Benzathine Penicillin
Indications
Benzathine Penicillin is indicated in-
- The treatment of penicillin-sensitive infections where initial high blood levels are not required.
- The prophylaxis of penicillin-sensitive secondary infections especially in children. It is particularly valuable in continuous prophylaxis against rheumatic fever and streptococcal infections.
- Prophylaxis of streptococcal impetigo
- Treatment of acute otitis media
- Treatment of syphilis
- Treatment of diphtheria carriers
Pharmacology
Inhibits bacterial cell wall synthesis by
binding to one or more of the penicillin-binding proteins (PBPs); which
in turn inhibits the final transpeptidation step of peptidoglycan
synthesis in bacterial cell walls, thus inhibiting cell wall
biosynthesis. Bacteria eventually lyse due to ongoing activity of cell
wall autolytic enzymes (autolysins and murein hydrolases) while cell
wall assembly is arrested.
Dosage & Administration
Treatment of infection: 0.3 to 1.2 million units repeated every five to seven days.
Prophylaxis of rheumatic fever: 1.2 million units every three weeks.
Specific dosage schedule: Treatment of group-A β-haemolytic streptococcal infections: A single intramuscular dose of 600,000 units.
Prevention of rheumatic fever: Monthly injection of a single dose of 1.2 million units is the most effective regimen for preventing further attacks of rheumatic fever.
Treatment of acute otitis media: A single injection of 6 million units.
Prophylaxis of rheumatic fever: 1.2 million units every three weeks.
Specific dosage schedule: Treatment of group-A β-haemolytic streptococcal infections: A single intramuscular dose of 600,000 units.
Prevention of rheumatic fever: Monthly injection of a single dose of 1.2 million units is the most effective regimen for preventing further attacks of rheumatic fever.
Treatment of acute otitis media: A single injection of 6 million units.
- Early syphilis- 2.4 million units as a single dose.
- Late syphilis: 2.4 million units weekly for three successive weeks.
- Neurosyphilis: Benzylpenicillin, intravenously, 2 to 4 million units every 4 hours for 10 days, followed by benzathine penicillin intramuscularly, 2.4 million units weekly for three successive weeks.
- Congenital syphilis: Asymptomatic infants with normal cerebrospinal fluid, intramuscularly 50,000 units per kg in a single dose.
Interaction
No potentially hazardous interactions have been described.
Contraindications
Hypersensitivity to penicillins
Side Effects
The toxicity of penicillins is generally
low, but in a small number of patients penicillin can cause
sensitization and allergic reactions. Acute, lifethreatening
anaphylactic reactions are rare, but they do occur.
Intramuscular injection of benzathine penicillin can cause moderate burning discomfort, local pain, and deep muscle soreness and tenderness at the site of injection, lasting for one to three days in about 10% of patients. Some patients had low-grade fever (102˚F) associated with local pain and tenderness. This febrile reaction disappeared within 24 to 48 hours.
Intramuscular injection of benzathine penicillin can cause moderate burning discomfort, local pain, and deep muscle soreness and tenderness at the site of injection, lasting for one to three days in about 10% of patients. Some patients had low-grade fever (102˚F) associated with local pain and tenderness. This febrile reaction disappeared within 24 to 48 hours.
Pregnancy & Lactation
Pregnancy category B. Benzathine Penicillin
should not be administered during pregnancy unless in the judgment of
the physician such administration is clinically justifiable. Special
care should be taken in the first three months of pregnancy.
As penicillin appears in breast milk, it is probably best for a mother to stop breast-feeding while being given penicillin to avoid exposing the infant to the drug unnecessarily.
As penicillin appears in breast milk, it is probably best for a mother to stop breast-feeding while being given penicillin to avoid exposing the infant to the drug unnecessarily.
Precautions & Warnings
Patient with previous hypersensitivity
reactions to cephalosporins, history of allergy, asthma, seizure
disorder. Not intended for IV or intra-arterial admin or inj near major
peripheral nerves of blood vessels. Prolonged use may result in
bacterial or fungal superinfection. Renal impairment.
Therapeutic Class
Long acting penicillin
Storage Conditions
Store between 2-8°C. Do not freeze.
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