Cholinergic Agonists and Acetylcholinesterase Inhibitors

Parasympathomimetics or muscarinic agonists

By either direct agonist effect or by preventing the breakdown of ACh by AChE

The desired drug action targets a specific organ, while the ADRs affect other organs

<p>Ganglionic stimulants</p> Signup and view all the answers

<p>In the eye, heart, blood vessels, lung, GI tract, urinary bladder, and sweat glands</p> Signup and view all the answers

<p>By both activating muscarinic receptors on target organs and inhibiting the release of neurotransmitters from nerve terminals</p> Signup and view all the answers

<p>It increases the tone of the detrusor urinae muscle.</p> Signup and view all the answers

<p>It can cause excessive secretion of gastric acid.</p> Signup and view all the answers

<p>It is highly susceptible to cholinesterase.</p> Signup and view all the answers

<p>Treating glaucoma.</p> Signup and view all the answers

<p>Its effects peak in 60 minutes for the oral dose.</p> Signup and view all the answers

<p>It can increase pressure within the urinary tract.</p> Signup and view all the answers

<p>It acts at both muscarinic and nicotinic receptors.</p> Signup and view all the answers

<p>Its effects are more prolonged than those of ACh.</p> Signup and view all the answers

<p>It can stimulate muscarinic receptors in the lungs, resulting in bronchoconstriction.</p> Signup and view all the answers

<p>It is active at muscarinic receptors only.</p> Signup and view all the answers

<p>Cardiovascular disease</p> Signup and view all the answers

<p>It causes increased heart rate due to increased NE release.</p> Signup and view all the answers

<p>Subcutaneous</p> Signup and view all the answers

<p>All of the above</p> Signup and view all the answers

<p>10-50 mg</p> Signup and view all the answers

<p>2.5 mg</p> Signup and view all the answers

<p>Take 1 hour before or 2 hours after meals</p> Signup and view all the answers

<p>0.4 mg</p> Signup and view all the answers

<p>All of the above</p> Signup and view all the answers

<p>Treatment of urinary retention due to neurogenic atony of the bladder</p> Signup and view all the answers

<p>7%</p> Signup and view all the answers

<p>20%</p> Signup and view all the answers

<p>95%</p> Signup and view all the answers

<p>16 mg/day</p> Signup and view all the answers

<p>Primarily by cholinesterase-mediated hydrolysis</p> Signup and view all the answers

<p>Decreases clearance by 64%</p> Signup and view all the answers

<p>Renal excretion</p> Signup and view all the answers

<p>Category C</p> Signup and view all the answers

<p>Category B</p> Signup and view all the answers

<p>Category B</p> Signup and view all the answers

<p>Donepezil should be titrated to response and tolerability</p> Signup and view all the answers

<p>The dosage should not exceed 14 mg</p> Signup and view all the answers

<p>All of the above</p> Signup and view all the answers

<p>They are well tolerated, with few adverse reactions</p> Signup and view all the answers

<p>Temporarily reducing the dose or taking the drug with meals</p> Signup and view all the answers

<p>They can exacerbate bronchospastic symptoms</p> Signup and view all the answers

<p>Suppression of warning symptoms of overdose with atropine and belladonna derivatives</p> Signup and view all the answers

<p>They can increase cholinergic activity in the brain</p> Signup and view all the answers

<p>They undergo significant metabolism by the CYP enzyme systems of the liver</p> Signup and view all the answers

<p>No dosage adjustments are recommended</p> Signup and view all the answers

<p>Increases it due to inhibition of CYP 3A4</p> Signup and view all the answers

<p>CYP 2D6</p> Signup and view all the answers

<p>Decrease renal clearance</p> Signup and view all the answers

<p>Loop diuretics</p> Signup and view all the answers

<p>Neostigmine and pyridostigmine</p> Signup and view all the answers

<p>By administering small initial doses followed by titration to an optimal dose</p> Signup and view all the answers

<p>They prevent the degradation of ACh by acetylcholinesterase (AChE)</p> Signup and view all the answers

<p>Organophosphate cholinesterase inhibitors</p> Signup and view all the answers

<p>It is a cholinesterase inhibitor used to treat Alzheimer's disease</p> Signup and view all the answers

<p>They bind to the active center of AChE, preventing the breakdown of ACh</p> Signup and view all the answers

<p>It is a piperidine-type AChE inhibitor with increased affinity for the CNS</p> Signup and view all the answers

<p>They can intensify ACh activity at all cholinergic junctions (muscarinic, ganglionic, and nicotinic)</p> Signup and view all the answers

<p>It is a potent selective inhibitor of AChE in the cortex and hippocampus</p> Signup and view all the answers

<p>Increased production of AChE</p> Signup and view all the answers

<p>They are found in pesticides and chemical weapons</p> Signup and view all the answers

<p>Alzheimer's disease is associated with profound cholinergic depletion</p> Signup and view all the answers

<p>The drug's selectivity for the brain</p> Signup and view all the answers

<p>It results in slower dissociation from AChE compared to ACh</p> Signup and view all the answers

<p>Pseudo-irreversible</p> Signup and view all the answers

<p>The plasma half-life is shorter than the duration of AChE inhibition</p> Signup and view all the answers

<p>Enhancing the effect of ACh on nicotinic receptors</p> Signup and view all the answers

<p>The drugs become less effective as the disease progresses</p> Signup and view all the answers

<p>Noncompetitive antagonism of NMDA receptors</p> Signup and view all the answers

<p>Rivastigmine has lower bioavailability due to a significant first-pass effect</p> Signup and view all the answers

<p>Primarily as unchanged drug in the urine</p> Signup and view all the answers

<p>Primarily by CYP 2D6 and 3A4 isoenzymes in the liver</p> Signup and view all the answers