Benzylpenicillin Benzathine

Brands of Benzylpenicillin Benzathine  in Kenya

Dawadur , Dawa Limited

Retardpen, Medisel Kenya Ltd

Benzathine benzylpenicillin, is also known as benzathine penicillin G.


Benzylpenicillin Benzathine in Kenya : Side effects, Price, Cost uses, Brands
Benzylpenicillin Benzathine Chemical Structure

MODE OF ACTION

This type of antibiotic inhibits biosynthesis of the cell wall peptidoglycan during the stage of active multiplication. This results in an osmotically unstable cell wall, leading to lysis of the cell wall, subsequent destruction of the bacterial cell, and death.

It is in the penicillin class of medications. It is slowly absorbed into the circulation, after intramuscular injection, and hydrolysed to benzylpenicillin in vivo. It is the drug-of-choice when prolonged low concentrations of benzylpenicillin are required and appropriate, allowing prolonged antibiotic action over 2–4 weeks after a single IM dose.

Benzathine is used as stabilizer to prolong its effect

INDICATIONS

Benzylpenicillin benzathine is indicated in adults, adolescents, children and neonates for the treatment and prophylaxis of the following infections:

For the treatment of:

– erysipelas

– syphilis: early syphilis (primary and secondary)

– latent syphilis (except for neurosyphilis and presence of pathological CSF findings)

– yaws

– pinta

For the prophylaxis of:

– rheumatic fever (chorea, rheumatic carditis)

– poststreptococcal glomerulonephritis

– erysipelas

Consideration should be given to official guidance on the appropriate use of antibacterial agents.

DOSAGE AND ADMINISTRATION

The dosing recommendations depend on the severity and the type of infection, the age and the hepato-renal function of patients.

Dosage and duration of treatment

1. General therapy:

 

– Adults and adolescents:1.2 Million I.U.
– Children (> 30 kg body weight):1.2 Million I.U.
– Children (< 30 kg body weight):0.6 Million I.U.
Duration of treatment:Single dose

 

Note: In streptococcal diseases, a 10-day minimum course of treatment should be observed to avoid secondary diseases. This is generally ensured with a single injection of 0.6 Million I.U., 1.2 Million I.U. or 2.4 Million I.U..

2. Treatment of syphilis:

Primary and secondary stage

 

– Adults and adolescents:2.4 Million I.U.
– Children:50,000 IU per kg body weight; however not more than 2.4 Million I.U.
Duration of treatment:Single dose (If clinical symptoms recur or laboratory findings remain strongly positive, treatment should be repeated.)

 

Late-stage syphilis (latent seropositive syphilis)

 

– Adults and adolescents:2.4 Million I.U.
– Children:50,000 IU per kg body weight per week; however not more than 2.4 Million I.U.
Duration of treatment:Once weekly for 3 weeks

 

Treatment of congenital syphilis (without neurological involvement)

 

– Neonates and infants:50,000 IU per kg body weight
Duration of treatment:Single dose

 

3. Treatment of yaws and pinta:

 

Adults and adolescents:1.2 Million I.U.
– Children (> 30 kg body weight):1.2 Million I.U.
– Children (< 30 kg body weight):0.6 Million I.U.
Duration of treatment:Single dose

 

4. Prophylaxis of rheumatic fever, poststreptococcal glomerulonephritis and erysipelas:

 

– Adults and adolescents:1.2 Million I.U.
– Children (> 30 kg body weight):1.2 Million I.U.
– Children (< 30 kg body weight):0.6 Million I.U.
Duration of treatment:
a) without cardiac involvement:at least 5 years (or up to 21 years of age) every 3-4 weeks
b) transient cardiac involvement:at least 10 years (or up to 21 years of age) every 3-4 weeks
c) persistent cardiac involvement:at least 10 years (or up to 40 years of age) every 3-4 weeks; life-long prophylaxis is sometimes necessary

CONTRAINDICATIONS

– Hypersensitivity to penicillins or any of the excipients.

– History of a severe immediate hypersensitivity reaction (e.g. anaphylaxis) to another beta-lactam agent (e.g. cephalosporin, carbapenem or monobactam).

DRUG INTERACTIONS

Concomitant administration of benzylpenicillin benzathine is not recommended with:

– bacteriostatic antibiotics: based on the general principle not to combine bactericidal and bacteriostatic antibiotics.

Caution should be exercised when co-administering the following:

– probenecid: the administration of probenecid leads to inhibition of the tubular secretion of benzylpenicillin, resulting in an increase in the serum concentration and prolongation of the elimination half-life. Furthermore, probenecid inhibits the penicillin transport from the cerebrospinal fluid, so that the concomitant administration of probenecid reduces the penetration of benzylpenicillin into brain tissue even further.

– methotrexate: when taken at the same time as benzylpenicillin benzathine, the excretion of methotrexate is reduced. This can lead to increased methotrexate toxicity. The combination with methotrexate is not recommended.

– anticoagulants: concomitant use with oral anticoagulants may increase the antivitamin K effect and the risk of bleeding. It is recommended that the International Normalised Ratio (INR) is monitored frequently and the posology of the antivitamin K drug adjusted accordingly, both during and after treatment with benzylpenicillin benzathine.

ADVERSE EFFECTS

MedDRA

System Organ class

Common (> 1/100 to < 1/10)Uncommon (> 1/1,000 to < 1/100)Rare (> 1/10,000 to < 1/1,000)Very rare (< 1/10,000)Frequency not known (cannot be estimated from available data)
Infections and infestationsCandidiasis
Blood and lymphatic system disordersHaemolytic anaemia

Leukopenia

Thrombocytopenia

Agranulocytosis

Immune system disordersAllergic reactions

Urticaria

Angioedema

Erythema multiform

Exfoliative dermatitis

Fever

Arthralgia

Anaphylactic shock with collapse and anaphylactoid reactions (asthma, purpura, gastrointestinal symptoms)

Serum sickness
Gastrointestinal disordersDiarrhoea

Nausea

Stomatitis and glossitis

Vomiting

Pseudomembr anous colitis
Hepatobiliary disordersHepatitis

Cholestasis

Renal and urinary disordersNephropathy

Interstitial nephritis

General disorders and administration site conditionsPain at the injection site

Injection site infiltrates

Hoigné syndrome

Nicolau syndrome

InvestigationsPositive direct

Coombs’ test

False-positive urinary protein determination when precipitation techniques are used (Folin- Ciocalteu-Lowry method, biuret method)

False-positive urinary amino acid determination (ninhydrin method)

Simulation of pseudobisalbumin aemia when using electrophoresis methods to determine albumin

False-positive nonenzymatic urinary glucose detection and urobilinogen detection

Increased levels when determining 17ketosteroids in urine (when the Zimmermann reaction is used) (see section 4.4)

Reporting of suspected adverse reactions:

The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting, and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorization of the medicinal product are important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, pv@pharmacyboardkenya.org or clicking below button:


Benzylpenicillin Benzathine in Kenya
Benzylpenicillin Benzathine in Kenya
Benzylpenicillin Benzathine in Kenya
Benzylpenicillin Benzathine in Kenya
Benzylpenicillin Benzathine in Kenya
Penicillin G benzathine Price / Brands in Kenya

Clinical | Pharmacokinetic data


Pregnancy Category: B (No risk in non-human studies)
Routes of Administration: IM
Bioavailability: Not Available
Protein Binding: Not Available
Metabolosim: Not Available
Onset of Action: Not Available
Elimination Half life: Not Available
Excretion: Not Available

Legal Status | Dosage forms & Strengths


Prescription Category:
Prescription only Medicine (POM) , ℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This drug is not a controlled substance under Narcotic Drugs and Psychotropic Substances (Control ) Act
Dosage Forms | Strengths:


Drug Indentifiers:

CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
E number
  • E708
CompTox Dashboard (EPA)
ECHA InfoCard


Drug Images

References/ Citation:




What was the patient being treated for
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