Lorpiprazole
Lorpiprazole Uses, Dosage, Side Effects, Food Interaction and all others data.
Lorpiprazole is a serotonin antagonist and reuptake inhibitor used for the treatment of major depressive disorder. It is a piperazinyl-triazole derivative.
Drugs like lorpiprazole that fit in the category of serotonin antagonists and reuptake inhibitors present a wide variety of effects when administered. They inhibit serotonin receptors like 5-HT2A as well as prevent the reuptake of serotonin, norepinephrine and dopamine. Additionally, they antagonize some adrenergic receptors. This diverse functional profile allows lorpiprazole to have a large therapeutic spectrum from symptom control as an adjuvant of other drugs to control of depressive syndromes as a monotherapy.
| Trade Name | Lorpiprazole |
| Generic | Lorpiprazole |
| Lorpiprazole Other Names | Lorpiprazole |
| Type | |
| Formula | C21H26F3N5 |
| Weight | Average: 405.469 Monoisotopic: 405.214030346 |
| Protein binding | The plasma protein binding of serotonin antagonists and reuptake inhibitors like lorpiprazole is expected to be very high and correspond to even 89-99% of the administered dose. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
In 2016, lorpiprazole was classified in the "Chemical structure-related drug-like criteria of global approved drugs" as an antipsychotic and anxiolytic. An antipsychotic is a medication used to treat a state of delusion, hallucination, paranoia or disordered thought. On the other hand, an anxiolytic is a medication used for the treatment of severe, chronic or debilitating anxiety. The anxiety state can be defined as an unpleasant state of tension, apprehension or uneasiness.
How Lorpiprazole works
Lorpiprazole is a serotonin antagonist and reuptake inhibitor thus, its activity is performed by antagonizing the 5-HT2A and the 5-HT2C serotoninergic receptors as well as the alpha1 and alpha2 adrenergic receptors, H1 histaminergic receptors and at high doses, inhibiting the SERT serotonin transporter.
Toxicity
The serotonin antagonists and reuptake inhibitors' side effects are minor with rare reports of cardiotoxicity. They have been reported to cause an unbalance between the sympathetic and parasympathetic system. There are also reports regarding a potential hepatotoxic effect of this drugs.
Volume of Distribution
The serotonin antagonists and reuptake inhibitors as lorpiprazole are quickly distributed through the blood-brain-barrier getting concentrated in the brain to even higher levels than the ones found in plasma.
Elimination Route
After oral administration, the serotonin antagonist and reuptake inhibitors are rapidly absorbed in the gastrointestinal tract. This absorption can be slow down depending on the type of diet. The maximum plasma concentration of this kind of drugs occurs approximately 1 hour after administration.
Half Life
The estimated half-life for drugs like lorpiprazole, a serotonin antagonist and reuptake inhibitor, is in the range of 11-23 hours.
Elimination Route
The elimination of drugs that fit in the category of serotonin antagonists and reuptake inhibitors like lorpiprazole is expected to have a biphasic profile in which most of the metabolized drug should be disposed of by the urine.
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