药品详细
Pilocarpine(毛果芸香碱)
化学结构式图
中文名
毛果芸香碱
英文名
Pilocarpine
分子式
C11H16N2O2
化学名
(3S,4R)-3-ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]oxolan-2-one
分子量
Average: 208.2569
Monoisotopic: 208.121177766
Monoisotopic: 208.121177766
CAS号
54-71-7
ATC分类
N07A 未知;S01E 抗青光眼制剂及缩瞳药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma. [PubChem]
生产厂家
- Akorn inc
- Alcon inc
- Alcon laboratories inc
- Corepharma llc
- Eisai inc
- Impax laboratories inc
- Lannett holdings inc
- Roxane laboratories inc
封装厂家
- Actavis Group
- Advanced Pharmaceutical Services Inc.
- Akorn Inc.
- Alcon Laboratories
- Bausch & Lomb Inc.
- Corepharma LLC
- Dispensing Solutions
- E. Fougera and Co.
- Eisai Inc.
- Falcon Pharmaceuticals Ltd.
- Global Pharmaceuticals
- Impax Laboratories Inc.
- Lannett Co. Inc.
- Mallinckrodt Inc.
- MGI Pharma
- Murfreesboro Pharmaceutical Nursing Supply
- Novartis AG
- OMJ Pharmaceuticals
- Optopics
- Patheon Inc.
- Pharmedix
- Physicians Total Care Inc.
- Prescript Pharmaceuticals
- Rebel Distributors Corp.
- Roxane Labs
- Sandoz
- Taylor Pharmaceuticals
- Wa Butler Co.
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
|
| Substructures |
|
适应症
药理
| Indication | For the treatment of radiation-induced dry mouth (xerostomia) and symptoms of dry mouth in patients with Sjögrens syndrome. |
| Pharmacodynamics | Pilocarpine is a choline ester miotic and a positively charged quaternary ammonium compound. Pilocarpine, in appropriate dosage, can increase secretion by the exocrine glands. The sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract may be stimulated. When applied topically to the eye as a single dose it causes miosis, spasm of accommodation, and may cause a transitory rise in intraocular pressure followed by a more persistent fall. Dose-related smooth muscle stimulation of the intestinal tract may cause increased tone, increased motility, spasm, and tenesmus. Bronchial smooth muscle tone may increase. The tone and motility of urinary tract, gallbladder, and biliary duct smooth muscle may be enhanced. Pilocarpine may have paradoxical effects on the cardiovascular system. The expected effect of a muscarinic agonist is vasodepression, but administration of pilocarpine may produce hypertension after a brief episode of hypotension. Bradycardia and tachycardia have both been reported with use of pilocarpine. |
| Mechanism of action | Pilocarpine is a cholinergic parasympathomimetic agent. It increase secretion by the exocrine glands, and produces contraction of the iris sphincter muscle and ciliary muscle (when given topically to the eyes) by mainly stimulating muscarinic receptors. |
| Absorption | There was a decrease in the rate of absorption of pilocarpine from SALAGEN Tablets when taken with a high fat meal by 12 healthy male volunteers |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism |
Possibly occurs at the neuronal synapses and in the plasma
|
| Route of elimination | Not Available |
| Half life | 0.76 hours |
| Clearance | Not Available |
| Toxicity | Not Available |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | ||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
|
|||||||||||||||||||||||||||||||||||||||
| Predicted Properties |
|
|||||||||||||||||||||||||||||||||||||||
药物相互作用
| Drug | Interaction |
|---|---|
| Tacrine | The acetylcholinesterase inhibitor, Tacrine, may increase the adverse/toxic effects of Pilocarpine, a cholinergic agonist. Monitor for increased cholinergic effects and toxicity. |
食物相互作用
Not Available
收藏