Pharmacology · MU Sofia

92. Antidotes.

Introduces antidotes as agents that counteract poisons or overdoses, through neutralising the poison, preventing absorption, promoting elimination or reversing physiological effects. It then goes through eight common antidote pairings in turn, giving for each the antidote, route of administration and mechanism, covering acetaminophen, opioids, benzodiazepines, methanol and ethylene glycol, organophosphates, warfarin, anticholinergics and beta-blockers. It ends with five recap questions.

Inside: 3 sections · 5 labelled pictures · 10 flashcards · 2 min

Topic 91 of 93 in the MU Sofia syllabus for Pharmacology (Medicine, Year 3). The free AceMed note covers it in 3 sections, about 325 words (2 min of reading), with 10 flashcards.

In this note

  1. Antidotes
  2. Common Antidotes and Their Mechanisms
  3. RECAP QUESTIONS

Antidotes

Antidotes are agents used to counteract the toxic effects of poisons or overdoses.

They may work by:

  • Neutralizing the poison
  • Preventing absorption
  • Promoting elimination
  • Reversing or blocking physiological effects

Common Antidotes and Their Mechanisms

1. Acetaminophen (Paracetamol)

  • Antidote: N-acetylcysteine (NAC)
  • Administration: Oral or IV; most effective within 8–10 hours of overdose.

Mechanism:

- Replenishes hepatic glutathione.

- Detoxifies NAPQI, the toxic metabolite of acetaminophen.

2. Opioids (e.g., Morphine, Heroin)

  • Antidote: Naloxone
  • Administration: Intranasal, IM, SC, or IV

Mechanism:

- Competitive antagonist at μ-opioid receptors.

- Rapidly reverses CNS and respiratory depression.

3. Benzodiazepines (e.g., Diazepam, Lorazepam)

  • Antidote: Flumazenil
  • Administration: IV

Use with caution: Can trigger withdrawal seizures in dependent patients.

Mechanism:

- Competitive antagonist at GABA-A benzodiazepine receptor site.

- Reverses sedation and respiratory depression.

4. Methanol and Ethylene Glycol

  • Antidote: Fomepizole (preferred) or Ethanol
  • Administration: IV

Mechanism:

- Inhibits alcohol dehydrogenase.

- Prevents conversion into toxic metabolites (e.g., formic acid, oxalic acid).

5. Organophosphates (e.g., insecticides)

  • Antidote: Atropine + Pralidoxime
  • Administration: IV

Mechanism:

- Atropine: Blocks muscarinic receptors to reduce secretions and bradycardia.

- Pralidoxime: Reactivates acetylcholinesterase enzyme inhibited by the toxin.

6. Warfarin

  • Antidote: Vitamin K1 (Phytonadione)
  • Administration: Oral or IV depending on INR and bleeding severity.

Mechanism:

- Promotes synthesis of clotting factors II, VII, IX, X.

- Reverses anticoagulant effects of warfarin.

7. Anticholinergics (e.g., Atropine, Diphenhydramine)

  • Antidote: Physostigmine
  • Administration: IV (use with caution)

Mechanism:

- Acetylcholinesterase inhibitor.

- Increases synaptic acetylcholine to counteract anticholinergic symptoms.

- Caution: Can cause seizures or bradycardia.

8. Beta-blockers

  • Antidote: Glucagon
  • Administration: IV

Mechanism:

- Activates adenylate cyclase independently of beta-receptors.

- Increases cAMP → enhances cardiac contractility and heart rate.

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