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

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Showing 3361 - 3370 of 3491 results

Alprenolol is a beta adrenoreceptor blocking agent and 5HT1A antagonist, developed by AstraZeneca and now available as generic drug. It is used for treatment of hypertension, angina pectoris due to coronary atherosclerosis and acute myocardial infarction.
Status:
Possibly Marketed Outside US
Source:
NCT02294396: Phase 4 Interventional Completed Overactive Bladder (OAB)
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Propiverine is a well established antimuscarinic agent. It’s indicated in adults for the symptomatic treatment of urinary incontinence and/or increased urinary frequency and urgency in patients with overactive bladder syndrome or neurogenic detrusor overactivity (detrusor hyperreflexia) from spinal cord injuries, e.g. transverse legion paraplegia. As well as blocking muscarinic receptors in the detrusor muscle, the drug also inhibits cellular calcium influx, thereby diminishing muscle spasm. Overdose with the muscarinic receptor antagonist propiverine hydrochloride can potentially result in central anticholinergic effects, e.g. restlessness, dizziness, vertigo, disorders in speech and vision and muscular weakness. Moreover, severe dryness of mucosa, tachycardia and urinary retention may occur.
Thiobutabarbital is a barbiturate derivative invented in the 1950s. It has sedative, anticonvulsant and hypnotic effects, it is used in veterinary medicine for induction in surgical anaesthesia. Thiobutabarbital was formerly used as anesthetic Inactin. ‘Inactin’ (sodium thiobutabarbital) produces smooth induction of anaesthesia after intravenous administration and has a prolonged duration of action. It has variable analgesic activity.
Amezinium is a sympathomimetic used for its vasopressor effects in the treatment of hypotensive states. Amezinium inhibited monoamine oxidase (MAO) activity. Amezinium antagonized the response to tyramine and blocked neuronal uptake of noradrenaline. Side effects revealed are: palpitation, headache, nausea/vomiting, hot flashes, high blood pressure.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

1,6-Dimethyl-3-carbethoxy-4-oxo-6,7,8,9-tetrahydro-homopyrimidazol (rimazolium, MZ-144) is an analgesic (non-narcotic). It proved to be effective in all the analgesic assays used (independently of the nociceptive stimulus applied) (hot plate, tail flick, writhing tests, Randall-Selitto test, tail clip, surgical pain) differing in this respect from the nonsteroidal antiinflammatory analgetics. Rimazolium lacks the capacity of producing opiate-like physiological dependence. Also rimazolium fails to show any indication of narcotic-like abuse liability by any of clinical assessments. Rimazolium is registered in Hungary under the brand name Probon. In Hungary among analgesics Probon is the first of choice especially in case of chronic pain accompanying chronic respiratory tract diseases.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Chlorproethazine (Neuriplege) is a neuroleptic, antipsychotic and muscle relaxant. Neuriplege® cream was available as a non‐prescription medication in France until its withdrawal from the market by regulatory authorities in January 2007. Neuriplege caused phototoxicity and photocontact allergy.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Hexacarbacholine is a long-acting muscle-relaxant drug that had been used extensively in Europe in surgical anesthesia, but had had considerably less clinical usage in US. There is no precise agreement concerning the mode of action of hexacarbacholine at the myoneural junction. Therapeutic doses of the drug do not appear to influence the cardiovascular system, cardiac activity, or blood pressure, although large doses do cause slight and transient increases in blood pressure in laboratory animals. The intraocular tension in man is increased temporarily following the administration of hexacarbacholine. Since hexacarbacholine is a cumulative drug, repeated administrations should be avoided. It may cause cardiac arrest due to a hyperkalaemia.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Casopitant (GW679769) is a novel substituted piperidine derivative that competitively binds with NK1 receptors. The full occupancy of the receptor by their piperidine compound inhibits its binding with tachykinin neurotransmitters, including SP. Casopitant, in a series of in vitro and in vivo experimentations, has exhibited a potent NK1 receptor antagonism. On 29 May 2008, GlaxoSmithKline announced the submission of a new drug application to the FDA for intravenous and oral formulations of casopitant mesylate. This drug was proposed for the prevention of chemotherapy-induced nausea and vomiting as an add-on therapy to the standard dual therapy of 5-HT3 receptor antagonists + dexamethasone. The submission also included a proposed indication for postoperative nausea and vomiting prevention. Rezonic™ is the proposed trade name for casopitant mesylate in the United States; Zunrisa™ is the proposed trade name for casopitant mesylate for GlaxoSmithKline’s global group of companies. In September 2009, GlaxoSmithKline decided to discontinue all regulatory filings for casopitant based on an estimate of the amount of additional safety data.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Fenpiverinium is a quaternary ammonium compound, it is an anticholinergic and antispasmodic agent. It is a constituent of Baralgin. The effects of the constituents of Baralgin (metamizole , fenpiverinium, and pitofenone ) on mechanical activity were studied in isolated human preparations of the upper urinary tract. Fenpiverinium blocked the increase in frequency of phasic-rhythmic contractions and the tonic tension development induced by acetylcholine. Fenpiverinium did influence neither spontaneous phasic activity nor activation by high potassium or norepinephrine. Fenpiverinium has exclusively anticholinergic properties. Fenpiverinium is a muscarinic acetylcholine receptor antagonist.
Status:
Possibly Marketed Outside US
Source:
Oxyfedrine by Chemiewerk Homburg
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Oxyfedrine, an amino ketone derivative and partial agonist at beta receptors, has been shown to have potent antianginal properties and to increase coronary blood flow in normal and ischemic myocardial regions.

Showing 3361 - 3370 of 3491 results