![]() ![]() ![]() Cytochromes P-450 3A4, 1A2, and, to a lesser extent, 2D6, mediate N-demethylation, one of the oxidative pathways for cyclobenzaprine. (n=18), peak plasma concentration was 25.9 ng/mL (range, 12.8-46.1 ng/mL), and area under the concentration-time (AUC) curve over an 8-hour dosing interval was 177 ng.hr/mL (range, 80-319 ng.hr/mL).Ĭyclobenzaprine is extensively metabolized, and is excreted primarily as glucuronides via the kidney. At steady state in healthy subjects receiving 10 mg t.i.d. Drug accumulates when dosed three times a day, reaching steady-state within 3-4 days at plasma concentrations about four-fold higher than after a single dose. Cyclobenzaprine exhibits linear pharmacokinetics over the dose range 2.5 mg to 10 mg, and is subject to enterohepatic circulation. Cyclobenzaprine caused slight to moderate increase in heart rate in animals.Įstimates of mean oral bioavailability of cyclobenzaprine range from 33% to 55%. Pharmacological studies in animals showed a similarity between the effects of cyclobenzaprine and the structurally related tricyclic antidepressants, including reserpine antagonism, norepinephrine potentiation, potent peripheral and central anticholinergic effects, and sedation. Evidence suggests that the net effect of cyclobenzaprine is a reduction of tonic somatic motor activity, influencing both gamma (γ) and alpha (α) motor systems. Such studies show that cyclobenzaprine acts primarily within the central nervous system at brain stem as opposed to spinal cord levels, although its action on the latter may contribute to its overall skeletal muscle relaxant activity. Animal studies indicate that cyclobenzaprine does not act at the neuromuscular junction or directly on skeletal muscle. ![]() It is ineffective in muscle spasm due to central nervous system disease.Ĭyclobenzaprine reduced or abolished skeletal muscle hyperactivity in several animal models. Dorixina Relax (Cyclobenzaprine Hydrochloride) contains the following inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, dibasic calcium phosphate, hydroxypropyl cellulose, hypromellose, polyethylene glycol, magnesium stearate, microcrystalline cellulose, and titanium dioxide.ĭorixina Relax relieves skeletal muscle spasm of local origin without interfering with muscle function. Cyclobenzaprine HCl is designated chemically as 3-(5 H-dibenzocyclohepten-5-ylidene)- N,N-dimethyl-1-propanamine hydrochloride, and has the following structural formula:ĭorixina Relax (Cyclobenzaprine Hydrochloride) is available for oral administration as 7.5 mg tablets. If aqueous solutions are made alkaline, the free base separates. It is freely soluble in water and alcohol, sparingly soluble in isopropanol, and insoluble in hydrocarbon solvents. It has a melting point of 217☌, and a pK a of 8.47 at 25☌. Further informationĪlways consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.Dorixina Relax (Cyclobenzaprine Hydrochloride) ® (cyclobenzaprine hydrochloride) is a white, crystalline tricyclic amine salt. Consult with your healthcare professional before taking any medication. It should not be construed to indicate that the use of any medication in any country is safe, appropriate or effective for you. It is not intended as a substitute for the expertise and judgement of your physician, pharmacist or other healthcare professional. This means it is still under development and may contain inaccuracies. Important Notice: The international database is in BETA release. Ingredient matches for Dorixina Relax ClonixinĬlonixin lysine (a derivative of Clonixin) is reported as an ingredient of Dorixina Relax in the following countries:Ĭyclobenzaprine is reported as an ingredient of Dorixina Relax in the following countries:Ĭyclobenzaprine hydrochloride (a derivative of Cyclobenzaprine) is reported as an ingredient of Dorixina Relax in the following countries: Dorixina Relax may be available in the countries listed below. ![]()
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