Muscle relaxants chlorzoxazone

A 73-year-old woman had rhabdomyolysis, cholestatic hepatitis, and mild renal insufficiency 14 days after she started to take the centrally acting muscle relaxant chlorzoxazone while also taking simvastatin (79). Withdrawal of the causal medication and conservative therapy with volume substitution and forced diuresis was followed by almost complete resolution of the symptoms. 

Some other interesting substituted benzoxazolones are also used as pharmaceuticals, for example the muscle relaxant Chlorzoxazone [Scheme 185] (Ref. 237). 

There are several chemically unrelated skeletal muscle relaxants. Chlorzoxazone is an example of a drug that evolved from a discovery that certain benzimidazoles had mephen-esinlike activity. Chlorzaxazone, the benzoxazole isostere, appears to have the same spectrum of activity and mechanism(s) as the polyol carbamates. 

K(+) channels by the muscle relaxant chlorzoxazone and structurally related compounds. J Pharmacol Exp Ther 296(3) 683-689,2001. 

Anticonvulsants Mephenytoin (Wang et al. 2004b) Skeletal muscle relaxants Chlorzoxazone (Gurley et al. 2002,2005)... 

As pointed out earlier, the most generally accepted noninvasive human assay involves 6-hydroxy lation of the muscle relaxant chlorzoxazone [1016, 1027]. Studies with humans show little effect of diabetes [1016, 1071] but an effect of body weight/obesity [1071, 1072]. As mentioned before, genotype has shown little impact on the in vivo parameters to date [69,1072]. 

The mode of action of many skeletal muscle relaxants, for example carisoprodol (Soma), baclofen (Lioresal), and chlorzoxazone (Paraflex), is not clearly understood. Many of tiiese dragp do not directly relax skeletal muscles, but dieir ability to relieve acute painful musculoskeletal conditions may be due to their sedative action. Cyclobenzaprine (Flexeril) appears to have an effect on muscle tone, tiius reducing muscle spasm. 

Skeletal Muscle Relaxant Combinations Carisoprodol Compound—carisoprodol, aspirin Mexaphen—chlorzoxazone, acetaminophen Lobac—salicylamide, phenyltoloxamine, acetaminophen Norgesic Fbrte—orphenadrine citrate, aspirin, caffeine Norgesic—orphenadrine citrate, aspirin, caffeine Robaxisal—methocarbamol, aspirin Sodol Compound—carisoprodol, aspirin Soma Compound—carisoprodol, aspirin... 

Centrally acting muscle relaxants are also widely used (baclofen, cyclobenzaprin, carisoprodol, methocarbamol, chlorphenesin, chlorzoxazone, orphenadrine, and... 

Geriatric Considerations - Summary Chlorzoxazone is a centrally acting skeletal muscle relaxant that at higher doses can cause CNS depression. It appears to have modest clinical benefits and is most often used for acute muscle discomfort as compared to chronic muscle pain. It is often taken in combination with acetaminophen. Transient CNS depressant effects place the older adult at risk for falls and related accidents when taking this drug. 

Muscle relaxants and antispasmodics methocarbamol (Robaxin), carisoprodol (Soma), chlorzoxazone (Paraflex), metaxalone (Skelaxin), cyclobenzaprine (Flexeril), and oxybutynin (Ditropan) Do not consider the extended-release Ditropan XL Most muscle relaxants and antispasmodic drugs are poorly tolerated by elderly patients, because these cause anticholinergic adverse effects, sedation, and weakness. Additionally, their effectiveness at doses tolerated by elderly patients is questionable. High... 

II. Centrally acting muscle relaxants Mephenesin Chlorzoxazone (MOBIZOX) 250 mg TDS... 

There is a very great demand for drugs for the relief of anxiety. This was formerly met by the use of alcohol, bromides or barbiturates, which carried the risk of abuse or dangerous toxicity. The first of the modern minor tranquilizers, introduced from 1946 onwards, were drugs described as skeletal muscle relaxants. These were mainly derivatives of polyhydric alcohols, but heterocyclic examples included metaxolone (161), which is related to the aryl ethers of glycerol, chlorzoxazone (162) and chlormezanone (163). Dantrolene sodium (164) is a muscle relaxant and CNS depressant. 

Chlorzoxazone (Paraflex, Parafon Forte DSC, Others) [Skeletal Muscle Relaxant/ANS Drug] Uses Adjunct to rest physical therapy to relieve discomfort associated w/ acute, painful musculoskeletal conditions Action Centrally acting skeletal muscle relaxant Dose Adults. 250-500 mg PO tid-qid Peds. 20 mg/kg/d in 3-4 + doses Caution [C, ] Avoid EtOH CNS depressants Contra Severe liver Dz Disp Tabs SE Drowsiness, tach, dizziness, hepatotox, angioedema Interactions T Effects W/ antihistamines, CNS depressants, MAOIs, TCAs, opiates, EtOH, watercress EMS Use of CNS depressants and concurrent EtOH use can T sedation urine may turn reddish purple or orange OD May cause N/V/D, dizziness, HA, X deep tendon reflexes, hypotension and resp depression symptomatic and supportive, activated charcoal may be effective... 

Chlorzoxazone is a centrally acting benzoxazole derivative with a weak muscle relaxing effect (1). It is usually used in combination with paracetamol for the treatment of painful muscle spasms. The usual dose is 500 mg tds. Drowsiness, weakness, dizziness, and gastrointestinal complaints are the most frequent unwanted effects. 

Chlorzoxazone is used as a centrally acting skeletal muscle relaxant and as an analgesic. It is also a strong oxidizing agent. 

Acsal.Par,Ph.mepro- Separation muscle-relaxant-bamate,methocarbamol,-analgesic mixtures carisoprodol. chlorzoxazone... 

Chlorzoxazone, a benzoxazole derivative with skeletal muscle relaxant properties (250 to 750 mg p.o. t.i.d.), is used as an adjunct medication in the treatment of acute and painful musculoskeletal conditions. 

The oxidation of 4-nitrophenol to 4-nitrocate-chol has been used as an in vitro marker of human P450 2E1 (ref [633]). Chlorzoxazone 6-hydroxyla-tion was demonstrated to be a relatively specific reaction catalyzed by human P450 2E1 other enzymes (e.g., P450 1 Al) can catalyze the reaction but with poor catalytic efficiency - Chlorzoxazone is a relatively iimocuous muscle relaxant and the assay can be used in vivo to estimate hepatic P450 2E1 function noninvasively ... 

Two structural analogues of benzoxazole have gained prominence as potent muscle relaxants. Examples Chlorzoxazone Zoxazolamine. 

Chlorzoxazone (Parafon Forte), a muscle relaxant, to a client on bed rest. 

The client with low back pain syndrome is prescribed chlorzoxazone (Parafon Forte), a skeletal muscle relaxant. Which statement by the client would warrant intervention by the nurse ... 

Chlorzoxazone [95-25-0], muscle relaxant, 63. The 5-chloro-2(3H)-benzoxazolone 63 is prepared with phosgene [49]. 

Jiao and co-workers reported in 2014 a simple and practical catalytic methodology for the direct formation and application of isocyanates for the synthesis of carbamates [48]. This chemistry provides an efficient and practical approach to synthesize carbamates from simple organic azides, CO atmosphere and alcohols. The broad scope, mild and neutral conditions, and only N2 as the byproduct make this transformation very useful. Moreover, simple examples of modilication of bioactive molecules and constmction of macrocycles were achieved through this protocol. By utilizing this protocol, the marketed dmgs Chlorzoxazone (a centrally acting muscle relaxant) and Chlorpropham (an important herbicide and sprout suppressant) were easily prepared from simple and readily available aromatic azides, CO, and alcohols in high yields (Scheme 5.17). The mechanism is proposed... 

---