Anti-Diabetic Drugs Flashcards Preview

systemic pharmaco > Anti-Diabetic Drugs > Flashcards

Flashcards in Anti-Diabetic Drugs Deck (16):
1

Classes of anti-diabetic drugs & examples

Insulins
- Ultra short acting (insulin lispro, insulin aspart, insulin glulisine)
- Short acting (regular insulin)
- Intermediate acting (NPH, insulin detemir)
- Long acting (insulin glargine, insulin detemir)

Oral Hypoglycemic Agents
- Insulin Secretagogues
1. Sulphonylureas (Glibenclamide, Glipizide)
2. Prandial Glucose Regulators/Meglitinides (Repaglinide)
3. Dipeptidyl peptidase-4 Inhibitors (Sitagliptin)
- Insulin Sensitisers
4. Biguanides (Metformin)
5. Thiazolidinediones (Rosiglitazone)
- Insulin Release Sparers
6. α-glucosidase Inhibitors (Acarbose)

2

Toxicity of insulins (4)

1. Hypoglycemia
2. Lipodystrophy - lipoatrophy, lipohypertrophy
3. Factitious hypoglycemia
4. Allergy, redness at injection site

3

Mechanism of action of sulphonylureas

Blocks ATP sensitive K channels - depolarisation - opens voltage gated Ca channels - stimulates insulin release

4

Toxicity of sulphonylureas (5)

1. GIT related
2. Rash
3. Hypoglycemia (esp glibenclamide, long half life)
4. Tolbutamide (1G) - Hypothyroidism, liver damage, nephrotic syndrome, teratogenicity in animals
5. Drug interactions - increases hypoglycemic effects of sulphonylureas
- Salicylates, NSAIDs - displace sulphonylureas from plasma protein binding sites
- Sulphonamides - inhibit hepatic metab of sulphonylureas

5

Mechanism of action of meglitinides

Acts on 3 binding sites (overlaps with sulphonylureas) - regulates K+ efflux through ATP-dependent K+ channels - increased Ca influx - more insulin release

6

Toxicity of meglitinides

No major adverse effects
No cross allergy with sulphonylureas
Use with caution in liver/renal impairment

7

Mechanism of action of DPP-4 inhibitors

Inhibits hydrolytic action (breakdown) of DPP-4 on incretins - increases blood levels of GLP-1 & GIP - increases insulin and decreases glucagon levels - normalizes glucose levels

GLP-1 - glucagon-like peptide - promotes insulin release
GIP - gastric inhibitory peptide - reduces release of glucagon from pancreas

8

Toxicity of DPP-4 inhibitors

1. Nasopharyngeal, URTI
2. Headaches
3. Dose reduction req in renal-impaired patients

Lower occurrence of hypoglycemia & weight gain

9

Mechanism of action of biguanides

1. Increases insulin receptor density & sensitivity (main action)
2. Directly stimulates glycolysis in peripheral tissues
3. Reduces hepatic gluconeogenesis
4. Decreases glucose absorption from GIT
5. Reduces glucagon release

10

Uses of biguanides

1. Obesity related type 2 DM - reduces TG levels & promotes weight loss

11

Toxicity of biguanides (4)

1. GIT related
2. Metallic taste
3. Weight loss
4. Lactic Acidosis - inhibits lactate conversion to glucose

12

Mechanism of action of thiazolidinediones

Activates PPAR-

13

Toxicity of thiazolidinediones (5)

1. Water retention
2. Weight gain (not used in obesity related type 2 DM)
3. Increased HDL levels
4. Induced ovulation
5. Hepatic impairment

14

Mechanism of action of α-glucosidase inhibitors

Does not depend on insulin for its effects
- Competitively inhibits intestinal glucosidases - decreased digestion of carbohydrates & decreased glucose production

15

Uses of α-glucosidase inhibitors

Blunts rise in post-prandial blood glucose
- Does not work on lactose!! lactase still functions - decrease milk intake
- Use in combination with sulphonylureas/insulin to improve glucose control

16

Toxicity of α-glucosidase inhibitors (3)

1. Flatulence
2. Diarrhea
3. Hepatitis (high doses)