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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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (0)

              Serious - Use Alternative (4)

              • fexinidazole

                fexinidazole and asenapine transdermal both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels and/or prolong QT interval.

              • levodopa inhaled

                asenapine transdermal decreases effects of levodopa inhaled by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Atypical (2nd generation) antipsychotics inhibit dopamine D2 receptors in varying degrees (clozapine and quetiapine are lower risk). .

              • metoclopramide intranasal

                asenapine transdermal increases toxicity of metoclopramide intranasal by pharmacodynamic synergism. Avoid or Use Alternate Drug. Potential for additive effects, including increased frequency and severity of tardive dyskinesia, other extrapyramidal symptoms, and neuroleptic malignant syndrome.

              • selinexor

                selinexor, asenapine transdermal. unspecified interaction mechanism. Avoid or Use Alternate Drug. Patients treated with selinexor may experience neurological toxicities. Avoid taking selinexor with other medications that may cause dizziness or confusion.

              Monitor Closely (10)

              • fenfluramine

                asenapine transdermal decreases effects of fenfluramine by pharmacodynamic antagonism. Use Caution/Monitor. Potent serotonin receptor antagonists may decrease fenfluramine efficacy. If coadministered, monitor appropriately.

              • fluvoxamine

                fluvoxamine will increase the level or effect of asenapine transdermal by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Dose reduction may be necessary

              • fostemsavir

                asenapine transdermal and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.

              • lasmiditan

                lasmiditan, asenapine transdermal. Either increases effects of the other by sedation. Use Caution/Monitor. Coadministration of lasmiditan and other CNS depressant drugs, including alcohol have not been evaluated in clinical studies. Lasmiditan may cause sedation, as well as other cognitive and/or neuropsychiatric adverse reactions.

              • lemborexant

                lemborexant, asenapine transdermal. Either increases effects of the other by sedation. Modify Therapy/Monitor Closely. Dosage adjustment may be necessary if lemborexant is coadministered with other CNS depressants because of potentially additive effects.

              • oliceridine

                oliceridine, asenapine transdermal. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.

              • remimazolam

                remimazolam, asenapine transdermal. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely. Coadministration may result in profound sedation, respiratory depression, coma, and/or death. Continuously monitor vital signs during sedation and recovery period if coadministered. Carefully titrate remimazolam dose if administered with opioid analgesics and/or sedative/hypnotics.

              • sodium sulfate/?magnesium sulfate/potassium chloride

                sodium sulfate/?magnesium sulfate/potassium chloride increases effects of asenapine transdermal by unknown mechanism. Use Caution/Monitor. Closely monitor for evidence of enhanced CNS depression when using higher dose of magnesium sulfate together with a CNS depressant.

              • sodium sulfate/potassium sulfate/magnesium sulfate

                sodium sulfate/potassium sulfate/magnesium sulfate increases effects of asenapine transdermal by unknown mechanism. Use Caution/Monitor. Closely monitor for evidence of enhanced CNS depression when using higher dose of magnesium sulfate together with a CNS depressant.

              • voclosporin

                voclosporin, asenapine transdermal. Either increases effects of the other by QTc interval. Use Caution/Monitor.

              Minor (0)

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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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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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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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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.