(continued)

Pharmacodynamics:
Mechanisms of Action
• Receptor interaction
• Enzyme interaction
• Nonspecific interactions
 Instructors may wish to insert
EIC Image #2:

Drugs and Receptors

and possibly
EIC Image #7:

Drug-Receptor Interactions: Definitions

• Receptor: Any cellular macromolecule that a
drug binds to initiate its effects.
• Drug: A chemical substance that interacts with
a biological system to produce a physiologic
effect
• All drugs are chemicals but not all chemicals
are drugs.
• ability to bind to a receptor is mediated by the
chemical structure of the drug that allows it to
interact with complementary surfaces on the
receptor.
• Drugs that interact with receptors can be
classified as being either agonists or
antagonists
 Antagonists
• have the ability to bind to the receptor but do
not initiate a change in cellular function.
• Because they occupy the receptor, they can
prevent the binding and the action of
agonists. Hence the term antagonist.
• Antagonists are also referred to as blockers.
• Unlike competitive antagonists, the blocking
activity of irreversible receptor antagonists
can not be overcome by increasing the
agonist concentration
 Full and Partial Agonists
• Full Agonists: Compounds that are able to
elicit a maximal response following receptor
occupation and activation.
• Partial Agonists: Compounds that can activate
receptors but are unable to elicit the maximal
response of the receptor system.
receptors
 Factors Governing Drug Action
• Affinity is a measure of the tightness that a
drug binds to the receptor.

• Intrinsic activity is a measure of the ability of

a drug once bound to the receptor to
generate an effect activating stimulus and
producing a change in cellular activity.
 The binding of a drug to a receptor is
determined by the following forces:
• Hydrogen bonds

• Ionic bonds

• Van der Waals forces

• Covalent bonds
 Dose-Response Curves
• Dose-response relationships are a common
way to portray data in both basic and clinical
science.
• For example, a clinical study may examine
the effect of increasing amounts of an
analgesic on pain threshold
• A plot of drug concentration ([D]) versus effect (E/Emax) (or
for that matter DR/RT) is a rectangular hyperbola. Notice how
the drug effect reaches a plateau or maximum. This is
because there are a finite number of receptors. Hence, the
response must eventually reach a maximum
• However, the hyperbolic plot is a cumbersome graph because
drug concentrations often vary over 100 to 1000-fold. This
necessitates a long X-axis. To overcome this problem, the log
of the drug concentration is plotted versus the effect. A plot
of the log of [D] versus E/Emax is a sigmoid curve.
• The Therapeutic Index
• The therapeutic index is the ratio of the ED50
of a drug to produce a toxic effect to the ED50
to produce a therapeutic effect.
 DRUG AND SOLUTION MEASUREMENTS

• oz. Ounce • mcg microgram

• G, gm gram • mEq milliequivalent
• gr grain • mg milligram
• gtt drop • ml milliliter
• Kg kilogram • pt pint
• L liter • qt quart
• Tbs, T tablespoon
• Tsp, t teaspoon
 DRUG DOSAGE FORMS
• cap capsule
• DS double strength
• EC enteric coated
• Elix elixir
• Liq liquid
• Sol solution
• Supp suppository
• Susp suspension
• Syr syrup
• Tab tablet
 ROUTES OF DRUGADMINISTRATION
• IM intramuscular
• IV intravenous
• IVPB intravenous piggyback
• 10
• V, PV vaginally
• PO by mouth
• R, PR by rectum
• Subcut subcutaneous
• S&S swish & swallow
 TIMES OF DRUG
ADMINISTRATION
• ac before meals • Daily Every day
• ad lib as desired • Qh (hr) every hour
• Bid twice a day • Q2h (hr) every 2 hours
• Tid three times a day • Q3h (hr) every 3 hours
• Qid four times a day • Stat-immediately
• pc after meals
• Prn as needed