Raiyyan Tahsan

Raiyyan Tahsan
Hello I'm Raiyyan Tahsan
Brand Model and Executive

Antibiotics Case No 4.Antibiotics cell wall synthesis inhibitors

Cell wall synthesis inhibitors :

যে সব এন্টিবায়োটিক ব্যাকটেরিয়ার cell wall synthesis হতে দেয়না,

সেগুলিকে Cell wall synthesis inhibitors বলে।

এইসব এন্টিবায়োটিক এর Molecular structure এ বিটা ল্যাকটাম রিং থাকে।

Cell wall synthesis inhibitors শ্রেণীতে ৪ প্রকার ড্রাগ রয়েছে।

১.. পেনিসিলিন

২…সেফালোস্পোরিন

৩.. কার্বাপিনেম

৪. মনোব্যাকটাম

Beta lactamase Enzyme : সাধারণত গ্রাম নেগেটিভ ব্যাকটেরিয়া থেকে রিলিজ হওয়া এক প্রকার এনজাইম,

যা উপরের ৪ প্রকারের মধ্যে পেনিসিলিন গ্রুপের এন্টিবায়োটিক সমূহের বিটা ল্যাকটাম রিং কে ভেংগে দিয়ে তাদের কার্যকরিতা নষ্ট করে দেয়।

Beta lactamase inhibitors :

যেইসব ড্রাগস দিয়ে beta lactamase enzyme এর কাজ কে inhibit করে দেওয়া হয়, তাকে beta lactamase inhibitors বলে, For example, Clavulanic acid, sulbactam, Tazobactam etc.

Example

এবার জানতে হবে, Beta lactamase এনজাইম কোথায় sensitive আর কোথায় Resistance.

পেনিসিলিন গ্রুপের প্রতি beta lactamase sensitive,, আর cephalosporin এর 2nd G থেকে নিয়ে উপরের দিকে Beta lactamase resistant বলা যায়,

অর্থাৎ Beta lactamase যদিও পেনিসিলিন এর beta lactam ring কে ভেংগে দিয়ে তার কার্যকরিতা নষ্ট করে দেয়,

তবে 2nd or 3rd Generation এর প্রতি beta lactamase enzyme টা resistant..

তাই পেনিসিলিন (Amoxicillin) এর সাথে Beta lactamase enzyme inhibitors (Clavulanic acid) ব্যবহার হলেও 2nd /3rd generation cephalosporin এর সাথে Clavulanic acid ব্যবহার হয়না।

তাই তো আমরা দেখি, Cefixime, ceftriaxone, Cefoperazone কোনোটার সাথেই Clavulanic acid এর কম্বিনেশন নাই,

একই ভাই Cefuroxime ও Beta lactamase resistant Cephalosporin, তাই Cefuroxime এর সাথে Clavulanic acid ব্যবহার এর কোন রুলস নাই,

Cefuroxime + Clavulanic acid এর যেই কাজ, কেবল Cefuroxime ও একই কাজ করবে, Efficacy তে কোনো কম বেশ হবনা।

cephalosporin এর মধ্যে ceftazidime ও Cefepime এর সাথে beta lactamase inhibitors ব্যবহার হয় ESBL infection with psudomonas coverage এর জন্য।।

.Exampale Injection 1:-Tazid 1gm/vial IM/IV (AS A ceftazidime Pentahydrate AS A Third generation Cephalosporins).

Indications of Injection 1:-Tazid 1gm/vial IM/IV (AS A ceftazidime Pentahydrate AS A Third generation Cephalosporins).

Tazid Injection is indicated for the treatment of patients with infections caused by susceptible strains of the designated organisms in the following diseases:

Lower Respiratory Tract Infections, including pneumonia, caused by Pseudomonas aeruginosa and other Pseudomonas spp., Haemophilus influenzae, including ampicillin-resistant strains; Klebsiella spp.; Enterobacter spp.; Proteus mirabilis; Escherichia coli; Serratia spp.; Citrobacter spp.; Streptococcus pneumoniae; and Staphylococcus aureus (methicillin susceptible strains).

Skin and Skin Structure Infections caused by Pseudomonas aeruginosa; Klebsiella spp.; Escherichia coli; Proteus spp., including Proteus mirabilis and indole-positive Proteus, Enterobacter spp.; Serratia spp.; Staphylococcus aureus (methicillin susceptible strains); and Streptococcus pyogenes (group A beta-hemolytic streptococci).

Urinary Tract Infections, both complicated and uncomplicated, caused by Pseudomonas aeruginosa; Enterobacter spp.; Proteus spp., including Proteus mirabilis and indole-positive Proteus, Klebsiella spp.; and Escherichia coli.

Bacterial Septicemia caused by Pseudomonas aeruginosa, Klebsiella spp., Haemophilus influenzae, Escherichia coli, Serratia spp., Streptococcus pneumoniae and Staphylococcus aureus (methicillin susceptible strains).

Bone and Joint Infections caused by Pseudomonas aeruginosa, Klebsiella spp., Enterobacter spp., and Staphylococcus aureus (methicillin susceptible strains).

Gynecologic Infections, including endometritis, pelvic cellulitis, and other infections of the female genital tract caused by Escherichia coli.

Intraabdominal Infections, including peritonitis caused by Escherichia coli, Klebsiella spp., and Staphylococcus aureus (methicillin susceptible strains) and polymicrobial infections caused by aerobic and anaerobic organisms and Bacteroides spp.

Central Nervous System Infections, including meningitis, caused by Haemophilus influenzae and Neisseria meningitidis, Pseudomonas aeruginosa and Streptococcus pneumoniae

Pharmacology of  Injection 1:-Tazid 1gm/vial IM/IV (AS A ceftazidime Pentahydrate AS A Third generation Cephalosporins).

Ceftazidime is a semisynthetic, broad-spectrum, beta-lactam antibiotic for parenteral administration. Ceftazidime is bactericidal in action exerting its effect by inhibition of enzymes responsible for cell-wall synthesis. A wide range of gram-negative organisms is susceptible to ceftazidime in vitro, including strains resistant to gentamicin and other aminoglycosides. In addition, ceftazidime has been shown to be active against gram-positive organisms. It is highly stable to most clinically important beta-lactamases, plasmid or chromosomal, which are produced by both gram-negative and gram-positive organisms and, consequently, is active against many strains resistant to ampicillin and other cephalosporins.

Dosage of  Injection 1:-Tazid 1gm/vial IM/IV (AS A ceftazidime Pentahydrate AS A Third generation Cephalosporins).

 

The usual adult dosage is 1 gram administered intravenously or intramuscularly every 8 to 12 hours. The dosage and route should be determined by the susceptibility of the causative organisms, the severity of infection and the condition, and renal function of the patient.

Ceftazidime is to be used by the parenteral route, the dosage depending upon the severity, sensitivity & type of infections and the age, weight & renal function of the patient.

Adults: The adult dosage range for ceftazidime is 1 to 6 gm per day 8 or 12 hourly (IM/IV) in the majority of infections, 1 gm 8 hourly or 2 gm 12 hourly should be given.

  • In urinary tract infections and many less serious infections: 500 mg or 1 gm 12 hourly is usually adequate.
  • In severe infections, especially immunocompromised patients, including those with neutropenia: 2 gm 8 or 12 hourly should be administered. When used as a prophylactic agent in prostatic surgery 1 gm should be given at the induction of anesthesia. A second dose should be considered at the time of catheter removal.

Elderly: In view of the reduced clearance of Ceftazidime in acutely ill elderly patients, the daily dosage should not normally exceed 3 gm, especially in those over 80 years of age.

  • Cystic fibrosis: In fibrocystic adults with normal renal function who have pseudomonal lung infections, high doses of 100 to 150 mg/kg/day as three divided doses should be used.

Infants and Children: The usual dosage range for children aged over two months is 30 to 100 mg/kg/day, given as two or three divided doses. Doses up to 150 mg/kg/day (maximum 6 gm daily) in three divided doses may be given to infected immunocompromised or fibrocystic children or children with meningitis.

Neonates and Children up to 2 months of age: The usual dosage range is 25 to 60 mg/kg/day as two divided doses.

Contraindications of  Injection 1:-Tazid 1gm/vial IM/IV (AS A ceftazidime Pentahydrate AS A Third generation Cephalosporins).

Ceftazidime is contraindicated in patients who have shown hypersensitivity to Ceftazidime or the cephalosporin group of antibiotics.

Side Effects of  Injection 1:-Tazid 1gm/vial IM/IV (AS A ceftazidime Pentahydrate AS A Third generation Cephalosporins).

The most common side-effects are local reactions following IV injection and allergic and gastrointestinal reactions. Hypersensitivity reactions are pruritus, rash, and fever. Angioedema and anaphylaxis have been reported very rarely. Gastrointestinal symptoms are diarrhea, nausea, vomiting, and abdominal pain. Central nervous system reactions included headache, dizziness, and paresthesia.

Pregnancy & Lactation of  Injection 1:-Tazid 1gm/vial IM/IV (AS A ceftazidime Pentahydrate AS A Third generation Cephalosporins).

Pregnancy: No adequate and well-controlled studies in pregnant women have been conducted with Ceftazidime. Because animal reproduction studies are not always predictive of human response this drug should be used during pregnancy only if clearly needed.

Lactation: Ceftazidime is excreted in human milk in low concentrations. Because many drugs are excreted in human milk and because the safety of the component of the injections in nursing infants has not been established, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Therapeutic Class of  Injection 1:-Tazid 1gm/vial IM/IV (AS A ceftazidime Pentahydrate AS A Third generation Cephalosporins).

Third generation Cephalosporins

Example

AND Injection 2:-Ultrapime IM/IV 1gm /vial (AS A Cefepime Hydrochloride AS A Fourth generation Cephalosporins).

Indications of  Injection :-Ultrapime IM/IV 1gm /vial (AS A Cefepime Hydrochloride AS A Fourth generation Cephalosporins):-

 

Ultrapime is indicated for the treatment of the following infections caused by susceptible strains of the microorganisms:

  • Pneumonia (moderate to severe): caused by Streptococcus pneumoniae, including cases associated with concurrent bacteremia, Pseudomonas aeruginosa, Klebsiella pneumoniae, or Enterobacter species.
  • Febrile Neutropenia: Ultrapime as monotherapy is indicated for empiric treatment of febrile neutropenic patients. In patients at high risk for severe infection (including patients with a history of recent bone marrow transplantation, with hypotension at presentation, with an underlying hematologic malignancy, or with severe or prolonged neutropenia), antimicrobial monotherapy may not be appropriate. Insufficient data exist to support the efficacy of cefepime monotherapy in such patients.
  • Uncomplicated and Complicated Urinary Tract Infections (including pyelonephritis): caused by Escherichia coli or Klebsiella pneumoniae, when the infection is severe, or caused by Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis, when the infection is mild to moderate, including cases associated with concurrent bacteremia with these microorganisms.
  • Uncomplicated Skin and Skin Structure Infections: caused by Staphylococcus aureus (methicillin- susceptible strains only) or Streptococcus pyogenes.
  • Complicated Intra-abdominal Infections (used in combination with metronidazole): caused by Escherichia coli, viridians group streptococci, Pseudomonas aeruginosa, Klebsiella pneumoniae, Enterobacter species, or Bacteroides fragilis.

Pharmacology of  Injection :-Ultrapime IM/IV 1gm /vial (AS A Cefepime Hydrochloride AS A Fourth generation Cephalosporins):-

 

Cephalosporins are bactericidal and have the same mode of action as other beta-lactam antibiotics (such as penicillins). Cephalosporins disrupt the synthesis of the peptidoglycan layer of bacterial cell walls. The peptidoglycan layer is important for cell wall structural integrity, especially in Gram-positive organisms. The final transpeptidation step in the synthesis of the peptidoglycan is facilitated by transpeptidases known as penicillin binding proteins (PBPs).

Dosage & Administration of  Injection :-Ultrapime IM/IV 1gm /vial (AS A Cefepime Hydrochloride AS A Fourth generation Cephalosporins):-

 

Cefepime should be administered intravenously over approximately 30 minutes.

  • Moderate to Severe Pneumonia due to S. pneumoniae, *P. aeruginosa, K. pneumoniae, or Enterobacter species: 1-2 gm IV 12 hourly for 10 days.
  • Empiric therapy for febrile neutropenic patients: 2 gm IV 8 hourly for 7** days.
  • Mild to Moderate Uncomplicated or Complicated Urinary Tract Infections, including pyelonephritis, due to E. coli, K. pneumoniae, or P. mirabilis*: 0.5-1 gm IV/IM*** 12 hourly for 7-10 days.
  • Severe Uncomplicated or Complicated Urinary Tract Infections, including pyelonephritis, due to E. coli or K. pneumoniae*: 2 gm IV 12 hourly for 10 days.
  • Moderate to Severe Uncomplicated Skin and Skin Structure Infections due to S. aureus or S. pyogenes: 2 gm IV 12 hourly for 10 days.
  • Complicated Intra-abdominal Infections (used in combination with metronidazole) caused by E. coli, viridans group streptococci, P. aeruginosa, K. pneumoniae, Enterobacter species, or B. fragilis: 2 gm IV 12 hourly for 7-10 days.

Note:
*including cases associated with concurrent bacteremia.
**or until resolution of neutropenia. In patients whose fever resolves but who remain neutropenic for more than 7 days, the need for continued antimicrobial therapy should be re evaluated frequently.
*** IM route of administration is indicated only for mild to moderate, uncomplicated or complicated UTls due to E. coli when the IM route is considered to be a more appropriate route of drug administration.

Interaction of  Injection :-Ultrapime IM/IV 1gm /vial (AS A Cefepime Hydrochloride AS A Fourth generation Cephalosporins):-

Renal function should be monitored carefully if high doses of aminoglycosides are to be administered with Ultrapime because of the increased potential of nephrotoxicity and ototoxicity of aminoglycoside antibiotics. Nephrotoxicity has been reported following concomitant administration of other cephalosporins with potent diuretics such as furosemide.

Contraindications of  Injection :-Ultrapime IM/IV 1gm /vial (AS A Cefepime Hydrochloride AS A Fourth generation Cephalosporins):-

Cefepime is contraindicated in patients who have shown immediate hypersensitivity reactions to cefepime or the cephalosporin class of antibiotics, penicillin, or other betalactum antibiotics.

Side Effects of  Injection :-Ultrapime IM/IV 1gm /vial (AS A Cefepime Hydrochloride AS A Fourth generation Cephalosporins):-

Ultrapime is contraindicated in patients who have shown immediate hypersensitivity reactions to cefepime or the cephalosporin class of antibiotics, penicillin, or other betalactum antibiotics.

Pregnancy & Lactation of  Injection :-Ultrapime IM/IV 1gm /vial (AS A Cefepime Hydrochloride AS A Fourth generation Cephalosporins):-

Pregnancy Category B. There are, however, no adequate and well-controlled studies of cefepime use in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. Cefepime is excreted in human breast milk in very low concentrations (0.5 pg/ml). Caution should be exercised when cefepime is administered to a nursing woman.

Therapeutic Class of  Injection :-Ultrapime IM/IV 1gm /vial (AS A Cefepime Hydrochloride AS A Fourth generation Cephalosporins):-

Fourth generation Cephalosporins

মূলকথা —

Cefuroxime এর সাথে Clavulanic acid এর কম্বিনেশন এ-র কোনো প্রয়োজন নাই

Cefuroxime 2nd Generation cephalosporin

এইটার গ্রাম পজিটিভ ও গ্রাম নেগেটিভ কাভারেজ আছে

তাই এইটা Broad spectrum antibiotics

Exampale tablet 3:-Cefotil 500mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

Indications of Exampale tablet 1:-Cefotil 500mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

It is indicated for the treatment of infections caused by sensitive bacteria.

  • Pharyngitis/Tonsillitis caused by Streptococcus pyogenes.
  • Acute Bacterial Otitis Media caused by Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis (beta-lactamase producing strains) or Streptococcus pyogenes.
  • Acute bacterial maxillary sinusitis caused by Streptococcus pneumoniae or Haemophilus influenzae (non beta-lactamase producing strains)
  • Lower respiratory tract infections including pneumoniae, caused by Streptococcus pneumoniae, Haemophilus influenzae (including beta lactamase-producing strains), Klebsiella spp., Staphylococcus aureus (penicillinase- and non-penicillinase-producing strains), Streptococcus pyogenes, E. coli
  • Acute bacterial exacerbation of chronic bronchitis and Secondary bacterial infections of Acute bronchitis caused by Streptococcus pneumoniae, Haemophilus influenzae (beta-lactamase negative strains) or Haemophilus parainfluenzae (beta-lactamase negative strains).
  • Skin and skin-structure infections caused by Staphylococcus aureus (including beta-lactamase producing strains) or Streptococcus pyogenes.
  • Urinary tract infections caused by E.coli or Klebsiella pneumoniae.
  • Bone and Joint Infections caused by Staphylococcus aureus (penicillinase- and non-penicillinase-producing strains).
  • Gonorrhoea caused by penicillinase-producing and non-penicillinase producing strains of Neisseria gonorrhoeae.
  • Early Lyme Disease (erythema migrans) caused by Borrelia burgdorferi.

Pharmacology of Exampale tablet 1:-Cefotil 500mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

Cefuroxime is a well-characterized and effective antibacterial agent, which has broad-spectrum bactericidal activity against a wide range of common pathogens, including β-lactamase producing strains. Cefuroxime has good stability to bacterial β-lactamase and consequently, is active against many ampicillin-resistant and amoxycillin-resistant strains.

Dosage of Exampale tablet 1:-Cefotil 500mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

Tablet or Suspension-

Adolescents and adults (13 years and older)-

  • Pharyngitis/tonsillitis: 250 mg b.i.d. for 5-10 days
  • Acute bacterial maxillary sinusitis: 250 mg b.i.d. for 10 days
  • Acute bacterial exacerbation of chronic bronchitis: 250-500 mg b.i.d. for 10 days
  • Secondary bacterial infections of acute bronchitis: 250-500 mg b.i.d. for 5-10 days
  • Uncomplicated skin and skin structure infections: 250-500 mg b.i.d. for 10 days
  • Uncomplicated urinary tract infections: 250 mg b.i.d. for 7-10 days
  • Uncomplicated Gonorrhoea: 1000 mg Single dose
  • Community acquired pneumonia: 250-500 mg b.i.d. for 5-10 days
  • MDR Typhoid Fever: 500 mg b.i.d. for 10-14 days
  • Early Lyme disease: 500 mg b.i.d. for 20 days

Paediatric Patients (3 months to 12 years)-

  • Pharyngitis/Tonsillitis: 20 mg/kg/day b.i.d for 5-10 days
  • Acute otitis media: 30 mg/kg/day b.i.d for 10 days
  • Acute bacterial maxillary sinusitis: 30 mg/kg/day b.i.d for 10 days
  • Impetigo: 30 mg/kg/day b.i.d for 10 days

Parenteral-

  • Adult: 750 mg three times daily by IM or IV injection. In severe infections, dose can be increased upto 1.5 gm three times daily by IV injection. The frequency may be increased to four times daily, if necessary, giving total daily doses of 3 to 6 gms.
  • Children (above 3 months of age): 30 – 100 mg/kg/day given in 3 or 4 equally divided doses. A dose of 60 mg/kg/day is appropriate for most infections.
  • Neonate: 30 – 100 mg/kg/day given in 2 or 3 equally divided doses.
  • Surgical prophylaxis: 1.5 gm by IV injection at induction of anaesthesia; up to 3 further doses of 750 mg may be given by IV/IM injection every 8 hours for high risk procedures.
  • Pneumonia: 1.5 gm IV injection twice daily for 2-3 days, followed by 500 mg twice daily (oral) for 7-10 days.

  • Acute exacerbations of chronic bronchitis    : 750 mg twice daily (IM or IV injection) for 2-3 days, followed by 500 mg twice daily (oral) for 5-10 days. (Duration of both parenteral and oral therapy is determined by the severity of the infection and the clinical status of the patient.)
  • In Gonorrhoea: Adult: 1.5 gm as a single dose (as 2 x 750mg injections intramuscularly with different sites, e.g. each buttock).

In Meningitis:

  • Adult: 3 gm IV injection three times daily.
  • Children (above 3 months of age): 200-240 mg/kg/day by IV injection in 3 or 4 divided doses reduced to 100 mg/kg/day after 3 days or on clinical improvement.
  • Neonate: 100 mg/kg/day by IV injection at initial dose, reduced to 50 mg/kg/day, When clinically indicated.

In bone and joint infections:

  • Adult: 1.5 gm IV injection four times daily.
  • Children (above 3 months of age): 150 mg/kg/day (not to exceed the maximum adult dose) in equally divided doses every 8 hours.

Administration of Exampale tablet 1:-Cefotil 500mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

The use of freshly reconstituted solution is recommended. However, it maintains potency for at least 24 hours at room temperature or 48 hours at 5o C

Interaction of Exampale tablet 1:-Cefotil 500mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

No potentially hazardous interactions have been reported.

Contraindications of Exampale tablet 1:-Cefotil 500mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

Cefuroxime is contraindicated in patients with known allergy to Cephalosporins.

Side Effects of Exampale tablet 1:-Cefotil 500mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

Adverse effects to Cefotil have occurred infrequently and have been generally mild and transient in nature. Effects reported include rashes and gastrointestinal disturbances. As with other antibiotics, prolonged use may result in the overgrowth of non susceptible organisms e.g. Candida.

Pregnancy & Lactation of Exampale tablet 1:-Cefotil 500mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

US FDA pregnancy category of Cefuroxime is B. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. Cefuroxime have been shown to be excreted in human milk. So, caution should be exercised when Cefuroxime is administered to a nursing woman.

Precautions & Warnings of Exampale tablet 1:-Cefotil 500mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

Cefotil should be given with care to patients receiving concurrent treatment with potent diuretics & who has history of colitis. Cephalosporin antibiotics may in general be given safely to patients who are hypersensitive to penicillin although cross reactions have reported. Cefotil has shown, that is not likely to be a problem at the recommended to dose levels.

Therapeutic Class of Exampale tablet 1:-Cefotil 500mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

Second generation Cephalosporins

ENT infection (nasal, throat, ear, for example, sinusitis. Otitis media, laryngitis, pharyngitis etc,) and also UTI, Cystitis. এইসব ক্ষেত্রে ব্যবহার হয়।

sexually active women দের UTI তে Drug of Choice বলা যেতে পারে।।

Raiyyan Tahsan ❤️Date:07-01-2025 Tuesday Time:-8-23-33 Pm

Leave a Comment

Your email address will not be published. Required fields are marked *

Scroll to Top