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Rosiglitazone is an anti-diabetic drug in the thiazolidinedione class of drugs. It is marketed by the pharmaceutical company GlaxoSmithKline as a stand-alone drug (Avandia) and in combination with metformin (Avandamet) or with glimepiride (Avandaryl). Like other thiazolidinediones, the mechanism of action of rosiglitazone is by activation of the intracellular receptor class of the peroxisome proliferator-activated receptors (PPARs), specifically PPARγ.
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Rosiglitazone is an anti-diabetic drug from the thiazolidinedione class. Like other thiazolidinediones, its mechanism of action is by activation of the intracellular receptor class of the peroxisome proliferator-activated receptors (PPARs), specifically PPAR-gamma. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Apart from its effect on insulin resistance, it appears to have an infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।" data-rx-term="inflammation" data-rx-definition="Inflammation is the body’s response to injury, infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।">inflammation, pain, or swelling. সহজ বাংলা: প্রদাহ/ফোলা/ব্যথা কমায়।" data-rx-term="anti-inflammatory" data-rx-definition="Anti-inflammatory means reducing inflammation, pain, or swelling. সহজ বাংলা: প্রদাহ/ফোলা/ব্যথা কমায়।">anti-inflammatory effect: nuclear factor kappa-B (NF& #954; B) levels fall and inhibitor levels increase in patients on rosiglitazone (Mohanty et al). It increases glyceroneogenesis and reduces the release of free fatty acids from adipocytes; Rosiglitazone is an anti-diabetic drug from the thiazolidinedione class. It is being marketed as Avandia by the pharmaceutical company GlaxoSmithKline, both as a standalone preparation and in combination with metformin (Avandamet). Another combination drug approved by the FDA is Avandaryl (with glimepiride); Like other thiazolidinediones, its mechanism of action is by activation of the intracellular receptor class of the peroxisome proliferator-activated receptors (PPARs), specifically PPAR-gamma. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha binding action. Apart from its effect on insulin resistance, it appears to have an anti-inflammatory effect: nuclear factor kappa-B (NFkB) levels fall and inhibitor (IkB) levels increase in patients on rosiglitazone (Mohanty et al). It increases glyceroneogenesis and reduces the release of free fatty acids from adipocytes.
Mechanism of Action of Rosiglitazone
Rosiglitazone acts as a highly selective and potent agonist at peroxisome proliferator activated receptors (PPAR) in target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR-gamma receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In this way, rosiglitazone enhances tissue sensitivity to insulin.
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Indications of Rosiglitazone
- Type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">Diabetes Mellitus
- Nonalcoholic Fatty Liver Disease
- To improve glycemic control in adult patients with type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">diabetes mellitus as an adjunct to diet and exercise.
Therapeutic Uses
- Type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">Diabetes Mellitus
- Antidiabetic agent
- Rosiglitazone is indicated as monotherapy and as adjunctive therapy to diet and exercise in the management of patients with type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">diabetes mellitus (previously referred to as non-insulin-dependent diabetes mellitus). Rosiglitazone is also indicated for use in combination with a sulfonylurea, metformin, or insulin when diet, exercise, and either rosiglitazone alone, a sulfonylurea alone, metforminalone or insulin alone do not result in adequate glycemic control in patients with type 2 diabetes. Rosiglitazone is also indicated for use in combination with a sulfonylurea plus metformin when diet, exercise, and both agents do not result in adequate glycemic control.
- 1-Methyl-4-phenylpyridinium ion (MPP(+)), an inhibitor of mitochondrial complex I, has been widely used as a neurotoxin because it elicits a severe Parkinson’s disease-like syndrome with elevation of intracellular reactive oxygen species (ROS) level and apoptotic death. Rosiglitazone, a peroxisome proliferator-activated receptor (PPAR)-gamma agonist, has been known to show various non-hypoglycemic effects, including infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।" data-rx-term="inflammation" data-rx-definition="Inflammation is the body’s response to injury, infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।">inflammation, pain, or swelling. সহজ বাংলা: প্রদাহ/ফোলা/ব্যথা কমায়।" data-rx-term="anti-inflammatory" data-rx-definition="Anti-inflammatory means reducing inflammation, pain, or swelling. সহজ বাংলা: প্রদাহ/ফোলা/ব্যথা কমায়।">anti-inflammatory, anti-atherogenic, and anti-apoptotic.
- In the present study, /the authors/ investigated the protective effects of rosiglitazone on MPP(+) induced cytotoxicity in human neuroblastoma SH-SY5Y cells, as well as underlying mechanism. /Their/ results suggested that the protective effects of rosiglitazone on MPP(+) induced apoptosis may be ascribed to its anti-oxidative properties, anti-apoptotic activity via inducing expression of SOD and catalase and regulating the expression of Bcl-2 and Bax. These data indicated that rosiglitazone might provide a valuable therapeutic strategy for the treatment of progressive neurodegenerative disease such as Parkinson’s disease.
Contra Indication of Rosiglitazone
- Low blood sugar
- Severe Heart Failure
- Liver problems
- Decreased Calcification or Density of Bone
- Visible Water Retention
- Weight gain
- Abnormal liver function tests
- Broken Bone
- Macular Edema
Dosages of Rosiglitazone
Strengths:2 mg; 4 mg; 8 mg
insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">Diabetes Type 2
- Initial dose: 4 mg orally once a day
- Maintenance dose: If inadequate response is not achieved after 8 to 12 weeks, increase to 8 mg once a day
- Maximum dose: 8 mg per day
Side Effects of Rosiglitazone
Most common
- Chest pain
- decreased urine output
- dilated neck veins
- extreme fatigue
- abdominal pain,
- physical weakness (asthenia)
- diarrhea
- gas (flatulence)
- symptoms of weakness, muscle pain (myalgia)
- upper respiratory tract infection
- low blood sugar (hypoglycemia)
- abdominal pain (GI complaints), lactic acidosis (rare)
- low blood levels of vitamin B-12
- nausea,vomiting
- chest discomfort
- chills, dizziness
- bloating/abdominal distention
- constipation
- heartburn
More common
- Abdominal or stomach discomfort
- cough or hoarseness
- decreased appetite
- diarrhea
- fast or shallow breathing
- fever or chills
- general feeling of discomfort
- lower back or side pain
- muscle pain or cramping
- painful or difficult urination
Less common
- Anxiety
- confusion
- dark urine
- depression
- Abnormal stools
- bad, unusual, or unpleasant (after) taste
- change in taste
- difficulty with moving
- discoloration of the fingernails or toenails
- flu-like symptoms
- joint pain
- rash
- runny nose
- sneezing
- stuffy nose
- swollen joints
Drug Interactions of Rosiglitazone
Rosiglitazone may interact with following drugs ,suppliments & may decrease the efficacy of drug
- angiotensin converting enzyme inhibitors (ACEIs; captopril, enarapril,ramipril)
- alcohol
- antipsychotic medications (e.g., chlorpromazine, haloperidol, olanzapine,
- atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine, risperidone)
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- barbiturates (e.g., pentobarbital, phenobarbital)
- cyclosporine
- insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">diabetes medications (e.g., chlorpropamide, glipizide, glyburide, insulin, metformin,nateglinide, pioglitazone)
- diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
- phenytoin
- pregabalin
- irbesartan
- lapatinib
- losartan
- mifepristone
- corticosteroids (e.g., dexamethasone, prednisone)
- diabetic drugs (e.g., glyburide, insulin, repaglinide, sitagliptin)
- diuretics (e.g., furosemide, hydrochlorothiazide)
- HIV protease inhibitors (e.g., atazanavir, indinavir, ritonavir, saquinavir)
- phenytoin
- quinolone antibiotics (e.g., levofloxacin, moxifloxacin)
- selective serotonin reuptake inhibitors (SSRIs; citalopram, fluoxetine, sertraline paroxetine,
- trimethoprim
- vancomycin
- verapamil
- warfarin
Pregnancy & Lactation of Rosiglitazone
FDA Pregnancy Category : C
Pregnancy
This medication should not be used during pregnancy. Usually insulin is used to control high blood sugars during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.
Breast-feeding
It is not known if rosiglitazone passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.
References
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Rosiglitazone
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Rosiglitazone
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Rosiglitazone
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Rosiglitazone
https://ec.europa.eu/health/documents/community-register/html/h137.htm
Rosiglitazonehttps://ec.europa.eu/health/documents/community-register/html/h139.htm
Rosiglitazonehttps://ec.europa.eu/health/documents/community-register/html/h138.htm
rosiglitazone / metforminhttps://ec.europa.eu/health/documents/community-register/html/h258.htm
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5-{[4-({2-[methyl(2-pyridinyl)amino] ethyl} oxy)phenyl]methyl}-1,3-thiazolidine-2,4-dione
https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/9426
BRL 49653https://echa.europa.eu/substance-information/-/substanceinfo/100.102.969
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Patent:8236345
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Rosiglitazone
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Avandamet
http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0012046/
Avandarylhttp://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0012045/
Rosiglitazone (By mouth) -
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rosiglitazone
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