PT 112 Pharmacology in PT

Marsha Angela Y. Manuel

mymanuel@mmsu.edu.ph
 Objectives
At the end of the session, the student will be able to:
1. Discuss adrenergic drugs and its sub-classifications
2. Identify other drugs that inhibit adrenergic
neurons
ADRENERGIC DRUGS
INTRODUCTION
• Many adrenergic agonists and antagonists exert their effects by
binding directly to the appropriate postsynaptic receptor. Since a
great deal of the specificity (or lack of specificity) of these drugs
depends on the drug-receptor interaction.
Adrenergic Receptor
Subclassifications
• Adrenergic receptors can be divided into two primary categories:
alpha and beta receptors.
• Each category can then be subdivided, so that five receptor
subtypes are commonly identified: alpha-1, alpha-2, beta-1, beta-2,
and beta-3.
• Alpha-1 receptors have been further categorized as alpha 1a, 1b,
and 1d receptors, and alpha-2 receptors have been subdivided into
alpha 2a, 2b, and 2c receptors.
Adrenergic Agonists
Alpha Agonists
Alpha-1–Selective Agonists
General Indications
• Alpha-1 agonists bind directly to and activate the alpha-1 receptor
located primarily on vascular smooth muscle, thus leading to
smooth-muscle contraction and vasoconstriction.
• Used to treat acute hypotension occurring in emergencies such as
shock or during general anesthesia
• Common clinical application of these drugs is the treatment of
nasal congestion (i.e., runny nose and stuffy head feelings
associated with the common cold)
• Alpha-1 agonists is used to decrease heart rate during attacks of
paroxysmal supraventricular tachycardia by increasing peripheral
vascular resistance, these drugs bring about a reflex decrease in
heart rate through the cardiac baroreceptor reflex.
Adverse Effects
• Some of the more frequent side effects include increased blood
pressure, headache, and an abnormally slow heart rate (because of
reflex bradycardia), chest pain, difficulty breathing, and feelings of
nervousness.
Alpha-2–Selective
Agonists
General Indications
• Alpha-2–selective drugs are used primarily in the treatment of
hypertension and spasticity. When treating hypertension, these
drugs stimulate alpha-2 receptors located in the brain and
brainstem. When stimulated, these central alpha-2 receptors exert
an inhibitory effect on sympathetic discharge from the vasomotor
center in the brainstem.
• Alpha-2 receptors have also been identified on interneurons in the
spinal cord. Stimulation of these receptors causes interneuron
inhibition, and a subsequent decrease in excitability of motor
neurons supplied by the interneurons.

• Spasticity is a symptom associated with damage to the brain, spinal

cord or motor nerves, and is seen in individuals with neurological
conditions
Adverse Effects
• Use of alpha-2–specific drugs may be associated with some
relatively minor side effects such as dizziness, drowsiness, and dry
mouth.
• More pronounced adverse effects such as difficult breathing, an
unusually slow heart rate, and persistent fainting may indicate a
toxic accumulation or overdose of these drugs.
Beta Agonists
Beta-1–Selective Agonists
General Indications
• The beta-1 receptor is located primarily on the myocardium, and
stimulation of the receptor results in increased heart rate and
increased force of myocardial contraction (i.e., increased cardiac
output).
• Also used primarily to increase cardiac output in emergency
situations such as cardiovascular shock or if complications develop
during cardiac surgery.
Adverse Effects
• Because of their cardiostimulatory effects, beta- 1–selective drugs
may induce side effects such as chest pain and cardiac arrhythmias
in some patients as well as shortness of breath and difficulty in
breathing (i.e., feelings of chest constriction).
Beta-2–Selective Agonists
General Indications
• One important location of beta-2 receptors is on bronchiole smooth
muscle. When stimulated, the receptor mediates relaxation of the
bronchioles.
• Beta-2 agonists are administered to treat the bronchospasm
associated with respiratory ailments such as asthma, bronchitis, and
emphysema.
• Beta-2–selective bronchodilators. This group of drugs includes
albuterol (Proventil, Ventolin, others), fenoterol (Berotec).
• Since a nonselective beta agonist will also stimulate the
myocardium (beta-1 effect), beta-2–selective agonists are often
used preferentially in treating asthma, especially if the patient has a
cardiac abnormality such as ischemia or arrhythmias.
• Another clinically important location of beta-2 receptors is on
uterine muscle.
• eg. ritodrine and terbutaline
Adverse Effects
• The primary side effects associated with beta-2– specific drugs
include nervousness, restlessness, and trembling.
• Excessive use of beta-2 agonists may cause increased airway
hyperresponsiveness, which could lead to severe and possibly fatal
asthmatic attacks
• Increase in maternal heart rate and systolic blood pressure, as well
as maternal pulmonary edema that could be quite severe and may
be fatal to the mother.
Drugs with Mixed Alpha and
Beta-Agonist Activity
General Indications
• Several drugs are available that display a rather mixed agonistic
activity with regard to adrenergic receptor subtypes.
• Some drugs, like epinephrine, appear to be able to stimulate all
four adrenergic receptor subtypes.
• Other drugs, such as norepinephrine, bind to both types of alpha
receptors, bind to beta-1 receptors to a lesser extent, and show little
or no affinity for beta-2 receptors.
• Another group of indirect adrenergic agonists (ephedrine,
metaraminol) appear to act as nonselective agonists because of
their ability to increase the release of norepinephrine from
presynaptic storage sites.
• eg. Amphetamines, ephedrine, epinephrine
Adverse Effects
• Nervousness, restlessness, and anxiety.
• Prolonged or excessive use may also lead to complications such as
hypertension, arrhythmias, and even cardiac arrest.
• Prolonged administration via inhalation may also cause some
degree of bronchial irritation with some agents.
Adrenergic Antagonists
• These agents are often referred to as sympatholytic drugs because
of their ability to block the receptors that typically mediate
sympathetic responses (i.e., alpha and beta receptors).

• Clinically useful adrenergic antagonists usually show a fairly high

degree of specificity for one of the major receptor classifications.
Alpha Antagonist
General Indications
• Alpha antagonists are administered primarily to reduce peripheral
vascular tone by blocking the alpha- 1 receptors located on
vascular smooth muscle.
• Consequently, alpha antagonists are used in conditions where
peripheral vasodilation would be beneficial. A principal application
of these agents, for instance, is in treating hypertension
• These drugs have been used to promote vasodilation in conditions
of vascular insufficiency, including peripheral vascular disease and
Raynaud phenomenon.
• Alpha-1 receptors located on smooth muscle in the prostate
capsule, neck of the bladder, and urethra cause muscle constriction
that restricts urine flow and the ability to empty the bladder.
• By blocking these receptors, alpha-1 antagonists relax these
smooth muscles and allow voiding urine more easily and
completely.
• BPH-doxazosin
• A group of drugs known collectively as ergot derivatives display
some alpha-blocking ability.
• Ergot alkaloids and ergoloid mesylates and are used clinically for
diverse problems, including the treatment of vascular headache and
improvement of mental function in presenile dementia.
Adverse Effects Of Alpha-1 Antagonists
• One of the primary adverse effects associated with alpha
antagonists is reflex tachycardia. By blockingalpha-1 receptors,
these drugs tend to decrease blood pressure by decreasing
peripheral vascular resistance.
• A second major problem with these drugs is orthostatic
hypotension. Dizziness and syncope following changes in posture
are quite common due to the decrease in peripheral vascular tone.
Beta Antagonists
General Indications
• Beta antagonists are generally administered for their effect on the
beta-1 receptors that are located on the heart.
• When stimulated, these receptors mediate an increase in cardiac
contractility and rate of contraction.
• Used to decrease cardiac workload in conditions such as
hypertension and certain types of angina pectoris and normalize
heart rate in certain forms of cardiac arrhythmias.
Adverse Effects
• The antagonism of beta-2 receptors on bronchiole smooth muscle
often leads to some degree of bronchoconstriction and an increase
in airway resistance
• Patients with respiratory problems such as asthma, bronchitis, and
emphysema may be adversely affected by nonselective beta
antagonists.
• In these patients, one of the beta-1–selective antagonist drugs
should be administered.
• Excessive depression of cardiac output, orthostatic hypotension,
dizziness and syncope
• Depression, lethargy, and sleep disorders
THE END
References
• Ciccone, Charles D. Pharmacology in Rehabilitation, 5th Edition,
2015. F.A. Davis Company
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