[6] MIDTERMS | DRUGS ACTING ON THE ANS Flashcards
Major involuntary, unconscious, automatic portion of the nervous system
Autonomic Nervous System
Major divisions of the ANS (3)
- Parasympathetic ANS
- Sympathetic ANS
- Enteric Nervous System
The Enteric Nervous Systerm consists of the myencentric plexus of ____ and submucous plexus of ____
The Enteric Nervous Systerm consists of the myencentric plexus of Auerbach and submucous plexus of Meissner
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: ____
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
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
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
HORMONES IN ANS
- Sympathetic Division: ____
- Parasympathetic Division: ____
- Sympathetic Division: Norepinephrine
- Parasympathetic Division: Acetylcholine
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)
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)
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.
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.
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 ____
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
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
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
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
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
ADRENERGIC PHARMACOLOGY
SYMPATHOMIMETICS - Alpha-1 Adrenergic Effects on Tissues
- Most vascular smooth muscle - ____
- Pupillary dilator muscle - ____
- Pilomotor smooth muscle - ____
- Liver - stimulate ____
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
ADRENERGIC PHARMACOLOGY
SYMPATHOMIMETICS - Beta-1 Adrenergic Effects on Tissues (Heart Function)
- Heart - stimulates ____ and ____
- Juxtaglomerular cells of kidney - stimulates ____
SYMPATHOMIMETICS - Beta-1 Adrenergic Effects on Tissues (Heart Function)
- Heart - stimulates rate and force
- Juxtaglomerular cells of kidney - stimulates renin
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
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 ____
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
ADRENERGIC PHARMACOLOGY
SYMPATHOMIMETICS - Classifications (6)
- Non-Selective Alpha Agonist
- Alpha 1-selective
- Alpha 2-selective
- Non-selective Beta Agonist
- Beta 1-selective
- Beta 2-selective
ADRENERGIC PHARMACOLOGY
Epinephrine
- ____ (non-selective, direct-acting)
- Activates ____ and ____
- Uses: Cardiac arrest, ____ (drug of choice), asthma, ____, hemostasis
- Side effects: ____, Tachycardia, ____, Hyperglycemia
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
ADRENERGIC PHARMACOLOGY
Dopamine
- ____ (non-selective, direct-acting)
- Activates ____, ____, and ____ adrenergic receptors
- Uses: ____, heart failure
- Side effects: Cardiovascular disturbance, ____
Dopamine
- Sympathomimetic (non-selective, direct-acting)
- Activates α, β, and D1 adrenergic receptors
- Uses: Cardiogenic shock, heart failure
- Side effects: Cardiovascular disturbance, arrhythmias
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 ____
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
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
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
ADRENERGIC PHARMACOLOGY
Methyldopa (Preeclampsia)
- Sympathomimetic ( ____ )
- Activates ____ adrenergic receptors
- Uses: Preeclampsia, ____
- Side effects: Sedation, ____
Methyldopa (Preeclampsia)
- Sympathomimetic (alpha 2-selective)
- Activates α2 adrenergic receptors
- Uses: Preeclampsia, gestational hypertension
- Side effects: Sedation, hemolytic anemia
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 ____
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
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: ____
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
ADRENERGIC PHARMACOLOGY
PHENOXYBENZAMINE
- ____ (alpha non-selective)
- Irreversibly blocks ____
- Uses: ____ (pre-surgical)
- Side effects: ____, ____, gastrointestinal irritation, ____
- Forms covalent bond with ____ (effects last for several days)
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)
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
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
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)
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)
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)
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)
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
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
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
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
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
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
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
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
CHOLINERGIC PHARMACOLOGY
CHOLINORECEPTORS
* ____ - nerve endings
* ____ - heart, some nerve endings
* ____ - effector cells, smooth muscle glands, endothelium
* ____ - ANS ganglia
* ____ - neuromuscular end plate
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
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)
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)
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
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
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)
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)
CHOLINERGIC PHARMACOLOGY
DIRECT-ACTING CHOLINOMIMETICS: Pilocarpine
____ - autoimmune disorder characterized by triad of: (3)
DIRECT-ACTING CHOLINOMIMETICS: Pilocarpine
Sjogren Syndrome - autoimmune disorder characterized by triad of:
* xerostomia (dry mouth)
* xerophthalmia (dry eyes)
* rheumatoid arthritis
CHOLINERGIC PHARMACOLOGY
INDIRECT-ACTING CHOLINOMIMETICS
* Bind to ____ and undergo prompt hydrolysis
* No significant actions at uninnervated sites where Ach is not normally
INDIRECT-ACTING CHOLINOMIMETICS
* Bind to cholinesterase and undergo prompt hydrolysis
* No significant actions at uninnervated sites where Ach is not normally
CHOLINERGIC PHARMACOLOGY
DIRECT-ACTING CHOLINOMIMETICS: Muscarinic Toxicity
* CNS stimulation
* Eye: ____
* Lungs: ____
* GIT/GUT: ____ gastrointestinal and genitourinary smooth muscle activity
* Increased ____
* Vasodilation
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
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 ____
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
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
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
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
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
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 ____
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
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
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
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
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
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
CHOLINERGIC PHARMACOLOGY
INDIRECT-ACTING CHOLINOMIMETICS: Organophosphate Poisoning
* ____ - insecticide
* ____ - nerve gases
INDIRECT-ACTING CHOLINOMIMETICS: Organophosphate Poisoning
* Malathion and Parathion - insecticide
* Sarin, Tabun, and Soman - nerve gases
CHOLINERGIC PHARMACOLOGY
INDIRECT-ACTING CHOLINOMIMETICS: Signs and Symptoms of Organophosphate Poisoning (DUMBBELSS)
- ____
- Urination
- ____
- Bronchospasm
- ____
- Excitation
- ____
- Sweating
- ____
INDIRECT-ACTING CHOLINOMIMETICS: Signs and Symptoms of Organophosphate Poisoning (DUMBBELSS)
- Diarrhea
- Urination
- Miosis
- Bronchospasm
- Bradycardia
- Excitation
- Lacrimation
- Sweating
- Salivation
CHOLINERGIC PHARMACOLOGY
INDIRECT-ACTING CHOLINOMIMETICS: Atropine Toxicity
* ____
* ____
* Decreased secretions
* Tachycardia
* ____
* Constipation
* Blurred vision
* ____
INDIRECT-ACTING CHOLINOMIMETICS: Atropine Toxicity
* Atropine fever (hyperthermia)
* Atropine flush (cutaneous vasodilation)
* Decreased secretions
* Tachycardia
* Arrhythmias (intraventricular conduction blocks)
* Constipation
* Blurred vision
* CNS toxicity
CHOLINERGIC PHARMACOLOGY
INDIRECT-ACTING CHOLINOMIMETICS: Atropine Toxicity Mnemonic
* Hot as a ____
* ____ as a bone
* Red as a ____
* ____ as a bat
* Mad as 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
CHOLINERGIC PHARMACOLOGY
INDIRECT-ACTING CHOLINOMIMETICS: C/I to Muscarinic Blockers
* Cautious use in infants - ____ due to decreased sweating
* ____ (causes increases intraocular pressure)
* Benign ____
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
