Term
| Where do ganglionic blockers act? |
|
Definition
| At the nicotinic receptor in the ganglion |
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Term
| Where to NMJ blockers act? |
|
Definition
At the nicotinic receptor in the NMJ
Affect Muscle Contraction |
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Term
| Where do antimuscarinic drugs act? |
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Definition
At the post-ganglionic muscarinic receptor (in the effector organ)
Parasympathetic Nervous System |
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Term
| Describe how the muscarinic antagonists work. |
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Definition
| They sit in the muscarinic receptor and do nothing (block acetylcholine from binding). |
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Term
| Name two muscarinic antagonists |
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Definition
|
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Term
| Cholinergic Antagonist on Heart |
|
Definition
Increase Rate & Conduction Velocity
LIttle effect on contractility |
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Term
| Cholinergic Antagonist on Eye |
|
Definition
Mydriasis (dilation)
Inability to focus (cycloplegia) |
|
|
Term
| Cholinergic Antagonist on GI |
|
Definition
|
|
Term
| Cholinergic Antagonist on Respiration |
|
Definition
Bronchodilation
Decreased Secretions |
|
|
Term
| Cholinergic Effects on GU |
|
Definition
|
|
Term
| What is the prototypic anti-muscarinic? |
|
Definition
| Atropine, highly selective for muscarinic receptors |
|
|
Term
| What 3 drugs can be used preoperatively to reduce secretions? |
|
Definition
Atropine
Scopolamine
Glycopyrollate |
|
|
Term
| What anti-muscarinic can prevent motion sickness by acting primarily on the CNS? |
|
Definition
|
|
Term
| What anti-muscarinic is used to produce bronchial dilation in COPD? |
|
Definition
|
|
Term
| Describe how atropine effects are dose dependent. |
|
Definition
Low - slight cardiac slowing, some dry mouth, sweat inhibition
Middle - rapid heart rate, palpitation, VERY dry mouth, pupil dilation, blurred near vision
High - hallucinations, delirium, coma |
|
|
Term
| Why do low doses of atropine cause slight cardiac slowing? |
|
Definition
| Early low doses are mediated by the vagus - which slows the heart |
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Term
| What drug regenerates cholinesterase and do not enter CNS? |
|
Definition
|
|
Term
| What drug blocks Ach action and enters the CNS? |
|
Definition
|
|
Term
| What 2 drugs are given together as antidotes for nerve gas? |
|
Definition
|
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Term
| Compare mechanism of cholinergic antagonists and adrenergic antagonists on airways. |
|
Definition
Chol Antag - blocks constriction (blocks M receptors)
Adren Ag - bronchodilates (activates B2) |
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|
Term
| Compare receptors for Chol. Antag. and Adren. Ago. as bronchodilators |
|
Definition
Chol. Ant - No change
Adren Ag - Reduce number in old people |
|
|
Term
| Compare Receptor locations for chol. antag. and adren. ag. (bronchodilators). |
|
Definition
Chol. Antag. = Large central airways
Adren. Ag. = Small peripheral airways |
|
|
Term
| Cholinergic Antagonist for Airways |
|
Definition
|
|
Term
| Adrenergic Agonist for Airways |
|
Definition
|
|
Term
| Trace the pathway to bronchial smooth muscle cells relaxation. |
|
Definition
| ATP --(adenylyl cyclase)--> cAMP --> Bronchial Smooth muscle relaxation |
|
|
Term
| What enzymes to musacrinic antagonists and adrenergic agonists act on to relax bronchial smooth muscles. |
|
Definition
| Increase action of adenylyl cyclase. |
|
|
Term
|
Definition
Inhibit Phosphodiesterase (PDE)
Stops cAMP --> AMP
Causes bronchial smooth muscle dilation |
|
|
Term
|
Definition
Adrenergic Agonist
B2 Receptor
Bronchodilator
Tx: Asthma & COPD
Side Effects: Allergic, Chest Pain, Arrythmias |
|
|
Term
|
Definition
Cholinergic Antagonist
M receptor
Bronchodilator
Tx: asthma, COPD
Side Effects: Dry mouth, sedation |
|
|
Term
|
Definition
Type: Methyl xanthine
Receptor: adenosine
Bronchodilator
Tx: asthma, COPD
Side Effects: CNS, Increased HR, Increased force of contraction, Increased Gastric Acid |
|
|
Term
|
Definition
Albuterol
Theophylline
Ipratropium |
|
|
Term
| How do you treat an atropine overdose? |
|
Definition
1. Treat symptomatically
2. Provide cholinesterase inhibitor (physostigmine) in small doses
3. Blankets and diazepam for seizure control |
|
|
Term
| Mechanism of Ganglionic Blockers |
|
Definition
| Interfering with the post-synaptic action of Ach at the nicotinic receptors of all autonomic ganglia (different from NMJ nicotinic receptors) |
|
|
Term
| Use of ganglionic blockers |
|
Definition
Treat hypertension (emergencies)
**Limited Clinical Use |
|
|
Term
| Side Effects of Ganglionic Blockers |
|
Definition
NM blockade
Hypotension
Impotence |
|
|
Term
| Name 2 ganglionic blockers |
|
Definition
|
|
Term
|
Definition
Treat spastic disorders of the GI and lower urinary tract
Treat organophosphate poisoning
Suppress respiratory secretions prior to surgery |
|
|
Term
| Name 4 Muscarinic Blockers |
|
Definition
**I <3 Cats
Ipratropium
Cyclopentolate
Atropine
Tropicamide
Scopolamine |
|
|
Term
| What 3 drugs can be used in opthalmology to produce mydriasis and cycloplegia prior to refraction? |
|
Definition
Cyclopentolate
Atropine
Tropicamide |
|
|
Term
| Name 2 Ganglionic Blockers |
|
Definition
|
|
Term
| Does nicotine have any therapeutic uses? |
|
Definition
|
|
Term
|
Definition
| Treat moderate to severe hypertension |
|
|
Term
|
Definition
Drug that binds competitively to the nicotinic receptor at the NMJ
- Depolarizing or non-depolarizing depending on the mechanism of action |
|
|
Term
| Depolarizing NMJ Blocker Action |
|
Definition
Binds to the Nm receptor
Opens the Channel
Depolarizes the end-plate and then gets stuck |
|
|
Term
| Use of a depolarizing NMJ antagonist |
|
Definition
| Produce skeletal relaxation |
|
|
Term
| Name a depolarizing NMJ blocker |
|
Definition
|
|
Term
|
Definition
Reversible depolarizing NMJ blocker
Use: relax muscles during surgery
Half Life: <1 minute, just support and wait |
|
|
Term
| Describe the 2 phases of depolarizing NMJ blocker action |
|
Definition
1. Membrane depolarizes = initial discharge that produces transient fasciculations followed by flaccid paralysis
2. Membrane repolarizes, receptor is desensitized to affect of acetylcholine |
|
|
Term
| What is the only clinically useful depolarizing NMJ blocker? |
|
Definition
|
|
Term
| Action of Non-Depolarizing NMJ Antagonists |
|
Definition
Competitive Antagonist
Binds to the NMJ receptor
Does not open the channel |
|
|
Term
| Use of non-depolarizing NMJ antagonist |
|
Definition
| To produce skeletal muscle relaxation |
|
|
Term
| Name 4 Non-Depolarizing NMJ Blockers |
|
Definition
D-tubocurarine
Pancuronium
Atracurium
Gallamine |
|
|
Term
| Describe the toxicity of Non-depolarizing NMJ blockers |
|
Definition
Respiratory Paralysis
Patient will asphyxiate if mechanical ventilation is not provided |
|
|
Term
| How would you bring a patient off of one of the nondepolarizing blockers? |
|
Definition
| Give cholinesterase inhibitor + muscarinic antagonist |
|
|
Term
|
Definition
Cholinergic Agonist
Acetylcholine Receptor
No Use
Half Life: 1-2 SECONDS |
|
|
Term
Order these Drugs by half-life
d-tubocurarine
gallamine
succinylcholine
acetylcholine |
|
Definition
Acetylcholine = 1-2s
Succinylcholine = <1min
D-Tubocurarine = 1-2 hour
Gallamine = 2 hour |
|
|
Term
|
Definition
Inherited - Autosomal Dominant
Rapid Increase in Body Temperature
Rapid Rise In Serum Potassium
Response to Inhaled anesthetics/muscle relaxants - halothane or succinylcholine
Calcium released from muscle cell SR
Myosin ATPase activated - heat generated
Muscular Contraction generated - adds heat |
|
|
Term
| What is the treatment for malignant hyperthermia? |
|
Definition
Dantrolene
Blocks release of calcium from SR
Reduces muscle tone and heat production
(also cool with ice packs) |
|
|
Term
| What is the mechanism of botulium toxin (botox)? |
|
Definition
| Prevents the release of acetylcholine |
|
|
Term
| What are the uses of botox? |
|
Definition
Focal dystonia (local movement disorders)
Strabismus (eyes not aligned)
Cervical dystonia (head tilt)
Cosmetic - smooth facial lines by paralyzing/weakening facial muscles |
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