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

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Showing 31 - 40 of 286 results

Cocaine is an alkaloid ester extracted from the leaves of plants including coca. Cocaine is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. Cocaine is addictive due to its effect on the reward pathway in the brain. After a short period of use, there is a high risk that dependence will occur. Its use also increases the risk of stroke, myocardial infarction, lung problems in those who smoke it, blood infections, and sudden cardiac death. Cocaine sold on the street is commonly mixed with local anesthetics, cornstarch, quinine, or sugar which can result in additional toxicity. Following repeated doses, a person may have decreased the ability to feel pleasure and be very physically tired. Cocaine acts by inhibiting the reuptake of serotonin, norepinephrine, and dopamine. This results in greater concentrations of these three neurotransmitters in the brain. It can easily cross the blood-brain barrier and may lead to the breakdown of the barrier.
Status:
US Approved OTC
Source:
21 CFR 357.110 anthelmintic pyrantel pamoate
Source URL:
First approved in 1971
Source:
Antiminth by Roerig (Pfizer)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pyrantel is an anthelmintic, which acts as an agonist of nicotinic receptors (AChRs) of nematodes and exerts its therapeutic effects by depolarizing their muscle membranes. It is used to treat a number of parasitic worm infections. This includes ascariasis, hookworm infections, enterobiasis (pinworm infection), trichostrongyliasis and trichinellosis. Common adverse reactions include diarrhea, nausea, vomiting, dizziness, headache and somnolence.
Diphenhydramine is an antihistamine which is used in the combination with naproxen sodium for the relief of occasional sleeplessness when associated with minor aches and pains. Diphenhydramine has a role nighttime sleep-aid and naproxen sodium is a pain reliever. In addition, diphenhydramine used in relieving symptoms in patients with moderate-to-severe seasonal allergic rhinitis. Diphenhydramine acts as an antagonist of histamine H1 receptor. Besides, was shown potential to repurpose diphenhydramine as an anti-melanoma therapeutic agent, it induces melanoma cell apoptosis by suppressing STAT3/MCL-1 survival signaling pathway.
Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic and anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages.
Status:
US Approved OTC
Source:
21 CFR 346.18(a) anorectal:astringent calamine
Source URL:
First marketed in 1921
Source:
Solution of Ferric Subsulphate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Ferric Ammonium EDTA Solution is normally used as a photographic chemical for a bleaching agent in the process of colour washing. It is also used as a complexing, and oxidizing agent & as a fertilizer and catalyst. EDTA acid are colourless, water-soluble solid that are widely used to dissolve scale. The usefulness of these ammonium salts arise because of its role as a chelating agent, i.e. its ability to "sequester" metal ions such as Ca2+ and Fe3+.
Status:
US Approved OTC
Source:
21 CFR 331.11(e) antacid:citrate-containing citrate (containing active ingredients: citrate ion, as citric acid or salt)
Source URL:
First marketed in 1921
Source:
Citric Acid U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Potassium citrate is indicated for the management of renal tubular acidosis with calcium stones, hypocitraturic calcium oxalate nephrolithiasis of any etiology, uric acid lithiasis with or without calcium stones. WhenPotassium citrate is given orally, the metabolism of absorbed citrate produces an alkaline load. The induced alkaline load in turn increases urinary pH and raises urinary citrate by augmenting citrate clearance without measurably altering ultrafilterable serum citrate. Thus, potassium citrate therapy appears to increase urinary citrate principally by modifying the renal handling of citrate, rather than by increasing the filtered load of citrate. Potassium citrate is used as a food additive (E 332) to regulate acidity.
Glycine (Cly) is a natural amino acid neurotransmitter that acts as a co-agonist at Glutamate [NMDA] receptors in the brain and is an activator of glycine receptors, GLRA1-3, GLRB. The abnormal Gly levels have been implicated in neuropsychiatric disorders. Alterations in Gly levels are implicated in several diseases of the central nervous system. Glycine was studied in phase II of clinical trials in patients with schizophrenia. The results have shown that using of glycine was associated with reduced symptoms with promising effect sizes and a possibility of improvement in cognitive function. Besides, glycine was also studied in clinical trials phase II in children with cystic fibrosis. The clinical, spirometric and inflammatory status of subjects with cystic fibrosis improved after just 8 weeks of glycine intake, suggesting that this amino acid might constitute a novel therapeutic tool for these patients. In addition, Gly was proposed as a biomarker for brain tumor malignancy. Glycine is a component of a nutrients mixture for peripheral administration to well-nourished mildly catabolic adult patients who require only short-term parenteral nutrition.
Status:
Investigational
Source:
NCT01699152: Phase 1 Interventional Completed Chronic Lymphocytic Leukemia
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT02651688: Phase 2 Interventional Completed Acquired Hypogonadotropic Hypogonadism
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Enclomiphene (Androxal), in development by Repros Therapeutics Inc, is a non-steroidal estrogen receptor antagonist that promotes gonadotropin-dependent testosterone secretion by the testes. Enclomiphene constitutes the trans-stereoisomer of clomiphene citrate, a drug that has been widely prescribed for several decades for the treatment of female ovulatory dysfunction. Because of the antagonistic effects of enclomiphene, the drug has the potential to increase serum testosterone levels in men with secondary hypogonadism by restoring physiological endogenous testosterone secretion while maintaining testicular volume and, potentially, spermatogenesis. In clinical trials conducted to date, enclomiphene demonstrated significant efficacy in the physiological restoration of testosterone levels in males with secondary hypogonadism. The compound also exhibited an unanticipated favorable effect on fasting plasma glucose; this result has been accompanied by rapidly accumulating evidence from other researchers for a bidirectional relationship between low serum testosterone and obesity/metabolic syndrome (syndrome X) in men.