Antihypertensive Agents Overview

S(OH),S(CH3) = Inhibit sympathetic output Guanethidine = Prevent release of norepinephrine at high doses Hydralazine hydrochloride = Activate ATP-modulated potassium channels Parenteral Vasodilators = Used in hypertensive emergencies, may cause hyperglycemia

Centrally Acting Sympatholytics = Stimulate a2 and I1 receptors in CNS Adrenergic Neuron Blocking Agents = Release 'false neurotransmitters' at usual doses Vasodilators = Primarily act on arterial system Long-term therapy agents = Show activity in alopecia

Highly selective for I1 receptor = Centrally Acting Sympatholytics Integral N-oxide function = Vasodilators for unresponsive hypertension Effective control of blood pressure without adverse effects = Centrally Acting Sympatholytics Used in hypertensive emergencies = Parenteral Vasodilators

<p>S(OH),S(CH3) = Both are inactive Guanadrel = Acts as false neurotransmitter Hydralazine hydrochloride = Side effects include long-term therapy issues Parenteral Vasodilators = Can lead to hyperglycemia</p> Signup and view all the answers

<p>Guanethidine = Blocks adrenergic neuron at high doses S(OH),S(CH3) = Has no therapeutic effect Hydralazine hydrochloride = Indirectly causes opening of potassium channels Centrally Acting Sympatholytics = Inhibit sympathetic nervous system activity</p> Signup and view all the answers

<p>Norepinephrine = Maintain blood pressure in acute hypotensive states Epinephrine = Used by injection in anaphylactic reactions Phenylephrine = Vasoconstrictor for nasal congestion R(-) 2-Amino-1-(3,4-dihydroxy-phenyl)-ethanol = Bronchodilation and cardiac stimulation</p> Signup and view all the answers

<p>Norepinephrine = I.V Epinephrine = Used by inhalation in asthma Phenylephrine = Given orally R(-) 1-(3,4-dihydroxy-phenyl)-2-N-methylamino-ethanol = Injection</p> Signup and view all the answers

<p>Norepinephrine = Direct non-selective α ≤ β Epinephrine = Direct non-selective α, β Phenylephrine = Direct selective α1 R(-) 2-Amino-1-(3,4-dihydroxy-phenyl)-ethanol = Direct non-selective α ≤ β</p> Signup and view all the answers

<p>Norepinephrine = Possible CNS side effects Epinephrine = Stimulates CNS Phenylephrine = No CNS side effects R(-) 1-(3,4-dihydroxy-phenyl)-2-N-methylamino-ethanol = Minimal CNS stimulation</p> Signup and view all the answers

<p>Norepinephrine = Treatment of hypotension Epinephrine = Bronchodilation Phenylephrine = Treatment of glaucoma R(-) 1-(3,4-dihydroxy-phenyl)-2-N-methylamino-ethanol = Used in hemorrhage</p> Signup and view all the answers

<p>Norepinephrine = Not effective by oral route Epinephrine = Client-side scripting for web applications Phenylephrine = Does not cause increase in heart rate R(-) 2-Amino-1-(3,4-dihydroxy-phenyl)-ethanol = Not effective orally</p> Signup and view all the answers

<p>Norepinephrine = Acute hypotensive states Epinephrine = Anaphylactic reactions Phenylephrine = Surgery to maintain blood pressure R(-) 1-(3,4-dihydroxy-phenyl)-2-N-methylamino-ethanol = Nasal congestion</p> Signup and view all the answers

<p>Xylometazoline = a1-agonist, vasoconstrictor Oxymetazoline = a1-agonist, nasal decongestant Clonidine hydrochloride = Selective a2-agonist Methyl dopa = Centrally acting a2-agonist</p> Signup and view all the answers

<p>Isoproterenol = Short duration Salmeterol = Very long acting (12 hours) Dobutamine = Used in congestive heart failure Clonidine hydrochloride = Lower blood pressure</p> Signup and view all the answers

<p>Clonidine hydrochloride = Inhibit sympathetic nervous system output Dobutamine = Dopamine analogue Salmeterol = Direct selective β2 Methyl dopa = Suppress CNS sympathetic output</p> Signup and view all the answers

<p>Clonidine hydrochloride = CNS side effects: depression, anxiety Methoxamine = Dangerous adverse effects Salmeterol = Risk of cardiovascular events Isoproterenol = Potential for tachycardia</p> Signup and view all the answers

<p>Methoxamine = Bronchial asthma Dobutamine = Cardiac surgery Clonidine hydrochloride = Management of hypertension Methyl dopa = Used in pregnancy-induced hypertension</p> Signup and view all the answers

<p>Xylometazoline = Vasoconstriction Clonidine hydrochloride = Lowering blood pressure Oxymetazoline = Decongestant effect Methoxamine = Potential increase in blood pressure</p> Signup and view all the answers

<p>Methoxamine = β1 &amp; β2 Salmeterol = β2 Dobutamine = β1 Clonidine hydrochloride = α2</p> Signup and view all the answers

<p>Tolazoline = First dose phenomenon characterized by dizziness Prazosin = Improvement of bioavailability up to 90% Terazosin hydrochloride = Selective ß1-blockers Carvedilol = Mixed a/β-Blockers</p> Signup and view all the answers

<p>Prazosin = Short duration of action Terazosin hydrochloride = Long duration of action Labetalol = Short duration of action Carvedilol = Long duration of action</p> Signup and view all the answers

<p>Prazosin = Selective a1-antagonist Carvedilol = S(-) enantiomer is both an a and nonselective β-blocker Labetalol = R(+) enantiomer is an a1-blocker Tolazoline = Causes peripheral vasodilation</p> Signup and view all the answers

<p>Carvedilol = CNS side effects Terazosin hydrochloride = Improvement of bioavailability Prazosin = First dose phenomenon Labetalol = Mixed action with both a and β-blocking effects</p> Signup and view all the answers

<p>S(-) enantiomer of Carvedilol = Nonselective β-blocker R(OH),R(CH3) of Labetalol = Active β-blocker R(+) enantiomer of Carvedilol = a1-blocker R(OH),S(CH3) of Labetalol = Predominantly an a1-blocker</p> Signup and view all the answers

<p>Prazosin = Dizziness, palpitation, syncope with first dose Tolazoline = Peripheral vasodilation Labetalol = Mixed action on both receptors Terazosin hydrochloride = Long-acting a1-blocker</p> Signup and view all the answers

<p>Tolazoline = Peripheral vasodilator Prazosin = Selective a1-antagonist Labetalol = Mixed a/β-Blocker Terazosin hydrochloride = Selective a1-antagonist</p> Signup and view all the answers

<p>Carvedilol = S(-) enantiomer for nonselective blocking Labetalol = R(OH),S(CH3) is predominantly an a1 blocker Prazosin = Bioavailability of 55% Terazosin hydrochloride = Bioavailability improvement to 90%</p> Signup and view all the answers

<p>Amphetamine = Treatment of ADHD Propylhexedrine = Relief of nasal congestion D-(-)-Ephedrine = Nasal decongestant Phenoxybenzamine = Treatment of pheochromocytoma</p> Signup and view all the answers

<p>Carvedilol = CNS side effects Prazosin = First dose phenomenon effects Tolazoline = Used for vasodilation Terazosin hydrochloride = Better bioavailability than Prazosin</p> Signup and view all the answers

<p>Dextroamphetamine = S-isomer more potent than R-isomer Pseudoephedrine = Used as a nasal decongestant Non-selective α-antagonist = Reversible action causing vasodilatation Indirect Adrenergic agents = Act through the release of norepinephrine</p> Signup and view all the answers

<p>Amphetamine = Suppresses appetite Propylhexedrine = Used orally, I.V., I.M., and topically D-(-)-Ephedrine = (S,S) diastereomer of ephedrine Phenoxybenzamine = Forms a permanent covalent bond</p> Signup and view all the answers

<p>D-(-)-Ephedrine = Effective for asthma and hay fever Propylhexedrine = Nasal decongestant Pseudoephedrine = Alleviates nasal congestion symptoms Phenoxybenzamine = Non-selective (α1 and α2) inhibitor</p> Signup and view all the answers

<p>Propylhexedrine = Used topically for nasal congestion D-(-)-Ephedrine = Administered as nasal decongestant Phenoxybenzamine = Used for managing pheochromocytoma Amphetamine = Used for ADHD treatment</p> Signup and view all the answers

<p>Dextroamphetamine = More potent S-isomer Phenoxybenzamine = Irreversible α-adrenergic antagonist Pseudoephedrine = Directly reduces nasal congestion Amphetamine = Increases release of norepinephrine</p> Signup and view all the answers

<p>D-(-)-Ephedrine = Acts indirectly and as a nasal decongestant Propylhexedrine = Most active of the four isomers Phenoxybenzamine = Alleviates sympathetic effects Amphetamine = Also used to treat narcolepsy</p> Signup and view all the answers

<p>D-(-)-Ephedrine = Nasal decongestant agent Propylhexedrine = Adrenergic decongestant Amphetamine = Stimulant for ADHD Phenoxybenzamine = Alpha antagonist for tumors</p> Signup and view all the answers

<p>Propylhexedrine = Dilation of the pupil D-(-)-Ephedrine = Used in treating asthma Phenoxybenzamine = Results in tachycardia Amphetamine = Appetite suppressant</p> Signup and view all the answers

Drugs that act by reducing sympathetic nervous system activity in the central nervous system, leading to lowered blood pressure.

A type of antihypertensive drug that inhibits the release of norepinephrine from nerve endings, reducing sympathetic activity.

A vasodilator that works by opening potassium channels in arteries, causing them to relax and widen, lowering blood pressure.

A class of antihypertensive drugs that act by directly relaxing arterial blood vessels, leading to decreased peripheral resistance and lower blood pressure.

A type of antihypertensive drug that acts on the central nervous system to lower blood pressure. It is highly selective for the I1 receptor and has low affinity for the α2 receptor.

A powerful vasoconstrictor that directly stimulates both alpha and beta receptors. It is commonly used to raise blood pressure in emergencies. It's given intravenously due to poor oral absorption.

A potent drug that directly stimulates both alpha and beta receptors. It's used for anaphylactic reactions, asthma, and nasal congestion. It's administered via injection or inhalation.

A selective alpha-1 agonist that causes vasoconstriction. It's used orally for hypotension, nasal congestion and glaucoma. It has no impact on beta receptors, so it doesn't affect heart rate.

A selective alpha-1 agonist that helps to maintain blood pressure during surgery. It doesn't affect the central nervous system.

A type of drug that directly acts on alpha and/or beta receptors to cause a specific physiological response.

Alpha-1 receptors are responsible for vasoconstriction. Activation of these receptors causes blood vessels to narrow, increasing blood pressure.

Beta receptors are involved in heart rate and contractility. Beta-1 receptors primarily affect the heart, while Beta-2 receptors mainly influence bronchodilation.

A beta-agonist that directly stimulates both beta-1 and beta-2 receptors. Used for relief of bronchospasms and bronchial asthma. Can be administered by inhalation, injection, or sublingual.

A direct beta-2 agonist that is more effective than isoproterenol but has a shorter duration of action. Taken orally.

A selective beta-2 agonist with very long acting (12 hours) due to its lipophilic Phenyl alkyl substituent on nitrogen. This means it stays in the body longer and works for a longer time.

A direct beta-1 agonist that is a dopamine analogue. It is used as a cardiac stimulant after surgery and in congestive heart failure.

Alpha-1 agonists that are vasoconstrictors. Used in ophthalmic (eye) and nasal decongestants.

A selective alpha-2 agonist that stimulates alpha-2 receptors in the central nervous system (CNS). This causes inhibition of sympathetic output, which lowers blood pressure.

A centrally acting alpha-2 agonist that inhibits the sympathetic nervous system output, leading to lower blood pressure. It is no longer used due to its side effects in the CNS, such as depression, anxiety, and Parkinsonism.

A stimulant drug that indirectly activates the sympathetic nervous system by releasing norepinephrine from presynaptic nerve terminals. Used for treating conditions like ADHD and narcolepsy, and also for suppressing appetite.

A specific isomer of amphetamine, known for its effectiveness in treating narcolepsy and ADHD. It's also used to suppress appetite.

An indirect adrenergic agent used as a nasal decongestant, acting on the sympathetic nervous system to relieve congestion. It can also be used orally, intravenously, intramuscularly, and topically.

A naturally occurring indirect adrenergic agent, found in ephedra plants. It acts as a nasal decongestant and bronchodilator, directly stimulating adrenergic receptors.

A diastereomer of ephedrine, commonly used as a nasal decongestant. It acts indirectly by releasing norepinephrine from nerve terminals, stimulating the sympathetic response.

A non-selective alpha-adrenergic antagonist that irreversibly binds to alpha receptors, leading to vasodilation. It's used to alleviate the effects of pheochromocytoma, a condition that causes excessive adrenaline release.

A non-selective alpha-adrenergic antagonist that binds reversibly to alpha receptors, causing vasodilation and tachycardia. Primarily used to treat pheochromocytoma.

A group of drugs that act on alpha receptors in the sympathetic nervous system. These drugs can either stimulate (agonists) or block (antagonists) the actions of adrenaline and noradrenaline, leading to various effects like vasoconstriction, dilation, and heart rate changes.

A condition characterized by excessive release of adrenaline and noradrenaline from the adrenal gland tumors, leading to symptoms like high blood pressure, headaches, and palpitations.

The state of a drug binding to its receptor and triggering a biological response. It refers to the activation of the receptor by the drug.

Tolazoline is a selective alpha-1 antagonist producing peripheral vasodilation. Its unique initial response, often characterized by dizziness, palpitations, and syncope, is called the "first dose phenomenon".

Prazosin is another selective alpha-1 antagonist, similar to Tolazoline. However, its structural variations lead to a significantly faster metabolic rate, resulting in a higher bioavailability (90%) compared to Tolazoline (55%).

Terazosin Hydrochloride is a selective alpha-1 antagonist, just like Tolazoline and Prazosin. Its unique characteristic is a short duration of action, leading to rapid effects but also a short-lived effect.

Carvedilol is a mixed alpha/beta-blocker, meaning it affects both alpha and beta receptors. The S(-) enantiomer is a potent alpha and nonselective beta blocker, while the R(+) enantiomer is a selective alpha-1 blocker.

Labetalol has a unique combination of alpha and beta blocking properties. The R(OH),R(CH3) is the active beta blocker, while the R(OH),S(CH3) diastereomer works primarily as an alpha-1 blocker.

Beta 1-Blockers target Beta 1 receptors, typically found in the heart. They are commonly used to manage conditions like high blood pressure and irregular heart rhythms.

Most beta-blockers have a specific duration of action - they are either short-acting or long-acting. This duration determines how often they need to be taken and how long their effects last.

Short-acting beta-blockers have a relatively brief duration of action, requiring more frequent administration. Their effects wear off quickly, often within a few hours.

Long-acting beta-blockers provide a longer duration of action. They are often given once a day or twice a day, providing extended control throughout the day.

Central Nervous System (CNS) side effects are common with medications that target the nervous system, including beta-blockers. These effects can vary from mild to severe, and can impact things like mood, sleep, and cognitive function.