penicillin G
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Introduction
penicillin G. 1st generation penicillin.
Indications
- bacterial infections due to susceptible organisms[4]
- congenital syphlis, tertiary syphilis, neurosyphilis
- tertiary yaws, pinta, bejel, tertiary bejel
- rheumatic fever
- bolulism
- anthrax, cutaneous anthrax, inhalation anthrax
- rat bite fever
- erysipeloid
- pasteurellosis
- diphtheria
- scarlet fever
- meningococcemia
- actinomyocosis
- Lyme disease
- omphalitis
- pulmonary infection
- CNS infection
- gastrointestinal infection
- urogenital infection
- eye infection
- infections associated with necrosis[4]
Dosage
Pneumonia: 1-1.5 x 10E5 U/kg/day
- (8-12 x 10E6 U {adults})
- IV divided every 4-6 hours.
Meningitis: 2.5-3.0 x 10E5 U/kg/day
- (20-30 x 10E6 U {adults})
- IV divided every 4 hours.
- do NOT give intrathecally (neurotoxic)
Powder for injection: 1 x 10E6 U, 5 x 10E6 U, 20 x 10E6 U
Dosage adjustment in renal failure
Table
creatinine clearance | dosage* |
---|---|
> 30 mL/min | 1-2 x 10E6 units IV every 4 hours |
10-30 mL/min# | 1-2 x 10E6 units IV every 6 hours |
< 10 mL/min | 1-2 x 10E6 units IV every 12 hours |
post-dialysis | 2 x 10E6 units |
* higher doses (3-4 x 10E6 units) should be considered for streptococcal endocarditis or pneumococcal meningitis
# same dose for continuous arteriovenous hemofiltration
Pharmacokinetics
- distribution
- poor penetration across blood-brain barrier despite inflamed meninges
- crosses placenta
- appears in breast milk
- protein-binding 65%
- metabolized in liver (30%) to penicilloic acid
- time to peak serum concentration: within 1 hour
- elimination 1/2life is 20-50 minutes (6-20 hours ESRD)
- eliminated in the urine
elimination via kidney
lifetime = 20-50 minutes
Antimicrobial activity
- Streptococcus species
- Listeria
- Neisseria meningitidis
- Neisseria gonorrhoeae
- Actinomyces
- Clostridium
- Treponema pallidum
- Pasteurella multocida
Adverse effects
- uncommon (< 1%)
- thrombophlebitis, convulsions, confusion, drowsiness, fever, rash, electrolyte imbalance, hemolytic anemia, positive direct antiglobulin (Coomb's) test (DAT), myoclonus, acute interstitial nephritis, Jarisch-Herxheimer reaction, hypersensitivity reactions, anaphylaxis 1:10,000
More general terms
More specific terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Harrison's Principles of Internal Medicine, 13th ed. Companion Handbook. Isselbacher et al (eds), McGraw-Hill Inc. NY, 1995, pg 161
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 4.0 4.1 4.2 4.3 Deprecated Reference