Cloxacillin

Cloxacillin Belongs to the pharmacological class of Beta-Lactam Antibiotics.

Cloxacillin Has been approved to relieve symptoms and also for the treatment and maintenance of Bloodstream infection due to methicillin-susceptible S. aureus, Endocarditis due to methicillin-susceptible staphylococci, Osteomyelitis due to methicillin-susceptible S. aureus, Localized purulent skin lesions, impetigo, Arthritis (septic), Methicillin-sensitive Staphylococcus aureus, Endocarditis, Osteomyelitis, Pneumonia, MSSA, Pneumonia, nosocomial, Septicemia and Skin, and soft tissues.

Cloxacillin is well-absorbed after oral administration, with peak plasma concentrations reached within 1-2 hours. Its bioavailability is approximately 35-55%, and it is not affected by food. Cloxacillin is widely distributed in body fluids and tissues, including bone, skin, lungs, and pleural fluid. It has a low protein binding of approximately 85%. Cloxacillin is not metabolized in the liver and is eliminated unchanged in the urine. Cloxacillin is primarily eliminated by the kidneys, with a half-life of approximately 30 minutes in patients with normal renal function. In patients with renal impairment, the elimination half-life may be prolonged, and dosage adjustments may be necessary.

The commonly occurring side effects involving the use of Cloxacillin are Nausea, Vomiting, Diarrhea, Abdominal pain, Skin rash or itching, Headache, Dizziness, Urticaria , Local Injection site.

Cloxacillin Is available in the form of Capsules, Powder for Oral Suspensions , Injections .

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

Cloxacillin Belongs to the pharmacological class of Beta-Lactam Antibiotics.

Cloxacillin Is a beta-lactam antibiotic that works by inhibiting the growth of bacterial cell walls. It binds to penicillin-binding proteins (PBPs) in the bacterial cell wall, which interferes with the cross-linking of peptidoglycan chains, ultimately leading to bacterial cell death.

Cloxacillin has been approved to relieve symptoms and also for the treatment and maintenance of Bloodstream infection due to methicillin-susceptible S. aureus, Endocarditis due to methicillin-susceptible staphylococci, Osteomyelitis due to methicillin-susceptible S. aureus, Localized purulent skin lesions, impetigo, Arthritis (septic), Methicillin-sensitive Staphylococcus aureus , Endocarditis , Osteomyelitis , Pneumonia, MSSA , Pneumonia, nosocomial , Septicemia and Skin and soft tissues.

The peak concentration (Cmax)of cloxacillin in the blood is typically reached within 30 to 60 minutes after oral administration. The reported Cmax for a single oral dose of 500 mg of cloxacillin ranges from 10 to 25 mcg/mL. The time to reach maximum concentration (Tmax) of cloxacillin in the blood is typically within 30 to 60 minutes after oral administration.

The onset of action of cloxacillin is typically within a few hours after administration, although this can vary depending on the type and severity of the infection being treated. The duration of action of cloxacillin is generally 4 to 6 hours, although this can also vary depending on the patient and the specific infection being treated.

Cloxacillin is available in the form of Capsules, Powder for Oral Suspensions, Injections.

Cloxacillin can be used in the following treatment:

• Bloodstream infection due to methicillin-susceptible S. aureus
• Endocarditis due to methicillin-susceptible staphylococci
• Osteomyelitis due to methicillin-susceptible S. aureus
• Localized purulent skin lesions, impetigo
• Arthritis (septic)
• Methicillin-sensitive Staphylococcus aureus
• Endocarditis
• Osteomyelitis
• Pneumonia, MSSA
• Pneumonia, nosocomial
• Septicemia
• Skin and soft tissues

Cloxacillin can help to relieve symptoms and also for the treatment and maintenance of Bloodstream infection due to methicillin-susceptible S. aureus, Endocarditis due to methicillin-susceptible staphylococci, Osteomyelitis due to methicillin-susceptible S. aureus, Localized purulent skin lesions, impetigo, Arthritis (septic), Methicillin-sensitive Staphylococcus aureus , Endocarditis , Osteomyelitis , Pneumonia, MSSA , Pneumonia, nosocomial , Septicemia and Skin and soft tissues.

Cloxacillin is approved for use in the following clinical indications:

• Bloodstream infection due to methicillin-susceptible S. aureus
• Endocarditis due to methicillin-susceptible staphylococci
• Osteomyelitis due to methicillin-susceptible S. aureus
• Localized purulent skin lesions, impetigo
• Arthritis (septic)
• Methicillin-sensitive Staphylococcus aureus
• Endocarditis
• Osteomyelitis
• Pneumonia, MSSA
• Pneumonia, nosocomial
• Septicemia
• Skin and soft tissues

Bloodstream infection due to methicillin-susceptible S. aureus:

IV: 2 g every 4 to 6 hours

Endocarditis due to methicillin-susceptible staphylococci:

Native valve: IV: 12 g/day in 4 to 6 divided doses for 4 to 6 weeks

Prosthetic valve: IV: 12 g/day in 4 to 6 divided doses for ≥6 weeks, in combination with rifampin and gentamicin

Osteomyelitis due to methicillin-susceptible S. aureus:

IV: 2 g every 4 hours for ≥6 weeks

Localized purulent skin lesions, impetigo:

Oral: 250 to 500 mg every 6 hours for 5 to 7 days

Susceptible infections (manufacturer’s labeling):

Oral:Children ≤20 kg: 25 to 50 mg/kg/day into divided doses every 6 hours

IM, IV: Children ≤20 kg: 25 to 50 mg/kg/day into divided doses every 6 hours

Arthritis (septic) (off-label dosing):

Empiric therapy: Infants ≥2 months, Children, and Adolescents: IM, IV: 25 to 50 mg/kg/dose

Methicillin-sensitive Staphylococcus aureus:

Infants ≥2 months and Children ≤5 years: IM, IV: 25 to 50 mg/kg/dose (maximum: 2 g/dose) every 4 to 6 hours

Children >5 years and Adolescents: IM, IV: 25 to 50 mg/kg/dose (maximum: 2 g/dose) every 4 to 6 hours

Endocarditis:

Children and Adolescents: IV: 50 mg/kg/dose

Osteomyelitis (off-label dosing):

Infants ≥2 months and Children ≤5 years: IM, IV: 25 to 50 mg/kg/dose (maximum: 2 g/dose)

Children >5 years and Adolescents: IM, IV: 25 to 50 mg/kg/dose (maximum: 2 g/dose)

Pneumonia, MSSA:

Infants ≥2 months and Children ≤5 years: Oral: 25 to 50 mg/kg/dose (maximum: 2 g/dose) every 6 hours for at least 3 weeks with concomitant gentamicin.

Children >5 years and Adolescents: IM, IV: 50 mg/kg/dose (maximum: 2 g/dose) every 6 hours for 10 to 14 days.

Pneumonia, nosocomial (off-label dosing):

Empiric therapy: Children and Adolescents: IV: 50 mg/kg/dose (maximum: 2 g/dose) every 6 hours with concomitant gentamicin for 7 days

Septicemia (off-label dosing): Empiric therapy:

Infants ≥2 months to 5 years: IV: 50 mg/kg/dose (maximum: 2 g/dose) every 4 to 6 hours with concomitant ceftriaxone.

Children >5 years and Adolescents: IV: 2 g every 4 to 6 hours with concomitant gentamicin.

Skin and soft tissue infections (off-label dosing): Empiric therapy:

Contaminated soft tissue injuries: Children and Adolescents: IM, IV: 25 to 50 mg/kg/dose (maximum: 2 g/dose) every 6 hours for 5 to 10 days with concomitant gentamicin and metronidazole; with clinical improvement, may switch to oral cloxacillin 12.5 to 25 mg/kg/dose (maximum: 500 mg) every 6 hours.

Localized purulent skin lesions, impetigo: Children and Adolescents: Oral: 12.5 to 25 mg/kg/dose (maximum: 500 mg/dose) every 6 hours for 5 to 7 days.

Pyomyositis: Children and Adolescents: IM, IV: 25 to 50 mg/kg/dose (maximum: 2 g/dose) every 6 hours for 5 to 10 days; with clinical improvement, may switch to oral cloxacillin 12.5 to 25 mg/kg/dose (maximum: 500 mg/dose) every 6 hours.

Cloxacillin is available as follows:

• Oral capsules: 250 mg, 500 mg
• Oral suspension : 125 mg/5 mL, 250 mg/5 mL
• Injection: 250 mg, 500 mg, 1 gram

Capsules, Powder for Oral Suspensions, Injections.

• Dosage Adjustments in Kidney Patients:

For adults with a creatinine clearance (CrCl) of 10-50 mL/min, the usual dose is 250-500 mg every 6 hours. For severe infections, the dose may be increased to 1 gram every 6 hours. The maximum daily dose is 4 grams.

For adults with a CrCl of less than 10 mL/min, the usual dose is 250-500 mg every 8-12 hours. The maximum daily dose is 2 grams.

For pediatric patients with a CrCl of 10-50 mL/min, the usual dose is 25-50 mg/kg/day into divided doses every 6 hours. The maximum daily dose is 4 grams.

For pediatric patients with a CrCl of less than 10 mL/min, the usual dose is 25-50 mg/kg/day into divided doses every 8-12 hours. The maximum daily dose is 2 grams.

• Dosage Adjustments in Pediatric Patients:

For pediatric patients with a creatinine clearance (CrCl) of 10-50 mL/min, the usual dose is 25-50 mg/kg/day into divided doses every 6 hours. The maximum daily dose is 4 grams.

For pediatric patients with a CrCl of less than 10 mL/min, the usual dose is 25-50 mg/kg/day into divided doses every 8-12 hours. The maximum daily dose is 2 grams.

There are no specific dietary restrictions for patients taking Cloxacillin, according to the US FDA. However, it is recommended that Cloxacillin be taken on an empty stomach or with a light meal, as food may decrease the absorption of the medication. Patients should follow their healthcare provider's instructions regarding the timing and frequency of their doses. Additionally, patients should avoid consuming alcohol while taking Cloxacillin, as alcohol may increase the risk of side effects such as gastrointestinal upset, dizziness, and headache. Patients should also be sure to drink plenty of fluids while taking Cloxacillin to help prevent dehydration and promote proper kidney function. Overall, patients should follow a healthy and balanced diet while taking Cloxacillin to support their overall health and immune system function.

Cloxacillin may is contraindicated under the following conditions:

• Hypersensitivity to Cloxacillin: Cloxacillin should not be used in patients who have a known hypersensitivity to the drug or to other beta-lactam antibiotics such as penicillin. Patients with a history of hypersensitivity reactions, such as anaphylaxis, urticaria, or angioedema, should not receive Cloxacillin.
• Methicillin-resistant Staphylococcus aureus (MRSA): Cloxacillin is not effective against MRSA, a type of bacteria that is resistant to many antibiotics. Therefore, Cloxacillin should not be used to treat infections caused by MRSA.
• Infectious mononucleosis: Cloxacillin should not be used to treat infections caused by infectious mononucleosis. The use of antibiotics in patients with infectious mononucleosis may lead to the development of a rash.
• Cholestatic jaundice or hepatic dysfunction: Cloxacillin may cause cholestatic jaundice or hepatic dysfunction in some patients. Therefore, Cloxacillin should not be used in patients with a history of hepatic dysfunction or cholestatic jaundice.
• Clostridium difficile-associated diarrhea: Cloxacillin may cause Clostridium difficile-associated diarrhea, a type of diarrhea caused by a bacterial infection. Therefore, Cloxacillin should not be used to treat diarrhea unless the diarrhea is caused by a bacterial infection.
• Severe renal impairment: Cloxacillin is primarily eliminated by the kidneys, and patients with severe renal impairment may experience delayed elimination and increased serum levels of the drug. Therefore, Cloxacillin should not be used in patients with severe renal impairment.
• Concurrent use of tetracyclines: Cloxacillin may reduce the effectiveness of tetracycline antibiotics. Therefore, Cloxacillin should not be used concurrently with tetracyclines
• Gonorrhea: Cloxacillin is not effective against gonorrhea and should not be used for this indication.

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

Allergic reactions: Cloxacillin can cause severe allergic reactions, which can be life-threatening in some cases. If you experience symptoms such as hives, difficulty breathing, or swelling of the face or throat, seek immediate medical attention.

CNS effects: Although not reported with cloxacillin, the transport of penicillins across the blood-brain barrier may be enhanced by inflamed meninges or during cardiopulmonary bypass. An increased risk of myoclonia, seizures, or reduced consciousness may be observed in these patients

Liver damage: Cloxacillin can cause liver damage, especially in patients with liver disease or who are taking other medications that affect liver function. If you experience symptoms such as abdominal pain, jaundice (yellowing of the skin or eyes), or dark urine, contact your doctor right away.

Kidney damage: Cloxacillin can also cause kidney damage, especially in patients with kidney disease or who are taking other medications that affect kidney function. If you experience symptoms such as decreased urine output, swelling of the legs or feet, or confusion, contact your doctor immediately.

Blood disorders: Cloxacillin can cause blood disorders such as anemia, leukopenia (low white blood cell count), and thrombocytopenia (low platelet count). If you experience symptoms such as fatigue, weakness, shortness of breath, or easy bruising or bleeding, contact your doctor right away.

Drug interactions: Cloxacillin can interact with other medications, including oral contraceptives, blood thinners, and other antibiotics. Be sure to inform your doctor of all medications you are taking, including over-the-counter medications, supplements, and herbal products.

Resistance: Overuse of antibiotics can lead to antibiotic resistance, which can make infections more difficult to treat in the future. Use Cloxacillin only as prescribed by your doctor, and do not share it with others.

Pregnancy and breastfeeding: Cloxacillin is generally considered safe to use during pregnancy and breastfeeding, but you should discuss the risks and benefits with your doctor before taking this medication.

There is no specific alcohol warning for Cloxacillin. However, it is generally recommended to avoid alcohol while taking antibiotics, including cloxacillin. Alcohol can interfere with the efficacy of the medication and may also increase the risk of side effects such as stomach upset and liver damage.

Cloxacillin is excreted in human milk, and there is a risk of adverse effects on the nursing infant. Women who are breastfeeding should consult with their healthcare provider before taking cloxacillin.

Pregnancy Category B

Cloxacillin is classified as a pregnancy category B medication by the FDA. Animal studies have not shown any adverse effects on the fetus, and there are found to be no adequate and well-controlled studies in pregnant women. However, cloxacillin should only be used during pregnancy if the potential benefits outweigh the potential risks to the fetus.

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

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

Common adverse reactions (occurring in 1-10% of people taking cloxacillin):

• Nausea, vomiting, and diarrhea
• Skin rash or hives
• Itching
• Injection site reactions (pain, redness, or swelling)
• Abnormal liver function tests
• Headache

Less common adverse reactions (occurring in 0.1-1% of people taking cloxacillin):

• Serious allergic reactions (anaphylaxis)
• Seizures or convulsions
• Kidney damage or failure
• Low white blood cell count (neutropenia)
• Joint pain or swelling
• Abnormal blood clotting

Rare adverse reactions (occurring in less than 0.1% of people taking cloxacillin):

• Stevens-Johnson syndrome
• Toxic epidermal necrolysis (a life-threatening skin reaction)
• Hemolytic anemia
• Interstitial nephritis (an inflammation of the kidney tubules)
• Clostridioides difficile-associated diarrhea (a severe and potentially life-threatening infection of the colon).

The clinically relevant drug interactions of Cloxacillin are briefly summarized here:

• Oral contraceptives: Cloxacillin can reduce the effectiveness of oral contraceptives, leading to an increased risk of pregnancy. Women who take oral contraceptives should use an alternative form of contraception while taking cloxacillin.
• Warfarin: Cloxacillin can increase the effect of warfarin, an anticoagulant medication used to prevent blood clots. Patients taking both medications should be monitored closely for signs of bleeding.
• Methotrexate: Cloxacillin can increase the toxicity of methotrexate, a medication used to treat cancer and autoimmune disorders. Patients taking both medications should be monitored closely for side effects of methotrexate.
• Probenecid: Probenecid, a medication used to treat gout, can increase the levels of cloxacillin in the blood. Patients taking both medications should be monitored closely for side effects of cloxacillin.
• Aminoglycosides: Cloxacillin can reduce the effectiveness of aminoglycosides, a group of antibiotics used to treat bacterial infections. Patients taking both medications should be monitored closely for signs of infection.
• Other antibiotics: Cloxacillin can interact with other antibiotics, such as tetracyclines and erythromycin. Patients taking both medications should be monitored closely for side effects and efficacy of the antibiotics.
• Food: Cloxacillin should be taken on an empty stomach, as food can reduce its absorption. It is recommended to take cloxacillin one hour before or two hours after meals.

The following are the side effects involving Cloxacillin:

• Fever
• Swelling
• Skin rash
• Joint Pain
• Anaphylaxis
• Hives
• Jaundice
• Hypersensitivity reactions
• Headache
• Chills
• Nausea
• Vomiting
• Diarrhea
• Stomach pain

• Pregnancy

Pregnancy Category B

Cloxacillin is classified as a pregnancy category B medication by the FDA. Animal studies have not shown any adverse effects on the fetus, and there are found to be no adequate and well-controlled studies in pregnant women. However, cloxacillin should only be used during pregnancy if the potential benefits outweigh the potential risks to the fetus.

• Lactation

Cloxacillin is excreted in human milk, and there is a risk of adverse effects on the nursing infant. Women who are breastfeeding should consult with their healthcare provider before taking cloxacillin.

• Pediatric

Cloxacillin is approved for use in children, but dosing will depend on the child's weight and age. The safety and effectiveness of cloxacillin in children under one month of age have not been established.

• Geriartic

Elderly patients may be more susceptible to certain side effects of cloxacillin, such as diarrhea and liver problems. Dosing adjustments may be necessary in elderly patients with impaired renal or hepatic function.

Physicians should be knowledgeable as well as vigilant about the treatment and identification of over dosage of Cloxacillin.

Cloxacillin is an antibiotic medication used to treat bacterial infections. However, taking too much cloxacillin can lead to an overdose, which can be harmful.

The symptoms of a cloxacillin overdose may include nausea, vomiting, diarrhea, stomach pain, dizziness, confusion, seizures, and allergic reactions. In severe cases, an overdose can cause kidney and liver damage, and even lead to coma or death.

Pharmacodynamics

Cloxacillin is said to be a semisynthetic antibiotic in the same class as penicillin. Cloxacillin is for use against staphylococci that produce beta-lactamase.

Pharmacokinetics

• Absorption: Cloxacillin is well-absorbed after oral administration, with peak plasma concentrations reached within 1-2 hours. Its bioavailability is approximately 35-55%, and it is not affected by food.

• Distribution: Cloxacillin is widely distributed in body fluids and tissues, including bone, skin, lungs, and pleural fluid. It has a low protein binding of approximately 85%.

• Metabolism: Cloxacillin is not metabolized in the liver and is eliminated unchanged in the urine.

• Elimination: Cloxacillin is primarily eliminated by the kidneys, with a half-life of approximately 30 minutes in patients with normal renal function. In patients with renal impairment, the elimination half-life may be prolonged, and dosage adjustments may be necessary.

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