How does saphris work?

SAPHRIS® 5mg and 10mg sublingual wafers

Asenapine

Consumer Medicine Information

What is in this leaflet

This leaflet answers some common questions about SAPHRIS.

It does not contain all the available information.

It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor has weighed the risks of you taking SAPHRIS against the benefits they expect it will have for you.

If you have any concerns about taking this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine. You may need to read it again.

What SAPHRIS is used for

SAPHRIS is used to treat the mental illnesses:

  • Schizophrenia – an illness with disturbances in thinking, feelings and behaviour.
  • Bipolar 1 disorder – an illness in which there are sustained mood swings either up (mania) or down (low moods). During mania, patients experience episodes of overactivity, elation or irritability. During low moods, patients may feel depressed or guilty, lack energy, lose their appetite and have trouble sleeping.

SAPHRIS belongs to a group of medicines called antipsychotics. It helps to correct chemical imbalances in the brain, which may cause these mental illnesses.

Your doctor may have prescribed SAPHRIS for another reason.

Ask your doctor if you have any questions about why SAPHRIS has been prescribed for you.

SAPHRIS is not addictive.

This medicine is available only with a doctor’s prescription.

Before you take SAPHRIS

When you must not take it

Do not take SAPHRIS if you have an allergy to:

  • asenapine the active ingredient in SAPHRIS
  • any of the other ingredients listed at the end of this leaflet

Some of the symptoms of an allergic reaction to SAPHRIS may include shortness of breath, wheezing or difficulty breathing; swelling of the face, lips, tongue or other parts of the body; rash, itching or hives on the skin or you may feel faint.

If you have diabetes or risk factors for diabetes, such as being overweight or a family history of diabetes, your blood sugar should be tested at the beginning of and throughout treatment with SAPHRIS. Complications of diabetes can be serious and even life-threatening. Tell your doctor if you have blood sugar problems or signs of diabetes, such as being thirsty all the time, going to the bathroom a lot, or feeling weak or hungry.

Asenapine may cause sleepiness, sudden drops in blood pressure when you stand up, dizziness and changes in your ability to move and balance, which may lead to falls and, consequently, fractures or other injuries. Patients at risk for fall should be evaluated prior to prescribing asenapine.

Do not take SAPHRIS if you are pregnant or breast-feeding unless your doctor tells you so. Ask your doctor about the risks and benefits involved. It is not known if it is safe for you to take SAPHRIS while you are pregnant. However, if you need to take SAPHRIS during your pregnancy, the doctor will discuss the risks and benefits of taking it with you.

The following symptoms may occur in newborn babies, of mothers that have used antipsychotics in the last trimester (last three months of their pregnancy): shaking, muscle stiffness and/or weakness, sleepiness, agitation, breathing problems, and difficulty in feeding. If your baby develops any of these symptoms contact your doctor.

It is recommended that you do not breast-feed while taking SAPHRIS.

SAPHRIS is not recommended for use in children below 18 years of age.

Do not take SAPHRIS after the expiry date printed on the pack.

Do not use SAPHRIS if the packaging is torn or shows signs of tampering. If it has expired or is damaged, return it to your pharmacist for disposal.

If you are not sure whether you should start taking SAPHRIS, talk to your doctor or pharmacist.

Before you start to take it

Tell your doctor if:

you have allergies to:

  • any other medicines
  • any other substances, such as foods, preservatives or dyes.

you have or have had any medical conditions, especially the following:

  • dementia (in elderly patients) or dementia with Lewy Bodies
  • Parkinson’s disease
  • heart disease / low blood pressure
  • liver disease
  • diabetes or family history of diabetes
  • difficulty in swallowing
  • epilepsy (seizures)
  • higher levels of the hormone, prolactin, in your blood
  • neuroleptic malignant syndrome – a reaction to some medicines with a sudden increase in body temperature, extremely high blood pressure and severe convulsions
  • tardive dyskinesia – a reaction to some medicines with worm-like movements of the tongue, or other uncontrolled movements of the mouth, tongue, cheeks or jaws which may progress to the arms and legs

Depression and other mental illnesses can lead to suicide. It is important to discuss all the risks of treating depression and mental illness as well as the risks of not treating it. You should discuss all treatment choices with your doctor, not just the use of anti-depressants.

Patients (and caregivers of patients) need to monitor for any worsening of their condition and/or the emergence of thoughts of suicide or suicidal behaviour or thoughts of harming themselves and to seek medical advice immediately if these symptoms present.

If you have not told your doctor about any of the above, tell him/her before you start taking SAPHRIS.

The long-term safety and effectiveness of SAPHRIS beyond 12 weeks has not been assessed in Bipolar disorder.

Taking other medicines

Tell your doctor or pharmacist if you are taking any other medicines, including any that you buy without a prescription from your pharmacy, supermarket or health food shop.

Some medicines and SAPHRIS may interfere with each other. These may include:

  • blood pressure lowering medicines
  • antidepressant drugs (e.g. paroxetine, , fluvoxamine or fluoxetine)

These medicines may be affected by SAPHRIS, or may affect how well it works. You may need different amounts of your medicine, or you may need to take different medicines.

Other medicines not listed above may also interfere with SAPHRIS. Your doctor and pharmacist have more information on medicines to be careful with or avoid while taking this medicine.

Use in children

SAPHRIS is not recommended for use in children below 18 years of age.

How to take Saphris

Follow all directions given to you by your doctor or pharmacist carefully. They may differ from the information contained in this leaflet.

If you do not understand the instructions on the box, ask your doctor or pharmacist for help.

How much to take

The dose of SAPHRIS is one wafer to be taken twice a day. Your doctor will tell you how many wafers you will need to take each day and how long you need to take it. This depends on your condition and whether or not you are taking any other medicines.

How to take it

Do not remove the wafer until ready to take.

Use dry hands when handling the wafer.

Do not push the wafer through the blister. Do not cut or tear the blister. Peel back the coloured tab.

Gently remove the wafer from the blister. Do not crush the wafer.

Place the wafer under your tongue and allow it to completely dissolve.

Do not chew or swallow the wafer.

Do not eat or drink for 10 minutes after taking the wafer. Otherwise SAPHRIS will not be absorbed completely and it may not work as effectively.

How long to take it

Continue taking the wafers for as long as your doctor tells you.

SAPHRIS helps control your condition, but does not cure it. Therefore you must take SAPHRIS every day.

Do not stop taking SAPHRIS unless your doctor tells you to – even if you feel better.

If you forget to take it

If it is almost time for your next dose, skip the dose you missed and take your next dose when you are meant to.

Otherwise, take it as soon as you remember and then go back to taking your medicine as you would normally.

Do not take a double dose to make up for the dose that you missed.

If you are not sure what to do, ask your doctor or pharmacist.

If you have trouble remembering to take your medicine, ask your pharmacist for some hints.

If you take too much (overdose)

Immediately telephone your doctor or the Australian Poisons Information Centre (telephone 13 11 26) or go to Accident and Emergency at the nearest hospital, if you think that you or anyone else may have taken too much SAPHRIS. Do this even if there are no signs of discomfort or poisoning.

Keep telephone numbers for these places handy. You may need urgent medical attention.

If you take too much SAPHRIS, you may feel restless, confused, drowsy, dizzy, sleepy or have a fast heart beat.

While you are taking SAPHRIS

Things you must do

Tell any other doctors, dentists, and pharmacists who are treating you that you are taking SAPHRIS.

If you are about to be started on any new medicine, tell your doctor, dentist or pharmacist that you are taking SAPHRIS.

If you plan to have surgery that needs a general anaesthetic, tell your doctor or dentist that you are taking SAPHRIS.

If you become pregnant while taking SAPHRIS, tell your doctor immediately.

If you are about to have any blood tests, tell your doctor that you are taking SAPHRIS. SAPHRIS may interfere with the results of some tests.

Be sure to keep all of your doctor’s appointments so that your progress can be checked. Your doctor will check your progress and may want to take some blood tests from time to time. This helps to reduce unwanted side effects.

If you or someone you know is demonstrating any of the following warning signs of suicide while taking SAPHRIS, contact your doctor or mental health professional immediately or go to the nearest hospital for treatment:

  • thoughts or talk of death or suicide
  • thoughts or talk of self-harm or harm to others
  • any recent attempts of self-harm
  • increase in aggressive behaviour, irritability or agitation
  • worsening of depression

Occasionally, the symptoms of depression may include thoughts of suicide or self-harm. These symptoms may continue or get worse during the early stages of treatment until the effect of the medicine becomes apparent.

All mentions of suicide or violence must be taken seriously.

Things you must not do

Do not give SAPHRIS to anyone else, even if they have the same condition as you.

Do not take SAPHRIS to treat any other complaints unless your doctor tells you to.

Do not stop taking SAPHRIS, or change the dosage, even if you are feeling better, without checking with your doctor. If you stop taking SAPHRIS suddenly, your condition may worsen or your chance of getting an unwanted side effect may increase. To prevent this, your doctor may gradually reduce the amount of SAPHRIS you take each day before stopping completely.

Do not take any medicines that cause drowsiness while you are taking SAPHRIS, unless recommended by your doctor.

Things to be careful of

Be careful driving or operating machinery until you know how SAPHRIS affects you. SAPHRIS may cause dizziness, and tiredness, in some people. Make sure you know how you react to SAPHRIS before you drive a car, operate machinery, or do anything else that could be dangerous if you are dizzy or sleepy.

If SAPHRIS makes you feel light-headed, dizzy or faint when getting out of bed or standing up, get up slowly. Standing up slowly, especially when you get up from bed or chairs, will help your body get used to the change in position and blood pressure. If this problem continues or gets worse, talk to your doctor.

Be careful when drinking alcohol while taking SAPHRIS. Combining SAPHRIS and alcohol can make you more sleepy or dizzy.

Your doctor may suggest you avoid alcohol while you are being treated with SAPHRIS.

Make sure you keep cool in hot weather and keep warm in cool weather. SAPHRIS may affect the way your body reacts to temperature changes.

Side effects

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are taking SAPHRIS.

SAPHRIS helps most people with the symptoms of schizophrenia or with manic episodes associated with Bipolar 1 disorder. But it may have unwanted side effects in a few people. All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Therefore, it is important that you tell your doctor as soon as possible if you notice anything that is making you feel unwell, even if you think the problems are not connected with the medicine. Your doctor may then decide to adjust your dose or use a different medicine.

Ask your doctor or pharmacist to answer any questions you may have.

The following is a list of possible side effects. Do not be alarmed by this list. You may not experience any of them.

Tell your doctor or pharmacist if you notice any of the following and they worry you:

  • sleepiness
  • increased appetite, weight gain
  • drowsiness
  • tremor
  • sensation of numbness in the mouth
  • dizziness
  • change in taste
  • fatigue
  • dry mouth
  • mouth ulcers and pain in the mouth
  • increased saliva (drooling)
  • nausea
  • constipation
  • restlessness, agitation, anxiety, excitement or difficulty concentrating
  • an overwhelming urge to move such as feeling the need to pace, swing the legs while seated or rock from foot to foot
  • difficulty sleeping
  • headache
  • hot, dry skin
  • increased or decreased sweating
  • signs of increased blood sugar levels such as excessive thirst, hunger, weakness, urination or onset or worsening of diabetes.
  • falls may occur as a result of one or more adverse events such as: sleepiness, sudden drops in blood pressure when you stand up, dizziness and changes in your ability to move and balance.

These side effects are usually mild. Some of these side effects may go away after a while.

If any of the following happen, tell your doctor or pharmacist immediately or go to Accident and Emergency at your nearest hospital:

  • signs of frequent infections such as fever, chills, sore throat or mouth ulcers
  • extremely high body temperature
  • worm-like movements of the tongue, or other uncontrolled movements of the tongue, mouth, cheeks, or jaw which may progress to arms and legs
  • sudden onset of uncontrollable muscle spasms affecting the eyes, head, neck and body
  • fainting
  • convulsions, fits or seizures
  • severe spasms in the muscles of the shoulders, neck and upper body
  • sudden increase in body temperature, with sweating, fast heart beat, muscle stiffness and fluctuating blood pressure which may lead to coma
  • abnormal electrocardiogram (prolongation of the QT interval)
  • sudden signs of allergy such as skin rash, itching or hives, swelling of the face, lips, tongue or other parts of the body, shortness of breath, wheezing or difficulty breathing

These are very serious side effects. You may need urgent medical attention or hospitalisation. Occasionally, SAPHRIS may be associated with changes in liver function or blood such as cholesterol or triglyceride levels.

These can only be found when your doctor does tests from time to time to check your progress.

Other side effects not listed above may occur in some patients. Tell your doctor or pharmacist if you notice anything that is making you feel unwell.

Do not be alarmed by this list of possible side effects. You may not experience any of them.

After using Saphris

Storage

Keep your wafers in the original packaging until it is time to take them. If you take the wafers out of their packaging, they will not keep well.

Keep your wafers in a cool dry place where the temperature stays below 30°C.

Do not store SAPHRIS or any other medicine in the bathroom or near a sink.

Do not leave it on a windowsill or in the car on hot days. Heat and dampness can destroy some medicines.

Keep it where children cannot reach it. A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

Disposal

If your doctor tells you to stop taking SAPHRIS or the wafers have passed their expiry date, ask your pharmacist what to do with any that are left over.

Product description

What it looks like

SAPHRIS wafers come in two strengths.

5mg – white to off-white round wafer with a “5” marking on one side.

10mg – white to off-white round wafer with a “10” marking on one side.

SAPHRIS is available in blister packs of 20, 60 and 100 wafers*.

Ingredients

Active ingredients:

SAPHRIS 5mg – 5mg asenapine

SAPHRIS 10mg – 10mg asenapine

Other ingredients:

  • gelatin
  • mannitol

Supplier/Sponsor

In Australia

SAPHRIS is supplied in Australia by:

Lundbeck Australia Pty Ltd
1 Innovation Road
North Ryde NSW 2113
Ph: +61 2 8669 1000

Sponsor:

Merck Sharp & Dohme (Australia) Pty Limited
Level 1, Building A, 26 Talavera Road
Macquarie Park, NSW 2113
Australia

This leaflet was revised in December 2017

AUST R number(s):

SAPHRIS 5 mg AUST R 166562

SAPHRIS 10mg AUST R 166561

* Not all pack sizes may be marketed.

Ref no: S-CCPPI-MK8274 -SB-T-102017

Published by MIMS February 2018

Choose region and then country

Below is a copy of the content of the Consumer Medicine Information Leaflet provides with the Fluanxol medicine.

SAPHRIS®

5mg and 10mg sublingual wafers

Asenapine

Consumer Medicine Information

What is in this leaflet

This leaflet answers some common questions about SAPHRIS.

It does not contain all the available information.

It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor has weighed the risks of you taking SAPHRIS against the benefits they expect it will have for you.

If you have any concerns about taking this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine.

You may need to read it again.

What SAPHRIS is used for

SAPHRIS is used to treat the mental illnesses:

  • Schizophrenia – an illness with disturbances in thinking, feelings and behaviour.
  • Bipolar 1 disorder – an illness in which there are sustained mood swings either up (mania) or down (low moods). During mania, patients experience episodes of overactivity, elation or irritability. During low moods, patients may feel depressed or guilty, lack energy, lose their appetite and have trouble sleeping.

SAPHRIS belongs to a group of medicines called antipsychotics. It helps to correct chemical imbalances in the brain, which may cause these mental illnesses.

Your doctor may have prescribed SAPHRIS for another reason.

Ask your doctor if you have any questions about why SAPHRIS has been prescribed for you.

SAPHRIS is not addictive.

This medicine is available only with a doctor’s prescription.

Before you take SAPHRIS

When you must not take it

Do not take SAPHRIS if you have an allergy to:

  • asenapine the active ingredient in SAPHRIS
  • any of the other ingredients listed at the end of this leaflet

Some of the symptoms of an allergic reaction to SAPHRIS may include shortness of breath, wheezing or difficulty breathing; swelling of the face, lips, tongue or other parts of the body; rash, itching or hives on the skin or you may feel faint.

If you have diabetes or risk factors for diabetes, such as being overweight or a family history of diabetes, your blood sugar should be tested at the beginning of and throughout treatment with SAPHRIS. Complications of diabetes can be serious and even life-threatening. Tell your doctor if you have blood sugar problems or signs of diabetes, such as being thirsty all the time, going to the bathroom a lot, or feeling weak or hungry.

Do not take SAPHRIS if you are pregnant or breast-feeding unless your doctor tells you so. Ask your doctor about the risks and benefits involved.

It is not known if it is safe for you to take SAPHRIS while you are pregnant. However, if you need to take SAPHRIS during your pregnancy, the doctor will discuss the risks and benefits of taking it with you.

The following symptoms may occur in newborn babies, of mothers that have used antipsychotics in the last trimester (last three months of their pregnancy): shaking, muscle stiffness and/or weakness, sleepiness, agitation, breathing problems, and difficulty in feeding. If your baby develops any of these symptoms contact your doctor.

It is recommended that you do not breast-feed while taking SAPHRIS.

SAPHRIS is not recommended for use in children below 18 years of age.

There is not enough information on its effects in children.

Do not take SAPHRIS after the expiry date printed on the pack.

Do not use SAPHRIS if the packaging is torn or shows signs of tampering.

If it has expired or is damaged, return it to your pharmacist for disposal.

If you are not sure whether you should start taking SAPHRIS, talk to your doctor or pharmacist.

Before you start to take it

Tell your doctor if:

you have allergies to:

  • any other medicines
  • any other substances, such as foods, preservatives or dyes.

you have or have had any medical conditions, especially the following:

  • dementia (in elderly patients) or dementia with Lewy Bodies
  • Parkinson’s disease
  • heart disease / low blood pressure
  • liver disease
  • diabetes or family history of diabetes
  • difficulty in swallowing
  • epilepsy (seizures)
  • higher levels of the hormone, prolactin, in your blood
  • neuroleptic malignant syndrome – a reaction to some medicines with a sudden increase in body temperature, extremely high blood pressure and severe convulsions
  • tardive dyskinesia – a reaction to some medicines with worm-like movements of the tongue, or other uncontrolled movements of the mouth, tongue, cheeks or jaws which may progress to the arms and legs

Depression and other mental illnesses can lead to suicide. It is important to discuss all the risks of treating depression and mental illness as well as the risks of not treating it. You should discuss all treatment choices with your doctor, not just the use of anti-depressants.

Patients (and caregivers of patients) need to monitor for any worsening of their condition and/or the emergence of thoughts of suicide or suicidal behaviour or thoughts of harming themselves and to seek medical advice immediately if these symptoms present.

If you have not told your doctor about any of the above, tell him/her before you start taking SAPHRIS.

Taking other medicines

Tell your doctor or pharmacist if you are taking any other medicines, including any that you buy without a prescription from your pharmacy, supermarket or health food shop.

Some medicines and SAPHRIS may interfere with each other. These may include:

  • blood pressure lowering medicines
  • antidepressant drugs (e.g. paroxetine)

These medicines may be affected by SAPHRIS, or may affect how well it works. You may need different amounts of your medicine, or you may need to take different medicines.

Other medicines not listed above may also interfere with SAPHRIS. Your doctor and pharmacist have more information on medicines to be careful with or avoid while taking this medicine.

Use in children

The safety and effectiveness of SAPHRIS in children (below 18 years of age) has not been established.

How to take Saphris

Follow all directions given to you by your doctor or pharmacist carefully.

They may differ from the information contained in this leaflet.

If you do not understand the instructions on the box, ask your doctor or pharmacist for help.

How much to take

The dose of SAPHRIS is one wafer to be taken twice a day. Your doctor will tell you how many wafers you will need to take each day and how long you need to take it. This depends on your condition and whether or not you are taking any other medicines.

How to take it

Do not remove the wafer until ready to take.

Use dry hands when handling the wafer.

Do not push the wafer through the blister. Do not cut or tear the blister. Peel back the coloured tab.

Gently remove the wafer from the blister. Do not crush the wafer.

Place the wafer under your tongue and allow it to completely dissolve.

Do not chew or swallow the wafer.

Do not eat or drink for 10 minutes after taking the wafer.

Otherwise SAPHRIS will not be absorbed completely and it may not work as effectively.

How long to take it

Continue taking the wafers for as long as your doctor tells you.

SAPHRIS helps control your condition, but does not cure it. Therefore you must take SAPHRIS every day.

Do not stop taking SAPHRIS unless your doctor tells you to – even if you feel better.

If you forget to take it

If it is almost time for your next dose, skip the dose you missed and take your next dose when you are meant to.

Otherwise, take it as soon as you remember and then go back to taking your medicine as you would normally.

Do not take a double dose to make up for the dose that you missed.

If you are not sure what to do, ask your doctor or pharmacist.

If you have trouble remembering to take your medicine, ask your pharmacist for some hints.

If you take too much (overdose)

Immediately telephone your doctor or the Australian Poisons Information Centre (telephone 13 11 26) or the New Zealand National Poison Centre (telephone 0800 POISON or 0800 764 766) or go to Accident and Emergency at the nearest hospital, if you think that you or anyone else may have taken too much SAPHRIS. Do this even if there are no signs of discomfort or poisoning.

Keep telephone numbers for these places handy.

You may need urgent medical attention.

If you take too much SAPHRIS, you may feel restless, confused, drowsy, dizzy, sleepy or have a fast heart beat.

While you are taking SAPHRIS

Things you must do

Tell any other doctors, dentists, and pharmacists who are treating you that you are taking SAPHRIS.

If you are about to be started on any new medicine, tell your doctor, dentist or pharmacist that you are taking SAPHRIS.

If you plan to have surgery that needs a general anaesthetic, tell your doctor or dentist that you are taking SAPHRIS.

If you become pregnant while taking SAPHRIS, tell your doctor immediately.

If you are about to have any blood tests, tell your doctor that you are taking SAPHRIS.

SAPHRIS may interfere with the results of some tests.

Be sure to keep all of your doctor’s appointments so that your progress can be checked.

Your doctor will check your progress and may want to take some blood tests from time to time. This helps to reduce unwanted side effects.

If you or someone you know is demonstrating any of the following warning signs of suicide while taking SAPHRIS, contact your doctor or mental health professional immediately or go to the nearest hospital for treatment:

  • thoughts or talk of death or suicide
  • thoughts or talk of self-harm or harm to others
  • any recent attempts of self-harm
  • increase in aggressive behaviour, irritability or agitation
  • worsening of depression

Occasionally, the symptoms of depression may include thoughts of suicide or self-harm. These symptoms may continue or get worse during the early stages of treatment until the effect of the medicine becomes apparent.

All mentions of suicide or violence must be taken seriously.

Things you must not do

Do not give SAPHRIS to anyone else, even if they have the same condition as you.

Do not take SAPHRIS to treat any other complaints unless your doctor tells you to.

Do not stop taking SAPHRIS, or change the dosage, even if you are feeling better, without checking with your doctor.

If you stop taking SAPHRIS suddenly, your condition may worsen or your chance of getting an unwanted side effect may increase. To prevent this, your doctor may gradually reduce the amount of SAPHRIS you take each day before stopping completely.

Do not take any medicines that cause drowsiness while you are taking SAPHRIS, unless recommended by your doctor.

Things to be careful of

Be careful driving or operating machinery until you know how SAPHRIS affects you.

SAPHRIS may cause dizziness, and tiredness, in some people. Make sure you know how you react to SAPHRIS before you drive a car, operate machinery, or do anything else that could be dangerous if you are dizzy or sleepy.

If SAPHRIS makes you feel light-headed, dizzy or faint when getting out of bed or standing up, get up slowly.

Standing up slowly, especially when you get up from bed or chairs, will help your body get used to the change in position and blood pressure. If this problem continues or gets worse, talk to your doctor.

Be careful when drinking alcohol while taking SAPHRIS.

Combining SAPHRIS and alcohol can make you more sleepy or dizzy.

Your doctor may suggest you avoid alcohol while you are being treated with SAPHRIS.

Make sure you keep cool in hot weather and keep warm in cool weather.

SAPHRIS may affect the way your body reacts to temperature changes.

Side effects

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are taking SAPHRIS.

SAPHRIS helps most people with the symptoms of schizophrenia or with manic episodes associated with Bipolar 1 disorder. But it may have unwanted side effects in a few people. All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Therefore, it is important that you tell your doctor as soon as possible if you notice anything that is making you feel unwell, even if you think the problems are not connected with the medicine. Your doctor may then decide to adjust your dose or use a different medicine.

Ask your doctor or pharmacist to answer any questions you may have.

The following is a list of possible side effects. Do not be alarmed by this list. You may not experience any of them.

Tell your doctor or pharmacist if you notice any of the following and they worry you:

  • sleepiness
  • increased appetite, weight gain
  • drowsiness
  • tremor
  • sensation of numbness in the mouth
  • dry mouth
  • mouth ulcers and pain in the mouth
  • nausea
  • constipation
  • restlessness, agitation, anxiety, excitement or difficulty concentrating
  • an overwhelming urge to move such as feeling the need to pace, swing the legs while seated or rock from foot to foot
  • difficulty sleeping
  • headache
  • hot, dry skin
  • increased or decreased sweating
  • signs of increased blood sugar levels such as excessive thirst, hunger, weakness, urination or onset or worsening of diabetes.

These side effects are usually mild. Some of these side effects may go away after a while.

If any of the following happen, tell your doctor or pharmacist immediately or go to Accident and Emergency at your nearest hospital:

  • signs of frequent infections such as fever, chills, sore throat or mouth ulcers
  • extremely high body temperature
  • worm-like movements of the tongue, or other uncontrolled movements of the tongue, mouth, cheeks, or jaw which may progress to arms and legs
  • sudden onset of uncontrollable muscle spasms affecting the eyes, head, neck and body
  • fainting
  • convulsions, fits or seizures
  • severe spasms in the muscles of the shoulders, neck and upper body
  • sudden increase in body temperature, with sweating, fast heart beat, muscle stiffness and fluctuating blood pressure which may lead to coma
  • abnormal electrocardiogram (prolongation of the QT interval)
  • sudden signs of allergy such as skin rash, itching or hives, swelling of the face, lips, tongue or other parts of the body, shortness of breath, wheezing or difficulty breathing

These are very serious side effects. You may need urgent medical attention or hospitalisation. Occasionally, SAPHRIS may be associated with changes in liver function or blood such as cholesterol or triglyceride levels.

These can only be found when your doctor does tests from time to time to check your progress.

Other side effects not listed above may occur in some patients. Tell your doctor or pharmacist if you notice anything that is making you feel unwell.

Do not be alarmed by this list of possible side effects.

You may not experience any of them.

After using Saphris

Storage

Keep your wafers in the original packaging until it is time to take them.

If you take the wafers out of their packaging, they will not keep well.

Keep your wafers in a cool dry place where the temperature stays below 30°C.

Do not store SAPHRIS or any other medicine in the bathroom or near a sink.

Do not leave it on a windowsill or in the car on hot days.

Heat and dampness can destroy some medicines.

Keep it where children cannot reach it.

A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

Disposal

If your doctor tells you to stop taking SAPHRIS or the wafers have passed their expiry date, ask your pharmacist what to do with any that are left over.

Product description

What it looks like

SAPHRIS wafers come in two strengths.

5mg – white to off-white round wafer with a “5” marking on one side.

10mg – white to off-white round wafer with a “10” marking on one side.

SAPHRIS is available in blister packs of 20, 60 and 100 wafers*.

Ingredients

Active ingredients:

SAPHRIS 5mg – 5mg asenapine

SAPHRIS 10mg – 10mg asenapine

Other ingredients:

  • gelatin
  • mannitol

Supplier/Sponsor

In Australia

SAPHRIS is supplied in Australia by:

Lundbeck Australia Pty Ltd
1 Innovation Road
North Ryde NSW 2113
Ph: +61 2 8669 1000

Sponsor:

Merck Sharp & Dohme (Australia) Pty Limited
Level 1, Building A, 26 Talavera Road
Macquarie Park, NSW 2113
Australia

In New Zealand

SAPHRIS is supplied in New Zealand by:

Healthcare Logistics
PO Box 62027
Mt Wellington, Auckland
Ph: +64 9 918 5100

Toll Free Medical Enquiries Line (NZ consumers): 0800 540 554

Sponsor:

Merck Sharp & Dohme (New Zealand) Pty Limited
PO Box 99851
Newmarket
Auckland 1149
Phone number: (09) 375 9210

This leaflet was revised in October 2015

AUST R number(s):
SAPHRIS 5 mg AUST R 166562
SAPHRIS 10mg AUST R 166561

* Not all pack sizes may be marketed.

Ref no: CCPPI-MK8274-ASP-SB-102012

asenapine (Saphris, Saphris Black Cherry)

Brand Names: Saphris, Saphris Black Cherry

Generic Name: asenapine

  • What is asenapine (Saphris, Saphris Black Cherry)?
  • What are the possible side effects of asenapine (Saphris, Saphris Black Cherry)?
  • What is the most important information I should know about asenapine (Saphris, Saphris Black Cherry)?
  • What should I discuss with my healthcare provider before taking asenapine (Saphris, Saphris Black Cherry)?
  • How should I take asenapine (Saphris, Saphris Black Cherry)?
  • What happens if I miss a dose (Saphris, Saphris Black Cherry)?
  • What happens if I overdose (Saphris, Saphris Black Cherry)?
  • What should I avoid while taking asenapine (Saphris, Saphris Black Cherry)?
  • What other drugs will affect asenapine (Saphris, Saphris Black Cherry)?
  • Where can I get more information (Saphris, Saphris Black Cherry)?

What is asenapine (Saphris, Saphris Black Cherry)?

Asenapine is an antipsychotic medication. It works by changing the actions of chemicals in the brain.

Asenapine is used to treat schizophrenia in adults, and bipolar I disorder in adults and children who are at least 10 years old.

Asenapine may also be used for purposes not listed in this medication guide.

Saphris 10 mg

round, white, imprinted with 10

Saphris 5 mg

round, white, imprinted with 5

What are the possible side effects of asenapine (Saphris, Saphris Black Cherry)?

Get emergency medical help if you have signs of an allergic reaction: hives; fast heartbeats, feeling light-headed; wheezing, difficult breathing; swelling of your face, lips, tongue, or throat.

Asenapine can cause serious neurologic problems. Stop taking this medicine and call your doctor at once if you have: very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, feeling light-headed, tremors, twitching, or uncontrollable movements of your eyes, lips, tongue, face, arms, or legs.

High doses or long-term use of asenapine can cause a serious movement disorder that may not be reversible. Symptoms of this disorder include uncontrollable muscle movements of your lips, tongue, eyes, face, arms, or legs. The longer you take asenapine, the more likely you are to develop a serious movement disorder. The risk of this side effect is higher in women and older adults.

Call your doctor at once if you have:

  • slow heartbeats, a light-headed feeling (like you might pass out);
  • uncontrolled muscle movements in your face (chewing, lip smacking, frowning, tongue movement, blinking or eye movement);
  • sudden weakness or ill feeling, fever, chills, sore throat, swollen gums, painful mouth sores, skin sores, cold or flu symptoms, cough;
  • breast pain or swelling, nipple discharge;
  • trouble swallowing; or
  • sudden numbness or weakness (especially on one side of the body), sudden severe headache, slurred speech, problems with vision or balance.

Common side effects may include:

  • dizziness, drowsiness, feeling tired;
  • feeling restless or being unable to sit still;
  • numbness or tingling inside or around your mouth;
  • ulcers, blisters, swelling, or peeling of your gums;
  • nausea, altered sense of taste; or
  • increased appetite, weight gain.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What is the most important information I should know about asenapine (Saphris, Saphris Black Cherry)?

You should not use asenapine if you are allergic to it, or if you have severe liver disease.

Asenapine can cause serious neurologic problems. Stop taking this medicine and call your doctor at once if you have: very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, feeling light-headed, tremors, twitching, or uncontrollable movements of your eyes, lips, tongue, face, arms, or legs.

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.

Generic Name: Asenapine (a-SEN-a-peen)

Drug Class: Atypical Antipsychotics

Table of Contents

  • Overview
  • How to Take It
  • Side Effects
  • Warnings & Precautions
  • Drug Interactions
  • Dosage & Missing a Dose
  • Storage
  • Pregnancy or Nursing
  • More Information

Overview

Saphris (asenapine) is an antipsychotic medication used to treat symptoms conditions such as schizophrenia and bipolar disorder (manic depression) in adults, and for bipolar disorder in younger patients, ages 10–17. It may decrease hallucinations and prevent mood swings. It may also help those who take it to feel less anxious, think more clearly, and take more of an active role in everyday life.

This information is for educational purposes only. Not every known side effect, adverse effect, or drug interaction is in this database. If you have questions about your medicines, talk to your health care provider.

It works by helping change certain chemicals in the brain, which professionals refer to as “neurotransmitters.” It is not yet well-understood why changing these neurochemicals results in symptom relief for the conditions this drug is commonly prescribed for.

How to Take It

Follow the directions for using this medicine provided by your doctor. Continue to take this medicine even if you feel well. Do not miss any doses.

Side effects that may occur while taking this medicine include:

  • weight gain
  • excessive tiredness
  • dry mouth
  • headache
  • drowsiness
  • stomach pain
  • irritability/restlessness
  • change in taste
  • dizziness

Contact your doctor immediately if you experience:

  • lightheadedness
  • confusion
  • change in heartbeat (fast or irregular)
  • brown / red colored urine
  • rash or hives
  • hoarseness
  • wheezing / trouble breathing
  • fever
  • sweating

Warnings & Precautions

  • Let your doctor know if you have a family history of diabetes. Your blood sugar may be elevated while taking this medication, even if you do not already have diabetes.
  • Stop taking Saphris and call your doctor immediately if you have high fever, irregular heartbeats, tremors, rigid muscles, twitching, confusion, uncontrollable movements of the eyes, face, arms or legs, or sweating. This medicine can cause serious neurologic problems.
  • If you are allergic to asenapine or any other medications, let your doctor know.
  • It may be harder to cool your body down while you are taking this medication. You should drink plenty of water, dress lightly when the weather is hot, avoid a lot of exercise, and stay inside as much as possible.
  • Tell your doctor if you have seizures or epilepsy, low white blood cell count, a personal history of Long QT syndrome, Parkinson’s disease, liver or heart disease, or a history of breast cancer.
  • Consult with a doctor before administering this medication to any person younger than 18-years-old.
  • For an overdose, seek medical attention immediately. For non-emergencies, contact your local or regional poison control center at 1-800-222-1222.

Drug Interactions

Before taking any new medicine, either prescription or over-the-counter, check with your doctor or pharmacist. This includes supplements and herbal products.

Dosage & Missed Dose

Follow the instructions on your prescription label carefully. It is available in the form of a sublingual tablet, that should dissolve under the tongue. Generally it is taken 2x/day. After the tablet dissolves in your mouth, do not drink or eat anything for 10 minutes.

If you skip a dose, take your next dose as soon as you remember. If it is time for your next dose, skip the missed dose and go back to your regular schedule. Do not double doses or take extra medicine to make up for the missed dose.

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (preferably not in the bathroom). Throw away any medication that is outdated or no longer needed.

Pregnancy/Nursing

If you are pregnant, or plan to become pregnant, let your doctor know immediately. If taken during the last months of pregnancy, Saphris could cause problems in newborn babies.

More Information

For more information, talk to your doctor, pharmacist or health care provider, or you can visit this website, https://www.nlm.nih.gov/medlineplus/druginfo/meds/a610015.html for additional information from the manufacturer of this drug.

Saphris

Saphris (Black Cherry) Tablet, Sublingual

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 persist or worsen, 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 your doctor has prescribed this medication because he or she 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.

Infrequently, 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: signs of infection (such as fever, persistent sore throat).

Get medical help right away if you have any very serious side effects, including: severe dizziness, fainting, slow heartbeat, seizures, interrupted breathing during sleep.

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.

Antipsychotic drugs a last resort for these 5 conditions

2. Altamura AC, Serati M, Buoli M, Dell’Osso B. Augmentative quetiapine in partial/nonresponders with generalized anxiety disorder: a randomized, placebo-controlled study. Int Clin Psychopharmacol. 2011; 26(4):201-205.

3. Altamura AC, Serati M, Buoli M, et al. Augmentative quetiapine in partial/nonresponders with generalized anxiety disorder: a randomized, placebo-controlled study. Int Clin Psychopharmacol. 2011.21403524.

6. Armenteros JL, Lewis JE, Davalos M. Risperidone augmentation for treatment-resistant aggression in attention-deficit/hyperactivity disorder: a placebo-controlled pilot study. J Am Acad Child Adolesc Psychiatry. 2007;46(5):558-65.17450046.

8. Bandelow B, Chouinard G, Bobes J, et al. Extended-release quetiapine fumarate (quetiapine XR): a once-daily monotherapy effective in generalized anxiety disorder. Data from a randomized, double-blind, placebo-and active-controlled study. Int J Neuropsychopharmacol. 2009:1-16.19691907.

12. Correia Filho AG, Bodanese R, Silva TL, et al. Comparison of risperidone and methylphenidate for reducing ADHD symptoms in children and adolescents with moderate mental retardation. J Am Acad Child Adolesc Psychiatry. 2005;44(8):748-55.16034276.

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16. Hirschfeld RM, Weisler RH, Raines SR, Macfadden W; BOLDER Study Group. Quetiapine in the treat-ment of anxiety in patients with bipolar I or II depression: a secondary analysis from a randomized, double-blind, placebo-controlled study. J Clin Psychiatry. 2006; 67(3):355-362.

18. Joyce M, Khan A, Eggens I, et al. Efficacy and safety of extended release quetiapine fumarate (quetiapine XR) monotherapy in patients with generalized anxiety disorder (GAD). Poster presented at: 161st Annual Meeting of the American Psychiatric Association; May 3-8, 2008; Washington, DC.

21. Khan A, Atkinson S, Mezhebovsky I, She F, Leathers T, Pathak S. Efficacy and safety of once-daily extended release quetiapine fumarate (quetiapine XR) as an adjunct therapy in patients with treatment non-responsive generalized anxiety disorder (GAD). Poster presented at: 49th Annual New Clinical Drug Evaluation Unit Meeting; June 29-July 2, 2009; Hollywood, FL.

22. Khan A, Atkinson S, Mezhebovsky I, et al. Efficacy and safety of once-daily extended release quetiapine fumarate (quetiapine XR) as an adjunct therapy in patients with treatment nonresponsive generalized anxiety disorder (GAD). 49th Annual New Clinical Drug Evaluation Unit Meeting. June 29 -July 2, 2009:Poster.

25. McIntyre A, Gendron A, McIntyre A. Quetiapine adjunct to selective serotonin reuptake inhibitors or venlafaxine in patients with major depression, co-morbid anxiety, and residual depressive symptoms: a randomized, placebo-controlled pilot study. Depress Anxiety. 2007;24(7):487-494.

26. McIntyre A, Gendron A. Quetiapine adjunct to selective serotonin reuptake inhibitors or venlafaxine in patients with major depression, comorbid anxiety, and residual depressive symptoms: a randomized, placebo-controlled pilot study. Depress Anxiety. 2007;24(7):487-94.17177199.

27. Merideth C, Cutler A, Neijber A, et al. Efficacy and tolerability of extended release quetiapine fumarate monotherapy in the treatment of GAD. European Neuropsychopharmacology. 2008;18(Supplement 4):S499-S500.

28. Merideth C, Cutler A, Neijber A, She F, Eriksson H. Efficacy and tolerability of extended release quetiapine fumarate monotherapy in the treatment of GAD. Eur Neuropsychopharmacol. 2008;18(suppl 4): S499-S500.

33. Pollack MH, Simon NM, Zalta AK, et al. Olanzapine augmentation of fluoxetine for refractory generalized anxiety disorder: a placebo-controlled study. Biol Psychiatry. 2006;59(3):211-215.

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35. Reich DB, Winternitz S, Hennen J, et al. A preliminary study of risperidone in the treatment of post-traumatic stress disorder related to childhood abuse in women. J Clin Psychiatry. 2004;65(12):1601-6.

37. Sankaranarayanan J, Puumala SE. Antipsychotic use at adult ambulatory care visits by patients with mental health disorders in the United States, 1996-2003: national estimates and associated factors. Clin Ther. 2007;29(4):723-41.17617297.

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45. Zeni CP, Tramontina S, Ketzer CR, et al. Methylphenidate Combined with Aripiprazole in Children and Adolescents with Bipolar Disorder and Attention-Deficit/Hyperactivity Disorder: A Randomized Crossover Trial. Journal of Child and Adolescent Psychopharmacology. 2009;19(5):553-61.19877980.

The SGAs approved for use in the USA include clozapine, olanzapine, risperidone, paliperidone, quetiapine, ziprasidone, and aripiprazole, as well as two more that were approved in late 2009: iloperidone and asenapine. SGAs can be divided into classes based on chemical structure or mechanism of action. If divided by mechanism of action, classes would include serotonin/dopamine antagonists (all except aripiprazole) and partial dopamine agonist/serotonin antagonists (aripiprazole). The following are the SGAs in the order they were approved by the FDA:

1.

Clozapine is a dibenzodiazepine with a seven-member central ring that resembles a tricyclic antidepressant. At therapeutic levels, clozapine has low D2 occupancy, which likely leads to a lower incidence of EPS. It also has high affinity for 5-HT2A, 5-HT1C, adrenergic and cholinergic receptors, with higher 5-HT2A relative to D2 affinity, which was subsequently modeled by the atypical class. Clozapine is available in oral tablet form. Peak plasma concentration is 2 hours after administration with an elimination half-life of 12 hours. It is primarily metabolized by CYP 1A2 with some 2D6 and 3A3 (Marder and Wirshing, 2009).

2.

Risperidone is a benzisoxazole derivative with high D2 and 5‐HT2 affinity in vivo. It has little to no effect on muscarinic receptors and some effect on H1 receptors. Because of higher occupancy of D2 receptors, risperidone may lead to more EPS in patients compared to other atypicals. It also has relatively potent α2-adrenergic activity. Risperidone is available in oral and oral-dissolving formulations. It is rapidly absorbed and peak plasma levels are within 1 hour. It is 90% protein-bound. A long-acting injectable formulation of risperidone (Risperdal Consta) is comprised of risperidone embedded in biodegradable glycolide-lactide microspheres. These are not reliably released until approximately 3 weeks following administration with maximal release at 5 weeks, so oral risperidone must be administered during this time. Risperdal Consta injections must be administered every 2 weeks. Risperidone is hydroxylated by CYP2D6 and can be affected by other substances that alter metabolism in this pathway (Goff, 2009).

3.

Olanzapine is a thiobenzodazepine derivative with higher 5-HT2 affinity compared to D2, making it most similar to clozapine. It also has high affinity to H1 and α-adrenergic receptors (Ballon et al., 2009). It is available in both oral and oral-dissolving tablet forms, as well as in a short-acting injectable form for acute agitation. It is well absorbed orally, with a quicker onset of action for the oral-dissolving form. Peak plasma concentration for the injectable form is 15–45 minutes postadministration. CYP1A2 is primarily responsible for olanzapine’s metabolism and this can be impacted by CYP1A2 inducers (cigarette smoke) or inhibitors.

4.

Quetiapine is a dibenzothiazepine derivative. Like clozapine, it has relatively low affinity for D2 receptors (30% binding) compared to other antipsychotics (60–80%). Despite its low binding affinity, it is postulated that in the first 2 hours after administration D2 occupancy is higher (60–70%), but with more rapid dissociation from receptors correlating with the episodic dopamine surges into the synapses. Quetiapine also has effects at many other receptors, including the 5-HT2 family, α1-adrenergic and histaminic receptors (Buckley and Foster, 2009). Quetiapine is available in both direct-release and extended-release oral tablet forms. For direct release, peak plasma levels are achieved in 2 hours and sustained for 6 hours, leading to twice-daily dosing regimens. It is metabolized by CYP3A4 and can interact with inducers or inhibitors of this isoenzyme, and is secreted in the kidney. The XR formulation may have a lower incidence of side-effects such as sedation (Buckley and Foster, 2009).

5.

Ziprasidone is a benzisothiazolyl piperazine derivative with greater 5-HT2 affinity than dopamine, though it does have more D2 activity than olanzapine or clozapine. Limited affinity for histaminic and α-adrenergic receptors decreases the sedative and orthostatic effects in comparison with other medications. Ziprasidone is available as oral tablet and intramuscular injection for acute agitation. When administered orally, absorption is enhanced by the presence of food and it is recommended that ziprasidone be administered with at least 500 calories. With intramuscular administration, bioavailability is 100% and peak plasma concentration is within 30 minutes. Ziprasidone is hepatically metabolized through the P450 system as well as through reduction and S-methylation (Newcomer and Fallucco, 2009).

6.

Aripiprazole is a dihydroquinolinone with potent antagonism at 5-HT2A receptors and a unique feature of partial agonism at D2 receptors, and could be considered a “third-generation” antipsychotic (Rosenbaum et al., 2005). The development of this novel mechanism was prompted by the prevailing “dopamine hypothesis” of schizophrenia, that there is a biphasic disturbance in dopamine pathways with underactive dopamine in mesocortical pathways (negative, cognitive symptoms) and overactive dopamine in mesolimbic pathways (positive symptoms). In addition, it has high affinity for D3, D4, 5-HT2C, 5-HT7, α1-adrenergic, and H1 receptors (Sharif and Lieberman, 2009). Aripiprazole is available in oral tablet form as well as oral-dissolving, oral solution, and intramuscular injectable forms. Aripiprazole and its active metabolites are more than 99% protein-bound. It is primarily metabolized by CYP2D6 and CYP3A4.

7.

Paliperidone is the active metabolite of risperidone, 9-hydroxyrisperidone, and has a similar receptor profile. Compared to risperidone, however, it minimally binds to H1 receptors (Goff, 2009). It is available in an extended-release formulation. Absorption of this medication is enhanced by food administration by 50%. In comparison to risperidone, paliperidone is 74% protein-bound. In contrast, paliperidone is primarily excreted unchanged in the urine and can be safely administered to patients with liver dysfunction (Goff, 2009). The usual daily dose is 3–12 mg. The FDA recently approved a long-acting injectable formulation of paliperidone known as paliperidone palmitate (Invega Sustenna), which is approved for once-monthly administration.

8.

Iloperidone is a recently approved oral SGA with a serotonin 5-HT2A and dopamine D2 antagonist profile. Its efficacy is similar to that of other members of the atypical class. Iloperidone’s relatively higher affinity for the norepinephrine α1 receptor accounts for its tendency to cause orthostatic hypotension during the initial up-titration. It has a benign EPS, metabolic, and prolactin profile. It is metabolized by CYP3A4 and CYP206. Pharmacogenetic studies have indicated that response to, and side-effects with, iloperidone can be predicted using specific genetic markers. The usual daily dose is 12–24 mg.

9.

Asenapine is the only recently approved SGA that is available only in a sublingual formulation. It is also a serotonin 5-HT2A and dopamine D2 antagonist, with overall efficacy similar to other atypicals. It seems to have a better efficacy on negative symptoms than risperidone. It has a benign EPS, metabolic, and prolactin side-effects profile. The usual daily dose is 5 mg bid for schizophrenia and 10 mg bid for bipolar mania.

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