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BRS Pharm > Diabetes Pharmacology > Flashcards

Diabetes Pharmacology Flashcards

1
Q

What are the drugs for diabetes? (4)

A

Metformin

Sitagliptin

Gliclazide

Dapaglifozin

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2
Q

What is the drug class of metformin?

A

metformin

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3
Q

What is the drug target for metformin?

A

5′-AMP-activated protein kinase (AMPK)

The primary site of metformin action is the hepatocyte mitochondria

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4
Q

What is the primary method of action of metformin?

A

Primary effect – it activates AMPK in hepatocyte mitochondria
- This inhibits ATP production
- This blocks gluconeogenesis and subsequent glucose output
It also blocks adenylate cyclase which promotes fat oxidation. Both help to restore insulin sensitivity.

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5
Q

What are the main side effects of metformin?

A

GI side effects (20-30% of patients)
e.g. Abdominal pain, decreased appetite, diarrhoea, vomiting)

Particularly evident when very high doses are given. A slow increase in dose may improve tolerability.

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6
Q

What does metformin require to access tissues?

A

Metformin is highly polar and requires organic cation transporter-1 (OCT-1) to access tissues. This explains why it can accumulate in the liver (therapeutic effect) and gastrointestinal tract (side effects)

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7
Q

When is metformin most efective?

A

Metformin is most effective in the presence of endogenous insulin so is most effective with some residual functioning pancreatic islet cells

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8
Q

What drug class is sitagliptin?

A

Dipeptidyl-peptidase 4 (DPP-4) inhibitors

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9
Q

What is the drug target of siptiglabin?

A

DPP-4 (Dipeptidyl peptidase 4 (DPP-4))

The primary site of DPP-4 inhibitor action is the vascular endothelium

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10
Q

What is the primary mechanism of action of siptiglabin?

A

Primary effect - Work by inhibiting the action of DPP-4. This enzyme is present in vascular endothelium and can metabolise incretins in the plasma.
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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11
Q

What are side effects of sitagliptin?

A

Upper respiratory tract infections (5% of patients) Flu-like symptoms e.g. headache, runny nose, sore throat
Less common but serious:
Serious allergic reactions/ avoid in patients with pancreatitis

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12
Q

Compared to other anti-diabetic drugs (although not metformin) what do sitagliptin not do?

A

cause weight gain

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13
Q

How do DDP-4 inhibitors act mainly by?

A

DPP-4 I’s act mainly by augmenting insulin secretion and consequently are effective only when some residual pancreatic beta-cell activity is present.

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14
Q

What drug class is gliclazide?

A

sulphonylurea

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15
Q

What is the drug target for sulphonylurea?

A

ATP-sensitive potassium channel

The primary site of SUs inhibitor action is the pancreatic beta cell

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16
Q

What is the primary mechanism of action for sulphonylureas?

A

Primary effect – Inhibit the ATP-sensitive potassium (KATP) channel on the pancreatic beta cell. This channel controls beta cell membrane potential. Inhibition causes depolarisation which stimulates Ca2+ influx and subsequent insulin vesicle exocytosis.

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17
Q

What is are likely side effects of sulphonylurea?

A

weight gain is a likely side effect

hypoglycaemia (2nd most common)

18
Q

How do sulphonylureas mainly act?

A

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

19
Q

Weight gain from sulphonylureas are mitigated by what else?

A

by the concurrent administration with metformin

20
Q

What drug class is dapaglifozin?

A

Sodium-glucose co-transporter (SGLT2) inhibitors

21
Q

What is the drug target for Sodium-glucose co-transporter (SGLT2) inhibitors?

A

SGLT2

The primary site of SGLT2 inhibitor action is the proximal convoluted tubule

22
Q

What is the primary mechanism of action for sodium-glucose co-transporter (SGLT2) inhibitors?

A

Reversibly inhibits sodium-glucose co-transporter 2 (SGLT2) in the renal proximal convoluted tubule to reduce glucose reabsorption and increase urinary glucose excretion.

23
Q

What are side effects of SGLT2 inhibitors?

A

Uro-genital infections due to increased glucose load (5% of patients)
Slight decrease in bone formation

Can worsen diabetic ketoacidosis (stop immediately)

24
Q

What “benefits” do SGLT2 inhibitors cause?

A

weight loss and reduction in BP

25
Q

What does SGLT2 inhibitors depend on?

A

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

26
Q
A

Lose weight – reduces insulin resistance and reduces cardiovascular disease.

Reduce blood pressure – reduces cardiovascular disease.

Improve lipid profile – reduces cardiovascular disease.

Reduce blood glucose – reduces microvascular and macrovascular complications of diabetes.

27
Q
  • Obesity
  • High Blood pressure
  • Dyslipidaemia
  • High HBA1c (Diabetes = > 48mmol/L) she has 65
A

lifestyle modification

metformin if required

28
Q

What is the first line treatment for HbA1c over 48 when already given lifestyle advice?

A

metformin+ another type of med… (check flashcard b4 this)

29
Q

when should metformin be prescribed in patients with T2DM?

A

HbA1c above 48mmol/mol even with lifestyle intervention

30
Q

when is the first intensification of metformin treatment for T2DM?

A

HbA1c 58mmol/mol despite on metformin

dual therapy with 2 of DPP4i, SGLT2i, gliclazide, pioglitazone

31
Q

What is first line treatment for HbA1c over 58?

A

metformin

32
Q

why may you not choose to prescribe sulphonylureas (gliclazide)?

A

can cause weight gain - not for people with already high BMI

hypoglycaemic risk

33
Q

what patients would you choose to prescribe GLP-1 agonists and SGLT-2 inhibitors to?

A

patients with CVD risk - prevention

34
Q

when are thiazolidinediones contraindicated (pioglitazone)?

A

heart failure

35
Q

what diabetes drug is most tolerable?

A

DPP-4 inhibitors

moderately effective

36
Q
A

Metformin works in the liver (hepatocytes)
Metformin pka= 12.4, so even in most alkaline tissue (bile 9), it will still be polar
Organic cation transporter (OCT-1) is expressed in hepatocytes, enterocytes and proximal tubule

37
Q
A

Small bowel OCT-1 allows it to be
absorbed

Hepatocyte OCT-1 allows it to be distributed to the site of action.

Proximal tubule OCT-1 helps excretion.

38
Q

And why?

A
39
Q

Give drug target type and location of drugs for diabetes.

A
40
Q

How does diabetic ketoacidosis (DKA) develop?

A

BRS Pharm (9 decks)

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