Asenapine

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Asenapine falls into category C.  There are no well-controlled studies that have been done in pregnant women. Asenapine should be used during pregnancy only if the possible benefit outweighs the possible risk to the unborn baby.

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The recommended dose range of asenapine (Saphris) for the treatment of schizophrenia is 10-20 mg/day given in two doses.

The recommended dose range of asenapine (Saphris), if used alone, for the treatment of bipolar disorder is 10-20 mg/day given in two doses.

The recommended dose range of asenapine (Saphris), if used with another medication, for the treatment of bipolar disorder is 10-20 mg/day given in two doses.

You should not use asenapine if you are allergic to it, or if you have:

• severe liver disease; or

• a history of severe allergic reaction to asenapine.

Asenapine is not approved for use in psychotic conditions related to dementia. Asenapine may increase the risk of death in older adults with dementia-related conditions.

To make sure asenapine is safe for you, tell your doctor if you have:

• liver disease;

• heart disease, high blood pressure, heart rhythm problems;

• a history of heart attack or stroke;

• a history of breast cancer;

• seizures or epilepsy;

• diabetes (asenapine may raise your blood sugar);

• trouble swallowing;

• Parkinson's disease;

• a history of low white blood cell (WBC) counts; or

• a personal or family history of Long QT syndrome.

It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

Taking antipsychotic medication during the last 3 months of pregnancy may cause problems in the newborn such as withdrawal symptoms, breathing problems, feeding problems, fussiness, tremors, and limp or stiff muscles. However, you may have withdrawal symptoms or other problems if you stop taking your medicine during pregnancy. If you become pregnant while taking asenapine, do not stop taking it without your doctor's advice.

It is not known whether asenapine passes into breast milk or if it could affect the nursing baby. Tell your doctor if you are breast-feeding.

Asenapine should not be given to a child younger than 10 years old. Asenapine is not approved for schizophrenia in anyone younger than 18 years old.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

• Tell all of your health care providers that you take asenapine. This includes your doctors, nurses, pharmacists, and dentists.
• Avoid driving and doing other tasks or actions that call for you to be alert until you see how this medicine affects you.
• To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs.
• Low white blood cell counts have happened with drugs like this one. This may lead to a higher chance of getting an infection. Deadly infections have rarely happened. Tell your doctor if you have ever had a low white blood cell count. Call your doctor right away if you have signs of infection like fever, chills, or sore throat. Talk with your doctor.
• Have blood work checked as you have been told by the doctor. Talk with the doctor.
• High blood sugar or diabetes, high cholesterol, and weight gain have happened with drugs like this one. These changes may raise the chance of heart and brain blood vessel disease. Talk with the doctor.
• Check your blood sugar as you have been told by your doctor.
• Avoid drinking alcohol while taking asenapine.
• Talk with your doctor before you use other drugs and natural products that slow your actions.
• Be careful in hot weather or while being active. Drink lots of fluids to stop fluid loss.
• Dizziness, sleepiness, and feeling less stable may happen with this medicine. These may lead to falling. Broken bones or other health problems can happen from falling. Talk with the doctor.
• Older adults with dementia taking drugs like this one have had a higher number of strokes. Sometimes these strokes have been deadly. This drug is not approved to treat mental problems caused by dementia. Talk with your doctor.
• If you are 65 or older, use asenapine with care. You could have more side effects.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using this medicine while you are pregnant.
• Taking asenapine in the third trimester of pregnancy may lead to muscle movements that cannot be controlled and withdrawal in the newborn. Talk with the doctor.
• Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

Use this medicine as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Wash and dry your hands before you take asenapine. Do not touch the tablet with wet or damp hands.
• Do not take this medicine out of the blister pack until you are ready to take it. Take asenapine right away after opening the blister pack. Do not store the removed drug for future use.
• Place tablet under the tongue and let melt.
• Do not swallow whole. Do not chew, break, or crush.
• Do not eat or drink for at least 10 minutes after taking this medicine.
• To gain the most benefit, do not miss doses.
• Keep taking asenapine as you have been told by your doctor or other health care provider, even if you feel well.

What do I do if I miss a dose?

• Take a missed dose as soon as you think about it.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet Sublingual, Sublingual:

Saphris: 2.5 mg [black cherry flavor]

Saphris: 5 mg

Saphris: 5 mg [black cherry flavor]

Saphris: 10 mg

Saphris: 10 mg [black cherry flavor]

• Saphris

• Antimanic Agent
• Second Generation (Atypical) Antipsychotic

Clearance is decreased, increasing exposure by 30% to 40%.

Psychosis/agitation associated with dementia

Based on the American Psychiatric Association practice guideline on the use of antipsychotics to treat agitation or psychosis in patients with dementia, antipsychotics, such as asenapine, may be considered for the treatment of agitation and psychosis in certain patients with dementia; however, evidence for efficacy is modest and use should be limited to patients whose symptoms are dangerous, severe, or cause significant patient distress due to safety risks associated with antipsychotic use.

Severe hepatic impairment (Child-Pugh class C); hypersensitivity to asenapine or any component of the formulation (eg, anaphylaxis, angioedema, hypotension, tachycardia, swollen tongue, dyspnea, wheezing, rash)

Refer to adult dosing.

Psychosis/agitation associated with dementia (off-label use): Sublingual: Initial: One-third to one-half the usual dose to treat psychosis in younger adults or the smallest available dosage. In patients without a clinically significant response after 4 weeks, taper and withdraw therapy. In patients with an adequate response, attempt to taper and withdraw therapy within 4 months, unless symptoms recurred with a previous taper attempt. Assess symptoms at least monthly during taper and for at least 4 months after withdrawal of therapy (APA [Reus 2016]).

Sublingual tablets should be placed under the tongue and allowed to completely dissolve. Do not split, crush, chew, or swallow. Avoid eating or drinking for at least 10 minutes after administration.

Mental status; vital signs (as clinically indicated); blood pressure and pulse (baseline; repeat 3 months after antipsychotic initiation, then yearly); weight, height, BMI, waist circumference (baseline; repeat at 4, 8, and 12 weeks after initiating or changing therapy, then quarterly; consider switching to a different antipsychotic for a weight gain more than 5% of initial weight [ADA 2004]); CBC (as clinically indicated; monitor frequently during the first few months of therapy in patients with preexisting low WBC or history of drug-induced leukopenia/neutropenia); electrolytes and liver function (annually and as clinically indicated); personal and family history of obesity, diabetes, dyslipidemia, hypertension, or cardiovascular disease (baseline; repeat annually); fasting plasma glucose level/HbA1c (baseline; repeat 3 months after starting antipsychotic, then yearly); fasting lipid panel (baseline; repeat 3 months after initiation of antipsychotic; if low-density lipoprotein level is normal, repeat at 2- to 5-year intervals or more frequently if clinical indicated [ADA 2004]); prolactin level (baseline [NICE 2014]); changes in menstruation, libido, development of galactorrhea, and erectile and ejaculatory function (yearly); abnormal involuntary movements or parkinsonian signs (baseline; repeat weekly until dose stabilized for at least 2 weeks after introduction and for 2 weeks after any significant dose increase); tardive dyskinesia (every 12 months; high-risk patients every 6 months); ocular examination (yearly in patients older than 40 years; every 2 years in younger patients) (ADA 2004; Lehman 2004; Marder 2004; NICE 2014).

Antipsychotic use during the third trimester of pregnancy has a risk for abnormal muscle movements (extrapyramidal symptoms [EPS]) and/or withdrawal symptoms in newborns following delivery. Symptoms in the newborn may include agitation, feeding disorder, hypertonia, hypotonia, respiratory distress, somnolence, and tremor; these effects may be self-limiting or require hospitalization; monitoring of the neonate is recommended. Asenapine may cause hyperprolactinemia, which may decrease reproductive function in both males and females.

The ACOG recommends that therapy during pregnancy be individualized; treatment with psychiatric medications during pregnancy should incorporate the clinical expertise of the mental health clinician, obstetrician, primary healthcare provider, and pediatrician. Safety data related to atypical antipsychotics during pregnancy is limited and routine use is not recommended. However, if a woman is inadvertently exposed to an atypical antipsychotic while pregnant, continuing therapy may be preferable to switching to a typical antipsychotic that the fetus has not yet been exposed to; consider risk:benefit (ACOG 2008).

Healthcare providers are encouraged to enroll women 18-45 years of age exposed to asenapine during pregnancy in the Atypical Antipsychotics Pregnancy Registry (866-961-2388 or http://www.womensmentalhealth.org/pregnancyregistry).

Summary of Use during Lactation

Because there is no published experience with asenapine during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.

Drug Levels

Maternal Levels. Relevant published information was not found as of the revision date.

Infant Levels. Relevant published information was not found as of the revision date.

Effects in Breastfed Infants

Relevant published information was not found as of the revision date.

Effects on Lactation and Breastmilk

Asenapine has caused elevated prolactin serum in patients taking the drug.[1] The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

References

1. Anon. Saphris package insert. Merck & Co., Inc. 2009.