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;
56 Cards in this Set
- Front
- Back
what are the the 2 direct acting cholinomimetic: muscarinic receptor agonists that we have to know?
|
1. bethanichol
2. pilocarpine |
|
cholinergic agonist used primarily to stimulate smooth muscle cells in the GI tract or urinary bladder?
|
bethanichol
|
|
Highly resistant to hydrolysis by endogenous acetylcholinesterase = long duration of action
|
bethanichol
|
|
what are the preperations of bethanichol that are availible?
|
1. oral
2. parentarel |
|
used for GI or urinary bladder paralysis (postoperative, neurogenic bladder)
|
bethanichol
|
|
What am I? Overdose causes signs associated with muscarinic excess: nausea, vomiting, diarrhea, salivation. These effects are blocked competitively by atropine, a muscarinic antagonist.
|
bethanechol
|
|
what is the cholinergic agonist used primarily to stimulate M3 receptors on smooth muscle cells in the iris causing miosis and on ciliary muscle increasing outflow of aqueous humor?
|
pilocarpine
|
|
what are the preparations availible for pilocarpine?
|
opthalmic (topical)
|
|
Used for treatment of glaucoma. Stimulates smooth muscle cells on the ciliary body, facilitating outflow of aqueous humor through trabecular meshwork (wide-angle glaucoma) and contracts sphincter muscle of iris leading to opening of Canal of Schlemm (treats narrow angle glaucoma).
|
pilocarpine
|
|
Side effects: Blurred distant vision (Pilocarpine stimulates smooth muscle cells on the ciliary body of the eye causing the lens to thicken, which interferes with distant vision).
|
pilocarpine
|
|
what are the 2 main nicotinic agonists?
|
1. nicotine
2. succinylcholine |
|
Higher affinity for ganglionic nicotinic receptors
Directly stimulates nicotine receptors |
nicotine
|
|
Sympathomimetic and parasympathomimetic actions
Effects: hypertension, tachycardia, nausea, vomiting, diarrhea |
nicotine
|
|
The only depolarizing neuromuscular blocking drug used clinically in the U.S. to induce paralysis during surgery
|
succinylcholine
|
|
It produces a longer effect at the myoneural junction (NMJ) than does acetylcholine
It stimulates the nicotinic receptor, opening the channel and depolarizing the motor end-plate |
succinylcholine
|
|
This results in a brief period of excitation that manifests itself by widespread fasciculations in muscle cells
Because _____ is not metabolized effectively at the synapse, the depolarized membranes remain depolarized and unresponsive to subsequent impulses, resulting in a flaccid paralysis |
Succinylcholine
|
|
what are the 3 main indirect cholinomimetic agonists: reversible acetylcholinesterase inhibitors?
|
1. Neostigmine
2. Physostigmine 3. Edrophonium |
|
a quaternary compound that does not cross the blood-brain-barrier (B.B.B.), but peripherally blocks cholinesterase. It also activates nAChRs at the neuromuscular junction for 3-7 hours
|
Neostigmine
|
|
Indirect cholinomimetic: stimulates acetylcholine receptors by increasing the concentration of endogenous Ach at the synapse.(Hydrolysis is the major mechanism of terminating Ach actions.)
|
Neostigmine
|
|
Preparations available: oral, parenteral
Uses: treatment of myasthenia gravis |
Neostigmine
|
|
a tertiary compound similar to neostigmine but crosses B.B.B. Used to treat CNS toxicity from atropine overdose.
|
Physostigmine
|
|
a short-acting (2-10 minutes) cholinesterase inhibitor
|
Edrophonium
|
|
what is the 1 main Indirect acting cholinomimetic agonists: Irreversible Acetylcholinesterase Inhibitor?
|
pralidoxime
|
|
Organophosphates are used as insecticides or nerve gases in chemical warfare. When poisoned, if patient is rapidly treated with ____ , inhibited enzymes can be reactivated
|
pralidoxime
|
|
what are the 4 Cholinergic Antagonists we have to know?
|
1. Atropine
2. Scopolamine 3. Pirenzepine 4. Ipratropium |
|
blocks muscarinic receptors preventing their activation by agonists like acetylcholine?
|
atropine
|
|
Does not differentiate between muscarinic receptor subtypes 3) Most sensitive tissues: salivary, bronchi, and sweat glands 4) Effects are opposite to those mediated by muscarinic agonists: e.g. increased heart rate, bronchodilation, decreased GI motility
|
atropine
|
|
Uses: Cardiovascular disorders (diseases with cardiac slowing), Respiratory disorders (asthma, preoperative treatment to prevent increased airway secretion induced by anesthetics), Urinary and GI disorders (spastic bowel disorder, inflammatory bowel disorders)
|
atropine
|
|
Side effects: symptoms related to inhibition of parasympathetic activity. (dry mouth, dilated pupils, tachycardia, flushed skin, agitation, delirium)
|
atropine
|
|
produces more CNS effects than atropine and is used to prevent motion sickness?
|
Scopolamine
|
|
is a selective M1 and M4 receptor antagonist used to treat peptic ulcers?
|
Pirenzepine
|
|
is a quaternary ammonium compound used in the treatment of chronic but is less effective in treating asthma?
|
Ipratropium
|
|
Nm or Nn receptor antagonist? Produces nondepolarizing (competitive) neuromuscular blockade during surgical procedures (e.g., d-tubocurarine)
|
Nm receptor antagonist
|
|
Nm or Nn receptor antagonist? Acts by preventing endogenous Ach from binding to nicotinic receptors and causing muscle cell depolarization without excitatory fasciculations
|
Nm receptor antagonist
|
|
Nm or Nn receptor antagonist?
Results in flaccid paralysis similar to myasthenia gravis |
Nm receptor antagonist
|
|
Nm or Nn receptor antagonist?
Long-lasting agents = d-tubocurarine and pancuronium Intermediate-lasting agents = vecuronium and rocuronium Rapidly degraded compounds = mivacurium |
Nm receptor antagonist
|
|
Nm or Nn receptor antagonist?
May cause variable side effects (i.e., hypertension) due to ganglionic blockade or cause apnea due to paralysis of respiratory muscles These toxic side effects can be reversed by administration of AChE inhibitors (e.g. neostigmine) |
Nm receptor antagonist
|
|
Nm or Nn receptor antagonist?
Most commonly used agents = triimethophan or mecamylamine |
Nn receptor antagonist
|
|
Nm or Nn receptor antagonist?
Used to treat hypertension in patients with acute dissecting aortic aneurysms |
Nn receptor antagonist
|
|
what is the predominant tone maintained by in arterioles?
|
sympathetic (adrenergic)
|
|
what is the predominant tone maintained by in veins?
|
sympathetic (adrenergic)
|
|
what is the predominant tone maintained by in heart?
|
parasympathetic (cholinergic)
|
|
what is the predominant tone maintained by in iris?
|
parasympathetic (cholinergic)
|
|
what is the predominant tone maintained by in ciliary muscles?
|
parasympathetic (cholinergic)
|
|
what is the predominant tone maintained by in GI tract?
|
parasympathetic (cholinergic)
|
|
what is the predominant tone maintained by in Urinary bladder?
|
parasympathetic (cholinergic)
|
|
what is the predominant tone maintained by in salivary glands?
|
parasympathetic (cholinergic)
|
|
what is the predominant tone maintained by in sweat glands?
|
sympathetic (cholinergic)
|
|
drugs that mimic sympathetic nerve stimulation?
|
Sympathomimetics
|
|
which classes of adrenergic drugs are sympathomimetrics?
|
alpha agonists
beta agonists MAO inhibitors uptake inhibitors |
|
what are the two important nonselective adrenergic agonists?
|
epinephrine and norepinephrine
|
|
what is NE used to treat?
|
shock
|
|
at low concentrations of epi, what adrenergic receptors are stimulated?
|
B1 and B2
|
|
what is epi used to treat?
|
asthma and anaphylaxis because it dilates the bronchial smooth muscle
|
|
NE acts on what adrenergic receptors?
|
A1, A2, B1
|
|
Epi works on what receptors?
|
A1, B1, and B2
|