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Carboprost tromethamine
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DB00429 |
[A nonsteroidal abortifacient agent that is effective in both the first and second trimesters of pregnancy.] |
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Kojic acid
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DB01759 |
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Streptozocin
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DB00428 |
[An antibiotic that is produced by Stretomyces achromogenes. It is used as an antineoplastic agent and to induce diabetes in experimental animals.] |
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Zolpidem
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DB00425 |
[Zolpidem, also known as _Ambien_, is a hypnotic drug that was initially approved by the FDA in 1992 [FDA label]. Zolpidem improves sleep in patients with insomnia. It is aimed for use in patients with difficulties initiating sleep. This drug decreases the time to fall asleep (sleep latency), increases the duration of sleep, and decreases the number of awakenings during sleep in patients with temporary (transient) insomnia. It is available in both immediate acting and extended release forms [FDA label], [F3802].
Its tolerability profile is favorable when administered according to the manufacturer’s instructions, with a low risk of drug withdrawal, drug dependence, and drug tolerance [A175426]. In addition, zolpidem improves sleep quality in patients suffering from chronic insomnia and can show mild muscle relaxant properties [L5584]. Research also shows that zolpidem is rapid and effective in restoring brain function for patients in a vegetative state following brain injury. This drug has the propensity to completely or partially reverse the abnormal metabolism of damaged brain cells after injury [L5584], [A175444].] |
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4-phospho-L-threonic acid
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DB01756 |
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N-[Isoleucinyl]-N'-[adenosyl]-diaminosufone
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DB01755 |
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Hyoscyamine
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DB00424 |
[Hyoscyamine is a chemical compound, a tropane alkaloid it is the levo-isomer to atropine. It is a secondary metabolite of some plants, particularly henbane (Hyoscamus niger.)
Hyoscyamine is used to provide symptomatic relief to various gastrointestinal disorders including spasms, peptic ulcers, irritable bowel syndrome, pancreatitis, colic and cystitis. It has also been used to relieve some heart problems, control some of the symptoms of Parkinson's disease, as well as for control of respiratory secretions in end of life care.] |
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3-Iodo-Tyrosine
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DB01758 |
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Triprolidine
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DB00427 |
[First generation histamine H1 antagonist used in allergic rhinitis; asthma; and urticaria. It is a component of cough and cold medicines. It may cause drowsiness.] |
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Famciclovir
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DB00426 |
[Famciclovir, marketed as Famvir by Novartis, is a guanine analogue used to treat herpes virus infections. It is most commonly used to treat herpes zoster (shingles). Famciclovir is a prodrug of penciclovir with higher oral bioavailability.] |
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S-adenosyl-L-homocysteine
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DB01752 |
[5'-S-(3-Amino-3-carboxypropyl)-5'-thioadenosine. Formed from S-adenosylmethionine after transmethylation reactions.] |
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Spironolactone
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DB00421 |
[Spironolactone is a potassium sparing diuretic like [eplerenone] that competitively inhibits mineralocorticoid receptors in the distal convoluted tubule to promote sodium and water excretion and potassium retention.[A11837]. Spironolactone was originally developed purely for this ability before other pharmacodynamic properties of the drug were discovered.[A11837,A178246] It is indicated to treat a number of conditions including heart failure, deem, hyperaldosteronism, adrenal hyperplasia, hypertension, and nephrotic syndrome.[Label] Off label uses of spironolactone involving its antiandrogenic activity include hirsutism, female pattern hair loss, and adult acne vulgaris.[A178135] Spironolactone is also frequently used in medical gender transition.[A178138]
Spironolactone was developed in 1957, marketed in 1959, and approved by the FDA on January 21, 1960.[A178243,L6187]] |
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3,3',5,5'-Tetraiodothyroacetic Acid
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DB01751 |
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Promazine
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DB00420 |
[A phenothiazine with actions similar to chlorpromazine but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic. It is currently not approved for use in the United States.] |
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Methocarbamol
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DB00423 |
[Methocarbamol was developed in the early 1950s as a treatment for muscle spasticity and the associated pain.[A178441,A178450] It is a guaiacol glyceryl ether.[A178450]
Methocarbamol tablets and intramuscular injections are prescription medicines indicated in the United States as an adjunct to rest, physical therapy, and other measures for the relief of discomforts associated with acute, painful musculoskeletal conditions.[Label,L6268] In Canada, methocarbamol can be sold as an over the counter oral medicine at a lower dose that may be combined with [acetaminophen] or [ibuprofen].[L6295] A combination product with [acetylsalicylic acid] and [codeine] is available in Canada by prescription.[L6295]
Methocarbamol was FDA approved on 16 July 1957.[L6265]] |
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3,4-Dihydroxy-1-Methylquinolin-2(1h)-One
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DB01754 |
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Methylphenidate
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DB00422 |
[Methylphenidate is a central nervous system stimulant used most commonly in the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD) and for narcolepsy. Also known as the marketed products Ritalin, Concerta, or Biphentin, methylphenidate is used with other treatment modalities (psychological, educational, cognitive behaviour therapy, etc) to improve the following group of developmentally inappropriate symptoms associated with ADHD: moderate-to-severe distractibility, short attention span, hyperactivity, emotional lability, and impulsivity. Long-acting formulations of psychostimulants such as methylphenidate, [DB01576], and [DB01255] are considered the most effective and widely used treatment for ADHD, and are considered first-line options for children, adolescents, and adults as recommended by CADDRA (Canadian ADHD Resource Alliance). [L6037] CADDRA recommends the use of methylphenidate due to long term studies, of over twenty years in duration, which show methylphenidate is safe and effective.
While its exact mechanism is unclear, methylphenidate (MPH) has been shown to act as a norepinephrine and dopamine reuptake inhibitor (NDRI), thereby increasing the presence of these neurotransmitters in the extraneuronal space and prolonging their action.[A177541] There is a dose-related effect of psychostimulants on receptor stimulation, where higher doses are shown to increase norepinephrine (NE) and dopamine (DA) efflux throughout the brain which can result in impaired cognition and locomotor-activating effects. In contrast, low doses are found to selectively activate NE and DA neurotransmission within the prefrontal cortex which is an area of the brain thought to play a prominent role in ADHD pathophysiology, thereby improving clinical efficacy and preventing side effects.[A177547] The lower doses used to treat ADHD are not associated with the locomotor-activating effects associated with higher doses and instead reduce movement, impulsivity, and increase cognitive function including sustained attention and working memory.[A177541, A177544] Methylphenidate's beneficial effects in sustaining attention have also been shown to be mediated by alpha-1 adrenergic receptor activity.[A177550] Clinical findings have shown that children with ADHD have an abnormality in the dopamine transporter gene (DAT1), the D4 receptor gene (DRD-4), and/or the D2 receptor gene that may be at least partly overcome by the dopaminergic effects of methylphenidate, suggesting a possible mode of action.[F4474]
When provided as Biphentin®, methylphenidate is released through a multi-layer release delivery system (MLRTM) where 40% of the dose is provided as an immediate release and 60% is provided through a gradual release. Biphentin was designed to be an alternative to separate doses of immediate-release (IR) methylphenidate by providing a biphasic concentration-time profile when given as a single dose. The MLRTM release system allows for a sustained effect for 10-12 hours, allowing for once-daily dosing that covers the major times that ADHD impairment might occur (such as school, homework periods, during the work day, etc).
When provided as Concerta®, methylphenidate is released through the patented Osmotic Controlled-Release Oral Delivery (OROS) system where 22% of the dose is provided as an immediate release and 78% is provided through a gradual release.[A631] OROS is comprised of an osmotically active trilayer core surrounded by a semipermeable membrane with an immediate-release drug overcoat. Within an aqueous environment, such as the stomach, the drug overcoat, which consists of 22% of the dose, dissolves within one hour, providing an initial immediate-release formulation of methylphenidate. Water then permeates through the membrane into the tablet core where the osmotically active polymer excipients expand, allowing methylphenidate to release slowly through the orifice over a period of 6-7 hours. Concerta also provides a sustained 10-12 hour effect, allowing for once-daily dosing.
Methylphenidate contains a blackbox warning stating that CNS stimulants, including methylphenidate-containing products and amphetamines, have a high potential for abuse and dependence. This abuse potential is likely related to the effects associated with higher doses of methylphenidate, which induce surface expression of the dopamine transporter (DAT).[A177553] In particular, increased dopamine in key brain areas is associated with the reinforcing and addictive properties of psychostimulants such as methylphenidate, and even amplifies the potency and reinforcing effects of other drugs of abuse such as amphetamines, making ADHD sufferers more susceptible to their addictive effects.[A177556] Concerns about abuse potential have spurred research into medications with fewer effects on DAT and the use of non-stimulant ADHD medications including [DB00289] and [DB01018].] |
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4-Oxo-nicotinamide-adenine dinucleotide phosphate
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DB01753 |
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1-naphthaleneacetic acid
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DB01750 |
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Carbamide peroxide
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DB11129 |
[Carbamide peroxide, also known as urea-hydrogen peroxide, is a water-soluble, white crystalline solid compound consisting of hydrogen peroxide and urea. As it is a source of hydrogen peroxide, it can be found in disinfecting and dental bleaching products. Some adverse effects of carbamide peroxide as a dental bleaching agent include dentin sensitivity and/or gingival irritation led by unstable and reactive H+ free radicals and low pH from prolonged use. It may also alter enamel surface morphology via enamel mineral loss and surface roughening [A32336]. The FDA considers carbamide peroxide to be safe in oral mucosal injury drug products as an oral wound healing agent, although there is insufficient data to establish general recognition of the effectiveness of this ingredient as an oral wound healing agent [L1976]. It is available in OTC otic drugs as non-water, non-oil-based solutions used to soften, loosen and remove excessive ear wax, or cerumen.] |
