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Insulin Drugs > Oral Antidiabetic Agents > Flashcards

Oral Antidiabetic Agents Flashcards

1
Q

Insulin secretagogues

A

Sulfonylureas (-amide)
E.g. Glibenclamide, Tolbutamide, Chlorpropamide
- activate secretion of insulin
- stimulate additional insulin

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2
Q

Clinical action of Sulfonylureas

A
  1. Increase insulin release from pancreatic B cells
  2. Reduction of serum glucagons concentrations
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3
Q

Clinical uses for Sulfonylureas

A

Type 2 DM

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4
Q

Adverse effects of Sulfonylureas

A
  1. Hypoglycemia
  2. Weight gain
  3. Gastrointestinal upsets
  4. Allergic skin rash, bone marrow damage
  5. Increase in cardiovascular death
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5
Q

Insulin sensitisers

A

Biguanides (Metformin)
Thiazolidinediones (-glitazone)
E.g. rosiglitazone, pioglitazone
- increase or restore tissue sensitivity dependent on having insulin

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6
Q

Biguanides (Metformin)
Pharmacokinetics

A
  1. Metformin is not bound to plasma proteins
  2. It is not metabolites and is excreted by kidneys as the active compound
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7
Q

Actions of Metformin

A
  1. Increase insulin sensitivity by increasing insulin receptor density (more of receptors to receive signals)
  2. Direct stimulation of glycolysis in tissues; increased glucose removal from blood
  3. Reduced hepatic and renal gluconeogenesis
  4. Slowing glucose absorption from GIT
  5. Reduction of plasma glucagon levels
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8
Q

Clinical uses of Metformin

A
  1. Type 2 diabetes
  2. Insulin resistance syndrome (early stage, pre diabetic syndrome)
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9
Q

Adverse effects of Metformin

A
  1. Anorexia, nausea, vomiting, abdominal discomfort, diarrhoea
  2. Reduced vitamin B12 absorption
  3. Contraindications: renal disease, alcoholism, hepatic disease or conditions predisposing to tissue anoxia (not enough O2 in tissue)

Note: before surgery, do not eat Metformin as it can cause decrease in oxygen levels especially if surgery requires GA

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10
Q

Mechanism of action of Tzds (-glitazone)

A

Peroxisome proliferator activated receptor gamma (PPAR-y) is known to heterodimerise with another transcription factor, retinoid X receptor (RXR).

Tzds bind to PPAR-y-RXR complex so that the complex binds DNA and promotes transcription of several genes with products that are important in insulin signalling including lipoprotein lipase, fatty acid transporter protein, adipocyte fatty acid binding protein, Glut-4 and others.

  1. Reduce hepatic glucose output
  2. Increase glucose uptake into muscle tissue
  3. Decrease triglyceride levels in blood
  4. Increase lipogenesis and enhance uptake of fatty acids and glucose
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11
Q

Clinical uses of Tzds

A

Type 2 diabetes

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12
Q

Adverse effects of Tzds

A
  1. Hypoglycemia (+Sulfonylureas/insulin)
  2. Hepatotoxicity
  3. Fluid retention, weight gain
  4. Contraindication: liver disease, heart failure (rosiglitazone)
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13
Q

Insulin sparring agents

A

Acarbose
GLP-1 receptor agonists (exenatide, -glutide)
DPP-4 inhibitors (-gliptin)
SGLT2 inhibitors (-gliflozin)
- allow insulin to work more effectively so the body does not need to secrete as much insulin as before

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14
Q

Action of Acarbose (Alpha-glucosidase inhibitors)

A

Compared to dietary carbohydrates, Acarbose has 1000x stronger affinity for the active binding site of glucosidase enzymes. It delays the digestion of specific polysaccharides and thus absorption of sugars.

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15
Q

Pharmacokinetics of Acarbose

A

Acarbose is taken just prior to ingesting a meal.
Acarbose blunts the rise in postprandial blood sugar levels by 30-50% so that the insulin secretory response in return is also less.

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16
Q

Clinical uses of Acarbose

A
  1. Type 2 diabetics
    - mono therapy
    - (+) sulphonylurea/Biguanides
17
Q

Adverse effects of Acarbose

A
  1. Elevated liver enzymes
  2. Flatulence (bacteria metabolism in GIT due to unabsorbed glucose -> produce lots of gas)
  3. Diarrhoea
18
Q

GLP-1 Receptor agonists (exenatide, liraglutide, albiglutide, dulaglutide)
DPP-4 inhibitors (sitagliptin, saxagliptin, linagliptin, alogliptin, vildagliptin)

A
19
Q

Action of SGLT2 inhibitors (Gliflozin drugs)

A

Blocks reabsorption of glucose in the kidney, increase glucose excretion, and lower blood glucose levels.

Other mechanisms: allow increased insulin sensitivity and uptake of glucose in the muscle cells, decreased gluconeogenesis and improved first phase insulin release from beta cells.

20
Q

Clinical uses of SGLT2 inhibitors

A
  1. Type 2 diabetes
  2. Diabetes with cardiovascular diseases
21
Q

Adverse effects of SGLT2 inhibitors

A

Incidence of genital infections and urinary tract infections

Insulin Drugs (1 decks)

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