

Increased risk of bleeding

Inhibit PG mediated effects in kidney (fluid retention)

Hypersensitivity with aspirin

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27
Q

What are three major drug interactions with NSAIDs?

A

ACE inhibitors

Glucocorticoids

Warfarin

28
Q

What is the MoA of aspirin?

A

Irreversible inhibitor of cyclo-oxygenase

Acetyl salicylate

Acetylates the enzyme

29
Q

What are the uses for aspirin?

A

Antipyretic, anti-inflammatory and analgesic agent

*rarely used as anti-inflammatory agent

Analgesic activity at localized area and in brain, does not interact with opioid receptor

30
Q

What is the analgesic/antipyretic dose of aspirin?

A

Adults - 325-650mg every 4 hours

2-3hr half life

31
Q

What is the anti-inflammatory dose for aspirin?

A

4-6g daily

Half life is 12 hours

32
Q

What is the fatal dose for aspirin?

A

10-30g

half life 15-30 hours

33
Q

What is aspirin’s effect on platelets?

A

Irreversibly inhibits platelet COX

Low doses can irreversibly inhibit TXA2 production

Prevents platelet aggregation

34
Q

What are the clinical uses for aspirin?

A

Low dose - decreases incidence of TIAs, unstable angina, coronary artery thrombosis with MI and thrombosis after CABG

Risk reduction for Preeclampsia

35
Q

What are the side effects of aspirin?

A

GI pain, bleeding and ulcers

Variable urate excretion

Reye’s syndrom in children w/ varicella

36
Q

What is salicylism?

A

Mild intoxication with aspirin

Characterized by tinnitis, high frequency hearing loss, headache, nausea, dimness of vision

Reversible

37
Q

What are the propionic acid derivative NSAIDs?

A

Ibuprogen, Naproxen

38
Q

What is the MoA of Ibuprogen and naproxen?

A

Competitive, reversible active-site inhibitors of COX 1 and 2

39
Q

What are the uses for for Ibuprogen and Naproxen?

A

Analgesic for mild pain

Antipyretic

Anti-inflammatory - symptoms of RA and osteoarthritis

40
Q

What are the uses for ibuprofen?

A

Fever in children

Dysmenorrhea

Acute migrain attacks

RA and osteoarthritis

41
Q

What are uses for naproxen that ibuprofen can’t be used for?

A

Acute gout

Tendonitis

Ankylosing spondylitis

42
Q

What are the ADRs for Naproxen (Aleve)?

A

Increased risk of stroke/HA with prolonged use

43
Q

What are the drug interactions with naproxen?

A

ACE inhibitors

Antacids and Sucralfate (cation chelation)

44
Q

What are the heteroaryl acetic acid derivative NSAIDs?

A

Ketorolac

45
Q

What is the use for the ophthalmic prep of Ketorolac?

A

Seasonal allergy

Recovery from cataract surgery

46
Q

What are the other uses for Ketorolac?

A

Excellent analgesic action

Used for postoperative pain

47
Q

What are the ADRs for Ketorolac?

A

GI bleeding

Bleeding

Decreased hepatic function

Lower dose in patients under 110 lbs or elevated creatinine

48
Q

What are the contraindications for ketorolac?

A

History of peptic ulcer or GI bleeding

Stop before surgery

Concurrent use with aspirin or NSAID

During labor/delivery or during lactation

49
Q

What is the phenylacetic acid derivative NSAID?

A

Diclofenac

50
Q

What are the uses for diclofenac?

A

RA, osteoarthritis and ankylosing spondylitis

Primary Dysmenorrhea

Postoperative pain and inflammation following cataract surgery

51
Q

What is Arthrotec used for?

A

In patients with risk of gastric or duodenal ulcers

Diclofenac + Misoprostol

52
Q

What are the ADRs of Diclofenac (and Arthrotec)?

A

GI symptoms

Modest ALT elevation

Dizziness, Headache

Arthrotec contraindicated in pregnancy

Metabolized by Cyp2C9

53
Q

What is oral indomethacin and its uses?

A

Indoel derivative, slightly specific for COX1

Acute gouty arthritis

RA and osteoarthritis

Tendinitis

Ankylosing sponylitis

54
Q

What is IV indomethacin used for?

A

Nonsurgical repair of patent ductus arteriosus

Decreases PGE levels

55
Q

What are the ADRs of Indomethacin?

A

GI pain - take with food

Severe frontal headache

Displacement of bilirubin from albumin

Decreased urine output

56
Q

What are the contraindications for indomethacin?

A

Hyperbilirubinemia

Renal failure

57
Q

What is celecoxib?

A

Selective COX-2 inhibitor

58
Q

What are the uses for celecoxib?

A

RA and Osteroarthritis

Ankylosing spondylitis

Primary dysmenorrhea

59
Q

What are the drug interactions of celecoxib?

A

Metabolized by P450 Cyp2C9

Fluconazole

Inhibits 2D6

60
Q

What are the ADRs of celecoxib?

A

GI pain

Nausea

61
Q

What are the effects of NSAIDs during pregnancy?

A

Inhibit uterine motility

Induce bleeding in last trimester

Premature closing of ductus arteriosus

62
Q

What are the functions of PGE2 in the kidney?

A

Increase GFR and renal blood flow

Inhibits Cl reabsorption in the TAL of LoH

Inhibits ADH on collecting tubules

Stimulate renin release

*NSAIDS reduce these effects

63
Q

What are the effects of NSAIDs on the kidney?

A

Hyperkalemia and Water Retention

64
Q

What is the MoA of acetominophen?

A

Weak inhibitor of COX-1/2

65
Q

What are the therapeutic uses for acetominophen?

A

MIld to moderate pain

Preferred in children with viral fever

66
Q

What are the ADRs of acetaminophen?

A

Hepatic toxicity (#1 drug cause)

Renal toxicity with chronic use

67
Q

What are DMARDs?

A

Disease Modifying Anti-Rheumatic Drugs

Immune modulators believed to resotre normal immune environment within the joint synovium

Does not inhibit COX

PoD Test 3 (25 decks)

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