Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
31 Cards in this Set
- Front
- Back
Alpha-Latrotoxin (Black Widow Spider)
|
Facilitate Spontaneous ACh Release to Excess
|
|
Botulinum Toxin aka Botox (Clostridium botulinum)
|
Mx: Block ACh Release
Causes Flaccid Paralysis Uses: 1) Wrinkle Reduction 2) Eye Squinting 3) Certain types of Headaches 4) Jaw Clenching 5) Movement Disorders 6) Bladder Spasms 7) Excessive Sweating |
|
Hexamethonium
|
Preferentially Blocks GANGLIONIC (NN or NG) AChR in Autonomic Ganglia and Adrenal Medulla
|
|
d-Tubocurarine aka Tubarine aka Tubadil
|
Competitive (Non-Depolarizing)
Preferentially Blocks NEUROMUSCULAR (NM) AChR at Neuromuscular Synapses of Somatic System NOT Completely Selective, and can produce some degree of Ganglionic Blockade, possibly contributing to Hypotensive Effects Active Ingredient of Curare, Plant from SA NOT Absorbed Orally due to 2 Quaternary Nitrogen Functions Duration = 20-40 Minutes Releases Histamine: 1) Reduces BP 2) Increases Respiratory Secretions 3) Produces some Bronchospasm 4) Increases Salivary Secretion Sequence of Paralysis: Small Rapid Muscles (eyes, ears, mouth, fingers, toes) > Limbs, Neck > Intercostal Muscles > Diaphrahm (last) |
|
Cevimeline
|
Mx: Selective M1 Muscarinic AChR AGONIST
Uses: 1) Treat Dry Mouth in SJOGREN'S SYNDROME 2) Possibly useful in Alzheimer's to reduce symptoms and plaque lesions |
|
Side Effects of Muscarinic Cholinergic AGONISTS
|
Most Serious:
1) Hypotension 2) Bradycardia 3) Bronchial Constriction 4) Exacerbation of Peptic Ulcers Most Common: ***"SLUDS" Syndrome*** S = Salivation L = Lacrimation U = Urination D = Defection S = Sweating Antidote = ATROPINE! |
|
Methacholine (Mecholyl)
|
Selective Muscarinic AChR AGONIST (due to β-methyl group)
Resistant to hydrolysis via PLASMA Cholinesterases Hydrolyzed by Acetylcholinesterases at 1/3 rate of ACh Uses: 1) Diagnostically to test responses of Bronchial Hyper-reactivty for Asthma |
|
Carbachol (Doryl or Carcholin)
|
LITTLE Selectivity for AChR Types
Carbamate Substitution in Acetyl Moiety protects it from Hydrolysis from BOTH Plasma Cholinesterases AND Acetylcholinesterases = Long Duration (2-3 Hours) Uses: 1) Topically in Eye for GLAUCOMA |
|
Bethanechol (Urecholine)
|
Combines Structural Features of METHACHOLINE (β-methyl group) and CARBACHOL (carbamate substition)
Selective for Muscarinic AChR Long Duration (2-3 Hours) Uses: 1) Orally or SC - Increases Tone and Contractions of the Intestine and Urinary Bladder 2) IV or IM - Negates Specificty and Increases Toxicity - DO NOT ADMINISTER THIS WAY |
|
Pilocarpine
|
Natural Plant Alkaloid
Primarily Muscarinic AChR AGONIST NOT a Choline Ester NOT a Substrate for AChE Long Duration (2-3 Hours) Uses: 1) Topically in Eye for GLAUCOMA 2) Very Potent actions on Sweat Glands 3) Prominent and Complicated actions on CV 4) Effects in CNS Thus, NOT used Systemically! |
|
Nicotine
|
Natural Plant Alkaloid
Central Effects: 1) Mild CNS Stimulant 2) Stimulates Respiration 3) Induces Vomiting Peripheral Effects: 1) Stimulate Ganglionic NAChR --> Release of NE, leading to: 2) Tachycardia 3) Increase in BP 4) Increased GI Secretions and Motility Very high doses can block NAChR by inducing persistent Depol. Thus, effects of Nicotinic Ganglionic Agonists are UNPREDICTABLE = NOT useful for Therapeutics (exception = Varenicline) |
|
Varenicline
|
Some Selectivity for NN α4β2
Uses: 1) Smoking Cessation/Withdrawl |
|
Physostigmine aka "Eserine"
|
Reversible (Carbamate) AChE Inhibitor
3 Amine --> Crosses BBB Natural Plant Alkaloid from Calabar or "Ordeal" Beans from West Africa Uses: 1) Antidote against Atropine Poisoning 2) Topically in Eye for Glaucoma 3) Possibly improve symptoms of Alzheimer's (Donepezil is a new, more selective alternative) |
|
Neostigmine (Prostigmin)
|
Reversible (Carbamate) AChE Inhibitor
4 Amine --> Does NOT Cross BBB Stimulates GI Contractions and Secretions Stimulates Urinary Contractions Improves Neurotansmission at Jx of Somatic Nerves and Skeletal Muscle Uses: 1) Nonobstructive Intestinal and Urinary Bladder Atony 2) Management of MYASTHENIA GRAVIS |
|
Edrophonium (Tensilon)
|
Reversible (Carbamate) AChE Inhibitor
4 Amine --> Does NOT Cross BBB Short Duration Uses: 1) Very Useful for Functional Tests, e.g. Dx of MYASTHENIA GRAVIS |
|
Echothiophate (Phospholine)
|
Irreversible (Organophosphate) AChE Inhibitor
Long Duration (100 Hours) Does NOT readily penetrate the Skin and is Stable in Solution (Unique to Organophosphates) Uses: 1) Topically in the Eye for Glaucoma |
|
Sarin
|
Irreversible (Organophosphate) AChE Inhibitor
Prototype Military "Nerve Gas" (others include Tabun and Soman) Crosses the BBB and induces both Central and Peripheral AChE Inhibition. NOT used as a drug. |
|
Malathion
|
Irreversible (Organophosphate) AChE Inhibitor
Prototype Organophosphate INSECTICIDE Because mammals detoxify it readily, large amounts are required to suffer intoxication. |
|
Pralidomide aka Protopam (PAM)
|
AChE REACTIVATOR
4 Amine --> Does NOT Cross BBB Treatment for Organophosphate Intoxication must be initiated quickly after exposure. If the P-Enzyme has fully "Aged", it is USELESS. |
|
Pirenzepine
|
M1 Selective Muscarinic AChR ANTAGONIST
Uses: 1) Inhibitor of Acid Secretion without the normal side effects (PEPTIC ULCER DISEASE) |
|
Tolterodine
|
M3 Selective Muscarinic AChR ANTAGONIST
Uses: 1) Adults with Urinary Incontinence 2) Bladder Antispasmodic Agent to Inhibit Contractions After Bladder Surgery |
|
Atropine
|
Non-Selective Muscarinic AChR ANTAGONIST
Natural Plant Alkaloid from Belladonna Plants and Jimson Weed 3 Amine - Can Cross BBB Half Life = 2-4 Hours Sx: 1) Eye - Produces Mydriasis (Pupil Dilation) and Cycloplegia (Loss of Accommodation) 2) GI Tract - Reduces Secretions and Motility 3) Decreases Thermoregulatory (Sudomotor) Sweating 4) Mild Tachycardia 5) Bronchial Relaxation 6) ***One Effect NOT related to Muscarinic Blockade***: Dilation of Blood Vessels in Facial Blush Area = ATROPINE FLUSH (Due to DIRECT, NON-Muscarinic Effect on Vascular Smooth Muscle) Uses: 1) Preanesthetic Medications to reduce salivary/respiratory secretions and to induce amnesia (Scopolamine also can be used). 2) Examination of the Retina and Treatment of Acute Iritis - Topically in Eye to induce Mydriasis and Cycloplegia 3) Treatment of Organophosphate AChE Inhibitor Poisoning In Children, low dose can Block Sweating --> Increased Temp = "Atropine Fever" Antidote for Atropine Poisoning = Physostigmine (penetrates CNS) |
|
Scopolamine
|
Natural Belladonna Alkaloid, Similar to Atropine in many ways
3 Amine --> Can Cross BBB Differences from Atropine: 1) Exerts MORE CNS Action, especially Drowsiness (Dreamless Sleep - Loss of REM) and Amnesia 2) Antimotion Sickness Agent - Blocks Muscarinic AChRs in Vestibular System and in Brain |
|
Propantheline
|
Synthetic Muscarinic AChR ANTAGONIST
4 Amine --> Does NOT Cross BBB Uses: 1) Peptic Ulcer Disease (Pirenzepine is better as it is more specific (M1) and thus less side effects) |
|
Ipratropium (Atrovent)
|
Synthetic Muscarinic AChR ANTAGONIST
4 Amine --> Does NOT Cross BBB Uses: 1) Reversible Airway Disease (Tiotropium is a very similar alternative which gives a LONGER bronchodilation) 2) Marginal Benefits to treatment of Common Colds (reduce secretions of Nasopharynx) |
|
What class of drugs is beneficial in the management of Parkinson's Disease?
|
Muscarinic Recetor ANTAGONISTS!
May be given concomitantly with Levodopa. |
|
Trimethaphan (Arfonad)
|
The ONLY Clinically Relevant Ganglionic Blocking Drug
Uses: 1) Lower BP Rapidly in Hypertensive Crisis Side Effects: 1) Constipation (Blockade of Enteric Ganglia) 2) Urinary Bladder Atony 3) Cycloplegia 4) Decreased Sweating 5) Tachycardia (Baroreceptors) |
|
Atracurium (Tracrium)
|
Competitive (Non-Depolarizing) Motor End-Plate Blockade
Presently Popular |
|
Succinylcholine (Anectine)
|
Depolarizing Motor End-Plate Blockade
Nicotinic Agonists which produce a Transient Contraction, followed by PERSISTENT Depol and PREVENTED Repol Intensified with AChEI and by Hypothermia Ester of TWO Choline Residues w/ Succinic Acid Short Duration (2-3 Minutes) - usually given by IV Drip Uses: 1) Adjunct in Surgical Anesthesia - Muscle relaxation while using lower levels of general anesthetic 2) Orthopedic Procedures 3) Intubation (useful due to short duration) 4) Electroshock Therapy Contraindications: 1) Can Exacerbate Hyperkalemia in patients with Extensive Soft-tissue damage (burn victims) 2) In individuals with Genetic Mutations in Ryanodine Receptor, combination with Halothane leads to widespread muscular rigidity + rapid rise in temp = Malignant Hyperthermia. Treated with Dantrolene (blocks Ca2+ Release) 3) In individuals with Genetic Deficiency causing Reduced Plasma AChE, can cause Prolonged Apnea |
|
Ether and Halothane (volatile anesthetics) interactions with Neuromuscular Blockers
|
Stabilize a Hyperpolarization of Post-Synaptic Membrane
INCREASE Blockade by COMPETITIVE Blockers (tubocurarine) |
|
Aminoglycosides, Tetracycline, and Certain Peptide Antibiotics (certain antibiotics) interactions with Neuromuscular Blockers
|
Have Curare-Like Activity
Enhance Blockade by adding their OWN Component! |