AntiHypertensives Flashcards
MOA of Thiazide Diuretics
- increase the excretion of Na+ and water by blocking Na+ reabsorption
- decreases blood volume and arterial resistance
- # 1 drug choice in most cases
- for HTN or edema
Hydrochlorothiazide
- aka HCTZ, thiazide diuretic
- blocks Na+ reabsorption in early segment of distal convoluted tubule
- PO only
Chlorthalidone
- thiazide diuretic
- 1.5-2 times more potent as HCTZ
- PO only
Adverse effects of thiazide diuretics
- hyponatremia/dehydration
- hypokalemia
- hyperuricemia
- hyperglycemia
- hyperlipidemia
- photosensitivity
- contraindicated if sulfa-allergy or CKD
MOA of Loop Diuretics
- inhibit co-transport of Na+/K+/2Cl- –> increases Na+ and K+ excretion
- more diuresis than thiazides, shorter duration
- for HTN or edema
Furosemide
- Loop Diuretic
- most freq. prescribed of this class
- prevents passive reabsorption of water –> profound diuresis
- PO or IV
Bumetanide
- Loop diuretic
- more potent than Furosemide
- PO or IV
Adverse Effects of Loop Diuretics
- Orthostatic hypotension
- electrolyte imbalance (hyponatremia, dehydration)
- hypokalemia
- hyperuricemia
- hyperglycemia
- hyperlipidemia
- photosensitivity
- ototoxicity ( esp. in IV route)
- contraindicated if sulfa-allergy
MoA of Potassium sparing diuretics
- less potent than thiazides and loop diuretics
- provide modest increase in urine production with less potassium excretion
- meds often coupled with HCTZ
- for HTN or edema
Amiloride
- Potassium Sparing diuretic
- MoA: directly blocks Na+/K+ pump; prevents Na+ reabsorption and K+ secretion in collecting tubule
- PO only
Triamtrene
- Potassium Sparing diuretic
- directly blocks Na+/K+ pump
- mild diuresis; excretes Na+, prevents secretion of K+
- PO only
Spironolactone or Eplerenone
- Potassium sparing Diuretics
- aldosterone antagonist to work in collecting duct –> Na+ excretion, K+ reabsorption
- PO only
Adverse Effects of potassium sparing diuretics
- hyperkalemia (esp if in combo with ACE, ARB, or K+ supplement)
- contraindicated in patients with CKD or hyperkalemia
Adverse effects specific to spironolactone
- gynecomastia in males
- abnormal vaginal bleeding
- BBW: tumorigenic
MoA of ACE Inhibitors
- inhibit angiotensin I converting enzyme –> block formation of angiotensin II –> decreased angiotensin II levels
- inhibit bradykinin degradation –> increased bradykinin levels in lung (cough)
Enalapril or Lisinopril
- ACE inhibitors
- Enalapril –> PO or IV
- Lisinopril –> PO
Adverse Effects of ACE inhibitors
- BBW: injury/death to developing fetus
- first dose hypotension (abrupt drop of angiotensin II
- dry cough (bronchial/laryngeal irritation)
- Hyperkalemia
- Angioedema (increased permeability of capillaries, esp if IV)
Indications of ACE inhibitors
- HTN
- MI
- prevention of MI, stroke, and death in patients at high risk of CVD
- CHF
MoA of ARBs
- bind to angiotensin II receptor subtype –> block action of angiotensin II
- relaxes smooth muscle and promotes vasodilation
- decreases aldosterone release and increases renal Na+/water excretion
- alternate to ACEs
Losartan or Valsartan
- ARBs
- both PO only
- Losartan 1st choice for this class
- higher cost, reserved for patients who develop cough with ACE inhibitors
Indications of ARBs
- HTN
- MI
- CHF
- Prevention of stroke in patients with high risk of CVD
Adverse effects of ARBs
- BBW: can cause injury/death to developing fetus
- no problems with cough
- hyperkalemia
- hypotension
- angioedema (rare)
- acute renal insufficiency
- additive hypotensive effects when in combo with other antihypertensives
ACE inhibior/ARB warning
- start with smallest dose possible due to hypotension risk
- may cause hyperkalemia in CKD patients or patients on other K+ sparing meds
- absolutely contraindicated in pregnancy
MoA of Renin inhibitor
- Inhibits angiotensinogen to angiotensin I conversion
- does not block bradykinin breakdown (less cough than ACE-Is)
Aliskiren
- Renin inhibitor; inhibits angiotensinogen to angiotensin I conversion
- can be used alone or in combo with other antihypertensives
- PO
adverse effects of Renin inhibitors
- orthostatic hypotension
- hyperkalemia
- angioedema
- BBW: injury/death to developing fetus
MoA of all types of CCBs
- inhibit influx of calcium via the voltage-dependent calcium channels in vascular smooth muscle
- relaxation of peripheral vasculature –> peripheral vasodilation
- each agent produces different degrees of systemic/coronary arterial vasodilation
Dihydropyridines
- CCBs that act primarily on artieroles
- end in (-dipine)
- ex. Nifedipine, Amlodipine, Clevidipine
Nifedipine
- dihydropyridine CCB, acts on arterioles
- the 1st choice of drug for this class
- more potent
- PO
Amlodipine
- dihydropyridine CCB, acts on arterioles
- more potent
- PO
Clevidipine
- dihydropyridine CCB, acts on arterioles
- IV only
Non-dihydropyridines
- CCBs that act on arterioles and on the heart
- inhibit influx of calcium via voltage-dependent calcium channels in vascular smooth muscle AND in th heart
- decrease HR, AV conduction, and force of contraction
Verapamil
- Non-dihydropyridine CCB; acts on artieroles AND heart
- PO or IV
Diltiazem
- Non-dihydropyridine CCB; acts on artieroles AND heart
- PO or IV
adverse effects of CCBs (dihydropyridines)
- dizziness, headache, flushing
- reflex tachycardia (avoided by using B-blocker in combo)
- peripheral edema
- gingival hyperplasia
adverse effects of CCBs (non-dihydropyridines)
- peripheral edema
- headache
- gingival hyperplasia
- CV effects (bradycardia, AV block, decrease myocardial contractility, hypotension)
- constipation
indications of CCBs
- HTN
- Angina pectoris (dihydro)
- cardiac dysrhythmias (non-dihydro)
MoA of B-Blockers
- competitively antagonize the response of catecholamines mediated by beta-receptors
- decreased heart contractility and HR
- decreased cardiac output and peripheral resistance
- decreased renin release and blood volume
Selective B1 blockers
- greater tendency to occupy B1 receptors in the heart rather than B2 in the lungs
- AtBM –> Atenolol, Bisoprolol, Metoprolol
Metoprolol
- Selective B1 blocker
- PO
Atenolol
- Selective B1 blocker
- PO
Bisoprolol
- Selective B1 blocker
- PO
Non-selective B1 and B2 blockers
- most adverse effects on lungs
- ex. propranolol
Propranolol
-Non-selective B1 and B2 blocker
- PO, IV
- prototype for this class of drugs
Nebivolol
- B1 selective with Nitric oxide dependent vasodilation
- PO
Partial agonist B blockers
- have intrinsic sympathomimetic activity –> prevents bronchoconstriction and other B-blocking actions
- ability to maintain satisfactory HR
- ex. Acebutolol
Acebutolol
- Partial agonist B blocker
- depresses HR less than other B blockers
- PO
Nonselective B blockage drugs with A blockade
- alpha blockade –> promotes vasodilation (but also orthostatic hypotension)
- B blockade on heart –> decreased HR and contractility
- B blockade on juxtaglomerular cells –> suppresses release of renin
- ex. Carvedilol, Labetolol
Carvedilol
- Nonselective B blockage drugs with A blockade
- PO
Labetolol
- Nonselective B blockage drugs with A blockade
- alternative med for chronic HTN in pregnancy
- PO, IV
Indications of B blockers
- HTN
- Angina
- MI
- Antiarrhythmics
- Migraine
- Glaucoma
Adverse effects of B blockers
- bradycardia, AV block, worsening HF
- induce/worsen bronchospasm (Asthma, some COPD)
- sexual impairment
- depression, fatigue, nightmares, confusion, hallucinations
- hyperglycemia, hyperTGemia
- allergy to propranolol
BBW of b blockers
- abrupt d/c may cause rebound HTN or unstable angina, MI, and death in patients with high CAD
MoA of alpha 1 blockers
- blocks A1 receptors (competitive antagonists) –> competes with norepinephrine and epinephrine on vascular smooth muscle and prevents vasoconstriction
- dilation of arterioles
- reduce prostatic symptoms in men
Terazosin
- Alpha 1 blocker
- PO
Tamsulosin
- Alpha 1 blocker
- selective for prostate smooth muscle vs vascular smooth muscle
- PO
indications for A1 blockers
- HTN
- BPH
adverse effects of A1 blockers
- CV: reflex tachy and ortho hypotension
- salt and water retention
- blurred vision
- nasal congestion
- erectile dysfunction
MoA of A2 agonist
- 2nd line agents
- selective activation of A2 receptors in the CNS –> vasodilation, reduce HR and cardiac output
Methyldopa
- A2 agonist
- drug of choice for chronic HTN in pregnancy
- PO
Clonidine
- A2 agonist
- used in resistant HTN (2nd and 3rd line agent, high side effects)
- adjunct therapy in cancer pain
- off label use for opioid/alc withdrawal symptoms, nicotine dependence, PMS
- PO
Indications for A2 agonists
- HTN
- ADHD
- Pain (clonidine)
adverse effects of A2 agonists
- CNS depression –> drowsiness
- dry mouth
- Rebound HTN –> large jump in BP occurring to abrupt clonidine withdrawal (requires slow weaning)
MoA of Direct Arteriolar Vasodilators
- selective dilation of arterioles (not veins)
- produce peripheral vasodilation –> decreased peripheral resistance
- increase HR/myocardial contractility by baroreceptor activation
Hydralyzine
- Direct Arteriolar Vasodilator
- PO or (IV in hypertensive emergencies)
- used prior to labor in pre-eclampsia
Minoxidil
- Direct Arteriolar Vasodilator
- not first choice drug (pericardial effusion side effects), only used for pts who do not respond to first line
- PO
adverse effects of arteriolar vasodilators
- reflex tachycardia
- vascular headache
- Lupus-like syndrome (hydralazine)
Specific to Minoxidil –> pericardial effusion (BBW); Hirsutism
drugs used in chronic HTN in pregnancy
- methyldopa
- labetolol
Drugs for hypertensice emergency
- nitroglycerin
- hydralyzine
- labetolol
- clevidipine