asenapine transdermal (Rx)

Brand and Other Names:Secuado
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

transdermal system

3.8mg/24hr

5.7mg/24hr

7.6mg/24hr

Schizophrenia

Atypical antipsychotic indicated for adults with schizophrenia

Apply 3.8 mg/24 hr patch initially; may increase dosage to 5.7 mg/24 hr or 7.6 mg/24 hr after 1 week

Dosage Modifications

Renal impairment

  • Mild-to-severe (GFR 15-90 mL/min): No dosage adjustment necessary
  • Patients on dialysis: Not studied
  • Effect of renal function on the excretion of other metabolites has not been studied

Hepatic impairment

  • Mild-to-moderate (Child-Pugh A or B): No dosage adjustment necessary
  • Severe (Child-Pugh C): Contraindicated

Dosing Considerations

In a short-term, placebo-controlled trial, no suggestion of added benefit was found at a dosage of 7.6 mg/24 hr; there was an increase in certain adverse reactions

Safety of doses >7.6 mg/24 hr has not been evaluated in clinical studies

Based on AUC of asenapine, asenapine transdermal 3.8 mg/24 hr corresponds to 5 mg PO BID of sublingual (SL) asenapine and asenapine transdermal 7.6 mg/24 hr corresponds to 10 mg PO BID of SL asenapine

Safety and efficacy not established

Schizophrenia

Based on a pharmacokinetic study in elderly patients with asenapine SL, dosage adjustments are not recommended based on age alone

Exposure in elderly patients is 30-40% higher as compared with adults

Not indicated for dementia-related psychosis

May increase risk of mortality in elderly patients with dementia-related psychosis

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Interactions

Interaction Checker

and asenapine transdermal

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Application site reactions (14-15%)

            Extrapyramidal symptoms (8-13%)

            1-10%

            Headache (9%)

            Increased weight (4-6%)

            Constipation (4-5%)

            Akathisia (4%)

            Somnolence (3-4%)

            Increased hepatic transaminases >3x ULN (1.6-3.1%)

            Dyspepsia (1-3%)

            Diarrhea (1-3%)

            Blood glucose increased (1-3%)

            Dystonia (1-3%)

            Nasopharyngitis (1-3%)

            Upper respiratory tract infection (1-3%)

            Creatine kinase elevations ≥3 x ULN at any time (1.6-2.1%)

            Hypertension (2%)

            Vomiting (<2%)

            Dry mouth (<2%)

            Asthenia (<2%)

            Myalgia (<2%)

            Increased prolactin levels (1.3%)

            <1%

            Anemia

            Temporary bundle-branch block

            Accommodation disorder

            Swollen tongue

            Hyponatremia

            Dysarthria

            Thrombocytopenia

            Postmarketing Reports

            Choking

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            Warnings

            Increased mortality and dementia-related psychosis

            Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death

            Not approved for treatment of dementia-related psychosis

            Contraindications

            Severe hepatic impairment (Child-Pugh C)

            Hypersensitivity to asenapine or any components of the transdermal system

            Cautions

            Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death; in placebo-controlled trials, patients, especially those taking atypical antipsychotic drugs, showed an increased risk of death in treated patients (1.6-1.7x) compared with placebo patients

            Neuroleptic malignant syndrome associated with use; monitor for symptoms; discontinue if suspected, and provide intensive symptomatic treatment and monitoring

            In placebo-controlled trials in elderly subjects with dementia, patients randomized to risperidone, aripiprazole, and olanzapine had a higher incidence of stroke and transient ischemic attack, including fatal stroke

            Not approved for treatment of dementia-related psychosis

            Atypical antipsychotic drugs, including asenapine transdermal, have caused metabolic changes, including hyperglycemia, diabetes mellitus, dyslipidemia, and body weight gain

            Hypersensitivity reactions have been observed

            Atypical antipsychotics cause orthostatic hypotension and syncope; risk is greatest during initial dose titration and when increasing the dose

            May cause somnolence, postural hypotension, motor instability, and sensory instability, which may lead to falls and, consequently, fractures or other injuries; complete fall risk assessments in patients with diseases, conditions, or medications that could exacerbate these effects, when initiating antipsychotic treatment and recurrently for patients on long-term antipsychotic therapy

            Leukopenia, neutropenia, and agranulocytosis reported with use; perform a CBC count during first few months of therapy; in such patients, consider discontinuation of therapy at first sign of clinically significant decline in WBC count in absence of other causative factors

            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)

            Can elevate prolactin levels, and elevation can persist during long-term administration; hyperprolactinemia may suppress hypothalamic GnRH, resulting in reduced pituitary gonadotropin secretion; this, in turn, may inhibit reproductive function by impairing gonadal steroidogenesis in both female and male patients

            Use with caution in patients with a history of seizures or with conditions that potentially lower the seizure threshold; conditions that lower the seizure threshold may be more prevalent in patients ≥65 years

            Potential disruption of body temperature regulation

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

            Dysphagia, esophageal dysmotility, and aspiration may occur

            Both the rate and extent of absorption are increased when heat is applied to application; avoid exposing patch to direct external heat sources (eg, hair dryers, heating pads, electric blankets, heated water beds)

            Local skin reactions, such as irritation, were reported

            Tardive dyskinesia

            • Tardive dyskinesia may develop in patients treated with antipsychotic drugs, including asenapine transdermal
            • Risk appears highest among elderly patients, especially elderly women, but it is not possible to predict which patients are likely to develop the syndrome
            • Reserve long-term antipsychotic treatment for patients who have a chronic illness that is responsive to antipsychotic drugs, or in patients in whom effective alternative therapies are not available or appropriate
            • In patients who do require long-term treatment, use lowest dose and shortest duration of treatment producing a satisfactory clinical response; periodically reassess if it needs to be continued
            • If signs and symptoms of tardive dyskinesia appear, consider discontinuing treatment

            Drug interaction overview

            • Asenapine is a CYP1A2 and UGT1A4 substrate; weak CYP2D6 inhibitor
            • Coadministration of asenapine with a CYP1A2 inhibitor increases AUC and plasma levels of asenapine; reduce dose based on clinical response, if necessary
            • Owing to its alpha1-adrenergic antagonism with potential for inducing hypotension, asenapine may enhance the effects of certain antihypertensive agents; monitor blood pressure and adjust dosage of antihypertensive drug accordingly
            • 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])
            • Asenapine may enhance inhibitory effects of paroxetine on its own metabolism by CYP2D6; concomitant use with paroxetine increases paroxetine AUC and plasma levels; reduce paroxetine dose by half when used in combination with asenapine
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            Pregnancy & Lactation

            Pregnancy

            Studies have not been conducted in pregnant women

            No human data available informing the drug-associated risk

            Animal data

            • In a pre-and post-natal study in rats, IV administration of asenapine at doses up to 0.7 times the MRHD of 10 mg of sublingual asenapine twice daily produced increases in postimplantation loss and early pup deaths, and decreases in subsequent pup survival and weight gain
            • Doses were up to 1.1x the maximum recommended human dose (MRHD) of 12.8 mg transdermal asenapine daily.
            • Advise pregnant women of the potential risk to a fetus

            Pregnancy exposure registry

            Clinical considerations

            • Extrapyramidal and/or withdrawal symptoms, including agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress and feeding disorder have been reported in neonates who were exposed to antipsychotic drugs during the third trimester of pregnancy
            • Symptoms have varied in severity
            • Some neonates recovered within hours or days without specific treatment; others required prolonged hospitalization; monitor neonates for extrapyramidal and/or withdrawal symptoms and manage symptoms appropriately

            Lactation

            Studies have not been conducted to assess the presence of asenapine in human milk, the effects of asenapine on the breastfed infant, or the effects of asenapine on milk production

            Asenapine is excreted in rat milk

            Consider developmental and health benefits of breastfeeding along with the mother's clinical need for asenapine transdermal and any potential adverse effects on the breastfed infant from asenapine transdermal or from the underlying maternal condition

            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 is unknown

            Efficacy thought to be mediated via combined antagonist activity at dopamine D2 and serotonin type 2 (5-HT2) receptors

            Absorption

            Peak plasma time: 12-24 hr

            Steady-state plasma concentrations are achieved in ~72 hr after the first application

            Application of a heating pad on asenapine transdermal patch for 8 hr led to a faster absorption rate (median peak plasma time ~8 hr) as compared with no heating pad

            Distribution

            Protein bound: 95% (including albumin and alpha1-acid glycoprotein)

            Vd: 20-25 L/kg

            Metabolism

            Direct glucuronidation by UGT1A4

            Oxidative metabolism predominantly by CYP1A2

            Elimination

            Half-life: 30 hr

            Excretion: Urine (~50%); feces (40%)

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            Administration

            Transdermal Administration

            Transdermal use only

            Apply patch every 24 hr; do not wear longer than 24 hr

            Apply to clean, dry, and intact skin at the selected application sites: hip, abdomen, upper arm, or upper back area

            Wear only 1 patch at any time

            Apply to a different application site each time a new patch is applied

            Do not cut open the pouch until ready to apply; do not use if the individual pouch seal is broken or appears to be damaged

            Apply whole transdermal patch; do not cut

            If patch lifts at the edges, reattach by pressing firmly and smoothing down the edges of the patch

            If patch comes off completely, apply a new one

            After use, fold used patch so that the adhesive side sticks to itself and safely discard

            If irritation or a burning sensation occurs while wearing patch, remove and apply a new patch to a new application site

            Showering is permitted, but use during swimming or taking a bath has not been evaluated

            Do not apply external heat sources (eg, heating pad) over the patch

            Storage

            Store at room temperature 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)

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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
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            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.