Anti-Inflammatory,
Antiarthritis, and
Related Agents
Chapter 16
Inflammatory Response
• Protects the body from injury and pathogens
• Used chemical mediators to produce a reaction that helps destroy
pathogens and promotes healing
• Signs of inflammation
 Swelling
 Fever (heat)
 Pain
 Pus
Anti-Inflammatory, Antiarthritis,
and Related Agents
• Several different types of drugs
• Corticosteroids
• Block or alter the chemical reactions associated with the
inflammatory response
• Over-the-counter (OTC)
• Adverse effects
Salicylates
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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
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
Common Salicylates (cont.)
• Olsalazine (Dipentum): Converted to mesalamine in the colon; has
the same direct anti-inflammatory effects
• Salsalate (Argesic and Others): Used to treat pain, fever, and
inflammation
• Sodium Thiosalicylate (Rexolate): Treats episodes of acute gout
and muscular pain, and rheumatic fever
Salicylates
• Actions /Indications
– Inhibit synthesis of prostagladin, 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
Salicylates
• Adverse Effects
– GI upset
– Bleeding
– Salicylism – dizziness, tinnitus,
N/V/D, confusion
• Salicylate Toxicity:
– Hyperpnea, tachypnea,
hemorrhage, excitement,
confusion, pulmonary edema,
convulsions, tetany, metabolic
acidosis, fever, coma, CV, renal,
respiratory collapse
Prototype Salicylates
Question
Please answer the following statement as true or false.
A person who does not respond to one salicylate may respond to a
different one.
Answer
True.
Rationale: Salicylates are some of the oldest anti-inflammatory 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.
NSAIDs
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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
Nonsteroidal Anti-inflammatory and Related
Agents
•Inhibit prostaglandin synthesis
– Anti-inflammatory, antipyretic, analgesic effects
•Block two enzymes:
– COX 1 – present in all tissues
• Involved in blood clotting, protecting stomach lining, and
maintaining sodium & water balance
– COX 2 – active at sites of trauma or injury
•Adverse effects:
– R/T blocking of these 2 enzymes:
• GI integrity changes, bleeding, sodium & water retention
• May block vasodilation – CV problems
Nonsteroidal Anti-inflammatory and Related
Agents
• Analgesia (mild to moderate), Antipyretic, Osteoarthritis, RA,
Dysmenorrhea
• Contraindications
– Allergy to NSAIDs/salicylates or sulfonamides for Celebrex
– Cardiac, hepatic, renal dysfunction
– Peptic ulcer or GI bleeding
– Pregnancy, lactation
Nonsteroidal Anti-inflammatory and Related
Agents
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Propionic acids – ibuprofen, naproxen
Acetic acids – indomethacin, ketorolac (Toradol)
Fenamates – meclofenamate
Oxicam derivative – meloxicam (Mobic)
COX 2 Inhibitor – celecoxib (Celebrex)
Nursing Implications:
– Watch for any unusual bleeding, such as in the stool
– Enteric-coated tablets should not be
crushed or chewed
– Take with food to avoid GI irritation
– Therapeutic effects may not be seen for 3 to 4 weeks
Nonsteroidal Anti-inflammatory and Related
Agents
• Adverse Effects
– Nausea, dyspepsia, GI pain, constipation, diarrhea, flatulence, GI
bleed
– Headache, dizziness, fatigue
– Bleeding, platelet inhibition, HTN, bone marrow depression
• Drug-Drug Interactions
– Decreased loop diuretic effect
– Decreased effect of beta blockers
– Lithium toxicity
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 diphtheria–pertussis–tetanus
(DPT) immunizations
• Relief of musculoskeletal pain associated with arthritis
Acetaminophen
• Contraindications
– Caution in liver dysfunction or chronic alcoholism
• Adverse Reactions
– HA, hemolytic anemia, skin rash & fever
– Hepatotoxcity
– Antidote: acetylcysteine
• Drug-to-Drug Interactions
– Oral anticoagulants increase bleeding
– Liver toxicity with ETOH, barbituates, carbamazepine, hydantoins,
rifampin
Acetaminophen (cont.)
• Pharmacokinetics
– Absorbed from GI tract
– Peak ½ to 2 hours
– Metabolized in the liver
– Excreted in the urine
– T ½ is about 2 hours
• Contraindications
– Known allergy
– Use with caution in pregnancy and lactation
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
(Chrysotherapy)
• Indicated to treat selected cases of:
– Rheumatoid arthritis
– Juvenile rheumatoid arthritis
– In patients whose disease has been unresponsive to standard
therapy
• Indications/Action
– Absorbed by macrophages, which results in inhibition of
phagocytosis
– Tissue destruction is decreased
Gold Compounds (cont.)
• Pharmacokinetics
– Absorptions varies based on site of administration
– Widely distributed throughout the body
• Excreted in urine and feces
• Cross the placenta and cross into breast milk (Barrier
contraceptives)
• Contraindications
– Known allergy
– Diabetes, CHF, renal or hepatic impairment
Gold Compounds (cont.)
• Adverse Reactions
– Stomatitis, glossitis, gingivitis, bone marrow depression,
dermatitis
• Drug-to-Drug Interactions
– Do not combine with: Penicillamine, Antimalarials , Cytotoxic
drugs, Immunosuppressive agents
Prototype Gold Compound
Disease Modifying AntiRheumatic Drugs
• Available for treating arthritis by blocking the process of inflammation
• They alter the course of the inflammatory process
• Therapeutic Actions and Indications
– Some restrict the immune system
– Some block pathways inside select immune cells
– Some work on cytokines
Disease Modifying AntiRheumatic Drugs (DMARDs)
SQ meds:
– Anakinra (Kineret) – stops cartilage degradation
• Etanercept (Enbrel) – prevents damage of TNF
PO meds:
• Leflunomide (Arava) – blocks enzyme contributing to inflammatory
process
• Penicillamine (Depen) – decreases rheumatoid factor decreasing
inflammation
Knee injections: weekly for 3-5 weeks
– Hyaluronidase derivative (Synvisc)
– Sodium hyaluronidase (Hyalgan)
Disease Modifying AntiRheumatic Drugs
• Antineoplastics (chemotherapy)
– Methotrexate
– Cyclophosphamide
• Monoclonal antibodies
– Infliximib (Remicade)
– Adalimumab (Humira)
• T cell suppressors
– Abatacept (Orencia)
• Immune modulators
– Cyclosporine A
– Azathioprine
• Antimalarials
Nursing Considerations for
Patients Receiving Antiarthritis
Agents
• Similar to those for patients receiving NSAIDS and related agents
Drug Therapy Across the
Lifespan
IN REVIEW
NCLEX-style questions
• Nursing program exam questions differ because they ask you to
APPLY what you have learned (as opposed to showing your
comprehension).
– Your PrepU homework assignments use NCLEX style
questions…these are a good example of how your exams will
look.
– At the end of some chapter’s PPT will be questions to help you
apply what you have learned to real-life concepts.
• Answers will be found after the questions
Application Review #1
What are the therapeutic actions of salicylates and NSAIDs?
Application Review #2
Why is aspirin contraindicated in children with viral illnesses? If the
child has a fever and cannot use aspirin, what antipyretic would be
recommended?
Answers
Application Review #1
What are the therapeutic actions of salicylates and NSAIDs?
• Salicylates and NSAIDs work by inhibiting the synthesis of
prostaglandin, an important mediator of the inflammatory process.
Application Review #2
Why is aspirin contraindicated in children with viral illnesses? If the
child has a fever and cannot use aspirin, what antipyretic would be
recommended?
• Aspirin is contraindicated due to risk of Reye’s syndrome.
Acetaminophen is a recommended alternative to aspirin.