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

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Showing 341 - 350 of 816 results

The anticholinergic agent Flutropium is a classic competitive antagonist of acetylcholine. In in vitro experiments it is more effective than atropine. A poor enteral absorption is to be expected; this can be concluded from the low relative effectiveness after oral administration. After local administration as an aerosol it is superior to atropine with regard to both effectiveness and duration of action. It is used in Japan to treat asthma and chronic obstructive pulmonary disease. Flutropium can be described as a preparation which is free of side effects.
Pridinol mesilate is a centrally acting muscle relaxant that is used in the symptomatic treatment of muscle spasm. It is also used as the hydrochloride salt for its antimuscarinic activity in the management of parkinsonism.
Status:
Possibly Marketed Outside US
Source:
Japan:Fasoracetam Hydrate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Fasoracetam is a cognition enhancer that interacts with GABA(B) receptors, stimulates neuronal ACh receptors and modulates mGlu receptors. The drug is being tested in phase III/II of clinical trials for the treatment of Attention Deficit Disorder With Hyperactivity in people with genetic disorders impacting mGlu receptors and never been approved by FDA. Fasoracetam is also being marketed in the form of capsules for research purposes aimed at investigation of cognition and memory disorders.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Derquantel is a so-called spiroindole, is obtained from fermentation extracts of Penicillium simplicissimum, a particular species of soil fungi. This drug is used in veterinary under brand name Startect, in combination with abamectin against several gastrointestinal roundworms that affect sheep. At the recommended therapeutic dose derquantel is highly effective against Haemonchus spp, Cooperia spp, and Trichostrongylus spp, including those resistant to most classic anthelmintics (benzimidazoles, levamisole, macrocyclic lactones). However it has a lower and variable efficacy against Ostertagia spp (= Teladorsagia), and is basically ineffective against Oesophagostomum spp and Trichuris spp, other important gastrointestinal worms of sheep. It is also ineffective against lungworms and other roundworms that infect sheep outside the gastrointestinal system. Derquantel is a nicotinic cholinergic antagonist: it blocks cholinergic neuromuscular transmission. The effect on the worms is that they are paralyzed and die or are expelled.
Tiemonium (often used in a form of iodide or methylsulphate salt) is a muscarinic acetylcholine receptor antagonist, which is available in Asia (mainly Bangladesh) for the alleviation of muscle spasms of the intestine, biliary system, uterus and urinary bladder in gastrointestinal, biliary, urinary and gynecological diseases.
Status:
Possibly Marketed Outside US
Source:
Japan:Diponium Bromide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Diponium bromide ((2-[alpha,alpha-dicyclopentylacetoxy)- ethyl] triethylammonium bromide) is a muscarinic cholinergic receptor antagonist. It exerts antispasmodic action.
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.
cis-Dosulepin is a stereoisomer of Dothiepin (trade name Prothiaden, Dothep, Thaden, and Dopress; Dosulepin (INN, BAN) a tricyclic antidepressant that is used in several European and South Asian countries, as well as Australia, South Africa, and New Zealand. Dosulepin is used for the treatment of the major depressive disorder and neuropathic pain. Dosulepin is only Therapeutic Goods Administration and Medicines and Healthcare products Regulatory Agency approved for the treatment of the major depressive disorder. Dothiepin is not used in the United States. The central action of cis-dosulepin was compared with that of its antidepressant stereoisomer trans-dosulepin, cis-dosulepin exerted weaker anti-reserpine, anti-tetrabenazine, and 3H-5-HT (serotonin) uptake inhibiting actions than trans-dosulepin, but cis-dosulepin's inhibition of 3H-dopamine and 3H-norepinephrine uptake was slightly more potent than that of trans-dosulepin. On the other hand, cis-dosulepin exhibited extremely potent anticholinergic action in oxotremorine induced tremor, isolated ileum and the 3H-quinuclidinyl benzilate binding test. It also showed potent apomorphine enhancing the action and shortened the period of immobility in the forced swimming test in animals.
Status:
Possibly Marketed Outside US
Source:
NCT00934973: Phase 4 Interventional Completed Irritable Bowel Syndrome
(2010)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Mebeverine is an antispasmodic with a direct action on the smooth muscle of the gastrointestinal tract. The exact mechanism of action is not known, but multiple mechanisms, such as a decrease in ion channel permeabilities, blockade of noradrenaline reuptake, a local anesthetic effects, as well as weak anti-muscarinic and phosphodiesterase inhibitory effect might contribute to the local effects of Mebeverine. This medicine is used to treat symptoms of irritable bowel syndrome (IBS) and similar problems such as chronic irritable colon, spastic constipation, mucous colitis and spastic colitis. Most people will not have problems with Mebeverine, but some may get some side effects, such as: difficulty in breathing, swelling of face, neck, tongue or throat, skin rash, red itchy skin.
Flupenthixol is a thioxanthene antipsychotic used in the treatment of schizophrenia and other psychoses, with the exception of mania and psychomotor hyperactivity due to an activating effect associated with this drug. It may also be employed as an antidepressant. Flupenthixol has a wide range of pharmacological actions. Flupenthixol blocks dopaminergic receptors, thus interfering with dopaminergic transmission in the brain. Flupenthixol also inhibits serotonin 5-HT, histamine H1, muscarinic and alpha-1 adrenergic receptors.

Showing 341 - 350 of 816 results