NURSING PHARMACOLOGY
LEARNING OUTCOMES: ABSORPTION
At the end of the lesson, the nursing student can: • Movement of a drug from the site of
• Differentiate the three phases of drug action; administration into the bloodstream
• Describe the four processes of pharmacokinetics; • Absorption determines how long it takes for a
• Explain the meaning of pharmacodynamic; and,
drug to take effect
• Define the terms half- life, therapeutic index,
• Usually the more rapid the absorption, faster the
therapeutic drug range, side effects, adverse reaction
and drug toxicity. drug works
• the movement of drug particles from the G.I. tract
PHARMACOLOGY to body fluids by:
a. Passive absorption
• The study of the action of drugs on a biologic b. Active absorption
system. c. Pinocytosis
A. Passive absorption
THREE PHASES OF DRUG ACTION
• Does not require energy to move across the
1. Pharmaceutic membrane.
▪ Solid dosage form → Liquid • Drugs can be absorbed through plasma
2. Pharmacokinetics primarily by: Diffusion (movement from
▪ ADME (Absorption, Distribution, higher concentration to lower concentration)
Metabolism, Excretion) B. Active absorption
3. Pharmacodynamics • Requires a carrier such as an enzyme or
▪ Drug action: Onset, Peak, Duration protein
▪ Receptors, Enzymes, Hormones • Energy is required for active absorption
PHARMACEUTIC PHASE
• First phase of drug action
• Disintegration – is the breakdown of tablet into
smaller particles
• Dissolution - dissolving of the smaller particles in
the GI fluid before absorption
• Dissolution time – time it takes for the drug to
disintegrate and dissolve to become available for C. Pinocytosis
the body to absorb it. • Process by which cells carry drug across
their membrane by engulfing the drug
PHARMACOKINETIC PHASE particles
Factors Affecting Absorption
• Surface area
• Second phase of drug action
• Contact time with surface
• The process of drug movement to achieve drug
• Circulation
action
• Solubility (water soluble vs lipid soluble)
• What the body does to the drug
• Ionization (weak versus strong acid/base)
• Refers to the study of how the body processes
• Drug form & drug concentration
drugs
• Bioavailability (after first pass thru liver)
• Route of administration (enteral & parenteral)
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NURSING PHARMACOLOGY
• Additives: alter the location of disintegration of • There will be less active drug available for action
drugs as well as increase or decrease the rate in the body cells after this first Pass through the
of absorption Liver
• Enteric coating allows a drug to dissolve only
in an alkaline (pH greater than 7.0)
environment such as the small intestine.
• Sustained release drugs: allow drugs to be
released slowly over time, rather than quickly,
like conventional tablets.
• Size of drug particles: smaller the particle,
faster the onset.
Drug Absorption varies by Dosage Form
(fastest → slowest)
1. Liquids solutions (Elixirs, Syrups)
2. Suspension
3. Powders
4. Capsules
5. Tablets
6. Coated tablets Variations in Metabolism
7. Enteric-coated tablets
• Pharmacogenetics - hereditary influences on drug
DISTRIBUTION
responses, refers to variations in which
• the transport of drugs from the blood to the site of
individuals metabolize drugs.
action. A drug must be distributed to its site of
• Circadian Rhythms - the rate of drug absorption,
action to have an effect
hepatic clearance, half-life and duration of action,
• Drugs are also distributed to tissues where it has
have all been shown to differ depending upon the
no effect. Competition for drug binding sites
time of day a drug is administered.
affects the amount of drug available for action in
• Effects of Gender and Age
the body.
• Some enzymes have higher activity in females
• Volume of Distribution (Vd) - The degree of
than males, and others are more active in
distribution of a drug into various body
males than in females.
compartments and tissue
• Ageing is associated with a reduction in first-
pass metabolism. This is probably due to a
reduction in liver mass and blood flow. As a
result, the bioavailability of drugs undergoing
extensive first-pass metabolism can be
significantly increased.
• Enzyme activity is typically reduced in the
neonate, but rapidly develops over the first
Factors Affecting Distribution year of life.
• Perfusion Rate EXCRETION
• Permeability of Membranes • process where drugs are removed from the body
• Protein binding • Kidneys are the major organs of excretion
• Tissue Localization
• Blood Brain Barrier
• Placenta
METABOLISM
• Breaking down the drug
• Biotransformation: process by which the body
changes the chemical structure of a drug to
another form called a metabolite.
• Metabolite: a more water-soluble compound that
can be easily excreted. The major organ for this
process is the liver
• First Pass Phenomenon - Drugs are first • Lungs excrete gaseous drugs
absorbed through the small intestine then arrive • Biliary excretion (bile & feces) is important for a
at the liver via the portal circulation few drugs. These drugs may be reabsorbed when
• There they undergo considerable passing through the intestines from the liver
biotransformation before entering the systemic (enterohepatic re-circulation)
circulation.
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NURSING PHARMACOLOGY
• Intestines, sweat, saliva and breast milk c) Substitutive (replaces body fluids or
constitute minor routes of drug excretion substances)
• Clearance of drugs - elimination of drugs from d) Chemotherapeutic (destroys malignant cells)
circulation by all routes. It affects the time a drug e) Restorative (returns the body to health)
remains in the body and the dosage required. • Adverse Drug Reaction is an unwanted or harmful
• Renal Clearance reaction experienced following the administration
• Hepatic clearance of a drug or combination of drugs under normal
• Effects of Gender and Age - Elimination of the conditions of use and is suspected to be related to
drug from the body is directly influenced by age. the drug. An ADR will usually require the drug to
Newborns and elderly experience the effects of be discontinued or the dose reduced.
drugs for longer and the drug takes a lot longer to • Adverse event is harm that occurs while a patient
be eliminated from the body. is taking a drug, irrespective of whether the drug
• Newborns: When babies are born to term, is suspected to be the cause.
their renal function is very quick to establish • Side-effect is any effect caused by a drug other
similar levels to adults within one week after than the intended therapeutic effect, whether
birth. If the baby is born prematurely it can beneficial, neutral or harmful. The term ‘side-
take 8 weeks or more to reach the level of effect’ is often used interchangeably with ‘ADR’
enzymes necessary. If drugs are given before although the former usually implies an effect that
the renal function is at this level, the drug is less harmful, predictable and may not even
elimination from the body takes a lot longer require discontinuation of therapy (e.g. ankle
and so do the effects of the drugs. edema with vasodilators).
• Elderly: Renal filtration rate begins to decline • Drug toxicity describes adverse effects of a drug
at 20 years of age and by 50 years of age it that occur because the dose or plasma
has declined by 50%. This again will affect the concentration has risen above the therapeutic
elimination of drugs from the body. range, either unintentionally or intentionally (drug
PLASMA HALF-LIFE overdose).
• The elimination half-life of a drug is a • Drug abuse is the misuse of recreational or
pharmacokinetic parameter that is defined as the therapeutic drugs that may lead to addiction or
time it takes for the concentration of the drug in dependence, serious physiological injury (such as
the plasma or the total amount in the body to be damage to kidneys, liver, heart), psychological
reduced by 50%. In other words, after one half- harm (abnormal behavior patterns, hallucinations,
life, the concentration of the drug in the body will memory loss), or death.
be half of the starting dose. • Hypersensitivity / allergy: exaggerated adverse
• Drugs with short half-lives are quickly eliminated reaction to drug
from the body. (Ex: analgesics: given several
ADDITIONAL NOTES
doses per day)
CHEMICAL INTERACTIONS
• Drugs with longer half-lives stay in the body
• Additive Effect: 2+2=4
longer (Ex: Digoxin given once a day)
-Summation of effects of drugs taken
PHARMACODYNAMIC PHASE concurrently
• What the drug does to the body • Synergistic Effect: 2 + 2 = >4
• refers to the study of the mechanism of drug -Effect of drug is higher than the sum of their
action on living tissue individual effects
• Drugs may increase, decrease or replace • Potentiating Effect: 0 + 2 = >2
enzymes, hormones or body metabolic functions. -Effect of drug is enhanced by another drug or
• Chemotherapeutic drugs alter an abnormal substance
parasite or growth on the body such as bacteria, • Antagonistic Effect 2 + 2 = <2
viruses or neoplastic tissue (Ex: antibiotics and -One drug cancels or blocks effects of another
antineoplastic drugs) Potency – amount of a given drug that is required to
produce a given effect
Efficacy – max effect that a given drug will produce
Toxicity – capacity of a drug to do damage or cause
adverse effects in the body
Therapeutic index – determine how close a toxic dose
is to an effective one
Therapeutic window – range of plasma concentration
Effects of Drugs between the Minimum Effective Concentration (MEC)
• Therapeutic / Desired effect and the Minimum Toxic Concentration (MTC)
a) Curative (cures a disease or condition) Onset of action – length of time it takes for a medicine
b) Supportive (supports a body function until to start to work
other treatments or the body's response can Duration of action – length of time a particular drug is
active
take over)
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