NSAIDS Flashcards
Physiological response of the body to tissue injury and infection
Inflammation
Four cardinal signs of inflammation
Calor - heat
Dolor - pain
Rubor - redness
Tumor - swelling
Hot si calor, Nasaktan si Dolor, RR
Mediate responses
Vascular diameter (vasodilation) and Vascular permeability
Explain what happens during vascular diameter (vasodilation)
Increased blood flow resulting in rubor (reddening) and calor (heating)
Explain what happens during vascular permeability
Increased permeability resulting to slow leakage of fluid resulting in swelling (edema)
Leukocytes arrive to site of injury and phagocytize the pathogens releasing _________
Soluble mediators: cytokine, leukotriene, prostaglandins
Inflammation can be ____ and ____
Acute and Chronic
Acute inflammation occurs _______
In response to tissue injury
Chronic inflammation
Leads to progressive destruction
Two systems involved in acute inflammatory response
Clotting systems and Kinin systems
Explain clotting system (acute inflam response)
Fibrin produces clots to stop spread of infection through the blood
Explain kinin system (acute inflam response)
Produces bradykinin which results to vasodilation and permeability
During acute inflammation, what dominates the landscape?
Non-protein based soluble factors (eicosanoids, bioamines)
Represents a diverse family of lipid mediators with fundamental roles in physiology and disease
Eicosanoids
Chronic inflammation results from what?
Continuous exposure to offending element
T or F: Pathogen persistence causes continuous activation of T-cells and cancers
True
In chronic inflammation, the following are activated and accumulated
Macrophages, Lymphocytes, Fibroblast
T or F: In chronic inflammation, cytokines, chemokines, growth factors are the primary factors
True
Give the 2 treatment strategies
- Relief of symptoms - NSAIDs
- Maintain function and slowing of tissue-damaging process - DMARDs
Phospholipids are converted into ____ by the enzyme ____
Into arachidonic acid by phospholipase
What are given to remove the enzyme phospholipase, inhibiting arachidonic acid production?
Corticosteroids
Arachidonic acid is converted into ____ by the enzyme ____
Into leukotrienes by lipoxygenase
What are given to prevent conversion of AA to Leukotrienes?
Lipoxygenase inhibitors
Responsible for an increase in vascular permeability and constriction of smooth muscles (e.g., bronchial airways)
Leukotrienes C, D, E
Functions for phagocytic attraction or activation by engulfing pathogens, hence, releasing chemicals responsible for inflammation
Leukotriene B
What is given to prevent the phagocytic action of Leukotriene B?
Colchicine
What are given to inhibit binding of leukotrienes to their receptors?
Receptor Antagonists (e.g., Montelukast)
AA can also be converted to ___, ___, and ___ by the enzyme ____
Into prostaglandin, prostacyclin, thromboxane by cyclooxygenase
Cyclooxygenase may be inhibited by ___ and ___?
NSAIDs and Aspirin
T or F: Prostaglandins inhibit platelet aggregation
False, prostacyclins
From what family are AA?
Eicosanoids
Most abundant eicosanoid precursor
AA
T or F: Linolenic acid (Omega 3) is converted to Linoleic acid (Omega 6) to form AA
False, Linoleic acid (Omega 6) –> Linolenic acid (Omega 3) –> AA
Straight-chain derivatives of eicosanoids
Leukotrienes
Cyclic derivatives of eicosanoids
PG, PC, TX
Condition common in newborn infants where the opening between aorta and pulmonary artery dose not close resulting to mixing of oxygenated and deoxygenated blood
Patent Ductus Arteriosus
To prevent Patent Ductus Arteriosus, we inhibit ___
Production of Prostaglandins
T or F: All NSAIDs inhibit PG synthesis
True
Enzyme responsible for prostaglandin synthesis
Cyclooxygenase
Two forms of COX
COX 1 - constitutive
COX 2 - inducible
Generates prostanoids for “housekeeping” functions
COX 1
Main source of prostanoids responsible for inflammation and cancer
COX 2
T or F: NSAIDs are for pain but ironically causes headache as side effect
True
Irreversibly inhibits platelet COX and the only NSAID to bind irreversibly
Aspirin
T or F: Aspirin is still used as anti-inflammatory
False, rarely used
Decreases incidence of transient ischemic attacks, unstable angina, coronary artery thrombosis with MI, and thrombosis after coronary bypass grafting
Aspirin
Contraindication of Aspirin
Patients with hemophilia and those at risk for GI bleeding
Anti-inflammatory drugs to do not inhibit platelet aggregation
Nonacetylated salicylates
T or F: Nonacetylated salicylates are preferred when COX inhibition is undesirable
True
COX-2 Selective Inhibitors at usual doses have ____ impact on platelet aggregation
No impact
Do COX-2 inhibitors offer cardioprotective effects?
No
Benzenesulfonamide COX-2 inhibitor for the treatment of OA, RA, JRA, AS
Celecoxib
Inflammation of big joints such as knees and elbows
Osteoarthritis (OA)
Inflammation of small joints such as palms of the hand, feet
Rheumatoid Arthritis (RA)
Arthritis in children that causes joint swelling and stiffness
Juvenile Rheumatoid Arthritis (JRA)
Arthritis that causes inflammation in joints and ligaments of the spine, causing stiffness
Ankylosing spondylitis (AS)
Racemic acetic acid derivative COX-2 inhibitor
Etodolac
Uses of Etodolac
Treatment of OA, RA, JRA
Enolcarboxamide COX-2 inhibitor
Meloxicam
Indication of Meloxicam
Treatment of OA, RA, JRA
Indole derivative and a potent non-selective COX inhibitor
Indomethacin
T or F: Indomethacin does not inhibit phospholipase A and C
False, it inhibits
Indomethacin are used less than common NSAIDs, why?
Due to toxicity
Indications of Indomethacin
Treatment of OA, RA, AS
Adverse effects of Indomethacin
Depression, epilepsy, parkinsonism
Propionic acid derivative that non-selectively inhibits COX and inhibits lipoxygenase
Ketoprofen
Indications of Ketoprofen
Treatment of OA and RA
Ketoprofen ADRs
Thrombocytopenia, Agranulocytosis, Cholestatic hepatitis
Only nonacid NSAID which is a ketone prodrug
Nabumetone
Nabumetone resembles what drug in its structure?
Naproxen
Indication of Nabumetone
Treatment of OA and RA
Nabumetone ADR
Diarrhea, Dyspepsia, Abdominal pain
Enolcarboxamide derivative that is a non-selective COX inhibitor that also inhibits lymphocyte function
Piroxicam
Indication of Piroxicam
Treatment of OA and RA
Piroxicam ADR
Peptic ulcer
Sulfoxide nonselective prodrug whose active metabolite is a non-selective COX inhibitor
Sulindac
Indications of Sulindac
OA, RA, AS, acute gouty arthritis
Drug that can be used to inhibit development of colon, breast, and prostate cancer
Sulindac
Sulindac ADR
Thrombocytopenia, Agranulocytosis, Nephrotic syndrome
Phenylacetic acid derivative
Dicloflenac
Difluorophenyl derivative of salicylic acid
Diflunisal
Propionic acid derivative
Flurbiprofen, Oxaprozin
Simple phenylpropionic acid derivative
Ibuprofen
Naphthyl-propionic acid derivative
Naproxen
Pyrrole alkanoic acid derivative
Tolmetin
