Loracarbef

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

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

Loracarbef is an orally administered antibiotic with good bioavailability and rapid absorption from the gastrointestinal tract, with a time to peak plasma concentration (Tmax) of approximately 1-2 hours. It ha a relatively short elimination half-life of approximately 1-1.5 hours and is primarily eliminated via the kidneys. Loracarbef is widely distributed throughout the body, with concentrations achieved in the respiratory tract, urine, and skin, among other tissues. The pharmacokinetics of loracarbef are not significantly affected by age, gender, or food intake. However, renal impairment can significantly alter the pharmacokinetics of the drug, requiring dose adjustment in patients with impaired renal function.

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

Loracarbef is available in the form of Oral capsules, Oral suspension.

Loracarbef is approved in the Germany, Japan, Malaysia, India, and China.

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

Loracarbef is an orally administered, synthetic antibiotic belonging to the carbacephem class. Unlike cephalosporins, carbacephems have a methylene group substituted for a sulfur atom in the dihydrothiazine ring. Loracarbef's spectrum of activity is similar to that of second-generation cephalosporins, and it is structurally identical to cefaclor, except for the substitution of a methylene group for a sulfur atom. This change provides greater chemical stability in solution and enables storage at room temperature.

Loracarbef, like other beta-lactams and cephalosporins, inhibits the action of penicillin-binding proteins, which are enzymes responsible for creating the cross-linkages of the peptidoglycan polymer. As a result, loracarbef interferes with the formation and remodeling of the bacterial cell wall structure.

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

The Tmax (time to maximum concentration) of loracarbef is approximately 1 to 2 hours after oral administration. The onset of action of loracarbef is relatively rapid, with significant concentrations achieved in the bloodstream within 1 to 2 hours after administration. The half-life of loracarbef is approximately 3 to 4 hours in adults, which means that the drug is eliminated from the body relatively quickly. After discontinuation of loracarbef, it takes approximately 12 to 24 hours for the drug to be eliminated from the body.

The duration of action of loracarbef varies depending on the type as well as severity of the infection being treated, as well as the patient's individual response to the medication. In general, loracarbef is usually administered for a period of 7 to 14 days for most infections.

Loracarbef is found to be available in the form of Oral capsules, Oral suspension.

Loracarbef can be used in the following treatment:

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

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

Loracarbef is approved for use in the following clinical indications:

● Acute bacterial exacerbation of chronic bronchitis

● Pneumonia

● Pharyngitis/tonsillitis

● Skin and skin-structure infections

● Otitis media, acute

● Urinary tract infection

● Impetigo

Lower Respiratory Tract

Secondary Bacterial Infection of Acute Bronchitis: 200-400 mg every 12 hours for 7 days

Acute Bacterial Exacerbation of Chronic Bronchitis: 400 mg every 12 hours for 7 days

Pneumonia: 400 mg every 12 hours for 14 days

Upper Respiratory Tract

Pharyngitis/Tonsillitis: 200 mg every 12 hours for 10 days

Sinusitis: 400 mg every 12 hours for 10 days

Skin and Skin Structure

Uncomplicated Skin as well as Skin Structure Infections: 200 mg every 12 hours for seven days

Urinary Tract

Uncomplicated cystitis: 200 mg once daily for 7 days

Uncomplicated pyelonephritis: 400 mg every 12 hours for 14 days.

Loracarbef 200mg capsules

Loracarbef 400mg capsules

Loracarbef 100mg/5mL oral suspension

Oral capsules, Oral suspension.

• Dosage Adjustments in Kidney Patients:

For patients with creatinine clearance (CrCl) greater than 30 mL/min, no dosage adjustment is necessary.

For patients with CrCl between 15 and 30 mL/min, the recommended daily dose should be reduced by 50%.

For patients with CrCl less than 15 mL/min, the recommended daily dose should be reduced by 75%.

• Dosage Adjustments in Pediatric Patients:

For pediatric patients aged 6 months to 12 years:

Upper Respiratory Tract:

Acute Otitis Media: A 30 mg/kg/day in divided doses every 12 hours for ten days

Acute maxillary sinusitis: A 30 mg/kg/day in divided doses every 12 hours for ten days

Pharyngitis/Tonsillitis: A 15 mg/kg/day in divided doses every 12 hours for ten days

Skin and Skin Structure:

Impetigo: 15 mg/kg/day in divided doses every 12 hours for 7 days.

There are no known dietary restrictions related to the use of loracarbef. However, it is generally recommended to take the medication with food or milk to help reduce the incidence of gastrointestinal side effects such as nausea, vomiting, and diarrhea. It is important to follow the instructions of the prescribing healthcare provider regarding the timing and dosage of the medication, and to avoid consuming alcohol while taking loracarbef as it may increase the risk of adverse effects.

Loracarbef may be contraindicated under the following conditions:

• Hypersensitivity to the drug or other β-lactam antibiotics such as penicillin or cephalosporins.
• In patients with a history of cholestatic jaundice or hepatic dysfunction associated with the use of loracarbef or other cephalosporins.
• In patients with renal impairment or in those who have shown hypersensitivity reactions to any component of the formulation.
• It is important to note that loracarbef is not effective against infections caused by MRSA (methicillin-resistant Staphylococcus aureus) or Pseudomonas aeruginosa. Therefore, it should not be used to treat infections caused by these pathogens.

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

Before starting therapy with Lorabid (loracarbef), healthcare providers should inquire about the patient's history of hypersensitivity reactions to drugs loracarbef, cephalosporins, penicillins, or other drugs. Patients with a history of penicillin allergy might have cross-hypersensitivity reactions to β-lactam antibiotics, including loracarbef, in up to 10% of cases. If an allergic reaction occurs, the drug should be discontinued immediately, and emergency measures may be necessary.

Pseudomembranous colitis has been reported with nearly all antibacterial agents, and also it is important to consider this diagnosis in patients who present with diarrhea after antibiotic administration. Treatment with broad-spectrum antibiotics can alter the normal flora of the colon and may allow the overgrowth of Clostridium difficile, which is the primary cause of antibiotic-associated colitis.

Patients with known or suspected renal impairment should be carefully observed, and appropriate laboratory studies should be performed before and during therapy with loracarbef. The total daily dose of loracarbef should be reduced in these patients because high and/or prolonged plasma antibiotic concentrations can occur with the usual doses. Loracarbef should also be given with caution to patients receiving concurrent treatment with potent diuretics, which may adversely affect renal function.

Prolonged use of loracarbef might result in the overgrowth of nonsusceptible organisms, and if superinfection occurs during therapy, appropriate measures should be taken. Individuals with a history of colitis should be prescribed loracarbef with caution.

There is a moderate interaction between alcohol and Loracarbef. It is generally recommended to avoid drinking alcohol while taking Loracarbef 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 Loracarbef in treating bacterial infections.

Loracarbef is excreted in human milk, and caution should be exercised when it is administered to nursing mothers. If the drug is necessary, the benefits and risks should be weighed carefully before making a decision about breastfeeding.

Pregnancy Category B

Loracarbef is classified as a pregnancy category B drug, which means that animal studies have not demonstrated any fetal risk, but there are no adequate studies in pregnant women. Therefore, it should be used during pregnancy only if clearly needed and after consulting with a healthcare provider.

There is found to be no sufficient scientific evidence regarding the use and safety of Loracarbef in concurrent use with any particular food.

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

Common:

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

Less Common:

• Dyspepsia (indigestion)
• Fatigue
• Insomnia
• Itching
• Hives
• Joint pain
• Elevated liver enzymes
• Anemia
• Decreased white blood cell count

Rare:

• Stevens-Johnson syndrome (a severe skin reaction)
• Toxic epidermal necrolysis (a life-threatening skin reaction)
• Anaphylaxis (a severe allergic reaction)
• Clostridium difficile-associated diarrhea (a bacterial infection)
• Hepatitis (inflammation of the liver)
• Acute renal failure (sudden loss of kidney function)
• Hemolytic anemia (destruction of red blood cells)
• Thrombocytopenia (low platelet count)

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

Probenecid: Probenecid can increase the plasma levels of loracarbef by decreasing its renal clearance. This can lead to an increased risk of side effects.

Anticoagulants: Loracarbef may enhance the effects of anticoagulant medications, such as warfarin, by inhibiting their metabolism. This can increase the risk of bleeding.

Methotrexate: Concurrent use of loracarbef and methotrexate may increase the plasma levels of methotrexate, leading to increased toxicity.

Oral contraceptives: Loracarbef may reduce the efficacy of oral contraceptives by altering their metabolism. Additional or alternative contraceptive measures may be needed.

Live vaccines: Loracarbef may interfere with the efficacy of live vaccines, such as measles, mumps, and rubella (MMR) vaccine. It is recommended to avoid the use of live vaccines during treatment with loracarbef.

Other antibiotics: Concurrent use of loracarbef with other antibiotics, such as aminoglycosides or vancomycin, may enhance the risk of nephrotoxicity or ototoxicity.

The following are the side effects involving Loracarbef :

• Vomiting
• Diarrhea
• Abdominal pain
• Dyspepsia
• Skin rash
• Itching
• Hives
• Leukopenia
• Thrombocytopenia
• Hepatitis
• Jaundice

• Pregnancy

Pregnancy Category B

Loracarbef is classified as a pregnancy category B drug, which means that animal studies have not demonstrated any fetal risk, but there are no adequate studies in pregnant women. Therefore, it should be used during pregnancy only if clearly needed and after consulting with a healthcare provider.

• Lactation:

Loracarbef is excreted in human milk, and caution should be exercised when it is administered to nursing mothers. If the drug is necessary, the benefits and risks should be weighed carefully before making a decision about breastfeeding.

• Pediatrics:

The safety and efficacy of loracarbef in pediatric patients have not been established in clinical trials. However, the drug has been used in children over the age of 6 months with mild-to-moderate infections caused by susceptible organisms. The dosage as well as duration of treatment should be adjusted based on the child's age, weight, and clinical condition.

• Geriatric:

No specific information is available regarding the use of loracarbef in the elderly. However, caution should be exercised in this population due to the possibility of decreased renal function, which may require a reduction in dosage or an increase in dosing interval. Additionally, the potential for drug interactions and adverse effects may be greater in older adults, and close monitoring is recommended.

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

Signs and Symptoms—An overdose of β-lactams may result in various toxic symptoms, such as nausea, vomiting, epigastric distress, and diarrhea.

Loracarbef is mainly eliminated from the body through the kidneys. There is no established evidence that forced diuresis, peritoneal dialysis, hemodialysis, or hemoperfusion can be helpful in treating an overdose of loracarbef. However, hemodialysis has been proven effective in accelerating the elimination of loracarbef from plasma in the patients with chronic renal failure.

Pharmacodynamics

Loracarbef belongs to the class of second-generation cephalosporin antibiotics. Cephalosporin antibiotics offer several benefits such as a wide range of activity against both gram-negative and gram-positive bacteria, safety in children with minimal dose-related toxicity, and no need for therapeutic drug monitoring. The drug's side effects are rare and mainly involve hypersensitivity reactions such as urticaria, pruritus, and a nonspecific rash. Loracarbef is indicated for treating various bacterial infections including upper respiratory tract bacterial infections, pneumonia, chronic bronchitis, sinusitis, pharyngitis, and tonsillitis, skin abscesses, urinary tract infections, and pyelonephritis caused by E. coli, S. pyogenes, S. aureus, S. saprophyticus, S. pneumoniae, H. influenzae, and M. catarrhalis.

Pharmacokinetics

Loracarbef is well-absorbed orally, with an average of 90% absorption from the gastrointestinal tract. The rate and extent of absorption of loracarbef were affected by food, with peak plasma concentrations being 50-60% lower and occurring 30-60 minutes later when capsules were taken with food. However, total absorption, as measured by urinary recovery and AUC, was unchanged. The pharmacokinetics of loracarbef were found to be linear over the recommended dosage range of 200 to 400 mg, with no accumulation noted when given twice daily. The elimination half-life was approximately 1.0 hour in patients with normal renal function, but was prolonged to approximately 5.6 hours in subjects with moderate renal impairment and approximately 32 hours in subjects with severe renal impairment. Loracarbef is not metabolized in humans, and approximately 25% of circulating loracarbef is found to be bound to plasma proteins. Middle-ear fluid concentrations of loracarbef were found to be approximately 48% of the plasma concentration 2 hours after drug administration in pediatric patients, and the peak concentration of loracarbef in a blister fluid was approximately half that obtained in plasma.

1. https://pubchem.ncbi.nlm.nih.gov/compound/Loracarbef
2. https://www.medicinenet.com/loracarbef/article.htm
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5. https://www.accessdata.fda.gov/drugsatfda_docs/nda/96/050667ap.pdf
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