Chemical formula: C₁₆H₁₈N₂O₄S Molecular mass: 334.39 g/mol PubChem compound: 5904
Benzylpenicillin interacts in the following cases:
For doses of 0.6-1.2 g (1-2 mega units) the dosing interval should be no more frequent than every 8-10 hours.
For high doses e.g. 14.4 g (24 mega units) required for the treatment of serious infections such as meningitis, the dosage and dose interval of benzylpenicillin sodium should be adjusted in accordance with the following schedule:
Creatinine clearance (ml per minute) | Dose (g) | Dose (mega units) | Dosing interval (hours) |
---|---|---|---|
125 | 1.2 or | 2 or | 2 |
1.8 | 3 | 3 | |
60 | 1.2 | 2 | 4 |
40 | 0.9 | 1.5 | 4 |
20 | 0.6 | 1.0 | 4 |
10 | 0.6 | 1.0 | 6 |
Nil | 0.3 or | 0.5 | 6 |
0.6 | 1.0 | 8 |
The dose in the above table should be further reduced to 300 mg (0.5 mega units) 8 hourly if advanced liver disease is associated with severe renal failure.
If haemodialysis is required, an additional dose of 300 mg (0.5 mega units) should be given 6 hourly during the procedure.
For doses of 0.6-1.2 g (1-2 mega units) the dosing interval should be no more frequent than every 8-10 hours.
For high doses e.g. 14.4 g (24 mega units) required for the treatment of serious infections such as meningitis, the dosage and dose interval of benzylpenicillin sodium should be adjusted in accordance with the following schedule:
Creatinine clearance (ml per minute) | Dose (g) | Dose (mega units) | Dosing interval (hours) |
---|---|---|---|
125 | 1.2 or | 2 or | 2 |
1.8 | 3 | 3 | |
60 | 1.2 | 2 | 4 |
40 | 0.9 | 1.5 | 4 |
20 | 0.6 | 1.0 | 4 |
10 | 0.6 | 1.0 | 6 |
Nil | 0.3 or | 0.5 | 6 |
0.6 | 1.0 | 8 |
The dose in the above table should be further reduced to 300 mg (0.5 mega units) 8 hourly if advanced liver disease is associated with severe renal failure.
If haemodialysis is required, an additional dose of 300 mg (0.5 mega units) should be given 6 hourly during the procedure.
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.
Massive doses of benzylpenicillin can cause hypokalaemia and sometimes hypernatraemia. Use of a potassium-sparing diuretic may be helpful. In patients undergoing high-dose treatment for more than 5 days, electrolyte balance, blood counts and renal functions should be monitored.
Pseudomembranous colitis should be considered in patients who develop severe and persistent diarrhoea during or after receiving benzylpenicillin. In this situation, even if Clostridium difficile is only suspected, administration of benzylpenicillin should be discontinued and appropriate treatment given.
Benzylpenicillin has been taken by a large number of pregnant women and women of childbearing age without an increase in malformations or other direct or indirect harmful effects on the foetus having been observed.
Although it is not known if benzylpenicillin may be excreted into the breast milk of nursing mothers, it is actively transported from the blood to milk in animals and trace amounts of other penicillins in human milk have been detected.
None.
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).
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).
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.
Rare (0.01%-0.1%): Interstitial nephritis has been reported after intravenous benzylpenicillin sodium at doses of more than 12 g per day.
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