Benzathine- benzylpenicillin

Benzathine- benzylpenicillin belongs to the pharmacological class of Beta-Lactam Antibiotics.

Benzathine- benzylpenicillin has been approved to relieve symptoms and also for the treatment and maintenance of Skin and soft tissue infection, streptococcus, Streptococcus, Group A, Syphilis, Yaws , Bejel and Pinta disease.

After intramuscular injection, benzathine- benzylpenicillin is slowly absorbed into the bloodstream, reaching peak concentrations within 2-4 hours. Benzathine- benzylpenicillin is distributed throughout the body, including the lungs, liver, kidneys, and spleen. It does not readily cross the blood-brain barrier. Benzathine- benzylpenicillin is not metabolized by the body. Benzathine- benzylpenicillin is eliminated from the body primarily through renal excretion. The half-life of the drug is approximately 12-24 hours in adults and 8-14 hours in children.

The common side effects involving the use of Benzathine- benzylpenicillin are Diarrhea, Nausea, Vomiting, Skin rash or hives, Fever, Joint pain or swelling, Headache, Dizziness, Fatigue and Pain or redness at the injection site

Benzathine- benzylpenicillin is available in the form of Intramuscular Injections

Benzathine- benzylpenicillin is approved in the Germany, Japan, Malaysia, India, U.S., U.K., and China.

Benzathine- benzylpenicillin belongs to the pharmacological class of Beta-Lactam Antibiotics.

Benzathine- benzylpenicillin 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, interfering with the cross-linking of peptidoglycan chains, ultimately leading to cell death.

Benzathine- benzylpenicillin has been approved to relieve symptoms and also for the treatment and maintenance of Skin and soft tissue infection, streptococcus, Streptococcus, Group A, Syphilis, Yaws , Bejel and Pinta disease.

The onset of action is slow, with therapeutic levels achieved within several hours of injection, and peak plasma concentrations are usually reached within 24 to 48 hours.

The duration of action of benzathine- benzylpenicillin is prolonged, typically lasting for several days or even up to several weeks, depending on the dose and the indication being treated. The drug is designed to provide sustained release of penicillin over time, allowing for once-daily dosing in many cases.

Benzathine- benzylpenicillin is available in the form of Intramuscular Injections.

Benzathine- benzylpenicillin can be used in the following treatment:

• Skin and soft tissue infection, streptococcal
• Streptococcus, Group A
• Syphilis
• Yaws , Bejel and Pinta disease.

Benzathine- benzylpenicillin can help to relieve symptoms and also for the treatment and maintenance of Skin and soft tissue infection, streptococcus, Streptococcus, Group A, Syphilis, Yaws , Bejel and Pinta disease.

Benzathine- benzylpenicillin is approved for use in the following clinical indications:

• Skin and soft tissue infection, streptococcal
• Streptococcus, Group A
• Syphilis
• Yaws , Bejel and Pinta disease.

• Skin and soft tissue infection: The dosage for skin and soft tissue infections is not well established. However, in some cases, a single intramuscular dose of 1.2 million units of benzathine- benzylpenicillin may be given for mild to moderate infections caused by susceptible organisms.
• Streptococcus, group A:

Children under 27 kg: 600,000 units as a single dose

Children over 27 kg and adults: 1.2 million units as a single dose

• Syphilis:

Primary, secondary, or early latent syphilis: 2.4 million units as a single dose

Late latent syphilis: 2.4 million units once weekly for three weeks

• Yaws, bejel, and pinta: The recommended dosage of benzathine- benzylpenicillin for the treatment of yaws, bejel, and pinta is 1.2 million units given intramuscularly as a single dose for uncomplicated cases, or 2.4 million units given intramuscularly as a single dose for severe cases. In some cases, additional doses may be required. The exact treatment regimen may vary depending on the severity of the disease and the specific guidelines of the healthcare provider.

Injectable solution

• 600,000 units/1mL
• 1.2 million units/2mL
• 2.4 million units/4mL

Intramuscular Injections

• Dosage Adjustments in Pediatric Patients:

Infants (up to 1 month old): The recommended dose is 50,000 to 100,000 units per kg of body weight every 12 to 24 hours.

Children (1 month to 12 years old): The recommended dose is 50,000 to 200,000 units per kg of body weight every 6 to 8 hours.

There are no specific dietary restrictions for patients receiving benzathine- benzylpenicillin. However, it is recommended to take this medication on an empty stomach, at least 1 hour before or 2 hours after meals, to maximize its absorption. Additionally, it is important to stay well-hydrated while receiving this medication, so drinking plenty of fluids is recommended. If you have any concerns about your diet or fluid intake while receiving benzathine- benzylpenicillin, it is best to consult with your healthcare provider.

Benzathine- benzylpenicillin may is contraindicated under the following conditions:

• Allergy to penicillin: Patients with a known allergy to penicillin or cephalosporin antibiotics should not take Benzathine- benzylpenicillin.

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

The medication, Penicillin G benzathine, should not be injected intravenously or mixed with other intravenous solutions, as it can lead to serious cardiopulmonary complications and even death. Before administering this medication, it is important to carefully read the warnings, adverse reactions, and dosage and administration sections of the monograph. Penicillin G benzathine should only be prescribed for the indications listed in the monograph.

Anaphylaxis: There have been reports of serious and occasionally fatal hypersensitivity reactions, including anaphylaxis, in patients on penicillin therapy. These reactions are more likely to occur in individuals with a history of penicillin hypersensitivity and/or a history of hypersensitivity to multiple allergens. It is important to inquire about previous hypersensitivity reactions to penicillins, cephalosporins, or other allergens before initiating therapy with Benzathine- benzylpenicillin. If an allergic reaction occurs, Benzathine- benzylpenicillin should be discontinued and appropriate therapy should be instituted immediately.

Clostridium difficile-associated disease: The use of Benzathine- benzylpenicillin may lead to Clostridium difficile-associated disease (CDAD), which can range from mild diarrhea to fatal colitis. CDAD should be considered in patients who present with diarrhea or symptoms of colitis, pseudomembranous colitis, toxic megacolon, or perforation of the colon after the administration of any antibacterial agent. Treatment with antibacterial agents may alter the normal flora of the colon and may permit overgrowth of Clostridium difficile. If the diagnosis of CDAD is suspected or confirmed, appropriate therapeutic measures should be initiated.

Susceptibility/Resistance: Prescribing Benzathine- benzylpenicillin in the absence of a proven or strongly suspected bacterial infection is unlikely to provide benefit to the patient and risks the development of drug-resistant bacteria. Therefore, it should only be prescribed for the indications listed in the monograph.

Usage of alcohol should be avoided while on Benzathine- benzylpenicillin medication, as alcohol might worsen the effects of any underlying disease condition, which includes conditions such as blurred vision, dizziness, etc.

According to the US Food and Drug Administration (FDA), Benzathine- benzylpenicillin is excreted in breast milk in small amounts, but there is no evidence of harm to the nursing infant.

Pregnancy Category B

The use of Benzathine- benzylpenicillin during pregnancy is not well studied, and it is not known if this drug can harm the fetus. While penicillin are generally considered safe during pregnancy, Benzathine- benzylpenicillin should only be used if it is absolutely necessary. Penicillin can cross the placenta, but the effect on the fetus is unknown.

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

The adverse reactions related to Benzathine- benzylpenicillin can be categorized as follows:

Common

• Pain or tenderness at the injection site
• Swelling, redness or hardness at the injection site
• Mild diarrhea, nausea or vomiting
• Skin rash or itching

Less common

• Headache
• Dizziness
• Joint pain
• Difficulty in breathing
• Palpitations
• Swelling of the face, lips, tongue or throat

Rare

• Anaphylactic reactions
• Serum sickness-like reactions
• Hemolytic anemia
• Thrombocytopenia
• Stevens-Johnson syndrome
• Toxic epidermal necrolysis

The clinically relevant drug interactions of Benzathine- benzylpenicillin are briefly summarized here:

• Probenecid: Probenecid is a medication used to treat gout and can also increase the levels of Benzathine- benzylpenicillin in the blood by reducing its excretion from the body. This can result in an increased risk of side effects from Benzathine- benzylpenicillin. Therefore, patients taking probenecid and Benzathine- benzylpenicillin should be closely monitored for adverse effects, and the dosage of Benzathine- benzylpenicillin may need to be adjusted.
• Methotrexate: Methotrexate is a medication used to treat cancer and certain autoimmune diseases, and Benzathine- benzylpenicillin can decrease its excretion from the body, leading to increased levels of methotrexate in the blood. This can increase the risk of methotrexate toxicity, such as bone marrow suppression and gastrointestinal toxicity. Patients taking both drugs should be closely monitored for adverse effects, and the dosage of methotrexate may need to be adjusted.
• Aminoglycosides: Aminoglycosides, such as gentamicin and tobramycin, are antibiotics that can be used to treat serious infections. Benzathine- benzylpenicillin can interact with aminoglycosides, leading to decreased effectiveness of both drugs. This is because Benzathine- benzylpenicillin can inactivate the aminoglycosides in the bloodstream. If a patient needs to take both drugs, their healthcare provider may need to adjust the dosages or choose an alternative antibiotic.
• Tetracyclines: Tetracyclines, such as doxycycline and minocycline, are antibiotics used to treat various infections. Benzathine- benzylpenicillin can interact with tetracycline antibiotics, leading to decreased effectiveness of both drugs. This is because Benzathine- benzylpenicillin can inactivate the tetracyclines in the bloodstream. Patients taking both drugs may need to be monitored closely for adverse effects, and the dosage of either drug may need to be adjusted.
• Oral contraceptives: Benzathine- benzylpenicillin can decrease the effectiveness of oral contraceptives, increasing the risk of unintended pregnancy. This is because Benzathine- benzylpenicillin can interfere with the absorption and metabolism of estrogen in the body. Women taking oral contraceptives and Benzathine- benzylpenicillin should use a backup method of contraception, such as condoms, during treatment with Benzathine- benzylpenicillin and for a few days afterward.
• Warfarin: Warfarin is a blood thinner used to prevent blood clots. Benzathine- benzylpenicillin can interact with warfarin, leading to an increased risk of bleeding. This is because Benzathine- benzylpenicillin can decrease the metabolism of warfarin in the liver, leading to increased levels of warfarin in the blood. Patients taking both drugs should be closely monitored for signs of bleeding, and the dosage of warfarin may need to be adjusted.

The following are the side effects involving Benzathine- benzylpenicillin:

• Injection site pain or discomfort
• Swelling at the injection site
• Skin rash or itching
• Nausea
• Vomiting
• Diarrhea
• Headache
• Fever or chills
• Joint pain or muscle pain
• Fatigue or weakness
• Dizziness or lightheadedness.

• Pregnancy

Pregnancy Category B

The use of Benzathine- benzylpenicillin during pregnancy is not well studied, and it is not known if this drug can harm the fetus. While penicillins are generally considered safe during pregnancy, Benzathine- benzylpenicillin should only be used if it is absolutely necessary. Penicillins can cross the placenta, but the effect on the fetus is unknown.

• Lactation

According to the US Food and Drug Administration (FDA), Benzathine- benzylpenicillin is excreted in breast milk in small amounts, but there is no evidence of harm to the nursing infant.

• Pediatric use

No Specific Data is available

• Geriartic

There is not enough data to determine if elderly patients respond differently to Benzathine- benzylpenicillin compared to younger patients. Therefore, it is recommended to use caution when selecting the dose for elderly patients and start at the lower end of the dosing range. Since the drug is excreted by the kidneys, patients with impaired renal function may be at a higher risk for toxic reactions. Therefore, it may be useful to monitor renal function in elderly patients.

Physicians should be knowledgeable and vigilant about the treatment and identification of over dosage of Benzathine- benzylpenicillin.

An overdose of benzathine- benzylpenicillin can lead to adverse effects, including hypersensitivity reactions, neurotoxicity, and nephrotoxicity.

Hypersensitivity reactions can range from mild skin rash to severe anaphylactic shock, which can be life-threatening. Patients with a history of penicillin allergy are at increased risk of developing an allergic reaction to benzathine- benzylpenicillin. Immediate medical attention should be sought if any signs of an allergic reaction occur, such as hives, difficulty breathing, swelling of the face or throat, or severe itching.

Neurotoxicity can manifest as seizures, confusion, agitation, or hallucinations. This adverse effect is more common in patients with renal impairment or those receiving high doses of the drug. The drug should be used with caution in patients with a history of seizures or other neurological disorders.

Nephrotoxicity can occur due to the accumulation of the drug or its metabolites in the kidneys, leading to tubular necrosis or interstitial nephritis. Patients with impaired renal function or those receiving high doses of the drug are at increased risk of developing this adverse effect. The drug's dosage should be adjusted in patients with renal impairment, and renal function should be monitored during treatment.

In case of an overdose, supportive care and symptomatic treatment should be initiated. The drug can be removed from the body by hemodialysis or peritoneal dialysis in patients with severe toxicity or renal impairment.

Overall, benzathine- benzylpenicillin should be used with caution, and its dosage should be adjusted according to the patient's renal function and susceptibility to allergic reactions. Immediate medical attention should be sought in case of any adverse effects.

Pharmacodynamics

The pharmacodynamics of benzathine- benzylpenicillin involves its mechanism of action against susceptible bacteria. Penicillin, including benzathine- benzylpenicillin, work by inhibiting the synthesis of the bacterial cell wall, leading to cell lysis and death.

Benzathine- benzylpenicillin exhibits bactericidal activity against a wide range of gram-positive and some gram-negative bacteria, including Streptococcus pyogenes, Streptococcus pneumoniae, and Neisseria meningitidis. The drug's efficacy depends on the bacterial strain's susceptibility, the site of infection, and the host's immune response.

The time above the minimum inhibitory concentration (MIC) is an important pharmacodynamic parameter that affects the drug's efficacy. In general, prolonged exposure to drug concentrations above the MIC results in better bactericidal activity. Benzathine- benzylpenicillin has a long half-life and can maintain serum concentrations above the MIC for several days, allowing for effective treatment of bacterial infections with a single dose.

However, the drug's efficacy can be compromised by bacterial resistance, which can occur due to various mechanisms, including the production of beta-lactamase enzymes that hydrolyze the penicillin molecule or alterations in the bacterial cell wall target sites.

Pharmacokinetics

When intramuscular penicillin G benzathine is injected, it is slowly absorbed into the bloodstream and then converted into penicillin G through hydrolysis. Due to this slow absorption and hydrolysis process, the blood serum levels of penicillin G benzathine are lower but more sustained than other parenteral penicillin.

A dose of 300,000 units of penicillin G benzathine in adults will result in blood levels of 0.03 to 0.05 units per mL that can last for 4 to 5 days. Larger doses of 600,000 units and 1,200,000 units can maintain similar blood levels for up to 10 and 14 days, respectively. Even after 4 weeks, blood concentrations of 0.003 units per mL can still be detected following a dose of 1,200,000 units.

Around 60% of penicillin G is bound to serum protein, and the drug is distributed throughout the body's tissues, with the highest concentrations found in the kidneys, followed by the liver, skin, and intestines. Penicillin G can penetrate all other tissues to a lesser degree, with only a small amount found in the cerebrospinal fluid.

When kidney function is normal, the drug is excreted quickly through tubular excretion. However, excretion may be delayed in neonates, young infants, and individuals with impaired kidney function.

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