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Inflammatory Response
Protects the body from injury and pathogens
Used chemical mediators to produce a reaction that helps
destroy pathogens and promotes healing
Salicylates
Can block the inflammatory response
Have antipyretic properties (fever-blocking)
Have analgesic (pain-blocking) properties
Therapeutic actions and indications
Pharmacokinetics
Contraindications and cautions
Adverse effects
Clinically important drug-to-drug interactions
Copyright 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Common Salicylates
Aspirin (Bayer, etc.): Treats inflammatory conditions
Balsalazide (Colazal): New drug treats ulcerative colitis
Choline magnesium trisalicylate (Trilisate): Treats mild
pain and fevers and arthritis
Choline Salicylate (Arthropan): Treats mild pain and fevers
as well as arthritis
Mesalamine (Pentasa and others): Treats inflammation of
the large intestine
Salicylates
Actions /Indications
Inhibit synthesis of prostaglandin, used to treat mild to
moderate pain and fever
Pharmacokinetics
Absorbed from the stomach, peak in 5-30 min.,
metabolized in the liver, excreted in the urine
Contraindications
Known allergy, bleeding abnormalities, impaired renal
function
Drug-to-Drug Interactions
Interact with other drugs by interfering with absorption
Copyright 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Prototype Salicylates
Question
Please answer the following statement as true or false.
Answer
True.
Rationale: Salicylates are some of the oldest antiinflammatory drugs used. They were extracted from
willow bark, poplar trees, and other plants by ancient
peoples to treat fever, pain, and what we now call
inflammation. They are generally available without
prescription and are relatively nontoxic when used as
directed. A person who does not respond to one salicylate
may respond to a different one.
Acetic Acids
Declofenac
Fenamates
Mefenamic acid
Cyclooxygenase-2
Inhibitors
Celecoxib
Etodolac
NSAIDs
Provide strong anti-inflammatory and analgesic effects
Sold over the counter, which may lead to abuse
Therapeutic actions and indications
Pharmacokinetics
Contraindications and cautions
Adverse effects
Clinically important drug-to-drug interactions
Prototype NSAIDs
Acetaminophen
Actions /Indications
Acts directly on the thermoregulatory cells of the
hypothalamus
Not sure of the mechanism of action related to analgesic
effects
Used to treat pain and fever
Treat pain and fever associated with a variety of
conditions, including influenza
Prophylaxis of children receiving diphtheriapertussis
tetanus (DPT) immunizations
Relief of musculoskeletal pain associated with arthritis
Copyright 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Acetaminophen (cont.)
Pharmacokinetics
Absorbed from GI tract
Peak to 2 hours
Metabolized in the liver
Excreted in the urine
T is about 2 hours
Contraindications
Known allergy
Use with caution in pregnancy and lactation
Copyright 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Acetaminophen (cont.)
Adverse Reactions
Headache, hemolytic anemia, renal dysfunction,
skin rash and fever
Hepatotoxicity usually associated with chronic
use and overdose
Drug-to-Drug Interactions
Oral anticoagulants increase bleeding
Question
When are NSAIDs contraindicated?
A. Allergy to penicillin
B. Allergy to sulfonamides
C. Allergy to antihistamines
D. Allergy to thiazines
Answer
B. Allergy to sulfonamides
Rationale: The NSAIDs are contraindicated in the presence
of allergy to any NSAID or salicylate/ Celecoxib is also
contraindicated in the presence of allergy to
sulfonamides.
Antiarthritis Agents
Potentially debilitating inflammatory process
Antiarthritis drugs
Prevent and suppress arthritis in selected patients with
rheumatoid arthritis
Gold Compounds
Indications/Action
Absorbed by macrophages, which results in inhibition of
phagocytosis
Tissue destruction is decreased
Pharmacokinetics
Absorptions varies based on site of administration
Widely distributed throughout the body
Contraindications
Known allergy
Diabetes, CHF, renal or hepatic impairment
Pharmacokinetics
Absorbed at varying rates
Excreted in urine and feces
Cross the placenta and cross into breast milk
Barrier contraceptives