Aplexal - General Information
Aplexal is an anti-histaminic drug which is mainly used for the control of vomiting due to motion sickness. Aplexal was first synthesized by Janssen Pharmaceutica in 1955.
It acts by interfering with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus. The disparity of signal processing between inner ear motion receptors and the visual senses is abolished, so that the confusion of brain whether the individual is moving or standing is reduced. Vomiting in motion sickness is actually a physiological compensatory mechanism of the brain to keep the individual from moving so that it can adjust to the signal perception.
Aplexal could be also viewed as a nootropic drug because of its vasorelaxating abilities (due to calcium channel blockage), which happen mostly in brain. It is also effectively combined with other nootropics, primarily piracetam; in such combination each drug potentiate the other in boosting brain oxygen supply.
Pharmacology of Aplexal
Aplexal is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities such as contraction of smooth muscle of the airways and gastrointestinal tract, vasodilatation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release and chemotaxis of eosinophils and mast cells. Competitive antagonists at histamine H1 receptors may be divided into first (sedating) and second (non-sedating) generation agents. Some, such as Aplexal also block muscarinic acetylcholine receptors and are used as anti-emetic agents. Aplexal through its calcium channel blocking ability also inhibits stimulation of the vestibular system.
Additional information about Aplexal
Aplexal Indication: For the treatment of vertigo/meniere's disease, nausea and vomiting, motion sickness and also useful for vestibular symptoms of other origins.
Mechanism Of Action: Binds to the Histamine H1 receptor and to muscarinic acetylcholine receptors. Aplexal also inhibits contractions of vascular smooth muscle cells by blocking L type calcium channels. Aplexal has also been implicated in binding to dopamine D2 receptors.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Cinnarizine
Synonyms: Not Available
Drug Category: Anti-Allergic Agents; Calcium Channel Blockers; Histamine H1 Antagonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Cinnarizine: Abitrate; Aplactan; Aplexal; Apotomin; Artate; Carecin; Cerebolan; Cerepar; Cinaperazine; Cinazyn; Cinnacet; Cinnageron; Cinnarizine Stugeron; Corathiem; Denapol; Dimitron; Dimitronal; Eglen; Folcodal; Giganten; Glanil; Hilactan; Ixertol; Katoseran; Labyrin; Lazeta; Marisan; Midronal; Mitronal; Olamin; Processine; Sedatromin; Sepan; Siptazin; Spaderizine; Stugeron; Stutgeron; Stutgin; Toliman;
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: Not Available
Biotransformation: Not Available
Half Life: Not Available
Dosage Forms of Aplexal: Not Available
Chemical IUPAC Name: 1-[di(phenyl)methyl]-4-(3-phenylprop-2-enyl)piperazine
Chemical Formula: C26H28N2
Cinnarizine on Wikipedia: http://en.wikipedia.org/wiki/Cinnarizine
Organisms Affected: Humans and other mammals