Neostigmine - Mechanism of action, indications and side effects
- 1. Mohammad saleh Moallem SHANDONG UNIVERSITY
- 2. What is the neostigmine? Please talk about its medical uses, mechanism of action and side effects. Question
- 3. Neostigmine Neostigmine is a medication used to treat myasthenia gravis, Ogilvie syndrome, and urinary retention without the presence of a blockage. It is also used in Anaesthesia to end the effects of non-depolarizing neuromuscular blocking medication. It is given by injection either into a vein, muscle, or under the skin. After injection effects are generally greatest within 30 minutes and last up to 4 hours.
- 4. Indications of Neostigmine Myasthenia gravis (MG) is a chronic autoimmune disorder in which antibodies destroy the communication between nerves and muscle, resulting in weakness of the skeletal muscles. Myasthenia gravis affects the voluntary muscles of the body, especially those that control the eyes, mouth, throat and limbs.
- 5. Indications of Neostigmine Ogilvie syndrome is the acute dilatation of the colon in the absence of any mechanical obstruction in severely ill patients. Ogilvie syndrome may occur after surgery, especially following coronary artery bypass surgery and total joint replacement. Drugs that disturb colonic motility (such as anticholinergics or opioid analgesics) contribute to the development of this condition.
- 6. Neostigmine Neostigmine is a cholinesterase inhibitor used in the symptomatic treatment of myasthenia gravis by improving muscle tone. Cholinesterase is a family of enzymes that catalyzes the hydrolysis of the neurotransmitter acetylcholine (ACh) into choline and acetic acid, a reaction necessary to allow a cholinergic neuron to return to its resting state after activation. So cholinesterase decrease the amount of Ach
- 7. Description Acetylcholine is the chief neurotransmitter of the parasympathetic nervous system, the part of the autonomic nervous system (a branch of PNS) that contracts smooth muscles, dilates blood vessels, increases bodily secretions, and slows heart rate. In most people with myasthenia gravis, the immune system blocks or damages these acetylcholine receptors. The acetylcholine cannot then attach to the receptor and so the muscle is less able to contract.
- 8. Description Cholinergic drugs stimulate the activation of the parasympathetic nervous system by activating receptors for acetylcholine. Anticholinergic drugs inhibit the parasympathetic nervous system by blocking the action of acetylcholine so that it cannot bind to receptors that initiate the parasympathetic response.
- 9. Neostigmine Neostigmine is a cholinesterase inhibitor used in the symptomatic treatment of myasthenia gravis by improving muscle tone. Neostigmine is in the cholinergic family of medications. It works by blocking the action of acetylcholinesterase and therefore increases the levels of acetylcholine. Neostigmine: Cholinesterase inhibitor = ↑ ACh
- 10. Neostigmine Neostigmine: Cholinesterase inhibitor = ↑ Ach Neostigmine works by slowing the breakdown of acetylcholine when it is released from nerve endings. This means that there is more acetylcholine available to attach to the muscle receptors and this improves the strength of your muscles. Neostigmine, unlike physostigmine, does not cross the blood-brain barrier.
- 11. Neostigmine Neostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. The drug inhibits acetylcholinesterase which is responsible for the degradation of acetylcholine. So, with acetylcholinesterase inhibited, more acetylcholine is present By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors which are involved in muscle contraction. It does not cross the blood-brain barrier.
- 12. How it acts as anticholinesterase? Neostigmine is an anticholinesterase inhibitor and inhibits the hydrolysis of acetylcholine by competing with acetylcholine for binding to acetylcholinesterase at the site of cholinergic transmission. By reducing the hydrolysis of acetylcholine, the transmission of nerve impulses is facilitated.
- 13. Why neostigmine is given with atropine in myasthenia gravis? At the end of surgery, neostigmine has been given for the reversal of neuromuscular blocking agents with several adverse effects such as bradycardia and profuse secretion. Atropine has been used to prevent those side effects of neostigmine.
- 14. Usage after surgery The use of neostigmine significantly reduces the risk that a patient will be left with muscle weakness in the recovery room. Many anesthesiologists routinely use neostigmine because postoperative muscle weakness may lead to adverse events after surgery. Neostigmine also relieves gastric contraction after surgery by increasing the stimulation and tone of gastric muscles. Atropine has been used to prevent those side effects of neostigmine.
- 15. Neostigmine Neostigmine can induce generic ocular side effects including: headache, brow pain, blurred vision, phacodonesis, pericorneal injection, congestive iritis, various allergic reactions, and rarely, retinal detachment. Neostigmine has a wide variety of side-effects such as reduced heart rate (bradycardia), due to the increase of acetylcholine at nerve terminals. For this reason it is usually given along with an anti- cholinergic drug such as atropine or glycopyrrolate.
- 16. Neostigmine Gastrointestinal symptoms occur earliest after ingestion and include anorexia, nausea, vomiting, abdominal cramps, and diarrhea. Side effects titles as review: . Nausea, headache, insomnia, dry mouth, dizziness, vomiting, allergic reactions, skin rash, hot flashes, joint pain, stroke, weakness, muscle cramps, frequent urination
- 17. Pharmacokinetics of drug Neostigmine is rapidly absorbed after intramuscular injection (IM). Neostigmine binding to human serum albumin is approximately 15 to 25%. Neostigmine is metabolized in the liver by microsomal enzymes. The apparent excretory half- life of neostigmine is between 24 and 113 minutes.
- 18. Mohammad saleh Moallem SHANDONG UNIVERSITY 默汉 201816230152