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This article needs additional citations for verification. Please help improve this article by adding reliable references (ideally, using inline citations). Unsourced material may be challenged and removed. (July 2008)CyclobenzaprineSystematic (IUPAC) name3-(5H-dibenzocyclohepten-5-ylidene)- N,N-dimethyl-1-propanamineIdentifiersCAS number303-53-7ATC codeM03BX08PubChem2895DrugBankAPRD00213ChemSpider2792Chemical dataFormulaC20H21N Mol. mass275.387 g/molSMILESeMolecules & PubChemPharmacokinetic dataBioavailability32.5% to 55%MetabolismhepaticHalf life18 hours (range 8-37 hours; n=18)ExcretionrenalTherapeutic considerationsPregnancy cat.Category BLegal statusUnscheduledRoutesPO (Per Oral)Cyclobenzaprine is a tricyclic antidepressant compound that is used clinically as a long-acting skeletal muscle relaxant and analgesic. It is marketed as Flexeril (5 and 10 mg tablets), and also as Fexmid (7.5 mg tablet). Both Flexeril and Fexmid are available generically. Once-a-day extended release formulation, Amrix, has been approved by the United States FDA in 2007 and is available in 15 and 30 mg capsules.// Mechanism of actionCyclobenzaprine is structurally related to the first-generation tricyclic antidepressants such as imipramine and amitriptyline. Cyclobenzaprine has major contraindications with monoamine oxidase inhibitors (MAOIs). At least one study also found increased risk of hyperserotonemia, or serotonin syndrome, when cyclobenzaprine was taken with duloxetine, an SSNRI.The exact mechanism of action for cyclobenzaprine is unknown. Current research appears to indicate that cyclobenzaprine has effects on the locus coeruleus, where it acts--like many tricyclic antidepressants--to inhibit the uptake of norepinephrine, resulting in increased transynaptic norepinephrine concentration. Tricyclic compounds with norepinephrine reuptake-inhibiting properties (e.g. amitriptyline) have been shown to exert analgesic effects in chronic nerve and muscle pain. Cyclobenzaprine also causes inhibition of descending serotonergic systems in the spinal cord by blocking 5-HT2A and 5-HT2C receptors. This action is thought to have an inhibitory effect on the alpha motor neurons in the ventral horn of the spinal cord, thereby resulting in decreased firing of alpha-motor neurons and a reduction in spinal mono- and polysynaptic reflexes. IndicationsCyclobenzaprine is typically prescribed to relieve pain and muscle spasms. Typically, muscle spasms occur in an injury to stabilize the affected body part and prevent further damage. The spasm of the muscles can increase the pain level. It is believed that by decreasing muscular spasm, pain is diminished. A common application would be that of a whiplash injury in a car accident. Muscle relaxants such as Cyclobenzaprine (Flexeril) and Orphenadrine Citrate (Norflex) have also been studied in the treatment of fibromyalgia. In a study of 120 fibromyalgia patients, those receiving Cyclobenzaprine (10 to 40 mg) over a 12 week period had significantly improved quality of sleep and pain score. There was also a reduction in the total number of tender points and muscle tightness.Like other tricyclic antidepressants, it is also prescribed off-label as a sleep-aid. The sedative effects of cyclobenzaprine are likely due to its antagonistic effect on histamine H1, serotonin 5-HT2A and muscarinic acetylcholine receptors.To avoid possible stomach upset, it should be taken with food and a full glass of water. Side effectsCommon side effects include drowsiness, depression, headaches, severe dizziness, and blurred vision. Other side effects are respiratory depression and decreased functionality in various muscles. Long term use has been associated with vision damage. Another side effect is dryness of the mouth. Agitation is a common side effect observed especially in the elderly. InteractionsDue to potential interactions, it is important to discuss the use of any of the following before taking them while using cyclobenzaprine:AlcoholCentral nervous system (CNS) depressants (medicines that cause drowsiness) orTricyclic antidepressants (amitriptyline , amoxapine , clomipramine , desipramine , doxepin , imipramine , nortriptyline , protriptyline , trimipramine ) The chance of side effects may be increasedMonoamine oxidase (MAO) inhibitors (furazolidone , phenelzine , procarbazine , selegiline , tranylcypromine ) Taking cyclobenzaprine while taking or within 2 weeks of taking MAO inhibitors may result in serious, life-threatening side effects. LegalityThis section does not cite any references or sources. Please help improve this article by adding citations to reliable sources. Unverifiable material may be challenged and removed. (November 2008)Cyclobenzaprine is regulated in the U.S. for prescription use only. Cyclobenzaprine does not fall within most governmental guidelines as a controlled substance, however possession without a valid / current prescription may be illegal depending upon various state and local laws. AbuseWhen used for illicit purposes, the drug is often referred to as "cyclone" or "mellow yellow". Users report mild to moderate drowsiness and relaxation as the primary effects. Compared with other commonly abused CNS depressants, cyclobenzaprine's effects are considered to be mild, limiting its popularity as a recreational drug.More commonly, cyclobenzaprine is used as a potentiator of opioids, the weak and intermediate strength painkillers such as codeine, dihydrocodeine, and hydrocodone. In this respect it is similar to the first-generation antihistamines. However, Cyclobenzaprine can induce moderate to severe anticholinergic effects at higher doses. At even higher doses, cyclobenzaprine may cause severe ataxia. OverdoseAlthough reportedly unpleasant, cyclobenzaprine is relatively benign in case of overdose. However, depending on the amount taken and on the many different factors unique each individual, harmful overdose effects can occur. Note that the susceptibility to these potentially damaging effects is greatly increased when cyclobenzaprine is used in conjunction with other drugs, particularly central nervous system depressants and antidepressants. Use of cyclobenzaprine with an MAOI (monoamine oxidase inhibitor) can possibly result in fatality. A case of rhabdomyolysis (muscle breakdown) associated with its overdose has been reported in the scientific literature. This is a rare though potentially fatal complication. Treatment protocols and support should follow the same as for any tricyclic antidepressant.
Buy From a wide range of Muscle Relaxants and Pain Medicines such as Tramadol, Zanaflex, Carisoprodol, Fioricet, Cyclobenzaprine, Flexeril, Flextra DS, Skelaxin, Ultracet, Ultram, Motrin and MANY MANY More! See MedicineRx.Soma is a muscle relaxant used to relieve the pain and stiffness of muscle spasms and discomfort due to strain and sprain.Net
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flexeril
Learn about the prescription medication Flexeril (Cyclobenzaprine Hcl), drug uses, dosage, side effects, drug interactions, warnings, and patient labeling.
Flexeril (Cyclobenzaprine Hcl) Drug Information: Uses, Side Effects ...
Learn about Flexeril from the publishers of the Physicians Desk Reference. Find prescription drug information resources including interactions, side effects, symptoms, treatment ...
Flexeril | Prescription Drug Information, Side Effects | PDRHealth
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