Antimicrobial Drugs and Selection Process
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Antimicrobial drugs have the ability to injure or kill an invading microorganism without harming the cells of the __________.

host

Selection of the most appropriate antimicrobial agent requires knowing the organism’s __________.

identity

A rapid assessment of the nature of the pathogen can sometimes be made on the basis of the __________ stain.

Gram

Patients require __________ therapy when immediate treatment is necessary.

<p>empiric</p> Signup and view all the answers

Identifying the __________ of the infection is essential to choosing the correct antimicrobial agent.

<p>site</p> Signup and view all the answers

Characterizing the organism is central to the selection of the proper __________.

<p>drug</p> Signup and view all the answers

It is generally necessary to __________ the infective organism for a conclusive diagnosis.

<p>culture</p> Signup and view all the answers

Factors such as patient __________ and cost of therapy are important in the selection of an antimicrobial agent.

<p>factors</p> Signup and view all the answers

Some β-lactam antibiotics can enter the ______.

<p>CSF</p> Signup and view all the answers

A compound with a ______ molecular weight has an enhanced ability to cross the blood–brain barrier.

<p>low</p> Signup and view all the answers

Compounds with a high molecular weight penetrate poorly, even in the presence of ______ inflammation.

<p>meningeal</p> Signup and view all the answers

A high degree of ______ binding of a drug restricts its entry into the CSF.

<p>protein</p> Signup and view all the answers

The amount of ______ drug in serum is important for CSF penetration.

<p>free</p> Signup and view all the answers

Multidrug-resistant organisms (MDROs) have developed resistance to multiple classes of ______.

<p>antibiotics</p> Signup and view all the answers

Elimination of infecting organisms from the body depends on an intact ______ system.

<p>immune</p> Signup and view all the answers

Poor ______ function may cause accumulation of certain antibiotics.

<p>kidney</p> Signup and view all the answers

Serum creatinine levels are used as an index of ______ function for adjustment of drug regimens.

<p>renal</p> Signup and view all the answers

Direct monitoring of serum levels is preferred for identifying ______ toxicities.

<p>potential</p> Signup and view all the answers

Certain combinations of antibiotics show ______, meaning the combination is more effective than either of the drugs used separately.

<p>synergism</p> Signup and view all the answers

Drug A activity 30% + Drug B activity 20% = ______ for the addition effect.

<p>50%</p> Signup and view all the answers

Drug A activity 30% + Drug B activity 20% = ______ for the synergistic effect.

<p>80%</p> Signup and view all the answers

A bacteriostatic agent may interfere with the action of a ______ agent.

<p>bactericidal</p> Signup and view all the answers

Most gram-negative organisms are inherently resistant to ______.

<p>vancomycin</p> Signup and view all the answers

Acquired antibiotic resistance often involves the gain or alteration of bacterial ______ information.

<p>genetic</p> Signup and view all the answers

Resistance can develop from DNA undergoing spontaneous ______ or through movement between organisms.

<p>mutation</p> Signup and view all the answers

Other antimicrobial agents, such as ______, have less specificity and are reserved for life-threatening infections.

<p>chloramphenicol</p> Signup and view all the answers

The choice of therapy usually centers on the site of infection, severity of the illness, and ______ to take oral medications.

<p>ability</p> Signup and view all the answers

Treatment of methicillin-resistant ______ aureus (MRSA) generally includes drugs like vancomycin and linezolid.

<p>Staphylococcus</p> Signup and view all the answers

Parenteral administration is used for drugs that are poorly absorbed from the ______ tract.

<p>gastrointestinal</p> Signup and view all the answers

Rational dosing of antimicrobial agents is based on their pharmacodynamics and ______ properties.

<p>pharmacokinetic</p> Signup and view all the answers

Three important properties that influence the frequency of dosing are concentration dependent killing, time-dependent killing, and ______ effect.

<p>post antibiotic</p> Signup and view all the answers

The oral route of administration is appropriate for ______ infections that can be treated on an outpatient basis.

<p>mild</p> Signup and view all the answers

Some antibiotics, such as ______ and aminoglycosides, are poorly absorbed from the gastrointestinal tract.

<p>vancomycin</p> Signup and view all the answers

The cost of therapy can vary widely among drugs that show similar ______ in treating an infection.

<p>efficacy</p> Signup and view all the answers

Safety is related not only to the inherent nature of the drug but also to ______ factors that can predispose to toxicity.

<p>patient</p> Signup and view all the answers

Certain antimicrobial agents, including aminoglycosides and daptomycin, show a significant increase in the rate of bacterial killing as the concentration of antibiotic increases from 4- to 64-fold the ______ of the drug for the infecting organism.

<p>MIC</p> Signup and view all the answers

In contrast, β-lactams, glycopeptides, macrolides, clindamycin, and linezolid do not exhibit ______-dependent killing.

<p>concentration</p> Signup and view all the answers

The clinical efficacy of these antimicrobials is best predicted by the percentage of time that blood concentrations of a drug remain above the ______.

<p>MIC</p> Signup and view all the answers

The PAE is a persistent suppression of microbial growth that occurs after levels of antibiotic have fallen below the ______.

<p>MIC</p> Signup and view all the answers

Antimicrobial drugs exhibiting a long PAE often require only one dose per day, particularly against ______ negative bacteria.

<p>gram</p> Signup and view all the answers

Chemotherapeutic agents acting only on a single or a limited group of microorganisms are said to have a ______ spectrum.

<p>narrow</p> Signup and view all the answers

Extended spectrum is the term applied to antibiotics that are modified to be effective against gram-positive organisms and also against a significant number of ______ negative bacteria.

<p>gram</p> Signup and view all the answers

Drugs such as tetracycline, fluoroquinolones, and carbapenems affect a wide variety of microbial species and are referred to as ______-spectrum antibiotics.

<p>broad</p> Signup and view all the answers

It is therapeutically advisable to treat patients with a single agent that is most specific to the ______ organism.

<p>infecting</p> Signup and view all the answers

This strategy reduces the possibility of ______ infections.

<p>super</p> Signup and view all the answers

Flashcards

Antimicrobial drugs

Drugs that combat infections by targeting invading microbes without harming human cells.

Selective Toxicity

The ability of a drug to harm a microorganism while leaving human cells unharmed.

Antimicrobial agent selection

Choosing the best drug to treat an infection, considering several factors.

Organism's identity

Identifying the specific microbe causing the infection.

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Organism's susceptibility

Determining if a microbe is vulnerable to a particular drug.

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Site of infection

Location of the infection in the body.

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Patient Factors

Characteristics of the patient that impact drug choice (e.g., allergies, health).

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Empiric therapy

Administering an antimicrobial drug before the specific microbe is identified (immediate treatment).

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Drug Combinations in Treatment

Combining antimicrobial drugs can sometimes improve treatment effectiveness, especially for complex diseases like tuberculosis.

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Synergistic Drug Effect

When two drugs together produce a better outcome than either drug alone.

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Bacteriostatic Drugs

Drugs that stop bacterial growth but don't kill them.

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Bactericidal Drugs

Drugs that kill bacteria.

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Drug Resistance (bacteria)

Bacteria's ability to survive even when exposed to maximum levels of an antibiotic.

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Inherent Drug Resistance

Some bacteria are naturally resistant to certain antibiotics.

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Acquired Drug Resistance

Bacteria develop resistance to antibiotics through changes in their genetic material.

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CSF penetration

The ability of a drug to enter the cerebrospinal fluid (CSF).

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Molecular weight and BBB

Lower molecular weight drugs cross the blood-brain barrier (BBB) more easily than higher molecular weight drugs.

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High protein binding

Drugs with high protein binding have reduced ability to enter the CSF because they are mostly attached to proteins in the blood.

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Multidrug Resistant Organisms (MDROs)

Microorganisms that are resistant to multiple antibiotics.

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Immune system and infections

A healthy immune system is crucial in fighting infections; compromised immune systems may require higher antibiotic doses.

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Renal dysfunction and antibiotics

Poor kidney function can lead to antibiotic buildup, so dosage adjustments are necessary.

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Serum creatinine levels

Used to assess kidney function and adjust antibiotic dosages.

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Antibiotic selection

Choosing the right antibiotic depends on patient factors, such as the immune system and kidney function.

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Bactericidal agents

Antibiotics that kill bacteria.

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Dosage Adjustments

Adjusting antibiotic dose based on the patient's kidney function and overall health.

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Antimicrobial agent toxicity

Some antimicrobial drugs can be harmful if administered to certain patients.

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MRSA treatment options

Different drugs (vancomycin, clindamycin, daptomycin, or linezolid) are used to treat methicillin-resistant Staphylococcus aureus infections.

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Cost of antimicrobial therapy

Different drugs for the same infection can have different prices.

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Oral administration of antibiotics

Mild infections appropriately treated outside of hospital.

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Intravenous antibiotics

Used for hospitalized patients with serious infections

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Poorly absorbed antibiotics

Some antibiotics do not effectively enter the bloodstream through the gut.

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Pharmacodynamics

How drug concentrations affect the infection-fighting ability of the drugs.

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Pharmacokinetics

Describes the way the body processes drugs (absorption, distribution, metabolism, and elimination).

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Concentration-dependent killing

The effectiveness of some antibiotics depends on their high blood levels.

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Time-dependent killing

Some antibiotics are most effective when continuously present in the blood at a sufficient level.

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Post-antibiotic effect (PAE)

Continued suppression of bacterial growth after the antibiotic concentration falls below the minimum inhibitory concentration (MIC).

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Narrow-spectrum antibiotic

An antibiotic effective against only a limited group of microorganisms.

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Extended-spectrum antibiotic

An antibiotic effective against both Gram-positive and Gram-negative bacteria.

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Broad-spectrum antibiotic

An antibiotic effective against a wide variety of microbial species.

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Aminoglycosides

Antibiotics exhibiting concentration-dependent killing and a long post-antibiotic effect.

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Beta-lactams

Antibiotics that exhibit time-dependent killing.

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Single-drug therapy

Treatment with a specific antibiotic effective against the infecting microorganism.

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Minimizing toxicity

Using the fewest possible antibiotics to limit side effects.

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Study Notes

Antimicrobial Drugs

  • Antimicrobial drugs work by selectively targeting invading microorganisms without harming host cells.
  • Antimicrobial drugs are effective because of their selective toxicity.
  • They can injure or kill invading microorganisms.

Selection of Antimicrobial Agents

  • Choosing the right antimicrobial agent depends on the organism's identity, its susceptibility to different agents, the site of the infection, patient factors, safety, and cost.
  • Identifying the infecting organism is crucial for selecting the appropriate drug.
  • Rapid assessment can sometimes be made based on a Gram stain, but culture and susceptibility testing are often necessary for definitive diagnosis
  • Empiric therapy may be needed immediately for critically ill patients before the infecting organism or its susceptibility is identified.

Bacteriostatic versus Bactericidal Drugs

  • Bacteriostatic drugs inhibit the growth and replication of bacteria, allowing the immune system to eliminate them.
  • Bactericidal drugs kill the bacteria at the achievable serum levels within the patient.
  • Bactericidal agents are usually the drugs of choice in seriously ill or immunocompromised patients.

Minimum Inhibitory Concentration (MIC)

  • MIC is the lowest concentration of an antimicrobial agent that prevents visible growth of an organism after 24 hours.
  • It is used to evaluate the susceptibility of microorganisms to antimicrobials in vitro.
  • MIC helps in choosing the appropriate antibiotic therapy.

Minimum Bactericidal Concentration (MBC)

  • MBC is the lowest concentration of an antimicrobial agent that results in a 99.9% decline in colony counts after overnight broth dilution incubations.
  • MBC determines the minimum amount of drug needed to effectively kill most of the bacteria.

Effect of Site of Infection on Therapy: The Blood-Brain Barrier

  • Adequate antibiotic levels at the infection site are crucial for effective treatment.
  • Factors such as lipid solubility, molecular weight, and protein binding influence the penetration of antimicrobials into various tissues, including the central nervous system (CNS).

Patient Factors

  • Patient factors, such as immune system status, kidney function, liver function, age, and pregnancy, influence antimicrobial selection and dosing.
  • Chronic conditions like alcoholism and diabetes can compromise the immune response.
  • Age, kidney, and liver function can affect drug metabolism, necessitating dosage adjustments.

Safety of the Agent

  • Certain antibiotics, like penicillin, have low toxicity and are effective for diverse infections.
  • Others, like chloramphenicol, are more toxic and should be reserved for life-threatening conditions.
  • Safety considerations must encompass both the drug's inherent toxicity and patient-specific factors.

Cost of Therapy

  • Antimicrobial drug costs vary significantly based on several factors including the agent and the duration of the course.

Route of Administration

  • Oral administration is suitable for mild infections treated as outpatients..
  • Intravenous administration is initially used in hospitalized patients, but oral treatment can often be used afterward if possible.
  • Certain antibiotics are poorly absorbed from the GI tract, necessitating parenteral administration

Determining Rational Dosing

  • Rational antibiotic dosing is influenced by the relationship between drug concentrations and antimicrobial effect, and drug pharmacokinetics (absorption, distribution, metabolism, and elimination).
  • Factors to consider:
    • Concentration-dependent killing – higher concentrations are more effective
    • Time-dependent killing – maintaining above a specific concentration for extended durations is key
    • Post-antibiotic effect – some drugs continue suppressing growth even after concentration falls below the MIC

Prophylactic Use of Antibiotics

  • Prophylactic use of antibiotics is necessary in certain situations (surgical procedures, dental work).
  • Prophylaxis should be carefully calculated to prevent resistance.

Complications of Antimicrobial Therapy

  • Some drugs cause hypersensitivity (allergic reactions).
  • Some produce direct toxicity unrelated to antimicrobial activity.

Superinfections

  • Broad-spectrum antibiotics can disrupt the normal flora, leading to an overgrowth of other microorganisms.
  • This can cause superinfections, sometimes needing additional treatments.

Combinations of Antimicrobial Drugs

  • Often, a combination of antimicrobials is more efficient than a singular agent
  • Combinations, especially in severe cases, can reduce infection time and limit the development of antibiotic resistance.
  • Some combinations interfere with each other's mechanisms.

Drug Resistance

  • Bacteria can develop resistance, reducing the effectiveness of antibiotics.
  • Resistance arises from genetic changes within the bacterial organisms; these can appear naturally or be acquired.

Narrow, Extended, and Broad-Spectrum Antibiotics

  • Narrow-spectrum antimicrobials combat a limited group of microorganisms.
  • Extended-spectrum antimicrobials target a wider range, encompassing gram-positive and diverse gram-negative bacteria.
  • Broad-spectrum antimicrobials target a wide variety of bacterial types, but overuse can contribute to antimicrobial resistance.

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Description

This quiz covers the fundamental concepts of antimicrobial drugs, including their selective toxicity and the criteria for selecting appropriate agents. It highlights the importance of identifying the infecting organism and discusses the differences between bacteriostatic and bactericidal drugs. Test your knowledge on these critical aspects of antimicrobial therapy.

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