[6] MIDTERMS | DRUGS ACTING ON THE ANS

Question 1

Major involuntary, unconscious, automatic portion of the nervous system

Answer 1

Autonomic Nervous System

Question 2

Major divisions of the ANS (3)

Answer 2

• Parasympathetic ANS
• Sympathetic ANS
• Enteric Nervous System

Question 3

The Enteric Nervous Systerm consists of the myencentric plexus of ____ and submucous plexus of ____

Answer 3

The Enteric Nervous Systerm consists of the myencentric plexus of Auerbach and submucous plexus of Meissner

Question 4

Sympathetic Nervous System

• Spinal Roots of Origin: ____ and ____ segments of the spinal cord
• Location of Ganglia: ____ that lie along the spinal column, some along the anterior aspect of the abdominal aorita
• Preganglionic Fibers: ____
• Postganglionic Fibers: ____

Answer 4

Sympathetic Nervous System

• Spinal Roots of Origin: thoracic (T1-T12) and lumbar (L1-L5) segments of the spinal cord
• Location of Ganglia: paravertebral chains that lie along the spinal column, some along the anterior aspect of the abdominal aorita
• Preganglionic Fibers: short
• Postganglionic Fibers: long

Question 5

Parasympathetic Nervous System

• Spinal Roots of Origin: ____ and ____ segments of the spinal cord
• Location of Ganglia: most are located in the organs innervated, more distant from the spinal cord
• Preganglionic Fibers: long
• Postganglionic Fibers: short

Answer 5

Parasympathetic Nervous System

• Spinal Roots of Origin: CN III, IX, X, and sacral segments of the spinal cord
• Location of Ganglia: most are located in the organs innervated, more distant from the spinal cord
• Preganglionic Fibers: long
• Postganglionic Fibers: short

Question 6

HORMONES IN ANS

• Sympathetic Division: ____
• Parasympathetic Division: ____

Answer 6

• Sympathetic Division: Norepinephrine
• Parasympathetic Division: Acetylcholine

Question 7

Sympathetic Effects on Organs:

• Pupils: ____ (α1)
• Heart Rate: ____ (β1)
• Heart Contractility: ____ (β1)
• Blood Vessels (skin, sphlanic): ____ (α1)
• Blood Vessels (skeletal): ____ (β2, M3)
• Bronchi: ____ (β2)
• GIT Walls: ____ (α2, β2)
• GIT Sphincters: ____ (α1)
• GIT Secretions: ____
• Bladder Wall: ____ (β2)
• Bladder Sphincter: ____ (α1)
• Uterus: ____ (α1) / ____ (β2)
• Penis: ____ (α)

Answer 7

Sympathetic Effects on Organs:

• Pupils: Mydriasis (α1)
• Heart Rate: Tachycardia (β1)
• Heart Contractility: Increased (β1)
• Blood Vessels (skin, sphlanic): Constriction (α1)
• Blood Vessels (skeletal): Dilation (β2, M3)
• Bronchi: Dilation (β2)
• GIT Walls: Relaxation (α2, β2)
• GIT Sphincters: Contraction (α1)
• GIT Secretions: no effect
• Bladder Wall: Relaxation (β2)
• Bladder Sphincter: Contraction (α1)
• Uterus: Contraction (α1) / Relaxation (β2)
• Penis: Ejaculation (α)

Question 8

The Parasympathetic Nervous Systerm is a ____.

____.

• Primary transmitter in all autonomic ganglia and at the synapses between parasympathetic postganglionic neurons and their effector cells
• Primary transmitter at the somatic (voluntary) skeletal muscle neurotransmitter junction.

Answer 8

The Parasympathetic Nervous Systerm is a Cholinergic System.

Acetylcholine

• Primary transmitter in all autonomic ganglia and at the synapses between parasympathetic postganglionic neurons and their effector cells
• Primary transmitter at the somatic (voluntary) skeletal muscle neurotransmitter junction.

Question 9

ADRENERGIC PHARMACOLOGY

SYMPATHOMIMETICS - Alpha-2 Adrenergic Effects on Tissues

• Adrenergic and Cholinergic Nerve Terminals - inhibits ____
• Platelets - stimulates ____
• Some vascular smooth muscle - ____
• Fat cells - inhibits ____
• Pancreatic B cells - inhibits ____

Answer 9

SYMPATHOMIMETICS - Alpha-2 Adrenergic Effects on Tissues

• Adrenergic and Cholinergic Nerve Terminals - inhibits transmitter release
• Platelets - stimulates aggregation
• Some vascular smooth muscle - contracts
• Fat cells - inhibits lipolysis
• Pancreatic B cells - inhibits insulin release

Question 10

The Sympathetic Nervous Systerm is an ____

____.

• Primary transmitter at the sympathetic postganglionic neuron-effector cell synapses in most tissues.
• EXCEPTIONS: eccrine sweat glands and vasodilators in the sympathetic fibers of skeletal muscles

Answer 10

The Sympathetic Nervous Systerm is an Adrenergic System

Norephinerphine

• Primary transmitter at the sympathetic postganglionic neuron-effector cell synapses in most tissues.
• EXCEPTIONS: eccrine sweat glands and vasodilators in the sympathetic fibers of skeletal muscles

Question 11

ADRENERGIC PHARMACOLOGY

SYMPATHOMIMETICS
Mode of Action:

• Direct activation of ____
• Indirect activation by increasing concentration of available ____ in the synapse - release of stored ____; Inhibition of reuptake

Answer 11

SYMPATHOMIMETICS
Mode of Action:

• Direct activation of adrenoceptors
• Indirect activation by increasing concentration of available catecholamines in the synapse - release of stored catecholamines; Inhibition of reuptake

Question 12

ADRENERGIC PHARMACOLOGY

SYMPATHOMIMETICS - Alpha-1 Adrenergic Effects on Tissues

• Most vascular smooth muscle - ____
• Pupillary dilator muscle - ____
• Pilomotor smooth muscle - ____
• Liver - stimulate ____

Answer 12

SYMPATHOMIMETICS - Alpha-1 Adrenergic Effects on Tissues

• Most vascular smooth muscle - contracts (increase vascular resistance)
• Pupillary dilator muscle - dilation (mydriasis)
• Pilomotor smooth muscle - contracts (erects hair)
• Liver - stimulate glycogenolysis

Question 13

ADRENERGIC PHARMACOLOGY

SYMPATHOMIMETICS - Beta-1 Adrenergic Effects on Tissues (Heart Function)

• Heart - stimulates ____ and ____
• Juxtaglomerular cells of kidney - stimulates ____

Answer 13

SYMPATHOMIMETICS - Beta-1 Adrenergic Effects on Tissues (Heart Function)

• Heart - stimulates rate and force
• Juxtaglomerular cells of kidney - stimulates renin

Question 14

ADRENERGIC PHARMACOLOGY

Adrenergic Receptors:
* α1: vasoconstriction, increases BP
* α2: decreases central sympathetic outflow
* β1: increased heart rate, conduction, and contractility
* β2: bronchodilation
* D1: vasodilation in splanchnic and renal vessels

Question 15

ADRENERGIC PHARMACOLOGY

SYMPATHOMIMETICS - Beta-2 Adrenergic Effects on Tissues

• Airway, uterine, and vascular smooth muscle - ____
• Liver - stimulates ____
• Pancreatic (B) cells - stimulates ____
• Somatic motor neuron terminals (voluntary muscles) - causes ____
• Heart - stimulates ____ and ____

Answer 15

SYMPATHOMIMETICS - Beta-2 Adrenergic Effects on Tissues

• Airway, uterine, and vascular smooth muscle - relaxes
• Liver - stimulates glycogenolysis
• Pancreatic (B) cells - stimulates insulin release
• Somatic motor neuron terminals (voluntary muscles) - causes tremor
• Heart - stimulates rate and force

Question 16

ADRENERGIC PHARMACOLOGY

SYMPATHOMIMETICS - Classifications (6)

Answer 16

1. Non-Selective Alpha Agonist
2. Alpha 1-selective
3. Alpha 2-selective
4. Non-selective Beta Agonist
5. Beta 1-selective
6. Beta 2-selective

Question 17

ADRENERGIC PHARMACOLOGY

Epinephrine

• ____ (non-selective, direct-acting)
• Activates ____ and ____
• Uses: Cardiac arrest, ____ (drug of choice), asthma, ____, hemostasis
• Side effects: ____, Tachycardia, ____, Hyperglycemia

Answer 17

Epinephrine

• Sympathomimetic (non-selective, direct-acting)
• Activates alpha and beta adrenergic receptors
• Uses: Cardiac arrest, anaphylaxis (drug of choice), asthma, COPD, hemostasis
• Side effects: Hypertension, Tachycardia, Ischemia, Hyperglycemia

Question 18

ADRENERGIC PHARMACOLOGY

Dopamine

• ____ (non-selective, direct-acting)
• Activates ____, ____, and ____ adrenergic receptors
• Uses: ____, heart failure
• Side effects: Cardiovascular disturbance, ____

Answer 18

Dopamine

• Sympathomimetic (non-selective, direct-acting)
• Activates α, β, and D1 adrenergic receptors
• Uses: Cardiogenic shock, heart failure
• Side effects: Cardiovascular disturbance, arrhythmias

Question 19

ADRENERGIC PHARMACOLOGY

Clonidine (Catapres)

• Sympathomimetic ( ____ )
• Activates ____ adrenergic receptors
• Uses: ____, Cancer pain, ____
• Side effect: ____, rebound hypertension, ____
• Taper use prior to discontinuation to avoid ____
• To treat rebound hypertension, administer ____

Answer 19

Clonidine (Catapres)

• Sympathomimetic (alpha 2-selective)
• Activates α2 adrenergic receptors
• Uses: Hypertension, Cancer pain, Opioid withdrawal
• Side effect: Sedation, rebound hypertension, dry mouth
• Taper use prior to discontinuation to avoid rebound hypertension
• To treat rebound hypertension, administer Phentolamine

Question 20

ADRENERGIC PHARMACOLOGY

Albuterol/Salbutamol

• Sympathomimetic ( ____ )
• Activates ____ in bronchial smooth muscle causing bronchodilation
• Uses: ____ (drug of choice), Tocolysis for ____ (terbutaline and ritodrine)
• Side effects: ____, Tremors, ____, Restlessness, ____ when used excessively, Loss of ____ (tolerance)
• May precipitate arrhytmias in patients with concurrent ____ and heart disease

Answer 20

Albuterol/Salbutamol

• Sympathomimetic (beta 2-selective)
• Activates beta 2-receptors in bronchial smooth muscle causing bronchodilation
• Uses: Acute asthmatic attacks (drug of choice), Tocolysis for preterm labor (terbutaline and ritodrine)
• Side effects: Tachycardia, Tremors, Nervousness, Restlessness, Arrhythmias when used excessively, Loss of responsiveness (tolerance)
• May precipitate arrhytmias in patients with concurrent COPD and heart disease

Question 21

ADRENERGIC PHARMACOLOGY

Methyldopa (Preeclampsia)

• Sympathomimetic ( ____ )
• Activates ____ adrenergic receptors
• Uses: Preeclampsia, ____
• Side effects: Sedation, ____

Answer 21

Methyldopa (Preeclampsia)

• Sympathomimetic (alpha 2-selective)
• Activates α2 adrenergic receptors
• Uses: Preeclampsia, gestational hypertension
• Side effects: Sedation, hemolytic anemia

Question 22

ADRENERGIC PHARMACOLOGY

Nursing Responsibilities:

• Monitor VS and UO
• C/I in patients with ____, narrow angle glaucoma, ____
• Report s/e: ____, palpitations, ____, dizziness, ____
• Continuous nasal spray can cause ____

Answer 22

Nursing Responsibilities:

• Monitor VS and UO
• C/I in patients with cardiac dysrhythmias, narrow angle glaucoma, cardiogenic shock
• Report s/e: tachycardia, palpitations, tremors, dizziness, HPN
• Continuous nasal spray can cause nasal congestion rebound

Question 23

ADRENERGIC PHARMACOLOGY

ADRENORECEPTOR BLOCKERS
Alpha Blockers

• Non-Selective: ____ (irreversible) and ____ (reversible)
• Alpha 1-Selective: ____
• Alpha 2-Selective: ____

Beta-Blockers

• Non-Selective: ____
• Beta 1-Selective: ____
• Beta 2-Selective: ____

Answer 23

ADRENORECEPTOR BLOCKERS
Alpha Blockers

• Non-Selective: Phenoxybenzamine (irreversible) and Phenotalamine (reversible)
• Alpha 1-Selective: Prazosin
• Alpha 2-Selective: Yohimbime

Beta-Blockers

• Non-Selective: Propranolol
• Beta 1-Selective: Atenolol
• Beta 2-Selective: Butoxamine

Question 24

ADRENERGIC PHARMACOLOGY

PHENOXYBENZAMINE

• ____ (alpha non-selective)
• Irreversibly blocks ____
• Uses: ____ (pre-surgical)
• Side effects: ____, ____, gastrointestinal irritation, ____
• Forms covalent bond with ____ (effects last for several days)

Answer 24

PHENOXYBENZAMINE

• Adrenergic antagonist (alpha non-selective)
• Irreversibly blocks alpha adrenergic receptors (α1>α2)
• Uses: Pheochromocytoma (pre-surgical)
• Side effects: Orthostatic hypotension, reflex tachycardia, gastrointestinal irritation, myocardial ischemia
• Forms covalent bond with α receptors (effects last for several days)

Question 25

# ADRENERGIC PHARMACOLOGY **PHENOTALAMINE, TOLAZOLINE** * Adrenergic antagonist ( ____ ) * Reversibly blocks alpha adrenergic receptors (α1>α2) * Uses: ____ (pre-surgical), antidote to ____, rebound hypertension * Side effects: Orthostatic hypotension, reflex tachycardia, gastrointestinal irritation

Answer 25

**PHENOTALAMINE, TOLAZOLINE** * Adrenergic antagonist (**alpha non-selective**) * Reversibly blocks alpha adrenergic receptors (α1>α2) * Uses: **Pheochromocytoma** (pre-surgical), **antidote to α1 agonist overdose**, rebound hypertension * Side effects: Orthostatic hypotension, reflex tachycardia, gastrointestinal irritation

Question 26

# ADRENERGIC PHARMACOLOGY **PRAZOSIN** * Adrenergic antagonist ( ____ ) * Selectively blocks ____ * Uses: ____, hypertension * Side effects: First dose orthostatic hypotension, Reflex tachycardia (less common and less severe compared to non selective types)

Answer 26

**PRAZOSIN** * Adrenergic antagonist (**alpha 1-selective**) * Selectively blocks **α1 adrenergic receptors** * Uses: **Benign prostatic hyperplasia (BPH)**, hypertension * Side effects: First dose orthostatic hypotension, Reflex tachycardia (less common and less severe compared to non selective types)

Question 27

# ADRENERGIC PHARMACOLOGY **PROPANOLOL** * Adrenergic antagonist ( ____ ) * Blocks ____. Blocks sympathetic effects on heart and BP. * Reduce ____ release * Uses: ____ prophylaxis (chest pain), hypertension, ____, migraine, ____, hyperthyroidism * Side effect: ____, ____, heart failure, CNS sedation, ____ * May mask symptoms of hypoglycemia in diabetics * ____ and ____ has combined alpha and beta blockade (may be used for pheochromocytoma)

Answer 27

**PROPANOLOL** * Adrenergic antagonist (**beta non-selective**) * Blocks **β1 and β2 receptors**. Blocks sympathetic effects on heart and BP. * Reduce **renin** release * Uses: **Angina prophylaxis (chest pain)**, hypertension, **arrhythmias**, migraine, **performance anxiety**, hyperthyroidism * Side effect: **Bronchospasm**, **AV block**, heart failure, CNS sedation, **erectile dysfunction** * May mask symptoms of hypoglycemia in diabetics * **Carvedilol and Labetalol** has combined alpha and beta blockade (may be used for pheochromocytoma)

Question 28

# ADRENERGIC PHARMACOLOGY **ATENOLOL** * Adrenergic antagonist ( ____ ) * Selectively blocks ____ receptors. Blocks sympathetic effects on heart and BP * Uses: Angina, ____, heart failure * Side effects: Bronchospasm (less common), AV block, ____, ____, erectile dysfunction

Answer 28

**ATENOLOL** * Adrenergic antagonist (**beta 1-selective**) * Selectively blocks **β1 receptors**. Blocks sympathetic effects on heart and BP * Uses: Angina, **hypertension**, heart failure * Side effects: Bronchospasm (less common), AV block, **heart failure**, **CNS sedation**, erectile dysfunction

Question 29

# ADRENERGIC PHARMACOLOGY **Nursing Responsibilities** * Monitor VS esp BP and HR * Report any complaint of ____ * For clients with DM, have ____ available and follow adjustment of insulin dose as ordered * Not to stop abruptly the medication * ____ from supine or sitting to standing position

Answer 29

**Nursing Responsibilities** * Monitor VS esp BP and HR * Report any complaint of **stuffy nose** * For clients with DM, have **glucagon** available and follow adjustment of insulin dose as ordered * Not to stop abruptly the medication * **Slowly rise** from supine or sitting to standing position

Question 30

# CHOLINERGIC PHARMACOLOGY ____. * Primary transmitter in all autonomic ganglia and at the synapses between parasympathetic postganglionic neurons and their effector cells. * Primary transmitter at the somatic (voluntary) skeletal muscle neuromuscular junction

Answer 30

**ACETYLCHOLINE** * Primary transmitter in all autonomic ganglia and at the synapses between parasympathetic postganglionic neurons and their effector cells. * Primary transmitter at the somatic (voluntary) skeletal muscle neuromuscular junction

Question 31

# CHOLINERGIC PHARMACOLOGY **CHOLINERGIC DRUG EFFECTS** * Not very useful for systemic therapy because their effects are not sufficiently selective - parasympathetic and sympathetic ganglia and somatic neuromuscular junctions all may be blocked * Botulinum toxin is a very large molecule and diffuses very slowly - injection for relatively selective local effects

Answer 31

**CHOLINERGIC DRUG EFFECTS** * Not very useful for systemic therapy because their effects are not sufficiently selective - parasympathetic and sympathetic ganglia and somatic neuromuscular junctions all may be blocked * Botulinum toxin is a very large molecule and diffuses very slowly - injection for relatively selective local effects

Question 32

# CHOLINERGIC PHARMACOLOGY **CHOLINORECEPTORS** * ____ - nerve endings * ____ - heart, some nerve endings * ____ - effector cells, smooth muscle glands, endothelium * ____ - ANS ganglia * ____ - neuromuscular end plate

Answer 32

**CHOLINORECEPTORS** * **M1** - nerve endings * **M2** - heart, some nerve endings * **M3** - effector cells, smooth muscle glands, endothelium * **N(N)** - ANS ganglia * **N(M)** - neuromuscular end plate

Question 33

# CHOLINERGIC PHARMACOLOGY **CHOLECEPTOR-ACTIVATING and CHOLINESTERASE-INHIBITING DRUGS** **Direct-Acting** * ____ - Choline Esters and Alkaloids * **Nicotinic** **Indirect-Acting** * ____ (short-acting) * **Carbamates** (intermediate to long-acting) * ____ (very long-acting)

Answer 33

**CHOLECEPTOR-ACTIVATING and CHOLINESTERASE-INHIBITING DRUGS** **Direct-Acting** * **Muscarinic** - Choline Esters and Alkaloids * **Nicotinic** **Indirect-Acting** * **Edrophonium** (short-acting) * **Carbamates** (intermediate to long-acting) * **Organophosphates** (very long-acting)

Question 34

# CHOLINERGIC PHARMACOLOGY **DIRECT-ACTING CHOLINOMIMETICS: Betanechol** * ____ (direct-acting, muscarinic) * Similar to ____ * Activates **muscarinic (M1-M3) receptors**. Act on M receptors only * Uses: **Bladder and bowel atony (post-surgery or spinal cord injury)** * Side effects: **Cyclospasm**, diarrhea, urinary urgency, **vasodilation**, **reflex tachycardia**, sweating

Answer 34

**DIRECT-ACTING CHOLINOMIMETICS: Betanechol** * **Cholinomimetic** (direct-acting, muscarinic) * Similar to **Carbachol** * Activates **muscarinic (M1-M3) receptors**. Act on M receptors only * Uses: **Bladder and bowel atony (post-surgery or spinal cord injury)** * Side effects: **Cyclospasm**, diarrhea, urinary urgency, **vasodilation**, **reflex tachycardia**, sweating

Question 35

# CHOLINERGIC PHARMACOLOGY **DIRECT-ACTING CHOLINOMIMETICS: Pilocarpine** * Cholinomimetic ( ____ ) * Activates ____ receptors in ciliary muscle (increasing aqueous humor outflow) and salivary glands (increasing salivation) * Uses: ____, ____ syndrome * Side effects: ____, Blurring of vision (due to cyclospasm)

Answer 35

**DIRECT-ACTING CHOLINOMIMETICS: Pilocarpine** * Cholinomimetic (**direct-acting, muscarinic**) * Activates **M3 receptors** in ciliary muscle (increasing aqueous humor outflow) and salivary glands (increasing salivation) * Uses: **Glaucoma**, **Sjogren syndrome** * Side effects: **Miosis**, Blurring of vision (due to cyclospasm)

Question 36

# CHOLINERGIC PHARMACOLOGY **DIRECT-ACTING CHOLINOMIMETICS: Pilocarpine** ____ - autoimmune disorder characterized by triad of: (3)

Answer 36

**DIRECT-ACTING CHOLINOMIMETICS: Pilocarpine** ***Sjogren Syndrome*** - autoimmune disorder characterized by triad of: * **xerostomia (dry mouth)** * **xerophthalmia (dry eyes)** * **rheumatoid arthritis**

Question 37

# CHOLINERGIC PHARMACOLOGY **INDIRECT-ACTING CHOLINOMIMETICS** * Bind to ____ and undergo prompt hydrolysis * No significant actions at uninnervated sites where **Ach** is not normally

Answer 37

**INDIRECT-ACTING CHOLINOMIMETICS** * Bind to **cholinesterase** and undergo prompt hydrolysis * No significant actions at uninnervated sites where **Ach** is not normally

Question 38

# CHOLINERGIC PHARMACOLOGY **DIRECT-ACTING CHOLINOMIMETICS: Muscarinic Toxicity** * CNS stimulation * Eye: ____ * Lungs: ____ * GIT/GUT: ____ gastrointestinal and genitourinary smooth muscle activity * Increased ____ * Vasodilation

Answer 38

**DIRECT-ACTING CHOLINOMIMETICS: Muscarinic Toxicity** * CNS stimulation * Eye: **Miosis, spasm of accommodation** * Lungs: **Bronchoconstriction** * GIT/GUT: **Excessive** gastrointestinal and genitourinary smooth muscle activity * Increased **secretory activity (sweat glands, airway, gastrointestinal tract, lacrimal glands)** * Vasodilation

Question 39

# CHOLINERGIC PHARMACOLOGY **DIRECT-ACTING CHOLINOMIMETICS: Nicotine** * ____ (direct-acting, nicotinic) * Activates nicotinic Ach receptors (Nn and Nm) * Uses: ____ * Side effects: ____ (hypertension, tachycardia, nausea, vomiting, diarrhea) * Overdose leads to ____, **paralysis**, and ____

Answer 39

**DIRECT-ACTING CHOLINOMIMETICS: Nicotine** * **Cholinomimetic** (direct-acting, nicotinic) * Activates nicotinic Ach receptors (Nn and Nm) * Uses: **Smoking cessation** * Side effects: **Generalized ganglionic stimulation** (hypertension, tachycardia, nausea, vomiting, diarrhea) * Overdose leads to **convulsion**, **paralysis**, and **coma**

Question 40

# CHOLINERGIC PHARMACOLOGY **DIRECT-ACTING CHOLINOMIMETICS: Muscarinic Toxicity** * **Ganglionic** stimulation * Blockade of **neuromuscular end plate depolarization** leading to fasciculations and paralysis * CNS Toxicity: stimulation (**convulsions**) followed by **CNS depression**

Answer 40

**DIRECT-ACTING CHOLINOMIMETICS: Muscarinic Toxicity** * **Ganglionic** stimulation * Blockade of **neuromuscular end plate depolarization** leading to fasciculations and paralysis * CNS Toxicity: stimulation (**convulsions**) followed by **CNS depression**

Question 41

# CHOLINERGIC PHARMACOLOGY **HYDROLYSIS** * Alcohol portion released * Acidic portion retained and released slowly 1. Prevents the binding and hydrolysis of ____ 2. Amplify ____ wherever Ach is released

Answer 41

**HYDROLYSIS** * Alcohol portion released * Acidic portion retained and released slowly 1. Prevents the binding and hydrolysis of **endrogenous acetylcholine** 2. Amplify **acetylcholine effects** wherever Ach is released

Question 42

# CHOLINERGIC PHARMACOLOGY **INDIRECT-ACTING CHOLINOMIMETICS: Edrophonium** * ____ (indirect-acting) * Inhibits ____, amplifies endogenously released acetylcholine * Uses: ____ (diagnosis – ____), differentiation of cholinergic crisis and myasthenic crisis * Side effects: ____, salivation, nausea, vomiting, diarrhea, ____ * Very short acting upon ____

Answer 42

**INDIRECT-ACTING CHOLINOMIMETICS: Edrophonium** * **Cholinomimetic** (indirect-acting) * Inhibits **acetylcholinesterase**, amplifies endogenously released acetylcholine * Uses: **Myasthenia gravis** (diagnosis – **Tensilon test**), differentiation of cholinergic crisis and myasthenic crisis * Side effects: **Miosis**, salivation, nausea, vomiting, diarrhea, **bradycardia** * Very short acting upon **IV administration**

Question 43

# CHOLINERGIC PHARMACOLOGY **INDIRECT-ACTING CHOLINOMIMETICS: Neostigmine** * Cholinomimetic (indirect-acting) * Inhibits acetylcholinesterase, amplifies endogenously released acetylcholine * Uses: Myasthenia gravis (treatment - drug of choice), reversal of nondepolarizing * neuromuscular blockade, glaucoma (Physostigmine/Pyridostigmine, echothiophate, demercarium) * Side effects: Miosis, salivation, nausea, vomiting, diarrhea, bradycardia * Muscarinic effects are blocked by atropine

Question 44

# CHOLINERGIC PHARMACOLOGY **INDIRECT-ACTING CHOLINOMIMETICS: Myasthenia Gravis** Autoimmune destruction of nicotinic Ach receptors characterized by: (4) ____ Crisis ( ____ ) Acute worsening of symptoms due to infection, stress or undermedication ____ Crisis ( ____ ) Excessive activation of cholinoreceptors (skeletal muscle weakness and parasympathetic signs) due to overmedication ***How does edrophonium differentiate myasthenic crisis from cholinergic crisis?*** * Improves muscle strength in ____ crisis * Weakens muscle strength in ____ crisis

Answer 44

**INDIRECT-ACTING CHOLINOMIMETICS: Myasthenia Gravis** Autoimmune destruction of nicotinic Ach receptors characterized by: * **Fluctuating muscle weakness** * **Ocular symptoms** * **Bulbar symptoms** * **Proximal muscle weakness** ***Myasthenic Crisis (Undermedication)*** Acute worsening of symptoms due to infection, stress or undermedication ***Cholinergic Crisis (Overmedication)*** Excessive activation of cholinoreceptors (skeletal muscle weakness and parasympathetic signs) due to overmedication ***How does edrophonium differentiate myasthenic crisis from cholinergic crisis?*** * Improves muscle strength in **myasthenic** crisis * Weakens muscle strength in **cholinergic** crisis

Question 45

# CHOLINERGIC PHARMACOLOGY **INDIRECT-ACTING CHOLINOMIMETICS: Atropine** * Prototype nonselective ____ * Found in ____ * ____ that readily crosses membrane barriers * Cholinergic antagonist (muscarinic) * Competitively blocks all muscarinic receptors * Uses: ____, cycloplegic, ____, bradycardia, hypersalivation (prevent ____) * Side effects: ____, ____, cycloplegia, skin flushing, ____, hallucinations

Answer 45

**INDIRECT-ACTING CHOLINOMIMETICS: Atropine** * Prototype nonselective **muscarinic blocker** * Found in **Atropa belladonna** * **Tertiary amine** that readily crosses membrane barriers * Cholinergic antagonist (muscarinic) * Competitively blocks all muscarinic receptors * Uses: **Mydriatic**, cycloplegic, **antidote for organophosphate poisoning (first choice)**, bradycardia, hypersalivation (prevent **asphyxiation**) * Side effects: **Tachycardia**, **mydriasis**, cycloplegia, skin flushing, **delirium**, hallucinations

Question 46

# CHOLINERGIC PHARMACOLOGY **INDIRECT-ACTING CHOLINOMIMETICS: Organophosphate Poisoning** * ____ - insecticide * ____ - nerve gases

Answer 46

**INDIRECT-ACTING CHOLINOMIMETICS: Organophosphate Poisoning** * **Malathion and Parathion** - insecticide * **Sarin, Tabun, and Soman** - nerve gases

Question 47

# CHOLINERGIC PHARMACOLOGY **INDIRECT-ACTING CHOLINOMIMETICS: Signs and Symptoms of Organophosphate Poisoning (DUMBBELSS)** * ____ * Urination * ____ * Bronchospasm * ____ * Excitation * ____ * Sweating * ____

Answer 47

**INDIRECT-ACTING CHOLINOMIMETICS: Signs and Symptoms of Organophosphate Poisoning (DUMBBELSS)** * **Diarrhea** * Urination * **Miosis** * Bronchospasm * **Bradycardia** * Excitation * **Lacrimation** * Sweating * **Salivation**

Question 48

# CHOLINERGIC PHARMACOLOGY **INDIRECT-ACTING CHOLINOMIMETICS: Atropine Toxicity** * ____ * ____ * Decreased secretions * Tachycardia * ____ * Constipation * Blurred vision * ____

Answer 48

**INDIRECT-ACTING CHOLINOMIMETICS: Atropine Toxicity** * **Atropine fever (hyperthermia)** * **Atropine flush (cutaneous vasodilation)** * Decreased secretions * Tachycardia * **Arrhythmias (intraventricular conduction blocks)** * Constipation * Blurred vision * **CNS toxicity**

Question 49

# CHOLINERGIC PHARMACOLOGY **INDIRECT-ACTING CHOLINOMIMETICS: Atropine Toxicity Mnemonic** * Hot as a ____ * ____ as a bone * Red as a ____ * ____ as a bat * Mad as a ____

Answer 49

**INDIRECT-ACTING CHOLINOMIMETICS: Atropine Toxicity Mnemonic** * Hot as a **hare** * **Dry** as a bone * Red as a **beet** * **Blind** as a bat * Mad as a **hatter**

Question 50

# CHOLINERGIC PHARMACOLOGY **INDIRECT-ACTING CHOLINOMIMETICS: C/I to Muscarinic Blockers** * Cautious use in infants - ____ due to decreased sweating * ____ (causes increases intraocular pressure) * Benign ____

Answer 50

**INDIRECT-ACTING CHOLINOMIMETICS: C/I to Muscarinic Blockers** * Cautious use in infants - **hyperthermia** due to decreased sweating * **Acute angle-closure glaucoma** (causes increases intraocular pressure) * **Benign prostatic hyperplasia**