See the DrugPatentWatch profile for tizanidine
Tizanidine is a muscle relaxant that works by acting on the central nervous system to reduce spasticity [1]. It is believed to exert its effects as an alpha-2 adrenergic agonist [2]. This means it stimulates alpha-2 adrenergic receptors in the brain and spinal cord [2].
How does tizanidine reduce muscle spasticity?
By stimulating alpha-2 adrenergic receptors, tizanidine inhibits the release of excitatory neurotransmitters from spinal interneurons [2]. This reduction in excitatory neurotransmission leads to decreased spasticity [2]. Essentially, it helps to calm down the overactive nerve signals that cause involuntary muscle contractions [2].
What conditions is tizanidine used for?
Tizanidine is primarily used to treat muscle spasticity associated with conditions such as multiple sclerosis, spinal cord injury, and stroke [1]. It is not typically used for muscle spasms caused by orthopedic injuries [1].
What are the common side effects of tizanidine?
Common side effects include drowsiness, dizziness, dry mouth, and fatigue [1]. Some patients may also experience weakness, hallucinations, or liver problems [1].
How is tizanidine metabolized and eliminated?
Tizanidine is extensively metabolized in the liver, primarily by the enzyme CYP1A2 [3]. Its elimination is mainly through the kidneys [3].
Can tizanidine interact with other medications?
Yes, tizanidine can interact with several other medications. Drugs that inhibit CYP1A2, such as fluvoxamine and ciprofloxacin, can significantly increase tizanidine levels in the body, potentially leading to exaggerated side effects [3]. Conversely, CYP1A2 inducers can decrease tizanidine levels [3].
What is the recommended dosage for tizanidine?
Dosage for tizanidine is typically individualized based on patient response and tolerability. It is usually started at a low dose and gradually increased [1].
Sources:
[1] https://www.ncbi.nlm.nih.gov/books/NBK459213/
[2] https://www.drugbank.ca/drugs/DB00544
[3] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3003415/