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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