テルブタリン 化学特性,用途語,生産方法
効能
気管支拡張薬, β2アドレナリン受容体作動薬
説明
Terbutaline is a synthetic congener of adrenaline that acts at the
β2-receptor causing bronchodilation and tocolytic effects. It
was the first β2-selective adrenoreceptor agonist in general
clinical use. In 2011, the Food and Drug Administration (FDA)
placed a black-boxed warning on terbutaline stating that terbutaline
injections should not be given to pregnant women nor
should be used to prevent preterm labor or for long-term
(greater than 48–72 h) treatment of preterm labor. Oral terbutaline
should not be used at all due to its potential for
cardiac toxicity and death. Terbutaline is on the World Anti-
Doping Agency’s list of prohibited drugs for Olympic athletes
(except when a Therapeutic Use Exemption has been granted in
advance and when used by inhalation).
使用
Terbutaline is used for preventing and relieving bronchospasms in bronchial asthma, chronic bronchitis, pulmonary emphysema, and other broncho-pulmonary diseases.
適応症
Terbutaline (Brethine, Bricanyl) is a relatively specific
β
2-adrenoceptor agonist.
Terbutaline can prevent premature labor, especially in
individuals who are more than 20 weeks into gestation
and have no indication of ruptured fetal membranes or
in whom labor is not far advanced. Its effectiveness in
premature labor after 33 weeks of gestation is much less
clear. Terbutaline can decrease the frequency, intensity,
and duration of uterine contractions through its ability
to directly stimulate β
2-adrenoceptors. While it appears
to be especially selective for β
2-receptor activation,
terbutaline does have some β
1 activity as well.
定義
ChEBI: A member of the class of phenylethanolamines that is catechol substuted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group.
作用機序
Terbutaline is a synthetic sympathomimetic amine. It is one of the most selective direct–acting
stimulants of β2-adrenoreceptors. It stimulates smooth muscle β2-adrenoreceptors in the
bronchi, relaxing them and relatively minutely acting on the β1—receptors of the heart.
臨床応用
Terbutaline should be initially used only in an
appropriate hospital setting where any obstetric complications
can be readily addressed. After initial administration,
it can be used in the outpatient setting.
Concomitant use of β
2-adrenergic agonists and corticosteroids
have additional diabetic effects and may
rarely lead to pulmonary edema.The combination of β
2-
adrenergic agonists and magnesium sulfate can cause
cardiac disturbances, while coadministration of terbutaline
with other sympathomimetics can lead to the potentiation
of the actions of the latter drugs.
副作用
Terbutaline is frequently used in the management of
premature labor, although it has not been marketed for
such use. Its effectiveness, side effects, precautions, and
contraindications are similar to those of all β
2-adrenergic
agonists. Terbutaline can cause tachycardia, hypotension,
hyperglycemia, and hypokalemia. It can be
given orally in addition to subcutaneous or intravenous
administration.
環境運命予測
Terbutaline is administered as the sulfate. It is a white to graywhite,
crystalline powder; nearly odorless or with the faint odor
of acetic acid. Terbutaline has a slightly bitter taste. It has
a melting point of 247°C. Terbutaline sulfate is soluble at 1 g
per 1.5 ml water or 250 ml of ethanol. It is soluble in 0.1 N
hydrochloric acid, slightly soluble in methanol, and insoluble
in chloroform. While terbutaline is stable under normal
conditions as a solid, it is unstable in light. Terbutaline is
degraded through oxidative processes; this is enhanced in the
presence of trace levels of metals and in the presence of oxygen.
No information is currently available on breakdown in soil,
groundwater, or surface water.
テルブタリン 上流と下流の製品情報
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