anti-inflammatory drugs. insert inflammation diagram
TRANSCRIPT
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Anti-InflammatoryDrugs
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Insert Inflammation Diagram
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Analgesics, Anti-inflammatories and Anti-gout Agents
This group is comprised of drugs that reducemild to moderate pain (analgesic) • of a different type or quality than narcotics and• by a different mechanism than the narcotic analgesics
The analgesics within this group are not interchangeable for the relief of pain associatedwith gout, muscle ache, or muscle ischemia
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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)
Reduce elevated body temperature (fever) (antipyretic)
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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
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Nonnarcotic analgesics relieve pain byselectively 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)
Mechanism of Action
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Nonnarcotic analgesics differ in their chemical class and ability to produce analgesia, antipyresis, and/or be antiinflammatory
• N-acetyl-p-aminophenol acetaminophen
• Salicylates aspirin, diflusinal
• Synthetic nonsteroidal antiinflammatory (NSAID)–Naprosyn - Naproxen–Fenoprofen - Nalfon–Ibuprofen- Advil, Motrin–Indomethacin - Indocin
Types of Nonnarcotic Analgesics
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Salicylates & Aspirin
Oldest group, from willow bark, known to
• reduce fever and pain
• increase peripheral blood flow (vasodilation)
•prophylactically inhibit clotting
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Gastrointestinal • Nausea due to erosion of stomach lining• Decrease prostaglandin cytoprotective mucus secretion
Cardiovascular• Inhibit platelet aggregation & clot formation• Reduce the risk of death & reinfarction following myocardial infarction
Pharmacological Effects
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Salicylates Adverse Effects• Nausea, heartburn, dyspepsia
• Vomiting
• Gastrointestinal bleeding
• Prolong bleeding time
• Hepatoxicity (elevated serum enzymes)
• Hypersensitivity (in sensitive patients)- rash, laryngeal edema, asthma
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Nonsteroidal Antiinflammatory Drugs (NSAIDs)
• reduce pain associated with inflammation
• are not steroids (e.g. cortisone)
• include aspirin and salicylates
• are useful in the management of
o headache (nonmigraine)
o muscle aches and pain,
o Dysmenorrhea
o joint pain of osteoarthritis
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Nonsteroidal Antiinflammatory Drugs (NSAIDs)
Inflammation is characterized by local
• swelling (edema)
• redness (erythema, vasodilation)
• warmth
• pain
Intermediated by prostaglandins (G2, H2, E2, F2ά)
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NSAIDs Mechanism of Action
Inhibit inflammation and reduce pain by
blocking the synthesis of prostaglandins
Stabilize cell membranes to prevent further
leakage of substances (edema)
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NSAIDs Adverse Effects• Nausea
• Gastrointestinal distress, ulceration,bleeding
• Vomiting
• CNS stimulation
• Headache
• Vertigo
• Mental confusion
• Hypersensitivity reactions (rash, fever)
• Hepatic damage (elevated serum enzymes)
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NSAIDs Special ConsiderationsAspirin sensitive patients may develop• anaphylactic reactions• angioedema• asthma
Chronic toxicity is the same as for aspirin• tinnitus• gastrointestinal bleeding• black tarry stools
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Chronic Salicylate Toxicity
Salicylism is a constellation of symptoms that
occur in some patients with the chronic use of
large doses of aspirin and other salicylates
• Nausea• Vomiting• Headache• Tinnitus (ringing in the ears)• Hyperglycemia• Delirium
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Acute Salicylate Poisoning
Accidental ingestion of a large dose bychildren or attempted suicide may produce
» Depression of respiratory centers» Respiratory acidosis» CNS depression» Sweating» Dehydration, electrolyte imbalance» Hypotension & vasodilation» Coma» Death
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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
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Acetaminophen Adverse Effects
Acute toxicity
• Nausea
• Vomiting
• Hepatoxicity (elevated serum enzymes)
• Acidosis
• Respiratory depression
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Special Caution
Aspirin and acetaminophen in children and
teenagers who have active viral infections
(flu or chicken pox) may result in Reye’s
syndrome, potentially life-threatening
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Insert Gout Diagram
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Antigout DrugsClinical 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
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Antigout DrugsDrugs 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
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Drug InteractionsNSAIDs are highly bound to albumen and will displace other drugs from these binding sitescausing increased concentration of active drugs in
the blood such as – Oral anticoagulants, e.g., warfarin– Antibiotics, Anticonvulsants, Methotrexate
Increased risk of hepatotoxicity when given withalcohol, barbiturates, anticonvulsants, rifampin
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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
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Insert Immune Diagram
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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
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Immunosuppressant Drugs
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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
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Cytotoxic Immunosuppressant Drugs
• Azathioprine inhibits the synthesis of immune cell DNA and is mainly used to prevent organ transplant rejection
• Cyclophosphamide is an alkylating drug used in immune-based diseases to decrease antibody production by B-cells
• Mycophenolate inhibits T- and B-cell activity and is used to prevent renal organ transplant rejection
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Noncytotoxic Immunosuppressant Drugs
• Cyclosporine inhibits the function of interleukin-2 and is widely used to prevent organ rejection following transplantation
• Tacrolimus is similar to cyclosporine in action and clinical usage
• Leflunomide inhibits the synthesis of DNA in T- and B-cells and is indicated for the treatment of rheumatoid arthritis
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Immunosuppressive Monoclonal Antibodies
• Muromonab-CD3 binds to and inhibits the action of T-cells involved in organ transplant rejection
• Daclizumab binds to and blocks the interleukin-2 receptor; it is used to prevent renal allograft rejection
• Infliximab inhibits TNF-alpha which is an inflammatory factor active in Crohn’s disease
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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
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