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Reversal Agents

  1. Cholinesterase inhibitors or anticholinesterase
  2. Mechanism Of Action. Increase the amount of Ach available to compete with Non – Dep. Agent by reversibly binding with enzyme Cholinesterase.
  3. Resp. Acidosis and Metabolic alkalosis impairs reversal
  4. Muscarinic S/E decrease dysrhythmias
  5. Important: Reversal of non depolarizing muscle relaxant action is done by administration of neostigmine + atropine. Neostigmine being an anticholinesterase, causes accumulation of acetylcholine at cholinergic synaptic clefts. This acetylcholine competes with the non-depolarizing muscle relaxant and thus neuromuscular block is reversed. Atropine, when administered with neostigmine, prevents any muscarinic side effects due to accumulation of acetylcholine at muscarinic sites.
    1. Bronchospasm, bronchial secretions
    2. Intestinal spasm, increased salivation, increased sweating
    3. Increased bladder tone, pupillary constriction


  1. Quaternary ammonium – Effect comes in 5-10 min and lasts > 1 hrs.
  2. Dose – 0.04 to 0.08 mg/kg (more)
  3. Other uses: For treatment for Myasthenia Gravis, Urinary bladder atony, paralytic ileus, adjunct to intrathecal anesth.
  4. Important: Neostigmine is an anticholinesterase (MCQ) and thus causes accumulation of. acetylcholine at neuromuscular junction. This acetylcholine competes with tubocurare for the NM receptor site and thus tubocurare-induced neuromuscular block is reversed.


  1. Crosses BBB
  2. Dose 0.1 – 0.3 mg/kg.
  3. Because it crosses blood brain barrier, it is a drug of choice of central anti cholinergic syndrome.


  1. Dose: (0.5 – 1mg/kg)
  2. Most Rapid onset and shortest duration
  3. Note: Anticholinergic Drug is given in the reversal to prevent muscarinic side effects of cholinesterase inhibitors.
  4. Atropine 0.4mg to be given with every 1mg neostigmine at the time of reversal.
  5. Atropine causes maximum tachycardia and Bronchodilation
  6. Glycopyrrolate 2mg to be given with every 1mg neostigmine at the time of reversal.
  7. The amnesia, anti emetic, sedation and Antisialagogue effect are unique properties of Scopolamine (Hysocine)
  8. Large dose  cause cutaneous vasodilation, Atropine flush, decreased gastric secretion, decrease Salivary secretion, decreased GIT motility and peristalsis and decrease Lower Oesophageal Sphincter  tone.
  9. Mydriasis and Cycloplegia
  10. Decreased ureter and bladder tone
  11. Decreased sweating – increased temp
Central anticholinergic syndrome
  1. Caused by Atropine, Hyoscine, Tricyclic Antidepressant (TCAD), Antihistaminics, Antipsychotics, Belladonna alkaloid except Glycopyrrolate.
  2. Common in elderly
  3. S/S Drowsiness or coma, excitation and agitation, hallucinations, motor incoordination and pyrexia, dry mouth, increased P.R. flushing, improper vision,
  4. Treatment - physostigmine, .01-0.3 mg/kg

Cholinergic Crises

  1. Due to excessive Ach because of high dose of anticholinesterase
  2. C/F – Muscle weakness, increase secretion, fasciculation, nausea and vomiting, decrease P.R. decrease B.P., respiratory paralysis, aspiration pneumonia
  3. Treatment
    1. Mechanical ventilation,
    2. Tracheobronchial lavage,
    3. Atropine,
    4. PAM
Signs of Adequate reversal
  1. Regular respiration with adequate tidal volume
  2. Spontaneous eye opening
  3. Spontaneous limb movement
  4. Able to protrude tongue
  5. Able to cough
  6. No cyanosis
  7. Able to lift head > 5 sec - Best clinical sign.



Recent advances- Sugammadex is a novel agent for reversal of neuromuscular blockade by the agent rocuronium in general anaesthesia. It is the first selective relaxant binding agent (SRBA). The main advantage of sugammadex is reversal of neuromuscular blockade without relying on inhibition of acetylcholinesterase. Therefore it does not cause the autonomic instability produced by anticholinesterases such as neostigmine, and antimuscarinic agents such as atropine do not need to be co-administered. Its administration is associated with much greater cardiovascular and autonomic stability than the traditional reversal agents.

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