Ceftibuten

Ceftibuten belongs to the pharmacological class of Third-generation cephalosporin antibiotics.

Ceftibuten has been approved to relieve symptoms and also for the treatment and maintenance of Acute bacterial otitis media, Acute bacterial exacerbations of chronic bronchitis, Pharyngitis/tonsillitis

Ceftibuten is rapidly and completely absorbed after oral administration, with a bioavailability of approximately 50% and a peak plasma concentration (Cmax) of approximately 2.5 mcg/mL occurring within 2 to 4 hours after a single 400 mg dose. The drug is primarily eliminated unchanged in the urine, with a half-life of approximately 2.5 to 3 hours in adults, and dose adjustments may be necessary in patients with the impaired renal function. Ceftibuten's duration of action varies depending on the specific infection being treated, but in general, a 10-day course of treatment is recommended to ensure complete eradication of the infection.

The common side effects which are involved in the use of Ceftibuten are nausea, headache, vomiting, rashes or itching at the site of injection , itching, diarrhea, headache,upset stomach, etc.

Ceftibuten is available in the form of Oral suspension, Capsules, Tablets.

Ceftibuten is approved in Germany, Japan, Malaysia, India, U.K., and China.

Ceftibuten belongs to the pharmacological class of Third-generation cephalosporin antibiotics.

Ceftibuten works by inhibiting bacterial cell wall synthesis. Specifically, it targets the bacterial cell wall by binding to and inhibiting the activity of enzymes called penicillin-binding proteins (PBPs), which are responsible for cross-linking the peptidoglycan strands that make up the bacterial cell wall. This results in a weakened cell wall and ultimately, the death of the bacterial cell.

Ceftibuten has been approved to relieve symptoms and also for the treatment and maintenance of Acute bacterial exacerbations of chronic bronchitis, Acute bacterial otitis media, Pharyngitis/tonsillitis

After oral administration, Ceftibuten is rapidly and completely absorbed from the gastrointestinal tract, with a peak plasma concentration (Cmax) of approximately 2.5 mcg/mL occurring within 2 to 4 hours after a single 400 mg dose. The bioavailability of ceftibuten is approximately 50% and is not affected by food.

The onset of action of ceftibuten depends on the specific infection being treated and the severity of the condition. In general, it can take several days for symptoms to improve and for the infection to be completely eradicated.

The half-life of ceftibuten is approximately 2.5 to 3 hours in adults and may be longer in patients with renal impairment. The drug is primarily excreted unchanged in the urine, and dose adjustments may be necessary in patients with impaired renal function.

The duration of action of ceftibuten varies depending on the specific infection being treated, but in general, a 10-day course of treatment is recommended to ensure complete eradication of the infection. It is important to complete the full course of treatment as prescribed by a healthcare professional, even if symptoms improve before the medication is finished.

Ceftibuten is found to be available in the form of Oral suspension, Capsules, Tablets.

Ceftibuten can be used in the following treatment:

• Acute bacterial exacerbations of chronic bronchitis
• Acute bacterial otitis media
• Pharyngitis/tonsillitis

Ceftibuten can help to relieve symptoms and also for the treatment and maintenance of acute bacterial exacerbations of chronic bronchitis, acute bacterial otitis media, pharyngitis/tonsillitis.

Ceftibuten is approved for use in the following clinical indications:

• Acute bacterial exacerbations of chronic bronchitis

• Acute bacterial otitis media

• Pharyngitis/tonsillitis

• Acute bacterial exacerbations of chronic bronchitis: The recommended oral dose of Ceftibuten is 400 mg taken once daily for 10 days.
• Acute bacterial otitis media: The recommended oral dose of Ceftibuten is 400 mg taken once daily for 10 days.
• Pharyngitis/tonsillitis: The recommended oral dose of Ceftibuten is 400 mg taken once daily for 10 days.

Oral suspension: 90 mg per 5 mL

Capsule: 200 mg and 400 mg

Tablet: 400 mg

Oral suspension, Capsules, Tablets.

Dosage Adjustments in Kidney Patients:

• For infants aged 6 months and above, children, and adolescents with a creatinine clearance (CrCl) of 50 mL/minute or higher, Ceftibuten does not require any dose adjustment.
• For patients with CrCl ranging from 30 to 49 mL/minute, the oral dose of Ceftibuten is 4.5 mg/kg/dose taken once every 24 hours, up to a maximum dose of 200 mg/dose.
• For patients with CrCl ranging from 5 to 29 mL/minute, the oral dose of Ceftibuten is 2.25 mg/kg/dose taken once every 24 hours, up to a maximum dose of 100 mg/dose.

• For end-stage renal disease patients who undergo intermittent hemodialysis 2 or 3 times weekly, Ceftibuten is dialyzable, and around 65% of the drug is removed by a 2- to 4-hour hemodialysis session. The recommended oral dose of Ceftibuten after each hemodialysis session is 9 mg/kg/dose, up to a maximum dose of 400 mg/dose.
• Dosage Adjustments in Pediatric Patients:

Chronic Bronchitis: For the treatment of acute bacterial exacerbations of chronic bronchitis in adolescents and children aged 12 years or older, the recommended oral dose of Ceftibuten is 400 mg taken once daily for 10 days.

Acute Otitis Media: Ceftibuten is not included in the acute otitis media guidelines by the American Academy of Pediatrics. For infants aged 6 months and above and children under 12 years of age with acute otitis media, the oral dose of Ceftibuten is 9 mg/kg/dose once daily for 10 days, up to a maximum dose of 400 mg/dose. For children aged 12 years or older and adolescents, the recommended oral dose is 400 mg taken once daily for 10 days.

Streptococcus Infectoin: For the treatment of group A streptococcus pharyngitis/tonsillitis, narrow-spectrum cephalosporins such as cephalexin are preferred over broad-spectrum cephalosporins like Ceftibuten. For infants aged 6 months and above and children under 12 years of age, the recommended oral dose of Ceftibuten is 9 mg/kg/dose once daily for 10 days, up to a maximum dose of 400 mg/dose. For children aged 12 years or older and adolescents, the recommended oral dose is 400 mg taken once daily for 10 days.

There are found to be no specific dietary restrictions associated with the use of ceftibuten. However, it is important to follow a healthy, balanced diet to support the body's immune system during the treatment of bacterial infections.

Ceftibuten may be contraindicated under the following conditions:

• In patients who have had a previous hypersensitivity reaction to ceftibuten, other cephalosporins, penicillins, or any other beta-lactam antibiotics. Patients with a history of anaphylaxis, severe allergic reactions, or hypersensitivity to any component of the drug should not receive ceftibuten.
• In patients with a known history of cholestasis or other liver impairment, as it can lead to a further decline in liver function.
• In premature infants and neonates with a gestational age less than 4 weeks due to their immature renal function, which may result in increased accumulation of the drug and potential toxicity.
• In patients with a history of gastrointestinal disease or colitis, particularly Clostridium difficile-associated diarrhea, should exercise caution when using ceftibuten as it may exacerbate their condition.

The physician should closely monitor the patients and keep pharmacovigilance as follows:

Prior to administering therapy with Ceftibuten, it is essential to conduct a thorough investigation in order to determine whether the patient has a history of hypersensitivity reactions to ceftibuten, other cephalosporins, penicillins, or any other medications. Caution must be exercised when administering this medication to patients with a penicillin allergy because cross hypersensitivity among beta-lactam antibiotics had been clearly documented and might occur in up to 10% of patients. If a patient has an allergic reaction to Ceftibuten, the drug should be discontinued immediately. Serious acute hypersensitivity reactions might require treatment with epinephrine as well as other emergency measures, including oxygen, intravenous fluids, antihistamines, corticosteroids, pressor amines, as well as airway management, as clinically indicated.

Pseudomembranous colitis, which can range in severity from mild to life-threatening, has been reported with almost all antibacterial agents, including ceftibuten. As a result, it is crucial to consider this diagnosis in patients who develop diarrhea after receiving antibacterial treatment. Treatment with antibacterial agents can alter the normal flora of the colon and may allow for the overgrowth of clostridia, which produce a toxin that causes "antibiotic-associated colitis."

After the diagnosis of pseudomembranous colitis had been established, appropriate therapeutic measures should be initiated. In mild cases, discontinuing the medication may be sufficient. In moderate to severe cases, management with fluids and electrolytes, protein supplementation, and an antibacterial drug that is clinically effective against Clostridium difficile may be necessary.

It is recommended that patients avoid consuming alcohol while taking ceftibuten. Combining alcohol with ceftibuten may increase the risk of certain side effects such as stomach upset, nausea, vomiting, and dizziness. Additionally, alcohol consumption can weaken the immune system, making it more difficult for the body to fight infections. Therefore, it is best to avoid alcohol while taking ceftibuten to ensure the medication's efficacy and minimize the risk of side effects. Patients should consult with their healthcare provider for more information about alcohol consumption while taking ceftibuten.

Limited data suggest that ceftibuten is excreted in human milk after oral administration. Therefore, caution should be exercised when ceftibuten is administered to a nursing mother. The potential risk to the infant is unknown. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of ceftibuten to the mother.

Pregnancy Category B

Ceftibuten is classified as a pregnancy category B medication, which means that animal reproduction studies had not demonstrated a fetal risk but there are no adequate as well as well-controlled studies in pregnant women.

The use of ceftibuten during pregnancy should be considered only if clearly needed. It is important to weigh the potential benefits of ceftibuten against the potential risks to the fetus. Ceftibuten should be prescribed to pregnant women only if the potential benefits outweigh the potential risks.

There are no known food warnings related to the use of Ceftibuten. However, taking the medication with food may help to reduce stomach upset.

The adverse reactions related to Ceftibuten can be categorized as follows:

Common

• Diarrhea
• Nausea
• Abdominal pain
• Vomiting
• Headache
• Dizziness
• Skin rash
• Itching

Less Common

• Diarrhea
• Nausea
• Abdominal pain

Rare

• Severe skin reactions such as Stevens-Johnson syndrome or toxic epidermal necrolysis
• Anaphylactic reactions
• Clostridium difficile-associated diarrhea
• Hepatitis
• Nephritis
• Hemolytic anemia
• Thrombocytopenia

The clinically relevant drug interactions of Ceftibuten is briefly summarized here:

Theophylline: In a study conducted on twelve healthy male volunteers, each received a 200-mg ceftibuten capsule twice daily for six days. On the morning of the sixth day, a single intravenous infusion of theophylline (4 mg/kg) was administered, and the pharmacokinetics of theophylline were not affected. However, the effect of ceftibuten on the pharmacokinetics of orally administered theophylline has not been studied.

Antacids or H2-receptor antagonists: The impact of increased gastric pH on the bioavailability of drug ceftibuten had been assessed in 18 healthy adult volunteers. Each volunteer was given a single 400-mg ceftibuten capsule. A single dose of liquid antacid did not have an impact on the Cmax or AUC of ceftibuten. However, taking 150 mg of ranitidine every 12 hours for three days raised the Cmax of ceftibuten by 23% and the AUC by 16%. The clinical importance of these increases remains uncertain.

The following are the side effects involving Ceftibuten :

• Diarrhea
• Nausea
• Vomiting
• Stomach pain
• Headache
• Dizziness
• Rash
• Itching
• Hives
• Vaginal itching or discharge
• Mouth sores
• Swollen or tender tongue
• Unusual bleeding or bruising
• Yellowing of the skin or eyes (jaundice)
• Dark urine
• Pale stools
• Difficulty breathing or swallowing
• Chest pain

Pregnancy

Pregnancy Category B

Ceftibuten is classified as a pregnancy category B medication, which means that animal reproduction studies have not demonstrated a fetal risk but there are no adequate and well-controlled studies in pregnant women.

The use of ceftibuten during pregnancy should be considered only if clearly needed. It is important to weigh the potential benefits of ceftibuten against the potential risks to the fetus. Ceftibuten should be prescribed to pregnant women only if the potential benefits outweigh the potential risks.

Nursing Mothers:

Limited data suggest that ceftibuten is excreted in human milk after oral administration. Therefore, caution should be exercised when ceftibuten is administered to a nursing mother. The potential risk to the infant is unknown. 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.

Pediatric Use:

Ceftibuten has been studied in pediatric patients. In clinical trials, ceftibuten was found to be safe and effective in the treatment of acute bacterial exacerbation of chronic bronchitis, uncomplicated urinary tract infections, and pharyngitis/tonsillitis caused by susceptible bacteria in pediatric patients. The recommended dosage for pediatric patients depends on the type and severity of the infection and the patient's weight. It is important to note that ceftibuten should not be used in premature infants or neonates due to the risk of renal impairment. As with any medication, it is important to consult with a healthcare provider before giving ceftibuten to a pediatric patient.

Geriatric Use:

The pharmacokinetics of ceftibuten have been studied in a group of individuals aged 65 years and above, comprising of eight men and four women. These volunteers were given 200-mg capsules of ceftibuten twice a day for 3½ days, and the average Cmax was found to be 17.5 (3.7) µg/mL after 3½ days of dosing, as opposed to 12.9 (2.1) µg/mL after the first dose. Plasma levels of ceftibuten increased by 40% at steady state, but information about the renal function of these participants was not available. It is therefore unclear how clinically relevant these findings are for elderly patients using Ceftibuten Capsules. It may be necessary to adjust the dosage of ceftibuten in elderly patients.

Physicians should be knowledgeable and vigilant about the treatment and identification of overdosage of Ceftibuten.

An overdose of ceftibuten may cause symptoms such as nausea, vomiting, stomach pain, diarrhea, and allergic reactions. In case of an overdose, the patient should seek immediate medical attention.

Treatment of ceftibuten overdose involves supportive measures to manage symptoms, as well as measures to eliminate the drug from the body. Gastric lavage or induction of vomiting may be performed to remove any remaining drug in the stomach. Activated charcoal may also be given to help absorb the drug in the digestive system.

In addition, the patient may be given intravenous fluids to maintain hydration and electrolyte balance, and medications may be administered to manage symptoms such as nausea and vomiting.

Pharmacodynamics

Ceftibuten is a beta-lactam antibiotic that works by binding to and inhibiting the activity of bacterial cell wall synthesis. Specifically, it targets the penicillin-binding proteins (PBPs) that are responsible for cross-linking the peptidoglycan strands of the bacterial cell wall, leading to bacterial cell death.

Ceftibuten has a broad spectrum of activity against both gram-positive and gram-negative bacteria, including many strains of the Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis. Its mechanism of action and spectrum of activity make it a useful treatment option for a variety of bacterial infections, including community-acquired pneumonia, acute exacerbations of chronic bronchitis, and uncomplicated urinary tract infections.

The pharmacokinetics of ceftibuten are such that it is administered orally and is rapidly and well-absorbed from the gastrointestinal tract. It is widely distributed throughout the body, including into the lungs, where it is able to reach concentrations sufficient for activity against respiratory pathogens. Ceftibuten is eliminated from the body primarily by renal excretion.

Pharmacokinetics

Ceftibuten Capsules and Oral Suspension are both forms of the antibiotic ceftibuten, which is absorbed rapidly after oral administration. In healthy adult male volunteers, a single 400-mg dose of Ceftibuten Capsules resulted in an average plasma concentration of ceftibuten of 15 µg/mL after 1 hour and a Cmax of 17.9 µg/mL on day 7 of once-daily administration for 7 days. Ceftibuten accumulation in plasma at steady state was about 20%. In pediatric patients aged 6 months to 12 years who received a single 9-mg/kg dose of Ceftibuten Oral Suspension, the average plasma concentration of ceftibuten was 9.3 µg/mL after 1 hour and a Cmax of 13.4 µg/mL. The plasma concentrations of ceftibuten in pediatric patients are dose-proportional following single doses of Ceftibuten Capsules of 200 mg and 400 mg and of Ceftibuten Oral Suspension between 4.5 mg/kg and 9 mg/kg. Ceftibuten is 65% bound to plasma proteins, and the protein binding is an independent of plasma ceftibuten concentration. Ceftibuten has been found to penetrate bronchial mucosa and epithelial lining fluid, sputum, and middle-ear fluid, but data on its penetration into tonsillar tissue and cerebrospinal fluid are not available.

• https://reference.medscape.com/drug/Ceftibuten-ceftibuten-342508
• https://www.rxlist.com/Ceftibuten-drug.htm
• https://www.drugs.com/dosage/ceftibuten.html
• https://go.drugbank.com/drugs/DB01415
• https://www.pdr.net/drug-summary/Ceftibuten-ceftibuten-1540
• https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/050686s016lbl.pdf