Cyclobenzaprine Use and Side Effect and Mechanism of Action

How Cyclobenzaprine is Works in the Treatment of

Spasm ?

Use of cyclobenzaprine

Cyclobenzaprine is mainly use for the treatment of acute muscle spasm in the old age group and condition like skeletal muscle pain . it affecting through some sign
and symptoms like pain ,tenderness, restriction in the activity , limitation in the motion .
Cyclobenzaprine is come to the market in the brand name known as flexeril.
Cyclobenzaprine capsule
Cyclobenzaprine capsule

This medicine are not taking for the long time period maximum two to three week because
skeletal muscle pain are come for the short time period .

Cyclobenzaprine is not use for the Spasticity (stiffness) or any type of nerve problem.
This medicine is block the nerve impulse which is send to the brain to feeling the pain like
other pain blocking medicine .

Side effect

All the medicine is having some common side effect as like other this medicine have some
side effect like
  • Nausea
  • Dry mouth
  • Dizziness
  • Fatigue
  • Constipation
  • Drowsiness
  • Fatigue
  • Blurred vision
When the medicine are showing serious side effect you must call the 1800-222-1222 for the
emergency in the US residency. If you are in the India you can call the medical emergency
number 112.
  • Showing serious heart problem
  • Fainting
  • Irregular heart beat
  • Confusion
  • Speaking problem
  • Understanding problem are also seen
  • Vision problem
  • Lose the control in face or hand

Mechanism of action

Cyclobenzaprine is also known as the named CBZ. This medicine is a centrally acting
muscle relaxant. This medicine clinical trial is doing on the animal like rat .

It is mainly activating the locus coeruleus , which is helps to synthesis of noradrenaline .
so the synthesis of noradrenaline is more and these noradrenaline is inhibit the motor
neurons to muscle relaxation. In the ventral horn cyclobenzaprine also increase the
metabolism of noradrenaline but it is very less amount.
Cyclobenzaprine structure
Cyclobenzaprine structure

It directly does not acting on the skeletal muscle or  in the neuronal junction to show their

Finally it reduce the tonic somatic motor activity (which helps to sending the signal to
various body part to reflex arch) by influencing the gamma and alpha motor system.


Oral bioavailability of cyclobenzaprine is 33% to 55%. It show the constant pharmacokinetics when dose is given to to the
patient 2.5 mg to 10 mg.

This medicine is reabsorbed from the blood in the live so it called enterohepatic circulation.
This medicine plasma protein binding capacity is high. It takes 3- 4 hours to get plasma
peak concentration. Metabolism of cyclobenzaprine is by the helps enzyme cytochrome
P450 3A4,1A2 and 2D6 and glucuronide conjugation in the kidney.Plasma concentration of cyclobenzaprine in the older age group like more
than 65 year is generally higher than the normal people.

Precaution and warning

Cyclobenzaprine is structurally and functionally related to tricyclic antidepressants like amitriptyline and
imipramine which is use for the treatment of acute skeletal muscle spasm if a patient is
taking this medicine slightly more than the normal dose of tricyclic antidepressant it shows
more serious central nervous system action like arrhythmias,sinus tachycardia ,more time
for conduction of myocardial infarction and stocks.this medicine is increase the action of
alcohol, barbiturates and other CNS depressant.

Interaction with other medicine

This medicine it interact with monoamine oxidase inhibitor very rapidly and it may block the
antihypertensive action of guanethidine and similarly acting compound and it also interact
with tramadol hydrochloride .

Dose of cyclobenzaprine

Doctor prescribe the dose to the patient 5 mg three time per day if the dose is not working
then you can increase the dose to 10 mg three time per day with consulting the doctor or
pharmacist. Don’t take this medicine continuously three to two weeks.
Those patients are suffer the hepatic impairment and old age group recommended for
lower dose as much as possible .

Brand and price of cyclobenzaprine

FLEXERIL Tablets are manufacturing by the company janssen pharmaceutical strength
of the tablets are 5 mg and 10 mg. 5 mg tablets retail price is 13$ for the 10 tablets.
In India macleods pharmaceutical manufacturing the brand name as FLEXABENZ 5 mg
tablets and capsule in the 84.70 rupees for 10 tablets.
Cyclobenzaprine tablets
Cyclobenzaprine tablets

This drug is also use for topical preparation like gel and ointment with combination of other

Sun pharmaceutical ltd manufacturing the brand name SKELEBENZ capsule 15 mg  in the
price 189 rupees for 10 tablets.

Cyclobenzaprine Use and Side Effect and Mechanism of Action Cyclobenzaprine Use and Side Effect and Mechanism of Action Reviewed by aboutmedicine on 21:45 Rating: 5

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