Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

The Endocrine System > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Meformin: What class of drug?

A

Biguanide

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

Meformin: Originates from where?

A

French Lilac

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

Meformin: Structure

A

Two guanidine stuck together with two methyl groups

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

Meformin: Mechanism of Action

A

Inhibits Complex I of the Mitochondrial Respiratory Chain to cause a fall in cellular ATP which reduces gluconeogenesis via activating AMPK

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

Meformin: Impact on hepatic glucose production

A

Decreased

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

Meformin: Impact on gut glucose mobilisation and metabolism

A

Increased

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

Meformin: Impact on GLP-1 secretion

A

Increased

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

Meformin: Alters what in the GIT?

A

Microbiome

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

Meformin: Impact on lipogenesis

A

Decreased

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

Meformin: Why is it not readily uptaken by the cell?

A

Hydrophilic

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

Meformin: Mechanism of transport into cells?

A

Organic Cation Transporters

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

Meformin: Transporters are present in what organs? (3)

A

Intestines
Liver
Kidney

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Meformin: Excretion route

A

Urine

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

Meformin: Mechanism of metabolism

A

Not metabolised - excreted as metformin in urine

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

Meformin: How does this impact weight?

A

Promotes weight loss

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

Meformin: Dose

A

500mg-1g twice per day

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

Meformin: Side Effects - Gastrointestinal (5)

A

Diarrhoea
Bloating
Abdominal Pain
Dyspepsia
Metallic taste in mouth

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Meformin: Side Effects - How to reduce GI side effects?

A

Initiate dose slowly - 500mg once daily for 1 week then increase per week or use a modified release formulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Meformin: Side Effects - MALA

A

Metformin Associated Lactic Acidosis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Meformin: Side Effects - Metformin increases the production of what in the liver and gut?

A

Lactate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Meformin: Side Effects - Metforming is associated with a greater risk of Lactic Acidosis during what? (2)

A

Sepsis
Impaired liver clearance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Meformin: Side Effects - If renal function becomes reduced what should happen to dose?

A

eGFR <45 ml/min - Reduce to a maximum dose of 1g daily
eGFR <30ml/min - Contraindicated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Sulphonylureas: 1st generation examples (2)

A

Tolbutamide
Chlorpropamide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Sulphonylureas: 2nd generation examples (4)

A

Gliclazide
Glipizide
Glimepiride
Gilbenclamide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Sulphonylureas: Derived from what?
Sulphonamides
26
Sulphonylureas: These are insulin ...
Secretagogues
27
Sulphonylureas: Mechanism of Action - Binds to what?
Extracellular SUR1 subunits
28
Sulphonylureas: Mechanism of Action - On binding what happens to the SUR1 subunits?
ATP Sensitive K channel close
29
Sulphonylureas: Mechanism of Action - Closure of the ATP sensitive K channel causes what to occur to the cell?
Exocytosis of Insulin due to activation of calcium channels (calcium influx)
30
Sulphonylureas: Mechanism of Action - Enables what process to occur even when glucose is not increased?
Glucose-independent insulin secretion
31
Sulphonylureas: Impact on weight
Increased by 1-2 kg
32
Sulphonylureas: Major risk of what?
Hypoglycaemia
33
Sulphonylureas: Gliclazide dose - Start and Maximum
Start - 40-80 mg once daily Maximum - 160mg twice daily
34
Sulphonylureas: Side Effects - Why may they cause hypoglycaemia?
As they are not glucose dependent
35
Sulphonylureas: Side Effects - Increased risk of Hypoglycaemia (4)
Increased age Increased diabetic diagnosis time Creatinine Lower HbA1c - <50 mmol/mol
36
Sulphonylureas: Side Effects - Why may weight increase?
Insulin is anabolic meaning carbohydrate stores increase and increases appetite
37
TZDs
Thiazolidinediones
38
Thiazolidinediones: Mechanism of Action
PPAR-gamma ligands to increase the transcription of target genes
39
Thiazolidinediones: Impact on adipocytes
Increase differentiation from pre-adipocytes to adipocytes to increase fat mass storage
40
Thiazolidinediones: How do they reduce lipotoxicity?
Increase subcutaneous fat mass to increase the uptake of FFA to remove it from the viscera
41
Thiazolidinediones: Lipid Steal Mechanism
FFA uptake removes fat from the liver, pancreas and muscle to reduce lipotoxicity
42
Thiazolidinediones: Impact on adiponectin
Increased adiponectin to increase insulin sensitivity in the liver
43
Thiazolidinediones: Reduces what inflammatory cytokines? (2)
TNF-alpha and IL-6 from macrophages
44
Thiazolidinediones: Characteristics - Impact on weight
Increase in weight
45
Thiazolidinediones: Characteristics - Which is the only available TZD?
Pioglitazone
46
Thiazolidinediones: Characteristics - Pioglitazone dose
15-30mg once daily
47
Thiazolidinediones: Side Effects - (3)
Weight gain Peripheral oedema Fracture risk
48
Thiazolidinediones: Side Effects - Why is fracture risk increased?
Fat accumulation in bone marrow and reduced bone density
49
Incretin Drugs: What is produced from K cells?
GIP
50
Incretin Drugs: What is produced from L cells?
GLP-1
51
Incretin Drugs: GIP and GLP-1 are broken down by what?
DPP-4
52
Incretin Drugs: Amplifying Pathway
GLP-1/GIP receptor activation increases cAMP to increase insulin secretion
53
Incretin Drugs: Triggering Pathway
Activation of Glucokinase by Glucose forms Glucose-6-Phosphate to increase ATP and thus calcium channel activation for insulin exocytosis
54
Gliptins: Examples (3)
Sitagliptin Alogliptin Saxagliptin
55
DPP4 Inhibitors
Dipeptidyl Peptidase 4 Inhibitors
56
DPP4 Inhibitors: Mechanism of Action
Inhibit the breakdown of GLP-1 and GIP by binding and inhibiting DPP4 to increase the incretin effect
57
DPP4 Inhibitors: These are insulin ...
Secretagogues
58
DPP4 Inhibitors: Why is there a reduced risk of hypoglycaemia?
Glucose dependent insulin secretion
59
DPP4 Inhibitors: Does this impact weight?
No
60
DPP4 Inhibitors: Sitagliptin dose
100mg once daily
61
GLP-1 Receptor Agonists: Structure
Modified GLP-1 structure to prevent breakdown by DPP4 to act directly on the receptor to increase insulin secretion in a glucose-dependent manner and inhibit glucagon secretion
62
GLP-1 Receptor Agonists: Example
Semaglutide
63
GLP-1 Receptor Agonists: Semaglutide structure
Addition of SNAC fatty acid group increases gastric absorption
64
GLP-1 Receptor Agonists: Mechanism of Action (4)
Promote insulin secretion in a glucose-dependent manner Inhibit glucagon secretion Acts on hypothalamus to reduce appetite Acts on intestines to reduce gastric emptying
65
GLP-1 Receptor Agonists: Do they impact weight?
Yes - reduce weight
66
GLP-1 Receptor Agonists: Impact on BP
Reduced
67
GLP-1 Receptor Agonists: Impact on HR
Increased
68
GLP-1 Receptor Agonists: Liraglutide dose
1.2 mg daily
69
GLP-1 Receptor Agonists: Semaglutide dose
0.5mg weekly
70
GLP-1 Receptor Agonists: Side effects (3)
Nausea or Vomiting - improves after 6 weeks Gallstones Pancreatitis
71
GLP-1 Receptor Agonists: Why is there a risk of Pancreatitis?
Sustained increase in pancreatic lipase and amylase
72
GLP-1 Receptor Agonists: Why may nausea and vomiting occur?
Early satiety with reduced gastric emptying
73
GLP-1 Receptor Agonists: May reduce the onset of what?
Macroalbuminuria
74
SGLT-2 Inhibitors: Examples (3)
Empagliflozin Dapagliflozin Canagliflozin
75
SGLT-2 Inhibitors: Mechanism of action
Inhibit the channel on the kidneys to increase uptake of sugar within the nephrons to increase urinary glucose loss
76
SGLT-2 Inhibitors: Direct Effects - Glucose loss results in osmotic ...
Diuresis
77
SGLT-2 Inhibitors: Direct Effects - Inhibition of SGLT-2 reduces the reabsorption of what?
Sodium
78
SGLT-2 Inhibitors: Direct Effects - Osmotic diuresis and reduced Na reabsorption causes what type of action?
Mild diuretic
79
SGLT-2 Inhibitors: Direct Effects - Impact on urate excretion?
Increased - to reduce plasma urate concentration
80
SGLT-2 Inhibitors: Direct Effects - How does it protect the kidneys? (3)
Increased sodium delivery to the DCT - increases uptake of Na at the macula densa Increases adenosine secretion - reduced renal afferent vasodilation Reduces filtration pressure
81
SGLT-2 Inhibitors: Indirect Effects - Impact on glucose
Reduced
82
SGLT-2 Inhibitors: Indirect Effects - Impact on lipolysis
Increased - increases FFA to the liver to increase Ketone Body production
83
SGLT-2 Inhibitors: Indirect Effects - How are cardiac bioenergetics improved?
FFA and Ketones increase
84
SGLT-2 Inhibitors: Indirect Effects - Increase the risk of what?
Ketosis and Ketoacidosis
85
SGLT-2 Inhibitors: Glucose-lowering effects relies on what?
Renal glucose filtration
86
SGLT-2 Inhibitors: Efficacy is reduced at an eGFR of what?
<90ml/min
87
SGLT-2 Inhibitors: Efficacy is 0 at an eGFR of what?
<45ml/min
88
SGLT-2 Inhibitors: Impact on blood pressure
Reduced
89
SGLT-2 Inhibitors: Impact on cholesterol
Increases LDL and HDL cholesterol
90
SGLT-2 Inhibitors: Dose of Empagliflozin
10mg once daily
91
SGLT-2 Inhibitors: Side effects (5)
Thrush - secondary to glycosuria Fournier Gangrene Hypovolaemia Hypotension Diabetic Ketoacidosis
92
SGLT-2 Inhibitors: When should these be omitted?
Prolonged fasting Acute illness

The Endocrine System (5 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions