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5 - Pharmacology > Diabetes Drugs > Flashcards

Diabetes Drugs Flashcards

(45 cards)

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1
Q

What is the normal range for blood glucose levels?

A

3.5 - 8 mmol/L

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2
Q

What are some of insulins actions?

A 
Increased:
- glucose uptake
- glycogenesis
- glycolysis
- lipogenesis
- esterification of FAs
- lipoprotein lipase activity
- amino acid uptake and protein synthesis
Decreased:
- gluconeogenesis
- lipolysis
- ketogenesis
- proteolysis
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3
Q

What are some of the actions of glucagon?

A 
Increased:
- glycogenolysis
- gluconeogenesis
- ketogenesis
- lipolysis
Decreased glygogenesis
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4
Q

How does insulin bring about action?

A

Circulates free in the blood plasma and binds to surface receptors which stimulates enzymes and proteins inside the cell to act.

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5
Q

How does glucagon bring about action?

A

Binds to glucagon receptors in cell membranes and stimulates adenylate cyclase, increase cAMP. This activates protein kinase A which phosphorylates and activates enzymes inside the target cell.

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6
Q

How can you describe diabetes mellitus?

A

An inability to regulate plasma glucose withing normal range.

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7
Q

Give some characteristics of diabetes mellitus

A
  • absolute/relative insulin deficiency
  • hyperglycaemia
  • glycosuria
  • polyuria- polydipsia
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8
Q

What is the first line of treatment when someone is diagnosed with type 2 diabetes?

A

Use diet and exercise to try and maintain adequate glucose control.

  • limit fat intake
  • increase intake of complex carbohydrates
  • reduce alcohol
  • stop smoking
  • increase amount of exercise
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9
Q

Give some of the major groups of oral hyperglycaemics

A 
Sulphonureas
Biguanides
Thiazolidinediones/glitazones
Gliptins/DPP-4 inhibitors
SGLT2 Inhibitors/Gliflozins
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10
Q

Describe the mechanism of action of sulphonylureas

A

They antagonise K+/ATPase activity of beta cells, causing depolarisation. VOCCs open and increase Ca2+ causes insulin vesicles to fuse with the membrane and release increased amounts of insulin.

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11
Q

Why can you only prescribe sulphonylureas in certain patients?

A

Patients need to have residual beta cell activity- helps to enhance the remaining activity.

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12
Q

What are some ADRs that can arise from taking oral suphonureas?

A

Hypoglycaemia
GI disturbance
Weight gain

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13
Q

Give some examples of some sulphonureas

A

Tolbutamide
Glibencamide
Glipizide

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14
Q

When would you not prescribe sulphonureas?

A

Breastfeeding women
Elderly
Patients with renal or hepatic insufficiency

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15
Q

Describe the mechanism of action of biguanides

A

Unclear mostly

  • increase insulin receptor sensitivity
  • enhances skeletal muscle and adipose uptake of glucose- inhibits hepatic gluconeogenesis
  • does not induce hypoglycaemia
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16
Q

Give an example of a biguanide

A

Metformin

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17
Q

When would you prescribe a biguanide?

A

In type 2 diabetes when there is endogenous insulin presence

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18
Q

When would you not prescribe a biguanide?

A

With compromised:

  • Heart function
  • Renal function
  • Hepatic function
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19
Q

Give some ADRs of biguanides

Study These Flashcards
A 
GI disturbances (slow titration limits this)
Lactic acidosis
20
Q

Give the mechanism of action of Thiazolidinediones

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A

PPAR-gamma agonist

  • binds to a nuclear hormone receptor site
  • reduces gluconeogenesis
  • increases glucose uptake into muscles(PPARG regulates FA storage and glucose metabolism)
21
Q

Give some examples of thiazolidinediones

Study These Flashcards
A

RosiglitazonePioglitazone

22
Q

When would you prescribe a thiazolidinediones?

Study These Flashcards
A

In uncontrolled, non-insulin dependent diabetes

23
Q

Give some ADRs for thiazolineinediones

Study These Flashcards
A

GI disturbance

Weight gain

24
Q

Give a drug-druf interation for thiazolineinediones

Study These Flashcards
A

Are heavily protein bound so could potentially be displaced

25
Give the mechanism of action for meglitidines
K+/ATP antagonists on beta cells, causing depolarisation, calcium entry and fusion of insulin containing vesicles with the cell membrane
26
Give some examples of meglitidines
Repaglinide | Nateglinide
27
Why have insulin analogues been developed?
- Do not have to rely on extraction of insulin from animals- can give an injection containing different types of insulin with varying characteristics e.g. rapid acting + intermediate acting + long acting. This helps to give the best control of blood glucose levels as possible.
28
When would you use ultra rapid and short acting insulin?
Afters mealsWith acute hyperglycaemia
29
When would you use intermediate and long acting insulin?
Basal insulinOvernight control
30
What are the different types of insulin regimes?
Pre-mixed insulin - given twice a day with mealsIntermediate/long acting insulin + Fast or short acting insulin- intermediate insulin provides a basal level that acts overnight and short acting insulin is given with meals for an acute response.
31
Which insulin regimen gives a better level of glycaemic control?
The mix of different insulins
32
Describe the monitoring that must occur with acute treatment
- Need to monitor several times a day with advanced diabetes- Helps to initially determine the dosing levels of insulin
33
Describe the monitoring in chronic diabetes treatment
Glucose reacts with the terminal valine on Hb to produce glycosylated Hb (HbA1c). The HbA1c is a good indicator of how effective blood glucose control has been.
34
How often do you need to measure HbA1c levels?
3 months - this is how long RBCs stay in the circulation
35
What HbA1c percentage would be indicative of poorly controlled diabetes?
10% and above
36
What are the main types of anti-obesity agents?
Orlistat Sibutramine Rimonabant
37
Describe the mechanism of action of orlistat
Is an inhibitor of gastric and pancreatic lipase. This means there is a reduction in conversion of dietary fat to FAs and glycerol by 30%.
38
Give some ADRs for orlistat
Soft fatty stools Flatus Faecal discharge/ incontinence
39
Describe the mechanism of action for sibutramine
Is a noradrenaline and seratonin re-uptake inhibitor which causes appetite suppression and increased thermogenesis
40
Give some ADRs for sibutramine
Increased heart rateIncreased blood pressure
41
Describe the mechanism of action for rimonbant
Is an endocannabinoid antagonist- decreases body weight- helps regulate body-weight gain
42
Give some ADRs for rimonabant
Depression -- has been withdrawn from use by NICE
43
Describe the mechanism of action for gliptins
DPP-4 inhibitors - block action of DPP-4, an enzyme which breaks down incretin - Increased incretin levels acts to stimulate insulin release
44
Give some examples of glilptins
Sitagliptin | Anagliptin
45
Give the mechanism of action of SGLT2 inhibitors
Inhibit SGLT2 channel in kidney, so there is less glucose reabsorption, causing a reduction in blood glucose levels. - increase insulin sensitivity - increase glucose uptake in muscles - decreased gluconeogenesis - improved first phase insulin release

5 - Pharmacology (17 decks)

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