Linagliptin

BRAND NAMES:

Tradjenta- The type 2 diabetes medication that was prescribed. Linagliptin is the active component found in it. When used in conjunction with a healthy diet and regular exercise, it is FDA-approved to help adults with type 2 diabetes manage their blood sugar levels.

Trijardy – as a combination product containing Empagliflozin, linagliption, metformin) 

Glyxambi- containing linagliptin 5 mg and Empagliflozin 25 mg

Jantadueto- combination of linagliptin 2.5 mg and metformin 1000 mg

MECHANISM OF ACTION:

Linagliptin helps to keep the levels of sugar in your blood from becoming too high. Linagliptin inhibits an enzyme called DPP-4. Blocking DPP-4 increases the levels of your body's natural hormones known as Incretins. It helps to reduce blood sugar by raising insulin levels, particularly after meals. They also decrease the quantity of blood sugar produced by the liver. 

PHARMACOKINETICS:

Absorption: Linagliptin has an absolute bioavailability of around 30%. A high-fat lunch decreased Cmax by 15% and raised AUC by 4%, but this effect is not clinically significant. Linagliptin can be taken with or without food.

Distribution: The mean estimated volume of administration at constant level after a single intravenous dose of linagliptin 5 mg in healthy persons is around 1110 L, showing that linagliptin is widely distributed to the tissues.

Metabolism: Linagliptin metabolism is mediated by cytochrome P450 3A4, aldo-keto reductases, and carbonyl reductases. After oral treatment, the majority of linagliptin is excreted unaltered, implying that metabolism is a minor elimination mechanism. A tiny fraction of absorbed linagliptin is converted to pharmacologically inactive metabolites, resulting in a 13.3% steady-state exposure compared to linagliptin.

Excretion: The elimination of linagliptin is eliminated in the urine (5.4%) and feces (84.7%)
PHARMACODYNAMICS:

Compounds that prevent incretin breakdown by inhibiting Dipeptidyl-Peptidase Ⅳ. This helps to address the faulty insulin and glucagon secretion found in type 2 diabetes by boosting insulin production while inhibiting glucagon release.

ADMINISTRATION:

Linagliptin is administered through orally with or without food. The recommended dose of tradjenta is 5 mg once daily. The tablets can be taken with or without food.

DOSAGE AND STRENGTHS:

The amount of medicine you take is determined by its strength. The amount of pills you take each day, the period between doses, and the duration of your medication use are all determined by the medical problem for which you are using it. 
The pill dosages for type 2 diabetes people are 5mg once a day.

DRUG INTERACTIONS:

The interactions of linagliptin include 

• Heart problems- Digoxin
• Diuretics- Furosemide
• Steroids – budesonide 
• Antibiotic – rifampin
• Anti-epileptic drugs- Phenytoin, topiramate and lamotrigine
• Beta blocker medication- metoprolol, propranolol

​​​​​​CONTRAINDICATIONS:

Linagliptin is contraindicated for patients having previous experience of hypersensitive responses to linagliptin, such as urticaria, angioedema, or bronchial hyperreactivity. 

SIDE EFFECTS:

The common side effects of linagliptin include

• Diarrhea
• Decreased appetite
• Nausea
• Vomiting
• Itching

Serious side effects includes

• Lacto-Acidosis- weakness, muscle pain and stomach pain
• Hypoglycemia- fast heart rate and dizziness
• Allergic reactions- swelling of the face and skin rash

OVERDOSE:

Taking more than prescribed dose of linagliptin it cause overdose. The symptoms of overdose includes:

• Stomach pain
• Nausea and vomiting
• Feel dizzy

TOXICITY:

Linagliptin was not found to be mutagenic, clastogenic, or have any effect on fertility. No dose change is required due to race, age, weight, gender, renal or hepatic impairment. The original drug clearance did not include efficacy and safety studies in pediatric populations, however current clinical trials suggest that linagliptin is well tolerated in individuals aged 10 to 18.

STORAGE CONDITIONS:

This compound must be stored between 68°F and 77°F, or 20°C and 25°C, at room temperature. It may be subjected to temperatures between 15°C and 30°C, or 59°F and 86°F.