Treating Diabetes with Injection but not Insulin

The search for a new medicine for Diabetes is a never ending process. A new medicine is available which belongs to the incretin family.

Incretins are a type of gastrointestinal hormone that cause an increase in the amount of insulin released from the beta cells of the pancreas after eating, even before blood glucose levels become elevated.

They also slow the rate of absorption of nutrients into the blood stream by reducing gastric emptying and may directly reduce food intake.

Initial group of this medicine was available as two injections a day, but now it is available once a day injection. Good news is that same medicine will be available once a week injection soon.

This medicine has two positive points (No low sugar, weight loss) and two negative points (Injection and cost).

Injectable Diabetes Medicine, not Insulin – GLP-1 Analogue

Name	Mech of Action	Group
GLP 1 Analogue	Enhance insulin production, secretion & responsiveness & suppress appetite	- Exenatide - Liraglutide - Lixisenatide - Dulaglutide - Semaglutide

Exenatide

Mechanism of action: Exanatide is a GLP-1 receptor agonist that enhances glucose-dependent insulin secretion by the pancreatic beta-cell, suppresses inappropriately elevated glucagon secretion, and slows gastric emptying.

Exenatide has acute effects on pancreatic beta-cell responsiveness to glucose leading to insulin release predominantly in the presence of elevated glucose concentrations.

This insulin secretion subsides as blood glucose concentrations decrease and approach euglycemia.

Hence Exanatide improves glycaemic control by reducing fasting and postprandial glucose concentrations in patients with type 2 diabetes.

Dose: Exanatide should be initiated at 5 mcg administered twice daily before meals.

Based on clinical response, the dose of Byetta can be increased to 10 mcg twice daily. Initiation with 5 mcg reduces the incidence and severity of gastrointestinal side effects. Each dose should be administered as a subcutaneous (SC) injection in the thigh, abdomen, or upper arm.

ADVERSE REACTIONS: nausea, hypoglycemia, vomiting, diarrhea, feeling jittery, dizziness, headache, dyspepsia. Nausea usually decreases over time.

CONTRAINDICATIONS: Pancreatitis, Renal Impairment, Severe Gastrointestinal Disease, Hypoglycemia.

Liraglutide

Mechanism of action:

liraglutide activates the GLP-1 receptor, a membrane-bound cell-surface receptor coupled to adenyl cyclase by the stimulatory G-protein, Gs, in pancreatic beta cells.

Liraglutide increases intracellular cyclic AMP (cAMP) leading to insulin release in the presence of elevated glucose concentrations.

This insulin secretion subsides as blood glucose concentrations decrease and approach euglycemia. The mechanism of blood glucose-lowering also involves a delay in gastric emptying.

Dose: Administer once daily at any time of day, independently of meals. Inject subcutaneously in the abdomen, thigh or upper arm.

Initiate at 0.6 mg per day for one week. This dose is intended to reduce gastrointestinal symptoms during initial titration and is not effective for glycaemic control. After one week, increase the dose to 1.2 mg. If the 1.2 mg dose does not result in acceptable glycemic control, the dose can be increased to 1.8 mg

Available in pre-filled, multi-dose pen that delivers doses of 0.6 mg, 1.2 mg,
or 1.8 mg (6 mg/mL, 3 mL)

ADVERSE REACTIONS

Headache, nausea, diarrhea, urticaria (0.8%) .

CONTRAINDICATIONS: Pancreatitis, medullary thyroid carcinoma and the symptoms of thyroid tumours. Hypoglycemia can occur when Victoza is used with sulfonylurea. Consider lowering the dose of sulfonylurea to reduce the risk of hypoglycemia.

Dulaglutide

We have now once a week injection available with similar efficacy as Liraglutide. It is flexible, can be taken any time of the day, once a week but a day or two early or late is the same.

There is an oral preparation of the same group of medicine is going to be in the market soon called Semaglutide.