Amitriptyline Tablets

Also Amitriptyline hydrochloride BP

Pharmacology
Amitriptyline is a tricyclic depressant.

It’s a potent inhibitor of noradrenaline re-uptake at noradrenergic nerve endings. It’s also a potent inhibitor of 5-hydroxytryptamine (Serotonin) re-uptake with equal efficacy for both mono-amines.

Amitryptyline also has antagonist effects at muscarinic acetycholine receptors and is one of the most potent tricyclic antidepressants. It blocks muscarinic acetycholine receptors in the central nervous system and in the periphery.

Tricyclic antidepressants also posses affinity for muscarinic and histamine H-1 receptors to varying degrees. The mechanism of action of amitriptyline as an antidepressant is usually attributed to it’s ability to inhibit monoamine re-uptake.

Pharmacokinetics
Amitryptyline is readily absorbed from the gastro-intestinal tract, with peak plasma concentrations occuring within a few hours of oral administration.

Amitriptyline undergoes extensive first-pass metabolism and is demethylated in the liver to it’s primary active metabolite — noratriptyline.

Amitriptyline is widely distributed throughout the body and is extensively bound to plasma and tissue protein. It has an elimination half-life ranging from 9 to 25hours, which may be considerably extended in overdosage.

Amitriptyline crosses the placenta and is distributed into breast milk.

Indication
Amitriptyline is an antidepressant of the tricyclic group. It’s indicated for symptoms of depressive illness especially when sedation is required.

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