MUSCLE RELAXANTS MUSCLE RELAXANTS

Muscle relaxants were known as curare and were introduced to Europe from South America during the 1700s. Curare was known as “arrow poison” at the time and was used for hunting. Hunters used plants to create a paste and apply it to their arrowheads. When preys were struck by the arrowhead, it died within minutes. The mechanism of how curare worked was found to act as a competitive antagonist of nicotinergic neuromuscular synaptic junctions. Curare was first used clinically in anesthetic practice in 1942. This began the start of discovering derivates and developing modern drugs.

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Muscle relaxants can target cells in the muscle, neurons, or in the central nervous system (CNS). To relax the muscles, the relaxants work by the following mechanisms:

An example of an abused muscle relaxant is cyclobenzaprine which targets the CNS to relieve muscle spasms. When this medication is abused, patients commonly report effects of sedation, relaxation, and euphoric “highs ” It is commonly abused in many ways of administration such as taking it orally, crushing it to snort, mixing with other drugs, or dissolving it into alcohol. Abusing cyclobenzaprine, and other muscle relaxants targeting the CNS, can lead to an increased risk of addiction and dependence.

Releasing excitatory neurotransmitters which inhibit afferent nerves

Inhibit interneuron activity which leads to prevention of nerve signal transmission

Release of acetylcholine, the neurotransmitter involved with muscle contraction, is blocked

Prevent release of calcium in the skeletal muscle cells; decrease in calcium activity

Increase GABA levels which results in neuronal activity being blocked

Depress CNS which leads to sedation and relaxation in muscles

Alcohol amplifies the effect of muscle relaxants, especially depressant effects in the CNS, and the combination of the two can lead to overdose risks. It can also cause increased risk of addiction.

Medications that cause drug-drug interactions include opioid drugs, benzodiazepines, tricyclic antidepressants, monoamine oxidase inhibitors, fluvoxamine (SSRI), and ciprofloxacin (antibiotic).

There are a select few muscle relaxants that are controlled substances. carisoprodol and diazepam are schedule IV-controlled substances.Schedule IVcontrolled substances are drugs that can result in limited dependence and abuse potential. As these are controlled substances, these medications require prescriptions. There are also medications that are not under the Controlled Substances Act, like cyclobenzaprine, but still require a prescription to be legally obtained.