Types Of Medications For Diabetes

Types Of Medications For Diabetes

The popular picture that comes to one’s mind when you think of diabetes is insulin shots. But insulin is mainly given in all type 1 diabetes patients and in inadequately controlled type 2 diabetes cases. Most cases of type 2 diabetes are treated with other hypoglycemic (lowering blood glucose) drugs that can be given orally (so-called “oral hypoglycemic drugs”), in contrast to insulin, which has to be given by injection because if it is given orally it is degraded by the stomach juices.

The oral hypoglycemic drugs are (1) Sulfonylureas, (2) Biguanides, (3) Alpha-glucosidase inhibitors, (4) Thiazolidinediones, (5) Meglitinides, and (6) DPP-IV inhibitors. When oral hypoglycemic drugs fail to control the type 2 diabetes, insulin can be added to the therapy.
Types Of Medications For Diabetes


Medications for Diabetes

Insulin

Initially, insulin was obtained from pancreata of cows and pigs (bovine and porcine insulins) and some people still continue to use animal insulins. The use of recombinant DNA technology has enabled large-scale production of human insulin. Human insulin has a more rapid onset and shorter duration of action than porcine insulin.


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Insulin is injected subcutaneously into the anterior abdominal wall, upper arms, outer thighs and buttocks. Repeated injection at the same site should be avoided. Battery-powered portable pumps are available, which provide continuous subcutaneous or intravenous infusion of insulin.


Types of Insulin

Short- and Rapid-Acting Insulins

Types Of Medications For Diabetes Short-acting (i.e., regular) insulin has a rapid onset of action (30-40 min) but short duration (5-8 hr). Recently, modified recombinant insulins (rapid-acting insulins) have been introduced with even more rapid onset (15 min) and shorter duration of action (insulin lispro – 2-5 hr; insulin aspart – 3-5 hr; insulin glulisine – 1-2.5 hr).

Regular insulin usually is injected subcutaneously 30-45 min before meal to allow adequate time for absorption. Rapid-acting insulins may be injected immediately before or after a meal. Inhaled insulin is also available, which is inhaled through the mouth before eating using a special inhalation device.


Intermediate-Acting Insulins

These insulins are formulated to dissolve more gradually when injected (onset of action – 1-2 hr); thus, their durations of action are longer (18-24 hr). The two preparations used most frequently are neutral protamine Hagedorn (NPH) insulin (isophane insulin suspension) and lente insulin (insulin zinc suspension). These insulins are given either once a day before breakfast or twice a day.


Long-Acting Insulins

One long-acting insulin is ultralente insulin (extended insulin zinc suspension), which has a slower onset (4-6 hr), prolonged peak (16-18 hr) and longer duration (20-36 hr) of action. Some of the not-so-ideal properties of ultralente insulin have led to the development of insulin analogs. Insulin glargine is a long-acting analog of human insulin that provides better once-daily 24-hour insulin coverage than ultralente insulin or NPH insulin.

Glargine can be administered at any time during the day. Another such analog is insulin detemir, which is given twice a day, and has a smoother time-action profile and a reduced prevalence of hypoglycemia as compared with NPH insulin. It should not be mixed with any other insulin preparations.


Insulin Regimens

The choice of regimen depends on the degree of glycemic (blood glucose) control, your lifestyle and your ability to adjust the insulin dose. Most people require two or more injections of insulin daily. Once-daily injections rarely achieve satisfactory glycemic control. The simplest and most commonly used regimen is twice-daily administration of short-acting and intermediate-acting insulin, given in combination (1:2) before breakfast (2/3rds of the daily requirement) and dinner (1/3rd). Several pre-mixed formulations are available.


Sulfonylureas

Types Of Medications For Diabetes Sulfonylureas act by stimulating the release of insulin from pancreas and reducing the release of glucose by liver. They are valuable in the treatment of non-obese patients with type 2 diabetes who fail to respond to dietary measures alone.


First-Generation Sulfonylureas

Tolbutamide is very well tolerated and rarely causes toxic reactions. Its dose ranges from 500 mg to 3000 mg/day given 8- or 12-hourly. Tolazamide dose is 100-1000 mg/day. Chlorpropamide is rarely used nowadays. Its dose is 250-750 mg once daily.


Second-Generation Sulfonylureas

Of the second-generation sulfonylureas, gliclazide (40-320 mg once daily) and glipizide (5-40 mg/day in divided doses when dose > 15 mg) cause few side effects, but glibenclamide or glyburide (2.5-20 mg/day) is prone to induce severe hypoglycemia (low blood glucose) and should be avoided in the elderly.  Glimepiride is given in the dose of 0.5-8 mg once daily.


Side Effects of Sulfonylureas

Adverse effects occur in 4% of patients taking first-generation sulfonylureas, and less often in those taking second-generation sulfonylureas. They can cause hypoglycemic reactions, including coma. Other side effects include nausea and vomiting, jaundice, anemia, hypersensitivity reactions and rashes. They can interact with other drugs like sulfonamides, clofibrate and salicylates.


Biguanides

Types Of Medications For Diabetes Metformin is the only biguanide available. It is less widely used than the sulfonylureas because of a higher incidence of side effects. Its mechanism of action is through impairment of glucose absorption by the gut and inhibition of glucose synthesis by liver.

It does not increase insulin secretion. Its dose is 500 mg 12-hourly, increasing up to a maximum of 1 g 8-hourly, and is given along with food. Its side effects include diarrhea, abdominal discomfort, nausea, metallic taste, and anorexia. It is contraindicated in patients with liver or kidney impairment, history of lactic acidosis, heart failure, or chronic hypoxic lung disease.


Alpha-Glucosidase Inhibitors

These delay the intestinal absorption of carbohydrates in the gut. Acarbose and miglitol are the two drugs in this category. Their dose is 25-100 mg thrice a day, taken at the start of a meal. They can be combined with a sulfonylurea. Their main side effects are abdominal bloating, flatulence and diarrhea.


Thiazolidinediones (Glitazones)

Types Of Medications For Diabetes These drugs work mainly by enhancing the action of insulin through activation of insulin-responsive genes that regulate carbohydrate and lipid metabolism. They may also lower production of glucose by liver. Rosiglitazone and pioglitazone are the two drugs in this category. The dose of rosiglitazone is 4-8 mg once daily, and that of pioglitazone is 15-30 mg once daily, unrelated to meals. Their main side effects are liver toxicity, weight gain and fluid retention. They are contraindicated in people with cardiac failure.


Meglitinides

Repaglinide acts by stimulating insulin secretion. It is taken immediately before food (1-2 mg thrice daily). Nateglinide has similar mechanism of action and is usually prescribed with metformin. Its dose is 60-120 mg thrice daily 1-10 min before a meal. Hypoglycemia is more common with repaglinide. They should be used with caution by those with liver or kidney insufficiency.


DPP-IV Inhibitors

Types Of Medications For Diabetes These are the latest drugs for the treatment of diabetes. The drugs in this group are sitagliptin, linagliptin and saxagliptin. These work by increasing insulin levels via inhibition of the enzyme DPP-IV, which enhances the incretin action through a gut hormone GLP-1.

The once daily doses of these drugs are as follows: sitagliptin – 100 mg; linagliptin – 5 mg; saxagliptin – 2.5-5 mg. Some of their side effects are nausea and vomiting, stomach pain, headache, swelling of hands and feet, and easy bruising and bleeding.


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