Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

IPE Pharmacology > Diabetic Drugs > Flashcards

Diabetic Drugs Flashcards

1
Q

Name a biguanide

A

Metformin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Mechanism of action of metformin

A

enhances the effect of insulin
Reduction in insulin resistance via modification of glucose metabolic pathways
Decreases hepatic gluconeogenesis and intestinal glucose absorption
Increases peripheral insulin sensitivity
Lowers postprandial and fasting blood glucose levels
Reduces LDL, increases HDL

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Benefits of metformin

A

Glycemic efficacy: lowers HbA1c by 1.2–2%) over 3 months
Weight loss or weight stabilization
No risk of hypoglycemia
Beneficial effect on dyslipidemia
Studies show metformin reduces the risk of macroangiopathic complications in diabetic patients.
Cost-effective

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Common side effects of biguanides

A
  • metformin associated lactic acidosis
  • GI- nausea, diarrhoea, flatulance
  • B12 deficiency
  • metallic taste in mouth
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Contraindications to metformin

A

Renal failure (if creatinine clearance < 30 mL/min)
Severe liver failure
Intravenous iodinated contrast medium
Pause metformin prior to surgery
Chronic pancreatitis, starvation ketosis, ketoacidosis, sepsis
Heart failure (NCYA III and IV), respiratory failure, shock, sepsis
Alcoholism

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Interactions with metformin

A

Sulfonylureas- increase in Cardiovascular mortality

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Name some thiazolidinediones

A

Pioglitazone

Rosiglitazone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Mechanism of action of thiazolidinediones

A

activation of the transcription factor PPARγ (peroxisome proliferator-activated receptor of gamma type) → ↑ transcription of genes involved in glucose and lipid metabolism → increased storage of triglycerides and subsequent reduction of products of lipid metabolism (e.g., free fatty acids) that enhance insulin resistance → glucose utilization is increased and hepatic glucose production reduced

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Benefits of thiazolidinediones

A

Glycemic efficacy: lowers HbA1c by 1% in 3 months
Favorable effect on lipid metabolism: ↓ triglyceride, ↓ LDL, ↑ HDL
No risk of hypoglycemia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Sid effects of pioglitazone

A

Fluid retention and oedema
Weight gain
Increased risk of heart failure
Increased risk of bone fractures (osteoporosis!)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Contraindications to pioglitazone

A

Congestive heart failure (NYHA III or IV)
Liver failure
Pioglitazone: history of bladder cancer or active bladder cancer; macrohematuria of unknown origin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Give some sulfonylureas

A 
Glyburide: the standard substance of this class with a relatively long half-life 
Glipizide: a short-acting agent
Gliclazide
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Mechanism of action of sulfonylureas

A

Sulfonylureas block ATP-sensitive potassium channels of the pancreatic β-cells → depolarization of the cell membrane → calcium influx → insulin secretion
Extrapancreatic effect: decreases hepatic gluconeogenesis and increases peripheral insulin sensitivity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Benefits of sulfonylureas

A

Glycemic efficacy: lowers HbA1c by 1.2% over 3 months
Long-term experience
Low-cost

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Side effects of sulfonylureas

A

Life-threatening hypoglycemia
Weight gain
Hematological changes: granulocytopenia, hemolytic anemia
Allergic skin reactions
Alcohol intolerance
Compared to metformin, sulfonylureas are associated with more cardiovascular (macrovascular) complications.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Contraindications to sulfonylureas

A 
Severe cardiovascular comorbidity 
Obesity
Sulfonamide allergy (particularly long-acting substances)
Severe liver failure
Severe kidney failure

Beta-blockers may mask the warning signs of hypoglycemia (e.g., tachycardia) and decrease serum glucose levels even further. Since sulfonylureas also increase the risk of hypoglycemia, the combination of these two substances should be avoided!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Give some examples of meglitinides

A 
Repaglinide: the leading agent in the class of meglitinides, which is well tolerated by patients with chronic kidney disease
Nateglinide
18
Q

Mechanism of action of meglitinides

A

Enhances insulin secretion (similar mechanism of action to that of the sulfonylureas)
Meglitinides should be taken shortly before meals.

19
Q

Benefits of meglitinides

A

Glycemic efficacy: lowers HbA1c by 0.75% over 3 months

More expensive than sulfonylureas

20
Q

Side effects of meglitinides

A

Life-threatening hypoglycemia (less risky than sulfonylureas)
Weight gain
Hepatotoxicity (rare)

21
Q

Contraindications to meglitinides

A

Severe liver failure
Severe renal failure
Interactions: sulfonylureas - same mechanism of action

22
Q

Examples of GLP-1 agonists

A

Exenatide
Liraglutide: rapid-release formula that is administered daily
Albiglutide: extended-release formula that is administered once weekly
Dulaglutide

23
Q

Mechanism of action of GLP-1

A

Incretin effect: food intake → activation of enteroendocrine cells in the gastrointestinal tract → release of GLP-1 → GLP-1 degradation via the enzyme DPP-4 → end of the GLP-1 effect
Incretin mimetic drugs bind to the GLP-1 receptors and are resistant to degradation by DPP-4 enzyme → increase insulin secretion, decrease glucagon secretion, slow gastric emptying (↑ feeling of satiety, ↓ weight)

24
Q

Benefits of GLP-1 agonists

A

Glycemic efficacy: lowers HbA1c by 0.5–1.5% over 3 months
Subcutaneous injection
Weight loss
No risk of hypoglycemia

25
Q

Side effects of GLP-1 agonists

A 
Gastrointestinal complaints (particularly impaired gastric emptying!) 
Increased risk of pancreatitis and potentially pancreatic cancer
26
Q

GLP-1 agonist contraindications

A

Preexisting symptomatic gastrointestinal motility disorders

Chronic pancreatitis or a family history of pancreatic tumors

27
Q

Examples of DP-4 inhibitors

A

Sitagliptin

Saxagliptin

28
Q

Mechanism of action of DP-4 inhibitors

A

Gliptins indirectly increase the endogenous incretin effect by inhibiting the dipeptidyl peptidase-4 enzyme that breaks down glucagon-like peptide 1 → increased insulin secretion, decreased glucagon secretion, delayed gastric emptying

29
Q

Benefits of DP-4

A

Glycemic efficacy: lowers HbA1c by 0.5–0.75% over 3 months

No risk of hypoglycemia unless insulin and/or insulinotropic drugs are used simultaneously

30
Q

Side effects of gliptins

A

Gastrointestinal complaints: diarrhea, constipation (milder than in GLP-1 agonist exposure)
Arthralgia
Headaches, dizziness
Increased risk of pancreatitis

31
Q

Contraindications to gliptins

A

Hypersensitivity
Liver failure
Moderate to severe renal failure

32
Q

Examples of SGLT-2 inhibitors

A

Dapagliflozin
Empagliflozin
Canagliflozin

33
Q

Mechanism of action of SGLT-2 inhibitors

A

reversible inhibition of the sodium-dependent glucose co-transporter (SGLT-2) in the proximal tubule of the kidney → reduced glucose reabsorption in the kidney → glycosuria and polyuria

34
Q

Benefits of SGLT-2 inhibitors

A

Glycemic efficacy: lowers HbA1c by 0.6% over 3 months
Promotes weight loss
Reduces blood pressure

35
Q

Side effects of SGLT-2 inhibitors

A

Urinary tract infections, genital infections (vulvovaginitis, balanitis)
Dehydration as a result of polyuria
Severe diabetic ketoacidosis

36
Q

Contraindications to SGLT-2 inhibitors

A

Chronic kidney disease

Recurrent urinary tract infections (e.g., in patients with anatomical or functional anomalies of the urinary tract)

37
Q

Examples of alpha-glucosidase inhibitors

A

Acarbose

38
Q

Acarbose method of action

A

Inhibits alpha-glucosidase → decreased intestinal glucose absorption → The drug is particularly effective in controlling postprandial blood glucose levels.
The undigested carbohydrates reach the colon, where they are degraded by intestinal bacteria, resulting in the production of intestinal gas.

39
Q

Benefits of acarbose

A

Glycemic efficacy: lowers HbA1c by 0.8% over 3 months

No risk of hypoglycemia

40
Q

Side effects of acarbose

A

gastrointestinal complaints (flatulence, abdominal discomfort, diarrhea)

41
Q

Contraindications to acarbose

A

Inflammatory bowel disease
Conditions associated with malabsorption
Severe renal failure

IPE Pharmacology (3 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions