Pharmacology of Hypertension Flashcards
(42 cards)
What are the 4 anti-hypertensive drug classes?
- ACEi (angiotensin converting enzyme inhibitors)
- Calcium channel blockers
- Thiazide or thiazide-like diuretics
- ARB (angiotensin receptor blockers)
What are some examples of ACEi?
Ramipril
Lisinopril
Perindopril
What is the primary mechanism of action of ACEi?
Inhibit the angiotensin converting enzyme
Prevent the conversion of angiotensin I to angiotensin II by ACE
What is the drug target site of ACEi?
ACE (angiotensin converting enzyme)
What are the main side effects of ACEi?
Cough
Hypotension
Hyperkalaemia (care with K+ supplements or K+ sparing diuretics)
Foetal Injury (AVOID IN PREGNANT WOMEN)
Renal failure (in patients with renal artery stenosis)
Urticaria / Angioedema (fluid buildup and swelling under the skin)
What is some extra information about ACEi?
Most ACEi (not lisinopril) are pro-drugs - require hepatic activation to generate active metabolites
eGFR and serum potassium must be regularly monitored when prescribing ACEi
Most trials indicate that ARBs are not as effective as ACEi
What are some examples of calcium channel blockers?
Amlodipine
Felodipine
What is the primary mechanism of action of calcium channel blockers?
Block L-type calcium channels – predominantly on vascular smooth muscle
Results in a decrease in calcium influx = inhibition of myosin light chain kinase and cross-bridge formation
Results in vasodilation = reduces peripheral resistance
What is the drug target site of calcium channel blockers?
L-type calcium channel
What are the main side effects of calcium channel blockers?
Ankle oedema
Constipation
Palpitations
Flushing/Headaches
What is some extra information about calcium channel blockers?
Dihydropyridine type calcium channel blockers demonstrate a higher degree of vascular selectivity
What are some examples of thiazide or thiazide-like diuretics?
Bendro-flumethiazide (thiazide)
Indapamide (thiazide-like)
What is the primary mechanism of action of thiazide or thiazide-like diuretics?
They block the Na+, Cl- co-transporter in the early DCT = Na+ and Cl- reabsorption is inhibited
Osmolarity of the tubular fluid increases = decreasing the osmotic gradient for water reabsorption in the collecting duct
What is the drug target site of thiazide or thiazide-like diuretics?
Sodium/chloride cotransporter
What are the main side effects of thiazide or thiazide-like diuretics?
Hypokalemia
Hyponatremia
Metabolic alkalosis (increased hydrogen ion excretion)
Hypercalcemia
Hyperglycemia (hyperpolarised pancreatic beta cells).
Hyperuricemia
What is some extra information about thiazide or thiazide-like diuretics?
Thiazide and thiazide-like diuretics both lose their diuretic effects within 1-2 weeks of treatment
Continuing anti-hypertensive action appears to be due to vasodilating properties (these are more pronounced for the thiazide-like diuretics)
What are some examples of ARB?
Losartan
Irbesartan
Candesartan
What is the primary mechanism of action of ARB?
Act as insurmountable (i.e. non-competitive) antagonists at AT1 receptors (found on kidneys and on the vasculature)
What is the drug target site of ARB?
Angiotensin receptor
What are the main side effects of ARB?
Hypotension
Hyperkalaemia (care with K+ supplements or K+ sparing diuretics)
Foetal Injury (AVOID IN PREGNANT WOMEN)
Renal failure (in patients with renal artery stenosis)
What is some extra information about ARB?
Most trials indicate that ARBs are not as effective as ACEi
Losartan and candesartan are pro-drugs = require hepatic activation to generate the active metabolites
Case Study: Mrs Turner
64F - Rheumatoid arthritis for 9 years, in the last year her mobility is severely restricted, in pain even at rest
Pre-op for arthroplasty (replacement) revealed: BP = 149/93mmHg
GP measures 147/92mmHg and 145/91mmHg on 2 different occasions.
She is offered ambulatory blood pressure monitoring by her GP. Apart from RA pain, Mrs Turner feels well, although she does smoke (< 10 per day). She is 167cm and 85kg.
What is the patient’s problem?
BMI = 30.4
Pain from RA
Hypertension
What is a q-risk score?
What are the 5 biggest risk factors for cardiovascular-related events?
Large database from which the algorithm can find your risk for cardiovascular related diseases / conditions e.g. strokes, MIs, CVD
Hypertension Hypercholsterolaemia Family history Diabetes Smoking
What is Mrs Turner’s calculated q-risk score?
14.9