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Nitrofural
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DB00336 |
[A topical anti-infective agent effective against gram-negative and gram-positive bacteria. It is used for superficial wounds, burns, ulcers, and skin infections. Nitrofurazone has also been administered orally in the treatment of trypanosomiasis.] |
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8-azaguanine
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DB01667 |
[8-azaguanine is one of the early purine analogs showing antineoplastic activity. It functions as an antimetabolite and is easily incorporated into ribonucleic acids.] |
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Pyrazinamide
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DB00339 |
[A pyrazine that is used therapeutically as an antitubercular agent.] |
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Metribolone
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DB02998 |
[A synthetic non-aromatizable androgen and anabolic steroid. It binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors.] |
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Quisqualate
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DB02999 |
[An agonist at two subsets of excitatory amino acid receptors, ionotropic receptors that directly control membrane channels and metabotropic receptors that indirectly mediate calcium mobilization from intracellular stores. The compound is obtained from the seeds and fruit of Quisqualis chinensis. [PubChem]] |
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Virginiamycin M1
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DB01669 |
[Pristinamycin IIA is a macrolide antibiotic, a member of the streptogramin A group of antibiotics, and one component of pristinamycin. It is produced by Streptomyces graminofaciens and other bacteria.] |
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Omeprazole
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DB00338 |
[Originally approved by the FDA in 1989, omeprazole is a _proton-pump inhibitor_, used to treat gastric acid-related disorders. These disorders may include gastroesophageal reflux disease (GERD), peptic ulcer disease, and other diseases characterized by the oversecretion of gastric acid. This drug was the first clinical useful drug in its class, and its approval was followed by the formulation of many other proton pump inhibitor drugs [A174232]. Omeprazole is generally effective and well-tolerated, promoting its popular use in children and adults [FDA label].] |
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2-(Thiomethylene)-4-Methylpentanoic Acid
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DB02996 |
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Methadone
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DB00333 |
[Methadone is a potent synthetic analgesic that works as a full µ-opioid receptor (MOR) agonist and N-methyl-d-aspartate (NMDA) receptor antagonist. As a full MOR agonist, methadone mimics the natural effects of the body's opioids, endorphins, and enkephalins through the release of neurotransmitters involved in pain transmission. It also has a number of unique characteristics that have led to its increased use in the last two decades; in particular, methadone has a lower risk of neuropsychiatric toxicity compared to other opioids (due to a lack of active metabolites), minimal accumulation in renal failure, good bioavailability, low cost, and a long duration of action.[F4685,F4688,F4691,A185885,A185900,A185903]
Due to its unique mechanism of action, methadone is particularly useful for the management of hard to treat pain syndromes such as neuropathic pain and cancer pain requiring higher and more frequent doses of shorter-acting opioids.[A185888,A185891,A185897] Compared with [morphine], the gold standard reference opioid, methadone also acts as an agonist of κ- and σ-opioid receptors, as an antagonist of the N-methyl-D-aspartate (NMDA) receptor, and as an inhibitor of serotonin and norepinephrine uptake.[A497,A5344] Specifically by inhibiting the NMDA receptor, methadone dampens a major excitatory pain pathway within the central nervous system.[A185876] Compared to other opioids, methadone's effects on NMDA inhibition may explain it's improved analgesic efficacy and reduced opioid tolerance.[A185891,A185894]
Methadone shares similar effects and risks of other opioids such as [morphine], [hydromorphone], [oxycodone], and [fentanyl]. However, it also has a unique pharmacokinetic profile. Compared with short-acting and even extended-release formulations of [morphine], methadone displays a comparatively longer duration of action and half-life. These effects make methadone a good option for the treatment of severe pain and addiction as fewer doses are needed to maintain analgesia and prevent opioid withdrawal symptoms. However, methadone also has an unpredictable half-life with interindividual variability, which leads to an unpredictable risk of respiratory depression and overdose when initiating or titrating therapy.[A183995]
Overall, methadone's pharmacological actions result in analgesia, suppression of opioid withdrawal symptoms, sedation, miosis, sweating, hypotension, bradycardia, nausea and vomiting (via binding within the chemoreceptor trigger zone), and constipation. At higher doses, methadone use can result in respiratory depression, overdose, and death.[F4685,F4688,F4691]
Treatment of opioid addiction with methadone, [buprenorphine], or slow-release oral [morphine] (SROM) is termed Opioid Agonist Treatment (OAT) or Opioid Substitution Therapy (OST). The intention of substitution of illicit opioids with the long-acting opioids used in OAT is to prevent withdrawal symptoms for 24-36 hours following dosing to ultimately reduce cravings and drug-seeking behaviours. Use of OAT is also intended to lead to social stabilization by reducing crime rates, incarceration, use of illicit opioids such as [heroin] or [fentanyl], and ultimately marginalization.[A185882] Illegally purchased opioids present many other harms in addition to overdose as they can be injected and may be laced with other substances that increase the risk of harm or overdose. Provision of OAT is often combined with education about harm reduction including use of clean needles and injection supplies in an effort to reduce the risks associated with injection drug use such as contraction of HIV and Hepatitis C and other complications including skin infections, abscesses, or endocarditis.] |
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(S)-DES-ME-AMPA
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DB01664 |
|
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Ipratropium
|
DB00332 |
[Ipratropium is a quaternary ammonium derivative of [atropine][A176957] that acts as an anticholinergic agent.[A176939] It is commonly administered through inhalation which allows producing a local effect without presenting a significant systemic absorption.[A176957]
Ipratropium as a therapeutic agent was developed by Boehringer Ingelheim and its first monotherapy product was FDA approved in 1986.[L5891] On the other hand, the combination product of ipratropium and [albuterol] was approved in 1996.[L5894]] |
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lambda-bis(2,2'-bipyridine)-(5-methyl-2-2'-bipyridine)-C9-adamantane ruthenium (II)
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DB01663 |
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Atenolol
|
DB00335 |
[Atenolol is a cardioselective beta-blocker used in a variety of cardiovascular conditions.
Sir James Black, a scottish pharmacologist, pioneered the use of beta-blockers for the management of angina pectoris in 1958 for which he received the Nobel Prize.[A178429] Beta-blockers quickly became popular in clinical use and where subsequently investigated for use in myocardial infarction, arrhythmias, and hypertension during the 1960s. Later they continued to be investigated for use in heart failure throughout the 1970-1980s. Atenolol itself was developed early on in this history by Alvogen Malta under the trade name Tenormin and received FDA approval in September, 1981.[label]] |
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D-Myo-Inositol-Hexasulphate
|
DB01666 |
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Cacodylic acid
|
DB02994 |
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Cyclohexylammonium Ion
|
DB02995 |
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Olanzapine
|
DB00334 |
[Olanzapine is a thienobenzodiazepine classified as an atypical or second-generation antipsychotic agent.[A176996] The second-generation antipsychotics were introduced in the 90s and quickly widespread due to the presumed higher efficacy, less extrapyramidal side effects and fewer drug-drug interactions.[A177011] Olanzapine presents a very close resemblance to [clozapine] and it only differs by two additional methyl groups and the absence of a chloride moiety.[T554] It was obtained by the research of Eli Lilly and approved to be marketed in the US in 1996.[T548]] |
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2H-Benzimidazol-2-amine
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DB01665 |
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1-Deoxy-6-O-Phosphono-1-[(Phosphonomethyl)Amino]-L-Threo-Hexitol
|
DB02992 |
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8-Methyl-9-Oxoguanine
|
DB02993 |
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