WHAT YOU NEED TO

KNOW
Basic Pharmacology for Health Fitness
Practitioners
by Marcus W. Kilpatrick, Ph.D., FACSM, and Carlos Rodriguez, M.D.

LEARNING OBJECTIVE
Learn basic principles of general pharmacology and specific
knowledge related to pharmaceutical agents that are encountered
frequently by health and fitness professionals.

making certain that exercise is safe and effective for Rx and OTC users. Therefore, the
purpose of this article is to introduce pharmacological concepts and provide health fitness
practitioners a guide to the impact of medications on the exercise response.

BASIC PHARMACOLOGICAL PRINCIPLES

Key words:
Pharmacology, Drugs, Medications, Exercise

INTRODUCTION

Given the intricacies of drugs and how they

impact human physiology, the abundance of
terms with technical descriptions is not surprising.
Although a high level of understanding is not a
requirement for health fitness practitioners, a
basic understanding of terms like those provided
within Table 1 and the sections that follow empower the practitioner to access this important
information more comfortably.

ecent data indicate that about one half

of all Americans use a prescription
(Rx) drug monthly, with one fifth of
adults reporting taking three or more Rx drugs
(2). These numbers represent significant increases from 20 years ago (2) and do not
include the use of over-the-counter (OTC)
medications, in which sales have ballooned to
about $15 billion dollars annually (1). These
figures coincide with increased efforts to
prescribe exercise as a means of maintaining
and improving health. Specifically, the American College of Sports Medicine and the
American Medical Association teamed to
launch the Exercise is MedicineA initiative. This
initiative calls on patients and physicians to
discuss the role of physical activity in disease
prevention and medical treatment. The need for
increased physical activity among all Americans and especially those individuals regularly
taking medications is clear, and health fitness
professionals will play an important role in
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What You Need to Know

TABLE 1: Terminology
Term

Description

Notes

Pharmaceutical

A drug, medicine, or chemical substance intended to produce

a desired clinical outcome.

All related words based on the Greek word pharmakeia, which

translates as drug in modern Greek and poison in ancient
Greek.

Pharmacology

Science of medicine and biology of pharmaceutical agents.

The field as a discipline dates to ancient times, but scientific history

dates to the mid-19th centurys resurgence of biomedical research.

Pharmacodynamics

Study of the actions of the drug on the body or the mechanism of

action (biochemical) and medicinal effect (physiological effects).

Includes considerations of how the drug functions, drug interactions,

and side effects.

Pharmacokinetics

Study of how the body acts on the drug, including the absorption,
distribution, metabolism, and elimination from the body.

Regulation
The control of pharmacological agents within the United States is
managed by the Drug Enforcement Administration (DEA) and the
Food and Drug Administration (FDA). The DEA is primarily
concerned with the control of substances with a high potential for
abuse and addiction. In contrast, the FDA functions to ensure the
safety and efficacy of medications. The FDA also serves important
roles in regulating which drugs are available by Rx only (or
available OTC) and approves the development of generic drugs.
Importantly, the FDA oversees drug approval and monitors drugrelated side effects to ensure consumer safety. Collectively, these
two agencies have authority and responsibility in promoting public
safety and health with respect to pharmacological agents.

Administration
Formal administration of the pharmaceutical relates to how the
medication enters the body. The most common delivery
methods are listed and briefly described in Table 2. Routes of
administration vary dependent on the characteristics of the
medication. Some medications must be delivered through
specific routes to achieve the desired effect because administration through alternative routes may result in drug metabolism
and lessened drug potency, whereas other treatments can be

achieved by using multiple methods. For example, pain may be

treated via OTC oral medications such as ibuprofen, Rx cream
medications such as naproxen, prescribed transdermal pain
patches such as lidocaine, and intravenous medications such as
hydromorphone. This example makes clear that medications
come in a variety of forms, which provides numerous options
for pain management, including new versions that can be
delivered via lollipops! As such, delivery method is influenced
by desired onset, speed of absorption, and other factors.

Medication Safety
The appropriateness of a pharmaceutical agent significantly
depends on safety and effectiveness. Medications are described
as being indicated when use is considered safe, appropriate,
and effective. In contrast, medications are contraindicated
when use is not recommended because of safety or other
concerns. For example, angiotensin converting enzyme (ACE)
inhibitors are indicated in the treatment of hypertension, but
their use is contraindicated in women who are pregnant.
Importantly, many drugs are approved for specific medical
conditions but used in an off-label manner at the discretion of
the clinician for the treatment of other conditions. Migraine
sufferers, for example, are sometimes prescribed a variety of

TABLE 2: Common Routes of Administration

Route

Description and Notes

Examples

Oral

By mouth. Most common route for Rx and OTC. Swallowed as pill or liquid.

Lipitor (atorvastatin) for treatment of

hyperlipidemia.

Sublingual

Below the tongue. Selected when rapid absorption is important. Primarily via drops or film.

Nitrostat (nitroglycerin) for treatment of angina.

Inhalation

By nasal passages or orally inhaled. Often taken via inhaler or nebulizing treatment
and machine.

Proventil (albuterol) for treatment of

asthma-related symptoms.

Topical

By skin through the use of a cream or ointment. Intended for local effect only.

Voltaren (diclofenac) for treatment of joint pain

Transdermal

By skin through the use of a patch. Intended for a general effect on the body.

Duragesic (fentanyl) for treatment of pain.

Subcutaneous

By injection into fat tissue below the skin. Selected for slow absorption.

Humulin (insulin) for treatment of diabetes.

Intramuscular

By injection into muscular mass, typically either the deltoid or gluteus. Selected
when relatively rapid absorption is desired.

Toradol (ketorolac) for treatment of pain.

Intravenous

By injection into a vein. Typically using an intravenous bag.

Cardene SR (nicardipine) for treatment of

hypertension.

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FDA-approved medications, including beta-blockers, diuretics,

and antidepressants for the prevention of headaches. An issue
closely related to safety is the presence of adverse effects, which
are harmful and undesirable side effects of medical treatment.
Increased awareness of common adverse effects from medications in general and specific medications represents a great
opportunity for health fitness practitioners to better serve their
clients and patients.

CATEGORIES OF PHARMACEUTICALS
Although the division and organization of pharmaceutical drug
categories might be of some interest to health and fitness
professionals, the focus within this article is the presentation of
classes of drugs (some Rx and some OTC) that commonly are
encountered by practitioners promoting physical activity.
Special attention will be given to medications that alter the
exercise response in ways that could impact fitness assessments

and exercise prescriptions. The sections that follow provide a

brief introduction to the various drug classes, whereas Table 3
serves as a quick reference for information related to their
impact on important physiological responses.

Antihypertensive Medications
A variety of drug classes are available to treat hypertension by
regulation of contractile force and electrical activity of the heart,
dilatation of the vasculature, and vascular blood volume.
Importantly, many of these medications significantly impact
heart rate (HR) and blood pressure (BP) and therefore require
the attention of the health fitness practitioner. Four important
types of medications within this category are diuretics, betablockers, calcium-channel blockers, nitrates, and ACE inhibitors. The best and perhaps most powerful example is provided
by way of beta-blockers. These drugs function to reduce the
activity of the sympathetic nervous system so as to reduce the

TABLE 3: Quick Reference to Impacts of Common Drugs on the Exercise Response

Drug Class

Examples Drugs Brand (Generic)

Heart
Rate

Blood
Pressure

Diuretics

Hydrodiuril (hydrochlorothiazide)

Tenormin (atenolol)

HR reductions are 10 to 30 BPM on average

Procardia (nifedipine)

Effect on HR depends on class of

calcium-channel blocker used

Beta-blockers

Notes and Considerations

Lopressor (metoprolol)
Calcium-channel
blockers

Cardizem (diltiazem)

ACE inhibitors

Prinivil (lisinopril)

Lipid medications

Lipitor (atorvastatin), Zocor (simvastatin)

Analgesic agents

Advil (ibuprofen), Deltasone (prednisone),

Celebrex (celecoxib)

Anticholinergic
agents

Spiriva (tiotropium), Atrovent (ipratropium)

Beta-agonists

Norepinephrine, amphetamine

Vasodilators

Nitrostat (nitroglycerin)

Antiarrhythmic
agents

Betapace (sotalol), Lanoxin (digoxin)

Antidepressants

Paxil (paroxetine), Prozac (fluoxetine)

Notable exception is nicotinic acid,

which may decrease BP

Effects depend on formulation, dose,

and length of use

Alcohol

Potential increase in BP is linked to chronic use

Caffeine

Acutely may increase HR and BP; chronically has

little impact on HR and BP

Nicotine

Antihistamines

Zyrtec (cetirizine), Benadryl

(diphenhydramine)

Hypothyroid agents

Synthroid (levothyroxine)

Decreased BP occurs in about half of patients

Weight loss agents

Alli or Xenical (orlistat), Qsymia

(phentermine/topiramate)

Increased HR and BP occur with the use

of weight loss agents that are stimulants

More detailed descriptions of impacts on physiological and electrocardiographic responses can be located in other documents including ACSMs Guidelines for
Exercise Testing and Prescription, 8th edition; 2010.

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What You Need to Know

stress on the heart. Utilization of beta-blockers significantly
reduces both HR (20 to 30 BPM on average) and BP (reductions
are variable) during exercise, which requires an adjustment to
HR-based exercise prescriptions and increases the utility of
ratings of perceived exertion in monitoring exercise intensity.
Importantly, beta-blockers tend to increase exercise capacity in
cardiovascular disease patients by way of reducing ischemia and
subsequent chest pain. Such reductions in angina-related
symptoms is in fact a primary goal of many cardiovascular
medications, including calcium-channel blockers and nitrates,
whereas ACE inhibitors and diuretics provide cardiovascular
benefit by reducing plasma volume and overall cardiac stress.

pulmonary drug categories. These medications can have a

significant impact on the ability to exercise, especially in
asthmatics. In both asthmatics and nonasthmatics, beta-agonists
and anticholinergics potentially can enhance athletic performance
and their use in competition is restricted by many sanctioning
organizations. With respect to normal exercise participation,
individuals with asthma also are encouraged to include more
purposeful warm-ups and cooldowns, limit or avoid exercise when
cold-related symptoms are present, and to stop exercise immediately and use a short-acting bronchodilator (like albuterol) if
asthma symptoms develop during exercise.

Stimulants
Lipid-Lowering Medications
Medications designed to lower blood lipids are among the most
commonly prescribed drugs in medicine. Importantly, there are a
variety of blood lipids that impact health including low-density
lipoproteins (LDLs), high-density lipoproteins (HDLs), and
triglycerides. LDLs and triglycerides are associated with increased
cardiovascular risk and intravascular plaque formation whereas
HDL is considered to be cardioprotective. One class of lipid
medications commonly prescribed is the group referred to as
statins. These drugs function to block an enzyme linked to the
production of cholesterol. Importantly, the impact of statins on the
physiologic response to exercise generally is limited and therefore
not a major consideration for exercise prescription. One notable
exception is that some patients taking statins experience occasional
or persistent muscle soreness, discomfort, or weakness that could
lead to a severe condition known as rhabdomyolysis. Patients who
complain of unusual persistent muscle soreness should follow-up
with a physician because these specific symptoms serve as
contraindications for intense muscular activity.

Pulmonary Medications
Many pulmonary medications are classified as bronchodilators and
function to open up the bronchial tubes within the lungs to allow for
better flow of air. Beta-agonists are among the most common types
of bronchodilators. These drugs bind to receptors in smooth muscle
of the lungs, causing bronchodilation, and are formulated in both
short-acting and long-acting versions. Short-acting versions take
effect in minutes but dissipate quickly, whereas long-acting versions
take longer to take effect but last for hours. As such, short-acting
versions are considered rescue medications and used as needed
before or during exercise, whereas long-acting medications are for
prophylaxis (or prevention) and used daily. Asthmatics with mild
symptoms typically use a short-acting bronchodilator approximately 15 to 20 minutes before initiating exercise to prevent more
severe asthma symptoms during exercise, referred to as exerciseinduced asthma or EIA. Anticholinergic medications cause
bronchodilation by blocking chemicals that cause bronchial
constriction. Notably, many contemporary pulmonary medications
are combination drugs that include two agents from different

26

The class of drugs known as stimulants is characterized by their

actions on the body that increase psychomotor activities such as
wakefulness and alertness. These drugs typically are referred to in a
general way as uppers because of the produced effects. Drugs
categorized as stimulants include caffeine, nicotine, amphetamines,
cocaine, and ecstasy. Given the illicit nature of many stimulant
drugs, only caffeine, nicotine, and amphetamine-like medications
used to treat attention-related disorders such as attention deficithyperactivity disorder (ADHD) will be considered here. Caffeine is
a naturally occurring stimulant found primarily in food items such
as coffee, tea, and cocoa but also is processed as an additive for
products such as soft drinks and energy drinks. Similarly, nicotine is
found naturally in most tobacco products and has been synthesized
for inclusion in smoking cessation aids such as patches, gums, and
electronic cigarettes. Unlike caffeine and nicotine, ADHD
medications (e.g., Adderall, Ritalin) are available by Rx only
but are taken widely by adults and function as powerful central
nervous system stimulants. Each of these agents has significant
addictive potential and can increase resting HR and BP acutely.
One consideration related to caffeine consumption is that
relatively large intakes can produce a variety of symptoms that
could impact exercise participation, namely, feeling jittery
(sometimes to the point of feeling panicked), dehydration, and
emotional fatigue.

Diabetes Medications
The pharmacological treatment of diabetes is varied and
dependent on the specific type of diabetes mellitus that is
present. Those with type 1 diabetes are insulin dependent and
therefore receive some form of insulin therapy to help maintain
their blood glucose within a normal range. Importantly, insulin
can be administered using a variety of methods, and modern
approaches tend to be less invasive and center on providing a
plan that will maximize the ability of the patient to regulate
blood glucose levels. Importantly, diabetics should avoid
injecting insulin into the limbs before initiating an exercise
session and should instead administer the injection to the
abdominal region and limit abdominal or core-related exercise
in the period after injection. Likewise, significant physical

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activity should be avoided during the time frame associated

with peak insulin activity, which would be dependent on the
preparation of insulin being used. It is clear, therefore, that
patients with type 1 diabetes have much to consider, and
informed health fitness specialists can be an invaluable resource
for these individuals. In contrast to type 1 diabetes, most people
with type 2 diabetes are not insulin dependent and instead tend
to use a variety of oral medications to reduce and regulate blood
glucose. These medications include subclasses such as
sulfonylureas, biguanides, meglitinides, and thiazolidinediones.
Each functions to increase insulin production, insulin sensitivity, and/or reduce formation of glucose in the blood but also
have the potential side effect of inducing hypoglycemia.
Practitioners working with diabetic patients are encouraged to
be mindful of potential symptoms of hypoglycemia, including
hunger, dizziness, confusion, nervousness, and weakness. Such
symptoms are possible for any diabetic medication but more
likely with insulin therapy and sulfonylureas. In addition,
although diabetic medications tend to have a limited impact on
the exercise response, patients with diabetes must plan the
onset, duration, and intensity of exercise carefully because of
the insulin-like effect of exercise.

pain intensities that prevent participation in regular aerobic

exercise. In contrast, practitioners routinely will encounter
individuals seeking professional help from individuals taking
Rx or OTC medications. As such, the focus here will be on
acetaminophen and NSAIDs. The primary distinction between
these two drug classes is that acetaminophen helps to manage
pain, whereas NSAIDS have the ability to combat both pain and
inflammation. The most common NSAIDs available OTC
include aspirin, ibuprofen, and naproxen. Likewise, both groups
of medications also are available in higher dosages via Rx.
Although these groups of medications are known to provide
significant pain relief, they also are linked to many side effects
including problems related to the kidneys, gastrointestinal tract,
and blood clotting. One relatively new form of NSAID is a
group of medications referred to as COX-2 inhibitors. One such
drug is Celebrex (celecoxib), which is more selective in its
location of action and therefore tends to produce fewer side
effects in efforts to treat joint pain. Importantly, these
medications do not tend to impact the exercise response but
can impact the ability to exercise, and awareness regarding
client and patient usage is advised.

Weight Loss Medications

An important consideration for health fitness professionals is

recognition of the potential limitations related to their
education, knowledge, credentials, and experiences in pharmacology. Practitioners are encouraged to engage in ongoing
formal or informal education on this important issue that
impacts patients and clients in part because the increasingly
professional nature of employment linked to exercise science
demands knowledge in this area. However, health fitness
professionals are advised to seek the counsel of a physician or
other appropriately trained clinician when the issue is complex
or seems likely to have important health-related impacts. That
is, practitioners should work within the scope of their training

SCOPE OF PRACTICE
Drugs designed to combat obesity are available both by Rx and
OTC. These medications work through a variety of mechanisms
but typically exert their effects by reducing appetite, increasing
metabolism, or reducing caloric absorption from food. Among
the most popular weight loss drugs is orlistat, which is available
OTC as Alli and by Rx as Xenical. Recently, the FDA approved
two new Rx weight loss drugs, Qsymia (phentermine/
topiramate) and Belviq (lorcaserin). Clinical evidence suggests
that each of these drugs produces at least modestly beneficial
results but do so with a range of side effects, most of which
are relatively mild. Similarly, a wide range of OTC nutritional
supplements are available and represent big business for health
food and supplement stores, but there are ongoing concerns
related to the efficacy and safety of these products. Importantly,
practitioners should ask clients and patients to report their use
of any weight-regulation medication so that prescription of
exercise can be handled in the safest manner possible because
some of these agents can impact the cardiovascular response
modestly.

Analgesic Medications
Drugs used to treat pain and inflammation are diverse and used
in a wide variety of settings for aches, pains, and arthritisrelated symptoms. Primary pain medication classes are
acetaminophen, nonsteroidal anti-inflammatory drugs
(NSAIDs), steroids (or corticosteroids), and opioids. Although
practitioners may encounter individuals treating pain by way of
steroids and opioids, these individuals likely are dealing with
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What You Need to Know

and make certain that their role within any organization is defined
clearly. This structure allows practitioners to provide the best
possible counsel and care to members, clients, and patients.

TREATMENT COMPLIANCE ADVOCACY

One additional consideration for health fitness practitioners is
their role as an advocate for compliance with physician orders
related to drug usage or other clinical recommendations. This
issue is important given research data suggesting that patient
compliance with physician recommendations related to filling
and properly using Rx and OTC drugs is quite poor (3). The
personal relationship that often exists between the practitioner
and client or patient provides a unique opportunity to facilitate
improved compliance with prescribed pharmacological therapies. These relationships are built primarily around practitioner
expertise related to exercise and fitness, but the presence of a
personal relationship allows the practitioner to be well
positioned to provide social support and guidance that can
generate great benefit. Practitioners with a base of knowledge
related to pharmacology can engage their clients and patients
on the extent of their use of Rx and OTC drug usage, which can
create a significant pill burden or polypharmacy situation that
increases the risk of adverse effects. More generally, practitioners with a measure of knowledge and competence related to
pharmacology can assist the patient in recognizing signs,
symptoms, and side effects linked to medication usage and
noncompliance with drug therapy. Importantly, practitioners
should consider their individual skill sets and existing employer
guidelines when making decisions about their scope of practice
with respect to discussing pharmacological topics with patients
and clients. However, it is noteworthy that an encouraging
word from a trusted professional to take medications according
to labels and physician orders and to report any challenges
related to medication compliance represents another avenue for
health fitness professionals to make a difference in the life and
health of the people they serve. As such, knowledge related to
pharmacological concepts further demonstrates the importance
of the health fitness practitioner in promoting health and fitness
within our society.

SUMMARY
A very clear reality is that the daily work of the health fitness
practitioner is evolving toward the expectation that the
practitioner is knowledgeable about clinical issues such as
pharmacology. These changes are linked significantly to the
increased professional profile within our field. Embracing these
changes requires continued commitment on the part of our
excellent practitioners to be involved proactively in the health
and wellness of the patients and clients encountered on a daily
basis. This article serves to continue movement toward the goal
of healthier people and communities, a worthy goal that reflects
our important profession.

28

SMART PHONE RESOURCES

A variety of smart phone applications designed to
provide basic information about prescription drugs are now
available through the iTunes App Store and the Android
Market. Two popular low- and zero-cost options include
PocketPharmacist and Epocrates Rx.

References
1. Consumer Healthcare Products Association. OTC Retail SalesY1964Y2011.
Washington, (D.C.): Consumer Healthcare Products Association; 2012.
2. National Center for Health Statistics. Health, United States, 2011: With
Special Feature on Socioeconomic Status and Health. Hyattsville (MD):
National Center for Health Statistics; 2012.
3. Vermeire E, Hearnshaw H, Van Royen P, Denekens J. Patient adherence to
treatment: three decades of research. A comprehensive review. J Clin
Pharm Ther. 2001;26(5):331Y42.

Disclosure: The authors declare no conflicts of interest and do

not have any financial disclosures.
Marcus W. Kilpatrick, Ph.D., FACSM, is an
associate professor of Exercise Science in the
School of Physical Education and Exercise
Science at the University of South Florida. His
education is in the areas of nutrition, kinesiology, and health education. He teaches exercise
testing and prescription for healthy and clinical
populations, and his research interests include physical activity
motivation, perceived exertion, and mood.
Carlos Rodriguez, M.D., is an affiliate
assistant professor of Family Medicine at
the University of South Florida College of
Medicine. He also is the director of the Sports
Medicine Fellowship and assistant director
of the Family Medicine Residency at Bayfront
Medical Center. He is a board-certified
family physician with a Certificate of Added Qualifications in
Sports Medicine. His research interests include platelet-rich plasma
therapy injections, sports nutrition, and sports supplements.

CONDENSED VERSION AND BOTTOM LINE

Health fitness practitioners routinely provide services to
individuals taking a wide variety of prescription and overthe-counter medications. Increased knowledge regarding
terminology, drug categories, and impacts on the exercise
response is important to daily professional practice. This
article aims to provide an overview that empowers practitioners with knowledge that will allow for improved skill
in working with a wide range of populations.

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