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Basic Pharmacology

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BASIC

PHARMACOLOGY
Prepared By: Cristina Benito
LEARNING OUTCOMES:

1. Define the word Pharmacology.

2. Outline the steps involved in developing ad approving a new drug in the

United States.

3. Differentiate between generic and brand-name drugs and over -the-counter

and prescription drugs.

4. Describe how body cells respond to the presence of drugs that are capable

of altering their function.


Learning Outcomes:
5. Outline the process of dynamic equilibrium that determines the actual
concentratiion of a drug in the body.
6. Explain the meaning of half-life oa a drug and calculate the half-life of
given drugs.
7. Define the term adverse drug reaction and explain the clinical
significance of this reaction
8. List the responsibilities of the nurse in drug therapy.
9. Describe the key points that must be incorporated into the
assessment of a patient receiving drug therapy.
10. Describe the role of the nurse and the patient in preventing
medication errors.
Introduction to Pharmacology
PHARMACOLOGY: The study of the biological effects of chemicals.
> branch of medicine concerned with the uses, effects, and modes of
action of drugs.
DRUGS: Chemicals that are introduced into the body to cause some
sort of change.
CLINICAL PHARMACOLOGY: The study of drugs in humans.
PHARMACOTHERAPEUTICS: Branch of pharmacology that uses drugs
to treat, prevent, and diagnose disease
NURSING RESPONSIBILITIES ON DRUG THERAPY:
Administering drugs
Assessing drug effects
Intervening to make the drug regimen more tolerable
Providing patient teaching about drugs and the drug regimen
Monitoring the overall patient care plan to prevent medication errors
SOURCES OF DRUGS
Natural Sources:
1. Plants: Almost all parts of the plants are used.
Synthetic version of the active chemical found in a plant
a. Leaves:
>Digitalis Purpurea Digitoxin and Digoxin
>Eucalyptus Cough Syrup
> Atropa Belladonna Atropine
FOXGLOVE (Digitalis Purpurea)
EUCALYPTUS
ATROPA BELLADONA
b. Flowers:
> Poppy Papaver Somniferum Morphine
c. Fruits:
> Senna Pod Senokot
d. Seeds:
> Castor Oil Seeds Castor Oil
e. Roots:
> Rauwolfia Serpentina Reserpine
f. Bark:
> Cinchona Bark Quinidine
2. Animal Sources
>Used to replace human chemicals that are not produced because of
disease or genetic problems.
>Various organs and tissue of animals are used as source of drug.
Insulin PANCREAS
Cod Liver Oil Cod Liver
hCG (human chorionic Urine of pregnant mother
gonadotropin)
NATURAL SOURCES
3. Mineral and Earth Sources:
Metallic and non metallic sources
Natural Sources
Natural Sources
Sources of Drugs
4. Synthetic Sources: Some drugs which are earlier obtained from
plants, animals, or the environment are now synthesized in the
laboratory.
>Genetic engineering alter bacteria to produce chemicals that are
therapeutic and effective

Advantages:
Quality can be controlled
Process is easier and cheaper
More potent and safer
Large scale production
SYNTHETIC DRUGS
AMOXICILLIN
MARIJUANA (cannabis)
Active ingredient delta-9-tetra hydrocannabinol
Drug Names

BRAND NAME/TRADE NAME: a medicine that is discovered,


developed and marketed by a pharmaceutical company.
GENERIC NAME: the nonproprietary name assigned by the United
States Adopted Names (USAN) Council.
CHEMICAL NAME: names that reflect the chemical structure of a drug.
Drug Nomenclature
OVER-THE-COUNTER DRUGS: products that are available without
prescription for self treatment of variety of complaints

Prescription Drugs:
MUST: Be prescribed by a doctor
Bought at a pharmacy
Prescribed for and intended to be used by one person
Drug Evaluation:
U.S. Food and Drug Administration (FDA): an agency of the U.S.
Department of Health and Human services that regulates the
development and sale of drugs.

STAGES OF DEVELOPMENT:
a.) Preclinical Trials:
Subject: Animals
FDA: reviews extensive animal studies and data on the safety and
effectiveness of the proposed drugs.
Chemicals that may have therapeutic value are tested on laboratory
animals for two main purposes:
1. determine whether they have the presumed effects in living tissue
2. evaluate any adverse effects

*Limited data on the safety, toxicity, pharmacokinetics, and metabolism


of the new chemical.
FDA approves an application for an Investigational New Drug (IND)
Preclinical Trials
At the end of the preclinical trials, some chemicals are discarded for the
following reasons:
a. the chemical lacks the therapeutic activity when used with living
animals.
b. the chemical is too toxic to living animals to be worth the risk of
developing into a drug.
c. the chemical is highly teratogenic
d. the safety margins are so small that the chemical would not be useful
in the clinical setting.
Stages of Development
b.) Phase I Studies:
Uses human volunteers to test the drugs (20-80)
These studies are more tightly controlled than preclinical trials
Performed by specially trained clinical investigators
Some chemicals are therapeutic in animals but have no effects in
humans
Investigators scrutinize the drugs being tested for effects in humans
> Toxicity and adverse effects
Phase I Studies
At the end of phase I studies, many chemicals are dropped from the
process for the following reasons:

They lack therapeutic effect in humans


They cause unacceptable adverse effects
They are highly teratogenic
They are too toxic
Stages of Development
c.) Phase II Studies:
Allows clinical investigators to try out the drug in patients who have the
disease that the drug is designed to treat.
Subjects are informed about the possible benefit and risk of the drug.
>they are monitored very closely and evaluate the drugs effects
Performed at various sites across the country
Monitored by the representatives of the pharmaceutical company
studying the drug
Phase II Studies
At the end of phase II studies, a drug may be removed from further
investigation for the following reasons:
It is less effective than anticipated
Its is too toxic when used with patients
It produces unacceptable adverse effects
It has a low benefit-to- risk ratio
It is no more effective than other drugs already on the market, making
the cost of continued research and production less attractive to the drug
company
Stages of Development
d.) Phase III Studies:
Large number of patient in medical research centers will be receiving
the drug
Prescribers observe patients closely, monitoring them for any adverse
effects.
Prescribers evaluate the reported effects to determine whether they are
caused by the disease or by the drug
> Data is collected by the drug company and the FDA
A New Drug Application (NDA): submitted to FDA when sufficient data
has been collected to justify a request approval of the drug. (marketed)
FDA evaluates and approves the drug
An approved drug is given:
1. brand name
2. generic name
3. chemical name
Stages of Development
e.) Phase IV Studies: the phase of continual evaluation
Drug is approved for marketing
The new drug is released for general use, permitting observation
of its effects in a large population. (harmful)
The prescribers are obligated to report to the FDA any untoward or
unexpected adverse effects associated with the drugs they are using
The FDA continually evaluates this information
PHASES OF DRUG DEVELOPMENT:
Legal Regulation Of Drugs:
Safety During Pregnancy
Controlled Substances
EXAMPLE OF DRUG MONOGRAPH
DRUGS AND THE BODY
PHARMACOKINETICS: the study of drug movement throughout the
body.
 How the human body act on the drugs
The four basic pharmacokinetic processes:
1. Absorption
2. Distribution
3. Metabolism
4. Excretion
I. Absorption:

1. The transfer of a drug from its site of administration, across


the membranes, into the blood stream.
*Drugs must be absorb/cross membranes to enter the blood
from their site of administration.
*Once in the blood, drugs must cross membranes to leave the
vascular system and reach their sites of action.
*In addition, drugs must cross membranes to undergo
metabolism and excretion.
STRUCTURE OF A CELL MEMBRANE
Three Ways to Cross the Membrane:
A.Passing through channels or pores: Channels and pores are very
small, generally only small ions, such as sodium and potassium, are
able to pass through.
B.Utilizing a transport system: One Common transporter is P-
glycoprotein (PGP) or multidrug transporter protein, which is a
transmembrane protein that transports a wide variety of drugs out of
cells. This transporter is present in cells at many sites, including the liver,
kidney, placenta, intestine, and capillaries of the brain. In the kidney, it
pumps drugs into the urine for excretion. In the placenta, it transports
drugs back into the maternal blood, thereby reducing fetal drug
exposure.
C.Directly Penetrating the membrane: This is the most common
mechanism. In order to directly penetrate a membrane, the drug must
be lipid soluble (lipophilic/hydrophobic) because the membrane is
composed of phospholipids.
FACTORS AFFECTING RATE OF DRUG
ABSORPTION
Bioavailabilty: how much of the drug is absorbed into the bloodstream
1. Rate of Dissolution:
Before a drug can be absorbed, it must first dissolve. Thus,
the rate of dissolution helps determine the rate of absorption.
Drugs in formulations that allow rapid dissolution have a faster
onset than drugs formulated for slow dissolution.
2. Route of Administration:
Example: IV, Sublingual, Inhalation
Oral, IM, SC route
3. Surface Area: The larger the surface area, the faster the absorption.
4. Blood Flow: Drugs are absorbed most rapidly from sites where blood
flow is high.
FACTORS AFFECTING RATE OF DRUG
ABSORPTION
5. Lipid-Solubility: A drug needs to be lipid soluble (fat) to
penetrate membrane.
6. Interactions with food and other medications:
Example:
1. Antacids delay absorption of beta-adrenergic blockers
(metropolol)
2. Food decreases the absorption of ACE inhibitors (captopril)
3. Tetracyclines with food or drugs containing calcium, iron, or
magnesium can significantly delay absorption.
Comparison of Drug Administration Routes and their
Effects on Absorption

ENTERAL
a. Absorption is rapid in small intestine
b. Presence of food often diminishes absorption
c. Absence of food may increase absorption
d. Liquids absorb more rapidly than solid
e. Absorption occurs within 3 to 5 minutes with sublingual or
buccal administration
f. Absorption from the GI tract may be undependable
Comparison of Drug Administration Routes and their
Effects on Absorption

PARENTERAL
a. IM injection has effects within 10 to 15 minutes
b. IV route requires no absorption and has immediate effects
c. Poor circulation may hinder IM or SC absorption
d. Shock, edema, trauma, and coolness of tissue slow
absorption
Comparison of Drug Administration Routes and their
Effects on Absorption

TOPICAL

a. Local application of drugs may have a systemic effect


Example: Lidocaine (Xylocaine) + Epinephrine (Adrenalin)
b. Some medications may be applied locally for a systemic
effect
Example: Nitro-patch (nitroglycerin)
c. Perfusion or blood flow
d. Integrity of the skin
Comparison of Drug Administration Routes and their
Effects on Absorption

INHALATION:

a. May be absorbed systematically


Example: Anesthetic agents
b. May be absorbed locally
Example: Corticosteriods (budesonide.)
c. Absorption is enhanced because of the large surface area
of the lungs.
d. Expect results within 2-3 minutes
Comparison of Drug Administration Routes and their
Effects on Absorption

MUCOUS MEMBRANE:

a. May produce either local or systemic effect


b. Rectal route may result in incomplete absorption if feces is
present in the sigmoid colon or there are numerous internal
hemorrhoids
c. Absorption is rapid through the rectal route because of the large
vascular surface
Example: acetylsalycylic acid (Aspirin)- expect results in 10-15
minutes
d. Absorption by vaginal route usually enhanced because of the
dense vascularity
II. Distribution: Process that allows drug delivery to tissues and fluid of
the body

a. Sites of action (receptor sites): Where the drug attaches and exerts
its effect
Example: Narcotic drug (Codein)- endorphin receptor site of the neurons
of our brain (receptor site)
Antihistamine (alegra): bind to histamine receptor site.
a. b. Inactive sites (acceptor sites): Where the drugs accumulates but
with no effect on that part of the body.
Example: Tetracycline: tends to accumulate in bone and teeth.
Factors affecting drug distribution:
a. Blood Flow
Drug is distributed rapidly to organs with a large blood supply.
It is distributed more gradually to other internal organs, skin, fat and
muscle.
Example: A diabetic client with lower leg infection and patient with
peripheral arterial disease (Raynaud Syndrome)
b. Drug Solubility
> a lipid soluble drug can cross the cell membrane more quickly than
water soluble drugs can.
FACTORS AFFECTING DRUG DISTRIBUTION
c. Protein-Binding Capability: refers to the degree to which medications
attach to proteins within the blood. (plasma protein albumin)
 Some drugs are tightly bound and are released very slowly thus they
have a very long duration of action because they are not free to be
broken down or excreted
 Drugs that are loosely bound tend to act quickly and be excreted
quickly.
FACTORS AFFECTING DRUG DISTRIBUTION
d. Blood-Brain Barrier: A protective system of cellular activity that keeps
many things 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.
III. Metabolism/Biotransformation:
• It alters a drug to a more active or less active form
• Helps convert the drug to a more water soluble form, facilitating
excretion
• Primary Site for drug metabolism: Liver
• other site: plasma, kidneys, and membranes of the intestines
• First pass effect: Inactivation of drug by enzymes in the liver before
the drug reaches the systemic circulation for distribution.
• large number of oral drugs are rendered inactive by hepatic metabolic
reactions.
FACTORS AFFECTING DRUG METABOLISM
 Age:
Infants: not fully developed liver
Elderly: a decline in liver size, blood flow, and enzyme production that
can also slow metabolism.
 Disease, such as cirrhosis and heart failure:
1. reduction in the dosage of the drugs.
2. frequent monitoring for adverse drug effects.
If the liver is not functioning effectively, the drug will not be
metabolized as it should be, and toxic levels could develop rather
quickly.
 Genetics
IV. Excretion: Elimination of drugs from the body
Routes Of Excretion:
Kidneys via urine: Check kidney function test (BUN and Serum
Creatinine Level)
Toxicity (blood level of the drug will increase)
Liver via bile and into feces
Lungs via exhaled air
Saliva, sweat, and tears
Processes by which a drug is handled by the Body
ONSET, PEAK, AND DURATION
 Onset of Action: refers to the time period from a
drug’s administration to the beginning of its
therapeutic effect.
 Peak Level: occurs when the body absorbs more
drug, the level rises in the blood, and more drug
reaches the site of action.
 Duration of Action: the length of time a drug
produces therapeutic effects.
Minimum effective concentration: Plasma drug level below which
therapeutic effects will not occur.
Drug must be present in concentrations at or above MEC for it be
beneficial.

Toxic concentration: Toxicity occurs when plasma drug levels climb


too high.
Doses must be small enough so that toxic concentration is not reached.

Therapeutic Range: Range falling between the MEC and toxic


concentration.
To maintain plasma drug levels within the therapeutic range.
ONSET OF ACTION/ DURATION OF ACTION/ PEAK
ACTION
HALF- LIFE
 The time needed for the total amount of a
drug in the body to decrease by 50%
 Half-life is affected by absorption, distribution,
metabolism, and excretion
HALF-LIFE

 It determines the dosing interval (frequency)

a. Drugs with short half-life: Short interval


• Drugs that have short half-life must be administered more frequently
than drugs that have a long half-life.
• A drug that’s administered at regular intervals, however, reaches a
steady concentration (or steady state) after about four or five half-
lives. Steady state occurs when the rate of drug administration equals
the rate of drug excretion.
HALF-LIFE
b. Drugs with long half-life: Long interval
A drug that’s given only once is eliminated from the body almost
completely after four or five half-lives

Example: Morphine 50 mg. with half life (t1/2) of 3 hours


Morphine will decrease by 50% every 3 hours
HALF LIFE
HALF-LIFE
DRUG ½ LIFE
1. Penicillin 1 hour
2. Acetaminophen 3 hours
3. Morphine 4 hours
4. Tetracycline 8 hours
5. Digoxin 4 days
CALCULATING HALF-LIFE
PHARMACODYNAMICS
Pharmacodynamics: The study of the mechanisms by which a drug
produce biochemical and physiologic changes in the body.
A drug can modify cell function or the rate of function, but a drug can’t
impart a new function to a cell or target tissue. Therefore, the drug effect
depends on what the cell is capable of accomplishing.
How a DRUG acts:
1. Changes cell environment physically or chemically
2. Acts as an agonist, binding with and stimulating receptors, which
creates a response
3. Acts as an antagonist, binding with but not stimulating receptors,
which prevents a response
Receptor Sites
Receptor sites react to certain chemicals to cause
an effect within the cell.
Agonists
Noncompetitive antagonists
Competitive antagonists
Drug- enzyme interactions
Selective toxicity
Stimulating response
• Agonist is an example of a drug that interacts with receptors.
• An agonist drug has an attraction, or affinity, for a receptor and
stimulates it.
• The drug then binds with the receptor to produce its effect.
• Intrinsic activity: The drug’s ability to initiate a response after binding
with the receptor
Preventing response
1. Antagonist: a drug has an affinity for a receptor but displays little or
no intrinsic activity.
The antagonist prevents a response from occurring.
Antagonists can be competitive or noncompetitive:
A. A competitive antagonist competes with the agonist for receptor sites.
Because this type of drug binds reversibly to the receptor site,
administering large doses of an agonist can overcome the antagonist’s
effects.
B. A noncompetitive antagonist binds to receptor sites and blocks the
effects of the agonist. Administering large doses of the agonist can’t
reverse its action.
Potent quotient
Drug potency: the relative amount of a drug required to produce a
desired response.
Drug potency is also used to compare two drugs.
If drug X produces the same response as drug Y but at a lower
dose, then drug X is more potent than drug Y.
Example:
Pain relief medication like morphine and meperidine.
The required dose of meperidine is larger than the required dose of
morphine. Because morphine produces pain relief at lower doses than
meperidine, we would say that morphine is more potent than meperidine.

A potent drug is one that produces its effects at low doses.


Maximal Efficacy
Efficacy is defined as the largest effect that a drug can produce.
EFFECTS OF DRUGS
1. Local: usually affecting one part; the effect occurs at the site of
application
Example: Acyclovir (Zovirax) cream for herpes simplex viral infection
eye drops or topical skin creams or ointments
2. Systemic: may affect more than one body part; effect may not occur
at the site of administration.
Example: promethazine hydrochloride (Phenergan) given IM for nausea
DRUG EFFECTS AND INTERACTIONS
1. Primary effect: that which is intended
2. Secondary: any other effects other than those intended
a. Drug allergy:
• Unique tissue response, example: dermatitis
• Anaphylactic shock: systemic reaction within minutes that requires
immediate attention
• Serum sickness: reaction 1 week after administration of a drug
b. Idiosyncrasy: an individual sensitivity to the effects of a drug caused
by inherited or other bodily constitution factor.
c. Side effect: an undesirable or unintended effect of the drug
DRUG EFFECTS AND INTERACTIONS
d. Iatrogenic effect: unintentional adverse effects that are physician-or
health care-induced or treatment induced, including renal damage,
hepatic toxicity, and blood dyscrasias like anemia.
e. Photosensitivity: an abnormal reaction to light, particulary sunlight.
f. extraphyramidal effect: Exhibiting movement disorders similar to
Parkinsons disease
g. Toxicity: blood level above the therapeutic level
h. Teratogenicity: causing harm to the fetus
THANKS

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