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

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Showing 1 - 10 of 24 results

Lisdexamfetamine (LDX) is a d-amphetamine (d-AMPH) pro-drug used to treat Attention Deficit and Hyperactivity Disorder (ADHD) and Binge Eating Disorder (BED). After oral administration, lisdexamfetamine dimesylate is rapidly absorbed from the gastrointestinal tract and converted to dextroamphetamine, which is responsible for the drug’s activity. Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space. Most common adverse reactions in children, adolescents and/or adults with ADHD were anorexia, anxiety, decreased appetite, decreased weight, diarrhea, dizziness, dry mouth, irritability, insomnia, nausea, upper abdominal pain, and vomiting. Agents that alter urinary pH can alter blood levels of amphetamine. Acidifying agents decrease amphetamine blood levels, while alkalinizing agents increase amphetamine blood levels. Needs to adjust Lisdexamfetamine dosage accordingly.
Status:
Investigational
Source:
INN:cathinone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Cathinone is one of the biologically active alkaloids found in the khat shrub (Catha edulis). Due to its psychoactive properties, khat has been known and utilized for ages by the inhabitants of East Africa and the northeastern parts of Arabian Peninsula. In many regions, chewing of freshly collected khat leaves (thus liberating cathinone, which affects the central nervous system) is considered a matter of culture and local tradition. Because of their structural similarity to amphetamine, cathinone and its analogs are often denoted as “natural amphetamines”, and the only structural difference between amphetamine and cathinone is the presence of a carbonyl group in the α-position of cathinone’s side chain. Similar to amphetamine, cathinone and its analogs are characterized by stimulating, euphoric, and empathogenic properties. Due to their effects on the central nervous system, the first synthetic cathinone derivatives were synthesized for medicinal purposes in the early twentieth century, but they began attracting wider attention around the year 2000. At that time, synthetic cathinones were included in a broader group of psychoactive compounds denoted as “legal drugs” or “designer drugs”
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
US Previously Marketed
Source:
VASOCORT HYDROXYAMPHETAMINE HYDROBROMIDE by SKF
(1961)
Source URL:
First marketed in 1935

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Hydroxyamphetamine is a derivative of amphetamines. Hydroxyamphetamine is intended mainly as local eye drops for diagnostic purposes. It is indirect sympathomimetic agent which cause dilation of the eye pupil before diagnostic test. Among the minor side effects from its use are: change in color vision, difficulty seeing at night, dry mouth, headache, increased sensitivity of eyes to sunlight, muscle stiffness or tightness and temporary stinging in the eyes. The main use of hydroxyamphetamines as eye drops is the diagnosis of Horner's syndrome which is characterized by nerve lesions. Hydroxyamphetamine hydrobromide is a component of FDA approved brand drug - Paremyd sterile ophthalmic solution (Hydroxyamphetamine hydrobromide, USP 1.0%, Tropicamide, USP 0.25%). Hydroxyamphetamine is an indirect-acting sympathomimetic, while tropicamide acts as a parasympatholytic.
Status:
US Previously Marketed
Source:
Benzaldehyde U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Benzaldehyde U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Benzaldehyde is the simplest and possibly the most industrially useful member of the family of aromatic aldehydes. Benzaldehyde exists in nature, primarily in combined forms such as a glycoside in almond, apricot, cherry, and peach seeds. The characteristic benzaldehyde odor of oil of bitter almond occurs because of trace amounts of free benzaldehyde formed by hydrolysis of the glycoside amygdalin. Benzaldehyde is a versatile intermediate because of its reactive aldehyde hydrogen, its carbonyl group, and the benzene ring. Benzaldehyde is formed from phenylpyruvic acid, derived by the aminotransferase activity on phenylalanine, in the presence of high levels of Mn2+, and contributes to the generation of flavor compound during cheese ripening. Benzaldehyde is a synthetic flavoring substance, sanctioned by the U.S. Food and Drug Administration (FDA) to be generally recognized as safe (GRAS) for foods. Benzaldehyde is also recognized as safe for use as a bee repellant in the harvesting of honey. Benzaldehyde's most important use is in organic synthesis, where it is the raw material utilized to produce various aldehydes. Because Benzaldehyde rapidly metabolizes to Benzoic Acid in the skin, the available dermal irritation and sensitization data demonstrating no adverse reactions to Benzoic Acid were considered supportive of the safety of Benzaldehyde.
Status:
Possibly Marketed Outside US
Source:
Japan:Piperazine Adipate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Adipic acid has been incorporated into controlled-release formulation matrix tablets to obtain a pH-independent release for both weakly basic and weakly acidic drugs. It has also been incorporated into the polymeric coating of hydrophilic monolithic systems to modulate the intragel pH, resulting in zero-order release of hydrophilic drugs. The disintegration at intestinal pH of the enteric polymer shellac has been reported to improve when adipic acid was used as a pore-forming agent without affecting release in the acidic media. Adipic acid is used to make bisobrin an antifibrinolytic.
Status:
Possibly Marketed Outside US
Source:
NCT01227616: Phase 4 Human clinical trial Completed Anemia, Iron-Deficiency/etiology
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Glucaric acid is a non-toxic, naturally occurring compound, which is found in small amounts in plants and mammals, including humans. Salts of glucaric acid have potent antiproliferative properties in vivo. The risk of cancer development can be reduced by ingesting food rich in glucaric acid or self-medication with its salts. Glucaric acid inhibits bacterial beta-glucuronidase, thus increasing the excretion of conjugated xenobiotic compounds and decreasing activity of harmful substances. Inhibition of beta-glucuronidase ultimately results in potentially decreasing the risk of carcinogenesis. Calcium salt of the acid demonstrated anti-cancer activity in patients with breast cancer (phase I clinical trial) and in preclinical models of liver, lung, colon and skin cancers. Calcium-D-glucarate is being marketed as a dietary supplement.