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penicillin G
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
- aspiration pneumonia
- pulmonary abscess
- CNS infection
- gastrointestinal infection
- urogenital infection
- gonorrhea
- syphilis
- eye infection
- ophthalmia neonatorum
- 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:
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:
1) distribution
a) poor penetration across blood-brain barrier despite inflamed meninges
b) crosses placenta
c) appears in breast milk
2) protein-binding 65%
3) metabolized in liver (30%) to penicilloic acid
4) time to peak serum concentration: within 1 hour
5) elimination 1/2life is 20-50 minutes (6-20 hours ESRD)
6) eliminated in the urine
Antimicrobial activity:
- Streptococcus species
- Listeria
- Neisseria meningitidis
- Neisseria gonorrhoeae
- Actinomyces
- Clostridium
- Clostridium perfringens [4]
- not Clostridium difficile
- 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
Interactions
drug interactions
Specific
benzathine penicillin (Bicillin L-A)
procaine penicillin (Wycillin)
General
1st generation penicillin (natural)
Properties
MISC-INFO: elimination route KIDNEY
pregnancy-category B
safety in lactation ?
lifetime 20-50 MINUTES
Database Correlations
PUBCHEM correlations
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
- Deprecated Reference
Component-of
penicillin g/procaine