Brands, Medical Use, Clinical Data
Drug Category
- Antipsychotics
- Phenothiazines
Dosage Forms
- Tablet (10 mg, 25 mg, 50 mg, 100 mg) for oral administration
- Ampuls (1 mL) for intramuscular administration
- Concentrate for oral administration
Brands / Synonyms
Calodal; Lidanar; Lidanil; Serentil; Serentil Concentrate; Thioridazien Thiomethyl Sulfoxide; Thioridazine Monosulfoxide Analog; Thioridazine Thiomethyl Sulfoxide; TPS-23; TPS23
Indications
Used in the treatment of schizophrenia, organic brain disorders, alcoholism and psychoneuroses.
Pharmacology
Mesoridazine, the besylate salt of a metabolite of thioridazine, is a phenothiazine tranquilizer. Pharmacological studies in laboratory animals have established that mesoridazine has a spectrum of pharmacodynamic actions typical of a major tranquilizer. In common with other tranquilizers it inhibits spontaneous motor activity in mice, prolongs thiopental and hexobarbital sleeping time in mice and produces spindles and block of arousal reaction in the EEG of rabbits. It is effective in blocking spinal reflexes in the cut and antagonizes d-amphetamine excitation and toxicity in grouped mice. It shows a moderate adrenergic blocking activity in vitro and in vivo and antagonizes 5-hydroxytryptamine in vivo. Intravenously administered, it lowers the blood pressure of anesthetized dogs. It has a weak antiacetylcholine effect in vitro.
Mechanism of Action
Based upon animal studies, mesoridazine, as with other phenothiazines, acts indirectly on reticular formation, whereby neuronal activity into reticular formation is reduced without affecting its intrinsic ability to activate the cerebral cortex. In addition, the phenothiazines exhibit at least part of their activities through depression of hypothalamic centers. Neurochemically, the phenothiazines are thought to exert their effects by a central adrenergic blocking action.
Absorption
Well absorbed from the gastrointestinal tract.
Toxicity
Oral LD50 is 560 ± 62.5 mg/kg and 644 ± 48 mg/kg in mouse and rat, respectively. Symptoms of overdose may include emesis, muscle tremors, decreased food intake and death associated with aspiration of oral-gastric contents into the respiratory system.
Biotrnasformation / Drug Metabolism
Not Available
Contraindications
As with other phenothiazines, Serentil® (mesoridazine besylate) is contraindicated in severe
central nervous system depression or comatose states from any cause including drug induced central nervous system
depression .
Serentil® (mesoridazine besylate) is contraindicated in individuals who have previously shown
hypersensitivity to the drug.
Drug Interactions
No information provided.
|
