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Ticarcillin

Ticarcillin ??? ???
?? ??:
34787-01-4
???:
Ticarcillin
???(??):
Temocillin Disodium;icarcillin;TICARCILLIN;TRIARCILLIN;Ticarcillin acid;Ticcarcillin acid;Ticarcillin USP/EP/BP;Ticarcillin free base;Ticarcillin Impurity 11;Ticarcillin See T437901
CBNumber:
CB7224768
???:
C15H16N2O6S2
??? ??:
384.43
MOL ??:
34787-01-4.mol

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)
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
??? ?? Xn
?? ???? ?? 42/43
????? 22-36/37-45
WGK ?? 3
????(GHS): Health Hazard (GHS08)
?? ?: Danger
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H317 ????? ?? ??? ??? ? ?? ?? ??? ?? ?? 1 ?? P261, P272, P280, P302+P352,P333+P313, P321, P363, P501
H334 ?? ? ????? ??, ?? ?? ?? ?? ?? ??? ? ?? ??? ??? ?? ?? 1 ?? P261, P285, P304+P341, P342+P311,P501
??????:
P261 ??·?·??·???·??·...·????? ??? ????.
P280 ????/???/???/?????? ?????.
P342+P311 ??? ??? ???? ????(??)? ??? ????.

Ticarcillin C??? ??, ??, ??

??

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: Negligible
Cmax 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 ?? ??

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Ticarcillin ?? ??:

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