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Y2 Pharmaco > Hypoglycaemic Agents > Flashcards

Hypoglycaemic Agents Flashcards

1
Q

Name the 2 insulin sensitizers:

A
  1. Biguanide - Metformin
  2. Thiazoldinediones - Pioglitazone
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2
Q

Name the 2 Meglitinides.

A
  1. Repaglinide
  2. Nateglinide
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3
Q

Name the 2 naturally occurring incretin hormones.

A
  1. Glucose-dependent insulinotropic polypeptide (GIP)
  2. Glucagon-like peptide-1
  • increases insulin secretion when there is an increase in glucose levels
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4
Q

Why do Incretin hormones have a short half life?

A
  • due to rapid inactivation by dipeptidyl peptidase-4

(So in incretin based therapy, we inhibit dipeptidyl peptidase-4, so that incretin hormones will exist for longer and more insulin is secreted)

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5
Q

Name the 3 SGLT2 inhibitors.

A
  1. Empaglifozin
  2. Canagliflozin (increases risk of lower limb amputation)
  3. Dapaglifozin
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6
Q

SGLT2 inhibitors have what effect?

A
  • cardiorenal protective effects
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7
Q

List out the 5 types of Hypoglycaemic Agents.

A
  1. Insulin sensitisers
  2. Insulin secretagogues
  3. α glucosidase inhibitors
  4. Incretin based therapy
  5. Sodium-glucose co-transporter 2 inhibitors
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8
Q

What are the 2 types of hypoglycaemic agents that cause weight gain?

A
  1. Thiazoldinediones - Pioglitazone
  2. Sulfonylureas e.g. Gibenclamide
  • better not give in obese patients
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9
Q

Which Hypoglycaemic agents are preferred for obese patients?

A
  1. GLP-1 receptor agonist
    - incretin mimic, promotes secretion of insulin + feeling of satiety
  2. Sodium-Glucose co-transporter 2 inhibitors
    - prevents reabsorption of glucose, glucose gets excreted
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10
Q

What is the main difference between sulfonylureas and meglitinides? + implications

A

Dependency on glucose levels

Sulfonylureas NOT dependent, Meglitinides DEPENDENT

Sulfonylureas have a higher risk for hypoglycaemia as it is not glucose dependent
Meglitinides diminish at low glucose concentrations => reduces risk of hypoglycaemia

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11
Q

What are some negative side effects of incretin mimetics?

A
  1. GIT issues: nausea, vomiting, diarrhea, indigestion
  2. Use w caution in patient w renal problems.
    => contraindicated in patients w severe renal impairment
  3. Increased risk of Vit B12 malabsorption => vit b12 deficiency, can worsen symptoms of neuropathy

TLDR: git, renal, vit b12

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12
Q

Simply put, what do Sulfonylureas do?

A
  • bind to potassium channel => cause insulin to be released whether or not glucose is present
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13
Q

Side effects of Sulfonylureas?

A
  1. Weight gain
  2. High risk for hypoglycemia
    - esp in elderly n those w renal/hepatic impairment
    - renal impairment=> metabolism impaired=> sulfonylurea stays in system for longer
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14
Q

Name all the Sulfonylurea drugs:

A
  1. Gibenclamide
    - longest acting sulfonylurea, highest risk of hypoglycemia
    - 50% renal 50% faecal excretion
  2. Glipizide
    - shortest duration of action
    - excreted in urine
  3. Glimepiride (2nd gen)
  4. Gliclazide
  5. Tolbutamide (1st gen)
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15
Q

What are insulin secretagouges and which are the 2 classes of insulin secretagouges?

A

Insulin secretagouges: gets pancreatic β-cells to secrete insulin

  1. Sulfonylureas
    - independent of glucose levels => higher risk of hypoglycemia
    - side effect: weight gain
  2. Meglitinides
    - dependent on glucose levels, diminishes at low glucose concentrations => reduced risk of hypoglycemia
    - more rapid onset + shorter duration than sulfonylureas
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16
Q

Name the 3 DPP-4 inhibitors:

A
  1. Sitagliptin
  2. Vildagliptin
  3. Linagliptin*
    - suitable for px w renal impairment!!
    -> no dose adjustment in patients w chronic kidney disease cuz it is excreted 80% thru faeces (other 2 are excreted via renal)
17
Q

Which DPP-4 inhibitor is suitable in patients w renal impairment?

A

Linagliptin
- no dose adjustment in patients w chronic kidney disease cuz it is excreted 80% thru faeces (other 2 are excreted via renal)

18
Q

What are the glucose-dependent hypoglycaemic drugs?

A

Glucose-dependent: works only in presence of hyperglycemia)
1. Incretin based therapy
- DPP-4 inhibitors (Sitagliptin, Vildagliptin, Linagliptin)
- GLP-1 receptor agonists (Exanatide, Liraglutide)
2. Meglitinides (insulin secretagouges)
- Nateglinide
- Repaglinide

19
Q

What do α-glucosidase inhibitors do? Mechanism of action?

A

TLDR: prevent absorption of glucose in intestine

Mechanism:
1. Reversibly inhibits α-glucosidase in intestinal brush borders
2. Slow down increase in glucose levels after a meal => inhibit postprandial hyperglycaemia
3. Bacteria breaks down remaining carbs
- α-glucosidase hydrolyse oligosaccharide to glucose & other sugars
- stronger affinity to α-glucosidase than carbs (inhibitor + α-glucosidase > carbs + α-glucosidase)

20
Q

Name the hypoglycaemic drugs that can be orally administered

A

All hypoglycaemic drugs except GLP-1 receptor agonists(subcutaneous injection).

Aka.
1. Biguanide - Metformin
2. Thiazoldinediones - Pioglitazone
3. Sulfonyureas
4. Meglitinides
5. α-glucosidase inhibitor
6. DPP-4 inhibitors
7. SGLT2 inhibitors

21
Q

Name the hypoglycaemic drug that blocks glucose reabsorption at the kidneys.

A

SGLT2 inhibitors

Sodium-Glucose Co-Transporter 2 inhibitors

22
Q

Mechanism of action for SGLT2 inhibitors?

A
  1. Inhibits SGLT2
    - decreases reabsorption of filtered glucose
    - decreases renal threshold for glucose (cannot hold as much glucose => pee out)
  2. Increases urinary glucose excretion
23
Q

What is unique adverse effect of Canagliflozin?

A

Increased risk of lower limb amputation

24
Q

Adverse effects of SGLT2 inhibitors?

A
  1. Urinary tract infection (due to increased glucose in urine, which bacteria will feed on)
  2. Increased urination (cuz water leaves w the glucose)
  3. Female genital mycotic infections (fungal)
  4. Diabetic ketoacidosis (even if blood glucose normal)
    +
  5. Canagliflozin: increased risk of lower limb amputation
25
Q

Which hypoglycaemic drug is administered subcutaneously

A

Glucagon-like peptide-1 (GLP-1) receptor agonists
E.g. Exenatide, Liraglutide

26
Q

Name a α-glucosidase inhibitor.

A

Acarbose

27
Q

Gibenclamide is also known as..

A

Glyburide

28
Q

Liraglutide is a..

A

Incretin mimic. GLP-1 receptor agonist

29
Q

Exenatide is a..

A

Incretin mimic. GLP-1 receptor agonist

30
Q

What is the 1st line hypoglycemic drug given during therapy?

A

Metformin

31
Q

What are the 2nd line hypoglycemic drugs given during therapy?

A
  1. SGLT 2 inhibitors
  2. Sulfonylureas
  • given when metformin is not enough (all 3 drugs are relatively cheap)
32
Q

Which drugs are contraindicated in px w renal impairment?

A
  1. Metformin (biguanide)
  2. Pioglitazone (thiazoldinediones)
33
Q

Which drugs are contraindicated in px w pancreatitis?

A

Incretin based therapy
- DPP-4 inhibitors
- GLP-1 agonists

34
Q

Which hypoglycemic drug cannot be given in px w inflammatory bowel syndrome?

A

Acarbose

Y2 Pharmaco (22 decks)

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