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Status:
US Approved OTC
Source:
21 CFR 341.14(a)(2)(ii) cough/cold:antitussive codeine phosphate
Source URL:
First marketed in 1921
Source:
Codeine Sulphate U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Codeine is an opiate used to manage mild to moderate pain severe enough to require an opioid. Codeine is a selective agonist for the mu opioid receptor and has an affinity to delta and kappa-opioid receptors. In some countries, this drug is regulated under various narcotic control laws, because its chronic use can cause physical dependence. In others, it is available without a medical prescription in combination with paracetamol.
Status:
US Approved OTC
Source:
21 CFR 344.1 otic:earwax removal aid carbamide peroxide 6.5% (in anhydrous glycerin)
Source URL:
First marketed in 1921
Class (Stereo):
CHEMICAL (ACHIRAL)
Hydrogen peroxide has been used in medicine for more than 100 years. It is known in surgery as a highly useful irrigation solution by virtue of both its hemostatic and its antimicrobial effects. Hydrogen peroxide is a mild antiseptic used on the skin to prevent infection of minor cuts, scrapes, and burns. It may also be used as a mouth rinse to help remove mucus or to relieve minor mouth irritation (e.g., due to canker/cold sores, gingivitis). This product works by releasing oxygen when it is applied to the affected area. The release of oxygen causes foaming, which helps to remove dead skin and clean the area. Hydrogen peroxide is a strong oxidizing agent used in aqueous solution as a ripening agent, bleach, and topical anti-infective. It is relatively unstable and solutions deteriorate over time unless stabilized by the addition of acetanilide or similar organic materials.
Status:
US Approved OTC
Source:
21 CFR 341.16(d) cough/cold:bronchodilator epinephrine
Source URL:
First marketed in 1901
Source:
Adrenalin by Parke Davis
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Epinephrine is a sympathomimetic catecholamine. It acts as a naturally occurring agonist at both alpha and beta-adrenergic receptors. Three pharmacologic types have been identified: alpha 1-, alpha 2-, and beta-adrenergic receptors. Each of these has three subtypes, characterized by both structural and functional differences. The alpha 2 and beta receptors are coupled negatively and positively, respectively, to adenylyl cyclase via Gi or Gs regulatory proteins, and the alpha 1 receptors modulate phospholipase C via the Go protein. Subtype expression is regulated at the level of the gene, the mRNA, and the protein through various transcriptional and postsynthetic mechanisms. Through its action on alpha-adrenergic receptors, epinephrine lessens the vasodilation and increased vascular permeability that occurs during anaphylaxis, which can lead to loss of intravascular fluid volume and hypotension. Through its action on beta-adrenergic receptors, epinephrine causes bronchial smooth muscle relaxation and helps alleviate bronchospasm, wheezing and dyspnea that may occur during anaphylaxis. Epinephrine also alleviates pruritus, urticaria, and angioedema and may relieve gastrointestinal and genitourinary symptoms associated with anaphylaxis because of its relaxer effects on the smooth muscle of the stomach, intestine, uterus and urinary bladder.
Epinephrine increases glycogenolysis, reduces glucose up take by tissues, and inhibits insulin release in the pancreas, resulting in hyperglycemia and increased blood lactic acid.
Status:
US Approved OTC
Source:
21 CFR 346.20(b) anorectal:keratolytic resorcinol
Source URL:
First marketed in 1894
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Resorcinol is a benzenediol. Resorcinol is commonly used in hair dyes and acne medication. Resorcinol works by breaking down rough, scaly, or hardened skin. Resorcinol also disinfects the skin to help fight infection. Resorcinol topical (for the skin) is used to treat pain and itching caused by minor cuts and scrapes, burns, insect bites, poison ivy, sunburn, or other skin irritations. Resorcinol topical is also used to treat acne, eczema, psoriasis, seborrhea, corns, calluses, warts, and other skin disorders. Resorcinol is included in the FDA final rule list of all permitted active ingredients for OTC topical acne products. Permitted combination active ingredient product - Resorcinol in 2 percent concentration in combination with sulfur in concentrations of between 3 and 8 percent. In oxidative hair dyes, resorcinol is regulated to 5% or below in practice, however, many manufacturers limit the level of free resorcinol in oxidative hair dyes to 1.25%. Resorcinol is limited to 0.5% in shampoos and hair lotions. Resorcinol is usually present in anti-acne preparations at a maximum concentration of 2%. The concentration of resorcinol can be much higher in peels, in some cases around 50%. Jessner’s solution (resorcinol in ethyl alcohol, 14% w/v; lactic acid, 14%; and salicylic acid, 14%) is commonly used in chemical peeling. A specialized medical use of resorcinol is in biological glues (gelatin–resorcinol–formaldehyde glue) for cardiovascular surgery, in particular aortic operations.
Status:
Investigational
Source:
NCT04657926: Phase 2 Interventional Completed Osteoarthritis
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Apocynin, also known as acetovanillone, is a natural organic compound related to vanillin. It has been isolated from a variety of plant sources. Metabolites of apocynin are able to block the activity of NADPH oxidase, thus giving apocynin antioxidant and anti-inflammatory capabilities. Effects of apocynin on the concentration of reactive oxygen and nitrogen species in patients with asthma and chronic obstructive pulmonary disease were investigated in phase I clinical trials. In preclinical models, it was found that apocynin provides neuroprotective effects in models of stroke and Parkinson's disease.
Status:
Investigational
Source:
INN:narazaciclib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
ON-123300 is a potent and multi-targeted kinase inhibitor with potential application for brain tumor chemotherapy. ON123300 strongly inhibits Ark5 and CDK4, as well as growth factor receptor tyrosine kinases such as β-type platelet-derived growth factor receptor (PDGFRβ). ON123300 inhibited U87 glioma cell proliferation and reduced phosphorylation of Akt, yet it also unexpectedly induced Erk activation, both in a dose- and time-dependent manner that subsequently was attributed to relieving Akt-mediated C-Raf S259 inactivation and activating a p70S6K-initiated PI3K-negative feedback loop. ON123300 demonstrated high brain and brain tumor accumulation and favorable pharmacokinetic characteristics.
Status:
Investigational
Source:
NCT04277884: Phase 3 Interventional Completed Hypertension
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
QGC-001 (also known as RB-150) is an aminobutane-1-sulfonic acid derivative patented by Institut National de la Sante et de la Recherche Medicale as antihypertensive agent. QGC-001 acts as aminopeptidase A inhibitor and suppress conversion of angiotensin II to angiotensin III in brain tissues Oral administration of RB150 in conscious deoxycorticosterone acetate (DOCA)–salt rats inhibited brain aminopeptidase A activity, resulting in values similar to those obtained with the brains of normotensive rats, demonstrating the central bioavailability of RB150. Oral RB150 treatment resulted in a marked dose-dependent reduction in blood pressure in DOCA-salt but not in normotensive rats. In clinical trials single oral administration of QGC001 up to 1,250 mg in healthy volunteers was well-tolerated. Following oral administration, QGC001 is absorbed via the gastrointestinal tract and converted partially into its active metabolite EC33 in plasma. As in animal experiments, in normotensive subjects QGC001 had no effect on the systemic renin-angiotensin-aldosterone parameters and on PCop concentrations, a marker of vasopressin release.
Status:
Investigational
Class (Stereo):
CHEMICAL (UNKNOWN)
FENHARMANE, a reserpine-like substance, is a neuroleptic developed and clinically tested in the Czech Republic.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Femoxetine is a selective serotonin re-uptake inhibitor. It was being studied in the treatment of narcolepsy, migraine, depressive states and eating disorder. Femoxetine development has been discontinued.
Status:
Investigational
Source:
NCT00621270: Phase 2 Interventional Completed Major Depressive Disorder
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Coluracetam (code name BCI-540; formerly MKC-231) is a nootropic agent of the racetam family. It was initially developed and tested by the Mitsubishi Tanabe Pharma Corporation for Alzheimer's disease. After the drug failed to reach endpoints in its clinical trials it was in-licensed by BrainCells Inc for investigations into major depressive disorder (MDD). Like most racetam compounds, Coluracetam increases choline uptake, but it also increases uptake in damaged neurons. Specifically, Coluracetam interacts with the HACU process, which is responsible for absorbing choline into the neurons. This increased uptake occurs during the Acetylcholine synthesis process. Since Coluracetam improves choline preservation during this process, a larger amount is converted into Acetylcholine. This results in increased memory, attention and alertness. It is important to note here, that these benefits were only seen in subjects with previously impaired neurons, not in subjects with normally functioning neurons. Coluracetam is also shown to improve AMPA potentiation, which is a process that triggers cognitive function and alertness. Although Coluracetam interacts with choline transporters as well, there isn’t enough evidence to explain why or how this interaction occurs, or what occurs after the interaction. Coluracetam has been in phase II clinical trials for the treatment of major depression and anxiety. However, this research has been discontinued.