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Florencia G. dela Cruz-Munsayac, MD, FPSECP, MBA, RMT THERAPY OF HYPERTENSION
 
 
Hypertension ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Hypertension   ,[object Object],[object Object],[object Object]
Normal Regulation of Blood Pressure ABP  =  cardiac output x peripheral  vascular resistance Regulating the volume of intravascular fluid Baroreflexes, act in combination with RAAS Local release of vasoactive substances from vascular endothelium
Classification of Blood Pressure for  Adults >/= 18 years: JNC 7 ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Etiology of Hypertension ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Etiology of Hypertension ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Genetic influences + Environmental Factors ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Principles of Antihypertensive Therapy ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Classification of Antihypertensive Drugs ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Classification of Antihypertensive Drugs ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Diuretics:  Mechanisms of Action & Hemodynamic Effects ,[object Object],[object Object],[object Object],[object Object],[object Object]
Diuretics:  Mechanisms of Action & Hemodynamic Effects ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Diuretics: Benzothiadiazine & Related Compounds ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Diuretics: Benzothiadiazine & Related Compounds ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Diuretics: Loop diuretics ,[object Object],[object Object],[object Object],[object Object],[object Object]
Diuretics: Loop diuretics ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Diuretics: Loop diuretics ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Diuretics: Potassium-sparing diuretics ,[object Object],[object Object],[object Object],[object Object],[object Object]
Diuretics: Potassium-sparing diuretics ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents –  β - Adrenergic Receptor Antagonists ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents –  β - Adrenergic Receptor Antagonists BETA – ADRENOCEPTOR BLOCKING DRUGS Nonselective Selective With alpha-blocking ability Nadolol  Propranolol Timolol Sotalol Tetralol Pindolol Penbutolol Carteolol Alprenolol Dilevatol Oxyprenolol Atenolol Esmolol Metoprolol Bevantolol Bisoprolol Betaxolol Acebutolol (Practolol) Celiprolol Labetalol Bucindolol Carvedilol
Sympatholytic Agents –  β - Adrenergic Receptor Antagonists Propranolol   ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents –  β - Adrenergic Receptor Antagonists Metoprolol ,[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents –  β - Adrenergic Receptor Antagonists Nadolol, Carteolol, Atenolol, Betaxolol, & Bisoprolol ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents –  β - Adrenergic Receptor Antagonists Pindolol, Acebutolol, & Penbutolol ,[object Object],[object Object],[object Object]
Sympatholytic Agents –  β - Adrenergic Receptor Antagonists Labetalol & Carvedilol ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents –  β - Adrenergic Receptor Antagonists Labetalol & Carvedilol ,[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents –  β - Adrenergic Receptor Antagonists Esmolol ,[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents –  β - Adrenergic Receptor Antagonists ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents –  β - Adrenergic Receptor Antagonists ,[object Object],[object Object],[object Object]
Sympatholytic Agents –   1 -  Adrenergic Antagonists ,[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents –   1 -  Adrenergic Antagonists ,[object Object],[object Object],[object Object]
Sympatholytic Agents –   1 -  Adrenergic Antagonists ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents –   1 -  Adrenergic Antagonists ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents –  Non-selective   Adrenergic Antagonists ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents – Centrally-Acting Agents ,[object Object],Methyldopa Guanfacine guanabenz clonidine Moxonidine Rilmenidine  Alpha-adrenoreceptor Imidazoliine receptor Nucleus Tractus solitarius Salivary  glands Dry mouth Nucleus coeruleus Sedation Rostral  Ventrolateral medulla Inhibition of Sympathetic Nerve Activity Inhibition of norepinephrine release Decrease in vasoconstriction Vasodilation  Lower BP
Sympatholytic Agents – Centrally-Acting Agents Methyldopa   ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents – Centrally-Acting Agents Methyldopa ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents – Centrally-Acting Agents Methyldopa ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents – Centrally-Acting Agents Methyldopa ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents – Centrally-Acting Agents Clonidine, Guanabenz, & Guanfacine  ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents – Centrally-Acting Agents Clonidine, Guanabenz, & Guanfacine ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents – Centrally-Acting Agents Clonidine, Guanabenz, & Guanfacine ,[object Object],[object Object]
Sympatholytic Agents – Adrenergic Neuron Blocking Agents ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents – Adrenergic Neuron Blocking Agents  Guanadrel ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents – Adrenergic Neuron Blocking Agents  Guanadrel ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents – Adrenergic Neuron Blocking Agents  Reserpine ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents – Adrenergic Neuron Blocking Agents  Reserpine ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytic Agents – Adrenergic Neuron Blocking Agents Guanethidine ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Angiotensin-Converting Enzyme Inhibitors ,[object Object],[object Object],[object Object],[object Object],[object Object]
Angiotensin-Converting Enzyme Inhibitors ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Angiotensin-Converting Enzyme Inhibitors ,[object Object],[object Object],[object Object],[object Object],[object Object]
Angiotensin-Converting Enzyme Inhibitors ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Angiotensin-Converting Enzyme Inhibitors ,[object Object],[object Object],[object Object],[object Object],[object Object]
Angiotensin-Converting Enzyme Inhibitors ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Angiotensin-Converting Enzyme Inhibitors 3-7 hours perindoprilat 75% / 35% * perindoprilat Perindopril 1.5 hours 13% Moexiprilat Moexipril 1 hour / 3 hours Ramiprilat Pamipril 2 hours / 25 hours 1hour / 2 hours Quinaprilat Quinapril 4-10 hours trandolaprilat 10% / 70% Trandolaprilat Trandolapril 11.5 hours Fosinoprilat 3 hours Fosinoprilat Fosinoprilat Glucoronide conjugate Fosinopril 10-11 hours benazeprilat 0.5-1 hr / 1-2 hours 35% Benazeprilat Glucuronide conjugates Benazepril 12 hours 7 hours 25% * Lisinopril-lysine analog of enalaprilat 1.3 hrs / 11 hrs 1 hrs / 3-4hrs 60% * Enalaprilat Enalapril 2 hours 1 hour 75% Disulfide dimers & cysteine disulfide Captopril Half-life Peak Plasma Concentration Bioavailability Metabolites Drugs
Angiotensin-Converting Enzyme Inhibitors ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Angiotensin-Converting Enzyme Inhibitors ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Angiotensin-Converting Enzyme Inhibitors ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
AT 1  Angiotensin II Receptor Antagonists ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
AT 1  Angiotensin II Receptor Antagonists ,[object Object],[object Object],[object Object],[object Object]
AT 1  Angiotensin II Receptor Antagonists liver 9 hours 2-4 hoours Valsartan Biliary  24 hours 0.5-1 hour Telmisartan Renal & biliary Olmesartan Between 10 & 15 hours 1.4-2.8 hours Olmesartan medoxomil Renal & hepatic EXP 3174 2.5 & 9 hours  1-3 hours Losartan Renal & biliary Glucuronide conjugate 11-15 hours 1.5-2 hours Irbisartan Renal & biliary Glucuronide conjugate 5-9 hours 1-2 hours Eprosartan Renal & biliary Candesartan 9 hours 3-4 hours Candesartan Cilexetil Elimination Metabolite Plasma Half-life Peak Plasma Concentration Drugs
AT 1  Angiotensin II Receptor Antagonists ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object]
Vasodilators ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Calcium Channel Blocking Drugs Hypotension, cardiac depression, edema 75-150ug/kg IV 80-160mg q 8 hrs angina, HTN, arrhythmia, migraine, CMP Verapamil Dizziness, flushing, nausea 75-150ug/kg IV 30-80mg q 6 hrs Angina, HTN Diltiazem Arrhythmia, nausea, dizziness 200-400mg od angina Misc. Bepridil Same as nifedipine 20mg od/bid angina Niterndipine Same as nifedipine 20-40mg q 8 h HTN Nisoldipine Headache, LBM 60mg q 4 hrs SAH, migraine Nimodipine Hypotension, dizziness, flushing, edema, nausea, Constipation,  20-40mg q 8 hrs Angina, HTN, migraine, CMP, Raynaud’s phenomenon Nifedipine Peripheral edema, HA, dizziness 20-40mg Angina, HTN, CHF Nicardipine HA, fatigue 2.5-10mg HTN Isradipine HA, dizziness 5-10mg HTN, CHF Felodipine HA, peripheral edema 5-10mg Angina, HTN Amlodipine Dihydropyridine  group Toxicity Dose Indication Drugs
 

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T herapy of hypertension1

  • 1. Florencia G. dela Cruz-Munsayac, MD, FPSECP, MBA, RMT THERAPY OF HYPERTENSION
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  • 6. Normal Regulation of Blood Pressure ABP = cardiac output x peripheral vascular resistance Regulating the volume of intravascular fluid Baroreflexes, act in combination with RAAS Local release of vasoactive substances from vascular endothelium
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  • 24. Sympatholytic Agents – β - Adrenergic Receptor Antagonists BETA – ADRENOCEPTOR BLOCKING DRUGS Nonselective Selective With alpha-blocking ability Nadolol Propranolol Timolol Sotalol Tetralol Pindolol Penbutolol Carteolol Alprenolol Dilevatol Oxyprenolol Atenolol Esmolol Metoprolol Bevantolol Bisoprolol Betaxolol Acebutolol (Practolol) Celiprolol Labetalol Bucindolol Carvedilol
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  • 59. Angiotensin-Converting Enzyme Inhibitors 3-7 hours perindoprilat 75% / 35% * perindoprilat Perindopril 1.5 hours 13% Moexiprilat Moexipril 1 hour / 3 hours Ramiprilat Pamipril 2 hours / 25 hours 1hour / 2 hours Quinaprilat Quinapril 4-10 hours trandolaprilat 10% / 70% Trandolaprilat Trandolapril 11.5 hours Fosinoprilat 3 hours Fosinoprilat Fosinoprilat Glucoronide conjugate Fosinopril 10-11 hours benazeprilat 0.5-1 hr / 1-2 hours 35% Benazeprilat Glucuronide conjugates Benazepril 12 hours 7 hours 25% * Lisinopril-lysine analog of enalaprilat 1.3 hrs / 11 hrs 1 hrs / 3-4hrs 60% * Enalaprilat Enalapril 2 hours 1 hour 75% Disulfide dimers & cysteine disulfide Captopril Half-life Peak Plasma Concentration Bioavailability Metabolites Drugs
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  • 65. AT 1 Angiotensin II Receptor Antagonists liver 9 hours 2-4 hoours Valsartan Biliary 24 hours 0.5-1 hour Telmisartan Renal & biliary Olmesartan Between 10 & 15 hours 1.4-2.8 hours Olmesartan medoxomil Renal & hepatic EXP 3174 2.5 & 9 hours 1-3 hours Losartan Renal & biliary Glucuronide conjugate 11-15 hours 1.5-2 hours Irbisartan Renal & biliary Glucuronide conjugate 5-9 hours 1-2 hours Eprosartan Renal & biliary Candesartan 9 hours 3-4 hours Candesartan Cilexetil Elimination Metabolite Plasma Half-life Peak Plasma Concentration Drugs
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  • 86. Calcium Channel Blocking Drugs Hypotension, cardiac depression, edema 75-150ug/kg IV 80-160mg q 8 hrs angina, HTN, arrhythmia, migraine, CMP Verapamil Dizziness, flushing, nausea 75-150ug/kg IV 30-80mg q 6 hrs Angina, HTN Diltiazem Arrhythmia, nausea, dizziness 200-400mg od angina Misc. Bepridil Same as nifedipine 20mg od/bid angina Niterndipine Same as nifedipine 20-40mg q 8 h HTN Nisoldipine Headache, LBM 60mg q 4 hrs SAH, migraine Nimodipine Hypotension, dizziness, flushing, edema, nausea, Constipation, 20-40mg q 8 hrs Angina, HTN, migraine, CMP, Raynaud’s phenomenon Nifedipine Peripheral edema, HA, dizziness 20-40mg Angina, HTN, CHF Nicardipine HA, fatigue 2.5-10mg HTN Isradipine HA, dizziness 5-10mg HTN, CHF Felodipine HA, peripheral edema 5-10mg Angina, HTN Amlodipine Dihydropyridine group Toxicity Dose Indication Drugs
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