Acetylcholinesterase

How is acetylcholinesterase dangerous to humans?

How is acetylcholinesterase dangerous to humans?
  1. Why is acetylcholinesterase harmful?
  2. What are the effects of acetylcholinesterase?
  3. Why can inhibiting acetylcholinesterase cause death?
  4. What is the most common side effect of acetylcholinesterase?
  5. What happens if you inhibit acetylcholinesterase?
  6. Are cholinesterase inhibitors poisonous?
  7. Why do we need acetylcholinesterase?
  8. What are acetylcholinesterase inhibitors used for?
  9. How is acetylcholinesterase inhibitor poisoning treated?
  10. How is organophosphate poisoning treated?
  11. How does organophosphate inhibit acetylcholinesterase?
  12. Why do acetylcholinesterase inhibitors cause excessive salivation?
  13. How do acetylcholinesterase inhibitors work to treat Alzheimer's?

Why is acetylcholinesterase harmful?

Acetylcholinesterase (AChE), the enzyme involved in the hydrolysis of the neurotransmitter acetylcholine, has been implicated in non-cholinergic actions which may play a role in neurodegenerative diseases such as Alzheimer's disease.

What are the effects of acetylcholinesterase?

The most common adverse effects of cholinesterase inhibitors include nausea, diarrhea, vomiting, decreased appetite, dyspepsia, anorexia, muscle cramps, fatigue, insomnia, dizziness, headache, and asthenia.

Why can inhibiting acetylcholinesterase cause death?

Severe cholinesterase inhibition can result in death primarily because of respiratory failure. This failure results from a combination of bronchial secretions, bronchial constriction, weakened respiratory muscle function, and inhibited respiratory drive.

What is the most common side effect of acetylcholinesterase?

The ChEIs share a common profile of adverse effects, the most frequent of which are nausea, vomiting, diarrhea, and dizziness. These are typically dose related and can be mitigated with slow up-titration to the desired maintenance dose.

What happens if you inhibit acetylcholinesterase?

The inhibition of the enzyme leads to accumulation of ACh in the synaptic cleft resulting in over-stimulation of nicotinic and muscarinic ACh receptors and impeded neurotransmission. The typical symptoms of acute poisoning are agitation, muscle weakness, muscle fasciculations, miosis, hypersalivation, sweating.

Are cholinesterase inhibitors poisonous?

Cholinesterase inhibitors fall into two classes, organophosphorus compounds, and carbamates. The former are generally have higher toxicity, longer duration of action and more commonly cause CNS toxicity.

Why do we need acetylcholinesterase?

Acetylcholinesterase (AChE) is a cholinergic enzyme primarily found at postsynaptic neuromuscular junctions, especially in muscles and nerves. ... [1] The primary role of AChE is to terminate neuronal transmission and signaling between synapses to prevent ACh dispersal and activation of nearby receptors.

What are acetylcholinesterase inhibitors used for?

The main use of cholinesterase inhibitors is for the treatment of dementia in patients with Alzheimer's disease. People with Alzheimer's disease have reduced levels of acetylcholine in the brain. Cholinesterase inhibitors have been shown to have a modest effect on dementia symptoms such as cognition.

How is acetylcholinesterase inhibitor poisoning treated?

Start with 1-2 g (20-40 mg/kg) IV in 100 mL isotonic sodium chloride over 15-30 min; repeat in 1 h if muscle weakness is not relieved; then repeat q3-8h if signs of poisoning recur; other dosing regimens have been used, including continuous drip.

How is organophosphate poisoning treated?

The definitive treatment for organophosphate poisoning is atropine, which competes with acetylcholine at the muscarinic receptors. The initial dose for adults is 2 to 5 mg IV or 0.05 mg/kg IV for children until reaching the adult dose.

How does organophosphate inhibit acetylcholinesterase?

Organophosphate (OP) and carbamate esters can inhibit acetylcholinesterase (AChE) by binding covalently to a serine residue in the enzyme active site, and their inhibitory potency depends largely on affinity for the enzyme and the reactivity of the ester.

Why do acetylcholinesterase inhibitors cause excessive salivation?

Indirect muscarinic stimulants are primarily inhibitors of the acetylcholinesterase enzyme, they increase acetylcholine to stimulate muscarinic and nicotinic receptors which results in an increased saliva flow.

How do acetylcholinesterase inhibitors work to treat Alzheimer's?

Donepezil, rivastigmine and galantamine all prevent an enzyme called acetylcholinesterase from breaking down acetylcholine. This means there is a higher concentration of acetylcholine in the brain, which leads to better communication between nerve cells. This may ease some symptoms of Alzheimer's disease for a while.

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