MIDTERM TOPICS

PHARMACOLOGY

Challenges to effective drug therapy

 Changes in Health Care in the 21st Century

o Access to medical and pharmacological information is available from many sources.

o Consumers are taking steps to demand specific treatments and considerations.

o Alternative therapies are being offered and advertised.

o Financial pressures are leading to early discharge.

o Patient teaching and home care provisions are vital.

 Federal Guidelines - Drug Advertising

o When the advertisement states the indication, it must also include:

1. Contraindications

2. Adverse effects

3. Precautions

 Consumer awareness: Internet Sources for Drug Information

o Pharmaceutical company information sites

o Chat rooms with other people who are taking the drug

o Online pharmacies

o Lists of government regulations

o Research reports about the drug and its effectiveness

 Internet Site Evaluation

o Address Identification (.com, edu, gov, net, org)

o Navigation- Is the site easy to access and navigate or confusing?

o Contributor- Who prepared the site and what are his or her qualifications? Is it

reviewed, or is it purely commercial?

o Dates- Is the site updated frequently?

o Accuracy/ Reliability- Is the information supported by other sites, accurate, and in

agreement with other sources you have reviewed? Are the other links listed?

 OTC Medications/Issue That Can Arise

 o Can mask the signs and symptoms of disease

o Can interact with prescription drugs

o Can be taken in greater than the recommended dose, leading to toxicity

 OTC Drugs

o Drugs that were “grandfathers in”

o Former prescription drugs that have been tested and found to be safe for use by the

general public is used as directed.

 Alternative Therapies and Herbal Medicine

o The active ingredient has not been tested by the FDA.

o Incidental ingredients are unknown

o Patients do not always mention these therapies to their health care providers

o Drug- alternative therapy interactions may occur

 Controls for Alternative Therapies

o Herbal medications of alternative therapies are not controlled or tested by the FDA.

o Advertisement for these drugs is not restricted because they are considered dietary

supplements.

o No regulation by any industry.

 Off- Label Medications

Definition

o The use of a drug for an indication not approved by the FDA.

Occurrence

o Commonly done for groups of patients for which there is little premarketing

testing.

o Used with pediatric and geriatric population

 Health Care in Crisis

o Skyrocketing cost of medical care and drugs

o Huge research and equipment requirements to meet consumer demands

o Rising cost of health insurance

o Earlier discharge from hospitals

  Cost Considerations

o HMO’s

o Home Care

o Other cost considerations:

1. Insurance coverage

2. Trade name vs. Generic

Chapter 7: Introduction to Cell Physiology

Chemotherapeutic Drugs #1

 Alter cellular function or disrupting cellular integrity, causing cell death

 Prevent cellular reproduction, eventually leading to cell death

Chemotherapeutic Drugs #2

 To destroy organisms that invade the body

o Bacteria, viruses, parasites, protozoa, fungi

 To destroy abnormal cells within the body

o Neoplasms or cancers

Chemotherapeutic Drugs #3

 May alter the cell membrane, causing the cell to rupture and die

 May deprive the cell of certain nutrients, altering the proteins that the cell produces and

interfering with normal cell functioning and cell division

 May affect the normal cells of patients to some extent as well.

Parts of Human Cell #1

 Nucleus

 Cell Membrane

 Cytoplasm
Parts of Human Cell #2

Components of Cell Membrane

 Cell membrane is made up of lipids and proteins

 Several lipids make up the cell membrane

o Phospholipids

o Glycolipids

o Cholesterol

 Lipid layer provides a barrier for the cell and maintains homeostasis of the cell
Cell Membrane #2

Receptor Sites

 Found on the cell membrane

 Specific receptor sites that allow interaction with various chemicals

Identifying Markers

 Surface antigens

 Important in the role of cellular immunity

 Histocompatibility proteins that allow for self-identification

 The body’s immune system recognizes these proteins and acts to protect self-cells and to

destroy non-self-cells.

Channels

 Channels or pores that allow for the passage of substances into and out of the cell

 Some drugs are designed to affect certain channels within the cell
Organelles of the Cytoplasm

 Mitochondria

 Endoplasmic Reticulum

 Free Ribosomes

 Golgi Apparatus

 Lysosomes

Cell Properties

Endocytosis

o Involves incorporation of material into the cell

o Pinocytosis and phagocytosis occur

Exocytosis

o Removing substances from a cell to pushing them through the cell membrane and secrete

the substance outside the cell

o Hormones, neurotransmitters, and enzymes are excreted into the body by this process

Homeostasis of the Cell

Passive Transport

o Happens without the expenditure of energy and can occur across any semi-permeable

membrane

o Occurs by diffusion, osmosis, and facilitated diffusion

Active Transport

o Energy-requiring process

o Movement of particular substances against a concentration gradient

o Important in maintaining cell homeostasis

Passive Transport

Diffusion

o Does not require energy

 o The movement of solutes from a region of high concentration to a region of lower

concentration across a concentration gradient

Osmosis

o Does not require energy

o Movement of water from an area low in solutes to an area high in solutes

Phases of the Cell Cycle

G0 Phase

o Resting phase

G1 Phase

o Gathering phase

S Phase

o Synthesizing phase

G2 Phase

o Last substances needed for division are collected and produced

M Phase

o Actual cell division occurs, producing two identical daughter cells

Cell Physiology
Chapter 8: Anti-infective Agents

Development of Anti-Infective Therapy

1920s

o Paul Ehrlich worked on developing a synthetic chemical effective only against infection-

causing cells

o Scientists discovered penicillin in a mold sample

1935

 The sulfonamides were introduced

Therapeutic Action #1

 Interfere with biosynthesis of the bacterial cell wall

 Prevent the cells of the invading organism from using substances essential to their growth

and development

 Interfere with steps involved in protein synthesis

Therapeutic Action #2

 Interfere with DNA synthesis

 Alter the permeability of the cell membrane to allow essential cellular components to

leak out

Drug Therapy Across the Lifespan

Anti-Infective Activity

 Anti-infectives vary in their effectiveness against invading organisms.

 Some are selective – only effective for a few numbers of organisms

 Bactericidal – kill the cell

 Bacteriostatic – prevent reproduction of the cell

Narrow Spectrum vs. Broad Spectrum

Narrow Spectrum of Activity

 Effective against only a few microorganisms with a very specific metabolic pathway or

enzyme

Broad Spectrum of Activity

 Useful in treating a wide variety of infections

Therapeutic action of Anti-Infective Agents

Human Immune Response

 Goal of anti-infective therapy is reduction of the population of the invading organism.

 Drugs that would eliminate all traces of any invading pathogen might be toxic to the host

as well.

 Immune response is a complex process involving chemical mediators, leukocytes,

lymphocytes, antibodies, and locally released enzymes and chemicals.

Resistance

 Natural or acquired: Ability over time to adapt to an anti-infective drug and produce cells

that are no longer affected by a particular drug.

 Anti- infectives act on specific enzyme system or biological process, many

microorganisms that do not act on this system are not affected by this particular drug

Acquired Resistance

 Microorganisms that were once sensitive to the particular drug have begun to develop

acquired resistance.

 This results in serious clinical problems.

Ways Anti-Infective Agents Resistance Develops

 Producing an enzyme that deactivates the antimicrobial drug

 Changing cellular permeability to prevent the drug from entering the cell

 Altering transport systems to exclude the drug from active transport into the cell

 Altering binding sites on the membranes or ribosomes, which then no longer accept the

drug

 Producing a chemical that acts as an antagonist to the drug

Preventing Resistance

 Limit the use of antimicrobial agents to the treatment of specific pathogens sensitive to

the drug being used

 Make sure doses are high enough, and the duration of drug therapy long enough

 Be cautious about the indiscriminate use of anti-infectives

Factors Affecting Prescribing Anti-Infective Agents

  Identification of the correct pathogen

 Selection of the right drug

- One that causes the least complications for that particular patient

 One that is most effective against the pathogen involved

Problems With Treating Infections in Immunosuppressed Patients

 Anti-infective drugs cannot totally eliminate the pathogen without causing severe

toxicity in the host.

 These patients do not have the immune response in place to deal with even a few

invading organisms.

Identification of the Pathogen

 Identification of the infecting pathogen is done by culture

 A culture of a tissue sample from the infected area is done

- A swab of infected tissue is allowed to grow on an agar plate

- Staining techniques and microscopic examination identify the bacterium

 Stool can be examined for ova and parasites

Sensitivity of Pathogen

 Shows which drugs are capable of controlling the particular microorganism

 Is important with microorganisms that have known resistant strains

 Along with a culture, identifies the pathogen and appropriate drug for treatment

Combination Therapy

 Use of a smaller dosage of each drug

 Some drugs are synergistic

 In infections caused by more than one organism, each pathogen may react to a different

anti-infective agent

 Sometimes, the combined effects of the different drugs delay the emergence of resistant

strains

Prophylaxis of Anti-Infective Agents

 People traveling to an area where malaria is endemic

  Patients who are undergoing GI or genitourinary surgery

 Patients with known cardiac valve disease, valve replacements, and other conditions

requiring invasive procedures

Adverse Reactions to Anti-Infective Therapy

 Kidney Damage

 Gastrointestinal (GI) Tract Toxicity

 Neurotoxicity

 Hypersensitivity Reactions

 Superinfections

Chapter 9: Antibiotics

Antibiotics

 Antibiotics are defined as:

- Chemicals that inhibit specific bacteria

- Made in three ways

1. By living microorganisms

2. By synthetic manufacture

3. Through genetic engineering

Signs of Infection

 Fever

 Lethargy

 Slow-wave sleep induction

 Classic signs of inflammation (redness, swelling, heat, and pain)

Antibiotic Use Across the Life Span

 Pediatric Population

 Adult Population

 Geriatric Population

 (See box 9.1)

Types of Antibiotics

 Bacteriostatic

- Those substances that prevent the growth of bacteria

 Bactericidal

- Those that kill bacteria directly

Bacteria and antibiotics

 Gram positive/negative

 Aerobic

 Anaerobic

Goal of Antibiotic Therapy

 Decrease the population of the invading bacteria to a point where the human immune

system can effectively deal with the invader

Selecting Treatment

 Identification of the causative organism

 Based on the culture report, an antibiotic is chosen that has been known to be effective at

treating the invading organism

Bacteria Classification

 Gram-positive

The cell wall retains a stain or resists decolorization with alcohol

 Gram-negative

The cell wall loses a stain or is decolorized by alcohol

  Aerobic

Depend on oxygen for survival

 Anaerobic

Do not use oxygen

Bacteria and Resistance to Antibiotics

 Adapt to their environment

 The longer an antibiotic has been in use, the greater the chance that the bacteria will

develop into a resistant strain

Aminoglycosides #1

 A group of powerful antibiotics used to treat serious infections caused by gram-negative

aerobic bacilli

 Common medications:

- Amikacin (Amikin), Gentamicin (Garamycin)

- Kanamycin (Kantrex)

- Neomycin (Mycifradin)

- Streptomycin

- Tobramycin (Nebcin, Tobrex)

Aminoglycosides #2

 Bactericidal

 Indications:

- Treatment of serious infections caused by susceptible bacteria

 Actions:

- Inhibits protein synthesis in susceptible strains of gram-negative bacteria causing cell

death

Aminoglycosides #3

Pharmacokinetics
  Poorly absorbed from the GI tract, but rapidly absorbed after IM injection, reaching peak

levels within 1 hour

 Widely distributed throughout the body, crossing the placenta and entering breast milk

 Excreted unchanged in the urine and have an average half-life of 2 to 3 hours

 Depend on the kidney for excretion and are toxic to the kidney

Aminoglycosides #4

Contraindications-

- Known allergies, renal or hepatic disease, hearing loss

Adverse Effects-

- Ototoxicity and nephrotoxicity are the most significant

Drug-to-Drug Interactions-

- Diuretics, neuromuscular blockers, succinylcholine, or citrate anticoagulated blood

Nursing Considerations for Patients Receiving Aminoglycosides

Assess:

 For possible contraindications or cautions: allergy to any aminoglycoside

 Perform a physical assessment

 Perform culture and sensitivity tests at the site of infection

 Conduct orientation and reflex assessment

 Assess vital signs

 Perform renal and liver function tests

Prototype Summary: Gentamicin

Carbapenems #1

New class of broad-spectrum antibiotics effective against gram-positive and gram-negative

bacteria

Common medications:

- Doripenem (Doribax)

- Ertapenem (Invanz)

- Imipenem– Cilastatin (Primaxin)

- Meropenem (Merrem IV).

Carbapenems #2

Bactericidal

Indications-

- Treatment of serious infections caused by susceptible bacteria

Actions: Inhibit cell membrane synthesis in susceptible bacteria, leading to cell death
Carbapenems #3

Pharmacokinetics

- These drugs are rapidly absorbed if given IM and reach peak levels at the end of the

infusion if given IV.

- They are widely distributed throughout the body, although it is not known whether

they cross the placenta or enter breastmilk

- Excreted unchanged in the urine and have an average half-life of 1 to 4 hours

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