U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 11 - 20 of 36 results

Status:
First approved in 1957

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Methocarbamol is a central muscle relaxant for skeletal muscles, used to treat spasms. It is structurally related to guaifenesin. Methocarbamol's exact mechanism of causing skeletal muscle relaxation is unknown. It is thought to work centrally, perhaps by general depressant effects. It has no direct relaxant effects on striated muscle, nerve fibers, or the motor endplate. It will not directly relax contracted skeletal muscles. The drug has a secondary sedative effect. Methocarbamol is used for use as an adjunct to rest, physical therapy, and other measures for the relief of discomforts associated with acute, painful musculoskeletal conditions. Under the trade name Robaxin, Methocarbamol is marketed by Actient Pharmaceuticals in the United States and Pfizer in Canada.
Succinylcholine also known as suxamethonium is a quaternary skeletal muscle relaxant usually used in the form of its halogen salt. It is is indicated under brand name anectine as an adjunct to general anesthesia, to facilitate tracheal intubation, and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Succinylcholine activates the muscle-type nicotinic acetylcholine receptor followed by desensitization. Succinylcholine does not inhibit the presynaptic alpha3beta2 autoreceptor at clinically relevant concentrations, that provides a possible mechanistic explanation for the typical lack of tetanic fade in succinylcholine-induced neuromuscular blockade. Finally, was explored, that cardiovascular side effects (e.g., tachyarrhythmias) of succinylcholine were not mediated via direct activation of the autonomic ganglionic alpha3beta4 subtype because succinylcholine didn’t not activate the neuronal nicotinic acetylcholine receptor (nAChR) subtypes.
Status:
US Approved OTC
Source:
21 CFR 341.18 cough/cold:expectorant guaifenesin
Source URL:
First approved in 1961
Source:
BRONKODYL GLYCERYL GUAIACOLATE by PRL
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Guaifenesin is an expectorant the action of which promotes or facilitates the removal of secretions from the respiratory tract. The precise mechanism of action of guaifenesin is not known; however, it is thought to act as an expectorant by increasing the volume and reducing the viscosity of secretions in the trachea and bronchi. In turn, this may increase the efficiency of the cough reflex and facilitate removal of the secretions. Guaifenesin is over-the-counter drug for the treatment of cough and common cold.
Status:
US Previously Marketed
Source:
ANALEXIN PHENYRAMIDOL HYDROCHLORIDE by MALLINCKRODT
(1961)
Source URL:
First approved in 1960
Source:
Analexin by Irwin, Neisler (Mallinckrodt)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

PHENYRAMIDOL (ANALEXIN®), also known as fenyramidol, is an aminopyridine derivative, used as analgesic and muscle relaxant. It is considered as a drug that possibly causes hepatotoxicity.
Status:
US Previously Marketed
Source:
Sinaxar by Armour
(1958)
Source URL:
First approved in 1958
Source:
Sinaxar by Armour
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Styramate is a nonsedative skeletal muscle relaxant drug, developed by the Armour Pharmaceutical Company in 1952. The drug induces relaxation of skeletal musculus by interruption of nerve transmission in the spinal cord and brain stem rather than by exerting a blocking effect at the junction between the motor nerves and the muscles. In mouse studies styramate was found to exert a selective antagonism to hindleg extensor tonic spasm, induced by maximal electroshock, pentylenetetrazol, and strychnine sulfate. In the clinic, the drug was used in patients with neurologic and neuromuscular disorders, secondary muscular spasms. Styramate is marketed in South Africa under tradename Sinaxamol.
Status:
US Previously Marketed
Source:
Trancopal by Winthrop
(1958)
Source URL:
First approved in 1958
Source:
Trancopal by Winthrop
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Chlormezanone (TRANCOPAL®) is a non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm. It binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways. Chlormezanone (TRANCOPAL®) was discontinued worldwide in 1996 by Sanofi due to confirmed serious and rare cutaneous reactions (toxic epidermal necrolysis also known as Stevens-Johnson syndrome).
Status:
US Previously Marketed
Source:
Mylaxen by Irwin, Neisler (Mallinckrodt)
(1955)
Source URL:
First approved in 1955
Source:
Mylaxen by Irwin, Neisler (Mallinckrodt)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Hexafluorenium inhibits the enzyme cholinesterase in the plasms, but apparently not at the neuromuscular juntion. It also has some nondepolarizing activity (tubocurarine-like) at the postjunctional membrane. In man hexafluorenium potentiates the muscle relaxant effects of succinylcholine. As such, smaller doses of succinylcholine are required and fewer side effects like fasciculations, twitching and postoperative muscle pain are experienced.
Status:
US Previously Marketed
Source:
Tolserol by Squibb
(1948)
Source URL:
First approved in 1948
Source:
Tolserol by Squibb
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Mephenesin is a centrally acting muscle relaxant. This medication is prescribed for muscle spasm. It can be used as an antidote for strychnine poisoning. Most common side effects are: lassitude, drowsiness, weakness, loss of appetite, nausea and vomiting, hypersensitivity reactions. Its clinical usefulness is considered to be limited by its brief duration of action.
Tubocurarine, a naturally occurring alkaloid, is used to treat smoking withdrawl syndrom. Tubocurarine, the chief alkaloid in tobacco products, binds stereo-selectively to nicotinic-cholinergic receptors at the autonomic ganglia, in the adrenal medulla, at neuromuscular junctions, and in the brain. Two types of central nervous system effects are believed to be the basis of Tubocurarine's positively reinforcing properties. A stimulating effect is exerted mainly in the cortex via the locus ceruleus and a reward effect is exerted in the limbic system. At low doses the stimulant effects predominate while at high doses the reward effects predominate. Intermittent intravenous administration of Tubocurarine activates neurohormonal pathways, releasing acetylcholine, norepinephrine, dopamine, serotonin, vasopressin, beta-endorphin, growth hormone, and ACTH. Tubocurarine competes with acetylcholine for post-synaptic nicotinic NM receptors and blocks them.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dimethyltubocurarine (metocurine) is a non-depolarizing muscle relaxant. It binds to muscle acetylcholine receptor by bridging the to alpha and non-alpha subunits from the ligand binding site. Dimethyltubocurarine was used as an anesthesia adjunct to induce skeletal muscle relaxation and to reduce the intensity of muscle contractions in convulsive therapy.

Showing 11 - 20 of 36 results