Cyclobenzaprine

Cyclobenzaprine is a muscle relaxant closely related to the class of drugs known as tricyclic antidepressants.
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Common Trade Names: Flexeril, Amrix, Fexmid, Apo-Cyclobenzaprin, Novo-Cycloprine

Other Names: 3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethyl-propan-1-amine

It is an FDA-approved medication for the relief of muscle spasm associated with musculoskeletal injuries. Cyclobenzaprine comes in either immediate-release tablets or extended-release capsules.  On its own, cyclobenzaprine is considered non-habit forming, but evidence indicates that psychological addiction to cyclobenzaprine can occur.

A Brief History of Cyclobenzaprine

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Cyclobenzaprine was synthesized and developed in 1961 by the pharmaceutical company Merck and Co. Because of its structural similarity to cyclical antidepressants, the drug was originally studied for its use in depression. Eventually, it was found to have limited efficacy as an antidepressant, but further studies uncovered its benefits as an anti-spasmodic medication. Since 1977, it has been widely used in the medical field as an adjunctive therapy for muscle spasms caused by musculoskeletal disorders.

Cyclobenzaprine was listed as the 43rd most commonly prescribed medication in the US in 2018, with more than 18 million recorded prescriptions.

How Does Cyclobenzaprine Work in the Human Body?

Cyclobenzaprine is a centrally acting muscle relaxant belonging to the heterogeneous class of anti-spasmodic medications. It is primarily used for the relief of muscle spasms. Cyclobenzaprine is a derivative of and is closely related to the class of drugs known as tricyclic antidepressants, which are drugs used in the treatment of depression, attention-deficit hyperactivity disorder (ADHD), neuropathic pain, and migraine.

The exact mechanism of action of cyclobenzaprine has not yet been fully elucidated, but previous studies have demonstrated its actions on the brainstem and spinal cord, particularly on the gamma and alpha motor neurons. It has been shown to reduce tonic somatic motor activity resulting in the control of muscular hyperactivity. It is also considered a central nervous system depressant and has sedative properties.

As mentioned above, cyclobenzaprine is FDA-approved for the treatment of muscle spasms associated with painful musculoskeletal injuries, as an adjunct to rest and physical therapy. In general, treatment with cyclobenzaprine results in improvement of range of motion and relief of pain, tenderness, and spasticity. Patients treated with cyclobenzaprine also show recovery from restrictions in daily activities. It has not shown benefit in the treatment of muscle spasms secondary to neurologic diseases such as cerebral palsy or conditions affecting the spinal cord. Off-label use of cyclobenzaprine includes relief of pain and reduction of sleep disturbances in patients suffering from fibromyalgia.

Cyclobenzaprine is only indicated for short-term therapy lasting two to three weeks as there is no sufficient evidence that shows benefits from prolonged use, and because muscle spasms resulting from musculoskeletal conditions are generally acute in nature. Patients diagnosed with hyperthyroidism, heart failure, arrhythmias, conduction disorders, or heart block should not take cyclobenzaprine. Similarly, it is contraindicated in patients during the acute recovery phase of myocardial infarction or those who took monoamine oxidase inhibitors during the past 14 days.

How Is Cyclobenzaprine Taken or Administered?

Cyclobenzaprine is available in either immediate-release tablets or extended-release capsules taken orally. Cyclobenzaprine tablets come in 5mg, 7.5mg, and 10mg formulations, while the capsules come in 15mg and 30mg formulations. The recommended dosage of cyclobenzaprine for use in muscle spasms is 5mg every 8 hours for the immediate-release tablets and 15mg once a day for the extended-release capsules. The extended-release capsules must be taken at the same time each day.

What Are the Immediate and Long-Term Effects of Cyclobenzaprine Abuse?

Cyclobenzaprine may be associated with immediate adverse effects such as:

  • Dizziness and drowsiness
  • Fatigue
  • Headache
  • Nervousness

Like other tricyclic antidepressants, cyclobenzaprine has anticholinergic properties and may thus produce anticholinergic symptoms including:

  • Dry mouth
  • Increased heart rate
  • Dilated pupil
  • Confusion and hallucinations
  • Reduced gastric motility
  • Urinary retention

Signs of Cyclobenzaprine Use Disorder

The use of cyclobenzaprine has not been directly evidenced to result in or cause addiction, but because of its relaxing and sedative effects, long-term use of cyclobenzaprine can predispose one to substance use disorder (SUD). The DSM-5 Criteria for SUD lists four main categories of pathological behaviors related to drug abuse, including abuse of cyclobenzaprine:

  1. Impaired control
  2. Social impairment
  3. Risky use
  4. Pharmacological indicators (tolerance and withdrawal)

These categories cover all 11 criteria for the diagnosis of SUDs:

Impaired control

  1. Taking the substance in larger amounts or for longer than intended
  2. Wanting to reduce or stop using the substance, yet being unsuccessful
  3. Spending excessive amount of time getting, using, or recovering from use of the substance
  4. Intense cravings and urges to use the substance

Social impairment

  1. Drug use causing problems with school, work, or family obligations including absenteeism, poor classroom performance, or disregard for household responsibilities
  2. Continued use despite having interpersonal or relationship problems
  3. Giving up important social, occupational, or recreational activities because of substance use

Risky Use

  1. Repeated use of substances in potentially dangerous situations, such as while driving a vehicle
  2. Continuing to use, despite causing or exacerbating psychological and physical problems

Physical tolerance

  1. Needing more of the substance to achieve the desired effect (tolerance)
  2. Physical withdrawal symptoms, including headaches, listlessness, or dizziness, which are relieved by taking of the substance

While individuals who take cyclobenzaprine have not been observed to have developed a physical dependency on the drug, psychological addiction to the substance can still occur. Typically, the drug is only prescribed for periods of up to three weeks, and continuing to use the substance beyond this prescription period may indicate a larger cause for concern.

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Rehab and Treatment for Cyclobenzaprine Use Disorder

Just like the treatment for misuseof other drugs, treatment for cyclobenzaprine abuse must be comprehensive and patient-centered. There are several treatment options for individuals suffering from cyclobenzaprine abuse and these can be done in either an inpatient or outpatient setting. Listed below are some examples of rehab strategies for cyclobenzaprine abuse.

Detoxification. There are two approaches to detoxification: medical and non-medical. Medical detoxification involves the use of pharmacologic interventions to cleanse the body of the substance and reverse its actions on the body. Presently, there are no FDA-approved medications to facilitate the detoxification process in cyclobenzaprine abusers. But a general approach would be to replace cyclobenzaprine with an alternative medication with similar efficacy and safety profile but less abuse potential.

The non-medical strategy of detoxification allows the patient to wean off the drug at their own pace under the guidance and supervision of medical practitioners. This approach uses psychological and behavioral interventions to help the patient stay on track of their detox process.

Counselling. One of the goals of counselling is to uncover problem areas in an individual’s life that could hinder their rehab process and provide resolutions thereto. Counselling also helps a patient stick to their treatment plan by encouraging abstinence, providing emotional support, identifying potential roadblocks, and referring the patient to other specialized services whenever necessary. The role of counselling in the rehab process has long been well-established, and studies have shown that effective counselling leads to significant reductions in drug use. Counselling can be done either by a licensed professional or by former drug abusers who have already achieved full recovery.

Psychotherapy. There are many forms of psychotherapy, but the ones most widely used in drug rehabilitation are cognitive-behavioral psychotherapy and psychodynamic therapy. Cognitive-behavioral therapies (CBT), such as relapse prevention, aversion therapy, and contingency contracting, have been proven to be of substantial use both as a monotherapy and as part of combination therapies in addressing cases of SUD. CBT aims to identify maladaptive behaviors that may lead to drug abuse and teach patients to correct and cope with the challenges of daily life using different strategies.

On the other hand, psychodynamic therapy enables individuals to have a deeper sense of self-awareness and awareness of their inner conflicts, motivations, and desires. Using this awareness, patients will be endowed with the choice for self-improvement that will help stop the cycle of addiction.

Outpatient treatment. The outpatient treatment for drug addiction involves the use of combination therapies, including the ones mentioned above. In this setting, patients will be able to continue receiving treatment on a part-time basis without disruption of their everyday life. They can still continue to work and fulfill household and social responsibilities, all while completing their treatment program. Outpatient treatment is generally less costly than its inpatient counterpart and is more appropriate for use among individuals with relatively milder symptoms and less severe addiction issues.

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