Asenapine side effects
Asenapine Sublingual: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing
Warnings:
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.
Warnings:
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.
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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 Asenapine 10 Mg Sublingual Tablet Antipsychotics (Excluding Select Aripiprazole Formulations)
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 not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).
Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).
This medication may make you sweat less, making you more likely to get heat stroke. Avoid doing things that may cause you to overheat, such as hard work or exercise in hot weather, or using hot tubs. When the weather is hot, drink a lot of fluids and dress lightly. If you overheat, quickly look for a place to cool down and rest. Get medical help right away if you have a fever that does not go away, mental/mood changes, headache, or dizziness.
Older adults may be more sensitive to the side effects of this drug, especially drowsiness, dizziness, lightheadedness, and QT prolongation (see above). Drowsiness, dizziness, and lightheadedness can increase the risk of falling.
During pregnancy, this medication should be used only when clearly needed. Babies born to mothers who have used this drug during the last 3 months of pregnancy may rarely develop symptoms including muscle stiffness or shakiness, drowsiness, feeding/breathing difficulties, or constant crying.
If you notice any of these symptoms in your newborn especially during their first month, tell the doctor right away.
Since untreated mental/mood problems (such as schizophrenia, bipolar disorder, depression) can be a serious condition, do not stop taking this medication unless directed by your doctor. If you are planning pregnancy, become pregnant, or think you may be pregnant, immediately discuss with your doctor the benefits and risks of using this medication during pregnancy.
It is unknown if this medication passes into breast milk. Consult your doctor before breast-feeding.
Interactions
Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.
Asenapine can slow down the removal of other medications from your body, which may affect how they work. One example is paroxetine, among others.
Tell your doctor or pharmacist if you are taking other products that cause drowsiness such as opioid pain or cough relievers (such as codeine, hydrocodone), alcohol, marijuana (cannabis), drugs for sleep or anxiety (such as alprazolam, lorazepam, zolpidem), muscle relaxants (such as carisoprodol, cyclobenzaprine), or antihistamines (such as cetirizine, diphenhydramine).
Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.
Does Asenapine 10 Mg Sublingual Tablet Antipsychotics (Excluding Select Aripiprazole Formulations) interact with other drugs you are taking?
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Overdose
If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911.
Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe drowsiness/deep sleep, agitation, confusion, fainting.
If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.
Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
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Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.
CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.
Asenapine (Saphris) | NAMI: National Alliance on Mental Illness
Brand names:
- Saphris®
- Sublingual tablet: 2.
5 mg, 5 mg, 10 mg
- Sublingual tablet: 2.
- Secuado®
- Extended-release transdermal patch: 3.8mg, 5.7mg, 7.6mg
Generic name: asenapine (a SEN a peen)
- Asenapine
- Sublingual tablet: 2.5 mg, 5 mg, 10 mg
All FDA black box warnings are at the end of this fact sheet. Please review before taking this medication.
What Is Asenapine And What Does It Treat?
Asenapine is a medication that works in the brain to treat schizophrenia. It is also known as a second-generation antipsychotic (SGA) or atypical antipsychotic. Asenapine rebalances dopamine and serotonin to improve thinking, mood, and behavior.
Symptoms of schizophrenia include:
- Hallucinations - imagined voices or images that seem real
- Delusions - beliefs that are not true (e.g., other people are reading your thoughts)
- Disorganized thinking or trouble organizing your thoughts and making sense
- Little desire to be around other people
- Trouble speaking clearly
- Lack of motivation
Asenapine may help some or all of these symptoms.
Asenapine is also FDA approved for the following indications:
- Acute treatment of manic or mixed episodes of bipolar I disorder in adults (alone or in combination with lithium or valproic acid)
- Acute treatment of manic episodes of bipolar I disorder in pediatrics (10 – 17 years old)
- Maintenance treatment of bipolar I disorder
This medication sheet will focus primarily on schizophrenia. You can find more information about bipolar disorders here.
This medication may be prescribed for other uses; ask your health care provider for more information.
What Is The Most Important Information I Should Know About Asenapine?
Schizophrenia requires long-term treatment. Do not stop taking asenapine, even when you feel better.
With input from you, your health care provider will assess how long you will need to take the medication.
Missing doses of asenapine may increase your risk for a relapse in your symptoms.
Do not stop taking asenapine or change your dose without talking with your health care provider first.
For asenapine to work properly, it should be taken every day as ordered by your health care provider.
Are There Specific Concerns About Asenapine And Pregnancy?
If you are planning on becoming pregnant, notify your health care provider to best manage your medications. People living with schizophrenia or certain other mental illness who wish to become pregnant face important decisions. This is a complex decision since untreated schizophrenia or other mental illness has risks to the fetus, as well as the mother. It is important to discuss the risks and benefits of treatment with your doctor and caregivers.
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.
Breastfeeding is not recommended in women who are taking asenapine. It is not known if asenapine passes into breast milk.
What Should I Discuss With My Health Care Provider Before Taking Asenapine?
- Symptoms of your condition that bother you the most
- If you have thoughts of suicide or harming yourself
- If you have ever had low white blood cell counts (low white blood cell counts have occurred with this drug which could increase risk of infections)
- Medications you have taken in the past for your condition, whether they were effective or caused any adverse effects
- If you ever had muscle stiffness, shaking, tardive dyskinesia, neuroleptic malignant syndrome, or weight gain caused by a medication
- If you experience side effects from your medications, discuss them with your provider. Some side effects may pass with time, but others may require changes in the medication.
- Any psychiatric or medical problems you have, such as liver problems, heart rhythm problems, long QT syndrome, heart attacks, diabetes, high cholesterol, or seizures
- If you have a family history of diabetes or heart disease
- All other medications you are currently taking (including over the counter products, herbal and nutritional supplements) and any medication allergies you have
- Other non-medication treatment you are receiving, such as talk therapy or substance abuse treatment.
Your provider can explain how these different treatments work with the medication. - If you are pregnant, plan to become pregnant, or are breastfeeding
- If you smoke, drink alcohol, or use illegal drugs
How Should I Take Asenapine?
Asenapine may help control your symptoms but will not cure your condition.
It may take two to three months before you feel the full effect of asenapine
Asenapine orally disintegrating sublingual tablets are usually taken 2 times per day. Do not eat or drink for 10 minutes after taking asenapine.
The sublingual tablets will dissolve within seconds when placed under your tongue. They should not be split, crushed, chewed, or swallowed.
Asenapine orally disintegrating tablets must remain in their original packaging. Open the package with clean dry hands before each dose. Do not put tablets in a pillbox if you take the orally disintegrating tablets.
The transdermal system is applied every 24 hours.
The transdermal system can get applied to the hip, abdomen, upper arm, or upper back area. Typically, patients begin at a low dose of medication and the dose is increased slowly over several weeks.
For the orally disintegrating sublingual tablet, the dose usually ranges from 5 mg to 10 mg.
For the transdermal system, the recommended starting dose is 3.8 mg/24 hours. This may increase to 5.7 mg/24 hours or 7.6 mg/24 hours after one week.
Only your health care provider can determine the correct dose for you.
Use a calendar, alarm clock, or cell phone alert to help you remember to take your medication. You may also ask a family member or friend to remind you or check in with you to be sure you are taking your medication.
What Happens If I Miss A Dose Of Asenapine?
It is important to take your medication everyday as directed by your health care provider. Do not miss or skip a dose.
If you miss a dose of asenapine, take it as soon as you remember, unless it is closer to the time of your next dose.
Discuss this with your health care provider. Do not double your next dose or take more than what is prescribed.
What Should I Avoid While Taking Asenapine?
Avoid drinking alcohol or using illegal drugs while you are taking asenapine. They may decrease the benefits (e.g., worsen your confusion) and increase adverse effects (e.g., sedation) of the medication.
If using the skin patch, avoid using a heating pad or other heating devices on the treated area.
What Happens If I Overdose With Asenapine?
If an overdose occurs call your doctor or 911. You may need urgent medical care. You may also contact the poison control center at 1-800-222-1222.
A specific treatment to reverse the effects of asenapine does not exist.
What Are The Possible Side Effects Of Asenapine?
This is not a complete list. Talk with your health care provider for more information.
Common side effects
Drowsiness, insomnia, restlessness, fatigue, extrapyramidal symptoms, headache, weight gain, increased glucose, cholesterol abnormalities, temporary numbness of the mouth or tongue
A skin reaction may occur by the transdermal system site during wear time or immediately after removal.
Use a different transdermal system application site each day to limit the occurrence of skin reactions.
Rare/serious side effects
Asenapine may increase the blood levels of a hormone called prolactin. Side effects of increased prolactin levels include females losing their period, production of breast milk and males losing their sex drive or possibly experiencing erectile problems. Long term (months or years) of elevated prolactin can lead to osteoporosis, or increased risk of bone fractures.
Some people may develop muscle related side effects while taking asenapine. The technical terms for these are “extrapyramidal symptoms” (EPS) and “tardive dyskinesia” (TD). Symptoms of EPS include restlessness, tremor, and stiffness. TD symptoms include slow or jerky movements that one cannot control, often starting in the mouth with tongue rolling or chewing movements.
Temperature regulation: Impaired core body temperature regulation may occur; caution with strenuous exercise, heat exposure, and dehydration.
Second generation antipsychotics (SGAs) increase the risk of weight gain, high blood sugar, and high cholesterol. This is also known as metabolic syndrome. Your health care provider may ask you for a blood sample to check your cholesterol, blood sugar, and hemoglobin A1c (a measure of blood sugar over time) while you take this medication.
- Information on healthy eating and adding exercise to decrease your chances of developing metabolic syndrome may be found at the following sites:
- http://www.helpguide.org/articles/healthy-eating/healthy-eating.htm
- http://www.helpguide.org/home-pages/exercise-fitness.htm
SGAs have been linked with higher risk of death, strokes, and transient ischemic attacks (TIAs) in elderly people with behavior problems due to dementia.
All antipsychotics have been associated with the risk of sudden cardiac death due to an arrhythmia (irregular heart beat). To minimize this risk, antipsychotic medications should be used in the smallest effective dose when the benefits outweigh the risks.
Your doctor may order an EKG to monitor for irregular heartbeat.
Neuroleptic malignant syndrome is a rare, life threatening adverse effect of antipsychotics which occurs in <1% of patients. Symptoms include confusion, fever, extreme muscle stiffness, and sweating. If any of these symptoms occur, contact your health care provider immediately.
All antipsychotics can cause sedation, dizziness, or orthostatic hypotension (a drop in blood pressure when standing up from sitting or lying down). These side effects may lead to falls which could cause bone fractures or other injuries. This risk is higher for people with conditions or other medications that could worsen these effects. If falls or any of these symptoms occur, contact your health care provider.
Are There Any Risks For Taking Asenapine For Long Periods Of Time?
Tardive dyskinesia (TD) is a side effect that develops with prolonged use of antipsychotics. Medications such as asenapine have been shown to have a lower risk of TD compared to older antipsychotics, such as Haldol® (haloperidol).
If you develop symptoms of TD, such as grimacing, sucking, and smacking of lips, or other movements that you cannot control, contact your health care provider immediately. All patients taking either first- or second-generation antipsychotics should have an Abnormal Involuntary Movement Scale (AIMS) completed regularly by their health care provider to monitor for TD.
Second generation antipsychotics (SGAs) increase the risk of diabetes, weight gain, high cholesterol, and high triglycerides. (See “Serious Side Effects” section for monitoring recommendations).
What Other Medications May Interact With Asenapine?
Tell your health care provider about all medications that you take, have recently taken or plan to take including prescription and nonprescription medications, vitamins, herbal products, and nutritional supplements. This medication may affect the way other medications work, and other medications may affect how this medication works.
Asenapine may block the effects of agents used to treat Parkinson’s disease such as levodopa/carbidopa (Sinemet®), bromocriptine, pramipexole (Mirapex®), ropinirole (Requip®), and others.
The following medications may increase the risk of heart problems when used with asenapine:
- Antipsychotics, including chlorpromazine (Thorazine®), thioridizine (Mellaril®), iloperidone (Fanapt®), paliperidone (Invega®), quetiapine (Seroquel®), and ziprasidone (Geodon®).
- Antiarrhythmics (heart rhythm medications), including procainamide, quinidine, amiodarone (Cordarone®), dronedarone (Multaq®), and sotalol (Betapace®).
The following medications may increase the levels and effects of asenapine:
- Fluvoxamine (Luvox®), paroxetine (Paxil®), and ciprofloxacin (Cipro®).
How Long Does It Take For Asenapine To Work?
It is very important to tell your doctor how you feel things are going during the first few weeks after you start taking asenapine. It will probably take several weeks to see big enough changes in your symptoms to decide if asenapine is the right medication for you.
Antipsychotic treatment is generally needed lifelong for persons with schizophrenia. Your doctor can best discuss the duration of treatment you need based on your symptoms and illness.
- Hallucinations, disorganized thinking, and delusions may improve in the first 1-2 weeks
- Sometimes these symptoms do not completely go away
- Motivation and desire to be around other people can take at least 1-2 weeks to improve
- Symptoms continue to get better the longer you take asenapine
- It may take 2-3 months before you get the full benefit of asenapine
Summary of FDA Black Box Warnings
Increased mortality in elderly patients with dementia related psychosis
- Both first generation (typical) and second generation (atypical) antipsychotics are associated with an increased risk of mortality in elderly patients when used for dementia related psychosis.
- Although there were multiple causes of death in studies, most deaths appeared to be due to cardiovascular causes (e.
g., sudden cardiac death) or infection (e.g., pneumonia). - Antipsychotics are not indicated for the treatment of dementia related psychosis.
Provided by
(November 2022)
©2022 The College of Psychiatric and Neurologic Pharmacists (CPNP) and the National Alliance on Mental Illness (NAMI). CPNP and NAMI make this document available under the Creative Commons Attribution-No Derivatives 4.0 International License. Last Updated: January 2016.
This information is being provided as a community outreach effort of the College of Psychiatric and Neurologic Pharmacists. This information is for educational and informational purposes only and is not medical advice. This information contains a summary of important points and is not an exhaustive review of information about the medication. Always seek the advice of a physician or other qualified medical professional with any questions you may have regarding medications or medical conditions.
Never delay seeking professional medical advice or disregard medical professional advice as a result of any information provided herein. The College of Psychiatric and Neurologic Pharmacists disclaims any and all liability alleged as a result of the information provided herein.
Content
- Pharmacological mechanism
- INSTALLY
- Features of use
- Side effects
- Medicine interactions
- Contraindications
Azenapine - atypic anti -and -photograph -Plough. According to the corporation, taking the drug causes minimal anticholinergic and cardiovascular side effects and little weight gain. By the end of summer 2009a full series of clinical trials was conducted in which more than 3,000 patients participated. A majority of FDA agency advisors voted to approve the drug. On August 14, 2009, a positive decision by the agency approved the use of the drug for schizophrenia and bipolar disorder, and asenapine joined the list of antipsychotics used in psychiatry.
Some American clinician psychiatrists have begun prescribing asenapine also to war veterans for the treatment of post-traumatic stress disorder accompanied by nightmares, although the use of the drug for this purpose has not yet been approved by the US Department of Veterans Affairs. nine0003
Mechanism of pharmacological action
Azenapine exhibits high affinity for many types of receptors, including serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT5A, 5-HT6 and 5-HT7 receptors , adrenergic α1, α2A, α2B and α2C, dopamine D1, D2, D3 and D4, histamine h2 and h3. It exhibits significantly less affinity for muscarinic acetylcholine receptors. Asenapine is a partial agonist of 5-HT1A- and D1-receptors, it exhibits antagonist properties to the rest of the mentioned receptors. nine0003
Since asenapine is still less of a histamine receptor blocker than some of the other atypical antipsychotics (olanzapine, quetiapine), it is expected to be less likely to cause weight gain and sedation.
Blocking dopamine receptors weaker than haloperidol, asenapine rarely causes extrapyramidal disorders and an increase in prolactin. Therefore, this drug can be considered as a treatment option in patients who are at risk of developing the metabolic syndrome, and also in the case when other drugs have been discontinued due to intolerable side effects, such as akathisia. In addition, asenapine is less likely to cause QT interval prolongation on electrocardiogram than ziprasidone. However, all the mentioned effects are inherent in it to one degree or another, although relatively infrequently. nine0003
Indications
Asenapine has been approved by the FDA for the treatment of adult acute episodes of schizophrenia and acute manic or mixed episodes (with or without psychotic symptoms) in bipolar I affective disorder.
The drug is not indicated for the treatment of depression, in clinical trials it was not found to reduce depressive symptoms in both the short and long term.
Asenapine is not approved for the treatment of dementia associated with psychosis; in clinical trials in patients with dementia, it increased the risk of mortality. nine0003
Application features
Azenapine is taken sublingually (under the tongue). The drug requires a special mode of administration, taking into account, in particular, the time of nutrition and fluid intake. It is recommended to take asenapine twice a day, after which food and liquid intake should be avoided for at least 10 minutes.
When swallowed, this drug has a low bioavailability.
Side effects
Very common side effects (≥1/10): anxiety, drowsiness. nine0003
Frequent side effects (≤1/100 -
Uncommon (≤1/1000 -
Rare (≤1/10,000 -
Frequency unknown: allergic reactions, restless leg syndrome, nausea, lesions of the oral mucosa, salivary hypersecretion, neonatal withdrawal syndrome.
The FDA reports a risk of severe allergic reactions with asenapine, which include anaphylactic shock, angioedema, low blood pressure, increased heart rate, swollen tongue, shortness of breath, and rash.
In some cases, these symptoms appeared after the first dose of the drug. The FDA program encourages healthcare professionals and patients to report side effects. nine0003
With long-term use of asenapine, frequently occurring effects such as sedation, drowsiness, insomnia, depression, headaches, weight gain and changes in blood glucose levels, tremor, akathisia, parkinsonism, tardive dyskinesia were noted.
Precautions
Azenapine should be used with caution in the elderly, in patients with cardiovascular disease (myocardial infarction, ischemic heart disease, heart failure or conduction disturbance), cerebrovascular disease, and in the presence of factors predisposing to the development of hypotension (dehydration, hypovolemia, antihypertensive therapy). Caution should be exercised in the treatment of patients receiving simultaneously other drugs that can cause hypotension, bradycardia, respiratory depression or CNS. In all these cases, it is necessary to regularly carry out an orthostatic test, if hypotension occurs, the dose of asenapine should be reduced.
nine0003
Metabolic side effects may occur when taking asenapine, therefore it is necessary to monitor body weight, regularly measure fasting glucose and lipid levels. If the patient is diabetic or has any other signs of the metabolic syndrome prior to initiation of asenapine, the drug should be avoided and other options considered (eg, aripiprazole, ziprasidone that do not cause such side effects).
Drug interactions
Concomitant use of asenapine and other medicinal products known to prolong the QTc interval should be avoided, including class 1A antiarrhythmics (eg, quinidine, procainamide) or class 3 antiarrhythmics (eg, amiodarone, sotalol), antipsychotics (eg, ziprasidone, chlorpromazine , thioridazine), antibacterial agents (eg gatifloxacin, moxifloxacin). Asenapine should be avoided in patients with a history of cardiac arrhythmias and other factors that may increase the risk of torsade de pointes and / or sudden death due to the use of drugs that prolong the QTc interval (bradycardia, hypokalemia, hypomagnesemia), as well as with the presence of congenital long QT syndrome.
nine0003
Asenapine is a weak inhibitor of cytochrome P450 2D6, which reduces the likelihood of pharmacokinetic interactions, but nevertheless it should be used with caution in combination with those drugs that are metabolized by CYP2D6 (for example, paroxetine, most tricyclic antidepressants, amoxapine, captopril, duloxetine , fluoxetine, fluvoxamine, haloperidol). According to a clinical study, asenapine significantly increased the blood concentration of paroxetine. In addition, because asenapine is metabolized by CYP1A2, caution should be exercised when co-administered with substances that induce the CYP1A2 enzyme (eg, smoking, carbamazepine, rifampicin) or inhibit this enzyme (eg, fluvoxamine, ciprofloxacin, ketoconazole). nine0003
Contraindications
Asenapine should not be used in patients at risk of aspiration pneumonia. In patients with severe hepatic impairment (Child-Pugh class C), there was a 7-fold increase in the concentration of asenapine, so it is not recommended to prescribe this drug in such patients.
Arpimed
What Azaleptin is and what it is used for
Clozapine is the active ingredient in Azaleptin, which belongs to the group of antipsychotics (drugs used to treat certain mental disorders such as psychosis). nine0003
Azaleptin is used to treat schizophrenia in people who have not responded well to other drugs.
Schizophrenia is a mental illness that affects the way a person thinks, feels, and behaves. You should only use this drug if you have already used at least two other antipsychotics, one of which was a new-generation atypical antipsychotic, for schizophrenia that did not work or caused serious untreated side effects. nine0003
Azaleptin is also used to treat severe thinking, emotional and behavioral disorders in people with Parkinson's disease for whom other drugs have failed.
What you need to know before taking Azaleptin
The drug is also not used if you have a low level of leukocytes in the blood, due to previous chemotherapy, 
If any of the above apply to you, contact your doctor and stop taking Azaleptin.
Azaleptin should not be used in people who are unconscious or in a coma.
Special instructions and precautions
The safety precautions mentioned in this section are very important. You must follow them to minimize your risk of developing serious, life-threatening side effects.
Before starting treatment with Azaleptin, tell your doctor if you have or have ever had:0006 Tell your doctor right away before taking Azaleptin tablets if: Medical examinations and blood tests Before you start taking Azaleptin, your doctor will need to review your medical history and do blood tests to make sure your white blood cell count is normal. It is important to be aware of this, as the body needs white blood cells to fight infections. It is necessary to conduct periodic blood tests before starting treatment, during treatment and after discontinuation of Azaleptin. nine0092 Your doctor can also do physical examinations before starting treatment. To check the condition of the heart, he may do an electrocardiogram (ECG), but only if necessary or if you have an indication for this. nine0003 If you have impaired liver function, you should have regular tests to evaluate liver function throughout the course of taking Azaleptin. If you have high blood sugar (diabetes mellitus), your doctor will need to monitor your blood sugar regularly. Azaleptin may cause changes in blood lipid levels. Azaleptin may cause weight gain. If you experience dizziness or weakness while taking Azaleptin, gently get up from a sitting or lying position. If you are scheduled for surgery or if for some reason you are unable to walk for a long period of time, talk to your doctor about taking Azaleptin as there is a risk of thrombosis (venous thrombosis). Children and adolescents under 16 If you are under 16 years old, you should not take Azaleptin because there is not enough data on its use in this age group. Elderly people (aged 60 years and older) In older people (aged 60 years and older), the following side effects may more often occur during treatment with Azaleptin: weakness or dizziness after a change in body posture, fast heartbeat, difficulty urinating and constipation. nine0003 Tell your doctor or pharmacist if you have dementia. Other medicines and Azaleptin Tell your doctor or pharmacist if you are taking, have recently taken or should take any other medicines. This includes over-the-counter or herbal medicines. You may need to change the dosage of the drug or take other drugs. Do not take Azaleptin at the same time as medicines that depress the bone marrow and/or reduce the number of blood cells, such as: These drugs increase the risk of agranulocytosis (low white blood cell count). Use of Azaleptin concomitantly with other medicinal products that may affect the effects of Azaleptin and/or other medicinal products. This is not an exhaustive list. Your doctor and pharmacist may have more information about medicines that you should be careful about or avoid taking Azaleptin. They can also tell you if the drugs you are taking are in the above groups or not. Consult with them. nine0003 Azaleptin with food and drink Avoid alcohol while using Azaleptin. Tell your doctor if you smoke and how often you drink caffeinated drinks (coffee, tea, cola). Sudden changes in smoking habits or intake of caffeinated beverages may also affect the effects of Azaleptin. How to take Azaleptin In order to minimize the risk of falling blood pressure, seizures and drowsiness, it is necessary that your doctor gradually increase the dose of the drug. You should always take Azaleptin exactly as prescribed by your doctor. If you have any doubts, you should consult your doctor or pharmacist. nine0003 In the first place, it is important not to change the dosage or stop taking Azaleptin without notifying your doctor. If the dose you have been prescribed cannot be reached with this dose, there are other doses of this drug that must be used to reach the desired dose of the drug. nine0003 Azaleptin tablets can be divided into equal doses. Treatment of schizophrenia The recommended starting dose is 12.5 mg (half a 25 mg tablet) once or twice on the first day followed by 25 mg once or twice on the second day. Swallow the tablet with water. If this dose is well tolerated, your doctor may gradually increase the dose in steps of 25 to 50 mg over the next 2-3 weeks until the dose reaches 300 mg per day. Thereafter, if necessary, the daily dose may be increased further in steps of 50 to 100 mg at half a week, or preferably at weekly intervals. The recommended daily dose is 200 to 450 mg divided into several single doses per day. Some people may need a higher dose. The permissible daily dose can be up to 900 mg. Frequent side effects (in particular, convulsions) are possible at daily doses of more than 450 mg. Always take the individually determined minimum effective dose of the drug for you. Most people take part of their dose in the morning and another part in the evening. Your healthcare professional will advise you on how to properly divide your daily dose. If your daily dose is only 200 mg, then you can take it once in the evening. During a certain period of time when you are taking Azaleptin and you have positive results, your doctor may reduce the dose. It is necessary to take Azaleptin for at least 6 months. nine0003 Treatment of severe thought disorders in patients with Parkinson's disease The recommended starting dose is 12. The recommended daily dose is 25 to 37.5 mg taken once in the evening. The dose of 50 mg per day should only be exceeded in exceptional cases. The maximum daily dose is 100 mg. Always take the minimum effective dose of the drug individually selected for you. If you have taken more Azaleptin than recommended . nine0003 Symptoms of overdose include: salivation, pupil dilation, blurred vision, low blood pressure, collapse, fast or irregular heartbeat, shallow or labored breathing. If you forget to take Azaleptin If you forget to take your next dose, take it as soon as you remember. If it is time for your next dose, skip the missed dose and take your next dose at the usual recommended time. Do not take a double dose to make up for a missed dose. Contact your doctor as soon as possible if you have not taken Azaleptin at all for more than 48 hours. If you stop taking Azaleptin Do not stop taking Azaleptin without your doctor's advice as you may experience withdrawal symptoms. It includes sweating, headache, nausea, vomiting, and diarrhea. If you experience any of the above symptoms, tell your doctor right away. These symptoms may be followed by more serious side effects if not treated immediately. nine0092 Symptoms of the underlying disease may reappear. A gradual dose reduction in 12.5 mg increments over one to two weeks is recommended if treatment is to be discontinued. If your doctor decides to resume treatment with Azaleptin and the last dose of Azaleptin was taken more than two days ago, then the recommended initial dose should be 12.5 mg. nine0003 If you have any further questions about the use of this medicine, ask your doctor or pharmacist. Pregnancy and breastfeeding If you are pregnant or breastfeeding, think you may be pregnant or are planning to become pregnant, ask your doctor or pharmacist before taking this medicine. Your doctor can discuss with you the benefits and possible risks of taking the drug during pregnancy. Contact your doctor immediately if you become pregnant while taking Azaleptin. nine0003 Pregnancy Newborns whose mothers took Azaleptin during the last trimester (last three months) of pregnancy may experience the following symptoms: trembling, muscle rigidity and/or weakness, drowsiness, irritability, breathing problems and difficulty when feeding. Breastfeeding Do not breastfeed while taking Azaleptin. Clozapine, the active ingredient in Azaleptin, is excreted in breast milk and may harm your baby. Women of childbearing age Some women who take certain medications for mental illness have irregular or no periods. If you have this observed, you can restore the regularity of menstruation if you replace the medication you are taking with Azaleptin. This means that you must use effective contraception. nine0003 Effects on the ability to drive and use machines Azaleptin may cause fatigue, drowsiness and convulsions, especially at the beginning of treatment. You should not drive or operate machinery while you have these symptoms. Azaleptin contains lactose If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicine. Possible side effects Like all medicines, Azaleptin can cause side effects, although not everyone gets them. Some side effects can be serious and require medical attention: Call your doctor right away before using Azaleptin tablets if you experience any of the following side effects: Very common ( may affect more than 1 in 10 people ) : Common (may affect up to 1 in 10 people): Uncommon (may affect up to 1 in 100 people): Rare (may affect up to 1 in 1,000 people): Very rare (may affect up to 1 in 10,000 people): Unknown (frequency of adverse reactions has not been estimated according to available data): neck and upper abdomen), shortness of breath, sweating, weakness, dizziness, nausea, vomiting, and palpitations (symptoms of a heart attack). You must seek emergency medical attention immediately. nine0006 Other side effects0148 ) : Drowsiness, dizziness, increased salivation. Common (may affect up to 1 in 10 people): weight gain, blurred vision, headache, trembling, stiffness, restlessness, convulsions, impaired movement, inability to start moving, inability to control movement of different parts of the body, ECG changes, high blood pressure, weakness or dizziness after changing body posture, nausea, vomiting , loss of appetite, dry mouth, minor liver function test abnormalities, loss of urinary control, difficulty urinating, fatigue, fever, increased sweating, fever, speech disturbances (eg, slurred speech). nine0003 Uncommon (may affect up to 1 in 100 people): Decreased levels of white blood cells (agranulocytosis), speech problems (eg, stuttering). Rare (may affect up to 1 in 1,000 people): surrounding the heart muscle (pericarditis), accumulation of fluid in the pericardial cavity (pericardial exudate), high blood sugar, diabetes mellitus, increased levels of the enzyme creatine phosphokinase in the blood. Very rare (may affect up to 1 in 10,000 people) behavior (obsessive-compulsive symptoms), skin reactions, salivary gland enlargement, difficulty breathing, complications from uncontrolled blood sugar (eg, coma or ketoacidosis), elevated blood triglycerides or cholesterol, heart muscle disease (cardiomyopathy), cardiac arrest , sudden unexplained death. nine0003 Not known (frequency of adverse reactions not estimated to the available data): Liver disorders including hepatic steatosis (fatty liver), liver cell necrosis, liver toxicity, liver disorders that include replacement of normal liver tissue coarse fibrous (scar) tissue leading to loss of liver function, including those that lead to life-threatening consequences such as liver failure (which can lead to death), liver damage (damage to liver cells, liver bile ducts, or both) together) and liver transplantation, electroencephalogram (EEG) changes, diarrhea, stomach discomfort, heartburn, stomach discomfort after eating, muscle weakness, muscle spasms, muscle pain, nasal congestion, bedwetting, sudden, uncontrolled increase in blood pressure ( pseudopheochromocytoma), uncontrolled bending of the body to one side (pleura totonus) if you are a man; ejaculation disorders, accompanied by an abnormal passage of seminal fluid, as a result of which the ejaculate enters the cavity of the bladder instead of ejaculating through the penis (orgasm without semen or retrograde ejaculation), rash, purplish-red spots, fever or itching due to inflammation of the blood vessels, inflammation large intestine leading to diarrhea, abdominal pain, fever, discoloration of the skin, butterfly rash on the face, joint pain, muscle pain, fever and fatigue (lupus erythematosus). Older people with dementia have been reported to experience a slight increase in the number of deaths among those taking antipsychotics compared with patients not taking antipsychotics. Reporting side effects: Tell your doctor, pharmacist or nurse if you notice any side effects. This includes any possible side effects not listed in this package insert. You can also report side effects to Arpimed LLC by going to the website www.arpimed.com and filling out the appropriate form “Report a side effect or ineffectiveness of a drug” and to the Scientific Center for Expertise of Drugs and Medical Technologies named after. Academician E.Gabrielyan, by going to the website www.pharm.am in the section “Report a side effect of a drug” and fill out the form “Map of reporting a side effect of a drug”. Scientific center hotline: +37410237665; +37498773368 How to store Azaleptin Keep out of the reach of children, dry, dark place at a temperature of 15 0 C-25 0 C. Shelf life - 3 years. Do not take Azaleptin after the expiry date which is stated on the package and on each blister. When specifying the expiration date, the last day of the specified month is meant. Do not dispose of medicines in wastewater or sewers. Ask your pharmacist how to dispose of a medicine you no longer need. These measures are aimed at protecting the environment. nine0003 Contents of the pack and additional information What Azaleptin contains One tablet contains: active ingredient: 1 mg clozapine 90 248 excipients: microcrystalline cellulose, lactose monohydrate, corn starch, povidone, sodium starch glycolate, magnesium stearate. What Azaleptin looks like and contents of the pack Yellow, round, biconvex tablets, notched on one side, odorless. Packaging description 10 tablets in a blister pack (PVC/aluminium).
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Your health care provider should treat constipation to avoid further complications. nine0006
Between weeks 18 and 52, tests should be done at least every 2 weeks. Later tests should be done at least once a month. nine0006 
Your healthcare provider should monitor your weight and blood lipid levels. nine0003 
Tell your doctor if you plan to take, are taking (even if your treatment is ending), or if you have recently had to stop taking any of the following medicines:
Continue taking the drug for as long as your doctor tells you to. If you are 60 years of age or older, your doctor may start treatment at a lower dosage and increase it gradually, as patients in this age group are more likely to develop some unwanted side effects (See "What you need to know before using Azaleptin"). 
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5 mg (half a 25 mg tablet) in the evening. Swallow the tablet with water. Your healthcare provider may then gradually increase your dose in 12.5 mg steps, no faster than two steps per week, up to a maximum dose of 50 mg by the end of the second week. Increasing the dosage should be stopped or postponed if you feel weak, dizzy or confused. In order to avoid these symptoms, blood pressure should be measured during the first weeks of treatment. nine0003 
Your doctor will tell you how to reduce the daily dose of the drug. If you have to suddenly stop treatment with Azaleptin, you will need to consult your doctor for this. 
If your child has any of the above symptoms, you should contact your doctor. 
nine0003 severe constipation. Your doctor must treat this side effect so that you can avoid further complications.
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