Drug Metab Dispos. 1978 Mar-Apr;6(2):184-92.
Metabolism of cyclobenzaprine in the dog.

Hucker HB, Balletto AJ, Arison BH, Zacchei AG.

Ten metabolites of cyclobenzaprine, accounting for approximately 50% of the urinary radioactivity, were identified in the urine of dogs to which the labeled drug had been given orally. These included the 1,2-dihydrodiol, three phenolic derivatives, the N-oxide, the 10,11-epoxide, the 10,11-glycol, desmethylcyclobenzaprine, and the glucuronide conjugates of desmethylcyclobenzaprine and cyclobenzaprine. The metabolites were excreted in both the free and conjugated states. Unchanged cyclobenzaprine was present in only minor amounts.

Online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=26535&dopt=Abstract cyclobenzaprine Flexeril





Drug Metab Dispos. 1978 Nov-Dec;6(6):659-72.
Physiological disposition and metabolism of cyclobenzaprine in the rat, dog, rhesus monkey, and man.

Hucker HB, Stauffer SC, Balletto AJ, White SD, Zacchei AG, Arison BH.

The absorption, distribution, excretion, and metabolism of 3-(5 H-dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethyl-1-propanamine (cyclobenzaprine) were investigated in the rat, dog, rhesus monkey, and man. The drug was well absorbed in all species after oral administration. The rat eliminated the drug primarily in the feces, but urinary excretion was predominant in the dog, monkey, and man. The drug was rapidly and widely distributed into rat tissues, highest concentrations being found in the small intestine, lung, kidney, and liver. The drug was highly bound in human plasma. Extensive biliary excretion of the labeled compound was observed in the rat. Major metabolites in the rat were phenolic derivatives but in man the major metabolites were 10,11-dihydroxynortriptyline and cyclobenzaprine glucuronide. Only minor amounts of unchanged drug were present in the urine.

Online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=33029&dopt=Abstract cyclobenzaprine Flexeril





Am J Med. 1986 Sep 29;81(3A):63-6.
Pharmacotherapeutics in fibrositis.

Gatter RA.

Fibrositis (fibromyalgia) is best treated by attaining patient acceptance of and compliance with a comprehensive treatment program. This includes education, physical therapy, muscle and mental relaxation, examination and adjustment of goals and priorities, and pacing of activities, as well as pharmacotherapeutics. Of the medications in use, anti-inflammatory agents with a high degree of analgesia are more effective than "pure" anti-inflammatory agents. Tricyclic derivatives are beneficial muscle relaxants. The use of long-acting agents improves compliance and is therefore favored. Local agents are of adjunctive value in some cases. Double-blind, placebo-controlled studies show cyclobenzaprine to be an effective medication in the treatment of fibrositis (fibromyalgia).

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Am J Med. 1986 Sep 29;81(3A):7-14.
The clinical syndrome of fibrositis.

Wolfe F.

Fibrositis is a disorder of musculoskeletal pain and aching with at least a five to one female-to-male ratio. It is most commonly seen between the ages of 40 and 60, and has a prevalence in the clinic of 6 to 15 percent. Its most common mode of presentation involves generalized musculoskeletal pain and aching, but articular pain, axial skeletal pain, myalgias, and neurovascular complaints sometimes predominate. All patients have multiple areas of local tenderness called "tender points" that are easily identified during physical examination, and are diagnostic. Essential symptoms of fibrositis are disturbed sleep, morning stiffness, and fatigue. Additional rheumatic symptoms include subjective swelling, paresthesias, and numbness. Headaches and irritable bowel syndrome are common nonrheumatic complaints. Modest improvement follows treatment by tricyclic agents such as low-dose cyclobenzaprine and amitriptyline, by physical measures, and by reduction in stress. Remission occurs in 20 percent of patients, but is generally short-lived.

Online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3464212&dopt=Abstract cyclobenzaprine Flexeril