DRUGS FOR INFLAMMATION Flashcards
what are the signs of inflammation?
pain, warmth, redness, edema
causes of inflammation
infection, cell death, hypersensitivity reactions, extreme heat, chemical injury, physical trauma
what is acute inflammation?
- associated with minor physical injury, chemical damage, infection, antigens
- typically lasts 8-10 days, followed by repair an healing
- usually self limiting; consider non pharmacological methods, topical antiinflammatories should be used whenever possible
what is chronic inflammation?
- may occur if the body is not able to contain or neutralize the trigger of the into; inflammation; associated with many chronic conditions (SLE, rheumatoid arthritis)
- leads to tissue damage, with symptoms becoming worse overtime
what is maladaptive?
body unable to adapt to pain on its own
bradykinin
present in an active form in plasma and also stored an released by mast cells; vasodilator that causes pain; effects are similar to those of histamine
complement
series of at least 20 proteins that combines in a cascade fashion to neutralize or destroy an antigen
histamine
stored and released by mast cells; causes dilation of blood vessels, smooth muscle constriction, tissue swelling and itching
leukotrienes
stored an released by mast cells; effects are similar of those of histamine
prostaglandins
present in most tissues and stored and released by mast cells; increase capillary permeability, attract white blood cells to site of inflammation, an cause pain
arachidonyl ester is covered into arachidonic acid by which enzyme?
phospholipase A2
when tissue is damaged, what acid is produced?
arachidonic acid (AA)
cyclooxygenase
converts AA into prostaglandins
prostaglandins
enhance vasodilation, gastric cytoprotection, decrease gastric acid secretion
thromboxane A2
stimulates platelet aggregation
lipoxygenase
converts AA into leukotrienes
leukotrienes
phagocyte activation, neutrophil chemotaxis, bronchoconstriction
what are the two anti-inflammatory drug classes?
NSAIDS, glucocorticoids drugs
what’s the difference between NSAIDS and glucocorticoids drugs?
NSAIDS: used for management of mild to moderate pain, inflammation an fever
Glucocorticoids drugs: used for short term management of severe or disabling inflammation
additional drug classes have been developed for which diseases?
IBD (ulcerative colitis, crohn’s disease), rheumatoid arthritis
what additional drug classes were developed for specific disease states?
immunosuppressive drug, anti-TNF agents
are NSAIDS non specific or specific?
non specific - all prostaglandin synthesis is inhibited
is aspirin irreversible inhibitor or reversible?
irreversible inhibitor of cyclooxygenase enzyme
- significant impact on platelets; potent anticoagulant effect
what do non selective NSAIDS inhibit?
COX-1 an COX-2 enzymatic activity
what are the function of non selective NSAIDS?
- reduces inflammation an fever
- inhibits the formation of gastric mucosa, increases gastric acid secretion
- inhibits platelet aggregation (significant inhibition - thromboxane A2)
what is the second leading cause of peptic ulcer disease?
NSAIDS, significant risk GI bleeding
what are the risks of selective NSAIDS?
high risk of MI, stroke and asymptomatic hypertension
what are the 3 examples of aspirin?
A. coated
B. original strength
C. with stomach guard
what is coated aspirin?
enteric coated products are intended to absorb in the alkaline environment of the small intestine (NOT ABSORBED IN THE STOMACH)
what is original strength aspirin?
regular product that dissolves and begins to absorb in the stomach
what is stomach guard aspirin?
buffered products contain ions that decrease gastric acidity and slow absorption
prolonged excessively high fevers can induce what?
febrile seizures (especially in children), tissue damage, reduced mental acuity, delirium or coma
what are the two antipyretic therapies?
NSAIDS and acetaminophen
NSAIDS (Reye’s syndrome) - antipyretic therapy
- most common between 4-14 years
- associated with previous viral illness (chicken pox, influenza) and use of aspirin, causing brain inflammation, fatty deposits in the liver, death within days
- overdose of aspirin
acetaminophen - antipyretic therapy
direct action on hypothalamus and dilation of peripheral blood vessels (enables sweating and fever)
why should you never use aspirin in paediatric patients with a fever?
you don’t know what’s causing the fever
when is histamine released?
during an allergic reaction
what are antihistamines?
block the action of histamine at the H1 receptor for the treatment of allergic rhinitis; provide symptomatic relief of runny nose, sneezing, itchy eyes an throat, most effective when administered prophylactically
what effects do antihistamines produce?
sedative effects - more prominent in 1st general H1 antagonists (eg. diphenhydramine (Benadryl) vs loratadine (Claritin))
- can also be used for treatment of motion sickness an vertigo
anaphylaxis
- hyperimmune and hyper inflammatory response to an antigen
- body responds within minutes to the antigen, releasing massive amounts of histamine and other chemical mediators of inflammation
symptoms of anaphylaxis
itching, hives, tightness in throat and chest, swelling of the larynx, causing cough, rapid decrease in BP, reflex tachycardia, difficulty breathing (bronchoconstriction)
anaphylaxis of pharmacological management (epinephrine (IM) adrenergic agonist drug)
alpha1 receptor - increases BP
beta2 receptor - bronchodilation
beta1 receptor - cardiac output
anaphylaxis of pharmacological management (in cases of continued upper airway obstruction - what should be given?)
nebulized epinephrine
anaphylaxis of pharmacological management (in cases of persistent wheeze - what should be given?)
- beta2 adrenergic agonists (eg. salbutamol - inhaled) - promotes bronchodilation
- systemic glucocorticoids (eg. prednisolone - PO) or hydrocortisone (IV); inhibits immune and inflammatory responses to the antigen
