Anti-Hypertensive Flashcards by Jamie Pytel

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

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Diuretics

Drugs of choice in uncomplicated hypertension

Mild/moderate hypertension with lifestyle modification

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Thiazides

Hydrochlorothiazide, Chlorthalidone
Inhibits Na/Cl cotransporter
Initial volume contraction
Decreased peripheral resistance (prostaglandins)
Mild Na excretory effects

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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

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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)

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Ca Channel Blockers

Nondihydropyridine

Can do heart and smooth muscle receptors

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Ca Channel Blockeres

Dihydropyridines

More selective for vascular smooth muscle

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Ca Channel Blockers

MoA: Reduce vascular resistance by reducing Ca influx

Non-dihydropyridine reduce pacemaker potentials, AV node conduction, and contractility

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Ca Channel Blockers

Nifedipine

Dihydropyridine
Limited affect on pacemaker or conduction
SE: acute tachycardia, headache, peripheral edema (arteriolar dilation > venodilation), flushing

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Ca Channel Blockers

Diltiazem

Non-dyhydropyridine
Reduces pacemaker and conduction current
SE: dizziness, headache, edema, bradycardia

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Ca Channel Blockers

Verapamil

Non-dihydropyridine
More pronounced reduction of current
SE: dizziness, headache, edema, constipation, bradycardia

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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

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Sympatholytic Drugs

MOA: Reduces sympathetic-mediated vasoconstriction, Co, and renin release

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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

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Guanfacine

Longer half-life than clonidine

Less chance of rebound hypertension

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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

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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

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Alpha Adrenergic Receptor Antagonists

Block a-adrenergic-mediated vasoconstriction at receptor

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Phenoxybenzamine

Alpha adrenergic receptor antagonist
Non selective
Primary use in PHEOCHROMOCYTOMA
SE: Tachycardia

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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

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Beta Blockers

Decrease cardiac contractility and CO
Decrease renin secretion
Decrease angiotensin II production

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Propranolol

Nonselective B-blocker
Mild/moderate hypertension
Adjunct to prevent tachycardia with vasodilators
Lipophilic

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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

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