Diabetes Flashcards

1
Q

Primary mech. of metformin

A

activates AMPK in hepatocyte mitochondria to inhibit ATP
blocks gluconeogenesis (and more glucose output)
blocks adenylate cyclase to help fat oxidation
= help restore insulin sensitivity

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2
Q

Metformin drug targets?

A

AMPK (5’- Activated protein kinase)

in hepatocyte mitochondria

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3
Q

Metformin side effects

A

GI (20-30% of patients)
Abdominal pain, low appetite, diarrhoea, vomiting)
esp in high doses
slowly increasing dose can help improve tolerability instead

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4
Q

How does metformin have therapeutic and side effects? (3 marks)

A

accumulates in liver (therapeutic) and in GI tract (side effect) as it needs organic-cation-transporter1 (OCT-1) to access tissues because its v polar (3 marks)

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5
Q

examples of DPP-4 inhibitors

A

Dipeptide Peptidase 4 inhibitors

=Sitagliptin

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6
Q

Prim mech of DPP-4 inhibitors?

A

inhibit DPP-4
present in vascular endothelium and metabolises incretins in plasma

basically stops incretic metabolism

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7
Q

what do incretins do

A

Incretins (e.g. GLP-1) are secreted by enteroendocrine cells and help stimulate the production of insulin when it is needed (e.g. after eating) and reduce the production of glucagon by the liver when it is not needed (e.g. during digestion). Incretins also slow down digestion and decrease appetite.

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8
Q

sitaglipin drug target

A

DPP-4 inhibitor

mainly in vascular endothelium

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9
Q

examples of sulphonylurea

A

Glicazide

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10
Q

Prim mech of sulphonylurea

A

inhibit KATP channel on pancreatic beta cells, causes depolarisation and Ca2+ influx causes insulin vesicle exocytosis

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11
Q

what does the KATP channel do?

A

the ATP-sensitive potassium (KATP) channel on the pancreatic beta cell. This channel controls beta cell membrane potential

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12
Q

Drug target of sulphonylurea

A

KATP channel in pancreatic beta cells

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13
Q

Glicazide side effects?

A

weight gain

hypoglycemia

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14
Q

When are sulphonylureas most effective?

A

The sulfonylureas act mainly by augmenting insulin secretion and consequently are effective only when some residual pancreatic beta-cell activity is present.

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15
Q

SGLT2 inhibitor example and full form?

A

Sodium-glucose co-transporter (SGLT2) inhibitors

Dapaglifozin

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16
Q

Primary mech. of SGLT2 inhibitors?

A

SGLT2 inhibited in PCT so less glucose reabsorbed and more is excreted in urine

17
Q

Dapaglifozin drug target?

A

SGLT2 in PCT

18
Q

SGLT2 inhibitor side effects

A

Uro-genital infections due to increased glucose load,
slight bone formation decrease,
DKA can worsen (then must stop immediately)

19
Q

in what patients can SGLT2 inhibitors be less effective?

A

SGLT2i action depends on normal renal fucntion so they are less effective in patients with renal impairment

20
Q

other (kinda positive) side effects of SGLT2 inhibitors

A

weight loss and lower BP