section name header

Pronunciation

a-SEN-a-peen

Classifications

Therapeutic Classification: antipsychotics, mood stabilizers

Pharmacologic Classification: dibenzo oxepino pyrroles

Indications

BEERS REMS


Action

  • May act through combined antagonism of dopaminergic (D2) and 5-HT2A receptors.
Therapeutic effects:
  • Decreased symptoms of acute schizophrenia and mania/mixed episodes of bipolar I disorder.

Pharmacokinetics

Absorption: 35% absorbed following SL administration; 60% released from transdermal system.

Distribution: Extensively distributed to extravascular tissues.

Protein Binding: 95%

Metabolism/Excretion: Primarily metabolized by CYP1A2 and UGTA14 enzyme systems; 50% excreted in urine, 40% in feces, primarily as metabolites.

Half-Life: 24 hr.

Time/Action Profile

(plasma concentrations)

ROUTEONSETPEAKDURATION
SLunknown0.5–1.5 hr12 hr
TDunknown12–24 hr24 hr



Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: bradycardia, orthostatic hypotension, QT interval prolongation, tachycardia

Endo: hyperglycemia, hyperprolactinemia

GI: oral hypoesthesia, dry mouth, dyspepsia, dysphagia, oral blisters, oral inflammation, oral peeling/sloughing, oral ulcers

Hemat: AGRANULOCYTOSIS, leukopenia, neutropenia

Local: application site reactions ( in African Americans)

Metab: weight gain, appetite, dyslipidemia

Neuro: akathisia, dizziness, drowsiness, extrapyramidal symptoms, anxiety, fatigue, NEUROLEPTIC MALIGNANT SYNDROME, SEIZURES, SUICIDAL THOUGHTS, syncope, tardive dyskinesia

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions

Drug-drug:

Route/Dosage

Schizophrenia

Acute Manic/Mixed Episodes Associated with Bipolar I Disorder

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Saphris, Secuado

Code

NDC Code