Amino Alcohol

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Chapter: Medicinal Chemistry : Anticholinergic Drugs

Anticholinergic Drugs : Synthesis and Drug Profile - Synthesis and Drug Profile - i. Biperiden (Akineton Hydrochloride) ii. Procyclidine HCl (Kemadrin, Picidin, Prodine) iii. Trihexylphenidyl (Pacitane, Parkin, Triphen) - Structure, Properties, uses, Synthesis, Assay, Storage, Dosage forms, Dose | Synthesis and Drug Profile


SYNTHESIS AND DRUG PROFILE

Amino Alcohol


i. Biperiden (Akineton Hydrochloride)


Synthesis


Properties and uses: It is a white crystalline powder, slightly soluble in methylene chloride, in water, and in alcohol. It has a relatively strong musculotropic action, which is about equal to that of papaverine, in comparison with most synthetic anticholinergic drugs. It is used in all types of Parkinson’s disease.

Assay: Dissolve the sample in alcohol and titrate with 0.1 M alcoholic potassium hydroxide and determine the end point potentiometrically

Storage: It should be stored in well-closed airtight containers and protected from light.

Dose: For parkinsonism, 2 mg 3 or 4 times/day.


ii. Procyclidine HCl (Kemadrin, Picidin, Prodine)


Synthesis


Properties and uses: It exists as white crystalline powder, and it has been used for peripheral effects that are similar to methantheline. Its clinical usefulness lies in its ability to relieve voluntary muscle spasticity through its central action. Procyclidine is used in the treatment of Parkinson’s disease.

Assay: It is assayed by nonaqueous titration. The solution of the sample is titrated with 0.1 M perchloric acid using crystal violet as an indicator.

Dose: The initial oral dose is 7.5 mg/day in 3 or 4 divided doses after meals; maintenance dose is usually 20 to 30 mg per day.

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


iii. Trihexylphenidyl (Pacitane, Parkin, Triphen)


Synthesis


Properties and uses: It is a white crystalline powder, slightly soluble in water, sparingly soluble in alcohol and in methylene chloride. It is used as antispasmodic and antiparkinsonian agent. Trihexylphenidyl is more effective than levodopa against Parkinson’s tremor.

Assay: Dissolve the sample in alcohol and add 0.01 M hydrochloric acid. Perform potentiometric titration using 0.1 M sodium hydroxide.

Dose: Initial oral dose is 1 mg on first day, followed by 2 mg daily after 3 to 5 days; maintenance dose, 6 to 10 mg/day in 3 to 4 divided doses but not exceeding 20 mg/day.

Dosage forms: Trihexylphenidyl tablets B.P.


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