Brand Name: MODULIN
Generic Name: Linagliptin
Preparations: 2.5/5/10 mg tablets
Pharmacological Categories: Antidiabetic; Dipeptidyl Peptidase 4 (DPP-4) inhibitor
Mechanism of Action (MOA)
MODULIN (Linagliptin) is a competitive, reversible DPP-4 inhibitor. Inhibition of this enzyme slows the breakdown of glucagon-like peptide 1 (GLP-1) and glucose-dependant insulinotropic polypeptide (GIP). GLP-1 and GIP stimulate the release of insulin from beta cells in the pancreas while inhibiting release of glucagon from pancreatic apha cells. These effects together reduce the breakdown of glycogen in the liver and increase insulin release in response to glucose.
Pharmacokinetics
Absorption: Absorbed from gastrointestinal tract
Bioavailability: 30%
Peak Plasma Time: 1.5 hours
Distribution: Extensive
Protein Binding: 75-99%
Metabolism: Not extensively metabolized
Elimination Half-life: About 12 hours
Excretion: Faeces unchaged (80%), urine unchanged (5%)
Indication and Dosage
Type II Diabetes mellitus: 5 mg daily as an adjunct to diet and exercise
Method of administration: The tablets can be taken with or without a meal at any time of the day. If a dose is missed, it should be taken as soon as the patient remembers. A double dose should not be taken on the same day.
Renal impairment: No dose adjustment is required
Hepatic impairment: Pharmacokinetic studies suggest that no dose adjustment is required for patients with hepatic impairment but clinical experience in such patients is lacking.
Elderly: No dose adjustment is necessary based on age. However, clinical experience in patients> 80 years of age is limited and caution should be exercised when treating this population.
Paediatric population: The safety and efficacy of linagliptin in children and adolescent has not yet been established. No data are available.
Side Effects
COMMON: Hypoglycemia, increased serum lipase, nasopharyngitis, hyperuricemia, and cough
FREQUENCY NOT DEFINED: Urticaria, myalgia, and asthma
REPORTED: Acute pancreatitis, anaphylaxis, angioedema, bullous pemphigoid, exfoliation of skin, oral mucosa ulcer, severe arthralgia, severe hypersensitivity, skin rash, and stomatitis
Contraindications
Hypersensitivity, type 1 diabetes mellitus or diabetic ketoacidosis
Warnings/ Precautions
• Should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.
• There is risk of developing acute pancreatitis.
• Bullous pemphigoid has been observed in patients taking linagliptin.
Drug Interactions
• Thiazide and thiazide-like diuretics may diminish the therapeutic effect of linagliptin.
• Linagliptin enhances hypoglycemic effect of sulphonylureas.
• Salicylaytes may enhance the hypoglycemic effect of linagliptin.
• Ritonavir increases concentration of linagliptin.
• Quinolone may enhance the hypoglycemic effect of linagliptin.
Pregnancy Category: B; however it is preferable to avoid the use of linagliptin during pregnancy
Presentations
MODULIN 2.5 : 5 X 2 X 15’s
MODULIN 5 : 5 X 2 X 15’s
MODULIN 10 : 5 X 2 X 15’s
