Ceftibuten - Uses, Efficacy, Warnings, Pharmacology, and Side Effects

Overview:

Ceftibuten is an antibiotic that is usually prescribed for certain inflammatory conditions that are caused by bacterial infections. Moreover, it treats susceptible bacterial infections in major body parts, including the throat, ear, respiratory tract, and urinary tract. It comes in two significant forms: capsules and oral suspension (liquid). So, Ceftibuten is to be taken by mouth. The recommended frequency of this medication is once daily for about ten days.

Ceftibuten is a broad-spectrum antibiotic that is typically used for the treatment of a range of bacterial infections. Specifically, it is used to treat acute bacterial otitis media, acute exacerbations of chronic bronchitis (ABECB), tonsillitis, and pharyngitis. At times, it is also for other treatments, such as urinary tract infections, enteritis, pneumonia, and gastroenteritis.

Drug Class:

Ceftibuten is a typical antibiotic that belongs to the class of drugs called cephalosporin antibiotics. They are the class of beta-lactam antibiotics with the original derivation from the Acremonium fungi (previously known as Cephalosporium). They are commonly used to manage a distinct variety of infections resulting from both gram-positive and gram-negative bacteria. Ceftibuten belongs to the third generation of Cephalosporins, the third group of Cephalosporin antibiotics discovered.

Prescriptions:

Ceftibuten is prescribed for treating people with mild to moderate degrees of infection caused by susceptible strains of bacteria in the following distinctive conditions.

• Acute Bacterial Exacerbations of Chronic Bronchitis: The acute exacerbation of chronic bronchitis refers to the acute or sudden worsening of the clinical manifestations of the disease bronchitis. This includes worsening symptoms like breathlessness, wheezing, coughing, and sputum purulence. Ceftibuten is prescribed in this condition for those infections that are caused by susceptible strains such as Haemophilus influenza (particularly Beta-lactamase producing strains), Streptococcus pneumoniae (only Penicillin-susceptible strains), and Moraxella catarrhalis (particularly Beta-lactamase producing strains).

• Acute Bacterial Otitis Media: Acute otitis media is described as a painful infection (caused by bacteria) of the middle ear. It is considered to be the most prevailing pediatric diagnosis following an upper respiratory tract infection in the emergency room, though it occurs at any age. It results when the middle ear area behind the eardrum becomes infected and inflamed due to susceptible microbes. Ceftibuten is indicated for treating acute bacterial otitis media caused by Hemophilus influenza (particularly beta-lactamase-producing strains), Streptococcus pyogenes, and Moraxella catarrhalis (specifically beta-lactamase-producing strains).

• Pharyngitis: Pharyngitis is the painful and inflammatory condition of the mucous membrane associated with the oropharynx. It is commonly referred to as a sore throat. It can be caused by either bacterial or viral infection. Here, Ceftibuten is used against the bacterial infection caused by Streptococcus pyogenes.

• Tonsillitis: It is an inflammatory condition of the two oval-shaped tissues present at the back region of the throat called the tonsils. It is generally caused by a viral infection but less commonly by bacteria. The typical symptoms of tonsillitis include sore throat and pricking pain while swallowing. Ceftibuten is used against bacterial infections of tonsillitis, particularly Streptococcus pyogenes.

Drug and Its Strength:

Ceftibuten is an orally administered drug agent with two specific forms: capsules and oral suspension (liquid).

1. Ceftibuten Capsules: White opaque capsules containing 400 mg of Ceftibuten dihydrate.

2. Ceftibuten Oral Suspension: It is an off-white cream-based color powder that contains Ceftibuten amounting to 90 mg/5 mL or 180 mg/5 mL after reconstitution.

For Patients:

What Is Bronchitis?

Bronchitis is a common inflammatory condition of the airways (lining of the bronchial tubules) that typically carries oxygen from and to the lungs. So, the bronchial tubes become inflamed and swollen due to infection. The clinical manifestation of bronchitis includes coughing, often with mucus production. The causes include viruses, bacteria, irritants, and pollutants. The susceptible bacteria that commonly cause bronchitis are Bordetella pertussis, Chlamydia pneumonia, and Mycoplasma pneumonia. Bronchitis can occur in acute (short-term) and chronic (long-term), whereas the acute form is more prevalent.

• Acute Bronchitis: Acute bronchitis commonly occurs due to viral infection, which usually resolves on its own over time. Most people with acute forms do not require medical treatment. Bacteria can also cause it.

• Chronic Bronchitis: Chronic bronchitis is diagnosed when the person has a cough with mucus on most days of the month for about three months a year. Chronic bronchitis is often accompanied by chronic obstructive pulmonary disease (COPD).

Symptoms of Bronchitis:

The predominant symptom of bronchitis is a persistent cough with sputum lasting for about three weeks. A cough with mucus is common, but people can also experience a nagging dry cough.

The other symptoms of bronchitis include the following:

• Wheezing.

• Shortness of breath- Dyspnea.

• Tiredness.

• Fever.

• Runny nose.

Bronchitis or bronchial tube inflammation can lead to many complications and other conditions, such as acute exacerbations (sudden worsening of symptoms), middle ear infections, tonsil inflammation, and respiratory tract infections.

How Does Ceftibuten Work?

Ceftibuten is used to treat several infections that are typically caused by bacteria. Infections include bronchitis, inflammatory throat, tonsil and ear conditions. Ceftibuten belongs to the class of drugs called cephalosporin antibiotics. This works by killing the bacteria and inhibiting their growth. Nevertheless, Ceftibuten-like antibiotics are not meant to treat flu, colds, or other viral infections.

What Is the Dosage of Ceftibuten?

The doctors recommend the appropriate form, dosage, and strength, considering the patient's age, the condition or infection to be treated, the severity of the disease, and other general medical conditions. The usual recommendation is listed below:

1. Adults:

400 mg of Ceftibuten capsules once daily for ten days is generally recommended for adults.

2. Pediatrics:

• For children weighing under 45 pounds or 6 to 12 years old, 9 mg/kg or 400 mg/day for ten days.

• For children greater than 12 years old or greater than 45 pounds, the dosage recommendation is similar to that for adults.

• Safety and efficacy have not been determined for infants under six months of age.

What Are the Things to Consider and Inform the Doctor Before Using Ceftibuten?

• Inform the doctor and pharmacist if one is allergic to Ceftibuten or any other ingredient listed in the prescribed formulation. Addedly, tell the doctor if one has a known allergy to other cephalosporin groups of antibiotics, including Cefaclor, Cefepime, Cefadroxil, Cefdinir, Cefotaxime, Ceftaroline, Ceftazidime, Ceftriaxone, Cephalexin, Cefuroxine, and Penicillin antibiotics.

• One should tell the doctor whether one is taking prescription medications, non-prescription tablets, herbal products, vitamins, or other nutritional supplements. The doctors might alter the dosage or do some conscious monitoring.

• Inform the doctor if a person has ever had medical conditions or illnesses. Specifically, the presence of certain gastrointestinal diseases like colitis (an inflammatory condition presenting swelling of the colon, a part of the large intestine) and other kidney diseases should be noted.

• Tell the doctor if one has diabetes; the doctor might not recommend Ceftibuten oral suspension medication since it contains sucrose (a form of sugar).

• If a woman is pregnant or has any plans for pregnancy, inform the doctor without fail. Addedly, call and tell the doctor if one gets pregnant during Ceftibuten treatment.

• Inform the doctor if one is breastfeeding.

How Is Ceftibuten Administered?

Ceftibuten is available as a capsule and an oral suspension (liquid) to be taken orally. It is generally given once a day for about ten days.

Directions for Taking Ceftibuten Capsules:

• Ceftibuten capsules are to be taken by mouth.

• Take the capsules according to the frequency and duration prescribed by the doctor.

• The Ceftibuten capsules can be administered with or without food intake.

• One should swallow the capsule whole with a glass of water.

• Therefore, one should never chew or break the capsules.

• One should not stop taking Ceftibuten capsules without the doctor’s consent.

• It is recommended to complete the number of drugs as per the physician’s prescription, despite any improvement in the condition.

Directions for Ceftibuten Oral Suspension:

• One must take the Ceftibuten oral suspension on an empty stomach, so take it at least two hours before or one hour after the meal.

• Measure the appropriate medicine with a marked measuring cup or syringe before reconstitution (mixing).

• Shake the oral suspension before each use.

• After mixing, the oral suspension can be kept in the refrigerator for about 14 days.

• Keep them firmly closed.

Dietary Considerations:

No specific dietetic consideration is necessary unless the doctor utters any restrictions during Ceftibuten treatment. So, one can stick with a normal and well-balanced diet.

Important Note:

One should take antibiotics only when required or in the case of an infection. Taking antibiotics when they are not required could raise the risk of acquiring an infection later, and that also prevents antibiotic therapy.

How Effective Is Ceftibuten?

Ceftibuten is considered safe and effective in the treatment of several bacterial infections. It has been proven that Ceftibuten exerts good activity against several gram-negative bacteria, though its action against Gram-positive bacteria needs to be sufficiently good. Moreover, Ceftibuten is an effective medication for treating certain upper and lower respiratory tract infections like bronchitis, tonsillitis, pharyngitis, and middle ear infections caused by respiratory infections caused by bacteria. It works efficiently by killing the bacteria.

What Are the Side Effects of Ceftibuten?

Though Ceftibuten is safe to use, it can induce certain unwanted effects in many individuals. The common side effects of Cetibuten are as follows, which can go away over time. Tell the doctor and seek professional help if these symptoms become severe, distressing daily functions.

• Stomach pain.

• Diarrhea.

• Nausea.

• Vomiting.

• Heartburn.

• Headache.

• Dizziness.

In rare cases, Ceftibuten can cause some serious side effects. These side effects require emergency medical treatment, so reach out to the doctor right away if one experiences any of the following symptoms:

• Allergy Reactions: Individuals having allergies to this group of medications could experience symptoms like rashes, itching, hives, swelling of the face, breathing ailments, and wheezing.

• Gastrointestinal Ailments: Gastrointestinal problems like watery stools, stomach cramps, bloody stools, abdominal pain, or fever can occur during Ceftibuten treatment or for up to certain months following the stoppage of treatment.

• Signs of Infection: The signs of infection, including fever, sore throat, chills, and other signs, could result.

Missed Dose:

In the event of a missed dose, it is recommended to take the missed dose as fast as possible. Nevertheless, if it is nearly time for the subsequent dose, consider skipping the missed dose and continuing the routine dosing schedule. One should not take a double dose of Ceftibuten to compensate for the missed dose.

Overdose:

In the case of an overdose of Ceftibuten, reach out to the emergency services or poison control helpline. The toxic concentration of drugs in the body can have undesired effects, which can often be life-threatening. So, one should seek medical help at the earliest possible time.

Storage:

• It is advised to store the Ceftibuten capsules at a temperature of 2 to 25 degrees Celsius. Consider replacing the cap rigidly after every opening.

• Store Ceftibuten oral suspension powder at 2 to 25 degrees Celsius before reconstitution (mixing).

• After reconstitution, the Ceftibuten oral suspension can remain stable for about 14 days if stored in a refrigerator temperature of 2 to 8 degrees Celsius.

• So, one should discard the unused portion safely if it has been more than 14 days.

For Doctors:

Clinical Data for Ceftibuten:

Generic Name: Ceftibuten.

Drug Class: Third-generation cephalosporin antibiotics.

Route of Administration: Oral.

Chemical Formula: C15H14N4O6S2.

Molar Mass: 410.42 g.mol -1.

Indication:

Ceftibuten is chiefly indicated for the treatment of the bronchitis condition called the acute bacterial exacerbations of chronic bronchitis (ABECB), pharyngitis, tonsillitis, and bacterial otitis media.

Associated Conditions:

• Acute bacterial exacerbations of chronic bronchitis.

• Acute otitis media.

• Lower respiratory tract infection.

• Lower respiratory tract infections are caused by susceptible bacteria.

• Bacterial infections.

• Acute tracheobronchitis.

• Bacterial pneumonia.

• Pharyngitis.

• Streptococcal pharyngitis.

• Skin and soft tissue infections.

• Upper respiratory tract infection.

• Upper respiratory tract infections are caused by susceptible bacteria.

• Susceptible bacteria cause urinary tract infections.

• Bacterial otitis media.

• Uncomplicated lower respiratory tract infection.

• Uncomplicated upper respiratory tract infection.

• Uncomplicated urethritis- gonococcal.

• Tonsillitis.

• Streptococcal tonsillitis.

• Bacterial superinfections.

What Are the Pharmacological Aspects of Ceftibuten?

Mechanism of Action:

Ceftibuten belongs to the third-generation cephalosporins that inhibit cell wall mucopeptide synthesis. So, Ceftibuten employs its bacterial action by binding to the cell wall's vital target proteins, particularly penicillin-binding proteins (PBOs). Then, it inhibits the overall bacterial cell wall synthesis following the binding process.

Absorption:

1. Ceftibuten Capsules:

• Ceftibuten ensures rapid and good absorption after oral administration of Ceftibuten capsules.

• The average peak serum concentration (Cmax) was estimated to be 17.9 mg/mL on day seven when Ceftibuten capsules were taken once a day for seven successive days.

• Hence, the accumulation of Ceftibuten in plasma is nearly 20 percent at a steady state.

2. Ceftibuten Oral Suspension:

• Similar to capsules, Ceftibuten undergoes well and rapid absorption following the oral administration of Ceftibuten oral suspension.

• The oral bioavailability of the oral suspension form of Ceftibuten has not been designated.

• However, the plasma concentrations of Ceftibuten in the pediatric population are known to be dose proportional following single dosage Ceftibuten capsules of 200 mg and 400 mg and oral suspension forms between 4.5 mg/kg and 9 mg/kg.

Distribution:

1. Ceftibuten Capsules:

The standard assumed volume of distribution of Ceftibuten in six adult patients was estimated to be 0.21 L/kg.

2. Ceftibuten Oral Suspension:

The average assumed volume of distribution of Ceftibuten in 32 fasting pediatric individuals was known to be 0.5 L/kg.

Protein Binding:

• The plasma protein binding capacity is about 65 percent.

• The protein binding is irrelevant to the plasma Ceftibuten concentration.

Tissue Preparation:

• Bronchial Secretions: According to a study involving 15 adults administered a single dosage of 400 mg of a Ceftibuten capsule and cataloged for a bronchoscopy procedure, the assumed mean concentrations of Ceftibuten in the bronchial mucosa and epithelial lining fluid were 37 percent, and 15 percent consecutively, of the total plasma concentrations.

• Sputum: The sputum Ceftibuten level is approximately seven percent of the concurrent plasma Ceftibuten level. According to a study with 24 adult patients who were administered Ceftibuten 200 mg twice daily or 400 mg once daily, the average Cmax in sputum was about 1.5 mg/mL, resulting two hours after the dose. Subsequently, the Cmax in plasma was detected at 17 mg/mL, which occurred at two hours post-dose.

• Middle-Ear Fluid: As per the study of the involvement of 12 pediatric patients who were administered Ceftibuten at a dosage of 9 mg/kg, Ceftibuten middle-ear fluid area under the curve (AUC) was determined to be approximately 70 percent of the AUC of plasma. The Cmax values were about 14.3 + or - 2.7 mg/ mL in middle-ear fluid four hours after the dose, and Cmax was 14.5 + or - 3.7 mg/ mL at two hours post-dose.

• Tonsillar Tissue: Data regarding the Ceftibuten tissue penetration into the tonsillar tissue have not been determined.

• Cerebrospinal Fluid: Data is unavailable for Ceftibuten penetration into the cerebrospinal fluid.

Metabolism:

• A study of six healthy individuals administered radiolabeled Ceftibuten demonstrates that cis-Ceftibuten is assumed to be a significant component in both the urine and plasma.

• So, nearly ten percent of the Ceftibuten is being transferred to the trans-isomer.

• The antimicrobial potency of a trans-isomer is relatively one to eight times that of a cis-isomer.

Excretion:

• Ceftibuten is excreted by urine.

• However, approximately 95 percent of the administered radioactivity dose was recovered in the urine or feces.

• In a study of six healthy adult male individuals, about 56 percent of the Ceftibuten administered dose was recovered in urine and about 39 percent in the feces within 24 hours.

• As renal excretion is a profound pathway of excretion of Ceftibuten, dosage adjustment is required for patients with renal impairments and dysfunction and individuals undergoing hemodialysis.

Half-Life:

The estimated half-life of Ceftibuten was to be about 2.4 hours.

Effects of Food on Administration:

Food has a significant effect on the bioavailability of Ceftibuten in both capsules and oral suspension. The food tends to decrease the plasma concentration and the area of the curve (AUC). It is also known that food can often delay the Tmax of Ceftibuten.

Adverse Effects of Ceftibuten:

1. Common (1 to 10 Percent):

• Increased blood urea nitrogen.

• Diarrhea.

• Nausea.

• Vomiting.

• Headaches.

• Increased eosinophils.

• Decreased hemoglobin levels.

• Thrombocytosis.

• Dyspepsia.

• Abdominal pain.

• Dizziness.

• Increased alanine transaminase.

• Increased bilirubin.

2. Rare (Less Than 1 Percent):

• Candidiasis.

• Anorexia.

• Constipation.

• Fatigue.

• Insomnia.

• Paresthesia.

• Dysuria.

• Diaper rash.

• Rigors.

• Agitation.

• Dry mouth.

• Dyspnea.

• Irritability.

• Nasal congestion.

• Leukopenia.

• Increased creatinine.

• Increased transaminase.

What Are the Contraindications to Ceftibuten?

• Hypersensitivity: Ceftibuten is strictly contraindicated in individuals with known or documented allergies to Ceftibuten or the cephalosporin group of antibiotics in general.

What Are the Significant Warnings and Cautions for Ceftibuten?

• A cautious inquiry should be made to determine the history of hypersensitivity reactions to Ceftibuten, Penicillins, other Cephalosporins, and other common drugs before the initiation of treatment.

• Cross hypersensitivity reactions within beta-lactam antibiotics have been established and might result in nearly ten percent of the individuals with known penicillin allergy. So, caution should be taken if Ceftibuten is to be prescribed for penicillin-sensitive individuals.

• If there is an allergic reaction, discontinuation of the drug is recommended.

• Nevertheless, severe acute hypersensitivity reactions might demand acute treatment with epinephrine with other emergency methods such as oxygen, intravenous antihistamines, intravenous fluids, pressor amines, corticosteroids, and appropriate airway management.

• Pseudomembranous colitis has been reported with antibacterial treatments, and it might have mild to potentially life-threatening complications. As this can also occur with Ceftibuten treatment, it is essential to consider this form of diagnosis in individuals who have diarrhea episodes after Ceftibuten administration. Following the diagnosis of pseudomembranous colitis, initiate appropriate therapeutic actions. In mild cases, discontinuation of drugs can be effective. In moderate to severe cases, consider treatments including fluids, protein supplementation, electrolytes, and antibacterial medications potent against Clostridium difficile.

Other Precautions:

• Ceftibuten oral suspension is not generally recommended for diabetics since it contains about one gram of sucrose per teaspoon.

• Consider dosage modifications in cases of severe renal impairment because prolonged use might lead to superinfections. Consider dosage adjustment, especially in individuals with a creatinine clearance drop below 50 mL/minute.

• Dosage adjustment is also required in hemodialysis cases since Ceftibuten is known to be promptly dialyzable. There should be significant caution in hemodialysis cases, and immediate administration of Ceftibuten should be considered following dialysis..

• In conjunction with other broad-spectrum antibiotics for long-term treatment, Ceftibuten might cause the potential emergence and development of resistant organisms. In such cases, observe conscientiously and take appropriate measures if any superinfection results.

• Caution should be taken while prescribing Ceftibuten medication to people with a history of gastrointestinal disorders, specifically colitis.

• Use cautiously in the case of seizure disorders.

Considerations for Specific Populations:

• Pregnancy: Ceftibuten did not present any teratogenic effect in the pregnant rats and rabbits at oral dosages up to 400 mg/kg/day and 40 mg/kg/day, respectively. Animal studies validate that Ceftibuten does not harm the fetus. However, inadequate studies are validating its use and safety in pregnant women. As animal-based reproduction studies are not prognostic for the human response, it is recommended to use this drug only if required.

• Lactation: The studies do not reveal whether Ceftibuten can be excreted in human milk. Nevertheless, exercise caution during administration in the case of lactating women since many drugs are generally excreted in human milk.

• Geriatrics: The standard adult dosage prescription can be followed in geriatric individuals. However, this age group requires close monitoring, including monitoring their renal functions. In cases of renal insufficiency, consider dosage modification.

• Pediatrics: Ceftibuten's use, safety, and efficacy in children below six months of age have not been determined.