Cyclobenzaprine: a possible mechanism of action for its muscle relaxant effect. Monitoring of plasma drug levels should not guide management of the patient. COVID-19 is an emerging, rapidly evolving situation. 0000020932 00000 n They are supplied as follows:Store at 20°C to 25°C (68°F to 77°F); excursions permitted from 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. Intravenously administered cyclobenzaprine (CBZ) (Flexeril), a clinically used, centrally acting muscle relaxant, abolished muscle rigidity in the intercollicular decerebrate rat. 12.1 Mechanism of Action. This should include large volume gastric lavage followed by activated charcoal. cyclobenzaprine hydrochloride extended-release capsulescyclobenzaprine hydrochloride extended-release capsulesThis Instructions for Use has been approved by the U.S. Food and Drug Administration. Cyclobenzaprine relieves skeletal muscle spasm of local origin without interfering with muscle function. Proper Use. 0000022663 00000 n Safety and effectiveness of cyclobenzaprine hydrochloride extended-release capsules has not been studied in pediatric patients.Clinical studies of cyclobenzaprine hydrochloride did not include sufficient numbers of patients aged 65 and over to determine the safety and efficacy of cyclobenzaprine hydrochloride extended-release capsules in the elderly population.
Clinical studies have given supportive, albeit not conclusive, evidence for treatment roles in the short-term management of acute neck and back pain, and fibromyalgia. %PDF-1.3 %���� 0000000016 00000 n
All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.
In animal models, cyclobenzaprine reduced or abolished skeletal muscle hyperactivity. Some patients may require up to 30 mg/day, given as one (1) cyclobenzaprine hydrochloride extended-release capsule 30 mg taken once daily or as two (2) cyclobenzaprine hydrochloride extended-release capsules 15 mg taken once daily.Instruct patients to swallow cyclobenzaprine hydrochloride extended-release capsules intact. If signs of toxicity occur at any time during this period, extended monitoring is required. 0000024091 00000 n It is ineffective in muscle spasm due to central nervous system disease.
Cytochromes P-450 3A4, 1A2, and, to a lesser extent, 2D6, mediate N-demethylation, one of the oxidative pathways for cyclobenzaprine.
0000025375 00000 n doi: 10.1107/S1600536811024676. 0000030127 00000 n
Pharmacological studies in animals demonstrated 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. eep cyclobenzaprine hydrochloride extended-release capsules and all medicines out of the reach of children.General information about the safe and effective use of cyclobenzaprine hydrochloride extended-release capsules.
In rats, decreased pup body weight and survival was noted at cyclobenzaprine doses ≥10 mg/kg/day (approximately ≥3 times the maximum recommended human dose (MRHD) of 30 mg/day), when administered orally during pregnancy and lactation The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. 60505-3972-6,
cyclobenzaprine hydrochloride extended-release capsules Throw away any unused cyclobenzaprine hydrochloride extended-release capsule content and applesauce mixture. The mechanism of action of cyclobenzaprine may be to increase brainstem-mediated noradrenergic inhibition of spinal cord neurons. 0000062374 00000 n Other foods have not been tested and should not be substituted for applesauce.
Cyclobenzaprine has an elimination half-life of 32 hours (range 8-37 hours; n=18); plasma clearance is 0.7 L/min following single-dose administration of cyclobenzaprine hydrochloride extended-release capsules.In a pharmacokinetic study of immediate-release cyclobenzaprine in 16 subjects with hepatic impairment (15 mild, 1 moderate per Child-Pugh score), both AUC and CCyclobenzaprine HCl was not mutagenic or clastogenic in the following assays: an Cyclobenzaprine HCl, when administered 70 and 14 days prior to mating to male and female rats, respectively, had no effects on fertility or reproductive performance at oral doses up to 20 mg/kg/day (approximately 6.5 times the MRHD on a mg/mIn a 67-week study with rats that received cyclobenzaprine at oral doses of 10, 20, or 40 mg/kg/day (3 to 15 times the MRHD on mg/mIn a 26-week study with Cynomolgus monkeys that received cyclobenzaprine at oral of doses of 2.5, 5, 10, or 20 mg/kg/day, one monkey at 20 mg/kg/day (15 times the MRHD on mg/mEfficacy was assessed in two double-blind, parallel-group, active-controlled, placebo-controlled studies of identical design of cyclobenzaprine hydrochloride extended-release capsules 15 mg and 30 mg taken once daily, between 6:00 and 7:00 PM, cyclobenzaprine 10 mg three times a day, or placebo for 14 days in patients with muscle spasms associated with acute painful musculoskeletal conditions. In animals in which the locus coeruleus was lesioned bilaterally previously, CBZ failed to attenuate the electromyogram. Cyclobenzaprine has an oral bioavailability of about 55% and approximately 93% is bound to proteins in plasma. Further and more exacting science is warranted to explore the value of this drug in other neurological and psychiatric contexts.
The recommended adult dose for most patients is one (1) cyclobenzaprine hydrochloride extended-release capsule 15 mg taken once daily. 0000179247 00000 n