外觀描述：

白色乾粉、透明玻璃小瓶。

醫令代碼：

30545P

商品名：

EXTENCILLINE 2.4MIU/5ML(專案進口)

學名：

Benzathine benzylpenicillin

劑型：

VIAL

健保碼：

X000346219

仿單下載：

用藥指導單張：

ATC7藥理類別：

結構式 ：

UpToDate：

藥理作用 ：

The mechanism of action of benzathine benzylpenicillin is based on inhibition of bacterial cell wall synthesis (during the growth phase) by binding to penicillin-binding proteins (PBPs), such as inhibition of transpeptidases. This results in a bactericidal action.

適應症：

對青黴素具有感受性菌所引起之感染症。

用法用量：

Dose and duration of treatment

Standard treatment:

Adults and adolescents: 1.2 MIU once a week.

Children > 30 kg of body weight: 1.2 MIU once a week.

Children < 30 kg of body weight: 600,000 MIU once a week. Duration of treatment: single dose.

Treatment of syphilis：

Primary and secondary stage

Adults and adolescents: 1 x 2.4 MIU.

Children: 50,000 IU/kg of body weight, without however exceeding 2.4 MIU.

(The treatment should be repeated if clinical symptoms reappear or if the laboratory results remain

strongly positive).

Duration of treatment: single dose.

Late-stage syphilis (latent seropositive syphilis)

Adults and adolescents: 2.4 MIU once a week.

Children: 50,000 IU/kg of body weight without however exceeding 2.4 MIU.

Duration of treatment: 3 weeks.

Treatment of congenital syphilis: without neurological involvement
Neonates and infants: 1 x 50,000 IU/kg of body weight. Duration of treatment: single dose.

Treatment of yaws and pinta:
Adults and adolescents: 1 x 1.2 MIU.
Children > 30 kg of body weight: 1 x 1.2 MIU.

Children < 30 kg of body weight: 1 x 600,000 IU.
Duration of treatment: single dose.

 

Prophylactic treatment of acute articular rheumatism, post-streptococcal glomerulonephritis and erysipelas:
Adults and adolescents: 1 x 1.2 MIU every 3 to 4 weeks. Children > 30 kg of body weight: 1 x 1.2 MIU every 3 to 4 weeks.
Children < 30 kg of body weight: 1 x 600,000 IU every 3 to 4 weeks. Duration of treatment:
a) without cardiac involvement: at least 5 years or until the age of 21 (whichever is longer),

b) transient cardiac involvement: at least 10 years or until the age of 21 (whichever is longer),
c) persistent cardiac involvement: at least 10 years or until the age of 40 (whichever is longer); lifelong prophylactic treatment is sometimes necessary.

副作用：

注射部位疼痛、噁心、過敏、腹瀉。

藥物動力學：

Distribution
Following injection by the deep IM route, benzathine benzylpenicillin is absorbed very slowly releasing benzylpenicillin.
The serum peak is obtained 12 to 24 h after injection. The long plasma half-life ensures stable, prolonged penicillinaemia.
On day 14 after IM injection of 2,400,000 IU, the serum level is 0.12 µg/ml. On day 21 after injection of 1,200,000 IU, 89.0 to 97.4% of subjects have a penicillinaemia of 0.06 µg/ml (it should be remembered that 1 IU = 0.6 µg).
Humoral diffusion is good, but tissue diffusion is poor. Plasma protein binding is 40 to 60%.
Biotransformation
Biotransformation is low.
Elimination
It is mainly excreted in the urine.

交互作用：

Concomitant administration of benzathine benzylpenicillin is inadvisable with:
Based on the general principle of refraining from combining bactericidal and bacteriostatic antibiotics, EXTENCILLINE must not be combined with bacteriostatic antibiotics.
Caution is required when co-administering the following medicinal products:
Probenecid: administration of probenecid inhibits the tubular secretion of benzylpenicillin, resulting in an increase in serum concentration and a prolongation of the elimination half-life. Probenecid also inhibits the transport of penicillin from cerebrospinal fluid, and consequently concomitant administration of probenecid further reduces the penetration of benzylpenicillin into brain tissue.
Methotrexate:
excretion of methotrexate is reduced when administered with benzathine benzylpenicillin. This may result in an increase in the toxic effects of methotrexate. Combination with methotrexate is not recommended.
Anticoagulants:
concomitant use with oral anticoagulants may increase the effect of anti-vitamin K agents and the risk of bleeding. It is recommended that the International Normalized Ratio (INR) be monitored regularly, and that the dosage of anti-vitamin K drugs be adjusted accordingly, during and after treatment with EXTENCILLINE.

禁忌：

先前曾對任何penicillin類藥物產生過敏反應者。

警語：

Hypersensitivity to the active substance benzathine benzylpenicillin, to other penicillins, to soyabean phospholipids, to arachides (peanuts) or to any of the excipients.

過量處理：

beta-lactam antibiotics expose the patient to a risk of encephalopathy (confusion, impaired consciousness, epilepsy or abnormal movements) and particularly in case of overdosage or kidney failure. At extremely high doses, penicillins may cause neuromuscular excitability or epileptic seizures. If overdose is suspected, clinical monitoring and symptomatic measures are indicated. Benzylpenicillin can be removed by haemodialysis.

藥品保存方式：

室溫儲存。