Pioglitazone: Difference between revisions

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==Common Strengths of Pioglitazone==
==Common Strengths of Pioglitazone==
Pioglitazone is available in three strengths:
Pioglitazone is available in three strengths:
*15 mg
*15 mg, 30 mg, 45 mg tablets
*30 mg
*45 mg


==Drug Trade Names of Pioglitazone==
==Drug Trade Names of Pioglitazone==
Actos is the trade name for pioglitazone. It is also sold under various brand names when combined with other medications, such as:
Actos is the trade name for pioglitazone.  
*Actoplus Met (pioglitazone and metformin)
 
*Duetact (pioglitazone and glimepiride)
It is also sold under various brand names when combined with other medications, such as:
*Oseni (pioglitazone and alogliptin)
*ACTOSMET TABLET 15MG/850MG: Pioglitazone 15mg + Metformin 850mg
*OSENI TABLET 25MG/15MG: Alogliptin 25mg + pioglitazone 15mg
*OSENI TABLET 25MG/30MG: Alogliptin 25mg + pioglitazone 30mg
 
==Drug Usage==
Treatment of type 2 diabetes mellitus


==Mechanism of Action==
==Mechanism of Action==
Pioglitazone is a thiazolidinedione that works by enhancing insulin sensitivity. It activates peroxisome proliferator-activated receptor-gamma (PPARγ) in fat, muscle, and liver tissues, which helps control the production of hormones and enzymes that improve insulin sensitivity, lower blood sugar, reduce glucose production in the liver, and maintain the function of pancreatic β-cells.
Activates peroxisome proliferator-activated receptor gamma (PPAR-γ), increasing insulin sensitivity in peripheral tissues (in fat, muscle and liver tissues).


==Route of Administration==
==Route of Administration==
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==Dosages==
==Dosages==
*Normal People (without congestive heart failure)
*Initially, 15 - 30 mg once daily, may increase to 45 mg once daily
**Initial dose is 15 mg or 30 mg once daily. The dose can be increased up to 45 mg once daily based on glycemic response.
*Heart failure (NYHA Class I-II): Start at 15 mg once daily
*Hypertension
*No dose adjustment is needed for hypertension or mild-moderate renal impairment
**No specific dosage adjustment for hypertension alone, but careful monitoring is required due to potential fluid retention.
*Severe renal impairment (eGFR <30 mL/min): Use with caution, start at a lower dose
*Heart Failure (NYHA Class I or II)
 
**Initial dose is 15 mg once daily. Dose adjustments should be made cautiously with careful monitoring for signs of heart failure.
*Diabetic Kidney Disease
**No specific dosage adjustment, but careful monitoring is required due to potential fluid retention and renal function.


==Side Effects==
==Side Effects==
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!Adverse reactions
!Adverse reactions
|-
|-
| rowspan="2" | '''Very common (≥1/10)
| rowspan="6" | '''Common
| Edema
| Upper respiratory tract infection
|-
|-
| Weight gain
| Weight gain
|-
|-
| rowspan="6" | '''Common (≥1/100 to <1/10)
| Edema
| Upper respiratory tract infection
|-
| Headache
|-
|-
| Sinusitis
| Sinusitis
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| Myalgia
| Myalgia
|-
|-
| Tooth disorder
| Visual disturbances
|-
| Pharyngitis
|-
| rowspan="3" | '''Uncommon (≥1/1,000 to <1/100)
| Anemia
|-
|-
| Hypoglycemia (when used with other antidiabetic drugs)
| rowspan="5" | '''Uncommon
| Flatulence
|-
|-
| Increased appetite
| Insomnia
|-
|-
| rowspan="3" | '''Rare (≥1/10,000 to <1/1,000)
| Liver dysfunction
| Liver dysfunction
|-
|-
| Macular edema
| Macular edema
|-
|-
| Heart failure
| Bladder cancer
|-
| rowspan="2" | '''Very Rare (<1/10,000)
| Bladder cancer (long-term use)
|-
| Severe allergic reactions
|}
|}


==Pharmacokinetics==
==Pharmacokinetics==
*Absorption
*Absorption
**Well absorbed orally. Peak plasma concentrations of unchanged pioglitazone are usually achieved 2 hours after administration.
**Well absorbed orally. The peak effect reached approximately 2 hours after administration.
*Metabolism
*Metabolism
**Primarily metabolized in the liver via CYP2C8.
**Primarily metabolized in the liver via CYP2C8.
*Half-life
**About 7 hours.
*Excretion
*Excretion
**Mainly excreted in faeces; 15 - 30% excreted in urine.
**Mainly excreted in faeces; 15 - 30% excreted in urine.
*Half-life
** 3 to 7 hours.
*Drug duration
**up to 24 hours


==Precautions for Use==
==Drug Precautions==
'''Fluid retention and cardiac failure
 
Pioglitazone can cause fluid retention, which may exacerbate or precipitate heart failure. Not recommended for patients with cardiac failure (NYHA stages 1 to IV), active bladder cancer, or severe liver disease.
 
'''Pregnancy
'''Pregnancy


Not recommended due to potential risks.
Not recommended, potential risk of fetal harm.


'''Breastfeeding
'''Breastfeeding
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'''Children and Elderly
'''Children and Elderly
 
*Children: Safety and efficacy not established
Not recommended for children; elderly patients should be monitored closely due to increased risk of heart failure.
*Elderly: No dose adjustment required, use with caution


'''Renal Impairment
'''Renal Impairment


No specific dosage adjustment, but careful monitoring is required.
Use with caution in severe impairment


'''Monitoring Requirements
'''Monitoring Requirements
 
*Liver function tests
Regular monitoring of liver enzymes, blood glucose, and signs of heart failure is recommended.
*Hemoglobin
*Blood glucose
*HbA1c


'''Drug Interactions
'''Drug Interactions


Caution with CYP2C8 inhibitors (e.g., gemfibrozil), insulin, and other antidiabetic drugs due to increased risk of hypoglycemia.
May interact with gemfibrozil, rifampicin, CYP2C8 inhibitors/inducers


==FAQs==
==FAQ==
'''How should I take the tablet?
'''How Should I Take the Tablet?


Take Pioglitazone exactly as prescribed by your doctor, usually once daily, with or without food.
Take a tablet once daily with or without food.


'''What should I avoid while taking?
'''What Should I Avoid While Taking?
    
    
Avoid excessive alcohol consumption as it can increase the risk of hypoglycemia and liver damage. Avoid using Pioglitazone if you have severe heart failure or active bladder cancer.
Avoid excessive alcohol consumption.


'''What happens if I miss a dose?
'''What Happens if I Miss a Dose?
    
    
Take the missed dose as soon as you remember, but skip it if it is almost time for your next dose. Do not take two doses at one time.
If you miss a dose: Take the missed dose as soon as you remember, but skip it if it is almost time for your next dose. Do not take two doses at one time.
 
==Reference==
[1] https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021842s014s015lbl.pdf
 
[2] https://www.rxlist.com/actos-drug.htm
 
[3] https://www.drugs.com/availability/generic-actos.html
 
[4] https://www.drugs.com/actos.html
 
[5] https://en.wikipedia.org/wiki/Pioglitazone

Latest revision as of 22:29, 4 July 2024


Antidiabetic Drug

Drug class: Thiazolidinedione

Pioglitazone (ACTOS) (中文：吡格列酮)

Pronunciation[edit]

Pioglitazone 30mg[edit]

Common Strengths of Pioglitazone[edit]

Pioglitazone is available in three strengths:

  • 15 mg, 30 mg, 45 mg tablets

Drug Trade Names of Pioglitazone[edit]

Actos is the trade name for pioglitazone.

It is also sold under various brand names when combined with other medications, such as:

  • ACTOSMET TABLET 15MG/850MG: Pioglitazone 15mg + Metformin 850mg
  • OSENI TABLET 25MG/15MG: Alogliptin 25mg + pioglitazone 15mg
  • OSENI TABLET 25MG/30MG: Alogliptin 25mg + pioglitazone 30mg

Drug Usage[edit]

Treatment of type 2 diabetes mellitus

Mechanism of Action[edit]

Activates peroxisome proliferator-activated receptor gamma (PPAR-γ), increasing insulin sensitivity in peripheral tissues (in fat, muscle and liver tissues).

Route of Administration[edit]

Pioglitazone is administered orally in tablet form.

Dosages[edit]

  • Initially, 15 - 30 mg once daily, may increase to 45 mg once daily
  • Heart failure (NYHA Class I-II): Start at 15 mg once daily
  • No dose adjustment is needed for hypertension or mild-moderate renal impairment
  • Severe renal impairment (eGFR <30 mL/min): Use with caution, start at a lower dose


Side Effects[edit]

Frequency Adverse reactions
Common Upper respiratory tract infection
Weight gain
Edema
Sinusitis
Myalgia
Visual disturbances
Uncommon Flatulence
Insomnia
Liver dysfunction
Macular edema
Bladder cancer

Pharmacokinetics[edit]

  • Absorption
    • Well absorbed orally. The peak effect reached approximately 2 hours after administration.
  • Metabolism
    • Primarily metabolized in the liver via CYP2C8.
  • Excretion
    • Mainly excreted in faeces; 15 - 30% excreted in urine.
  • Half-life
    • 3 to 7 hours.
  • Drug duration
    • up to 24 hours

Drug Precautions[edit]

Pregnancy

Not recommended, potential risk of fetal harm.

Breastfeeding

Not recommended.

Children and Elderly

  • Children: Safety and efficacy not established
  • Elderly: No dose adjustment required, use with caution

Renal Impairment

Use with caution in severe impairment

Monitoring Requirements

  • Liver function tests
  • Hemoglobin
  • Blood glucose
  • HbA1c

Drug Interactions

May interact with gemfibrozil, rifampicin, CYP2C8 inhibitors/inducers

FAQ[edit]

How Should I Take the Tablet?

Take a tablet once daily with or without food.

What Should I Avoid While Taking? 

Avoid excessive alcohol consumption.

What Happens if I Miss a Dose?

If you miss a dose: Take the missed dose as soon as you remember, but skip it if it is almost time for your next dose. Do not take two doses at one time.

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