Cefprozil

Cefprozil belongs to the pharmacological class of Second-generation cephalosporin antibiotics.

Cefprozil has been approved to relieve symptoms and also for the treatment and maintenance of Acute bacterial exacerbation of chronic bronchitis, Pharyngitis/tonsillitis, Skin and skin structure infections, Otitis media, acute, Rhinosinusitis, Urinary tract infection

After oral administration, cefprozil is rapidly absorbed from the gastrointestinal tract and reaches peak plasma concentrations (Cmax) within 1 to 2 hours. The bioavailability of cefprozil is approximately 95%. The drug is widely distributed throughout the body, including in the respiratory tract, bone, and urine. Cefprozil is eliminated primarily by the kidneys through glomerular filtration and tubular secretion, with a half-life of approximately 1.5 hours in patients with normal renal function. In patients with impaired renal function, the elimination half-life is prolonged, and dosage adjustments are recommended. Cefprozil does not appear to be metabolized in the body, and approximately 85% of an oral dose is excreted unchanged in the urine within 24 hours.

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

Cefprozil is available in the form of Cefprozil is available in the form of Tablets, Oral suspensions.

Cefprozil is approved in the U.S., U.K., Germany, Japan, Malaysia, India, and China.

Cefprozil belongs to the pharmacological class of Second-generation cephalosporin antibiotics.

Cefprozil is a cephalosporin antibiotic that works by inhibiting bacterial cell wall synthesis. Specifically, it binds to and inhibits the activity of the penicillin-binding proteins (PBPs) located on the surface of the bacterial cell wall. PBPs are involved in the final stages of peptidoglycan synthesis, which is necessary for the structural integrity of bacterial cell walls.

Cefprozil's binding to PBPs results in the disruption of peptidoglycan synthesis, ultimately leading to the weakening and eventual lysis of the bacterial cell wall. This results in the death of susceptible bacteria.

Cefprozil has been approved to relieve symptoms and also for the treatment and maintenance of Acute bacterial exacerbation of chronic bronchitis, Pharyngitis/tonsillitis, Skin and skin structure infections, Otitis media, acute, Rhinosinusitis, Urinary tract infection

The maximum concentration of cefprozil in the blood after oral administration is usually reached within 1-2 hours. The time to reach Cmax (Tmax) after oral administration is around 1-2 hours.

The onset of action of cefprozil is relatively rapid, with therapeutic levels achieved soon after administration. The duration of action of cefprozil can vary, but the drug is typically effective for 12 hours, allowing for twice-daily dosing.

Cefprozil is found to be available in the form of Tablets, Oral suspensions.

Cefprozil can be used in the following treatment:

• Acute bacterial exacerbation of chronic bronchitis
• Pharyngitis/tonsillitis
• Skin and skin structure infections
• Otitis media, acute
• Rhinosinusitis
• Urinary tract infection

Cefprozil can help to relieve symptoms and also for the treatment and maintenance of Acute bacterial exacerbation of chronic bronchitis, Pharyngitis/tonsillitis, Skin and skin structure infections, Otitis media, acute, Rhinosinusitis, Urinary tract infection.

Cefprozil is approved for use in the following clinical indications:

● Acute bacterial exacerbation of chronic bronchitis

● Pharyngitis/tonsillitis

● Skin and skin structure infections

● Otitis media, acute

● Rhinosinusitis

● Urinary tract infection

Acute bacterial exacerbation of chronic bronchitis:

Oral: Take 500 mg every 12 hours for a total of 10 days.

Pharyngitis/tonsillitis:

Oral: Take 500 mg once a day for a total of 10 days. If the infection is due to S. pyogenes, continue treatment for at least 10 days.

Skin and skin structure infections, uncomplicated:

Oral: Take 250 mg or 500 mg every 12 hours or 500 mg once a day for a total of 10 days.

Tablets: 250 mg and 500 mg

Oral suspension: 125 mg/5 mL and 250 mg/5 mL

Tablets, Oral suspensions

• Dosage Adjustments in Kidney Patients:

The manufacturer's labeling for oral cefprozil dosing based on renal function is as follows:

For patients with a creatinine clearance (CrCl) of ≥30 mL/minute, no dosage adjustment is necessary.

For patients with a CrCl of <30 mL/minute, the dose should be reduced by 50%.

For patients with end-stage renal disease (ESRD) undergoing hemodialysis, the dose should be given after dialysis on dialysis days.

Alternative recommendations based on a study by Aronoff (2007) are as follows:

For patients with a CrCl >50 mL/minute, no dosage adjustment is necessary.

For patients with a CrCl <50 mL/minute, administer 50% of the usual dose every 12 hours.

For patients undergoing intermittent hemodialysis (IHD), supplement with 250 mg after dialysis on dialysis days.

For patients undergoing peritoneal dialysis, administer 50% of the usual dose every 12 hours.

• Dosage Adjustments in Pediatric Patients:

Acute bacterial exacerbation of chronic bronchitis: Adolescents can take 500 mg orally every 12 hours for 10 days.

Acute otitis media: Infants and children can take 15 mg/kg/dose orally every 12 hours for 10 days, with a maximum single dose of 500 mg/dose. Note that cefprozil is not routinely recommended for acute otitis media.

Pharyngitis/tonsillitis: Children ≥2 years can take 7.5 mg/kg/dose orally every 12 hours for 10 days, with a maximum single dose of 500 mg/dose. Adolescents can take 500 mg orally every 24 hours for 10 days.

Rhinosinusitis: Infants and children can take 7.5 to 15 mg/kg/dose orally every 12 hours for 10 days, with a maximum single dose of 500 mg/dose. Adolescents can take 250 to 500 mg orally every 12 hours for 10 days. Note that cefprozil is not recommended for empiric monotherapy of acute sinusitis due to the risk of resistance.

Uncomplicated skin and skin structure infection: Children ≥2 years can take 20 mg/kg/dose orally once daily for 10 days, with a maximum single dose of 500 mg/dose. Adolescents can take 250 mg orally every 12 hours or 500 mg every 12 to 24 hours for 10 days.

Urinary tract infection: Infants ≥2 months and children ≤2 years can take 15 mg/kg/dose orally twice daily for 7 to 14 days.

There are no specific dietary restrictions when taking cefprozil. However, it is generally recommended to take the medication with food to help reduce the risk of stomach upset or nausea. Avoiding alcohol while taking cefprozil is also recommended, as alcohol can increase the risk of certain side effects such as dizziness or drowsiness. It is important to follow the dosing instructions provided by your healthcare provider and to complete the full course of treatment, even if you start to feel better before the medication is finished.

Cefprozil may be contraindicated under the following conditions:

• Hypersensitivity or allergy to cefprozil or any other cephalosporin antibiotics.
• Previous history of a severe allergic reaction (anaphylaxis) to penicillins or other beta-lactam antibiotics.
• Severe renal impairment or kidney failure.
• Colitis or a history of gastrointestinal disease.
• Pregnancy or breastfeeding.
• Children under the age of 6 months.

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

Before starting treatment with Cefprozil, it is important to investigate whether the patient has had any previous allergic reactions to Cefprozil, cephalosporins, penicillins, or any other drugs. Patients with a history of penicillin allergy may have cross-sensitivity to β-lactam antibiotics and should be treated with caution. If an allergic reaction to Cefprozil occurs, treatment should be stopped immediately. In severe cases, emergency measures may be required, including epinephrine, oxygen, IV fluids, IV antihistamines, corticosteroids, pressor amines, and airway management.

Cefprozil, like many other antibiotics, may cause Clostridium difficile associated diarrhea (CDAD) ranging from mild diarrhea to fatal colitis. Antibacterial agents alter the normal flora of the colon, leading to an overgrowth of C. difficile. This bacterium produces toxins A and B which contribute to the development of CDAD. Hypertoxin-producing strains of C. difficile cause more severe infections, which can be resistant to antimicrobial therapy and may require colectomy. CDAD should be considered in all patients who present with diarrhea following antibiotic use. It is necessary to take a careful medical history since CDAD can occur up to two months after antibiotic administration.

If CDAD is suspected or confirmed, it may be necessary to discontinue ongoing antibiotic use not directed against C. difficile. Appropriate management such as fluid and electrolyte replacement, protein supplementation, antibiotic treatment of C. difficile, and surgical evaluation should be instituted as clinically indicated.

There is a moderate interaction between alcohol and Cefprozil. It is generally recommended to avoid drinking alcohol while taking Cefprozil because it may increase the risk of side effects such as dizziness, drowsiness, and gastrointestinal upset. Additionally, alcohol may also impair the body's ability to fight infections, which may reduce the effectiveness of Cefprozil in treating bacterial infections.

For nursing women, less than 1.0% of the maternal dose is excreted in human milk. Therefore, caution should be exercised when administering Cefprozil to nursing mothers. Temporary discontinuation of nursing and the use of formula feeding may be considered.

Pregnancy Category B

Reproduction studies in mice, rats, and rabbits have been conducted using doses of cefprozil up to 14, 7, and 0.7 times the maximum human daily dose (1000 mg) based on mg/m2, and no evidence of harm to the fetus has been observed. However, there are no sufficient and well-controlled studies in pregnant women. As animal studies may not always predict human response, the use of cefprozil during pregnancy should only be considered if the potential benefits outweigh the potential risks.

No sufficient scientific evidence is traceable regarding the use and safety of Cefprozil in concurrent use with any particular food.

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

Common:

• Diarrhea
• Nausea
• Vomiting
• Stomach pain
• Headache
• Dizziness
• Vaginal itching or discharge

Less Common:

• Rash
• Itching
• Hives
• Swelling of the face, lips, tongue, or throat
• Difficulty breathing or swallowing
• Seizures
• Joint pain or swelling

Rare:

• Severe allergic reactions (anaphylaxis)
• Blood disorders, such as low white blood cell count or thrombocytopenia
• Kidney damage
• Liver damage
• Clostridium difficile-associated diarrhea
• Stevens-Johnson syndrome (a severe skin reaction)
• Toxic epidermal necrolysis (a life-threatening skin condition)

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

The simultaneous use of aminoglycoside and cephalosporin antibiotics has been associated with kidney damage. Taking probenecid alongside cefprozil doubled its AUC. The intake of an antacid five minutes prior to a capsule of cefprozil did not impact the drug's bioavailability.

The following are the side effects involving Cefprozil :

• Diarrhea
• Nausea
• Vomiting
• Stomach pain
• Headache
• Dizziness
• Fatigue
• Skin rash
• Itching
• Vaginal itching or discharge

Pregnancy

Pregnancy Category B

Reproduction studies in mice, rats, and rabbits have been conducted using doses of cefprozil up to 14, 7, and 0.7 times the maximum human daily dose (1000 mg) based on mg/m2, and no evidence of harm to the fetus has been observed. However, there are no sufficient and well-controlled studies in pregnant women. As animal studies may not always predict human response, the use of cefprozil during pregnancy should only be considered if the potential benefits outweigh the potential risks.

Nursing Mothers:

For nursing women, less than 1.0% of the maternal dose is excreted in human milk. Therefore, caution should be exercised when administering Cefprozil to nursing mothers. Temporary discontinuation of nursing and the use of formula feeding may be considered.

Pediatric Use:

Comparable pharmacokinetic parameters have been observed in pediatric patients (between 6 months and 12 years of age) and adults following oral administration of cefprozil. Maximum plasma concentrations are achieved between 1-2 hours after dosing, and the plasma elimination half-life is approximately 1.5 hours.

In pediatric patients, the area under the concentration-time curve (AUC) after receiving doses of 7.5, 15, and 30 mg/kg of cefprozil is similar to that observed in normal adult subjects after receiving doses of 250, 500, and 1000 mg, respectively.

Geriatric Use:

When a single dose of 1 g cefprozil was given to elderly subjects (aged 65 years or older), the average AUC was found to be approximately 35-60% higher than that observed in healthy young adults. Females had an average AUC approximately 15-20% higher than males. However, the differences in pharmacokinetics based on age and gender are not significant enough to require a change in dosage.

Physicians should be knowledgeable and vigilant about the treatment and identification of over dosage of Cefprozil.

No cases of over dosage with cefprozil have been reported so far, and therefore, there is no specific information available regarding the symptoms or treatment of an overdose. However, in animal toxicology studies, high single doses of up to 5000 mg/kg did not result in serious or lethal consequences.

Cefprozil is eliminated from the body primarily by the kidneys. In the event of severe over dosage, particularly in patients with impaired renal function, hemodialysis may be helpful in removing the drug from the body.

Pharmacodynamics

Cefprozil is a bactericidal antibiotic that belongs to the cephalosporin class of drugs. It works by inhibiting bacterial cell wall synthesis, which results in the destruction of the bacterial cell. Cefprozil is effective against a broad range of gram-positive and gram-negative bacteria.

The pharmacodynamics of cefprozil are characterized by its minimum inhibitory concentration (MIC) values, which is the lowest concentration of the drug that is required to inhibit the growth of bacteria. The MICs of cefprozil vary depending on the bacterial strain and the susceptibility of the bacteria to the drug.

Cefprozil has been shown to be effective against a number of common bacterial pathogens, including Streptococcus pyogenes, Haemophilus influenzae, Moraxella catarrhalis, and Streptococcus pneumoniae. The drug has also been used to treat a variety of infections, including upper and lower respiratory tract infections, skin and soft tissue infections, and urinary tract infections.

The pharmacodynamic properties of cefprozil, including its potency and spectrum of activity, make it an effective treatment option for a wide range of bacterial infections. However, as with all antibiotics, appropriate use and proper dosing are important to minimize the development of resistance and to maximize the efficacy of the drug.

Pharmacokinetics

Cefprozil is easily absorbed when taken orally, regardless of whether the patient has eaten beforehand or not. Its oral bioavailability is around 90%, and taking it with food or antacids does not affect its pharmacokinetics.

After administering cefprozil to fasting subjects, the average plasma concentrations are as follows:

250 mg dose: approximately 2.2 mcg/mL after 1 hour, and 1.2 mcg/mL after 4 hours

500 mg dose: approximately 4.4 mcg/mL after 1 hour, and 2.3 mcg/mL after 4 hours

1 g dose: approximately 8.3 mcg/mL after 1 hour, and 4.2 mcg/mL after 4 hours

Around 60% of the administered dose is recovered in the urine during the first four hours after drug administration, with average urine concentrations ranging from 170 mcg/mL for the 250 mg dose to 600 mcg/mL for the 1 g dose.

In normal subjects, the average plasma half-life of cefprozil is 1.3 hours, and approximately 36% of the drug is bound to plasma proteins, which is independent of concentration within the range of 2 mcg/mL to 20 mcg/mL. There is no evidence of drug accumulation in the plasma of individuals with normal renal function even after taking multiple oral doses of up to 1 g every 8 hours for 10 days.

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