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[[Category: Drugs]]
[[Category: Drugs]][[Category: Dipeptidyl peptidase-4 (DPP-4) inhibitor]]


'''Alogliptin''' (中文：[[阿格列汀]])
[[:Category: Antidiabetic Drug | '''Antidiabetic Drug''']]
 
'''Drug class: [[:Category: Dipeptidyl peptidase-4 (DPP-4) inhibitor | Dipeptidyl peptidase-4 (DPP-4) inhibitor]]
 
'''Alogliptin (NESINA)'''（中文：[[阿格列汀]]）
==Common Strengths of Alogliptin==
==Common Strengths of Alogliptin==
Alogliptin is available in the following strengths:
Alogliptin is available in the following strengths:
*6.25 mg
*6.25 mg, 12.5 mg, 25 mg tablets
*12.5 mg
*25 mg


==Drug Trade Name of Alogliptin==
==Drug Trade Name of Alogliptin==
Alogliptin is marketed under several trade name, including:
*Nesina, Vipidia, Oseni
*Nesina
It is also sold under various brand names when combined with other antidiabetic medications, such as:
*Vipidia
*NESINA MET TABLET 12.5MG/1000MG: Alogliptin 12.5mg + Metformin 1000mg
*Kazano (when combined with metformin)
*NESINA MET TABLET 12.5MG/500MG: Alogliptin 12.5mg + Metformin 1000mg
*Oseni (when combined with pioglitazone)
*OSENI TABLET 25MG/15MG: Alogliptin 25mg + Pioglitazone 15mg
*OSENI TABLET 25MG/30MG: Alogliptin 25mg + Pioglitazone 30mg
 
==Drug Usage==
Treatment of type 2 diabetes mellitus in adults, as an adjunct to diet and exercise.


==Mechanism of Action==
==Mechanism of Action==
Alogliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor. It works by inhibiting the DPP-4 enzyme, which results in increased levels of incretin hormones. These hormones help regulate blood glucose by increasing insulin release and decreasing glucagon levels in a glucose-dependent manner.
Inhibits DPP-4 enzyme, increasing levels of incretin hormones which stimulate insulin release and decrease glucagon secretion, thereby lowering blood glucose.


==Route of Administration==
==Route of Administration==
Alogliptin is administered orally in tablet form.
Alogliptin is administered orally in tablet form.


==Dosages==
==Dosages==
*Normal People
*25 mg once daily  
**The usual dose is 25 mg once daily.
*Normal Renal Function or Mild Renal Impairment (eGFR ≥60 mL/min/1.73 m<sup>2</sup>): No dosage adjustment is required. The recommended dose is 25 mg once daily.
*Hypertension
*Moderate renal impairment (eGFR 30 to <60 mL/min/1.73 m<sup>2</sup>): 12.5 mg once daily
**No specific dosage adjustment is required, but caution is advised due to potential cardiovascular effects.
*Severe renal impairment/ESRD (eGFR 15 to <30 mL/min/1.73 m<sup>2</sup>): 6.25 mg once daily
*Heart Failure
*No dose adjustment needed for hypertension or heart failure
**No specific dosage adjustment is required, but caution is advised due to potential cardiovascular effects.
*Diabetic Kidney Disases
**Mild renal impairment (CrCl ≥ 60 to < 90 mL/min)
***No dose adjustment required.
**Moderate renal impairment (CrCl ≥ 39 to < 60 mL/min)
***12.5 mg once daily.
**Severe renal impairment (CrCl ≥ 15 to < 30 mL/min) or end-stage renal disease (ESRD) (CrCl < 15 mL/min)
***6.25 mg once daily.


==Side Effects==
==Side Effects==
Line 41: Line 39:
!Adverse reactions
!Adverse reactions
|-
|-
| '''Very common (≥1/10)
| rowspan="3" | '''Common
| None reported
| Upper respiratory tract infection
|-
| Nasopharyngitis
|-
|-
| rowspan="3" | '''Common (≥1/100 to <1/10)
| Headache
| Headache
|-
|-
| Nasopharyngitis
| rowspan="6" | '''Uncommon
| Hypoglycemia
|-
|-
| Upper respiratory tract infection
| Rash
|-
| rowspan="3" | '''Uncommon (≥1/1,000 to <1/100)
| Hypoglycemia (when used with other antidiabetic drugs)
|-
|-
| Pruritus
| Pruritus
|-
|-
| Rash
|-
| rowspan="3" | '''Rare (≥1/10,000 to <1/1,000)
| Pancreatitis
| Pancreatitis
|-
|-
| Hepatic dysfunction
| Angioedema
|-
|-
| Hypersensitivity reaction including anaphylaxis and angioedema
| Stevens-Johnson syndrome
|-
| '''Very Rare (<1/10,000)
| Severe cutaneous adverse reactions including Stevens-Johnson syndrome
|}
|}


==Pharmacokinetics==
==Pharmacokinetics==
*Absorption
*Absorption
**Rapidly absorbed with peak plasma concentrations occurring 1 - 2 hours after dosing. The absolute bioavailability is approximately 100%.
**Rapidly absorbed, 100% bioavailable. The peak inhibition of DPP-4 occurs within 2 to 3 hours after dosing.
*Distribution
**Alogliptin is 20 - 30% bound to plasma proteins
*Metabolism
*Metabolism
**Alogliptin does not undergo extensive metabolism, 60 - 70% of the dose is excreted as unchanged drug in the urine. Limited metabolism primarily via CYP2D6 and CYP3A4.
**Limited metabolism
*Elimination
*Elimination
**Primarily excreted unchanged in urine. The mean terminal half-life is approximately 21 hours.
**Primarily renal excretion, half-life approximately 21 hours
The inhibition of DPP-4, which is crucial for its glucose-lowering effects, peaks within 2 to 3 hours and remains significant for up to 24 hours.


==Drug Precautions==
==Drug Precautions==
'''Safety
Use with caution in patients with liver disease. Monitor liver functions tests regularly. Discontinue if pancreatitis or severe hypersensitivity reactions occur.
'''Pregnancy
'''Pregnancy


Not recommended due to lack of sufficient data on safety.
Not recommended, limited data available


'''Breast Feeding
'''Breast Feeding


Not recommended due to lack of sufficient data on safety.
Not recommended


'''Children and Elderly
'''Children and Elderly
 
*Children: Safety and efficacy not established in <18 years
Not recommended for children. Elderly patients should be monitored closely due to increased risk of adverse effects.
*Elderly: No dose adjustment is required based on age


'''Renal Impairment
'''Renal Impairment


Dose adjustments are required for patients with moderate to severe renal impairment and ESRD.
Dose adjustment required (see dosages above)


'''Monitoring Requirements
'''Monitoring Requirements
 
*Renal function
Regular monitoring of liver function tests and renal function is recommended.
*Blood glucose
*HbA1c
*Signs of pancreatitis
The main symptoms of pancreatitis include:
*Severe abdominal pain, typically in the upper abdomen, that may:
**Feel worse after eating
**Be sudden and intense in acute cases
*Nausea and vomiting
*Fever
*Rapid pulse/heart rate


'''Drug Interaction
'''Drug Interaction


Caution with CYP2D6 and CYP3A4 inhibitors. Monitor for hypoglycemia when used with insulin or insulin secretagogues.
May increase risk of hypoglycemia when used with insulin or sulfonylureas.


==FAQs==
==FAQ==
'''How should I take the tablet?
'''How should I take the tablet?


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


'''What should I avoid while taking?
'''What should I avoid while taking?


Avoid alcohol and other medications that can affect liver function. Avoid useing alogliptin if you have a history of severe hypersensitivity reactions to DPP-4 inhibitors.
Alcohol (may increase the risk of hypoglycemia)


'''What happens if I miss a dose?
'''What happens if I miss a dose?


Take the missed dose as soon as you remember, unless it is close to the time for your next dose. Do not take two doses at one time.
Take as soon as remembered unless close to the next dose, do not double dose.
 
==Reference==
[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6834733
 
[2] https://www.accessdata fda.gov/drugsatfda_docs/label/2015/022426s005lbl.pdf
 
[3] https://www.drugs.com/pro/alogliptin.html
 
[4] https://www.rxlist.com/alogliptin/generic-drug.htm
 
[5] https://n.wikipedia.org/wiki/Alogliptin

Latest revision as of 21:53, 4 July 2024


Antidiabetic Drug

Drug class: Dipeptidyl peptidase-4 (DPP-4) inhibitor

Alogliptin (NESINA)（中文：阿格列汀）

Common Strengths of Alogliptin[edit]

Alogliptin is available in the following strengths:

  • 6.25 mg, 12.5 mg, 25 mg tablets

Drug Trade Name of Alogliptin[edit]

  • Nesina, Vipidia, Oseni

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

  • NESINA MET TABLET 12.5MG/1000MG: Alogliptin 12.5mg + Metformin 1000mg
  • NESINA MET TABLET 12.5MG/500MG: Alogliptin 12.5mg + Metformin 1000mg
  • 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 in adults, as an adjunct to diet and exercise.

Mechanism of Action[edit]

Inhibits DPP-4 enzyme, increasing levels of incretin hormones which stimulate insulin release and decrease glucagon secretion, thereby lowering blood glucose.

Route of Administration[edit]

Alogliptin is administered orally in tablet form.

Dosages[edit]

  • 25 mg once daily
  • Normal Renal Function or Mild Renal Impairment (eGFR ≥60 mL/min/1.73 m2): No dosage adjustment is required. The recommended dose is 25 mg once daily.
  • Moderate renal impairment (eGFR 30 to <60 mL/min/1.73 m2): 12.5 mg once daily
  • Severe renal impairment/ESRD (eGFR 15 to <30 mL/min/1.73 m2): 6.25 mg once daily
  • No dose adjustment needed for hypertension or heart failure

Side Effects[edit]

Frequency Adverse reactions
Common Upper respiratory tract infection
Nasopharyngitis
Headache
Uncommon Hypoglycemia
Rash
Pruritus
Pancreatitis
Angioedema
Stevens-Johnson syndrome

Pharmacokinetics[edit]

  • Absorption
    • Rapidly absorbed, 100% bioavailable. The peak inhibition of DPP-4 occurs within 2 to 3 hours after dosing.
  • Metabolism
    • Limited metabolism
  • Elimination
    • Primarily renal excretion, half-life approximately 21 hours

The inhibition of DPP-4, which is crucial for its glucose-lowering effects, peaks within 2 to 3 hours and remains significant for up to 24 hours.

Drug Precautions[edit]

Pregnancy

Not recommended, limited data available

Breast Feeding

Not recommended

Children and Elderly

  • Children: Safety and efficacy not established in <18 years
  • Elderly: No dose adjustment is required based on age

Renal Impairment

Dose adjustment required (see dosages above)

Monitoring Requirements

  • Renal function
  • Blood glucose
  • HbA1c
  • Signs of pancreatitis

The main symptoms of pancreatitis include:

  • Severe abdominal pain, typically in the upper abdomen, that may:
    • Feel worse after eating
    • Be sudden and intense in acute cases
  • Nausea and vomiting
  • Fever
  • Rapid pulse/heart rate

Drug Interaction

May increase risk of hypoglycemia when used with insulin or sulfonylureas.

FAQ[edit]

How should I take the tablet?

Take once daily with or without food.

What should I avoid while taking?

Alcohol (may increase the risk of hypoglycemia)

What happens if I miss a dose?

Take as soon as remembered unless close to the next dose, do not double dose.

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