Clinical pharmacology of ticarcillin (alpha-carboxyl-3-thienylmethyl penicillin, BRL-2288).

Abstract

Clinical pharmacological studies of ticarcillin (alpha-carboxyl-3-thienylmethyl penicillin, BRL-2288) were conducted in patients with metastatic cancer and leukemia. After administration of 0.5 g intramuscularly, 1 g intramuscularly, and 1 g intravenously, the mean peak concentrations in serum were 18, 35, and 106 mug/ml, respectively. Greater than 80% of ticarcillin was excreted in the urine during the subsequent 6-h period. The mean concentrations in the serum of patients 15 min after they received an intravenous injection of 4 g of ticarcillin with and without probenecid were 508 and 519 mug/ml, respectively. Serum levels were determined in patients who received ticarcillin for therapy of infection in doses of 5 g every 6 h. The mean drug concentration in serum 15 min after the rapid administration of the first dose was 433 mug/ml. Subsequent doses were given during a 2-h infusion and the study was repeated 2 days later. The average initial serum level (4 h after the completion of the preceding dose) was 19 mug/ml, and the mean serum level at 15 min was 213 mug/ml. Drug concentrations in the serum of patients receiving ticarcillin by infusion in doses of 3.5 g every 4 h were also determined. In patients with normal renal function, the average initial serum level (2 h after completion of the preceding dose) was 49 mug/ml and the mean level at 15 min was 210 mug/ml. Drug concentrations in the serum of patients with impaired renal function were considerably higher. No detectable levels of ticarcillin were found in the cerebrospinal fluid.

• Authors: V Rodriguez, J Inagaki, G P Bodey
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 4 Issue 1 Pg. 31-6 (Jul 1973) ISSN: 0066-4804 [Print] United States
• PMID: 4791480 (Publication Type: Journal Article)

Chemical References

• Carboxylic Acids
• Penicillins
• Thiophenes

Topics

• Adolescent
• Adult
• Aged
• Carboxylic Acids (blood, metabolism, urine)
• Humans
• Injections, Intramuscular
• Injections, Intravenous
• Kidney Diseases (metabolism)
• Leukemia (metabolism)
• Middle Aged
• Neoplasms (metabolism)
• Penicillins (administration & dosage, blood, metabolism, urine)
• Thiophenes (blood, metabolism, urine)
• Time Factors