Ticarcillin
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Ticarcillin ??
- ?? ?
- 768.3±60.0 °C(Predicted)
- ??
- 1.62±0.1 g/cm3(Predicted)
- ?? ??
- 2-8°C
- ?? ?? (pKa)
- pKa 2.89±0.05(H2O t=25.0 I=0.15 (KCl)) (Uncertain);3.28±0.04 (Uncertain)
- CAS ??????
- 34787-01-4(CAS DataBase Reference)
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- ?? ? ?? ??
- ?? ? ???? ?? (GHS)
| ??? ?? | Xn | ||
|---|---|---|---|
| ?? ???? ?? | 42/43 | ||
| ????? | 22-36/37-45 | ||
| WGK ?? | 3 |
| ????(GHS): |
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| ?? ?: | Danger | |||||||||||||||||||||
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Ticarcillin C??? ??, ??, ??
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Temocillin disodium is a broad-spectrum, β-lactamase resistant, injectable penicillin. High serum levels and a five hour half-life allow once or twice-daily dosing.??
ChEBI: A penicillin compound having a 6beta-[(2R)-2-carboxy-2-thiophen-3-ylacetyl]amino side-group.Antimicrobial activity
Because it is hydrolyzed less rapidly than ampicillin, non-β- lactamase-producing strains of N. gonorrhoeae, ampicillin-susceptible H. influenzae and some Enterobacteriaceae are susceptible. Most aerobic and anaerobic Gram-positive bacteria are susceptible, with the exception of E. faecalis and β-lactamase-producing Staph. aureus. Anaerobic Gram-negative bacteria including B. fragilis are usually susceptible. Bactericidal synergy with aminoglycosides is demonstrable against Ps. aeruginosa and enterobacteria.??
Ticarcillin is generally cross-resistant with carbenicillin. It is somewhat stable to hydrolysis by AmpC-mediated β-lactamases of Gram-negative bacilli, but can be hydrolyzed by most other chromosomally and plasmid-mediated enzymes unless protected by a β-lactamase inhibitor.Pharmacokinetics
Oral absorption: NegligibleCmax 1 g intramuscular: 35 mg/L after 1 h
Plasma half-life: 1.3 h
Volume of distribution: 0.21 L/kg
Plasma protein binding: 50–60%
Absorption and distribution
It is not orally absorbed. On parenteral co-administration with gentamicin, the plasma concentration of ticarcillin is unaffected, but the concentration of gentamicin is lowered. It enters the serous fluids, providing concentrations up to 60% of those of the plasma. It does not cross the normal meninges but levels of up to 50% of those of the plasma can be found in meningitis.
Metabolism and excretion
Up to 15% is excreted as penicilloic acid, a higher percentage than for carbenicillin (up to 5%). Some is excreted in the bile, producing levels 2–3 times those in the plasma, but the main route of excretion is through the kidneys (80%), principally as unchanged drug, appearing in the urine in the first 6 h. It is more rapidly eliminated in children with cystic fibrosis.
Clinical Use
Serious infection, including septicemia, respiratory tract infections, genitourinary tract infections and skin and soft-tissue infections caused by susceptible bacteria???
As with all penicillins, hypersensitivity reactions may occur, but are less frequent and severe than those associated with benzylpenicillin. Rashes and eosinophilia occur; reversible abnormalities of liver function can develop. Since large doses of the drug have to be used, convulsions can occur, as with other penicillins, and being a disodium salt, electrolyte disturbances can result from the sodium load and from loss of potassium.Ticarcillin ?? ?? ? ???
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Ticarcillin ?? ??
???( 87)?? ??
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