ANTI-INFLAMMATORY DRUGS (s) Flashcards by Love Dog | Brainscape

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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Q

unsaturated fatty acid derivatives (eicosanoids)

A

PROSTAGLANDINS

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Q

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

A

PROSTAGLANDINS

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Q

from the Arachidonic acid there are two pathways

A

o cyclooxygenase pathway
o lipoxygenase pathway

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Q

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

A

COX-1

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Q

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

A

COX-2

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Q

enzymes produce the leukotrienes depending on the tissue

A

LIPOXYGENASE PATHWAY

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Q

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

A

LIPOXYGENASE PATHWAY

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Q

is a prototype of traditional NSAIDs; most commonly used

A

Aspirin

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Q

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

A

salicylates

Q

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

A

ASPIRIN

Q

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

A

salicylates

Q

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

A

Diflunisal

Q

ANTIPYRETIC ACTION

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

A

Salicylates

Q

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

A

Aspirin

Q

ANTIPYRETIC ACTION

does not reduce fever because does not cross BBB

A

Diflunisal

Q

GI EFFECTS

with aspirin, prostanoids are not formed so there is:

o ↑_____ gastric acid secretion
o ↓ decreased mucus protection

A

increased

Q

agents to prevent gastric and duodenal ulcers are misoprostol &
PPIs

A

Esomeprazole, Lansoprazole, Omeprazole, Pantoprazole

Q

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

A

Cimetidine, Ranitidine)

Q

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

A

aspirin

Q

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

A

ASPIRIN & OTHER SALICYLIC ACID DERIVATIVES

Q

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

A

aspirin

Q

should not be taken at least 1 week prior to surgery

A

aspirin

Q

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

A

aspirin/salicylates

Q

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

A

probenecid, sulfinpyrazone

Q

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

A

ketorolac

Q

alters platelet function and prolong bleeding time

A

Propionic acid derivatives

(Ibuprofen, Naproxen, Fenoprofen, Ketoprofen, Flurbiprofen, Oxaprozin)

Q

→ acute gouty arthritis
→ ankylosing spondylitis
→ OA of hip

A

Indomethacin

Q

closely related to indomethacin but less potent

A

Sulindac

Q

ACETIC ACID DERIVATIVES

A

Indomethacin, Sulindac, Etodolac

Q

Piroxicam, Meloxicam

A

OXICAM DERIVATIVES

Q

Mefenamic acid, Meclofenamate

o no advantages as anti-inflammatory over NSAIDs

A

FENAMATES

Q

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

A

FENAMATES

Q

Diclofenac, Tolmetin Ketorolac

A

HETEROARYL ACETIC ACIDS

Q

mode of action:
o selective inhibitor COX2 (time-dependent and reversible)

o does not inhibit platelet aggregation and does not increase
bleeding time

A

CELECOXIB

Q

contraindicated in patients allergic to sulfonamides

A

CELECOXIB

Q

increases serum celecoxib

A

Fluconazole, Fluvastatin, Zafirlukast

Q

increases beta blockers, antidepressants, antipsychotics

A

Celecoxib

Q

antipyretic and analgesic but weak anti-inflammatory

A

ACETAMINOPHEN

Q

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

A

ACETAMINOPHEN

Q

drug of choice in pedia patients with viral infection

A

ACETAMINOPHEN

Q

→ does not antagonize uricosuric drugs (probenecid,
sulfinpyrazone)

o can be used in gout under these meds

A

ACETAMINOPHEN

Q

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

A

METHOTREXATE

Q

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

A

METHOTREXATE

Q

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

A

HYDROXYCHLOROQUINE

Q

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

A

GOUT

Q

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

A

hyperuricemia

Q

to decrease movement of granulocytes into affected area

A

Indomethacin

Q

ACUTE GOUT

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

A

NSAIDs

Q

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

A

COLCHICINE

Q

neither uricosuric nor analgesic but relieves pain in acute attacks

A

COLCHICINE

Q

→ a purine analog
→ reduces UA production

A

ALLOPURINOL

Q

ADVERSE EFFECTS

alopecia (chronic use)

A

COLCHICINE

Q

weak organic acid; irreversibly acetylates COX

A

ASPIRIN & OTHER SALICYLIC ACID DERIVATIVES

Q

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

A

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

Q

mode of action:
o inhibits COX1 and COX2

A

OXICAM DERIVATIVES

Q

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

A

ALLOPURINOL