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Dimenhydrinate (then known as Compound 1694) was being tested as a potential treatment for hay fever and hives at Johns Hopkins Hospital in 1947 by allergists Dr. Leslie Gay and Dr. Paul Carliner. Among those who received the drug was a pregnant woman who had suffered from motion sickness her entire life.
Dimenhydrinate (used as an antiemetic and for motion sickness ... An H 3-antihistamine is a classification of drugs used to inhibit the action of histamine at the H 3 ...
Diphenhydramine, sold under the brand name Benadryl among others, is an antihistamine and sedative.It is a first-generation H 1-antihistamine and it works by blocking certain effects of histamine, which produces its antihistamine and sedative effects.
Dimenhydrinate; Alkylamines: The isomerism is a significant factor in the activity of the agents in this group. E-triprolidine, for example, is 1000-fold more potent than Z-triprolidine. This difference relates to the positioning and fit of the molecules in the histamine H 1-receptor binding site. [15]
The mechanisms of sympathomimetic drugs can be direct-acting (direct interaction between drug and receptor), such as α-adrenergic agonists, β-adrenergic agonists, and dopaminergic agonists; or indirect-acting (interaction not between drug and receptor), such as MAOIs, COMT inhibitors, release stimulants, and reuptake inhibitors that increase the levels of endogenous catecholamines.
Dimenhydrinate (Gravol, Dramamine) Doxylamine (Bonjesta, Unisom) Mirtazapine (Remeron) is an antidepressant that also has antiemetic effects. [5] [6] It is a potent histamine H1 receptor antagonist, K i =1.6 nM, [7] and also exhibits notable 5-HT 3 antagonism. [6] Meclizine (Bonine, Antivert)
Mechanism of action [ edit ] The altered state of consciousness produced by common or 'classical' deliriant substances such as scopolamine , atropine and diphenhydramine is mediated through the drug compounds' competitive antagonism of the peripheral and central muscarinic acetylcholine receptors , especially the M 1 muscarinic receptor.
Meclizine has low bioavailability (22–32%) and a delayed onset to action in part due to its poor solubility in water (0.1 mg/ml) and gastrointestinal fluid. [1] In children it has been found that taking meclizine with food increases its bioavailability slightly. [24] It is metabolized in the liver by the CYP2D6 enzyme. [2]