Ceftibuten; Uses, Side Effects, Interactions, Pregnancy

Ceftibuten is a semisynthetic, beta-lactamase-stable, third-generation cephalosporin with antibacterial activity. Ceftibuten binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Ceftibuten is only found in individuals that have used or taken this drug. It is a third-generation cephalosporin antibiotic. It is an orally-administered agent. Cefalexin is used to treat acute bacterial exacerbations of chronic bronchitis (ABECB), acute bacterial otitis media, pharyngitis, and tonsilitis. Ceftibuten exerts its bactericidal action by binding to essential target proteins of the bacterial cell wall. This binding leads to inhibition of cell-wall synthesis.

Mechanism of action of ceftibuten

Ceftibuten, like other beta-lactam antibiotics (e.g., penicillins), is mainly bactericidal. It inhibits the third and final stage of bacterial cell wall synthesis by preferentially binding to specific penicillin-binding proteins (PBPs) that are located inside the bacterial cell wall. Penicillin-binding proteins are responsible for several steps in the synthesis of the cell wall and are found in quantities of several hundred to several thousand molecules per bacterial cell. Penicillin-binding proteins vary among different bacterial species. Thus, the intrinsic activity of ceftibuten, as well as the other cephalosporins and penicillins against a particular organism, depends on its ability to gain access to and bind with the necessary PBP. Like all beta-lactam antibiotics, the ability of ceftibuten to interfere with PBP-mediated cell wall synthesis ultimately leads to cell lysis. Lysis is mediated by bacterial cell wall autolytic enzymes (i.e., autolysins). The relationship between PBPs and autolysins is unclear, but it is possible that the beta-lactam antibiotic interferes with an autolysin inhibitor.In general, third-generation cephalosporins are more active and have a broader spectrum against gram-negative species than do the earlier generations of cephalosporins. They are less active, however, against the gram-positive species than are their first-generation counterparts. In vitro and clinical data suggest ceftibuten is effective against infections caused by the following organisms: Haemophilus influenzae (beta-lactamase negative), Haemophilus influenzae (beta-lactamase positive), Moraxella catarrhalis (including beta-lactamase-producing strains), Streptococcus pneumoniae (penicillin-susceptible strains only), and Streptococcus pyogenes (group A beta-hemolytic streptococci). Ceftibuten is inactive in vitro against Acinetobacter, Bordetella, Campylobacter, Enterobacter, Enterococcus, Flacovacterium, Hafnia, Listeria, Pseudomonas, Staphylococcus, and Streptococcus (except pneumoniae and pyogenes) species. Additionally, ceftibuten shows little in vitro activity against most anaerobes, including most species of Bacteroide.

Indications of ceftibuten

• Used to treat acute bacterial exacerbations of chronic bronchitis (ABECB), acute bacterial otitis media, pharyngitis, and tonsilitis.
• Pneumonia
• Bladder infection
• Bronchitis
• Otitis media
• Sinusitis
• Strep throat
• Tonsillitis/pharyngitis
• Skin or soft tissue infection
• Bacterial infections
• Community acquired pneumonia
• Streptococcal pharyngitis
• Streptococcal tonsillitis
• Acute bacterial exacerbation of chronic bronchitis
• Bacterial infections
• Otitis media bacterial
• Streptococcal Pharyngitis
• Streptococcal tonsillitis

Contra Indications of ceftibuten

• Clostridium difficile infection
• Inflammation of the Large Intestine
• Moderate to Severe Kidney Impairment
• Renal impairment
• Concurrent nephrotoxic agent use
• Seizure disorder
• Allergies Cephalosporins & Betalactams

Dosages of ceftibuten

Strengths: 90 mg/5 mL; 180 mg/5 mL ;400 mg;

Otitis Media

• 400 mg orally every 24 hours for 10 days

Tonsillitis/Pharyngitis

• 400 mg orally every 24 hours for 10 days

Bronchitis

• 400 mg orally every 24 hours for 10 days

Cystitis

• 400 mg orally every 24 hours for 7 days

Pneumonia

• 200 mg orally every 12 hours for 7 to 14 days

Sinusitis

• 400 mg orally every 24 hours for 10 to 14 days

Pediatric Dose

Bronchitis

• >12 years: 400 mg orally every 24 hours for 10 days

Cystitis

• >12 years: 400 mg orally every 24 hours for 7 days

Pneumonia

• >12 years: 200 mg orally every 12 hours for 7 to 14 days

Sinusitis

• >12 years: 400 mg orally every 24 hours for 10 to 14 days

Otitis Media

• >6 months: 9 mg/kg/day (maximum 400 mg) every 24 hours for 10 days

Tonsillitis/Pharyngitis

• >6 months: 9 mg/kg/day (maximum 400 mg) every 24 hours for 10 days

Side Effects of ceftibuten

The most common

• Diarrhea or loose stools
• Nausea
• Abdominal pain
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• leukopenia/leukemia
• hemolytic anemia
• serum sickness
• agranulocytosis
• pain, swelling, irritation where injected
• stomach upset
• sweating
• skin color change, mild diarrhea
• mild nausea
• loss of appetite
• vaginal discharge and itching
• swelling of feet or legs
• chest pain
• constipation
• cough
• diarrhea or loose stools
• difficulty with breathing
• dizziness
• heartburn

• aminoglycosides such as amikacin , gentamicin (Garamycin), and tobramycin
• furosemide 
• probenecid
• methotrexate 
• birth control pills
• theophylline
• antacids such as Tums and Citracal
• H2 blockers such as cimetidine , ranitidine , and famotidine 

This is not a complete list of ceftibuten drug interactions. Ask your doctor or pharmacist for more information.

Pregnancy & Lactation of ceftibuten

FDA pregnancy risk category B

Ceftibuten is classified in FDA pregnancy risk category B. Animal data reveal no teratogenic or embryocidal effects. There are, however, no adequate and well-controlled studies of ceftibuten use in pregnant women. Because animal studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. Ceftibuten has not been studied for use during labor and delivery. Treatment should be given only if clearly needed.

Lactation

Limited information indicates that ceftibuten produces low levels in milk that are not expected to cause adverse effects in breastfed infants. Occasionally disruption of the infant’s gastrointestinal flora, resulting in diarrhea or thrush have been reported with cephalosporins, but these effects have not been adequately evaluated. Ceftibuten is acceptable in nursing mothers.

References

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