Ceftibutene

Uses

Ceftibutene is used for the treatment of:

• Upper respiratory tract infections, including acute sinusitis; otitis media, pharyngitis, tonsillitis and scarlet fever.

• Lower respiratory tract infections including acute bronchitis, acute exacerbations of chronic bronchitis and acute pneumonia in patients appropriately considered for oral therapy ie, those with primary community-acquired infections.

• Urinary tract infections both complicated and uncomplicated infections.

• Enteritis and gastroenteritis caused by Salmonella, Shigella or E. coli.

Ceftibutene is also used to associated treatment for these conditions: Acute Bacterial Exacerbation of Chronic Bronchitis (ABECB), Acute Otitis Media, Acute Sinusitis, Acute Tracheobronchitis, Bacterial Infections, Bacterial Pneumonia, Lower Respiratory Tract Infection (LRTI), Lower Respiratory Tract Infection (LRTI) caused by susceptible bacteria, Pharyngitis, Skin and Soft Tissue Infections, Streptococcal Pharyngitis, Streptococcal tonsillitis, Superinfection bacterial, Tonsillitis, Upper Respiratory Tract Infection, Upper Respiratory Tract Infection caused by susceptible bacteria, Urinary Tract Infection caused by susceptible bacteria, Bacterial otitis media, Uncomplicated Lower Respiratory Tract Infection (LRTI), Uncomplicated Upper Respiratory Tract Infection, Uncomplicated Urethritis gonococcal

How Ceftibutene works

Ceftibutene exerts its bactericidal action by binding to essential target proteins of the bacterial cell wall. This binding leads to inhibition of cell-wall synthesis.

Dosage

Ceftibutene dosage

Adults (12 years of age and older): 400 mg once daily for 10 days.

Pediatric (<12 years of age): 9 mg/kg once daily for 10 days.

Maximum daily dose is 400 mg.

Suspension should be taken on an empty stomach (take 2 hr before or 1 hr after meals.);

Capsule may be taken with or without food.

Renal Impairment

Ceftibutene may be administered at normal doses in the presence of impaired renal function with creatinine clearance (Cr Cl) of 50 mL/min or greater. The recommendations for dosing in patients with varying degrees of renal insufficiency; Cr Cl > 50 mL/min: normal dosing schedule; Cr Cl 30-49 mL/min: 4.5 mg/kg or 200 mg once daily; Cr Cl 5-29 mL/min: 2.25 mg/kg or 100 mg once daily

Directions for mixing of Oral Suspension

First tap the bottle to loosen powder. Then add 45 ml water in two portions, shake well after adding each portion.

Final concentration of the suspension will be 90 mg per 5 mL.

After mixing, the suspension may be kept for 14 days and must be stored in the refrigerator. Keep tightly closed. Shake well before each use. Discard any unused portion after 14 days.

Side Effects

Common side effects may include Nausea, diarrhoea, and headache. Rarely, dyspepsia, gastritis, vomiting, abdominal pain & dizziness may occur.

Toxicity

Overdosage of cephalosporins can cause cerebral irritation leading to convulsions.

Precaution

Special precaution should be taken before use in Penicillin-allergic patients; patients with impaired renal function, history of complicated GI disease, particularly chronic colitis.

Interaction

High-dose aluminium-magnesium hydroxide antacid, ranitidine, and single dose intravenous theophylline. No significant drug interaction occurred. The effect of Ceftibutene on the plasma levels or pharmacokinetics of theophylline administered orally is not known. No other significant drug interactions have been reported to date.

Food Interaction

• Take separate from meals. Take ceftibuten oral suspension at least one hour after eating, or two hours before eating.
• Take with or without food. Separating the administration of ceftibuten from food is not required for ceftibuten capsules because the impact of food on bioavailability is less significant.

[Moderate] ADJUST DOSING INTERVAL: Food reduces the oral absorption and bioavailability of ceftibuten.

According to the product labeling, administration of ceftibuten oral suspension with a high-fat breakfast decreased the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) by 26% and 17%, respectively.

Administration of ceftibuten capsules with a standardized breakfast decreased the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) by 18% and 8%, respectively.

MANAGEMENT: To ensure maximal oral absorption, ceftibuten oral suspension should be taken at least two hours before or one hour after a meal.

Ceftibutene multivitamins interaction

[Moderate] ADJUST DOSING INTERVAL: Oral products containing zinc such as mineral supplements and multivitamins may interfere with the gastrointestinal absorption of cephalexin, ceftibuten or cephradine.

In one pharmacokinetic study (n=12), concurrent administration of zinc sulfate (250 mg, single oral dose) and cephalexin (500 mg, single oral dose) decreased cephalexin maximum concentration (Cmax) and systemic exposure (AUC; 0-inf) by 31.05% and 27.4%, respectively.

However, in the same study, when zinc sulfate was administered 3 hours after the cephalexin dose, no significant alteration in cephalexin pharmacokinetics were observed.

Oral medications or mineral supplements that contain zinc are recommended to be administered at least 3 hours after the cephalexin, ceftibuten or cephradine dose.

Ceftibutene Drug Interaction

Unknown: aspirin, aspirin, barium sulfate, barium sulfate, dexamethasone, dexamethasone, dextran, low molecular weight, dextran, low molecular weight, dextran, high molecular weight, dextran, high molecular weight, epoetin alfa, epoetin alfa, ginkgo, ginkgo, glipizide, glipizide, acetaminophen, acetaminophen, cholecalciferol, cholecalciferol

Ceftibutene Disease Interaction

Major: colitisModerate: renal dysfunction, diabetes, dialysis, liver disease, seizure disorders

Volume of Distribution

• 0.21 L/kg [adult subjects]
• 0.5 L/kg [fasting pediatric patients]

Elimination Route

Rapidly absorbed following oral administration.

Elimination Route

Ceftibutene is excreted in the urine; 95% of the administered radioactivity was recovered either in urine or feces.

Pregnancy & Breastfeeding use

Use in pregnancy & lactation: Pregnancy category B. There are no adequate and controlled studies in pregnant women or during labor and delivery. Because animal reproduction studies are not always predictive of human response, administration of Ceftibutene during such clinical situations should be weighed in terms of potential risk and benefit to both mother and fetus. Ceftibutene has not been detected in the milk of nursing mothers.

Use in children: Safety and efficacy of Ceftibutene in infants <6 months have not been established.

Contraindication

Ceftibutene is contraindicated in patients with known allergy to the cephalosporin group of antibiotics.

Special Warning

Use in children: Safety and efficacy of Ceftibutene in infants <6 months have not been established.

Adult Patients with Renal Impairment: Ceftibutene pharmacokinetics are not affected sufficiently to require dosage modifications unless creatinine clearance values are <50 mL/min. If creatinine clearance is from 49 to 30 mL/min, the daily dose should be decreased to 200 mg. With creatinine clearance values of 29 to 5 mL/min, the recommended daily dose is 100 mg.

If alteration of dosing frequency is preferred, a 400-mg dose of Ceftibutene may be administered every 48 hrs (every 2 days) to a patient with a creatinine clearance of 30-49 mL/min, and every 96 hrs (every 4 days) if creatinine clearance is 5-29 mL/min.

In patients undergoing hemodialysis 2 or 3 times weekly, a single dose of Ceftibutene 400 mg may be administered at the end of each hemodialysis session.

Acute Overdose

Overdose symptoms may include seizure (convulsions).

Interaction with other Medicine

No significant drug interactions have been reported to date. Food taken concomitantly does not interfere with the efficacy of capsules. However, the rate and extent of absorption of suspension may be affected by concomitant food intake.

Storage Condition

Store in a cool (below 30º C) dry place, away from light and children. Store in a cool (below 30º C) dry place, away from light and children.

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