필로카르핀

필로카르핀 C화학적 특성, 용도, 생산

개요

Pilocarpine acts by stimulating muscarinic receptors, therefore making it similar in action to acetylcholine when systematically introduced. This compound differs from acetylcholine in that it does not react with any nicotinic receptors, but by stimulating the CNS. Its effects are blocked by atropine. It has found therapeutic use in ophthalmology as a myotic agent.

화학적 성질

Colorless crystalline solid or an oil; melts at34°C (93.2°F); dissolves in water, alcohol,and chloroform; slightly soluble in ether andbenzene.

물리적 성질

Appearance: colorless crystal or white crystalline powder. Solubility: freely soluble in water; slightly soluble in ethanol; insoluble in chloroform or diethyl ether. Melting point: 174–178?°C.

역사

It has a history of hundreds of years since pilocarpine was used to treat glaucoma .
In 1933, the chemical synthesis of pilocarpine was firstly reported. However, pilocarpine couldn’t be used for treatments, because its synthetic route is so long and focuses on isopilocarpine, of which the pharmacological activities are 1/20– 1/50 of pilocarpine. In 1972, DeGraw successfully synthesized the cis-homopilopic acid employing catalytic hydrogenation of precious metals and obtained pilocarpine as the main part product. Therefore, the study on the production of pilocarpine by chemical synthesis has made new progress and has been artificially synthesized .

용도

Pilocarpine occurs in the leaves of variousspecies of pilocarpus. It is used as an antidotefor atropine poisoning and in ophthalmologyto produce contraction of the pupil.

정의

ChEBI: The (+)-enantiomer of pilocarpine.

건강위험

Pilocarpine is a tropane alkaloid. Toxicsymptoms are characterized by muscariniceffects. Toxic effects include hypersecretionof saliva, sweat, and tears; contraction of thepupils of the eyes; and gastric pain accom panied with nausea, vomiting, and diarrhea.Other symptoms are excitability, twitching,and lowering of blood pressure. High dosesmay lead to death due to respiratory failure.A lethal dose in humans is estimated withinthe range of 150–200 mg.

Pharmacology

Pilocarpine activates cholinergic M-receptor and has an obvious effect on eyes and salivary glands. Pilocarpine nitrate eye drops take part in the actions of myosis, depressing intraocular pressure and alleviating cyclospasm. It increases glandular secretions at 10–20? mg, i.h., including the sweat gland, salivary gland, lacrimal gland, gastric gland, pancreas, intestinal gland, respiratory mucosa, and so on. Pilocarpine activates intestinal smooth muscle and promotes its tension and peristalsis. It induces asthma by activating bronchial smooth muscle and activates smooth muscles of uterus, bladder, gallbladder, and biliary passage as well

Clinical Use

Pilocarpine nitrate is mainly used to treat glaucoma clinically. Characterized with the progressive cupping of the optic disk, hypopsia, and elevated intraocular pressure, the severe patients will go blind. Patients with angle-closure glaucoma (congestive glaucoma) generally have the narrow anterior chamber angle, the obstruction of aqueous humor outflow, and the elevation of intraocular pressure, and these can be reversed by a low-concentration pilocarpine. But it is noted that a highconcentration pilocarpine will promote the progress of glaucoma. Pilocarpine is also used to treat open-angle glaucoma. The mechanism of the action is not entirely clear. Using atropine and pilocarpine alternately prevents posterior synechiae. In addition, pilocarpine is orally used to treat Zagari’s disease after neck radiotherapy, increasing salivary secretion and sweat secretion

Safety Profile

A human poison by subcutaneous route. Poison experimentally by ingestion, intravenous, intraperitoneal, and subcutaneous routes. A very poisonous alkaloid that is used to remove excess fluid accumulations from the body. Its action on the sweat glands makes it a powerful sudorific. It very rarely causes death, but, when it does, it is by paralysis of the heart or edema of the lungs. Dangerous; on heating to decomposition it emits toxic fumes of NOx.

참고 문헌

Hardy., Bull. Soc. Chim. Fr., 24,497 (1875) Gerrard., Pharm. J., 5,865,965 (1875)
Gerrard., ibid, 7,255 (1877)
Hardy, Calmels., Compt. rend., 102,1116,1251,1562 (1886)
Wagenaar., Pharm. Weekbl., 67, 285 (1930)
Preobrashenski et al., Ber., 63,460 (1930)
Preobrashenskietal., ibid, 69, 1835 (1936)
Roche, Lynch., Analyst, 73,311 (1948) Pharmacology: Hollander., Gastroenterology, 2, 20 I (1944)

필로카르핀 준비 용품 및 원자재

원자재

준비 용품

필로카르핀 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Henan Fengda Chemical Co., Ltd	+86-371-86557731 +86-13613820652	info@fdachem.com	China	7377	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21695	55
Shanghai Zheyan Biotech Co., Ltd.	18017610038	zheyansh@163.com	CHINA	3620	58
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28180	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58
Hefei TNJ Chemical Industry Co.,Ltd.	0551-65418671	sales@tnjchem.com	China	34572	58
Qiuxian Baitai New Material Co., LTD	+8618330912755	sale2@hbyalin.com	China	1677	58
ANHUI WITOP BIOTECH CO., LTD	+8615255079626	eric@witopchemical.com	China	23556	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	29474	58

필로카르핀 관련 검색: