Apiz: Product Information
Apiz - Product Information
Pharmacology
Aripiprazole possesses a novel mechanism of action when compared to the other FDA approved atypical antipsychotics. Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. Partial agonism at D2 receptors has been shown to modulate dopaminergic activity in areas where dopamine activity may be high or low, such as the mesolimbic and mesocortical areas of the schizophrenic brain, respectively. In addition to partial agonist activity at the D2 receptor, aripiprazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors.
Pharmacokinetics
Aripiprazole displays linear kinetics with an elimination half-life of approximately 75 hours. Accordingly, steady state plasma concentrations are achieved in about 14 days. Cmax (maximum plasma concentration) is achieved in 3-5 hours after oral dosing. The bioavailabilty of the oral tablets is about 90%. The drug undergoes extensive hepatic metabolization (dehydrogenation, hydroxylation, and N-dealkylation). The active major metabolite is dehydro-aripiprazole with an elemination half-life of about 94 hours. The parent drug is excreted only in traces and the metabolites, whether active or not, are excreted via feces and urine.
Metabolism
Aripiprazole is metabolized by the cytochrome P450 isoenzymes 3A4 and 2D6. Accordingly, coadministration of aripiprazole with medications that may inhibit (e.g paroxetine, fluoxetined) or induce (e.g. carbamazepine) these metabolic enzymes may increase or decrease, respectively, plasma concentrations of aripiprazole
Adverse events
Adverse events reported in the package insert for aripiprazole include headache, nausea, vomiting, somnolence, insomnia and akathisia. It appears that aripiprazole has a very low incidence of EPS (extrapyramidal side effects). The risk of tardive dyskinesia with prolonged aripiprazole use is unclear.
Dosage forms
Apiz is available as 10 and 15 mg tablets.
Dosage:
10 -15mg per day or as directed by physician. It has been observed that increasing the dose beyond 15 mg per dayb does not impart any particular therapeutic benefit. On the other hand, it may only add to the cost of treatment.
Warning about drugs having similar names
A warning has gone out recently because of this drug's name. The '-prazole' ending of this drug name makes this drug sound like it is one of the proton pump inhibitors (such as omeprazole, pantoprazole, lansoprazole) which are used in treating peptic ulcer disease. However, aripiprazole and these drugs are in an entirely different class of drugs altogether and confusing the two can lead to some unnecessary side effects.
Why is aripiprazole prescribed?
Aripiprazole is used to treat the symptoms of schizophrenia (a mental illness that causes disturbed or unusual thinking, loss of interest in life, and strong or inappropriate emotions). It is also used to treat episodes of mania (frenzied, abnormally excited or irritated mood) or mixed episodes (symptoms of mania and depression that happen together) in patients with bipolar I disorder (manic depressive disorder; a disease that causes episodes of depression, episodes of mania, and other abnormal moods). Aripiprazole is in a class of medications called atypical antipsychotics. It works by changing the activity of certain natural substances in the brain.
How should this medicine be used?
Aripiprazole comes as a tablet to be taken by mouth. It is usually taken once a day with or without food. Take aripiprazole at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take aripiprazole exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Your doctor may start you on a low dose of aripiprazole and increase your dose after at least 2 weeks.
Aripiprazole controls schizophrenia but does not cure it. It may take 2 weeks or longer before you feel the full benefit of aripiprazole. Continue to take aripiprazole even if you feel well. Do not stop taking aripiprazole without talking to your doctor.
What special precautions should I follow?
Before taking aripiprazole,
tell your doctor and pharmacist if you are allergic to aripiprazole or any other medications. Tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking. Be sure to mention any of the following: amiodarone (Cordarone, Pacerone); antidepressants (mood elevators); antifungals such as fluconazole (Diflucan), itraconazole (Sporanox), and ketoconazole (Nizoral); antihistamines; bupropion (Wellbutrin); carbamazepine (Tegretol); celecoxib (Celebrex); chlorpromazine (Thorazine); cimetidine (Tagamet); clarithromycin (Biaxin); clomipramine (Anafranil); cyclosporine (Neoral, Sandimmune); danazol (Danocrine); delavirdine (Rescriptor); dexamethasone (Decadron); diltiazem (Cardizem, Dilacor, Tiazac); doxorubicin (Adriamycin); erythromycin (E.E.S., E-Mycin, Erythrocin); ethosuximide (Zarontin); fluoxetine (Prozac, Sarafem); fluvoxamine (Luvox); HIV protease inhibitors such as indinavir (Crixivan) and ritonavir (Norvir); ipratropium (Atrovent); isoniazid (INH, Nydrazid); medications for anxiety, blood pressure, irritable bowel disease, mental illness, motion sickness, Parkinson's disease, seizures, ulcers, or urinary problems; metoclopramide (Reglan); methadone (Dolophine); metronidazole (Flagyl); nefazodone (Serzone); oral contraceptives (birth control pills); paroxetine (Paxil); phenobarbital (Luminal, Solfoton); phenytoin (Dilantin); primidone (Mysoline); quinidine (Cardioquin, Quinaglute, Quinidex); ranitidine (Zantac); rifabutin (Mycobutin); rifampin (Rifadin, Rimactane); sedatives; sertraline (Zoloft); sleeping pills; terbinafine (Lamisil); tranquilizers; troglitazone (Rezulin); troleandomycin (TAO); verapamil (Calan, Covera, Isoptin, Verelan); and zafirlukast (Accolate). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
tell your doctor if you have or have ever had heart disease, heart failure, high or low blood pressure, a stroke, a ministroke, seizures, Alzheimer's disease, any condition that makes it difficult for you to swallow, or if you or anyone in your family has or has ever had diabetes. Also tell your doctor if you have ever had to stop taking a medication for mental illness because of severe side effects.
tell your doctor if you are pregnant or plan to become pregnant. If you become pregnant while taking aripiprazole, call your doctor. Do not breastfeed while taking aripiprazole. If you are having surgery, including dental surgery, tell the doctor or dentist that you are taking aripiprazole.
you should know that aripiprazole may make you drowsy. Do not drive a car or operate machinery until you know how this medication affects you.
remember that alcohol can add to the drowsiness caused by this medication. Do not drink alcohol while taking aripiprazole.
you should know that you may have increases in your blood sugar (hyperglycemia) while you are taking this medication, even if you do not already have diabetes. If you have schizophrenia, you are more likely to develop diabetes than people who do not have schizophrenia, and taking aripiprazole or similar medications may increase this risk. Tell your doctor immediately if you have any of the following symptoms while you are taking aripiprazole: extreme thirst, frequent urination, extreme hunger, blurred vision, or weakness. It is very important to call your doctor as soon as you have any of these symptoms, because high blood sugar can cause more serious symptoms, such as dry mouth, upset stomach and vomiting, shortness of breath, breath that smells fruity, or decreased consciousness, and may become life-threatening if it is not treated at an early stage.
you should know that aripiprazole may cause dizziness, lightheadedness, and fainting when you get up too quickly from a lying position. This is more common when you first start taking aripiprazole. To avoid this problem, get out of bed slowly, resting your feet on the floor for a few minutes before standing up.
you should know that aripiprazole may make it harder for your body to cool down when it gets very hot. Tell your doctor if you plan to do vigorous exercise or be exposed to extreme heat. Make sure to drink plenty of fluids.
What special dietary instructions should I follow?
Talk to your doctor about drinking grapefruit juice while taking this medicine.
What should I do if I forget a dose?
Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
What side effects can this medication cause?
Aripiprazole may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
Pharmacology
Aripiprazole possesses a novel mechanism of action when compared to the other FDA approved atypical antipsychotics. Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. Partial agonism at D2 receptors has been shown to modulate dopaminergic activity in areas where dopamine activity may be high or low, such as the mesolimbic and mesocortical areas of the schizophrenic brain, respectively. In addition to partial agonist activity at the D2 receptor, aripiprazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors.
Pharmacokinetics
Aripiprazole displays linear kinetics with an elimination half-life of approximately 75 hours. Accordingly, steady state plasma concentrations are achieved in about 14 days. Cmax (maximum plasma concentration) is achieved in 3-5 hours after oral dosing. The bioavailabilty of the oral tablets is about 90%. The drug undergoes extensive hepatic metabolization (dehydrogenation, hydroxylation, and N-dealkylation). The active major metabolite is dehydro-aripiprazole with an elemination half-life of about 94 hours. The parent drug is excreted only in traces and the metabolites, whether active or not, are excreted via feces and urine.
Metabolism
Aripiprazole is metabolized by the cytochrome P450 isoenzymes 3A4 and 2D6. Accordingly, coadministration of aripiprazole with medications that may inhibit (e.g paroxetine, fluoxetined) or induce (e.g. carbamazepine) these metabolic enzymes may increase or decrease, respectively, plasma concentrations of aripiprazole
Adverse events
Adverse events reported in the package insert for aripiprazole include headache, nausea, vomiting, somnolence, insomnia and akathisia. It appears that aripiprazole has a very low incidence of EPS (extrapyramidal side effects). The risk of tardive dyskinesia with prolonged aripiprazole use is unclear.
Dosage forms
Apiz is available as 10 and 15 mg tablets.
Dosage:
10 -15mg per day or as directed by physician. It has been observed that increasing the dose beyond 15 mg per dayb does not impart any particular therapeutic benefit. On the other hand, it may only add to the cost of treatment.
Warning about drugs having similar names
A warning has gone out recently because of this drug's name. The '-prazole' ending of this drug name makes this drug sound like it is one of the proton pump inhibitors (such as omeprazole, pantoprazole, lansoprazole) which are used in treating peptic ulcer disease. However, aripiprazole and these drugs are in an entirely different class of drugs altogether and confusing the two can lead to some unnecessary side effects.
Why is aripiprazole prescribed?
Aripiprazole is used to treat the symptoms of schizophrenia (a mental illness that causes disturbed or unusual thinking, loss of interest in life, and strong or inappropriate emotions). It is also used to treat episodes of mania (frenzied, abnormally excited or irritated mood) or mixed episodes (symptoms of mania and depression that happen together) in patients with bipolar I disorder (manic depressive disorder; a disease that causes episodes of depression, episodes of mania, and other abnormal moods). Aripiprazole is in a class of medications called atypical antipsychotics. It works by changing the activity of certain natural substances in the brain.
How should this medicine be used?
Aripiprazole comes as a tablet to be taken by mouth. It is usually taken once a day with or without food. Take aripiprazole at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take aripiprazole exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Your doctor may start you on a low dose of aripiprazole and increase your dose after at least 2 weeks.
Aripiprazole controls schizophrenia but does not cure it. It may take 2 weeks or longer before you feel the full benefit of aripiprazole. Continue to take aripiprazole even if you feel well. Do not stop taking aripiprazole without talking to your doctor.
What special precautions should I follow?
Before taking aripiprazole,
tell your doctor and pharmacist if you are allergic to aripiprazole or any other medications. Tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking. Be sure to mention any of the following: amiodarone (Cordarone, Pacerone); antidepressants (mood elevators); antifungals such as fluconazole (Diflucan), itraconazole (Sporanox), and ketoconazole (Nizoral); antihistamines; bupropion (Wellbutrin); carbamazepine (Tegretol); celecoxib (Celebrex); chlorpromazine (Thorazine); cimetidine (Tagamet); clarithromycin (Biaxin); clomipramine (Anafranil); cyclosporine (Neoral, Sandimmune); danazol (Danocrine); delavirdine (Rescriptor); dexamethasone (Decadron); diltiazem (Cardizem, Dilacor, Tiazac); doxorubicin (Adriamycin); erythromycin (E.E.S., E-Mycin, Erythrocin); ethosuximide (Zarontin); fluoxetine (Prozac, Sarafem); fluvoxamine (Luvox); HIV protease inhibitors such as indinavir (Crixivan) and ritonavir (Norvir); ipratropium (Atrovent); isoniazid (INH, Nydrazid); medications for anxiety, blood pressure, irritable bowel disease, mental illness, motion sickness, Parkinson's disease, seizures, ulcers, or urinary problems; metoclopramide (Reglan); methadone (Dolophine); metronidazole (Flagyl); nefazodone (Serzone); oral contraceptives (birth control pills); paroxetine (Paxil); phenobarbital (Luminal, Solfoton); phenytoin (Dilantin); primidone (Mysoline); quinidine (Cardioquin, Quinaglute, Quinidex); ranitidine (Zantac); rifabutin (Mycobutin); rifampin (Rifadin, Rimactane); sedatives; sertraline (Zoloft); sleeping pills; terbinafine (Lamisil); tranquilizers; troglitazone (Rezulin); troleandomycin (TAO); verapamil (Calan, Covera, Isoptin, Verelan); and zafirlukast (Accolate). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
tell your doctor if you have or have ever had heart disease, heart failure, high or low blood pressure, a stroke, a ministroke, seizures, Alzheimer's disease, any condition that makes it difficult for you to swallow, or if you or anyone in your family has or has ever had diabetes. Also tell your doctor if you have ever had to stop taking a medication for mental illness because of severe side effects.
tell your doctor if you are pregnant or plan to become pregnant. If you become pregnant while taking aripiprazole, call your doctor. Do not breastfeed while taking aripiprazole. If you are having surgery, including dental surgery, tell the doctor or dentist that you are taking aripiprazole.
you should know that aripiprazole may make you drowsy. Do not drive a car or operate machinery until you know how this medication affects you.
remember that alcohol can add to the drowsiness caused by this medication. Do not drink alcohol while taking aripiprazole.
you should know that you may have increases in your blood sugar (hyperglycemia) while you are taking this medication, even if you do not already have diabetes. If you have schizophrenia, you are more likely to develop diabetes than people who do not have schizophrenia, and taking aripiprazole or similar medications may increase this risk. Tell your doctor immediately if you have any of the following symptoms while you are taking aripiprazole: extreme thirst, frequent urination, extreme hunger, blurred vision, or weakness. It is very important to call your doctor as soon as you have any of these symptoms, because high blood sugar can cause more serious symptoms, such as dry mouth, upset stomach and vomiting, shortness of breath, breath that smells fruity, or decreased consciousness, and may become life-threatening if it is not treated at an early stage.
you should know that aripiprazole may cause dizziness, lightheadedness, and fainting when you get up too quickly from a lying position. This is more common when you first start taking aripiprazole. To avoid this problem, get out of bed slowly, resting your feet on the floor for a few minutes before standing up.
you should know that aripiprazole may make it harder for your body to cool down when it gets very hot. Tell your doctor if you plan to do vigorous exercise or be exposed to extreme heat. Make sure to drink plenty of fluids.
What special dietary instructions should I follow?
Talk to your doctor about drinking grapefruit juice while taking this medicine.
What should I do if I forget a dose?
Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
What side effects can this medication cause?
Aripiprazole may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
- headache
- nervousness
- difficulty falling asleep or staying asleep
- drowsiness
- lightheadedness
- restlessness
- upset stomach
- vomiting
- constipation
- increased salivation
- weight gain
- coughing
- runny nose
- shaking hands that you cannot control
- dry skin
- itchy eyes
- loss of appetite
Some side effects can be serious. The following symptoms are uncommon, but if you experience any of them or those listed in the SPECIAL PRECAUTIONS section, call your doctor immediately:
- rash
- dizziness
- fainting
- slow, fast, or irregular heartbeat
- chest pain
- swelling of hands, feet, ankles, or lower legs
- depression
- seizures
- difficulty swallowing
- unusual movements of your body or face that you cannot control
- urgent need to urinate
- high fever
- muscle stiffness
- confusion
- sweating
- abnormal excitement
Aripiprazole may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.
For further information on Apiz, please write to:
Mr. Mukesh Vanakani – General Manager
Or
Mr. Deepak Shah B.Pharma. MBA
At
posted by Reliance Formulation Pvt. Ltd. | 10:56 PM
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