(roe si gli' ta zone)
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CONGESTIVE HEART FAILURE AND MYOCARDIAL ISCHEMIA
— Thiazolidinediones, including rosiglitazone, cause or exacerbate congestive heart failure in some patients. After initiation of rosiglitazone maleate, and after dose increases, observe patients carefully for signs and symptoms of heart failure (including excessive, rapid weight gain, dyspnea, and/or edema). If these signs and symptoms develop, the heart failure should be managed according to current standards of care. Furthermore, discontinuation or dose reduction of rosiglitazone maleate must be considered.
— Rosiglitazone Maleate is not recommended in patients with symptomatic heart failure. Initiation of rosiglitazone maleate in patients with established NYHA Class III or IV heart failure is contraindicated.— A meta-analysis of 42 clinical studies (mean duration 6 months; 14,237 total patients), most of which compared rosiglitazone maleate to placebo, showed rosiglitazone maleate to be associated with an increased risk of myocardial ischemic events such as angina or myocardial infarction. Three other studies (mean duration 41 months; 14,067 total patients), comparing rosiglitazone maleate to some other approved oral antidiabetic agents or placebo, have not confirmed or excluded this risk. In their entirety, the available data on the risk of myocardial ischemia are inconclusive.
Monotherapy and Combination Therapy
Rogislitazone tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Important Limitations of Use
|Dosage & Administration||
The management of antidiabetic therapy should be individualized. All patients should start rosiglitazone maleate tablets at the lowest recommended dose. Further increases in the dose of rosiglitazone maleate tablets should be accompanied by careful monitoring for adverse events related to fluid retention.
Rosiglitazone maleate tablets may be administered at a starting dose of 4 mg either as a single daily dose or in 2 divided doses. For patients who respond inadequately following 8 to 12 weeks of treatment, as determined by reduction in fasting plasma glucose (FPG), the dose may be increased to 8 mg daily as monotherapy or in combination with metformin, sulfonylurea, or sulfonylurea plus metformin. Rosiglitazone maleate tablets may be taken with or without food.
The total daily dose of rosiglitazone maleate tablets should not exceed 8 mg.
The usual starting dose of rosiglitazone maleate tablets is 4 mg administered either as a single dose once daily or in divided doses twice daily. In clinical trials, the 4-mg twice-daily regimen resulted in the greatest reduction in FPG and hemoglobin A1c (HbA1c).
Combination With Sulfonylurea or Metformin
When rosiglitazone maleate tablets is added to existing therapy, the current dose(s) of the agent(s) can be continued upon initiation of therapy with rosiglitazone maleate tablets.
When used in combination with sulfonylurea, the usual starting dose of Rosiglitazone maleate is 4 mg administered as either a single dose once daily or in divided doses twice daily. If patients report hypoglycemia, the dose of the sulfonylurea should be decreased.
The usual starting dose of Rosiglitazone Maleate in combination with metformin is 4 mg administered as either a single dose once daily or in divided doses twice daily. It is unlikely that the dose of metformin will require adjustment due to hypoglycemia during combination therapy with Rosiglitazone Maleate.
Combination With Sulfonylurea Plus Metformin
The usual starting dose of rosiglitazone maleate tablets in combination with a sulfonylurea plus metformin is 4 mg administered as either a single dose once daily or divided doses twice daily. If patients report hypoglycemia, the dose of the sulfonylurea should be decreased.
Specific Patient Populations
No dosage adjustment is necessary when Rosiglitazone maleate is used as monotherapy in patients with renal impairment. Since metformin is contraindicated in such patients, concomitant administration of metformin and Rosiglitazone maleate is also contraindicated in patients with renal impairment.
Liver enzymes should be measured prior to initiating treatment with rosiglitazone maleate. Therapy with rosiglitazone maleateshould not be initiated if the patient exhibits clinical evidence of active liver disease or increased serum transaminase levels (ALT >2.5X upper limit of normal at start of therapy). After initiation of rosiglitazone maleate, liver enzymes should be monitored periodically per the clinical judgment of the healthcare professional.
PediatricData are insufficient to recommend pediatric use of rosiglitazone maleate.
|Overdosage||Supportive treatment is recommended.|
|Contraindications||NYHA (New York Heart Association) class I to IV heart failure, acute coronary syndrome, ischaemic heart disease, Type 1 DM. Not to be used in treatment of diabetic ketoacidosis.|
|Special Precautions||Restrict for use in Type 2 DM patients who are unable to achieve adequate glycaemic control with other medications. Rosiglitazone can cause fluid retention, and may cause or exacerbate CHF; monitor patients for signs and symptoms of heart failure. Caution in patients with oedema. May be associated with elevated risk of myocardial ischaemic events such as angina and MI. Co-admin with insulin or nitrates is not recommended. Liver impairment; monitor liver function prior to- and periodically during treatment. Discontinue therapy if ALT> 3x ULN or if jaundice occurs. May cause resumption of ovulation in some premenopausal anovulatory female, contraception is recommended. Not recommended for patients with peripheral arterial disease. Do not use during pregnancy or lactation.|
|Adverse Drug Reaction(s)||Hypoglycaemia; dose-related wt gain, oedema and anaemia; upper respiratory tract infections, nasopharyngitis, sinusitis, constipation, hypertension, back pain, increased risk of bone fractures (especially in females), fatigue, macular oedema, hepatitis, elevated liver enzymes, hyperlipidaemia.
Potentially Fatal: CHF; may increase risk of myocardial ischaemia.
|Drug Interactions||Increased effect with NSAIDs, pioglitazone, gemfibrozil, fluconazole, sulfonamides. Decreased effect with carbamazepine, phenytoin, secobarbital, phenobarbital and rifampicin. Increased risk of fluid retention when used with NSAIDs. Increased risk of hypoglycaemia when used with quinolones.
Potentially Fatal: Increased effect with NSAIDs, pioglitazone, gemfibrozil, fluconazole, sulfonamides. Decreased effect with carbamazepine, phenytoin, secobarbital, phenobarbital and rifampicin. Increased risk of fluid retention when used with NSAIDs. Increased risk of hypoglycaemia when used with quinolones.
|Food Interaction||May decrease serum levels when used with St John's wort. Avoid alcohol.|
|Pregnancy Category (FDA)||Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.|
|Storage||Oral: Store at 25°C.|
|Pharmacology||Rosiglitazone is a thiazolidinedione antidiabetic agent which improves insulin sensitivity by lowering blood glucose level without increasing pancreatic insulin secretion. It is dependent on the presence of insulin. Rosiglitazone is a potent agonist for the peroxisome proliferator-activated receptor-gamma, which in turn regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport and utilisation.
Duration: 12 wk.
Absorption: Well absorbed from the GI tract after oral admin. Peak plasma concentrations after 1 hr.
Distribution: Protein-binding: 99.8%.
Metabolism: Extensively metabolised by CYP2C8.
Excretion: Urine (64%); faeces (23%); 3-4 hr (elimination half-life).
|ATC Classification||A10BG02 - rosiglitazone; Belongs to the class of thiazolidinediones. Used in the treatment of diabetes.|
|Brand Name||Manufacturer/Marketer||Composition||Dosage Form||Pack Size & Price|
|ROGLIT 4||Pacific Pharmaceuticals Ltd.||Rosiglitazone maleate INN 4mg||Film Coated Tablet||30's: 240.00 MRP|
|ROMEROL||Drug International Ltd||Rosiglitazone maleate INN 2mg & 4mg||Film Coated Tablet||2mg x50's, 4mg x30's: 250.00 & 240.00 MRP|
|TAZON-4||Kemiko Pharmaceuticals Ltd||Rosiglitazone maleate INN 4mg||Film Coated Tablet||30's: 240.00 MRP|
Rosiglitazone may cause fluid retention (a condition where the body keeps excess fluid) that may lead to or worsen congestive heart failure (condition in which the heart is unable to pump enough blood to the other parts of the body). Before you start to take rosiglitazone, tell your doctor if you have or have ever had congestive heart failure, especially if your heart failure is so severe that you must limit your activity and are only comfortable when you are at rest or you must remain in a chair or bed. Also tell your doctor if you were born with a heart defect, and if you have or have ever had swelling of the arms, hands, feet, ankles, or lower legs; heart disease, high blood pressure; coronary artery disease (narrowing of the blood vessels that lead to the heart); a heart attack; an irregular heartbeat; or high cholesterol or fats in the blood. Your doctor may tell you not to take rosiglitazone or may monitor you carefully during your treatment.
If you develop congestive heart failure or other heart problems, you may experience certain symptoms. Tell your doctor immediately if you have any of the following symptoms, especially when you first start taking rosiglitazone or after your dose is increased: large weight gain in a short period of time; shortness of breath; swelling of the arms, hands, feet, ankles, or lower legs; swelling or pain in the stomach; waking up short of breath during the night; the need to sleep with extra pillows in order to breathe while lying down; frequent dry cough; or increased tiredness.
Taking rosiglitazone may increase the risk that you will experience a heart attack. This risk may be higher if you take insulin along with rosiglitazone. Your doctor may tell you not to take rosiglitazone if you are taking insulin. Tell your doctor or get emergency medical care immediately if you experience any of the following symptoms: shortness of breath; pain in the jaw, arm, back, neck, or stomach; pain in the center of the chest that lasts for a more than a few minutes or that goes away and comes back; uncomfortable pressure, fullness, or squeezing in the chest; breaking out in a cold sweat; nausea or vomiting; or lightheadedness.
A program has been set up to limit the use of rosiglitazone and to inform people about the increased the risk of heart attack while taking this medication. Only people are already taking rosiglitazone and people whose blood sugar cannot be controlled by other medications should consider taking rosiglitazone. The program also makes sure that everyone who takes rosiglitazone understands the risks and benefits of taking the medication and has talked to his or her doctor about these risks.
You will be able to take rosiglitazone only if you and the doctor who prescribes your medication have enrolled in the program. You will receive your medication by mail from a participating pharmacy; you will not be able to get your medication from a local retail pharmacy. Ask your doctor if you have any questions about participating in the program or receiving your medication.
Your doctor or pharmacist will give you the manufacturer's patient information sheet (Medication Guide) when you begin treatment with rosiglitazone and each time you refill your prescription. Read the information carefully and ask your doctor or pharmacist if you have any questions. You can also visit the Food and Drug Administration (FDA) website (http://www.fda.gov/Drugs) or the manufacturer's website to obtain the Medication Guide.
Talk to your doctor about the risks of taking rosiglitazone.
Why is this medication prescribed?
Rosiglitazone is used along with a diet and exercise program and sometimes with one or more other medications to treat type 2 diabetes (condition in which the body does not use insulin normally and therefore cannot control the amount of sugar in the blood). Because of the risk of serious side effects, rosiglitazone should only be used to treat people who are already taking the medication, or people whose blood sugar cannot be controlled with other medications and who have decided not to take pioglitazone (Actos, a medication that is similar to rosiglitazone but that may not cause the same serious side effects) for medical reasons. Rosiglitazone is in a class of medications called thiazolidinediones. It works by increasing the body's sensitivity to insulin, a natural substance that helps control blood sugar levels. Rosiglitazone is not used to treat type 1 diabetes (condition in which the body does not produce insulin and therefore cannot control the amount of sugar in the blood) or diabetic ketoacidosis (a serious condition that may occur if high blood sugar is not treated).
How should this medicine be used?
Rosiglitazone comes as a tablet to take by mouth. It is usually taken once or twice daily with or without meals. Take rosiglitazone at about the same time(s) 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 rosiglitazone exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Your doctor may increase your dose of rosiglitazone after 8-12 weeks, based on your body's response to the medication.
Rosiglitazone helps control type 2 diabetes but does not cure it. It may take 2 weeks for your blood sugar to decrease, and 2-3 months or longer for you to feel the full benefit of rosiglitazone. Continue to take rosiglitazone even if you feel well. Do not stop taking rosiglitazone without talking to your doctor.
Other uses for this medicine
- tell your doctor if you are allergic to rosiglitazone or any other medications.
- tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: gemfibrozil; other medications for diabetes; medications for high blood pressure, high cholesterol, heart failure, or prevention of heart attack or stroke; and rifampin. 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 any of the conditions mentioned in the IMPORTANT WARNING section or diabetic eye disease such as macular edema (swelling of the back of the eye); or liver disease. Also tell your doctor if you have ever taken troglitazone, especially if you stopped taking it because you experienced side effects.
- tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking rosiglitazone, call your doctor.
- if you have not yet experienced menopause (change of life; end of monthly menstrual periods) you should know that rosiglitazone may increase the chance that you will become pregnant even if you do not have regular monthly periods or you have a condition that prevents you from ovulating (releasing an egg from the ovaries). Talk to your doctor about methods of birth control that will work for you.
What special dietary instructions should I follow?
runny nose and other cold symptoms
- back pain
Some side effects can be serious. If you experience any of the following symptoms, or those listed in the IMPORTANT WARNING section, call your doctor immediately:
loss of appetite
yellowing of the skin or eyes
difficulty seeing colors
difficulty seeing in the dark
swelling of the eyes, face, lips, tongue, or throat
difficulty swallowing or breathing
Rosiglitazone may cause other side effects. Call your doctor if you experience any unusual problems while you are taking this medication.
Taking rosiglitazone may increase the risk that you will experience a fracture, usually in the upper arms, hands, or feet. Talk to your doctor about the risk of taking this medication and about ways to keep your bones healthy during your treatment.
What should I know about storage and disposal of this medication?
In case of overdose, consult your doctor. If the victim has collapsed or is not breathing, consult local medical emergency services.
What other information should I know?
You should always wear a diabetic identification bracelet to be sure you get proper treatment in an emergency.
Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.
It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.
This information is provided for reference only and not a replacement for and should only be used in conjunction with full consultation with a registered medical practitioner. It may not contain all the available information you require and cannot substitute professional medical care, nor does it take into account all individual circumstances. Although great effort has been made to ensure content accuracy, mph-bd shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise.
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*Trademark name & prescribing information are the property of their respective Manufacturers.