procaine penicillin (Wycillin)
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Introduction
Tradename: Wycillin. 1st generation penicillin.
Indications
- moderately severe infections due to Neisseria gonorrhoeae
- syphilis
Dosage
- adults
- 0.6-4.8 x 10E6 U/day IM divided QD-BID
- uncomplicated gonorrhea:
- probenecid 1 g PO
- 4.8 x 10E6 U procaine PCN divided in 2 separate IM injection sites 30 minutes later
- Streptococcus viridans endocarditis
- 1.2 x 10E6 U IM every 6 hours for 2-4 weeks
- used in conjunction with an aminoglycoside
- children:
- 25-50,000 U/kg/day IM divided QD-BID
- gonorrhea:
- probenecid 25 mg/kg up to 1 g PO
- 100,000 U/kg divided in 2 separate IM injection sites 30 minutes later
Injection: 600,000 units (1 mL, 2 mL, 4 mL).
Pharmacokinetics
- time to peak serum concentration: 1-4 hours
- 60-90% is excreted unchanged in the urine by tubular secretion
- 30% of the drug is metabolized & inactivated in the liver
- elimination delayed in neonates, young infants & patients with renal insufficiency
- moderately dialyzable: 20-50%
elimination via kidney
Adverse effects
- common (> 10%)
- pain at injection site
- uncommon (< 1%)
- CNS stimulation, seizures, myocardial depression, vasodilation, cardiac conduction disturbances, confusion, drowsiness, hemolytic anemia, positive direct antiglobulin (Coomb's) test (DAT), sterile abscess at site of injection, myoclonus, interstitial nephritis, pseudoanaphylactic reactions, Jarisch-Herxheimer reaction, hypersensitivity reactions