シクランデラート 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
効能
血管拡張薬
説明
Almond (Amygdalus communis L) is a kind of nut from Xinjiang, China.
Traditional Chinese medicine believes that almond can promote blood circulation to
dispel blood stasis, lubricate bowels to relieve constipation, and relieve cough and
asthma. The indications include amenorrhea, fever, wind arthralgia, malaria, blood
stasis and pain, injuries, and blood stasis with constipation.
物理的性質
Appearance: white or almost white amorphous powder, special smell, and bitter
taste. Solubility: very soluble in ethanol or acetone and almost insoluble in water.
Melting point: 50–62 °C.
来歴
The chemical synthesis of cyclandelate was first synthesized by Funcke et al. from
Elan Corporation in Ireland using a-hydroxyphenylacetic acid and cis-3,3,5-cycloalkyl
cyclohexanol. The raw material of mandelic acid was obtained by hydrolysis
after benzaldehyde reacted to sodium cyanide. However, sodium cyanide is hypertoxic, and because of its unique structure of a-hydroxy acid, it is easy to
decompose under the acid condition, which leads to more by-products and low
yield. A series of improved methods have been developed, which can reduce the
environmental pollution under the premise of ensuring the yield of Zn/HCOONH4/
C2H5OH system . The method was used to synthesize cyclandelate since then.
However, this drug has not yet been approved by the Food and Drug Administration
in the United States, Canada, and other countries because it easily causes white
blood cell deficiency. It has been withdrawn from the market after drug approval in
Japan, France, and other countries in the 1970s.
使用
vasodilator
定義
ChEBI: The ester obtained by formal condensation of mandelic acid and 3,3,5-tricyclohexanol. It is a direct-acting smooth muscle relaxant used to dilate blood vessels.
適応症
The indications of cyclandelate are arteriosclerosis obliterans, acrocyanosis, cerebral
arteriosclerosis, cerebral insufficiency, cerebrovascular disease, brain trauma,
and post-traumatic brain syndrome.
世界保健機関（WHO）
Cyclandelate is a papaverine type spasmolytic and vasodilating
drug intended for symptomatic treatment of various peripheral vascular disorders,
such as intermittent claudication in arteriosclerosis obliterans as well as a
treatment for cognitive dysfunction in patients suffering from senile dementia of
the multi-infarct or Alzheimer's type. Cyclandelate remains registered in several
countries.
薬理学
The chemical structure and effect of cyclandelate are similar to papaverine. It can
directly relax vascular smooth muscle and relieve the spasm of ileum and uterus
smooth muscle induced by acetylcholine, histamine, and barium chloride in guinea
pig. This effect is three to five times stronger than papaverine. Cyclandelate can also
expand the cardiovascular, cerebrovascular, and renal blood vessels and limb peripheral
vascular and coronary artery, increase blood flow, and promote blood circulation
. It can also increase the tolerance to hypoxia, but the effect on human cerebral
blood flow has not been confirmed. It was reported that cyclandelate can promote
collateral circulation but has little effect on respiration, blood pressure, cardiac output,
and myocardial oxygen consumption. It is safe for long-term administration .
臨床応用
Cyclandelate can be used for clinical treatment of cerebral arteriosclerosis, cerebral
vascular accident and its sequelae, post-traumatic brain syndrome, coronary arteriosclerosis,
hypertensive heart disease, Raynaud’s disease, thromboangiitis obliterans,
acrocyanosis, and Meniere’s disease .
シクランデラート 上流と下流の製品情報
原材料
準備製品