Drug intelligence / Profile preview

methylphenidate + mirtazapine

Development stage
Phase 3
Modality
Small Molecules
Administration
Oral, Transdermal
01

Overview

This is a combination of two pharmaceutical drugs, methylphenidate and mirtazapine. Methylphenidate is a central nervous system stimulant primarily used to treat attention deficit hyperactivity disorder (ADHD) and narcolepsy. It acts mainly by inhibiting the reuptake of dopamine and norepinephrine, increasing their synaptic concentrations in the brain[4][6]. Mirtazapine is an antidepressant classified as a noradrenergic and specific serotonergic antidepressant (NaSSA). It works by antagonizing presynaptic alpha-2 adrenergic receptors, thereby increasing noradrenergic and serotonergic neurotransmission; it also blocks postsynaptic serotonin 5-HT2 and 5-HT3 receptors, contributing to its anxiolytic, sleep-improving, and appetite-stimulating effects[5][6]. The combination has been studied for use in several clinical scenarios: - As add-on therapy for depression in terminally ill cancer patients to accelerate antidepressant response[1]. - To mitigate weight loss and insomnia associated with stimulant treatment (such as methylphenidate) in children with ADHD[2]. - In adults with ADHD where adjunctive mirtazapine may help reduce stimulant-induced insomnia or address comorbid depressive symptoms[3].

02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)HTR3A (5-hydroxytryptamine receptor 3A)ADRA2A (α2A)DAT (Dopamine plasma membrane transport protein)HRH1 (Histamine H1 Receptor)NET (Norepinephrine Transporter)5-HT2 (5-HT2 receptor family)

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