Difference Between the Quaternary and the Tertiary Antimuscarinics

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Chapter: Medicinal Chemistry : Anticholinergic Drugs

Anticholinergic Drugs : Difference Between the Quaternary and the Tertiary Antimuscarinics


DIFFERENCE BETWEEN THE QUATERNARY AND THE TERTIARY ANTIMUSCARINICS


Quaternary Amines

  • These drugs do not pass through the blood brain barrier, and hence, lack CNS actions.

  • Penetrate poorly into the eye from the blood stream or cornea.

  • The quaternary compounds have greater affinity for nicotinic receptors, so that a great degree of ganglionic blockade may result.

  • These are mostly excreted unchanged into the urine.


Tertiary Amines

  • These drugs can penetrate the cell membranes in the nonionized form, and hence, can pass through the blood brain barrier. In the brain, they can exert both therapeutic and toxic actions.

  • These drugs penetrate through the cornea and cause mydriasis and cycloplegia.

  • They do not have nicotinic receptor affinity.

  • These drugs are biotransformed in the liver.


Therapeutic Uses

  1. Used topically to dilate the pupil and paralyze accommodation.

  2. Used as a preanaesthetic medication, to inhibit excessive salivary, bronchial secretions, and to prevent bronchospasm and laryngospasm.

  3. The antisecretory effects are also sought in the treatment of acute coryza, hay fever, and rhinitis.

  4. Used in the treatment of bronchial asthma and peptic ulcer.

  5. Used in the treatment of Parkinson’s disease.


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