Procaine benzylpenicillin


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intramuscular
Bejel, Pinta, Syphilis, Yaws
Adult: For early stage: 600 mg once daily via deep injection for 10 days. For late stage: 600 mg once daily via deep injection for 17 days.

Intramuscular
Neurosyphilis
Adult: In combination with probenecid: 1.8-2.4 g once daily via deep injection for 17 days.

Intramuscular
Congenital syphilis
Child: For early stage and patient with abnormal CSF: ≤2 years 50 mg/kg once daily via deep injection for 10 days.

Intramuscular
Fusospirochetosis (Vincent's infection) of the oropharynx, Invasive Group A beta-hemolytic streptococcal disease, Pneumococcal pneumonia, Staphylococcal infections
Adult: For moderately severe to severe cases: 1.5 g daily via deep injection for 2-5 days. The 4th and 5th doses are dependent on the severity of infection.

Intramuscular
Pneumococcal pneumonia
Child: 50 mg/kg once daily via deep injection for 10 days.

Intramuscular
Uncomplicated gonorrhoea
Adult: 1 g once daily via deep injection for 7-14 days. Alternatively, up to 4.8 g as a single dose in combination with probenecid.

Intramuscular
Diphtheria
Adult: As adjunctive therapy with antitoxin: 300-600 mg once daily via deep injection. Carrier state: 300 mg once daily for 10 days.
Child: Carrier state: 300 mg once daily via deep injection for 10 days.

Intramuscular
Treatment and postexposure prophylaxis of inhalation anthrax
Adult: 1.2 g via deep injection every 12 hours for 60 days.
Child: 25 mg/kg every 12 hours for 60 days via deep injection. Max: 1.2 g/dose.

Intramuscular
Cutaneous anthrax
Adult: 0.6-1 g once daily via deep injection.
Chống chỉ định
Hypersensitivity to penicillin.
Thận trọng
Patient with hypersensitivity to cephalosporins, procaine (known or suspected) or to other allergens, asthma, Brugada syndrome, cardiac conduction abnormalities. Renal impairment. Children. Pregnancy and lactation. Not intended for injection into or near a blood vessel or nerve or for intravascular administration.
Phản ứng phụ
Significant: Increased risk of neutropenia and of serum sickness-like reactions (prolonged treatment), superinfection. Rarely, procaine-related reactions manifested as transient mental disturbances (e.g. weakness, anxiety, agitation, combativeness, confusion, depression, hallucinations, seizures, sensation of impending death); quadriceps femoris fibrosis and atrophy (after repeated intramuscular administration into the anterolateral thigh).
Gastrointestinal disorders: Nausea, vomiting, diarrhoea.
Immune system disorders: Jarisch-Herxheimer reaction (for syphilis).
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Rashes.
Potentially Fatal: Rarely, anaphylactic reactions (e.g. maculopapular eruptions, exfoliative dermatitis, urticaria, laryngeal oedema, serum sickness-like reactions), pseudomembranous colitis.
IM/Parenteral: B
MonitoringParameters
Perform susceptibility tests especially for staphylococcal infections prior to treatment. Periodically monitor CBC and renal function if prolonged treatment. Perform monthly serological test for at least 4 months and dark-field examination if syphilis is suspected.
Tương tác
Decreased effect with tetracycline.
Lab Interference
False-positive urinary glucose test using cupric sulfate.
Tác dụng
Description: Procaine benzylpenicillin is an equimolecular compound of procaine and benzylpenicillin. After IM administration, it is gradually hydrolysed into benzylpenicillin; thus, prolonging its action. Benzylpenicillin is a long-acting penicillin antibacterial which is active against a variety of susceptible gram-positive and gram-negative organisms. It binds to penicillin-binding proteins (PBPs) which inhibits transpeptidation step of peptidoglycan synthesis in bacterial cell wall thus arresting assembly.
Synonym: benzylpenicillin novocaine, penicillin G procaine, procaine penicillin, procaine penicillin G.
Duration: 15-24 hours.
Pharmacokinetics:
Absorption: Slowly absorbed after IM administration. Highly distributed in kidneys, lesser amount in liver, skin and intestines. Time to peak plasma concentration: 1-4 hours.
Distribution: Enters breastmilk. Plasma protein binding: Approx 60%.
Excretion: Mainly via urine (60-90%, as unchanged drug).
Đặc tính

Chemical Structure Image
Procaine benzylpenicillin

Source: National Center for Biotechnology Information. PubChem Database. Procaine penicillin G, CID=5903, https://pubchem.ncbi.nlm.nih.gov/compound/Procaine-penicillin-G (accessed on Jan. 23, 2020)

Bảo quản
Store between 2-8°C. Do not freeze.
Phân loại MIMS
Phân loại ATC
J01CE09 - procaine benzylpenicillin ; Belongs to the class of beta-lactamase sensitive penicillins. Used in the systemic treatment of infections.
References
Anon. Penicillin G Procaine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 06/06/2018.

Anon. Penicillin G Procaine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/06/2018.

Buckingham R (ed). Procaine Benzylpenicillin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/06/2018.

Buckingham R (ed). Syphilis (Antibacterials-Sexually Transmitted Diseases). Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/06/2018.

Penicillin G Procaine Injection, Suspension (Pfizer Laboratories Div Pfizer Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 06/06/2018.

Pharmacy Retailing (NZ) Limited. Cilicaine Syringe data sheet 1 June 2017. Medsafe. http://www.medsafe.govt.nz/. Accessed 06/06/2018.

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