Core pharmacology

Class Group

Antidepressant - Serotonin-Noradrenaline reuptake inhibitors

Legacy Cicm Level

Level 3

Mechanism of action

Inhibition of serotonin re-uptake (SERT) and noradrenaline re-uptake (NET).

Low affinity for NET at low doses.

Little muscarinic, H1 or alpha1 antagonism effects

Adverse Effects Toxicity

1. Serotonin A/E
2. Norad- HTN, tachycardia

Absorption

High first pass- F=45%

Protein binding

much lower PB (30%)

Volume of distribution

Large Vd

Metabolism

Hepatic 2D6 metabolism to desvenlafaxine (active)

Excretion

Renal elimination.

Half-life

T1/2= 10 hours