Pioglitazone
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Pioglitazone
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| Systematic (IUPAC) name | |
| 5-((4-(2-(5-ethyl-2-pyridinyl) ethoxy)phenyl)methyl)-,(+-)- 2,4-thiazolidinedione, |
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| Identifiers | |
| CAS number | |
| ATC code | A10 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C19H20N2O3S |
| Mol. mass | 356.44 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | >99% |
| Metabolism | liver (CYP2C8) |
| Half life | 3–7 hours |
| Excretion | in bile |
| Therapeutic considerations | |
| Licence data |
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| Pregnancy cat. |
C |
| Legal status |
PoM (UK), Rx (US) |
| Routes | oral |
Pioglitazone is a prescription drug of the class thiazolidinedione with hypoglycemic (antihyperglycemic, antidiabetic) action. Pioglitazone is marketed as trademarks Actos in the USA and Glustin in Europe by pharmaceutical companies Takeda and Eli Lilly.
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[edit] Pharmacology
Pioglitazone selectively stimulates nuclear gamma-receptors, activated by peroxisome proliferator (PPAR). It modulates the transcription of the insulin sensitive genes involved in the control of glucose and lipid metabolism in the lipidic, muscular tissues and in the liver. Pioglitazone does not directly stimulate insulin secretion, but rather affects the insulin-synthetic function of the pancreas. Pioglitazone also reduces insulin resistance in the liver and peripheral tissues; increases the expense of insulin-dependent glucose; decreases withdrawal of glucose from the liver; reduces quantity of glucose, insulin and glycated haemoglobin in the bloodstream. Pioglitazone decreases the level of triglycerides and increases that of high-density lipoproteins (HDL) without changing low-density lipoproteins (LDL) and general cholesterol in patients with disorders of the lipid metabolism.
[edit] Indications and Usage
Pioglitazone is used for the treatment of diabetes type 2 (non-insulin-dependent diabetes mellitus, NIDDM) in monotherapy and combination therapy with sulfonylurea, metformin, or insulin when diet and exercise plus the single agent have no effect in glycemic control. Also Pioglitazone is indicated as an adjunct to diet and exercise therapy in patients with type 2 diabetes. Pioglitazone has also been used to treat non-alcoholic steatohepatitis (fatty liver), but this use should currently only be considered experimental.[1]
[edit] Contraindications
- hypersensitivity to Pioglitazone, thiazolidinediones or any of components of its pharmaceutical forms
- diabetes type 1
- diabetic ketoacidosis
- acute diseases of the liver
- pregnancy
- lactation
- pediatric use in patients under 18 years of age (there are no data about safety and efficiency of Pioglitazone in this group of patients)
[edit] Side effects
Pioglitazone Adverse reactions/Side effects include:
- hypoglycemia
- edema
- upper respiratory tract infection
- anaemia
- headache
- sinusitis
- myalgia
- tooth disorder
- diabetes mellitus aggravated
- pharyngitis
- reduction of haemoglobin, hematocrit and bilirubin
[edit] Drug Interactions
Sulfonamides, metformin, and insulin reciprocally exponentiate hypoglycemia. Therapy with Pioglitazone increased risk for pregnancy during contraception.
[edit] Overdosage
In the event of overdosage of Pioglitazone, appropriate symptomatic therapy.
[edit] How supplied
Pioglitazone as Actos® is supplied in:
