SHEPHERD PENICILLIN INJECTIONS
ACTIONS AND USES
The penicillins act mainly by interfering with the synthesis of the bacterial cell membrane and are therefore more effective when the bacterial cell is growing. The penicillins are mainly used to treat infections by the Gram-positive pyrogenic organisms. As Benzylpenicillin is largely destroyed by the acid in the gastric juice it is administered parenterally.
a) Penicillin G Sodium Potassium: Each vial contains Benzylpenicillin Sodium or Potassium BP equivalent to 300, 600, 3.000 or 6.000mg Benzylpenicillin (abt. 0,5;1;5 or 10 Mega units).
b) Procaine Penicillin: Each vial contains 3.000mg Procaine Penicillin BP/USP (abt. 3 Mega units) as powder for injection, in aqueous or oily suspension.
c) Benzathine Penicillin: Each vial contains 900 or 1.800 mg Benzathine Penicillin BP/USP (abt. 1,2 or 2,4 Mega units).
d) Fortified Procaine Penicillin: Each vial contains 60,120, 150 or 600 mg Benzylpenicillin BP and 300, 600, 750 or 3.000 mg Procaine Penicillin BP (abt. 0,4; 0,8; 1 or 4 Mega units).
e) Bipenicillin: Each vial contains 240 mg Benzylpenicillin BP and 600 mg Procaine Penicillin BP (abt. 1 Mega units).
f) Tripenicillin: Each vial contains 180mg Benzylpenicillin Sodium or Potassium BP, 300 mg Procaine Penicillin BP and 450 mg Benzathine Penicillin BP (abt. 1,2 Mega units).
Penicillins are used in the treatment of a variety of infections due to susceptible organisms, including wound infections, abscesses, boils, diphteria, acute tonsilllitis, actinomycosis, anthrax, gas gangrene, tetanus, erysipelas, pneumococcal pneumonia, scarlet fever, rheumatic fever, some types of subacute bacterial endo-carditis, acute osteomyelitis, otitis media, mastoiditis, meningo-coccal infections, Vincent’s infection, gonorrhoea, syphilis, rat-bite fever, leptospirosis, yaws and pinta.
Benzathine Penicillin is used for the treatment of infections due to microorganisms highly susceptible to Benzylpenicillin. In acute infections, and when bacteraemia is present, the initial treatment should be with Benzylpenicillin by injection. Benzathine Penicillin may be used in the treatment of syphilis.
However, Procaine Penicillin is often preferred.
Benzathine Penicillin should not be used in the treatment of gonorrhoea.
Procaine Penicillin Is suitable for domiciliary treatment, its use should be restricted to infections caused by microorganisms that are highly sensitive to penicillin. For the treatment of severe acute infections, when an immediate high concentration of penicillin in the blood is necessary, Benzylpenicillin may be injected simultaneously with Procaine Penicillin. The duration of detectable amounts of penicillin in the serum has been still further prolonged by intramuscular injection of Procaine Penicillin in suspension of an oily vehicle.
Penicillin must not be given to patients known to be sensitive to penicillins and it must not be used for the treatment of infections due to penicillinase -producing organisms.
In general, penicillin is well tolerated. As in the case of all penicillins, however, anaphylactic reactions may supervene. In such cases of hypersensitivity treatment must be discontinued, it is also possible that nausea, diarrhea, digestive disorders, or skin rashes in the form of maculopapular exanthem maybe seen. Large doses of procaine containing preparations given more frequently than once daily may give rise to undesirable effects due to the absorption of procaine and leave painful lumps at the injection site.
As with all antibiotics, penicillins should not be used either prophylactically or for an established infection unless there is a positive indication that it is necessary. Penicillins should only be given to patients thought to be allergic to it if there is no satisfactory alternative and the infection is life threatening. Preparations should be made to deal with anaphylactic shock before the first dose is given. When high doses are given the effect of the associated sodium or potassium ions should be taken into account and the appropriate salt or mixture of salts should be used.
Penicillins cross the placenta. Although problems in humans have not been documented, risk-benefit during pregnancy must be considered. Penicillins are excreted in breast milk, some in low concentrations. Although significant problems in humans have not been documented, risk-benefit must be considered.
TREATMENT OF ADVERSE EFFECTS
When cutaneous reactions occur they may subside spontaneously within a few hours or days or when penicillin is withdrawn.
At the first sign of an immediate reaction to penicillin treatment, 0,3 to 1ml of Adrenalin injection should be given intramuscularly (or in severe cases 0,2 ml well diluted intravenously) followed by a further dose if no improvement occurs. This should be followed by an antihistamine, such as diphenhydramine, chlorpheniramine, given parenterally, and a corticosteroid given intravenously, If bronchospasm is severe aminophylline (250 mg in 10 ml) may be given intravenously. Assisted respiration is necessary if there is upper airways obstruction. Plasma or suitable electrolyte solutions should be given intravenously if circulatory failure occurs. Urticaria and joint pains, if severe, may be treated with corticosteroids by mouth.
Concurrent use of Allopurinol may increase the possibility of skin rash, especially in hyperuricemic patients. Effects of Coumarin and indandione-derivative anticoagulants may be increased when used concurrently. Concurrent or subsequent administration of antipenstaltic antidiarrheals is not recommended since they may delay the removal of toxins from the colon, thereby prolonging and/or worsening the diarrhea.
Chloramphenicol, Erythromycins, Sulfonamides, Tetracyclines may interfere with the bactericidal effect of penicillins in the treatment of meningitis or other situations where a rapid bactericidal effect is necessary, it is best to avoid concurrent therapy. Concurrent use with oral Contraceptives may decrease the effectiveness of oral contraceptives, resulting in menstrual irregularities, intermenstrual bleeding and unplanned pregnancies; patients should be advised to use an alternate method of contraception while taking penicillins. Probenecid may decrease renal tabular secretion of penicillins when used concurrently. Resulting in increased and more prolonged penicillin serum concentrations, prolonged half -life, and/or toxicity.
a) Penicillin G: The usual intramuscular dose is 600 to 3.000mg Mega units 4 to 6 times daily. It may also be given by intravenous, intrathecal, subconjunctival and by intraocular injection. In subacute endocarditis and fulminating infections as much as 12,0g daily may be given by continuous intravenous infusion.
b) Procaine Penicillin: In the treatment of gonorrhoea 4.8g is given as a single dose with probenecid, usually lg, taken at the same time. Patients with early syphilis are given procaine penicillin 600mg or occasionally 1.200mg daily for 8 to 10 days or for longer in late syphilis. Children with congenital syphilis have been given 10 to 50mg per kg body weight daily for 10 days.
c) Benzathine Penicillin: Benzathine penicillin is given by deep intramuscular injection in a usual dose of 900 mg for the treatment of streptococcal infections and for the prophylaxis of secondary infections before tonsillectomy or dental extractions. Children may be given intramuscular doses of 300 mg according to body weight. To prevent recurrences of acute rheumatic fever 900 mg may be given intramuscularly every 4 weeks; doses of 450 mg have been recommended for children.
In group A streptococcal upper respiratory tract infections, the equivalent of 900 mg as a single dose is given intramuscularly.
Note: Syphilis (primary, secondary, and latent) intramuscular 1.800mg as a single dose. Syphilis (tertiary and neurosyphilis) intramuscular 1.800mg once a week for two to three weeks.
d) Combinations of Penicillins: All combinations contain Benzylpenicillin to establish an initial Penicillin serum level. This one will be maintained by releasing Benzyl-penicillin from the injected depot of the Benzathine Penicillin or Procaine Penicililin. The usual dosages for i.m. injection shall be derived from the dosage statements under b and c, considering the needs of the patient.
a) Penicillin G: Prepare solution immediately before use. Intramuscular doses up to 300mg may be dissolved in 1 ml, larger doses in 2 ml of Water for injection. For intravenous injections prepare a final solution of approximately 0,3 to 6 mg per ml in 0,9% Sodium Chloride intravenous infusion. Doses of 6,0g or more should be given intravenously. Dilution in Dextrose intravenous infusion is to be preferred in these cases, considering that each 600 mg Benzylpenicillin contains 1.7 mEq of Sodium.
b) Procaine Penicilllin and Benzathine Penicillin: Prepare suspensions immediately before use. Suspend the contents of the sealed containers to maintain a strength of 300mg per ml for intramuscular injection.
c) Fortified Procaine Penicillin: Prepare suspension immediately before use. Suspend the content of the sealed container to maintain a strength of 400.000 units per ml for intramuscular injection (approx. 0,8 ml Water for injection are required to obtain 1 ml suspension from 0,4 Mega units of powder for injection).
d) Bipenicillin/Tripenicillin: Prepare suspensions immediately before use. Suspend the contents of the sealed containers to maintain a strength of 0,5 Mega units per ml for intramuscular injection.
Powders for Injection: Store in a cool (below 25°C) and dry place. Ready-to-use preparations maintain their activities up to 14 days if stored between 2-8°C. However, storage of injectable preparations should be avoided whenever possible as decomposition products may develop.
Procaine Penicillin in aqueous or oily Suspension: Store below 20°C protected from light. Shake well before using.
Clinical cartons with 10, 50 or 100 vials.
Injectcare Parenteral Pvt. Ltd.,
Plot 130, Silvassa Road, GIDC, VAPI – 396 195. Dist.: Valsad, India.
Shepherd Health & Veterinary Ltd
24, MONTGOMERY ROAD, YABA, LAGOS.