are reasonably certain that therapy does not affect them adversely Dysphagia, dysmotility, and aspiration may occur; use cautiously in patients at risk for aspiration Potential disruption of body temperature regulation; strenuous exercise, exposure to extreme heat, dehydration, and anticholinergic medications may contribute to elevation in core body temperature; use with caution in patient who may experience these conditions Not recommended with severe hepatic impairment (Child-Pugh class C) Inherent suicide risk with population treated warrants close supervision when drug therapy is changed Atypical antipsychotic drugs have been associated with metabolic changes including hyperglycemia, dyslipidemia, and body weight gain, which may increase cardiovascular/ cerebrovascular risk; all of the drugs in the class have been shown to produce some metabolic changes but each drug has its own specific risk profile Monitor weight gain in pediatric patients and assess against that expected for normal growth Can elevate prolactin levels, and elevation can persist during chronic 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 Orthostatic vital signs should be monitored in patients who are vulnerable to hypotension (elderly patients, patients with dehydration, hypovolemia, concomitant treatment with antihypertensive medications May cause somnolence, postural hypotension, motor and sensory instability, which may lead to falls and, consequently, fractures or other injuries; perform complete fall risk assessments when initiating antipsychotic treatment and recurrently for patients on long-term antipsychotic therapy Extrapyramidal symptoms, including acute dystonic reactions, pseudoparkinsonism, akathisia, and tardive dyskinesia reported QT prolongation Based on clinical trials, therapy should be avoided in combination with other drugs known to prolong QTc including Class 1A antiarrhythmics (eg, quinidine, procainamide) or Class 3 antiarrhythmics (e.g., amiodarone, sotalol), antipsychotic medications (eg, ziprasidone, chlorpromazine, thioridazine), and antibiotics (eg, gatifloxacin, moxifloxacin) Treatment should also be avoided in patients with a history of cardiac arrhythmias and in other circumstances that may increase risk of occurrence of torsade de pointes and/or sudden death in association with use of drugs that prolong QTc interval, including bradycardia; hypokalemia or hypomagnesemia; and presence of congenital prolongation of QT interval Tardive dyskinesia Risk of tardive dyskinesia and likelihood that it will become irreversible increase with duration of treatment and cumulative dose Syndrome can develop after a relatively brief treatment period, even at low doses; may also occur after discontinuation of treatment; prescribe in a manner most likely to reduce risk of tardive dyskinesia Chronic antipsychotic treatment should generally be reserved for patients who suffer from a chronic illness that is known to respond to antipsychotic drugs and for whom alternative, effective, but potentially less harmful treatments are not available or appropriate; some patients may require treatment despite presence of syndrome In patients who do require chronic treatment, use lowest dose and shortest duration of treatment producing a satisfactory clinical response; periodically reassess need for continued treatment Pregnancy category: C Neonates exposed to antipsychotic drugs during 3rd trimester of pregnancy are at risk for EPS or withdrawal symptoms after delivery; these complications vary in severity, with some being self-limited and others requiring ICU unit support and prolonged hospitalization Lactation: Excretion in milk unknown; use with cautionPregnancy 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. Mechanism of Action Mechanism of action unknown; efficacy thought to be mediated via combined antagonist activity at dopamine D2 and serotonin type 2 (5-HT2) receptors Absorption Bioavailability: SL, 35%; swallowed, ≤2% Peak plasma time: 0.5-1.5 hr Peak plasma concentration: 4 ng/mL Distribution Protein bound: 95% Vd: 20-25 L/kg Metabolism Metabolized by UGT1A4 and CYP450 (predominantly isoenzyme 1A2) Enzymes inhibited: CYP2D6 (weakly) Elimination Half-life: 24 hr Clearance: 52 L/hr Excretion: Urine (50%), feces (40%) Instructions Sublingual tablet; to allow optimal absorption, place under tongue and allow to dissolve completely (dissolves within seconds) Do not chew, split, crush, or swallow sublingual tablet Do not eat or drink for at least 10 minutes after administration BRAND FORM. UNIT PRICE PILL IMAGE asenapine sublingual- 10 mg tabletasenapine sublingual- 2.5 mg tabletasenapine sublingual- 10 mg tabletSaphris sublingual- 2.5 mg tabletSaphris sublingual- 10 mg tabletSaphris sublingual- 5 mg tabletSaphris sublingual- 10 mg tabletSaphris sublingual- 10 mg tabletCopyright © 2010 First DataBank, Inc.Print Patient Educationasenapine sublingual ASENAPINE - SUBLINGUAL (a-SEN-a-peen) COMMON BRAND NAME(S): Saphris WARNING: There may be a slightly increased risk of serious, possibly fatal side effects (such as stroke, heart failure, fast/irregular heartbeat, pneumonia) when this medication is used by older adults with dementia. This medication is not approved for the treatment of dementia-related behavior problems. Discuss the risks and benefits of this medication, as well as other effective and possibly safer treatments for dementia-related behavior problems, with the doctor.If you are using asenapine in combination with other medication to treat depression, also carefully read the drug information for the other medication. USES: This medication is used to treat certain mental/mood disorders (such as schizophrenia, bipolar disorder). Asenapine helps you to think more clearly, feel less nervous, and take part in everyday life. It may also help to decrease hallucinations (hearing/seeing things that are not there) and prevent severe mood swings. Asenapine is a psychiatric medication that belongs to the class of drugs called atypical antipsychotics. It works by helping to restore the balance of certain natural substances in the brain (neurotransmitters). HOW TO USE: Take this medication as directed by your doctor, usually 2 times a day. Gently remove the medication from the packaging with dry hands by peeling back the tab. Do not push the tablet through the packaging. Place your dose of this medication under the tongue and allow it to dissolve completely in your saliva. Do not chew, crush, split, or swallow the tablet whole. Do not eat or drink anything for 10 minutes after taking this medication.The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Take this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day. It may take several weeks before you get the full benefit of this drug.Keep taking this medication even if you feel well. Do not increase your dose or take this drug more often than prescribed. Your condition will not improve any faster, and your risk of side effects will increase. Do not stop taking this medication without consulting your doctor.Tell your doctor if your condition does not improve or if it worsens. SIDE EFFECTS: Drowsiness, dizziness, lightheadedness, and weight gain may occur. Numbness/tingling of the mouth may also occur but usually goes away within 1 hour. Sores, blisters, or pain under the tongue may rarely occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Dizziness and lightheadedness can increase the risk of falling. Get up slowly when rising from a sitting or lying position.This drug may cause muscle/nervous system problems (extrapyramidal symptoms-EPS). Your doctor may prescribe another medication to decrease these side effects. Tell your doctor right away if you notice any of the following side effects: feelings of anxiety/agitation/jitteriness, drooling/trouble swallowing, restlessness/constant need to move, shaking (tremor), shuffling walk, stiff muscles, severe muscle spasms/cramping (such as twisting neck, arching back, eyes rolling up), mask-like expression of the face.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Rarely, this medication may cause face/muscle twitching and uncontrollable movements (tardive dyskinesia). In some cases, this condition may be permanent. Tell your doctor right away if you develop any uncontrollable movements such as lip smacking, mouth puckering, tongue thrusting, chewing, or unusual arm/leg movements.This drug may rarely make your blood sugar rise, which can cause or worsen diabetes. Weight gain from this drug may increase the risk of this side effect. Tell your doctor right away if you have symptoms of high blood sugar such as increased thirst/urination. If you already have diabetes, check your blood sugar regularly as directed and share the results with your doctor. Your doctor may need to adjust your diabetes medication, exercise program, or diet.In rare cases, asenapine may increase your level of a certain substance made by the body (prolactin). For females, this increase in prolactin may result in unwanted breast milk, missed/stopped periods, or difficulty becoming pregnant. For males, it may result in decreased sexual ability, inability to produce sperm, or enlarged breasts. If you develop any of these symptoms, tell your doctor right away.Rarely, with similar drugs, males may have a painful or prolonged erection lasting 4 or more hours. If this occurs, stop using this drug and get medical help right away, or permanent problems could occur.Tell your doctor right away if you have any serious side effects, including: interrupted breathing during sleep (sleep apnea), signs of infection (such as sore throat that doesn't go away, fever).Get medical help right away if you have any very serious side effects, including: severe dizziness, fainting, slow heartbeat, seizures.This medication may rarely cause a very serious condition called neuroleptic malignant syndrome (NMS). Get medical help right away if you have any of the following symptoms: fever, muscle stiffness/pain/tenderness/weakness, severe tiredness, severe confusion, sweating, fast/irregular heartbeat, dark urine, signs of kidney problems (such as change in the amount of urine).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345. PRECAUTIONS: See also Warning section.Before taking asenapine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver problems, heart problems (such as past heart attack, angina, abnormal heart rhythm), stroke, diabetes (including family history), obesity, low blood pressure, seizures, low white blood cell count, dehydration, breast cancer, substance use disorder (such as overuse of or addiction to drugs/alcohol), Alzheimer's disease, dementia, trouble swallowing, breathing trouble during sleep (sleep apnea).Asenapine may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using asenapine, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using asenapine safely.This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do