Asenapine
Asenapine. Atypical antipsychotic; very high-affinity D2 / 5-HT2A antagonist with a broad multireceptor profile. Given SUBLINGUALLY because… Sublingual half-life 24 h.
Atypical antipsychotic; very high-affinity D2 / 5-HT2A antagonist with a broad multireceptor profile. Given SUBLINGUALLY because swallowed oral bioavailability is near-zero (<2%, extensive first-pass); SL F ~35%. Also a once-daily transdermal patch.
PK: THE PATCH CARRIED THE SUBLINGUAL BIOAVAILABILITY. F 0.35 is verbatim for the sublingual tablet ("Total bioavailability is 35%") and was copied onto the transdermal row, where the source reports only RELATIVE bioavailability - the 3.8 mg/24 h patch matches 10 mg/day sublingual on AUC, implying a patch availability near 0.92. As stored the patch delivered 2.0 mg/day against the sublingual 3.5, a 2.6x under-delivery on the marketed product. Because patch strengths are already expressed as DELIVERED mg/24 h, F is pinned to 1 rather than set to a figure nobody published. TD t-half 33 was a TRUNCATION of "Terminal half-life ... was 33.9 hours", measured on the 1.9 mg/24 h patch, the lowest and non-marketed strength. Both sublingual values were verbatim under the WRONG citation and now point at the papers that state them. V 1500 L survives unsourced and is declared so: the search for an asenapine volume of distribution returns ZERO PubMed records, and the default is worse than a label figure. ka 5.23 is an exact inversion of "a T (max) value of about 1 h" - three significant figures extracted from the word about.
Pharmacokinetics
- Sublingual — t½ 24 h · F 35% · ka 5.23 h⁻¹ · Vd 1500 L
- Transdermal — t½ 33.9 h · F 100% · Vd 1500 L
Sources: PMID:22936407, PMID:24793403, PMID:33734167, PMID:18308814, PMID:8935801, PMID:32943849