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PHARMACOLOGY

JUDITH B. LUTRANIA , LPT, RN, MAN


PHARMACOLOGY
◦ derived from the Latin words, “pharmakon” (medicines
or drugs) and “logos” (study).
◦ Thus Pharmacology is most simply defined as the study
of medicines or drugs and their actions on living
organisms.
◦ Drug is “any chemical agents that affects the processes
of living.”
History
◦ The Babylonians recorded the earliest surviving ‘prescriptions’ on clay tablets in
3000 B.C.
◦ the Chinese recorded the Pen Tsao (Great Herbal), a 40 volume compendium
of plant remedies dating to 2700 B.C.
◦ The Egyptians followed in 1500 B.C. by archiving their remedies on a
document known as the Eber’s papyrus.
◦ “Pharmacologia sen Manductio and Materiam Medicum”
- by Samuel Dale in 1693
- The first recorded reference to the word pharmacology
SCOPES OF STUDY WITHIN
PHARMACOLOGY
PHARMACOLOGY

PHARMACOTHERAPEUTICS TOXICOLOGY

PHARMACOKINETICS PHARMACODYNAMICS
Pharmacotherapeutics
◦ Is the area of pharmacology that refers to the use of specific drugs to prevent, treat or
diagnose disease.
◦ Purpose: To know the effects of drugs on humans.
Pharmacokinetics
derived from the Greek words “pharmaco” (medicines/drugs) and “kinetics”
(movement).

Thus, pharmacokinetics is the study of drug movements throughout the body or the
study of how it deals with drug in terms of the way the drug is absorbed, distributed and
eliminated.

The core subject in pharmacology


A. Drug Absorption: Bioavailability

◦Bioavailability- the extent to which the drug


reaches the systemic circulation.
◦ Depends on the route of administration as well as the
drug’s ability to cross membrane barriers.
◦ Absorption – process involving the movement of a
substance from its site of administration, across body
membrane to circulating fluids.
The rate of Absorption depends on three (3)
factors:
◦solubility of drugs/digestive motility
◦route of administration
◦degree of blood flow through the tissue
A. Enteral
- drug is absorbed into the systemic circulation
through the mucosa of the stomach or small intestine

Oral – absorbed from the intestinal lumen

Sublingual and Buccal – absorbed into the highly


vascularized tissue under the tongue (oral mucosa)
Routes of Drug Administration
◦ IV
◦ IM, SQ
◦ Oral
◦ Sublingual
◦ Rectal
◦ Topical
◦ Transdermal
B. Parenteral
- is a general term meaning any route of administration
other than the GI tract.
- most commonly refers to injection by any method
although topical and transdermal medications can also be
considered parenteral dosage forms as can sublingual and
buccal medication.
- drugs can be injected intradermally, subcutaneously,
Intra-arterial, IM, intrathecally, Intra-articularly or IV
◦ Subcutaneous, Intradermal and Intramuscular

Subcutaneous – under the dermal layer of skin


Intradermal – under the more superficial skin layers
immediately underneath the epidermal layer of the skin
and into the dermal layer.
Intramuscular – muscle beneath the subcutaneous fatty
tissue
C. Topical
- involves application of medications to various
surfaces.
- applied on skin, eyes, ears, nose, lungs, rectum
and vagina

Transdedermal – drug delivery through adhesive drug


patches. Ex: Nitroglycerine

Inhaled –drugs delivered directly to the lungs. Ex:


Pentamidine
B. Distribution
- refers to the transport of a drug in the body by the
bloodstream to its site of action.

Liver – Major site of drug metabolism


Kidneys – Major site of drug excretion
C. Metabolism
- also referred as biotransformation because it
involves biochemical alteration of a drug into an inactive
metabolite
D. Excretion
- is the elimination of drug from the kidney
Drug Elimination rate
Clearance
◦ ability of the organs and tissues to eliminate the drug
(systemic clearance) or the ability of a single organ
tissue to eliminate the drug.
◦ to calculate the clearance from s specific organ, two
primary factors must be considered

◦ 1. Blood flow to the organ (Q) determines how much drug


will be delivered to the organ for elimination.
2. Fraction of the drug removed from the plasma as it passes
through the organ, called the extraction ratio, is equal to the
difference in concentration of drug entering (Ci) and exiting
(Co) the organ, divided by the entering concentration (Ci)

Ci - Co
◦ CL = Q --------------
Ci
Half Life
- is the time required for one half of a given amount
of drug in the body to be removed and is measured of
the rate at which the drug is eliminated from the body.
- is the amount of time requirement for 50% of the
drug remaining in the body to be eliminated.
Purpose of knowing the half-life
◦ Help determine the dosage and frequency needed
for administration of different drugs.(If a drug has a
long half life, it may need to be administered only
once a day or vise versa)
e.g. Long half-life - digoxin at 36 hrs. to be
eliminated
Short half-life - aspirin at 5 hrs. to be
administered q 4 hrs. or q 6 hrs to maintain therapeutic
effect.
Onset, Peak and Duration
Drug Actions
- are the cellular processes involved in the interaction between a
drug and cell

Drug Effects
- are the physiologic reactions of the body to the drug

Onset of Action
- is the time required for the drug to elicit a therapeutic response
Peak Effect
- is the time required for a drug to reach its maximum
therapeutic response

Duration of Action
- length of time that the drug concentration is sufficient to
elicit therapeutic response

Toxicity
- peak blood level of the drug is too high, drug become
poisonous
Mechanism of Drug Absorption
◦ Passive Diffusion/transport
◦ absorption of substances from the area of high concentration to that of low
concentration/ pressure gradient, “down-hill”
◦ doesn’t need energy to move substances
◦ Active transport/carrier-Mediated transport
◦ Involves using membrane proteins to transport substances across the cell
membrane.
◦ Transport of substance from low concentration to area of concentration, “up-hill”.
◦ Needs energy to fuel the carrier system (ATP hydrolysis)
◦ Facilitated Diffusion
◦ Bears some features of both active transport and passive diffusion.
◦ Endocytosis
◦ Drug is engulfed by the cell via an invagination of the cell
membrane.
◦ Osmosis
◦ Refers to the special case of diffusion where the diffusing
substance of water, moves from an area where it is highly
concentration to an area of low concentration.
Pharmacodynamics
“pharmaco” (drugs/medications) and “dynamics” (change)

It is the analysis of what the drug does to the body, including the
mechanism by which the drug exerts its effect.

Concerned with the mechanisms of drug action and the


relationships between the drug concentration and responses in
the body.
◦ Ceiling Effect / Maximal Efficacy
◦ The point in which there is no further increase in response.
◦ Dose response curves
◦ Used to provide information about the dosage range over
which the drug is effective, as well as the peak response
that can be expected from the drug.
◦ Potency – related to dosage that produces a given response
in a specific amplitude.
◦ the more potent drug requires, a lower dosage to produce
the same effect as a higher dose of the other drug.
◦ Maximal efficacy – magnitude of maximal response that can
be produced from a particular drug.
◦ efficacy is almost always more important than potency.
Types of Drug-Receptors Interactions
1. Agonist – a drug that binds to a receptor and initiates a change in
the function of the cell.
- a drug that produces the same type of response as the
endogenous substance.
- It has both efficacy and affinity.
2. Antagonist- that the drug will bind to the receptor, but will not cause
any change in the function of the receptor or cell.
- are often referred to as BLOCKERS. It compete with agonists
for the receptor binding sites.
- has only affinity.
- e.g. Beta blockers
3. Partial Agonists – drugs that attach, elicit some
response and also block other responses
Toxicology
◦ is the study of the harmful effects of chemicals.

◦ Adverse effects of the medication to the body.


SOURCES OF DRUGS
A. Plants
◦ Plants and plant parts have used as medicines since prehistoric
times. Even though, plants are an important source of chemicals
that are developed into drugs. For example, digitalis products
used to treat cardiac disorders and various opiates used for
sedation are still derived from plants.
B. Animal Products
◦Animal products are use to replace human
chemicals that are produced because of
disease or genetic problems.
◦Ex
1. Insulin - from pancreas of cows and pigs
2. Thyroid drugs and growth hormone - from animals thyroid
and hypothalamus tissues.
C. Inorganic Compounds
◦ Salts of various elements can have therapeutic effects in the
body. Aluminum, fluoride, iron, and even gold are used to treat
various conditions. The effects of these elements usually were
discovered accidentally when cause-effect relationship was
observed.
DRUG CHARACTERISTICS
& FORMULATIONS
Type Route Description
Aerosol Topical Colloidal solution dispensed in the form of a mist.

Capsule Oral Gelatin-covered single dose of a drug; prevents


patients from tasting the drug; gelatin dissolves in
either stomach or intestine.

Elixir Oral Sweetened, aromatic, hydroalcoholic liquid used


in the compounding of oral drugs.

Emulsion Oral or topical Drug mixture containing oil and water or any
other two liquids that are not mutually soluble.
Type Route Description

Extract Oral Concentrated drug preparation made by evaporating the


hydroalcoholic solvent.

Fluidextract Oral Concentrated liquid drug preparation of vegetable drugs.

Gel(jelly) Topical Semisolid drug that liquefies when applied to the skin.

Gel Oral Viscous suspension of a substance in water, needs to be shaken


well before using.

Lotion Topical Liquid preparation (clear, suspension, or emulsion) used for


soothing or medicinal purposes.

Lozenge Oral Flat disk held in the mouth until it dissolves


(troche)
Type Route Description

Ointment Topical Soft, fatty substance applied to the skin or


mucous membrane.

Powder Topical/parenteral Fine ground drugs; usually mixed with


sterile water for parenteral use and used
dry for topical application.

Suppository Topical Semisolid substance for insertion into the


rectum, vagina, or urethra, where it
dissolves, releasing the drug.

Suspension Oral Small particles of a drug mixed with, but


not dissolve in, a fluid.

Syrup Oral Concentrated solution of sugar in water,


often with flavorings; often used to
disguise unpleasant taste of a drug
Type Route Description

Tablet Oral Powdered drug compressed into a small


disk, most common form of oral drug
preparations

Tincture Oral Alcoholic (or alcohol-and-water) extract


of drug derived from vegetable or animal
substances.

Transdermal Topical Patch-like devices that adheres to the


patch skin; contains the drug, thin membrane
between the drug and the skin, and
water-resistant covering.
PREGNANCY
CATEGORIES
Category A
 adequate studies in pregnant woman have not
demonstrated a risk to the fetus in the first trimester of
pregnancy, and there is no evidence of risk in later trimester.
Category B
 animal studies have not demonstrated a risk to the fetus but
there are no adequate studies in pregnant women, or animal
studies have shown an adverse effect, but adequate studies in
pregnant women have not demonstrated a risk to the fetus
during the first trimester of pregnancy, and there is no evidence
of risk in later trimester.
Category C
 animal studies have shown an adverse effect on the fetus but
there is no adequate studies on humans; the benefits from the
use of the drug on pregnant woman may be acceptable
despite its potential risks, or there are no animal reproduction
studies and no adequate studies in humans.
Category D
 there is no evidence of human risk, but the potential benefits
from the use of the drug to a pregnant a woman my be
acceptable despite its potential risks.
Category X
 studies in animals or humans demonstrate fetal abnormalities
or adverse reaction; reports indicate evidence of fetal risk. The
risk of use of pregnant woman clearly outweighs any possible
benefit.
ORPHAN DRUGS
◦ These are drugs that have been discovered but are not
financially viable and therefore have not been “adopted” by
any drug company. Orphan drugs may be useful in treating a
rare disease, or they may have potentially dangerous adverse
effects.
OVER-THE-COUNTER DRUGS
◦ OTC drugs are products that are available without
prescription for self-treatment of variety of complaints.
Considerations to Several Problems in
Taking OTC
◦ Taking these drugs could mask the signs and symptoms of
underlying disease, making diagnosis difficult.
◦ Taking these drugs with prescription medications could result in
drug interactions and interfere with drug therapy.
◦ Not taking these drugs as directed could result in serious
overdose.
SOURCES OF DRUG INFORMATION
•Package Inserts
•Nursing Journals and Indices
1.Cumulative Index to Nursing and allied Health
Literature (CINAHL)
2.American Journal of Nursing (AJN)
3.Nursing, RN
4.Nursing Clinics of North America
5.Nursing Journals (Heart and Lung, Geriatrics
Nursing, Cancer Nursing)

◦ Textbooks and Nursing guides
◦ Mosby’s Drug Hand Book for Nurses
◦ Davi’s Drug Guide for Nurses
◦ References sources
◦ Hospital Formulary
◦ Facts and comparison published by J.B. Lippincott
◦ Physician’s Desk reference (PDR)
◦ United Sates Pharmacopoeia Dispensing Information
(USPDI)
◦ The National Formulary
◦ AMA drug Evaluation
◦ Internet Information
DRUG NOMENCLATURE AND
CLASSIFICATION OF DRUGS
◦ Chemical name
◦ refers to the specific structure/biochemistry of the compound
and nature of the drug.
◦ A drug has only one chemical name.
◦ Using standard nomenclature established by the International
Union of Pure and Applied Physics (IUPAC).
◦Generic/ Official/ Nonpropriety Name
◦ Somewhat shorter and is often derived from the
chemical name, and it is less complicated and
easier to remember.
◦ Are provided by the United States Adopted
Names (USAN) council, an organization sponsored
by the united States Pharmacopoeial Covention,
the American Medical Association, and
Amer5ican Pharmaceutical Association, and FDA,
WHO.
E.g. Lithium carbonate
◦ Calcuim gluconate
◦ Sodium Chloride
◦ Flouroquinones
◦ Cephalosphorins
◦ Phenothiazines
◦ Thiazides
Trade Names/ Brand Name/ Propriety
name/ Product name
◦are assigned to the compound by the
pharmaceutical company and may or may
not bear any reference at all to the
chemical and generic terminology.
Examples of Drug Nomenclature

Chemical Name Generic Trade


(Nonpropriety (Propriety
N-Acetyl-p-aminophenol acetaminophen Tylenol, Panadol
3,4-Dihydroxyphenyl-L-alanine levodopa Larodopa
5,5-Phenylethylbarbituric acid phenobarbital Luminal, Eskabarb
7-chloro-1,3-dihydro-1-methyl- diazepam Valium
5-phenyl-2H-1,4-benzodiazepin-2-one tetracycline Achromycin,panmyc
4-Dimethyamino-1,4a,5,5a,6,11,12a- in
Octahydro-3,6,10,12a-pentahydro-6-
Methyl-1,11,dioxo-2-naphthacenecar-
Boxamide
TOXIC DRUG
EFFECTS OF DRUG
ADVERSE EFFECTS
- Adverse effects are undesired effects that may be unpleasant or even
dangerous. They can occur for many reasons, including:
◦ The drug may have other effects on the body besides the therapeutic
effects.
◦ The patient is sensitive to the drug being given.
◦ The drug’s action on the body causes other responses that are
undesirable or unpleasant.
◦ The patient is taking too much or too little of the drug, leading to adverse
effects.
Adverse drug effects can be of
several types:
A. Primary Actions – it is an adverse effect due to over dosage.

B. Secondary Actions – are drug effect besides from the desired


pharmacological effect.

C. Hypersensitivity – are excessive response to either primary or the


secondary effects of drug
DRUG ALLERGY
◦occurs when the body forms antibodies to a particular drug,
causing an immune response when the person is re-
exposed to the drug.
Four main classification of drug
allergies
i. Anaphylactic reaction
 an allergy that involves an antibody that reacts with specific sites in
the body to cause the release of chemicals including histamine,
that produces immediate reaction that can lead to respiratory
distress and even respiratory arrest.
ii. Cytotoxic reaction
 Allergy that involves antibodies that circulate in the blood and
attack antigens on cell sites, causing death of that cell.
iii. Serum-sickness reaction
 It involves antibodies that circulate in the
blood and cause damage to various tissue
by depositing in blood vessels.
iv. Delayed allergic reaction
 This reaction occurs several hours after
exposure and involves antibodies that are
bound to specific white blood cells.
DRUG-INDUCED TISSUE AND ORGAN
DAMAGE

1. Dermatological Reactions
are adverse reactions involving the skin
These can range from simple rash to potentially fatal
exfoliative dermatitis or irritation to the skin.
Ex.
a. Rashes, Hives
b. stomatitis
Interventions:
◦ provide frequent skin care
◦ instruct the patient to avoid rubbing, tight or
rough clothing, and harsh soaps and perfume
◦ administer antihistamine
◦ In severe cases, discontinue the drug and
notify the care provider
Intervention:
◦provide frequent mouth care with nonirritating
solution.
◦For nutrition, provide a small but frequent
meals.
2. Superinfections
- due to destruction of the normal flora of
the body.
 assessment:
fever
 diarrhea
black or hairy tongue
inflamed and swollen tongue
mucous membrane lesion
vaginal discharge with or without itching
Interventions:
frequent mouth care
skin care
access to bathroom facilities
small and frequent diet
In severe cases, discontinue the drug
3. Blood dyscrasia
– is a bone marrow suppression caused by
a drug effects.
◦This occurs when drugs that can cause cell
death (e.g. antineoplastics, antibiotics) are
used
assessment:
fever
chills
sore throats
weakness
back pain
dark urine
decrease hematocrit
low platelet count
low white blood cells
Interventions:
◦monitor blood count
◦protection from exposure to infection
◦protection from injury
◦avoidance of activities that might result in injury
and bleeding
4. Toxicity
◦ Liver injury
 assessment:
fever
malaise
nausea
vomiting
jaundice
change in color of urine or stools
abdominal pain or colic
elevated liver enzymes
alteration in bilirubin levels
changes in clotting factors
Interventions:
discontinue the drug and notify the prescriber
Offer supportive measures
5. Renal injury
 assessment:
elevated blood urea nitrogen
elevated creatinine concentration
decrease hematocrit
electrolyt imbalances
fatigue
malaise
edema
irritability
◦Interventions:
◦ discontinue drug, notify the prescriber
◦ in severe cases, dialysis maybe required
6. Poisoning
occurs when an overdose of a drug
damages multiple body systems, leading to
potential for fatal reactions.
Alteration in glucose metabolism
◦Hypoglycemia
 assessment:
Fatigue
drowsiness
Hunger
anxiety
headache
cold and clammy skin
shaking and lack of coordination.
Increase heart rate, blood pressure,
numbness and tingling of the mouth, tongue
and lips,
confusion, rapid and shallow respiration.
In severe cases seizure and or coma may
occur. *
◦ Interventions:
◦restore glucose intravenously
◦institute safety measure to prevent injury or falls
◦Hyperglycemia:
 assessment:
fatigue
increase urination
increase thirst
deep respiration
restlessness
increase hunger
nausea
fruity odor to breath
◦ Interventions:
◦ administer insulin therapy
◦ Provide support to help the patient deal with signs and
symptoms

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