Asenapine

SAPHRIS

Open Asenapine in the interactive console ↗

Pronunciation: a-SEN-a-peen

Asenapine ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Asenapine ballicule

Asenapine SAPHRIS mascot mnemonic cartoon — Visual mnemonic: Asenapine mascot
**“Sapphire (for this) Ass in a pine”**
Antipsychotics are represented with spooky mascots
Saphris is sublingual

What it isSecond-generation antipsychotic; schizophrenia and bipolar disorder.

Why this oneSublingual and transdermal routes bypass first-pass metabolism, which suits poor oral adherence.

What limits itMust not be swallowed and nothing eaten or drunk for ten minutes. Oral hypoesthesia and dysgeusia.

Asenapine molecular structure (skeletal formula) — Molecular structure: Asenapine

Asenapine prescription history

Animated chart of estimated U.S. prescriptions per year, Antipsychotics (1954–2026). Asenapine enters in 2009 (estimated).

FDA-approved for

schizophrenia (2009)
bipolar mania (2009)

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability2 / 4

Sedation liability2 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityMetabolic effects, extrapyramidal symptoms/tardive dyskinesia and agent-specific QT or orthostatic risk.

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Increased mortality in elderly patients with dementia-related psychosis.

FDA dosing	Population	Start	Target	Max
Schizophrenia, acute	adults	5 mg SL BID	5 mg SL BID	10 mg SL BID
Schizophrenia, maintenance	adults	5 mg SL BID	5-10 mg SL BID	10 mg SL BID
Bipolar I mania, monotherapy (acute & maintenance)	adults	5-10 mg SL BID	5-10 mg SL BID	10 mg SL BID
Bipolar I mania, monotherapy	peds 10-17 y	2.5 mg SL BID	2.5-10 mg SL BID	10 mg SL BID
Bipolar I mania, adjunct to lithium/valproate	adults	5 mg SL BID	5-10 mg SL BID	10 mg SL BID

Titration Schizophrenia: may increase to 10 mg SL BID after ≥1 week if tolerated.

Renal No adjustment needed

Hepatic Severe (Child-Pugh C): contraindicated; mild-moderate: no adjustment.

Instructions

Place sublingual tablet under the tongue and let it dissolve completely (dissolves within seconds).
Do not split, crush, chew, or swallow the tablet.
No eating or drinking for 10 minutes after administration.

Available strengths

SL tab 2.5, 5, 10 mg
patch 3.8, 5.7, 7.6 mg/24 hr

Contraindications

Severe hepatic impairment (Child-Pugh C)

Cautions

Elderly dementia-related psychosis: increased cerebrovascular events
Neuroleptic malignant syndrome
Tardive dyskinesia
Metabolic changes: hyperglycemia/diabetes, dyslipidemia, weight gain
Orthostatic hypotension and syncope
Leukopenia, neutropenia, agranulocytosis
QT interval prolongation — avoid other QT-prolonging drugs
Hyperprolactinemia
Seizures
Hypersensitivity reactions (anaphylaxis, angioedema)

Adverse reactions

Akathisia
Oral hypoesthesia
Somnolence
Dizziness
Extrapyramidal symptoms

Pregnancy Third-trimester exposure: risk of neonatal extrapyramidal and/or withdrawal symptoms; no human data.

Lactation No human data; excreted in rat milk.

Cost

Asenapine (SAPHRIS)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $/mo	CostPlus
2.5 mg	SL tab	60 BID	$185.28	offered
5 mg	SL tab	60 BID	$121.95	offered
10 mg	SL tab	60 BID	$157.63	offered

Other forms: Asenapine transdermal (SECUADO)

Generic entry2033 est.

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Memory aids: interaction avatars

CYP1A2 substrate

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Self-check

After sublingual asenapine, how long must food and drink be avoided?
Ten minutes.
Why do sublingual and transdermal asenapine routes help?
They bypass first-pass metabolism.