Endocrine and Metabolic Drugs Flashcards
What class of drug is Insulin (NovoRapid, Levemir, Lantus, Humalog)?
Anti-diabetic medication
What class of drug is Metformin (Diabex)?
Anti-diabetic medication
What class of drug is Glibenclamide (Daonil, Glimel)?
Sulfonylurea anti-diabetic medication
What class of drug is Exenatide (Byetta, Bydureon)?
GLP-1 analogue
What class of drug is Risedronate (Actonel)?
Bisphosphonate
What class of drug is Raloxifene (Evista)?
Selective oestrogen receptor modulator
What class of drug is Denosumab (Prolia)?
RANK-L inhibitor
What class of drug is Disulfiram (Antabuse)?
Aldehyde dehydrogenase inhibitor
What class of drug is Thyroxine (Oroxine)?
Thyroid hormone
What class of drug is Liothyronine (Tertroxin)?
Thyroid hormone
What class of drug is Carbimazole (Neo-Mercazole)?
Anti-thyroid drug
What class of drug is Propylthiouracil (PTU)?
Anti-thyroid drug
What is the mechanism of action of Insulin (NovoRapid, Levemir, Lantus, Humalog)?
Increases or restores ability to metabolise glucose by enhancing cellular glucose uptake; inhibits endogenous glucose output and lipolysis
What is the mechanism of action of Metformin (Diabex)?
Acts on liver to decrease insulin resistance
Reduces hepatic glucose production; increases peripheral utilisation of glucose
What is the mechanism of action of Glibenclamide (Daonil, Glimel)?
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
What is the mechanism of action of Exenatide (Byetta, Bydureon)?
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
What is the mechanism of action of Risedronate (Actonel)?
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
What is the mechanism of action of Raloxifene (Evista)?
Oestrogen agonistic effects on bone mass and lipid; antagonistic effects at other oestrogen-receptive tissues, eg breast and endometrium
What is the mechanism of action of Denosumab (Prolia)?
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
What is the mechanism of action of Disulfiram (Antabuse)?
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
What is the mechanism of action of Thyroxine (Oroxine)?
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
What is the mechanism of action of Liothyronine (Tertroxin)?
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
What is the mechanism of action of Carbimazole (Neo-Mercazole)?
Inhibits thyroid peroxidase, which usually catalyses the addition of iodide to tyrosine during synthesis of thyroid hormones
What is the mechanism of action of Propylthiouracil (PTU)?
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
What are the side effects of Insulin (NovoRapid, Levemir, Lantus, Humalog)?
- Hypoglycaemia
- Weight gain
- Allergic reactions
Local reactions including erythema, itching, lipodystrophy, lipoatrophy
What are the side effects of Metformin (Diabex)?
- Malabsorption of vitamin B12
- Nausea
- Vomiting
- Anorexia
- Diarrhoea
What are the side effects of Glibenclamide (Daonil, Glimel)?
- Hypoglycaemia
- Weight gain
- Nausea
- Diarrhoea
- Metallic taste
- Headache
- Rash
What are the side effects of Exenatide (Byetta, Bydureon)?
- Headache
- Dizziness
- Feeling jittery
- Nausea and/or vomiting
- Diarrhoea
- Constipation
- Dyspepsia
- GORD
- Abdominal pain
- Hypoglycaemia
- Injection site reactions
- Taste disturbance
What are the side effects of Risedronate (Actonel)?
- Nausea
- Vomiting
- Diarrhoea
- Headache
- Hypocalcaemia
- Musculoskeletal pain
- Oesophagitis
- Oesophageal erosions and ulcers
- Gastritis
- Duodenitis
- Glossitis
- Rash
- Osteonecrosis of jaw
What are the side effects of Raloxifene (Evista)?
- Hot flushes
- Sweating
- Leg cramps
- Peripheral oedema
- Sleep disorders
- VTE (venous thromboembolism)
What are the side effects of Denosumab (Prolia)?
- Eczema
- Hypercholesterolaemia
- Musculoskeletal pain (in men)
- Cataracts
- Urinary retention
What are the side effects of Disulfiram (Antabuse)?
- Drowsiness
- Nausea
- Headache
- Fatigue
- Taste disturbance
What are the side effects of Thyroxine (Oroxine)?
- Tachycardia
- Arrhythmia
- Excitability
- Insomnia
- Flushing
- Sweating
- Diarrhoea
- Excessive weight loss
- Worsening ischaemic symptoms in those with IHD
Decreased bone density
What are the side effects of Liothyronine (Tertroxin)?
- Tachycardia
- Arrhythmia
- Excitability
- Insomnia
- Flushing
- Sweating
- Diarrhoea
- Excessive weight loss
- Worsening ischaemic symptoms in those with IHD
Decreased bone density
What are the side effects of Carbimazole (Neo-Mercazole)?
- Itching
- Rash
- Mild leukopenia
- Nausea
- Vomiting
- Gastric discomfort
- Headache
- Arthralgia
- Agranulocytosis
- Goitre
What are the side effects of Propylthiouracil (PTU)?
- Itching
- Rash
- Mild leukopenia
- Nausea
- Vomiting
- Gastric discomfort
- Headache
- Arthralgia
- Agranulocytosis
- Hepatotoxicity
Goitre
What are the indications for use of Insulin (NovoRapid, Levemir, Lantus, Humalog)?
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
What are the indications for use of Metformin (Diabex)?
Administration: oral tablet
- Type 2 diabetes in patients > 10 years
Contraindications:
Type 1 diabetes
What are the indications for use of Glibenclamide (Daonil, Glimel)?
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.
What are the indications for use of Exenatide (Byetta, Bydureon)?
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
What are the indications for use of Risedronate (Actonel)?
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
What are the indications for use of Raloxifene (Evista)?
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
What are the indications for use of Denosumab (Prolia)?
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
What are the indications for use of Disulfiram (Antabuse)?
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
What are the indications for use of Thyroxine (Oroxine)?
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
What are the indications for use of Liothyronine (Tertroxin)?
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
What are the indications for use of Carbimazole (Neo-Mercazole)?
Administration: oral tablet
- Graves’ disease
- Short-term treatment before thyroid surgery, or before and after radioactive iodine treatment
- Thyroid storm
Contraindications:
First trimester pregnancy
What are the indications for use of Propylthiouracil (PTU)?
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.
