Venlafaxine (Effexor, Effexor XR)

Class

SNRI (Serotonin-Norepinephrine Reuptake Inhibitor)

Mechanism

Enhances serotonergic and noradrenergic activity in the prefrontal cortex by inhibiting the reuptake of serotonin and norepinephrine; at lower doses it primarily affects serotonin, while higher doses also engage norepinephrine reuptake inhibition. Dopaminergic effects in the prefrontal cortex have also been observed at higher doses, possibly contributing to energy and motivation enhancement.

FDA-Approved Use

Major depressive disorder (MDD), generalized anxiety disorder (GAD), panic disorder, social anxiety disorder (SoAD)

Off-Label Use

Premenstrual dysphoric disorder (PMDD), posttraumatic stress disorder (PTSD), obsessive-compulsive disorder (OCD), neuropathic pain, fibromyalgia, migraine prophylaxis, post-stroke depression (PSD), depression in Parkinson’s disease (PD)

Formulation

Oral immediate-release and extended-release capsules/tablets (37.5 mg, 75 mg, 150 mg, 225 mg)

Titration

37.5 mg p.o. daily, titrated in 37.5–75 mg increments every 4–7 days as tolerated

Dose Range

75–375 mg/day (lower range for anxiety, higher for depression)

Kinetics

Half-life ~5 hours (IR) and ~15 hours (XR); metabolized by CYP2D6 to active metabolite (O-desmethylvenlafaxine); steady state reached in ~3 days

Common AEs

Nausea, dizziness, insomnia, dry mouth, diaphoresis, weight loss, constipation, sexual dysfunction, and dose-dependent increases in blood pressure

Serious/Rare AEs

Hypertension (especially >150 mg/day), serotonin syndrome, SIADH, angle-closure glaucoma, withdrawal symptoms with abrupt cessation

Monitoring

Monitor blood pressure regularly, particularly at doses > 150 mg/day. Assess for suicidality and withdrawal symptoms during discontinuation or missed doses.

Black Box Warning

Increased risk of suicidal thoughts and behaviors in children, adolescents, and young adults with MDD.

Considerations

Venlafaxine requires dose adjustments in patients with renal or hepatic impairment, with reductions of 25–50% recommended. In individuals with seizure disorders or traumatic brain injury (TBI), venlafaxine may lower the seizure threshold, especially at higher doses. In patients with neurodegenerative disorders such as Parkinson’s disease (PD) or dementia (e.g., Alzheimer’s disease [AD], Lewy body dementia [LBD]), it may exacerbate agitation, anxiety, or confusion, though it can still be beneficial for depressive symptoms when used cautiously. Older adults may be more prone to orthostatic hypotension and should begin at lower doses with slow titration.