Pharmacology Intro

Pharmacology
 Approximately 80% of drugs are

taken by mouth
 A drug taken by mouth goes
Pharmacology through three phases:
 Pharmaceutic (dissolution)
 Pharmacokinetic
 Pharmacodynamic
 In this phase, the drug becomes a solution so
that it can cross the biologic membrane
 Tablets are not 100% drug. Fillers and inert
substances, called excipients, are used in drug
preparation to allow the drug to take on
Pharmaceutic
particular size, shape and to enhance dissolution
Phase
 Disintegration is the breakdown of a tablet into
smaller particles
 Dissolution is the dissolving of the smaller
particles in the GI fluid before absorption
 Is the process of drug movement to
achieve drug action
 The four phases are:
Pharmacokineti  Absorption
c Phase
 Distribution
 Metabolism (biotransformation)
 Excretion
 Is the movement of drug particles from the GI to
body fluids by passive absorption, active
absorption, or phagocytosis
 Passive absorption occurs mostly by diffusion
 Active absorption requires a carrier such as an
Absorption enzyme or protein to move the drug against a
concentration gradient
 Phagocytosis is a process by which cells carry a
drug across their membrane by engulfing the drug
particles
 First-pass effect or hepatic first
pass – the process by which the
drug will pass through the liver
first.
Absorption  Bioavailability – it is the
percentage of the administered
drug dose that reaches the systemic
circulation
 Is the process by which the drug
becomes available to body fluids
and body tissues
Distribution  It is influenced by blood flow, the
drug’s affinity to the tissue, and the
protein-binding effect
 Drugs can be metabolized in both GI tract and liver
 Most drugs are inactivated by liver enzymes and are then
converted into water-soluble substances for excretion
 Half-life of a drug is the time it takes for one-half of the
Metabolism or drug concentration to be eliminated
Biotransformati  Example: if a patient takes 650mg of aspirin and the
on half life is3 hours, it takes 3 hours for the first half-life
to eliminate 325 mg, 6hours for second half-life to
eliminate the additional 162 mg, and so on until the
sixth half-life (or 18 hours
 The main route of drug elimination
is through the kidneys
Excretion or  Other routes include hepatic
Elimination
metabolism, bile, feces, lungs,
saliva, sweat, and breast milk
 Onset of action – is the time it takes
to reach the minimum effective
concentration after a drug is
administered
Onset, Peak,  Peak action occurs when the drug
and Duration of reaches its highest blood or plasma
Action
concentration
 Duration of action is the length of
time the drug has a pharmacologic
effect
 Is the study of drug concentration
and its effects on the body
 Drug response can cause a primary
or secondary physiologic effect or
Pharmacodynamic
Phase both
 The primary effect is desirable and
the secondary effect is undesirable
 Example: Ceterizine
 Agonists – drugs that produce a
response
 Antagonists – drugs that block a
Agonists and response
Antagonists  Example:
 Albuterol stimulates the beta 2
receptor
 Cimetidine blocks H2 receptor
 Nonspecific drugs - Drugs that
affect various sites
 Example: general anesthesia
Nonspecific and  Nonselective drugs – drugs that
Nonselective
affect various receptors
Drug Effects
 Example: epinephrine acts on
the alpha, beta1, and beta2
receptors
 Stimulation or depression
 Stimulates cell activity or secretion
from glands
 Replacement
Categories of  Such as insulin
Drug Action  Inhibition or killing of organisms
 Bacterial inhibition
 Irritation
 Laxatives that irritate the inner wall
of the colon
 Peak Drug Level – is the highest
plasma concentration of drug at a
Peak and
Trough Drug specific time
Levels  Trough Drug Level – is the lowest
plasma concentration of a drug
 When immediate drug response is
desired, a large initial dose known
as the loading dose, of drug is
Loading Dose given to achieve a rapid minimum
effective concentration in the
plasma
 Side effects – are physiologic effects not
related to desired drug effects
 Adverse reactions – are more severe than
side effects; they are a range of untoward
Side Effects,
Adverse effects (unintended and occurring at normal
Reactions, and dose) of drugs that cause mild to severe side
Toxic Levels effects including anaphylaxis
 Toxic effects – can be identified by
monitoring the plasma therapeutic range of
the drug
 Is the effect of a drug action that
varies from a predicted drug
Pharmacogenetics response because of genetic factors
or hereditary influence
 Example: Ace inhibitors
 Tolerance – refers to a decreased responsiveness
over the course of therapy
 Dependence is a physiologic or psychological
need for a drug.
 Physical dependence is the physiologic need
Tolerance and for a drug to avoid physical withdrawal
Dependence symptoms (e.g., tachycardia in an opioid-
addicted patient).
 Psychological dependence is also known as
addiction and is the obsessive desire for the
euphoric effects of a drug.
 Is a psychologic benefit from a
Placebo Effect compound that may not have the
chemical structure of a drug effect

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Pharmacology

 Approximately 80% of drugs are

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