Fundamental Concepts of Pharmacology 2

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OBJECTIVES

o Define Pharmacology and Drugs


o Differentiate the Three Phases of Drug Action
o Describe the Processes of Pharmacokinetics
o Analyze the Factors Affecting Responses to Drugs
o Describe the Nursing Implications of Pharmacokinetics
and Pharmacodynamics
DRUG DEFINITION

• A branch of biomedical science, encompassing


clinical pharmacology, that is concerned with the
effects of drugs/ pharmaceuticals and other
xenobiotics on living systems, as well as their
development and chemical properties.
DRUG DEFINITION

• A chemical substance of known structure, other


than a nutrient of an essential dietary ingredient,
which when administered to a living organism
produces a biological effect.
DRUG DEFINITION

• A pharmaceutical drug, also called medicine, is a


chemical substance used to treat, cure, prevent or
diagnose a disease or to promote well-being
PHASES OF DRUG ACTION

Pharmaceutic Phase

Pharmacokinetic Phase

Pharmacodynamic Phase
PHARMACEUTIC PHASE

• A process where drugs in solid form (tablet or


capsule) must disintegrate into small particles to
dissolve into liquid.
PHARMACEUTIC PHASE

DISINTEGRATION- breakdown of a tablet into


smaller particles
DISSOLUTION- dissolving of the smaller particles in
the GI fluid before absorption
PHARMACOKINETIC PHASE
• Process of drug movement to achieve drug action
• This phase describes the time course and disposition of a
drug in the body, based on its absorption, distribution,
metabolism and elimination.
• 4 Processes:

ABSORPTION DISTRIBUTION METABOLISM/ EXCRETION/


BIOTRANSFORMATION ELIMINATION
ABSORPTION
• For a drug to be absorbed and used by the body, it
must first pass through various anatomical barriers.

• Refers to the movement of drug particles from the GI


tract to body fluids by passive absorption, active
absorption or pinocytosis.
ABSORPTION
ABSORPTION
 Other factors that affect absorption:
Lipid/ water solubility
Ionization
Acidity of the stomach
Blood flow
pH
Presence/absence of food
Pain / Stress
ABSORPTION
• First-Pass Effect/ Hepatic First Pass- the process in
which the drug passes to the liver first

• Bioavailability- percentage of the administered drug


dose that reaches the systemic circulation. Factors that
affect include the drug form, route, GI mucosa, food
and other drugs and changes in liver metabolism.
DISTRIBUTION
• The process by which the drug becomes available to
body fluids and body tissues.
DISTRIBUTION
• Only free drugs(drugs that are not
bound to protein) are active and can
cause a pharmacologic response
• When two highly-protein drugs are
given concurrently, they compete for
protein-biding sites, thus causing
more free drug to be released in the
circulation.
METABOLISM
• Liver- primary site of metabolism
• The liver metabolizes lipid-soluble drugs to water-
soluble drugs for excretion. However, some drugs are
transformed into active metabolites.
• Half-life- time it takes for one half of the drug
concentration to be eliminated
EXCRETION
• Kidney- main route of drug elimination
• Factors that affect drug excretion:
– Urine pH
– Kidney disease
PHARMACODYNAMIC PHASE

• It is the study of drug concentration and its effects on


the body.
• Primary effect- desirable; Secondary effect- either
desirable or not
• No drug exerts a simple isolated action solely on the
diseased part of an abnormal organ
PHARMACODYNAMIC PHASE

• Dose Response- relationship between the minimal


versus the maximal amount of drug dose needed to
produce the desired drug response
• All drugs have a maximum drug effect (maximal
efficacy)
PHARMACODYNAMIC PHASE

• Onset of action- the time it takes to


reach the minimum effective
concentration (MEC) after a drug is
administered
• Peak action- highest plasma
concentration
• Duration of action- length of time
the drug has a pharmacologic effect
PHARMACODYNAMIC PHASE

• Receptor theory:
– Cell membrane embedded enzymes
– Ligand-gated ion channels
– G protein-coupled receptor systems
– Transcription factors
PHARMACODYNAMIC PHASE
PHARMACODYNAMIC PHASE

• Agonists- drugs that produce


a response
• Antagonists- drugs that block
a response
PHARMACODYNAMIC PHASE

• A receptor produces a variety of


physiologic responses, depending
on where that receptor is located
• Nonspecific drugs affect various
sites
• Nonselective drugs affect various
receptors
PHARMACODYNAMIC PHASE

• Categories of drug action:


1. Stimulation or depression
2. Replacement
3. Inhibition or killing of organisms
4. Irritation
PHARMACODYNAMIC PHASE

• Therapeutic Index(TI)- estimates


the margin of a drug through the
use of a ratio that measures the
effective dose (ED) and lethal dose
(LD). The closer the ratio is to 1,
the greater the danger of toxicity
PHARMACODYNAMIC PHASE

• Peak drug level- highest plasma concentration of drug


at a given time and indicate rate of absorption of drug
• Trough level- lowest plasma concentration and
measures the rate at which drug is eliminated
• Loading dose- initial dose given to achieve rapid MEC
in the plasma
PHARMACODYNAMIC PHASE

• Side effects- physiologic effects not related to the


desired drug effect
• Adverse reactions- more severe than side effects;
range of untoward effects of drugs that cause mild to
severe effects including anaphylaxis.
• Tachyphlaxis- drug tolerance to a frequently repeated
administration of a certain drug
PHARMACODYNAMIC PHASE

• Placebo effect- physiologic benefit from a compound


that may not have the chemical structur of a drug
effect.
• Pharmacogenetics- effect of drug action that varies
from a predicted drug response because of genetic
factors or hereditary influence.
DETERMINANTS THAT AFFECT
DRUG THERAPY
Clinical Factors: Administration:
Age and Weight Drug Form
Present Health Disorder Route
Other Disease Entities Multiple Drug Therapy
Client Drug Compliance Drug Interactions

DRUG
Pharmacokinetics: Pharmacodynamics:
Absorption Onset, Peak, Duration
Distribution (PB) Therapeutic Range
Metabolism (t1/2) Side Effects, Adverse Reactions
Excretion
LEGISLATION-CONTROLLED
SUBSTANCES
• A drug or other substance that is tightly controlled by the
government because it may be abused or cause addiction.
• Controlled substances include opioids, stimulants,
depressants, hallucinogens, and anabolic steroids.
• Controlled substances such as morphine, Valium, and
Ritalin are available only by prescription from a licensed
medical professional.
GENERIC DRUGS

• A generic drug is a pharmaceutical drug that contains


the same chemical substance as a drug that was
originally protected by patents.
• Generic drugs marketed without brand names are
generally less expensive than brand-name drugs, even
though they are chemically identical to brand-name
drugs and meet the same standards
ORPHAN DRUGS

• An orphan drug is a pharmaceutical agent developed to


treat medical conditions which, because they are so
rare, would not be profitable to produce without
government assistance.
OVER-THE-COUNTER DRUGS

• Over-the-
counter (OTC) drugs are medicines s
old directly to a consumer without
a prescription from a healthcare
professional
NURSING IMPLICATIONS

• Recognize that drugs in liquid form are absorbed faster


than those in solid form
• Assess for signs and symptoms of drug toxicity when
giving two drugs that are highly protein bound
• Identify side effects of drugs that are nonspecific
• Check peak levels and trough levels of drugs that have
a narrow therapeutic range
NURSING IMPLICATIONS

• Advise client not to eat fatty foods before ingesting


enteric-coated tablet
• Check the drug literature for the protein-binding
percentage of the drug
• Report to health care provider if drugs with a long half-
life are given more than once a day

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