Drug intelligence / Profile preview

cyproheptadine + methylphenidate

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral, Transdermal
01

Overview

Cyproheptadine + methylphenidate is a non-branded combination of two small molecule drugs, each with distinct mechanisms and indications. Cyproheptadine is an antihistamine with additional antiserotonergic and anticholinergic properties, primarily used to treat allergic symptoms but also used off-label for appetite stimulation and to counteract stimulant-induced weight loss or insomnia in patients treated for attention deficit hyperactivity disorder (ADHD)[4][5][7]. Methylphenidate is a central nervous system stimulant commonly prescribed for ADHD and narcolepsy. The combination is sometimes used in clinical practice—though not as a fixed-dose product—to manage side effects such as appetite suppression or insomnia caused by stimulants like methylphenidate[7]. There are no known direct pharmacological interactions between the two agents, but their combined use should be monitored due to potential additive side effects such as sedation or CNS effects[1][2].

02

Targets

HTR2A (Serotonin receptor 5-HT2A)M1 (Muscarinic acetylcholine receptor M1)HTR2C (5-hydroxytryptamine 2C receptor)HRH1 (Histamine H1 Receptor)DAT (Dopamine plasma membrane transport protein)HTR2B (5-Hydroxytryptamine Receptor 2B)NET (Norepinephrine Transporter)

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