PHARMACOLOGY REVIEWER
• the process of drugs passing through the
Pharmacokinetics
the study of the way the body deals with drugs-
includes Absorption, Distribution, Metabolism
(Biotransformation), and Excretion of drugs.
= study the events that happen to a drug from
its *administration to the time it is secreted from
the body.
PHARMACOKENETIC CONSIDERATIONS
1. onset of drug action (how long it will take to see
the beginning of the therapeutic effect)
2. drug half-life
3. timing of the peak effect (how long it will take to
see the maximum effect of the drug)
4. duration of drug effects (how long the patient will
experience the drug effects)
5. metabolism or biotransformation of the drug and
the site of excretion
 ABSORPTION
• describes the rate and extent at which a
drug leaves its site of administration
• it is the movement of drug particles to body
fluids
• usually takes place in the small intestine
and to a lesser extent, in the stomach
• They pass in the intestine to the liver,
wherein the liver is the primary site of
metabolism.
• HCPs are concerned with bioavailability. It
is the percentage of the administered drug
that reaches the systemic circulation and
eventually its site of action
• some drugs do not go directly into the
systemic circulation after absorption. They
pass from the intestine to the liver. In the
liver, some drugs are metabolized to an
inactivate form and then excreted. This
reduces the amount of active drug
liver first before distribution to the different
sites of action is called first-pass effect.
• if the active drug is inactivated before it
reaches the systemic circulation and the
metabolic or excretory capacity of the liver
for the drug is great, bioavailability is
substantially decreased.
• the decrease in bioavailability due to hepatic
first-pass metabolism depends on the
anatomical site where absorption takes
place and on the route of administration
• Bioavailability is measured after absorption
and hepatic drug metabolism
• to obtain the desired effect of a drug, oral
doses should be 3 to 5 times larger than the
drug dose for intravenous (IV) use
FACTORS THAT AFFECT ABSORPTION AND
BIOAVAILABILITY
1. form and solubility- drugs in aqueous solution
are more rapidly absorbed than those oily solutions
- the rate at which the drug dissolves may be a
limiting factor if the drug is solid
- local conditions at the site of absorption, like pH,
can alter solubility. This is especially true in the GI
tract, e.g. aspirin is relatively insoluble in acidic
gastric contents.
2. concentration- more concentrated solutions of a
drug are more extensively absorbed
3. route of administration- parenterals (especially
intravenous injections) are more actively absorbed
than orally administered drugs
TOPICAL- directly applied to the body
Ex. Ointments, oil, eye cream
4. blood circulation at the site of absorption-
shock and some diseases decrease the rate of
absorption while local application of heat and
massage increase blood flow and enhance
absorption
5. surface area available for absorption- drugs
are rapidly absorbed at the sites where epithelial
membranes have larger surface areas
PHARMACOLOGY REVIEWER
e.g. pulmonary alveolar epithelium, the intestinal
mucosa, and in cases of extensive application, the
skin. Absorption in the stomach is not as rapid or
extensive
6. presence of food and other drugs
7. changes in liver metabolism caused by
dysfunction and inadequate blood supply
 DISTRIBUTION
• is the process by which a drug is made
available to body tissues
• it refers to the ways by which drugs are
transported by circulating body fluids to the
sites of action (receptors)
• the amount of drug that gets to the receptor
sites determines the extent of
pharmacological activity
PROTEIN BINDING:
• most drugs are bound to some extent to
proteins in the blood to be carried into
circulation. The protein-drug complex is
relatively large and cannot enter into
capillaries and then into tissues to react.
The drug must be freed from the protein’s
binding site at the tissues.
• some drugs are tightly bound and are
released very slowly. These drugs have a
very long duration of action because they
are not free to be broken down. Therefore,
they are released very slowly into the
reactive tissue.
• some drugs are loosely bound; they tend to
act quickly
• some drugs compete with each other for
protein- binding sites, altering effectiveness
or causing toxicity when the two drugs are
given together
BLOOD- BRAIN BARRIER:
• is a protective system of cellular activity that
keeps many things (e.g. foreign invaders,
poisons) away from the CNS
• drugs that are highly lipid soluble are more
likely to pass through the blood-brain barrier
and reach the CNS.
• drugs that are not lipid soluble are not able
to pass the blood-brain barrier, almost all
antibiotics are not lipid soluble
*Lipid solubility- ability of a chemical to partition
between oil and water phases
• this is clinically significant in treating a brain
infection with antibiotics
• effective antibiotic treatment can occur only
when the infection is severe enough to alter
blood-brain barrier and allow antibiotics to
cross
Permeability-measure of the case of the passage.
- Ability of membranes to allow soluble
substances to pass through them.
 Semi Permeable- a membrane that allows
the passage of some molecules but not
others.
 Non-Permeable- not allowed to enter
PLACENTA AND BREAST MILK:
• many drugs readily pass through the
placenta and affect the developing fetus in
pregnant women.
• it is best not to administer any drugs to
pregnant women because of the possible
risk to the fetus. Drugs should be given only
when the benefit clearly outweighs any risk
• many other drugs are secreted into breast
milk and therefore have the potential to
affect the neonate. Because of this
possibility the nurse must always check the
ability of a drug to pass into breast milk
when giving a drug to a breastfeeding
mother.
 METABOLISM
The process by which the body inactivates
drugs.
• Most drugs are inactivated by liver
enzymes, changing them into metabolites
that may or may not be metabolically active.
The active metabolites are readily excreted.
PHARMACOLOGY REVIEWER
• Those metabolic which are still active can (GFR) or decreased renal tubular secretion,
cause an increase in pharmacologic slowing down drug
response.
excretion, causing drug accumulation with
• Liver disease like cirrhosis and hepatitis severe drug reactions
alter drug metabolism in the liver. The slow
Decreased blood flow to the kidneys can also
of drug metabolism may cause drug
affect drug excretion
accumulation and subsequent toxicity.
• the most reliable test to determine normal
• another factor to be considered in the
renal function is creatinine clearance
metabolism of drugs is half life
• creatinine is a metabolic by-product of
• is the time needed for one half of the drug
muscle metabolism that is excreted by the
concentration to be eliminated. If the liver or
kidneys
kidney is dysfunctional, the half-life is
prolonged and causes drug accumulation • creatinine values vary with age and gender.
and toxicity Lower values are expected with elderly and
female patients because of decreased
e.g. a patient takes 650mg of acetylsalicylic
muscle mass
acid (ASA) with a half-life of three hours, it will take
3 hours to metabolize 325mg. • a decrease in renal GFR values results in
an increase in serum creatinine level and a
BORDERLINE OF mmHg- 140/90
decrease in urine creatinine clearance
Captopril- used to treat hypertension
• the creatinine clearance test entails
- an ACE inhibitor collection of urine samples
Losartan- another antihypertensive drugs but an over 12-24 hrs. and extraction of blood sample
ARB(angiotensin receptor blocker)
*Nephron is the basic functional unit of kidney
*If the drugs are film coated, antacid is not
*normal creatinine clearance is 0.74-1.35
advisable.
*increased in creatinine pt may show dyspnea, it
*Suppository drugs are given rectally because it
only means that the patient has a high salt diet that
has lots of capillaries.
increased the creatinine.

 EXCRETION or Elimination
E. Factors influencing responses to drugs
• the major route for drug elimination is
• when administering a drug to a patient, the
through the urine
nurse must be aware that the human factor
• the kidneys filter free or unbound drugs and has influence on what happens to a drug
drugs that are unchanged when it enters the body
• protein bound drugs cannot be filtered • no two people react in exactly the same way
through the kidneys. However, as soon as to any given drug
the drug is released from the protein, it is
1. weight
excreted in the urine
• recommended dose of a drug is based on
• other routes include hepatic metabolism,
drug evaluation studies and is targeted at a
bile, feces, lungs, saliva, sweat and breast
150-pound person
milk
• much heavier people may require larger
• kidney diseases result in decreased
doses to get a therapeutic effect
glomerular filtration rate
PHARMACOLOGY REVIEWER
• people who weigh less may require smaller
doses of a drug
2. age
• is primarily in children and older adults
• children have immature systems for
handling drugs, many drugs come with
recommended pediatric doses
• older adults undergo many physical
changes that are part of the aging process,
their bodies may respond very differently in
all aspcets of pharmacokinetics
• many drugs now come with recommended
doses fr patients who are older
• the doses of other drugs also may need to
be decreased for the older adult
*** if the effects are not what would normally be
ecpected, one should consider the need for a dose
adjustment
3. gender
• physiological differences between men and
women can influence a drug’s effect
e.g. when giving IM injections, it is important to
remember that men have more vascular muscles,
so the effects of the drug will be seen sooner in
men than in women
• women have more fat cells than men do, so
drugs that deposit in fat may be slowly
released and cause effects for a prolonged
period
e.g. gas anesthesia have an affinity for
depositing in fat
and can cause drowsiness and sedation
sometimes weeks
after surgery
• women who are given any drug should
always be questioned
about the possibility of pregnancy
4. metabolic rate
• patients with high metabolic rate tend to
metabolize drugs more rapidly and require
larger doses or more frequent
administration
• chronic smoking enhances the metabolism
of some drugs (e.g. theophylline) requiring
larger doses for a desired effect
5. illnesses and other pathologic conditions
may alter the rate of absorption, distribution,
metabolism and excretion of drugs. For example:
• patients with shock who have reduced
peripheral vascular circulation will absorb
drugs injected intramuscularly and
subcutaneously very slowly
• patients who keep vomiting and may not be
able to retain medication in the stomach
long enough for absorption of drugs
6. psychological (attitudes and expectations)
conditions
• patients with diseases (like insulin-
dependent diabetes) of rapid consequences
may manifest good rate of compliance
• patients with “silent” illnesses are less
compliant with treatment regimens, like in
hypertension
• the use of a placebo (a dosage form with
no pharmacologic activity) is beneficial for
patients being treated for anxiety
Drug legislation controlled substances, generic
drugs, orphan drugs and over-the-counter
drugs
CONTROLLED SUBSTANCES:
Controlled Substances Act of 1970
• established categories for ranking of the
abuse potential of various drugs
PHARMACOLOGY REVIEWER
• the FDA studies the drugs and determines
their abuse potential; the DEA (Drug
Enforcement Agency) enforces their control
• drugs with abuse potential are called
controlled substances
• the DEA closely monitors prescription,
distribution, storage and use of controlled
substances in an attempt to decrease
substance abuse
*** each prescriber has a DEA number, which
allows the DEA to monitor prescription patterns
and possible use
CONTROLLED SUBSTANCES:
Controlled Substances belong to five schedules:
1. schedule I- drugs with high potential for abuse,
have no accepted medical use,
and have no given safety regulationsfor
their use, even under medical supervision
e.g. marijuana
2. schedule II- drugs with high potential for abuse,
but are
currently acceptable for medical use
e.g. meperidine, morphine
3. schedule III- drugs with a high potential for
abuse (but to a lesser extent than I and II) and are
acceptable for medical use. Their abuse potential
leads to moderate physical or psychological
dependence
e.g. Tylenol with codeine
4. schedule IV- drugs with lower potential for abuse
compared with III and have current medical use.
Use of drugs under this schedule leads to limited
physical and psychological dependence.
e.g. Phenobarbital
5. schedule V- drugs with lower abuse potential
than IV, with accepted medical use, and limited
physical and psychological dependence compared
with IV, and may be purchased without a
prescription
e.g. Guaifenesin (Robitussin AC)
GENERIC DRUGS:
• when a drug receives approval for
marketing from the FDA the drug formula is
given a time-limited patent, in much the
same way as an invention is patented
• Generic drugs- chemicals that are produced
by companies, because they do not have
the research, the advertising or sometimes
the quality control they can produce the
drug more cheaply. In the past, some
quality control problems were found with
generic products.
• many states require that a drug has a
generic form, this keeps down the cost of
drugs
• when a drug receives approval for
marketing from the FDA the drug formula is
given a time-limited patent, in much the
same way as an invention is patented
• Generic drugs- chemicals that are produced
by companies, because they do not have
the research, the advertising or sometimes
the quality control they can produce the
drug more cheaply. In the past, some
quality control problems were found with
generic products.
• many states require that a drug has a
generic form, this keeps down the cost of
drugs
ORPHAN DRUGS:
• are drugs that have been discovered but are
not financially viable and not been “adopted”
by any drug company
• may be useful in treating a rare disease, or
they may have potentially dangerous
adverse effects
• are often abandoned after preclinical trials
or phase I studies
Orphan Drug Act of 1983:
PHARMACOLOGY REVIEWER
• provides financial incentives to drug PEDIA=60 microset
companies to adopt and develop these
drugs
• incentives help the companies put the drug Regulation of IV fluid in QMC
through the rest of the testing process, even
Q6H
though the market for the drug in the long
run may be very small (drugs used to treat Q8H
rare diseases)
Q10H
Q12H
OVER-THE-COUNTER-DRUGS:
Q16H
• are products that are available without
prescription for self-treatment of a variety of Q20H
complaints
Q24H
• nurses should consider several problems
related to OTC drug use: Q48H
1. taking these drugs could mask the signs
and symptoms of underlying disease,
How to get cc/hr?
making diagnosis difficult
1000
2. taking these drugs with prescription =mL /hr
Rx Time
medications could result in drug
interactions and interfere with drug therapy
3. not taking these drugs as directed could
result in serious overdoses

FORMULAS
D
S
x Q

d- desire
s- stock
q- quantity

IV Fluid Theraphy
Volume ( 1000∨50 ) x gtts factor
=drops/min
Rx Time x 60
ADULT= 15 macroset