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Status:
US Previously Marketed
Source:
PROCAINE HYDROCHLORIDE by GD SEARLE LLC
(1982)
Source URL:
First marketed in 1905
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine. Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.
Status:
Possibly Marketed Outside US
Source:
Unknown by Leonard, N.J.|Hauck, F.P.Jr.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Pempidine is a nicotinic antagonist most commonly used as an experimental tool. It has been used as a ganglionic blocker in the treatment of hypertension but has largely been supplanted for that purpose by more specific drugs. In preclinical models Pempidine blocks the effects of intravenous nicotine and of peripheral vagal stimulation on the blood pressure; it also causes dilatation of the pupil after removal of the sympathetic innervation. On the guinea-pig ileum, the predominant effect of the compound is to inhibit nicotine contractions. Pempidineis well absorbed from the gastrointestinal tract as judged by (a) the low ratio (6.9) of oral to intravenous toxicities, (b) the rapid development of mydriasis in mice after oral administration of small doses, and (c) the rapid onset of hypotension when the compound is injected directly into the duodenum of anaesthetized cats. Other actions include neuromuscular paralysis of curare-like type when large doses of the compound are injected intravenously and central effects such as tremors which occur with near toxic doses. In cats with a low blood pressure, large intravenous doses have a slight pressor action.
Status:
US Approved Rx
(1997)
Source:
ANDA074900
(1997)
Source URL:
First approved in 1983
Source:
TRACRIUM PRESERVATIVE FREE by HOSPIRA
Source URL:
Class:
MIXTURE
Conditions:
Atracurium is an intermediate-duration, nondepolarizing, skeletal muscle relaxant for intravenous administration. It is used, as an adjunct to general anesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Most adverse reactions were suggestive of histamine release. Common side effects include flushing of the skin and low blood pressure. Drugs which may enhance the neuromuscular blocking action of atracurium include: enflurane; isoflurane; halothane; certain antibiotics, especially the aminoglycosides and polymyxins; lithium; magnesium salts; procainamide; and quinidine.
Status:
US Previously Marketed
Source:
MIVACRON by ABBVIE
(1992)
Source URL:
First approved in 1992
Source:
MIVACRON by ABBVIE
Source URL:
Class:
MIXTURE
Conditions:
Mivacurium chloride (Mivacron) is a new benzylisoquinolinium choline-like diester neuromuscular blocking drug with an onset of action at equipotent doses that is comparable to atracurium and vecuronium but slower than succinylcholine. MIVACRON (a mixture of three stereoisomers) binds competitively to cholinergic receptors on the
motor end-plate to antagonize the action of acetylcholine, resulting in a block of neuromuscular
transmission. This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine. MIVACRON is a short-acting neuromuscular blocking agent indicated for inpatients and outpatients,
as an adjunct to general anesthesia, to facilitate tracheal intubation and to provide skeletal muscle
relaxation during surgery or mechanical ventilation.
Status:
US Previously Marketed
Source:
NUROMAX by ABBVIE
(1991)
Source URL:
First approved in 1991
Source:
NUROMAX by ABBVIE
Source URL:
Class:
MIXTURE
Conditions:
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 for endotracheal intubation or to facilitate mechanical ventilation. Unlike a number of other related skeletal muscle relaxants, it is rarely used adjunctively to facilitate endotracheal intubation. Doxacurium chloride is a mixture of three trans, trans stereoisomers, a dl pair [(1R,1'R ,2S,2'S ) and (1S,1'S ,2R,2'R )] and a meso form (1R,1'S,2S,2'R). NUROMAX binds competitively to cholinergic receptors on the motor end-plate to antagonize the action of acetylcholine, resulting in a block of neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine.