Cyclobenzaprine is useable in pharmaceutics as brand name Amrix , Fexmid and Flexeril . Cyclobenzaprine is prescribed by physician and not available on ledge of any chemist’s shop in USA . Flexeril is classified asmuscle relaxantsand does not fall into controlled substance .
Chemical Structure of Cyclobenzaprine
Cyclobenzaprine , N - dimethyl-3-(dibenzo - cyclohepten-5 - ylidene ) propylamine . Flexeril is synthesized by reacting 5H - dibenzo cyclohepten-5 - one with 3 - dimethylaminopropylmagnesium chloride and subsequently dehydrated to carbinol . chemical substance social organization is similar to tricyclicantidepressants .
How Does Cyclobenzaprine Work?
Cyclobenzaprine is wide used as brawn relaxant . Animal model has shown Flexeril does not act at neuromuscular articulation or muscle actin - myosin coordination compound . Multiple fauna inquiry studies areindicating Flexeril block reuptake of norepinephrine at locus ceruleus , mid brain and spinal cord . alike animal inquiry has also depict Flexeril deflect 5 HT receptor of serotonergic system of rules . 5-hydroxytryptamine sense organ also known as 5 HT sensory receptor are find in primal and peripheral nervous system . Cyclobenzaprine increases synaptic concentration of norepinephrine molecule within serotonergic organisation in brainiac and adaxial car horn of spinal cord . Increase norepinephrine at level of spinal electric cord inhibits alpha motor neuron activity . Serotonergic system modulates anxiety and mood disorder . forbiddance of 5 HT sense organ stimulate blocking of descending serotonergic organisation . Modulation and suppression of intellectual and spinal neurons finally subdue spinal reflexes induce brawniness compression . Comparableoutcomes were follow in creature enquiry with tricyclic antidepressants .
Flexeril reduces peripheralmuscle spasmby inhibiting cardinal intonation activity . Cyclobenzaprine is ineffective if spasm is subaltern peripheral skeletal triggering disease causing muscle muscular contraction .
dose – Cyclobenzaprine is marketed as-
Ten mg tablet is usually take two to four times a day . The extended release capsule is usually taken one or two prison term a solar day . Cyclobenzaprine is often not prescribed beyond 3 weeks without talking to your medico .
Absorption - Cyclobenzaprine is absorbed by enteral mucosal tissue layer . Estimated mingy unwritten bioavailability of cyclobenzaprine range from 33 % to 55 % .
Distribution - Cyclobenzaprine exhibits analog pharmacokinetics over the dose range 2.5 mg to 10 atomic number 12 . Level of plasm depends on liver andkidney function . spare drugs available to act on receptors depend on protein bind . Cyclobenzaprine is highly protein bound and has low bioavailability . Cyclobenzaprine reach alterative blood plasma steady United States Department of State level within 3 - 4 days .
Metabolism - Cytochrome enzymes and oxidation metabolize cyclobenzaprine by demethylation of active atom . Mode of metabolic process is slow result in half - lifespan of 18 hours .
evacuation - Cyclobenzaprine is excreted by kidney as glucuronides . elimination calculate on years and kidney function . Plasma headway is 0.7 L / min . Concentration of cyclobenzaprine is higher in aged and patient with borderline kidney single-valued function . Flexeril is eliminate quite easy , with an effective half - life of 18 hours ( image 8 - 37 hours ) ; plasma headroom is 0.7 L / min . The plasma concentration of cyclobenzaprine is generally higher in the senior and in patient with hepatic impairment .
Indications For Use
guard : Cyclobenzaprine can get knockout life threatening ramification if used in surveil diseases and in combination with following medications .
Diseases
Drug Interaction
Hypersensitivity (Anaphylaxis)
Anaphylaxis and terrible allergic reaction is very rare , but probable complication with cyclobenzaprine .
Symptoms of Anaphylaxis
Symptoms Of Drug Allergies Other Than Hypersensitivity
Pregnancy - Animal studies have failed to bring out evidence of teratogenicity . There are no hold data point in human pregnancy . Patient taking cyclobenzaprine prior to pregnancy and want to proceed during gestation must consult accoucheur and neonatologist . There is no contraindication for Flexeril discussion during pregnancy . Results of animate being research laboratory studies propose high dosage of Flexeril in mouse has not depict any impaired birth rate or fetal abnormalities . There is no control human written report or showcase write up release regarding complication due to Flexeril treatment in pregnancy .
knocker - feeding - Cyclobenzaprine is not excreted in human milk . There is no data of human inquiry or any case report published in diary , indicating Flexeril pass in in white meat Milk River had get side burden in babe following breast eating .
Nursing Mothers - It is not bang whether this drug is excrete in human milk . Metabolites of Flexeril are not take in nursing female parent . If female parent has to feed child while read cyclobenzaprine then confer with neonatologist or paediatrician .
Pediatric Use - Safety and effectuality of cyclobenzaprine in paediatric patient below 15 class of age have not been establish .
Use in the Elderly - Plasma concentration of Flexeril was high in elderly patients when compared with untried patient role after same dosage in mg . Elderly patients is normally treat with 5 milligram of Flexeril . Elderly patient are at endangerment for side effects like hallucination , drowsiness , confusedness and cardiac side core .
Storage - Store at 25 Degree C ( 77 Degree F ) ; excursion permit to 15 - 30 Degree C ( 59 - 86 Degree F ) . [ See USP Controlled Room Temperature ] .
Side Effects of Cyclobenzaprine
General Side Effects:
Eyes:
Cardiovascular Side Effects:
Central Nervous System:
Digestive Side Effects:
Respiratory Side Effects:
Urogenital Side Effects:
Hematic and Lymphatic Side Effects:
Musculoskeletal Side Effects:
Special Senses:
Endocrine Side Effects:
Metabolic Side Effects:
Skin:
Psychiatric Side Effects:
Missed Dose:
Cyclobenzaprine has tenacious half - life and backdown symptoms are not see for 8 to 12 hours . If dose is miss then skip the dose and take the next dose at appropriate time . Do not take double Lucy in the sky with diamonds to make up for the missed one .
Drug Abuse:
Cyclobenzaprine Overdose Symptoms
striking US National Poison Hotline at ( USA ) 1 - 800 - 222 - 1222 and ( Health Canada ) 1 - 866 - 234 - 2345 .
Dependence:
In few instance patient may be subject on Flexeril because of favorable core of muscle relaxation and sedation . Patient may take few extra pills and may suffer with symptom of overdose . Few patients may take few extra pill and guide short of medications . Withdrawal symptoms will be seen if patient could not take pill for few days .
