Benzylpenicillin

Brands of Benzylpenicillin in Kenya

Benzapene , Crown Healthcare

Carepenlin , Careplus Limited

LC Xpen Benzyl Penicillin Sodium, Reyoung Pharmaceuticals Co. Ltd

Injpen , Inject Care Parenterals Pvt Ltd

Medipen , Medisel Kenya Ltd

Penicillin G Sodium , Dawa Limited

Benzylpenicillin, is also known as penicillin G.


Benzylpenicillin in Kenya : Brands, Uses, Dose in Syphilis, Price in Kenya
Benzylpenicillin Chemical Structure

MODE OF ACTION

By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, penicillin G inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that penicillin G interferes with an autolysin inhibitor

INDICATIONS

Benzylpenicillin is indicated for most wound infections, pyogenic infections of the skin, soft tissue infections and infections of the nose, throat, nasal sinuses, respiratory tract and middle ear, etc.

It is also indicated for the following infections caused by penicillin-sensitive microorganisms: Generalised infections, septicaemia and pyaemia from susceptible bacteria. Acute and chronic osteomyelitis, sub-acute bacterial endocarditis and meningitis caused by susceptible organisms. Suspected meningococcal disease. Gas gangrene, tetanus, actinomycosis, anthrax, leptospirosis, rat-bite fever, listeriosis, severe Lyme disease, and prevention of neonatal group B streptococcal infections. Complications secondary to gonorrhoea and syphilis (e.g. gonococcal arthritis or endocarditis, congenital syphilis and neurosyphilis). Diphtheria, brain abscesses and pasteurellosis.

Consideration should be given to official local guidance (e.g. national recommendations) on the appropriate use of antibacterial agents.

Susceptibility of the causative organism to the treatment should be tested (if possible), although therapy may be initiated before the results are available

DOSAGE AND ADMINISTRATION

The following dosages apply to both intramuscular and intravenous injection.

Alternate sites should be used for repeated injections.

Adults

600 to 3,600 mg (1 to 6 mega units) daily, divided into 4 to 6 doses, depending on the indication. Higher doses (up to 14.4 g/day (24 mega units) in divided doses) may be given in serious infections such as adult meningitis by the intravenous route.

In bacterial endocarditis, 7.2 to 12 g (12 to 20 mega units) or more may be given daily in divided doses by the intravenous route, often by infusion.

Doses up to 43.2 g (72 mega units) per day may be necessary for patients with rapidly spreading gas gangrene.

High doses should be administered by intravenous injection or infusion, with intravenous doses in excess of 1.2g (2 mega units) being given slowly, taking at least one minute for each 300 mg (0.5 mega unit) to avoid high levels causing irritation of the central nervous system and/or electrolyte imbalance.

High dosage of benzylpenicillin sodium may result in hypernatraemia and hypokalaemia unless the sodium content is taken into account.

For the prevention of Group B Streptococcal disease of the newborn, a 3 g (5 mega units) loading dose should be given to the mother initially, followed by 1.5 g (2.5 mega units) every 4 hours until delivery.

Children aged 1 month to 12 years

100 mg/kg/day in 4 divided doses; not exceeding 4 g/day.

 

Infants 1-4 weeks

75 mg/kg/day in 3 divided doses.

 

Newborn Infants

50 mg/kg/day in 2 divided doses.

 

Meningococcal disease

 

Children 1 month to 12 years:180-300 mg/kg/day in 4-6 divided doses, not exceeding 12 g/day.
Infants 1-4 weeks:150 mg/kg/day in 3 divided doses.
Newborn infants:100 mg/kg/day in 2 divided doses.
Adults and children over 12 years:2.4 g every 4 hours

 

Suspected meningococcal disease

If meningococcal disease is suspected general practitioners should give a single dose of benzylpenicillin sodium, before transferring the patient to hospital, as follows:

 

Adults and children over 10 years:1,200 mg IV (or IM)
Children 1-9 years:600 mg IV (or IM)
Children under 1 year:300 mg IV (or IM)

 

Premature babies and neonates

Dosing should not be more frequent than every 8 or 12 hours in this age group, since renal clearance is reduced at this age and the mean half-life of benzylpenicillin may be as long as 3 hours.

Since infants have been found to develop severe local reactions to intramuscular injections, intravenous treatment should preferably be used.

CONTRAINDICATIONS

Allergy to penicillins. Hypersensitivity to any ingredient of the preparation.

Cross allergy to other beta-lactams such as cephalosporins should be taken into account.

DRUG INTERACTIONS

The efficacy of oral contraceptives may be impaired under concomitant administration of benzylpenicillin sodium, which may result in unwanted pregnancy. Women taking oral contraceptives should be aware of this and should be informed about alternative methods of contraception.

There is reduced excretion of methotrexate (and therefore increased risk of methotrexate toxicity) when used with benzylpenicillin sodium.

Probenecid inhibits tubular secretion of benzylpenicillin sodium and so may be given to increase the plasma concentrations.

Penicillins may interfere with:

  • Urinary glucose test
  • Coomb’s tests
  • Tests for urinary or serum proteins
  • Tests which use bacteria e.g. Guthrie test.

ADVERSE EFFECTS

Blood and Lymphatic System Disorders

Rare (0.01% – 0.1%)

Haemolytic anaemia and granulocytopenia (neutropenia), agranulocytosis, leucopenia and thrombocytopenia, have been reported in patients receiving prolonged high doses of benzylpenicillin sodium (eg. Subacute bacterial endocarditis).

Immune System Disorders

Very Common (>10%)

Patients undergoing treatment for syphilis or neurosyphilis with benzylpenicillin may develop a Jarisch-Herxheimer reaction.

Common (1-10%)

Hypersensitivity to penicillin in the form of rashes (all types), fever, and serum sickness may occur (1-10% treated patients). These may be treated with antihistamine drugs.

Rare (0.01%-0.1%)

More rarely, anaphylactic reactions have been reported (<0.05% treated patients).

Nervous System Disorders

Rare (0.01%-.01%)

Central nervous system toxicity, including convulsions, has been reported with massive doses over 60 g per day and in patients with severe renal impairment.

Renal and Urinary Disorders

Rare (0.01%-0.1%)

Interstitial nephritis has been reported after intravenous benzylpenicillin sodium at doses of more than 12 g per day.

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:


Clinical | Pharmacokinetic data


Pregnancy Category: B (No risk in non-human studies)
Routes of Administration: IV, IM
Bioavailability: Not Available
Protein Binding: 60%
Metabolosim: Liver
Onset of Action: N/A
Elimination Half life: 30 min
Excretion: Kidney

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
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
E number
CompTox Dashboard (EPA)
ECHA InfoCard


Drug Images

References/ Citation:




What was the patient being treated for
%d bloggers like this: