Lorpiprazole

Absorption

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.

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.

The Uses of Lorpiprazole

Lorpiprazole is a triazole based compound with analgesic and anxiolytic activities.

Background

Lorpiprazole is a serotonin antagonist and reuptake inhibitor used for the treatment of major depressive disorder. It is a piperazinyl-triazole derivative.

Indications

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.

Pharmacokinetics

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.

Metabolism

Serotonin antagonists and reuptake inhibitors like lorpiprazole are metabolized in the liver by the CYP450 isoenzymes, mainly CYP2D6 and CYP3A4.