Drugs Flashcards
(46 cards)
What is the primary indication for SGLT2 inhibitors?
SGLT2 inhibitors are primarily used for the management of type 2 diabetes mellitus. They can also be used to reduce the risk of cardiovascular events in people with diabetes and chronic kidney disease.
Name a common SGLT2 inhibitor medication.
Dapagliflozin, Empagliflozin and canagliflozin are commonly prescribed SGLT2 inhibitors.
What is the mechanism of action of SGLT2 inhibitors?
SGLT2 inhibitors work by inhibiting the sodium-glucose cotransporter 2 (SGLT2) in the proximal renal tubule. This reduces glucose reabsorption, leading to increased glucose excretion in urine and a lowering of blood glucose levels.
What are the common adverse effects of SGLT2 inhibitors?
Common adverse effects include urinary tract infections (UTIs), genital mycotic infections, and polyuria (increased urination). There is also a risk of dehydration, hypotension, and electrolyte imbalances.
What is a rare but serious side effect of SGLT2 inhibitors?
A rare but serious side effect of SGLT2 inhibitors is diabetic ketoacidosis (DKA), which can occur even when blood glucose levels are not significantly elevated.
Can SGLT2 inhibitors be used in patients with type 1 diabetes?
No, SGLT2 inhibitors are not recommended for patients with type 1 diabetes due to the increased risk of diabetic ketoacidosis (DKA).
How do SGLT2 inhibitors benefit patients with chronic kidney disease (CKD)?
Reducing Proteinuria: SGLT2 inhibitors help reduce albuminuria (protein in the urine), which is a key marker of kidney damage. Proteinuria is a strong predictor of disease progression in CKD. By lowering protein levels in the urine, SGLT2 inhibitors help protect the kidneys from further damage.
Slowing the Progression of CKD: SGLT2 inhibitors have been shown to slow the decline of kidney function in patients with CKD, particularly those with diabetic nephropathy.
Cardiovascular Benefits: SGLT2 inhibitors have shown cardiovascular protective effects. They help reduce the risk of heart failure, stroke, myocardial infarction (heart attack), and death in patients with CKD and/or diabetes. Since cardiovascular disease is common in CKD patients, this dual benefit is important.
Reducing Blood Pressure: SGLT2 inhibitors also lower blood pressure, which is helpful in managing CKD because high blood pressure is a common contributor to kidney damage and CKD progression. Their ability to lower blood pressure, along with improving kidney function, provides added benefit in managing CKD.
Should SGLT2 inhibitors be used in patients with severe renal impairment?
No, SGLT2 inhibitors are contraindicated in patients with severe renal impairment (eGFR < 30 mL/min/1.73m²) as they are less effective and may increase the risk of adverse effects such as dehydration and acute kidney injury.
Can SGLT2 inhibitors be used in patients who are pregnant or breastfeeding?
No, SGLT2 inhibitors are contraindicated during pregnancy and breastfeeding due to potential risks to the foetus or infant.
How should SGLT2 inhibitors be taken?
SGLT2 inhibitors are typically taken once daily, with or without food. The dose is usually taken in the morning.
What is the impact of SGLT2 inhibitors on body weight?
SGLT2 inhibitors can lead to modest weight loss due to the excretion of glucose in urine, which reduces calorie absorption.
Name eGFR ranges for SGLT2.
Dapagliflozin - Avoid initiation if eGFR less than 15 mL/minute/1.73 m2.
When used for Type 2 diabetes mellitus:
Consider additional antidiabetic drugs with dapagliflozin if eGFR less than 45 mL/minute/1.73 m2 (reduced efficacy).
Empagliflozin - Avoid initiation if eGFR less than 20 mL/minute/1.73 m2.
When used for Type 2 diabetes mellitus:
Limit dose to 10 mg once daily if eGFR less than 60 mL/minute/1.73 m2. Consider addition of other hypoglycemic agents if eGFR less than 45 mL/minute/1.73 m2 (reduced efficacy).
Canagliflozin - not licensed in CKD. Caution if eGFR less than 60 mL/minute/1.73 m2.
Avoid initiation when baseline eGFR less than 30 mL/minute/1.73 m2.
Limit dose to 100 mg once daily when eGFR less than 60 mL/minute/1.73 m2; consider addition of other hypoglycaemic agents if further glycaemic control needed. If eGFR falls to less than 30 mL/minute/1.73 m2 during treatment, continue with 100 mg once daily. See Prescribing in renal impairment.
What is vasopressin and what receptors does it act on?
Vasopressin (antidiuretic hormone) is a natural hormone that acts on V1 (vasoconstriction) and V2 (renal water reabsorption) receptors.
What are the clinical uses of vasopressin?
Diabetes insipidus, vasodilatory shock, and sometimes variceal bleeding.
What are the key side effects of vasopressin?
Hyponatraemia, vasoconstriction, headache, hypertension, and ischaemia in high doses.
How does desmopressin differ from vasopressin?
Desmopressin is a synthetic analogue of vasopressin with selective V2 agonism, minimal vasopressor activity.
What are the main indications for desmopressin?
Central diabetes insipidus
Nocturnal enuresis
Mild/moderate haemophilia A & von Willebrand disease (stimulates factor VIII and vWF release)
What are the side effects of desmopressin?
Hyponatraemia (due to water retention), headache, nausea, facial flushing, and seizures (if severe hyponatraemia develops).
What is an important counselling point for desmopressin in enuresis?
Limit fluid intake from 1 hour before dose to 8 hours after to avoid water intoxication and hyponatraemia.
What is demeclocycline and how is it used in SIADH?
A tetracycline antibiotic that causes nephrogenic diabetes insipidus, reducing renal response to ADH → used off-label in SIADH.
What are major side effects of demeclocycline?
Nephrotoxicity
Photosensitivity
Nausea/diarrhoea
Tooth discolouration (esp. in children)
What is the mechanism of action of terlipressin?
It is a vasopressin analogue with strong V1 receptor agonist activity → causes splanchnic vasoconstriction.
What monitoring is needed with terlipressin?
Watch for ischaemia, bradycardia, and hyponatraemia; monitor renal function and electrolytes.
What is a contraindication to terlipressin use?
Severe ischaemic heart disease or peripheral vascular disease, due to vasoconstriction risk.
