This document discusses several classes of drugs that act on adrenergic receptors or ganglia: alpha adrenoceptor antagonists, beta adrenoceptor antagonists, and ganglion-blocking drugs. It provides details on the pharmacological effects, clinical uses, and adverse effects of representative drugs within each class. The document is intended to serve as a comprehensive overview and reference for these drug categories.
Adrenergic blockers, also known as sympatholytics, are drugs that bind to adrenergic receptors but do not trigger the usual intracellular effects. They have the opposite effect of adrenergic agents and block alpha and beta receptor sites. Major classes include alpha blockers, beta blockers, and drugs that affect neurotransmitter release or uptake. Alpha blockers are further divided into non-selective, alpha1-selective, and drugs with additional beta blocking effects. Beta blockers include non-selective, cardioselective, and those with partial agonist activity. Drugs like reserpine and guanethidine deplete neurotransmitters from adrenergic nerves by blocking storage or release.
Adrenergic blockers, also known as sympatholytics, are drugs that bind to adrenergic receptors but do not trigger the usual intracellular effects. They have the opposite effect of adrenergic agents and block alpha and beta receptor sites. Major classes include alpha blockers, beta blockers, and drugs that affect neurotransmitter release or uptake. Alpha blockers are further divided into non-selective, alpha1-selective, and drugs with additional beta blocking effects. Beta blockers include non-selective, cardioselective, and those with partial agonist activity. Drugs like reserpine and guanethidine deplete neurotransmitters from nerve endings. Common uses are for hypertension, angina, migraine and
Adrenergic blockers work by binding to adrenergic receptors and preventing the action of adrenergic drugs. They can block alpha receptors, beta receptors, or both. Alpha blockers are classified as non-selective or selective. Prazosin is a highly selective alpha-1 blocker used to treat hypertension and benign prostatic hypertrophy. Beta blockers decrease heart rate, contraction force and blood pressure. They are used to treat hypertension, angina, arrhythmias and other conditions. Labetalol blocks both alpha-1 and beta receptors and is used to treat hypertension and hypertensive emergencies.
Vasodilators and beta blockers are drugs that relax blood vessels or interfere with sympathetic nervous system response to lower blood pressure. Specific agents include metoprolol, labetalol, and esmolol beta blockers. Alpha blockers like prazosin work by blocking alpha-1 receptors to cause vasodilation. Angiotensin converting enzyme (ACE) inhibitors and angiotensin receptor blockers (ARBs) prevent the formation or effects of angiotensin II to lower blood pressure. Calcium channel blockers like amlodipine and nifedipine work by inhibiting calcium influx into vascular smooth muscle cells to cause vasodilation. Each class of drug has different mechanisms, pharmac
The document discusses adrenal receptor antagonists, classifying them as alpha or beta antagonists and describing their selectivity, mechanisms of action, pharmacokinetics, clinical uses, and adverse effects. Alpha antagonists are used to treat hypertension and benign prostatic hyperplasia, while beta blockers are commonly used for cardiovascular conditions like hypertension, angina, and arrhythmias. The document provides details on specific drugs in each class, their properties, and factors like receptor selectivity and half-life that determine clinical applications.
This document discusses adrenal receptor antagonists or adrenergic receptor blockers. It describes their classification based on receptor selectivity, including alpha and beta receptor subtypes. It covers topics like mechanisms of action, pharmacokinetics, effects, uses and adverse effects of various alpha and beta blocking drugs. Key drugs discussed include prazosin, doxazosin, propranolol, metoprolol, atenolol and others. It provides a detailed overview of these important cardiovascular drug classes.
The document discusses different types of beta blockers and their mechanisms and uses:
- Cardioselective beta blockers like esmolol and propranolol lower blood pressure and increase exercise tolerance but have less effect on pulmonary function and metabolism than non-selective blockers. They are useful for hypertension in patients with lung issues.
- Beta blockers with intrinsic sympathomimetic activity (ISA) like acebutolol and pindolol weakly stimulate beta receptors in addition to blocking them, diminishing their effect on heart rate and output. They have less metabolic side effects and are used for hypertension in patients with bradycardia.
- Alpha-beta blockers like labetalol and carved
These are the drugs which antagonize the receptor action of adrenaline and related drugs.
These drugs act by blocking a and/or ß-adrenergic receptors.
α-blockers
PRAZOSIN is a competitive antagonist effective in the management of hypertension. Similar drugs with longer half-lives (e.g. doxazosin, terazosin).
β-blockers
Heart - Decrease heart rate, force of contraction and cardiac output.
Blood Pressure - Decrease in blood pressure (blockage).
Respiratory System – bronchoconstriction.
Eye – Beta-blocking agents reduce intraocular pressure, especially in glaucoma. The mechanism usually reported is decreased aqueous humor production.
Metabolic - Increase LDL and decrease HDL.
Uterus - Relaxation of uterus.
Local anaesthetic - Propranolol has some local anaesthetic action
Adrenergic blockers, also known as sympatholytics, are drugs that bind to adrenergic receptors but do not trigger the usual intracellular effects. They have the opposite effect of adrenergic agents and block alpha and beta receptor sites. Major classes include alpha blockers, beta blockers, and drugs that affect neurotransmitter release or uptake. Alpha blockers are further divided into non-selective, alpha1-selective, and drugs with additional beta blocking effects. Beta blockers include non-selective, cardioselective, and those with partial agonist activity. Drugs like reserpine and guanethidine deplete neurotransmitters from adrenergic nerves by blocking storage or release.
Adrenergic blockers, also known as sympatholytics, are drugs that bind to adrenergic receptors but do not trigger the usual intracellular effects. They have the opposite effect of adrenergic agents and block alpha and beta receptor sites. Major classes include alpha blockers, beta blockers, and drugs that affect neurotransmitter release or uptake. Alpha blockers are further divided into non-selective, alpha1-selective, and drugs with additional beta blocking effects. Beta blockers include non-selective, cardioselective, and those with partial agonist activity. Drugs like reserpine and guanethidine deplete neurotransmitters from nerve endings. Common uses are for hypertension, angina, migraine and
Adrenergic blockers work by binding to adrenergic receptors and preventing the action of adrenergic drugs. They can block alpha receptors, beta receptors, or both. Alpha blockers are classified as non-selective or selective. Prazosin is a highly selective alpha-1 blocker used to treat hypertension and benign prostatic hypertrophy. Beta blockers decrease heart rate, contraction force and blood pressure. They are used to treat hypertension, angina, arrhythmias and other conditions. Labetalol blocks both alpha-1 and beta receptors and is used to treat hypertension and hypertensive emergencies.
Vasodilators and beta blockers are drugs that relax blood vessels or interfere with sympathetic nervous system response to lower blood pressure. Specific agents include metoprolol, labetalol, and esmolol beta blockers. Alpha blockers like prazosin work by blocking alpha-1 receptors to cause vasodilation. Angiotensin converting enzyme (ACE) inhibitors and angiotensin receptor blockers (ARBs) prevent the formation or effects of angiotensin II to lower blood pressure. Calcium channel blockers like amlodipine and nifedipine work by inhibiting calcium influx into vascular smooth muscle cells to cause vasodilation. Each class of drug has different mechanisms, pharmac
The document discusses adrenal receptor antagonists, classifying them as alpha or beta antagonists and describing their selectivity, mechanisms of action, pharmacokinetics, clinical uses, and adverse effects. Alpha antagonists are used to treat hypertension and benign prostatic hyperplasia, while beta blockers are commonly used for cardiovascular conditions like hypertension, angina, and arrhythmias. The document provides details on specific drugs in each class, their properties, and factors like receptor selectivity and half-life that determine clinical applications.
This document discusses adrenal receptor antagonists or adrenergic receptor blockers. It describes their classification based on receptor selectivity, including alpha and beta receptor subtypes. It covers topics like mechanisms of action, pharmacokinetics, effects, uses and adverse effects of various alpha and beta blocking drugs. Key drugs discussed include prazosin, doxazosin, propranolol, metoprolol, atenolol and others. It provides a detailed overview of these important cardiovascular drug classes.
The document discusses different types of beta blockers and their mechanisms and uses:
- Cardioselective beta blockers like esmolol and propranolol lower blood pressure and increase exercise tolerance but have less effect on pulmonary function and metabolism than non-selective blockers. They are useful for hypertension in patients with lung issues.
- Beta blockers with intrinsic sympathomimetic activity (ISA) like acebutolol and pindolol weakly stimulate beta receptors in addition to blocking them, diminishing their effect on heart rate and output. They have less metabolic side effects and are used for hypertension in patients with bradycardia.
- Alpha-beta blockers like labetalol and carved
These are the drugs which antagonize the receptor action of adrenaline and related drugs.
These drugs act by blocking a and/or ß-adrenergic receptors.
α-blockers
PRAZOSIN is a competitive antagonist effective in the management of hypertension. Similar drugs with longer half-lives (e.g. doxazosin, terazosin).
β-blockers
Heart - Decrease heart rate, force of contraction and cardiac output.
Blood Pressure - Decrease in blood pressure (blockage).
Respiratory System – bronchoconstriction.
Eye – Beta-blocking agents reduce intraocular pressure, especially in glaucoma. The mechanism usually reported is decreased aqueous humor production.
Metabolic - Increase LDL and decrease HDL.
Uterus - Relaxation of uterus.
Local anaesthetic - Propranolol has some local anaesthetic action
This document discusses adrenergic receptors and their classification into alpha and beta receptors. It describes the differences between alpha and beta adrenergic receptors and provides details about various types of drugs that act as adrenergic antagonists including:
- Alpha blockers which are used to treat hypertension and benign prostatic hyperplasia. They cause vasodilation and reduce blood pressure. Examples include prazosin and doxazosin.
- Beta blockers which are classified as non-selective or cardioselective. Non-selective blockers are contraindicated in asthma while cardioselective blockers reduce their side effects. Examples of beta blockers mentioned are propranolol and atenolol.
This document summarizes beta-adrenergic blockers (beta blockers). It describes that beta blockers are drugs that bind to beta receptors in the sympathetic nervous system to block the effects of epinephrine and norepinephrine. There are two main types of beta receptors, beta 1 and beta 2. Beta blockers are either cardioselective (blocking beta 1) or non-selective (blocking both beta 1 and beta 2). Common uses of beta blockers include treating hypertension, angina, myocardial infarction, and glaucoma. Side effects can include fatigue, dizziness, bronchospasm, and sexual dysfunction.
Beta-blockers are a class of drugs that are used to manage various cardiac conditions by blocking the effects of epinephrine and other stress hormones on beta receptors. They were first developed in the 1950s and revolutionized cardiology. Beta-blockers are indicated for conditions like hypertension, arrhythmias, heart attack, and glaucoma. While they provide important benefits, they can also cause adverse effects like fatigue, dizziness, and bronchospasm. Different beta-blockers have varying levels of selectivity for beta-1 versus beta-2 receptors and some have additional alpha-blocking properties. Guidelines provide recommendations on the appropriate use of specific beta-blockers for different cardiac indications.
1. Prazosin is a potent and selective α1 adrenergic receptor blocker used to treat hypertension. It has a first-dose phenomenon that can cause severe hypotension, so the initial dose should be small.
2. Beta blockers block the effects of sympathetic stimulation by competitively blocking beta receptors. They are used to treat hypertension, angina, migraines, hyperthyroidism and other conditions. Common side effects include bradycardia, heart block, bronchospasm and hypoglycemia.
3. Drug interactions can occur between beta blockers and calcium channel blockers, local anesthetics, or bile acid sequestering resins which can affect absorption of the beta blockers
Sympatholytic drugs act by blocking the sympathetic nervous system in three ways: by blocking receptors in effector organs, blocking transmission at sympathetic ganglia, or blocking activity in the brain. Alpha-adrenergic blocking drugs specifically inhibit responses mediated by alpha receptors. They are used to treat conditions like hypertension, benign prostatic hyperplasia, and congestive heart failure. Beta-adrenergic blocking drugs inhibit responses mediated by beta receptors and are used for hypertension, angina, arrhythmias, glaucoma, and other conditions. Both types of sympatholytic drugs have important effects and side effects mediated through their receptor blocking actions.
1. The document discusses drug therapy for hypertension, outlining several classes of drugs and their mechanisms of action, including diuretics, beta-blockers, ACE inhibitors, angiotensin receptor blockers, calcium channel blockers, and other central acting agents.
2. Beta-blockers are recommended for mild to moderate hypertension but have adverse effects like fatigue and should not be used in diabetes or asthma. ACE inhibitors are first-line for essential hypertension and have benefits for conditions like diabetes.
3. Diuretics are commonly used first-line but have side effects like hypokalemia. Combination therapy with multiple drug classes is often needed to control resistant hypertension.
Anti-adrenergic drugs antagonize the action of adrenaline and related drugs by competitively blocking alpha and/or beta receptors. Alpha blockers such as prazosin are used to treat hypertension and benign prostatic hyperplasia by dilating arteries and reducing prostate tone. Beta blockers like propranolol non-selectively block both beta 1 and 2 receptors and are used for hypertension, angina, arrhythmias and migraine. Drugs for glaucoma work by reducing intraocular pressure through various mechanisms such as decreasing aqueous humor production or increasing outflow.
This document discusses adrenergic antagonists, which are drugs that inhibit the function of adrenergic receptors. There are five types of adrenergic receptors divided into alpha and beta receptors. Adrenergic antagonists are classified as alpha-selective, beta-selective, competitive, or non-competitive. Common adrenergic antagonists are discussed along with their mechanisms of action, pharmacological effects, clinical uses, pharmacokinetics, and adverse effects. Key uses include treating hypertension, congestive heart failure, pheochromocytoma, and benign prostatic hyperplasia.
This document discusses antihypertensive drugs used to treat hypertension. It defines hypertension and its causes. It then classifies and describes the mechanisms and properties of major classes of antihypertensive drugs, including diuretics, ACE inhibitors, angiotensin receptor blockers, calcium channel blockers, beta blockers, and others. For each class, it provides details on representative drugs, dosages, effects, advantages, and disadvantages in treating hypertension.
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.
Antiadrenergics drugs : By Dr Rahul R KunkulolRahul Kunkulol
This document discusses antiadrenergic drugs that antagonize the actions of adrenaline. It describes the pharmacological effects of alpha-adrenergic blockers and beta blockers. Alpha blockers are classified as alpha1 selective or alpha2 selective. Common alpha blockers mentioned include prazosin, terazosin, and tamsulosin. Beta blockers are classified as nonselective, cardioselective, or those with intrinsic sympathomimetic activity. Common uses of alpha and beta blockers include hypertension, benign prostatic hyperplasia, pheochromocytoma, and angina. Adverse effects include hypotension, bradycardia, and bronchospasm.
Anti-adrenergic drugs work by antagonizing the effects of adrenaline at alpha and beta adrenergic receptors. They are classified as alpha-adrenergic blocking drugs or beta-adrenergic blocking drugs. Alpha blockers are further classified as nonselective, alpha1 selective, or alpha2 selective. They are used to treat conditions like hypertension, benign prostatic hyperplasia, and congestive heart failure. Beta blockers are classified as nonselective or cardioselective. They decrease heart rate and cardiac output, lower blood pressure, and are used to treat hypertension, angina, arrhythmias, and migraines. Common side effects of beta blockers include fatigue, bradycardia
This document discusses adrenergic blockers, including their classification, mechanisms of action, effects and uses. It describes how alpha and beta blockers work by preventing the interaction of neurotransmitters like norepinephrine with corresponding adrenergic receptors. Common alpha blockers mentioned are prazosin, terazosin and doxazosin. Beta blockers discussed include metoprolol, atenolol, propranolol and esmolol. Their effects on the cardiovascular, respiratory and other systems are summarized. Therapeutic uses for conditions like hypertension, heart failure and prostate issues are also highlighted.
α blockers work by inhibiting adrenergic responses mediated through α adrenergic receptors. They reduce peripheral resistance and blood pressure by blocking vasoconstrictor α1 receptors. Common side effects include reflex tachycardia, nasal stuffiness, miosis, and reduced ejaculation. Phenoxybenzamine is irreversibly binds to receptors. Prazosin is highly selective for α1 receptors. It is used to treat hypertension and benign prostatic hyperplasia. Tamsulosin is relatively selective for α1A/α1D receptors in the bladder and prostate and causes fewer side effects than non-selective α blockers. α blockers are used to treat pheochromocytoma,
Diuretics are commonly used as first-line therapy for hypertension. Thiazide diuretics such as hydrochlorothiazide are often used due to their effectiveness and favorable side effect profile. If blood pressure is not controlled with one drug, a second drug from a different class is added. Patient compliance is important for successful treatment and selecting a regimen with fewer side effects can help improve compliance. Different drug classes may work better for certain patient populations, such as calcium channel blockers for elderly patients. The document discusses various classes of antihypertensive drugs including diuretics, beta blockers, ACE inhibitors, and vasodilators.
Beta Blockers And Diuretics In Treatment Of Hypertension.pptxJumaAwar3
This document discusses beta blockers and diuretics used in the treatment of hypertension. It describes the mechanisms and sites of action of various beta blockers including selective beta-1 blockers like atenolol and metoprolol, non-selective blockers like propranolol, and alpha-beta blockers like labetalol. It also discusses the pharmacokinetics and uses of specific beta blockers. The document then discusses thiazide and loop diuretics, their mechanisms of action in inhibiting sodium transport in the kidney, and their toxicities which can include hypokalemia, hyperglycemia, and hypomagnesemia.
Normal Blood Pressure
Blood Pressure of < 140/ 90
Blood Pressure of 130 to 139/ 85 to 89 should be closely watched
High Blood Pressure
Blood Pressure > 140/ 90
How can I tell if I have High Blood Pressure?
Usually NO SYMPTOMS!
“The Silent Killer”
May have: Headache, Blurry vision, Chest Pain, Frequent urination at night
Definition: These are the drugs used to lower BP in hypertension
Types of Hypertension:
1. Primary/ Essential / Idiopathic:
Definite cause is unknown
Characterized by - BP, normal CO, P.V.R.
2. Secondary Hypertension:
Secondary to-
Renal – Glomerulonephritis, pylonephritis etc
Endocrine – Hyperaldosteronism, Cushing’s syndrome etc
Vascular Diseases- renal artery disease etc.
Glycogen is a polymer of glucose residues stored predominantly in liver and muscle cells. Glycogenesis is the synthesis of glycogen from glucose-6-phosphate after a meal when blood glucose levels are high, while glycogenolysis is the breakdown of glycogen into glucose-1-phosphate during fasting or exercise. Both processes are regulated by insulin, glucagon, and epinephrine to maintain blood glucose homeostasis. Deficiencies of enzymes involved in glycogen metabolism can result in glycogen storage diseases.
Antihelminthic and antiprotozoal drugs work by killing or expelling parasitic worms and protozoa. Common antihelminthics discussed include mebendazole, albendazole, pyrantel, and levamisole which are used to treat nematode, cestode, and trematode infections. Their mechanisms of action involve inhibiting microtubule assembly, inducing paralysis, or activating nicotinic receptors in the parasites. Common antiprotozoals discussed include metronidazole for amebiasis, giardiasis and trichomoniasis, and drugs for malaria such as chloroquine, primaquine, and antifol combinations. Adverse
This document discusses adrenergic receptors and their classification into alpha and beta receptors. It describes the differences between alpha and beta adrenergic receptors and provides details about various types of drugs that act as adrenergic antagonists including:
- Alpha blockers which are used to treat hypertension and benign prostatic hyperplasia. They cause vasodilation and reduce blood pressure. Examples include prazosin and doxazosin.
- Beta blockers which are classified as non-selective or cardioselective. Non-selective blockers are contraindicated in asthma while cardioselective blockers reduce their side effects. Examples of beta blockers mentioned are propranolol and atenolol.
This document summarizes beta-adrenergic blockers (beta blockers). It describes that beta blockers are drugs that bind to beta receptors in the sympathetic nervous system to block the effects of epinephrine and norepinephrine. There are two main types of beta receptors, beta 1 and beta 2. Beta blockers are either cardioselective (blocking beta 1) or non-selective (blocking both beta 1 and beta 2). Common uses of beta blockers include treating hypertension, angina, myocardial infarction, and glaucoma. Side effects can include fatigue, dizziness, bronchospasm, and sexual dysfunction.
Beta-blockers are a class of drugs that are used to manage various cardiac conditions by blocking the effects of epinephrine and other stress hormones on beta receptors. They were first developed in the 1950s and revolutionized cardiology. Beta-blockers are indicated for conditions like hypertension, arrhythmias, heart attack, and glaucoma. While they provide important benefits, they can also cause adverse effects like fatigue, dizziness, and bronchospasm. Different beta-blockers have varying levels of selectivity for beta-1 versus beta-2 receptors and some have additional alpha-blocking properties. Guidelines provide recommendations on the appropriate use of specific beta-blockers for different cardiac indications.
1. Prazosin is a potent and selective α1 adrenergic receptor blocker used to treat hypertension. It has a first-dose phenomenon that can cause severe hypotension, so the initial dose should be small.
2. Beta blockers block the effects of sympathetic stimulation by competitively blocking beta receptors. They are used to treat hypertension, angina, migraines, hyperthyroidism and other conditions. Common side effects include bradycardia, heart block, bronchospasm and hypoglycemia.
3. Drug interactions can occur between beta blockers and calcium channel blockers, local anesthetics, or bile acid sequestering resins which can affect absorption of the beta blockers
Sympatholytic drugs act by blocking the sympathetic nervous system in three ways: by blocking receptors in effector organs, blocking transmission at sympathetic ganglia, or blocking activity in the brain. Alpha-adrenergic blocking drugs specifically inhibit responses mediated by alpha receptors. They are used to treat conditions like hypertension, benign prostatic hyperplasia, and congestive heart failure. Beta-adrenergic blocking drugs inhibit responses mediated by beta receptors and are used for hypertension, angina, arrhythmias, glaucoma, and other conditions. Both types of sympatholytic drugs have important effects and side effects mediated through their receptor blocking actions.
1. The document discusses drug therapy for hypertension, outlining several classes of drugs and their mechanisms of action, including diuretics, beta-blockers, ACE inhibitors, angiotensin receptor blockers, calcium channel blockers, and other central acting agents.
2. Beta-blockers are recommended for mild to moderate hypertension but have adverse effects like fatigue and should not be used in diabetes or asthma. ACE inhibitors are first-line for essential hypertension and have benefits for conditions like diabetes.
3. Diuretics are commonly used first-line but have side effects like hypokalemia. Combination therapy with multiple drug classes is often needed to control resistant hypertension.
Anti-adrenergic drugs antagonize the action of adrenaline and related drugs by competitively blocking alpha and/or beta receptors. Alpha blockers such as prazosin are used to treat hypertension and benign prostatic hyperplasia by dilating arteries and reducing prostate tone. Beta blockers like propranolol non-selectively block both beta 1 and 2 receptors and are used for hypertension, angina, arrhythmias and migraine. Drugs for glaucoma work by reducing intraocular pressure through various mechanisms such as decreasing aqueous humor production or increasing outflow.
This document discusses adrenergic antagonists, which are drugs that inhibit the function of adrenergic receptors. There are five types of adrenergic receptors divided into alpha and beta receptors. Adrenergic antagonists are classified as alpha-selective, beta-selective, competitive, or non-competitive. Common adrenergic antagonists are discussed along with their mechanisms of action, pharmacological effects, clinical uses, pharmacokinetics, and adverse effects. Key uses include treating hypertension, congestive heart failure, pheochromocytoma, and benign prostatic hyperplasia.
This document discusses antihypertensive drugs used to treat hypertension. It defines hypertension and its causes. It then classifies and describes the mechanisms and properties of major classes of antihypertensive drugs, including diuretics, ACE inhibitors, angiotensin receptor blockers, calcium channel blockers, beta blockers, and others. For each class, it provides details on representative drugs, dosages, effects, advantages, and disadvantages in treating hypertension.
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.
Antiadrenergics drugs : By Dr Rahul R KunkulolRahul Kunkulol
This document discusses antiadrenergic drugs that antagonize the actions of adrenaline. It describes the pharmacological effects of alpha-adrenergic blockers and beta blockers. Alpha blockers are classified as alpha1 selective or alpha2 selective. Common alpha blockers mentioned include prazosin, terazosin, and tamsulosin. Beta blockers are classified as nonselective, cardioselective, or those with intrinsic sympathomimetic activity. Common uses of alpha and beta blockers include hypertension, benign prostatic hyperplasia, pheochromocytoma, and angina. Adverse effects include hypotension, bradycardia, and bronchospasm.
Anti-adrenergic drugs work by antagonizing the effects of adrenaline at alpha and beta adrenergic receptors. They are classified as alpha-adrenergic blocking drugs or beta-adrenergic blocking drugs. Alpha blockers are further classified as nonselective, alpha1 selective, or alpha2 selective. They are used to treat conditions like hypertension, benign prostatic hyperplasia, and congestive heart failure. Beta blockers are classified as nonselective or cardioselective. They decrease heart rate and cardiac output, lower blood pressure, and are used to treat hypertension, angina, arrhythmias, and migraines. Common side effects of beta blockers include fatigue, bradycardia
This document discusses adrenergic blockers, including their classification, mechanisms of action, effects and uses. It describes how alpha and beta blockers work by preventing the interaction of neurotransmitters like norepinephrine with corresponding adrenergic receptors. Common alpha blockers mentioned are prazosin, terazosin and doxazosin. Beta blockers discussed include metoprolol, atenolol, propranolol and esmolol. Their effects on the cardiovascular, respiratory and other systems are summarized. Therapeutic uses for conditions like hypertension, heart failure and prostate issues are also highlighted.
α blockers work by inhibiting adrenergic responses mediated through α adrenergic receptors. They reduce peripheral resistance and blood pressure by blocking vasoconstrictor α1 receptors. Common side effects include reflex tachycardia, nasal stuffiness, miosis, and reduced ejaculation. Phenoxybenzamine is irreversibly binds to receptors. Prazosin is highly selective for α1 receptors. It is used to treat hypertension and benign prostatic hyperplasia. Tamsulosin is relatively selective for α1A/α1D receptors in the bladder and prostate and causes fewer side effects than non-selective α blockers. α blockers are used to treat pheochromocytoma,
Diuretics are commonly used as first-line therapy for hypertension. Thiazide diuretics such as hydrochlorothiazide are often used due to their effectiveness and favorable side effect profile. If blood pressure is not controlled with one drug, a second drug from a different class is added. Patient compliance is important for successful treatment and selecting a regimen with fewer side effects can help improve compliance. Different drug classes may work better for certain patient populations, such as calcium channel blockers for elderly patients. The document discusses various classes of antihypertensive drugs including diuretics, beta blockers, ACE inhibitors, and vasodilators.
Beta Blockers And Diuretics In Treatment Of Hypertension.pptxJumaAwar3
This document discusses beta blockers and diuretics used in the treatment of hypertension. It describes the mechanisms and sites of action of various beta blockers including selective beta-1 blockers like atenolol and metoprolol, non-selective blockers like propranolol, and alpha-beta blockers like labetalol. It also discusses the pharmacokinetics and uses of specific beta blockers. The document then discusses thiazide and loop diuretics, their mechanisms of action in inhibiting sodium transport in the kidney, and their toxicities which can include hypokalemia, hyperglycemia, and hypomagnesemia.
Normal Blood Pressure
Blood Pressure of < 140/ 90
Blood Pressure of 130 to 139/ 85 to 89 should be closely watched
High Blood Pressure
Blood Pressure > 140/ 90
How can I tell if I have High Blood Pressure?
Usually NO SYMPTOMS!
“The Silent Killer”
May have: Headache, Blurry vision, Chest Pain, Frequent urination at night
Definition: These are the drugs used to lower BP in hypertension
Types of Hypertension:
1. Primary/ Essential / Idiopathic:
Definite cause is unknown
Characterized by - BP, normal CO, P.V.R.
2. Secondary Hypertension:
Secondary to-
Renal – Glomerulonephritis, pylonephritis etc
Endocrine – Hyperaldosteronism, Cushing’s syndrome etc
Vascular Diseases- renal artery disease etc.
Similar to Alpha Adrenoceptor Antagonists.ppt (20)
Glycogen is a polymer of glucose residues stored predominantly in liver and muscle cells. Glycogenesis is the synthesis of glycogen from glucose-6-phosphate after a meal when blood glucose levels are high, while glycogenolysis is the breakdown of glycogen into glucose-1-phosphate during fasting or exercise. Both processes are regulated by insulin, glucagon, and epinephrine to maintain blood glucose homeostasis. Deficiencies of enzymes involved in glycogen metabolism can result in glycogen storage diseases.
Antihelminthic and antiprotozoal drugs work by killing or expelling parasitic worms and protozoa. Common antihelminthics discussed include mebendazole, albendazole, pyrantel, and levamisole which are used to treat nematode, cestode, and trematode infections. Their mechanisms of action involve inhibiting microtubule assembly, inducing paralysis, or activating nicotinic receptors in the parasites. Common antiprotozoals discussed include metronidazole for amebiasis, giardiasis and trichomoniasis, and drugs for malaria such as chloroquine, primaquine, and antifol combinations. Adverse
This document discusses drugs used to treat cough. It begins by defining cough and classifying it based on duration and characteristics. Nonspecific therapies for cough include demulcents to soothe the throat, expectorants to enhance mucus secretion or reduce viscosity, and antitussives to suppress the cough center. Demulcents include lozenges and cough drops. Expectorants include bronchial secretagogues like guaifenesin and mucolytics like bromhexine that break down mucus. Antitussives include opioids like codeine, nonopioids like dextromethorphan, and antihistamines. Specific treatments depend on the underlying cause of cough such as antibiotics for infection
This document discusses antitussive drugs, which are used to suppress coughing. It defines antitussives and expectorants, and describes the mechanism of cough production involving cough receptors in the lungs and the cough center in the medulla. It classifies cough and antitussives, and discusses the mechanisms of action and indications of centrally- and peripherally-acting antitussives. Common antitussive drugs like codeine, hydrocodone, and dextromethorphan are described along with their effects and side effects. Various animal models used to screen for antitussive effects are outlined, including methods using guinea pigs, cats, and dogs exposed to irritants to induce coughing.
- A dose response relationship describes how the magnitude of a drug's effect varies with increasing or decreasing doses. Dose response curves plot this relationship, with dose on the x-axis and response on the y-axis.
- There are two main types of dose response curves: graded/quantitative curves where response increases continuously with dose, and quantal/all-or-none curves where responses are binary above a threshold dose.
- The shape, slope, efficacy and potency of a dose response curve provide information about a drug's effects, safety, and relative potencies of similar drugs. Steep curves indicate higher potency while flatter curves suggest a drug has less impact over a range of doses.
Antihelminthic and antiprotozoal drugs work by killing or expelling parasitic worms and protozoa. Common antihelminthics discussed include mebendazole, albendazole, pyrantel, and levamisole which are used to treat nematode, cestode, and trematode infections. Their mechanisms of action involve inhibiting microtubule assembly, inducing paralysis, or activating nicotinic receptors in the parasites. Common antiprotozoals discussed include metronidazole for amebiasis, giardiasis and trichomoniasis, and drugs for malaria such as chloroquine, primaquine, and antifol combinations. Adverse
This document discusses antitussive drugs, which are used to suppress coughing. It defines antitussives and expectorants, and describes the mechanism of cough production involving cough receptors in the lungs and the cough center in the medulla. It classifies cough and antitussives, and discusses the mechanisms of action and indications of centrally- and peripherally-acting antitussives. Common antitussives discussed include codeine, hydrocodone, dextromethorphan, and benzonatate. The document also describes several animal models used to screen for antitussive effects, such as measuring coughs induced by irritants in guinea pigs and mechanical stimulation in anesthetized guinea pigs and cats.
Antitussives are drugs that suppress coughing by reducing activity in the brain's cough center. Codeine is the most commonly used antitussive and works by raising the threshold for cough reflexes. It has antitussive effects at doses of 15-60mg and has a plasma half-life of 3-4 hours. Codeine is converted to morphine in some individuals, explaining its analgesic effects as an opioid receptor agonist. Common side effects include nausea, vomiting, constipation, drowsiness, and dry mouth.
Scabies is a skin infection caused by mites that burrow into the skin. It is transmitted through direct skin-to-skin contact with an infected person. Symptoms include an itchy rash. Diagnosis is usually made based on symptoms and history of contact with infected individuals. Treatment involves applying prescription topical creams or lotions to kill the mites. Proper treatment of all infected individuals and environmental cleaning is important to prevent outbreaks. Treatment may need to be repeated if symptoms persist or new burrows appear.
Antihelminthic and antiprotozoal drugs are used to treat infections caused by helminths (worms) and protozoa. The major classes of antihelminthics discussed are mebendazole, albendazole, pyrantel, levamisole, and piperazine which are used against nematodes, trematodes, and cestodes. Antiprotozoal drugs discussed include metronidazole for amoebiasis, giardiasis, and trichomoniasis. Drugs for malaria discussed are quinine, chloroquine, antifolates, primaquine, and nitrofurans. Melarsoprol
This document provides an overview of commonly used antibiotics, including their classification, mechanisms of action, spectra of activity, clinical uses, and pharmacokinetic properties. It discusses six major classes of antibiotics: beta-lactams, aminoglycosides, fluoroquinolones, macrolides, tetracyclines, and glycopeptides. For each class, it summarizes the antibiotic names, mechanisms, spectra, uses, and considerations for optimizing treatment such as dosing principles and preventing toxicity. Key messages emphasize the importance of early sepsis diagnosis/treatment and selecting antibiotics based on the infection site and tissue penetration properties.
The document summarizes the axial skeleton, which includes the skull, vertebral column, and thoracic cage. It describes the three regions of the axial skeleton and provides figures and descriptions of the individual bones that make up each region, including the skull, vertebrae, ribs, and sternum. Key functions of the axial skeleton are also summarized, such as protecting internal organs and serving as attachment sites for muscles involved in posture, respiration, and limb movement.
Antihelminthic and antiprotozoal drugs are used to treat infections caused by parasites. The major classes of antihelminthics discussed target nematodes, trematodes, and cestodes. Specific drugs mentioned include mebendazole, albendazole, pyrantel, levamisole, and praziquantel. These drugs work through various mechanisms including disrupting microtubule assembly, inducing muscle paralysis, or causing calcium leakage. Common side effects include abdominal pain, diarrhea, and allergic reactions. Antiprotozoal drugs discussed treat infections caused by protozoa like Entamoeba histolytica, Giardia lamblia, and Plasmodium
Antihelminthic and antiprotozoal drugs are used to treat infections caused by parasites. The major classes of antihelminthics discussed target nematodes, trematodes, and cestodes. Specific drugs mentioned include mebendazole, albendazole, pyrantel, levamisole, and praziquantel. These drugs work through various mechanisms including disrupting microtubule assembly, inducing muscle paralysis, or causing calcium leakage. Common side effects include abdominal pain, diarrhea, and allergic reactions. Antiprotozoal drugs discussed treat infections caused by protozoa like Entamoeba histolytica, Giardia lamblia, and Plasmodium
Heart failure is the inability of the heart to pump enough blood to meet the body's needs. There are two main types - left-sided and right-sided failure. Symptoms include breathlessness and swelling. Treatment focuses on reducing preload and afterload through medications like ACE inhibitors, diuretics, vasodilators, and positive inotropes. Digoxin increases cardiac contractility by inhibiting the sodium-potassium pump, allowing more calcium to enter heart cells and strengthen contractions. While improving cardiac output, it can also decrease heart rate through vagal stimulation.
This lecture discusses opioid analgesics including natural, semisynthetic, and synthetic opioids. It defines opioids as substances that produce morphine-like effects by binding to opioid receptors in the brain. Natural opioids discussed include morphine and codeine, which are extracted from the poppy plant. Semisynthetic opioids are derived from natural opioids through chemical modification, such as heroin from acetylation of morphine. Synthetic opioids include agonists like fentanyl, antagonists like naloxone that block opioid receptors, and mixed agonist-antagonists. The lecture covers pharmacological properties, therapeutic uses, and adverse effects of various opioid analgesics.
This document provides definitions and information about seizures, epilepsy, and antiepileptic drugs. It defines seizures as a temporary change in brain function due to high-frequency neuronal impulses in the brain. Epilepsy is characterized by recurrent seizures. Several types of seizures are described, including focal onset seizures which start in one brain area and generalized onset seizures which affect large brain regions. Causes of epilepsy include genetic and acquired factors like brain damage. Antiepileptic drugs work via mechanisms like enhancing GABA inhibition, blocking sodium channels, or inhibiting excitatory neurotransmitters. First and second generation antiepileptic drugs are outlined with their mechanisms of action and adverse effect profiles.
This document discusses dose-response relationships and toxicity studies. It provides details on:
- Acute and chronic toxicity studies which determine lethal doses, target organs, and appropriate doses for further studies.
- Factors that influence toxicity like dose, exposure route, chemical properties, and individual variability in things like genetics, age and sex.
- Dose-response curves which illustrate the relationship between dose and effect and are used to determine safe exposure levels.
- Various terms used in toxicity assessments like NOAEL, LOAEL, BMD, RfD, and ADI.
Pharmacology is the study of drugs and their actions within the body. It deals with how drugs are absorbed, distributed, metabolized and excreted by the body, as well as their physiological effects. The document provides a brief historical overview of pharmacology and important discoveries. It discusses the development process for new drugs, which includes preclinical testing in animals followed by clinical trials in humans in four phases. Stringent regulations and guidelines govern the development and approval of new drugs to ensure safety and efficacy.
This document provides an introduction to the field of pharmacology. It defines pharmacology as dealing with all aspects of drugs, including their sources, effects, side effects, metabolism, and elimination in the body. It then discusses key terms in pharmacology like pharmacokinetics, pharmacodynamics, and toxicology. The document also covers drug nomenclature, essential drug concepts, orphan drugs, factors governing drug administration routes, and special features of transdermal drug delivery systems. Finally, it discusses pharmacokinetic effects of drugs including absorption, distribution to tissues, metabolism, and excretion.
Cell Therapy Expansion and Challenges in Autoimmune DiseaseHealth Advances
There is increasing confidence that cell therapies will soon play a role in the treatment of autoimmune disorders, but the extent of this impact remains to be seen. Early readouts on autologous CAR-Ts in lupus are encouraging, but manufacturing and cost limitations are likely to restrict access to highly refractory patients. Allogeneic CAR-Ts have the potential to broaden access to earlier lines of treatment due to their inherent cost benefits, however they will need to demonstrate comparable or improved efficacy to established modalities.
In addition to infrastructure and capacity constraints, CAR-Ts face a very different risk-benefit dynamic in autoimmune compared to oncology, highlighting the need for tolerable therapies with low adverse event risk. CAR-NK and Treg-based therapies are also being developed in certain autoimmune disorders and may demonstrate favorable safety profiles. Several novel non-cell therapies such as bispecific antibodies, nanobodies, and RNAi drugs, may also offer future alternative competitive solutions with variable value propositions.
Widespread adoption of cell therapies will not only require strong efficacy and safety data, but also adapted pricing and access strategies. At oncology-based price points, CAR-Ts are unlikely to achieve broad market access in autoimmune disorders, with eligible patient populations that are potentially orders of magnitude greater than the number of currently addressable cancer patients. Developers have made strides towards reducing cell therapy COGS while improving manufacturing efficiency, but payors will inevitably restrict access until more sustainable pricing is achieved.
Despite these headwinds, industry leaders and investors remain confident that cell therapies are poised to address significant unmet need in patients suffering from autoimmune disorders. However, the extent of this impact on the treatment landscape remains to be seen, as the industry rapidly approaches an inflection point.
Recomendações da OMS sobre cuidados maternos e neonatais para uma experiência pós-natal positiva.
Em consonância com os ODS – Objetivos do Desenvolvimento Sustentável e a Estratégia Global para a Saúde das Mulheres, Crianças e Adolescentes, e aplicando uma abordagem baseada nos direitos humanos, os esforços de cuidados pós-natais devem expandir-se para além da cobertura e da simples sobrevivência, de modo a incluir cuidados de qualidade.
Estas diretrizes visam melhorar a qualidade dos cuidados pós-natais essenciais e de rotina prestados às mulheres e aos recém-nascidos, com o objetivo final de melhorar a saúde e o bem-estar materno e neonatal.
Uma “experiência pós-natal positiva” é um resultado importante para todas as mulheres que dão à luz e para os seus recém-nascidos, estabelecendo as bases para a melhoria da saúde e do bem-estar a curto e longo prazo. Uma experiência pós-natal positiva é definida como aquela em que as mulheres, pessoas que gestam, os recém-nascidos, os casais, os pais, os cuidadores e as famílias recebem informação consistente, garantia e apoio de profissionais de saúde motivados; e onde um sistema de saúde flexível e com recursos reconheça as necessidades das mulheres e dos bebês e respeite o seu contexto cultural.
Estas diretrizes consolidadas apresentam algumas recomendações novas e já bem fundamentadas sobre cuidados pós-natais de rotina para mulheres e neonatos que recebem cuidados no pós-parto em unidades de saúde ou na comunidade, independentemente dos recursos disponíveis.
É fornecido um conjunto abrangente de recomendações para cuidados durante o período puerperal, com ênfase nos cuidados essenciais que todas as mulheres e recém-nascidos devem receber, e com a devida atenção à qualidade dos cuidados; isto é, a entrega e a experiência do cuidado recebido. Estas diretrizes atualizam e ampliam as recomendações da OMS de 2014 sobre cuidados pós-natais da mãe e do recém-nascido e complementam as atuais diretrizes da OMS sobre a gestão de complicações pós-natais.
O estabelecimento da amamentação e o manejo das principais intercorrências é contemplada.
Recomendamos muito.
Vamos discutir essas recomendações no nosso curso de pós-graduação em Aleitamento no Instituto Ciclos.
Esta publicação só está disponível em inglês até o momento.
Prof. Marcus Renato de Carvalho
www.agostodourado.com
Rasamanikya is a excellent preparation in the field of Rasashastra, it is used in various Kushtha Roga, Shwasa, Vicharchika, Bhagandara, Vatarakta, and Phiranga Roga. In this article Preparation& Comparative analytical profile for both Formulationon i.e Rasamanikya prepared by Kushmanda swarasa & Churnodhaka Shodita Haratala. The study aims to provide insights into the comparative efficacy and analytical aspects of these formulations for enhanced therapeutic outcomes.
Osteoporosis - Definition , Evaluation and Management .pdfJim Jacob Roy
Osteoporosis is an increasing cause of morbidity among the elderly.
In this document , a brief outline of osteoporosis is given , including the risk factors of osteoporosis fractures , the indications for testing bone mineral density and the management of osteoporosis
TEST BANK For Community Health Nursing A Canadian Perspective, 5th Edition by...Donc Test
TEST BANK For Community Health Nursing A Canadian Perspective, 5th Edition by Stamler, Verified Chapters 1 - 33, Complete Newest Version Community Health Nursing A Canadian Perspective, 5th Edition by Stamler, Verified Chapters 1 - 33, Complete Newest Version Community Health Nursing A Canadian Perspective, 5th Edition by Stamler Community Health Nursing A Canadian Perspective, 5th Edition TEST BANK by Stamler Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Pdf Chapters Download Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Pdf Download Stuvia Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Study Guide Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Ebook Download Stuvia Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Questions and Answers Quizlet Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Studocu Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Quizlet Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Stuvia Community Health Nursing A Canadian Perspective, 5th Edition Pdf Chapters Download Community Health Nursing A Canadian Perspective, 5th Edition Pdf Download Course Hero Community Health Nursing A Canadian Perspective, 5th Edition Answers Quizlet Community Health Nursing A Canadian Perspective, 5th Edition Ebook Download Course hero Community Health Nursing A Canadian Perspective, 5th Edition Questions and Answers Community Health Nursing A Canadian Perspective, 5th Edition Studocu Community Health Nursing A Canadian Perspective, 5th Edition Quizlet Community Health Nursing A Canadian Perspective, 5th Edition Stuvia Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Pdf Chapters Download Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Pdf Download Stuvia Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Study Guide Questions and Answers Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Ebook Download Stuvia Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Questions Quizlet Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Studocu Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Quizlet Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Stuvia
Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...Oleg Kshivets
Overall life span (LS) was 1671.7±1721.6 days and cumulative 5YS reached 62.4%, 10 years – 50.4%, 20 years – 44.6%. 94 LCP lived more than 5 years without cancer (LS=2958.6±1723.6 days), 22 – more than 10 years (LS=5571±1841.8 days). 67 LCP died because of LC (LS=471.9±344 days). AT significantly improved 5YS (68% vs. 53.7%) (P=0.028 by log-rank test). Cox modeling displayed that 5YS of LCP significantly depended on: N0-N12, T3-4, blood cell circuit, cell ratio factors (ratio between cancer cells-CC and blood cells subpopulations), LC cell dynamics, recalcification time, heparin tolerance, prothrombin index, protein, AT, procedure type (P=0.000-0.031). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and N0-12 (rank=1), thrombocytes/CC (rank=2), segmented neutrophils/CC (3), eosinophils/CC (4), erythrocytes/CC (5), healthy cells/CC (6), lymphocytes/CC (7), stick neutrophils/CC (8), leucocytes/CC (9), monocytes/CC (10). Correct prediction of 5YS was 100% by neural networks computing (error=0.000; area under ROC curve=1.0).
Basavarajeeyam is an important text for ayurvedic physician belonging to andhra pradehs. It is a popular compendium in various parts of our country as well as in andhra pradesh. The content of the text was presented in sanskrit and telugu language (Bilingual). One of the most famous book in ayurvedic pharmaceutics and therapeutics. This book contains 25 chapters called as prakaranas. Many rasaoushadis were explained, pioneer of dhatu druti, nadi pareeksha, mutra pareeksha etc. Belongs to the period of 15-16 century. New diseases like upadamsha, phiranga rogas are explained.
Does Over-Masturbation Contribute to Chronic Prostatitis.pptxwalterHu5
In some case, your chronic prostatitis may be related to over-masturbation. Generally, natural medicine Diuretic and Anti-inflammatory Pill can help mee get a cure.
2. Alpha-Receptor Antagonist Drugs
• Pharmacologic Effects
• Cardiovascular Effects
• Decrease peripheral vascular resistance and blood
pressure.
• Prevent the pressor effects of usual doses of α
agonists
• Alpha-receptor antagonists often cause orthostatic
hypotension and reflex tachycardia; nonselective (α 1
= α 2,) blockers usually cause significant tachycardia if
blood pressure is lowered below normal, more marked
with agents that block α 2-presynaptic receptors
3. • Other Effects
• Miosis (small pupils) and nasal stuffiness.
• decreases resistance to the flow of urine so
used for the treatment of urinary retention due
to prostatic hyperplasia .
4. Non selective alpha blockers
Phenoxybenzamine
irreversible blockade of long duration (14–48 h).
Blocks α1& to less extent α2 receptors.
Also inhibits reuptake of NE and blocks histamine
(H1),ACh, and serotonin receptors.
little fall in BP in normal supine individuals, it reduces BP
when sympathetic tone is high, eg, as a result of
upright posture.
Absorbed poorly but usually given orally.
Its major use is in the treatment of pheochromocytoma
Adverse effects
Orthostatic hypotension and tachycardia, Nasal
stuffiness and inhibition of ejaculation.
5. • Phentolamine
• Competitive α1 and α2 blocker.
• Reduces peripheral resistance (α1) and causes
cardiac stimulation).
• Minor inhibitory effects at serotonin receptors &
agonist at muscarinic & histamine receptors.
• Adverse effects are severe tachycardia,
arrhythmias, and myocardial ischemia.
• Used in the treatment of pheochromocytoma.
6. • Selective alpha 1 blockers
• Prazosin
• Relaxes both arterial and venous vascular smooth
muscle & smooth muscle in the prostate, due to
blockade of α 1 receptors with no or little
tachycardia
• Bioavailability 50% & the half-life is 3 hours.
• Terazosin
• Effective in hypertension & in benign prostatic
hyperplasia (BPH).
• High bioavailability. The half-life is 9–12 hours.
• Doxazosin
• Effective in of hypertension and BPH.
• Has a longer half-life of about 22 hours.
Their major adverse effect is orthostatic hypotension,
which may be severe after the first few doses but is
otherwise uncommon (First-Dose Phenomenon).
7. Tamsulosin
High bioavailability and a half-life of 9–15 hours.
Has relatively greater potency in inhibiting
contraction in prostate smooth muscle versus
vascular smooth muscle compared with other α
1-selective antagonists.
used to treat BPH.
has less effect on standing blood pressure in
patients.
8. Other Alpha- Adrenoceptor Antagonists
Labetalol
Has both α1 and β-antagonistic effects
Chlorpromazine and haloperidol
Neuroleptic drugs & also block α receptors.
Ergot derivatives, eg, ergotamine and
dihydroergotamine are reversible α blockers.
• Yohimbine
• An indole alkaloid, is α 2-selective antagonist.
• It is sometimes used in the treatment of orthostatic
hypotension because it promotes NErelease through
blockade of presynaptic α 2 receptors.
• It was once widely used to improve male erectile
dysfunction but has been superseded by
phosphodiesterase-5 inhibitors like sildenafil.
9. Uses of the Alpha-Receptor–Blocking Drugs
1- Pheochromocytoma
Phenoxybenzamine (orally) preoperative & for the
chronic treatment of inoperable or metastatic
pheochromocytoma, given with β blockers.
Metyrosine (α -methyltyrosine), an inhibitor of tyrosine
hydroxylase, useful in inoperable or metastatic
pheochromocytoma.
2-Hypertensive Emergencies
Labetalol is used in Hypertensive Emergencies
3-Chronic Hypertension
α 1-selective antagonists in mild to moderate
hypertension butNot recommended as monotherapy
because other drugs are more effective in preventing
heart failure.
10. 4-Peripheral Vascular Disease
Raynaud's phenomenon (excessive reversible
vasospasm in the peripheral circulation) Prazosin or
phenoxybenzamine are used but calcium channel
blockers may be preferable for most patients.
5-Urinary Obstruction
Benign prostatic hyperplasia (BPH) is common in elderly
men.
Improving urine flow involves partial reversal of smooth
muscle contraction in the enlarged prostate and in the
bladder base.
Prazosin, doxazosin, and terazosin are all effective.
Tamsulosin is α 1A-receptor antagonists effective in
BPH and has relatively minor effects on blood
pressure at a low dose.
11. β- Adrenoceptor Antagonist Drugs
Differ in their relative affinities for β 1 and β 2 receptors.
The selectivity is dose-related; it tends to diminish at
higher drug concentrations.
Other major differences relate to their pharmacokinetic
characteristics and local anesthetic (membrane-
stabilizing) effects. However, the concentration in
plasma is too low for the anesthetic effects.
Absorption
Most of the drugs are well absorbed after oral
administration; peak concentrations occur 1–3 hours
after ingestion. Propranolol & penbutolol are
lipophilic and readily cross the blood-brain barrier .
Most β antagonists have half-lives of 3–10 hours.
12. Selectivity Partial Agonist Local Anesthetic t½
Acebutolol β1 Yes Yes 3–4hours
Atenolol β1 No No 6–9 hours
Bisoprolol β1 No No 9–12 hours
Esmolol β1 No No 10 minutes
Labetalol None (α blocker) Yes Yes 5 hours
Metoprolol β 1 No Yes 3–4 hours
Nadolol None No No 14–24 hours
Penbutolol None Yes No 5 hours
Pindolol None Yes Yes 3–4 hours
Propranolol None No Yes 3.5–6 hours
Sotalol None No No 12 hours
Timolol None No No 4–5 hours
13. Pharmacodynamics
Effects on the Cardiovascular System
Chronic administration leads to a fall in peripheral
resistance in patients with hypertension.
This may acutely lead to a rise in peripheral resistance
from unopposed α -receptor-mediated effects as the
sympathetic nervous system is activated in response to
the fall in cardiac output.
Nonselective and β 1-blocking drugs antagonize the release of
renin caused by the sympathetic nervous system.
Effects on the Respiratory Tract
Increase in airway resistance in patients with asthma.
β 1-selective blocker are not sufficiently specific to
completely avoid interactions with β 2 adrenoceptors.
Many patients may tolerate these drugs the risks.
14. Effects on the Eye
Reduce intraocular pressure in glaucoma by decreasing
aqueous humor production.
The open-angle glaucoma is a chronic condition, and
treatment is largely pharmacologic.
Glaucoma is treated by:
1- reduction of aqueous humor secretion.
2- enhancement of aqueous out-flow.
Drugs useful in reducing intraocular pressure:
1-cholinomimetics
2-α agonists
3- β blockers
4- prostaglandin F2 analogs.
5- diuretics
Prostaglandin analogs & β blockers are the most
popular.
15. • Metabolic and Endocrine Effects
• Beta-receptor antagonists inhibit lipolysis.
• Glycogenolysis in the liver is inhibited after β
2-receptor blockade.
• β –blockers should be used with caution in
insulin-dependent diabetic patients.
16. Effects Not Related to Beta-Blockade
Partial agonists Pindolol & Penbutolol are
useful in patients who develop bradycardia or
bronchoconstriction.
Local anesthetic action the concentration in
plasma is too low for the anesthetic effects .
These membrane-stabilizing β- blockers are not
used topically on the eye, where local
anesthesia of the cornea would be undesirable.
Sotalol is a nonselective β blocker that has
marked class III antiarrhythmic effects, (used
to treat both ventricular & supraventricular
arrhythmias).
17. Specific Agents
• Propranolol
• Prototype of β -blocking drug.
• Low and dose-dependent bioavailability &there is
great individual variability in the plasma concentrations
achieved after oral propranolol.
• No partial agonist action at β receptors.
• Metoprolol, Atenolol.
• β1-selective antagonists, Safer in asthma, but their β
1 selectivity is modest, so they should be used with
great caution in patients with a history of asthma.
• However, the benefits may exceed the risks, eg, in
patients with myocardial infarction.
• Beta1-selective antagonists are preferred in patients
with diabetes or peripheral vascular disease since
β 2 receptors are important in liver (recovery from
hypoglycemia) and blood vessels (vasodilation).
18. Nebivolol, the most highly selective β 1 blocker, causes
vasodilation due to nitric oxide pathway.
Nadolol, has a very long duration of action.
Timolol, nonselective used topically to treat glaucoma.
Pindolol, acebutolol, and celiprolol.
Have partial β -agonist activity.
Effective in hypertension & angina and less likely to
cause bronchoconstriction, bradycardia and
abnormalities in plasma lipids.
Pindolol, non-selective beta-adrenoceptor/accelerates
the antidepressant effect of selective serotonin
reuptake inhibitors (SSRI).
Celiprolol, a β 1-selective antagonist with a partial β2 -
agonist activity & may have less adverse
bronchoconstrictor effect in asthma and may even
promote bronchodilation.
Acebutolol is also a β 1-selective antagonist.
19. • Labetalol
• (Causes Hypotension with less tachycardia.
• Carvedilol
• A nonselective beta blocker/alpha-1 blocker indicated
in congestive heart failure (CHF) and hypertension.
• Esmolol
• β 1-selective blocker.
• An ester so esterases in red blood cells rapidly
metabolize it. half-life 10 minutes. During continuous
infusions of esmolol, steady-state concentrations
are achieved quickly, and actions of the drug are
terminated rapidly when its infusion is discontinued.
• Esmolol may be safer in critically ill patients who
require a β -adrenoceptor antagonist.
20. Clinical uses
• Hypertension
• often used with either a diuretic or a vasodilator.
• Ischemic Heart Disease
• Reduce the frequency of anginal episodes and
improve exercise tolerance in patients with angina.
• They decrease cardiac work, reduce oxygen demand
& Slow heart rate which contribute to clinical benefits.
• The long-term use of timolol, propranolol, or
metoprolol in patients who have had a myocardial
infarction prolongs survival
• β -adrenoceptor antagonists are strongly indicated in
the acute phase of a myocardial infarction.
• Contraindications include bradycardia, hypotension,
moderate or severe left ventricular failure, shock, heart
block, and active airways disease.
•
21. • Cardiac Arrhythmias
• Effective in supraventricular & ventricular arrhythmias
• β antagonists slow ventricular response rates in atrial
flutter and fibrillation & reduce ventricular ectopic
beats, particularly if the ectopic activity has been
precipitated by catecholamines.
• Sotalol has a marked class III antiarrhythmic effects,
due to potassium channel blockade (treats both
ventricular & supraventricular arrhythmias).
• Heart Failure
• Metoprolol, bisoprolol, and carvedilol are effective in
reducing mortality in selected patients with chronic heart
failure.
• Cautious long-term use with gradual dose increments in
patients who tolerate them may prolong life.
• Although mechanisms are uncertain, there appear to be
beneficial effects on myocardial remodeling and in
decreasing the risk of sudden death.
22. • Glaucoma
• Timolol and related β antagonists are suitable for
local use in the eye because they lack local anesthetic
properties.
• have efficacy comparable to that of epinephrine or
pilocarpine in open-angle glaucoma and are far
better tolerated. Sufficient timolol may be absorbed
from the eye to cause serious adverse effects on the
heart and airways in susceptible individuals.
• Hyperthyroidism
• The effects are due to blockade of adrenoceptors
and perhaps in part to the inhibition of peripheral
conversion of thyroxine to triiodothyronine.
• Propranolol has been used extensively in thyroid
storm (severe hyperthyroidism) to control
supraventricular tachycardias that often precipitate
heart failure.
23. • Neurologic Diseases
• Propranolol reduces the frequency and intensity of
migraine headache.
• Other β -receptor antagonists with preventive efficacy
include metoprolol , atenolol, timolol, and nadolol.
• The mechanism is not known.
• β antagonists reduce certain tremors.
• The somatic manifestations of anxiety may
respond dramatically to low doses of propranolol,
particularly when taken prophylactically. Benefit has
been found in musicians with performance anxiety
("stage fright").
• Propranolol may be used in symptomatic treatment
of alcohol withdrawal in some patients.
24. • Clinical Toxicity of the Beta Blockers
• Bradycardia, cold hands & feet in winter. mild
sedation, vivid dreams, and rarely, depression.
• worsening of preexisting asthma.
• Caution in patients with severe peripheral vascular
disease and in patients with compensated heart
failure. A very small dose of a β antagonist may
provoke severe cardiac failure. interact with the
calcium antagonist verapamil causing heart failure
heart block.
• Stopping β blockers suddenly is dangerous due to up-
regulation of β receptors.
• Insulin-dependent diabetic patients with frequent
hypoglycemic reactions better use β 1 antagonists.
25. Ganglion-Blocking Drugs
Tetraethylammonium (TEA)
First ganglion blocker, very short duration of action.
Hexamethonium (The first drug effective for
hypertension. Decamethonium, the analog of
hexamethonium, is a depolarizing neuromuscular
blocking agent.
Mecamylamine
A secondary amine, was developed to improve
absorption from the GIT because the quaternary
amine were poorly absorbed after oral administration.
Trimethaphan
A short-acting ganglion blocker, is inactive orally and is
given by intravenous infusion.
26. • Organ System Effects
• Central Nervous System
• Mecamylamine enters the CNS causing Sedation,
tremor, choreiform movements, and mental
abnormalities.
• Eye
• Cycloplegia with loss of accommodation & moderate
dilation of the pupil because parasympathetic tone
usually dominates this tissue.
• Cardiovascular System
• Marked decrease in arteriolar and venomotor tone.
• BP may fall because both peripheral vascular
resistance and venous return are decreased
• Orthostatic or postural hypotension, diminished
contractility and, because the sinoatrial node is
usually dominated by the parasympathetic nervous
system, a moderate tachycardia.
27. • Other Effects:
• Inhibit secretion & Motility & cause constipation,
• urinary retention in men with prostatic hyperplasia.
• Sexual function is impaired & Sweating is reduced.
• . Clinical Applications & Toxicity
• Rarely used because more selective agents are available.
• Mecamylamine
• Blocks central nicotinic receptors could be an adjunct with
the transdermal nicotine patch to reduce nicotine craving
in patients attempting to quit smoking.
• Trimethaphan
• Occasionally used in the treatment of hypertensive
emergencies and in producing hypotension in
neurosurgery to reduce bleeding in the operative field.
• The toxicity of the ganglion-blocking drugs is limited to the
autonomic effects.
• These effects are intolerable except for acute use.