チカルシリン 化学特性,用途語,生産方法
効能
抗生物質, 細胞壁合成阻害薬
説明
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.
定義
ChEBI: A penicillin compound having a 6beta-[(2R)-2-carboxy-2-thiophen-3-ylacetyl]amino side-group.
抗菌性
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.
獲得抵抗性
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.
薬物動態学
Oral absorption: Negligible
C
max 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.
臨床応用
Serious infection, including septicemia, respiratory tract infections,
genitourinary tract infections and skin and soft-tissue infections caused
by susceptible bacteria
副作用
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.
チカルシリン 上流と下流の製品情報
原材料
準備製品