Gramalil 10%
Gramalil 10% Uses, Dosage, Side Effects, Food Interaction and all others data.
Gramalil 10% is a selective D2 and D3 dopamine receptor blocker in the brain.
Gramalil 10% has a high degree of regional selectivity for limbic areas. One study found that tiapride shows over three times as much affinity for limbic areas than striatal areas as opposed to the near equal selectivity for limbic and striatal regions shown by haloperidol.Another study in rats found tiapride's affinity for the septum, a limbic region, to be over thirty times as high as for the striatum.Efficacy at the D2 receptor is moderate, with 80 percent of receptors occupied even in the presence of excess tiapride concentrations.
| Trade Name | Gramalil 10% |
| Generic | Tiapride |
| Tiapride Other Names | Thiapride, Tiaprida, Tiapride, Tiapridum |
| Type | |
| Formula | C15H24N2O4S |
| Weight | Average: 328.427 Monoisotopic: 328.145677956 |
| Protein binding | Negligible |
| Groups | Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Japan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Gramalil 10% is a dopamine D2 and D3 receptor antagonist indicated in the treatment of chorea in Huntington's disease, as well as agitation and anxiety in the elderly or with acute or chronic alcoholism.
Gramalil 10% is indicated for the treatment of a variety of neurological and psychiatric disorders including dyskinesia, alcohol withdrawal syndrome, negative symptoms of psychosis, and agitation and aggression in the elderly.
Gramalil 10% is also used to associated treatment for these conditions: Behavioural Disorders, Chorea
How Gramalil 10% works
Gramalil 10% is a selective dopamine D2 and D3 receptor antagonist, offering an advantage over other neuroleptic drugs, such as haloperidol and risperidone, which bind a range of targets including four of the five known dopamine receptor subtypes (D1-4), serotonin (5-HT2A, 2C), α1- and α2-adrenergic, and histamine H1 receptors. Compared to these drugs, tiapride has a relatively moderate affinity for its target receptors, displacing 50 percent of 3H-raclopride binding at a concentration of 320 nM at D2 receptors and a concentration of 180 nM at D3 receptors.
Volume of Distribution
Gramalil 10% distributes rapidly and exhibits virtually no binding to plasma proteins, giving it a relatively high volume of distribution
Elimination Route
The bioavailability of tiapride is approximately 75 percent. It has a Tmax is 0.4-1.5 hours and Tss is 24-48 hours with 3 time daily dosing. Benzamide and its derivatives are highly water-soluble but known to cross the blood-brain barrier, necessitating carrier-mediated transport.
Half Life
2.9–3.6 hours
Clearance
16.6 l/h.
Elimination Route
Urine (70% as unchanged tiapride)
Innovators Monograph
You find simplified version here Gramalil 10%
