Drug intelligence / Profile preview

methadone + tizanidine

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Subcutaneous
01

Overview

Methadone + tizanidine is a combination of two pharmaceutical drugs, methadone and tizanidine. Methadone is a synthetic opioid agonist primarily used for pain management and as part of medication-assisted treatment (MAT) for opioid dependence. It acts mainly as a full agonist at the mu-type opioid receptor, producing analgesia, sedation, and suppression of withdrawal symptoms[4]. Tizanidine is an alpha-2 adrenergic receptor agonist used as a muscle relaxant to manage spasticity associated with conditions such as multiple sclerosis or spinal cord injury[6]. The combination of these two drugs can result in additive central nervous system (CNS) depression, leading to increased risk of drowsiness, dizziness, impaired judgment and psychomotor skills; in severe cases it may cause hypotension or respiratory depression[1][2][3]. This combination should generally be avoided unless specifically indicated under close medical supervision due to the risk profile.

02

Targets

MOR (Mu opioid receptor)ADRA2A (α2A)

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