PHARMACODYNAMICS

(HOW THE DRUGS

AFFECT THE BODY)

Module II
Regie De Jesus, MAN

College of Health Sciences

Pharmacology
 PHARMACODYNAMICS
(“what a drug does to the body”)

• 1. Process by which drugs

influence the cell physiology to
achieve the desired result.
• 2. Pharmacodynamics refers to
how drugs alter body function at
the cellular level. It addresses the
therapeutic as well as the adverse
effects of drugs. 2
 How the Drugs Produce
their Effects
• All but a small number of drugs
interact with specific sites called
receptors.
• The receptor sites react with
certain chemicals to cause an
effect within the cell.
• 
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• Lock and Key Principle
– To better understand this process,
think of how a key works in a lock.
The specific chemical (the key)
approaches a cell membrane and finds
a perfect fit (the lock) at a receptor
site

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• a. Agonists (activators) bind to the
receptor on the cell membrane and
act on the cell through the receptor
to produce a pharmacologic effect.
• b. Antagonists (blockers) bind to
the receptor and prevent the cell
from producing an effect.
– May block the action of another drug.

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 Classification Examples

Agonists Salbutamol (a beta-2 agonist) binds to

(Activators) and activates beta-2 receptors in the
bronchiolar smooth muscles,
producing bronchodilation.
 
  Propranolol - a selective beta-blocker
Antagonists blocks beta- 1 receptors in the heart,
(Blockers) reducing the heart rate;
 
Ranitidine blocks H-2 (histamine)
receptors in the gastrointestinal tract,
reducing gastric acid and promoting
healing of duodenal and gastric ulcers.
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 Receptor Examples of drugs used to stimulate or
Subtypes block receptors
Adrenergic 
Propranolol blocks beta-1 and beta-2
receptors: receptors in the myocardium, reducing
alpha-1, heart rate and contractility. Used in
alpha-2 beta-1, hypertension and angina.
beta-2 
Doxazosin blocks alpha-1 receptors in
blood vessels, producing vasodilation.
Used in treatment of hypertension.

Salbutamol stimulates beta-2 receptors
on smooth muscles in bronchi,
producing bronchodilation. Used in
asthma.

Clonidine stimulates alpha-2 receptors
in the brain stem, thus reducing the
sympathetic nervous system outflow.
Used in hypertension.
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Cholinergic  Atropine is a muscarinic antagonist that blocks
receptors – bind the effect of acetylcholine. It is used to block the
acetylcholine parasympathetic nerve. Resulting effects include:
Muscarinic increased heart rate (M2) when used in the
receptors: management of bradycardia; reduced bronchial
M1 (neural, and gastrointestinal secretions (M1) when used
glandular), M2 as a pre-med in surgery; dilation of the pupils
(cardiac), M3 (M3) as an adverse effect.
(glandular), M4 and  Galantamine is used in the treatment of dementia
M5 (neural) to increase levels of acetylcholine in the brain. It
Nicotinic achieves this by inhibiting the action of
receptors: N1, N2 acetylcholinesterase. Galantamine also acts on
  nicotinic receptors in the brain to increase the
release of acetylcholine.
Serotonin • 5-HT antagonists, such as ondansetron (5HT3)
receptors and granisetron (5HT3), are used to treat nausea
• 5- by blocking the effect of serotonin in the
hydroxytryptamine gastrointestinal system and the vomiting center in
Subtypes: the medulla. These drugs are strong anti-emetics,
5-HT1, 2, 3 and 5 which is useful in patients receiving cytotoxic
drugs such as cisplatin, which releases 5-HT.
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Histamine 
H2 (gastric) antagonists, such as
receptors cimetidine and ranitidine, reduce gastric
Subtypes: acid production by blocking the effect of
H1, H2 and H3 histamine on the parietal cell. Used in
the treatment of peptic ulcer.

H1 antagonists, such as cyclizine, are
used to treat extreme nausea. H1
receptors are mainly located in the
bronchioles and gastrointestinal smooth
muscles. Other examples of drugs that
target these receptors are
antihistamines such as bilastine and
cetirizine

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 Term used to describe Definition
drug’s action at a receptor
site
Potency The ability of a drug to produce a
response when it binds to a receptor
 

Efficacy The ability of a drug to produce a

response when it binds to a receptor
 

Specificity The ability of a drug to combine with one

particular type of receptor. Examples of
receptors: acetylcholine, histamine and
adrenoreceptors.
 

Affinity The strength of attraction between a drug

and a receptor.
 
Therapeutic Index The relationship between a drug’s
desired therapeutic effects and its
adverse effects (margin of safety)
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 Interactions
• Drugs may interact with other drugs
or food to potentiate (synergize) or
antagonize block effects.
• For example, if hydrochlorothiazide
decreases blood pressure by 5 mm Hg
and metroprolol also decreases blood
pressure by 5 mm Hg, then giving
both of these agents to a hypertensive
patient would lower blood pressure by
10 mm Hg. 
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 Types of Interactions

• Potentiation, or synergy, means

that the action of one drug is
increased by the presence of a
second drug.
• An antagonistic effect occurs
when the action of one drug
reduces or blocks the effect of a
second.
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Example of Interactions
– For example, steroids administered to
a diabetic client block the effect of
insulin.
– For instance, when food that contains
Vitamin K (such as green, leafy
vegetables) is eaten by a person
taking warfarin, the drug’s
anticoagulation properties are
decreased and blood clots may form.

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 Examples of Drug
Interactions
Key Drug Additional Drug Likely Therapeutic/ Adverse
Outcome
Benzodiazepines, Alcohol Enhanced sedation or severe
e.g. diazepam central nervous system
depression resulting from additive
effects, as both drugs have
similar actions.
Beta-blocker Salbutamol In asthmatic patients, beta-
blockers may cause
bronchoconstriction and
precipitate an asthma attack.
Potassium Ace inhibitors Combination results in
Supplements hyperkalaemia.

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Contraindications or cautions

• Factor indicating that the use of a

particular drug will cause harm.
(allergy)
• Life- threatening situations.
(pregnancy and lactation)

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 Side Effects vs Adverse Effects

• Side effects - expected effect that

may or may not cause harm.
– Sometimes side effects become
intended effects. For example, anti-
coagulation is a side effect of aspirin
when aspirin is given for inflammation.
Yet at certain times, aspirin is given for
its anticoagulant activity.

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 Side Effects vs Adverse
Effects
• Adverse effects - Harmful and
unexpected. It may be seen as an
effect in any organ.
– Adverse reactions can assume many
forms and are highly dependent on the
specific drug.
• No drug does only what is desired of
it. All drugs have adverse effects
associated with them
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 Selective Toxicity
• Ideally, all chemotherapeutic agents
would act only on enzyme systems
that are essential for the life of a
pathogen or neoplastic cell and
would not affect healthy cells.
• The ability of a drug to attack only
those systems found in foreign cells
is known as selective toxicity.

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• For example
– Penicillin, an antibiotic used to
treat bacterial infections, has
selective toxicity. It affects an
enzyme system unique to bacteria,
causing bacterial cell death without
disrupting normal human cell
functioning.
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• Unfortunately, most other
chemotherapeutic agents also
destroy normal human cells,
causing many of the adverse effects
associated with antipathogen and
anti- neoplastic chemotherapy. (e.g.,
bone marrow cells, gastrointestinal
[GI] cells, hair follicles)

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 Toxicity
• The drug is acting as a toxin or poison.
• Nephrotoxicity is common because drugs
(parent compounds and metabolites) are
excreted here.
• Hepatotoxicity may occur because drugs are
chemicals and can easily damage the liver as
it metabolizes drugs.  
• Hematologic effects also occur and noted as
blood dyscrasia.

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 Hypersensitivty Reaction

• This occurs when the client is

sensitive to the effects of the
drug, has adverse symptoms, but
does not have a full allergic
reaction.

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 Allergic Reaction 
• An allergic reaction occurs when
the body recognizes the drug as
foreign and responds by histamine
release. The allergic reaction may
be mild and manifested by a rash,
urticaria, nausea, and diarrhea. Or
it may be very severe, causing
anaphylaxis.
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 Allergic Reaction 

• A patient cannot be allergic to a

drug that has never been taken,
(This is why skin testing is not
done among newborns) although
patients can have cross-allergies
to drugs within the same drug
class as one formerly taken.

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 Drug Hypersensitivity Examples Nursing Interventions
Allergy Reactions
Type
Type 1 • On first exposure to • Penicillin  Administer epinephrine as
Immediate drug, antibody • Iodine- ordered. Massage the site
(Anaphyla becomes attached to based to speed absorption rate.
ctic) surface of mast cells. contrast Repeat the dose every
• On second media 15–20 min, as appropriate.
exposure, the drug  Notify the prescriber and/
interacts with or primary caregiver and
antibodies (IgE) that discontinue the drug.
are fixed onto mast  Be aware that prevention
cells, triggering the is the best treatment.
release of histamine,  Counsel patients with
inducing anaphylaxis. known allergies to wear
Medic-Alert identification
and, if appropriate, to carry
an emergency epinephrine
kit.

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 Drug Hypersensitivity Examples Nursing
Allergy Reactions Interventions
Type
Type II • On first exposure, • Methyldopa  Notify the
Cytotoxic antibody attached to • Clozapine- prescriber and/or
surface of red cells. induced primary caregiver
• On second exposure, agranulocytosis and discontinue the
antibody and drug drug.
combination on surface  Support the patient
of red blood cell activates to prevent infection
complement, resulting in and conserve
destruction/ lysis of red energy until the
cells. White cells may allergic response is
also be destroyed. over.
Outcome depends on
blood cells involved in
reaction.
 
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Drug Allergy Hypersensitivity Examples Nursing
Type Reactions Interventions
Type III Antibody and antigen Gold or Notify the
Serum combine in the penicillamine prescriber and/or
sickness circulation forming an therapy used in primary caregiver
immune complex. This rheumatoid arthritis and discontinue the
complex stays in the drug.
circulation or in the  
tissue, activating Provide comfort
complement which then measures to help
stimulates inflammation. the patient cope
The inflammatory with the signs and
response damages the symptoms (cool
walls of blood vessels environment, skin
or tissue complex care, positioning,
becomes lodged in ice to joints,
tissues such as the administer
joints and kidneys. antipyretics or anti-
  inflammatory
• Resulting symptoms agents, as
include: rash, fever appropriate).
arthritis, swollen lymph 31
nodes.
Drug Allergy Hypersensitivity Examples Nursing
Type Reactions Interventions
Type IV T-lymphocytes react Gold therapy Notify the
Rashes with the drug to (serious rashes) prescriber and/or
(Delayed) stimulate an Ampicillin (mild primary caregiver
inflammatory response. rashes) and discontinue
This type of reaction drug.
may be delayed for at  
least 12 hours and Provide skin care
usually causes rashes, and comfort
contact dermatitis and measures that may
eczema. include
  antihistamines or
Most are non-life topical
threatening but toxic corticosteroids.
epidermal necrolysis (an
inflammatory skin
condition resulting in
breakdown of the skin)
can occur very rarely.
This is associated with a
35% mortality rate.
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 Pharmacotherapeutics/
INDICATIONS
• 1. The desired effect is the intended
effect or the reason the drug is
administered to a particular client at a
given time.
• 2. At times the drug needed has toxic side
effects, and the benefits must outweigh
the risks
• 3. The intended effect of the drug must be
appropriate for the client and the illness.

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 Not All Therapy is the same
• Acute Therapy, if the patient is critically
ill and requires acute intensive therapy
• Empiric therapy, based on practical
experience rather than on pure scientific
data
• Maintenance Therapy, for patients with
chronic conditions that don’t resolve

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• Supplemental or Replacement Therapy, to
replenish or substitute for missing substances
in the body
• Supportive Therapy, which doesn’t treat the
cause of the disease but maintains other
threatened body systems until the patient’s
condition resolves
• Palliative Therapy, used for end-stage or
terminal diseases to make the patient as
comfortable as possible.

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