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Jul 19, 2007

Muscle Relaxants' Abuse

by SirGan

SteadyHealth.com - Health Topics Forum Index -> Articles archive

Well, we all already know that substance abuse and dependence are steadily increasing problems in the United States. This isn't something that has been a problem for a couple of months- but rather extremely serious because many substances of abuse are prescription medications. Although most doctors are aware of the most commonly abused prescription medications, such as benzodiazepines and narcotics- it is important to know that centrally acting skeletal muscle relaxants are also being abused but this is not as well recognized. Some statistical data are telling that about 1% of American adults are taking muscle relaxants, often on a chronic basis. Some of these users are taking these muscle relaxants because they have all the proper indications but- vast majority use them as they develop a habit!

Where is the line between the actual need for them and abuse?

 

Biochemical structure and mechanism of action of muscle relaxants

Muscle relaxants are divided into several biochemical groups of drugs! Biochemically, skeletal muscle relaxants are a diverse group of drugs. Some of them belong to the group of tricyclic antidepressants such as Cyclobenzaprine (Flexeril); some of them are derivates of gamma-aminobutyric acid such as Baclofen (Lioresal) and some of them are similar chemical structure to other medications like with carisoprodol (Soma) which is chemically related to meprobamate (Equanil, Miltown). If we talk about their mechanism of action then we should know that the mechanism of action of skeletal muscle relaxants is unknown. However, there were some animal studies that suggested that they depress polysynaptic reflexes. Because of their various chemical structures- there could be some big problems! This is because all the parameters such as the risk for misuse, the lethal dose and the treatment in case of overdosage are specific to the drug ingested and therefore- there is no rules! Beside all these properties, almost all of them posses some kind of sedative property and that’s why- they are being abused in a first place! Therefore, several studies done recently have confirmed that, when taken in high doses- they cause a buzz, sense of euphoria and mood enhancement and pleasant misperceptions.

Drugs classified as skeletal muscle relaxants include:

cyclobenzaprine (Flexeril)

·         dantrolene (Dantrium)

·         metaxalone (Skelaxin)

·         baclofen (Lioresal)

·         carisoprodol (Soma)

·         chlorzoxazone (Paraflex)

·         methocarbamol (Robaxin)

·         orphenadrine (Norflex)

·         tizanidine (Zanaflex)

History of muscle relaxants abuse

Well, like we have already said- muscle relaxants were not a subject of abuse debates until a few years back, when they have taken center stage after several reports of deaths due to abuse of the drug. That’s when- some medication approval agencies started to recognize the problem. Not only that; few years later, somewhere in the 1996 and 1997, several members of hospital staff was charged for murdering six elderly hospital patients by giving those overdoses of two muscle relaxants. Which relaxants were in game? Well, these are Pavulon and succinylcholine chloride, commonly known as SUCC – today very commonly abused medications! According to the medical charts of these patients- they started to choke, because medications started to shut down their respiratory systems. Another incident occurred with medication called Raplon, which was very popular muscle relaxant until the report of five deaths related to it! This is why, although useful, Raplon was pulled from the market because it interferes with normal breathing! To understand the whole picture about the danger of these muscle relaxants- we should point out that Raplon is the twelfth drug removed from the market since 1997. How The US Food and Drug Administration (FDA) reacted after all this happened? Well, FDA still didn’t pool these medications from the market although many people questioning the FDA's rapid approval of drugs.

Indications for Muscle Relaxants use

What are the exact indications for muscle relaxants use? Well, most of the experts agree that the main indications are two different types of underlying conditions:

·        spasticity from upper motor neuron syndromes

What exactly is this muscle spasticity? We should know that  the term spasticity indicates on one specific clinical condition characterized by velocity dependent increase in tonic stretch reflexes or muscle tone. This condition is often associated with exaggerated tendon jerks, resulting from hyper-excitability of the stretch reflex. There are several conditions that are specifically associated with spasticity and some of the most recognizable are multiple sclerosis, spinal cord injury, traumatic brain injury, cerebral palsy…

·        muscular pain or spasms from peripheral musculoskeletal conditions

We should know that muscle spasm is defined as a sudden involuntary contraction of one or more muscle groups. It usually represents one acute condition associated with muscle strain or sprain.

What are the common symptoms of musculoskeletal conditions? Well, the most usual symptoms are tenderness and muscle spasms, fibromyalgia, tension headaches, myofascial pain and low back or neck pain. Well, when used in these situations and conditions- muscle relaxants can be extremely useful because they relax certain muscles in the body and relieve the stiffness, pain and discomfort caused by strains, sprains or other injury to your muscles.

Although we have mentioned that there are several different types of muscle relaxants- the truth is that the FDA has approved only a few medications in this class for treatment of spasticity. All others are prohibited or still under the investigation of FDA!

Muscle relaxants abuse facts

Big diagnostic and therapeutic problem, beside the fact that these muscle relaxants are being abused, is the fact that they are rarely taken alone! In most cases – they are used in combination with other central nervous system depressants, such as alcohol, benzodiazepines or narcotics. What do abusers use them? Well, the answer is simple! Several researches have proven that they normally prolong the effect of alcohol or a narcotic drug or even increase it!   

Not only that, experts are saying that prescriptions for skeletal muscle relaxants are usually easier to obtain than prescriptions for narcotics! They are also often less expensive and that they can’t do nothing about it! Like we have already mentioned- the fact is that skeletal muscle relaxants are less commonly used alone or as the primary drug of abuse. It is interesting to point out that sometimes addicts take muscle relaxants to demonstrate signs of tolerance, and also suffer withdrawal symptoms of anxiety, tremors, insomnia and, occasionally, hallucinations or seizures.

 

Side Effects and Adverse reactions

It is important to point out that all skeletal muscle relaxants may cause sedation (drowsiness, dizziness).

This is characteristic and almost rule for them! There are also some other die effects which are characteristic to some of them individually; for example- Baclofen may cause severe central nervous system depression with cardiovascular collapse and respiratory failure, Dantrolene has a potential for hepatotoxicity.  Carisoprodol, like many other muscle relaxants, has some potential for dependence and withdrawal symptoms. Several patients, after using Methocarbamol and chlorzoxazone, have noticed that their urine have changed color into something like orange or reddish-purple. This is reported by many patients later and classified as harmless side effect! Good thing is that the urine will return to its normal color when the patient stops taking the medicine.

 

The conclusion  

It is logical to assume that, because of the fact that the relaxants act in the central nervous system, their actions may produce some side effects associated with CNS functioning. That’s why- in most countries they are strictly prohibited while in other countries, some muscle relaxants can be sold even without prescription. Although before, they are being sold and used widely with no control of medication agencies because no side effects were reported- today, the situation has changed! Because of so many reported abuse and deaths using muscle relaxants, patients and governments agencies have become cautious. However- they still are the extremely useful medications in clinical practice for muscle relaxation in clinical practice. Like all other medications, they surely can cause several possible side effects, and that’s why they be used with extreme caution. Countries where muscle relaxants can be bought easily even without a doctor’s prescription should change their pharmacy lows and prohibit this in future! 

 

 

 


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