Antihypertensives Flashcards
Name 4 first line treatments for hypertension
- ACE-Inhibitors, AT I Blockers
- Beta blockers
- Calcium channel blockers
- Diuretics (Thiazides)
Name 3 second line treatments for hypertension
- Alpha blockers
- Mineralocorticoid receptor antagonists
- Hydralazine
Name 2 ACE-I and give their suffix
Lisinopril, enalopril, captopril
Suffix is pril
Give 2 MOA of ACE-I
Overall decrease in BP by:
1. Inhibiting conversion of Ang I to Ang II (causing decreased vasoconstriction and aldosterone)
2. Inhibiting breakdown of bradykinin (causing increase in NO and PG thus increasing vasodilation)
Give 4 clinical uses of ACE-I
- Hypertension
- Cardiac failure
- Renal insufficiency
- Following myocardial infarction
Give 5 ADRs of ACE-I
- Severe hypotension
- Hyperkalemia
- Acute renal failure
- Dry cough
- Angioedema
How does ACE-I cause dry cough?
Increased accumulation of bradykinin and PG which is postulated to increase sensitivity of bradykinin-dependent airway sensory nerve fibres
How does ACE-I cause angioedema?
Increased PG and NO production causes inflammatory like responses like vasodilation, thus causing extravasation of plasma fluid into interstitial space
ACE-I is contraindicated in
Pregnancy (due to increase risk of fatal renal failure)
Name 2 AT1 blockers and give their suffix
- Losartan, Valsartan, Candesartan, Irbesartan, Telmisartan
- suffix is -sartan
MOA of Angiotensin II Type 1 blockers
Directly binds to Ang II Type 1 receptors, which prevents the binding of Ang II, thus decreasing Ang II effects, eventually lowers BP (similar to ACE-Is)
Which side effect of ACE-I is reduced with AT 1 blocker and why?
Reduced dry cough / productive cough.
AT 1 blocker does not interfere with breakdown of bradykinin
Name 3 non-selective beta blockers
- Propanolol
- Pindolol
- Carvedilol
A non-selective beta blocker that can be used to treat both hypertension and heart failure
Carvedilol
Name 3 cardioselective beta 1 blockers
- Atenolol
- Bisoprolol
- Metoprolol XL / metoprolol succinate
Name 2 cardioselective beta 1 blockers that can be used to treat both hypertension and heart failure
Bisoprolol and metoprolol XL
Name a 3rd generation / mixed beta blocker
Nebivolol
Give 2 MOA / features of nebivolol
- Dose dependent selectivity: cardioselective at low doses, but non-selective at high doses
- Vasodilation effect due to NO release
Give 5 clinical uses of beta blockers
- Hypertension
- Cardiac failure
- Arrythmias
- Following myocardial infarction
- Anxiety disorders
Give 6 ADRs of beta blockers
- Hypotension
- Bradycardia
- Bronchoconstriction especially in asthmatics
- AV nodal block
- Decreased exercise capacity
- CNS Effects: vivid dreams, CNS depressant (beta-blocker blues)
Name the 2 types of beta blocker blockades
- beta 1 blockade
- beta 2 blockade
How does beta 1 blockade result in decreased cardiac contraction?
Inhibits activation of adenylyl cyclase, thus inhibiting cAMP production, causing inhibition of PKA, thus inhibiting CICR, decreasing formation of Ca-calmodulin complex, decrease activation of MLCK, inhibit actvation of myosin LC, thus decrease contraction
How does beta 2 blockade cause bronchoconstriction / smooth muscle contraction
Inhibit cAMP production, thus inhibiting phosphorylation of MLCK, decrease bronchodilation, thus increase bronchoconstriction
Which part of the nephron do thiazides work at?
Distal convoluted tubule
MOA of thiazides
Inhibits Na+Cl- reabsorption by blocking the apical Na+ Cl- cotransporter of the DCT cells, leading to increased activity of the basolateral Na+ Ca2+ exchanger, thus enhancing calcium reabsorption
Name 2 thiazides
- Hydrochlorothiazide
- Indapamide
Name a class of drugs that interferes with thiazide action and explain why
NSAIDs
Action of thiazides depend on renal PG synthesis. NSAIDs reduce PG synthesis, thus interfere with thiazide action
Name 4 clinical uses for thiazides
- Hypertension
- Congestive heart failure
- Nephrolithiasis due to idiopathic hypercalciuria
- Nephrogenic diabetes insipidus
Name 6 ADRs of thiazides
- Hypokalemia metabolic alkalosis
- Hyponatremia
- Hyperglycemia
- Hyperlipidemia
- Hyperuricemia
- Hypercalcemia
Name 3 alpha-1 adrenergic antagonists and state their suffix
- Prazosin
- Alfuzosin
- Terazosin
Suffix: -zosin
MOA of alpha 1 adrenergic antagonists
Antagonises / reduces alpha 1 mediated vasoconstriction effect, which keeps vessels dilated, thus increasing TPR which lowers BP
Alpha-1 antagonists are safe to use in 2 kinds of patients
- Renal impairment: No effect on renal blood flow and GFR
- Pregnant patients: No known teratogenicity
Name 3 common early ADRs of alpha-1 antagonists
- Reflex tachycardia
- Palpitations
- Orthostatic hypotension
Name 3 other ADRs of alpha-1 antagonists
- Depression
- Urinary frequency
- Flushing
