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Analgesics and Antipyretics
N/A
41
Pharmacology
Graduate
01/10/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
NSAIDs are effective against what type of pain?
Definition
Low to moderate intensity
Term
FCT of NSAIDS
Definition
Analgesics, Antipyretics (via IL-1 block), anti-inflammatory, primary dysmenorrhea, PDA, colon cancer prevention.
Term
Side effects of NSAIDs
Definition
GI ulceration and intolerance, Blockage of platelet aggregation (via inhibition of TXA2), inhibition of uterine motility, inhibition of prostaglandin-mediated renal effects--> nephritis and papillary necrosis, Hypersensitivity (asthma, urticaria, angioedema, cross reactivity)
Term
The only analgesic that causes irreversible inhibition of platelet aggregation
Definition
Aspirin: acetylates COX
Term
Use and Mechanism of Action of Aspirin
Definition

Use: analgesic, antipyretic, anti-inflammatory

MOA: inhibit PG synthesis by irreversible acetylation of COX

Term
How long does aspirin's effect on platelets last?
Definition
The entire platelet life (8-10days)
Term
Side effects of COX inhibitors not seen in Selective COX 2 inhibitors
Definition
GI ulceration, inhibition of platelet fct
Term

Aspirin

Route of Administration

Half life

Elimination

Side Effects

Use

Definition

ROA: Oral

t 1/2: 15-30 min

Excreted as salicyluric acid by kidney

 

Tinnitus or deafness (early sign of toxicity)

Transient decrease in renal fct, GI intolerance, hepatotoxicity, Salicylate intoxication, hypersensitivity

 

Use: juvenile rheumatoid arthritis, MI, colon cancer prevention

 

Term
Salicylate toxicity
Definition

Disturbance of acid-base balance leading to respiratory alkalosis and metabolic acidosis

 

Sx: Headache, dizzy, ringing in ear, mental confusion, drowsiness and sweating

Term
Contraindications of Aspirin use
Definition
Gout, ulcer, asthma, influenza (Reye's Syndrome)
Term
Duflunisal
Definition

Diflurophenyl derivative of salicylic acid

 

More potent anti-inflammatory fct than aspirin but no antipyretic and poor penetration to CNS

 

Less auditory side effects than aspirin

Term
Mesalamine
Definition

Salicylate used for local effect on IBD

 

Asacol (effective in ulcerative colitis)

Term

Acetaminophen

Use:

Route of Admin:

t 1/2:

Side Effect:

 

Definition

Use: Analgesic and antipyretic. NOT ANTI-INFLAMMATORY

ROA: Oral

t 1/2: 1-4 hr

Side Effects: Fatal hepatic necrosis due to toxic metabolite

 

Term
N-acetylcysteine
Definition
Antidote for hepatic toxicity seen in acetominophen. Gives a cysteine to help make glutathione, which detoxifies N-acetyl-Beta-benzoquinone imine. 
Term

Indomethacin

ROA:

Use:

t 1/2:

Side Effects:

Definition

ROA: Oral rapid absorption in GI

Use: Acute gout and ankylosing spondylitis, tx PDA in premature infants

t 1/2: 2-3 hour

Side Effects: Nausea, vomiting, anorexia, abdominal pain, frontal headache associated with dizziness, confusion and depression.

 

Term
What prohibits renal secretion of Indomethacin
Definition
Probenecid
Term

Sulindac

Use:

t 1/2:

Side effects:

Definition

Pro-drug with sulfide derivative as active metabolite

Suppress polyp formation in colon cancer, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis

t 1/2: 7 hours for pro-drug and 18 hours for active

Side effects: Renal stone

Less ulceration, GI irritation and blood loss than with aspirin. 

Term

Tolmetin

Use:

Side Effects:

 

Definition

Heteroaryl Acetic Acid Derivative

Use: juvenile rheumatoid arthritis

Side Effects: Epigastric pain, N/V

Term

Diclofenac

MOA:

Route:

T 1/2:

Side effects:

Definition

Reduce synthesis of both PGs and leukotrienes

Oral

2 hour

 

Increased hepatic transaminase, not recommended for children, nursing mothers, or pregnant women

Less likely than aspirin to cause peptic ulcer and GI bleed

Term

Ketorolac

MOA

Use:

Definition

NSAID with analgesic activity. PG synthesis inhibition.

Use: <5 days for management of moderately to severe acute pain

 

Term

Ibuprofen

Use:

Route:

t 1/2:

 

Definition

Mild inflammatory and analgesic drug with reduced gastric irritation

 

Route: Oral, protein bound, extensively metabolized in liver

 

t1/2: 2 hr

Term

Naproxen

Use:

Route:

t 1/2:

Side effects:

Definition

Use: Only propionic acid derivative approved for ankylosing spondylitis and juvenile RA as well as acute gout. 20x more potent than aspirin

 

Route: Oral; high protein bound excreted entirely in urine

 

t 1/2: 14 hour

Side effects: Crosses the placenta and appears in milk of lactating women

Term

Ketoprofen

MOA:

t 1/2

Side effects

Definition

MOA: Inhibits COX and lipoxygenase

t 1/2: 2 hr

Side Effects: GI, CNS

Term

Oxaprozin

 

Definition

Propionic Acid Derivative

t 1/2 40-60 hours

Term
Salicylates
Definition
Aspirin, Diflunisal, Mesalamine
Term
Para-Aminophenol Derivatives
Definition
Acetaminophen
Term
Indole derivatives
Definition
Indomethacin, Sulindac
Term
Heteroaryl Acetic Acid Derivatives
Definition
Tolmetin, Diclofenac, Ketorolac
Term
Arylproprionic Acid Derivatives
Definition
Ibuprofen, Naproxen, Ketoprofen, Oxaprozin
Term
Enolic Acids
Definition
Piroxicam, Mecloxicam
Term
Piroxicam
Definition

 t 1/2: 50-60 hr

COX inhibitor

Term
Meloxicam
Definition

Inhibits COX-2>>>COX -1

t 1/2: 20 hr

Tx: osteoarthritis

Term
Nabumetone
Definition

Alkanone

Only nonacid NSAID in use

Ketone prodrug converted to acetic acid derivative

 

Preferentially inhibits COX-2

t 1/2: 24 hour

 

GI ulceration much lower than other NSAIDS

Term
COX-2 inhibitors
Definition
Celecoxib, Rofecoxib, Valdecoxib
Term
Celecoxib
Definition

COX-2 selective inhibitor

First one on the market. At therapeutic concentrations COX-1 is not inhibited.

 

Causes less ulcers than naproxen or ibuprofen and does not affect platelet aggregation

 

TX: osteo- and rheumatoid arthritis

Term
Abatacept
Definition

Inhibits T cell activation

 

Tx: Adult rheumatoid arthritis and juvenile idiopathic arthritis in patients who are refractory to other regimens of NSAIDs

 

IV injection

Term
Rituximab
Definition

Chimeric monoclonal antibody for CD20 B lymphocytes

 

Used when other NSAIDs fail.

 

Side effect: fatal infusion rxn within 24 hours of IV

Term
Etanercept
Definition

Binds to TNF and blocks interaction with TNF receptors

 

t 1/2: 4.5 days

 

Route: Sub Q

Use: When other NSAIDS are refractory

Term
Adalimumab
Definition

Binds to TNF-alpha and blocks interaction with p55 and p75 cell surface TNF receptors

Given SC

t 1/2: 10-20 days so given every other week

Side effects: TB, invasive fungal diseases and other opportunistic infections

Term
Infliximab
Definition

Neutralizes TNF-alpha by binding to soluble and membrane bound ones and inhibiting the binding to receptors.

 

Increased risk of infections including progression. 

 

T 1/2: 9-12 days

Given IV every 8 weeks

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