Muscle Relaxant


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Your muscles help you move and help your body work. Different types of muscles have different jobs. There are many problems that can affect muscles. Muscle disorders can cause weakness, pain or even paralysis.

There may be no known cause for a muscle disorder. Some known causes include

  • Injury or overuse, such as sprains or strains, cramps or tendinitis
  • Genetics, such as muscular dystrophy
  • Some cancers
  • Inflammation, such as myositis
  • Diseases of nerves that affect muscles
  • Infections
  • Certain medicines

A spasm is a sudden, involuntary contraction of a muscle, a group of muscles, or a hollow organ, or a similarly sudden contraction of an orifice. It is sometimes accompanied by a sudden burst of pain, but is usually harmless and ceases after a few minutes. Spasmodic muscle contraction may also be due to a large number of medical conditions, including the dystonias.

By extension, a spasm is a temporary burst of energy, activity, emotion, stress, or anxiety.

A subtype of spasms is colic, an episodic pain due to spasms of smooth muscle in a particular organ (e.g. the bile duct). A characteristic of colic is the sensation of having to move about, and the pain may induce nausea or vomiting if severe. Series of spasms or permanent spasms are called a spasmism.

In very severe cases, the spasm can induce muscular contractions that are more forceful than the sufferer could generate under normal circumstances. This can lead to torn tendons and ligaments.Hysterical strength is argued to be a type of spasm induced by the brain under extreme circumstances.

A muscle relaxant is a drug which affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term “muscle relaxant” is used to refer to two major therapeutic groups: neuromuscular blockers and spasmolytics. Neuromuscular blockers act by interfering with transmission at the neuromuscular end plate and have no CNS activity. They are often used during surgical procedures and in intensive care and emergency medicine to cause paralysis. Spasmolytics, also known as “centrally-acting” muscle relaxants, are used to alleviate musculoskeletal pain and spasms and to reduce spasticity in a variety of neurological conditions. While both neuromuscular blockers and spasmolytics are often grouped together as muscle relaxants, the term is commonly used to refer to spasmolytics only.

Muscle relaxers, AKA “skeletal muscle relaxants “, make up an important category of prescription medication useful for the relief of muscle pain and muscle spasm.  Muscle relaxers are not available without a prescription in the U.S.  For those who must bear the challenges of chronic pain, multiple sclerosis, or spinal injury, prescription muscle relaxers are often the medications which allow them to enjoy a reasonable quality of life.  They are often used for short term relief of back or neck spasm or stiffness.  Sometimes finding the appropriate prescription muscle relaxer can be challenging.  As with many medications, what works well for one person may not work well for another.

Muscle relaxant

  

Neuromuscular-blocking drugs

Muscle relaxation and paralysis can theoretically occur by interrupting function at several sites, including the central nervous system, myelinated somatic nerves, unmyelinated motor nerve terminals, nicotinic acetylcholine receptors, the motor end plate, and the muscle membrane or contractile apparatus. Most neuromuscular blockers function by blocking transmission at the end plate of the neuromuscular junction. Normally, a nerve impulse arrives at the motor nerve terminal, initiating an influx of calcium ions which causes the exocytosis of synaptic vesicles containing acetylcholine. Acetylcholine then diffuses across the synaptic cleft. It may be hydrolysed by Acetylcholine esterase (AchE) or bind to the nicotinic receptors located on the motor end plate. The binding of two acetylcholine molecules results in a conformational change in the receptor that opens the sodium-potassium channel of the nicotinic receptor. This allows Na+ and Ca2+ ions to enter the cell and K+ ions to leave the cell causing a depolarization of the end plate, resulting in muscle contraction. Following depolarization, the acetylcholine molecules are then removed from the end plate region and enzymatically hydrolysed by acetylcholinesterase.

Normal end plate function can be blocked by two mechanisms. Nondepolarizing agents like tubocurarine block the agonist, acetylcholine, from binding nicotinic receptors and activating them, thereby preventing depolarization. Alternatively, depolarizing agents such as succinylcholine are nicotinic receptor agonists which mimic Ach, block muscle contraction by depolarizing to such an extent that it desensitizes the receptor and it can no longer initiate an action potential and cause muscle contraction. These neuromuscular blocking drugs are structurally similar to acetylcholine, the endogenous ligand, in many cases containing two acetylcholine molecules linked end-to-end by a rigid carbon ring system, as in pancuronium.

Carisoprodol

Carisoprodol is a centrally-acting skeletal muscle relaxant. It is a colorless, crystalline powder, having a mild characteristic odor and a bitter taste. Carisoprodol is slightly soluble in water and freely soluble in alcohol, chloroform and acetone. The drug’s solubility is practically independent of pH. Carisoprodol is marketed in the United States under the brand name Soma, and in the United Kingdom and other countries under the brand names Sanoma and Carisoma. The drug is available by itself or mixed with aspirin and in one preparation (Soma Compound With Codeine) along with codeine and caffeine as well.

Cyclobenzaprine is a muscle relaxant. It works by blocking nerve impulses (or pain sensations) that are sent to your brain.   Cyclobenzaprine is used together with rest and physical therapy to treat skeletal muscle conditions such as pain or injury. Cyclobenzaprine hydrochloride is a white, crystalline tricyclic amine salt with the empirical formula C20H21N•HCl and a molecular weight of 311.9. It has a melting point of 217°C, and a pKa of 8.47 at 25°C. It is freely soluble in water and alcohol, sparingly soluble in isopropanol, and insoluble in hydrocarbon solvents. If aqueous solutions are made alkaline, the free base separates. 

FLEXERIL 5 mg (Cyclobenzaprine HCl) is supplied as a 5 mg tablet for oral administration. FLEXERIL 10 mg (Cyclobenzaprine HCl) is supplied as a 10 mg tablet for oral administration.

FLEXERIL tablets contain the following inactive ingredients: hydroxypropyl cellulose, hydroxypropyl methylcellulose, iron oxide, lactose, magnesium stearate, starch, and titanium dioxide. FLEXERIL 5 mg tablets also contain Yellow D&C #10 Aluminum Lake HT, and Yellow FD&C #6 Aluminum Lake.

cyclobenzaprine

FLEXERIL is indicated as an adjunct to rest and physical therapy for relief of muscle spasm associated with acute, painful musculoskeletal conditions.

Improvement is manifested by relief of muscle spasm and its associated signs and symptoms, namely, pain, tenderness, limitation of motion, and restriction in activities of daily living.

FLEXERIL should be used only for short periods (up to two or three weeks) because adequate evidence of effectiveness for more prolonged use is not available and because muscle spasm associated with acute, painful musculoskeletal conditions is generally of short duration and specific therapy for longer periods is seldom warranted.

FLEXERIL has not been found effective in the treatment of spasticity associated with cerebral or spinal cord disease, or in children with cerebral palsy.

 Muscle relaxants

Generic Name Brand Name
carisoprodol Soma
cyclobenzaprine hydrochloride Flexeril
diazepam Valium
metaxalone Skelaxin
methocarbamol Robaxin

The muscle-relaxing effects of these medicines are most likely the result of their ability to depress the central nervous system. They are also called sedatives. Muscle relaxants can be helpful when severe muscle spasms follow the start of low back pain.Diazepam (Valium) and carisoprodol (such as Soma) are not recommended for use by pregnant women, older adults, or people who have depression or a history of drug or alcohol addiction.For acute low back pain, muscle relaxants improve pain, muscle tension, and mobility. But side effects are common.  For chronic low back pain, muscle relaxants may relieve pain and lead to overall improvement, but side effects are common.

Muscle relaxant Side Effects

Possible side effects of muscle relaxants include:

  • Drowsiness or dizziness.
  • Possible addiction or dependence.
  • Dry mouth.
  • Urinary retention.

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