Antibiotic Case No 14.Second Generation Cephalosporins Antibiotic

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Antibiotic Case No 14.Second Generation Cephalosporins Antibiotic

There are only 3 Component preparation of Second generation Cephalosporins they are:-

1.Cefaclor Monohydrate.

2.Cefuroxime Axetil.

3. Cefuroxime Axetil+Clavulanic Acid.

Descriptition:-

1.Cefaclor Monohydrate:-

Indications of Cefaclor Monohydrate:-

Cefaclor monohydrate is indicated for the treatment of the following infections:

Respiratory tract infections, including pneumonia, bronchitis, caused by Streptococcus Pneumoniae, Haemophilus Influenzae, and Streptococcus Pyogenes
Otitis media caused by Streptococcus pneumoniae, Haemophilus influenzae, Staphylococci, and Streptococcus pyogenes
Pharyngitis and Tonsillitis, caused by Streptococcus pyogenes
Urinary tract infections, including pyelonephritis and cystitis, caused by Escherichia coli, Proteus mirabilis, Klebsiella spp., and coagulase-negative Staphylococci
Skin and skin structure infections caused by Staphylococcus aureus and Streptococcus pyogenes.

Pharmacology of Cefaclor Monohydrate:-

Cefaclor is a second generation cephalosporin antibiotic which has stability against b-lactamase inactivation and possesses a broad spectrum of activity. Cefaclor is active against the following organisms in vitro: Alpha and beta haemolytic Streptococci, Staphylococci; including coagulase-positive, coagulase negative and penicillinase-producing strains, Streptococcus pneumoniae, Streptococcus pyogenes (Group A b-haemolytic Streptococci), Branhamella catarrhalis, Escherichia coli, Proteus mirabilis, Klebsiella species Haemophilus influenzae, including ampicillin-resistant strains. Cefaclor is generally effective in the eradication of Streptococci from the nasopharynx.

Dosage & Administration of Cefaclor Monohydrate:-

Capsule: Adult dose: The usual dose is 250 mg every 8 hourly. For severe infections or those caused by less susceptible organisms, doses may be doubled with a maximum dosage of 4 g/day. In case of β-hemolytic Streptococcal infections, therapy should be administered for at least 10 days.

Powder for suspension & Pediatric drops: Children: The usual daily dosage for paediatric patients over 1 month is 20 mg/kg/day in divided doses every 8 hours. In serious infections such as otitis media and infections caused by less susceptible organisms, 40 mg/kg/day are recommended, with a maximum dosage of 1 g/day. Safety and effectiveness of Cefaclor for use in infants less than 1 month of age have not been established.

<1 year (9 kg):

Powder for suspension: ½ tsp three times daily
Pediatric drops: 0.625 ml three times daily

1-5 years (9 kg-18 kg):

Powder for suspension: 1 tsp three times daily
Pediatric drops: 1.25 ml three times daily

Over 5 years:

Powder for suspension: 2 tsp three times daily

In renal impairment: Cefaclor may be administered in the presence of impaired renal function. Dose adjustments for patients with moderate or sever renal impairment are not usually required.

In patients undergoing haemodialysis: Haemodialysis shortens serum half-life by 25-30%. In patients undergoing haemodialysis, a predialysis loading dose of 250 mg-1 g is recommended. A maintaining dose of 250-500 mg every 6 hourly during interdialytic period may be used.

Geriatric use: Clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

Interaction of Cefaclor Monohydrate:-

Cefaclor may show a false-positive reaction for glucose in the urine with tests that use Benedict’s solution, Fehling’s solutions. When Cefaclor and oral anticoagulants were administered concomitantly there have been reports of increased anticoagulant effect and there have been rare reports of increased prothrombin time, with or without clinical bleeding, in patients receiving Cefaclor and anticoagulants (Warfarin) concomitantly. It is recommended that in such patients, regular monitoring of prothrombin time should be considered, with adjustment of dosage if necessary.

Contraindications of Cefaclor Monohydrate:-

Cefaclor is contraindicated in patients with known allergy to the Cephalosporin group of antibiotics.

Side Effects of Cefaclor Monohydrate:-

Gastro-intestinal symptoms may occur include diarrhea, nausea and vomiting in some patients receiving Cefaclor. As with some penicillins and some other Cephalosporins, transient hepatitis and cholestatic jaundice have been reported rarely. Fever, abdominal pain, superinfection, renal dysfunction, toxic nephropathy, hemorrhage, elevated LDH and pancytopenia may occur.

Pregnancy & Lactation of Cefaclor Monohydrate:-

There are no adequate and well-controlled studies in pregnant women. This drug should be used during pregnancy only if clearly needed. Small amounts of Cefaclor have been detected in mother’s milk. The effect on nursing infants is not known. Caution should be exercised when Cefaclor is administered to a nursing woman.

Precautions & Warnings of Cefaclor Monohydrate:-

Prescribing Cefaclor in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.

Prolonged use of Cefaclor may result in the overgrowth of nonsusceptible organisms. If superinfection occurs during therapy, appropriate measures should be taken. As with other β-lactam antibiotics, the renal excretion of Cefaclor is inhibited by Probenecid. Antibiotics, including Cephalosporins, should be prescribed with caution in individuals with a history of gastrointestinal disease, particularly colitis.

Before therapy with Cefaclor is instituted, careful inquiry should be made to determine whether the patient has had previous hypersensitivity reactions to Cefaclor, Cephalosporins, Penicillins or other drugs. If this product is to be given to penicillin-sensitive patients, caution should be exercised. Cefaclor should be administered cautiously to any patient who has demonstrated some form of allergy, particularly to drugs.

Overdose Effects of Cefaclor Monohydrate:-

The toxic symptoms following an overdose of Cefaclor may include nausea, vomiting, epigastric distress, and diarrhea.

Therapeutic Class of Cefaclor Monohydrate:-

Second generation Cephalosporins

1.Cefaclor Monohydrate:-

Capsule 1.Abaclor 250mg (AS A Cefaclor Monohydrate AS A Second generation Cephalosporins).

Capsule 2.Oticlor 500mg (AS A Cefaclor Monohydrate AS A Second generation Cephalosporins).

Syrup 3. Oticlor 125mg/5ml 100ml Bottle (AS A Cefaclor Monohydrate AS A Second generation Cephalosporins).

Pediatric Drop 4. Oticlor 125mg/1.25ml 15ml Bottle (AS A Cefaclor Monohydrate AS A Second generation Cephalosporins).

2.Cefuroxime Axetil:-

Indications of Cefuroxime Axetil:-

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 Cefuroxime Axetil:-

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 Cefuroxime Axetil:-

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 Cefuroxime Axetil:-

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

Interaction of Cefuroxime Axetil:-

No potentially hazardous interactions have been reported.

Contraindications of Cefuroxime Axetil:-

Cefuroxime is contraindicated in patients with known allergy to Cephalosporins.

Side Effects of Cefuroxime Axetil:-

Adverse effects to Cefuroxime 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 Cefuroxime Axetil:-

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 Cefuroxime Axetil:-

Cefuroxime 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. Cefuroxime has shown, that is not likely to be a problem at the recommended to dose levels.

Therapeutic Class of Cefuroxime Axetil:-

Second generation Cephalosporins

2.Cefuroxime Axetil:-

Tablet 1.Cefotil 250mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

Tablet 2.Cefotil 500 mg (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

Syrup 3. Cefotil 125mg/5ml 70ml Bottle (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

Injection 4. Cefotil IM/IV 750mg/vial (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

Injection 5. Cefotil -IV Injection 1.5gm/vial (AS A Cefuroxime Axetil AS A Second generation Cephalosporins).

3. Cefuroxime Axetil+Clavulanic Acid:-

Description:-

Indications of Cefuroxime Axetil+Clavulanic Acid:-

This combination 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).
Uncomplicated skin and skin-structure infections caused by Staphylococcus aureus (including beta-lactamase producing strains) or Streptococcus pyogenes.
Uncomplicated urinary tract infections caused by E.coli or Klebsiella pneumoniae.
Bone and Joint Infections caused by Staphylococcus aureus (penicillinase- and non-penicillinase-producing strains).
Uncomplicated Gonorrhoea caused by penicillinase-producing and non-penicillinase producing strains of Neisseria gonorrhoeae.
Early Lyme Disease (erythema migrans) caused by Borrelia burgdorferi.
Septicemia caused by Staphylococcus aureus, Streptococcus pneumoniae, E.coli, Haemophilus influenzae (including ampicillin-resistant strains) & Klebsiella spp.
Meningitis caused by Streptococcus pneumoniae, Haemophilus influenzae (including ampicillin-resistant strains), Neisseria meningitidis & Staphylococcus aureus (penicillinase and non-penicillinase producing strains)
Switch therapy (Injectable to oral)

Pharmacology of Cefuroxime Axetil+Clavulanic Acid:-

Cefuroxime is a bactericidal second generation cephalosporin antibiotic which is active against a wide range of Gram-positive and Gram-negative susceptible organisms including many beta-lactamase producing strains. Cefuroxime inhibits bacterial cell wall synthesis by interfering with the transpeptidation process.

Clavulanic acid is a naturally derived beta lactamase inhibitor produced by Streptomyces clavuligerus. It has similar structure to beta lactam antibiotics which binds irreversibly to beta-lactamase enzymes and inactivates them. Clavulanic acid gives protection of Cefuroxime from degradation by beta lactamase enzymes and provides a solution for the treatment of bacterial infections caused by beta lactam resistant bacteria.

Dosage & Administration of Cefuroxime Axetil+Clavulanic Acid:-

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 b.i.d. 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

Cefuroxime-Clavulanic Acid tablet may be taken without regard of food.

Interaction of Cefuroxime Axetil+Clavulanic Acid:-

Concomitant administration of probenecid with Cefuroxime-Clavulanic Acid increases the area under the serum concentration versus time curve by 50%. Drug that reduces gastric acidity may result in a lower bioavailability of Cefuroxime and tend to cancel the effect of postprandial absorption.

Contraindications of Cefuroxime Axetil+Clavulanic Acid:-

Cefuroxime-Clavulanic Acid is contraindicated in patients with known allergy to cephalosporin & in patients with Pseudomembranous Colitis.

Side Effects of Cefuroxime Axetil+Clavulanic Acid:-

Generally Cefuroxime-Clavulanic Acid is well tolerated. However, a few side effects like nausea, vomiting, diarrhea, abdominal discomfort or pain may occur. As with other broad-spectrum antibiotics, prolonged administration of Cefuroxime and Clavulanic acid combination may result in overgrowth of nonsusceptible microorganisms. Rarely (<0.2%) renal dysfunction, anaphylaxis, angioedema, pruritis, rash and serum sickness like urticaria may appear.

Pregnancy & Lactation of Cefuroxime Axetil+Clavulanic Acid:-

While all antibiotics should be avoided in the first trimester if possible. However, Cefuroxime-Clavulanic Acid can be safely used in later pregnancy to treat urinary and other infections. Cefuroxime-Clavulanic Acid is excreted into the breast milk in small quantities. However, the possibility of sensitizing the infant should be kept in mind.

Precautions & Warnings of Cefuroxime Axetil+Clavulanic Acid:-

Cefuroxime should be given with care to patients receiving concurrent treatment with potent diuretics & who has history of colitis.

Therapeutic Class of Cefuroxime Axetil+Clavulanic Acid:-

Second generation Cephalosporins, Vaccines, Anti-sera & Immunoglobulin

3. Cefuroxime Axetil+Clavulanic Acid:-

Tablet 1.Cefotil Plus (250mg+62.5mg) (AS A (Cefuroxime Axetil+Clavulanic Acid) AS A Second generation Cephalosporins, Vaccines, Anti-sera & Immunoglobulin).

Tablet 2.Cefotil Plus (500mg+125mg) (AS A (Cefuroxime Axetil+Clavulanic Acid) AS A Second generation Cephalosporins, Vaccines, Anti-sera & Immunoglobulin).

Syrup 3. Cefotil Plus (125mg+31.25mg)5ml 70 ml Bottle (AS A (Cefuroxime Axetil+Clavulanic Acid) AS A Second generation Cephalosporins, Vaccines, Anti-sera & Immunoglobulin).

Raiyyan Tahsan Date:-30-01-2025 Thursday Time:-11-58-54 Pm

Raiyyan Tahsan

Raiyyan Tahsan