Amino alcohol esters

| Home | | Medicinal Chemistry |

Chapter: Medicinal Chemistry : Anticholinergic Drugs

Anticholinergic Drugs: Amino alcohol esters - Synthesis and Drug Profile - i. Cyclopentolate HCl(Cyclopent, Cyclate, Dilate) ii. Clidinium Bromide iii. Dicyclomine HCl (Bentyl, Mesbentyl) iv. Glycopyrrolate Bromide v. Propanthelin bromide (Probanthine, Spastheline) - Structure, Properties, uses, Synthesis, Assay, Storage, Dosage forms, Dose | Synthesis and Drug Profile


SYNTHESIS AND DRUG PROFILE

Amino alcohol esters


i. Cyclopentolate HCl(Cyclopent, Cyclate, Dilate)


Synthesis

Route I. From: Sodium phenyl acetate


Route II. From: Phenyl acetate ion


Properties and uses: It exists as white crystalline powder, soluble in water, methanol, and ethanol, but insoluble in toluene. Cyclopentolate is usually employed as eye drops to cause cycloplegia and mydriasis. It acts much faster than atropine and possesses a relatively shorter duration of action.

Assay: Dissolve the sample in a mixture of 0.1 M hydrochloric acid and alcohol. Titrate with 0.1 M sodium hydroxide and determine the end point potentiometrically.

Dose: Topically for adult, 1 drop of 1 or 2% solution to the conjunctiva; for refraction 1 drop of a 0.5% solution repeated after 5 to 15 min.

Dosage forms: Cyclopentolate eye drops B.P.


ii. Clidinium Bromide


Synthesis


Uses: Used as a bronchodilator in asthmatic conditions. It has a longer lasting effect as compared to β-agonists.


iii. Dicyclomine HCl (Bentyl, Mesbentyl)


Synthesis


Properties and uses: It exists as a white, crystalline powder with a bitter taste, soluble in water and chloroform. Dicyclomine HCl behaves both as an antimuscarinic and a nonspecific antispasmodic agent. It was first introduced in 1950 and had minimized the adverse effects associated with the atropine type of compounds. Dicyclomine has spasmolytic effect on various smooth muscle spasms particularly those associated with the gastrointestinal (GI) tract. It is also used in dysmenorrhoea, pylorospasm, and biliary dysfunction.

Dose: By oral or I.M. 10 to 20 mg per day in four divided dose.


iv. Glycopyrrolate Bromide


Synthesis


Properties and uses: It exists as a white, crystalline powder with a bitter taste, soluble in water and alcohol. It is used for suppressing gastric secretion and in the treatment of peptic ulcer and gastrointestinal disorder associated with spasm.


v. Propanthelin bromide (Probanthine, Spastheline)


Synthesis

Route I. From: Xanthene-9-carboxylate


Route II. From: o-phenoxy benzoic acid


Properties and uses: It is a white or yellowish-white powder, slightly hygroscopic, soluble in water, in alcohol, and in methylene chloride. It is beneficial for the treatment of peptic ulcer, due to the decreased gastric motility by this drug, and it may relieve the pain in this condition.

Assay: Dissolve the sample in acetic anhydride. Titrate with 0.1 M perchloric acid and determine the end point potentiometrically.

Storage: It should be stored in well-closed airtight container, and protected from light. Dose: The usual initial dose is 15 mg thrice/day before meals; and 30 mg at bed time. Dosage forms: Propantheline bromide tablets I.P., Propantheline tablets B.P.


Contact Us, Privacy Policy, Terms and Compliant, DMCA Policy and Compliant

TH 2019 - 2022 pharmacy180.com; Developed by Therithal info.