Prokain Penicillin 3:1 800 000 Iu Injection Powder Iceren Vial

Prokain Penicillin 3:1 800,000 IU is a fixed-dose combination antibiotic formulation containing two forms of penicillin G in a 3:1 ratio. This injectable medication represents an important tool in the antimicrobial arsenal, particularly for infections requiring sustained antibiotic release. The formulation combines the immediate action of potassium penicillin G with the prolonged effect of procaine penicillin G, providing both rapid onset and extended duration of activity against susceptible microorganisms.

Composition and Classification

Prokain Penicillin 3:1 800,000 IU injection powder contains two active ingredients in specific proportions:

• 600,000 IU of Penicillin G Procaine (Benzylpenicillin Procaine)

• 200,000 IU of Penicillin G Potassium (Benzylpenicillin Potassium)

This medication belongs to the beta-lactam antibiotic class, specifically categorized as a natural penicillin. The “3:1” in the product name refers to the ratio of procaine penicillin G to potassium penicillin G. When reconstituted, it forms an injectable suspension designed for intramuscular administration only.

Mechanism of Action

The antimicrobial activity of Prokain Penicillin 3:1 stems from its ability to disrupt bacterial cell wall synthesis. Following administration, procaine penicillin G is slowly hydrolyzed to release active benzylpenicillin (penicillin G), which then attaches to penicillin-binding proteins on the bacterial cell wall. This interaction inhibits the transpeptidation enzyme responsible for cross-linking peptide chains in the peptidoglycan layer of the bacterial cell wall.

The final bactericidal event involves the inactivation of inhibitors of autolytic enzymes in the cell wall, leading to bacterial cell lysis. This mechanism makes the medication particularly effective against actively dividing bacteria. The procaine component serves a dual purpose: it extends the duration of action and reduces the pain associated with intramuscular injection.

Pharmacokinetic Properties

Absorption

After intramuscular injection, procaine penicillin G dissolves slowly at the site of injection, creating a depot effect. This results in a plateau-type blood level reaching its peak approximately 4 hours post-administration, followed by a gradual decline over the subsequent 15 to 20 hours. This sustained release profile allows for less frequent dosing compared to conventional penicillin formulations.

Distribution

Penicillin G is distributed throughout body tissues in varying concentrations. Highest levels are typically found in the kidneys, with lesser amounts in the liver, skin, and intestines. The medication penetrates the cerebrospinal fluid to a lesser degree, which may be relevant when treating central nervous system infections. Approximately 60% of penicillin G binds to serum proteins.

Metabolism and Elimination

The procaine component is metabolized in the body, while penicillin G is primarily eliminated unchanged through renal excretion. In patients with normal renal function, elimination occurs relatively quickly, but the sustained release nature of the formulation extends the duration of therapeutic levels.

Therapeutic Indications

Prokain Penicillin 3:1 is indicated for the treatment of moderate to severe infections caused by penicillin-sensitive microorganisms, including:

Respiratory Tract Infections

• Moderately severe pneumococcal pneumonia

• Upper respiratory tract infections caused by susceptible streptococci

Soft Tissue and Skin Infections

• Erysipelas

• Cellulitis

• Skin and soft tissue infections due to susceptible organisms

Specific Infections

• Diphtheria (as an adjunct to antitoxin)

• Neurosyphilis and other forms of syphilis (primary, secondary, and latent)

• Scarlet fever

• Streptococcal pharyngitis (strep throat)

• Vincent’s infection (fusospirochetosis)

Other Susceptible Infections

• Rat-bite fever (Streptobacillus moniliformis and Spirillum minus)

• Anthrax (cutaneous and post-exposure prophylaxis for inhalational anthrax)

• Erysipeloid

• Whipple’s disease (as part of combination therapy)

Administration and Dosage

Prokain Penicillin 3:1 must be administered exclusively via deep intramuscular injection. It should never be given intravenously, intra-arterially, or near a nerve. The medication is supplied as a powder that must be reconstituted with the appropriate diluent (sterile water for injection) immediately before use.

Standard Dosage Regimens

• For bacterial infections in adults: 600,000-1,200,000 units once daily

• For diphtheria in adults: 300,000-600,000 units daily, administered alongside diphtheria antitoxin

• For neurosyphilis in adults: 2.4 million units daily, divided into four doses, for 10-14 days

• For congenital syphilis in children: 50,000 units/kg/day for 10-14 days via intramuscular injection

Dosage adjustments are necessary for patients with renal impairment:

• Creatinine clearance 10-50 mL/min: Reduce dose by 25%

• Creatinine clearance <10 mL/min: Reduce dose by 50-70%

Contraindications

Prokain Penicillin 3:1 is absolutely contraindicated in:

• Patients with known hypersensitivity to penicillins

• Patients with known allergy to procaine

• Individuals who have previously experienced anaphylactic reactions to any beta-lactam antibiotic

Warnings and Precautions

Administration Precautions

• Must be administered by deep intramuscular injection only

• Care must be taken to avoid injection into or near arteries, veins, or nerves

• Should not be mixed with other medications in the same syringe

Clinical Precautions

• Thorough allergy history should be obtained before administration

• Skin testing for penicillin and procaine sensitivity is recommended before first administration

• Patients with asthma, eczema, or urticaria should receive this medication with caution

• Use with caution in patients with renal insufficiency or history of gastrointestinal diseases, especially antibiotic-associated colitis

• Cross-sensitivity between penicillins exists; patients allergic to one penicillin may react to others

• Emergency equipment for treating anaphylaxis should always be readily available when administering this medication

Side Effects

Hypersensitivity Reactions

• Anaphylactic shock (potentially fatal, occurring within minutes of administration)

• Generalized sensitivity reactions (occurring within 1-3 weeks): urticaria, fever, eosinophilia, joint pain, angioneurotic edema, erythema multiforme, exfoliative dermatitis

• Accelerated urticarial reactions (developing within hours)

Procaine-Related Reactions

• Acute toxic reactions to procaine can occur, particularly with large single doses

• Symptoms include anxiety, confusion, agitation, depression, seizures, hallucinations, and fear of imminent death

• These reactions are typically transient

Gastrointestinal Effects

• Glossitis

• Angular and aphthous stomatitis

• Darkening of the tongue

• Nausea, vomiting, diarrhea

• Antibiotic-associated colitis

Other Effects

• Pain at injection site

• Superinfections (overgrowth of non-susceptible organisms)

• Jarisch-Herxheimer reaction (when treating syphilis)

Drug Interactions

• Probenecid: Reduces renal tubular secretion of penicillin, resulting in higher and more prolonged blood levels

• NSAIDs (aspirin, indomethacin, phenylbutazone): Can reduce penicillin excretion and prolong its half-life

• Sulfonamides: May interfere with penicillin’s bactericidal effects

• Methotrexate: Penicillins may decrease methotrexate clearance, increasing toxicity risk

• Oral contraceptives: Effectiveness may be reduced

• Bacteriostatic antibiotics (tetracyclines, chloramphenicol): May interfere with the bactericidal action of penicillins

Use in Special Populations

Pregnancy

No definitive evidence of harm has been established in animal reproductive studies. However, the safety of procaine benzylpenicillin in pregnant women has not been fully established. This medication should be used during pregnancy only when the potential benefits outweigh the possible risks to the fetus.

Lactation

Small amounts of procaine benzylpenicillin are excreted in human milk. Caution should be exercised when administering this medication to nursing women.

Pediatric Use

In neonates and young infants, renal function may not be fully developed, potentially leading to delayed penicillin elimination. Appropriate monitoring and dosage adjustments may be necessary.

Renal Impairment

Dose adjustments are required for patients with significant renal impairment to prevent drug accumulation and toxicity.

Storage and Handling

The dry powder should be stored in a cool, dry place, protected from light. Once reconstituted, the solution should be used immediately and not stored for later use. Any unused portion should be discarded according to proper medical waste protocols.

Key Information

Conclusion

Prokain Penicillin 3:1 800,000 IU represents a valuable therapeutic option for treating moderate to severe infections caused by penicillin-sensitive microorganisms. Its unique formulation combining immediate and sustained-release penicillin provides extended antimicrobial coverage with less frequent dosing. However, the potential for serious hypersensitivity reactions and procaine-related adverse effects necessitates careful patient selection and monitoring. Proper administration technique is crucial to minimize complications, and the medication should only be used when clearly indicated based on the pathogen’s susceptibility and the patient’s clinical condition.

Healthcare providers should remain vigilant for signs of allergic reactions, particularly in patients receiving penicillin therapy for the first time. With appropriate precautions and monitoring, Prokain Penicillin 3:1 continues to be an effective treatment option for numerous bacterial infections, including those requiring prolonged antibiotic therapy.