Ticarcillin disodium Clavulanate potassium (15:1) (Timentin)

Ticarcillin disodium Clavulanate potassium (15:1) (Timentin)

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Category Antibiotics
Catalog number BBF-04323
CAS 116876-37-0
Molecular Formula 15(C15H14Na2N2O6S2).C8H8KNO5
Purity ≥99.0%

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Description

A broad-spectrum beta-lactam antibiotic in the carboxypenicillin family.

Specification

Related CAS 86482-18-0 (free acid)
Synonyms Ticarcillin disodium with Clavulanate potassium (15:1) (Timentin)
Storage Store at 2-8°C
IUPAC Name potassium;disodium;(2S,5R,6R)-6-[[(2R)-2-carboxylato-2-thiophen-3-ylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;(2R,5R)-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo[3.2.0]heptane-2-carboxylate
Source Mixture

Properties

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Reference Reading

1. Clinical pharmacology of timentin (ticarcillin and clavulanic acid)
E Yeo, B LeBlanc, K Rolston, D H Ho, G P Bodey Clin Pharmacol Ther . 1985 Aug;38(2):134-9. doi: 10.1038/clpt.1985.149.
Ticarcillin (4 gm) and clavulanic acid (0.1 gm) were simultaneously administered as timentin to patients with cancer as therapy for infections. The pharmacokinetics of both ticarcillin and clavulanic acid were studied in 15 patients after 30-minute and 2-hour intravenous infusions. The mean (+/- SD) ticarcillin plasma peak concentrations after the two infusions were 341 +/- 76 and 210 +/- 60 micrograms/ml. The plasma terminal t1/2 values of ticarcillin were 80 +/- 32 and 56 +/- 12 minutes. The AUCs were 631 +/- 189 and 601 +/- 230 mg/L X hr. The volumes of distribution of the area were 15 +/- 5 and 21 +/- 7 L and total clearances were 115 +/- 36 and 127 +/- 54 ml/min. The corresponding values for clavulanic acid after the infusions are as follows: mean peak concentrations, 5 +/- 1 and 4 +/- 1 micrograms/ml; plasma terminal t1/2 values, 84 +/- 24 and 74 +/- 36 minutes; AUCs, 11 +/- 3 and 11 +/- 6 mg/L X hr; volumes of distribution of the area, 22 +/- 3 and 32 +/- 6 L; and total clearances, 170 +/- 58 and 175 +/- 68 ml/min.
2. The pharmacokinetics of ticarcillin, clavulanic acid and their combination
G Höffken, P Koeppe, H Lode, H Tetzel J Antimicrob Chemother . 1986 May;17 Suppl C:47-55. doi: 10.1093/jac/17.suppl_c.47.
The pharmacokinetics of ticarcillin and clavulanic acid were examined both alone and combined (3.0 and 5.0 g ticarcillin + 0.2 g clavulanic acid as 3.2 or 5.2 g Timentin) after a 15-min infusion in ten healthy volunteers. The serum kinetics of both ticarcillin and clavulanic acid were described by an open two-compartment model. After the end of the infusion, the serum concentrations of ticarcillin (clavulanic acid) ranged between 576.2 +/- 98.7 mg/l (26.1 +/- 2.6 mg/l) after separate and 621.8 +/- 62.6 mg/l (22.9 +/- 4.6 mg/l) after combined administration. Both substances showed similar kinetic behaviour in serum with a T1/2 beta of 74.8 +/- 11.5 min for ticarcillin and 76.6 +/- 4.6 min for clavulanic acid. The total clearance of clavulanic acid was 158 +/- 23 ml/min and thus clearly exceeded that of ticarcillin (112 +/- 9 ml/min). The recovery rate in the 24 h urine was 41.3% for clavulanic acid as compared to 79.4% for ticarcillin. Concomitant administration of both substances had little effect on the kinetics of either agent alone. With increasing doses of ticarcillin, a decrease of the non-renal clearance of clavulanic acid was observed. The ratio of the two compounds in serum varied from 25:1 (for 5.2 g Timentin, 15:1 for 3.2 g Timentin) at the time of administration to 59:1 (34:1, respectively) 4 h after infusion.
3. Ertapenem or ticarcillin/clavulanate for the treatment of intra-abdominal infections or acute pelvic infections in pediatric patients
Jeffrey Johnson, Iliana Higareda, Albert E Yellin, Joseph West, Richard Gesser, Antonio C Arrieta, Blaise L Congeni, Doreen Fernsler Am J Surg . 2007 Sep;194(3):367-74. doi: 10.1016/j.amjsurg.2007.01.023.
Background:Ertapenem, a group I carbapenem antibiotic, has been shown to be safe and effective in treating adults with complicated intra-abdominal (cIAI) or acute pelvic infection (API). This study evaluated ertapenem for treating these infections in children.Methods:In an open-label study, children aged 2 to 17 years with cIAI or API were randomized 3:1 to receive ertapenem or ticarcillin/clavulanate. Children 13 to 17 years of age received 1 g parenterally daily, and those 2 to 12 years of age received 15 mg/kg twice daily. Patients < 60 kg received ticarcillin/clavulanate 50 mg/kg 4 to 6 times daily and 3.1 g 4 to 6 times daily for those > or = 60 kg. Patients were assessed for safety and tolerability throughout the study and for efficacy after the completion of therapy.Results:One hundred five patients, 72 (69%) with cIAI, received > or = 1 dose of study drug and were included in the safety analysis. Eighty-one patients were treated with ertapenem. Infusion site pain was the most common drug-related adverse event in both groups. In the modified intent-to-treat analysis, the age-adjusted posttreatment clinical response rates were 87% (43/50 patients) and 100% (25/25 patients) in the cIAI and API patients, respectively, for ertapenem and 73% (11/15 evaluable patients) and 100% (8/8 evaluable patients), respectively, for ticarcillin/clavulanate. Overall age-adjusted response rates were 91% (68/75 evaluable patients) for ertapenem and 83% (19/23 evaluable patients) for the comparator.Conclusions:This study suggests that ertapenem is generally safe and efficacious for treating cIAI or API in pediatric patients.

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