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Pharmacology > Diabetes > Flashcards

Diabetes Flashcards

1
Q

Describe the first line treatment for adults with type 2 diabetes who take metformin and the 1st and 2nd intensifications.

A

HbA1c @ 48mmol/mol (6.5%)
- Standard release metformin (500mg OD, oral)

HbA1c @ 58mmol/mol (7.5%)
- 1st intensification - dual therapy w/ metformin
(DPP-4 inhibitor, pioglitazone, SU (sulfonylurea), SGLT-2 inhibitor)

HbA1c @ 58mmol/mol (7.5%)
- 2nd intensification
(consider insulin based treatment, or triple treatment)

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2
Q

What is the pKa of metformin?

A

12.4

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3
Q

What is the optimal pKa in blood with a pH of 7.4 to diffuse out of the blood?

A

7.4

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4
Q

What does the pKa of metformin mean about it’s absorption and distribution about the body?

A

metformin pKa 12.4, so even in the most alkaline tissue (bile pH 9), metformin will be charged

therefore metformin is transported by organic cation transporter 1 (OCT1)

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5
Q

Where is OCT-1 expressed?

A

hepatocytes (liver)
enterocytes (small bowel)
proximal tubules (kidney)

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6
Q

Since metformin is so polar, how is it transported around body tissues?

A

organic cation transporter 1 (OCT1)

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7
Q

Since metformin is so polar, how is it transported around body tissues?

A

organic cation transporter 1 (OCT1)

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8
Q

Organic cation transporter 1 (OCT-1) is expressed in hepatocytes (liver), enterocytes (small bowel) and proximal tubules (kidney)

How is this relevant to the pharmocokinetics of orally administered metformin?

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.

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9
Q

What is a side effect of DPP-4 inhibitors?

A

upper resp tract infection

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10
Q

What is a side effect of SGLT-2 inhibitors?

A

urogenital infections

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11
Q

What is a side effect of Pioglitazone?

A

heart failure

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12
Q

What is a side effect of sulphonyurea?

A

weight gain

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13
Q

Which is cheaper, pioglitazone or DPP-4?

A

pioglitazone, by 30x

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14
Q

List the following for metformin:

  1. primary drug target
  2. drug target type
  3. location
  4. action
A
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15
Q

List the following for DPP-4 inhibitors:

  1. primary drug target
  2. drug target type
  3. location
  4. action
A
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16
Q

List the following for sulphonylureas:

  1. primary drug target
  2. drug target type
  3. location
  4. action
A
17
Q

List the following for SGLT-2 inhibitors:

  1. primary drug target
  2. drug target type
  3. location
  4. action
A
18
Q

List the following for SGLT-2 inhibitors:

  1. primary drug target
  2. drug target type
  3. location
  4. action
A
19
Q

How should metformin be a treatment be adjusted for patients with renal impairment (using eGFR)?

A
20
Q

Why does the dose of metformin need to be adjusted if a patient has renal impairment?

A

metformin levels become too high in blood as kidneys are not excreting int properly.

Pharmacology (10 decks)

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