Endocrine and Metabolic Drugs

Question 1

What class of drug is Insulin (NovoRapid, Levemir, Lantus, Humalog)?

Answer 1

Anti-diabetic medication

Question 2

What class of drug is Metformin (Diabex)?

Answer 2

Anti-diabetic medication

Question 3

What class of drug is Glibenclamide (Daonil, Glimel)?

Answer 3

Sulfonylurea anti-diabetic medication

Question 4

What class of drug is Exenatide (Byetta, Bydureon)?

Answer 4

GLP-1 analogue

Question 5

What class of drug is Risedronate (Actonel)?

Answer 5

Bisphosphonate

Question 6

What class of drug is Raloxifene (Evista)?

Answer 6

Selective oestrogen receptor modulator

Question 7

What class of drug is Denosumab (Prolia)?

Answer 7

RANK-L inhibitor

Question 8

What class of drug is Disulfiram (Antabuse)?

Answer 8

Aldehyde dehydrogenase inhibitor

Question 9

What class of drug is Thyroxine (Oroxine)?

Answer 9

Thyroid hormone

Question 10

What class of drug is Liothyronine (Tertroxin)?

Answer 10

Thyroid hormone

Question 11

What class of drug is Carbimazole (Neo-Mercazole)?

Answer 11

Anti-thyroid drug

Question 12

What class of drug is Propylthiouracil (PTU)?

Answer 12

Anti-thyroid drug

Question 13

What is the mechanism of action of Insulin (NovoRapid, Levemir, Lantus, Humalog)?

Answer 13

Increases or restores ability to metabolise glucose by enhancing cellular glucose uptake; inhibits endogenous glucose output and lipolysis

Question 14

What is the mechanism of action of Metformin (Diabex)?

Answer 14

Acts on liver to decrease insulin resistance

Reduces hepatic glucose production; increases peripheral utilisation of glucose

Question 15

What is the mechanism of action of Glibenclamide (Daonil, Glimel)?

Answer 15

Stimulates insulin secretion by binding to and blocking KATP channels on pancreatic β cells, thereby leading to depolarisation and exocytosis of insulin granules into the circulation

May also decrease insulin resistance

Question 16

What is the mechanism of action of Exenatide (Byetta, Bydureon)?

Answer 16

Analogues of glucagon-like peptide-1 (an incretin); increase glucose-dependent insulin secretion and suppress inappropriate glucagon secretion

They also delay gastric emptying, which slows glucose absorption, and decrease appetite

Question 17

What is the mechanism of action of Risedronate (Actonel)?

Answer 17

Decreases bone resorption by inhibiting osteoclasts

BPs are resorbed into bone matrix as bone mineralises

Bisphosphonates are toxic to osteoclasts when they are attempting to resorb bone

Question 18

What is the mechanism of action of Raloxifene (Evista)?

Answer 18

Oestrogen agonistic effects on bone mass and lipid; antagonistic effects at other oestrogen-receptive tissues, eg breast and endometrium

Question 19

What is the mechanism of action of Denosumab (Prolia)?

Answer 19

Human monoclonal antibody that binds receptor activator of nuclear factor-kappa B ligand (RANKL) preventing activation of the RANK receptor, resulting in decreased formation and activity of osteoclasts, thus reducing bone resorption

Question 20

What is the mechanism of action of Disulfiram (Antabuse)?

Answer 20

Deters alcohol use

Disulfiram prevents the usual metabolism of alcohol (irreversibly inhibits aldehyde dehydrogenase), blocking acetaldehyde breakdown, which causes unpleasant, potentially serious effects if alcohol is consumed:

e.g. flushing, sweating, nausea, vomiting, palpitations, headache, dyspnoea, chest pain, hypotension, cardiovascular collapse, seizures, arrhythmias

Question 21

What is the mechanism of action of Thyroxine (Oroxine)?

Answer 21

Thyroxine is the thyroid hormone T₄. It is converted to T₃, which is much more potent

However, T₄ is administered in preference to T₃ for hypothyroidism because it has a longer half-life and its levels better approximate TSH levels

Question 22

What is the mechanism of action of Liothyronine (Tertroxin)?

Answer 22

Liothyronine is also known as T₃ or tri-iodothyronine

It is administered in cases of severe hypothyroidism and myoedema coma because it is more active than T₄ and acts more rapidly

Question 23

What is the mechanism of action of Carbimazole (Neo-Mercazole)?

Answer 23

Inhibits thyroid peroxidase, which usually catalyses the addition of iodide to tyrosine during synthesis of thyroid hormones

Question 24

What is the mechanism of action of Propylthiouracil (PTU)?

Answer 24

Inhibits thyroid peroxidase, which usually catalyses the addition of iodide to tyrosine during synthesis of thyroid hormones

Also inhibits the conversion of T₄ to T₃

Question 25

What are the side effects of Insulin (NovoRapid, Levemir, Lantus, Humalog)?

Answer 25

* Hypoglycaemia * Weight gain * Allergic reactions Local reactions including erythema, itching, lipodystrophy, lipoatrophy

Question 26

What are the side effects of Metformin (Diabex)?

Answer 26

* Malabsorption of vitamin B12 * Nausea * Vomiting * Anorexia * Diarrhoea

Question 27

What are the side effects of Glibenclamide (Daonil, Glimel)?

Answer 27

* Hypoglycaemia * Weight gain * Nausea * Diarrhoea * Metallic taste * Headache * Rash

Question 28

What are the side effects of Exenatide (Byetta, Bydureon)?

Answer 28

* Headache * Dizziness * Feeling jittery * Nausea and/or vomiting * Diarrhoea * Constipation * Dyspepsia * GORD * Abdominal pain * Hypoglycaemia * Injection site reactions * Taste disturbance

Question 29

What are the side effects of Risedronate (Actonel)?

Answer 29

* Nausea * Vomiting * Diarrhoea * Headache * Hypocalcaemia * Musculoskeletal pain * Oesophagitis * Oesophageal erosions and ulcers * Gastritis * Duodenitis * Glossitis * Rash * Osteonecrosis of jaw

Question 30

What are the side effects of Raloxifene (Evista)?

Answer 30

* Hot flushes * Sweating * Leg cramps * Peripheral oedema * Sleep disorders * VTE (venous thromboembolism)

Question 31

What are the side effects of Denosumab (Prolia)?

Answer 31

* Eczema * Hypercholesterolaemia * Musculoskeletal pain (in men) * Cataracts * Urinary retention

Question 32

What are the side effects of Disulfiram (Antabuse)?

Answer 32

* Drowsiness * Nausea * Headache * Fatigue * Taste disturbance

Question 33

What are the side effects of Thyroxine (Oroxine)?

Answer 33

* Tachycardia * Arrhythmia * Excitability * Insomnia * Flushing * Sweating * Diarrhoea * Excessive weight loss * Worsening ischaemic symptoms in those with IHD Decreased bone density

Question 34

What are the side effects of Liothyronine (Tertroxin)?

Answer 34

* Tachycardia * Arrhythmia * Excitability * Insomnia * Flushing * Sweating * Diarrhoea * Excessive weight loss * Worsening ischaemic symptoms in those with IHD Decreased bone density

Question 35

What are the side effects of Carbimazole (Neo-Mercazole)?

Answer 35

* Itching * Rash * Mild leukopenia * Nausea * Vomiting * Gastric discomfort * Headache * Arthralgia * Agranulocytosis * Goitre

Question 36

What are the side effects of Propylthiouracil (PTU)?

Answer 36

* Itching * Rash * Mild leukopenia * Nausea * Vomiting * Gastric discomfort * Headache * Arthralgia * Agranulocytosis * Hepatotoxicity Goitre

Question 37

What are the indications for use of Insulin (NovoRapid, Levemir, Lantus, Humalog)?

Answer 37

Administration: usually subcutaneous injection, but IV during acute care * Type 1 diabetes * Type 2 diabetes inadequately controlled with diet, exercise and oral anti-diabetic drugs

Question 38

What are the indications for use of Metformin (Diabex)?

Answer 38

Administration: oral tablet * Type 2 diabetes in patients \> 10 years Contraindications: Type 1 diabetes

Question 39

What are the indications for use of Glibenclamide (Daonil, Glimel)?

Answer 39

Administration: oral tablet * Type 2 diabetes Contraindications: Hepatic impairment Elderly patients Renal impairment Ketoacidosis Type 1 DM Acute illness May be administered in fixed-dose combination with metformin (Glucovance). Should be taken with food to minimise risk of hypoglycaemia.

Question 40

What are the indications for use of Exenatide (Byetta, Bydureon)?

Answer 40

Administration: SC injection * Type 2 diabetes with metformin and/or a sulfonylurea, when these are inadequate * Type 2 diabetes with metformin and a basal insulin, when these are inadequate Contraindications: Treatment with insulin Severe GI disease History of pancreatitis with a GLP-1 analogue Pregnancy

Question 41

What are the indications for use of Risedronate (Actonel)?

Answer 41

Administration: oral tablet * Paget’s disease * Prevention and treatment of osteoporosis (including postmenopausal and corticosteroid-induced) Contraindications: Immobile patients Oesophageal disorders Upper GI conditions (e.g. dysphagia, gastritis) Hypocalcaemia Pregnancy

Question 42

What are the indications for use of Raloxifene (Evista)?

Answer 42

Administration: oral tablet * Prevention and treatment of postmenopausal osteoporosis * Primary prevention of invasive breast cancer in high-risk postmenopausal women Contraindications: Patients with previous venous thromboembolism or at high risk of VTE (venous thromboembolism) History of breast cancer Before surgery Pregnancy

Question 43

What are the indications for use of Denosumab (Prolia)?

Answer 43

Administration: injection * Treatment of postmenopausal osteoporosis * Increase bone mineral density in men with osteopenia or osteoporosis * Prevention of skeletal-related events due to bone metastases from solid tumours * Giant cell tumour of bone Contraindications: Hypocalcaemia Pregnancy

Question 44

What are the indications for use of Disulfiram (Antabuse)?

Answer 44

Administration: oral tablet * Maintenance of abstinence in alcohol dependence Contraindications: Ischaemic heart disease Psychosis Severe myocardial disease Severe renal disease Severe hepatic disease Pregnancy Breastfeeding

Question 45

What are the indications for use of Thyroxine (Oroxine)?

Answer 45

Administration: oral tablet * Hypothyroidism * Block-replacement regimen in hyperthyroidism * Suppressive regimen in thyroid cancer and euthyroid goitre Contraindications: Untreated hyperthyroidism Hypopituitarism and adrenal insufficiency Cardiovascular disorders Diabetes

Question 46

What are the indications for use of Liothyronine (Tertroxin)?

Answer 46

Administration: oral tablet, IV * Severe hypothyroidism, such as myxoedema coma * Thyroid cancer (may be used to shorten the period of symptomatic hypothyroidism due to thyroxine withdrawal before or after thyroid scanning during long-term follow up) Contraindications: Untreated hyperthyroidism Hypopituitarism and adrenal insufficiency Cardiovascular disorders Diabetes

Question 47

What are the indications for use of Carbimazole (Neo-Mercazole)?

Answer 47

Administration: oral tablet * Graves’ disease * Short-term treatment before thyroid surgery, or before and after radioactive iodine treatment * Thyroid storm Contraindications: First trimester pregnancy

Question 48

What are the indications for use of Propylthiouracil (PTU)?

Answer 48

Administration: oral tablet * Graves’ disease * Short-term treatment before thyroid surgery, or before and after radioactive iodine treatment * Thyroid storm Must be dosed more frequently than carbimazole.