PHARMACOLOGY: PRELIMS

Chapter 1: Basic Principles of Pharmacology

PHARMACOLOGY - study of drugs

- study of the effects of chemicals on living organisms

DRUG - any substance that, when taken into a living organism, may modify
one or more of its functions
- Includes any substance that alters physiological function in the
organism, regardless of whether the effect is beneficial or harmful
CLINICAL - deals primarily with the beneficial effects of specific drugs on humans
PHARMACOLOGY and the manner in which these drugs exert their therapeutic effects

RELEVANCE OF PHARMACOLOGY IN REHABILITATION

- When you know how the various drugs may affect a patient and the mechanisms behind
those effects, you can apply that knowledge to get an optimal response from the patient’s
therapy treatment. For instance, you can improve a patient’s therapy session dramatically
by scheduling the therapy when certain drugs reach their peak effect, such as drugs that
decrease pain (analgesics) or improve the patient’s motor skills (anti-Parkinson drugs)

- when you understand a drug’s pharmacological aspects, you can avoid or control any
adverse responses from occurring due to direct interaction between the therapy treatment
and certain medications
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SUBAREAS OF PHARMACOLOGY

PHARMACOTHERAPEUTICS - area of pharmacology that refers to the use of specifi c

drugs to prevent, treat, or diagnose a disease
- primary concern is of the effects of drugs on humans,
with animal pharmacology mentioned only in reference
to drug testing and research in animal

2 FUNCTIONAL AREAS OF PHARMACOTHERAPEUTICS

Pharmacokinetics - study of how the body absorbs, distributes, and eliminates
the drug
Pharmacodynamics - the analysis of what the drug does to the body, including the
mechanism by which the drug exerts its effect
TOXICOLOGY - study of the harmful effects of chemicals
PHARMACY - deals with the preparation and dispensing of medications
PHARMACOGENETICS - new area of pharmacology
- It deals with the genetic basis for drug responses, especially
variations in drug response from person to person

DRUG NOMENCLATURE

*Each drug can be identified according to its chemical, generic, or trade name

CHEMICAL NAMES - refer to the specific compound’s structure and are usually
fairly long and cumbersome

GENERIC NAME - also known as the official or nonproprietary name

- tends to be somewhat shorter and is often derived from the
chemical name

TRADE NAME - also known as the brand name

- is assigned to the compound by the pharmaceutical company
and may or may not bear any reference to the chemical and
generic terminology

GENERIC DRUG - less expensive than its brand-name counterparts

- substitution can help reduce health-care costs
- should be as safe and effective as the original brand-name
product, provided that the generic form satisfies certain criteria
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- should undergo testing to establish that it has the same type and
amount of the active ingredient(s), the same administration
route, the same pharmacokinetic profile (e.g., drug absorption
plasma levels, metabolism), and the same therapeutic effects as
the brand-name drug

 Food and Drug Administration (FDA) (United States) - is responsible for monitoring the
use of existing drugs and for developing and approving new ones

 Health Products and Food Branch of the Department of National Health and Welfare
- whether the drug is effective in treating a certain condition
- whether the drug is reasonably safe for human use

DRUG APPROVAL PROCESS

1. Animal (Preclinical) Studies

- Drugs are typically tested in animals initially, often using several different species
- animal trials provide preliminary information on the pharmacokinetic and
pharmacodynamic properties of the compound and information on dosage and
toxicity

2. Human (Clinical) Studies

Phase I
- drug is usually tested in a relatively small number of healthy volunteers
- purpose of this phase is to obtain some initial information about the
pharmacological actions and the drug’s possible toxic effects in humans
- 10 and 100 subjects are studied but the actual number of subjects will vary
according to the drug

Phase II
- The drug is tested in a relatively small sample (50 to 500 people) with a
specific disease or pathological condition
- primary goal is to evaluate the dosage range and effectiveness of the drug
and to assess the side effects and other risks

Phase III
- clinical evaluation is expanded to include more patients (several hundred to
several thousand) and more evaluators
- The larger patient population provides additional information regarding the
drug’s safety and effectiveness

*The time for the entire testing process from the beginning of animal trials to the end of phase III
human testing may be as long as 7 to 9 years
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 POSTMARKETING SURVEILLANCE - refers to all of the methods used to continue

monitoring drug safety and effectiveness after approval for public use
- These methods often consist of reports from health-care providers that
describe specific rare adverse effects that were not discovered during
clinical testing

ORPHAN DRUGS - drugs that treat rare diseases

OFF-LABEL - the use of a drug to treat conditions other than those that the drug
PRESCRIBING was originally approved to treat

PRESCRIPTION VERSUS OVER-THE-COUNTER MEDICATION

Nonprescription drugs or over Prescription Medications
the-counter (OTC) drugs - must be ordered or
- can be purchased directly by dispensed only by an
the consumer authorized practitioner
- are used to treat relatively
minor problems and to make
the consumer more
comfortable until the
condition is resolved

examples:
- ibuprofen (Advil, Motrin)
- loratadine (Claritin)
- cimetidine (Tagamet)

Comprehensive Drug Abuse Prevention and Control Act (or Controlled Substances Act) -
placed drugs into specific categories, or “schedules,” according to their potential for abuse
Schedule I
- drugs are regarded as having the highest potential for abuse and are not typically used as an
acceptable medical treatment
- include heroin, lysergic acid diethylamide (LSD), psilocybin, mescaline, peyote, and several
other hallucinogens

Schedule II
- Drugs in this category are approved for specific therapeutic purposes but still have a high
potential for abuse and possible addiction.
- include opioids, such as morphine and fentanyl, and drugs containing amphetamine
derivatives

Schedule III
- drugs have a lower abuse potential than those in schedules I and II
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- include certain opioids (e.g., codeine) that are combined in a limited dosage with other
nonopioid drugs. Other drugs in this category include anabolic steroids, certain
barbiturates, and amphetamines that are not included in schedule II

Schedule IV
- These drugs supposedly have a lower potential for abuse than schedule III drugs, with only
a limited possibility of physical dependence, psychological dependence, or both
- include certain antianxiety drugs (meprobamate), certain barbiturates (barbital,
phenobarbital), and a variety of other depressants and stimulants

Schedule V
- These drugs have the lowest relative abuse potential
- Drugs in this category consist primarily of low doses of opioids that are used in cough
medications and antidiarrheal preparations

BASIC CONCEPTS IN DRUG THERAPY

DOSE-RESPONSE - provides information about the dosage range over which the drug
CURVE is effective, as well as the peak response that can be expected from
the drug
- plateau indicates that there will be no further increment in the
response, even if the dosage continues to be increased
- ceiling effect, or maximal effect, of the drug - the point at which
there is no further increase in the response
POTENCY - related to the dose that produces a given response in a specific
amplitude
- less of the compound is required to produce a given response

MEDIAN TOXIC DOSE (TD50) - The dose at which 50 percent of the group exhibits the adverse
effect
MEDIAN LETHAL DOSE (LD50) - the dose that causes death in 50 percent of the animals studied
THERAPEUTIC INDEX

- used as an indicator of the drug’s safety

- greater the value, the safer the drug is considered to be
- indicates that it takes a much larger dose to evoke a toxic response than it does to cause a
beneficial effect