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Flashcards in Endocrine Drugs Deck (38)
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1
Q

What are the 3 main classes of drugs used to treat type 2 diabetes?

Give an example of each.

A

Biguanides (e.g. metformin)
Sulphonylureas (e.g. gliclazide)
GLP1 agonist (e.g. liraglutide)

2
Q

Describe the mechanism of action of metformin. (2)

What sort of drug is this?

A

Biguanide

  1. Increases the activity of AMP-dependent protein kinase (AMPK)
    a. This inhibits gluconeogenesis
  2. Also reduces insulin resistance
3
Q

List 2 indications for metformin.

A

Type 2 diabetes mellitus

Metabolic/reproductive abnormalities in PCOS

4
Q

List 7 side effects of metformin.

Which important side effect is NOT caused by metformin?

A
Diarrhoea
Weight loss
Nausea
Vomiting
Taste disturbances
Lack of appetite 
Lactic acidosis (in renal failure)

NOT CAUSED BY METFORMIN:
Hypoglycaemia

5
Q

Describe the important pharmacokinetics/dynamics of metformin. (3)

What would you tell the patient when prescribing metformin? (3)

A
PHARMA:
Avoid in:
-Pregnancy
-Renal failure (GFR <30ml/min)
Absorption reduced when taken with food 

PATIENT INFO:
Take at the same time everyday
Avoid alcohol
Will cause weight loss

6
Q

Give 2 examples of sulphonylureas.

List 1 indication for prescribing them.

A

Gliclazide
Glimepride

T2DM

7
Q

Describe the mechanism of action of sulphonylureas. (2)

A
  1. Stimulates beta cells in the pancreas to produce more insulin
  2. Increases cellular glucose uptake and glycogenesis
    a. Also reduces gluconeogenesis
8
Q

List 7 side effects of sulphonylureas.

A
Hypoglycaemia
Rashes
Nausea
Vomiting
Stomach pain
Indigestion
Weight gain
9
Q

Describe the important pharmacokinetics/dyanmics of sulphonylureas. (2)

What would you tell the patient when prescribing them? (3)

A

PHARMA:
Renal excretion - accumulate in renal failure
Gliclazide - short acting
Glimepride - long acting

PATIENT INFO:
Compliance is important
Maintain consistent diet
Avoid alcohol

10
Q

Give 2 examples of GLP1 (glucagon like peptide) agonists.

List 1 indication for prescribing them.

A

Exanatide
Liraglutide

T2DM

11
Q

Describe the mechanism of action of GLP1 agonists. (3)

A
  1. GLP1 is a hormone release after meals to increase insulin secretion
  2. GLP1 agonists mimic this, causing increase insulin secretion
  3. Also causes decreased glucagon secretion and reduces hunger
12
Q

List 4 side effects of GLP1 agonists.

A

Hypoglycaemia
Nausea
Vomiting
Diarrhoea

13
Q

Describe the important pharmacokinetics/dynamics of GLP1 agonists. (2)

What would you tell the patients when prescribing them? (2)

A

PHARMA:
Improves glucose control when given with metformin, SUs and/or insulin
Renal excretion - dose adjustment needed in renal failure

PATIENT INFO:
Only given as injections
Twice a day

14
Q

Apart from metformin, SUs and GLP1 agonists, which 6 other drugs can be used to treat T2DM?

Give an example of each.

A

Thiazolidinedione (TZDs), e.g. pioglitazone

DDP4 inhibitors, e.g. sitagliptin

Insulin, e.g. Novorapid

Sulphonylurea receptor binder, e.g. glibenclamide

Alpha glucosidase inhibitors, e.g. acarbose

SGLUT2 inhibitors, e.g. empagliflozin

15
Q

How do you treat hypothyroidism?

What type of drug is this?

A

Levothyroxine

Synthetic thyroid hormone

16
Q

Describe the mechanism of action of thyroxine. (4)

A
  1. Thyroxine (T4) increases the metabolic rate of all tissues in the body
  2. Levothyroxine is a synthetically prepared levo-isomer of thyroxine
  3. Levothyroxine acts like T4
    a. Converted into T3 in the liver and kidneys
  4. T3 maintains brain function, food metabolism and body temperature
17
Q

List 2 indications for levothyroxine.

A

Hypothyroidism

Chronic lymphocytic thyroiditis

18
Q

List 6 side effects of levothyroxine.

A
Chest pain
Coma
Diarrhoea
Tachycardia
Itching
Muscle cramps

NOTE: very uncommon is dosing is good

19
Q

Describe the important pharmacokinetics/dynamics of levothyroxine. (3)

What would you tell the patient when prescribing this? (1)

A

PHARMA:
Renal clearance
IV formulation is available
Long half life (6-7 days) therefore TFTs should be rechecked 6 weeks after dose adjustment

PATIENT INFO:
Take 30-60 mins before breakfast

20
Q

How would you treat hyperthyroidism?

Give 2 examples of this drug class.

A

Thionamides

Carbimazole
Propylthiouracil

21
Q

Describe the mechanism of action of thionamides. (3)

A
  1. Reduce activity of peroxidase enzyme
    a. Therefore inhibits thyroid hormone formation
  2. May also reduce peripheral conversion of T4 to T3
  3. Carbimazole is a pro-drug
22
Q

List 3 indications for thionamides.

A

Hyperthyroidism
Thyrotoxicosis
Preparing patients for thyroid surgery

23
Q

List 3 side effects of thionamides.

A

Rash
Agranulocytosis
Sore throat

24
Q

Describe the important pharmacokinetics/dyanmics of thionamides. (3)

What would you tell the patient when prescribing them? (2)

A

PHARMA:
Carbimazole metabolised to thiamazole within 1 hour
Thiamazole crosses the placenta and can be found in breast milk
Usually prescribed with a beta blocker to reduce symptoms

PATIENT INFO:
Compliance is important
Regular blood checks needed for treatment response, LFTs, U&Es and FBCs

25
Q

Which class of drug is used to treat osteoporosis?

Give 2 examples.

A

Bisphosphates

Alendronate (alendronic acid)
Ibandronate

26
Q

Describe the mechanism of action of bisphosphates. (2)

A
  1. Inhibit osteoclast bone resorption

2. No effect on bone formation

27
Q

List 3 indications for bisphosphates.

A

Post-menopausal osteoporosis
Reducing risk of vertebral and hip fractures
Paget’s disease of bone

28
Q

List 5 side effects of bisphosphates.

A
Abdominal pain
Dyspepsia
Acid regurgitation
Dysphagia
Headache
29
Q

Describe the important pharmacokinetics/dynamics of bisphosphates. (1)

What would you tell the patient when prescribing them? (2)

A

PHARMA:
Bioavailability reduced by coffee/orange juice

PATIENT INFO:
Take 30 minutes before food
Avoid caffeine

30
Q

Give 2 examples of the OCP.

What kinds of pill are they?

A

Microgynon (combined)

Cerazette (progesterone only)

31
Q

Describe the mechanism of action of the OCP. (4)

A
  1. OCP can be combined or progesterone-only
  2. OCP acts on the female reproductive tract, the mammary glands, hypothalamus and pituitary gland
  3. OCP reduces production of gonadotrophin releasing hormone (GnRH)
  4. This prevents the LH surge, therefore prevents ovulation
32
Q

List 3 indications for the OCP.

A

Contraception
Menopausal and postmenopausal disorders
PCOS

33
Q

List 5 side effects of the OCP.

A
Mood swings
Headache
Breast tenderness
Increased risk of breast/varian cancer
Increased risk of venous thromboembolism
34
Q

Describe the important pharmacokinetics/dynamics of the OCP. (1)

What would you tell the patient when prescribing it? (3)

A

PHARMA:
Antibiotics and St John’s Wort can reduce efficacy

PATIENT INFO:
Take at the same time every day
Take with food
Use alternative forms of contraception when taking antibiotics/enzyme inducers

35
Q

Describe the mechanism of action of thiazolidinediones (TZDs). (3)

What are they used for?

A

T2DM

  1. PPAR gamma agonist
  2. Acts as a transcription factor and stimulates genes involved in triglyceride storage in adipose tissue
    a. This prevents inappropriate fat deposition
    b. Therefore improves insulin sensitivity
  3. Decreases adipokine production
    a. Therefore improves insulin sensitivity
36
Q

List 4 side effects of DPP4 antagonists.

A

GI upset
Rash
Flu-like symptoms
Pancreatitis

37
Q

Describe the mechanism of action of SGLUT2 inhibitors.

What are they used for?

A

T2DM

  1. Inhibit glucose reabsorption in kidneys
  2. Increased excretion of glucose in urine
38
Q

List 4 side effects of SGLUT2 inhibitors.

A

UTIs
Acute kidney injury
DKA
Acute pancreatitis