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Antihypertensive Meds to Know

Antihypertensive Meds to Know

Antihypertensives

-ACEI, ARB and Renin = not combined, considered same class 

-Pregnancy: Labetalol and Nifedipine (first line); Methyldopa = old and second line

-ACEI, ARB, Renin, Thiazide, BB → not in pregnancy

-ACEI, ARB, CCB and Thiazide – first line HTN meds

-HTN emergency → nitroprusside (min-min titration); could use NO, CCB, BB, vasodilator

-Resistant HTN? Check meds (NSAIDs, sympathomimetics, steroids), diet, drinking, dose

 

Drug Class Drug Names MOA Indications Metabolize/ Excrete Interactions Adverse Effects
ACEI Ending in -pril

Enalapril

Vasodilation

Bradykinin inc Angioedema.

-Drug of choice for pts with HTN and HF (slows LVH post MI)

-renal protection in DM

-Combined with thiazide or CCB

Liver

Mostly Renal (30% feces)

Potassium sparing (hyperkalemia)

Lithium (ACEI elevates Lithium) 

Azathioprine (low RBC/ WBC)

Hyperkalemia

Dry cough

Angioedema

Fatigue

Dizziness

Hypotension

Altered taste

Rash

May induce ARF

NOT in pregnancy

ARBs – angiotensin II blockers Ending in -artan

Valsartan

ACE left alone = no bradykinin 

Block Angiotensin II receptors → vasodilation

Same as above but no cough or angioedema Liver

Feces

Potassium sparing (hyperkalemia) Neutropenia

Fatigue and HA

Abd Pain

Hyperkalemia

NOT in pregnancy

Renin Inhibitor Aliskiren Renin blocker Diarrhea at high dose

Cough

Angioedema

NOT in pregnancy

CCBs Dihydropyridine → ending in -ipine

Amlodipine

——————-

Nondihydropyridine:

Verapamil

Diltiazem

-Inhibit calcium channels in cardiac and smooth muscle

-Dilates coronary (inc O2) and peripheral arteries (dec PVR)

Decrease contractility, conductivity at SA/AV and O2 demand

HTN

Angina (Nifedipine, Amlodipine, Nicardipine and dihydropyridine)

Dysrhythmias

Headache prophylaxis

Nifedipine potent vasodilator

Diltiazem = middle

Verapamil potent negative inotrope; nonspecific action

Liver

Renal/ Bile/ Feces

Hepatic impairment

Aortic stenosis (significantly low CO)

Exacerbate CAD and unstable angina (MI)

Hypotension

Bradycardia

AV block

Headache

Vertigo

Dyspepsia, nausea, constipation

Flushed face

Gynecomastia

Peripheral Edema

Beta adrenergic blockers Ending in -olol

Selective (beta1 only):

Atenolol

Metoprolol

Nebivolol

—————–

Non-selective: 

Carvedilol

Labetalol

Nadolol

Propranolol

Timolol 

Dec HR and contractility

 

Nonselective – hypoglycemia and bronchospasm

Angina/ post MI (non ISA preferred; don’t stimulate heart)

Acebutolol, Penbutolol, and Pindolol = ISA (sympathomimetic)

Nebivolol (bystolic) has Nitric O effects in vasodilation 

Dysrhythmias

Panic attack/ Anxiety

Migraine Prophylaxis

Tremor

Hyperthyroidism

Asthmatic (consider using selective BB) Dec HR

Bronchoconstriction 

Fatigue

Parestesia (PAD)

Raynauds (cold ext)

Neurologic (insomnia, hallucination, nightmares)

ED

NOT in pregnancy

Alpha-1 adreno blocker (PNS)

Sympatholytic

Ending in -azosin 

Doxazosin

→ Reserpine (CNS+PNS)

Dec NE leads to dec CO and PVR HTN + BPH Liver

Mostly Feces (some renal)

Impaired Liver Function

Verapamil

Sildenafil

Tamsulosin 

→ all lead to excessive vasodilation

Orthostatic Hypotension (first dose)

Syncope

Arrhythmias

HA

Priapism

Fluid/urine retention

Alpha-1/ beta adreno blocker Labetalol

Carvedilol

HTN & HF – Carvedilol

Gestational HTN – Labetolol 

Alpha-2 adreno agonist (CNS)

Sympatholytic

Clonidine

Fenoldopam

Hydralazine

Methyldopa

Minoxidil

Nitroprusside

-Stimulate alpha 2 in brain to stop NE release

-Dec HR, contractility, CO and PVR

Mild-Mod HTN

Methyldopa indicated in pregnancy

Liver

Mostly Renal (some feces)

Hepatic Impairment

MAOIs

Oral Fe (dec effect of methyldopa)

Levodopa (severe hypotension)

Anesthetics

Sedation

Depression (CNS rxn)

HA

Dry mouth

Orthostatic Hypotension

Bradycardia

GI upset

Hemolytic Anemia

Rebound HTN

Direct Vasodilator Hydralazine

Minoxidil – more potent

-Relax smooth muscles in arteries through Ca++ and K+ activity

-Hydralazine also stimulates NO → vasodilation

-HTN urgency and emergency

-Uncontrollable HTN

Minoxidil indications: 

-Vasodilation but Lupus (so not Hydralazine)

-combined with BB (cardio) and thiazide (for renin) to counter baroreceptor reflex

Liver

Mostly Kidney (10% feces)

HA and Nausea

Tachycardia

Arrhythmia

Sweating

Angina

Baroreceptor Reflex (inc BP by cardiac and renin stimulation)

Hypertrichosis (minoxidil)

Lupus-like (hydralazine) 

Nitric Oxide Nitroprusside

Nitroglycerin

-NO relaxes smooth muscle

-Vasodilation

-HTN emergency and angin

-min-min titration due to short T½  

Thiocyanate toxicity (inc with kidney failure)

N/V

Muscle twitch

Sweating

 

Diuretics

-higher side effect profile

-ceiling effect; except Loop?

 

-Proximal, Descending Loop and Collecting Tube → weak

-Ascending Loop, Distal convoluted → strong

Drug Class Drug Names MOA/ Indications Indications Metabolize/ Excrete Interactions Adverse Effects
Thiazide Diuretics

(Distal Convoluted)

Chlorothiazide (low bioavailability) 

HCTZ

———–

Chlorthalidone

Indapamide

Metolazone

Distal Tube:

-excrete Na+ and Cl- 

-absorb Ca++

-reduce PVR

-distal administration?

-low ceiling effect

HTN

Edema

CHF

DM

Hypercalcuria

When GFR > 30ml/min

Not metabolized

Indapamide – Hepatic

Renal 

Diminished w/ NSAIDs

Renal Impairment 

Hypo: K+ (arrhythmia), Mg+, Na+

Hyper: uric acid (gout), glucose (diabetes), Ca++

Renal damage

Volume loss

NOT in pregnancy

Loop Diuretics

(Ascending Henle)

Bumetanide

Ethacrynic Acid

Furosemide

Torsemide

Ascending Loop: 

-excrete Na+, K+, Cl-, Ca++

-less water reabsorbed

-venodilation = reduce preload and PVR

Greatest diuresis

proximal admin?

-ceiling effect

Edema

Hypercalcemia

Hyperkalemia

When GFR < 30ml/min

-Bumetanide and Torsemide have high bioavailability and potency

Liver

Renal

Dehydration

Aminoglycosides

Lithium

NSAIDs lower renal perfusion

Hypovolemia

Hypokalemia

Alkalosis 

Ototoxicity

Hyperuricemia (gout

Diabetes?

Dizzy, HA

Blurred Vision

Urinary Freq

Neutropenia

Thrombocytopenia

Potassium Sparing (Collecting Tubule) Amiloride

Triamterene

———

Eplerenone

Spironolactone

Collecting tubule:

-excrete Na+

-absorb K+

Aldosterone Antagonist

Or Na+ channel blocker

Edema

Hypokalemia

HF

Resistant HTN

PCOS

-Combined with Loop

Eplerenone = CYP3A4 metabolism

Renal

Avoid with ACEI

Cardiac symptoms

Hyperkalemia

Gynecomastia (spironolactone)

Dizzy, HA

N/V/D 

Carbonic Anhydrase Inhibitor (Proximal Tubule) Acetazolamide -mild diuresis

-inc pH

Glaucoma

Altitude Sickness

Edema

Seizure

Alkalosis

Not metabolized

Renal

Hepatic Cirrhosis Acidosis

Drowsiness

Anorexia, N/V/D

Paresthesia

Blurred Vision

Dry Mouth

Hypokalemia

Renal Stone

Osmotic Diuretics (Proximal Tubule + Descending Henle) Mannitol (IV only) -inc osmotic pressure in filtrate = dec water reabsorption

no affect on Na+

Cranial Pressure post trauma

Glaucoma

Prevent ARF

Convulsions

Thrombophlebitis

Pulmonary congestion

HA, CP, Tachy

Blurred Vision

Fever/ chills

Electrolyte imbalance

 

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