• Shuffle
    Toggle On
    Toggle Off
  • Alphabetize
    Toggle On
    Toggle Off
  • Front First
    Toggle On
    Toggle Off
  • Both Sides
    Toggle On
    Toggle Off
  • Read
    Toggle On
    Toggle Off
Reading...
Front

How to study your flashcards.

Right/Left arrow keys: Navigate between flashcards.right arrow keyleft arrow key

Up/Down arrow keys: Flip the card between the front and back.down keyup key

H key: Show hint (3rd side).h key

A key: Read text to speech.a key

image

Play button

image

Play button

image

Progress

1/64

Click to flip

64 Cards in this Set

  • Front
  • Back
What is the pathway that Acetylcholine takes from it's creation the neuronal axon back to start?
1. Synthesis 2. Storage in Vessicles 3. Release of Neurotransmitter 4. Binding to the Receptor 5. Degradation of acetylcholine 6. Recycling of choline
What are cholinergic type receptors?
Muscarinic (M1, M2, M3) and Nicotinic (Nn and Nm)
Where are muscarinic M1 receptors typically located?
CNS neurons, sympathetic postganglionic neurons, some presynaptic sites;
What is the result of ligand binding of muscarinic M1 receptors?
Formation of IP3 and DAG, increased intracellular calcium.
Where are typical locations of Nicotinic Nn receptors?
Postganglionic neurons, some presynaptic cholinergic terminals.
What is the result of ligand binding to Nn receptors?
Opening of Na+, K+ channels, depolarization
What are the typical locations of Nicotinic Nm receptors?
Skeletal muscle neuromuscular endplates.
What is the result of ligand binding to the Nm receptors?
Opening of Na+, K+ channels, depolarization.
What is the typical location of Alpha1 receptor?
Postsynaptic effector cells, especially smooth muscle.
What is the result of ligand binding to Alpha1 receptors?
Formation of IP3 and DAG, increased intracellular calcium.
What is the result of ligand binding to Alpha2 receptors?
Inhibition of adenylyl cyclase, decreased cAMP.
What is the result of ligand binding to Beta1 receptors?
Stimulation of adenylyl cyclase, increased cAMP.
What is the result of ligand binding to Beta2 receptors?
Stimulation of adenylyl cyclase, increased cAMP.
What is the result of ligand binding to Beta3 receptors?
Stimulation of adenylyl cyclase, increased cAMP.
What is the typical location of Alpha2 receptors?
Presynaptic adrenergic nerve terminals, platelets, lipocytes, smooth muscle
What is the typical location of Beta1 receptors?
Postsynaptic effector cells, especially heart, lipocytes, brain, presynaptic adrenergic and cholinergic nerve terminals.
What is the typical location of Beta2 receptors?
Postsynaptic effector cells, especially smooth muscle and cardiac muscle.
What is the typical location of Beta3 receptors?
Postsynaptic effector cells, especially lipocytes.
What is a cholinergic crisis?
The clinical condition of excessive activation of cholinoceptors; it may include muscle weakness as well as parasympathetic signs.
What is a direct-acting cholinomimetic?
A drug that binds and activates cholinoceptors; the effects mimic those of acetylcholine.
What is EDRF?
Endothelium-derived relaxing factor which is a potent vasodilator substance, largely nitric oxide that is released from vascular endothelial cells.
What is an indirect-acting cholinomimetic?
A drug that amplifies the effects of endogenous acetylcholine by inhibiting achetylcholinesterase.
Muscarinic agonist
A cholinomimetic drug with primarily muscarine-like actions.
What is a Myasthenic Crisis?
In patients with myasthenia, an acute worsening of symptoms; often caused by inadequate cholinomimetic treatment.
What is a nicotinic agonist?
A cholinomimetic drug with primarily nicotine-like actions.
What is organophosphate aging?
A process whereby the organophosphate, after binding to cholinesterase, is chemically modified and becomes more firmly bound to the enzyme.
What is a parasympathomimetic?
A drug whose effects resemble those of stimulating the parasympathetic nerves.
What is parasympathomimetic agonist?
Muscarinic agonists
What are the adverse affect of cholinolytic agents?
Xerostomia, cycloplegia, photophobia, CNS stimulation/depression, precipitates attack acute glaucoma, atropine flush, constipation, tachycardia, anhidrosis, heat stroke, urinary retention
Atropine
found in deadly (belladonna) nightshade and jimson weed 3-4 hours for miotic agent (cholinolytic )
Scopolamine
found in henbane, long acting choinolytic drug (cholinolytic)
Propantheline
slows gastric emptying (used for peptic ulcer disease (but H2 blockers more common) (cholinolytic)
Pirenzepine
slows gastric emptying and preferentially blocks M1 receptor(cholinolytic)
Hyoscyamine sulfate (Nulev)
irritable bowel syndrome
Cyclopentolate (12-16 hours), Tropicamide (hours), Homatropine (several days)
topical mydriatics
Ipratropium
bronchodilator used in asthma
Oxybutynin
incontinence and urgency (virtually no xerostomia)
Tolterodine
incontinence and urgency (virtually no xerostomia)
Cholinolytic agents have many therapetuic uses
Mydriasis and cylcoplegia, peptic ulcer treatment, herperactive or IBS, symptomatic relief acute rhinitis, antidote for cholinomemetic overdose, mushroom poisoning, hyperactive carotid sinus reflex, antiparkinsonism, motion sickness, preanesthetic
Ganglionic neurotransmission therapeutic uses (Ganglionic Blocking Drugs)
Hypertensive cardiovascular disease emergency (disecting aortic aneurysm, controlled hypotension in surgery (neuro/skin), autonomic hyperreflexia with massive sympathetic discharge (common in sp. cord injury), acute pulmonary edema to reduce pulmonary vascular resistance
What is predominant system in arterioles? how does ganglionic blockade effect them?
Sympathetic; vasodilation, increased peripheral flow
What is predominant system in veins? how does ganglionic blockade effect them?
Sympathetic; venous pooling of blood with decreased cardiac output
What is predominant system in heart? how does ganglionic blockade effect them?
Parasympathetic; tachycardia
What is predominant system in iris? how does ganglionic blockade effect them?
Parasympathetic; mydriasis
What is predominant system in the ciliary muscle? how does ganglionic blockade effect them?
Parasympathetic; cycloplegia
What is predominant system in the GI tract? how does ganglionic blockade effect them?
Parasympathetic; decreased tone and motility, constipation
What is predominant system in the bladder? how does ganglionic blockade effect them?
Parasympathetic; urinary retention
What is predominant system in the salivary glands? how does ganglionic blockade effect them?
Parasympathetic; xerostomia
What is predominant system in the sweat glands? how does ganglionic blockade effect them?
Sympathetic; anhidrosis
What is a nicotinic receptor agonist and what are its affect?
Nicotine - increase HR, CNS stimulant; pesiticide can cause nicotine poisoning
What are three nicotinic-ganglinic receptor antagonists?
Hexamethonium-classical, Mecamylamine - can enter CNS, Trimethaphan - cannot enter CNS (these drugs are very dirty)
What are the adverse affects of ganglionic blockers?
Visual disturbances, xerostomia, urinary retention, impotence, CNS stimulation followed by depression, marked hypotension (including postural hypotension), constipation
What are the therapetic uses of neuromuscular blockers?
Muscle relaxation during anesthesia and surgery, prevent trauma from electroconvulsive shock therapy, reduce muscle spasms (diaphragm last!)
d-Tubocurarine
Prototype of non-depolarizing blocker; competitve Nm-R blocker, poor oral absorption; fast onset, longer acting, excreted liver and kidney, ganglionic blockade - decreases BP and venous return, vasodilation, release of histamine - vasodilation and bronchoconstriction
Vecuronium (Norcuron)
competitive Nm-R blocker, short acting, minimal ganglionic blockade, no histamine release, no change in heart rate or blood pressure
Mivacurium
competitive NmR blocker, ultrashort onset and duration of action, hydrolyzed by plasma cholinesterases, no effect on ganglionic transmission or cardiac M2 receptors, can cause histamine release (good alternative)
Succinylcholine
depolarizing antagonist, fast onset, short acting, release of histamine, no ganglionic blockade-depends on dose, hydrolyzed by pseudocholinesterase, release of K+, can result in arrhythmias, C-V reactions depends on ganglionic stimulation, can see decreased HR, BP (vagal) or increased BP (sympathetic)
What are the adverse effects of neuromuscular blockers?
Apnea, bronchoplasm, hypotension; 1. histamine relaxes arterioles, ganglionic blockade, pooling blood in muscles with paralysis
What is an antidote for nondepolarizing neuromuscular blockers?
Neostigmine or other ACHE inhibitor and supportive respiration it competes for binding with depolarizing antagonist
What are the adverse effects of succinylcholine?
Bradycardia, muscle pain after use, hyperkalemia, increased intraocular pressure important in patient with known glaucoma
What can gaseous anestetics and succinylcholine (adversely) cause?
General NM rigidity, elevated temperature, increases creatine phosphokinase and produce a syndrome-malignant hyperthermia
Dantrolene
blocks release of Ca2+, given PO, IV metabolized microsomes
What is Dantrolene used for?
a muscle relaxant used to treat spasticity due to stroke, spinal injury, multiple sclerosis, cerebral palsy, to treat malignant hyperthermia
What are the side effects of Dantrolene?
Dose-dependent muscle weakness, dizziness, drowsiness, fatigue, diarrhea, liver dysfunction increase aspartate aminotransferase; Counter Indications-Liver Disease, respiratory muscle weakness