أسئلة الـ 16 فارما PPPM (قبل التعديل)

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Questions and Answers

Which generation of cephalosporins is generally considered to be more effective against Gram-positive bacteria, including methicillin-susceptible Staphylococcus aureus (MSSA)?

  • First Generation (correct)
  • Fourth Generation
  • Third Generation
  • Fifth Generation

A patient with a known penicillin allergy requires antibiotic treatment for a Streptococcus pneumoniae infection. Which cephalosporin would be LEAST appropriate, considering potential cross-reactivity?

  • Cefazolin (correct)
  • Ceftriaxone
  • Cefuroxime
  • Aztreonam

A patient develops a Pseudomonas aeruginosa infection. Which cephalosporin would be most appropriate to target this specific bacteria?

  • Ceftazidime (correct)
  • Cephalexin
  • Cefazolin
  • Cefuroxime

Why is ceftriaxone contraindicated for co-administration with calcium-containing solutions?

<p>Formation of insoluble ceftriaxone-calcium salt precipitates (B)</p> Signup and view all the answers

Which of the following adverse effects is specifically associated with imipenem, especially at high doses or in patients with central nervous system (CNS) lesions or renal insufficiency?

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

A patient is prescribed imipenem, but the prescriber also includes cilastatin in the treatment regimen. What is the purpose of adding cilastatin to imipenem therapy?

<p>To inhibit the metabolism of imipenem in the kidneys (C)</p> Signup and view all the answers

Which of the following best describes the spectrum of activity of aztreonam?

<p>Narrow-spectrum, primarily targeting Gram-negative bacteria (D)</p> Signup and view all the answers

A patient with a severe penicillin allergy requires treatment for a Gram-negative bacterial infection. Which of the following antibiotics would be MOST appropriate to use?

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

Vancomycin is indicated for the treatment of which of the following infections?

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

What is the key mechanism of action of vancomycin?

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

A patient receiving vancomycin intravenously develops a rash, flushing, and fever shortly after the infusion begins. What is the MOST likely cause of these symptoms?

<p>Red man syndrome (A)</p> Signup and view all the answers

How does the mechanism of action of cotrimoxazole (trimethoprim/sulfamethoxazole) lead to its antibacterial effects?

<p>By inhibiting folate metabolism (C)</p> Signup and view all the answers

Why is the use of sulfonamides avoided near term in pregnancy or in neonates?

<p>Increased risk of kernicterus (A)</p> Signup and view all the answers

Bacitracin is primarily used for:

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

Mupirocin is particularly effective against which bacteria:

<p><em>Streptococcus pyogenes</em> (A)</p> Signup and view all the answers

Which of the following cephalosporins is LEAST likely to be effective against Pseudomonas aeruginosa?

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

A patient is prescribed cefuroxime for a respiratory tract infection. Which of the following statements regarding cefuroxime is most accurate?

<p>It is a second-generation cephalosporin that can cross the blood-brain barrier. (C)</p> Signup and view all the answers

Which of the following statements regarding the use of cephalosporins in patients with penicillin allergies is MOST accurate?

<p>Patients with immediate hypersensitivity reactions to penicillin should never receive cephalosporins. (D)</p> Signup and view all the answers

What is the primary reason meropenem is considered to have a lower risk of seizures compared to imipenem?

<p>Meropenem is less likely to disrupt the balance of inhibitory neurotransmitters in the brain. (A)</p> Signup and view all the answers

Why is aztreonam a suitable option for patients with penicillin allergies?

<p>It has a monobactam structure that minimizes cross-reactivity with penicillin antibodies. (A)</p> Signup and view all the answers

Which of the following statements is MOST accurate regarding the administration of vancomycin?

<p>Vancomycin is primarily administered intravenously due to poor oral absorption. (A)</p> Signup and view all the answers

What is the most likely mechanism behind 'Red man syndrome,' a common adverse effect associated with rapid vancomycin infusion?

<p>Release of histamine from mast cells. (D)</p> Signup and view all the answers

What is the rationale for using trimethoprim in combination with sulfamethoxazole?

<p>To synergistically inhibit folate synthesis at two different steps. (D)</p> Signup and view all the answers

What is the primary mechanism by which sulfonamides can cause kernicterus in neonates?

<p>Sulfonamides compete with bilirubin for binding sites on albumin, increasing free bilirubin levels. (A)</p> Signup and view all the answers

Which of the following best describes the clinical use of bacitracin, considering its mechanism of action and potential toxicities?

<p>It is primarily used topically for minor skin and eye infections due to its toxicity if administered systemically. (C)</p> Signup and view all the answers

Mupirocin is commonly used to treat impetigo. What is the MOST likely mechanism of action that makes it effective for this condition?

<p>Inhibition of bacterial protein synthesis. (A)</p> Signup and view all the answers

A patient is diagnosed with a mixed aerobic and anaerobic intra-abdominal infection following surgery. Which of the following cephalosporins would offer the broadest spectrum of activity against both types of bacteria?

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

While most cephalosporins are renally excreted, which of the following is primarily eliminated via the biliary route, a consideration in patients with renal impairment?

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

A patient is prescribed cotrimoxazole. Which of the following findings indicates a potential adverse drug reaction that warrants immediate attention?

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

A patient with a history of renal insufficiency is prescribed an aminoglycoside antibiotic in conjunction with a cephalosporin. Which cephalosporin adverse effect should be MOST closely monitored?

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

Flashcards

Cephalosporins

Inhibits bacterial cell wall synthesis; similar to penicillin, many generations exist.

Carbapenems

A group of antibiotics that inhibit the cell wall synthesis. Effective against bacteria that are resistant to beta-lactam antibiotics.

Monobactams

An antibiotic that is effective against narrow range of Gram-negative bacteria, including Pseudomonas aeruginosa. It can be used on patients allergic to penicillins or cephalosporins.

Vancomycin

An antibiotic that inhibits cell wall synthesis; used to treat serious infections like MRSA and Clostridium difficile.

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Folate Metabolism Inhibitors

Antibiotics that block folic acid synthesis, essential for bacterial DNA and RNA production.

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Mupirocin

Inhibits bacterial protein synthesis, effective against gram ve bacteria and used topically.

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Polymyxin B

An antibiotic that disrupts the structure of the bacterial cell membrane, effective against Gram-negative bacteria.

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Cilastatin

An agent to ↓ metabolism of imipenem by inhibiting a dehydropeptidase present in kidney tubules.

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Bacitracin

An antibiotic that inhibits bacterial cell wall synthesis. It is toxic if ingested.

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Kernicterus

Adverse reaction: If sulfonamide is used near term during pregnancy or in neonates that causes bilirubin encephalopathy

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Beta-lactamases

Beta-lactamases are enzymes produced by bacteria that inactivate beta-lactam antibiotics.

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Cephalosporin Generations

Drug class effective against many bacteria, but generations vary in spectrum and resistance to beta-lactamases.

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Cephalosporins Uses

Primarily used as alternatives to penicillins for ENT, upper respiratory, and skin infections.

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Cephalosporins: Diarrhea

May occur due to alteration of gut flora; more common with oral agents.

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Cephalosporins: Injection Pain

Pain after IM injection and thrombophlebitis after IV injection.

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Ceftriaxone Precaution

Condition to avoid mixing ceftriaxone with calcium-containing solutions to prevent precipitation.

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Sulfamethoxazole Action

Inhibits dihydrofolate synthase, preventing conversion of PAPA to DHFA.

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Trimethoprim Action

Inhibition of dihydrofolate reductase prevents DHFA to THFA conversion.

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Sulfa Drug Side Effects

Fever and rash are commonly associated with hypersensitivity reactions.

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Steven-Johnson Syndrome

Severe and rare hypersensitivity can have fatal consequences.

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Crystalluria & Nephropathy

This happens because of insoluble metabolites that affect the kidneys.

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Study Notes

Cell Wall Inhibitors

  • Includes Cephalosporins
  • Mechanism of action is similar to Penicillin

Cephalosporins

  • Classified into 5 generations: 1st, 2nd, 3rd, 4th, and 5th Generation
  • Cephalosporins are generally resistant to beta-lactamases, except for the 1st and 2nd generations, which are sensitive

1st Generation Cephalosporins

  • Cefazolin, Cephalexin (PO), Cefadoxil (PO)
  • Highly active on Gram-positive bacteria (including MSSA) and some activity against Gram-negative bacteria

2nd Generation Cephalosporins

  • Cefuroxime (IV/PO), Cefoxitin, Cefaclor (PO)
  • More active on Gram-negative than 1st generation, weaker on Gram-positive.
  • Active against anaerobes

3rd Generation Cephalosporins

  • Cefotaxime, Ceftriaxone, Cefixime (po), Cefoperazone, Ceftazidime (Antipseudomons)
  • Activity against Gram-negative bacteria and variable activity against Gram-positive bacteria

4th Generation Cephalosporins

  • Cefepime
  • Activity against Gram-positive, Gram-negative, and Pseudomonas

5th Generation Cephalosporins

  • Ceftaroline (Anti-MRSA)
  • Activity against Gram-positive, Gram-negative, and MRSA

Cephalosporin Uses

  • Commonly used antibiotic
  • Alternatives to penicillins for ENT, upper respiratory tract, and skin infections, particularly when 1st generation cephalosporins can be used
  • Treatment of penicillinase-producing staphylococcal infections
  • Treatment of respiratory, urinary, and soft tissue infections
  • Treatment of Septicemia, combined with aminoglycosides
  • Surgical prophylaxis: Cefazolin is used
  • Treatment and prophylaxis of Meningitis: Ceftriaxone is used
  • Treatment of Gonorrhoea
  • Treatment of Typhoid: Ceftriaxone and Cefoperazone are excreted mainly in bile
  • Treatment of Pseudomonal infections using anti-pseudomonal cephalosporins
  • Treatment of Mixed aerobic/anaerobic infections like Peritonitis & Pelvic Inflammatory Disease (PID) using Cefuroxime, cefotaxime, and ceftriaxone

Cephalosporin Adverse Effects

  • Hypersensitivity reactions: similar to penicillin but less common
  • 10% of patients allergic to penicillin show cross-reactivity with cephalosporins
  • Patients with an immediate-type reaction to penicillin should not be given cephalosporins
  • Diarrhea: due to alteration of gut flora, more common with oral agents
  • Pain after IM injection
  • Thrombophlebitis after IV injection
  • Hypoprothrombinaemia (bleeding) with cefoperazone and ceftriaxone
  • Low-grade nephrotoxicity with preexisting renal disease and concurrent use of aminoglycosides

Cephalosporin Precaution

  • Ceftriaxone should not be mixed or co-administered with calcium-containing solutions due to the risk of precipitation of ceftriaxone-calcium salt and should not be administered within 48 hours of each other

Carbapenems and Monobactams

  • Both are types of cell wall inhibitors

Carbapenems

  • Imipenem, Meropenem
  • Similar mechanism to penicillin (binds to specific PBP)
  • Administered via IV or IM injection
  • Broad spectrum: Effective against Gram-positive, Gram-negative, Pseudomonas, and anaerobic bacteria
  • Resistant to most beta-lactamases
  • May cause cross-sensitivity in patients allergic to other beta-lactam antibiotics.
  • Used for severe infections due to multi-resistant organisms, and serious mixed infections (pulmonary, intra-abdominal & soft-tissue)
  • Common side effects nausea and vomiting
  • Seizures (especially with imipenem) may occur with high doses, CNS lesions, or renal insufficiency
  • Imipenem is combined with cilastatin to inhibit its metabolism and prolong its activity
  • Imipenem decreases the metabolism of Imipenem which in turn, it prolings drug activity and prevent formation of nephrotoxic metabolites
  • Meropenem is not combined with cilastatin since it's not sensitive to renal dipeptidase

Monobactams

  • Aztreonam
  • Similar mechanism to penicillin (binds to specific PBP)
  • Administered via IV or IM injection
  • Narrow spectrum: Effective against Gram-negative bacteria including Pseudomonas aeruginosa
  • Resistant to narrow-spectrum beta-lactamases
  • No cross-sensitivity: can be used in patients allergic to penicillins or cephalosporins
  • Used for hospital-acquired infections (urinary, biliary, GI & female genital tracts)
  • May cause hepatotoxicity, especially in infants and young children

Vancomycin

  • Spectrum: Gram-positive bacteria, including MRSA, Enterococcus, and Clostridium difficile
  • Mechanism of Action: Inhibits cell wall synthesis by preventing the assembly of peptidoglycan units and cross-linking.
  • Route of Administration: Injection (not absorbed orally)
  • Can be administered Orally (in specific indications)
  • Systemic use targets MRSA infections (skin and soft tissue infections, pneumonia, osteomyelitis, septicemia, endocarditis, meningitis, surgical prophylaxis if MRSA areas) and as a penicillin substitute for allergic patients.
  • Oral use treats pseudomembranous colitis (second-line to metronidazole) and staphylococcal enterocolitis.
  • Adverse effects include ototoxicity (potentially permanent nerve damage), nephrotoxicity, and red man syndrome (rash, fever, and flushing due to rapid histamine release).

Folate Metabolism Inhibitors

  • Cotrimoxazole (Sulfamethoxazole + Trimethoprim)

Mechanism of Action

  • Cotrimoxazole (sulfamethoxazole/trimethoprim)
  • Bactericidal
  • Sulfamethoxazole inhibits dihydrofolate synthase
  • Prevents conversion of PAPA to DHFA (folic acid)
  • Trimethoprim: Inhibits dihydrofolate reductase, which prevents conversion of DHFA (folic acid) to THFA (folinic acid)
  • This process is essential for nucleic acid and protein synthesis

Folate Synthesis

  • THFA is needed for bacterial protein, DNA, and RNA synthesis
  • PABA is para-amino-benzoic acid
  • DHFA is di-hydro-folic acid
  • THFA is tetra-hydro-folic acid

Spectrum

  • Broad spectrum
  • Effective against Gram-positive and Gram-negative bacteria
  • Effective against Pneumocystis jiroveci (fungus) and malarial parasite

Uses

  • Upper Respiratory Tract Infections
  • Urinary Tract Infections (UTI)
  • Pneumocystis jiroveci pneumonia (PJP)
  • Bronchitis
  • Prostatitis and vaginitis
  • Malaria

Side Effects

  • Sulfamethoxazole causes hypersensitivity reactions, including fever, rash, and Steven-Johnson syndrome (rare but potentially fatal)
  • Crysalluria and nephropathy: due to insoluble metabolite
  • Jaundice and Kernicterus in neonates: If sulfonamide is used near term (last 2 weeks) during pregnancy or in neonates, it causes bilirubin encephalopathy
  • BCZ displaces bilirubin from plasma protein binding sites and bilirubin crosses BBB
  • Trimethoprim can cause megaloblastic anemia or neural tube defects in babies of pregnant women

Bacitracin

  • Mechanism of Action: Inhibits cell wall synthesis
  • Spectrum: Gram-positive bacteria
  • Only topical application (toxic if systemic)
  • Uses: Available in ophthalmic and dermatologic ointments

Polymyxin B

  • Mechanism of Action: Disrupts the structure of the bacterial cell membrane.
  • Works against Gram-negative bacteria
  • There are topical preparations of bacitracin that may include polymyxin and/or neomycin

Mupirocin

  • Mechanism of Action: Inhibits bacterial protein synthesis.
  • Spectrum: Gram-positive bacteria, with good activity against S. pyogenes, MSSA, and MRSA.
  • Administered topically only
  • Available as cream and ointment for dermatologic use and as an ointment for intranasal use
  • Indicated for the treatment of traumatic skin lesions and impetigo secondarily infected with S. aureus or S. pyogenes.
  • Side effects include irritation at the site of application and eye irritation (if there is eye contact)

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