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asenapine (Rx)Brand and Other Names:Saphris

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

sublingual tablet

  • 2.5mg
  • 5mg
  • 10mg
more...

Schizophrenia

5 mg SL q12hr initially; maintenance: after 1 week, may be increased up to 10 mg PO q12hr

Bipolar Disorder

Manic or mixed episodes associated with bipolar I disorder, either as monotherapy or as adjunct to lithium or valproate

Monotherapy: 10 mg PO q12hr initially; may be decreased to 5 mg PO q12hr on day 2 and subsequent days if warranted by adverse effects or individual tolerance (90% of patients typically remain on higher dose)

Adjunct to lithium or valproate: 5 mg PO q12hr initially; may be increased to 10 mg PO q12hr if warranted

If patient responds favorably, continue beyond initial acute phase (no recommendations at this time for duration of therapy)

Dosage Modifications

Renal impairment

  • Dose adjustment not necessary

Hepatic impairment

  • Mild to moderate impairment (Child-Pugh class A or B): Dose adjustment not necessary
  • Severe impairment (Child-Pugh class C): Contraindicated

Dosage Forms & Strengths

sublingual tablet

  • 2.5mg
  • 5mg
  • 10mg
more...

Bipolar Disorder

Indicated as monotherapy for acute treatment of manic or mixed episodes associated with bipolar I disorder

<10 years: Safety and efficacy not established

10-17 years: 2.5 SL q12hr initially; may increase to 5 mg SL q12hr after 3 days and to 10 mg SL q12hr after 3 additional days

Dosing Considerations

Pediatric patients are more sensitive to dystonia with initial dosing when recommended escalation schedule not followed

Safety and efficacy of doses >10 mg q12hr not established

Not indicated for dementia-related psychosis, in view of increased risk of death as compared with placebo (see Black Box Warnings)

In elderly patients with psychosis, asenapine exposure (area under curve [AUC]) was on average 40% higher than in younger adults

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Interactions

Interaction Checker

asenapine and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Somnolence (24%)

            Headache (12%)

            Dizziness (11%)

            Pediatric patients

            • Oral paraesthesia (27%)
            • Somnolence (49%)

            1-10%

            Extrapyramidal symptoms (EPS) other than akathisia (7%)

            Insomnia (6%)

            Weight gain (5%)

            Akathisia (4%)

            Anxiety (4%)

            Fatigue (4%)

            Oral hypoesthesia (4%)

            Dyspepsia (4%)

            Dry mouth (3%)

            Dysgeusia (3%)

            Arthralgia (3%)

            Toothache (3%)

            Depression (2%)

            Extremity pain (2%)

            Pediatric patients

            • Nausea (6%)
            • Abdominal pain (6%)
            • Fatigue (9%)
            • Increased weight (3%)
            • Hyperinsulinemia (2%)
            • Increased appetite (8%)
            • Headache (9%)
            • Dizziness (7%)
            • Dysgeusia (6%)
            • Akathisia (2%)
            • Insomnia (3%)
            • Suicidal ideation (3%)
            • Tachycardia (1%), Glossodynia (1%), Irritability (1%), Muscle pain (1%), Increased ALT (1%), Increased AST (1%), Dehydration (1%), Myalgia (1%), Parkinsonism (1%), Anger (1%), Dysmenorrhea (1%), Rash (1%), Nasal congestion (1%), Dyspnea (1%), Oropharyngeal pain (1%)

            Postmarketing Reports

            Sublingual administration: Application site reactions including oral ulcers, blisters, peeling/sloughing, and inflammation

            Choking reported by patients, some of whom may have also experienced oropharyngeal muscular dysfunction or hypoesthesia

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            Warnings

            Black Box Warnings

            Not indicated for dementia-related psychosis; increased risk of death in elderly patients with dementia-related psychosis; placebo-controlled trials with other atypical antipsychotics (ie, risperidone, aripiprazole, olanzapine) showed higher incidence of cerebrovascular adverse reactions (eg, cerebrovascular accidents [CVAs], transient ischemic attacks [TIAs]), including fatalities, in comparison with placebo

            Contraindications

            Known hypersensitivity

            Severe hepatic impairment (Child-Pugh C)

            Cautions

            Type 1 hypersensitivity reactions, including anaphylaxis and angioedema, have been reported (n=52), in several cases occurring after first dose; symptoms include anaphylaxis, angioedema, hypotension, tachycardia, tongue and laryngeal edema, difficulty breathing, wheezing, or rash

            Neuroleptic malignant syndrome associated with use; monitor for symptoms and discontinue if necessary

            Extrapyramidal symptoms, including acute dystonic reactions, pseudoparkinsonism, akathisia, and tardive dyskinesia reported

            Hyperglycemia (monitor patients with diabetes mellitus for worsening of glucose control)

            Weight gain may occur; monitor weight gain in pediatric patients and assess against that expected for normal growth

            Hypotension and syncope, especially early in treatment, because of drug's alpha1-antagonistic activity

            Leukopenia, neutropenia, and agranulocytosis reported with use

            Possible prolongation of QTc interval; avoid in patients with history of cardiac arrhythmias or other conditions that increase risk of torsades de pointes (eg, bradycardia, hypokalemia, hypomagnesemia)

            Coadministration with other drugs that prolong QTc interval may result in life-threatening arrhythmias (eg, class 1A antiarrhythmics [quinidine, procainamide], class 3 antiarrhythmics [amiodarone, sotalol], antipsychotics [ziprasidone, chlorpromazine, thioridazine], and antibiotics [moxifloxacin])

            Concurrent use of CNS-acting drugs or alcohol may increase toxicity

            Use caution in patients with history of seizures

            Cognitive or motor impairment may occur due to CNS depression

            Dysphagia, dysmotility, and aspiration may occur

            Potential disruption of body temperature regulation

            Not recommended with severe hepatic impairment (Child-Pugh class C)

            Inherent suicide risk with population treated warrants close supervision when drug therapy is changed

            May increase prolactin levels; significance unknown

            Atypical antipsychotic drugs have been associated with metabolic changes including hyperglycemia, dyslipidemia, and body weight gain, which may increase cardiovascular/ cerebrovascular risk; all of the drugs in the class have been shown to produce some metabolic changes but each drug has its own specific risk profile

            Monitor weight gain in pediatric patients and assess against that expected for normal growth

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            Pregnancy & Lactation

            Pregnancy category: C

            Neonates exposed to antipsychotic drugs during 3rd trimester of pregnancy are at risk for EPS or withdrawal symptoms after delivery; these complications vary in severity, with some being self-limited and others requiring ICU unit support and prolonged hospitalization

            Lactation: Excretion in milk unknown; use with caution

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Mechanism of action unknown; efficacy thought to be mediated via combined antagonist activity at dopamine D2 and serotonin type 2 (5-HT2) receptors

            Absorption

            Bioavailability: SL, 35%; swallowed, ≤2%

            Peak plasma time: 0.5-1.5 hr

            Peak plasma concentration: 4 ng/mL

            Distribution

            Protein bound: 95%

            Vd: 20-25 L/kg

            Metabolism

            Metabolized by UGT1A4 and CYP450 (predominantly isoenzyme 1A2)

            Enzymes inhibited: CYP2D6 (weakly)

            Elimination

            Half-life: 24 hr

            Clearance: 52 L/hr

            Excretion: Urine (50%), feces (40%)

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            Administration

            Instructions

            Sublingual tablet; to allow optimal absorption, place under tongue and allow to dissolve completely (dissolves within seconds)

            Do not chew, split, crush, or swallow sublingual tablet

            Do not eat or drink for at least 10 minutes after administration

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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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