Amino ethers

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Chapter: Medicinal Chemistry : Anticholinergic Drugs

Anticholinergic Drugs : Amino ethers - Synthesis and Drug Profile - i. Orphenadrine citrate (Orphipal) ii. Benztropine Mesylate - Structure, Properties, uses, Synthesis, Assay, Storage, Dosage forms, Dose | Synthesis and Drug Profile


SYNTHESIS AND DRUG PROFILE

Amino ethers


i. Orphenadrine citrate (Orphipal)


Synthesis


Properties and uses: It is a white or almost white crystalline powder, sparingly soluble in water, slightly soluble in alcohol. It is used for the symptomatic treatment of Parkinson’s disease. It is also used as a skeletal muscle relaxant.

Assay: Dissolve the sample in anhydrous acetic acid and titrate with 0.1 M perchloric acid. Determine the end point potentiometrically.

Storage: It should be stored in well-closed containers. If the substance is sterile, it should be stored in a sterile, airtight, tamper-proof container, and protected from light.

Dose: The initial oral dose is 100 mg twice/day; I.M. or I.V. 60 mg every 12 hrs.


ii. Benztropine Mesylate


Synthesis


Properties and uses: It is a white crystalline powder, insoluble in ether, but soluble in water and ethanol. It has anticholinergic, antihistaminic, and local anaesthetic activities. It is used in the treatment of Parkinsons’s disease.

Dosage forms: Benzatropine injection B.P., Benzatropine tablets B.P.


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