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Therapeutics > NSAIDs > Flashcards

NSAIDs Flashcards

1
Q

Signs of inflammation

A

SLHRP
Swelling, Loss of function, heat, redness and pain

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2
Q

Fill in the Eicosanoids Effects

A
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3
Q

When Eicosanoids bind to GPCRs in the target cells, the generation of what causes dilation? Constriction?

A

Generation of cAMP (Gs) = dilation
Release of calcium (Gq) = constriction

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4
Q

20-carbon polyunsaturated fatty acid that is the most abundant and important precursor of eicosanoids

A

Arachidonic acid

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5
Q

On Arachidonic acid, which carbon has an inflammatory effect?

A

6 carbon

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6
Q

PGH synthase has both ____ & _____ activities

A

COX and hydroperoxidase

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7
Q

“Housekeeping” function; COX 1
Constitutively expressed in various tissues

A

PGH synthase-I

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8
Q

Expressed upon stimulus in inflammatory and immune cells
COX 2
Stimulated by growth factors, tumor promoters, and cytokines

A

PGH synthase-2

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9
Q

What are PGH synthase 1 and 2 inhibited by?

A

NSAIDS

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10
Q

Synthesis of prostaglandins

A
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11
Q

What classification of drug is this?
PGE1
Relaxes smooth muscles and expand blood vessels
Used for erectile dysfunction by injection or as a suppository

A

Alprostadil
Eicosanoid drugs

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12
Q

What classification of drug is this?
PGE1 derivative; Cytoprotective
Prevents peptic ulcer
Terminates early pregnancy in combo with mifepristone

A

Misoprostol
Eicosanoid drugs

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13
Q

What classification of drug is this?
Topically active PGF2a derivative (prodrug)
Constrict blood vessels
Used in ophthalmology to treat high pressure inside the eye

A

Latanoprost
Eicosanoid drugs

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14
Q

What classification of drug is this?
PGI2; powerful vasodilator
Inhibitor of platelet aggregation
Used to treat pulmonary arterial hypertension by IV injection or inhalation
Should not be used with anticoagulants

A

Prostacyclin (epoprostenol)
Eicosanoid drugs

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15
Q

NSAIDs mechanism of action: inhibition of ____ & _______

A

prostaglandin and COX 1 and 2

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16
Q

Side effects of NSAIDs

A

Blood coagulation, hypersensitivity, Reye’s

17
Q

Synthetic PGE1 analog
Used prophylactically to prevent NSAID-induced gastric ulcers in patients at high risk

A

Misoprostol

18
Q

Many NSAIDs are highly bound to _____ ______

A

serum albumin

19
Q

Absorbed as an ionic form from the small intestine and, to lesser extend, from the stomach as an acid form
Inhibits COX 1 and 2 reversibly
May suppress COX-2 induction

A

salicylates

20
Q

The only NSAID that irreversibly inhibits COX by acetylating a serine residue in the active site

A

Aspirin (acetylsalicylic acid)

21
Q

What classification of drug is this?
Dimer of this group
Hydrolyzed to two salicylates in the small intestine and absorbed
Does not cause GI bleeding

A

Salsalate (Disalcid)
Salicylates

22
Q

What classification of drug is this?
More potent analgeic than aspirin but produces fewer side effects
Less antipyretic activity than aspirin
3-4 fold longer half life than aspirin

A

Diflunisal (Dolobid)
Salicylates

23
Q

What classification of drug is this?
One of the most potent NSAIDs in use
High incidence of side effects; not suitable for a long-term use
Not stable in solution due to the hydrolysis of the amide bond

A

Indomethacin
Arylacetic acid

24
Q

What classification of drug is this?
Prodrug; the sulfoxide group id reduced to the active sulfide intermediate in the circulatory system
Less GI side effects
Suitable for a long-term use to treat chronic inflammation

A

Sulindac
Arylacetic acids

25
Q

What classification of drug is this?
Pyranocarboxylic acid
As potent as indomethacin
Somewhat selective for COX-2
Less GI bleeding; suitable for long-term use to manage osteoarthritis

A

Etodolac
Arylacetic acids

26
Q

What classification of drug is this?
The most widely used NSAID in the world
As potent as indomethacin
Somewhat selective for COX-2
Inhibits both COX and lipoxygenase pathways

A

Diclofenac
Arylpropionic acid

27
Q

Popular OTC analgesic
More potent than aspirin, but less than indomethacin
Moderate degrees of gastric irritation
Bioequivalent racemic mixture

A

Ibuprofen
Arylpropionic acid

28
Q

S-(+)-enantiomer; more potent than ibuprofen
Moderate degrees of gastric irritation
Used to treat rheumatoid arthritis and osteoarthritis

A

Naproxen (Aleve)

29
Q

Cyclized heteroarylpropionic acid derivative
Short-term management of moderate to severe pain
Analgesic activity similar to centrally acting analgesics
Widely accepted alternative to narcotic analgesics

A

Ketorolac

30
Q

What classification of drug is this?
Nonacidic prodrug
Metabolized rapidly which is an effective inhibitor of COX
Minimum gastric side effects
Potent anti-inflammatory, but weak analgesic activity

A

Nabumetone
Non-carboxylate

31
Q

What classification of drug is this?
Belongs to the oxicam class, which resembles the peroxy radical intermediate in COX
Enolic acid
Long acting; single daily dose; somewhat COX-2 selective
As potent as indomethacin

A

Meloxicam

32
Q

Preferential inhibition of _____ gives anti-inflammatory effects with lower incidence of gastric ulceration

A

COX-2

33
Q

What is the suffix for COX-2 inhibitors?

A

(-coxib)

34
Q

First NSAID to be marketed as selective COX-2 inhibitor
Used for osteoarthritis and rheumatoid arthritis
Good efficacy against pain, inflammation, and fever
As potent as naproxen; less risk of GI side effects; no antiplatelet activity

A

Celecoxib (Celebrex)

35
Q

Analgesic and antipyretic effects similar to aspirin but with fewer adverse effects
not NSAID
Much weaker as an anti-inflammatory agent

A

Acetaminophen

Therapeutics (16 decks)

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