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203: The endocrine system > T2 DM drugs > Flashcards

T2 DM drugs Flashcards

1
Q

Insulin hepatic effects

A

Increases glycogenesis

Inhibits:

  • Gluconeogenesis
  • Glycogenolysis
  • Ketogenesis
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2
Q

Insulin skeletal muscle effects

A

Increases:

  • GLUT-4 translocation= more glucose uptake
  • Glucose oxidation
  • Glycogenesis
  • Amino acid uptake
  • Protein synthesis

Decreases:

  • Glycogenolysis
  • Amino acid release
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3
Q

Insulin adipocytes effects

A

Increase:

  • Glucose uptake
  • TG synthesis

Decreases:

  • FFA release
  • Glycerol release
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4
Q

Sulfonylurea examples

A

Glyburide

Glipizide- short half life

Glimepiride- long acting

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5
Q

Sulfonylurea drug properties

  • Oral activity
  • Protein bound
  • Side effects
A

Orally active

Bound to plasma protein

Side effect: Hypoglycaemia

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6
Q

Sulfonylurea indication

A

In T2 DM when:

  • Patient <40, but can now be younger.
  • DM for <10 yrs
  • Daily insulin <40 units.
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7
Q

Sulfonylurea primary mechanism of action

A

Stimulates endogenous insulin release from beta-cells

  • Binds to ATP-sensitive K+ channel to inhibit it
  • Triggers depolarisation of the cell
  • Entry of Ca2+ triggers release of insulin
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8
Q

Sulfonylurea secondary mechanism of action

A

Sensitise beta-cells to glucose

Decreased lipolysis

Decreased clearance of insulin by the liver

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9
Q

Biguanide/ Metformin

- Metabolic mechanism

A

Increase glucose uptake in muscle and decrease glucose production in the liver.

In hepatocytes

  • Stimulates AMP-activated protein kinase [AMPK] dependant and independant pathways.
  • AMPK inhibits expression of PEPCK and Glucose-6-phosphates by increasing SHP
  • PECK and Glucose-6-phosphatase drive gluconeogenesis
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10
Q

SHP

A

A nuclear transcription factor

It’s expression is increased by AMPK
- An effect of metformin

Inhibits expression of genes for PEPCK and Glucose-6-phosphatase

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11
Q

PEPCK

A

Phosphoenolypyruvate carboxykinase

Protein that drives gluconeogenesis

It’s synthesis is inhibited by SHP via AMPK pathway

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12
Q

Biguanides on insulin sensitivity

A

Increases insulin sensitivity

- Improves binding ability of insulin receptors.

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13
Q

Biguanides on peripheral glucose uptake.

A

Increases uptake

AMPK pathway
- Increases GLUT-4 translocation

AMPK-independant

  • Changes heart muscle to metabolise glucose more using p38 MAPCK
  • PKC-depedant
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14
Q

Biguanides effects on

  • Adipose tissue
  • GIT
A

Adipose [opposes insulin]
- Increases fatty acid oxidation by decreasing insulin-induced suppression of FA oxidation

GIT:
- Decreases glucose absorption

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15
Q

Metformin properties

  • Oral activity
  • Plasma proteins
  • Metabolism and excretion
  • Other indications
A

Orally active

Does not bind to plasma proteins

Not metabolised + excreted in urine

Other indications
- Polycystic ovarian syndrome

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16
Q

Adverse effects of biguanides

A

Lactic acidemia [increased glucose metabolism in muscle]
- Especially in those with renal impairment

GI symptoms [decreased glucose absorption]

  • Nausea
  • Abdominal discomfort
  • Diarrhoea
  • Metallic taste
  • Decreased Vit B12/ Folate absorption [chronic]

Anorexia

Metallic taste

MI/ Septicaemia

17
Q

Metformin contraindications

A

Hepatic disease

Lactic acidosis history

Cardiac failure

Chronic hypoxic lung disease

18
Q

Thiazolindinediones [glitazones]

  • Mechanism
  • Action on: liver, skeletal muscle, adipose
A

Mechanism
- Activates peroxisome proliferator-activated receptor-gamma [PPAR-gamma]

Liver
- Decreases: gluconeogenesis, glucose output, TG production

Muscle
- Increase glucose uptake and utilisation

Adipose

  • Increase glucose uptake
  • Decrease FA output
  • Causes differentiation of adipocytes
19
Q

Peroxisome proliferator-activated receptor-gamma [PPAR-gamma]

A

Receptor that is activated by Glitazones

Receptor involved in the transcription of insulin-responsive genes

Regulates adipose lipid mechanism.

20
Q

Use of glitazones

A

Can be used as monotherapy

Can be used with metformin or sulfonylureas.

Dose: one/twice daily

21
Q

Glitazones

  • Example
  • Plasma life
  • Metabolism
  • Excretion
A

Example
- Pioglitazone

Half life

  • 3-7hrs
  • Active metabolites= 16-24 hrs

Metabolism
- Liver

Excretion

  • Faeces [mainly]
  • Urine
22
Q

Glitazones

- Adverse effects

A

Fluid retention

  • Oedema
  • Mild anaemia

Weight gain

Not safe for breastfeeding and pregnancy

Requires regular blood tests if liver damaged
[due to liver metabolism]

23
Q

Glitazone drug interactions

A

Due to metabolism in the liver
- Interacts with enzymes

Lowers oral contraceptive level

24
Q

Glucagon-like peptide-1 [GLP-1] analogs

A

GLP-1 is an incretin released from intestinal cells

  • Stimulates the release from insulin from beta cells.
  • Its analogs perform a similar action

Example
- Exenatide

25
Q

Exenatide

  • Drug type
  • Mechanism [liver, stomach, satiety]
A

GLP-1 analog

  • Resistant to DPP-4 degradation
  • Long half life

Mechanism

  • Inhibits liver glucose output—> Suppresses release of glucagon in pancreas
  • Slows gastric emptying= allows more time for glucose control.
  • Reduces liver fat content
  • Reduces appetite + increases satiety
26
Q

Exenatide

- Use

A

Subcutaneous

- 30-60mins before last meal of the day.

27
Q

DPP-4 inhibitors
- Overall function

  • Examples
A

DPP-4 degrades incretins and inhibits insulin secretion.

  • Inhibitors act to increase GLP-1 and GIP levels = increased incretins
  • Increases the effects of incretins

Examples

  • Vildagliptin
  • Sitagliptin
  • Saxagliptin [irreversible]
28
Q

DPP-4 inhibitors

- Oral activity?

A

Orally active

29
Q

SGLT-2 inhibitors

- Examples

A

Increases excretion of glucose via the urine
- Inhibits low affinity, high capacity SGLT-2 protein carrier

Examples

  • Dapagliflozin
  • Canagliflozin
30
Q

SGLT-2 inhibitors

- Effects

A

Reverses hyperglycaemia by inhibiting glucose absorption

Increases insulin sensitivity in muscle and liver

Decreases gluconeogenesis

Improves beta cell function

31
Q

Adverse side effects of SGLT-2 inhibitors

A

Rapid weight loss

Fatigue

Dehydration

May worsen UTI/ thrush.

32
Q

First line drug for T2 DM

A

Metformin

203: The endocrine system (23 decks)

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