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AUTOCOIDS/NONSTEROIDAL
ANTIINFLAMMATORY/ASTHMATIC DRUGS (7.5 hr)
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Subcommittee:
1. Histamine (0.5 hr)
a) Distribution and synthesis
b) Storage and release
(immunologic and nonspecific)
c) Metabolism and elimination
d) Receptors (H1, H2,
H3 and H4)
e) Pharmacologic actions: smooth
muscles, exocrine glands, cardiovascular, and sensory nerve endings
2. Antihistaminic drugs (1 hr)
a) Mechanisms of action: on
receptor subtypes (H1, H2, H3 and H4)
b) Pharmacological properties
and side effects (desirable/adverse)
c) Therapeutic uses
3. Anti-motion sickness drugs (0.5 hr)
a) Understand the mechanisms of
motion sickness and the differences in mechanism and action between the
phenothiazine neuroleptics and those drugs that affect the vestibular
pathway.
4. Serotonin (5-HT) and pharmacology of
migraine (0.5 hr)
a) Distribution and synthesis
b) Storage and release
c) Metabolism, elimination
d) Receptors
e) Pharmacological actions (cardiovascular, cerebral
vasculature, gastrointestinal, sensory neurons)
f) Treatment of migraine (drugs for
prophylactic and abortive therapies, relative efficacies, their pharmacokinetics
and adverse effects, and primary cellular sites of action)
g) Treatment of
chemotherapy-induced emesis
5. Nitric oxide, donors and inhibitors (0.5 hr)
a) EDRF
b) Synthesis (nNOS, eNOS, iNOS);
constitutive vs inducible
c) Pharmacological
actions (cGMP; vasculature; erectile dysfunction etc)
6. Eicosanoids (0.5 hr)
a) Synthesis of prostaglandins,
thromboxanes, and leukotrienes from arachidonic acid. Know which are the
key enzymes in the overall pathway and what drugs affect each enzyme.
b) Pharmacological actions of
PGE2, PGF2, PGI2 (PROSTACYCLIN), TXA2,
and the leukotrienes (LTA4 thru LTE4): vascular,
airway, uterine, and GI smooth muscle; microvascular permeability;
platelet function; sensory nerve endings; gastric and intestinal
secretions; temperature regulation center.
c) Termination of action.
7. Treatment of asthma (1.0 hr)
a) Know the disease process of
asthma involving airway inflammation, bronchial smooth muscle
constriction and mast cell degranulation
b) Mediators (histamine, acetylcholine,
proteases, leukotrienes C4, D4; prostaglandins;
cytokines)
c) Describe the mechanisms of
action, adverse effects of each anti-asthmatic drug
d) Know the routes and
limitations of drug administration, systemic and inhalant
e) Describe the types of therapy
available: short term relief and long-term control
8. Hypersensitivity
and Immunopharmacology (0.5 hr)
a)
Role of
immunoglobulins (IgE, IgG, IgM) in drug allergy
b)
Differentiate
different types of allergic reactions (Type I-IV) and factors (e.g.
cytokines, MHC) involved
c)
Learn the release
of allergic mediators, and process leading to hypersensitivity
d)
Understand the
site of action of selected immunosuppressive agents on the immune
response.
9. Bradykinin (0.5 hr)
a) Synthesis and metabolism of kinins:
know what pathophysiological factors trigger kinin formation and how
bradykinin can influence the eicosanoid and EDRF pathways.
b) Realize the metabolism of
bradykinin by ACE and prolongation of bradykinin by ACE inhibitors
c) Pharmacological actions:
compare and contrast with actions of histamine and eicosanoids.
10. Analgesic, antipyretic, antiinflammatory
drugs (2.0 hr)
A. Antipyretic-analgesic drugs
a) Understand the physiological
basis of body temperature control and peripheral sensory pain fibers.
b) Understand the role of
eicosanoids and bradykinin in causing local pain, edema and fever.
c) Opiate analgesics (morphine,
etc.) are covered under CNS drugs.
d) Understand the difference in
mechanisms of action between acetaminophen and aspirin.
e) Compare the pharmacological
properties of acetaminophen and aspirin.
f) Understand the
metabolism of acetaminophen, the role of cytochrome P450, and the
mechanism of acetaminophen toxicity, as well as its reversal by
N-acetylcysteine.
g) Understand the adverse
effects of aspirin, as well as the acute toxic effects of aspirin
overdosage.
h) Understand the factors that
affect the absorption and elimination of aspirin.
i) Understand the hepatic
metabolism of aspirin.
j) Understand the
potentially detrimental consequences of plasma protein binding,
zero-order metabolism, and irreversible cyclooxygenase inhibition shown
by aspirin.
k) Understand the adverse drug
interactions possible with aspirin (coumadin anticoagulants, oral hypoglycemic
drugs, alcohol, others).
l) Understand the
principles of treatment of salicylate intoxication.
B. Antiinflammatory drugs (NSAIDs and
glucocorticoids)
a) Understand the
pathophysiology of acute and chronic inflammation.
b) Understand the adverse
effects and potential adverse drug interactions associated with
inhibition of the COX1 pathway. Understand the significance of COX2.
c) Glucocorticoids are covered
under steroid hormones
d) Describe the role of IL-1b
and TNF-α in inflammation
e) Critical discussion on the
potential serious side effects of COX2 inhibitors
C. Disease-Modifying Anti-Rheumatic
Drugs (DMARDs)
a) Understand that these drugs
have no analgesic or antipyretic activity; their mechanisms of action are
largely unknown.
b) Understand that their onset
of action is very long and the drugs are very toxic.
c) Understand the role of TNF in
chronic inflammation.
d) Discussion
of therapeutic use of monoclonal antibodies in addition to infliximab in
treatment of inflammation and immune disorders
D. Drugs used to treat gout
a) Understand the causes and
pathophysiology of acute gouty arthritis and chronic tophaceous gout.
b) Compare and contrast the
mechanisms of action of colchicine, allopurinol, probenecid, and
sulfinpyrazone.
c) Understand the dangerous side
effects of colchicine.
d) Understand the cause and
treatment of acute gouty flare-ups associated with the use of allopurinol
or probenecid in treating chronic tophaceous gout.
e) Understand that NSAIDs except
aspirin may be used as substitutes for colchicine. Why is aspirin
contraindicated?
f) Understand the
potential adverse drug interactions with allopurinol (i.e.
6-mercaptopurine).
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