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The metabolism of bupropion is highly variable: the effective doses of bupropion received by persons who ingest the same amount of the drug may differ by as much as 5.5 times (with a half-life of 12–30 hours), while the effective doses of hydroxybupropion may differ by as much as 7.5 times (with a half-life of 15–25 hours).
In clinical trials, the most common adverse events which occurred at a rate ≥5% and ≥1.5 times placebo included paraesthesia (tingling in fingers/toes), dizziness, altered taste, insomnia, constipation, and dry mouth.
Phentermine has been found to be completely inactive as a ligand or agonist of the serotonin 5-HT 2 receptors, including of the serotonin 5-HT 2A, 5-HT 2B, and 5-HT 2C receptors. [ 9 ] [ 10 ] [ 27 ] This is in contrast to the serotonin releasing agents (SRAs) fenfluramine , norfenfluramine , and to a lesser extent chlorphentermine .
The original synthesis at Janssen Pharmaceutica resulted in the preparation of a racemic mixture of two enantiomers, whose hydrochloride salt was reported to have a melting point of 264–265 °C; the free base of the racemate has a melting point of 87–89 °C. The racemic mixture is referred to as "tetramisole" - levamisole refers only to the ...
Irinotecan is metabolized by intrahepatic cytochrome P450 enzymes, CYP3A4 and CYP3A5 into inactive metabolites APC (7-ethyl-10-[4-N-(5-aminopentanoic acid)-1-piperidino] carbonyloxycamptothecin) and NPC (7-ethyl-10-[4-amino-1-piperidino] carbonyloxycamptothecin). NPC can be further converted by CES1 and CES2 in the liver to SN-38.
Tribenoside (Glyvenol) is a vasoprotective drug used to treat hemorrhoids. [1] It has mild anti-inflammatory, analgesic, and wound healing properties. [2] Tribenoside stimulates laminin α5 production and laminin-332 deposition to help repair the basement membrane during the wound healing process. [3]
Amantadine was initially developed to prevent replication of the influenza A virus. [18] Its main clinical use today is treatment of Parkinson's disease. [18] Other uses include treatment of drug-induced extrapyramidal side effects, motor fluctuations during levodopa therapy in Parkinson's disease, traumatic brain injury, and autistic spectrum disorders.
Extracts of unripe fruit from Asian cultivars of Citrus aurantium (commonly known as "bitter" orange), collected in China, were reported to contain synephrine levels of about 0.1–0.3%, or ~1–3 mg/g; [10] Analysis of dried fruit of C. aurantium grown in Italy showed a concentration of synephrine of ~1 mg/g, with peel containing over three times more than the pulp.