Prescriber's Guide: Antidepressants: Stahl's Essential Psychopharmacology by Stephen M. Stahl

Author:Stephen M. Stahl
Language: eng
Format: mobi
Publisher: Cambridge University Press
Published: 2014-09-24T21:00:00+00:00

Lofepramine

Lofepramine: THERAPEUTICS

Brands

• Deprimyl

• Gamanil

see index for additional brand names

Generic?

Yes

Class

• Tricyclic antidepressant (TCA)

• Predominantly a norepinephrine/noradrenaline reuptake inhibitor

Commonly Prescribed for

(bold for FDA approved)

• Major depressive disorder

• Anxiety

• Insomnia

• Neuropathic pain/chronic pain

• Treatment-resistant depression

How the Drug Works

• Boosts neurotransmitter norepinephrine/noradrenaline

• Blocks norepinephrine reuptake pump (norepinephrine transporter), presumably increasing noradrenergic neurotransmission

• Since dopamine is inactivated by norepinephrine reuptake in frontal cortex, which largely lacks dopamine transporters, lofepramine can increase dopamine neurotransmission in this part of the brain

• A more potent inhibitor of norepinephrine reuptake pump than serotonin reuptake pump (serotonin transporter)

• At high doses may also boost neurotransmitter serotonin and presumably increase serotonergic neurotransmission

How Long Until It Works

• May have immediate effects in treating insomnia or anxiety

• Onset of therapeutic actions usually not immediate, but often delayed 2–4 weeks

• If it is not working within 6–8 weeks for depression, it may require a dosage increase or it may not work at all

• May continue to work for many years to prevent relapse of symptoms

If It Works

• The goal of treatment of depression is complete remission of current symptoms as well as prevention of future relapses

• The goal of treatment of chronic neuropathic pain is to reduce symptoms as much as possible, especially in combination with other treatments

• Treatment of depression most often reduces or even eliminates symptoms, but not a cure since symptoms can recur after medicine stopped

• Treatment of chronic neuropathic pain may reduce symptoms, but rarely eliminates them completely, and is not a cure since symptoms can recur after medicine is stopped

• Continue treatment of depression until all symptoms are gone (remission)

• Once symptoms of depression are gone, continue treating for 1 year for the first episode of depression

• For second and subsequent episodes of depression, treatment may need to be indefinite

• Use in anxiety disorders and chronic pain may also need to be indefinite, but long-term treatment is not well studied in these conditions

If It Doesn’t Work

• Many depressed patients have only a partial response where some symptoms are improved but others persist (especially insomnia, fatigue, and problems concentrating)

• Other depressed patients may be nonresponders, sometimes called treatment-resistant or treatment-refractory

• Consider increasing dose, switching to another agent or adding an appropriate augmenting agent

• Consider psychotherapy

• Consider evaluation for another diagnosis or for a comorbid condition (e.g., medical illness, substance abuse, etc.)

• Some patients may experience apparent lack of consistent efficacy due to activation of latent or underlying bipolar disorder, and require antidepressant discontinuation and a switch to a mood stabilizer

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