Anti-Infectives: Tetracyclines and Sulfonamides
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Questions and Answers

Which mechanism primarily explains the lethality induced by natural penicillins?

  • Inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit.
  • Interference with the synthesis of peptidoglycans by binding to penicillin-binding proteins (PBPs), causing cell lysis. (correct)
  • Direct inhibition of bacterial DNA replication, leading to apoptosis.
  • Disruption of the bacterial cell membrane, causing leakage of cellular contents.

What is the primary mechanism of action (MOA) of Trimethoprim-Sulfamethoxazole (Bactrim)?

  • Interfering with bacterial DNA replication.
  • Inhibiting bacterial protein synthesis by binding to the 50S ribosomal subunit.
  • Disrupting the bacterial cell membrane.
  • Competitively inhibiting dihydropteroate synthase, which blocks folic acid synthesis. (correct)

A patient presents with a suspected bacterial infection. Which scenario would make Trimethoprim-Sulfamethoxazole (Bactrim) a less favorable choice compared to other antibiotics?

  • The infection is identified as Klebsiella pneumoniae.
  • The infection is identified as Haemophilus ducreyi.
  • The infection is identified as Streptococcus pneumoniae. (correct)
  • The infection is identified as methicillin-susceptible Staphylococcus aureus (MSSA).

Which antiviral agent would be most appropriate for a patient diagnosed with herpes zoster (shingles)?

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

A patient with a known penicillin allergy requires treatment for a bacterial infection. Which class of antibiotics would be the safest and most effective alternative, assuming resistance patterns do not dictate otherwise?

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

A patient is prescribed doxycycline. Which of the following instructions should the healthcare provider emphasize to ensure optimal therapeutic outcomes and minimize potential adverse effects?

<p>Avoid prolonged exposure to sunlight due to increased risk of photosensitivity. (A)</p> Signup and view all the answers

Which statement regarding the pharmacokinetics of penicillins is most accurate?

<p>Penicillins have a wide distribution in the body, high concentrations in tissues and fluids, and are rapidly eliminated renally. (C)</p> Signup and view all the answers

A patient is diagnosed with a localized herpes simplex virus (HSV) infection on the lip. Which topical antiviral medication is most appropriate for this condition?

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

Why is combination therapy with cell wall-active agents beneficial when administering Glecaprevir?

<p>It broadens the antimicrobial spectrum, enhances bacterial killing, and reduces resistance development. (D)</p> Signup and view all the answers

Which of the following mechanisms describes how Pibrentasvir inhibits viral replication?

<p>By acting as a next-generation NS5A inhibitor with pangenotypic antiviral activity. (C)</p> Signup and view all the answers

A patient undergoing treatment with an unspecified medication develops symptoms indicative of histamine-like effects shortly after drug administration. Which medication is most likely responsible?

<p>An unspecified medication administered intravenously. (C)</p> Signup and view all the answers

A pregnant patient requires treatment for a severe fungal infection. Considering the black box warnings, which antifungal medication should be avoided due to the risk of fetal hearing loss?

<p>Griseofulvin (Gris-PEG, Grifulvin V) (B)</p> Signup and view all the answers

What is the primary mechanism of action (MOA) of Griseofulvin in treating fungal infections?

<p>Binding to fungal microtubular proteins, disrupting microtubule assembly during metaphase. (B)</p> Signup and view all the answers

A researcher is investigating resistance mechanisms to Pibrentasvir in Hepatitis C virus (HCV). What aspect of resistance patterns should the researcher expect?

<p>Resistance patterns vary according to both bacterial strain and HCV genotype. (D)</p> Signup and view all the answers

A patient is prescribed Pibrentasvir for treatment-naive, noncirrhotic HCV. Which genotypes can this medication treat and what is the typical treatment duration?

<p>HCV genotypes 1-6; an 8-week course. (B)</p> Signup and view all the answers

A patient taking Nifurtimox reports experiencing nausea and myalgia. Which of the following is the MOST appropriate initial course of action?

<p>Continue Nifurtimox, as nausea and myalgia are common side effects that usually subside with continued use. (B)</p> Signup and view all the answers

A 7-year-old child is diagnosed with American Trypanosomiasis (Chagas Disease). Which of the following medications is FDA-approved for treating this condition in this age group?

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

A patient with a known G6PD deficiency is prescribed Nifurtimox. Which of the following potential adverse effects should the healthcare provider monitor for MOST closely?

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

Which mechanism of action (MOA) is associated with Fosfomycin's antibacterial activity in treating UTIs?

<p>Inhibition of MurA, impairing bacterial cell wall synthesis (D)</p> Signup and view all the answers

A patient is prescribed a medication that causes their urine to turn orange-brown. Which of the following medications is MOST likely responsible for this side effect?

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

A patient develops acute pneumonitis and pulmonary fibrosis during treatment. Which of the following medications, is MOST likely the cause?

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

Which mechanism explains the development of resistance to Amantadine in influenza A virus?

<p>Mutations in the RNA sequence encoding the M2 protein (D)</p> Signup and view all the answers

A patient is scheduled to start Benznidazole for treatment. What laboratory monitoring is MOST crucial to conduct regularly during the first few weeks of therapy?

<p>CBC every 2-3 weeks (C)</p> Signup and view all the answers

Which of the following statements accurately describes a key difference between Nifurtimox and Benznidazole?

<p>Benznidazole is FDA-approved for use in pediatric patients, while Nifurtimox is not. (D)</p> Signup and view all the answers

Why is Amantadine no longer widely used for influenza A treatment?

<p>Widespread resistance limits clinical use. (D)</p> Signup and view all the answers

Which characteristic of benznidazole presents the greatest challenge in maintaining consistent therapeutic drug levels in a patient with variable fluid intake?

<p>Its rapid absorption rate. (C)</p> Signup and view all the answers

A patient develops severe nephrotoxicity and ototoxicity after prolonged treatment with an aminoglycoside. What mechanism most likely underlies these adverse effects?

<p>Direct cytotoxic effect on renal tubular cells and cochlear hair cells due to high drug accumulation. (D)</p> Signup and view all the answers

A patient is prescribed clindamycin for a skin infection. Which statement best explains the rationale for its effectiveness against a broad spectrum of bacteria?

<p>Clindamycin's mechanism involves binding to the 50S ribosomal subunit, suppressing protein synthesis in both aerobic and anaerobic bacteria. (C)</p> Signup and view all the answers

Why is combination therapy often recommended when using Amphotericin B to treat systemic fungal infections?

<p>To minimize the adverse effects associated with high doses of Amphotericin B. (D)</p> Signup and view all the answers

Which of the following is the most critical consideration when selecting a Hep C medication regimen, such as sofosbuvir-velpatasvir, for a patient with advanced cirrhosis?

<p>The potential for drug-drug interactions and the impact on liver function. (D)</p> Signup and view all the answers

A researcher is investigating a new antifungal agent that disrupts fungal cell membranes. Which of the following mechanisms of action would most likely produce this effect?

<p>Interference with ergosterol synthesis or binding. (D)</p> Signup and view all the answers

Why is it important to closely monitor renal function in patients receiving aminoglycosides?

<p>To detect and prevent nephrotoxicity, a common adverse effect of aminoglycosides. (C)</p> Signup and view all the answers

A patient taking benznidazole reports experiencing persistent peripheral neuropathy. What is the most appropriate course of action?

<p>Discontinue benznidazole treatment and consider an alternative therapy due to the severity of the adverse effect. (A)</p> Signup and view all the answers

A patient undergoing treatment for Hepatitis C with interferon-cytokine develops severe depression. What is the most appropriate course of action?

<p>Reduce the dose of interferon-cytokine, initiate antidepressant therapy, and provide psychiatric support. (C)</p> Signup and view all the answers

A patient has a fungal infection resistant to fluconazole. Which medication would be the MOST appropriate to consider next?

<p>Amphotericin B (Fungizone). (A)</p> Signup and view all the answers

Why is clindamycin generally avoided for treating most upper respiratory tract infections?

<p>Because it alters normal gut flora, increasing the risk of <em>Clostridium difficile</em> infection without providing a clear benefit in typical upper respiratory infections. (D)</p> Signup and view all the answers

A patient with decompensated cirrhosis (Child-Pugh B/C) and chronic Hepatitis C (HCV) requires treatment. Which therapeutic regimen is most appropriate?

<p>12 weeks of Sofosbuvir-Velpatasvir in combination with Ribavirin. (D)</p> Signup and view all the answers

Which of the following statements best explains the mechanism of action of Sofosbuvir?

<p>It is a prodrug that, once metabolized, competes with uridine triphosphate for incorporation into HCV RNA by the NS5B polymerase, thus inhibiting viral replication. (A)</p> Signup and view all the answers

Why is it critical to avoid overdosing when administering Colistimethate?

<p>Overdosing causes fatal cardiac or cardiopulmonary arrest. (B)</p> Signup and view all the answers

Which adverse effect is most associated with clindamycin use, necessitating careful monitoring and consideration of alternative treatments?

<p>Pseudomembranous colitis caused by <em>Clostridium difficile</em> overgrowth. (D)</p> Signup and view all the answers

A patient is diagnosed with visceral leishmaniasis. Which of the following medications is most appropriate for treating this parasitic infection?

<p>Paromomycin, to address the parasitic protozoa. (C)</p> Signup and view all the answers

Why are third-generation cephalosporins generally favored over clindamycin for treating meningitis, except in specific cases?

<p>Clindamycin poorly penetrates the blood-brain barrier, limiting its efficacy against most causative agents of meningitis unlike third-generation cephalosporins. (D)</p> Signup and view all the answers

What is the rationale for using a combination of antibiotics, such as clindamycin, in treating bacterial endocarditis caused by Gram-positive organisms?

<p>To leverage synergistic effects that enhance the clinical response, particularly against resistant strains. (A)</p> Signup and view all the answers

What is a unique pharmacokinetic property of clindamycin that influences its distribution and elimination?

<p>It undergoes metabolism to N-demethylclindamycin and clindamycin sulfoxide, with excretion in both urine and bile. (D)</p> Signup and view all the answers

A patient receiving intravenous Colistimethate begins to exhibit fever, chills, tachypnea and stridor. What is the most appropriate immediate intervention?

<p>Administer meperidine to shorten and manage the infusion-related reaction. (B)</p> Signup and view all the answers

Flashcards

Bacteriostatic

Drugs that inhibit bacterial growth but do not kill bacteria.

Trimethoprim-Sulfamethoxazole (Bactrim)

A broad-spectrum bacteriostatic antibiotic, often a second-line drug of choice.

MOA of Sulfonamides

Competitively inhibits dihydropteroate synthase, blocking folic acid synthesis in bacteria.

MOA of Penicillin

Inhibition of penicillin-binding proteins. (PBPs)

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Natural Penicillins Activity

Active against aerobic, gram-positive organisms.

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Doxycycline Uses

A tetracycline antibiotic used for atypical pneumonia and malaria prophylaxis.

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Valacyclovir (Valtrex)

Converted to acyclovir for better VZV effectiveness.

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Famciclovir (Famvir)

HSV-1, HSV-2, VZV, EBV, Hepatitis B

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Nifurtimox MOA

Bacteriostatic; activated by enzymatic reduction, damages bacterial DNA.

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Benznidazole MOA

Trypanocidal effects through mitochondrial nitroreductase activation; nitro free radicals damage cellular DNA.

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Nifurtimox & Benznidazole Use

American Trypanosomiasis (Chagas Disease).

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Nifurtimox Side Effect

Orange/brown urine

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Serious Nifurtimox/Benznidazole SE

Liver injury, peripheral neuropathy, interstitial pneumonitis with progressive fibrosis, hemolytic anemia with G6PD deficiency.

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Benznidazole Toxicity

Urticarial dermatitis, bone marrow suppression.

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Fosfomycin MOA

Inhibits MurA which impairs bacterial cell wall synthesis.

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Fosfomycin Use

Prevention and treatment of UTI

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Fosfomycin Effective Against

E. coli and Enterococcus.

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Fosfomycin Ineffective Against

Pseudomonas & Acinetobacter

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Glecaprevir (GLE)

Inhibits HCV polyprotein cleavage.

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Pibrentasvir (PIB)

Next-generation NS5A inhibitor with pangenotypic antiviral activity.

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Therapeutic Drug Monitoring (TDM)

Optimizes efficacy and minimizes toxicity of drugs.

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Cell wall-active agents MOA

Disrupts cell wall synthesis, causing cell lysis.

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Black box warning of aminoglycosides

Avoid use in pregnant individuals due to the risk of fetal hearing loss.

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Resistance to echinocandins

Develops due to mutations in FKS1 & FKS2 (glucan synthase regions).

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Griseofulvin (Gris-PEG, Grifulvin V) MOA

Binds to fungal microtubular proteins and inhibits microtubule assembly.

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Benznidazole

Used to treat Chagas disease; side effects include GI distress, vaginitis, headache, and dizziness.

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Aminoglycosides

A class of antibiotics that inhibit bacterial protein synthesis by binding to the 30S ribosomal subunit.

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Aminoglycosides MOA

Bactericidal inhibitors of protein synthesis; disrupt initiation complexes → misreading mRNA.

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Lincosamides

A class of antibiotics that bind to the 50S ribosomal subunit to suppress bacterial protein synthesis.

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Common Lincosamides

Clindamycin and Lincomycin

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Atypical Antifungals

A class of medications used to treat fungal infections.

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Amphotericin B MOA

Binds to ergosterol in fungal cell membranes, forming pores.

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Hep C Medications

A medication class used to treat Hepatitis C viral infections.

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Epclusa

Sofosbuvir-Velpatasvir

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Interferons

A drug class and Cytokine.

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Sofosbuvir-Velpatasvir MOA

Inhibits HCV RNA replication by acting as a uridine analog and competing with uridine triphosphate for incorporation into the RNA by the NS5B polymerase.

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Sofosbuvir-Velpatasvir Use

Fixed-dose combination (400mg/100mg) FDA approved for chronic Hepatitis C (HCV) genotypes 1-6.

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Sofosbuvir (Sovaldi) MOA

A nucleotide analog inhibitor of hepatitis C virus NS5B polymerase—the key enzyme mediating HCV RNA replication.

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Leishmaniasis

Parasitic disease (Leishmania parasites) spread by sand flies. Can cause skin sores or affect spleen, liver, bone marrow.

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Pseudomembranous Colitis

Mild to life-threatening condition caused by an overgrowth of CDIFF.

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Amphotericin B infusion-related rx

Treat with meperidine to shorten reaction. Decrease reactions with tylenol, ibuprofen, or IV hydrocortisone

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Clindamycin Precautions

Avoid in non-bacterial infections, such as most upper respiratory tract infections. Alters normal gut flora, allowing CDIFF overgrowth.

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Clindamycin Adverse Effects

Reversible elevation of liver enzymes. Granulocytopenia, thrombocytopenia. Neuromuscular - potentiates blocking agents

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Aminoglycosides Treatment

Reserved for resistant cases of UTI; Gentamicin for lower UTI. Rarely used for meningitis

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Aminoglycosides Treatment

UTI: reserved for resistant cases; Gentamicin for lower UTI. Meningitis: rarely used (3rd-gen cephalosporins preferred), except for resistant gram (-) & listeria

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Study Notes

  • Infectious drugs serve as treatments for various infections, including bacterial, viral, and helminth infections
  • Classes include Tetracyclines, Sulfonamides, Beta-Lactam Antibiotics, Nucleoside Analogues, Fluoroquinolones and Glycopeptides

Tetracyclines

  • Effective against a wide range of bacteria, including gram-positive, gram-negative, and atypical organisms
  • Includes "-cycline" medications such as Demeclocycline, Tetracycline, Minocycline, and Doxycycline
  • Works by binding to the 30S bacterial ribosome subunit, inhibiting protein synthesis
  • Used as a second-line choice for broad-spectrum bacteriostatic
  • Effective against pneumonia, malaria prophylaxis, acne, and certain infections
  • Bind to fetal bone and teeth, are contraindicated for use during pregnancy (Category D)
  • Chelate formation with calcium, antacids, and minerals will absorption
  • Can reduce the effectiveness of oral contraceptives and potentiate warfarin

Sulfonamides

  • Disrupt DNA by inhibiting folic acid synthesis in susceptible bacteria
  • Sulfamethoxazole or Trimethoprim-Sulfamethoxazole (Bactrim) are common medications
  • Competitively inhibits dihydropteroate synthase, blocking folic acid synthesis
  • Works against some gram-positive and gram-negative bacteria, as well as parasites
  • Resistance is common, especially in strains of E. coli
  • Absorption occurs in the small intestine, with metabolism occurring in the liver
  • Avoid during pregnancy due to potential for neural tube defects from disrupted folic acid synthesis
  • Photosensitivty can occur, SJS is possible adverse effect, Stevens-Johnson syndrome and vasculitis may occur
  • Interactions with anticoagulants, sulfonylurea hypoglycemic agents, and hydantoin anticonvulsants

Beta-Lactam Antibiotics

  • Penicillins and Cephalosporins make up beta-Lactam antibiotics
  • Common medications include PCN, cephalosporins, carbapenems, and monobactams
  • Act by inhibiting the last step in peptidoglycan synthesis, inhibiting cell wall synthesis
  • Natural PCNs are effective against aerobic, gram-positive organisms
  • Penicillins have a wide distribution in the body, with high concentrations in tissues and fluids
  • Rapid renal elimination results in short half-lives
  • Considerations include allergy testing since the adverse effecst include IgE mediated reactions can also be a cross-hypersensitivity with cephalosporins

Nucleoside Analogues

  • Common medications include acyclovir, valacyclovir, famciclovir, penciclovir, ganciclovir, and valganciclovir
  • Inhibit viral DNA synthesis and replication, requiring either entry blockage or activation inside cells
  • Safe during pregnancy

Fluoroquinolones

  • Common medications include "-floxacin"
  • Generational classes have varying coverage
  • Generations 2 target Weak gram (+), Gram (-), Pseudomonas
  • Target bacterial DNA gyrase and topoisomerase IV essential for DNA replication
  • Can cause tendonitis and tendon rupture

Glycopeptides

  • Active against gram-positive bacteria, including MRSA, PCN-resistant strep & ampicillin-resistant enterococci; ineffective against Gram (-) bacteria & mycobacteria
  • Inhibit bacterial cell wall synthesis in gram-positive bacteria
  • Tissue irritation can occur, ototoxicity, and Red Man Syndrome can be adverse effects

Azole Antifungals

  • Inhibit 14-a-sterol demethylase, impairing ergosterol biosynthesis
  • Leads to growth arrest and increased cellular permeability
  • Can cause Hepatotoxicity

Helminth Infections

  • Includes Benzimidazoles (Albendazole and Mebendazole), Ivermectin, Moxidectin, Praziquantel
  • Albendazole and Mebendazole cause an inhibition of B-microtubule polymerization resulting in mitochondrial impairment
  • Ivermectin increase permeability of the cell membrane to chloride ions leading to paralysis and death of parasite

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Description

Explore tetracyclines and sulfonamides, key anti-infective drugs that combat bacterial, viral, and helminth infections. Learn about tetracyclines' broad-spectrum bacteriostatic action, contraindications, and interactions. Understand how sulfonamides disrupt DNA by inhibiting folic acid synthesis.

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