Reviewed by ehealthlyf.com and last updated on 04/02/2023
Generic name: Cefuroxime Axetil (Oral), Cefuroxime Sodium(IV or IM)
Drug class: second-generation cephalosporin
Dosage form: Injectable powder for injection (1.5g, 7.5g, 750mg), oral tablet (250mg, 500mg).
Brand names: Zinnat, Ceftin, Kefurox, Zinacef, Zinacef Twist Vial, Zinacef ADD-Vantage.
Regulatory Status: RX
Generic availability: Yes
Table of Contents
What Is Cefuroxime?
- Cefuroxime, a prescription medicine, is a cephalosporin antibiotic used to treat bacterial infections of the ears, throat, lungs, nose, skin, kidney, urinary bladder, bones, or joints.
- It also treats sepsis, gonorrhoea, early lymph disease, and sinusitis.
- Sometimes a cefuroxime injection is given before or after surgery to prevent infection.
- It is not known if Ceftin is safe for children below 3 months of age.
- Antibiotics such as cefuroxime will not work for the common cold or other similar infections.
- Antibiotic resistance develops when antibiotics are used inappropriately.
Chemistry
Cefuroxime is present in CEFTIN tablets and CEFTIN for oral suspension as cefuroxime axetil. CEFTIN is an oral semi-synthetic cephalosporin antibacterial medication.
Chemical name
(1-(acetoxy)ethyl ester of cefuroxime), is (RS)-1-hydroxyethyl(6R,7R)-7-[2-(2-furyl)glycoxyl-amido]-3-(hydroxymethyl)- 8-oxo-5-thia-1-azabicyclo[4.2.0.]-oct-2-ene-2-carboxylate,72-(z)-(o-methyl-oxime),1-acetate 3-carbamate.
Molecular formula: C20H22N4O10S
Molecular weight: 510.48.
Mechanism of Action
- Cefuroxime belongs to a class of second-generation antibiotics. They are broad-spectrum antibiotics, as they are effective against a wide range of bacteria.
- Compared to first-generation cephalosporins, second-generation cephalosporins have enhanced activity against gram-negative bacteria and beta-lactamase.
- Cephalosporins are bactericidal (they kill bacteria), and they work by blocking the activity of enzymes responsible for the formation of peptidoglycan, a vital component of the bacterial cell wall.
Pharmacokinetics
Absorption
Bioavailability: Fasting 37%, postprandial 52%
Peak serum Time: 2-3 hours(PO);15-60 minutes (IM);2-3 min(IV)
Distribution
Distributed all over the body tissues and fluids, including cerebrospinal fluid(CSF)
Protein-bound: 33-50%
Metabolism
Partially metabolized in the liver
Elimination
Half life:1-2 hours (prolonged with renal impairment
Excretion; urine( 66-100% as unchanged drugs)
What Are the Ingredients in Cefuroxime Axetil?
The film-coated tablets have a cefuroxime axetil equivalent dose of 250 or 500 mg.
Cefuroxime axetil tablets
Active ingredients: Cefuroxime axetil
Inactive ingredients: Colloidal silicon dioxide, croscarmellose sodium, hydrogenated vegetable oil, hypromellose, methylparaben, microcrystalline cellulose, propylene glycol, propylparaben, sodium benzoate, sodium lauryl sulphate, titanium dioxide.
Cefuroxime axetil oral suspension
Active ingredients: Cefuroxime axetil
Inactive ingredients: Acesulfame potassium, aspartame, povidone K30, stearic acid, sucrose, tutti-frutti flavouring, and xanthan gum
When reconstituted with water, oral suspension yields the same amount of cefuroxime as cefuroxime axetil 125 mg or 250 mg per 5 ml.
What are the uses of Cefuroxime?
Used to treat certain bacterial infections including
- Pharyngitis
- Otitis media
- Sinusitis
- Bronchitis
- Urinary tract infections
- Gonorrhea
- Lyme disease
- Impetigo
Dosage Forms and Strength
Generic name: cefuroxime
Form: oral tablet
Strengths: 125mg, 250mg, 500mg
Dose for Pharyngitis( Mild to Moderate)
The maximum dose is 500mg/day.
| Adult dose(18 years and above) | Child dose(13-17 years old) | Child dose (3 months-12 years old) |
| Tablets | Tablets | Suspension |
| Tablets 250 mg orally twice a day for 10 days. | Tablet 250 mg orally twice a day for 10 days. | Suspension of 20 mg/kg/day orally in two divided doses for 10 days. |
Dose for Tonsillitis (Mild to Moderate)
The maximum dose is 500 mg/day.
| Adult dose (18 years and above) | Child dose(13-17 years old) | Child dose (3 months-12 years) |
| Tablets | Tablets | Suspension |
| 250 mg orally twice a day for 10 days | 250 mg orally twice a day for 10 days | 20mg/kg/day orally in two divided doses for 10 days |
Dose for Acute Otitis Media
Maximum dose: 1g/day
| Age Group | Dosage Form | Dose | Days |
| Adult dose (18 years and above) | Tablets | 250 mg every 12 hours | 10 |
| Child dose (13-17 years old)(FDA Dosage) | Tablets | 250mg orally twice a day | 10 |
| Child dose (6-12 years with mild to moderate illness)(guideline dosage) | suspension | 30mg/kg/day orally in two divided doses | 5-7 |
| Child dose (3 months to 12 years) | Suspension | 30mg/kg/day orally twice a day | 10 |
| 2-5 years with mild to moderate illness (guideline dosage) | Suspension | 30 mg/kg/day in two divided doses | 7 |
Dosage for Acute Maxillary Sinusitis (Mild to Moderate)
Maximum dose:1g/day
| Adult dose (18 years and older) | Child dose (13–17 years old) | Child dose (3 months–12 years old) |
| Tablets | Tablets | Suspension |
| 250mg every 12 hours for 10 days | 250mg every 12 hours for 10 days | 30 mg/kg/day orally in two divided doses for 10 days |
General information
It has not been found to be safe or effective in children under the age of three months.
Warning
- Cefuroxime tablets and suspension cannot be substituted on an mg/mg basis.
- Children who cannot swallow tablets can be given cefuroxime suspension.
Dosage for Acute Bronchitis( Mild to Moderate)
| Age Group | Dose | Days |
| Adult dose (18 years old and above) | 250mg or 500 mg twice a day | 10 |
| Child dose (13–17 years old) | 250mg or 500 mg twice a day | 10 |
This medication should not be used in children with acute bronchitis of age less than 13
Secondary infection of acute bronchitis(mild to moderate)
| Adult dose (18 years and above) | Child dose (13-17 years old) |
| 250 mg or 500 mg twice a day for 5-10 days | 250 mg or 500 mg twice a day for 5-10 days |
Dosage for Uncomplicated Infections of the Skin or Subcutaneous Tissue
| Adult dose (18 years and above) | Child dose (13-17 years old) |
| 250mg or 500 mg twice a day for 10 days | 250mg or 500 mg twice a day for 10 days |
This medication should not be given to children under the age of 13.
Dosage of Uncomplicated Urinary Tract Infections
| Adult dose (18 years and above) | Child dose(13-17 years old) |
| 250 mg or 500 mg twice a day for 7-10 days | 250 mg or 500 mg twice a day for 7-10 days |
This condition is not typical in children under 13 years old.
Dosage for Uncomplicated Gonorrhoea
| Adult dose (18 years and above) | Child dose (13-17 years old) |
| 1000 mg as a single dose | 1000 mg as a single dose |
No dosage information is available for children below 13.
Dosage for Early Lyme Disease
| Adult dose (18 years and above) | Child dose (13-17 years old) |
| 500mg orally twice a day for 20 days-FDA dosage 500 mg orally twice a day for 14 days-guideline dosage | 500 mg twice a day for 20 days |
No dosage information is available for children below 13.
Dosage for Impetigo
Child dose(3 months-12 years)-suspension: 30mg/kg/day orally in 2 divided doses for 10 days.
Maximum dose: 1 g/day.
Dose adjustments
Renal impairment
- Creatinine clearance level 30ml/min or greater-NO adjustment needed.
- Creatinine clearance level 10 to <30ml/min-Administer standard individual dose every 24 hours.
- Creatinine clearance level <10ml/min without hemodialysis-Administer standard individual dose every 48 hours
- Hemodialysis: Administer 1 single additional standard dose at the end of each dialysis.
Adult and pediatric patient dosage guidelines
| Infection | Dosage | Duration |
| Adults and adolescents (13 years and older) | ||
| Pharyngitis/tonsilitis (mild to moderate) | 250mg every 12 hours | 10 |
| Acute bacterial maxillary sinusitis( mild to moderate) | 250mg every 12 hours | 10 |
| Acute exacerbations of chronic bronchitis (mild to moderate) | 250 or 500 mg every 12 hours | 10 |
| Uncomplicated skin and skin structure infections | 250 or 500 mg every 12 hours | 10 |
| Uncomplicated urinary tract infections | 250mg every 12 hours | 10 |
| Uncomplicated gonorrhoea | 1000mg | Single dose |
| Early lymph disease | 500mg every 12 hours | 20 |
| Pediatric patients below 13 years of age who can swallow whole tablets | ||
| Acute bacterial otitis media | 250mg every 12 hours | 10 |
| Acute bacterial maxillary sinusitis | 250mg every 12 hours | 10 |
Dosage of CEFTIN suspension for pediatric patients ( 3 months to 12 years)
| Infection | Recommended daily dose | Maximum daily dose | Duration |
| Pharyngitis/ tonsilitis | 20 mg/kg | 500 mg | 10 |
| Acute bacterial otitis media | 30 mg/kg | 1000 mg | 10 |
| Acute bacterial maxillary sinusitis | 30 mg/kg | 1000 mg | 10 |
| Impetigo | 30 mg/kg | 1000 mg | 10 |
Dosing in Adults With Renal Impairment
| Creatinine clearance(ml/min) | Recommended Dosage |
| ≥30 | No adjustment needed |
| 10 – <30 | The standard individual dose is given every 24 hours |
| <10 ( Without hemodialysis) | The standard individual dose is given every 48 hours |
| Hemodialysis | A single additional standard dose should be given at the end of each dialysis |
Preparation of Ceftin Oral Suspension
- Shake the bottle and loosen the powder.
- Remove the cap.
- Add in the water for reconstitution till the mark is provided in the bottle.
- Invert the bottle so that water rises through the powder.
- Shake vigorously in a diagonal direction at least for 1 minute.
- After reconstitution, a 1hr gap should be provided before giving to the patient.
Administration (Important Instructions)
Cefuroxime axetil
- Administer tablets and oral suspensions as per the guidelines provided.
- Ceftin tablets can be taken with or without food, whereas oral suspension should be taken with food.
- The paediatric patient who cannot swallow tablets can be provided with an oral suspension as crushed tablets have a bitter taste.
Administration
Cefuroxime sodium
IV incompatibilities
Additives: Aminoglycosides, sodium bicarbonate, ciprofloxacin, ranitidine.
Syringe: Doxapram
Y-site: Azithromycin, filgrastim, midazolam, fluconazole, vinorelbine, vancomycin, clarithromycin, cisatracurium(potentially; compatible at low Concentration [0.1mg/ml]
IV Compatibilities
Solution: D5W, NS
Additive: Clindamycin, midazolam, netilmicin, furosemide, gentamicin (incompatible with total parenteral nutrition [TPN]), metronidazole, and floxacillin.
Y-site(partial list): Allopurinol, propofol, acyclovir, linezolid, diltiazem, amiodarone, tacrolimus, ondansetron, morphine sulfate, milrinone
IV preparation
Direct injection: Reconstitute in 8 ml (for a 750 mg vial) or 16 ml(for a 1.5 g vial) to obtain approximately 90 mg/ml of solution.
Infusion: Reconstitute in 100 ml D5W or NS to obtain 7.5 mg/ml (750mg vial) or 15 mg/ml(1.5 vials)solution
IM preparation
Reconstitute 750mg in 3ml SWI to obtain an approximately 220mg/ml solution.
IV administration
Direct injection:
- Inject directly into the vein over 3-5 minutes or slow injection.
Infusion:
- Infuse intermittently over 15-60 minutes
How to Use the Cefuroxime?
- Follow the instructions provided in your prescription. Cefuroxime oral is taken by mouth.
- Swallow the tablet and do not crush it. You can consume food or consume it without food.
- Shake the oral suspension powder and mix it with the liquid provided, and prepare the corresponding dose. Take cefuroxime suspension only with food.
- Cefuroxime Axetil tablets should only be used for the short-term treatment of bacterial infections. It should not be used for viral infections such as the common cold.
- If you stop the drug suddenly or don’t take as much as prescribed, the infection may worsen.
- If you miss a dose or don’t take it as scheduled in the prescription, the medication may not work as planned, as a certain amount of drug should be present in the body throughout the scheduled time period.
Contraindications/Warnings
Contraindications
Known hypersensitivity(eg: anaphylaxis) to Cefuroxime or other beta-lactam antimicrobial drugs (eg: cephalosporins, penicillins)
Precautions
1. Avoid concomitant use with Histamine-2 (H-2) antagonists and also with Probenecid.
2. Phenylketonuria: Ceftin Suspension contains phenylalanine, which may cause allergic reactions in some people.
3. Gastrointestinal: Clostridium difficile- associated diarrhoea (CDAD) has been reported, including mild diarrhoea or fatal colitis.
4. Immunologic: Anaphylactic reactions have been reported, and there is an increased risk of an allergic reaction if there is a past history of beta-lactam antimicrobial allergy.
- Pregnancy Category: There is a possibility of foetal risk.
- Breastfeeding: Infant risk cannot be ruled out.
Before treating with CEFTIN, a complete history of patient hypersensitivity has to be obtained.
Adverse effects
Common effects include diarrhoea, nausea, vomiting, and vaginitis.
Serious effects: Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
What Are the Possible Side Effects of Cefuroxime?
- Diarrhoea (with or without a stool)
- Difficult or painful urination
- Skin rashes
- Yellowing of skin/eyes
- Severe stomach pain
- convulsions(seizure)
- Swelling of ankles, face, tongue
- Burning in eyes
- Soar throat
- Fever
- Shortness of breath
Toxicology
Clinical Effects
CEPHALOSPORINS
OVERDOSE
- Acute overdoses of cephalosporin result in nausea, vomiting, diarrhoea, and abdominal pain.
- Seizures have developed after a parenteral overdose.
ADVERSE EFFECTS
Common Adverse Effects
Hypersensitivity reactions, including anaphylaxis, may commonly occur with therapy; oral use is less likely to cause severe allergic reactions than parenteral use. Seizures are noticed with therapeutic overdose. Prolonged prothrombin times, thrombocytopenia, and coagulopathies associated with a qualitative platelet defect and aggregation abnormalities are noticed with IV cephalosporin therapy. Pseudocholelithiasis may follow intravenous administration of ceftriaxone. Children with haematological abnormalities and following IV ceftriaxone have been reported with fatal hemolytic reactions.
Treatment for an overdose of cephalosporins
GASTRIC LAVAGE: Not indicated in patients with no underlying health problems. Activated charcoal may be necessary for patients with underlying renal insufficiency.
Supportive care: Treatment is symptomatic and supportive.
Monitoring of patient: Monitor renal function, electrolytes, CBC including platelets.
Hypersensitivity reaction: In patients with acute allergic reactions, oxygen therapy, bronchodilators, diphenhydramine, corticosteroids, vasopressors, and epinephrine may be required.
Seizure: IV benzodiazepines, barbiturates
Blood coagulation disorder: Vitamin K, fresh frozen plasma
Intrathecal injection: Treat seizures with anticonvulsants (benzodiazepines, propofol, phenobarbital); endotracheal intubation and mechanical ventilation as needed. Keep the patient upright if possible. Drain out at least 20ml CSF as soon as possible. Adults can tolerate drainage of about 70ml. Then go with CSF (remove serial 20 mL aliquots CSF and replace with equivalent volumes of warmed, preservative-free normal saline or lactated ringers). For large overdoses, consult a neurosurgeon for placement of a ventricular catheter and begin ventriculi lumbar perfusion (infuse warmed preservative-free normal saline or lactated ringers through the ventricular catheter, drain fluid from the lumbar catheter; typical volumes 80 to 150 mL/hr). Dexamethasone 4 mg is given IV every 6 hours to prevent arachnoiditis.
Cefuroxime May Interact With Other Medicines
Cefuroxime can interact with various other drugs including vitamins, minerals, or herbs. Some of them are listed below:
- Cefuroxime hinders the absorption of oral contraceptives
Eg: Levonorgestrel/ Ethinyl estradiol
Norethindrone acetate/Ethinyl estradiol
- When taken along with drugs that reduce stomach acid, cefuroxime will not be absorbed.
Eg: Antacids such as calcium carbonate, and magnesium hydroxide
H2 antagonists- eg: cimetidine, and famotidine
Proton pump inhibitors (PPI)- eg: pantoprazole, omeprazole
H2 antagonists and PPI should be avoided during cefuroxime consumption.
- Probenecid increases the amount of cefuroxime in the body
Use in a Specific Population
Pregnancy
- Category B
- Research in animals has shown no risk, but human studies are not conducted. Thus pregnant women take this medicine only in emergencies.
Lactation
Since cefuroxime is excreted in breast milk, it is taken with caution
Pediatric use
Cefuroxime is not found safe and effective in children below 3 months of age.
Geriatric use
The kidney functioning in the elderly is not the same as in younger. The drug may take more time to process and as a result drug may retain in the body for a longer period. This may lead to cause any of the side effects.
What Should I Do if I Forget a Dose?
Take the missed dose as soon as possible. If it is almost time for your next dose, skip the missed dose and continue your normal dosing schedule. To cope with the missed dose, you should not take double the dose.
What Happens if I Overdose?
An overdose of cephalosporins can lead to cerebral irritation, which in turn causes convulsions. Call the Poison Control Helpline at 1-800-222-1222 if you suspect an overdose and need immediate medical attention. Information will also be available at https://www.poisonhelp.org/help. If the patient has a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.
Symptoms of overdose include:
- Seizure
How Can I Store and Dispose of Cefuroxime?
Storage
- Store tablets at a temperature between 59°F and 86°F(15°C and 30°C).
- Do not store in a moist or damp area.
Refills
- You do not need a new prescription for a refill. Your doctor will inform the number of refills required.
- Unrequired medication should be disposed of with the belief that pets, children, and other people cannot reach them.
A good option to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/ recycling department to learn about the take-back program in your community.
References
- Micromedex
- https://www.drugs.com/pro/cefuroxime-axetil.html
- https://www.webmed.com/drugs/2/drug-3779-5269/cefuroxime-axetil-oral/cefuroxime-suspension-ora/details
- https://reference.medscape.com/drug/ceftin-zinacef-cefuroxime-342500