2,6-ジイソプロピルフェノール 化学特性,用途語,生産方法
外観
無色～黄褐色又は褐色、液体
用途
イソプロピルフェノール誘導 体です。GABAA 受容体に作用し、麻酔作用 を示します。
用途
イソプロピルフェノール誘導
体です。GABAA 受容体に作用し、麻酔作用
を示します。
効能
静脈麻酔薬, GABA-A受容体作動薬
商品名
ディプリバン (アスペンジャパン); ディプリバン (アスペンジャパン)
説明
Propofol is an injectable, short-acting general anesthetic with a low incidence of side effects.
化学的特性
Light Yellow Liquid
使用
Propofol is an anesthetic used in veterinary medicine.
世界保健機関（WHO）
Propofol, a short acting injectable anaesthetic, was introduced in
1987. In April 1992, the Norwegian Medicines Control Board reported that
prolonged use of propofol had been associated with two fatalities in children
characterized by metabolic acidosis, liver enlargement, and cerebral oedema. The
UK Committee on the Safety of Medicines has received 5 reports of deaths
occurring in children who had received propofol while in intensive care.
生物学の機能
Propofol (Diprivan) is rapidly acting, has a short recovery
time, and possesses antiemetic properties. A rapid
onset of anesthesia (50 seconds) is achieved, and if no
other drug is administered, recovery will take place in 4
to 8 minutes.The recovery is attributed to redistribution
of the drug and rapid metabolism to glucuronide and
sulfate conjugates by the liver and extrahepatic tissues,
such as intestine and kidney.
Rapid recovery and its antiemetic properties make
propofol anesthesia very popular as an induction agent
for outpatient anesthesia. Propofol can also be used to
supplement inhalational anesthesia in longer procedures.
Both continuous infusion of propofol for conscious
sedation and with opioids for the maintenance of
anesthesia for cardiac surgery are acceptable techniques.
一般的な説明
Propofol is an injectable sedative–hypnotic used for the inductionand maintenance of anesthesia or sedation. Propofolis only slightly soluble in water with an octanol/water partitioncoefficient of 6,761:1; thus, it is formulated as an oil-inwateremulsion. The fat component of the emulsion consistsof soybean oil, glycerol, and egg lecithin. The pKa of thepropanol hydroxyl is 11 and the injectable emulsion has apH of 7 to 8.5. Formulations contain either disodium ethylenediaminetetraaceticacid (EDTA) (0.005%) or sodiummetabisulfite to retard the growth of microorganisms. EDTAis a metal chelator and patients on propofol containingEDTA for extended periods of time excrete more zinc andiron in their urine. The clinical consequence of this is notknown but the manufacturer recommends that a drug holidayor zinc supplementation be considered after 5 days of therapy.
生物活性
Intravenous general anesthetic and hypnotic with a mode of action which includes potentiation of GABA-mediated inhibitory synaptic transmission, direct activation of the GABA A receptor and inhibition of glutamate receptor mediated excitatory synaptic transmission. Also potentiates P2X 4 receptor-mediated currents in P2X 4 -HEK293 cells.
薬理学
Propofol is primarily a hypnotic drug with substantial
cardiorespiratory depressant actions and with no ability
to produce neuromuscular blockade. While propofol
lacks analgesic properties, its use permits lower doses of
opioids. Likewise, less propofol is required for adequate
hypnosis when it is administered with opioids.Thus, it is
said that propofol and opioids interact synergistically.
臨床応用
Generic formulations of propofol may contain sodiummetabisulfite as the antimicrobial agent, and patients allergicto sulfites, especially asthmatic patients, should avoid thisformulation. Aseptic technique must be followed and unusedportions of the drug must be discarded according to the manufacturer’s instructions to prevent microbial contaminationand possible sepsis.
副作用
The dose of propofol should be reduced in older patients;
however, it does have a relatively linear dose–
response characteristic, and patients generally can be safely titrated. The pain on injection, especially when
small veins are used, can be considerably reduced if lidocaine
20 mg is administered first.
Anesthesia induction with propofol causes a significant
reduction in blood pressure that is proportional to
the severity of cardiovascular disease or the volume status
of the patient, or both. However, even in healthy patients
a significant reduction in systolic and mean arterial
blood pressure occurs. The reduction in pressure
appears to be associated with vasodilation and myocardial
depression. Although propofol decreases systemic
vascular resistance, reflex tachycardia is not observed.
This is in contrast to the actions of thiopental.
The heart rate stabilization produced by propofol relative
to other agents is likely the result of either resetting
or inhibiting the baroreflex, thus reducing the tachycardic
response to hypotension.
Since propofol does not depress the hemodynamic
response to laryngoscopy and intubation, its use may
permit wide swings in blood pressure at the time of induction
of anesthesia. Propofol should be used with utmost
caution in patients with cardiac disease.
安全性プロファイル
Poison by intravenous
and intraperitoneal routes. Experimental
reproductive effects. Combustible when
exposed to heat or flame; can react with
oxidizing materials. To fight fire, use foam,
CO2, dry chemical. When heated to
decomposition it emits acrid smoke and
fumes. See also PHENOL
2,6-ジイソプロピルフェノール 上流と下流の製品情報
原材料
準備製品