Anti-Hypertensive Flashcards
First line drugs of choice
Diuretics Calcium Channel Blockers ACE inhibitors Angiotensin Receptor Blockers (BB are not first line because they do not work well in AA populations, and cause significant side effects
Diuretics
Drugs of choice in uncomplicated hypertension
Mild/moderate hypertension with lifestyle modification
Thiazides
Hydrochlorothiazide, Chlorthalidone Inhibits Na/Cl cotransporter Initial volume contraction Decreased peripheral resistance (prostaglandins) Mild Na excretory effects
Loop Diuretics
Furosemide (Lasix)
Blocks Na/K/2Cl co-transporter in TAL
Venous dilation from prostaglandins
Dehydration/hyponatremia, hypokalemia, impaired diabetes control, increased LDL/HDL, ototoxicity
Drug interactions: NSAIDs, Aminoglycosides
K Sparing Diuretics
Spironolactone, eplerenone, tramterene, amiloride
Aldosterone receptor blocker/prevent insertion of ENAC channels in collecting tubule
Side Effects: Hyperkalemia, gynecomastia (spironolactone)
Drug interactions: NSAIDs (block good effects of prostaglandins), ACE inhibitors and ARBs (also inhibit aldosterone)
Contraindications: RAS inhibitors (have both ACE inhibitors and ARBs)
Ca Channel Blockers
Nondihydropyridine
Can do heart and smooth muscle receptors
Ca Channel Blockeres
Dihydropyridines
More selective for vascular smooth muscle
Ca Channel Blockers
MoA: Reduce vascular resistance by reducing Ca influx
Non-dihydropyridine reduce pacemaker potentials, AV node conduction, and contractility
Ca Channel Blockers
Nifedipine
Dihydropyridine
Limited affect on pacemaker or conduction
SE: acute tachycardia, headache, peripheral edema (arteriolar dilation > venodilation), flushing
Ca Channel Blockers
Diltiazem
Non-dyhydropyridine
Reduces pacemaker and conduction current
SE: dizziness, headache, edema, bradycardia
Ca Channel Blockers
Verapamil
Non-dihydropyridine
More pronounced reduction of current
SE: dizziness, headache, edema, constipation, bradycardia
CCB therapeutic Notes
Non-dihydropyridines are contraindicated in patients with conduction disturbances
Use non-dihydropyridine with caution in patient given B-blockers
Avoid use of short acting CCBs for chronic hypertension
Sympatholytic Drugs
MOA: Reduces sympathetic-mediated vasoconstriction, Co, and renin release
Clonidine
Sympatholytic Drug
Centrally acting agent
a2 adrenergic receptor agonist in medullary CV center
Decreases sympathetic outflow from CNS
SE: sedation, dry mouth, bradycardia, dermatitis
Drug interactions: CNS depressants
Withdraw slowly to prevent rebound hypertension
Guanfacine
Longer half-life than clonidine
Less chance of rebound hypertension
Methyldopa
Sympatholytic Drug
a2-adrenergic receptor agonist (same MOA as clonidine)
Competes wtih L-DOPA for DOPA decarboxylase
Inhibits dopamine production
Drug interactions: levodopa
SE: Sedation, nightmares, movement disorders, hyperprolactinemia, anemia
Contraindications: Liver Dx
USED IN HYPERTENSION WITH PREGGOS
Reserpine
Indirect Acting Adrenergic Blocking Agent
Blocks VMAT vesicular transporter
Prevents storage of NE centerally and peripherally
Combined with diuretics for mild/moderate HTN
SE: sedation, diarrhea, depression, bradycardia, nasal congestion
Drug interactions: CNS depressant, MAOIs
Alpha Adrenergic Receptor Antagonists
Block a-adrenergic-mediated vasoconstriction at receptor
Phenoxybenzamine
Alpha adrenergic receptor antagonist
Non selective
Primary use in PHEOCHROMOCYTOMA
SE: Tachycardia
Prazosin
Alpha adrenergic receptor antagonist
Less tachycardia than direct vasodilators
Initial hypotension
Does not impair exercise tolerance
Terazosin and doxazosin have longer half-life
SE: Hypotension (first dose), dizziness, headaches, weakness
Also decreases LDL/HDL
Beta Blockers
Decrease cardiac contractility and CO
Decrease renin secretion
Decrease angiotensin II production
Propranolol
Nonselective B-blocker
Mild/moderate hypertension
Adjunct to prevent tachycardia with vasodilators
Lipophilic
Nadolol
Nonselective B-Blocker
Longer half-life than propranolol
Better compliance
Hydrophilic
Pindolol
Non-selective B-Blocker Partial agonist Less bradycardia Lipophilic Good for patients who still want to exercise
Metoprolol
B1-Selective
Fewer respiratory side effects
Lipophilic
Atenolol
B1-Selective
Hydrophilic
Excreted by kidney
Labetolol
B-Blocker Has some a-blocker capacity Orthostatic hypotension and sexual dysfunction Used for pheochromocytoma Lipophilic
Carvedilol
Nonselective B-Blocker a-receptor antagonist vasodilator Lipophilic Increases NO
BB SE
Bradycardia Impotence Increased TG Decreased HDLs Hyperglycemia Impaired exercise tolerance
BB Drug Interactions
CCB
Reduced contractility and conduction
BB Contraindication
Cardiogenic shocks
Sinus bradycardia
Asthma
Severe Heart Failure
BB and Diabetics
Can mask insulin-induced hypoglycemia
Give them ACEI instead
Vasodilators
Vasodilation of arterioles
Hydralazine
Vasodilator
Orally effective
Used in drug resistant hypertension and emergency
Long term use is poor
SE: Tachycardia, angina aggravation, fluid retention, nausea, vomiting, sweating, flushing, lupus-like symptoms
NSAIDs can reduce effectiveness
Minoxidil
Vasodilator
Used in drug resistant hypertension
SE: Same as hydralazine including hypertrichosis (werewolf syndrome)
Nitroprusside
Vasodilator Used in emergencies (BP > 200) Immediate onset Brief duration Promotes arterial and venous dilation SE: Nausea, vomiting, muscle twitch, cyanide poisoning (from metabolites in long-term usage)
ACE Inhibitors
Blocks production of angiotensin II and ATII-mediated vasoconstriction
ATII causes growth and aldosterone release
ACE inhibitors prevent breakdown of bradykinin so it can go on and increase prostaglandins and NO
Catopril
ACEI
Short half life
Multiple daily doses
Active metabolites
Enalapril
ACEI Converted to active metabolite enalaprilat Longer onset of action Longer half life Dose 1-2xday
Lisinopril
ACEI Water soluble Excreted unchanged by kidney Longer half-life Allows 1x daily dosing More predicitable onset and duration of action
ACEI SE
Hyperkalemia
Rash
Dry cough
Angioedema
ACEI Drug Interactions
Exacerbates hyperkalemic effect of K sparing drugs
ACEI Contraindications
PREGGOS
Bilat renal stenosis
ACEI Notes
Prolongs survival in pts with HF or LV dysfunction after MI (ATII promotes growth/inflammation so if we prevent that the heart wont get more damaged)
Preserves renal function in diabetic patients
Angiotensin II Receptor Blockers (ARBs)
Mediate vasoconstriction and Na retention
Less effective in Na-sensitive hypertensiv epatients (AA_
Reduce dose in hypovolemia or live disease
Better results with diuretic combo
Effect takes 1 week
Losartan
Selective ARB
SE: Hyperkalemia
Contraindications: PREGGOS (cause renal failure)
Drug interactions: exacerbates hyperkalemia in K sparing drugs
Good Combos
Thiaxaide or loop diurteic with K sparing diuretic
Thiazide with BB
CCB with ACEI
Bad Combos
ACEI with K sparing diuretics (exacerbate hyperkalemia)
ACEI and ARBs (no advantage in diuretics, but increased risk of hyperkalemia)
Don’t mix drugs with same MOA, efficacy won’t increase
Diabetes mellitus
ACEI (delay loss of renal function)
a-blockers
CCBs (limited effects on carbohydrate metabolism)
Hearth Failure
ACEIs (reduce mortality and recurrent MI)
Combine with diuretics for congestion
MI
ACEIs reduce remodeling
ACEIs reduce subsequent MI
BBs (but not the partial agonist pindolol) reduce arrhythmia and remodeling
Pregnancy
Avoid ACEI or ARBs and BBs (inhibits renin)
Methyldopa is widely used
African Americans
Monotherapy with diuretics, CCBs most efficacious
Monotherapy with BBs and ACEIs not as effective though good control can be done through combined diuretics
Elderly
Small doses with small increments
Simple regimens
Monitor side effects closely
Diabetes mellitis
ACEI
A-blockers
CCBs have some effects on carbohydrate metabolism
Hyperlipidemia
Low dose diuretics have little effects on cholesterol and TG
BB can raise TG
A-blockers can decrease LDL/HDL ration
CCBs, ACEIs, ARBs have little effect on lipid profile
Obstructive Airway Disease
Avoid BBs
