Pharmacology of Cephalosporins and Drug Action

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Questions and Answers

Which generation of cephalosporins is typically reserved for use after consultation with an infectious disease specialist?

  • First
  • Fifth
  • Fourth (correct)
  • Second

A patient requires antibiotic prophylaxis prior to surgery. Which cephalosporin generation is most suitable, according to the text?

  • First (correct)
  • Second
  • Fourth
  • Third

Which of the following best describes a key characteristic of third-generation cephalosporins?

  • Ineffective in the cerebrospinal fluid (CSF)
  • Limited activity against Gram-negative bacteria
  • Effective against methicillin-resistant *Staphylococcus aureus* (MRSA)
  • Increased activity against Gram-negative bacteria (correct)

Which cephalosporin generation should be considered for treating Pseudomonas aeruginosa?

<p>Fourth (B)</p> Signup and view all the answers

Which generation of cephalosporins is effective against infections caused by MRSA?

<p>Fifth (B)</p> Signup and view all the answers

What determines the maximal response a drug can elicit?

<p>The drug's efficacy (C)</p> Signup and view all the answers

If Drug A requires a higher dosage than Drug B to achieve the same effect, which statement is accurate?

<p>Drug B is more potent than Drug A. (D)</p> Signup and view all the answers

A drug that mimics the actions of endogenous norepinephrine will likely have what effect on cardiac output?

<p>Increase cardiac output by activating norepinephrine receptors (C)</p> Signup and view all the answers

Which of the following qualities is typically considered less important when selecting a drug?

<p>Potency (B)</p> Signup and view all the answers

What is the MOST probable outcome if you keep administering more of a drug to a patient?

<p>The response will become progressively larger (D)</p> Signup and view all the answers

What is the most common fungal pathogen causing Otomycosis?

<p><em>Aspergillus</em> (D)</p> Signup and view all the answers

Which of the following is a potential consequence of Necrotizing Otitis Externa (NOE) due to its invasive nature?

<p>Damage to cranial nerves IX, X, and XI (B)</p> Signup and view all the answers

A patient presents with intense pruritus, erythema, and suspected Otomycosis. If acidifying drops are ineffective, what is the recommended next step in management?

<p>Apply 1% clotrimazole. (C)</p> Signup and view all the answers

Which of the following is a potential symptom in the presentation of Necrotizing Otitis Externa (NOE)?

<p>Mastoid tenderness (Griesinger sign) (C)</p> Signup and view all the answers

What is the possible outcome if Necrotizing Otitis Externa erodes through the bone?

<p>Meningitis (D)</p> Signup and view all the answers

Which of the following beta-lactamase inhibitors can be combined with ampicillin to extend its antimicrobial spectrum?

<p>Sulbactam (D)</p> Signup and view all the answers

A patient is prescribed ticarcillin for a severe infection. Which potential adverse effect should the nurse monitor for, especially in patients receiving high doses?

<p>Sodium overload (C)</p> Signup and view all the answers

Which of the following organisms are antipseudomonal penicillins like piperacillin effective against, in addition to those susceptible to aminopenicillins?

<p>Pseudomonas aeruginosa (A)</p> Signup and view all the answers

Which route of administration is appropriate for Penicillin G?

<p>IM (D)</p> Signup and view all the answers

A patient is prescribed amoxicillin/clavulanate. Which route of administration should the nurse use?

<p>PO (A)</p> Signup and view all the answers

What is the primary mechanism of excretion for penicillins?

<p>Active tubular excretion (A)</p> Signup and view all the answers

Which of the following penicillinase-resistant penicillins is typically administered intravenously?

<p>Nafcillin (D)</p> Signup and view all the answers

A patient develops a rash after starting amoxicillin. What is the most appropriate initial action?

<p>Discontinue the amoxicillin and notify the healthcare provider (B)</p> Signup and view all the answers

What is the primary focus of Phase IV drug studies?

<p>Observing the drug's effects in a large population after it has been released for general use. (A)</p> Signup and view all the answers

According to the recommendations, when should new drugs be adopted?

<p>After carefully balancing potential benefits against inherent risks and doing due diligence. (A)</p> Signup and view all the answers

Which of the following is the LEAST likely reason that new drugs generally present greater risks than older ones?

<p>New drugs always have more side effects than old drugs. (A)</p> Signup and view all the answers

Which of the following drug names is typically used on national board exams?

<p>Generic name (D)</p> Signup and view all the answers

What is a potential problem associated with using trade names when prescribing medications?

<p>The same drug can have multiple trade names, leading to confusion. (B)</p> Signup and view all the answers

What is bioavailability in the context of drugs?

<p>The rate and extent to which the active ingredient or therapeutic moiety is absorbed from a drug product and becomes available at the site of action. (B)</p> Signup and view all the answers

A drug classified as a 'diuretic' would fall under which type of classification?

<p>Therapeutic (B)</p> Signup and view all the answers

Selective Serotonin Reuptake Inhibitors (SSRIs) are a classification of drugs grouped by the chemical structure/mechanism of action. What is this classification?

<p>Pharmacologic (C)</p> Signup and view all the answers

What is the primary mechanism by which aztreonam inhibits bacterial growth?

<p>Inhibition of cell wall production (C)</p> Signup and view all the answers

Which adverse effect is associated with rapid intravenous administration of vancomycin?

<p>Vancomycin Flushing Syndrome (VCS) (D)</p> Signup and view all the answers

A patient with a known penicillin allergy requires treatment for a Gram-negative bacterial infection. Which of the following antibiotics would be the safest choice?

<p>Aztreonam (D)</p> Signup and view all the answers

Which of the following organisms is least likely to be effectively treated with aztreonam?

<p><em>Staphylococcus aureus</em> (B)</p> Signup and view all the answers

A patient receiving vancomycin develops hearing loss. Which of the following factors would increase the likelihood that this adverse effect is due to the vancomycin?

<p>Concurrent administration of an aminoglycoside antibiotic (B)</p> Signup and view all the answers

Which route of administration allows aztreonam to be used to treat pulmonary infections caused by Pseudomonas aeruginosa?

<p>Inhalation (A)</p> Signup and view all the answers

A patient on vancomycin therapy develops thrombocytopenia. What is the underlying mechanism for this adverse effect?

<p>Platelets binding to vancomycin, leading to their removal (B)</p> Signup and view all the answers

In which scenario related to Acute Otitis Media (AOM) would antibacterial drugs be recommended?

<p>AOM in an infant &lt; 6 months old (B)</p> Signup and view all the answers

Flashcards

Phase IV Drug Trial

The phase of drug development where a new drug is released for general use and its effects are observed in a large population.

Exercise Discretion

A strategy that involves neither being the first to adopt a new idea nor the last to abandon an old one. It promotes making informed choices by balancing potential benefits and inherent risks.

Generic Name

The official name of a drug that is standardized and used across healthcare professionals and national exams.

Trade Name

The name given to a drug by its manufacturer for marketing purposes. It is usually a brand name.

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Bioavailability

The extent to which a drug is absorbed into the bloodstream and becomes available to the body. It can vary even among drugs with the same generic name.

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Therapeutic Classification

Classifying drugs based on what they treat. For example, drugs for high blood pressure or drugs for depression.

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Pharmacologic Classification

Classifying drugs based on their chemical structure or mechanism of action. For example, calcium channel blockers or selective serotonin reuptake inhibitors (SSRIs).

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Diuretics

A drug group that reduces the volume of plasma in the blood. They are often used to treat conditions like high blood pressure.

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Efficacy

The maximum effect a drug can produce, regardless of the dose.

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Potency

The amount of drug needed to produce a specific effect.

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Dose-Response Relationship

As the dose increases, the response also increases, but eventually plateaus.

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Potent Drug

A drug that produces the desired effect at a lower dose compared to another drug.

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Effective Drug

A drug that produces a stronger effect compared to another drug, even at the same dose.

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What are penicillinase-resistant penicillins?

Penicillinase-resistant penicillins are a type of penicillin that are not broken down by the enzyme penicillinase. This allows them to be effective against bacteria that produce penicillinase, which can make other penicillins ineffective.

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What are broad-spectrum penicillins?

Broad-spectrum penicillins are a type of penicillin that are effective against a wide range of bacteria. They work against both Gram-positive and Gram-negative bacteria.

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What are antipseudomonal penicillins?

Antipseudomonal penicillins are a type of penicillin that are specifically effective against the bacterium Pseudomonas aeruginosa, as well as other bacteria like Enterobacter, Proteus, Bacteroides fragilis, and Klebsiella.

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What are beta-lactamase inhibitors?

Beta-lactamase inhibitors are drugs that are used in combination with penicillinase-sensitive penicillins to prevent the breakdown of penicillin by the enzyme penicillinase. This allows the penicillin to be more effective.

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How is Penicillin G administered?

Penicillin G is administered via intramuscular (IM) or intravenous (IV) injection because it gets broken down in the acidic environment of the stomach.

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What side effect can occur with large doses of ticarcillin?

Large doses of ticarcillin can lead to sodium overload due to the high sodium content in the drug.

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How are penicillins eliminated from the body?

Penicillins are primarily eliminated from the body through active tubular excretion in the kidneys, with a smaller amount being filtered by the glomeruli.

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How do cephalosporins work?

Cephalosporins are a class of antibiotics that work by inhibiting the synthesis of peptidoglycans, which are essential components of bacterial cell walls. This weakens the cell wall and ultimately leads to bacterial death.

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First Generation Cephalosporins: Targets

First-generation cephalosporins effectively target gram-positive bacteria, including staphylococci (excluding MRSA) and non-enterococcal streptococci. They are commonly used as prophylaxis for surgical site wound infections.

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Second Generation Cephalosporins: Effectiveness

Second-generation cephalosporins demonstrate slight activity against gram-negative bacteria but are generally not the preferred choice for treating gram-negative infections.

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Third Generation Cephalosporins: Key Features

Third-generation cephalosporins exhibit increased resistance to beta-lactamase, a bacterial enzyme that inactivates many antibiotics. They possess enhanced activity against gram-negative bacteria, making them suitable for treating serious infections.

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Fourth Generation Cephalosporins: Properties

Fourth-generation cephalosporins exhibit a broad spectrum of activity, particularly against Pseudomonas aeruginosa. These cephalosporins are highly effective in treating infections that affect the central nervous system.

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Fifth Generation Cephalosporins: Unique Property

Fifth-generation cephalosporins are unique in their ability to target methicillin-resistant Staphylococcus aureus (MRSA). This makes them crucial for infections caused by MRSA, which are often difficult to treat.

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Necrotizing Otitis Externa (NOE)

A severe infection of the outer ear canal that can spread to the surrounding bones and even the brain, potentially leading to life-threatening complications.

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Griesinger Sign

A common symptom of NOE characterized by pain and tenderness over the mastoid bone behind the ear.

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Lateral Sinus Thrombosis

A potentially fatal complication of NOE, where a blood clot forms in the large vein near the brain.

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Fungal Otitis Externa (Otomycosis)

An infection of the outer ear canal caused by fungi, typically Aspergillus or Candida, leading to intense itching, redness, and potentially hearing loss.

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Acidifying Drops

A common treatment for fungal otitis externa that helps to create an acidic environment unfavorable for fungal growth, often used alongside thorough cleaning.

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Aztreonam

An antibiotic that inhibits cell wall synthesis. It is not a beta-lactam, so it can be safely administered to patients with penicillin allergies.

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Vancomycin Flushing Syndrome

Rapidly infused vancomycin can cause a severe reaction with flushing, hypotension, rash, and other symptoms.

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Vancomycin

A type of antibiotic that is commonly used to treat serious bacterial infections.

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Drug Excretion

The process by which the body eliminates a drug.

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Vancomycin Ototoxicity

A serious adverse effect of vancomycin that can damage the inner ear and cause hearing loss.

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Thrombophlebitis (Vancomycin)

A serious adverse effect of vancomycin that can cause blood clots in the veins.

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Immune-mediated thrombocytopenia (Vancomycin)

A serious side effect of vancomycin that can cause a decrease in the number of platelets in the blood.

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Drug Efficacy

The ability of a drug to produce the desired effect.

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Study Notes

Introduction to Pharmacology

  • Pharmacology is the study of drugs and their interactions with living systems.
  • Includes the study of drug effects in humans (clinical pharmacology).
  • Therapeutics (pharmacotherapeutics) involves using drugs for diagnoses, prevention or treatment of diseases.

The Therapeutic Objective

  • Drug therapy aims to provide maximal benefit with minimum harm.
  • Requires knowledge, skill, and judgment.
  • The goal is to provide greater good than harm, a key principle in pharmacology.

Ideal Drug Properties

  • Effectiveness: The most important feature of any drug.
  • Safety: No drug is truly safe; all have potential side effects.
  • Selectivity: No drug is entirely selective; all have potential side effects.

Drug Properties

  • Reversible Action: The drug's effects should be reversed when no longer needed, allowing for the body to return to normal function.
  • Predictability: The drug's effects should be consistent and reliable.
  • Ease of Administration: The drug should be easy to take (PO, IV, IM, etc.).
  • Freedom from Drug Interactions: It should not interact negatively with other drugs or foods, etc. to optimize the efficacy of the drug.
  • Low Cost: The drug should be affordable to enhance access to treatment.
  • Chemical Stability: The drug must keep its effectiveness over time.
  • Simple Generic Names: Using easily memorable generic names enhances communication among healthcare providers.

Adverse Drug Reactions

  • Idiosyncratic effect: An uncommon response due to genetic predisposition
  • Paradoxical effect: Opposite of intended effect
  • Physical dependence: Body adjusts to drug exposure.
  • Iatrogenic disease: Disease caused by treatment given.

Drug-Drug Interactions (Kinetics)

  • Intensification of effects: Combination of drugs produces a greater overall effect.
  • Reduction of effects: Combination of drugs produces a reduced overall effect.

Drug-Drug Interactions (Dynamics)

  • Addition/Potentiation: The combined effect is the sum of the individual drug effects.
  • Synergism: Combined effect is greater than the sum of individual drug effects.
  • Inhibition: One drug antagonizes the effect of another.

Factors That Determine the Intensity of Drug Responses

  • Administration: How the drug is given (oral, IV, IM, etc.).
  • Pharmacokinetics: What the body does to the drug (absorption, distribution, metabolism, excretion).
  • Pharmacodynamics: What the drug does to the body (drug-receptor interaction).
  • Individual Variations: Genetics, health conditions, age, etc.

Stages of New Drug Development

  • Preclinical testing (animals): Toxicity, pharmacokinetics.
  • Clinical testing (humans): Phases I, II, III, and IV.
  • Phase IV: Post-marketing surveillance.

Drug Naming Conventions

  • Drugs have chemical names, generic names, and trade names.
  • Generic names are the official names that are used on national board exams.

Ways to Classify Drugs

  • Therapeutic classification: Grouped by what they treat (e.g., hypertension, depression).
  • Pharmacologic classification: Grouped based on chemical actions.

Controlled Substances

  • Schedule I: High potential for abuse, no accepted medical use (e.g., heroin).
  • Schedule II: High potential for abuse, accepted medical use (e.g., morphine).
  • Schedule III: Moderate potential for abuse, accepted medical use (e.g., codeine).
  • Schedule IV: Low potential for abuse, accepted medical use (e.g., diazepam).
  • Schedule V: Lowest potential for abuse, accepted medical use (e.g., some cough syrups).

Drug Absorption, Distribution, Metabolism, and Excretion (ADME)

  • Absorption: Transfer of a drug from site of administration into the bloodstream.
  • Distribution: Movement of the drug from the bloodstream to the tissues and organs
  • Metabolism: Conversion of a drug into a more or less active compound.
  • Excretion: Removal of a drug from the body.

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