PH1.27 Describe the mechanisms of action, types, doses, side effects, indications and contraindications of antihypertensive drugs and drugs used in shock
PH1.27 Describe the mechanisms of action, types, doses, side effects, indications and contraindications of antihypertensive drugs and drugs used in shock
Antidiuretics help control fluid balance by reducing urination. They are divided into three categories: antidiuretic hormone and analogues like vasopressin; natriuretics like thiazides that cause sodium excretion and water retention; and miscellaneous agents like carbamazepine. Antidiuretic hormone and analogues work by binding to V1 and V2 receptors, promoting water reabsorption and vasoconstriction/vasodilation. Natriuretics inhibit sodium transporters. Miscellaneous agents enhance antidiuretic hormone effects. Common uses include treating diabetes insipidus. Side effects of antidiuretic hormone include headaches and gastrointestinal issues.
The document is a student submission on the topic of haemostasis and coagulation to their pharmacology department. It provides an overview of haemostasis and the three stages of coagulation, describes various coagulants, anticoagulants, vitamin K, heparin and other agents used to control bleeding and clotting. The submission also reviews the mechanisms, uses and adverse effects of different coagulation and anticoagulation drugs.
This document discusses cardiac glycosides, a class of organic compounds that increase the force of heart contractions and decrease the heart rate. It notes that digoxin, digitoxin, bufotoxin, and ouabain are examples obtained from plants like Digitalis lanata and toad skin. The document explains that cardiac glycosides act on the sodium-potassium ATPase pump, directly affecting myocardial contractility and mildly constricting blood vessels. While having little effect on the central nervous system, they can cause diuresis in congestive heart failure patients. The document outlines mechanisms of action and lists arrhythmias and other adverse effects, then discusses uses and interactions with other drugs.
This document discusses antiarrhythmic drugs, which are used to treat irregular heart rhythms. It describes the different classes of antiarrhythmic drugs including membrane stabilizers, beta blockers, drugs that widen the action potential, and calcium channel blockers. The document provides examples of drugs in each class and explains their mechanisms of action, such as blocking sodium or calcium channels. It also discusses the pharmacokinetics of lidocaine and the uses and adverse effects of antiarrhythmic drugs.
Cardiovascular pharmacology
Cardiovascular (=Circulatory) system – heart and blood vessels
Arteries – transport blood to tissues
Capillaries – sites of exchange, fluid O2, CO2, nutrients etc.
Venules – collect blood from capillaries
Veins – transport blood back to heart
Blood moves within vessels – higher pressure to lower pressure
Resistance to flow depends on vessel diameter, length and viscosity of blood
This document discusses cardiotonic drugs, which increase the contractility of the cardiac muscle without increasing oxygen demand. It focuses on two main types - cardiac glycosides like digoxin, and phosphodiesterase inhibitors. Digoxin increases calcium levels in cardiac cells, strengthening contractions. It has a positive inotropic effect and is used to treat heart failure and arrhythmias. The document outlines the mechanisms, effects, dosing, interactions, toxicity and nursing considerations for digoxin and phosphodiesterase inhibitors.
This document provides information about antianginal drugs used to treat angina pectoris. It discusses the three main types of angina and describes the mechanisms of action and uses of various antianginal drug classes including nitrates, beta-blockers, calcium channel blockers, and potassium channel openers. Specific drugs discussed include nitroglycerin, isosorbide mononitrate, atenolol, metoprolol, nifedipine, and nicorandil. Nursing responsibilities related to administration and patient education for these antianginal medications are also reviewed.
Antidiuretics help control fluid balance by reducing urination. They are divided into three categories: antidiuretic hormone and analogues like vasopressin; natriuretics like thiazides that cause sodium excretion and water retention; and miscellaneous agents like carbamazepine. Antidiuretic hormone and analogues work by binding to V1 and V2 receptors, promoting water reabsorption and vasoconstriction/vasodilation. Natriuretics inhibit sodium transporters. Miscellaneous agents enhance antidiuretic hormone effects. Common uses include treating diabetes insipidus. Side effects of antidiuretic hormone include headaches and gastrointestinal issues.
The document is a student submission on the topic of haemostasis and coagulation to their pharmacology department. It provides an overview of haemostasis and the three stages of coagulation, describes various coagulants, anticoagulants, vitamin K, heparin and other agents used to control bleeding and clotting. The submission also reviews the mechanisms, uses and adverse effects of different coagulation and anticoagulation drugs.
This document discusses cardiac glycosides, a class of organic compounds that increase the force of heart contractions and decrease the heart rate. It notes that digoxin, digitoxin, bufotoxin, and ouabain are examples obtained from plants like Digitalis lanata and toad skin. The document explains that cardiac glycosides act on the sodium-potassium ATPase pump, directly affecting myocardial contractility and mildly constricting blood vessels. While having little effect on the central nervous system, they can cause diuresis in congestive heart failure patients. The document outlines mechanisms of action and lists arrhythmias and other adverse effects, then discusses uses and interactions with other drugs.
This document discusses antiarrhythmic drugs, which are used to treat irregular heart rhythms. It describes the different classes of antiarrhythmic drugs including membrane stabilizers, beta blockers, drugs that widen the action potential, and calcium channel blockers. The document provides examples of drugs in each class and explains their mechanisms of action, such as blocking sodium or calcium channels. It also discusses the pharmacokinetics of lidocaine and the uses and adverse effects of antiarrhythmic drugs.
Cardiovascular pharmacology
Cardiovascular (=Circulatory) system – heart and blood vessels
Arteries – transport blood to tissues
Capillaries – sites of exchange, fluid O2, CO2, nutrients etc.
Venules – collect blood from capillaries
Veins – transport blood back to heart
Blood moves within vessels – higher pressure to lower pressure
Resistance to flow depends on vessel diameter, length and viscosity of blood
This document discusses cardiotonic drugs, which increase the contractility of the cardiac muscle without increasing oxygen demand. It focuses on two main types - cardiac glycosides like digoxin, and phosphodiesterase inhibitors. Digoxin increases calcium levels in cardiac cells, strengthening contractions. It has a positive inotropic effect and is used to treat heart failure and arrhythmias. The document outlines the mechanisms, effects, dosing, interactions, toxicity and nursing considerations for digoxin and phosphodiesterase inhibitors.
This document provides information about antianginal drugs used to treat angina pectoris. It discusses the three main types of angina and describes the mechanisms of action and uses of various antianginal drug classes including nitrates, beta-blockers, calcium channel blockers, and potassium channel openers. Specific drugs discussed include nitroglycerin, isosorbide mononitrate, atenolol, metoprolol, nifedipine, and nicorandil. Nursing responsibilities related to administration and patient education for these antianginal medications are also reviewed.
This presentation deals with the beta blockers commonly used in day-to-day practice alongwith some interesting mnemonics to remember their names & site of action
This document discusses antihypertensive agents used to treat hypertension. It describes different categories of agents including adrenergic agents, ACE inhibitors, angiotensin II receptor blockers, calcium channel blockers, diuretics, and vasodilators. For each category, the document outlines mechanisms of action, examples of medications, therapeutic uses, and potential side effects. It emphasizes the importance of monitoring blood pressure during therapy and avoiding abruptly stopping medications.
This document discusses antianginal drugs used to treat angina pectoris. It describes the three main types of angina and the mechanisms of four classes of antianginal drugs: nitrates, beta-blockers, calcium channel blockers, and potassium channel openers. Nitrates like nitroglycerin and isosorbide are first-line treatments that work by dilating blood vessels to reduce cardiac preload and afterload. Proper administration and storage of nitrates is important to avoid side effects like headaches. Nurses monitor patients and educate them about safe use of antianginal medications.
Cardiac glycosides like digoxin are used to treat heart failure and cardiac arrhythmias. They work by inhibiting sodium-potassium ATPase, increasing intracellular calcium levels, and enhancing cardiac contractility. Common side effects include nausea, arrhythmias, and toxicity at high levels. While they were once a standard treatment, newer heart failure drugs like ACE inhibitors, ARBs, beta blockers, and diuretics are now preferred due to their better safety profiles. Digitalis remains an option when symptoms are not adequately controlled by other treatments.
Diuretics act at different sites along the nephron to promote the excretion of sodium, chloride, and water. The main classes are carbonic anhydrase inhibitors, loop diuretics, thiazides, potassium-sparing diuretics, and osmotic diuretics. They are used to treat conditions like edema, hypertension, and liver cirrhosis. Each class has a distinct mechanism of action and side effect profile. For example, loop diuretics inhibit sodium reabsorption in the loop of Henle but can cause ototoxicity, while thiazides target the distal tubule and cause hypokalemia. The site and mechanism of the drug determines its clinical applications and adverse effects
The document discusses the benefits of exercise for mental health. Regular physical activity can help reduce anxiety and depression and improve mood and cognitive function. Exercise causes chemical changes in the brain that may help protect against mental illness and improve symptoms.
Angina is a symptom of coronary artery disease that occurs when the heart muscle does not get enough oxygen-rich blood. It is usually felt as chest pain or discomfort when one engages in physical exertion or is exposed to stress. There are two main types - stable angina, which occurs predictably in relation to activity or stress, and unstable angina, which occurs unpredictably even at rest. Diagnosis involves electrocardiograms, stress tests, and coronary angiography to detect blockages in the arteries. Treatment focuses on lifestyle changes, medications to manage risk factors and symptoms, and procedures like angioplasty or bypass surgery in severe cases.
Hypolipidemic agents, also known as cholesterol-lowering drugs or antihyperlipidemic agents, are a diverse group of pharmaceuticals that are used in the treatment of high levels of fats (lipids), such as cholesterol, in the blood (hyperlipidemia). They are also called lipid-lowering drugs.
Cardiac arrhythmias can be caused by abnormalities in heart rate, rhythm, origin of impulses, or conduction. The main mechanisms are reentry, automaticity, parasystole, and triggered activity. Reentry requires two pathways that form a loop with a block in one pathway and slow conduction in the other. Common arrhythmias include atrial fibrillation, ventricular tachycardia, and supraventricular tachycardia. First-line drugs for treating arrhythmias include lignocaine, amiodarone, adenosine, beta-blockers, and calcium channel blockers. These drugs work via different mechanisms such as blocking sodium, potassium, or calcium channels to suppress arrhythmias.
Antiarrhythmic drugs are classified into four classes based on their mechanism of action and effects on cardiac action potentials. Class I drugs like quinidine and procainamide are sodium channel blockers. Class II includes beta blockers like propranolol. Class III prolongs repolarization by blocking potassium channels, represented by drugs like amiodarone and bretylium. Class IV calcium channel blockers like diltiazem and verapamil slow conduction in the atrioventricular node. These drugs work to normalize abnormal electrical activity in the heart and treat arrhythmias of various origins.
1. Arrhythmias occur when the heart beats too fast, too slow, or with an irregular rhythm due to problems with the heart's electrical conduction system.
2. Several classes of antiarrhythmic drugs are used to treat arrhythmias by blocking sodium, calcium, or potassium channels to suppress abnormal automaticity or conduction in the heart.
3. Common antiarrhythmic drugs include quinidine, mexiletine, flecainide, propranolol, amiodarone, dofetilide, verapamil and diltiazem. These drugs have different mechanisms of action and potential side effects like cardiac toxicity that require careful monitoring.
This document discusses antidiuretic drugs, which reduce urine volume. It describes various classes of antidiuretic agents including antidiuretic hormone (ADH/vasopressin), thiazide diuretics, and miscellaneous drugs. ADH is synthesized and released by the posterior pituitary gland and acts on V1 receptors in blood vessels and V2 receptors in kidney collecting ducts to increase water permeability and reduce urine volume. Desmopressin is a synthetic ADH analogue used to treat diabetes insipidus and bedwetting. Side effects of ADH include headache, flushing, and fluid retention. Thiazide diuretics and drugs like amiloride and indomethac
1) Hypertension is defined as a systolic blood pressure over 140 mm Hg or a diastolic over 90 mm Hg. Antihypertensive drugs are used to reduce high blood pressure.
2) There are several classes of antihypertensive drugs, including ACE inhibitors, calcium channel blockers, beta blockers, diuretics, and angiotensin receptor blockers.
3) The document provides details on the mechanisms of several classes of antihypertensive drugs and examples of drugs within each class, such as ACE inhibitors decreasing angiotensin II and calcium channel blockers inhibiting calcium influx into vascular smooth muscle cells.
This presentation consists of various approaches to treat hypertension depending on severity. It also include treatment according to international guidelines. Classification and brief description of each antihypertensive agent has been mentioned.
This document summarizes different types of adrenergic receptor antagonists or β-blockers. It describes:
1) Nonselective β-blockers that block both β1 and β2 receptors like propranolol, and cardioselective β1 blockers like metoprolol.
2) β-blockers with intrinsic sympathomimetic activity like pindolol that can minimize metabolic side effects.
3) Dual α and β-blockers like labetalol and carvedilol that are used to treat hypertension and heart failure.
The document discusses calcium channel blockers (CCBs), which are a class of antihypertensive drugs. CCBs work by blocking calcium channels, thereby relaxing blood vessels and reducing blood pressure. They are classified into phenylalkylamines, dihydropyridines, and benzothiazepines. CCBs are effective antihypertensives and are also used to treat angina by dilating coronary arteries and reducing oxygen demand of the heart. Their adverse effects include headaches, dizziness, and hypotension. CCBs are contraindicated in conditions like heart failure and bradycardia.
This document discusses antihyperlipidemic agents used to treat hyperlipidemia, a condition of high lipid levels in the blood. It begins by defining hyperlipidemia and describing its causes such as diet, genetics, and medical conditions. It then covers the main classes of antihyperlipidemic drugs like HMG CoA inhibitors, fibrates, bile acid sequesterants, and their mechanisms and examples like lovastatin, atorvastatin, clofibrate, and cholestyramine. The document concludes by explaining how these drugs work to lower lipid levels through inhibiting cholesterol synthesis and absorption or increasing lipid catabolism.
Hypertension is a common cardiovascular condition caused by persistently high blood pressure that damages organs. Antihypertensive drugs work via different mechanisms like inhibiting the renin-angiotensin-aldosterone system, blocking calcium channels, promoting sodium excretion with diuretics, and reducing sympathetic nervous system activity. Common classes of antihypertensives include ACE inhibitors, angiotensin receptor blockers, calcium channel blockers, diuretics, sympatholytics, and vasodilators. Treatment involves beginning with certain drug classes based on patient characteristics and guidelines, and escalating treatment by adding other classes as needed to control blood pressure. Antihypertensive drug choice is also based on minimizing adverse effects and avoiding
hypertension and pathophysiology and nursing interventionswajidullah9551
This document discusses diagnosis and management of hypertension. It defines hypertension and describes types, risk factors, causes, classification, goals of treatment, lifestyle modifications, and drug therapy options. The main points are:
- Hypertension is defined as blood pressure over 140/90 mmHg or taking medication for it. It can be primary or secondary.
- Risk factors include age, obesity, diabetes, lifestyle factors, and genetics. Secondary causes include renal, endocrine, and other issues.
- Treatment goals are to reduce blood pressure below 140/90 mmHg or 130/80 mmHg for those with diabetes or kidney disease.
- Lifestyle changes like diet, exercise, weight loss and limiting alcohol/
Hypertension is defined as blood pressure over 140/90 mmHg or taking medication for it. The document discusses diagnosis and management of hypertension including lifestyle modifications like weight loss, exercise, and diet changes as well as drug therapies. Drug classes discussed are diuretics, beta-blockers, ACE inhibitors, calcium channel blockers, and ARBs. Treatment is aimed at reducing blood pressure below 140/90 mmHg or 130/80 for those with diabetes or kidney disease to decrease risk of heart disease, stroke, kidney disease and other complications. Selection of drug depends on individual patient factors and conditions.
This presentation deals with the beta blockers commonly used in day-to-day practice alongwith some interesting mnemonics to remember their names & site of action
This document discusses antihypertensive agents used to treat hypertension. It describes different categories of agents including adrenergic agents, ACE inhibitors, angiotensin II receptor blockers, calcium channel blockers, diuretics, and vasodilators. For each category, the document outlines mechanisms of action, examples of medications, therapeutic uses, and potential side effects. It emphasizes the importance of monitoring blood pressure during therapy and avoiding abruptly stopping medications.
This document discusses antianginal drugs used to treat angina pectoris. It describes the three main types of angina and the mechanisms of four classes of antianginal drugs: nitrates, beta-blockers, calcium channel blockers, and potassium channel openers. Nitrates like nitroglycerin and isosorbide are first-line treatments that work by dilating blood vessels to reduce cardiac preload and afterload. Proper administration and storage of nitrates is important to avoid side effects like headaches. Nurses monitor patients and educate them about safe use of antianginal medications.
Cardiac glycosides like digoxin are used to treat heart failure and cardiac arrhythmias. They work by inhibiting sodium-potassium ATPase, increasing intracellular calcium levels, and enhancing cardiac contractility. Common side effects include nausea, arrhythmias, and toxicity at high levels. While they were once a standard treatment, newer heart failure drugs like ACE inhibitors, ARBs, beta blockers, and diuretics are now preferred due to their better safety profiles. Digitalis remains an option when symptoms are not adequately controlled by other treatments.
Diuretics act at different sites along the nephron to promote the excretion of sodium, chloride, and water. The main classes are carbonic anhydrase inhibitors, loop diuretics, thiazides, potassium-sparing diuretics, and osmotic diuretics. They are used to treat conditions like edema, hypertension, and liver cirrhosis. Each class has a distinct mechanism of action and side effect profile. For example, loop diuretics inhibit sodium reabsorption in the loop of Henle but can cause ototoxicity, while thiazides target the distal tubule and cause hypokalemia. The site and mechanism of the drug determines its clinical applications and adverse effects
The document discusses the benefits of exercise for mental health. Regular physical activity can help reduce anxiety and depression and improve mood and cognitive function. Exercise causes chemical changes in the brain that may help protect against mental illness and improve symptoms.
Angina is a symptom of coronary artery disease that occurs when the heart muscle does not get enough oxygen-rich blood. It is usually felt as chest pain or discomfort when one engages in physical exertion or is exposed to stress. There are two main types - stable angina, which occurs predictably in relation to activity or stress, and unstable angina, which occurs unpredictably even at rest. Diagnosis involves electrocardiograms, stress tests, and coronary angiography to detect blockages in the arteries. Treatment focuses on lifestyle changes, medications to manage risk factors and symptoms, and procedures like angioplasty or bypass surgery in severe cases.
Hypolipidemic agents, also known as cholesterol-lowering drugs or antihyperlipidemic agents, are a diverse group of pharmaceuticals that are used in the treatment of high levels of fats (lipids), such as cholesterol, in the blood (hyperlipidemia). They are also called lipid-lowering drugs.
Cardiac arrhythmias can be caused by abnormalities in heart rate, rhythm, origin of impulses, or conduction. The main mechanisms are reentry, automaticity, parasystole, and triggered activity. Reentry requires two pathways that form a loop with a block in one pathway and slow conduction in the other. Common arrhythmias include atrial fibrillation, ventricular tachycardia, and supraventricular tachycardia. First-line drugs for treating arrhythmias include lignocaine, amiodarone, adenosine, beta-blockers, and calcium channel blockers. These drugs work via different mechanisms such as blocking sodium, potassium, or calcium channels to suppress arrhythmias.
Antiarrhythmic drugs are classified into four classes based on their mechanism of action and effects on cardiac action potentials. Class I drugs like quinidine and procainamide are sodium channel blockers. Class II includes beta blockers like propranolol. Class III prolongs repolarization by blocking potassium channels, represented by drugs like amiodarone and bretylium. Class IV calcium channel blockers like diltiazem and verapamil slow conduction in the atrioventricular node. These drugs work to normalize abnormal electrical activity in the heart and treat arrhythmias of various origins.
1. Arrhythmias occur when the heart beats too fast, too slow, or with an irregular rhythm due to problems with the heart's electrical conduction system.
2. Several classes of antiarrhythmic drugs are used to treat arrhythmias by blocking sodium, calcium, or potassium channels to suppress abnormal automaticity or conduction in the heart.
3. Common antiarrhythmic drugs include quinidine, mexiletine, flecainide, propranolol, amiodarone, dofetilide, verapamil and diltiazem. These drugs have different mechanisms of action and potential side effects like cardiac toxicity that require careful monitoring.
This document discusses antidiuretic drugs, which reduce urine volume. It describes various classes of antidiuretic agents including antidiuretic hormone (ADH/vasopressin), thiazide diuretics, and miscellaneous drugs. ADH is synthesized and released by the posterior pituitary gland and acts on V1 receptors in blood vessels and V2 receptors in kidney collecting ducts to increase water permeability and reduce urine volume. Desmopressin is a synthetic ADH analogue used to treat diabetes insipidus and bedwetting. Side effects of ADH include headache, flushing, and fluid retention. Thiazide diuretics and drugs like amiloride and indomethac
1) Hypertension is defined as a systolic blood pressure over 140 mm Hg or a diastolic over 90 mm Hg. Antihypertensive drugs are used to reduce high blood pressure.
2) There are several classes of antihypertensive drugs, including ACE inhibitors, calcium channel blockers, beta blockers, diuretics, and angiotensin receptor blockers.
3) The document provides details on the mechanisms of several classes of antihypertensive drugs and examples of drugs within each class, such as ACE inhibitors decreasing angiotensin II and calcium channel blockers inhibiting calcium influx into vascular smooth muscle cells.
This presentation consists of various approaches to treat hypertension depending on severity. It also include treatment according to international guidelines. Classification and brief description of each antihypertensive agent has been mentioned.
This document summarizes different types of adrenergic receptor antagonists or β-blockers. It describes:
1) Nonselective β-blockers that block both β1 and β2 receptors like propranolol, and cardioselective β1 blockers like metoprolol.
2) β-blockers with intrinsic sympathomimetic activity like pindolol that can minimize metabolic side effects.
3) Dual α and β-blockers like labetalol and carvedilol that are used to treat hypertension and heart failure.
The document discusses calcium channel blockers (CCBs), which are a class of antihypertensive drugs. CCBs work by blocking calcium channels, thereby relaxing blood vessels and reducing blood pressure. They are classified into phenylalkylamines, dihydropyridines, and benzothiazepines. CCBs are effective antihypertensives and are also used to treat angina by dilating coronary arteries and reducing oxygen demand of the heart. Their adverse effects include headaches, dizziness, and hypotension. CCBs are contraindicated in conditions like heart failure and bradycardia.
This document discusses antihyperlipidemic agents used to treat hyperlipidemia, a condition of high lipid levels in the blood. It begins by defining hyperlipidemia and describing its causes such as diet, genetics, and medical conditions. It then covers the main classes of antihyperlipidemic drugs like HMG CoA inhibitors, fibrates, bile acid sequesterants, and their mechanisms and examples like lovastatin, atorvastatin, clofibrate, and cholestyramine. The document concludes by explaining how these drugs work to lower lipid levels through inhibiting cholesterol synthesis and absorption or increasing lipid catabolism.
Hypertension is a common cardiovascular condition caused by persistently high blood pressure that damages organs. Antihypertensive drugs work via different mechanisms like inhibiting the renin-angiotensin-aldosterone system, blocking calcium channels, promoting sodium excretion with diuretics, and reducing sympathetic nervous system activity. Common classes of antihypertensives include ACE inhibitors, angiotensin receptor blockers, calcium channel blockers, diuretics, sympatholytics, and vasodilators. Treatment involves beginning with certain drug classes based on patient characteristics and guidelines, and escalating treatment by adding other classes as needed to control blood pressure. Antihypertensive drug choice is also based on minimizing adverse effects and avoiding
Similar to PH1.27 Describe the mechanisms of action, types, doses, side effects, indications and contraindications of antihypertensive drugs and drugs used in shock
hypertension and pathophysiology and nursing interventionswajidullah9551
This document discusses diagnosis and management of hypertension. It defines hypertension and describes types, risk factors, causes, classification, goals of treatment, lifestyle modifications, and drug therapy options. The main points are:
- Hypertension is defined as blood pressure over 140/90 mmHg or taking medication for it. It can be primary or secondary.
- Risk factors include age, obesity, diabetes, lifestyle factors, and genetics. Secondary causes include renal, endocrine, and other issues.
- Treatment goals are to reduce blood pressure below 140/90 mmHg or 130/80 mmHg for those with diabetes or kidney disease.
- Lifestyle changes like diet, exercise, weight loss and limiting alcohol/
Hypertension is defined as blood pressure over 140/90 mmHg or taking medication for it. The document discusses diagnosis and management of hypertension including lifestyle modifications like weight loss, exercise, and diet changes as well as drug therapies. Drug classes discussed are diuretics, beta-blockers, ACE inhibitors, calcium channel blockers, and ARBs. Treatment is aimed at reducing blood pressure below 140/90 mmHg or 130/80 for those with diabetes or kidney disease to decrease risk of heart disease, stroke, kidney disease and other complications. Selection of drug depends on individual patient factors and conditions.
This document discusses the diagnosis and management of hypertension. It defines hypertension as blood pressure above 140/90 mmHg or being on antihypertensive medication. The main types are essential and secondary hypertension. Lifestyle modifications like weight loss, exercise, and diet changes can help control hypertension before starting medications. Common drug classes for treatment include diuretics, ACE inhibitors, calcium channel blockers, angiotensin receptor blockers, and beta blockers. The goals of treatment are to reduce target organ damage and cardiovascular risk by achieving a blood pressure under 140/90 mmHg or 130/80 mmHg for those with diabetes or chronic kidney disease.
Hypertension is defined as systolic blood pressure over 140 mmHg or diastolic over 90 mmHg. The document discusses the diagnosis, management, treatment, and goals of treating hypertension. Treatment involves lifestyle modifications like weight loss, reduced salt intake, exercise, as well as pharmacologic treatments including diuretics, ACE inhibitors, calcium channel blockers, and others. The goals of treatment are to reduce cardiovascular and renal morbidity and mortality by achieving a blood pressure under 140/90 mmHg or under 130/80 for those with diabetes or chronic kidney disease.
This document discusses the diagnosis and management of hypertension. It defines hypertension as blood pressure above 140/90 mmHg or being on antihypertensive medication. The main types are essential and secondary hypertension. Lifestyle modifications like weight loss, exercise, and diet changes can help control hypertension before starting medications. Common drug classes for treatment include diuretics, ACE inhibitors, calcium channel blockers, angiotensin receptor blockers, and beta blockers. The goals of treatment are to reduce target organ damage and cardiovascular risk by achieving a blood pressure under 140/90 mmHg or 130/80 mmHg for those with diabetes or chronic kidney disease.
Hypertension is defined as systolic blood pressure over 140 mmHg or diastolic over 90 mmHg. The document discusses the diagnosis, management, treatment, and goals of treating hypertension. Treatment involves lifestyle modifications like weight loss, reduced salt intake, exercise, as well as pharmacologic treatments including diuretics, ACE inhibitors, calcium channel blockers, and others. The goals of treatment are to reduce cardiovascular and renal morbidity and mortality by achieving a blood pressure under 140/90 mmHg or under 130/80 for those with diabetes or kidney disease.
Hypertension is defined as systolic blood pressure over 140 mmHg or diastolic over 90 mmHg. The document discusses the diagnosis, management, treatment, and goals of treating hypertension. Treatment involves lifestyle modifications like weight loss, reduced salt intake, exercise, as well as pharmacologic treatments including diuretics, ACE inhibitors, calcium channel blockers, and others. The goals of treatment are to reduce cardiac and renal morbidity and mortality by achieving a blood pressure under 140/90 mmHg or under 130/80 for those with diabetes or kidney disease.
Hypertension is defined as systolic blood pressure over 140 mmHg or diastolic over 90 mmHg. The document discusses the diagnosis, management, treatment, and goals of treating hypertension. Treatment involves lifestyle modifications like weight loss, reduced salt intake, exercise, as well as pharmacologic treatments including diuretics, ACE inhibitors, calcium channel blockers, and others. The goals of treatment are to reduce cardiovascular and renal morbidity and mortality by achieving a blood pressure under 140/90 mmHg or under 130/80 for those with diabetes or chronic kidney disease.
Hypertension is defined as systolic blood pressure over 140 mmHg or diastolic over 90 mmHg. The document discusses the diagnosis, management, and treatment of hypertension through lifestyle modifications and pharmacotherapy. Treatment aims to reduce target organ damage by achieving blood pressure targets of less than 140/90 mmHg or 130/80 mmHg for those with diabetes or chronic kidney disease through lifestyle changes like weight loss, exercise, and diet as well as drug therapy including diuretics, ACE inhibitors, calcium channel blockers, and others. Close monitoring is needed to ensure treatment goals are met and side effects are managed.
Hypertension is defined as systolic blood pressure over 140 mmHg or diastolic over 90 mmHg. The document discusses the diagnosis, management, treatment, and goals of treating hypertension. Treatment involves lifestyle modifications like weight loss, reduced salt intake, exercise, as well as pharmacologic treatments including diuretics, ACE inhibitors, calcium channel blockers, and others. The goals of treatment are to reduce cardiac and renal morbidity and mortality by achieving a blood pressure under 140/90 mmHg or under 130/80 for those with diabetes or kidney disease.
This document discusses the diagnosis and management of hypertension. It defines hypertension as blood pressure above 140/90 mmHg or being on antihypertensive medication. The main types are essential and secondary hypertension. Lifestyle modifications like weight loss, exercise, and diet changes can help control hypertension before starting medications. Common drug classes for treatment include diuretics, ACE inhibitors, calcium channel blockers, angiotensin receptor blockers, and beta blockers. The goals of treatment are to reduce target organ damage and cardiovascular risk by achieving a blood pressure under 140/90 mmHg or 130/80 mmHg for those with diabetes or chronic kidney disease.
This document discusses the diagnosis and management of hypertension. It defines hypertension as blood pressure above 140/90 mmHg or being on antihypertensive medication. The main types are essential and secondary hypertension. Lifestyle modifications like weight loss, exercise, and diet changes can help control hypertension before starting medications. Common drug classes for treatment include diuretics, ACE inhibitors, calcium channel blockers, angiotensin receptor blockers, and beta blockers. The goals of treatment are to reduce target organ damage and cardiovascular risk by achieving a blood pressure under 140/90 mmHg or 130/80 mmHg for those with diabetes or chronic kidney disease.
Hypertension is defined as systolic blood pressure over 140 mmHg or diastolic over 90 mmHg. The document discusses the diagnosis, management, treatment, and goals of treating hypertension. Treatment involves lifestyle modifications like weight loss, reduced salt intake, exercise, as well as pharmacologic treatments including diuretics, ACE inhibitors, calcium channel blockers, and others. The goals of treatment are to reduce cardiovascular and renal morbidity and mortality by achieving a blood pressure under 140/90 mmHg or under 130/80 for those with diabetes or chronic kidney disease.
This document discusses the diagnosis and management of hypertension. It defines hypertension as blood pressure above 140/90 mmHg or being on antihypertensive medication. The main types are essential and secondary hypertension. Lifestyle modifications like weight loss, exercise, and diet changes can help control hypertension before starting medications. Common drug classes for treatment include diuretics, ACE inhibitors, calcium channel blockers, angiotensin receptor blockers, and beta blockers. The goals of treatment are to reduce target organ damage and cardiovascular risk by achieving a blood pressure under 140/90 mmHg or 130/80 mmHg for those with diabetes or chronic kidney disease.
Hypertension is defined as systolic blood pressure over 140 mmHg or diastolic over 90 mmHg. The document discusses the diagnosis, management, and treatment of hypertension through lifestyle modifications and pharmacotherapy. Treatment aims to reduce target organ damage by achieving blood pressure targets of less than 140/90 mmHg or 130/80 mmHg for those with diabetes or chronic kidney disease through lifestyle changes like weight loss, exercise, and diet as well as drug therapy including diuretics, ACE inhibitors, calcium channel blockers, and others. Close monitoring is needed to ensure treatment goals are met and side effects are managed.
Hypertension is defined as systolic blood pressure over 140 mmHg or diastolic over 90 mmHg. The document discusses the diagnosis, management, treatment, and goals of treating hypertension. Treatment involves lifestyle modifications like weight loss, reduced salt intake, exercise, as well as pharmacologic treatments including diuretics, ACE inhibitors, calcium channel blockers, and others. The goals of treatment are to reduce cardiac and renal morbidity and mortality by achieving a blood pressure under 140/90 mmHg or under 130/80 for those with diabetes or kidney disease.
Hypertension is defined as blood pressure above 140/90 mmHg or taking antihypertensive medication. It can be essential or secondary hypertension. Treatment involves lifestyle modifications like weight loss, exercise, and diet changes as well as pharmacologic treatments. Drug therapy aims to reduce blood pressure below 140/90 mmHg or 130/80 mmHg for those with diabetes or kidney disease to decrease risk of heart disease and stroke. Treatment involves diuretics, ACE inhibitors, calcium channel blockers, beta blockers, and other drugs depending on individual factors. Goals are to control blood pressure and reduce target organ damage through lifestyle and medical treatment.
Hypertension is defined as blood pressure above 140/90 mmHg or taking antihypertensive medication. It can be essential or secondary hypertension. Treatment involves lifestyle modifications like weight loss, exercise, and diet changes as well as pharmacologic treatments. Drug therapy aims to reduce blood pressure below 140/90 mmHg or 130/80 mmHg for those with diabetes or kidney disease to decrease risk of heart disease and stroke. Treatment involves diuretics, ACE inhibitors, calcium channel blockers, beta blockers, and other drugs depending on individual factors. Goals are to control blood pressure and reduce target organ damage through lifestyle and medical treatment.
This document summarizes various antihypertensive drugs. It discusses the etiology and classification of hypertension. It then covers different classes of antihypertensive drugs including diuretics, ACE inhibitors, angiotensin receptor blockers, calcium channel blockers, beta blockers, vasodilators, and others. For each drug class and examples, it provides the mechanism of action, clinical uses, and potential adverse effects. Treatment of hypertension is important to prevent damage to organs and risk of other conditions.
Similar to PH1.27 Describe the mechanisms of action, types, doses, side effects, indications and contraindications of antihypertensive drugs and drugs used in shock (20)
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PH1.28 Describe the mechanisms of action, types, doses, side effects, indications and contraindications of the drugs used in ischemic heart disease (stable, unstable angina and myocardial infarction), peripheral vascular disease
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PH1.27 Describe the mechanisms of action, types, doses, side effects, indications and contraindications of antihypertensive drugs and drugs used in shock
1. PH1.27 Describe the mechanisms of action, types,
doses, side effects, indications and
contraindications of antihypertensive drugs and
drugs used in shock
Dr Pankaj Kumar Gupta, MD
Assistant Professor,
Department of Pharmacology,
ESIC Medical College & Hospital,
Faridabad (HARYANA) INDIA
2. Objectives
• Definition
• Blood pressure regulation
• Etiology of hypertension
• Classification of hypertension
• Prevalence of hypertension
• Classification of anti-hypertensive drugs
• Pharmacology of diuretics
• Pharmacology of ACE-I/ARBs
• Pharmacology of B & α blockers
• Pharmacology of CCBs
• Pharmacology of central sympatholytics
• Pharmacology of vasodilators
3. Hypertension
• Blood pressure is
a measurement of
the force exerted
against the walls
of arteries as
heart pumps
blood to body.
4. Blood Pressure
• A force exerted against the walls of arteries by
heart.
• Blood pressure is made up of two numbers:
– Systolic pressure is the pressure when the
ventricles pump blood out of the heart.
– Diastolic pressure is the pressure between
heartbeats when the heart is filling with blood.
• Normal blood pressure is when blood pressure
is lower than 120/80 mm Hg most of the time.
https://medlineplus.gov/ency/article/000468.htm
https://www.nhlbi.nih.gov/health/high-blood-pressure
5. Hydraulic equation of BP
BP = CO X PVR
Blood Pressure = Cardiac output (CO) X Resistance to passage
of blood through pre-capillary arterioles (PVR)
6. Normal Blood Pressure Regulation
• Physiologically CO and PVR is maintained minute to
minute by:
– Arterioles
– Post-capillary Venules
– Heart
– Kidney
• In hypertensives – Baroreflex and renal blood-
volume control system – set at higher level
• All antihypertensives act via interfering with
normal mechanisms
It is regulated by
Baroreflex
Humoral mechanism
Renin-angiotensin-aldosterone
system
Local agents like Nitric oxide
9. Etiology
Primary HTN/Essential Secondary HTN
•No identifiable cause
•90-95% of cases
•Caused by an underlying condition
•Sleep apnea
•Drug-induced
•Chronic kidney disease
•Primary aldosteronism
•Renovascular disease
•Chronic steroid therapy and
Cushing’s syndrome
•Pheochromocytoma
•Coarctation of the aorta
•Thyroid or parathyroid disease
10. Classification of Hypertension
Category Systolic
(mmHg)
Diastolic
(mmHg)
Normal < 120 AND < 80
Pre-hypertension 120-139 OR 80-89
Hypertension
Stage-I 140-159 OR 90-99
Stage-II ≥160 OR ≥100
JNC – 8 Classification of BP
11. Prevalence
• It is estimated that at least one in four adults
in India has hypertension, but, only about 12%
of them have their blood pressure under
control.
• Uncontrolled blood pressure is one of the
main risk factors for cardiovascular diseases
(CVDs) such as heart attacks and stroke, and
are responsible for one-third of total deaths in
India.
https://www.who.int/india/news/detail/02-06-2022-india-hypertension-control-initiative--a-high-impact-and-low-cost-
solution#:~:text=It%20is%20estimated%20that%20at,blood%20pressure)%20by%2020253.
https://www.who.int/india/health-topics/hypertension
12. Classification of Anti-hypertensive Drugs
SN Drug Class Drug Examples
1 Diuretics •Thiazides: Hydrochorothazide, Chlorthalidone, Indapamide
•High ceiling: Furosemide
•K+Sparing: Spiranolactone, Amiloride, Eplerenone
2 ACE inhibitors Captopril, Enalapril, Lisinopril, Ramipril, Fosinopril
3 Angiotensin (AT 1
receptor) blockers
Losartan, Candesartan, Valsartan, Telmisartan, Irbesartan,
Olmesartan
4 Direct renin inhibitor Aliskiren
5 Calcium channel
blockers
Phenylalkylamine: Verapamil
Benzothiazepine: Diltiazem
Dihydropyridines: Nifedipine, Amlodipine, Cilnidipine
13. Classification of Anti-hypertensive Drugs
SN Drug Class Drug Examples
6 β-Adrenergic blockers Propranolol, Metoprolol, Atenolol
7 β+α Adrenergic
blockers
Labetalol, Carvedilol
8 α-Adrenergic blockers Prazosin, Terazosin, Doxazosin, Phentolamine
9 Central
sympatholytics
Clonidine, Methyldopa, Phenoxybenzamine
10 Vasodilators Arteriolar: Hydralazine, Minoxidil, Diazoxide
Arteiolar +Venous: Sodium nitroprusside
14. Diuretics
• Used as initial therapy alone or in combination with
drugs from other groups
• MOA: acts on Kidneys to increase excretion of Na
and H2O – decrease in blood volume – decreased
BP
– Thiazides: chlorothiazide, hydrochorothiazide
– Loop Diuretics: furosemide, bumetanide, ethacrynic
acid
– Potassium sparing diuretics: spironolactone,
triamterene, amiloride
15. Ter Maaten JM, et al, Nat Rev Cardiol. 2015;12(3):184-192.
16. Effects
Mechanism of
action
Diuretics
•Urinary Na, K, Ca, Mg
•Na/K/2Cl transporter in
TAL the most effective
Loop diuretics
Furosemide
•Urinary Na, K, Mg
•BUT↓ urinary Ca (hypercalcemia)
•Metabolic alkalosis
•Na and Cl cotransporter in
DCT
Thiazide diuretics
Hydrochlorothiazide
•↑ Urinary Na
•↓ K, H secretion
•Metabolic acidosis
•Competitive antagonist of
aldosterone in CCT
K-sparing diuretic
Spironolactone
•Urinary Na HCO3, K
•Urinary alkalosis
•Metabolic acidosis
•Inhibition of NaHCO3
reabsorption in PCT
CA inhibitors
Acetohexamide
Dorzolamide
•Urine excretion
•Little Na
•Osmotic effect in PCT
Osmotic diuretic
Mannitol
19. Pharmacology of ACE inhibitors Captopril
• Captopril, the first ACE
inhibitor to be
marketed, is a potent
ACE inhibitor. It is the
only ACE inhibitor
approved for use in
the U.S. that contains
a sulfhydryl moiety.
Mechanism of action
20. Pharmacokinetics
Absorption: •Given orally, absorbed rapidly
•Bioavailability 75%.
•Bioavailability is reduced by 25-30% with food, so Captopril
should be given 1 hour before meals.
Distribution •Peak concentrations in plasma occur within an hour
•Drug is cleared rapidly with a t1/2 2 hours.
Metabolism: •Partially metabolized.
Excretion: •Most of the drug is eliminated in urine,
•40-50% as captopril and the rest as captopril disulfide dimers
and captopril–cysteine disulfide
Dose: •6.25-150 mg orally, two to three times daily.
22. Angiotensin (AT 1 receptor) blocker
Losartan
• Approximately 14% of
an oral dose of losartan
is converted to the 5-
carboxylic acid
metabolite EXP 3174,
which is more potent
than losartan as an AT1
receptor antagonist.
23. Pharmacokinetics
Absorption: •Oral absorption is not affected by food
•Bioavailability is only 33% due to first pass metabolism
Distribution •Peak plasma levels of losartan and EXP3174 (active metabolite)
occur~1-3 hours
•Plasma half-lives are 2.5 and 6-9 hours, respectively.
Metabolism: •The metabolism of losartan to EXP3174 and to inactive
metabolites is mediated by CYP2C9 and CYP3A4.
Excretion: •The plasma clearances of losartan and EXP3174 are due to
renal clearance and hepatic clearance
Dose: •Orally once or twice daily for a total daily dose of 25-100 mg.
25. Pharmacology of Calcium Channel
Blocker Verapamil
Mechanism of action
• Voltage-sensitive Ca++ channels (L type or slow channels)
mediate the entry of extracellular Ca++ into smooth muscle
and cardiac myocytes and sinoatrial (SA) and atrio-ventricular
(AV) nodal cells in response to electrical depolarization.
• In both smooth muscle and cardiac myocytes, Ca++ is a trigger
for contraction. Ca++ channel antagonists, also called Ca++
entry blockers, inhibit Ca++ channel function.
• In vascular smooth muscle, this leads to relaxation, especially
in arterial beds. These drugs also may produce negative
inotropic and chronotropic effects in the heart.
26. Pharmacokinetics
Absorption: •Absorption is nearly complete after oral administration.
•Bioavailability is reduced, in some cases markedly, by first pass
hepatic metabolism.
•Intravenous administration of diltiazem or verapamil leads to a rapid
therapeutic response.
Distribution •Plasma protein binding is 70-98% for all CCBs;
Metabolism: •A major metabolite of diltiazem is des acetyl diltiazem, which has
about one-half of diltiazem's potency as a vasodilator.
•N-Demethylation of verapamil results in production of norverapamil,
which is biologically active but much less potent than the parent
compound.
•The t1/2 of norverapamil is~10hours.
Excretion: Their elimination half-lives vary widely and range from 1.3-64 hours
Dose: Amlodipine- 2.5-10 mg OD
27. Adverse effects •Constipation, Pretibial edema, Nausea, Flushing, and
Dizziness.
•Heart failure, AV blockade, Sinus node depression; these
are most common with verapamil and least common with
the dihydropyridines.
Uses 1.Hypertension
2.Cardiac arrhythmias
3.Hypertrophic cardiomyopathy
28. Pharmacology of β-blocker
(Propranolol)
Mechanism of action
• The negative Chronotropic and Inotropic effects of these agents (and the
reductions in heart rate, stroke volume, and cardiac output that follow)
account for the initial anti-hypertensive effect of the ß-antagonists.
• Decreased vasomotor tone, with a consequent decrease in systemic
vascular resistance, with longer-term therapy.
• Antagonism of ß1-adrenergic receptors in the kidney decreases secretion
of renin and thereby decreases production of the potent vasoconstrictor,
angiotensin II.
• On acute use- little change in BP, no direct action on blood vessels
• On chronic use- gradual fall in BP (1-3 wk) due to ↓ tpr in response to
↓CO, both SBP & DBP falls.
29.
30. Pharmacokinetics
Absorption: •Well absorbed orally
•Low bioavailability (BA) due to high first pass metabolism.
•Oral: Parenteral = 40:1
•BA is high when taken with meal as food ↓ first pass
metabolism
Distribution •>90% bound to plasma proteins.
•Lipophilic and penetrates in brain.
Metabolism: •Dependent on hepatic blood flow
•Repeat adm increases BA as propranolol ↓ HBF
•Many metabolites, Hydroxylated metabolite has ß-blocking
action.
Excretion: •Metabolites are excreted via urine mostly glucuronides.
Dose: •Oral-10 mg BD to 160 mg QID
•IV- 2-5 mg over 10 min
•IM/SC- no due to irritant property
31. Adverse effects •Cardiovascular adverse effects- bradycardia, atrio-ventricular
blockade and heart failure. (due to β-blockade)
•Patients with airway disease may suffer severe asthma attacks.
•Symptoms of hypoglycemia from insulin overdosage, for example,
tachycardia, tremor, and anxiety, may be masked.
•B-blockers block adrenergically induced lipolysis & glycogenolysis
resulting in hyperlipidemia, hypertryglyceridemia & hypoglycemia.
•Tiredness & reduced exercise capacity (due to blunting of B2
mediated blood flow to muscles)
•Cold hand & feet in winter (blunting of vasodilator B2 receptors
•Rebound hypertension in case of abrupt withdrawal
•CNS adverse effects include sedation, fatigue, and sleep alterations.
•Sexual dysfunction has been reported for most of the β-blockers in
some patients.
Interactions 1.Digitalis+Prpranolol=Depression of Sinus node and AV conduction,
cardiac arrest can occur
2.Delays recovery from hypoglyacemic effect of insulin
3.Indomethacin and other NSAIDs attenuate anti-hypertensive action.
4.Cimetidine inhibits its metabolism
32. Uses 1. Hypertension
2. Angina pectoris
3. Cardiac Arrhythmias
4. Myocardial Ischemia (MI)
5. Congestive Heart Failure (CHF)
6. Dissecting aortic aneurysm
7. Pheochromocytoma
8. Thyrotoxicosis
9. Migraine
10. Anxiety
11. Essential tremor
12. Glaucoma
13. Hypertrophic Obstructive Cardiomyopathy (HOCM)
Current Status •Mild anti-hypertensives
•Suffice in 30-40% of populations
•Response takes 1-3 weeks
•OD dosing is sufficient for most B-blockers (24 hrs action)
33. Pharmacology of α-Adrenergic
blockers (Prazosin)
Mechanism of action
• Blockade of α1 adrenergic receptors inhibits
vasoconstriction induced by endogenous
catecholamines; vasodilation may occur in both
arteriolar resistance vessels and veins.
• Blockade of α1 receptors also inhibits vasoconstriction
and the increase in blood pressure produced by the
administration of a sympathomimetic amine. The pattern
of effects depends on the adrenergic agonist that is
administered.
34. Pharmacokinetics
Absorption: •Well absorbed after oral administration, and
bioavailability is 50-70%.
•Peak concentrations in 1-3 hours after an oral dose.
Distribution •High plasma proteins bound (primarily α1-acid
glycoprotein)
•Only 5% of the drug is free in the circulation
Metabolism: •Extensively metabolized in the liver
Excretion: •Little unchanged drug excreted by the kidneys
•The plasma t1/2 is 3 hours (may be prolonged to 6-8
hours in congestive heart failure)
35. Adverse effects ‘First dose effect’ may cause dizziness and fainting.
Uses 1.Hypertension
2.Raynaud’sdisease
3.Benign Hypertrophy of Prostrate (BHP) Terazosin, Doxazosin and
Uroselective α1A & α1B blocker Tamsulosin is used
4.Pheochromocytoma
36. Pharmacology of β+α Adrenergic
blockers (Carvedilol)
Mechanism of action
• It blocks β1, β2, and α1 receptors similarly to labetalol, but
also has anti-oxidant and anti-inflammatory effects.
• It has membrane stabilizing activity but it lacks intrinsic
sympathomimetic activity. Carvedilol produces
vasodilation.
• Additional properties (e.g. anti-oxidant and anti-
inflammatory effects) may contribute to the beneficial
effects seen in treating congestive heart failure and in its
cardio protective effects.
• The drug is FDA-approved for use in hypertension,
congestive heart failure, and left ventricular dysfunction
following MI.
37. • Carvedilol is extremely liphophic and is able to
protect cell membranes from lipid peroxidation. It
prevents low density lipoprotein (LDL) oxidation.
• Carvedilol also inhibits ROS-mediated loss of
myocardial contractility, stress-induced
hypertrophy, apoptosis, and the accumulation
and activation of neutrophils.
• Labetalol is 5 times more potent in blocking β
than α receptor
38. Pharmacokinetics
Absorption: •Rapidly absorption
•Peak plasma concentrations in1-2 hours.
Distribution •Highly lipophilic and thus is extensively distributed into
extravascular tissues.
•>95%protein bound.
Metabolism: •Extensively metabolized in the liver, predominantly by
•CYP2D6 and CYP2C9.
•t1/2 is 7-10 hours
•Stereo selective first-pass metabolism results in more rapid
clearance of S(–)-carvedilol than R(+)-carvedilol.
•Because of carvedilol's extensive oxidative metabolism by
the liver, its pharmacokinetics can be profoundly affected by
drugs that induce or inhibit oxidation. These include the
inducer, rifampin, and inhibitors such as cimetidine,
quinidine, fluoxetine, and paroxetine
Excretion: Kidney
40. Pharmacology of Central
Sympatholytics
Clonidine
• Clonidine is a α2 receptors agonist
Mechanism of action
• Activation of α2 receptors in the lower brainstem region.
• Decreases discharges in sympathetic pre-ganglionic fibers
in the splanchnic nerve and in postganglionic fibers of
cardiac nerves.
• Also, stimulates parasympathetic outflow thus, slowing of
heart rate as a consequence of increased vagal tone and
diminished sympathetic drive.
• Activation of pre-synaptic α-2 receptors that suppress the
release of NE from postganglionic sympathetic nerves.
41. Pharmacokinetics
Absorption: •Well absorbed
•Bioavailability is nearly 100%
Distribution •Peak concentration in plasma and maximal
hypotensive effect are observed 1-3 hours after
an oral dose.
Metabolism: t1/2 of the drug ranges from 6-24 hours, with a
mean of~12hours.
Excretion: •About half of an administered dose can be
recovered unchanged in the urine
42. Adverse effects •Dry mouth and sedation
•Sexual dysfunction
•Marked bradycardia
•About 15-20% of patients develop contact dermatitis when using
clonidine in the transdermal system
•Withdrawal reactions follow abrupt discontinuation of long-term
therapy
Uses •Hypertension
•Opioid withdrawal
43. Pharmacology of Vasodilators
Arteriolar: Hydralazine
• Hydralazine (1-hydrazinophthalazine) was one of the first orally
active antihypertensive drugs to be marketed in the U.S
Mechanism of action
• Hydralazine directly relaxes arteriolar smooth muscle.
• There is evidence suggesting that hydralazine inhibits IP3-induced
release of Ca++ from intracellular storage sites in arteries, leading to
diminished contraction.
• There is also evidence that hydralazine promotes arterial dilation by
opening high conductance Ca++ -activated K+ channels.
Uses
• Moderate to severe hypertension not controlled by first line drugs.
• Hypertension in pregnancy
44. Pharmacokinetics
• Well absorbed , but the systemic bioavailability is low (16%
in fast acetylators and 35% in slow acetylators).
• Hydralazine is N-acetylated in the bowel and/or the liver.
• t1/2 of hydralazine is 1 hour, and systemic clearance of the
drug is ~50 mL/kg/min.
Averse effects
• Headache, nausea, flushing, hypotension, palpitations,
tachycardia, dizziness, and angina pectoris.
• Myocardial ischemia
• Lupus syndrome is the most common.
• Illness that resembles serum sickness, hemolytic anemia,
vasculitis, and rapidly progressive glomerulonephritis.
45. Pharmacology of Vasodilator
Arteiolar+Venous: Sodium nitroprusside
Mechanism of action
• Nitroprusside is a nitrovasodilator that acts by releasing NO.
• NO activates the guanylylcyclase-cGMP PKG pathway, leading to
vasodilation, mimicking the production of NO by vascular endothelial cells,
which is impaired in many hypertensive patients.
Pharmacokinetics
• Sodium nitroprusside is an unstable molecule that decomposes under
strongly alkaline conditions or when exposed to light.
• It is given by continuous intravenous infusion to be effective.
• The metabolism of nitroprusside by smooth muscle is initiated by its
reduction, which is followed by the release of cyanide and then NO.
• Cyanide is further metabolized by liver rhodanase to form thiocyanate,
which is eliminated almost entirely in the urine.
46. Adverse effects
• Due to excessive vasodilation, with hypotension.
• Less commonly, toxicity may result from conversion of
nitroprusside to cyanide and thiocyanate.
• Toxic accumulation of cyanide leading to severe lactic
acidosis.
Uses
• Used to produce controlled hypertension in CHF, pump
failure, etc.
Brands
• SONIDE, PRUSIDE, 50 mg in 5 ml inj.