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 |
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| 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 |
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| 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 |
