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Cyclobenzaprine

Cyclobenzaprine is a skeletal muscle relaxant and a Central Nervous System (CNS) Depressant. It is marketed as Flexeril (5 and 10 mg tablets). The 10 milligram tablets are available generically. more...

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Mechanism of Action

The exact mechanism of action for cyclobenzaprine is unknown. Current research appears to indicate that cyclobenzaprine 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 vetral horn of the spinal cord. Decreased firing of the alpha motor neuron results in decreased muscular tone.

Indications

Cyclobenzaprine 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 actually 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.

It is also prescribed off-label as a sleep-aid.

Side Effects

Common side effects include drowsiness, dizziness, and blurred vision. Other side effects are respiratory depression and decreased functionality in various muscles.

Legality

Cyclobenzaprine is regulated in the U.S. for prescription only. Cyclobenzaprine is unscheduled, however, and it is not illegal to have cyclobenzaprine in your possesion, even without a prescription.

Abuse

Cyclobenzaprine is not widely abused, despite having an arguably high potential for abuse. As a generality, habitual drug users tend to steer clear of anti-depressants, because of the possibility of contraindications with other psychoactive drugs. Cyclobenzaprine, on the other hand, can induce moderate to severe anticholinergic effects at higher doses, as well as benzodiazepine-like sedation and often pleasurable muscle-relaxation. At even higher doses, cyclobenzaprine may cause severe ataxia, and due to excessive muscle-relaxation, and possibly disorienting side-effects such as a floating sensation or other imagined movements (usually experienced when at rest.) Side-effects such as these are directly related to the favoritism of newer, more mild antidepressant medications over tricyclic antidepressants. Although purportedly unpleasant, cyclobenzaprine is relatively benign in case of overdose, depending on it's toxicity level in the user, and also on the susceptibility of the user to possibly harmful effects of overdose. Note that the susceptibility to these potentially damaging effects are greatly increased when cyclobenzaprine is used in conjunction with other drugs, particularly Central Nervous System Depressants and other antidepressants. Use of cyclobenzaprine with a MAOI (Mono Amine Oxidase Inhibitor) will very possibly result in fatality. Use of cyclobenzaprine with an SSRI (Selective Seratonin Reuptake Inhibitor) is not recommended and could lead to unpleasant and possibly damaging interactions. No deaths have been associated with cyclobenzaprine overdose, and permanent damage is almost always related to overactivity of relaxed muscles or contraindications with other drugs.

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Transdermal Treatment of Pain
From International Journal of Pharmaceutical Compounding, 9/1/05

What types of drugs are found in transdermal preparations?

* Many doctors choose to combine two or more types of medications in the transdermal preparation.

* Adjunct pain relievers: These medications are not anesthetics but reduce pain by blocking transmission of a pain signal to the brain. These include antidepressants such as amitriptyline and many other types of drugs.

* Anesthetics: Anesthetics relieve pain, and when used transdermally can be applied directly to a specific problem area. The most commonly used transdermal pain relievers are benzocaine, lidocaine, and tetracaine.

* Muscle relaxants: A muscle relaxant reduces the contractility of the muscle by blocking the transmission of nerve impulses. Common prescription examples include carisoprodol and cyclobenzaprine.

* Nonsteroidal anti-inflammatory drugs (NSAIDs): While NSAIDs act quickly and can relieve mild pain, their real therapeutic purpose is to minimize inflammation (swelling, redness) in the joints and tissues, which can affect movement in some cases. Examples of common NSAIDs are aspirin and ibuprofen.

Which specific ingredients are used?

Compounding pharmacists have far more options than commercial medicines provide, since commercial medicines are available only in fixed doses and in certain forms. (Many pain medications are available commercially only in oral form.) Transdermal pain formulations can include a number of drugs, including but not limited to those listed here. Some of these can be taken in oral form, but transdermal preparations usually cause fewer, if any, unwanted side effects.

* Amitriptyline

* Cyclobenzaprine

* Dexamethasone

* Gabapentin

* Ketamine

* Ketoprofen

* Lidocaine

* Piroxicam

What conditions are transdermal medications used for?

While there are many specific diagnoses for which transdermal pain medication may be ideal, the following are some of the most common:

* Arthritis

* Localized or acute injury

* Muscle and joint pain

* Nerve pain

Am I a candidate for transdermal pain medication?

Transdermal [trans = through; dermal = the skin] preparations are suitable for most people, and may be particularly useful in those who have an unusually sensitive digestive tract or difficulty swallowing. Transdermal pain medications may not be suitable for broken or raw skin or on very large surface areas. Patients who have allergies or sensitivities to any of the prescription components should not use these medications, and those who are allergic to soy may not be able to use preparations containing certain ingredients such as Pluronic lecithin organogel (PLO). As with any prescription, you should tell your Healthcare provider and pharmacist about all other prescription and overthe-counter medications and supplements you use so that they can screen for possible drug interactions. Talk to your doctor if you are pregnant or nursing a baby. Your pharmacist will advise you about possible side effects.

How are transdermal pain medications usually applied?

Your Healthcare provider will advise you how to apply the medication and for how long. This type of treatment typically is applied in the amount prescribed to the affected area(s) up to three times daily and rubbed in well. Some patients may gradually taper the amount they use as pain lessens. Application of a thin film onto clean, diy skin is generally all that is required to produce the needed effect.

How are transdermal medications dispensed?

Dispensing and packaging vaiy from pharmacy to pharmacy. The medication may come in a tube, a jar, or a syringe. In some cases, a jar with a special adapter is used, and a syringe will be dispensed along with it for easy application. Be sure to ask your pharmacist for a demonstration of how to measure your dose.

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