Reading...
Play button
Play button
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;
26 Cards in this Set
- Front
- Back
|
Nicotine
|
-CNS selective nicotinic agonist
-lipid soluble tobacco alkaloid -Stimulates ganglionic nicotinic receptor -Stimulation followed by depression -Clinical Use: cigarette smoking withdrawl, transdermal or oral -No application in dentistry |
|
|
Hexamethonium
|
-Nicotinic Ganglionic Blocker, Antagonist
-charged molecule, does not enter CNS -Once used as antihypertensive, but too many side effects -No application in dentistry |
|
|
Mecamylamine
|
-Nicotinic Ganglionic Blocker, Antagonist
-uncharged molecule, enters CNS -Once used as antihypertensive, but too many side effects -No application in dentistry |
|
|
Trimethapham
|
-Nicotinic Ganglionic Blocker, Antagonist
-Once used as antihypertensive, but too many side effects -Fast acting, short acting, not orally active, sometimes used in neurosurgery |
|
|
Tubocurarine
|
-Nicotinic Antagonist
-Neuromuscular Blocker -Dental Use: Muscle paralysis in oral surgery for mandibular repair |
|
|
Succinylcholine
|
-Nicotinic Antagonist: Neuromuscular Blocker
-Dental Use: To facilitate intubation, and to treat intractable laryngospasm |
|
|
Acetylcholine
|
-Muscarinic Agonist: Choline Ester
-Rapidly metabolized by acetylcholinesterase -Clinical Use: Eye surgery |
|
|
Methacholine (Provocholine)
|
-Muscarinic Agonist: Choline Ester
-Metabolized slowly -Clinical Use: test bronchial reactivity |
|
|
Bethanechol (Urecholine)
|
-Muscarinic Agonist: Choline Ester
-Not metabolized -Clinical Use: increase urinary voiding |
|
|
Muscarine
|
-Muscarinic Agonist: Alkaloid
-specificity for parasympathetic target organs -No clinical use |
|
|
Pilocarpine
|
-Muscarinic Agonist: Alkaloid
-specificity for parasympathetic target organs -Clinical Use: treatment of xerostomia, stimulate salivary glands, treat glaucoma (along with anticholinesterase) |
|
|
Atropine
|
-Muscarinic Antagonist
-Blocks slowing of the heart and CNS effects of nerve gas -Dentistry: produce xerostomia, an adjunct to general anesthesia, prevents reflex slowing of the heart |
|
|
Scopolamine
|
-Muscarinic Antagonist
-Motion Sickness -Dentistry: produce xerostomia, an adjunct to general anesthesia, prevents reflex slowing of the heart |
|
|
Ipratropium (Atrovent)
|
-Muscarinic Antagonist
-Topically active in lungs for asthma -Bronchodilator given as an inhaled aerosol, charged molecule stays in lung, limiting systemic effects |
|
|
Physostigmine
|
-Cholinesterase Inhibitor
-uncharged molecule, enters CNS -Dentistry: reverse neuromuscular blockade following surgery |
|
|
Neostigmine
|
-Cholinesterase Inhibitor
-charged molecule, does not enter CNS |
|
|
Cholinesterase Inhibitors
|
-Prolong the presence of acetylcholine in the synapse
-Used for: Myastenia gravis, glaucoma, reversal of neuromuscular blockade during/post surgery Alzheimer's Disease -Physostigmine and Neostigmine |
|
|
AntiMuscarinic Signs
|
-Hot as a hare, red as a beat, dry as a bone, mad as a wet hen
-mydriasis (dilation), blurred vision due to cycloplegia (loss of accomodation), inhibition of sweating, xerostomia, dry eyes, urinary retention, CNS effects, hallucination in high doses |
|
|
Atropine and Scopolamine
|
-Prototype AntiMuscarinics
-Belladonna: used to produce pupillary dilation (mydriasis) |
|
|
Clinical Use of AntiMuscarinics
|
-Eye Exam: to induce mydriasis (pupillary dilation)
-Asthma: blocks cholinergic component of bronchoconstriction -Myocardial Infarction: blocks vagal response to pain and permits increased HR -Oral Surgery: inhibit salivation -Insecticide Poisoning: used in people exposed to insecticides and nerve gases to prevent over-activation of muscarinic receptors in heart and brain |
|
|
Muscarinic Receptors
|
-SLUD: salivation, lacrimation, urination, defacation
-miosis (constricted pupils), decreased HR, decreased AV conduction, vasodilation, bronchoconstriction, increased GI motility and secretions |
|
|
Ganglionic Blockers
|
Hexamethonium, Mecamylamine, Trimethapham
|
|
|
Effect pf Ganglionic Blockers
|
-Arterioles: Symp - hypotension
-Veins: Symp - decreased CO -Heart: Para - tachycardia -Iris: Para - mydriasis -Ciliary Muscle: Para - cyclopeglia -GI: Para - constipation -Bladder: Para - urinary retention -Salivary Glands: Para - Xerostomia -Sweat Glands: Symp/Cholinergic - hyperthermia |
|
|
Cholinergic Transmission
|
1. Choline taken up by cell
2. Acetyl-CoA product of cell metabolism 3. Choline-acetyl transferase synthesizes ACh 4. ACh pumped into vesicles and stored 5. Nerve impulses reach terminal, causing increase in intracellular Calcium. Calcium stimulates fusion of vesicles with the membrane and the release of ACh into the synapse 6. ACH binds to receptors on postsynaptic cell and also presynaptic. 7. Ach is broken down by esterases (ACh-esterase, serum-esterase). |
|
|
Muscarinic Receptors
|
Agonists: Acetylcholine, Methacholine, Bethanechol, Muscarine, Pilocarpine
Antagonists: Atropine, Scopolamine, Ipratropium -IP3, Ca2+, cAMP, cGMP -gene regulation, kinases, phosphatases, proteases |
|
|
Muscarinic Cholinergic Actions
|
SLUD
miosis (constricted pupils) Dec. HR, Dec. AV conduction Inc. GI motility and secretions |
