AREAS OF PHARMACOLOGY

PHARMACEUTIC PHASE PASSIVE ABSORPTION

• Also the known as dissolution • Higher Concentration to Lower Concentration
• The first phase of drug action. • Occurs mostly by diffusion.
• In the gastrointestinal (GI) tract, drugs need to be in solution • Drugs does not require energy to move across the
so they can be absorbed. membrane.
• A drug in solid form (tablet or capsule) must disintegrate
into small particles to dissolve into a liquid, a process known ACTIVE ABSORPTION
as dissolution. • Requires a carrier.
• Disintegration ➢ Carrier can be in the form of enzymes or protein in
➢ The breakdown of a tablet into smaller particles. order to move the drug in a concentration gradient.
• Dissolution • Energy is required.
➢ The dissolving of the smaller particles in the GI
fluid before absorption. PINOCYTOSIS
➢ Rate of dissolution is the time it takes the drug to • A process by which cell carry drugs across the membrane
disintegrate and dissolve to become available for by engulfing the drug particles.
the body to absorb it.
• Drugs in liquid form are more rapidly available for GI
absorption than are solids.

EXCIPIENTS
• Tablets are not 100% drug.
• Fillers and inert substances, generally called excipients,
are used in drug preparation to allow the drug to take on a
particular size and shape and to enhance drug dissolution.
ENTERIC-COATED DRUGS
• They resist disintegration in the gastric acid of the stomach.
➢ So disintegration does not occur until the drug
reaches the alkaline environment of the small
intestine.
• These can remain in the stomach for a long time.
➢ Therefore, their effect may be delayed in onset.
• Enteric-coated tablets or capsules and sustained-release
(beaded) capsules should not be crushed.
➢ Crushing would alter the place and time of
absorption of the drug
AREAS OF PHARMACOLOGY
• It includes the following areas:
1. Pharmacokinetic Phase
2. Pharmacodynamics
3. Pharmacotherapeutics
PHARMACOKINETICS
• Study of the processes of the drug.
• The process of drug movement to achieve drug action.
• The process by which drug passes from the site of
administration into the bloodstream.
• 4 Processes:
1. Absorption
2. Distribution
3. Metabolism or Biotransformation
4. Excretion or Elimination
• The nurse applies knowledge of pharmacokinetics when
assessing the patient for possible adverse drug effects.
➢ Adverse Effects are much more severe compared
to Side Effects.
➢ These are unexpected negative effects.
ABSORPTION
• Taken into the body.
• The movement of drug particles from the GI tract to body
fluids by passive absorption, active absorption, or
pinocytosis.
• There are 3 Kinds of Absorption
1. Passive Absorption
2. Active Absorption
3. Pinocytosis
WATER-SOLUBLE VS. FAT-SOLUBLE
• GI membrane is composed mostly of lipid (fat) and protein,
• Lipid-Soluble Drugs
➢ Pass rapidly through the GI membrane.
• Water-Soluble Drugs
➢ Would need a carrier to pass the membrane.
• Large particles pass the cell membrane if they are non-
ionized (no positive or negative charge).
➢ Weak acid drugs such as aspirin are less ionized
in the stomach, and they pass through the
stomach lining easily and rapidly.
• Drugs that are lipid soluble and nonionized are absorbed
faster than water-soluble and ionized drugs.
FACTORS AFFECTING ABSORPTION
• It includes the following:
1. Blood flow
2. Pain, stress, food
3. Exercise
4. Nature of absorbing surface
5. Solubility of the drug
6. pH
7. Drug concentration
8. Dosage form
• Poor circulation to the stomach as a result of shock,
vasoconstrictor drugs, or disease hampers absorption.
• Pain, stress, and foods that are solid, hot, or high in fat can
slow gastric emptying time, so the drug remains in the
stomach longer.
• Exercise can decrease blood flow by causing more blood to
flow to the peripheral muscle, thereby decreasing blood
circulation to the GI tract.
DIFFERENT SITES OF ABSORPTION IN GIT
• Mouth or Oral Cavity
• Stomach
• Small Intestine
• Others:
➢ Drugs given IM are absorbed faster in muscles
that have more blood vessels (e.g., deltoids) than
in those that have fewer blood vessels (e.g.,
gluteals).
➢ Subcutaneous tissue has fewer blood vessels, so
absorption is slower in such tissue.

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 HEPATIC FIRST PASS
• Also known as the First-pass Effect
• The process in which the drug passes to the liver first.
BIOAVAILABILITY
• A subcategory of absorption.
• It is the percentage of the administered drug dose that
reaches the systemic circulation.
• For the oral route of drug administration, bioavailability
occurs after absorption and first-pass metabolism.
➢ The percentage of bioavailability for the oral route
is always less than 100%, but for the IV route it is
100%
FACTORS AFFECTING BIOAVAILABILITY
• Drug form
• Route of administration
• GI mucosa and motility
• Food and other drugs
• Changes in the liver metabolism caused by liver dysfunction
or inadequate hepatic blood flow.
➢ A decrease in liver function or a decrease in
hepatic blood flow can increase the bioavailability
of a drug, but only if the drug is metabolized by the
liver.
➢ Less drug is destroyed by hepatic metabolism in
the presence of liver disorder.
DISTRIBUTION
• Moved into various tissues.
• The transportation of a drug from its site of absorption to its
site of action.
• The process by which the drug becomes available to body
fluids and body tissues.
• Drug distribution is influenced by blood flow, the drug’s
affinity to the tissue, and the protein-binding effect.
• Drugs with a larger volume of drug distribution have a
longer half-life and stay in the body longer.
PROTEIN BINDING
• As drugs are distributed in the plasma, many are bound to
varying degrees (percentages) with protein (primarily
albumin).
> 89% Highly Protein-Bound Drugs
61% to 89% Moderately Highly Protein-Bound Drugs
30% to 60% Moderately Protein-Bound Drugs
<30% Low Protein-Bound Drugs
FREE DRUGS
• Drugs that are not bound to protein
• Only free drugs are active and can cause a pharmacologic
response.
• As the free drug in the circulation decreases, more bound
drug is released from the protein to maintain the balance of
free drug.
METABOLISM
• Also known as biotransformation or detoxification
• Changed into a form that can be excreted.
• Process by which the body inactivates/biotransforms drugs.
• A sequence of chemical events that change a drug to a less
active form after in enters the body.
• Principal Site: Liver
• Hepatic First Pass Effect
HALF-LIFE
• The half-life of a drug refers to the time it takes for one half
of the drug concentration to be eliminated.
• Metabolism and elimination affect the half-life of a drug.
EXCRETION OR ELIMINATION
• The primary process by which drugs are eliminated from the
body.
• The main route of drug elimination:
➢ Through the kidneys (urine)
➢ The kidneys filter free unbound drugs, water-
soluble drugs, and drugs that are unchanged.
• Drugs can be excreted by the kidneys, intestines, lungs,
mammary glands, sweat glands, and salivary glands.
FACTORS AFFECTING RENAL EXCRETION
• Glomerular Filtration Rate (GFR)
➢ A measure of howl well the kidneys filter blood.
• Tubular Secretion Rate
• Urine pH
• Decreased Blood Flow to the Kidney
• Other Drugs
• Blood Concentration Levels
• Half-life
PHARMACODYNAMICS
• The study of the way drugs affect the body.
• Drug response can cause a primary or secondary
physiologic effect or both.
➢ Primary effect is desirable.
➢ Secondary effect is desirable or undesirable.
• An example of a drug with a primary and secondary effect
is diphenhydramine (Benadryl), an antihistamine.
➢ Primary effect is to treat allergy symptoms.
➢ Secondary effect is CNS depression that causes
drowsiness.
➢ Second effect is undesirable when patient drives a
car but could become desirable if at bedtime since
it causes mild sedation.
MECHANISM OF ACTION (MOA)
• Explanation of how a drug produces is effect.
INDICATION
• Intended use(s) of any drug.
CONTRAINDICATION
• Refers to the situation or circumstance when a particular
drug should not be given.
MAINTENANCE DOSE
• Exact amount of a drug that is administered to maintain
drug blood level in the therapeutic range.
LOADING DOSE
• A large initial dose given to achieve immediate drug effect.
POTENCY
• A measure of the strength of a drug required to produce a
specific response.
RECEPTOR SITE
• Specific location on a cell membrane or within the cell
where a drug attaches to produce an effect.
DOSE RESPONSE
• Dose response is the relationship between the minimal
versus the maximal amount of drug dose needed to
produce the desired drug response.
• Some patients respond to a lower drug dose, whereas
others need a high drug dose to elicit the desired response.
• The drug dose is usually adjusted to achieve the desired
drug response.
MAXIMAL EFFICACY
• All drugs have a maximum drug effect (maximal efficacy).
• Example:
➢ Morphine and tramadol hydrochloride (Ultram) are
prescribed to relieve pain.
• The maximum efficacy of morphine is greater than tramadol
hydrochloride, regardless of how much tramadol
hydrochloride is given.
• The pain relief with the use of tramadol hydrochloride is not
as great as it is with morphine.
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 ONSET OF ACTION
• Onset of action is the time it takes to reach the minimum
effective concentration (MEC) after a drug is administered.
PEAK ACTION
• Occurs when the drug reaches its highest blood or plasma
concentration/
SUPPLEMENTAL OR REPLACEMENT
• To replenish or substitute for missing substances.
SUPPORTIVE
• Does not treat the cause of the disease but maintains other
threatened body systems until the patient’s condition
resolves.

DURATION OF ACTION PALLIATIVE

• The length of time the drug has a pharmacologic effect. • Used for end-stage or terminal diseases to make the patient
as comfortable as possible.

FACTORS AFFECTING A PATIENT’S RESPONSE TO

A DRUG
• Age
• Cardiovascular Function
• Diet
• Disease
• Drug Interaction
• GI Functions
• Hepatic Function
• Infection
• Renal Function
TIME-RESPONSE CURVE
• Gender
• Evaluates three parameters of drug action: the onset of
drug action, peak action, and duration of action.
PHARMACOGENETICS
• It is necessary to understand the time response in
relationship to drug administration. • The scientific discipline studying how the effect of a drug
action varies from a predicted drug response because of
• If the drug plasma or serum level decreases below
genetic factors or hereditary influence.
threshold or MEC, adequate drug dosing is not achieved.
➢ Too high a drug level above the minimum toxic • Because people have different genetic makeup, they do not
concentration (MTC) can result in toxicity. • always respond identically to a drug dosage or planned
drug therapy.
RECEPTORS • Genetic factors can alter the metabolism of the drug in
converting its chemical form to an inert metabolite; thus, the
• Most are protein in structure and are found on cells.
drug action can be enhanced or diminished.
• Drug binding sites are primarily on proteins, glycoproteins,
• Some persons are less or more sensitive to drugs and their
proteolipids, and enzymes.
drug actions because of genetic factors.
• Ligand Binding Domain
➢ The site on the receptor in which drugs bind.
PLACEBO EFFECT
• A psychological benefit from a compound that may not have
SIDE EFFECTS
the chemical structure of a drug effect.
• Physiologic effects not related to the drug’s desired effect.
• All drugs have side effects, desirable or not.

ADVERSE REACTIONS
• More severe than side effects.
• Range of untoward effects of drugs that cause mild to
moderate side effects including anaphylaxis.
• Always undesirable.

TOXIC EFFECTS OR TOXICITY

• Can be identified by monitoring the plasma (serum)
therapeutic range of drug.

THERAPEUTIC INDEX
• The relationship between a drug’s desired therapeutic
effect and its adverse effect.
• Measures the margin of safety of a drug expressed as the
ratio of LD50 to ED50.
➢ Therapeutic Ratio = LD50/ED50
➢ Therapeutic Range or Window
o Range of plasma concentration that
produces the desired effect without
toxicity.

PHARMACOTHERAPEUTICS
• The study of the therapeutic uses and effects of drugs.

ACUTE THERAPY
• If the patient is critically ill and requires acute intensive
therapy.

EMPIRIC THERAPY
• Based on practical experience rather than on pure scientific
data.

MAINTENANCE THERAPY
• For patients with chronic conditions that don’t resolve.

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