5-HT7 antagonist
5-HT7 serotonin receptor antagonist
- Receptors in cortex, thalamus and the circadian clock
- May enhance antidepressant/cognitive signaling
- May advance circadian phase
5-HT7 antagonist (1/2)
- Little is proven
- Possible cognitive benefit
- Possible early waking due to phase-advance
- Possible constipation
- Possible mitigation of antipsychotic-induced metabolic syndrome
- Possible ↑ neurogenesis & synaptic plasticity
- Potentially ↓ tau hyperphosphorylation and ↓ β-amyloid–induced toxicity
5-HT7 antagonist (2/2)
- Vortioxetine (Trintellix) is a neutral antagonist that does not block constitutive activity at 5-HT7 receptors—possible cognitive benefit but not theorized to prevent Alzheimer’s The red symbols flanking the peg represent microtubules in alignment (as opposed to tau tangles as seen in Alzheimer’s). The design is not intended to overvalue an unproven effect, but for memorability of an otherwise unremarkable mechanism.
Drugs with this mechanism (22)
- Aripiprazole — D2 partial agonist; weight-favorable, activating, low prolactin; can cause akathisia.
- Aripiprazole lauroxil LAI — Long-acting aripiprazole prodrug injection for schizophrenia; requires a loading strategy.
- Aripiprazole lauroxil LAI — Rapid-start aripiprazole lauroxil injection used only to initiate Aristada treatment.
- Aripiprazole monohydrate LAI — Extended-interval aripiprazole LAI for schizophrenia and bipolar maintenance.
- Aripiprazole monohydrate LAI — Long-acting aripiprazole for schizophrenia and bipolar maintenance; akathisia remains prominent.
- Asenapine — Sublingual/transdermal atypical; oral tablets are ineffective if swallowed.
- Asenapine transdermal — Once-daily asenapine patch - the only transdermal antipsychotic.
- Dehydroaripiprazole — Aripiprazole's long-lived active metabolite, with the same D2 partial agonism and a large share of steady-state exposure.
- Lurasidone — Weight-favorable atypical; must be taken with a 350-kcal meal.
- Paliperidone — Active metabolite of risperidone; extended-release oral and long-acting injectables.
- Paliperidone palmitate LAI — Long-acting paliperidone palmitate injection for schizophrenia-spectrum maintenance.
- Paliperidone palmitate LAI — Longest-interval paliperidone depot; requires prior stability on a shorter formulation.
- Paliperidone palmitate LAI — Long-acting paliperidone injection for schizophrenia and schizoaffective disorder.
- Paliperidone palmitate LAI — Extended-interval paliperidone LAI for schizophrenia; prior stabilization on a shorter formulation is required.
- Risperidone — Widely used atypical; dose-related EPS and the class's greatest prolactin burden.
- Risperidone LAI — Microsphere antipsychotic depot; delayed release requires oral overlap and relatively frequent injections.
- Risperidone LAI — Subcutaneous long-acting risperidone for schizophrenia; no oral supplementation after injection.
- Risperidone LAI — Long-acting risperidone depot for schizophrenia; formulated without a prolonged oral bridge.
- Risperidone LAI — Long-acting risperidone microsphere injection for schizophrenia and bipolar I maintenance.
- Risperidone LAI — Subcutaneous extended-release risperidone; no loading dose or oral overlap after initiation.
- Trifluoperazine — High-potency first-generation antipsychotic; low metabolic burden but high movement risk.
- Vortioxetine — Multimodal serotonergic antidepressant; cognitive benefits and less sexual dysfunction, but dose-related nausea.
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