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

Antipyretics, Anti-inflammatory and analgesics Flashcards

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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
What are the common therapeutic actions of aspirin and NSAIDs?
Antipyretics - inhibit PG synthesis in the hypothalamus Analgesics - reduction of mild to moderate pain associated with inflammation Anti-inflammatory properties - inhibits localized PG synthesis
26
What are four common side effects associated with aspirin and tNSAIDs?
Increased risk of GI ulcers and pain Increased risk of bleeding Inhibit PG mediated effects in kidney (fluid retention) Hypersensitivity with aspirin
27
What are three major drug interactions with NSAIDs?
ACE inhibitors Glucocorticoids Warfarin
28
What is the MoA of aspirin?
Irreversible inhibitor of cyclo-oxygenase Acetyl salicylate Acetylates the enzyme
29
What are the uses for aspirin?
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
What is the analgesic/antipyretic dose of aspirin?
Adults - 325-650mg every 4 hours 2-3hr half life
31
What is the anti-inflammatory dose for aspirin?
4-6g daily Half life is 12 hours
32
What is the fatal dose for aspirin?
10-30g half life 15-30 hours
33
What is aspirin's effect on platelets?
Irreversibly inhibits platelet COX Low doses can irreversibly inhibit TXA2 production Prevents platelet aggregation
34
What are the clinical uses for aspirin?
Low dose - decreases incidence of TIAs, unstable angina, coronary artery thrombosis with MI and thrombosis after CABG Risk reduction for Preeclampsia
35
What are the side effects of aspirin?
GI pain, bleeding and ulcers Variable urate excretion Reye's syndrom in children w/ varicella
36
What is salicylism?
Mild intoxication with aspirin Characterized by tinnitis, high frequency hearing loss, headache, nausea, dimness of vision Reversible
37
What are the propionic acid derivative NSAIDs?
Ibuprogen, Naproxen
38
What is the MoA of Ibuprogen and naproxen?
Competitive, reversible active-site inhibitors of COX 1 and 2
39
What are the uses for for Ibuprogen and Naproxen?
Analgesic for mild pain Antipyretic Anti-inflammatory - symptoms of RA and osteoarthritis
40
What are the uses for ibuprofen?
Fever in children Dysmenorrhea Acute migrain attacks RA and osteoarthritis
41
What are uses for naproxen that ibuprofen can't be used for?
Acute gout Tendonitis Ankylosing spondylitis
42
What are the ADRs for Naproxen (Aleve)?
Increased risk of stroke/HA with prolonged use
43
What are the drug interactions with naproxen?
ACE inhibitors Antacids and Sucralfate (cation chelation)
44
What are the heteroaryl acetic acid derivative NSAIDs?
Ketorolac
45
What is the use for the ophthalmic prep of Ketorolac?
Seasonal allergy Recovery from cataract surgery
46
What are the other uses for Ketorolac?
Excellent analgesic action Used for postoperative pain
47
What are the ADRs for Ketorolac?
GI bleeding Bleeding Decreased hepatic function Lower dose in patients under 110 lbs or elevated creatinine
48
What are the contraindications for ketorolac?
History of peptic ulcer or GI bleeding Stop before surgery Concurrent use with aspirin or NSAID During labor/delivery or during lactation
49
What is the phenylacetic acid derivative NSAID?
Diclofenac
50
What are the uses for diclofenac?
RA, osteoarthritis and ankylosing spondylitis Primary Dysmenorrhea Postoperative pain and inflammation following cataract surgery
51
What is Arthrotec used for?
In patients with risk of gastric or duodenal ulcers Diclofenac + Misoprostol
52
What are the ADRs of Diclofenac (and Arthrotec)?
GI symptoms Modest ALT elevation Dizziness, Headache Arthrotec contraindicated in pregnancy Metabolized by Cyp2C9
53
What is oral indomethacin and its uses?
Indoel derivative, slightly specific for COX1 Acute gouty arthritis RA and osteoarthritis Tendinitis Ankylosing sponylitis
54
What is IV indomethacin used for?
Nonsurgical repair of patent ductus arteriosus Decreases PGE levels
55
What are the ADRs of Indomethacin?
GI pain - take with food Severe frontal headache Displacement of bilirubin from albumin Decreased urine output
56
What are the contraindications for indomethacin?
Hyperbilirubinemia Renal failure
57
What is celecoxib?
Selective COX-2 inhibitor
58
What are the uses for celecoxib?
RA and Osteroarthritis Ankylosing spondylitis Primary dysmenorrhea
59
What are the drug interactions of celecoxib?
Metabolized by P450 Cyp2C9 Fluconazole Inhibits 2D6
60
What are the ADRs of celecoxib?
GI pain Nausea
61
What are the effects of NSAIDs during pregnancy?
Inhibit uterine motility Induce bleeding in last trimester Premature closing of ductus arteriosus
62
What are the functions of PGE2 in the kidney?
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
What are the effects of NSAIDs on the kidney?
Hyperkalemia and Water Retention
64
What is the MoA of acetominophen?
Weak inhibitor of COX-1/2
65
What are the therapeutic uses for acetominophen?
MIld to moderate pain Preferred in children with viral fever
66
What are the ADRs of acetaminophen?
Hepatic toxicity (#1 drug cause) Renal toxicity with chronic use
67
What are DMARDs?
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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