Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (2)
- dronedarone
asenapine transdermal and dronedarone both increase QTc interval. Contraindicated.
- thioridazine
asenapine transdermal and thioridazine both increase QTc interval. Contraindicated.
Serious - Use Alternative (120)
- alfuzosin
asenapine transdermal and alfuzosin both increase QTc interval. Avoid or Use Alternate Drug.
- amiodarone
asenapine transdermal and amiodarone both increase QTc interval. Avoid or Use Alternate Drug.
- amisulpride
asenapine transdermal and amisulpride both increase QTc interval. Avoid or Use Alternate Drug.
- anagrelide
asenapine transdermal and anagrelide both increase QTc interval. Avoid or Use Alternate Drug.
- apomorphine
asenapine transdermal and apomorphine both increase QTc interval. Avoid or Use Alternate Drug.
- aripiprazole
asenapine transdermal and aripiprazole both increase QTc interval. Avoid or Use Alternate Drug.
- arsenic trioxide
asenapine transdermal and arsenic trioxide both increase QTc interval. Avoid or Use Alternate Drug.
- artemether
asenapine transdermal and artemether both increase QTc interval. Avoid or Use Alternate Drug.
- artemether/lumefantrine
asenapine transdermal and artemether/lumefantrine both increase QTc interval. Avoid or Use Alternate Drug.
- atomoxetine
asenapine transdermal and atomoxetine both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine
asenapine transdermal and buprenorphine both increase QTc interval. Avoid or Use Alternate Drug.
- ceritinib
asenapine transdermal and ceritinib both increase QTc interval. Avoid or Use Alternate Drug.
- chlorpromazine
asenapine transdermal and chlorpromazine both increase QTc interval. Avoid or Use Alternate Drug.
- clarithromycin
asenapine transdermal and clarithromycin both increase QTc interval. Avoid or Use Alternate Drug.
- clozapine
asenapine transdermal and clozapine both increase QTc interval. Avoid or Use Alternate Drug.
- dasatinib
asenapine transdermal and dasatinib both increase QTc interval. Avoid or Use Alternate Drug.
- degarelix
asenapine transdermal and degarelix both increase QTc interval. Avoid or Use Alternate Drug.
- desflurane
asenapine transdermal and desflurane both increase QTc interval. Avoid or Use Alternate Drug.
- disopyramide
asenapine transdermal and disopyramide both increase QTc interval. Avoid or Use Alternate Drug.
- dofetilide
asenapine transdermal and dofetilide both increase QTc interval. Avoid or Use Alternate Drug.
- dolasetron
asenapine transdermal and dolasetron both increase QTc interval. Avoid or Use Alternate Drug.
- donepezil
asenapine transdermal and donepezil both increase QTc interval. Avoid or Use Alternate Drug.
- droperidol
asenapine transdermal and droperidol both increase QTc interval. Avoid or Use Alternate Drug.
- efavirenz
asenapine transdermal and efavirenz both increase QTc interval. Avoid or Use Alternate Drug.
- eliglustat
asenapine transdermal and eliglustat both increase QTc interval. Avoid or Use Alternate Drug.
- encorafenib
asenapine transdermal and encorafenib both increase QTc interval. Avoid or Use Alternate Drug.
- entrectinib
asenapine transdermal and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
- eribulin
asenapine transdermal and eribulin both increase QTc interval. Avoid or Use Alternate Drug.
- erythromycin base
asenapine transdermal and erythromycin base both increase QTc interval. Avoid or Use Alternate Drug.
- erythromycin ethylsuccinate
asenapine transdermal and erythromycin ethylsuccinate both increase QTc interval. Avoid or Use Alternate Drug.
- erythromycin lactobionate
asenapine transdermal and erythromycin lactobionate both increase QTc interval. Avoid or Use Alternate Drug.
- erythromycin stearate
asenapine transdermal and erythromycin stearate both increase QTc interval. Avoid or Use Alternate Drug.
- escitalopram
asenapine transdermal and escitalopram both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- fingolimod
asenapine transdermal and fingolimod both increase QTc interval. Avoid or Use Alternate Drug.
- flecainide
asenapine transdermal and flecainide both increase QTc interval. Avoid or Use Alternate Drug.
- fluconazole
asenapine transdermal and fluconazole both increase QTc interval. Contraindicated.
- fluvoxamine
asenapine transdermal and fluvoxamine both increase QTc interval. Avoid or Use Alternate Drug.
- foscarnet
asenapine transdermal and foscarnet both increase QTc interval. Avoid or Use Alternate Drug.
- gemifloxacin
asenapine transdermal and gemifloxacin both increase QTc interval. Avoid or Use Alternate Drug.
- gilteritinib
asenapine transdermal and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.
- glasdegib
asenapine transdermal and glasdegib both increase QTc interval. Avoid or Use Alternate Drug.
- goserelin
asenapine transdermal and goserelin both increase QTc interval. Avoid or Use Alternate Drug.
- granisetron
asenapine transdermal and granisetron both increase QTc interval. Avoid or Use Alternate Drug.
- histrelin
asenapine transdermal and histrelin both increase QTc interval. Avoid or Use Alternate Drug.
- hydroxychloroquine sulfate
asenapine transdermal and hydroxychloroquine sulfate both increase QTc interval. Avoid or Use Alternate Drug.
- hydroxyzine
asenapine transdermal and hydroxyzine both increase QTc interval. Avoid or Use Alternate Drug.
- ibutilide
asenapine transdermal and ibutilide both increase QTc interval. Avoid or Use Alternate Drug.
- iloperidone
asenapine transdermal and iloperidone both increase QTc interval. Avoid or Use Alternate Drug.
- inotuzumab
asenapine transdermal and inotuzumab both increase QTc interval. Avoid or Use Alternate Drug.
- isoflurane
asenapine transdermal and isoflurane both increase QTc interval. Avoid or Use Alternate Drug.
- itraconazole
asenapine transdermal and itraconazole both increase QTc interval. Avoid or Use Alternate Drug.
- ivosidenib
asenapine transdermal and ivosidenib both decrease QTc interval. Avoid or Use Alternate Drug.
- lapatinib
asenapine transdermal and lapatinib both increase QTc interval. Avoid or Use Alternate Drug.
- lefamulin
asenapine transdermal and lefamulin both increase QTc interval. Avoid or Use Alternate Drug.
- leuprolide
asenapine transdermal and leuprolide both increase QTc interval. Avoid or Use Alternate Drug.
- 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). .
- levofloxacin
asenapine transdermal and levofloxacin both increase QTc interval. Avoid or Use Alternate Drug.
- lithium
asenapine transdermal and lithium both increase QTc interval. Avoid or Use Alternate Drug.
- loperamide
asenapine transdermal and loperamide both increase QTc interval. Avoid or Use Alternate Drug.
- lopinavir
asenapine transdermal and lopinavir both increase QTc interval. Avoid or Use Alternate Drug.
- macimorelin
asenapine transdermal and macimorelin both increase QTc interval. Avoid or Use Alternate Drug.
- maprotiline
asenapine transdermal and maprotiline both increase QTc interval. Avoid or Use Alternate Drug.
- mefloquine
asenapine transdermal and mefloquine both increase QTc interval. Avoid or Use Alternate Drug.
- methadone
asenapine transdermal and methadone both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- midostaurin
asenapine transdermal and midostaurin both increase QTc interval. Avoid or Use Alternate Drug.
- mifepristone
asenapine transdermal and mifepristone both increase QTc interval. Avoid or Use Alternate Drug.
- mirtazapine
asenapine transdermal and mirtazapine both increase QTc interval. Avoid or Use Alternate Drug.
- mobocertinib
mobocertinib and asenapine transdermal both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- moxifloxacin
asenapine transdermal and moxifloxacin both increase QTc interval. Avoid or Use Alternate Drug.
- nilotinib
asenapine transdermal and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.
- octreotide
asenapine transdermal and octreotide both increase QTc interval. Avoid or Use Alternate Drug.
- ofloxacin
asenapine transdermal and ofloxacin both increase QTc interval. Avoid or Use Alternate Drug.
- ondansetron
asenapine transdermal and ondansetron both increase QTc interval. Avoid or Use Alternate Drug. Avoid with congenital long QT syndrome; ECG monitoring recommended with concomitant medications that prolong QT interval, electrolyte abnormalities, CHF, or bradyarrhythmias.
- oxaliplatin
asenapine transdermal and oxaliplatin both increase QTc interval. Avoid or Use Alternate Drug.
- paliperidone
asenapine transdermal and paliperidone both increase QTc interval. Avoid or Use Alternate Drug.
- panobinostat
asenapine transdermal and panobinostat both increase QTc interval. Avoid or Use Alternate Drug. Panobinostat is known to significantly prolong QT interval. Panobinostat prescribing information states use with drugs known to prolong QTc is not recommended.
- paroxetine
asenapine transdermal and paroxetine both increase QTc interval. Avoid or Use Alternate Drug.
- pazopanib
asenapine transdermal and pazopanib both increase QTc interval. Avoid or Use Alternate Drug.
- pentamidine
asenapine transdermal and pentamidine both increase QTc interval. Avoid or Use Alternate Drug.
- pimavanserin
asenapine transdermal and pimavanserin both increase QTc interval. Avoid or Use Alternate Drug.
- pimozide
asenapine transdermal and pimozide both increase QTc interval. Contraindicated.
- pitolisant
asenapine transdermal and pitolisant both increase QTc interval. Avoid or Use Alternate Drug.
- ponesimod
asenapine transdermal and ponesimod both increase QTc interval. Avoid or Use Alternate Drug.
- posaconazole
asenapine transdermal and posaconazole both increase QTc interval. Contraindicated.
- primaquine
asenapine transdermal and primaquine both increase QTc interval. Avoid or Use Alternate Drug.
- procainamide
asenapine transdermal and procainamide both increase QTc interval. Avoid or Use Alternate Drug.
- promethazine
asenapine transdermal and promethazine both decrease QTc interval. Avoid or Use Alternate Drug.
- propafenone
asenapine transdermal and propafenone both increase QTc interval. Avoid or Use Alternate Drug.
- quinidine
asenapine transdermal and quinidine both increase QTc interval. Avoid or Use Alternate Drug.
- quinine
asenapine transdermal and quinine both increase QTc interval. Avoid or Use Alternate Drug.
- ranolazine
asenapine transdermal and ranolazine both increase QTc interval. Avoid or Use Alternate Drug.
- ribociclib
asenapine transdermal and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- risperidone
asenapine transdermal and risperidone both increase QTc interval. Avoid or Use Alternate Drug.
- romidepsin
asenapine transdermal and romidepsin both increase QTc interval. Avoid or Use Alternate Drug.
- saquinavir
asenapine transdermal and saquinavir both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- sertraline
asenapine transdermal and sertraline both increase QTc interval. Avoid or Use Alternate Drug.
- sevoflurane
asenapine transdermal and sevoflurane both increase QTc interval. Avoid or Use Alternate Drug.
- siponimod
asenapine transdermal and siponimod both increase QTc interval. Avoid or Use Alternate Drug.
- solifenacin
asenapine transdermal and solifenacin both increase QTc interval. Avoid or Use Alternate Drug.
- sotalol
asenapine transdermal and sotalol both increase QTc interval. Avoid or Use Alternate Drug.
- sunitinib
asenapine transdermal and sunitinib both increase QTc interval. Avoid or Use Alternate Drug.
- tacrolimus
asenapine transdermal and tacrolimus both increase QTc interval. Avoid or Use Alternate Drug.
- telavancin
asenapine transdermal and telavancin both increase QTc interval. Avoid or Use Alternate Drug.
- tetrabenazine
asenapine transdermal and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.
- thiothixene
asenapine transdermal and thiothixene both increase QTc interval. Avoid or Use Alternate Drug.
- toremifene
asenapine transdermal and toremifene both increase QTc interval. Avoid or Use Alternate Drug. Concurrent use of toremifene with agents causing QT prolongation should be avoided. If concomitant use is required it's recommended that toremifene be interrupted. If interruption not possible, patients requiring therapy with a drug that prolongs QT should be closely monitored. ECGs should be obtained for high risk patients.
- trazodone
asenapine transdermal and trazodone both increase QTc interval. Avoid or Use Alternate Drug.
- triptorelin
asenapine transdermal and triptorelin both increase QTc interval. Avoid or Use Alternate Drug.
- umeclidinium bromide/vilanterol inhaled
asenapine transdermal and umeclidinium bromide/vilanterol inhaled both decrease QTc interval. Avoid or Use Alternate Drug. Exercise extreme caution when vilanterol coadministered with drugs that prolong QTc interval; adrenergic agonist effects on the cardiovascular system may be potentiated
- vandetanib
asenapine transdermal and vandetanib both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration with drugs known to prolong QT interval; if a drug known to prolong QT interval must be used, more frequent ECG monitoring is recommended
- vardenafil
asenapine transdermal and vardenafil both increase QTc interval. Avoid or Use Alternate Drug.
- vemurafenib
asenapine transdermal and vemurafenib both increase QTc interval. Avoid or Use Alternate Drug.
- venlafaxine
asenapine transdermal and venlafaxine both decrease QTc interval. Avoid or Use Alternate Drug.
- vilanterol/fluticasone furoate inhaled
asenapine transdermal and vilanterol/fluticasone furoate inhaled both increase QTc interval. Avoid or Use Alternate Drug. Exercise extreme caution when vilanterol coadministered with drugs that prolong QTc interval; adrenergic agonist effects on the cardiovascular system may be potentiated
- voriconazole
asenapine transdermal and voriconazole both increase QTc interval. Avoid or Use Alternate Drug.
- vorinostat
asenapine transdermal and vorinostat both increase QTc interval. Avoid or Use Alternate Drug.
- ziprasidone
asenapine transdermal and ziprasidone both increase QTc interval. Avoid or Use Alternate Drug.
Monitor Closely (55)
- albuterol
asenapine transdermal and albuterol both increase QTc interval. Use Caution/Monitor.
- amitriptyline
asenapine transdermal and amitriptyline both increase QTc interval. Use Caution/Monitor.
- amoxapine
asenapine transdermal and amoxapine both increase QTc interval. Use Caution/Monitor.
- arformoterol
asenapine transdermal and arformoterol both increase QTc interval. Use Caution/Monitor.
- azithromycin
asenapine transdermal and azithromycin both increase QTc interval. Use Caution/Monitor.
- bedaquiline
asenapine transdermal and bedaquiline both increase QTc interval. Modify Therapy/Monitor Closely. ECG should be monitored closely
- chloroquine
asenapine transdermal and chloroquine both increase QTc interval. Use Caution/Monitor.
- ciprofloxacin
asenapine transdermal and ciprofloxacin both increase QTc interval. Use Caution/Monitor.
- citalopram
asenapine transdermal and citalopram both increase QTc interval. Use Caution/Monitor.
- clomipramine
asenapine transdermal and clomipramine both increase QTc interval. Use Caution/Monitor.
- crizotinib
asenapine transdermal and crizotinib both increase QTc interval. Use Caution/Monitor.
- daridorexant
asenapine transdermal and daridorexant both increase sedation. Modify Therapy/Monitor Closely. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.
- desipramine
asenapine transdermal and desipramine both increase QTc interval. Use Caution/Monitor.
- deutetrabenazine
asenapine transdermal and deutetrabenazine both increase QTc interval. Modify Therapy/Monitor Closely. For patients requiring deutetrabenazine doses >24 mg/day and are taking other drugs known to prolong QTc, assess the QTc interval before and after increasing the dose of deutetrabenazine or other medications known to prolong QTc.
- difelikefalin
difelikefalin and asenapine transdermal both increase sedation. Use Caution/Monitor.
- doxepin
asenapine transdermal and doxepin both increase QTc interval. Use Caution/Monitor.
- ezogabine
asenapine transdermal and ezogabine both increase QTc interval. Use Caution/Monitor. Slight and transient QT-prolongation observed, particularly when dose titrated to 1200mg/day. QT interval should be monitored when ezogabine is prescribed with agents known to increase QT interval.
- 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.
- fluoxetine
asenapine transdermal and fluoxetine both increase QTc interval. Modify Therapy/Monitor Closely.
- fluphenazine
asenapine transdermal and fluphenazine both increase QTc interval. Use Caution/Monitor.
- 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
- formoterol
asenapine transdermal and formoterol both increase QTc interval. Use Caution/Monitor.
- fostemsavir
asenapine transdermal and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.
- ganaxolone
asenapine transdermal and ganaxolone both increase sedation. Use Caution/Monitor.
- gemtuzumab
asenapine transdermal and gemtuzumab both increase QTc interval. Use Caution/Monitor.
- haloperidol
asenapine transdermal and haloperidol both increase QTc interval. Use Caution/Monitor.
- imipramine
asenapine transdermal and imipramine both increase QTc interval. Use Caution/Monitor.
- indacaterol, inhaled
asenapine transdermal and indacaterol, inhaled both increase QTc interval. Use Caution/Monitor.
- indapamide
asenapine transdermal and indapamide both increase QTc interval. Use Caution/Monitor.
- isradipine
asenapine transdermal and isradipine both increase QTc interval. Use Caution/Monitor.
- 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.
- lenvatinib
asenapine transdermal and lenvatinib both increase QTc interval. Use Caution/Monitor.
- lofexidine
asenapine transdermal and lofexidine both increase QTc interval. Use Caution/Monitor.
- nortriptyline
asenapine transdermal and nortriptyline both increase QTc interval. Use Caution/Monitor.
- olanzapine
asenapine transdermal and olanzapine both increase QTc interval. Use Caution/Monitor. Limited data, including some case reports, suggest that olanzapine may be associated with a significant prolongation of the QTc interval in rare instances
- 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.
- olodaterol inhaled
asenapine transdermal and olodaterol inhaled both increase QTc interval. Use Caution/Monitor. Drugs that prolong the QTc interval and may potentiate the effects of beta2 agonists on the cardiovascular system; increased risk of ventricular arrhythmias
- osilodrostat
asenapine transdermal and osilodrostat both increase QTc interval. Use Caution/Monitor. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval
- osimertinib
asenapine transdermal and osimertinib both increase QTc interval. Use Caution/Monitor.
- ozanimod
asenapine transdermal and ozanimod both increase QTc interval. Modify Therapy/Monitor Closely. The potential additive effects on heart rate, treatment with ozanimod should generally not be initiated in patients who are concurrently treated with QT prolonging drugs with known arrhythmogenic properties.
- pasireotide
asenapine transdermal and pasireotide both increase QTc interval. Modify Therapy/Monitor Closely.
- perphenazine
asenapine transdermal and perphenazine both increase QTc interval. Use Caution/Monitor.
- prochlorperazine
asenapine transdermal and prochlorperazine both decrease QTc interval. Use Caution/Monitor.
- protriptyline
asenapine transdermal and protriptyline both increase QTc interval. Use Caution/Monitor.
- quetiapine
asenapine transdermal and quetiapine both increase QTc interval. Use Caution/Monitor.
- 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.
- rilpivirine
asenapine transdermal and rilpivirine both increase QTc interval. Use Caution/Monitor.
- selpercatinib
asenapine transdermal and selpercatinib both increase QTc interval. Use Caution/Monitor.
- 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.
- sorafenib
asenapine transdermal and sorafenib both increase QTc interval. Use Caution/Monitor.
- triclabendazole
asenapine transdermal and triclabendazole both increase QTc interval. Use Caution/Monitor.
- trimipramine
asenapine transdermal and trimipramine both increase QTc interval. Use Caution/Monitor.
- voclosporin
voclosporin, asenapine transdermal. Either increases effects of the other by QTc interval. Use Caution/Monitor.
Minor (0)
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
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
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
- Monitors pregnancy outcomes in women exposed to atypical antipsychotics during pregnancy
- For more information contact the National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-andresearch-programs/pregnancyregistry/
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.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%)
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)
Images
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
