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Drugs for General Anesthesia - NEET PG Anesthesia

Feb 17, 2023

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INHALATIONAL ANESTHETIC AGENTS

Commonly used inhalational agents

PHARMACOKINETICS AND PHARMACODYNAMICS

Blood gas partition coefficient or blood gas solubility

Smell of Agents

PHARMACODYNAMIC PROPERTIES

CNS Effects

Effects on CVS

Effects on Respiratory system

Effects on liver

Effects on kidney

Components of GA

MALIGNANT HYPERTHERMIA

Drugs triggering 

Mechanism 

Clinical features 

Management 

CARRIER GAS

Drugs for General Anesthesia

Drugs used for general anesthesia are an important topic in the NEET PG exam because anesthesia is a critical component of many medical procedures. A thorough understanding of the topic is essential for any medical professional. 

In the exam, questions related to the pharmacology, mechanism of action, adverse effects, and clinical applications of anesthetic drugs are often asked, making it all the more to study for the NEET PG exam.

Let’s learn more about this important anesthesia topic for NEET PG exam preparation.


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INHALATIONAL ANESTHETIC AGENTS

Commonly used inhalational agents

  • Inorganic Gas 
    • N2O: It is less potent, used as carrier gas
  • Volatile liquids: More potent
    • Halothane
    • Isoflurane
    • Sevoflurane
    • Desflurane
  • Volatile agents not in clinical use
    • Methoxyflurane: Most nephrotoxic
    • Enflurane: Causes epilepsy
  • Inert gas
    • Xenon: Carrier gas, but due to high cost, currently not in use

PHARMACOKINETICS AND PHARMACODYNAMICS

 

Properties of potent inhalation agent

Chemistry

Halothane

Isoflurane

Sevoflurane

Desflurane

 

Halogenated Ethane 

Halogenated Ethers

 
  • Isoflurane and Desflurane are structural analogues
  • Enflurane is isomer of isoflurane

Boiling point

  • 50° C ± 2° C
  • Room Temp. 22° C
  • TEC 2,3,4,7 or any other vaporizer can be used 
  • Highest vapor pressure
  • TEC 6 vaporizer is used  

Color coding

    Red

  Purple

  Yellow

   Blue

MAC50

    0.75

  1.12

    2

   6

PHARMACOKINETICS AND PHARMACODYNAMICS

Important Information

  • MAC: Minimal Alveolar concentration of the vapor / anesthetic agent to prevent movement (Motor Response) in 50% of subject in response to surgical stimulus.
    • ↑↑ MAC : Potency ↓↓
    • ↓↓ MAC : Potency ↑↑

Blood gas partition coefficient or blood gas solubility

HalothaneIsofluraneSevofluraneDesflurane
Blood gas partition coefficient2.251.30.630.42
Fastest speed of induction and Recovery
  • Blood gas partition coefficient tells about the
    • Speed of Induction
    • Speed of Recovery
  • Low blood gas partition coefficient: Faster speed of induction and recovery (Vice Versa).

Important Information

  • For induction we seldom use desflurane because of its irritant property: Causes Bronchospasm and Laryngospasm.
  • Sevoflurane is inhalational induction agent of choice, has sweet smell
  • Sevoflurane and Desflurane: Both good for day care surgery, since they give fast recovery.

Stability

Halothane

Isoflurane

Sevoflurane

Desflurane

  • Most unstable
  • Most metabolized
  • Can cause autoimmune hepatitis
  • Preservative Needed: Thymol (0.01%)
  • Stable
  • Stable
  • Most stable
  • Very good
  • Agent for the maintenance 

Smell of Agents

Halothane

Isoflurane

Sevoflurane

Desflurane

  • Fruity smell
  • Used both for induction & maintenance 
  • Little bit irritant 
  • Only used for maintenance 
  • Sweet smell
  • Induction & maintenance
  • Inhalational induction agent of choice
  • Irritant (max)
  • Maintenance 
  • For maintenance isoflurane > sevoflurane

PHARMACODYNAMIC PROPERTIES

CNS Effects

Halothane

Isoflurane

Sevoflurane

Desflurane

  • ↓ cerebral metabolic O2
  • ↓ Cerebral metabolic O2
  • ↓ Cerebral metabolic O2
  • ↓ Cerebral metabolic O2
  • CBF increase (maximum)
  • ↑↑↑ ICP maximum
  • CBF increase ↑ ICP
  • CBF increase ↑ ICP
  • CBF increase ↑ ICP
  • ↓ EEG 
  • ↓ EEG
  • ↓ EEG
  • ↓ EEG
  • Important Information
    • There is cerebral metabolic O2 requirement in all.
      • Inhalational agent are uncouplers of brain, they dilate the cerebral blood vessel: Cerebral Blood Flow (CBF) because of intrinsic vasodilation of cerebral blood vessel
      • In IV Anesthetic Agent it is opposite, Cerebral Metabolic O2:
        CBF.
  • All inhalational Agent cause ICP (intra cranial pressure).
    • Halothane not used for Neurosurgery, Rest of the inhalational agents can be used.
  • Best Agent of Neurosurgery: Desflurane 
  • 2nd best agent for Neurosurgery: Isoflurane

Effects on CVS

Halothane

Isoflurane

Sevoflurane

Desflurane

  • Direct Myocardial Depressant 
  • HR
  • CO
  • BP
  • Sensitize Heart to the Arrhythmogenic effect of catecholamines.
  • Contraindicated  for CVS surgery
  • Cardio stable
  • Systemic Vascular Resistance
  • For neurosurgery: Isoflurane > Sevoflurane 
  • Cause the Coronary steel phenomenon
   
  • All 3 can be used for CVS surgery

Important Information

  • Least cardio depressant: Desflurane > sevoflurane > isoflurane.
  • Best agent for CVS surgery: Desflurane.
  • Halothane not used for neurosurgery
  • Desflurane is best agent for neurosurgery    
  • Agent most commonly used for CVS surgery: Isoflurane because desflurane is not commonly available.
  • Sevoflurane not used for prolonged hours.

Effects on Respiratory system

  • All of the inhalational agents are respiratory depressants.
  • Blunts hypoxic/ hypercapnic drive.
  • All are bronchodilators.
    • Best bronchodilator: Halothane 
  • Sevoflurane is also a very good bronchodilator, so mostly used in developed countries.

Effects on liver

Halothane

Isoflurane

Sevoflurane

Desflurane

  • Autoimmune hepatitis
  • Disrupts dual blood flow of liver
  • Bad for liver 
  • All 3 can be used for Hepatic surgery.
  • Contraindicated for liver surgery
    • Good for liver surgery. 
  • Best for liver transplant surgery.
 
  • Best for liver surgery.

Important Information

  • For liver surgery Desflurane > isoflurane.

Effects on kidney 

HalothaneIsofluraneSevofluraneDesflurane
No effectNo effectBioproduct of metabolism (Compound – A Nephrotoxic)No effect

Components of GA

HalothaneIsofluraneSevofluraneDesflurane
LOCYesYesYesYes
LORRYesYesYesYes
AmnesiaYesYesYesYes
Muscle Relaxation(membrane stabilizing effect)YesYesYesYes
AnalgesiaNoNoNoNo
Malignant hyperthermiaUnsafeUnsafeUnsafeUnsafe
  • Skeletal muscle relaxation: Desflurane>sevoflurane>isoflurane>halothane.
  • All Inhalational agents provide good muscle relaxation but none of them provide analgesia.
  • All of them can precipitate malignant hyperthermia

MALIGNANT HYPERTHERMIA

  • Inhalational agents predisposes to this condition, but IV agents are safe in it.
  • Pharmacogenetic Disease: AD form is expressed.

Drugs triggering 

1. SuccinylCholine 

  • All halogenated Inhalational Agent 

2. Potent inhalational

  • Lignocaine 

Mechanism 

  • When a person having gene receives these drugs it gets activated and it stimulates SR which causes massive outflow of calcium inside the cell activating CGMP pathway and this increases the metabolism of our body by 2-3 times.

Clinical features 

  • It presents with
    • Hypercarbia 
    • Tachycardia
    • Hyperthermia 
    • Increased BP
    • Increased HR
    • Arrhythmias 
  • All occur due to hypermetabolism and result in cell lysis, and further cause myoglobinuria, acidosis, renal failure, hyperkalemia.

Management 

  • Discontinue the triggering Agent. 
  • Intravenous Dantrolene
    • Central Muscle Relaxant.
    • Stops release of Ca2+
    • Side Effects- Respiratory insufficiency and muscle weakness.
  • Symptomatic Management
  • Anesthesia safe in Malignant Hyperthermia: TIVA (Total Intravenous Anesthesia) 
    • Propofol: Agent of choice.

CARRIER GAS

N2OXenon
MAC: 104, least potentMAC: 70, more potent than N2O
Blood gas solubility: 0.45Blood gas solubility: 0.11-0.19 (fastest)
CVS unstable sympathetic stimulationCVS stable
Not metabolically inert
Peripheral neuropathy
Megaloblastic anemia 
Bone marrow depression
Metabolically inert
Environmental pollutantEnvironment friendly
-Expensive, not in clinical use

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