Anti-inflammatory,

Anti-arthritis, and
Related Agents
Anti-inflammatory Agents
• Generally block or alter the chemical reactions
associated with inflammatory response to stop
one or more of the signs and symptoms of
inflammation.
• Salicylates
• NSAIDS
Salicylates
• Are popular anti-inflammatory agents not only
because of their ability to block the
inflammatory response, but also because of their
antipyretic (fever-blocking) and analgesic (pain-
blocking) properties.
Salicylates
Aspirin
Balsalazide
Choline magnesium trisalicylate
Diflunisal
Mesalamine
Olsalazine
Salsalate
Sodium thiosalicylate
Salicylates
• Therapeutic actions and Indications:
• Inhibit the synthesis of prostaglandin, an
important mediator of the inflammatory reaction.
• Antipyretic effect may be r/t blocking of
prostaglandin mediator of pyrogens (chemicals
that cause an increase in body temperature and
that are released by active WBCs) at the
thermoregulatory center of the hypothalamus.
Salicylates
• Therapeutic actions and Indications:
• Aspirin also affects platelet aggregation by
inhibiting the synthesis of thromboxane A2, a
potent vasoconstrictor that normally increases
platelet aggregation and blot clot formation.
• Indicated for the treatment of mild to moderate
pain, fever, and numerous inflammatory
conditions, including rheumatoid arthritis and
osteoarthritis.
• Also indicated for TIA (or stroke) and MI.
Salicylates
• Contraindications and Cautions:
• Allergy to salicylates and NSAIDs
• Bleeding abnormalities
• Impaired renal function
• Chickenpox and influenza – Reye syndrome
• Surgery or other invasive procedures scheduled
within 1 week
• Pregnancy and lactation
Salicylates
• Adverse effects:
• GI: nausea, dyspepsia, heartburn, epigastric
discomfort
• Clotting system: blood loss, bleeding
abnormalities
• Salicylism: dizziness, ringing in the ear, difficulty
hearing, nausea, vomiting, diarrhea, mental
confusion, and lassitude
Nonsteroidal Anti-inflammatory
and Related Agents
• NSAIDs = provide strong anti-inflammatory and analgesic
effects without the adverse effects associated with the
corticosteroids.
• Acetaminophen has antipyretic and analgesic properties but does
not have the anti-inflammatory effects of the salicylates or the
NSAIDs.
Nonsteroidal Anti-inflammatory and Related Agents
Propionic acid Fenoprofen
Flurbiprofen
Ibuprofen
Ketoprofen
Naproxen
Oxaproxin
Acetic acids Diclofenac
Etodolac
Indomethacin
Ketorolac
Nabumetone
Sulindac
Tolmetin
Fenemates Meclofenamate
Mefenamic acid
Oxicam derivatives Meloxicam
Piroxicam
Cyclooxygenase-2 Inhibitors Celecoxib
Related agent Acetaminophen
Nonsteroidal Anti-inflammatory
and Related Agents
• Therapeutic actions and Indications:
• NSAIDs block two enzymes: COX-1 and COX-2
• COX-1 is present in all tissues, and involved in blood
clotting, protecting the stomach lining, and
maintaining sodium and water balance in the kidneys.
• COX-2 is active at sites of trauma or injury when more
prostaglandins are needed, but it does not seem to be
involved in other tissue functions.
• Most NSAIDs block both the enzymes – changes
in GI integrity, blood clotting, and water and Na
balance.
Nonsteroidal Anti-inflammatory
and Related Agents
• Therapeutic actions and Indications:
• NSAIDs are indicated for signs and symptoms of
rheumatoid arthritis and osteoarthritis, for relief of
mild to moderate pain, for treatment of primary
dysmenorrhea, and for fever reduction.
Nonsteroidal Anti-inflammatory
and Related Agents
• Contraindications and Cautions:
• Allergy to NSAIDs and salicylates
• Celecoxib = allergy to sulfonamides
• Cardiovascular dysfunction or hypertension
• Peptic ulcer or known GI bleeding
• Pregnancy and lactation
• Renal and hepatic dysfunction
Nonsteroidal Anti-inflammatory
and Related Agents
• Adverse Effects:
• GI: nausea, dyspepsia, GI pain, constipation, diarrhea, or
flatulence
• Blood: bleeding, platelet inhibition, bone marrow
depression
Nonsteroidal Anti-inflammatory
and Related Agents
• Acetaminophen
• Is most frequently used drug for managing pain and fever in
children.
• Available OTC drug.
• Can cause severe liver toxicity

• Therapeutic action:
• Acts directly on the thermoregulatory cells in the
hypothalamus to cause sweating and vasodilation; in turn
causes the release of heat and lowers fever.
• Indication:
• Treatment of pain and fever (influenza, DPT immunization,
arthritis)
Nonsteroidal Anti-inflammatory
and Related Agents
• Acetaminophen
• Contraindications and Cautions:
• Allergy
• Pregnancy or lactation
• Hepatic dysfunction
Nonsteroidal Anti-inflammatory
and Related Agents
• Acetaminophen
• Adverse effects:
• Hepatotoxicity
• Headache, hemolytic anemia, renal dysfunction, skin
rash, and fever
• Antidote: Acetylcysteine (Mucomyst)
Antiarthritis Agents
• They block the inflammatory process in the joints, that cause
pain and bone deformities.

• Chrysotherapy = the use of gold salts w/c can be taken up by

macrophages, w/c then inhibit phagocytosis.
• Auranofin
• Aurothioglucose
• Gold sodium thiomalate

• Therapeutic actions:
• Chrysotherapy results in inhibition of phagocytosis. The
release of lysosomal enzymes is inhibited and tissue
destruction is decreased.
Antiarthritis Agents
• These drugs do not repair damage; they prevent further
damage and so are most effective if used early in the disease.

• Contraindications:
• Allergy to gold
• Pregnancy and lactation
Disease Modifying
Antirheumatic Drugs
(DMARD)
• Are only indicated early in the diagnosis, before
damage to the joints has occurred.
• Anakinra
• Etanercept
• Leflunomide
• Penicillamine
• Hyaluronidase
• Sodium hyaluronate
• Antineoplastic (Methotrexate, Cyclophosphamide)
• Monoclonal antibodies (Infliximab, adalimumab)
Disease Modifying
Antirheumatic Drugs
(DMARD)
• Anakinra = is an interleukin-1 receptor antagonist. It blocks
the interleukin-1, w/c is responsible for the degradation of
cartilage in rheumatoid arthritis.
• Etanercept = a genetically engineered TNF receptors. These
receptors react w/ free-floating TNF released by active
leukocytes in autoimmune inflammatory disease.
• Hyaluronidase = have elastic and viscous properties. These
are injected directly into the joints of patients w/ severe
rheumatoid arthritis of the knee. They seem to cushion and
lubricate the joint and relieve the pain.
• Penicillamine = lowers the immunoglobulin M (IgM)
rheumatoid factor levels in patients with acute rheumatoid
arthritis.
Disease Modifying
Antirheumatic Drugs
(DMARD)
• Contraindications and Cautions:
• Allergy to the drugs
• Allergy to hamster and chicken
• Pregnancy and lactation
• Liver or renal impairment