Cyclobenz - General Information:Cyclobenz is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenz acts on the locus coeruleus where it results in increased norepinephrine release, potentially through the gamma fibers which innervate and inhibit the alpha motor neurons in the ventral horn of the spinal cord. It is structurally similar to Amitriptyline, differing by only one double bond.
Pharmacology:Cyclobenz, closely related to the antidepressant amitriptyline, is used as a skeletal muscle relaxant to reduce pain and tenderness and improve mobility. Unlike dantrolene, cyclobenzaprine cannot be used to treat muscle spasm secondary to cerebral or spinal cord disease.
Cyclobenz for patients
FLEXERIL, especially when used with alcohol or other CNS depressants, may impair mental and/or physical abilities required for performance of hazardous tasks, such as operating machinery or driving a motor vehicle. In the elderly, the frequency and severity of adverse events associated with the use of cyclobenzaprine, with or without concomitant medications, is increased. In elderly patients, FLEXERIL should be initiated with a 5 mg dose and titrated slowly upward.
FLEXERIL may have life-threatening interactions with MAO inhibitors.
FLEXERIL may enhance the effects of alcohol, barbiturates, and other CNS depressants.
Tricyclic antidepressants may block the antihypertensive action of guanethidine and similarly acting compounds.
Tricyclic antidepressants may enhance the seizure risk in patients taking tramadol.
Hypersensitivity to any component of this product.
Concomitant use of monoamine oxidase (MAO) inhibitors or within 14 days after their discontinuation. Hyperpyretic crisis seizures, and deaths have occurred in patients receiving cyclobenzaprine (or structurally similar tricyclic antidepressants) concomitantly with MAO inhibitor drugs.
Acute recovery phase of myocardial infarction, and patients with arrhythmias, heart block or conduction disturbances, or congestive heart failure.
Additional information about CyclobenzCyclobenz Indication: For use as an adjunct to rest and physical therapy for relief of muscle spasm associated with acute, painful musculoskeletal conditions.
Mechanism Of Action: Like other tricyclic antidepressants, cyclobenzaprine exhibits anticholinergic activity, potentiation of norepinephrine, and antagonism of reserpine. Cyclobenz does not directly act on the neuromuscular junction or the muscle but relieves muscle spasms through a central action, possibly at the brain stem level. Cyclobenz binds to the serotonin receptor and is considered a 5-HT2 receptor antagonist that reduces muscle tone by decreasing the activity of descending serotonergic neurons.
Drug Interactions: Donepezil Possible antagonism of action
Galantamine Possible antagonism of action
Rasagiline Increased risk of toxicity with this association
Rivastigmine Possible antagonism of action
Food Interactions: Take with food to reduce irritation.
Generic Name: Cyclobenzaprine
Synonyms: Cyclobenzaprine HCL
Drug Category: Tranquilizing Agents; Muscle Relaxants; Antidepressive Agents, Tricyclic; Skeletal Muscle Relaxants
Drug Type: Small Molecule; Approved
Other Brand Names containing Cyclobenzaprine: Cyclobenz; Flexeril; Flexiban; Proeptatriene; Proheptatriene;
Absorption: Slowly but well absorbed after oral administration
Toxicity (Overdose): Oral mouse and rat LD50 are 338 mg/kg and 425 mg/kg respectively. Signs of overdose include agitation, coma, confusion, congestive heart failure, convulsions, dilated pupils, disturbed concentration, drowsiness, hallucinations, high or low temperature, increased heartbeats, irregular heart rhythms, muscle stiffness, overactive reflexes, severe low blood pressure, stupor, and vomiting.
Protein Binding: Very high (93%)
Biotransformation: Extensively metabolized (gastrointestinal and hepatic).
Half Life: 18 hours (range 8-37 hours)
Dosage Forms of Cyclobenz: Tablet Oral
Chemical IUPAC Name: 3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethyl-1-propanamine
Chemical Formula: C20H21N
Cyclobenzaprine on Wikipedia: http://en.wikipedia.org/wiki/Cyclobenzaprine
Organisms Affected: Humans and other mammals
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