Oral hypoglycaemic agents Flashcards

1
Q

Name a biguanide:

A

Metformin

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2
Q

How does metformin work?

A

Insulin sensitizer. Reduces gluconeogenesis in the liver . It also slows intestinal absorption of sugars and improves peripheral glucose uptake and utilisation.
Reduces LDL and VLDL. and increase HDL.

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3
Q

What are the pharmacokinetics of metformin?

A

Well absorbed orally.
Not bound to serum proteins
Not metabolised
Excreted via urine.

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4
Q

ADR’s metformin?

A

GI
Lactic acidosis in those with renal failure. Rare
Vit B12 uncommon

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5
Q

Contraindications/DDIs of metformin?

A
Renal/heaptic disease
Diabetic ketoacidosis 
>80 years old
Congestive Heart Failure
Alcohol abuse
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6
Q

Give some examples of sulfonylureas:

A

Glicazide, glipizide, glimepiride

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7
Q

What is the mechanism of action of sulfonylureas?

A

Stimulation of beta cells to release insulin. Block ATP sensitive K+ channels resulting in depolarisation and Ca2+ influx and causing Insulin release.
Reduction in hepatic glucose production
increase peripheral insulin sensitivity.

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8
Q

Describe the PK’s of sulfonylureas:

A

Bind to serum proteins
Metabolised by the liver
Excreted by liver or kidney
Duration ranges fro 12 to 24 hrs

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9
Q

ADR’s of sulfonylureas:

A

Weight gain
Hyperinsulinaemia
Hypoglycaemia

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10
Q

Contraindications/DDI’s with sulfonylureas:

A

Renal impairment

Hepatic impairment

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11
Q

Name some examples of DDP-4 Inhibitors:

A

Sitagliptin, Vildagliptin, Saxagliptin, Linagliptin

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12
Q

What is the mechanism of action of DDP-4 Inhibitors?

A

Inhibit the DDP-4 enzyme which breaks down GLP-1. GLP-1 is responsible for increasing Insulin secretion and increasing sensitivity to Insulin.

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13
Q

What are some of the side effects of DDP-4 Inhibitors?

A

Nasopharyngitis
Headache
Pancreatitis

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14
Q

Name some examples of Sodium Glucose Co-transporter 2 Inhibitors:

A

Dapagliflozin
Canagliflozin
Empagloifozin

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15
Q

What is the mechanism of action of Sodium Glucose Co-transporter 2 Inhibitors:

A

Inhibit SGLT2 in the tubular lumen of the kidney. Less glucose is reabsorbed. Lowers blood glucose.

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16
Q

What are the adverse effects of SGLT2 inhibitors?

A

Female genital mycotic infections (e.g. vulvovaginal candidiasis)
UTI’s
Urinary frequency
Hypotension

17
Q

Name some examples of GLP -1 Receptor Agonists:

A

Exenatide

Lirlutide

18
Q

What is the mechanism of action of GLP-1 receptor agonists?

A

Act on GLP-1 receptors and increase native insulin release.

Enhance satiety Slow gastric emptying time

19
Q

What are the PK’s of GLP-1 Receptor agonists?

A

Polypeptides - must be administered subcut.

20
Q

What are the adverse effect of GLP-1 agonists?

A
Nausea
Vomiting
Diarrhoea
Constipation
Pancreatitis