Muscle relaxant

Spasmolytics, also known as "centrally acting" muscle relaxant, are used to alleviate musculoskeletal pain and spasms and to reduce spasticity in a variety of neurological conditions.

Its active ingredient, tubocurarine, as well as many synthetic derivatives, played a significant role in scientific experiments to determine the function of acetylcholine in neuromuscular transmission.

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.

It may be hydrolysed by acetylcholine esterase (AchE) or bind to the nicotinic receptors located on the motor end plate.

Nondepolarizing agents, such as tubocurarine, block the agonist, acetylcholine, from binding to nicotinic receptors and activating them, thereby preventing depolarization.

[20] Diazepam and carisoprodol are not recommended for older adults, pregnant women, or people who have depression or for those with a history of drug or alcohol addiction.

[21] Because of the enhancement of inhibition in the CNS, most spasmolytic agents have the side effects of sedation and drowsiness and may cause dependence with long-term use.

[5][25] Clonidine and other imidazoline compounds have also been shown to reduce muscle spasms by their central nervous system activity.

[27][28] Furthermore, several clinical trials indicate that tizanidine has a similar efficacy to other spasmolytic agents, such as diazepam and baclofen, with a different spectrum of adverse effects.

In normal muscle contraction, calcium is released from the sarcoplasmic reticulum through the ryanodine receptor channel, which causes the tension-generating interaction of actin and myosin.

Major adverse effects of dantrolene include general muscle weakness, sedation, and occasionally hepatitis.

[5] Other common spasmolytic agents include: methocarbamol, carisoprodol, chlorzoxazone, cyclobenzaprine, gabapentin, metaxalone, and orphenadrine.

People are normally advised not to drive vehicles or operate heavy machinery while under muscle relaxants' effects.

While the body adjusts to this medication, it is possible for patients to experience dry mouth, fatigue, lightheadedness, constipation or blurred vision.

Some serious but unlikely side effects may be experienced, including mental or mood changes, possible confusion and hallucinations, and difficulty urinating.

In a very few cases, very serious but rare side effects may be experienced: irregular heartbeat, yellowing of eyes or skin, fainting, abdominal pain including stomach ache, nausea or vomiting, lack of appetite, seizures, dark urine or loss of coordination.

[40] Common side effects eventually caused by metaxalone include dizziness, headache, drowsiness, nausea, irritability, nervousness, upset stomach and vomiting.

Severe side effects may be experienced when consuming metaxalone, such as severe allergic reactions (rash, hives, itching, difficulty breathing, tightness in the chest, swelling of the mouth, face, lips, or tongue), chills, fever, and sore throat, may require medical attention.

Chemical diagram of pancuronium , with red lines indicating the two acetylcholine "molecules" in the structure
A view of the spinal cord and skeletal muscle showing the action of various muscle relaxants – black lines ending in arrowheads represent chemicals or actions that enhance the target of the lines, blue lines ending in squares represent chemicals or actions that inhibit the target of the line