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Nonnarcotic Analgesics
Clinical Indication
Prevent or interrupt mild to moderate pain associated with inflammatory conditions without altering consciousness (analgesic, antiinflammatory)
Pain quality is often described as a dull ache in joint pain (osteoarthritis, gout) muscle pain (myalgia) headache (nonmigraine)
Sensation of Pain
Pain is composed of at least two elements
localized stimulation of peripheral nerves through damage or inflammation recognition of pain within the CNS
Mechanism of Action
Nonnarcotic analgesics relieve pain by selectively inhibiting prostaglandin synthesis (prostaglandin synthetase) centrally (hypothalamus) and peripherally
Prostaglandins stimulate peripheral nerve endings producing pain impulses that are carried to the CNS (prostaglandin G2 & H2) enhance local inflammation (prostaglandin E2) produce localized edema (E2) constrict blood vessels (local ischemia, G2 & H2)
Pharmacological Effects
Gastrointestinal Nausea due to erosion of stomach lining
Decrease prostaglandin cytoprotective mucus secretion
Acetaminophen
Weak prostaglandin synthetase inhibitor Useful for reducing fever and headache (nonmigraine) Should not substitute for antiinflammatory drugs Does not affect platelet aggregation/clotting May be used as an aspirin substitute in aspirin-sensitive patients
Special Caution
Aspirin and acetaminophen in children and teenagers who have active viral infections (flu or chicken pox) may result in Reyes syndrome, potentially life-threatening
Antigout Drugs
Clinical Indication
Treatment of gout, a special inflammatory condition in which uric acid deposits in the joint fluid of the toes, knees, or kidneys because uric acid is overproduced or not efficiently excreted
Phagocytes digest the uric acid and set up a cycle of localized inflammation
Antigout Drugs
Drugs in this class include Acute treatment Colchicine Aspirin, naproxen
Prophylaxis Allopurinol blocks uric acid production Probenecid for uric acid excretion Sulfinpyrazone for uric acid excretion
Drug Interactions
NSAIDs are highly bound to albumen and will displace other drugs from these binding sites causing increased concentration of active drugs in the blood such as Oral anticoagulants, e.g., warfarin Antibiotics, Anticonvulsants, Methotrexate
Increased risk of hepatotoxicity when given with alcohol, barbiturates, anticonvulsants, rifampin
Immunomodulating Agents
Immunosuppressive drugs decrease the activity of the immune system and are useful in severe allergic and inflammatory conditions, and in the prevention of organ rejection following transplantation Immunostimulant drugs activate the immune system and increase the ability of the body to resist infection and the growth of abnormal cancer cells
Immune Cells
Macrophages initiate the immune response Helper T-cells activate other T- and B-cells Killer T-cells attack and kill infectious organisms B-cells produce antibodies Suppressor cells inhibit the immune system Memory cells retain immunogenic information and provide long-term immunity
Immunosuppressant Drugs
Corticosteroid Drugs
Derivatives of adrenocorticosteroid hormones produced by the adrenal cortex Used to suppress the immune system in severe allergy, inflammation, and prevent rejection following organ transplantation Prednisone and prednisolone are two widely used corticosteroid drugs Corticosteroids are often used in combination with other immunosuppressant drugs
Immunostimulant Drugs
Alpha-, Beta-, and Gamma-interferon are antiviral factors normally produced by activated immune cells, they are used as drugs to activate the immune system in certain viral infections and cancers Interleukin-2 is an immune factor normally produced by lymphocytes, it is used as a drug to activate the immune system in certain cancers