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Cholinergic Drugs: Types, Uses, and Side Effects

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Hiraya Manawari

2/24/2023

Biology

Holinergic Drugs

Cholinergic Drugs: Types, Uses, and Side Effects

Cholinergic Drugs: Mechanism, Classification, and Effects

Cholinergic drugs act on the cholinergic system, affecting acetylcholine neurotransmission. They are classified as agonists or antagonists and have various therapeutic uses and side effects.

Key points:

  • Cholinergic drugs classification: Direct-acting and indirect-acting agonists, antagonists
  • Cholinergic drugs mechanism of action: Stimulate or block cholinergic receptors
  • Cholinergic drugs examples: Bethanechol, pilocarpine, neostigmine, atropine
  • Cholinergic drugs uses: Glaucoma, myasthenia gravis, overactive bladder
  • Side effects of cholinergic drugs: Dry mouth, blurred vision, urinary retention
...

2/24/2023

313

ACETYLCHOLINE
CHOLINE
NA*
6
RECYCLING
OF CHOLINE
Ca²+
S DEGRADA-
Pr
TION OF
ACETYLCHOLINE
+Cast
CHOLINE
Na*
ACETYLCHOLINE
CHOLINE
ACETATE
SY

View

Classification of Cholinergic Drugs

This page outlines the classification of cholinergic drugs. They are broadly categorized into cholinergic agonists cholinomimeticdrugscholinomimetic drugs and cholinergic antagonists. Cholinergic agonists are further divided into direct-acting and indirect-acting drugs.

Direct-acting cholinomimetics activate muscarinic and nicotinic receptors directly. They include choline esters and alkaloids. Indirect-acting cholinomimetics increase acetylcholine levels by inhibiting acetylcholinesterase. These include organophosphates and carbamates.

Definition: Cholinomimetic drugs are substances that mimic the action of acetylcholine in the body.

Example: Bethanechol is a direct-acting cholinomimetic used to treat urinary retention.

ACETYLCHOLINE
CHOLINE
NA*
6
RECYCLING
OF CHOLINE
Ca²+
S DEGRADA-
Pr
TION OF
ACETYLCHOLINE
+Cast
CHOLINE
Na*
ACETYLCHOLINE
CHOLINE
ACETATE
SY

View

Cholinergic Agonists: Direct-Acting Drugs

This page focuses on direct-acting cholinergic agonist drugs. Choline esters, a subclass of direct-acting cholinomimetics, include acetylcholine theprototypethe prototype, bethanechol forurinaryretentionfor urinary retention, carbachol forglaucomafor glaucoma, and methacholine forasthmadiagnosisfor asthma diagnosis.

Alkaloids, another subclass of direct-acting cholinomimetics, include pilocarpine, which is the drug of choice for emergency lowering of intraocular pressure in acute angle-closure glaucoma.

The page also mentions edrophonium, an indirect-acting cholinergic drug used in the diagnosis of myasthenia gravis through the Tensilon test.

Highlight: Pilocarpine is crucial in the emergency treatment of acute angle-closure glaucoma.

Vocabulary: Myasthenia gravis - An autoimmune disorder characterized by muscle weakness due to damaged acetylcholine receptors.

ACETYLCHOLINE
CHOLINE
NA*
6
RECYCLING
OF CHOLINE
Ca²+
S DEGRADA-
Pr
TION OF
ACETYLCHOLINE
+Cast
CHOLINE
Na*
ACETYLCHOLINE
CHOLINE
ACETATE
SY

View

Indirect-Acting Cholinergic Drugs and Cholinergic Antagonists

This page covers indirect-acting cholinergic drugs and introduces cholinergic antagonists. Carbamates, a class of indirect-acting cholinergics with intermediate duration, include physostigmine usedasanantidoteforanticholinergicpoisoningused as an antidote for anticholinergic poisoning and neostigmine thedrugofchoiceformyastheniagravistreatmentthe drug of choice for myasthenia gravis treatment.

Organophosphates, another class of indirect-acting cholinergics with long duration, include drugs used for glaucoma treatment and insecticides. The antidote for organophosphate poisoning is pralidoxime PAMPAM along with atropine.

The page also introduces cholinergic antagonists, which block cholinergic receptors. These are classified based on the type of receptor they block: muscarinic or nicotinic.

Example: Physostigmine is used as an antidote for anticholinergic poisoning caused by atropine, phenothiazines, or tricyclic antidepressants.

Highlight: The combination of pralidoxime and atropine is crucial in treating organophosphate poisoning.

ACETYLCHOLINE
CHOLINE
NA*
6
RECYCLING
OF CHOLINE
Ca²+
S DEGRADA-
Pr
TION OF
ACETYLCHOLINE
+Cast
CHOLINE
Na*
ACETYLCHOLINE
CHOLINE
ACETATE
SY

View

Muscarinic Blockers and Their Effects

This page focuses on muscarinic blockers, a type of cholinergic antagonist. Atropine is the prototype muscarinic blocker, with various derivatives used for different purposes. For instance, hyoscine scopolaminescopolamine is used to prevent motion sickness, often administered as a transdermal patch.

The page describes the classic anticholinergic effects using the mnemonic "dry as a bone, blind as a bat, hot as a hare, red as a beet." These effects include dry mouth, blurred vision, hyperthermia, and flushed skin.

Various muscarinic blockers are listed with their specific uses, such as ipratropium and tiotropium for asthma and COPD, and drugs like oxybutynin and tolterodine for overactive bladder.

Vocabulary: Anticholinergic effects - The physiological effects resulting from the blocking of acetylcholine receptors.

Example: Ipratropium, a quaternary derivative of atropine, is used as a bronchodilator in asthma treatment due to its more peripheral effects on the lungs and reduced CNS effects.

ACETYLCHOLINE
CHOLINE
NA*
6
RECYCLING
OF CHOLINE
Ca²+
S DEGRADA-
Pr
TION OF
ACETYLCHOLINE
+Cast
CHOLINE
Na*
ACETYLCHOLINE
CHOLINE
ACETATE
SY

View

Ganglionic and Neuromuscular Blockers

This final page discusses ganglionic blockers and neuromuscular blockers, both types of cholinergic antagonists. Ganglionic blockers, such as hexamethonium, block neurotransmission at nicotinic receptors in autonomic ganglia.

Neuromuscular blockers are divided into two categories:

  1. Non-depolarizing, competitive, reversible blockers e.g.,tubocurarine,atracuriume.g., tubocurarine, atracurium used as muscle relaxants.
  2. Depolarizing, irreversible, non-competitive blockers, with succinylcholine being the only one in clinical use.

The page highlights the risk of malignant hyperthermia associated with succinylcholine use, a life-threatening condition caused by excessive calcium release due to overactivation of ryanodine receptors.

Highlight: Succinylcholine, the only depolarizing muscle relaxant in clinical use, can cause malignant hyperthermia, a potentially fatal complication.

Vocabulary: Malignant hyperthermia - A severe reaction to certain anesthetic drugs, characterized by rapid temperature increase, muscle rigidity, and metabolic acidosis.

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Biology

313

Feb 24, 2023

6 pages

Cholinergic Drugs: Types, Uses, and Side Effects

Cholinergic Drugs: Mechanism, Classification, and Effects

Cholinergic drugs act on the cholinergic system, affecting acetylcholine neurotransmission. They are classified as agonists or antagonists and have various therapeutic uses and side effects.

Key points:

  • Cholinergic drugs classification: Direct-acting and indirect-acting... Show more

ACETYLCHOLINE
CHOLINE
NA*
6
RECYCLING
OF CHOLINE
Ca²+
S DEGRADA-
Pr
TION OF
ACETYLCHOLINE
+Cast
CHOLINE
Na*
ACETYLCHOLINE
CHOLINE
ACETATE
SY

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Classification of Cholinergic Drugs

This page outlines the classification of cholinergic drugs. They are broadly categorized into cholinergic agonists cholinomimeticdrugscholinomimetic drugs and cholinergic antagonists. Cholinergic agonists are further divided into direct-acting and indirect-acting drugs.

Direct-acting cholinomimetics activate muscarinic and nicotinic receptors directly. They include choline esters and alkaloids. Indirect-acting cholinomimetics increase acetylcholine levels by inhibiting acetylcholinesterase. These include organophosphates and carbamates.

Definition: Cholinomimetic drugs are substances that mimic the action of acetylcholine in the body.

Example: Bethanechol is a direct-acting cholinomimetic used to treat urinary retention.

ACETYLCHOLINE
CHOLINE
NA*
6
RECYCLING
OF CHOLINE
Ca²+
S DEGRADA-
Pr
TION OF
ACETYLCHOLINE
+Cast
CHOLINE
Na*
ACETYLCHOLINE
CHOLINE
ACETATE
SY

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Cholinergic Agonists: Direct-Acting Drugs

This page focuses on direct-acting cholinergic agonist drugs. Choline esters, a subclass of direct-acting cholinomimetics, include acetylcholine theprototypethe prototype, bethanechol forurinaryretentionfor urinary retention, carbachol forglaucomafor glaucoma, and methacholine forasthmadiagnosisfor asthma diagnosis.

Alkaloids, another subclass of direct-acting cholinomimetics, include pilocarpine, which is the drug of choice for emergency lowering of intraocular pressure in acute angle-closure glaucoma.

The page also mentions edrophonium, an indirect-acting cholinergic drug used in the diagnosis of myasthenia gravis through the Tensilon test.

Highlight: Pilocarpine is crucial in the emergency treatment of acute angle-closure glaucoma.

Vocabulary: Myasthenia gravis - An autoimmune disorder characterized by muscle weakness due to damaged acetylcholine receptors.

ACETYLCHOLINE
CHOLINE
NA*
6
RECYCLING
OF CHOLINE
Ca²+
S DEGRADA-
Pr
TION OF
ACETYLCHOLINE
+Cast
CHOLINE
Na*
ACETYLCHOLINE
CHOLINE
ACETATE
SY

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Indirect-Acting Cholinergic Drugs and Cholinergic Antagonists

This page covers indirect-acting cholinergic drugs and introduces cholinergic antagonists. Carbamates, a class of indirect-acting cholinergics with intermediate duration, include physostigmine usedasanantidoteforanticholinergicpoisoningused as an antidote for anticholinergic poisoning and neostigmine thedrugofchoiceformyastheniagravistreatmentthe drug of choice for myasthenia gravis treatment.

Organophosphates, another class of indirect-acting cholinergics with long duration, include drugs used for glaucoma treatment and insecticides. The antidote for organophosphate poisoning is pralidoxime PAMPAM along with atropine.

The page also introduces cholinergic antagonists, which block cholinergic receptors. These are classified based on the type of receptor they block: muscarinic or nicotinic.

Example: Physostigmine is used as an antidote for anticholinergic poisoning caused by atropine, phenothiazines, or tricyclic antidepressants.

Highlight: The combination of pralidoxime and atropine is crucial in treating organophosphate poisoning.

ACETYLCHOLINE
CHOLINE
NA*
6
RECYCLING
OF CHOLINE
Ca²+
S DEGRADA-
Pr
TION OF
ACETYLCHOLINE
+Cast
CHOLINE
Na*
ACETYLCHOLINE
CHOLINE
ACETATE
SY

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Improve your grades

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Muscarinic Blockers and Their Effects

This page focuses on muscarinic blockers, a type of cholinergic antagonist. Atropine is the prototype muscarinic blocker, with various derivatives used for different purposes. For instance, hyoscine scopolaminescopolamine is used to prevent motion sickness, often administered as a transdermal patch.

The page describes the classic anticholinergic effects using the mnemonic "dry as a bone, blind as a bat, hot as a hare, red as a beet." These effects include dry mouth, blurred vision, hyperthermia, and flushed skin.

Various muscarinic blockers are listed with their specific uses, such as ipratropium and tiotropium for asthma and COPD, and drugs like oxybutynin and tolterodine for overactive bladder.

Vocabulary: Anticholinergic effects - The physiological effects resulting from the blocking of acetylcholine receptors.

Example: Ipratropium, a quaternary derivative of atropine, is used as a bronchodilator in asthma treatment due to its more peripheral effects on the lungs and reduced CNS effects.

ACETYLCHOLINE
CHOLINE
NA*
6
RECYCLING
OF CHOLINE
Ca²+
S DEGRADA-
Pr
TION OF
ACETYLCHOLINE
+Cast
CHOLINE
Na*
ACETYLCHOLINE
CHOLINE
ACETATE
SY

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Ganglionic and Neuromuscular Blockers

This final page discusses ganglionic blockers and neuromuscular blockers, both types of cholinergic antagonists. Ganglionic blockers, such as hexamethonium, block neurotransmission at nicotinic receptors in autonomic ganglia.

Neuromuscular blockers are divided into two categories:

  1. Non-depolarizing, competitive, reversible blockers e.g.,tubocurarine,atracuriume.g., tubocurarine, atracurium used as muscle relaxants.
  2. Depolarizing, irreversible, non-competitive blockers, with succinylcholine being the only one in clinical use.

The page highlights the risk of malignant hyperthermia associated with succinylcholine use, a life-threatening condition caused by excessive calcium release due to overactivation of ryanodine receptors.

Highlight: Succinylcholine, the only depolarizing muscle relaxant in clinical use, can cause malignant hyperthermia, a potentially fatal complication.

Vocabulary: Malignant hyperthermia - A severe reaction to certain anesthetic drugs, characterized by rapid temperature increase, muscle rigidity, and metabolic acidosis.

ACETYLCHOLINE
CHOLINE
NA*
6
RECYCLING
OF CHOLINE
Ca²+
S DEGRADA-
Pr
TION OF
ACETYLCHOLINE
+Cast
CHOLINE
Na*
ACETYLCHOLINE
CHOLINE
ACETATE
SY

Sign up to see the contentIt's free!

Access to all documents

Improve your grades

Join milions of students

By signing up you accept Terms of Service and Privacy Policy

Acetylcholine Synthesis and Action

This page illustrates the synthesis, release, and degradation of acetylcholine at synapses. Acetylcholine is synthesized in the presynaptic neuron from choline and acetyl-CoA. It is then packaged into synaptic vesicles and released into the synaptic cleft when an action potential arrives. Acetylcholine binds to receptors on the postsynaptic membrane to transmit the signal. Acetylcholinesterase rapidly breaks down acetylcholine in the synaptic cleft to terminate its action.

Vocabulary: Acetylcholinesterase - The enzyme that breaks down acetylcholine in the synaptic cleft.

Highlight: The recycling of choline back into the presynaptic neuron is an important step in maintaining acetylcholine synthesis.

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The app is very easy to use and well designed. I have found everything I was looking for so far and have been able to learn a lot from the presentations! I will definitely use the app for a class assignment! And of course it also helps a lot as an inspiration.

Stefan S

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This app is really great. There are so many study notes and help [...]. My problem subject is French, for example, and the app has so many options for help. Thanks to this app, I have improved my French. I would recommend it to anyone.

Samantha Klich

Android user

Wow, I am really amazed. I just tried the app because I've seen it advertised many times and was absolutely stunned. This app is THE HELP you want for school and above all, it offers so many things, such as workouts and fact sheets, which have been VERY helpful to me personally.

Anna

iOS user

I think it’s very much worth it and you’ll end up using it a lot once you get the hang of it and even after looking at others notes you can still ask your Artificial intelligence buddy the question and ask to simplify it if you still don’t get it!!! In the end I think it’s worth it 😊👍 ⚠️Also DID I MENTION ITS FREEE YOU DON’T HAVE TO PAY FOR ANYTHING AND STILL GET YOUR GRADES IN PERFECTLY❗️❗️⚠️

Thomas R

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Knowunity is the BEST app I’ve used in a minute. This is not an ai review or anything this is genuinely coming from a 7th grade student (I know 2011 im young) but dude this app is a 10/10 i have maintained a 3.8 gpa and have plenty of time for gaming. I love it and my mom is just happy I got good grades

Brad T

Android user

Not only did it help me find the answer but it also showed me alternative ways to solve it. I was horrible in math and science but now I have an a in both subjects. Thanks for the help🤍🤍

David K

iOS user

The app's just great! All I have to do is enter the topic in the search bar and I get the response real fast. I don't have to watch 10 YouTube videos to understand something, so I'm saving my time. Highly recommended!

Sudenaz Ocak

Android user

In school I was really bad at maths but thanks to the app, I am doing better now. I am so grateful that you made the app.

Greenlight Bonnie

Android user

I found this app a couple years ago and it has only gotten better since then. I really love it because it can help with written questions and photo questions. Also, it can find study guides that other people have made as well as flashcard sets and practice tests. The free version is also amazing for students who might not be able to afford it. Would 100% recommend

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iOS user

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Marco B

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Elisha

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This app is phenomenal down to the correct info and the various topics you can study! I greatly recommend it for people who struggle with procrastination and those who need homework help. It has been perfectly accurate for world 1 history as far as I’ve seen! Geometry too!

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iOS user