HOW THE BODY

AFFECTS THE
DRUGS

Module I
Regie De Jesus, MAN
College of Health Sciences
Pharmacology
What is Pharmacology?
• Pharmacology (from pharmakon, the Greek
word for drug) is the study of drugs
(substances that produce changes in the
body) and the characterization of their:
– Structure, targets, and mechanisms of action
– Distribution in and handling by the body
– Effects on the body, including desirable
responses (efficacy) and undesirable side-
effects (toxicity)

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What is Pharmacology?
• Pharmacology can be studied at multiple
ways:
– Clinical pharmacology is the study of
drugs in human patients
– Toxicology is the study of harmful rather
than therapeutic effects
– Pharmacy involves manufacture,
preparation, and dispensing of drugs

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• Nurses deal with pharmacotherapeutics, or
clinical pharmacology, the branch of
pharmacology that uses drugs to treat,
prevent, and diagnose disease.

• Clinical pharmacology addresses two key

concerns: the drug’s effects on the body and
the body’s response to the drug.

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 What’s in a name?
• Drug’s Nomenclature
– Chemical name – a scientific name that
precisely describes its atomic and molecular
structure
– Generic name- an abbreviation of the
chemical name
• a.k.a the nonproprietary name because it is not
restricted by trademark.
• used worldwide as established through WHO
• Some have family ties

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• Trade name (aka
brand name or
proprietary name) -
selected by the drug
company selling the
product
– Trade names are
protected by copyright
with the symbol ®
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 Drug Nomenclature (Names)

Chemical Name Generic Name Trade Name

7-chloro-1,3-dihydro-1- Diazepam Valium

methyl-5 phenyl 2H-1,
4-benzodiazepin 2-one
Ethyl 1-methyl 4- meperidine Demerol
pheyli-sonipecotate
hydrochloride
acetylsalicyclic aspirin Ecotrin
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 REMEMBER!
• To avoid confusion, it’s best to use a
drug’s generic name because any one
drug can have a number of trade
names.

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 Drug Sources
• Plants - the leaves, roots, bulb, stem,
seeds, buds, and blossoms
– Isolating & intensifying the active
components
• Animals - body fluids or glands of
animals e.g. insulin, enzymes, pepsin,
vaccines

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 Drug Sources
• Minerals - occur in nature or are
combined with other ingredients
– E.g. iron, iodine
• Synthetic – laboratory-made drugs, e.g.
ranitidine

Copyright © 2007 by Thomson Delmar Learning. ALL RIGHTS RESERVED. 11

 Phases of New Drug
Development
• Phase I
– The drug is tested on healthy volunteers in
phase I.
• Phase II
– Phase II involves trials with people who
have the disease for which the drug is
thought to be effective.

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• Phase III
– Large numbers of patients in medical
research centers receive the drug in phase
III. This larger sampling provides
information about infrequent or rare
adverse effects.

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• Phase IV
– Phase IV is voluntary and involves
postmarket surveillance of the drug’s
therapeutic effects at the completion of
phase III. The pharmaceutical company
receives reports from doctors and other
health care professionals about the
therapeutic results and adverse effects of
the drug..

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 Pharmacokinetics
(“what the body does to a drug” )
• deals with a drug’s actions as it moves
through the body
• discusses how a drug is:
– absorbed (taken into the body)
– distributed (moved into various tissues)
– metabolized (changed into a form that can
be excreted)
– excreted (removed from the body).

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 Pharmacokinetics
• Onset of action is the time it takes for the
drug to reach its minimum effective
concentration.
• Peak effect occurs when the drug is
exerting its maximum effect and is at its
highest concentration.
• Duration of action is the length of time that
the drug remains above its minimum
effective concentration.
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 A. Absorption
• This covers a drug’s progress from the
time it’s administered, through its
passage to the tissues, until it reaches
systemic circulation.
• All administration routes (except the
intravenous route) require the drug to go
through absorption

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Factors affecting Absorption
• Taking a bite
– Pinocytosis is a unique form of active
transport that occurs when a cell engulfs a
drug particle (e.g. Vita A,D,E,K)
• Watch the speed limit!
– Typically, absorption occurs within seconds
or minutes when a drug is administered
sublingually, I.V., or by inhalation.

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• Not so fast
– Absorption occurs at a slower rate when drugs
are administered by the oral, I.M., or subQ routes
• At a snail’s pace
– Some drugs can take several hours or days to
reach peak. (e.g. rectally administered or
sustained-release drugs)
– The slowest form of absorption is through the
skin and mucous membranes.

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• Not enough time
– Other factors can affect how quickly a drug
is absorbed. (E.g. patient who has had
large sections of the small intestine
surgically removed, drug absorption is
decreased)

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• Look to the liver
– Drugs absorbed by the small intestine are
transported to the liver before being
circulated to the rest of the body.
– The liver may metabolize much of the drug
before it enters the circulation.
– This mechanism is referred to as the first-
pass effect.
• lowers the amount of active drug released into
the systemic circulation.
• Therefore, higher drug dosages must be
administered to achieve the desired effect.
•  

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• More blood, more absorption
– Increased blood flow to an absorption site
improves drug absorption, whereas
reduced blood flow decreases absorption
(deltoid is faster than gluteal)
• Slowed by pain and stress
– Pain and stress can decrease the amount
of drug absorbed because autonomic
response to pain
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• High fat doesn’t help
– High-fat meals and solid foods slow the rate
at which contents leave the stomach and
enter the intestines, delaying intestinal
absorption of a drug.
•  

• Dosage form factors

– Drug formulation (such as tablets, capsules,
liquids, sustained-release formulas) affects
the drug absorption rate 

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• Absorption increase or decrease?
– Combining one drug with another drug, or
with food, can cause interactions that
increase or decrease drug absorption,
depending on the substances involved.

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 First-Pass Effect
• drugs absorbed from the gastrointestinal
tract enter the liver via the hepatic portal
vein and are subjected to metabolism by
the liver before reaching the main
circulation.
• This is why oral doses must be higher
than intravenous (IV) doses, which will
directly enter the bloodstream without
entering the liver. 

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 Example:
– For instance, more than
90% of the anti- anginal
drug glyceryl trinitrate
(GTN) is eliminated by first-
pass metabolism.
– For this reason, a simple
tablet formulation of this
drug, administered orally,
will be almost completely
ineffective.
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• Bioavailability- is a measure of the rate
and extent of drug transfer from its
administration site to the systemic
circulation.
– Intravenous injection is deemed to have the
highest bioavailability (100%).

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 Distribution
• Drug distribution is the process by which
the drug is delivered from the systemic
circulation to body tissues and fluids

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Factors affecting Distribution
– Blood flow
• The drug is quickly distributed to organs with a
large supply of blood.
•  

– Solubility
• depends on whether the drug is water or lipid
(fat) soluble. Lipid-soluble drugs easily cross
through cell membranes; water-soluble drugs
can’t.
• Lipid-soluble drugs can also cross the blood-
brain barrier and enter the brain.
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 Example for Solubility
• Example
– A common example of this is dopamine,
which does not cross the BBB and therefore
cannot be used directly to treat the
dopamine deficiency seen in Parkinson’s
disease. Instead, the prodrug levodopa is
given. This is non-polar, and readily crosses
the BBB. Once the levodopa reaches the
brain, it is converted to dopamine 

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Factors affecting Distribution
– Protein binding
• A drug comes in contact with proteins such as the
plasma protein albumin.
• The drug can remain free or bind to the protein. Only
the free, or unbound, portion remains active and
can exert a pharmacological effect.
• Example
– Warfarin is a typical example, and shows about 99% binding
to plasma albumin. If any factor changes the degree of
plasma protein binding, such as hypoalbuminaemia. This may
lead to toxicity, in the form of an enhanced anticoagulant
effect and bleeding.

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 C. Metabolism
• Aka. Biotransformation
• Biotransformation is the process by
which a drug is enzymatically converted
to a simpler compound.
• It occurs in the liver, so that persons
with liver disease will have difficulty
metabolizing drugs.

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 Factors affecting Metabolism
– Conditional considerations
• Certain diseases can reduce metabolism such as cirrhosis.
– Stress test
• Environment, too, can alter drug metabolism. For example,
cigarette smoke & stressful situation such as prolonged illness,
surgery, or injury, can change how a person metabolizes drugs.
– The age game
• infants have immature livers that reduce the rate of metabolism,
and elderly patients experience a decline in liver size, blood
flow, and enzyme production that also slows metabolism.
 

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 D. Excretion
• Excretion, or elimination, is the
process by which a drug is removed
from the body along with its metabolite.
• The most important excretion routes are
through the kidney and liver.
• Other routes include respiration through
the lungs, sweating, or milk in nursing
mothers
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• Most drugs are eliminated in the kidney,
so elimination is highly influenced by renal
function.
• If the kidneys are not eliminating
properly, the parent drug and metabolites
accumulate and can cause prolonged
action or toxicity.
• Carefully assess the renal effect of ALL
drugs and check with the physician before
administering two nephrotoxic drugs
together.
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• The rate at which a drug is eliminated by
the body is known as drug clearance.
This process is influenced greatly by
renal function, which is often measured
by creatinine clearance (which reflects
the glomerular filtration rate).

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 – Carefully assess the renal effect of ALL
drugs and check with the physician before
administering two nephrotoxic drugs
together.
• Intestinal and biliary excretion
– The unabsorbed drug will be excreted
directly from the intestinal tract.

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 Drug Monitoring (Half-
Life=Half the Drug)
• The amount of time required for half of the drug
to leave the system is known as drug half-life.
• It is the time needed for 50% of the drug in the
plasma to be eliminated, or the blood
concentration of a drug to decrease by 50%.
• This information is important for appropriate
timing for a drug dose or determining the
duration of a drug’s effect on the body.

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 – Tolerance - when a patient develops a
decreased response to a drug over time.
The patient then requires larger doses to
produce the same response.
•  
– Dependence - patient displays a physical
or psychological need for the drug

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 Module Requirement
• Please answer Module 1 Activity in Page
11 – 12. To be submitted via Schoology.

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