Miscellaneous

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Chapter: Medicinal Chemistry : Narcotic Analgesics

Narcotic Analgesics - Synthesis and Drug Profile - a. Tramadol hydrochloride (Domadol, Stemadol, Tramazac) b. Tilidine HCl (Valoron, Tilidine) c. Sufentanil - Structure, Properties, uses, Synthesis, Assay, Storage, Dosage forms, Dose | Synthesis and Drug Profile |


SYNTHESIS AND DRUG PROFILE

Miscellaneous


a. Tramadol hydrochloride (Domadol, Stemadol, Tramazac)


Properties and uses: It is a white crystalline powder, freely soluble in water and in methanol, very slightly soluble in acetone. The drug possesses opioid activity, but has other analgesic activity that is not reserved by naloxone. It is also used as noradrenaline reuptake inhibitor.

Assay: Dissolve the sample in a mixture of anhydrous acetic acid and add acetic anhydride. Titrate with 0.1 M perchloric acid , and determine the end point potentiometrically.

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

Dose: I.M. or I.V. injection 50 to 100 mg; as suppository 100 mg.

Dosage forms: Tramadol capsules B.P.


b. Tilidine HCl (Valoron, Tilidine)


Properties and uses: It is a white or almost white crystalline powder, freely soluble in water, methylene chloride, and alcohol. It is a narcotic analgesic employed in the treatment of moderate to severe pain.

Assay: Dissolve the substance in a mixture of anhydrous acetic acid and acetic anhydride. Titrate with 0.1 M perchloric acid and determine the end point potentiometrically.

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

Dose: The usual dose is 50 to 100 mg 4 times/day.


c. Sufentanil


Properties and uses: It is a white or almost white powder soluble in water and in alcohol, freely soluble in methanol. It is a structural analogue of fentanyl, used in anaesthesia and as a narcotic analgesic.

Assay: Dissolve the sample in a mixture of 1 volume of anhydrous acetic acid and 7 volumes of methyl ethyl ketone and titrate with 0.1M perchloric acid, using naphtholbenzein solution as indicator.

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


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