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NR-NUR124 | Pharmacology > [6] MIDTERMS | DRUGS ACTING ON THE ANS > Flashcards

[6] MIDTERMS | DRUGS ACTING ON THE ANS Flashcards

1
Q

Major involuntary, unconscious, automatic portion of the nervous system

A

Autonomic Nervous System

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2
Q

Major divisions of the ANS (3)

A
  • Parasympathetic ANS
  • Sympathetic ANS
  • Enteric Nervous System
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3
Q

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

A

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

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4
Q

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: ____
A

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
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5
Q

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
A

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
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6
Q

HORMONES IN ANS

  • Sympathetic Division: ____
  • Parasympathetic Division: ____
A
  • Sympathetic Division: Norepinephrine
  • Parasympathetic Division: Acetylcholine
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7
Q

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)
A

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)
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8
Q

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.
A

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.
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9
Q

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 ____
A

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
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10
Q

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
A

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
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11
Q

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
A

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
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12
Q

ADRENERGIC PHARMACOLOGY

SYMPATHOMIMETICS - Alpha-1 Adrenergic Effects on Tissues

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

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
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13
Q

ADRENERGIC PHARMACOLOGY

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

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

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

  • Heart - stimulates rate and force
  • Juxtaglomerular cells of kidney - stimulates renin
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14
Q

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

A
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15
Q

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 ____
A

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
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16
Q

ADRENERGIC PHARMACOLOGY

SYMPATHOMIMETICS - Classifications (6)

A
  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
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17
Q

ADRENERGIC PHARMACOLOGY

Epinephrine

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

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
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18
Q

ADRENERGIC PHARMACOLOGY

Dopamine

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

Dopamine

  • Sympathomimetic (non-selective, direct-acting)
  • Activates α, β, and D1 adrenergic receptors
  • Uses: Cardiogenic shock, heart failure
  • Side effects: Cardiovascular disturbance, arrhythmias
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19
Q

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 ____
A

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
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20
Q

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
A

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
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21
Q

ADRENERGIC PHARMACOLOGY

Methyldopa (Preeclampsia)

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

Methyldopa (Preeclampsia)

  • Sympathomimetic (alpha 2-selective)
  • Activates α2 adrenergic receptors
  • Uses: Preeclampsia, gestational hypertension
  • Side effects: Sedation, hemolytic anemia
22
Q

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 ____
A

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
23
Q

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: ____
A

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
24
Q

ADRENERGIC PHARMACOLOGY

PHENOXYBENZAMINE

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

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)
25
Q

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
A

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
26
Q

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)
A

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)
27
Q

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)
A

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)
28
Q

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
A

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
29
Q

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
A

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
30
Q

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
A

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
31
Q

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
A

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
32
Q

CHOLINERGIC PHARMACOLOGY

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

A

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

33
Q

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)

A

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)

34
Q

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

A

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

35
Q

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)
A

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)
36
Q

CHOLINERGIC PHARMACOLOGY

DIRECT-ACTING CHOLINOMIMETICS: Pilocarpine

____ - autoimmune disorder characterized by triad of: (3)

A

DIRECT-ACTING CHOLINOMIMETICS: Pilocarpine

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

37
Q

CHOLINERGIC PHARMACOLOGY

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

A

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

38
Q

CHOLINERGIC PHARMACOLOGY

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

A

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

39
Q

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 ____

A

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

40
Q

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

A

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

41
Q

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

A

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

42
Q

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 ____

A

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

43
Q

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

A
44
Q

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

A

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

45
Q

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

A

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

46
Q

CHOLINERGIC PHARMACOLOGY

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

A

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

47
Q

CHOLINERGIC PHARMACOLOGY

INDIRECT-ACTING CHOLINOMIMETICS: Signs and Symptoms of Organophosphate Poisoning (DUMBBELSS)

  • ____
  • Urination
  • ____
  • Bronchospasm
  • ____
  • Excitation
  • ____
  • Sweating
  • ____
A

INDIRECT-ACTING CHOLINOMIMETICS: Signs and Symptoms of Organophosphate Poisoning (DUMBBELSS)

  • Diarrhea
  • Urination
  • Miosis
  • Bronchospasm
  • Bradycardia
  • Excitation
  • Lacrimation
  • Sweating
  • Salivation
48
Q

CHOLINERGIC PHARMACOLOGY

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

A

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

49
Q

CHOLINERGIC PHARMACOLOGY

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

A

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

50
Q

CHOLINERGIC PHARMACOLOGY

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

A

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

NR-NUR124 | Pharmacology (10 decks)

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