asenapine

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

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, history of MI/ischemic heart disease/HF/conduction abnormalities/cerebrovascular disease (↑ risk of hypotension);
Patients at risk for falls;
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.

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 African Americans)

Metab: weight gain, ↑appetite, dyslipidemia

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

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

Concurrent use of QTc interval prolonging drugs including Class 1A antiarrhythmics such as quinidine and procainamide or Class 3 antiarrhythmics including amiodarone and sotalol or other antipsychotics including ziprasidone, chlorpromazine or thioridazine or certain antibiotics such as 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.

Route/Dosage ⬆ ⬇

Schizophrenia

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

Acute Manic/Mixed Episodes Associated with Bipolar I Disorder

(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.
(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.

Availability ⬆ ⬇

(Generic available)

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

Assessment ⬆ ⬇

Monitor for clinical worsening and emergence of suicidal thoughts and behaviors, especially during the first few months of drug therapy and at times of dose changes. Assess mental status (orientation, mood, behavior) before and periodically during therapy. Assess for suicidal tendencies. Restrict amount of drug available to patient. Risk may be increased in children, adolescents, and adults ≤24 yrs.
Assess weight and BMI initially and during therapy.
Monitor BP (sitting, standing, lying) and pulse before and periodically during therapy.
Observe patient carefully when administering medication to ensure that medication is actually taken and not hoarded.
Monitor patient for onset of akathisia (restlessness or desire to keep moving) and extrapyramidal side effects (parkinsonian: difficulty speaking or swallowing, loss of balance control, pill rolling of hands, masklike face, shuffling gait, rigidity, tremors; and dystonic: muscle spasms, twisting motions, twitching, inability to move eyes, weakness of arms or legs) periodically throughout therapy. Report these symptoms.
Monitor for tardive dyskinesia (uncontrolled rhythmic movement of mouth, face, and extremities; lip smacking or puckering; puffing of cheeks; uncontrolled chewing; rapid or worm-like movements of tongue). Notify health care professional immediately if these symptoms occur, as these side effects may be irreversible.
Monitor for development of neuroleptic malignant syndrome (fever, muscle rigidity, altered mental status, respiratory distress, tachycardia, seizures, diaphoresis, hypertension or hypotension, pallor, tiredness, loss of bladder control). Discontinue asenapine and notify health care professional immediately if these symptoms occur.
Monitor for symptoms related to hyperprolactinemia (menstrual abnormalities, galactorrhea, sexual dysfunction).
Assess for falls risk. Drowsiness, orthostatic hypotension, and motor and sensory instability increase risk. Institute prevention if indicated.
Assess patient for signs and symptoms of hypersensitivity reactions, including anaphylaxis, angioedema, hypotension, tachycardia, swollen tongue, dyspnea, itching, wheezing, and rash.
Monitor for symptoms related to hyperprolactinemia (menstrual abnormalities, galactorrhea, sexual dysfunction).

Lab Test Considerations:

Obtain fasting blood glucose, lipid profile, and cholesterol levels initially and periodically during therapy.
- Monitor CBC frequently during initial mo of therapy in patients with pre-existing or history of low WBC. May cause leukopenia, neutropenia, or agranulocytosis. Monitor patients with neutropenia for fever or other symptoms of infection and treat promptly. Discontinue therapy if ANC <1000/mm³ occurs.
- May cause transient ↑ in serum ALT.

Implementation ⬆ ⬇

Open packet immediately before use by firmly pressing thumb button and pulling out tablet pack. Do not push tablet through or cut or tear tablet pack. Peel back colored tab and gently remove tablet. Place tablet under tongue and allow to dissolve completely; dissolves in saliva within sec. DNC: Do not split, crush, chew, or swallow tablets. Avoid eating or drinking for 10 min after administration. Slide tablet pack back into case until it clicks.
Transdermal patch: Once each day, apply to clean, dry, and intact skin of upper arm, upper back, abdomen, or hip. Rotate site with each application. Do not cut open pouch until ready to apply and do not use if pouch seal is broken or appears to be damaged. Do not cut patch; apply whole patch. If patch lifts at edges, reattach by pressing firmly and smoothing down edges. If patch comes off completely, apply a new patch. Remove old patch; apply only 1 patch at a time. Discard by folding patch so that adhesive side sticks to itself and safely discard. If irritation or a burning sensation occurs while wearing patch, remove the system and apply a new patch to a new application site. May wear during shower, but use during swimming or taking a bath has not been evaluated. Do not apply external heat sources (heating pad) over patch; prolonged application of heat over patch increases plasma concentrations of asenapine.

Patient/Family Teaching ⬆ ⬇

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.
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.
Advise patient and family to notify health care professional if thoughts about suicide or dying, attempts to commit suicide; new or worse depression; new or worse anxiety; feeling very agitated or restless; panic attacks; trouble sleeping; new or worse irritability; acting aggressive; being angry or violent; acting on dangerous impulses; an extreme increase in activity and talking; other unusual changes in behavior or mood or if signs and symptoms of hypersensitivity reactions (difficulty breathing, itching, swelling of the face, tongue or throat, feeling lightheaded) occur.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken, to avoid alcohol, and 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.
Rep: May cause fetal harm. Advise females 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/.
Emphasize the importance of routine follow-up exams and continued participation in psychotherapy as indicated.
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. 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 African Americans. Risk increases if worn longer that 24 hr or if site is used repeatedly.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇