CYCLANDELATE

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H319：눈에 심한 자극을 일으킴

• 예방조치문구

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

  P305+P351+P338：눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

CYCLANDELATE 화학적 특성, 용도, 생산

• 개요

  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.

• 물리적 성질

  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.

• 역사

  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 It has been withdrawn from the market after drug approval in Japan, France, and other countries in the 1970s.

• 용도

  vasodilator

• 정의

  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.

• Indications

  The indications of cyclandelate are arteriosclerosis obliterans, acrocyanosis, cerebral arteriosclerosis, cerebral insufficiency, cerebrovascular disease, brain trauma, and post-traumatic brain syndrome.

• World Health Organization (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.

• Pharmacology

  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 .

• Clinical Use

  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 .

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