Anti Hypertensive Drugs Flashcards by Tom O

Primary Risk Factors for HTN

Family history
African ethnicity
Male gender
Post-menopausal women
>20 lbs excess body weight

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Associated Risk Factors for HTN

Diabetes
Excess Alcohol
Oral contraceptives
Inactivity

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What are pre hypertensive BPs?

120-139/80-89

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What are stage 1 hypertensive BPs?

140-159/90-99

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What are stage 2 hypertensive BPs?

160/100 and up

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In patients less than 60 years old, what is the lowest blood pressure when you would prescribe anti-hypertensive meds?
What would you recommend before then to lower their BP?

When they get above 140/90, you need to prescribe meds.

Before that, use lifestyle modifications to treat HTN

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In patients older than 60, at what BP do you start prescribing meds for HTN?

150/90

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What are the 4 classes of first-line DOC anti-hypertensives?

Diuretics
Ca2+ channel blockers
ACE Inhibitors
Angiotensin receptor blockers

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Thiazide Diuretics

MOA

Block the Na+/Cl- channels in the distal convoluted tubule, increasing Na+ loss and urinary volume.
K+ wasting
Cause some vasodilation via prostaglandin release

Cause increased aldosterone production and insertion of ENaC channels into luminal membrane of principal cells, driving K+ out of the lumen

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Thiazide Diuretics

Adverse Effects

Hyponatremia
Hyperglycemia
Hypokalemia
Increased LDL/HDL
Metabolic alkalosis

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Thiazide Diuretics

What drugs would be OK to coadminister with thiazides to prevent K+ wasting?

Prevent aldosterone from reabsorbing more Na+ in collecting ducts, thus prevent K+ wasting

Beta Blockers
ACE inhibitors
Angiotensin receptor antagonists

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Thiazide Diuretics

What drugs should you not coadminister thiazides with?

NSAIDs

May block the vasodilatory effects of the prostaglandins released by the thiazides

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Thiazide Diuretics

Contraindications

Hypokalemia

Pregnancy

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Thiazide Diuretics

What is their interaction with beta blockers?

May cause hyperglycemia together, though beta blockers may be coadministered to help prevent hypokalemia

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List the thiazide diuretics

Hydrochlorothiazide

Chlorthalidone

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Loop Diuretics

MOA

Block the Na+/K+/Cl- channel in the thick ascending limb of the loop of Henle
K+ wasting
Venous dilation via Prostaglandin release
Also cause excretion of Mg2+ and Ca2+

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Loop Diuretics

List them

Furosemide
Ethacrynic acid (last resort)
Bumetanide
Torsemide

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Loop Diuretics

Side Effects

Hypokalemia
Metabolic alkalosis
Dehydration
Hyponatremia
Hypomagnesemia
Impaired diabetes control
Increased LDL/HDL
Ototoxicity

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Loop Diuretics

Drugs Interactions

Aminoglycosides - exacerbates ototoxicity

NSAIDs- block vasodilatory effects of prostaglandins

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List the K+ Sparing Diuretics

Spironolactone
Eplerenone
Amiloride
Triamterene

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Spironolactone

MOA

Blocks the aldosterone receptor, thus preventing insertion of ENaC channels into the luminal membrane of the principal cells.
Increase Na+ excretion and spare K+

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Spironolactone

Adverse Effects

Hyperkalemia

Anti-androgenic effects - gynecomastia, amenorrhea, impotence

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Eplerenone

MOA

Blocks the aldosterone receptor, thus preventing insertion of ENaC channels into the luminal membrane of the principal cells.
Increase Na+ excretion and spare K+

Does NOT have the anti-androgenic effects of spironolactone

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Spironolactone and Eplerenone

Drug Interactions

NSAIDs

ACE inhibitors and Angiotensin Receptor Blockers - can exacerbate hyperkalemia by inhibiting aldosterone’s production

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Amiloride and Triamterene | MOA

Block the ENaC channel in the principal cells

Amiloride and Triamterene | Drug Interactions

NSAIDs ACE Inhibitors and Angiotensin Receptor Blockers - may exacerbate hyperkalemia

Would you ever use a K+ sparing diuretic as a monotherapy?

No. Not very strong on their own, but they are good in combination with loop or thiazide diuretics (the K+ wasting drugs)

Ca2+ Channel Blockers | Dihydropyridines are selective for? What is the dihydropyridine drug and its MOA?

Selective for vascular smooth muscle. Nefedipine is used only in HTN by blocking vascular Ca2+ channels

Ca2+ Channel Blockers | What are the non-dihydropyridine drugs? What are they selective for?

Verapamil and Diltiazem They act on both vascular and cardiac smooth muscle (though verapamil has a much more potent effect on cardiac smooth muscle)

Nefedipine | Adverse Effects

Acute tachycardia | Peripheral edema

Diltiazem | Adverse Effects

Bradycardia

Verapamil | Adverse Effects

Constipation | Bradycardia

Verapamil and Diltiazem are contraindicated in...?

Patients with conduction disturbances (heart block, etc)

Clonidine | MOA

Alpha-2 receptor agonist | Activates a G-alpha-i cascade, inhibiting adenylyl cyclase to decrease sympathetic outflow from the CNS

Clonidine | Adverse Effects

Sudden withdrawal may lead to a hypertensive crisis Sedation Dry mouth Dermatitis

Why might guanfacine be used in place of clonidine?

Guanfacine has a longer half life, so it is less likely to cause rebound HTN when a patient misses a dose

Methyldopa | MOA

Alpha-2 receptor agonist | Also competes with LDOPA for dopamine decarboxylase, inhibiting dopamine production

Methyldopa | Indications

Used for hypertensive control in pregnant women

Methyldopa | Adverse Effects

Sedation Hyperprolactinemia Anemia

Reserpine | MOA

Blocks VMAT vesicular transporter, preventing storage of NE in vesicles. MAO will digest NT in the cytosol.

Reserpine | Indications

Hypertensive patients who are resistant to other drugs

Reserpine | Adverse Effects

Depression | Nasal Congestion

Reserpine | Drug Interactions

Do not give reserpine with a MAO inhibitor, which could reverse reserpine's effects and cause a hypertensive crisis

Phenoxybenzamine | MOA

Non selective alpha adrenergic antagonist

Phenoxybenzamine | Indications

Pheochromocytoma

Phenoxybenzamine | Adverse Effects

Tachycardia (due to NE binding beta receptors instead of alpha)

Prazosin | MOA

Selective alpha-1-antagonist

Prazosin | Indications

Primary HTN | Benign Prostatic Hyperplasia

Prazosin | Adverse Effects

Orthostatic Hypotension | Dizziness

Beta Blockers | General MOA

Lower contractility of the heart Lower HR Prevent renin release, thus decreasing angiotensin II production

What is the prototypical beta blocker?

Propranalol

Nadolol

Nonselective Beta blocker | Longer half life

Pindolol

Partial agonist of Beta receptors Nonselective Causes less bradycardia than other beta blockers

Metoprolol

B1-selective beta blocker | Lipophilic

Atenolol

B1-selective | Hydrophilic

Labetolol

Beta blocker with some alpha-blocking activity | Lipophilic

Carvedilol

Nonselective beta blocker that also has alpha-receptor antagonist activity Vasodilation Lipophilic

What are the lipophilic beta blockers?

Metoprolol Labetolol Carvedilol

Beta Blockers | Side Effects of all BBs

``` Bradycardia Increased triglycerides Decreased HDLs Hyperglycemia Impaired exercise tolerance ```

Beta Blockers | Side effects of Nonselective BBs

Bronchiole constriction (increased airway resistance)

Beta Blockers | Side Effects of Lipophilic BBs

Insomnia Chronic fatigue Depression

Contraindications for Beta Blockers

Sinus bradycardia Cardiogenic shock Heart block Asthma

Beta Blockers | Drug Interactions

Calcium Channel Blockers - causes reduced contractility and conduction

Vasodilators | General MOA

Vasodilation of small vessels, primarily the arterioles

Hydralazine | MOA and Indications

Vasodilator used in drug resistant HTN and emergencies

Hydralazine | Side Effects

Tachycardia Angina aggravation Fluid Retention NSAIDs can reduce effectiveness

Minoxidil | MOA and Indications

Vasodilator used for drug resistant HTN

Minoxidil | Adverse Effects

Hypertrichosis Tachycardia Angina Aggravation Fluid retention

Nitroprusside | MOA and Indications

Vasodilator used in emergencies

Nitroprusside | Adverse Effects

Cyanide poisoning (gets converted to a cyanide-like metabolite in the liver)

ACE Inhibitors | General MOA

``` Block production of angiotensin II Prevent vasoconstriction Prevent aldosterone activation Prevent bradykinin degradation Prevent some NE release, growth, and inflammation ```

List the ACE Inhibitors

Captopril Enalapril Lisinopril

Why is Lisinopril the most commonly used ACE inhibitor today?

Captopril had a very short half life. Enalapril had a longer half life but needed to be metabolically converted, making half life and drug effects more unpredictable Lisinopril has a rapid onset of action and a more predictable half life

ACE Inhibitors | Adverse Effects

Hyperkalemia Dry cough Angioedema (rare)

ACE Inhibitors | Contraindications

Should not be given with K+ sparing drugs Pregnancy Bilateral renal stenosis

How do ACE inhibitors help patients who have HF or LV dysfunction?

Prolongs survival by preventing cardiac remodeling

Angiotensin II Receptor Blockers | Which one do we use most?

Losartan | - selective AT1 receptor antagonist

Angiotensin II Receptor Blockers | Adverse Effects

Hyperkalemia

Angiotensin II Receptor Blockers | Contraindications

Pregnancy Should not be used with K+ sparing drugs

How should you best treat HTN in African Americans?

Monotherapy with diuretics or Calcium channel blockers

What anti-hypertensive meds should you avoid in pregnancy?

ACE inhibitors Angiotensin receptor blockers Beta Blockers

What anti-hypertensive meds should you use in pregnancy?

Methyldopa

Anti Hypertensive Drugs Flashcards

(82 cards)