asenapine

Contraindicated in:

Hypersensitivity;
Dementia-related psychoses;
Severe hepatic impairment.

Use Cautiously in:

History of cardiac arrhythmias, congenital QT prolongation, electrolyte abnormalities (especially hypomagnesemia or hypokalemia; correct prior to use), or concurrent use of medications known to prolong the QTc interval (may ↑ risk of life-threatening arrhythmias);
History of seizures or conditions/medications known to ↓ seizure threshold;
History of leukopenia/neutropenia;
Strenuous exercise, exposure to extreme heat, concurrent medications with anticholinergic activity, or risk of dehydration;
History of suicide attempt;
Dehydration, hypovolemia, concurrent use of antihypertensive medications, or history of MI/ischemic heart disease/HF/conduction abnormalities/cerebrovascular disease (↑ risk of hypotension);
Patients at risk for falls;
History of breast cancer;
OB: Neonates at ↑ risk for extrapyramidal symptoms and withdrawal after delivery when exposed during the 3rd trimester; use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Safety not established in breastfeeding;
Pedi: Children <10 yr (safety and effectiveness not established);
Geri:
Appears on Beers list. ↑ risk of stroke, cognitive decline, and mortality in older adults with dementia. Avoid use in older adults, except for schizophrenia or bipolar disorder (not indicated for dementia-related psychosis)
.

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 Black people)

Metab: weight gain, ↑appetite, dyslipidemia

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

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

QTc interval prolonging drugs, including Class 1A antiarrhythmics such as quinidine and procainamide; Class 3 antiarrhythmics, including amiodarone and sotalol; other antipsychotics, including ziprasidone, chlorpromazine, or thioridazine; or certain antibiotics, including moxifloxacin, may ↑ risk of torsades de pointes and/or sudden death; avoid concurrent use.
Strong CYP1A2 inhibitors, including fluvoxamine, may ↑ levels and risk of toxicity.
CYP2D6 inhibitors, including paroxetine, may ↑ levels and risk of toxicity.
↑risk of CNS depression with other CNS depressants, including antihistamines, some antidepressants, sedative/hypnotics, and alcohol.

Availability ⬆ ⬇

(Generic available)

Sublingual tablets (Saphris) black cherry flavor: 2.5 mg; 5 mg; 10 mg
Transdermal patch (Secuado): 3.8 mg/24 hr; 5.7 mg/24 hr; 7.6 mg/24 hr

Route/Dosage ⬆ ⬇

Schizophrenia

SL (Adults ): 5 mg twice daily; may ↑ to 10 mg twice daily after 1 wk.
Transdermal (Adults ): Apply 3.8 mg/24-hr patch once daily; may ↑ to 5.7 mg/24-hr or 7.6 mg/24-hr patch once daily after 1 wk.

Acute Manic/Mixed Episodes Associated With Bipolar I Disorder

SL (Adults ): Monotherapy: 10 mg twice daily; may ↓ to 5 mg twice daily if tolerated poorly; continue on the dose that caused stabilization as maintenance therapy; Adjunctive therapy with lithium or valproate: 5 mg twice daily; may ↑ to 10 mg twice daily.
SL (Children 10–17 yr): Monotherapy: 2.5 mg twice daily; may ↑ to 5 mg twice daily after 3 days; may ↑ to 10 mg twice daily after another 3 days.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

May act through combined antagonism of dopaminergic (D₂) and 5-HT_2A receptors.

Therapeutic effects:

Decreased symptoms of acute schizophrenia and mania/mixed episodes of bipolar I disorder.

Classifications ⬆ ⬇

Therapeutic Classification: antipsychotics, mood stabilizers

Pharmacologic Classification: dibenzo oxepino pyrroles

Pharmacokinetics ⬆ ⬇

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

Distribution: Extensively distributed to tissues.

Protein Binding: 95%

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

Half-Life: 24 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
SL	unknown	0.5–1.5 hr	12 hr
TD	unknown	12–24 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Explain the purpose and side effects of asenapine to patient. Do not stop taking drug without consulting health care professional. Instruct patient to take medication as directed and not to skip doses or double up on missed doses. Take missed doses as soon as remembered unless almost time for the next dose. Advise patient to read Instructions for Use before starting asenapine.
Emphasize the importance of routine follow-up exams and continued participation in psychotherapy as indicated.
Inform patient of possibility of extrapyramidal symptoms and tardive dyskinesia. Instruct patient to report these symptoms immediately.
Advise patient to make position changes slowly to minimize orthostatic hypotension. Protect from falls.
Medication may cause drowsiness and dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
May cause depression or suicide. Instruct patients and caregivers to monitor for emergence of suicidal thoughts and behaviors. Notify health care professional immediately if suicidal thoughts; new or worsening depression; anxiety; changes in behavior or mood; thoughts of suicide, dying, or hurting self; or acting on dangerous impulses occur. Instruct patient to carry wallet card and to call the National Suicide Prevention Lifeline at 1-800-273-8255 or visit www.988lifeline.org if they experience suicidal thoughts.
Advise patient and family to call 911 and immediately seek treatment for signs and symptoms of hypersensitivity reactions (difficulty breathing; chest tightness; hives; rash; light-headedness; itching; swelling of the face, lips, tongue, or throat).
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken; to consult health care professional before taking any new medications; and to avoid taking alcohol or other CNS depressants concurrently with this medication.
Advise patient that extremes in temperature should be avoided, because this drug impairs body temperature regulation.
Counsel patients on signs and symptoms of hyperprolactinemia and to contact their health care professional if these abnormalities occur.
Advise patient to notify health care professional of medication regimen prior to treatment or surgery.
Advise patients with diabetes to report worsening of glucose control due to potential for hyperglycemia.
SL: Tell patient not to eat or drink for 10 min after taking SL tablet. Inform patient that oral ulcers, blisters, peeling/sloughing, and inflammation may occur at application site. Advise patient to notify health care professional if these occur; may require discontinuation. Inform patient that numbness or tingling of mouth or throat may occur shortly after administration of asenapine; usually resolves within 1 hr.
Transdermal patch: Instruct patient in correct application of patch. Rotate the site each day. May cause erythema, pruritus, papules, discomfort, pain, edema, or irritation at site of application during wear time or immediately after removal; occurs more frequently in Black people. Risk ↑ if worn longer that 24 hr or if site is used repeatedly. Do not apply heat over the patch.
Rep: May cause fetal harm. Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. If used during 3rd trimester, may cause extrapyramidal and or withdrawal symptoms in infant (agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, feeding disorder). Monitor neonates closely. Encourage pregnant patients to enroll in registry by contacting National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

42794- Sigmapharm Laboratories, LLC
- 42794-016- ASENAPINE
  - 42794-016-08- 30 TABLET in 1 BOTTLE, PLASTIC (42794-016-08)

42794- Sigmapharm Laboratories, LLC
- 42794-016- ASENAPINE
  - 42794-016-10- 60 TABLET in 1 BOTTLE, PLASTIC (42794-016-10)

42794- Sigmapharm Laboratories, LLC
- 42794-016- ASENAPINE
  - 42794-016-22- 10 TABLET in 1 BOTTLE, PLASTIC (42794-016-22)

42794- Sigmapharm Laboratories, LLC
- 42794-017- ASENAPINE
  - 42794-017-08- 30 TABLET in 1 BOTTLE, PLASTIC (42794-017-08)

42794- Sigmapharm Laboratories, LLC
- 42794-017- ASENAPINE
  - 42794-017-10- 60 TABLET in 1 BOTTLE, PLASTIC (42794-017-10)

42794- Sigmapharm Laboratories, LLC
- 42794-017- ASENAPINE
  - 42794-017-22- 10 TABLET in 1 BOTTLE, PLASTIC (42794-017-22)

46708- Alembic Pharmaceuticals Limited
- 46708-198- Asenapine
  - 46708-198-31- 100 BLISTER PACK in 1 CARTON (46708-198-31) / 10 TABLET in 1 BLISTER PACK

46708- Alembic Pharmaceuticals Limited
- 46708-198- Asenapine
  - 46708-198-60- 60 BLISTER PACK in 1 CARTON (46708-198-60) / 10 TABLET in 1 BLISTER PACK (46708-198-10)

46708- Alembic Pharmaceuticals Limited
- 46708-199- Asenapine
  - 46708-199-31- 100 BLISTER PACK in 1 CARTON (46708-199-31) / 10 TABLET in 1 BLISTER PACK

46708- Alembic Pharmaceuticals Limited
- 46708-199- Asenapine
  - 46708-199-60- 60 BLISTER PACK in 1 CARTON (46708-199-60) / 10 TABLET in 1 BLISTER PACK (46708-199-10)

46708- Alembic Pharmaceuticals Limited
- 46708-544- Asenapine
  - 46708-544-31- 100 BLISTER PACK in 1 CARTON (46708-544-31) / 10 TABLET in 1 BLISTER PACK

46708- Alembic Pharmaceuticals Limited
- 46708-544- Asenapine
  - 46708-544-60- 60 BLISTER PACK in 1 CARTON (46708-544-60) / 10 TABLET in 1 BLISTER PACK (46708-544-10)

62332- Alembic Pharmaceuticals Inc.
- 62332-198- Asenapine
  - 62332-198-31- 100 BLISTER PACK in 1 CARTON (62332-198-31) / 10 TABLET in 1 BLISTER PACK

62332- Alembic Pharmaceuticals Inc.
- 62332-198- Asenapine
  - 62332-198-60- 60 BLISTER PACK in 1 CARTON (62332-198-60) / 10 TABLET in 1 BLISTER PACK (62332-198-10)

62332- Alembic Pharmaceuticals Inc.
- 62332-199- Asenapine
  - 62332-199-31- 100 BLISTER PACK in 1 CARTON (62332-199-31) / 10 TABLET in 1 BLISTER PACK

62332- Alembic Pharmaceuticals Inc.
- 62332-199- Asenapine
  - 62332-199-60- 60 BLISTER PACK in 1 CARTON (62332-199-60) / 10 TABLET in 1 BLISTER PACK (62332-199-10)

62332- Alembic Pharmaceuticals Inc.
- 62332-544- Asenapine
  - 62332-544-31- 100 BLISTER PACK in 1 CARTON (62332-544-31) / 10 TABLET in 1 BLISTER PACK

62332- Alembic Pharmaceuticals Inc.
- 62332-544- Asenapine
  - 62332-544-60- 60 BLISTER PACK in 1 CARTON (62332-544-60) / 10 TABLET in 1 BLISTER PACK (62332-544-10)

68968- Noven Therapeutics, LLC
- 68968-0172- SECUADO
  - 68968-0172-3- 30 POUCH in 1 CARTON (68968-0172-3) / 1 d in 1 POUCH

68968- Noven Therapeutics, LLC
- 68968-0172- SECUADO
  - 68968-0172-7- 7 POUCH in 1 CARTON (68968-0172-7) / 1 d in 1 POUCH

68968- Noven Therapeutics, LLC
- 68968-0173- SECUADO
  - 68968-0173-3- 30 POUCH in 1 CARTON (68968-0173-3) / 1 d in 1 POUCH

68968- Noven Therapeutics, LLC
- 68968-0173- SECUADO
  - 68968-0173-7- 7 POUCH in 1 CARTON (68968-0173-7) / 1 d in 1 POUCH

68968- Noven Therapeutics, LLC
- 68968-0174- SECUADO
  - 68968-0174-3- 30 POUCH in 1 CARTON (68968-0174-3) / 1 d in 1 POUCH

68968- Noven Therapeutics, LLC
- 68968-0174- SECUADO
  - 68968-0174-7- 7 POUCH in 1 CARTON (68968-0174-7) / 1 d in 1 POUCH

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇