Switching from Oral Antipsychotics to Lurasidone

• With aripiprazole, amisulpride, and paliperidone ER, immediate stop is possible; begin lurasidone at an intermediate dose

• Clinical experience has shown that quetiapine, olanzapine, and asenapine should be tapered off slowly over a period of 3–4 weeks, to allow patients to readapt to the withdrawal of blocking cholinergic, histaminergic, and alpha-1 receptors

• Clozapine should always be tapered off slowly, over a period of 4 weeks or more

* Benzodiazepine or anticholinergic medication can be administered during cross-titration to help alleviate side effects such as insomnia, agitation, and/or psychosis

Suggested Reading

Ishibashi T, Horisawa T, Tokuda K et al. Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther 2010;334(1):171–81.

Meyer JM, Loebel AD, Schweizer E. Lurasidone: A new drug in development for schizophrenia. Expert Opin Investig Drugs 2009;18(11):1715–26.

Nakamura M, Ogasa M, Guarino J et al. Lurasidone in the treatment of acute schizophrenia: A double-blind, placebo-controlled trial. J Clin Psychiatry 2009;70(6):829–36.

Stahl SM. The serotonin 7 receptor as a novel therapeutic target. J Clin Psychiatry 2010,71: 1414–1415.

Tarazi F, Stahl SM. Iloperidone, asenapine and lurasidone: a primer on their current status. Exp Opin Pharmacother 2013;13(13):1911–22.

MAPROTILINE

MAPROTILINE: THERAPEUTICS

Brands

• Ludiomil

see index for additional brand names

Generic?

Yes

Class

• Tricyclic antidepressant (TCA), sometimes classified as a tetracyclic antidepressant (tetra)

• Predominantly a norepinephrine/noradrenaline reuptake inhibitor

Commonly Prescribed for

(bold for FDA approved)

• Depression

• 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, maprotiline can thus 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

• 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 is 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