Lurasidone

pharmacological · nervous · Oral

Lurasidone. Second-generation antipsychotic with high-affinity D2 and 5-HT2A antagonism, 5-HT7 antagonism, 5-HT1A partial agonism, and negligible… Oral half-life 18 h.

Second-generation antipsychotic with high-affinity D2 and 5-HT2A antagonism, 5-HT7 antagonism, 5-HT1A partial agonism, and negligible H1 / M1 / α1 activity — predicts a favourable metabolic and sedation profile relative to older atypicals. Oral bioavailability is ~2× with a ≥350 kcal meal; FDA labelling requires food co-administration.

PK: V 420 L IS REFUTED BY ITS OWN CITATION, WHICH STATES A DIFFERENT NUMBER — "apparent volume of distribution of 6173 L". That published figure is now carried with F pinned to 1, because the abstract calls it APPARENT and pairing 6173 with the label 15% would manufacture a textbook double-division. F 0.15 IS NOT IN PUBMED AT ALL: a title-and-abstract search for lurasidone bioavailability returns zero records for the marketed product, so it is label-only — and it is the FASTED figure for a drug whose label REQUIRES food, under which exposure roughly doubles. The measured value is recorded here rather than stored. ka 2.02 is a BACK-DERIVATION reproducing 2.00 h, the exact midpoint of its cited "1-3 h" — class 4 inverted through class 9. That same 2.02 sits on quetiapine, which I had flagged as a cross-drug transplant; it is not, because 2.02 reproduces 1.50 h there, each drug own Tmax. The half-life of 18 h verifies verbatim.

Pharmacokinetics

Sources: PMID:27722855, PMID:20404009, PMID:28695535