ANTI-INFLAMMATORY DRUGS (s) Flashcards by Love Dog

Q

these secrete cytokines, tumor necrosis factor (TNF), interleukin (IL-1) into synovial cavity

A

monocytes and macrophages;

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Q

will cause:

o increased cellular infiltrations into endothelium due to the
release of histamines, kinins, and prostaglandins leading to
vasodilation

A

cytokines

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Q

increased production of C-reactive protein by hepatocytes
(marker of inflammation)

A

cytokines

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Q

increased production and release of proteolytic enzymes
(collagenases, metalloproteinases) by chondrocytes leading to degradation of cartilage and joint space narrowing

A

cytokines

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Q

o increased osteoclast activity and bone demineralization around joints
o systemic manifestations (heart, lungs, and liver are adversely affected)

A

cytokines

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Q

PHARMACOTHERAPY IN MANAGEMENT OF RHEUMATOID ARTHRITIS (RA

A

→ anti-inflammatory drugs
→ immunosuppressive agents

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Q

GOALS OF TREATMENT

A

→ modulate/reduce inflammatory process
→ halting or slowing progression of disease
→ reduce pain

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Q

Aspirin
Diflunisal
Diclofenac

A

Non-Steroidal Anti-Inflammatory Drugs (NSAID)

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Q

Etodolac
Fenamates
Flurbiprofen
Ibuprofen

A

Non-Steroidal Anti-Inflammatory Drugs (NSAID)

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Q

Indomethacin
Tolmetin

A

Non-Steroidal Anti-Inflammatory Drugs (NSAID)

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Q

Ketorolac
Meloxicam
Methyl salicylate

A

Non-Steroidal Anti-Inflammatory Drugs (NSAID)

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Q

Nabumetone
Naproxen
Oxaprozin

A

Non-Steroidal Anti-Inflammatory Drugs (NSAID)

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Q

Piroxicam
Sulindac

A

Non-Steroidal Anti-Inflammatory Drugs (NSAID)

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Q

Celecoxib

A

COX-2 Inhibitors

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Q

Acetaminophen

A

Other Analgesics

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Q

Abatacept
Adalimumab

A

Drugs for Arthritis

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Q

Anakinra
Chloroquine
Etanercept

A

Drugs for Arthritis

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Q

Etanercept
Gold Salts
Infliximab

A

Drugs for Arthritis

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Q

Methotrexate
D-Penicillamine

A

Drugs for Arthritis

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Q

Allopurinol
Colchicine

A

Drugs for Gout

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Q

Probenecid
Sulfinpyrazone

A

Drugs for Gout

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Q

→ inhibits the synthesis of prostaglandins

A

NSAIDs

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Q

primarily inhibits cyclooxygenase enzymes (catalyzes first step
prostanoid biosynthesis); leads to decreased prostaglandin
synthesis

A

NSAIDs

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Q

contraindicated in:
o perioperative pain like in coronary bypass graft surgery

o patients at risk for gastrointestinal adverse effects such as
bleeding, ulcer, or perforation of the stomach or intestine

A

NSAIDs

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unsaturated fatty acid derivatives (eicosanoids)

PROSTAGLANDINS

its precursor, Arachidonic acid, a 20-carbon fatty acid causes an increase of intracellular calcium and is a component of the phospholipid of the cell membrane

PROSTAGLANDINS

from the Arachidonic acid there are two pathways

o cyclooxygenase pathway o lipoxygenase pathway

described as the housekeeping enzyme that regulate the normal cellular processes such as vascular homeostasis, gastric cytoprotection, kidney function, and platelet aggregation

COX-1

causes the increased production of prostanoids in the disease sites and inflammation

COX-2

enzymes produce the leukotrienes depending on the tissue

LIPOXYGENASE PATHWAY

antileukotriene drugs such as Montelukast and Ziluton are useful in the treatment of moderate to severe asthma (allergic type)

LIPOXYGENASE PATHWAY

is a prototype of traditional NSAIDs; most commonly used

Aspirin

- blocks prostaglandin synthesis at thermo-regulatory centers in hypothalamus and peripheral target sites (antipyretic) - prevents sensitization of pain receptors (mechanical and chemical stimuli)

salicylates

may be given in prevention of cardiovascular events rather than for pain control

ASPIRIN

ANALGESIC ACTION used for low to moderate pain for musculoskeletal disorders than those pain from the viscera → pain caused by malignancy is treated with NSAID and opioids

salicylates

is 3-4x more potent than Aspirin as analgesic and anti-inflammatory but not antipyretic

Diflunisal

ANTIPYRETIC ACTION lowers body temperature in patients with fever by impeding PGE2 synthesis and release

Salicylates

ANTIPYRETIC ACTION resets “thermostat” to normal and rapidly lowers body temperature by heat dissipation as a result of peripheral VD and sweating; has no effect on normal body temperature

Aspirin

ANTIPYRETIC ACTION does not reduce fever because does not cross BBB

Diflunisal

GI EFFECTS with aspirin, prostanoids are not formed so there is: o ↑_____ gastric acid secretion o ↓ decreased mucus protection

increased

agents to prevent gastric and duodenal ulcers are misoprostol & PPIs

Esomeprazole, Lansoprazole, Omeprazole, Pantoprazole

GI EFFECTS H2 blockers relieves dyspepsia due to NSAID but mask serious GI complaints and are not as effective as PPIs in healing and preventing ulcers

Cimetidine, Ranitidine)

for long term, high dose of ____ treatment, both renal and hepatic functions should be monitored and avoid if creatinine clearance is less than 10 ml/min

aspirin

CONTRAINDICATIONS → pedia group (less than 15 years old) with varicella or influenza to prevent Reye’s syndrome

ASPIRIN & OTHER SALICYLIC ACID DERIVATIVES

should be taken with food and large amounts of fluid to diminish dyspepsia

aspirin

should not be taken at least 1 week prior to surgery

aspirin

Reye’s Syndrome fatal, fulminating hepatitis and cerebral edema seen in children given _______during viral infection (flu & varicella) o an option for fever would be acetaminophen or ibuprofen

aspirin/salicylates

patients taking_____ or _____ must avoid prolonged aspirin because it can cause increased renal UA excretion

probenecid, sulfinpyrazone

aspirin + ____ is contraindicated because there is increased risk of GI bleeding

ketorolac

alters platelet function and prolong bleeding time

Propionic acid derivatives (Ibuprofen, Naproxen, Fenoprofen, Ketoprofen, Flurbiprofen, Oxaprozin)

→ acute gouty arthritis → ankylosing spondylitis → OA of hip

Indomethacin

closely related to indomethacin but less potent

Sulindac

ACETIC ACID DERIVATIVES

Indomethacin, Sulindac, Etodolac

Piroxicam, Meloxicam

OXICAM DERIVATIVES

Mefenamic acid, Meclofenamate o no advantages as anti-inflammatory over NSAIDs

FENAMATES

adverse effect: o diarrhea (inflammation of bowel) o haemolytic anemia

FENAMATES

Diclofenac, Tolmetin Ketorolac

HETEROARYL ACETIC ACIDS

mode of action: o selective inhibitor COX2 (time-dependent and reversible) o does not inhibit platelet aggregation and does not increase bleeding time

CELECOXIB

contraindicated in patients allergic to sulfonamides

CELECOXIB

increases serum celecoxib

Fluconazole, Fluvastatin, Zafirlukast

increases beta blockers, antidepressants, antipsychotics

Celecoxib

antipyretic and analgesic but weak anti-inflammatory

ACETAMINOPHEN

→ alternative antipyretic or analgesic for patients with gastric complaints or with prolonged bleeding time

ACETAMINOPHEN

drug of choice in pedia patients with viral infection

ACETAMINOPHEN

→ does not antagonize uricosuric drugs (probenecid, sulfinpyrazone) o can be used in gout under these meds

ACETAMINOPHEN

→ mainstay treatment of RA and psoriatic arthritis → slows erosion of involved joints

METHOTREXATE

→ an immunosuppressant → much lower dose required than in cancer chemotherapy

METHOTREXATE

→ also used to treat malaria → used for early, mild RA

HYDROXYCHLOROQUINE

→ metabolic disorder with high UA in blood (hyperuricemia) → hyperuricemia leads to deposition of sodium urate crystals in tissues (joints and kidneys)

GOUT

is an overproduction of uric acid than the patient is able to excrete

hyperuricemia

to decrease movement of granulocytes into affected area

Indomethacin

ACUTE GOUT to decrease pain and inflammation; initial dose is doubled within first 24-48 hours then reduced in next days

NSAIDs

→ a plant alkaloid; used in treatment of acute gouty attacks and chronic gout

COLCHICINE

neither uricosuric nor analgesic but relieves pain in acute attacks

COLCHICINE

→ a purine analog → reduces UA production

ALLOPURINOL

ADVERSE EFFECTS alopecia (chronic use)

COLCHICINE

weak organic acid; irreversibly acetylates COX

ASPIRIN & OTHER SALICYLIC ACID DERIVATIVES

mode of action: o reversible inhibitors of cyclooxygenases and inhibits synthesis of prostaglandins but not leukotrienes

Propionic acid derivatives (Ibuprofen, Naproxen, Fenoprofen, Ketoprofen, Flurbiprofen, Oxaprozin)

mode of action: o inhibits COX1 and COX2

OXICAM DERIVATIVES

THERAPEUTIC USES → treatment of primary hyperuricemia of gout → treatment of hyperuricemia secondary to malignancies and renal disease

ALLOPURINOL