p.1
Adrenoceptor Agonists and Antagonists
What are adrenoceptor agonists?
Substances that activate adrenoceptors, mimicking the effects of adrenaline.
p.1
Adrenoceptor Agonists and Antagonists
What are adrenoceptor antagonists?
Substances that block adrenoceptors, inhibiting the effects of adrenaline.
p.1
Adrenergic Receptor Types and Functions
What is the primary function of adrenoceptors?
To mediate the effects of catecholamines like adrenaline and noradrenaline.
p.1
Clinical Applications of Adrenergic Drugs
What is the role of Dr. Ravi Rajput in the context of adrenoceptor research?
Professor specializing in adrenoceptor agonists and antagonists.
p.2
Sympathetic Nervous System Function
What should students apply knowledge of to understand medications acting on the sympathetic nervous system?
Anatomy, physiology, and cell biology.
p.2
Sympathetic Nervous System Function
What are the two main divisions of the autonomic nervous system?
Sympathetic and parasympathetic nervous systems.
p.22
Mechanisms of Action of Adrenergic Drugs
What is the mechanism of action of Tizanidine?
Presynaptic inhibition of motor neurons, blocking nerve impulses and decreasing spasticity without reducing muscle strength.
p.15
Direct and Indirect Sympathomimetics
What characterizes direct-acting sympathomimetic drugs?
They directly stimulate adrenergic receptors.
p.54
Clinical Applications of Adrenergic Drugs
How does Propranolol promote fibrinolysis?
By preventing platelet aggregation and promoting the breakdown of clots.
p.30
Mechanisms of Action of Adrenergic Drugs
What effect does norepinephrine have on peripheral vascular resistance?
It increases peripheral vascular resistance.
p.4
Neurotransmitters and Receptors
Where are receptors typically located?
On the surface of cells or within cells.
p.24
Adrenergic Receptor Types and Functions
What is the primary function of β3 selective agonists in the bladder?
They relax the detrusor muscle.
p.52
Adverse Effects of Adrenergic Medications
What is a metabolic effect of Propranolol?
It can lead to a deranged lipid profile, increasing total TG and LDL while decreasing HDL.
p.40
Clinical Applications of Adrenergic Drugs
What type of drug is amphetamine?
A powerful CNS stimulant.
p.39
Neurotransmitters and Receptors
What is tyramine?
A compound not used clinically.
p.39
Neurotransmitters and Receptors
In which foods is tyramine commonly found?
Cheese, beef, wine, beer, yoghurt, and yeast.
p.46
Clinical Applications of Adrenergic Drugs
How do Tamsulosin and Silodosin affect blood pressure compared to non-selective α blockers?
They have little effect on blood pressure.
p.8
Neurotransmitters and Receptors
What is the rate-limiting step in the synthesis of norepinephrine?
Tyrosine is hydroxylated by tyrosine hydroxylase (TH) to DOPA.
p.26
Adrenergic Receptor Types and Functions
What is the effect of α1 receptors in response to epinephrine?
Constriction of arterioles.
p.3
Neurotransmitters and Receptors
What should a student be able to recall regarding sympathetic neurons?
The location of cell bodies, autonomic ganglia, and axonal trajectories of preganglionic and postganglionic axons.
p.43
Adrenergic Receptor Types and Functions
What type of antagonist is phenoxybenzamine?
Nonselective antagonist at α1 and α2 receptors.
p.50
Beta-Blockers and Their Uses
How does Propranolol affect blood pressure in normal individuals?
Least affected compared to asthmatic patients.
p.8
Neurotransmitters and Receptors
What are the mechanisms for the termination of norepinephrine action?
Diffusion and reuptake by norepinephrine transporter (NET) or dopamine transporter (DAT).
p.34
Adrenergic Receptor Types and Functions
What receptors does Isoproterenol act on?
β1, β2, and β3, but no α action.
p.27
Adrenergic Receptor Types and Functions
How does epinephrine affect gut muscle?
It causes gut relaxation via α2 and β effects.
p.19
Sympathetic Nervous System Function
What effect does α1 stimulation have on peripheral vascular resistance and blood pressure?
It increases peripheral vascular resistance and blood pressure, which is associated with reflex bradycardia.
p.24
Adrenergic Receptor Types and Functions
How does the affinity of β3 receptors compare to β1 and β2 receptors?
β3 receptors have lower affinity compared to β1 and β2 receptors.
p.52
Adverse Effects of Adrenergic Medications
What effect does Propranolol have on glucose levels in normal individuals?
It has minimal effects on basal glucose levels.
p.38
Adverse Effects of Adrenergic Medications
What is one potential adverse effect of indirectly acting sympathomimetics?
Increased anxiety or agitation.
p.51
Clinical Applications of Adrenergic Drugs
What symptoms does the patient report before public speaking?
Rapid heart rate and diaphoresis.
p.31
Clinical Applications of Adrenergic Drugs
What effect does high-dose dopamine (> 10 mcg/kg/min) have?
May increase blood pressure and stimulate vasoconstriction.
p.26
Adrenergic Receptor Types and Functions
What is the effect of β2 receptors in response to epinephrine?
Dilation predominates in skeletal muscle, liver, and coronaries.
p.62
Clinical Applications of Adrenergic Drugs
What are α1 selective agonists used for?
They are used to increase vascular resistance and blood pressure.
p.3
Catecholamines and Their Metabolism
What should be correlated with the mechanisms of action of sympathetic medications?
The synthesis, storage, release, and termination of action of epinephrine, norepinephrine, and dopamine.
p.45
Mechanisms of Action of Adrenergic Drugs
Why does Prazosin cause lesser reflex tachycardia?
Due to lack of α2 blocking, which prevents the promotion of norepinephrine release.
p.28
Adverse Effects of Adrenergic Medications
What are some CNS side effects of epinephrine?
Anxiety, tremors, headache, and cerebral hemorrhage.
p.2
Sympathetic Nervous System Function
What should students describe regarding the central control mechanism?
The central control mechanism of the autonomic nervous system (ANS).
p.43
Adverse Effects of Adrenergic Medications
What is a significant adverse effect of phenoxybenzamine?
Marked postural hypotension.
p.62
Clinical Applications of Adrenergic Drugs
What are the clinical uses of norepinephrine?
Primarily used in treating severe hypotension and shock.
p.12
Mechanisms of Action of Adrenergic Drugs
What is the function of the α2 adrenergic receptor?
Inhibits further release of norepinephrine (NE) from the presynaptic adrenergic neuron.
p.53
Beta-Blockers and Their Uses
What is the cardiovascular use of Propranolol in Congestive Cardiac Failure (CCF)?
It prevents β1 hyperactivity and remodeling, retarding progression and prolonging life.
p.53
Adverse Effects of Adrenergic Medications
Why is Propranolol contraindicated in Prinzmetal’s angina?
Because β blocking will unmask α receptors, causing coronary vasoconstriction.
p.30
Clinical Applications of Adrenergic Drugs
In which conditions is norepinephrine used for hypotensive states?
Surgical shock and myocardial infarction (MI).
p.30
Clinical Applications of Adrenergic Drugs
How is norepinephrine used in conjunction with local anesthetics?
It is used to prolong the effects of local anesthetics.
p.10
Catecholamines and Their Metabolism
What are neuronal reuptake inhibitors and give examples?
Drugs like Cocaine and Tricyclic antidepressants that potentiate the effect of norepinephrine (NE) and epinephrine (E).
p.59
Beta-Blockers and Their Uses
What is a benefit of Metoprolol in patients with peripheral vascular disease (PVD)?
Safer because it has no β2 blockade.
p.20
Clinical Applications of Adrenergic Drugs
What effect do α2 selective agonists have on aqueous humor secretion in the eye?
They reduce aqueous humor secretion.
p.55
Clinical Applications of Adrenergic Drugs
How does Propranolol help in alcohol withdrawal?
It reduces sympathetic overactivity.
p.39
Neurotransmitters and Receptors
How is tyramine metabolized in the body?
By monoamine oxidase (MAO).
p.55
Clinical Applications of Adrenergic Drugs
How does Propranolol affect hyperthyroidism?
It reduces sympathetic overactivity and inhibits conversion of T4 to T3.
p.32
Adverse Effects of Adrenergic Medications
What are some adverse effects of dopamine?
Nausea, vomiting, tachycardia, hypertension, ectopic beats, and arrhythmias.
p.23
Clinical Applications of Adrenergic Drugs
What is one use of β2 selective agonists?
Immediate relief of asthma.
p.32
Clinical Applications of Adrenergic Drugs
In what conditions is dopamine used?
Cardiogenic shock, congestive cardiac failure (CCF), liver and renal failure, and hypotensive states.
p.28
Adverse Effects of Adrenergic Medications
What cardiovascular side effects can occur with epinephrine?
Angina, palpitations, and arrhythmias.
p.60
Adverse Effects of Adrenergic Medications
What are some adverse effects of Labetolol?
Postural hypotension and hepatotoxicity.
p.2
Neurotransmitters and Receptors
What types of fibers are involved in the functions of the peripheral nervous system (PNS)?
Noradrenergic and cholinergic fibers.
p.13
Adrenergic Receptor Types and Functions
What role do α1 adrenergic receptors play in male sex organs?
They facilitate ejaculation via the vas deferens.
p.62
Mechanisms of Action of Adrenergic Drugs
What is the mechanism of action of epinephrine?
It stimulates both α and β adrenergic receptors, leading to increased heart rate and blood pressure.
p.13
Adrenergic Receptor Types and Functions
What is the effect of α1 adrenergic receptors on the kidneys?
They decrease renin release.
p.12
Adrenergic Receptor Types and Functions
Where is the α2 adrenergic receptor primarily located?
On the presynaptic region.
p.22
Adrenergic Receptor Types and Functions
What type of drug is Tizanidine?
A centrally acting alpha 2 - adrenoceptor agonist.
p.57
Adverse Effects of Adrenergic Medications
What is the first step in treating a propranolol overdose?
Maintain ABC (Airway, Breathing, Circulation).
p.6
Catecholamines and Their Metabolism
What are catecholamines?
Compounds containing a catechol moiety.
p.22
Clinical Applications of Adrenergic Drugs
What condition is Tizanidine primarily used to manage?
Spasticity associated with multiple sclerosis (MS).
p.15
Direct and Indirect Sympathomimetics
What are the three classifications of sympathomimetic drugs?
Direct-acting, Indirect-acting, and Mixed-acting sympathomimetics.
p.58
Clinical Applications of Adrenergic Drugs
What is the primary use of Timolol?
Open angle glaucoma as eye drops.
p.15
Direct and Indirect Sympathomimetics
What is the mechanism of action for indirect-acting sympathomimetics?
They increase the release of norepinephrine or inhibit its reuptake.
p.6
Catecholamines and Their Metabolism
Name three examples of catecholamines.
Epinephrine (Adrenaline), Norepinephrine (Noradrenaline), and Dopamine.
p.53
Beta-Blockers and Their Uses
How does Propranolol affect cardiac workload in stable angina?
It decreases cardiac workload, leading to a decrease in myocardial oxygen demand.
p.15
Direct and Indirect Sympathomimetics
What do mixed-acting sympathomimetics do?
They both directly stimulate adrenergic receptors and increase norepinephrine release.
p.58
Clinical Applications of Adrenergic Drugs
What class of anti-arrhythmic drug is Sotalol?
Class III anti-arrhythmic drug.
p.54
Beta-Blockers and Their Uses
What is the cardiovascular use of Propranolol in arrhythmias?
Effective in all supraventricular arrhythmias due to an increase in refractory period at the AV node.
p.34
Adrenergic Receptor Types and Functions
What receptors does Epinephrine (Epi) act on?
α1, α2, β1, β2, and weak β3.
p.36
Mechanisms of Action of Adrenergic Drugs
What happens when epinephrine (Epi) is given after pretreatment with an α blocker?
Hypotension due to predominant β2 effect.
p.54
Beta-Blockers and Their Uses
How does Propranolol affect myocardial infarction?
It decreases the incidence, recurrence, and mortality with long-term use.
p.34
Adrenergic Receptor Types and Functions
What receptors does Norepinephrine (NE) act on?
α1, α2, β1, and β3, but no β2 action.
p.47
Clinical Applications of Adrenergic Drugs
What is Yohimbine primarily used for?
To treat male sexual dysfunction.
p.16
Direct and Indirect Sympathomimetics
What are direct-acting sympathomimetics?
Drugs that act directly on one or more of the adrenergic receptors.
p.5
Neurotransmitters and Receptors
What hormones are released by the adrenal medulla?
Epinephrine and norepinephrine.
p.10
Catecholamines and Their Metabolism
What are MAO-A inhibitors and provide examples?
Inhibitors like Clorgyline and Moclobemide, which are present in adrenergic neurons, intestine, liver, kidney, and placenta; rarely used in depression.
p.41
Adrenergic Receptor Types and Functions
What are adrenergic antagonists?
Drugs that block adrenergic receptors, inhibiting the effects of catecholamines.
p.61
Mechanisms of Action of Adrenergic Drugs
How does Carvedilol contribute to cardioprotection?
By inhibiting free radical induced lipid peroxidation and smooth muscle mitogenesis, and blocking L-type voltage gated Ca2+ channels.
p.31
Clinical Applications of Adrenergic Drugs
What is the effect of low-dose dopamine infusion?
May increase urine output and renal blood flow.
p.41
Adverse Effects of Adrenergic Medications
What are potential adverse effects of adrenergic antagonists?
Hypotension, bradycardia, and fatigue.
p.55
Clinical Applications of Adrenergic Drugs
What effect does Propranolol have on esophageal varices and portal hypertension?
It reduces bleeding and portal pressure.
p.39
Adverse Effects of Adrenergic Medications
What can happen if a patient on MAO inhibitors consumes tyramine?
It can trigger a hypertensive crisis.
p.3
Sympathetic Nervous System Function
What knowledge should be applied to understand medications acting on the parasympathetic nervous system?
Knowledge of anatomy, physiology, and cell biology.
p.2
Sympathetic Nervous System Function
What should students be able to compare regarding the sympathetic and parasympathetic nervous systems?
Organization, functions, location of cell bodies, ganglia, number of synapses, and effects on target tissues.
p.44
Clinical Applications of Adrenergic Drugs
What is a therapeutic use of Phentolamine in peripheral vascular disease?
To decrease peripheral vascular resistance.
p.2
Sympathetic Nervous System Function
What role does the autonomic nervous system (ANS) play in the body?
Maintenance of homeostasis.
p.13
Adrenergic Receptor Types and Functions
What is the function of α1 adrenergic receptors in the bladder?
Contraction of the trigone, sphincter, and prostatic urethra, leading to urinary retention.
p.2
Adverse Effects of Adrenergic Medications
What signs and symptoms should students recognize related to the ANS?
Signs and symptoms of ANS dysfunction.
p.21
Clinical Applications of Adrenergic Drugs
How does Clonidine help in the management of withdrawal symptoms?
It reduces sympathetic hyperactivity associated with withdrawal.
p.11
Mechanisms of Action of Adrenergic Drugs
What is the effect of Alpha2 adrenergic receptors on neurotransmitter release?
Decreases transmitter release in nerves.
p.21
Clinical Applications of Adrenergic Drugs
How does Clonidine help diabetic patients?
It controls diarrhea by reducing Aqueous Humor secretion.
p.54
Clinical Applications of Adrenergic Drugs
What effect does Propranolol have on platelet aggregation?
It prevents platelet aggregation.
p.16
Direct and Indirect Sympathomimetics
How do direct-acting sympathomimetics function?
By binding to adrenergic receptors.
p.27
Adrenergic Receptor Types and Functions
What is the effect of epinephrine on GIT sphincters?
Constriction via α1 effect.
p.7
Neurotransmitters and Receptors
What role does dopamine play in the brain?
It acts as a neurotransmitter.
p.33
Adrenergic Receptor Types and Functions
What type of receptors does Isoproterenol act on?
β1, β2, and β3 receptors.
p.38
Direct and Indirect Sympathomimetics
What are indirectly acting sympathomimetics?
Drugs that increase the levels of neurotransmitters in the synaptic cleft without directly stimulating adrenergic receptors.
p.59
Beta-Blockers and Their Uses
How do β1 selective blockers affect lipid profiles?
They have less deleterious effect on lipid profile.
p.31
Neurotransmitters and Receptors
What receptors does dopamine (DA) act on?
D1, D2, β1, with little α action.
p.46
Adrenergic Receptor Types and Functions
Where is α1A located?
On the bladder neck and urethra.
p.40
Adverse Effects of Adrenergic Medications
What is a downside of amphetamine use in ADHD?
Errors increase despite improved performance on simple tasks.
p.44
Clinical Applications of Adrenergic Drugs
How does Phentolamine affect peripheral vascular resistance?
It decreases peripheral vascular resistance.
p.32
Mechanisms of Action of Adrenergic Drugs
What effect does dopamine have on renal blood flow?
It maintains renal blood flow (D1 effect).
p.48
Beta-Blockers and Their Uses
What distinguishes carvedilol and labetalol from other β-blockers?
They are α- and β-antagonists.
p.28
Clinical Applications of Adrenergic Drugs
What is one of the primary uses of epinephrine?
To treat anaphylactic shock.
p.2
Neurotransmitters and Receptors
What components should students recognize in the somatic and autonomic nervous systems?
Neurotransmitters, receptors, agonists, and antagonists.
p.25
Sympathetic Nervous System Function
What effect does Dobutamine have on the His-Purkinje system?
Increases conduction velocity.
p.3
Adrenoceptor Agonists and Antagonists
What should be compared regarding adrenergic agonists and antagonists?
Their receptor profile, molecular mechanisms of action, clinical benefits, drug interactions, contraindications, rationale for use, and adverse effects.
p.11
Mechanisms of Action of Adrenergic Drugs
What signaling pathway is associated with Alpha1 adrenergic receptors?
Gq, leading to IP3 and DAG production.
p.13
Adrenergic Receptor Types and Functions
How do α1 adrenergic receptors affect the liver?
They increase glycogenolysis.
p.28
Clinical Applications of Adrenergic Drugs
In what situation is epinephrine used for cardiac resuscitation?
To reverse sudden cardiac arrest via the intracardiac route.
p.27
Adrenergic Receptor Types and Functions
What effect does epinephrine have on bronchial smooth muscle?
Bronchodilation via β2 effect.
p.27
Adrenergic Receptor Types and Functions
How does epinephrine affect bronchial secretion?
It decreases bronchial secretion via α1 effect.
p.30
Adverse Effects of Adrenergic Medications
What is a potential adverse effect of norepinephrine in cardiogenic shock?
It may cause renal shutdown.
p.19
Clinical Applications of Adrenergic Drugs
What are the common uses of Phenylephrine?
Nasal decongestant, mydriatic, and rarely for hypotension.
p.9
Catecholamines and Their Metabolism
Is COMT present in adrenergic neurons?
No, COMT is absent in adrenergic neurons.
p.61
Mechanisms of Action of Adrenergic Drugs
What are the prominent actions of Carvedilol?
It has prominent β1 and β2 blockade, with lesser α1 blockade.
p.20
Mechanisms of Action of Adrenergic Drugs
How do α2 selective agonists affect norepinephrine (NE) release?
They stimulate presynaptic α2 receptors on postganglionic sympathetic neurons to suppress NE release.
p.52
Clinical Applications of Adrenergic Drugs
How does Propranolol affect performance anxiety?
It suppresses performance anxiety.
p.50
Beta-Blockers and Their Uses
What is the effect of Propranolol on blood pressure after chronic use?
Patients show a gradual fall in blood pressure.
p.50
Beta-Blockers and Their Uses
What is the effect of Propranolol on cardiac output?
It decreases cardiac output.
p.3
Adrenergic Receptor Types and Functions
What should be correlated regarding adrenergic and dopaminergic receptors?
Their subtypes, anatomical locations, signaling mechanisms, and physiological responses to stimulation.
p.37
Clinical Applications of Adrenergic Drugs
What is the role of Phenylephrine in adrenergic therapy?
It is used as a nasal decongestant.
p.2
Adrenergic Receptor Types and Functions
What should students compare regarding epinephrine and norepinephrine?
Their effects based on affinities for alpha- and beta-adrenergic receptors and target tissues.
p.14
Adrenergic Receptor Types and Functions
What effect do β1 adrenergic receptors have on the AV node?
Increases conduction velocity.
p.36
Mechanisms of Action of Adrenergic Drugs
What is the phenomenon called when Epi causes hypotension after α blocker pretreatment?
Dale’s vasomotor reversal phenomenon.
p.9
Catecholamines and Their Metabolism
What are the two main enzymes involved in the metabolism of catecholamines?
Monoamine Oxidase (MAO) and Catecholamine-O Methyltransferase (COMT).
p.7
Neurotransmitters and Receptors
What is epinephrine?
A hormone secreted by the adrenal medulla.
p.4
Neurotransmitters and Receptors
What types of signals do receptors respond to?
Neurotransmitters, hormones, and other signaling molecules.
p.5
Neurotransmitters and Receptors
How do norepinephrine and epinephrine affect the body?
They prepare the body for 'fight or flight' responses.
p.41
Beta-Blockers and Their Uses
What is the primary function of beta-adrenergic antagonists?
To block beta-adrenergic receptors, reducing heart rate and contractility.
p.51
Clinical Applications of Adrenergic Drugs
What is the primary condition the 23-year-old man is experiencing?
Situational anxiety related to public speaking.
p.31
Clinical Applications of Adrenergic Drugs
What happens at medium doses of dopamine (2 - 10 mcg/kg/min)?
May increase renal blood flow, cardiac output, heart rate, and cardiac contractility.
p.40
Clinical Applications of Adrenergic Drugs
In which condition does amphetamine increase performance of simple tasks?
ADHD (Attention Deficit Hyperactivity Disorder).
p.51
Mechanisms of Action of Adrenergic Drugs
What physiological changes occur when the patient takes propranolol?
Decreased cardiac output and decreased peripheral resistance.
p.50
Beta-Blockers and Their Uses
How does Propranolol affect myocardial oxygen demand?
It reduces myocardial oxygen demand.
p.32
Mechanisms of Action of Adrenergic Drugs
How does dopamine improve cardiac function?
Through its Beta 1 effect.
p.48
Beta-Blockers and Their Uses
What is a common suffix for β-blockers?
The names typically end in '-olol'.
p.43
Clinical Applications of Adrenergic Drugs
What is a primary use of phenoxybenzamine?
Treatment of pheochromocytoma.
p.62
Adrenergic Receptor Types and Functions
Where are α1 adrenergic receptors primarily located?
In vascular smooth muscle, leading to vasoconstriction.
p.28
Clinical Applications of Adrenergic Drugs
How does epinephrine help in respiratory emergencies?
It relieves bronchospasm and angioneurotic edema of the larynx.
p.11
Adrenergic Receptor Types and Functions
What type of tissues do Alpha1 adrenergic receptors affect?
Smooth muscle and glands.
p.62
Direct and Indirect Sympathomimetics
What are indirectly acting sympathomimetics?
Drugs that increase the release of norepinephrine from nerve terminals.
p.62
Clinical Applications of Adrenergic Drugs
What is the clinical use of dopamine?
Used in treating heart failure and shock, depending on the dose.
p.37
Clinical Applications of Adrenergic Drugs
What is the function of Mirabegron in adrenergic therapy?
It is used for bladder control.
p.49
Beta-Blockers and Their Uses
Is Propranolol selective or nonselective?
Nonselective (β1 & β2 competitive blocker).
p.47
Clinical Applications of Adrenergic Drugs
Are the uses of Yohimbine well-established?
No, the uses are unestablished.
p.4
Neurotransmitters and Receptors
What is the primary function of receptors?
To bind to specific molecules and initiate a cellular response.
p.4
Neurotransmitters and Receptors
How do receptors contribute to cellular communication?
By transmitting signals that influence cellular activity.
p.10
Catecholamines and Their Metabolism
What are MAO-B inhibitors and their use?
Inhibitors like Selegiline, present in dopaminergic neurons, brain, platelets, and liver; used in Parkinson's disease.
p.52
Adverse Effects of Adrenergic Medications
What is a specific effect of Propranolol in diabetic patients?
It decreases the formation of aqueous humor and blocks sympathetic manifestations of hypoglycemia.
p.44
Adrenergic Receptor Types and Functions
What type of antagonist is Phentolamine?
Competitive, reversible antagonist of α1 and α2 receptors.
p.32
Clinical Applications of Adrenergic Drugs
What is the recommended dose of dopamine for cardiogenic shock?
5 mcg - 10 mcg/kg/min IV.
p.60
Clinical Applications of Adrenergic Drugs
What is one of the uses of Labetolol?
Hypertension in pregnant women.
p.62
Neurotransmitters and Receptors
What is the primary mechanism of adrenergic transmission?
The release of catecholamines like epinephrine and norepinephrine that bind to adrenergic receptors.
p.3
Neurotransmitters and Receptors
What neurotransmitters are released by sympathetic neurons?
Preganglionic and postganglionic sympathetic neurons release specific neurotransmitters, along with hormones from the adrenal medulla.
p.13
Adrenergic Receptor Types and Functions
What is the function of α1 adrenergic receptors in the eye?
Contraction of the radial (dilator) muscle leading to mydriasis.
p.62
Mechanisms of Action of Adrenergic Drugs
How is adrenergic transmission terminated?
Through reuptake of neurotransmitters, enzymatic degradation, or diffusion away from the receptor site.
p.3
Clinical Applications of Adrenergic Drugs
What systems should be recognized in relation to sympathetic medications?
The autonomic and hormonal control of cardiovascular function and the renin-angiotensin-aldosterone system (RAAS).
p.48
Beta-Blockers and Their Uses
What type of β-blocker is Timolol?
It is a nonselective β-blocker.
p.8
Neurotransmitters and Receptors
What substances block the norepinephrine transporter (NET)?
Cocaine and tricyclic antidepressants (TCA).
p.14
Adrenergic Receptor Types and Functions
What is the function of β1 adrenergic receptors in the SA node?
Increase heart rate (HR).
p.14
Adrenergic Receptor Types and Functions
Where are β1 adrenergic receptors located?
SA node, AV node, atrial and ventricular muscle, His-Purkinje system, kidney.
p.43
Mechanisms of Action of Adrenergic Drugs
How does phenoxybenzamine affect peripheral vascular resistance?
It decreases peripheral vascular resistance.
p.14
Adrenergic Receptor Types and Functions
What effect do β2 adrenergic receptors have on blood vessels?
Vasodilation: decreases total peripheral resistance (TPR) and diastolic blood pressure (DBP).
p.14
Adrenergic Receptor Types and Functions
What is the role of β2 adrenergic receptors in skeletal muscle?
Increase glycogenolysis and contractility (tremor).
p.36
Mechanisms of Action of Adrenergic Drugs
What happens when epinephrine (Epi) is given after pretreatment with a β blocker?
Accentuated hypertensive effect.
p.9
Catecholamines and Their Metabolism
What do MAO and COMT inactivate?
Norepinephrine (NE) and Epinephrine (E).
p.9
Catecholamines and Their Metabolism
Where are MAO and COMT widely distributed?
In the liver, intestine, kidney, and brain.
p.17
Mechanisms of Action of Adrenergic Drugs
Which enzymes do indirect-acting sympathomimetics block?
They block metabolizing enzymes such as MAO and COMT.
p.20
Mechanisms of Action of Adrenergic Drugs
What is the primary mechanism of action for α2 selective agonists like clonidine?
Stimulates central α2 receptors to decrease sympathetic outflow.
p.29
Clinical Applications of Adrenergic Drugs
How does NorEpinephrine affect diastolic blood pressure (DBP)?
Increases DBP via α1 action.
p.41
Clinical Applications of Adrenergic Drugs
What are common clinical uses of adrenergic antagonists?
Management of hypertension, heart failure, and anxiety disorders.
p.50
Beta-Blockers and Their Uses
What is the primary cardiovascular effect of β1 blockade by Propranolol?
Decreased heart rate and myocardial contractility.
p.50
Beta-Blockers and Their Uses
What happens to peripheral vascular resistance with β1 blockade?
Peripheral vascular resistance rises.
p.31
Adverse Effects of Adrenergic Medications
What is a potential risk when administering high doses of dopamine?
Increased risk of tachyarrhythmias.
p.51
Mechanisms of Action of Adrenergic Drugs
How does propranolol affect peripheral resistance?
It decreases peripheral resistance.
p.8
Neurotransmitters and Receptors
What is the role of the vesicular monoamine transporter (VMAT)?
It stores neurotransmitters in vesicles.
p.32
Mechanisms of Action of Adrenergic Drugs
What effect does dopamine have on blood pressure?
It maintains blood pressure (Alpha 1 effect).
p.25
Sympathetic Nervous System Function
What effect does Dobutamine have on the AV node?
Increases conduction velocity.
p.23
Clinical Applications of Adrenergic Drugs
What is another use of β2 selective agonists?
To arrest uncomplicated premature labor.
p.62
Mechanisms of Action of Adrenergic Drugs
What is the mechanism of α2 selective agonists?
They inhibit norepinephrine release, leading to decreased sympathetic outflow.
p.28
Mechanisms of Action of Adrenergic Drugs
How does epinephrine affect histamine release?
It prevents the release of histamine from mast cells.
p.11
Mechanisms of Action of Adrenergic Drugs
What is the effect of Alpha1 adrenergic receptors on calcium levels?
Increases Ca2+, causing contraction and increased secretion.
p.11
Adrenergic Receptor Types and Functions
What type of tissues do Alpha2 adrenergic receptors primarily affect?
Nerve endings and some smooth muscle.
p.14
Adrenergic Receptor Types and Functions
What is the effect of β1 adrenergic receptors on the atrial and ventricular muscle?
Increases force of contraction and oxygen consumption.
p.11
Adrenergic Receptor Types and Functions
What tissues do Beta2 adrenergic receptors affect?
Smooth muscle, liver, and heart.
p.14
Adrenergic Receptor Types and Functions
What is the function of D1 receptors in the renal, mesenteric, and coronary vasculature?
Vasodilation: increases renal blood flow (RBF) and glomerular filtration rate (GFR).
p.54
Clinical Applications of Adrenergic Drugs
What does Propranolol prevent during a second attack of myocardial infarction?
It prevents ventricular fibrillation.
p.4
Neurotransmitters and Receptors
What are receptors?
Proteins that receive and respond to signals from neurotransmitters or hormones.
p.19
Catecholamines and Their Metabolism
Why is Phenylephrine not metabolized by MAO or COMT?
It is a non-catecholamine.
p.17
Mechanisms of Action of Adrenergic Drugs
What is one mechanism by which indirect-acting sympathomimetics work?
Releasing or displacing NE from vesicles of sympathetic nerve varicosities.
p.5
Neurotransmitters and Receptors
What is the role of acetylcholine in the sympathetic nervous system?
It acts as a neurotransmitter at the synapse between preganglionic and postganglionic neurons.
p.24
Clinical Applications of Adrenergic Drugs
What condition is Mirabegron used to treat?
Overactive bladder (urinary urgency and frequency).
p.52
Adverse Effects of Adrenergic Medications
How does Propranolol affect the central nervous system?
It can cause sedation, lethargy, and disturbances in sleep.
p.61
Clinical Applications of Adrenergic Drugs
What conditions is Carvedilol used to treat?
Congestive heart failure (CCF), hypertension, and angina.
p.26
Adrenergic Receptor Types and Functions
What are the primary receptors that epinephrine acts on at low, moderate, and high doses?
β2 (low dose) > β1 (moderate dose) = α1 (high dose) = α2.
p.26
Vascular Effects of Adrenergic Drugs
What vascular effects does epinephrine have?
Constriction of arterioles in skin, mucous membranes, viscera, and renal beds through α1; dilation in skeletal muscle, liver, and coronaries through β2.
p.48
Beta-Blockers and Their Uses
What is the main action of selective β1-blockers?
They primarily block β1 adrenoceptors, affecting the heart.
p.23
Adrenergic Receptor Types and Functions
What is the primary effect of β2 selective agonists?
Relaxant effect on bronchi and uterus.
p.50
Beta-Blockers and Their Uses
How does Propranolol affect renin secretion?
It decreases renin secretion due to β1 block.
p.37
Clinical Applications of Adrenergic Drugs
What are the three main therapeutic classifications of adrenergic drugs?
1. Pressor agents, 2. Cardiac stimulants, 3. Bronchodilators.
p.60
Mechanisms of Action of Adrenergic Drugs
What are the effects of Labetolol on peripheral vasodilation and bronchodilation?
It causes peripheral vasodilation and bronchodilation due to β2 agonistic action.
p.13
Adrenergic Receptor Types and Functions
What effect do α1 adrenergic receptors have on veins?
Contraction, which increases venous return.
p.49
Beta-Blockers and Their Uses
What receptors does Propranolol block?
Both β1 and β2 receptors.
p.7
Neurotransmitters and Receptors
What is norepinephrine?
A transmitter released by sympathetic nerve terminals.
p.17
Mechanisms of Action of Adrenergic Drugs
How do indirect-acting sympathomimetics affect NE transport?
They block the transport of NE into sympathetic neurons.
p.29
Clinical Applications of Adrenergic Drugs
How does NorEpinephrine affect systolic blood pressure (SBP)?
Increases SBP via β1 action.
p.55
Clinical Applications of Adrenergic Drugs
How is Propranolol used in the treatment of anxiety?
It blocks peripheral manifestations like palpitations, tremors, and sweating.
p.40
Clinical Applications of Adrenergic Drugs
How does amphetamine affect physical performance?
It improves physical performance.
p.48
Beta-Blockers and Their Uses
What is a characteristic of nonselective β-blockers?
They block both β1 and β2 adrenoceptors.
p.26
Clinical Applications of Adrenergic Drugs
What is the final cumulative effect of epinephrine on blood pressure?
Increase in SBP (systolic blood pressure) and decrease in DBP (diastolic blood pressure).
p.31
Neurotransmitters and Receptors
Does dopamine enter the blood-brain barrier (BBB) when given parenterally?
No, it does not enter the BBB.
p.50
Beta-Blockers and Their Uses
What respiratory effect does β2 blockade have in asthmatic patients?
It causes bronchoconstriction.
p.8
Neurotransmitters and Receptors
How is dopamine converted to norepinephrine?
Dopamine is hydroxylated to norepinephrine (NE) inside the vesicle.
p.56
Adverse Effects of Adrenergic Medications
What general symptom related to energy can Propranolol cause?
Fatigue and exercise intolerance.
p.56
Adverse Effects of Adrenergic Medications
How does Propranolol affect lipid profiles?
It can lead to an adverse lipid profile.
p.28
Clinical Applications of Adrenergic Drugs
How does epinephrine prolong the duration of local anesthetic agents?
By causing vasoconstriction.
p.17
Direct and Indirect Sympathomimetics
What do indirect-acting sympathomimetics do?
Increase the availability of norepinephrine (NE) or epinephrine to stimulate adrenergic receptors.
p.10
Catecholamines and Their Metabolism
What is the function of vesicular reuptake inhibitors?
They affect the storage of catecholamines; an example is Reserpine, which was used in hypertension but is now considered obsolete.
p.38
Direct and Indirect Sympathomimetics
How do indirectly acting sympathomimetics work?
They promote the release of norepinephrine or inhibit its reuptake.
p.41
Adrenergic Receptor Types and Functions
What is the primary function of alpha-adrenergic antagonists?
To block alpha-adrenergic receptors, leading to vasodilation and decreased blood pressure.
p.38
Direct and Indirect Sympathomimetics
What is a key effect of indirectly acting sympathomimetics?
Increased heart rate and blood pressure.
p.40
Clinical Applications of Adrenergic Drugs
What are some effects of amphetamine on wakefulness?
Increases alertness and decreases sense of fatigue.
p.52
Clinical Applications of Adrenergic Drugs
How does Propranolol affect portal venous pressure in cirrhotic patients?
It reduces portal venous pressure.
p.60
Beta-Blockers and Their Uses
What type of antagonist is Labetolol?
Mixed (α + β) antagonist.
p.26
Cardiac Effects of Adrenergic Drugs
How does epinephrine affect heart rate and cardiac output?
Stimulation of Beta-1 increases heart rate, force of contraction, and cardiac output.
p.23
Adrenergic Receptor Types and Functions
What is a notable characteristic of β2 selective agonists regarding cardiac stimulation?
They have minimal cardiac stimulant property.
p.25
Adrenergic Receptor Types and Functions
What is the function of the D-form of Dobutamine?
α1 antagonist and β1 agonist.
p.45
Clinical Applications of Adrenergic Drugs
How does Prazosin help in Benign Prostatic Hyperplasia (BPH)?
Improves urine outflow by relaxing smooth muscle in the bladder neck, prostate capsule, and prostatic urethra.
p.25
Clinical Applications of Adrenergic Drugs
What is the primary effect of Dobutamine on the heart muscle?
Increases force of contraction and oxygen consumption.
p.56
Adverse Effects of Adrenergic Medications
What can occur upon withdrawal from Propranolol?
Rebound hypertension due to upregulation of β receptors.
p.45
Mechanisms of Action of Adrenergic Drugs
What additional effect does Prazosin have related to phosphodiesterase?
It acts as a potent phosphodiesterase inhibitor, adding to its vasodilating effect.
p.37
Clinical Applications of Adrenergic Drugs
What type of drug is Terbutaline classified as?
Bronchodilator and uterine relaxant.
p.13
Adrenergic Receptor Types and Functions
What effect do α2 adrenergic receptors have on platelets?
They promote aggregation.
p.11
Clinical Applications of Adrenergic Drugs
What is the effect of Beta2 adrenergic receptors on smooth muscle?
Relaxes smooth muscle and increases glycogenolysis.
p.43
Clinical Applications of Adrenergic Drugs
What condition can phenoxybenzamine be used for besides pheochromocytoma?
Raynaud’s syndrome and frostbite.
p.48
Beta-Blockers and Their Uses
What is Pindolol classified as?
A nonselective β-blocker.
p.25
Mechanisms of Action of Adrenergic Drugs
What are the effects of Dobutamine?
More selective ionotropic and chronotropic effects.
p.25
Clinical Applications of Adrenergic Drugs
What is a primary use of Dobutamine?
Heart failure: it increases cardiac output and stroke volume without increasing heart rate.
p.43
Adverse Effects of Adrenergic Medications
What is a potential sexual side effect of phenoxybenzamine?
Inhibition of ejaculation.
p.11
Adrenergic Receptor Types and Functions
What tissues are influenced by Beta1 adrenergic receptors?
Cardiac muscle and the juxtaglomerular apparatus.
p.13
Adrenergic Receptor Types and Functions
What is the function of α2 adrenergic receptors at prejunctional nerve terminals?
They decrease transmitter release and norepinephrine synthesis.
p.11
Clinical Applications of Adrenergic Drugs
What is the primary effect of Beta1 adrenergic receptors?
Increases heart rate, force of contraction, and renin release.
p.11
Clinical Applications of Adrenergic Drugs
What is the effect of Dopamine1 (D1) receptors on renal vascular smooth muscle?
Relaxes renal vascular smooth muscle.
p.28
Adverse Effects of Adrenergic Medications
What are some contraindications for using epinephrine?
Hypertension, angina, hyperthyroidism, and concomitant use of MAO inhibitors.
p.13
Adrenergic Receptor Types and Functions
How do α2 adrenergic receptors affect the pancreas?
They decrease insulin secretion.
p.14
Adrenergic Receptor Types and Functions
What is the function of β2 adrenergic receptors in the pancreas?
Increase insulin secretion.
