CHAPTER 1 ORIENTATION TO PHARMACOLOGY

I. FOUR BASIC TERMS

A. DRUG – defined as any chemical that can affect living processes and have
therapeutic applications

B. PHARMACOLOGY - defined as the study of drugs and their interactions with living
systems
- encompasses the study of the physical and chemical properties of
drugs as well as their
biochemical and physiologic effects
- includes knowledge of the history, sources, and uses of drugs as well
as knowledge of drug
absorption, distribution, metabolism, and excretion

C. CLINICAL PHARMACOLOGY – defined as the study of drugs in humans (patients as

well as healthy volunteers)
- interaction between drugs and people

D. THERAPEUTICS – also known as pharmacotherapeutics

- defined as the use of drugs to diagnose, prevent, or treat disease or to
prevent pregnancy
- medical use of drugs

II. PROPERTIES OF AN IDEAL DRUG - there is no such thing as a perfect drug

A. BIG THREE:

1. Effectiveness – an effective drug is one that elicits the responses for

which it is given.
- effectiveness is the most important property a drug can have
***IF A DRUG IS NOT EFFECTIVE, IT SHOULD NOT BE
USED***
2. Safety – a safe drug is one that cannot produce harmful effects – even
is administered in very high
doses and for a very long time
- there is no such thing as a safe drug
- pharmakon – Greek word meaning poison
3. Selectivity – one that elicits only the response for which it is given
- there is no such thing as a selective drug: All medications cause
side effects

B. ADDITIONAL PROPERTIES OF AN IDEAL DRUG

1. Reversible Action – it is important that effects be reversible

- we want drug actions to subside within an appropriate time
 2. Predictability – since each patient is unique, the accuracy of certain
predictions cannot be
guaranteed
3. Ease of Administration – an ideal drug should be simple to
administer, the route should be
convenient, and the number of doses per day should be low
a. Benefits:
- it can enhance patient adherence
- it can decrease errors in drug administration

4. Freedom from Drug Interactions – when taking two or more drugs,

those drugs can interact with
one another in that they either augment or reduce drug responses
- possible impact of drug interactions must be considered
5. Low Cost – an ideal drug would be easy to afford
6. Chemical Stability – some drugs lose effectiveness during storage;
others which are stable on a
shelf can rapidly lose effectiveness when put into a solution
- losses in efficacy result from chemical instability
7. Possession of a Simple Generic Name – generic names are usually
complex and difficult to
remember and pronounce
- as a rule, the trade name for a drug is simpler than its generic
name

III. THERAPEUTIC OBJECTIVE

The objective of drug therapy is to provide maximum benefit with
minimum harm.

IV. FACTORS THAT DETERMINE THE INTENSITY OF DRUG RESPONSES

A. ADMINISTRATION – dosage size, route and timing of administration are important

determinants of drug
responses

B. PHARMACOKINETICS – pharmacokinetic processes determine how much of an

administered dose gets to its
sites of action

1. Major Pharmacokinetic Processes (impact of the body on drugs):

a. drug absorption b. drug distribution
c. drug metabolism d. drug excretion

C. PHARMACODYNAMICS (IMPACT OF DRUGS ON THE BODY) – once at the site of action,

pharmacodynamic
processes determine the nature and intensity of the response
 - initial step leading to a response is the binding of a drug to its receptor
which is followed by a
sequence of events the ultimately results in a response

PRESCRIBED DOSE
↓
↓ Administrati ╟medication errors
↓ ╟patient compliance
ADMINISTERED DOSE
↓
↓ Pharmacoki ╟absorption
↓ ╟distribution
↓ ╟metabolism
↓ ╟excretion
CONCENTRATION @
SITES OF ACTION Sources of individual variation
╟physiologic variables
↓ ╟pathologic
variables
↓ ╟genetic
variables Pharmacodyna
↓ ╟drug
interactions
↓ ╟drug-receptor interaction
INTENSITY OF ╟patient’s functional state
RESPONSES ╟placebo effects

D. SOURCES OF INDIVIDUAL VARIATION

- characteristics unique to each patient can influence pharmacokinetic
and pharmacodynamic
processes and, by doing so, can help determine the patient’s
response to a drug
- sources include drug interactions, physiologic variables (age, gender,
weight), pathophysiologic
variables (especially diminished function of the kidneys and liver,
the major organs of drug
elimination), and genetic variables (can alter the metabolism of
drugs and can predispose the patient to unique drug reactions)

***PATIENT ALWAYS HAS THE RIGHT TO REFUSE MEDICIATIONS***

Critical Thinking: What would be the perfect drug for a patient in chronic
pain?

First of all, there is no perfect drug.

Then consider: effectiveness
fast acting
affordable
safe reversibility