query: how does d-tubocurarine act as a muscle relaxant

pos: Tubocurarine chloride a few enjoyed as much popularity as tubocurarine: pancuronium, vecuronium, rocuronium, atracurium, and cisatracurium. Succinylcholine is a widely used muscle relaxant drug which acts by activating, instead of blocking, the ACh receptor. The potassium channel blocker tetraethylammonium (TEA) has been shown to reverse the effects of tubocurarine. It is thought to do so by increasing ACh release, which counteracts the antagonistic effects of tubocurarine on the ACh receptor. Spiders of the genus "Latrodectus" have α-latrotoxin in their venom. The most well known spider in this genus is the black widow spider. α-latrotoxin causes the release of neurotransmitters into the synaptic

pos: Muscle relaxant 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, such as tubocurarine, block the agonist, acetylcholine, from binding to 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. Both

pos: Prostaglandin receptor 1 and 3 series prostanoids. There are 9 established prostanoid receptors. The following table gives these receptors: a) full name; b) shortened names; c) activating prostanoids (presented in order of decreasing potencies); d) time-honored classification as contractile (i.e. conracting smooth muscle), relaxant (i.e. relaxing smooth muscle), or inhibitory (i.e. inhibiting adenyl cyclase (AC) production of cyclic AMP [cAMP]); e) G proteins types to which they link and activate, i.e. those containing the Gs alpha subunit, Gi alpha subunit, Gq alpha subunit and/or G12 subunit; and f) signaling pathways which they regulate including Adenyl cyclase which when activated increases cellular cAMP

neg: Curare skeletal muscles, effectively paralyzing the muscles of the body. Since tubocurarine binds reversibly to the ACh receptors, treatment for curare poisoning involves adding an acetylcholinesterase (AChE) inhibitor, which will stop the destruction of acetylcholine so that it can compete with curare. Curare is an example of a non-depolarizing muscle relaxant that blocks the nicotinic acetylcholine receptor (nAChR), one of the two types of acetylcholine (ACh) receptors, at the neuromuscular junction. The main toxin of curare, d-tubocurarine, occupies the same position on the receptor as ACh with an equal or greater affinity, and elicits no response, making it a competitive antagonist.

neg: Muscle relaxant 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. The earliest known use of muscle relaxant drugs was by natives of the Amazon Basin in South America who used poison-tipped arrows that produced death by skeletal muscle paralysis. This was first documented in the 16th century, when European explorers encountered it. This poison, known today as curare, led to some of the earliest scientific studies in pharmacology. Its active ingredient, tubocurarine, as well

neg: Laudexium metilsulfate Laudexium metilsulfate Laudexium metilsulfate is a neuromuscular blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in surgical anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Laudexium is no longer used in clinical practice, though it was introduced clinically in the early 1950s. It has about half the potency, a slower onset of action and a duration of action much longer than that of "d"-tubocurarine. As with all clinically established (as well as experimental agents) with a non-depolarizing mechanism of action, its pharmacological action can be

neg: Laudexium metilsulfate antagonized by anticholinesterases. The displacement of laudexium from clinical use was assured owing to recurrent reports of significant post-operative re-curarization. Laudexium metilsulfate Laudexium metilsulfate is a neuromuscular blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in surgical anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Laudexium is no longer used in clinical practice, though it was introduced clinically in the early 1950s. It has about half the potency, a slower onset of action and a duration of action much longer than that of "d"-tubocurarine. As

neg: Muscle relaxant Muscle relaxant A muscle relaxant is a drug that 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 central nervous system (CNS) activity. They are often used during surgical procedures and in intensive care and emergency medicine to cause temporary paralysis. Spasmolytics, also known as "centrally acting" muscle relaxants, are used to alleviate musculoskeletal

neg: Tubocurarine chloride and causes hypotension. Tubocurarine chloride Tubocurarine (also known as "d"-tubocurarine or DTC) is a toxic alkaloid historically known for its use as an arrow poison. In the mid-1900s, it was used in conjunction with an anesthetic to provide skeletal muscle relaxation during surgery or mechanical ventilation. It is now rarely used as an adjunct for clinical anesthesia because safer alternatives, such as cisatracurium and rocuronium, are available. Tubocurarine is a naturally occurring mono-quaternary alkaloid obtained from the bark of the Menispermaceous South American plant "Chondrodendron tomentosum", a climbing vine known to the European world since the Spanish conquest of South

neg: Tubocurarine chloride Tubocurarine chloride Tubocurarine (also known as "d"-tubocurarine or DTC) is a toxic alkaloid historically known for its use as an arrow poison. In the mid-1900s, it was used in conjunction with an anesthetic to provide skeletal muscle relaxation during surgery or mechanical ventilation. It is now rarely used as an adjunct for clinical anesthesia because safer alternatives, such as cisatracurium and rocuronium, are available. Tubocurarine is a naturally occurring mono-quaternary alkaloid obtained from the bark of the Menispermaceous South American plant "Chondrodendron tomentosum", a climbing vine known to the European world since the Spanish conquest of South America. Curare had

neg: Tubocurarine chloride gap, including acetylcholine. Bites are usually not fatal, but do cause a significant amount of pain in addition to muscle spasms. The venom is the most damaging to nerve endings, but the introduction of "d"-tubocurarine chloride blocks the nAChr, alleviating pain and muscle spasms while an antivenom can be administered. An individual administered tubocurarine chloride will be unable to move any voluntary muscles, including the diaphragm. A large enough dose will therefore result in death from respiratory failure unless artificial ventilation is initiated. The LD for mice and rabbits are 0.13 mg/kg and 0.146 mg/kg intravenously, respectively. It releases histamine

neg: History of wound care healers repeatedly used an herbal remedy for a specific wound with the belief that it promoted healing. Numerous ancient herbal remedies and poisons now serve as models for modern medicine. For example, curare, which was an ancient South American arrow poison, was used in the 20th century as the muscle relaxant tubocurarine. Tribesmen conducted various observations on the effects of different plant parts, meaning roots, leaves, etc., on specific wounds. They also observed what seasons, time of day, or moon phase would result in a most active plant. The former however resulted in a minimal influence in modern medicine as

neg: Guaifenesin it is also included in many other over-the-counter cough and cold remedy combinations (usually in conjunction with dextromethorphan, paracetamol (acetaminophen), ephedrine, pseudoephedrine, or phenylephrine). Combination guaifenesin and pseudoephedrine is sold under the brand name Mucinex D, in which "D" refers to the presence of pseudoephedrine, which is a "decongestant". Guaifenesin's neurological properties first became known in the late 1940s. Guaifenesin is a centrally acting muscle relaxant used routinely in large-animal veterinary surgery. Guaifenesin is used in combination with, for example, ketamine, since guaifenesin does not produce analgesia nor does it produce unconsciousness. The guaifenesin protocol was studied as a method

neg: Neuromuscular-blocking drug the asymmetric structure of diester isoquinolinium compounds and the acyloxylated benzyl groups on the bisbenzyltropiniums destabilizes them and can lead to spontaneous breakdown and therefore possibly a shorter duration of action. These drugs fall into two groups: A neuromuscular non-depolarizing agent is a form of neuromuscular blocker that does not depolarize the motor end plate. The quaternary ammonium muscle relaxants belong to this class. Below are some more common agents that act as competitive antagonists against acetylcholine at the site of postsynaptic acetylcholine receptors. Tubocurarine, found in curare of the South American plant Pareira, "Chondrodendron tomentosum", is the prototypical non-depolarizing

neg: Sugammadex 'Recurarisation', a phenomenon of recurrence of neuromuscular block, may occur where the reversal agents wear off before a neuromuscular blocking drug is completely cleared. This is very unusual with all but the longest acting neuromuscular blocking drugs (such as gallamine, pancuronium or tubocurarine). It has been demonstrated to occur only rarely with sugammadex, and only when insufficient doses were administered. The underlying mechanism is thought to be related to redistribution of relaxant after reversal. It may occur for a limited range of sugammadex doses which are sufficient for complex formation with relaxant in the central compartment, but insufficient for additional

neg: Muscle relaxant difficulty breathing, tightness in the chest, swelling of the mouth, face, lips, or tongue), chills, fever, and sore throat, may require medical attention. Other severe side effects include unusual or severe tiredness or weakness, as well as yellowing of the skin or the eyes. When baclofen is administered intrathecally, it may cause CNS depression accompanied with cardiovascular collapse and respiratory failure. Tizanidine may lower blood pressure. This effect can be controlled by administering a low dose at the beginning and increasing it gradually. Muscle relaxant A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle

neg: Muscle relaxant at the level of the cortex, brain stem or spinal cord, or all three areas, they have traditionally been referred to as "centrally acting" muscle relaxants. However, it is now known not every agent in this class has CNS activity (e.g. dantrolene), so this name is inaccurate. Most sources still use the term "centrally acting muscle relaxant". According to MeSH, dantrolene is usually classified as a centrally acting muscle relaxant. The World Health Organization, in its ATC, uses the term "centrally acting agents", but adds a distinct category of "directly acting agents", for dantrolene. Use of this terminology dates back

neg: Pancuronium bromide Pancuronium bromide Pancuronium (trademarked as Pavulon) is an aminosteroid muscle relaxant with various medical uses. It is used in euthanasia and is the second of three drugs administered during most lethal injections in the United States. Pancuronium is a typical non-depolarizing curare-mimetic muscle relaxant. It competitively inhibits the nicotinic acetylcholine receptor at the neuromuscular junction by blocking the binding of acetylcholine. It has slight vagolytic activity, causing an increase in heart rate, but no ganglioplegic (i.e., blocking ganglions) activity. It is a very potent muscle relaxant drug, with an ED95 (i.e., the dose that causes 95% depression of muscle twitch

neg: Tofisopam action for its various therapeutic effects, and this action has been proposed to make tofisopam potentially useful as a treatment for schizophrenia. Tofisopam has been shown to act as an inhibitor of the liver enzyme CYP3A4, and this could cause dangerous drug interactions with other medications metabolised by this enzyme, although the clinical significance of these findings remains unclear. Tofisopam Tofisopam (Emandaxin, Grandaxin, Sériel) is an anxiolytic that is marketed in several European countries. Chemically, it is a 2,3-benzodiazepine. Unlike other anxiolytic benzodiazepines (which are generally 1,4- or 1,5-substituted) however, tofisopam does not have anticonvulsant, sedative, skeletal muscle relaxant, motor

neg: Neuromuscular-blocking drug to the studies of scientists like Claude Bernard. D-tubocurarine a "mono"-quaternary alkaloid was isolated from "Chondrodendron tomentosum" in 1942, and it was shown to be the major constituent in curare responsible for producing the paralysing effect. At that time, it was known that curare and, therefore, d-tubocurarine worked at the neuromuscular junction. The isolation of tubocurarine and its marketing as the drug Intocostrin led to more research in the field of neuromuscular-blocking drugs. Scientists figured out that the potency of tubocurarine was related to the separation distance between the two quaternary ammonium heads. Further research led to the development of

neg: Neuromuscular-blocking drug not clear. Metabolism and Hofmann elimination Deacetylating vecuronium at position 3 results in a very active metabolite. In the case of rapacuronium the 3-deacylated metabolite is even more potent than rapacuronium. As long as the D-ring acetylcholine moiety is unchanged they retain their muscle relaxing effect. "Mono"-quaternary aminosteroids produced with deacylation in position 17 on the other hand are generally weak muscle relaxants. In the development of atracurium the main idea was to make use of Hofmann elimination of the muscle relaxant "in vivo". When working with bisbenzyl-isoquinolinium types of molecules, inserting proper features into the molecule such as an

neg: Curare the pain though they were not able to do anything about it since they were essentially paralyzed. On January 23, 1942, Harold Griffith and Enid Johnson gave a synthetic preparation of curare (Intercostrin/Intocostrin) to a patient undergoing an appendectomy (to supplement conventional anesthesia). Safer curare derivatives, such as rocuronium and pancuronium, have superseded d-tubocurarine for anesthesia during surgery. When used with halothane d-tubocurarine can cause a profound fall in blood pressure in some patients as both the drugs are ganglion blockers. However, it is safer to use d-tubocurarine with ether. In 1954, an article was published by Beecher and Todd

neg: Muscle relaxant dantrolene, baclofen, Drugs once but no longer or very rarely used to relax skeletal muscles include meprobamate, barbiturates, methaqualone, glutethimide and the like; some subcategories of opioids have muscle relaxant properties, and some are marketed in combination drugs with skeletal and/or smooth muscle relaxants such as whole opium products, some ketobemidone, piritramide and fentanyl preparations and Equagesic. 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

neg: Gallamine triethiodide marketed in the United States, according to the FDA Orange Book. Gallamine triethiodide Gallamine triethiodide (Flaxedil) is a non-depolarising muscle relaxant. It acts by combining with the cholinergic receptor sites in muscle and competitively blocking the transmitter action of acetylcholine. Gallamine is a non-depolarising type of blocker as it binds to the acetylcholine receptor but does not have the biological activity of acetyl choline.Gallamine triethiodide has a parasympatholytic effect on the cardiac vagus nerve, which causes tachycardia and occasionally hypertension. Very high doses cause histamine release. Gallamine triethiodide is commonly used to stabilize muscle contractions during surgical procedures. It was

neg: Gallamine triethiodide Gallamine triethiodide Gallamine triethiodide (Flaxedil) is a non-depolarising muscle relaxant. It acts by combining with the cholinergic receptor sites in muscle and competitively blocking the transmitter action of acetylcholine. Gallamine is a non-depolarising type of blocker as it binds to the acetylcholine receptor but does not have the biological activity of acetyl choline.Gallamine triethiodide has a parasympatholytic effect on the cardiac vagus nerve, which causes tachycardia and occasionally hypertension. Very high doses cause histamine release. Gallamine triethiodide is commonly used to stabilize muscle contractions during surgical procedures. It was developed by Daniel Bovet in 1947. The pharmaceutical is no longer

neg: Rocuronium bromide Rocuronium bromide Rocuronium bromide (brand names Zemuron, Esmeron) is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia to facilitate tracheal intubation by providing skeletal muscle relaxation, most commonly required for surgery or mechanical ventilation. It is used for standard endotracheal intubation, as well as for rapid sequence induction (RSI) where suxamethonium chloride, the preferred drug for RSI, is contraindicated or unavailable. It was designed to be a weaker antagonist at the neuromuscular junction than pancuronium; hence its monoquaternary structure and its having an allyl group and a pyrrolidine group attached to the D ring quaternary nitrogen

neg: Muscle relaxant shown to be better than another, and all of them have adverse effects, particularly dizziness and drowsiness. Concerns about possible abuse and interaction with other drugs, especially if increased sedation is a risk, further limit their use. A muscle relaxant is chosen based on its adverse-effect profile, tolerability, and cost. Muscle relaxants (according to one study) were not advised for orthopedic conditions, but rather for neurological conditions such as spasticity in cerebral palsy and multiple sclerosis. Dantrolene, although thought of primarily as a peripherally acting agent, is associated with CNS effects, whereas baclofen activity is strictly associated with the CNS.

neg: Methocarbamol as Robaxisal in the U.S. and Canada. However, in Spain the tradename Robaxisal is used for the Paracetamol combination instead of Robaxacet. These combinations are also available from independent manufacturers under generic names. Methocarbamol Methocarbamol is a central muscle relaxant used to treat skeletal muscle spasms. Under the trade name Robaxin, it is marketed by Actient Pharmaceuticals in the United States and Pfizer in Canada. The mechanism of action of methocarbamol is currently unknown, but may involve the inhibition of carbonic anhydrase. The muscle relaxant effects of methocarbamol are largely attributed to central depressant effects; however, peripheral effects of methocarbamol

neg: Nicotinic agonist nAChRs. Succinylcholine chloride, which is a drug that’s already on the market, is a bischoline ester and a short acting muscle relaxant. Bischoline esters are compounds that can act as a competitive agonist on muscle type nAChRs and have been used in SAR studies. In a Torpedo (α1)β1δγ nAChR model it was demonstrated that the potency of bischoline ester agonists is dependent on the chain length as potency increases with longer chains. Efficacy seems to be independent of chain length since the highest efficacy is seen in bischoline esters with four to seven units and is lower for both fewer

neg: Diazepam the anticonvulsant effects. Diazepam is used for the emergency treatment of eclampsia, when IV magnesium sulfate and blood-pressure control measures have failed. Benzodiazepines do not have any pain-relieving properties themselves, and are generally recommended to avoid in individuals with pain. However, benzodiazepines such as diazepam can be used for their muscle-relaxant properties to alleviate pain caused by muscle spasms and various dystonias, including blepharospasm. Tolerance often develops to the muscle relaxant effects of benzodiazepines such as diazepam. Baclofen or tizanidine is sometimes used as an alternative to diazepam. Diazepam is marketed in over 500 brands throughout the world. It is

neg: Methocarbamol Methocarbamol Methocarbamol is a central muscle relaxant used to treat skeletal muscle spasms. Under the trade name Robaxin, it is marketed by Actient Pharmaceuticals in the United States and Pfizer in Canada. The mechanism of action of methocarbamol is currently unknown, but may involve the inhibition of carbonic anhydrase. The muscle relaxant effects of methocarbamol are largely attributed to central depressant effects; however, peripheral effects of methocarbamol to prolong muscle refractory period have also been reported. Potential side-effects include: drowsiness, dizziness, clumsiness (ataxia), upset stomach, flushing, blurred vision, and fever. Both tachycardia (fast heart rate) and bradycardia (slow heart rate)

neg: Calciseptine is required for muscle contraction, blockers of calcium channels prevent the muscles from building tension. Blockers of the L-type calcium channels, which occur in cardiac and smooth muscles, thus act as smooth muscle relaxants and inhibitors of cardiac contractions. Common blockers of L-type calcium channels are 1,4-dihydropyridines, which are used in treatment of cardiovascular diseases. Because of their activity as a relaxant, they can relax smooth muscles surrounding blood vessels, thus widening them and lowering the blood pressure. Calciseptine resembles the abovementioned 1,4-dihydropyridines in its biological action, as it has the same ability to bind and block the L-type calcium

neg: Muscle relaxant of these classes of 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 (a nondepolarizing agent). The generation of the neuronal signals in motor neurons that cause muscle contractions are dependent on the balance of synaptic excitation and inhibition the motor neuron receives. Spasmolytic agents generally work by either enhancing the level of inhibition, or reducing the level of excitation. Inhibition is enhanced by mimicking or enhancing the actions of endogenous inhibitory substances, such as GABA. Because they may act

neg: Clorazepate Clorazepate Clorazepate, sold under the brand names Tranxene among others, is a benzodiazepine medication. It possesses anxiolytic, anticonvulsant, sedative, hypnotic, and skeletal muscle relaxant properties. Clorazepate is an unusually long-lasting benzodiazepine and serves as a majoritive prodrug for the equally long-lasting desmethyldiazepam, which is rapidly produced as an active metabolite. Desmethyldiazepam is responsible for most of the therapeutic effects of clorazepate. Clorazepate is used in the treatment of anxiety disorders and insomnia. It may also be prescribed as an anticonvulsant or muscle relaxant. It is also used as a premedication. Clorazepate is prescribed principally in the treatment of alcohol withdrawal

neg: Tubocurarine chloride who are pregnant or lactating. However, the main disadvantage in the use of tubocurarine is its significant ganglion-blocking effect, that manifests as hypotension, in many patients; this constitutes a relative contraindication to its use in patients with myocardial ischaemia. Because of the shortcomings of tubocurare, much research effort was undertaken soon after its clinical introduction to find a suitable replacement. The efforts unleashed a multitude of compounds borne from structure-activity relations developed from the tubocurare molecule. Some key compounds that have seen clinical use are identified in the muscle relaxants template box below. Of the many tried as replacements, only

neg: Xylazine and muscle relaxant in dogs, cats, horses, elk, fallow deer, mule deer, sika deer, and white-tailed deer. The sedative and analgesic effects of xylazine are related to central nervous system depression. Xylazine’s muscle relaxant effect inhibits the transmission of neural impulses in the central nervous system. In scientific research, xylazine is a component of the most common anesthetic, ketamine-xylazine, which is used in rats, mice, hamster, and guinea pigs. The accounts of the actions and uses of xylazine in animals were reported as early as the late 1960s and early 1970s. Since the early 2000s, xylazine has become popular as

neg: Curare the skeletal muscle, and that this interference occurred at the neuromuscular junction. From 1887, the Burroughs Wellcome catalogue listed under its 'Tabloids' brand name, tablets of curare at grain (price 8 shillings) for use in preparing a solution for hypodermic injection. In 1914, Henry Hallett Dale (1875–1968) described the physiological actions of acetylcholine. After 25 years, he showed that acetylcholine is responsible for neuromuscular transmission, which can be blocked by curare. The best known and historically most important (because of its medical applications) toxin is d-tubocurarine. It was isolated from the crude drug — from a museum sample of curare

neg: Quazepam Quazepam is selective for type I benzodiazepine receptors containing the α subunit, similar to other drugs such as zaleplon and zolpidem. As a result, quazepam has little or no muscle relaxant properties. Most other benzodiazepines are unselective and bind to type1 GABA receptors and type2 GABA receptors. Type1 GABA receptors include the α subunit containing GABA receptors which are responsible for hypnotic properties of the drug. Type 2 receptors include the α, α and α subunits which are responsible for anxiolytic action, amnesia and muscle relaxant properties. Thus quazepam may have less side effects than other benzodiazepines but, it has

neg: Metaxalone for few analytical methods Metaxalone Metaxalone (marketed by King Pharmaceuticals under the brand name Skelaxin) is a muscle relaxant used to relax muscles and relieve pain caused by strains, sprains, and other musculoskeletal conditions. Its exact mechanism of action is not known, but it may be due to general central nervous system depression. It is considered to be a moderately strong muscle relaxant, with relatively low incidence of side effects. Skelaxin is available in an 800 mg scored tablet. Possible side effects include nausea, vomiting, drowsiness and CNS side effects, such as dizziness, headache, and irritability. The metabolism of metaxalone

neg: Metaxalone Metaxalone Metaxalone (marketed by King Pharmaceuticals under the brand name Skelaxin) is a muscle relaxant used to relax muscles and relieve pain caused by strains, sprains, and other musculoskeletal conditions. Its exact mechanism of action is not known, but it may be due to general central nervous system depression. It is considered to be a moderately strong muscle relaxant, with relatively low incidence of side effects. Skelaxin is available in an 800 mg scored tablet. Possible side effects include nausea, vomiting, drowsiness and CNS side effects, such as dizziness, headache, and irritability. The metabolism of metaxalone involves the liver cytochrome

neg: BW-A444 BW-A444 BW A444U was an experimental neuromuscular blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs, intended to be used adjunctively in surgical anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. It was synthesized and developed in the early 1980s. BW A444U represented the first-generation of tetrahydroisoquinoline neuromuscular-blocking drugs that are nicotinic acetylcholine receptor antagonists or antinicotinics. It was an intermediate-duration non-depolarizing neuromuscular-blocking drug or skeletal muscle relaxant. It was synthesized by Mary M. Jackson and James C. Wisowaty, PhD (both chemists within the Chemical Development Laboratories at

neg: Nectandra tannins play important roles as antioxidant compounds in the scavenging of free radicals. It is reported that an extract of "N. salicifolia" has potent relaxant activity on vascular smooth muscle. Researchers of the entire world agree that pre-clinical large studies on herbal medicine are important and urgent, specially high-quality clinical and pre-clinical trials. In pre-Columbian Peru the seeds, called "Amala" in Spanish, were used as a muscle relaxant. In sites of the Sican culture, collections of the seeds have been associated with human sacrifice, and used to incapcitate victims prior to being killed. "Nectandra" contains the following species (but this

neg: Candicine rectus at concentrations of 0.01–0.2 mg/mL, and blocked the response of the nerve-sartorius to direct or indirect electrical stimulation at similar concentrations. The contraction of the rectus was inhibited by pre-treatment with tubocurarine, as was the response of the nerve-sartorius (i.e., the normal muscle twitch was not reduced by the application of candicine subsequent to tubocurarine). The action of candicine in these assays was not affected by eserine. Taking additional observations into account, these researchers concluded that the effects on frog tissue of candicine most closely resembled those of the well-known depolarizing neuromuscular-blocking drug decamethonium. An earlier comparison of 0.2

neg: Voluntary euthanasia the most reliable and rapid way to accomplish euthanasia. A coma is first induced by intravenous administration of 20 mg/kg sodium thiopental (Nesdonal) in a small volume (10 ml physiological saline). Then a triple intravenous dose of a non-depolarizing neuromuscular muscle relaxant is given, such as 20 mg pancuronium bromide (Pavulon) or 20 mg vecuronium bromide (Norcuron). The muscle relaxant should preferably be given intravenously, in order to ensure optimal availability. Only for pancuronium bromide (Pavulon) are there substantial indications that the agent may also be given intramuscularly in a dosage of 40 mg. With regards to voluntary euthanasia, many

neg: Pancuronium bromide It was also used by the Skin Hunters to kill patients in the Polish city of Łódź. Pavulon was also used by Richard Angelo in 1987 to kill at least 10 patients under his care at the Good Samaritan Hospital in New York. Pancuronium bromide Pancuronium (trademarked as Pavulon) is an aminosteroid muscle relaxant with various medical uses. It is used in euthanasia and is the second of three drugs administered during most lethal injections in the United States. Pancuronium is a typical non-depolarizing curare-mimetic muscle relaxant. It competitively inhibits the nicotinic acetylcholine receptor at the neuromuscular junction by blocking

neg: Camazepam Camazepam Camazepam is a benzodiazepine psychoactive drug, marketed under the brand names Albego, Limpidon and Paxor. It is the dimethyl carbamate ester of temazepam, a metabolite of diazepam. While it possesses anxiolytic, anticonvulsant, skeletal muscle relaxant and hypnotic properties it differs from other benzodiazepines in that its anxiolytic properties are particularly prominent but has comparatively limited anticonvulsant, hypnotic and skeletal muscle relaxant properties. Camazepam, like others benzodiazepines, produce a variety of therapeutic and adverse effects by binding to the benzodiazepine receptor site on the GABA receptor and modulating the function of the GABA receptor, the most prolific inhibitory receptor within

neg: History of electroconvulsive therapy in the United Kingdom patient is given an anaesthetic and a muscle relaxant. A brief-pulse electric current of about 800 milliamperes is passed between two electrodes on the head for several seconds, causing a seizure. The resulting convulsion is modified by the muscle relaxant. ECT is usually given on an inpatient basis; about one in five treatments are given on an outpatient basis. Treatment is usually given twice a week (occasionally three times a week) for a total of 6–12 treatments, although courses may be longer or shorter. About 70 per cent of ECT patients are women. About 1,500 ECT patients a year in

neg: Alverine Alverine Alverine is a drug used for functional gastrointestinal disorders. Alverine is a smooth muscle relaxant. Smooth muscle is a type of muscle that is not under voluntary control; it is the muscle present in places such as the gut and uterus. The side effects of alverine include: It was reported that alverine may induce toxic hepatitis. Alverine acts directly on the muscle in the gut, causing it to relax. This prevents the muscle spasms which occur in the gut in conditions such as irritable bowel syndrome and diverticular disease. Diverticular disease is a condition in which small pouches form

neg: Atracurium besilate John B. Stenlake's medicinal chemistry research group in the Department of Pharmacy at Strathclyde University, Scotland. Dewar first named this compound "33A74" before its eventual emergence in the clinic as atracurium. Atracurium was the culmination of a rational approach to drug design to produce the first non-depolarizing non-steroidal skeletal muscle relaxant that undergoes chemodegradation "in vivo". The term chemodegradation was coined by Roger D. Waigh, Ph.D., also a pharmacist and a postdoctoral researcher in Stenlake's research group. Atracurium was licensed by Strathclyde University to the Wellcome Foundation UK, which developed the drug (then known as BW 33A) and its introduction

neg: Tracazolate different effects depending on the third type of subunit making up the receptor complex. Tracazolate Tracazolate (ICI-136,753) is an anxiolytic drug which is used in scientific research. It is a pyrazolopyridine derivative, most closely related to pyrazolopyrimidine drugs such as zaleplon, and is one of a structurally diverse group of drugs known as the nonbenzodiazepines which act at the same receptor targets as benzodiazepines but have distinct chemical structures. Tracazolate has primarily anxiolytic and anticonvulsant effects, with sedative and muscle relaxant effects only appearing at higher doses. It has a unique receptor binding profile involving allosteric modulation of several GABA

neg: Tracazolate Tracazolate Tracazolate (ICI-136,753) is an anxiolytic drug which is used in scientific research. It is a pyrazolopyridine derivative, most closely related to pyrazolopyrimidine drugs such as zaleplon, and is one of a structurally diverse group of drugs known as the nonbenzodiazepines which act at the same receptor targets as benzodiazepines but have distinct chemical structures. Tracazolate has primarily anxiolytic and anticonvulsant effects, with sedative and muscle relaxant effects only appearing at higher doses. It has a unique receptor binding profile involving allosteric modulation of several GABA receptor subtypes, being selective for GABA receptors containing α1 and β3 subunits, but exhibiting

neg: Plexaura homomalla in shallow waters and "P. h."forma "kuekenthali" occurring mostly at greater depths. "P. homomalla" contains a high level of the lipid prostaglandin A. This physiologically active substance is a million times more abundant in its tissues than in those of most other animals. The function of this large amount of prostaglandin in the coral is unknown. Its function in mammals is to act as a muscle relaxant. It is used to induce labour and it causes nausea and vomiting. "P. homomalla" contains 2 to 3% by weight of prostaglandin and was used as a source for the drug until methods

neg: Decamethonium acetylcholine release. Decamethonium does not produce unconsciousness or anesthesia, and its effects may cause considerable psychological distress while simultaneously making it impossible for a patient to communicate. For these reasons, administration of the drug to a conscious patient is strongly advised against, except in necessary emergency situations. Decamethonium was used clinically in the UK for many years, but it is now available only for research purposes. Decamethonium Decamethonium (Syncurine) is a depolarizing muscle relaxant or neuromuscular blocking agent, and is used in anesthesia to induce paralysis. Decamethonium, which has a short action time, is similar to acetylcholine and acts as

neg: Abecarnil and it looks likely to be developed for use both in the treatment of anxiety, and as a less addictive substitute drug for the treatment of benzodiazepine and alcohol addiction. Abecarnil may also have fewer problems of tolerance and withdrawal problems compared to nonselective full agonist benzodiazepine acting drugs. Abecarnil is a relatively subtype-selective drug which produces primarily anxiolytic effects, with comparatively less sedative or muscle relaxant properties, and does not significantly potentiate the effects of alcohol. The abuse potential of abecarnil is thought to be less than that of benzodiazepines, with only mild withdrawal symptoms noted after abrupt discontinuation

neg: GABAA receptor the following types. Unfortunately the literature often does not distinguish these types properly. Ligands which contribute to receptor activation typically have anxiolytic, anticonvulsant, amnesic, sedative, hypnotic, euphoriant, and muscle relaxant properties. Some such as muscimol and the z-drugs may also be hallucinogenic. Ligands which decrease receptor activation usually have opposite effects, including anxiogenesis and convulsion. Some of the subtype-selective negative allosteric modulators such as αIA are being investigated for their nootropic effects, as well as treatments for the unwanted side effects of other GABAergic drugs. A useful property of the many benzodiazepine site allosteric modulators is that they may display

neg: Guaifenesin expectorant by increasing the volume and reducing the viscosity of secretions in the trachea and bronchi. It has been said to aid in the flow of respiratory tract secretions, allowing ciliary movement to carry the loosened secretions upward toward the pharynx. Thus, it may increase the efficiency of the cough reflex and facilitate removal of the secretions. Guaifenesin has muscle relaxant and anticonvulsant properties and may act as an NMDA receptor antagonist. Similar medicines derived from the guaiac tree were in use as a generic remedy by American indigenous peoples when explorers reached North America in the 16th century. The

neg: Opioid endogenous opioid peptides. Some bacteria are capable of producing some semi-synthetic opioids such as hydromorphone and hydrocodone when living in a solution containing morphine or codeine respectively. Many of the alkaloids and other derivatives of the opium poppy are not opioids or narcotics; the best example is the smooth-muscle relaxant papaverine. Noscapine is a marginal case as it does have CNS effects but not necessarily similar to morphine, and it is probably in a category all its own. Dextromethorphan (the stereoisomer of levomethorphan, a semi-synthetic opioid agonist) and its metabolite dextrorphan have no opioid analgesic effect at all despite their

neg: Medazepam Medazepam Medazepam is a drug that is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, and skeletal muscle relaxant properties. It is known by the following brand names: Azepamid, Nobrium, Tranquirax (mixed with bevonium), Rudotel, Raporan, Ansilan and Mezapam. Medazepam is a long-acting benzodiazepine drug. The half-life of medazepam is 36–200 hours. Medazepam acts as a prodrug to diazepam, as well as nordazepam, temazepam and oxazepam. Benzodiazepine drugs including medazepam increase the inhibitory processes in the cerebral cortex by allosteric modulation of the GABA receptor. Benzodiazepines may also act via micromolar benzodiazepine-binding sites as Ca channel blockers and significantly inhibited

neg: Anticonvulsant or midazolam is usually tried first. Other barbiturates only have an anticonvulsant effect at anaesthetic doses. The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsive, amnestic and muscle relaxant properties. Benzodiazepines act as a central nervous system depressant. The relative strength of each of these properties in any given benzodiazepine varies greatly and influences the indications for which it is prescribed. Long-term use can be problematic due to the development of tolerance to the anticonvulsant effects and dependency. Of the many drugs in this class, only a few are used to treat epilepsy: The following benzodiazepines are used

neg: Camylofin Camylofin Camylofin is an antimuscarinic. Camylofin is a smooth muscle relaxant with both anticholinergic action as well as direct smooth muscle action. Anticholinergic action is produced by inhibiting the binding of acetylcholine to muscarinic receptors, but the action is less pronounced. Direct smooth muscle relaxation is achieved by inhibiting phosphodiesterase type IV, which leads to increased cyclic AMP and eventually reduced cytosolic calcium. Thus camylofin has a comprehensive action to relieve smooth muscle spasm. It is used to treat stomach ache in infants and children. Usually it is given in combination with paracetamol to treat stomach ache, as well as

neg: Muscle relaxant calcium by their sarcoplasmic reticulum involves a slightly different process. Major adverse effects of dantrolene include general muscle weakness, sedation, and occasionally hepatitis. Other common spasmolytic agents include: methocarbamol, carisoprodol, chlorzoxazone, cyclobenzaprine, gabapentin, metaxalone, and orphenadrine. Muscle relaxants are very powerful drugs that may produce negative effects, including heart failure and paralysis. Patients most commonly report sedation as the main adverse effect of muscle relaxants. Usually, people become less alert when they are under the effects of these drugs. People are normally advised not to drive vehicles or operate heavy machinery while under muscle relaxants' effects. Cyclobenzaprine produces confusion and

neg: Camylofin pyrexia. Camylofin Camylofin is an antimuscarinic. Camylofin is a smooth muscle relaxant with both anticholinergic action as well as direct smooth muscle action. Anticholinergic action is produced by inhibiting the binding of acetylcholine to muscarinic receptors, but the action is less pronounced. Direct smooth muscle relaxation is achieved by inhibiting phosphodiesterase type IV, which leads to increased cyclic AMP and eventually reduced cytosolic calcium. Thus camylofin has a comprehensive action to relieve smooth muscle spasm. It is used to treat stomach ache in infants and children. Usually it is given in combination with paracetamol to treat stomach ache, as well

neg: Benzodiazepine dependence When benzodiazepines are stopped, these neuroadaptations are "unmasked" leading to hyper-excitability of the nervous system and the appearance of withdrawal symptoms. Therapeutic dose dependence is the largest category of people dependent on benzodiazepines. These individuals typically do not escalate their doses to high levels or abuse their medication. Smaller groups include patients escalating their dosage to higher levels and drug misusers as well. It is unclear exactly how many people illicitly abuse benzodiazepines. Tolerance develops within days or weeks to the anticonvulsant, hypnotic muscle relaxant and after 4 months there is little evidence that benzodiazepines retain their anxiolytic properties. Some

neg: Tofisopam Tofisopam Tofisopam (Emandaxin, Grandaxin, Sériel) is an anxiolytic that is marketed in several European countries. Chemically, it is a 2,3-benzodiazepine. Unlike other anxiolytic benzodiazepines (which are generally 1,4- or 1,5-substituted) however, tofisopam does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic properties. While it may not be an anticonvulsant in and of itself, it has been shown to enhance the anticonvulsant action of classical 1,4-benzodiazepines (such as diazepam) and muscimol, but not sodium valproate, carbamazepine, phenobarbital, or phenytoin. Tofisopam is indicated for the treatment of anxiety and alcohol withdrawal, and is prescribed in a dosage of 50–300

neg: Pinazepam is rapidly absorbed after oral administration. The main active metabolites of pinazepam are depropargylpinazepam ("N"-desmethyldiazepam, nordazepam) and oxazepam. In humans pinazepam acts as a pure anxiolytic agent in that it does not possess to any significant degree the other pharmacological characteristics of benzodiazepines. Its lack of intellectual, motor and hypnotic impairing effects makes it more appropriate than other benzodiazepines for day time use. The elimination half-life is longer in the elderly. Pinazepam Pinazepam (marketed under the brand name Domar and Duna) is a benzodiazepine drug. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Pinazepam and its metabolite "N"-desmethyldiazepam

neg: Alverine mm vs. 50 mm, P = 0.047) and higher responder rate (46.8% vs. 34.3%, OR = 1.3; P = 0.01) as compared with the placebo group. The drug was firstly authorized for marketing on 03/06/2014. The marketing authorisation holder is Dr. Reddy's Laboratories (UK) Ltd. Alverine Alverine is a drug used for functional gastrointestinal disorders. Alverine is a smooth muscle relaxant. Smooth muscle is a type of muscle that is not under voluntary control; it is the muscle present in places such as the gut and uterus. The side effects of alverine include: It was reported that alverine may induce

neg: Muscle relaxant unique mechanism of action outside of the CNS. It reduces skeletal muscle strength by inhibiting the excitation-contraction coupling in the muscle fiber. 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. Dantrolene interferes with the release of calcium by binding to the ryanodine receptor and blocking the endogenous ligand ryanodine by competitive inhibition. Muscle that contracts more rapidly is more sensitive to dantrolene than muscle that contracts slowly, although cardiac muscle and smooth muscle are depressed only slightly, most likely because the release of

neg: Muscle relaxant Muscle relaxants are thought to be useful in painful disorders based on the theory that pain induces spasm and spasm causes pain. However, considerable evidence contradicts this theory. In general, muscle relaxants are not approved by FDA for long-term use. However, rheumatologists often prescribe cyclobenzaprine nightly on a daily basis to increase stage 4 sleep. By increasing this sleep stage, patients feel more refreshed in the morning. Improving sleep is also beneficial for patients who have fibromyalgia. Muscle relaxants such as tizanidine are prescribed in the treatment of tension headaches. Diazepam and carisoprodol are not recommended for older adults, pregnant

neg: Flutoprazepam ulcers. Flutoprazepam does not fall under the international Convention on Psychotropic Substances of 1971, and is currently unscheduled in the United States. Flutoprazepam Flutoprazepam (Restas) is a drug which is a benzodiazepine. It was patented in Japan by Sumitomo in 1972 and its medical use remains mostly confined to that country. Its muscle relaxant properties are approximately equivalent to those of diazepam - however, it has more powerful sedative, hypnotic, anxiolytic and anticonvulsant effects and is around four times more potent by weight compared to diazepam. It is longer acting than diazepam due to its long-acting active metabolites, which contribute

neg: Doxacurium chloride laudexium itself was invented by a cross-combination between the prototypical non-depolarizing agent, d-tubocurarine and the depolarizing agent, decamethonium. In the 1950s and 1960s, the present-day concept of a neuromuscular blocking agent with a rapid onset and an ultra-short duration of action had not taken root: researchers and clinicians were still on the quest for potent but non-depolarizing replacements devoid of the histamine release and the dreaded "recurarizing" effects seen with tubocurarine and, more importantly, the absence of a depolarizing mechanism of action as seen with succinylcholine and decamethonium. Doxacurium chloride Doxacurium chloride (formerly recognized as BW938U80 or BW A938U) is

neg: Carisoprodol Carisoprodol Carisoprodol, marketed under the brand name Soma among others, is a prescription drug marketed since 1959. It is a centrally acting skeletal muscle relaxant of the carbamate class and produces all the effects associated with barbiturates. It is a prodrug and is both structurally and pharmacologically related to meprobamate. The major metabolic pathway of carisoprodol involves its conversion to meprobamate. In the United States, carisoprodol is a Schedule IV controlled substance under the Controlled Substances Act of 1970. The diversion and abuse of the drug has increased in the last decade. It is manufactured and marketed in the U.S.

neg: Muscle relaxant as many synthetic derivatives, played a significant role in scientific experiments to determine the function of acetylcholine in neuromuscular transmission. By 1943, neuromuscular blocking drugs became established as muscle relaxants in the practice of anesthesia and surgery. The U.S. Food and Drug Administration (FDA) approved the use of carisoprodol in 1959, metaxalone in August 1962, and cyclobenzaprine in August 1977. Other skeletal muscle relaxants of that type used around the world come from a number of drug categories and other drugs used primarily for this indication include orphenadrine (anticholinergic), chlorzoxazone, tizanidine (clonidine relative), diazepam, tetrazepam and other benzodiazepines, mephenoxalone, methocarbamol,

neg: Capital punishment in Texas p.m. Huntsville (Central) time "by intravenous injection of a substance or substances in a lethal quantity sufficient to cause death and until such convict is dead". The law does not specify the substance(s) to be used; previously, according to the Texas Department of Criminal Justice the chemicals used for the lethal injection were the commonly-used three-drug combination of (in order) sodium thiopental (a dose which sedates the offender, but not enough to kill outright), pancuronium bromide (a muscle relaxant which collapses the diaphragm and lungs), and potassium chloride (which stops the heartbeat). The offender is usually pronounced dead approximately seven

neg: Euthanasia in the Netherlands reported to combine the two procedures: usually in these cases the patient drinks the potion, but this does not cause death. After a few hours, or earlier in the case of vomiting, the muscle relaxant is administered to cause death. By far, most reported cases concerned cancer patients. Also, in most cases the procedure was applied at home. A study in 2000 found that Dutch physicians who intend to provide assistance with suicide sometimes end up administering a lethal medication themselves because of the patient's inability to take the medication or because of problems with the completion of physician-assisted suicide.

neg: Butyrylcholinesterase potentially dangerous respiratory depression that needs to be treated with assisted ventilation. Mutant alleles at the BCHE locus are responsible for suxamethonium sensitivity. Homozygous persons sustain prolonged apnea after administration of the muscle relaxant suxamethonium in connection with surgical anesthesia. The activity of pseudocholinesterase in the serum is low and its substrate behavior is atypical. In the absence of the relaxant, the homozygote is at no known disadvantage. Finally, pseudocholinesterase metabolism of procaine results in formation of paraaminobenzoic acid (PABA). If the patient receiving procaine is on sulfonamide antibiotics such as bactrim the antibiotic effect will be antagonized by providing

neg: Assassination of Mahmoud Al-Mabhouh Dubai's police gave details of the death of al-Mabhouh after forensic tests. Al-Mabhouh was injected in his leg with succinylcholine, a quick-acting, depolarizing paralytic muscle relaxant. It causes almost-instant loss of motor skills, but does not induce loss of consciousness or anaesthesia. Then al-Mabhouh was suffocated. Al-Mazeina said, "The assassins used this method so that it would seem that his death was natural." Dubai's police chief, Lt. Gen. Dahi Khalfan Tamim, announced his preliminary conclusions on 18 February that, "Our investigations reveal that Mossad is involved in the murder of al-Mabhouh ... It is 99% if not 100% that Mossad

neg: Muscle relaxant compounds have also been shown to reduce muscle spasms by their central nervous system activity. Tizanidine is perhaps the most thoroughly studied clonidine analog, and is an agonist at α-adrenergic receptors, but reduces spasticity at doses that result in significantly less hypotension than clonidine. Neurophysiologic studies show that it depresses excitatory feedback from muscles that would normally increase muscle tone, therefore minimizing spasticity. 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. The hydantoin derivative dantrolene is a spasmolytic agent with a

neg: Azemiopsin and for intramuscular injection, it was 0.732 +/- 0.13 mg/kg. intramuscular injection of Azemiopsin at a dosis between 0.3 mg/kg and 0.7 mg/kg results in various symptoms, including impaired coordination of movements, loss of muscle tone, decreased motor activity, impaired breathing, and decreased response to external stimuli. The symptoms appeared roughly 5 to 7 minutes after injection and were the most severe between 10 to 20 minutes. After a period of 60 minutes, most mice showed almost complete recovery but still had lowered motor activity and muscle tone Azemiopsin has potential to be used therapeutically as a muscle relaxant because

neg: Chlorzoxazone Like metaxalone, no specific mechanism of action has been identified for chlorzoxazone, with general central nervous system depression being the only currently accepted aspect to its medical benefits. Search for the exact mechanism of action is ongoing but limited due to the existence of more-effective safe muscle relaxers (ex. diazepam, cyclobenzaprine, tizanidine) greatly limiting the potential benefit of identifying novel compounds which share chlozoxazone's mechanism of action. As of 2015 the cost for a typical course of medication in the United States is less than 25 USD. Chlorzoxazone Chlorzoxazone (INN) is a centrally acting muscle relaxant used to treat muscle

neg: Chlorzoxazone Chlorzoxazone Chlorzoxazone (INN) is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes. It is sold under the trade names "'Lorzone'", Paraflex and Muscol and in combination form as Parafon Forte, a combination of chlorzoxazone and acetaminophen (paracetamol). Possible side effects include dizziness, lightheadedness, malaise, nausea, vomiting, and liver dysfunction. Used with acetaminophen it has added risk of hepatoxicity, which is why the combination is not recommended. It can also be administered for acute pain in general and for tension headache (muscle contraction headache).

neg: Neuromuscular-blocking drug Most of the agents in this category would be classified as non-depolarizing. Gallamine is a trisquaternary ether with three ethonium heads attached to a phenyl ring through an ether linkage. Many other different structures have been used for their muscle relaxant effect such as alcuronium (alloferin), anatruxonium, diadonium, fazadinium (AH8165) and tropeinium. In recent years much research has been devoted to new types of quaternary ammonium muscle relaxants. These are asymmetrical diester isoquinolinium compounds and bis-benzyltropinium compounds that are bistropinium salts of various diacids. These classes have been developed to create muscle relaxants that are faster and shorter acting. Both

neg: Muscle relaxant women, or people who suffer depression or for those with a history of drug or alcohol addiction. Because of the enhancement of inhibition in the CNS, most spasmolytic agents have the side effects of sedation, drowsiness and may cause dependence with long-term use. Several of these agents also have abuse potential, and their prescription is strictly controlled. The benzodiazepines, such as diazepam, interact with the GABA receptor in the central nervous system. While it can be used in patients with muscle spasm of almost any origin, it produces sedation in most individuals at the doses required to reduce muscle tone.

neg: Levator ani syndrome syndrome also have "significant elevations on the hypochondriasis, depression, and hysteria scales of the Minnesota Multiphasic Personality Inventory," which is also the case in general among chronic pain sufferers. The discomfort may be relieved by walking or pelvic tightening exercises similar to Kegel exercises. Other treatments include massage of the muscle, warm baths, muscle relaxant medications such as cyclobenzaprine, therapeutic ultrasound and biofeedback. Electrical stimulation of the levator ani muscle has been used to try to break the spastic cycle. Injection of botulinum toxin A has also been used. Levator ani syndrome Levator ani syndrome (also called levator spasm, puborectalis

neg: History of electroconvulsive therapy in the United States effects of the muscle relaxant to a specific part of the body, allowing muscle to contract from the electrical current that is administered to the patient’s brain. It is important to see the physical signs along with activity on EEG to determine the effectiveness of the procedure. “Small amounts of physical movement may be seen in the face, feet, or hands. These movements are not nearly as severe as those that occurred before the advent of muscle relaxants”. After receiving ECT, “nurses will ensure the patient’s airway is maintained, monitor observations and administer prescribed medications to counter adverse effects…”. After

neg: Doxacurium chloride Doxacurium chloride Doxacurium chloride (formerly recognized as BW938U80 or BW A938U) is a neuromuscular-blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in anesthesia to provide skeletal muscle relaxation during surgery or mechanical ventilation. Unlike a number of other related skeletal muscle relaxants, it is rarely used adjunctively to facilitate endotracheal intubation. Doxacurium is a symmetrical molecule because it is a diester of succinic acid. The pharmacological action of doxacurium is a function of its competitive antagonism to acetylcholine receptors of the nicotinic type. The drug is marketed worldwide under the tradename of Nuromax,

neg: Dantrolene Dantrolene Dantrolene sodium is a postsynaptic muscle relaxant that lessens excitation-contraction coupling in muscle cells. It achieves this by inhibiting Ca ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors. It is the primary drug used for the treatment and prevention of malignant hyperthermia, a rare, life-threatening disorder triggered by general anesthesia. It is also used in the management of neuroleptic malignant syndrome, muscle spasticity (e.g. after strokes, in paraplegia, cerebral palsy, or patients with multiple sclerosis), and 2,4-dinitrophenol poisoning, and the related compounds dinoseb and dinoterb. It is marketed by Par Pharmaceuticals LLC as Dantrium (in North America)

neg: Neuromuscular-blocking drug fit between the receptive sites without bending. Mivacurium for example has a molecular length of 3.6 nm when stretched out, far from the 2 to 2.1 nm optimum. Mivacurium, atracurium, and doxacurium have greater N-N distance and molecular length than d-tubocurarine even when bent. To make them fit, they have flexible connections that give their onium heads a chance to position themselves beneficially. This bent N-N scenario probably does not apply to laudexium and decamethylene bisatropium, which prefer a straight conformation. It has been concluded that acetylcholine and related compounds must be in the "gauche" (bent) configuration when bound to

neg: Tetrazepam Tetrazepam Tetrazepam (is marketed under the following brand names, Clinoxan, Epsipam, Myolastan, Musaril, Relaxam and Spasmorelax) is a benzodiazepine derivative with anticonvulsant, anxiolytic, muscle relaxant and slightly hypnotic properties. It was formerly used mainly in Austria, France, Belgium, Germany and Spain to treat muscle spasm, anxiety disorders such as panic attacks, or more rarely to treat depression, premenstrual syndrome or agoraphobia. Tetrazepam has relatively little sedative effect at low doses while still producing useful muscle relaxation and anxiety relief. The Co-ordination Group for Mutual Recognition and Decentralised Procedures-Human (CMD(h)) endorsed the Pharmacovigilance Risk Assessment Committee (PRAC) recommendation to suspend the

neg: Tubocurarine chloride dart poison recipes themselves. Griffith and Johnson are credited with pioneering the formal clinical introduction of tubocurarine as an adjunct to anesthetic practice on 23 January 1942, at the Montreal Homeopathic Hospital. In this sense, tubocurarine is the prototypical adjunctive neuromuscular non-depolarizing agent. However, others before Griffith and Johnson had attempted use of tubocurarine in several situations: some under controlled study conditions while others not quite controlled and remained unpublished. Regardless, all in all some 30,000 patients had been given tubocurarine by 1941, although it was Griffith and Johnson's 1942 publication that provided the impetus to the standard use of

neg: Meprobamate is also a component of the combination drug Equagesic (discontinued in the UK in 2002), acting as a muscle relaxant. Meprobamate, like barbiturates, possesses an analgesic/anesthetic potential. It is also found as a component of the combination analgesic Stopayne capsules (along with paracetamol (acetaminophen), caffeine, and codeine phosphate). Symptoms of meprobamate overdose include drowsiness, sluggishness, unresponsiveness, or coma; loss of muscle control; severe impairment or cessation of breathing; or shock. Death has been reported with ingestion of as little as 12 g of meprobamate and survival with as much as 40 g. In an overdose, meprobamate tablets may form a

neg: Clorazepate Controlled Substances Act. Clorazepate is used in the form of a dipotassium salt. It is unusual among benzodiazepines in that it is freely soluble in water. Clorazepate can be synthesized starting from 2-amino-5-chlorobenzonitrile, which upon reaction with phenylmagnesium bromide is transformed into 2-amino-5-chlorbenzophenone imine. Reacting this with aminomalonic ester gives a heterocyclization product, 7-chloro-1,3-dihydro-3-carbethoxy-5-phenyl-2"H"-benzodiazepin-2-one. Upon hydrolysis using an alcoholic solution of potassium hydroxide forms a dipotassium salt, chlorazepate. Clorazepate Clorazepate, sold under the brand names Tranxene among others, is a benzodiazepine medication. It possesses anxiolytic, anticonvulsant, sedative, hypnotic, and skeletal muscle relaxant properties. Clorazepate is an unusually long-lasting benzodiazepine and

neg: Dantrolene and by Norgine BV as Dantrium, Dantamacrin, or Dantrolen (in Europe). A hospital is recommended to keep a minimum stock of 36 dantrolene vials totaling 720 mg, sufficient for a 70-kg person. As of 2015 the cost for a typical course of medication in the United States is 100 to 200 USD. Dantrolene was first described in the scientific literature in 1967, as one of several hydantoin derivatives proposed as a new class of muscle relaxant. Dantrolene underwent extensive further development, and its action on skeletal muscle was described in detail in 1973. Dantrolene was widely used in the management

neg: Chlorproethazine chlorproethazine. Chlorproethazine Chlorproethazine, sold under the brand name Neuriplege, is a drug of the phenothiazine group described as a muscle relaxant or tranquilizer which is or has been marketed in Europe as a topical cream for the treatment of muscle pain. It has been associated with photoallergic contact dermatitis. Chlorproethazine can be synthesized from a diphenylsulfide derivative. The general scheme is sufficiently flexible to permit the interchange of the order of some of the steps. Thus alkylation of aniline thioether () with 3-chloro-1-diethylaminopropane leads to the intermediate (). Ring closure as above by nucleophilic aromatic displacement leads to the antipsychotic

neg: Chlorproethazine Chlorproethazine Chlorproethazine, sold under the brand name Neuriplege, is a drug of the phenothiazine group described as a muscle relaxant or tranquilizer which is or has been marketed in Europe as a topical cream for the treatment of muscle pain. It has been associated with photoallergic contact dermatitis. Chlorproethazine can be synthesized from a diphenylsulfide derivative. The general scheme is sufficiently flexible to permit the interchange of the order of some of the steps. Thus alkylation of aniline thioether () with 3-chloro-1-diethylaminopropane leads to the intermediate (). Ring closure as above by nucleophilic aromatic displacement leads to the antipsychotic drug

neg: Stiff-person syndrome primary treatment for SPS. Drugs that increase GABA activity alleviate muscle stiffness caused by a lack of GABAergic tone. They increase pathways that are dependent upon GABA and have muscle relaxant and anticonvulsant effects, often providing symptom relief. Because the condition worsens over time, patients generally require increased dosages, leading to more side effects. For this reason, gradual increase in dosage of benzodiazepines is indicated. Baclofen, a GABA agonist, is generally used when individuals taking high doses of benzodiazepines have high side effects. In some cases it has shown improvements in electrophysiological and muscle stiffness when administered intravenously. Intrathecal baclofen

neg: Papaverine Merck (1794–1855), founder of the Merck corporation, a major German chemical and pharmaceutical company. Papaverine is approved to treat spasms of the gastrointestinal tract, bile ducts and ureter and for use as a cerebral and coronary vasodilator in subarachnoid hemorrhage (combined with balloon angioplasty) and coronary artery bypass surgery. Papaverine may also be used as a smooth muscle relaxant in microsurgery where it is applied directly to blood vessels. Papaverine is used as an erectile dysfunction drug, alone or sometimes in combination. Papaverine, when injected in penile tissue, causes direct smooth muscle relaxation and consequent filling of the corpus cavernosum

neg: Medication popularity of meprobamate paved the way for Librium and Valium, two minor tranquilizers that belonged to a new chemical class of drugs called the benzodiazepines. These were drugs that worked chiefly as anti-anxiety agents and muscle relaxants. The first benzodiazepine was Librium. Three months after it was approved, Librium had become the most prescribed tranquilizer in the nation. Three years later, Valium hit the shelves and was ten times more effective as a muscle relaxant and anti-convulsant. Valium was the most versatile of the minor tranquilizers. Later came the widespread adoption of major tranquilizers such as chlorpromazine and the drug

neg: Urinary bladder the M3 receptor, although M2 receptors are also involved and whilst outnumbering the M3 receptors they are not so responsive. The main relaxant pathway is via the adenylyl cyclase cAMP pathway, activated by β2 adrenergic receptors. The detrusor muscle is unusually able to change its length. It can also contract for a long time whilst voiding, and it stays relaxed whilst the bladder is filling. The urothelium and lamina propria (also termed the bladder mucosa) line the inside of the detrusor muscle, and can release regulators to influence general contractility of the detrusor muscle, maintain normal bladder tone, and potentially

neg: Candocuronium iodide centers, with appendages incorporating fragments of choline or acetylcholine. The discovery program initiated by Singh initially led to the synthesis of the "bis"-quaternary non-depolarizing agent HS-342 (4,17a-dimethyl-4,17a-diaza-D-homo-5α-androstane dimethiodide) that was equipotent with tubocurarine and with one-third its duration of action, but not suitable for further clinical evaluation. Modifications of the HS-342 structure led to two other notable agents, HS-347 and HS-310 (subsequently named chandonium, then candocuronium). HS-347 was equipotent with tubocurarine but exhibited considerable ganglion blocking activity; candocuronium appeared to be suitably placed for clinical trials following encouraging preclinical evaluations. However, candocuronium did not provide the desired profile, and a