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Questions and Answers
Cephalosporins are known for their high rate of cross-reactivity in penicillin-allergic patients.
Cephalosporins are known for their high rate of cross-reactivity in penicillin-allergic patients.
False
β-lactamase inhibitors are used to enhance the efficacy of penicillin antibiotics by preventing β-lactam ring destruction.
β-lactamase inhibitors are used to enhance the efficacy of penicillin antibiotics by preventing β-lactam ring destruction.
True
Cilastatin is added to imipenem to prevent its inactivation in renal tubules.
Cilastatin is added to imipenem to prevent its inactivation in renal tubules.
True
Carbapenems have a narrow spectrum of activity and are used primarily for minor infections.
Carbapenems have a narrow spectrum of activity and are used primarily for minor infections.
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All cephalosporins effectively cover Pseudomonas aeruginosa.
All cephalosporins effectively cover Pseudomonas aeruginosa.
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Cephalosporins can cover organisms like MRSA and Enterococcus faecalis, unlike earlier generations.
Cephalosporins can cover organisms like MRSA and Enterococcus faecalis, unlike earlier generations.
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Hypersensitivity reactions are a common side effect of β-lactam antibiotics.
Hypersensitivity reactions are a common side effect of β-lactam antibiotics.
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Imipenem is susceptible to breakdown by β-lactamases, which limits its effectiveness.
Imipenem is susceptible to breakdown by β-lactamases, which limits its effectiveness.
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Aminoglycosides are bacteriostatic agents.
Aminoglycosides are bacteriostatic agents.
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Tetracyclines can cause discoloration of teeth in children.
Tetracyclines can cause discoloration of teeth in children.
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Aminoglycosides are ineffective against anaerobes due to their requirement for oxygen.
Aminoglycosides are ineffective against anaerobes due to their requirement for oxygen.
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Chloramphenicol is a 30S inhibitor.
Chloramphenicol is a 30S inhibitor.
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Tigecycline is effective against multidrug-resistant organisms.
Tigecycline is effective against multidrug-resistant organisms.
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Doxycycline should be taken with milk to enhance absorption.
Doxycycline should be taken with milk to enhance absorption.
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Gentamicin is an example of a tetracycline.
Gentamicin is an example of a tetracycline.
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Ototoxicity is a side effect associated with aminoglycosides.
Ototoxicity is a side effect associated with aminoglycosides.
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Chloramphenicol is a bactericidal antibiotic.
Chloramphenicol is a bactericidal antibiotic.
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Clindamycin is used for treating anaerobic infections above the diaphragm.
Clindamycin is used for treating anaerobic infections above the diaphragm.
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Linezolid is primarily effective against Gram-negative organisms.
Linezolid is primarily effective against Gram-negative organisms.
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Macrolides use a mechanism of action that involves blocking translocation at the 50S ribosomal subunit.
Macrolides use a mechanism of action that involves blocking translocation at the 50S ribosomal subunit.
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All side effects of Clindamycin are dose dependent.
All side effects of Clindamycin are dose dependent.
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Chloramphenicol is commonly used due to its high cost and low toxicity.
Chloramphenicol is commonly used due to its high cost and low toxicity.
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Aplastic anemia associated with Chloramphenicol is dose dependent.
Aplastic anemia associated with Chloramphenicol is dose dependent.
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Peripheral neuropathy can occur as a side effect of Linezolid.
Peripheral neuropathy can occur as a side effect of Linezolid.
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Trimethoprim is primarily used in the treatment of Pneumocystis jirovecii pneumonia.
Trimethoprim is primarily used in the treatment of Pneumocystis jirovecii pneumonia.
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Dihydropteroate synthase is an enzyme that is crucial for human DNA replication.
Dihydropteroate synthase is an enzyme that is crucial for human DNA replication.
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Fluoroquinolones remain effective when taken with dairy products.
Fluoroquinolones remain effective when taken with dairy products.
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High doses of Trimethoprim may lead to hyperkalemia due to its mechanism of action.
High doses of Trimethoprim may lead to hyperkalemia due to its mechanism of action.
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Fluoroquinolones can be used safely during pregnancy without any concerns.
Fluoroquinolones can be used safely during pregnancy without any concerns.
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Agranulocytosis is a known side effect of Trimethoprim.
Agranulocytosis is a known side effect of Trimethoprim.
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Combination therapy of trimethoprim and sulfonamides is effective for treating urinary tract infections.
Combination therapy of trimethoprim and sulfonamides is effective for treating urinary tract infections.
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Leukopenia is not associated with the side effects of high doses of Trimethoprim.
Leukopenia is not associated with the side effects of high doses of Trimethoprim.
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Rifamycin inhibits DNA-Dependent RNA Polymerase, decreasing mRNA synthesis.
Rifamycin inhibits DNA-Dependent RNA Polymerase, decreasing mRNA synthesis.
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Rifampin resistance arises due to mutations in the gene encoding mycolic acid.
Rifampin resistance arises due to mutations in the gene encoding mycolic acid.
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Isoniazid inhibits mycolic acid synthesis, which is essential for the mycobacterial cell wall.
Isoniazid inhibits mycolic acid synthesis, which is essential for the mycobacterial cell wall.
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Ethambutol inhibits arabinosyltransferase, increasing cell wall synthesis.
Ethambutol inhibits arabinosyltransferase, increasing cell wall synthesis.
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Rifabutin is preferred over rifampin in HIV patients due to its increased CYP450 induction.
Rifabutin is preferred over rifampin in HIV patients due to its increased CYP450 induction.
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Isoniazid can lead to drug-induced lupus if overdosed.
Isoniazid can lead to drug-induced lupus if overdosed.
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Pyrazinamide works best at a neutral pH level.
Pyrazinamide works best at a neutral pH level.
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The side effect of ethambutol includes optic neuropathy, characterized by red-green color blindness.
The side effect of ethambutol includes optic neuropathy, characterized by red-green color blindness.
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Cephalosporins are mainly effective against Pseudomonas aeruginosa.
Cephalosporins are mainly effective against Pseudomonas aeruginosa.
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β-lactamase inhibitors are enzymes that enhance the action of β-lactam antibiotics.
β-lactamase inhibitors are enzymes that enhance the action of β-lactam antibiotics.
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Cefepime is known for high rates of nephrotoxicity, particularly when used with aminoglycosides.
Cefepime is known for high rates of nephrotoxicity, particularly when used with aminoglycosides.
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Imipenem requires cilastatin to prevent its inactivation by renal dehydropeptidase I.
Imipenem requires cilastatin to prevent its inactivation by renal dehydropeptidase I.
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Carbapenems are restricted to use in non-life-threatening infections due to their broad spectrum.
Carbapenems are restricted to use in non-life-threatening infections due to their broad spectrum.
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The mechanism of action for carbapenems involves binding to lipid A in bacterial membranes.
The mechanism of action for carbapenems involves binding to lipid A in bacterial membranes.
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Nephrotoxicity is a potential side effect of polymyxins.
Nephrotoxicity is a potential side effect of polymyxins.
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A common side effect of β-lactam antibiotics includes autoimmune hemolytic anemia.
A common side effect of β-lactam antibiotics includes autoimmune hemolytic anemia.
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Dapsone is a sulfonamide and shares the same mechanism of action with sulfonamides.
Dapsone is a sulfonamide and shares the same mechanism of action with sulfonamides.
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Sulfonamides inhibit bacterial replication by targeting dihydropteroate synthase.
Sulfonamides inhibit bacterial replication by targeting dihydropteroate synthase.
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Cefotaxime is an example of a first-generation cephalosporin.
Cefotaxime is an example of a first-generation cephalosporin.
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Clarithromycin and erythromycin can enhance the serum concentration of theophylline.
Clarithromycin and erythromycin can enhance the serum concentration of theophylline.
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Colistin is also known as polymyxin B.
Colistin is also known as polymyxin B.
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Hypersensitivity reactions are the only side effect associated with sulfonamides.
Hypersensitivity reactions are the only side effect associated with sulfonamides.
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Neurotoxicity can occur as a side effect of dapsone.
Neurotoxicity can occur as a side effect of dapsone.
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Stevens-Johnson syndrome is a rare but serious side effect of sulfonamides.
Stevens-Johnson syndrome is a rare but serious side effect of sulfonamides.
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Aminoglycosides are effective against anaerobes due to their bactericidal nature.
Aminoglycosides are effective against anaerobes due to their bactericidal nature.
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Tetracyclines are primarily effective against Gram-negative organisms due to their mechanism of action.
Tetracyclines are primarily effective against Gram-negative organisms due to their mechanism of action.
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Ototoxicity is a known side effect associated with the use of aminoglycosides.
Ototoxicity is a known side effect associated with the use of aminoglycosides.
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Doxycycline can be used safely in patients with renal failure.
Doxycycline can be used safely in patients with renal failure.
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The mechanism of action of tigecycline involves binding to the 50S ribosomal subunit.
The mechanism of action of tigecycline involves binding to the 50S ribosomal subunit.
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Clindamycin is effective against anaerobic infections below the diaphragm.
Clindamycin is effective against anaerobic infections below the diaphragm.
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Tetracyclines should not be taken with milk due to the interference of calcium with drug absorption.
Tetracyclines should not be taken with milk due to the interference of calcium with drug absorption.
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Linezolid is mainly effective against Gram-positive organisms.
Linezolid is mainly effective against Gram-positive organisms.
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Chloramphenicol exerts its effect by inhibiting peptidyltransferase at the 30S ribosomal subunit.
Chloramphenicol exerts its effect by inhibiting peptidyltransferase at the 30S ribosomal subunit.
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Aplastic anemia associated with Chloramphenicol is dose dependent.
Aplastic anemia associated with Chloramphenicol is dose dependent.
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Clindamycin is effective against anaerobic infections below the diaphragm.
Clindamycin is effective against anaerobic infections below the diaphragm.
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Linezolid can cause peripheral neuropathy as a side effect.
Linezolid can cause peripheral neuropathy as a side effect.
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The primary mechanism of action of macrolides involves inhibiting protein synthesis by binding to the 50S ribosomal subunit.
The primary mechanism of action of macrolides involves inhibiting protein synthesis by binding to the 50S ribosomal subunit.
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Rickettsial diseases can be treated using Chloramphenicol.
Rickettsial diseases can be treated using Chloramphenicol.
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Myelosuppression is a side effect specifically related to clindamycin use.
Myelosuppression is a side effect specifically related to clindamycin use.
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Macrolides have a mechanism of resistance that involves methylation of the 23S rRNA-binding site.
Macrolides have a mechanism of resistance that involves methylation of the 23S rRNA-binding site.
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Ceftriaxone is used as an antimicrobial prophylaxis for exposure to meningococcal infection.
Ceftriaxone is used as an antimicrobial prophylaxis for exposure to meningococcal infection.
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Doxycycline is recommended for malaria prophylaxis in travelers.
Doxycycline is recommended for malaria prophylaxis in travelers.
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Amoxicillin is used to prevent gonococcal conjunctivitis in newborns.
Amoxicillin is used to prevent gonococcal conjunctivitis in newborns.
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Trimethoprim-sulfamethoxazole (TMP-SMX) is indicated for patients with a history of recurrent UTIs.
Trimethoprim-sulfamethoxazole (TMP-SMX) is indicated for patients with a history of recurrent UTIs.
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Benzathine penicillin G is recommended for the prophylaxis of strep pharyngitis in a child with a history of rheumatic fever.
Benzathine penicillin G is recommended for the prophylaxis of strep pharyngitis in a child with a history of rheumatic fever.
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Chloroquine is effective for malaria in areas with resistant species.
Chloroquine is effective for malaria in areas with resistant species.
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Gentamicin is classified as a 50S inhibitor.
Gentamicin is classified as a 50S inhibitor.
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Intrapartum penicillin G is administered to pregnant patients carrying group B strep to prevent neonatal infections.
Intrapartum penicillin G is administered to pregnant patients carrying group B strep to prevent neonatal infections.
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Study Notes
Cephalosporins (5th Generation)
- Inhibit bacterial cell wall synthesis, more resistant to penicillinases than earlier generations.
- Bactericidal effect, effective against broad gram-positive and gram-negative organisms.
- Treats infections caused by Listeria, atypical pathogens (Chlamydia, Mycoplasma), MRSA, and Enterococcus faecalis; does not cover Pseudomonas.
- Side effects include hypersensitivity reactions, autoimmune hemolytic anemia, disulfiram-like reactions, and vitamin K deficiency.
- Low cross-reactivity risk for penicillin-allergic patients; potential nephrotoxicity if used with aminoglycosides.
β-lactamase Inhibitors
- Added to penicillin antibiotics to prevent destruction by β-lactamase enzymes produced by some bacteria.
- Help maintain antibiotic efficacy against target bacteria by inhibiting the enzymes that render them ineffective.
- Examples include Clavulanic acid, Avibactam, Sulbactam, and Tazobactam.
Carbapenems
- Broad-spectrum antibiotics, resistant to β-lactamase.
- Binds to penicillin-binding proteins (PBPs) to inhibit bacterial cell wall synthesis.
- Always given with cilastatin to prevent renal inactivation of the drug.
- Effective against gram-positive cocci, gram-negative rods, and anaerobes; used for life-threatening infections when other options fail.
- Risks include significant adverse effects limiting their use.
Aminoglycosides
- Bactericidal antibiotics that irreversibly inhibit protein synthesis by binding to the 30S subunit.
- Mechanism includes misreading of mRNA and blocking translocation; effectiveness requires oxygen, thus not effective against anaerobes.
- Common usage for severe gram-negative rod infections and synergistic with β-lactam antibiotics.
- Notable examples include Gentamicin, Neomycin, Amikacin, Tobramycin, and Streptomycin.
- Side effects involve nephrotoxicity, ototoxicity (especially with loop diuretics), and neuromuscular blockade (caution in myasthenia gravis).
Tetracyclines
- Bacteriostatic antibiotics that prevent aminoacyl-tRNA attachment to the 30S ribosomal subunit.
- Limited penetration to the CNS; Doxycycline can be used in renal failure due to fecal elimination.
- Interaction with divalent cations (Ca²⁺, Mg²⁺) can hinder absorption in the gut.
- Effective against Borrelia burgdorferi, Mycoplasma, Rickettsia, and Chlamydia; also used for acne treatment.
- Side effects include GI distress, teeth discoloration in children, photosensitivity, and teratogenic effects.
Tigecycline
- Tetracycline derivative; bacteriostatic with broad-spectrum activity against anaerobic, gram-negative, and gram-positive bacteria, including multidrug-resistant organisms (MRSA, VRE).
- Side effects include nausea and vomiting.
Chloramphenicol
- Blocks peptidyltransferase at the 50S ribosomal subunit, acting bacteriostatically.
- Suggested uses include meningitis from Haemophilus influenzae, Neisseria meningitidis, and Rickettsial infections.
- Limited use in developed countries due to toxicity; notable side effects include dose-dependent anemia, dose-independent aplastic anemia, and gray baby syndrome in premature infants.
Clindamycin
- Bacteriostatic antibiotic that blocks peptide transfer at the 50S subunit.
- Effective for anaerobic infections (Bacteroides spp., Clostridium perfringens) particularly in aspiration pneumonia and lung abscesses; also treats invasive group A streptococcal infections.
- Side effects include pseudomembranous colitis (due to C. difficile overgrowth), fever, and diarrhea.
Linezolid
- Inhibits protein synthesis via binding to the 23S rRNA of the 50S subunit.
- Effective against gram-positive species, including MRSA and VRE.
- Side effects include myelosuppression (thrombocytopenia), peripheral neuropathy, and risk of serotonin syndrome.
Macrolides
- Bacteriostatic antibiotics that inhibit protein synthesis by blocking translocation on the 50S subunit.
- Mechanism of resistance includes methylation of the 23S rRNA-binding site to prevent drug binding.
- Effective against atypical pneumonia pathogens (Mycoplasma, Chlamydia, Legionella) and for treating STIs (Chlamydia).
- Side effects involve potential hemolysis in G6PD deficiency, methemoglobinemia, and agranulocytosis.
Trimethoprim
- Inhibits dihydropteroate synthase, disrupting folate synthesis and bacterial replication; bactericidal when combined with sulfonamides.
- Commonly used for urinary tract infections, Shigella, Salmonella infections, and Pneumocystis jirovecii prophylaxis.
- Side effects include hyperkalemia, megaloblastic anemia, leukopenia, and granulocytopenia.
Fluoroquinolones
- Bactericidal agents that inhibit topoisomerase II (DNA gyrase) and topoisomerase IV, critical for DNA replication.
- Oral absorption significantly reduced with concurrent use of divalent cations (e.g., dairy, antacids).
- Used for ear infections and a variety of gram-positive and gram-negative infections, including Pseudomonas aeruginosa.
- Side effects include GI upset, superinfections, skin rashes, tendonitis, or tendon rupture risks, and potential QT interval prolongation.
Rifamycin
- Inhibits DNA-dependent RNA polymerase, blocking mRNA synthesis.
- Resistance arises from mutations in the RNA polymerase gene.
- Rifabutin preferred in HIV patients due to less CYP450 induction.
- Uses include tuberculosis while noting minor hepatotoxicity and reddish discoloration of body fluids as a benign side effect.
Isoniazid
- Inhibits mycolic acid synthesis vital for mycobacterial cell walls.
- Requires conversion by the catalase-peroxidase enzyme for activation; resistance often due to mutations in the katG gene.
- Given with vitamin B6 to prevent peripheral neuropathy; risks include hepatotoxicity and drug interactions.
Pyrazinamide
- Works best at acidic pH; mechanism of action remains uncertain.
- Used primarily for tuberculosis treatment, with risks of hepatotoxicity and hyperuricemia.
Ethambutol
- Inhibits arabinosyltransferase leading to decreased cell wall synthesis.
- Used in tuberculosis treatment, associated side effects include optic neuropathy, leading to red-green color blindness.
Cephalosporins (5th Generation)
- β-lactam antibiotics that inhibit cell wall synthesis, more resistant to penicillinases.
- Mechanism: Bactericidal, primarily targeting penicillin-binding proteins.
- Broad coverage against gram-positive and gram-negative organisms, including Listeria and MRSA, but not Pseudomonas.
- Side effects: Hypersensitivity reactions, nephrotoxicity (with aminoglycosides), autoimmune hemolytic anemia, and vitamin K deficiency.
β-lactamase Inhibitors
- Protect β-lactam antibiotics from being inactivated by β-lactamases.
- Include agents such as clavulanic acid and tazobactam.
- Important for preserving the effectiveness of penicillins and cephalosporins against resistant bacteria.
Carbapenems
- Broad-spectrum antibiotics that are resistant to β-lactamases; bind to penicillin-binding proteins.
- Administered alongside cilastatin to prevent renal inactivation.
- Used for serious infections caused by gram-positive cocci, gram-negative rods, and anaerobes.
- Side effects: Nephrotoxicity, potential for seizures with imipenem.
Aminoglycosides
- Bactericidal drugs that irreversibly bind to the 30S ribosomal subunit, causing misreading of mRNA.
- Require oxygen for uptake; ineffective against anaerobes.
- Commonly used for severe gram-negative infections and synergistic with β-lactam antibiotics.
- Side effects: Nephrotoxicity, ototoxicity, and neuromuscular blockade.
Tetracyclines
- Bacteriostatic agents that bind to the 30S ribosomal subunit, preventing tRNA attachment.
- Effective against a variety of bacteria including Borrelia and Mycoplasma.
- Doxycycline is suitable for patients with renal failure and has fecal elimination.
- Side effects include gastrointestinal distress, photosensitivity, and potential effects on bone growth in children.
Tigecycline
- A derivative of tetracyclines with broad-spectrum activity against gram-positive, gram-negative, and anaerobic bacteria.
- Generally bacteriostatic; used against multidrug-resistant organisms.
- Side effects primarily include nausea and vomiting.
Chloramphenicol
- Inhibits bacterial protein synthesis by blocking peptidyltransferase at the 50S ribosomal subunit.
- Used for meningitis and rickettsial diseases despite toxicity.
- Side effects: Anemia, aplastic anemia, and gray baby syndrome in neonates.
Clindamycin
- Blocks peptide transfer at the 50S ribosomal subunit, rendering it bacteriostatic.
- Effective for anaerobic infections and invasive streptococcal infections.
- Side effects can include pseudomembranous colitis due to C. difficile overgrowth.
Linezolid
- Binds to the 50S ribosomal subunit, inhibiting protein synthesis.
- Effective against gram-positive species including MRSA and VRE.
- Side effects: Myelosuppression, peripheral neuropathy, and risk of serotonin syndrome.
Macrolides
- Inhibit protein synthesis by blocking translocation at the 50S ribosomal subunit.
- Treat atypical pneumonias and some gram-positive cocci infections.
- Side effects: Gastrointestinal motility issues and interactions with cytochrome P-450 substrates.
Polymyxins
- Disrupt the cell membrane integrity of gram-negative bacteria by binding to phospholipids.
- Used for multidrug-resistant infections and included in topical preparations.
- Side effects: Nephrotoxicity and neurotoxicity.
Sulfonamides
- Inhibit dihydropteroate synthase, leading to impaired folate synthesis and bacteriostatic action.
- Effective against a variety of gram-positive and gram-negative bacteria.
- Side effects include hypersensitivity reactions, hemolysis in G6PD deficiency, and potential for Stevens-Johnson syndrome.
Dapsone
- Functions similarly to sulfonamides but is a structurally distinct agent.
- Inhibits dihydropteroate synthase, leading to inhibition of bacterial replication.
Antimicrobial Prophylaxis
- Meningococcal exposure: Ceftriaxone, Ciprofloxacin, Rifampin.
- Infective endocarditis: Amoxicillin for at-risk patients.
- Recurrent UTIs: TMP-SMX.
- Malaria prophylaxis: Atovaquone-proguanil, Doxycycline among others.
- Group B strep in pregnancy: Intrapartum penicillin G or ampicillin.
- Gonococcal conjunctivitis prevention: Erythromycin ointment for newborns.
- Prevent postsurgical S. aureus infections: Cefazolin, possibly vancomycin if MRSA positive.
- Strep pharyngitis prophylaxis: Benzathine penicillin G or oral penicillin V.
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Description
This quiz covers 5th generation cephalosporins, β-lactamase inhibitors, and carbapenems. Learn about their mechanisms, effectiveness against various pathogens, side effects, and their role in treating resistant infections. Test your understanding of these vital antibiotic classes.