Acute glomerulonephritis, Respiratory tract infections, Rheumatic fever and chorea, Rheumatic heart disease, Syphilis and other venereal diseases
#仿單變更2021
藥理
Interferes with bacterial cell wall synthesis during active multiplication, causing cell wall death and resultant bactericidal activity against susceptible bacteria
藥動學
Absorption:
1. IM: Slow
2. Duration: 1 to 4 weeks (dose dependent); larger doses result in more sustained levels
3. Time to peak, serum: Within 12 to 24 hours; serum levels are usually detectable for 1 to 4 weeks depending on the dose; larger doses result in more sustained levels rather than higher levels Distribution:
1. Minimal concentrations attained in CSF with inflamed or uninflamed meninges; highest levels in the kidney; lesser amounts in liver, skin, intestines
2. Protein Binding: ~60% Excretion:
Excreted by renal tubular excretion; penicillin G is detected in urine for up to 12 weeks after a single IM injection; renal clearance is delayed in neonates, young infants, and patients with impaired renal function
禁忌症
Hypersensitivity to penicillin(s) or any component of the formulation
懷孕分類
Adverse events have not been observed in animal reproduction studies. Penicillin G benzathine crosses the placenta . Maternal use of penicillins has generally not resulted in an increased risk of adverse fetal effects. Penicillin G is the drug of choice for treatment of syphilis during pregnancy.
哺乳分類
Soluble penicillin G is excreted in breast milk. The manufacturer recommends that caution be exercised when administering penicillin to nursing women. Nondose-related effects could include modification of bowel flora and allergic sensitization.
副作用
Common:
Dermatologic: Rash, Urticaria
Gastrointestinal: Nausea, Vomiting
Hematologic: Eosinophil count raised
Immunologic: Jarisch Herxheimer reaction, when used for syphilis
Other: Fatigue, Fever Serious:
Gastrointestinal: Clostridium difficile colitis
Immunologic: Anaphylaxis, severe skin adverse reaction (Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), drug reaction with eosinophilia and systemic symptoms (DRESS) , acute generalized exanthematous pustulosis(AGEP)). <20230531>
Neurologic: Agitation, Fear of death, Hallucinations, Seizure
Renal: Renal failure
Respiratory: Edema of larynx Postmarketing:
Severe cutaneous adverse reactions (SCAR) such as SJS, TEN, DRESS, AGEP; Nicolau syndrome <20210319>
劑量和給藥方法
Usual dosage:
IM 1.2 to 2.4 million units as a single dose; IM injection only, avoid IV injection <20210319> Streptococcus (group A):
1. Pharyngitis, acute treatment: (IM) 1.2 million units as a single dose
2. Secondary prophylaxis for rheumatic fever (prevention of recurrent attacks): (IM) 1.2 million units once every 21 to 28 days. Duration depends on risk factors and presence of valvular heart disease.
3. Secondary prophylaxis of glomerulonephritis: (IM) 1.2 million units every 4 weeks or 600,000 units twice monthly Syphilis:
1. Primary, Secondary, Early Latent (<1 year duration): (IM) 2.4 million units as a single dose
2. Late Latent, Latent with unknown duration, or Tertiary Syphilis (with normal CSF examination): (IM) 2.4 million units once weekly for 3 doses
3. Neurosyphilis (including Ocular Syphilis): Not indicated for initial treatment; aqueous penicillin G IV is preferred initial therapy (refer to Penicillin G Parenteral/Aqueous monograph for dosing). Following penicillin G IV initial treatment, may consider administration of penicillin G benzathine 2.4 million units IM once weekly for 3 weeks to provide a comparable total duration of therapy as for latent syphilis.
小兒調整劑量
腎功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling; use with caution
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling