Diabetes Medication

 

Drugs which reduce blood glucose

Insulins

These are versions of normal insulin which are given by subcutaneous injection.

– There are many different forms of insulin, which have different half-lives:

e.g. Insulin glulisine + insulin aspart + insulin lispro

These are rapidly acting [RAPID]

Regular Insulin

This is a recombinant form of human insulin.
– Must deliver to patients using an insulin syringe, as in normal syringe there are 100units/ml [REGULAR]

Neutral Protamine Hagedorn

This is intermediate acting. It is a suspension of insulin-zinc complexes with protamine which slows absorption [INTERMEDIATE]

Ultralente insulin + Detemir + Glargine

These are long acting. They have changes to the amino acid sequence which delays absorption [LONG]

Side effects
  • Overdose can result in hypoglycemia
  • Hypokalemia
  • Weight gain
  • Lipodystrophy (fat build up) at the injection site

Metformin
This reduces gluconeogenesis and increases peripheral insulin sensitivity.
– Also acts to decrease the intestinal absorption of glucose
– It does not depend of functioning ß-cells as it exerts most its effects at the liver
– Taken as a tablet and safe to use if breastfeeding
– Metformin is good in that it rarely causes hypoglycemia or weight gain on its own.

Side effects
  • Lactic acidosis in renal failure patients due to decreased drug excretion or in liver failure patients
  • GI upset –> if this occurs, switch to the modified release tablet

Sulphonylureas

These drugs bind to the SUR1 receptor on KATP channels on the beta-cells closing them, mainly increasing insulin release and also increasing tissue insulin sensitivity. These drugs are very useful in treating type II diabetes but are not effective against type 1 diabetes. 

1st generation:

Tolbutamide

This is a short acting sulphonylurea

Chlorpropamide

Long acting which used in the treatment of Neurogenic diabetes insipidus as it potentiates ADH action at V2 receptors.
– However, it is long acting and has highest chance of hypoglycemia, produces SIADH and has disulfiram-like reactions with alcohol. 

2nd generation:

Glipizide

This is an intermediate acting drug. 

3rd generation:

Glimepiride

This is a long acting sulphonylurea

Side effects
  • Hypoglycemia – proportional to how long the drug acts for
  • Weight gain
  • Not used in pregnancy as can cross the placenta
  • Some can cause SIADH leading to hyponatreamia
  • People develop tolerance due to downregulation of sulphonylurea receptors.

Meglitinides

e.g. Repaglinide
These drugs also block KATP channels causing an increase in insulin secretion.
– It is a very fast acting drug which is used to limit post-prandial hyperglycemia
– Also used in people with sulpha-drug allergies

Side effects
  • Hypoglycaemia
  • Weight Gain

Thiazolidinediones

e.g. Pioglitazone + Rosiglitazone (-glitazone)
These PPAR-y agonists increase tissue sensitivity to insulin and activate hormone adiponectin
– They also act on muscle and fat to increase glucose uptake and lipogenesis
– Therefore they reduce plasma glucose but do not cause hypoglycemia.

Side effects
  • Exacerbate congestive heart failure due to fluid retention
  • Osteoporosis
  • Bladder Cancer
  • Weight Gain

Alpha-glucosidase inhibitors

e.g. Acarbose + Miglitol
These inhibit amylase and glucoside enzymes which break down starch in the intestines
– Therefore, act to reduce the absorption of glucose into the bloodstream 

Side effects
  • Flatulence –> Not used in IBD or Liver cirrhosis

Incretins

e.g. Exenatide + Liraglutide
These are synthetic versions of GLP-1 which reduce appetite, taken by subcutaneous injection
– Acts by increasing insulin secretion, decreasing glucagon secretion and decreasing appetite

Side effects
  • Sickness
  • Pancreatitis
  • Also cause weight loss

DPP-4 inhibitors

e.g. Sitagliptin, Saxagliptin (-gliptin)
-These inhibit the DPP-4 enzyme which breaks down the incretins GLP-1 and GIP

Side effects
  • Indirectly cause sickness
  • Pancreatitis
  • Weight loss

Amylin analog

e.g. Pramlintide
This is a polypeptide stored and secreted by B-cells which acts with insulin to reduce blood sugar
– Treats type 1 and 2 diabetes by slowing gastric emptying and decreasing glucagon secretion.

SGLTI (selective sodium glucose transporter 2 inhibitor)

e.g. Empagliflozin (-gliflozin)
– Blocks glucose reabsorption in the kidneys to promote excretion of excess glucose in urine

Side effects
  • Genital infections
  • UTI due to increased glucose in urine
  • Diabetic Ketoacidosis

Drugs which increase blood glucose

Glucagon
This is a hormone which is made by the alpha cells of the pancreas and is gluconeogenic
– It used to rescue people from hypoglycaemic crisis acting to increase the serum glucose concentration
– Has minimal side effects

Diazoxide
This is a potassium channel opener that binds and opens ATP-sensitive K+ channels in the ß-cells causing hyperpolarization –> inhibits insulin release.
– Used to treat hypoglycemia secondary to an insulinoma
– Also used as a potent vasodilator used in hypertensive emergency

Disclaimer

The intended purpose of this website is to be used as a resource for revision for exams. It should not be used as a guideline or reference for clinical practice/decision making or by patients looking for medical information or advice. In2Med takes no responsibility for any loss or damaged resulting from the use of information from this website.

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