Benzathine benzylpenicillin parenteral
- Drugs List
- Therapeutic Indications
- Dosage
- Administration
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Injections of benzathine benzylpenicillin.
Drugs List
Therapeutic Indications
Uses
Infections sensitive to penicillin
Syphilis
Benzathine benzylpenicillin is indicated for the treatment of erysipelas, early syphilis (primary and secondary), latent syphilis (except for neurosyphilis and presence of pathological CSF findings), yaws and pinta.
Benzathine benzylpenicillin is indicated for the prophylaxis of rheumatic fever (chorea, rheumatic carditis), poststreptococcal glomerulonephritis and erysipelas.
Dosage
The dosing recommendations depend on the severity and the type of infection, the age and the hepato-renal function of patients.
Adults
General therapy
1.2 million I.U. in a single dose.
In streptococcal diseases, a minimum course of treatment is 10 days in order to avoid secondary diseases. Generally this is ensured with a single injection of 0.6 Million I.U., 1.2 Million I.U. or 2.4 Million I.U.
Treatment of syphilis
Primary and secondary stage: 2.4 Million I.U. in a single dose (if symptoms recur or laboratory findings remain strongly positive, treatment should be repeated).
Late-stage syphilis: 2.4 Million I.U. once weekly for 3 weeks.
Treatment of yaws and pinta
1.2 Million I.U. in a single dose.
Prophylaxis of rheumatic fever, poststreptococcal glomerulonephritis and erysipelas
1.2 Million I.U.
Duration of treatment in patients without cardiac involvement is at least 5 years (or up to 21 years of age) every 3 to 4 weeks.
Duration of treatment in patients with transient cardiac involvement is at least 10 years (or up to 21 years of age) every 3 to 4 weeks.
Duration of treatment in patients with persistent cardiac involvement is at least 10 years (or up to 40 years of age) every 3 to 4 weeks, life long prophylaxis is sometimes necessary.
Children
General therapy
Children with a bodyweight over 30kg: 1.2 Million I.U. in a single dose.
Children with a bodyweight less than 30kg: 0.6 Million I.U. in a single dose.
In streptococcal diseases, a minimum course of treatment is 10 days in order to avoid secondary diseases. Generally this is ensured with a single injection of 0.6 Million I.U., 1.2 Million I.U. or 2.4 Million I.U.
Treatment of syphilis
Primary and secondary stage
Adolescents: 2.4 Million I.U. in a single dose.
Children: 50,000 I.U. per kg bodyweight. Max 2.4 Million I.U. in a single dose.
If symptoms recur or laboratory findings remain strongly positive, treatment should be repeated.
Late-stage syphilis
Adolescents: 2.4 Million I.U. once weekly for 3 weeks
Children: 50,000 I.U. per kg bodyweight per week. Once weekly for 3 weeks. Max 2.4 Million I.U.
Treatment of congenital syphilis (without neurological involvement)
Neonates and infants: 50,000 I.U. per kg bodyweight in a single dose.
Treatment of yaws and pinta
Children with a bodyweight over 30kg: 1.2 Million I.U. in a single dose.
Children with a bodyweight less than 30kg: 0.6 Million I.U. in a single dose.
Prophylaxis of rheumatic fever, poststreptococcal glomerulonephritis and erysipelas
Children with a bodyweight over 30kg: 1.2 Million I.U.
Children with a bodyweight less than 30kg: 0.6 Million I.U.
Duration of treatment in patients without cardiac involvement is at least 5 years (or up to 21 years of age) every 3 to 4 weeks.
Duration of treatment in patients with transient cardiac involvement is at least 10 years (or up to 21 years of age) every 3 to 4 weeks.
Duration of treatment in patients with persistent cardiac involvement is at least 10 years (or up to 40 years of age) every 3 to 4 weeks, life long prophylaxis is sometimes necessary.
Patients with Renal Impairment
Creatinine clearance 15 to 59ml/min: 75% of the normal daily dose. 1 single administration.
Creatinine clearance of less than 15ml/min: 20 to 50% of the normal daily dose. 1 to 3 Million I.U. per day maximum. In 2-3 single administrations.
Administration
Benzathine benzylpenicillin is for intramuscular injection.
Benzathine benzylpenicillin should be administered by deep intramuscular injection into the upper, outer quadrant of the gluteus maximus or Hochstetter's ventrogluteal field, with the needle pointing towards the iliac crest or according to von Hochstetter's method. Aspiration must be performed prior to the injection. If aspiration of blood or pain occurs during the injection, treatment should be discontinued.
The mid-lateral thigh muscles are recommeded as an injection site in children. The deltoid muscle is only suitable if it is well formed.
In young children and infants, the peripheral area of the upper outer quadrant of the gluteal region should only be used as an injection site in exceptional cases in order to avoid sciatic nerve lesions.
Contraindications
None known
Precautions and Warnings
Atopy
History of serious hypersensitivity reactions
Asthma
Breastfeeding
Haemodialysis
Hepatic impairment
Pregnancy
Renal impairment - creatinine clearance below 60ml/minute
Jarisch-Herxheimer reaction possible in treatment of syphilis
Reduce dose in patients with creatinine clearance below 60ml/min
Advise ability to drive/operate machinery may be affected by side effects
Before initiating therapy enquire about previous hypersensitivity reactions
Consult national/regional policy on the use of anti-infectives
Contains polysorbate
Contains soya or soya derivative
To avoid side effects care should be taken when choosing the injection site
Monitor renal, hepatic and haematological parameters
Consider pseudomembranous colitis if patient presents with diarrhoea
Monitor for hypersensitivity reactions for at least 30 mins after admin
Para-allergic reactions may occur in patients with dermatomycosis
Prolonged use may result in superinfection with non-susceptible organisms
Test interference: May cause false positive Coombs test
May affect results of some laboratory tests
Discontinue at once if pseudomembranous colitis occurs
Discontinue if allergic reaction occurs
Not licensed for all indications in all age groups
If possible, a hypersensitivity test should be performed prior to treatment. Advise patients of the possible occurrence of allergic symptoms and the need to report them.
Beta-lactams are associated with a risk of encephalopathy (confusion, altered levels of consciousness, epilepsy or movement abnormalities), particularly in cases of over-dose or impaired renal function.
During treatment of syphilis, a Jarisch-Herxheimer reaction may occur. Within 2 to 12 hours after administration headaches, fever, sweating, shivering, myalgia, arthralgia, nausea, tachycardia, increased blood pressure followed by hypotension may occur. These symptoms resolve after 10 to 12 hours. Patients should be informed that this is a usual, transient sequela of antibiotic therapy. Appropriate therapy should be instituted to suppress a Jarisch-Herxheimer reaction.
If neurological involvement cannot be excluded in patients with congenital syphilis, forms of penicillin that reach a higher level in cerebrospinal fluid should be used.
Delayed excretion of povidone should be taken into consideration in patients with renal impairment. Frequent or prolonged use of benzathine benzylpenicillin may very rarely lead to the accumulation of povidone in the reticuloendothelial system (RES), or to local deposits and the formation of foreign body granulomas which may be confused with tumours.
Pregnancy and Lactation
Pregnancy
Use benzathine benzylpenicillin with caution during pregnancy.
The manufacturer advises caution if benzathine benzylpenicillin is used during pregnancy. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. 10-30% of maternal plasma concentrations are found in the foetal circulation. High concentrations are also reached in the amniotic fluid.
Lactation
Use benzathine benzylpenicillin with caution during breastfeeding.
The manufacturer advises benzathine benzylpenicillin should be used with caution during breastfeeding. Benzathine benzylpenicillin is excreted in human milk in small amounts, concentrations may reach 2 to 15% of the mother's serum concentrations. No undesirable effects in infants have been observed. Breastfeeding should be discontinued in the event of diarrhoea, candidosis or rash in the child. In infants that are also being fed on baby food, mothers should express and discard breast milk during treatment, breastfeeding can be resumed 24 hours after finishing treatment.
Side Effects
Agranulocytosis
Allergic reaction
Anaphylactic shock
Anaphylactoid reaction
Angioedema
Antibiotic-associated colitis
Arthralgia
Candidiasis
Cholestasis
Diarrhoea
Encephalopathy
Erythema multiforme
Exfoliative dermatitis
Fever
Glossitis
Haemolytic anaemia
Hepatitis
Hypersensitivity reactions
Interstitial nephritis
Jarisch-Herxheimer reaction
Leukopenia
Local pain (injection site)
Nausea
Necrosis (intramuscular injection site)
Nephropathy
Pseudomembranous colitis
Serum sickness
Stomatitis
Thrombocytopenia
Urticaria
Vomiting
Effects on Laboratory Tests
Positive direct Coombs' test often occurs in patients receiving 10 million I.U. benzylpenicillin or more per day. After discontinuation of treatment, the direct antiglobulin test may remain positive for 6 to 8 weeks.
Determination of urinary protein using precipitation techniques, the Folin-Ciocalteu-Lowry method or the biuret method may lead to false positive results. Urinary protein should therefore be determined by other methods.
False-positive results can occur using the ninhydrin method to determine urinary amino acids.
Pseudobisalbuminaemia may be simulated in electrophoresis methods to determine albumin.
Non-enzymatic urinary glucose detection and urobilinogen detection may exhibit a false positive.
When determining 17-ketosteroids (using the Zimmermann reaction) in the urine, increased values may occur during therapy with benzathine benzylpenicillin.
Further Information
Last Full Review Date: October 2021
Reference Sources
Summary of Product Characteristics: Benzylpenicillin benzathine 1.2 Million I.U. powder and solvent for suspension for injection. Brancaster Pharma Ltd. Revised August 2021.
Summary of Product Characteristics: Benzylpenicillin benzathine 2.4 Million I.U. powder and solvent for suspension for injection. Brancaster Pharma Ltd. Revised August 2021.
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