Question

Question 1

Muscarinic agonists and acetylcholinesterase inhibitors have similar therapeutic effects and share some side effects. Using a diagram, explain the mechanism of action of each drug and why they are therapeutically similar.

Question 2

You are a consultant for the FDA and have been asked to evaluate a New Drug Application. The executive summary claims the new drug is superior to existing therapies in three ways:

1. New drug is equally efficacious but more potent
2. Existing drugs are subject to approximately 50% loss due to first pass metabolism. The new drug is not affected by first pass metabolism (You may assume equal absorption)
3. The existing drugs have half-lives of approximately four hours. The half-life for the new drug is 24 hours.

Part I: Draw a graph for each of the above points that summarizes experiments supporting the claims being made. Clearly label the new drug and old drug on each graph.

Part II: The application claims that the new drug will allow for once a day dosing and have reduced side effects. In your opinion, do the data support this conclusion? Why or why not?

Answer 1

1.muscarinic agonists;

muscarinic receptor agonists ar Drugs That bind and activate muscarinic cholineagil receptors а ) t hеlрѕ a thias. Thе ѕmоот, muscle tone, especially in Gastrointestinal tract, urinary bladder and eye jetont & & also help is reducing the heart rate

Muscarinic agonist drugs;

muscarinte agonist daug: - choline esters sostenvado / coby Acetylcholine, me tha choline, cobachol, bethanechal alkaloids. a pilocarpine muscarine, are coline, sino They are directly act on muscarinic los reoptous.

Mechanism of action of muscarinic drugs;

mechanism of auton: * Drugs bind to muscarine the receptors of * Receptors are preserk is The smooth musul acts on the receptes, Increases the smooth muscles tone, * mainly & The Gastroinsterial tract, usinary Bloddler and age of

Acetylcholine esterase inhibitor;

Acetylcholinesterase inhibitor (AchEZ) 2. & Acetylcholinesterase inhibitor maisly irtibits The artykeholinesterase enzyme >> atelylcholinesterase enzyme helps is Breaking down acetylcholine Esto choline and acetats Finally increasing both The duration and level of action of the neurotransmitter autylcholine OA

Side effects of muscarinic and acetylcholine esterase inhibitor;

• Increasing the saliva and gastric secretion.
• Smooth muscle get relaxed.
• Bradycardia and hypotension.
• Asthma exacerbated.
• Nausea,vomiting,diarrhoea.
• Muscle cramps.
• Insomnia-not able to sleep for a long time.

Uses of acetylcholine esterase inhibitor;

uses of neetylcholinesterase Inhibitor :- used in the Treament and managment of dementia caused by alsheimer's diseases used is the treatment and managment & Parkinson's diseases glaucoma, myasthenia gran

Drugs of acetylcholine esterase inhibitor;

Acetylcholinesteras Thibitors Daugs * Donepezil * Rivastigmiru anh galantamine tambenonium * Tacaine

Mechanism of action of acetylcholine esterase inhibitor;

mechanism of action d en deity kholinesterase Inhibitors That inhibit The Enzyme acetylcholinesterase o todo lo . choline to bus totesis of a nosas ndard Word acetylcholine Autylcholinestras 1207 To B brud hul reino chEI dan and e autate scetylcholine Estoase arreto Thibitous

Diagram;

Presynaptic ) Katyl con coin terminal Achat SALLEI Ach muscarinic relepions Autylcholing choline & aurat post x2 synaptic terminal

Therapeutic similar between muscarinic and acetylcholine esterase inhibitor;

>> dcetylcholinesterase inhibits a down regulate the action of autylcholinesterase Enzyme, to Ach is not broken down tito acetate and chalen muscaréric agonist auck on The Quetylcholin, receptors, which are present is the post spray material, muscarinic agonisk drug bisel to receptors the muscle The tore to finally increas finally the Presynaptic " Ach ET) Eg: Rivastigmire Galantamine Acetylcholine musiarisie agonist Receptoget Estuas Acetat Ach + cholini past synopter Teemiral