METABOLIC PROFILE DRUGS - Glucocorticoid, Steroidal & Nonsteroidal Anti-Inflammatory Drugs Flashcards
Glucocorticoids are hormonal steroids
Having an important effect on intermediary metabolism, cardiovascular function, growth, and immunity
Inflammation is
A localized protective reaction of a tissue to irritation, injury, or infection, characterized by pain, redness,
swelling, and sometimes loss of function
An acute, transient phase, of inflammation is characterized by
Local vasodilatation and increased capillary permeability (phase of damage)
A delayed, subacute phase, of inflammation is characterized by
Infiltration of leucocytes and phagocytic cells (phase of exudation)
A chronic, proliferative phase, of inflammation is characterized by
Tissue degeneration and fibrosis occurrence (phase of proliferation)
The following substances are considered to be referred to as eicosanoids
- Prostaglandins
- Leukotrienes
- Thromboxanes
True or False about cortisol (hydrocortisone). Cortisol is synthesized from cholesterol
TRUE
True or False about cortisol (hydrocortisone). ACTH governs cortisol secretion
TRUE
True or False about cortisol (hydrocortisone). Most cortisol is inactivated in the liver
TRUE
True or False about cortisol (hydrocortisone). The half-life of cortisol in the circulations is normally about 60-90 hours.
FALSE
True or False about glucocorticoids. Effects of glucocorticoids are mediated by widely distributed glucocorticoid receptors that are members of the superfamily of nuclear receptors.
TRUE
True or False about glucocorticoids. Glucocorticoids have dose-related metabolic effects on carbohydrate, protein, and fat metabolism.
TRUE
True or False about glucocorticoids. Glucocorticoids have pro-inflammatory effects.
FALSE
True or False about glucocorticoids. Glucocorticoids have catabolic effects in lymphoid and connective tissue, muscle, fat, and skin.
TRUE
Physiologic doses of glucocorticoid can result in
- Increased liver glycogen stores, gluconeogenesis and lipolysis
- Maintenance of cardiovascular function (by potentiation of norepinephrine) and skeletal muscle function
- Increased hemoglobin synthesis, resulting in elevated of red blood cell count
Which glucocorticoids is a short- to medium-acting drug?
Prednisolon
Which glucocorticoids is an intermediate-acting drug?
Triamcinolone
Which glucocorticoids is a long-acting drug?
Dexamethasone
Which glucocorticoids have one fluoride atom in its chemical structure?
Triamcinolone
Which glucocorticoids have two fluoride atoms in its chemical structure?
Fluocinolone
Which glucocorticoids has no fluoride atoms in its chemical structure?
Prednisolon
Anti-inflammatory effect of glucocorticoids is caused by
- Reducing the prostaglandin and leukotriene which results from inhibition of phospholipase A2
- Reducing macrophages migration into the site of inflammation
- Decreasing capillary permeability
True or False about anti-inflammatory effect of glucocorticoids. Anti-inflammatory effect of glucocorticoids results from inhibition of cyclooxygenase
FALSE
True or False about anti-inflammatory effect of glucocorticoids. Anti-inflammatory effect of glucocorticoids results from inhibition of phospholipase A2 and reducing prostaglandin and leukotriene synthesis
TRUE
True or False about anti-inflammatory effect of glucocorticoids. Induction of cyclooxygenase II expression which results in reducing amount of an enzyme available to produce prostoglandins
FALSE
Immunosupressive effect of glucocorticoids is caused by
Reducing concentration of lymphocytes (T and B cells) and inhibiting function of tissue macrophages and
other antigen-presenting cells
True or False about anti-inflammatory effect of NSAIDs. Anti-inflammatory effect of NSAIDs results from inhibition of cyclooxygenase
TRUE
True or False about anti-inflammatory effect of NSAIDs. Anti-inflammatory effect of NSAIDs results from inhibition of phospholipase A2 and reducing prostaglandin and
leukotriene synthesis
FALSE
True or False about anti-inflammatory effect of NSAIDs. Anti-inflammatory effect of NSAIDs results from induction of cyclooxygenase II expression which results in reducing
the amount of an enzyme available to produce prostoglandins
FALSE
Indication of glucocorticoids is
- Chronic (Addison’s disease) and acute adrenocortical insufficiency
- Organ transplants (prevention and treatment of rejection – immunosuppression)
- Inflammatory conditions of bones and joints (arthritis, bursitis, tenosynovitis).
Indications of glucocorticoids are
- Gastrointestinal diseases (inflammatory bowel disease)
- Inflammatory conditions of bones and joints (arthritis, bursitis, tenosynovitis)
- Skin diseases (atopic dermatitis, dermatoses, localized neurodermatitis)
Serious side effects of glucocorticoids include
- Acute peptic ulcers
- Iatrogenic Cushing’s syndrome (rounding, puffiness, fat deposition and plethora alter the appearance of the face – moon faces)
- Hypomania or acute psychosis
Serious side effects of glucocorticoids include
- Adrenal suppression
- Insomnia, behavioral changes (primarily hypomania)
- Rounding, puffiness, fat deposition and plethora alter the appearance of the face – moon faces
True or False. Selective COX-2 inhibitors are safer than nonselective COX-1 inhibitors but without loss of efficacy.
TRUE
True or False. The constitutive COX-2 isoform tends to be homeostatic in function, while COX-1 is induced during inflammation and tends to facilitate the inflammatory response.
FALSE
Which property combinations is peculiar to the majority of NSAIDs?
Antipyretic, analgesic, anti-inflammatory
Which NSAIDs is a propionic acid derivative?
Ibuprofen
Which NSAIDs is an indol derivative?
Indomethacin
Which NSAIDs is a pyrazolone derivative?
Metamizole (Analgin)
Which NSAIDs is a fenamate derivative?
Meclofenamic acid
Which NSAIDs is an oxicam derivative?
Piroxicam
Which NSAIDs is a selective COX-2 inhibitor?
Celecoxib
Which NSAIDs is a nonselective COX inhibitor
Piroxicam
True or False. Aspirin inhibits phospholipase A2
TRUE
Indication for aspirin administration are
- Inflammatory conditions
- Decreasing the incidence of transient ischemic attack, unstable angina, coronary artery thrombosis with myocardial infarction, and thrombosis after coronary artery bypass grafting
- Reducing elevated body temperature
Side effects of aspirin include
- Gastric upset (intolerance)
- Salicylism (vomiting, tinnitus, decreased hearing, and vertigo)
- Gastric ulcers and upper gastrointestinal bleeding
Serious side effects of metamizole (analgin) include
Agranulocytosis, aplastic anemia
Side effects of indometacin include
- Abdominal pain, diarrhea, gastrointestinal hemorrhage and pancreatitis
- Dizziness, confusion and depression
- Trombocytopenia
True or False. Ketoprofen is a propionic acid derivative that inhibits both cyclooxygenase (nonselectively) and lipoxygenase.
TRUE
True or False. Ketorolac is an NSAID that is promoted for systemic use as an anti-inflammatory, not as an analgesic drug.
FALSE
Which drugs is a 5-lipoxygenase (5-LOG) inhibitor?
Zileuton (Zyflo)
Which drugs is a leucotreine D4 receptor (LTD4) blocker?
Zafirleukast (Accolate)
Which drugs is a thromboxane A2 receptor (TXA2) antagonist?
Sulotroban