Pharmacology Prelim Transes

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Nursing Pharmacology

AREAS OF PHARMACOLOGY

PRELIMS 1. Pharmacodynamics
● Refers to biologic and therapeutic
WEEK 1 AND 2 effects of drugs at the site of action
or on the target organs.
Pharmacology ● Deals with the physiological effects
● Derived from the Greek word of the drug on the body.
pharmakon, meaning “drugs” and
logos, means “study”. 2. Pharmacokinetics
● Is a branch of science that deals ● Deals with the movements of drugs
with the study of drugs and their in the body from absorption to
actions on living systems - that is, elimination.
the study of how drugs work in the ● Study of the absorption, distribution,
body (sometimes referred to as biotransformation (metabolism), and
‘drug actions’). (DOH) excretion of drugs.
● To understand this, we need to ● 4 Phases - ADME
consider: 1. Absorption
2. Distribution
A. What a drug is 3. Metabolism
B. How it affects our physical, 4. Excretion
emotional and psychological
wellbeing 3. Pharmacotherapeutics
C. The type of drug being used ● Is the clinical purpose or indication
D. The modes of administration for giving a drug.
E. How the drug is absorbed ● Deals with therapeutic uses of
F. The characteristics of the drugs.
person taking the drug. ● Study of how drugs may best be
used in the treatment of illnesses.
Why is Pharmacology important in ● Study of which drug would be most
nursing? appropriate to use for a specific
disease; what dose would be
● Nurses play an integral role in required; etc.
administering medication to
patients, and depending on the 4. Posology
environment in which they work, ● Deals with the drug dosages
could be doing so as often as every required to produce therapeutic
few minutes. As a result, it’s effects.
imperative that nurses have a solid ● Concerned with “treatment dosage”
understanding of pharmacology, and and “dosage regimen”
potentially fatal drug interactions. ● DOSE - quantitative amount
administered/taken by a patient for
intended medical effect.
Example: ● Studying compositions of natural
● Most drugs in children are dosed substances helps to gain knowledge
according to body weight (mg/kg) for developing synthetic versions.
● Care must be taken to properly
convert body weight from pounds to ❖ Synthetic drugs - are
kilogram (1kg = 2.2 lbs) compounds that are obtained
● Before calculating doses based on from chemical synthesis and
body weight whose source is the
● Order: Amoxicillin laboratory. Synthetic drugs
suspension 400mg/kg/day/5ml are aspirin, diazepam,
40mg/kg/day BID indomethacin, propranolol,
Pediatric patient’s weight = 22lbs etc.

7. Toxicology
CONVERT WEIGHT
● Study of poisons and poisonings.
Pounds to Kilogram ● Deals with the toxic effects of
(22 x 1/ 2.2lb = 10kg) substances on the living organism.

❖ REMEMBER: All drugs have


CALCULATE THE DOSE IN mg the potential to become toxic.

(10kg x 40mg/day = 400mg/day) 8. Pharmacogenetics


● Deals with the different drug
responses based on genetic factors
DIVIDE THE DOSE BY FREQUENCY
or hereditary influences.
(400mg/day/2 = 200mg/dose)
CLASSIFICATION OF THERAPEUTIC
AGENTS
CONVERT THE mg
Drugs
(200 mg/dose/400mg/5ml = 2.5ml BID) ● Derived from the Greek word
“pharma/con” meaning drug.
● Any chemical substances that affect
5. Clinical Pharmacology
the bodily functions of living
● Deals with the uses and effects of
organisms.
drugs in human beings.
● Any chemical substance that affects
or later the physiologic processes or
6. Pharmacognosy
a living organism
● Deals with the drugs derived from
● No suitable dosage form and dose
natural sources.
(Opium, cocaine)
● The study of drugs derived from
● Generally, not used directly for
herbal and other natural (plant and
treatment.
animal) drug sources.
Medicines Physiological Therapy
● Derived from the Latin word ● “Psychotherapy”, “talk therapy”
“medicus” meaning healing or ● Methods to identify and eliminate
physician. problems and stressors (ex. Anger
● Therapeutic drugs; used to prevent management)
or treat diseases
● Generally harmless when there is no Physiotherapy
excess or abuse ● Management using natural physical
● With definite dose and dosages form forces such as water, light, heat, and
(Paracetamol 500mg tablet) sound; this also includes
● Used directly for treatment mechanical, (massage & exercise),
electrical and magnetic energies.
Biologics ● A treatment to restore, maintain, and
● Wide range of medical products make the most of a client’s mobility,
isolated from natural sources. function, and well-being.
● May be produced by biotechnology
methods, like cell cultures and DRUG USES
manipulation of genetic material, and
not by chemical synthesis. Symptomatic treatment
● Treating the symptoms without
❖ Example: telling the basic cause of the
➢ Vaccines disease.
➢ Blood product
➢ Gene therapy ❖ Example:
➢ Recombinant ➢ Pain
therapeutic proteins ➢ Fever

Alternative Medicine/Therapy Prevention


● Any healing practice that does not ● To prevent symptomatic onset of a
fall under conventional medicines condition in a person who has
developed risk factors for a disease
❖ Example: that has not yet become clinically
➢ Acupuncture apparent.
➢ Hypnosis ● To prevent recurrence of a
➢ Herbalism disease/condition from which the
patient has recovered.
THERAPEUTIC METHODS
Diagnostic drugs
Drug Therapy ● Use to confirm or rule out conditions
● Treatment with the use of drugs or diseases.
(pharmacotherapy)
❖ Example
Diet Therapy ➢ eye drops that dilate
● Treatment by modification of diet the pupil to let the
ophthalmologist Brand Name or Trademark Name
examine the internal (Proprietary name)
structures of the eye. ● Name placed by the manufacturing
Curative company, followed by the symbol ®
● To cure a disease or promote ● The superscript ® is registered by
recovery from an illness, injury, or the US patent office and approved
impairment by the FDA (Food and Drug
Administration
❖ Example ● The drug has a registered
➢ Chemotherapeutic drugs to trademark; use of the name is
treat/cure cancer restricted by the drug’s owner
Health maintenance (usually the manufacturer)
● Medications prescribed to treat ● Allows the drug to be commercially
chronic illness/long-term conditions distributed
are taken regularly.
DRUG CLASSIFICATION
❖ Example
➢ Drugs used to treat According to:
high blood pressure,
asthma, diabetes, etc. Therapeutic Use or Clinical Indication
● Antibacterial, antihypertensive,
Contraception antipsychotic, antidepressants
● The birth control pill is a
contraceptive pill Physiologic or Chemical Action
● Safe, simple, and convenient way to ● Beta-receptor blockers,
prevent pregnancy calcium-channel blockers, selective
serotonin reuptake inhibitors,
DRUGS NAMES monoamine oxidase inhibitors.

Chemical Name Requirement of Prescription


● The drug’s chemical composition ● Prescription Drugs
and molecular structure. ● Non-prescription Drugs or
Over-the-counter Drugs
Generic Name or Non-proprietary Name
● Universal drug name/common name Prescription Drugs
entitled by the government. ● Are often strong medications
● Allows the drug to be marketed. requiring medical
● Prescribed by a doctor
● Prescribed for and intended to be
used by one person
● Regulated by FDA through the New
Drug Application (NDA) process.
Non-prescription Drugs or 5. Masking of symptoms may occur
Over-the-counter Drugs (OTC) making diagnosis more difficult
● Medicine that you can buy without 6. There is potential overdose
the prescription 7. Know the intention of Rx and OTC
● Safe and effective when you follow medicines to be taken
the directions on the label and as 8. Give children and appropriate
directed by your health care dosage for their weight and age
professional. 9. If pregnant, always ask your doctor
● Bought off-the-shelf in stores first before taking any drugs or
● Regulated by FDA through OTC supplement.
Drug monographs. OTC drug
monographs are a kind of “recipe
WEEK 3
book” covering acceptable
ingredients, doses, formulations, and
labeling. DRUGS STANDARDS AND LEGISLATION

CRITERIA FOR PRESCRIPTION STATUS United states Pharmacopeia National


OF DRUGS Formulary (USP-NF)
● Is the official publication for drugs
1. Drugs that treat conditions that marketed in the United States,
cannot be easily diagnosed by the designated by the Federal Food,
consumers Drug, and Cosmetic Act.
2. Drugs where effectiveness cannot ● Drugs included in the USP-NF have
be easily monitored by the met the high standards for
consumers. therapeutic use, patient safety,
3. Drugs with unfavorable adverse quality, purity, strength, packaging
event profiles safety, and dosage forms.
4. Drugs with vast drug-interaction
profiles International Pharmacopeia
5. Drugs with high potential for abuse ● Published in 1951 by WHO
6. Drugs that are not easy and practical ● Provides a basis for standards in
to use strength and composition of drugs
for use throughout the world.
PRECAUTIONS WITH THE USE OF OTC
DRUGS FEDERAL LEGISLATION

1. Read and understand the drug ● Through federal legislation, the


labels public is protected from drugs that
2. Know possible side effects and are impure, toxic, ineffective, or not
adverse reactions tested before public sale.
3. Determine possible interactions with ❖ PRIMARY PURPOSE of
other drugs and supplements legislation is to ensure safety.
4. There will be delay in professional ● Federal Pure Food and Drug Act
diagnosis and appropriate treatment of 1906 - America’s first law to
regulate drugs which did not include experimental drugs, and required
drug effectiveness and safety. that adverse reactions and
● Food, Drug and Cosmetic Act of contraindications must be labeled in
1938 - empowered the FDA to the literature.
ensure drug safety by monitoring ● The amendment also included:
and regulating the manufacturer and ❖ Provisions for the evaluation
marketing of drugs. of testing methods used by
● It is the FDA’s responsibility to manufacturers,
ensure that all drugs are: ❖ The process for withdrawal of
❖ Tested for harmful effects approved drugs when safety
❖ Have labels with accurate and effectiveness were in
information doubt,
❖ Enclose detailed literature in ❖ And establishment of new
the drug packaging that drugs before marketing.
explains adverse effects. ● 1978: Drug Regulation Reform Act
● 1952: Durham-Humphrey - shortened the time in which new
Amendment to the 1938 Act - drugs could be developed and
distinguished between drugs that marketed. Protects patient’s rights
can be sold with or without and facilitates the investigational
prescription and those that should process and promotes research.
be refilled without a new ● 1997: Food and Drug
prescription, such as: Administration Modernization Act
❖ Narcotics - has 5 provisions:
❖ Hypnotics ❖ Review and use of new
❖ Tranquilizers drugs is accelerated.
● 1962: Kefauver-Harris ❖ Drugs can be tested in
Amendment to the 1938 Act - children before marketing.
widely publicized thalidomide ❖ Clinical trials are necessary
tragedy 1950 in which European for experimental drug use for
patients who took the serious/life-threatening
sedative-hypnotic thalidomide during health conditions.
the first trimester of pregnancy gave ❖ Drug companies are required
birth to infants with extreme limb to give information on “off
deformities. label” drugs.
❖ Drug companies that plan to
discontinue drugs must
inform health professionals
and patients at least 6
months before stopping drug
production.
● 2002: Best Pharmaceuticals for
Children Act - gives manufacturers
● The amendment tightened controls extension of patents to evaluate
on drug safety, especially
drugs on the market for their safety CONTROLLED SUBSTANCE
and efficacy in children.
● 2003: Pediatric Research Equity ● Drugs with restricted availability;
Act - authorizes the FDA to require considered illegal unless dispensed
that drug manufacturers test drugs under a physician’s
and biologic products for their safety prescription-regulated because of
and effectiveness in children, noting potential for abuse, addiction,
that “children are not small adults”. physical and mental harm.
● The five classes of drugs are:
GENERIC DRUGS ❖ Narcotics
❖ Depressants
● ALL FDA-APPROVED GENERIC ❖ Stimulants
DRUGS MUST BE EQUIVALENT ❖ Hallucinogens
TO THE BRAND-NAME DRUG ❖ Anabolic steroids
● Generic drugs modeled after a
single, brand name drug must Effects of Controlled Substances
perform approximately the same in
the body as the brand name drug.
ABUSE
● There will always be a slight, but not
medically important level of natural ● Improper or harmful use when
variability just as there is for one drugs are used for non-therapeutic
batch of brand name drug compared but for recreation.
to the next batch of brand name
DEPENDENCE
product.
● Bioequivalent - comparison of 2 ● The necessity to continue the drug
pharmaceutical products to function properly.
administered at the same dose ● 2 types of dependence.
having the same effectiveness and ● Psychological - compulsive pursuit
for the drug for its pleasurable or
safety.
advantageous effect.
● REPUBLIC ACT NO. 6675 Generic ● Physical - drug intake is necessary
Acts of 1988 to prevent physical negative
❖ AN ACT TO PROMOTE, withdrawal symptoms.
REQUIRE AND ENSURE
THE PRODUCT OF AN ● 1970: Controlled Substances Act -
ADEQUATE SUPPLY, designed to remedy the escalating
DISTRIBUTION, USE AND problem of drug abuse.
ACCEPTANCE OF DRUGS
AND MEDICINES 1. Promotion of drug education
IDENTIFIED BY THEIR and research into the
GENERIC NAMES. prevention and treatment of
drug dependence.
2. Strengthening of
enforcement authority.
3. Establishment of treatment nurses or nurse midwives, currently
and rehabilitation facilities. have the authority to prescribe or
4. Designation of schedules, or dispense a range of drugs under
categories, for controlled their state laws.
substances according to ● However, the majority of states
abuse liability. enforce “physician-only” laws that
make abortion a crime unless
● Republic Act No. 9165, otherwise performed by a licensed physician.
known as the “Comprehensive
Dangerous Drugs Act of 2002” - ORPHAN DRUGS
“administer” means any act of
introducing any dangerous drug into ● Pharmacologic agents developed
the body of any person or animal, specifically to treat rare conditions
with or without his/her knowledge by like cystic fibrosis, sickle cell
injection, inhalation, ingestion or anemia, botulism and pneumocystis
other means, or of committing any pneumonia.
act of indispensable assistance to a ● These drugs are called “orphan”
person in administering a dangerous because under normal market
drug to himself/herself unless conditions the pharmaceutical
administered by a duly-licensed industry has little interest in
practitioner for purposes of developing and marketing products
medication. intended for only a small number of
patients less than 200,000.
● 1983: Drug Enforcement
Administration (DEA) - of the DOJ
was charged with the role of being
the nation’s sole legal drug
enforcement agency.
● 1983: Orphan Drug Act - designed
to promote the development and
manufacturer of orphan drugs.
● 1983: Orphan Drug Act - has three
primary incentives:

ABORTIFACIENT DRUGS 1. Federal funding of grants and


contracts to perform clinical
● Drugs that includes abortion, trials of orphan products.
dispense of these drugs for 2. 50% tax credits for costs of
intentional, non-indicated abortion is clinical testing.
considered illegal. 3. Exclusive right to market the
● “Physician-Only Laws” drug for 7 years from the
● Some non-physician health care marketing approval date.
providers, such as physician
assistants, advance registered
WEEK 4

Excipients
THREE PHASES OF DRUG ADDICTION
● Are fillers and inert substances used
in drug preparation to allow the drug
1. Pharmaceutic Phase
to enhance drug dissolution.
2. Pharmacokinetic Phase
● Disintegration is the breakdown of
3. Pharmacodynamic Phase
a tablet into smaller particles and
Dissolution is dissolving of the
smaller particles in the GI fluid
before absorption.

PHARMACEUTIC PHASE

● Also called DISSOLUTION


● The first phase of drug action. The Example:
drug becomes a solution so it can ❖ Ions Potassium and Sodium in
cross the cell membrane. Penicillin K+ and Na+ increase the
● A drug in solid form (tablet or absorbability of the drug.
capsule) must disintegrate into small ❖ Penicillin is the active antibiotic while
particles to dissolve into a liquid, a Na+ and K+ are the excipients.
process known as dissolution.
Rate-limiting-time or Rate of Dissolution
● The time it takes the drug to
disintegrate and dissolve to become
available for the body to absorb it.
● Liquid drugs are more rapidly
absorbed.
● Drugs in general are both
disintegrated and absorbed faster in
acidic fluids (pH 1 or 2 ) than in
alkaline fluids
● Very young and older adults have
less gastric acidity making drug
absorption slower.
1. ABSORPTION
● Enteric-coated tablets resist
● The movement of drug particles from
disintegration in the gastric acid.
the GI tract to the circulating body
● Enteric-coated tablets can remain in
fluids.
the stomach longer, so the onset of
effect may be delayed.
TYPES OF ABSORPTION
● Enteric-coated tablets/capsules and
❖ Passive absorption
sustained-release capsules should
❖ Active absorption
not be crushed to prevent altering
❖ Pinocytosis
their absorption.
● Food in GIT may interfere with drug
1. Passive absorption
dissolution.
● Occurs mostly by diffusion
● Some drugs irritate gastric mucosa,
(movement from higher
foods/fluids may be taken to dilute
concentration to lower
drug concentration and act as
concentration). The process of
potectants.
diffusion, the drug does not require
energy to move across the
PHARMACOKINETIC PHASE
membrane.
● 2 subtypes of passive absorption:
● The process of drug movement to
❖ Simple diffusion
achieve drug action.
❖ Facilitated diffusion
● Four processes (ADME)
❖ Absorption
❖ Distribution
❖ Metabolism
(biotransformation)
❖ Excretion
2. Active absorption
● Requires a carrier such as an
enzyme or protein to move the drug
against a concentration gradient.
Energy is required.

3. Pinocytosis
● Is a process by which cells carry a
drug across their membrane by
engulfing the drug particles.
6. Route of administration
Factors Affecting Drug Absorption
● Oral drugs the faster the
pharmaceutic phase.
1. Solubility
❖ IM - absorbed faster
● More fat soluble, faster the (deltoids)
absorption because cell ❖ Subcutaneous - slower
membranes are composed of (fat tissue beneath the
lipids. skin)

2. Ionization 7. External factors

● Non-ionized drugs have faster ● Blood flow, exercise, pain, stress


absorption compared to ionized and food will generally decrease
drugs. drug absorption.
❖ Aspirin-weak acid drug ❖ Poor circulation in the
❖ INFANTS - have higher stomach hampers drug
gastric pH (alkaline) than absorption.
adult, so they can absorb ❖ Pain, stress, and foods that
more penicillin. are solid, hot, or high in fat
can slow gastric emptying
3. Surface area of the membrane time and drug remains
longer in the stomach.
● Larger area, faster absorption. ❖ Exercise decreases blood
flow to the GIT.
4. Vascularity of site
8. First-pass effect
● More blood flow to site of
absorption, the faster the ● Passing of drug to the lover via
absorption. portal vein, after absorption before
● Example: distribution.
❖ Sublingual have many
capillaries and tiny blood 9. Bioavailability
vessels.
● The percentage of administered
5. Forms of drugs drug dosage that reaches the
systemic circulation.
● Elixirs more concentrated
First-Pass Effect
89% bound to protein
● The metabolism of a drug and its (Amitriptyline,
passage from the liver into the Chlorpromazine,
circulation. Diazepam)
❖ A drug given via the oral ❖ MODERATELY HIGHLY
route may be extensively PROTEIN-BOUND
metabolized by the liver DRUGS - 61% - 89%
bound to protein
before reaching the systemic (Erythromycin, Nafcillin,
circulation (high first-pass Phenytoin)
effect). ❖ MODERATELY
❖ The same drug - given IV - PROTEIN-BOUND
bypasses the liver, DRUGS - 30% - 60%
preventing the first-pass bound to protein (Aspirin,
Lidocaine, Meperidine)
effect from taking place, and
❖ LOW PROTEIN-BOUND
more drugs reach the DRUGS - less than 30%
circulation. bound to protein
(Amikacin, Amoxicillin,
2. DISTRIBUTION Atenolol)
● Process by which the drug becomes ● Portion of drug that is bound is
available to body fluids and body “inactive” because it is not
available to receptors.
tissues.
● The portion that remains unbound,
● Drug distribution is influenced by: is “free, active drugs”.
❖ Blood flow
❖ Drug’s affinity to the tissue
Three Forms of Drug in the blood after
❖ Protein-binding
First-pass Effect
❖ Blood-brain barrier
❖ Placental barrier
1. Metabolite
● In addition, volume of drug
● Fraction of the drug that underwent
distribution is dependent on drug
metabolism; mostly inactive and
dose and its concentration in the
excretable.
body.
● Drugs with a larger volume of drug
2. Protein bound
distribution have a longer half-life
● Fraction of the drug bound to plasma
and stay in the body longer.
protein (primarily albumin), thereby
held inactive because they will not
PROTEIN-BINDING be available to receptors (protein
binding prevents overdose).
● A common factor impacting
distribution of medication is
plasma protein in the blood. 3. Free form
Albumin is one of the most ● Drugs not bound to protein nor
important proteins in the blood. metabolized by the liver; active
❖ HIGHLY drugs that readily bind to specific
PROTEIN-BOUND receptors, thus producing the
DRUGS - greater than
pharmacologic response.
BLOOD-BRAIN BARRIER

● Impenetrable barricade/blockade
built from a tightly woven mesh of
capillaries that protect the brain
from potentially dangerous
substances such as “poison, virus
or bacteria”
● Example:
❖ Branded name drug
Sinemet is a combination
of Carbidopa and
Levodopa. Factors Affecting Drug Metabolism
❖ Diphenhydramine
(Benadryl)
AGE
PLACENTAL BARRIER
● Neonate and pediatrics and older
● Placenta is permeable to some adults
medications and can cause harm
to the unborn fetus during any DIET STATE & NUTRITION
trimester.
● Example: ● Low CHON diet decreases drug
❖ Opiates (Morphine), metabolism, grapefruit & sour
Atropine, Beta-blockers orange juice inhibits drug
metabolism.
3. METABOLISM (Biotransformation) GENDER
● Is the process by which the body
inactivates, or bio transform drugs. ● Women on contraceptive pills
● The enzymatic modification or metabolize some drugs at a slow
rate.
degradation of drug structure.
● LIVER - primary site of metabolism. PRESENCE OF LIVER & OTHER
❖ Most drugs inactivated by DISEASES
liver enzymes and
transformed to inactivate by ● Major effects are seen in diseases
affecting the LIVER.
liver enzymes and
transformed to inactive BODY TEMPERATURE
metabolites or water-soluble
substances for renal ● Mild & moderate hypothermia can
excretion. have an effect on some drug
metabolism.

GENETIC
VARIATION/PHARMACOGENETICS

● Genetic variants affect the function


of drug metabolizing enzymes.
Example:
ENVIRONMENTAL FACTORS
● If 100mg of a drug with a half-life of
● Cigarette smoke has an enzyme 60 minutes is taken, the following is
induction effect on drug estimated:
metabolism. Some insecticides ❖ 60 minutes after
and heavy metals such as administration, 50mg
mercury, nickel, cobalt, & arsenic
remains.
inhibit drug metabolizing activity of
enzymes. ❖ 120 minutes after
administration, 25mg
DRUG-DRUG INTERACTIONS remains
❖ 180 minutes after
PREGNANCY
administration, 12.5mg
● Pregnancy affects hepatic drug remains
metabolism due to elevated ❖ 240 minutes after
estrogen, progesterone, placental administration, 6.25 remains
growth hormone and prolactin. ❖ 300 minutes after
administration, 3.125mg
METABOLISM-HALF-LIFE remains
❖ Most drugs are considered
● HALF-LIFE (t ½) OF A DRUG to be effectively removed
● Is the time it takes for one half of the after about five half-lives.
drug concentration to be eliminated.
❖ Estimate the period of time Example Exercise:
that it takes for the ● If the patient takes 650mg of drug
concentration or amount in today and the half-life is 10 hours.
the body of that drug to be The next dose should be given or
reduced by exactly one half taken:
(50%). ❖ After 10 hours
❖ Metabolism and elimination ❖ Once a day
affect the half-life of a drug. ❖ Once a week
● FOR EXAMPLE: with liver and ❖ 3x a week
kidney dysfunction, the half-life of a ● A short half-life is considered to be 4
drug is prolonged, and less drug is to 8 hours, and a long half-life takes
metabolized and eliminated. When a several days for the body to
drug is taken continually, drug completely eliminate the drug.
accumulation can occur. ● Example:
❖ IV Gentamicin has a half-life ❖ Digoxin has 36 hours half-life
of 2-3 hours in a young
person with no kidney Steady State Concentration
disease but over 24 hours in ● Drug concentration in the blood that
someone with severe kidney must be maintained to achieve a
disease. desired effect.
● Physiologic state in which the
amount of drug removed via
elimination is equal to the amount of causing acidic urine thus
drug absorbed with each dose. inhibiting the elimination of
● Delayed drug metabolism results aspirin.
in: ● Kidney disease that results in
❖ Accumulation of drugs decreased glomerular filtration rate
❖ Prolonged action of the drugs (GFR) or decrease renal tubular
● Stimulating drug metabolism secretion can slow down or impair
causes: drug excretion.
❖ Diminished pharmacologic ● Decrease blood flow to the kidneys
effects can also alter drug excretion.

4. EXCRETION (or Elimination) 2 Types of Elimination


● Is the removal of unbound and
water-soluble drugs from the body.
Zero-order Kinetics
● Main route of elimination is through
the kidneys (urine). ● Elimination of the drug is
● Other routes include: independent of its concentration
❖ Liver-bile and decreases at a constant rate;
❖ Feces drugs that undergo zero-order
kinetics are phenytoin, ethanol
❖ Lungs
and aspirin.
❖ Sweat
❖ Breastmilk First-order Kinetics
❖ Tears
● Urine pH influences drug ● Elimination of the drug is
proportional to its concentration;
excretion.
most drugs undergo this
❖ Acidic urine promotes elimination pattern.
elimination of weak base
drugs.
PHARMACODYNAMIC PHASE
❖ Alkaline urine promotes
elimination of weak acid
● Is the study of the way drugs affect
drugs.
the body.
● Deals with the physiological effects
● Example:
of the drug on the body, whether
❖ Aspirin, is a weak acid, is
beneficial or harmful.
excreted rapidly in alkaline
● Types of Effects
urine.
❖ Primary - desirable,
❖ If a person takes an
expected therapeutic effect
overdose of aspirin, sodium
of the drug.
bicarbonate may be given to
❖ Secondary - additional effect
change the urine pH to
aside from the therapeutic
alkaline to promote excretion
effect of the drug.
of the drug.
● FOR EXAMPLE: Diphenhydramine
❖ Large quantities of cranberry
(Benadryl) is an example of a drug
juice can decrease urine pH,
with a primary and secondary effect.
❖ Primary effect is to treat the ONSET, PEAK, and DURATION of ACTION
symptoms of allergy.
❖ Secondary effect is a CNS ● Onset of Action - the time it takes
depression that causes to reach the minimum effective
drowsiness. concentration (MEC) after a drug is
❖ The secondary effect is administered.
undesirable when the patient ● Peak Action - occurs when the drug
drives a car, but at bedtime it reaches its highest blood and
could be desirable because it plasma concentration.
causes mild sedation. ● Duration of Action - is the length
of time the drug has a
DOSE RESPONSE AND MAXIMAL pharmacologic effect.
EFFICACY

● Dose response is the relationship


between the minimal versus the
maximal amount of drug dose
● TIME-RESPONSE CURVE -
needed to produce the desired drug
described by the dose-response
response.
curve that evaluates the drug onset
● Some patients respond to a lower
(concentration) and its effect.
drug dose, whereas others need a
● Drug plasma level decreases below
high drug dose to elicit the desired
MEC, adequate drug dosing is not
response.
achieved.
● Drug dose is usually adjusted to
● Too high drug level above MTC
achieve the desired drug response.
(minimum toxic concentration), can
● All drugs have a maximum drug
result in toxicity.
effect (maximal efficacy).
● FOR EXAMPLE
❖ Morphine and Tramadol
hydrochloride are prescribed
to relieve pain.
❖ The maximal efficacy of
Morphine is greater than
Tramadol hydrochloride,
regardless of how much
Tramadol HCl is given. The
pain relief of Tramadol is not Drug-Receptor Concept
as great as it is with RECEPTOR THEORY
Morphine.
● Drugs act through receptors by:
❖ Binding to the receptor to
produce (initiate)a response.
❖ Or to block (prevent) a
response.
❖ The activity of many drugs is
determined by the ability of
the drug to bind to a specific
receptor.
❖ The better the drug fits at a
receptor site, the more
biologically active the drug is.
● EXAMPLE:
❖ Osmotic laxative like
magnesium citrate attracts
and binds with water. This
medication works to pull
water content into the bowel
and increases the likelihood
DRUG EFFECTS
of a bowel movement.
● A receptor produces a variety of
● EXAMPLE:
physiologic responses, depending
❖ Antimicrobial and
on where in the body the receptor is
antineoplastic drugs
located.
commonly work by inhibiting
● Cholinergic receptors are
enzymes that are critical to
receptors on the surface of cells that
the function of the cell. With
get activated when they bind with
blockage of the enzyme
neurotransmitter “acetylcholine”.
binding site, the cell microbe
❖ Are located in the bladder,
or neoplastic cell is no longer
heart, blood vessels,
viable and cell death occurs.
stomach, bronchi, and eyes.
Agonist
NON-SPECIFIC DRUGS - drugs that affect
● A drug that binds to and stimulates
various sites have properties of no
the activity of one or more
specificity.
biochemical receptor types in the
● Drugs that stimulate or blocks the
body.
cholinergic receptors affect all
anatomic sites of location.
Antagonist
● Example:
● A drug that binds to and inhibits the
❖ Bethanechol (Urecholine)
activity of one or more biochemical
prescribed for postoperative
receptor types in the body
urinary retention to increase
EXAMPLE:
bladder contractions.
● Epinephrine (Adrenalin) stimulates
Cholinergic stes are also
beta1 and beta2 receptors
affected so the HR and BP
(AGONIST)
decreases, gastric acid
● Atropine blocks the histamine (H2)
secretions increases,
receptor, preventing excessive
bronchioles and pupils of the
gastric acid secretions
eyes constrict.
(ANTAGONIST).
NON-SELECTIVE DRUGS DOSE EFFECT PARAMETERS
● Drugs that act at different
receptors.
EFFICACY
● Drugs that affect various receptors
or have properties of non selectivity. ● Capacity for producing a desired
● EXAMPLE: result or effect.
❖ Chlorpromazine (Thorazine)
POTENCY
acts on norepinephrine,
dopamine, acetylcholine and ● Measure of drug activity
histamine receptors and a expressed in terms of the amount
variety of responses result required to produce an effect; a
from action at receptor sites. highly potent drug evokes a large
response at low dosages.
CATEGORIES OF DRUG ACTION
Therapeutic Window
● For every drug, there exists a dose
STIMULATION OR DEPRESSION
that is minimally effective and
● Stimulates the rate of cell activity another dose that is toxic. Between
or the secretion from the gland these doses is the therapeutic
increases. Depressed cell activity window, where the safest and most
and function of a specific organ effective treatment will occur.
are reduced.
● For example, Warfarin (Coumadin) is
REPLACEMENT a medication used to prevent blood
clotting and is monitored using a
● Drugs such as insulin replace blood test called INR. Too high of a
essential body compounds. dose of warfarin would cause the
INHIBITION OR KILLING OF INR to increase above the
ORGANISMS therapeutic window and put the
patient at risk of bleeding.
● Drugs that inhibit or kill organisms Conversely, too low of a dose of
interfere with bacterial cell growth warfarin would cause the INR to be
(e.g., penicillin exerts its
below the therapeutic window and
bactericidal effects by blocking the
synthesis of the bacterial cell wall). put the patient at risk of clotting.
❖ It is vital that the nurse
IRRITATION frequently monitors INR
levels for a patient receiving
● Drugs also can act by the warfarin to ensure the
mechanism of irritation, for
example laxatives irritate the inner dosage appropriately
wall of the colon, thus increasing reaches the therapeutic
peristalsis and defecation. window and does not place
the patient at risk for
bleeding or clotting.
PEAK AND TROUGH DRUG LEVELS

PEAK If either the peak and trough level is too


● the peak for a drug is when the level high, toxicity can occur.
of the drug in the patient’s body is If the peak is too low, no therapeutic effect
the highest. is achieved.
● Peak drug level is the highest
plasma concentration of a drug at a If the drug is given orally, the peak time
specific time. It indicates the rate of might be 1 to 3 hours after drug
administration.
absorption of the drug.
If a drug is given IV, the peak time might
TROUGH occur in 10 minutes.
● Trough drug levels indicate the rate
of elimination of the drug. If a peak drug level is ordered, a blood
sample should be drawn at the proposed
● The trough level is the lowest
peak time, according to the route of
concentration in the patient’s administration.
bloodstream, therefore, the
specimen should be collected just The trough drug level is the lowest
prior to administration of the drug. plasma concentration of a drug, and it
measures the rate at which the drug is
Peak and trough levels are requested for eliminated.
drugs that have a narrow therapeutic
index and are considered toxic, such as Trough levels are drawn immediately
aminoglycoside antibiotics. before the next dose of drug is given,
regardless of route of administration.

LOADING DOSE
● When immediate drug response is
desired, a large initial dose (loading
nose), of a drug is given to achieve a
rapid minimum effective
concentration in the plasma.
● A loading dose is most useful for
drugs that are eliminated from the
body slowly (with long systemic ❖ Rashes, jaundice, anemia,
half-life). decrease wbc, kidney
● Example of drugs that requires damage and nerve injury that
loading dose is DIGOXIN, a digitalis may impair vision or hearing.
preparation.
● Digitalization is the process by which TOXIC EFFECTS/TOXICITY
the minimum effective concentration ● Toxic effects/toxicity of a drug can be
level for digoxin is achieved in the identified by monitoring the plasma
plasma within a short time. (serum) therapeutic range of the
drug.
SIDE EFFECTS ● When the drug level exceeds the
● Are physiologic effects not related to therapeutic range, toxic effects are
desired drug effects. likely to occur from overdosing, or
● All drugs have desirable and drug accumulation.
undesirable side effects.
● It can occur even with the correct
dosage.
● Mostly side effects occur from drugs
that lack specificity, such as
Betanechol (Urecholine).
● Side effects are called adverse
reactions (at times).
● Can be used interchangeably but
they are different.
● Some side effects are expected as
part of drug therapy. And the
occurrence of these expected but
undesirable side effects is not a
reason to discontinue therapy.
TOLERANCE AND TACHYPHYLAXIS
ADVERSE REACTIONS ● TOLERANCE - refers to a
● Any noxious and untoward or decreased responsiveness over the
unintended response to a drug course of therapy.
which occurs at a dose for ● TACHYPHYLAXIS - refers to a rapid
prophylaxis, guide to establish or decrease in response to the drug.
indicate a diagnosis or therapy. ❖ An “acute tolerance”.
● Are more severe than side effects ❖ Drug categories that can
and always undesirable. cause tachyphylaxis include
● Adverse reactions must always be narcotics, barbiturates,
reported and documented because laxatives and psychotropic
they represent variances from agents.
planned therapy. ● FOR EXAMPLE: Drug tolerance to
● Example: narcotics can result in decreased
pain relief for the patient.
❖ If the nurse does not Culture
recognize the development ● Sets of learned behavior and ideas
of drug tolerance, the that human beings acquire as
patient’s request for more members of a community.
pain medication might be
interpreted as drug-seeking Community
behavior associated with ● Cluster of individuals who function
addiction. as a group to attain cultural
universals.
PLACEBO EFFECT
● A psychological benefit from a Cultural Universals
compound that may not have the ● Are designed to meet the
chemical structure of a drug effect. community’s survival needs and
● Placebo is effective in approximately common goals.
⅓ persons who take a placebo
compound. COMMUNICATION
● The placebo effect is when an
improvement of symptoms is ● Occurs verbally and nonverbally
observed, despite using a non active ● Nurses must be alert to different
treatment. It’s believed to occur due types of communication styles
to psychological factors like among patients to provide culturally
expectations or classical competent care.
conditioning. Research has found ● Examples of cultural competence in
that the placebo effect can ease nursing:
things like pain, fatigue, or ❖ Speaking in terms that are
depression. easy for the patient to follow
and understand.
❖ Not judging or disregarding a
WEEK 5
patient’s belief and religious
background, but encouraging
ETHNOPHARMACOLOGY them to do what works best
for them.
● The study of responses that may be ❖ Empathizing with the patient
unique to an individual owing to at all times.
social, cultural, and biologic
phenomena. LANGUAGE
● Pharmacogenetics integrates the
study of pharmacokinetics, ● Patient’s use of language other than
pharmacodynamics and variations of English.
the predicted response to a drug due ● Professional translators should be
to genetic factors. used whenever possible to
safeguard a patient’s confidentiality.
● There can be miscommunication SPACE
between the patient, the translator,
and the nurse. ● The amount of space around a
● Nurses should not confuse person’s body is an important
politeness with meaningful psychological consideration.
communication. ❖ Americans - desire a great
deal of personal space.
VERNACULAR ENGLISH ❖ Some cultures population
density may dictate limited
● Common language or words spoken personal space.
in particular social and cultural ● TOUCH - all cultures have taboos
groups. regarding touch and added
● Example: considerations when the patient is of
❖ “African-American Vernacular different gender than the nurse.
English”, used to describe a ❖ Nurses should inquire about
style of English speaking that a patient's preferences
is used among some African regarding touch before
Americans. implementing nursing care.
● More generally, vernacular English is
any style of English that varies from SOCIAL ORGANIZATION
standard English.
● Its used by patients can lead to ● Families are basic social units.
misunderstanding by the nurse or to ❖ Delivery of nursing care can
other communication difficulties. be enhanced by including the
family whenever appropriate.
GREETINGS AND COMMUNICATION ❖ American health care
STYLES long-standing practice is
limiting the amount of time a
● Nurses must keep in mind that patient can visit with
patient-nurse interactions in health members of the social group.
care settings are considered formal ❖ In Philippines, it is expected
and that informal styles of that family members will stay
communication should be used only by the patient’s bedside and
after careful consideration. participate in his or her care.
❖ Asian - some Asian descent
speak in a soft tone of voice TIME
and avoid direct eye contact.
❖ Asian Americans and ● Different perceptions of time
Native Americans - may be between nurses and their patients.
comfortable with periods of ❖ Time moves slowly for an
silence. anxious or in pain patient but
❖ Latin American, African, or moves quickly for a nurse
European - uneasy during who has a demanding
periods of silence. workload.
❖ Use of vague terms to dependence on strict time
denote may cause disparity schedules for economic and
between nurses’ and social activities.
patients’ perception of time ➢ Patients with
(words like now, soon, or present-oriented
later). perception of time
❖ Concepts of linear and people are more likely
circular time. to discontinue
➢ Linear time - present mainstream
flows into the future. prescriptive therapies
“I must do this now”. when they feel well.
➢ Circular time - ❖ Cultural groups steeped in
present has more traditional practices or
stability and the need perceive that their cultural
to do things at the identities are threatened
moment has less have a past orientation of
urgency. “I will have time.
the opportunity to do ➢ May lead to the use
this later”. of traditional health
● Cultural aspect of time has a practices.
profound effect on ● REMEMBER: Health behaviors of
pharmacotherapeutic adherence. individuals are also influenced by the
● All cultures have a concept of time quantity and quality of past
as it is related to the past, present, experiences with the healthcare
and future. system.
❖ Western European descent
exhibits a great deal of future ENVIRONMENTAL CONTROL
orientations.
➢ Can lead to health ● A major aspect of culture is the
practices perceived to desire to control nature to facilitate
prevent illness. the needs of human beings.
➢ Concern for the future ● Illness may be attributed to cosmic
serves as motivation forces and believed to be cured or
to take steps to make better by persons who
control chronic possess special abilities.
illness, which is likely ❖ Traditional healers - play a
to lead to greater role in traditional health
adherence to practiced (80% of the
long-term population nationwide).
pharmacotherapy. ❖ Healers and spiritual
❖ Non-European such as advisors - can be beneficial
African, Asian, Native in healthcare settings.
American or Latin American ➢ Canadian health
have exhibited less care system - First
Nation, Inuit and action of substrates and accounts for
Metis were developed the variations in drug metabolism in
to improve the health individuals and groups.
care of its indigenous ● Genetic markers - predominantly
people (the use of characteristics of a certain biologic
traditional healers group.
and spiritual guides). ● Example:
❖ Caucasian in the US have
BIOLOGIC VARIATIONS abnormally low CYP2D6
enzyme that metabolizes
● Human Genome Project - drugs such as
international collaborative research antidepressants,
program, the field of antipsychotics, and beta
pharmacogenomics is rapidly blockers than Asian or
expanding. African.
● Pharmacogenomics refers to the ❖ African Americans respond
general study of all different genes poorly to several classes of
that determine drug behavior. antihypertensive agents
● Example: (beta blockers and
❖ Cytochrome P-450 (CYP) angiotensin-converting
enzymes effect on drug enzyme inhibitors).
response, drug-drug ❖ Differences in skin structure
interactions and adverse and physiology can affect
drug events. response to dermatologic
● The Genographic Project - and topically applied
performed DNA testing on products.
populations worldwide, findings ➢ African Americans
reveal that human beings are 99.9% demonstrated lower
genetically identical (not multiple responses to
races but multiple genotypes). interferon-alpha
❖ Genomes - are a complete (treatment for
set of chromosomes and Hepatitis C).
make up a cell’s DNA ❖ Asian - has inherited variant
❖ Polymorphisms - are DNA H 1502LA-B gene,
variants that occur within recommending to be
specific population at a genetically tested before
frequency greater than 1% starting Carbamazepine
❖ Substrate - a substance that (Tegretol) because of
binds to and is metabolized association to serious skin
by one or more enzymes. reactions.
Drugs are chemical ➢ These intrinsic
substances of substrate. biologic factors along
● Cytochrome P-450 (CYP) enzyme with extrinsic factors
system either induces or inhibits the such as diet and
environmental and
● Exhibit moderate amounts of
sociocultural issues to touching among group members.
prescribe effective
therapies and provide LATIN AND NATIVE AMERICAN
holistic health care.
● Comfortable with a small amount
of personal space.
COMMUNICATION STYLES ● Latin American value touching
● Native Americans use touch
EUROPEAN lightly.

● Prefer eye contact SOCIAL ORGANIZATIONS


● Use moderate to loud vocal
volume.
● Use many words to describe EUROPEAN
symptoms.
● Uncomfortable with periods of ● Small, nuclear families
silence. ● Extended family members often
live a far distance away.
AFRICAN ● High degree of individualism

● Prefer direct eye contact AFRICAN


● Use moderate to loud vocal
volume ● Small, nuclear families in America
● Uncomfortable with periods of but might classify non related
silence persons as family.
● Important to recognize these
LATIN AND NATIVE AMERICAN members of the social group.

● Not likely to make direct eye LATIN AND NATIVE AMERICAN


contact with persons perceived to
be in authoritative positions. ● Large, extended families are
● Varying degrees of comfort with important to include family
silence. members in care.

SPATIAL PREFERENCES PERCEPTION OF TIME

EUROPEAN EUROPEAN

● Prefer a large amount of personal ● High level of importance placed on


space. the future.
● Value privacy ● Expect that the present level of
● Exhibit low to moderate amount of comfort be addressed.
touching among group members. ● Little focus on the past.

AFRICAN AFRICAN

● Comfortable with a smaller ● High level of importance placed on


amount of personal space. the present .
BIOLOGIC VARIATIONS
● Connected with the past as
evidenced by the use of home
remedies passed through EUROPEAN
generations.
● More concerned with the future as ● Poor metabolizers of
longevity increases. antidepressants, antipsychotics, or
cardiovascular agents, and
LATIN AND NATIVE AMERICAN isoniazid, which can lead to
toxicity.
● High level of importance placed on
the present. AFRICAN
● Connected with the past as
evidenced by the use of traditional ● May have diminished therapeutic
healers. effects from beta blockers, ACE
● More concerned with the future as inhibitors and warfarin sodium
longevity increases. (Coumadin).

LATIN AND NATIVE AMERICAN


ENVIRONMENTAL CONTROL
● Native American have a high
EUROPEAN incidence of lactose intolerance
resulting in low-calcium diets.
● Believe that healthy behaviors ● Also exhibit enhanced vasomotor
prevent illness. responses to alcohol.
● Secondary believer that illness is
caused by cosmic forces.
● Believe in being united with a deity
in the afterlife.

AFRICAN

● Spiritually oriented
● Important to include clergy in care.
● Believe in being united with a deity
in the afterlife.

LATIN AND NATIVE AMERICAN

● Spiritually oriented
● Followers of Christian religion
derive comfort from religious
artifacts such as rosary beads.
● There may be multiple deities in
indigenous religions.

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