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Drugs Affecting the Central Nervous System
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: It should be used with caution because the pregnancy experience in humans is limited, and the reproduction studies in animals have shown a risk of increased prenatal and postnatal pup mortality associated with the use of Tizanidine.
Pain and Its Management in Older Adults
Published in K. Rao Poduri, Geriatric Rehabilitation, 2017
Annie Philip, Diya Goorah, Rajbala Thakur
Muscle relaxants. This class of medications should be used in select individuals with extreme caution. Common medications used in this class are baclofen, tizanidine, and cyclobenzaprine (flexeril). Baclofen is a Gaba-b agonist with a starting dose of 5 mg three times per day. Older adults may be unable to tolerate more than 30–40 mg per day. Tizanidine should be started at a dose of 2 mg three times per day. Tizanidine is a centrally acting alpha2 adrenergic agonist and is used in the treatment of spasticity in spinal cord injury and multiple sclerosis. Older adults may be unable to tolerate more than 16 mg per day. Flexeril should be used very cautiously and started at low doses of 5 mg three times per day, with a maximum daily dose of 30 mg per day. The mechanism of action is not well understood but its effect could be due to inhibition of interneuronal activity in the descending reticular formation. General adverse effects associated with this class of medications are somnolence, cognitive effects, and orthostasis. Patients need close monitoring of liver functions when on tizanidine. Flexeril should not be used in patients with close angle glaucoma.
Oral Medication
Published in Valerie L. Stevenson, Louise Jarrett, Spasticity Management, 2016
Most of the reported studies have involved people with MS: these trials have been extensively reviewed.2,23,24 In comparison with placebo, tiza-nidine has been shown to reduce muscle tone, frequency of spasms and clonus; no functional benefit has, however, been demonstrated. In comparison studies with diazepam, baclofen and tet-razepam, all four drugs appear to be of equal efficacy, although tizanidine had fewer side effects than diazepam, but was comparable to baclofen. In a study of 124 patients with spinal cord injury, tizanidine was found to significantly reduce spasticity and spasms compared with placebo, but no changes in functional assessment were seen.36 Two studies in stroke revealed a reduction in tone and spasms compared with placebo37 and equal efficacy to baclofen.22 Tizanidine has also been shown to be clinically effective in the management of pain syndromes, such as myofascial pain, lower back pain and trigeminal neuralgia.38
Impact of chronic medications in the perioperative period: mechanisms of action and adverse drug effects (Part I)
Published in Postgraduate Medicine, 2021
Ofelia Loani Elvir-Lazo, Paul F White, Hillenn Cruz Eng, Firuz Yumul, Raissa Chua, Roya Yumul
Alpha2 agonists act predominantly on central α2-receptors. Their activation leads to inhibition of norepinephrine release from presynaptic neurons, sedation via stimulation of receptors in the locus coeruleus, and modification of centrally mediated pain via dorsal horn stimulation [11]. Clonidine is a mixed alpha2 agonist-antagonist used orally to treat hypertension, anxiety, attention deficit hyperactivity disorder (ADHD), chronic pain, postoperative shivering, and opioid withdrawal symptoms. Clonidines are metabolized mainly through CYP2D6 and to a lesser extent by CYP3A4/5 and CYP1A1/2. Tizanidine, another mixed α2 agonist/antagonist, is used to treat muscle spasms and cramps associated with a wide variety of CNS disorders. The primary cytochrome P450 isoenzyme involved in tizanidine metabolism is CYP1A2. Dexmedetomidine, a pure α2 agonist, is used for sedation and analgesia in the operating room (OR) and postanesthesia care unit (PACU) and in the intensive care unit (ICU) [11]. Dexmedetomidine is metabolized by cytochrome P450 (CYP2A6) and uridine diphosphate glucuronosyltransferase (UGTs), UGT1A4, and UGT2B10, to inactive metabolites.
Electroacupuncture with rehabilitation training for limb spasticity reduction in post-stroke patients: A systematic review and meta-analysis
Published in Topics in Stroke Rehabilitation, 2021
Jiyao Zhang, Luwen Zhu, Qiang Tang
Currently, the treatment of spasticity after stroke mainly includes both drug and non-drug treatments, such as anti-spasticity drugs, physical therapy, surgery, and acupuncture,8 which relieve increased muscle tension to some extent. However, oral anti-spasticity drugs, including tizanidine hydrochloride and baclofen, are associated with adverse reactions, such as drowsiness, dizziness, fatigue, and dry mouth, and are not helpful for the improvement of limb function. Intramuscular administrations of anti-spasticity drugs, such as botulinum toxin type A, have a significant therapeutic effect; however, it is expensive.9–12 Although physical therapy relieves pain and joint contracture due to post-stroke spasticity and improves motor function, treatment compliance is poor because of the long course of treatment and slow effect.13 Furthermore, surgical treatment is often difficult for patients and their families to accept because of its complexity and high risk.14 Thus, a better treatment for post-stroke spasticity is still needed.
Smoothened receptor inhibitor vismodegib for the treatment of basal cell carcinoma: a retrospective analysis of efficacy and side effects
Published in Journal of Dermatological Treatment, 2020
András Bánvölgyi, Pálma Anker, Kende Lőrincz, Norbert Kiss, Dalma Márton, Luca Fésűs, Nóra Gyöngyösi, Norbert Wikonkál
A 51-year-old female patient was referred to our department, who fulfilled the clinical criteria for NBCCS. BCC had been appearing from the age of 17, and the patient also presented palmar pitting, bone abnormalities and calcification of the flax cerebri. Previously, the patient received surgical treatment, radiotherapy and cryotherapy. Due to the extent of the disease, surgical and radiological treatment would not have been a definitive treatment option. Vismodegib therapy resulted in complete remission after 1 year; however, the patient developed severe muscle spasms and generalized alopecia throughout the treatment. The combination of tizanidine and amlodipine achieved slight reduction of muscle spasms. The treatment was administered for 4 years, then it was suspended due to intolerable muscle spasms, muscle weakness and dysgeusia. Three months after the therapy was stopped, BCCs reappeared (Figure 4), and the patient is now going to be operated.