BASIC PHARMACOLOGY OF DRUGS

USED IN GENERAL ANAESTHESIA

Dr. M.V. Bhimeshwar

Professor of Anaesthesiology
SD Eye Hospital
Member of Governing Council ISA National

Drugs used in General Anaesthesia

- Pre-medication
- Pre oxygenation

- Induction
- Intubation

- Maintenance
- Reversal

- Recovery
- Post Op

Basic Principles of Pharmacology and Anaesthesia

Anaesthesia necessitates administration of drugs in such a manner to produce the
desired effect yet avoid undesired effect.

Therapeutic objective : Maintain adequate drug conc.

The Art of Anaesthesia

Pharmacokinetics : quantitative study of ADME of inhaled or injected drugs (what

body does to drugs)
Pharmakokinetics : Is the study of the intrinsic sensitivity of responsiveness of
reception to a drug (what the drug does in body)

Pharmacokinetics of injected drugs

Absorption
Ionization
Route of administration
Transport across membrane

Bioavailability
Protein binding
Blood flow

Metabolism :

Phase I (Functionalization)
Oxidation : Reduction : Hydrolysis
Phase II : Conjugation

Elimination
Renal Excretion

Hepatobiliary excretion
Pulmonary excretion

Pharmacodynamics and Injected drugs

What effect a drug has on the body
Receptors
1

H1

H2

Opioid receptors
Muscarenic receptors
Nicotinic receptors

Pharmakokinetics of Inhaled Anaesthetics

Absorption from alveoli to pulmonary capillary blood

Distribution in body
Elimination by lungs

PA

Pa

Site of Action Brain

Conc. Effect
2nd gas effect

PBr

Pharmacodynamics of inhaled anaesthetics

MAC

MECHANISM OF ACTION
Meyer Overton theory

Protein receptor hypothesis

Alteration in neuro transmitter
availability

Pre Medication Drugs

Anxiolytics

Analgesics
Anti emetics
Anticholinergic drugs
Drugs which the patient might be taking

Anxiolytics
Benzodiazepines : Diazepam (long) : Midazolam (Short)
Lorazepam (Intermediate )
Effects :
Hypnotic
Sedative
Anxiolytic
Amnestic
Anti convulsant
Central muscle relaxation

 Brief History
Physiochemical characteristics
Metabolism
Pharmacokientics
Pharmacology : CVS ; CNS ; RS, skeletal muscle

Dose
Uses

Drug interaction
Comparative Pharmacology

BENZODIAZEPINES
Diazepam

Temazepam

Lorazepam

Triazolam

Midazolam

Chlorazepate

Oxazepam

Helozepam

Chlordiazepoxide

Prazepam

Clonazepam

(FLUMAZENIL)

Flurazepam

ANALGESICS

I.

Opioids

II. NSAIDS

CLASSIFICATION OF OPIOID AGONISTS AND ANTAGONISTS

Opioid Agonists

Opioid Agonists Antagonists

Morphine

Pentazocine

Meperidine

Butorophanol

Fentanyl

Nalbuphine

Sufentanyl

Buprenophine

Alfentanil

Nalophine

Phenoperidine

Dezocine

Codeine
Heroin

Opiod Antagonists
Naloxone
Naltrexone

Structure Actively relationship

Classification
Opioid receptors

Effects on various systems

Uses

Doses
Side effects
Drug interaction
Comparative Pharmacology

Non opioid and Non steroidal analgesics, Antipyretic and anti inflammatory
Drugs (NSAIDS)
1. Salicylates :

Aspirin & Salicylic acid

2. Phenylbutazone
3. Para aminophanol derivation : Phenacitin and acataminophen

4. Indomethacin
5. Propionic acid derivative : Ibuprofen, Naproxen ; Fevoprofen
6. Tolmetin

7. Zomapirac
8. Diflunisol
9. Gold
10. Colchicine
11. Allopurinol
12. Uricosuric drugs

probenacid
Sulfinpirzone

Gastric Antacids

Stimulants

Aluminum hydroxide

Metaclopramide

Calcium carbonate (MA syndrome)

Magnesium oxide
Sod. Bicarbonate
Particulate antacid

Non Particulate antacid

Anti Emetics
Droperidol
Domperidone
Benzquinamide
Tetrahydrocannabinol

Diphenidol
Ondensetron

Anticholinergic drugs

Competetively antagonisis the effects of Ach at muscarinic receptors (Heart

; Salivary glands ; smooth muscle)

Classification

Naturally occurring

Atropine

Scopalamine

Semi synthetic

Glycopyrollate

Structure activity relationship

Mechanism of action

Pharmacokinetics
Clinical uses
Central anticholinergic syndrome

Comparative pharmacology

Induction Agents

Intravenous

Barbiturates

Non Barbiturates

Inhalational

gases

volatile

Barbiturates
Physical characters
Structure activity relationship

Mechanism of action
Pharmacokinetics
Effects
Clinical uses
Side effects
Intra arterial injection
Comparative Pharmacology

Non Barbiturates I.V agents

Benzodiazepines
Opioids

Phencyclidine (Ketamine)

Imidazole (Ethomidate)

Isopropylphenol (Propofol)

Steroid ( Althesin )

Eugenol (propanidid )

Physical characteristics
Structure
Mechanism of action
Pharmacokinetics
Effects
Uses
Side effects
Comparative pharmacology

Inhalational
Gases
Inorganic

Organic

N2O

Un saturated

saturated

Xenon

Hydrocarbons

Hydrocarbon

Eg : Ethylene

Eg; Cycloprophyl

INHALATIONAL
Volatile liquids

Ethers

New Ethers

Halogens

Simple

Mixed

Chlroine

Fluorine

Diethyl

Ethyl vinyl

Chloroform

Halothane

Divinyl

Methyl propyl

Trilene

Methoxyflurane

Ethyl chloride
enflurane

Isoflurane
Sevoflurane
Desflurane

Comparative studies
Physical & Chemical properties
Effects on all systems
Metabolism
Side effects

Muscle Relaxants

(N-M Blocking drugs)

N-M Junction, History
Characteristic of Block
Depolarising

Non depolarising

Fasiculations

No fasiculations

Absence of fade

Fade present

Absence of PTP

PTP +

No need for reversal

Need for reversal

Classification
Depolarisers Succinyl choline
decamethonium
Non depolarizers Long acting dTC ; Metacurium, gallamine, Pancuronium

Intermedial acting Vecuronium, atracurium

Rocuronium, Rapacurium
Clinical Uses :

Structure activity relationship

Pharmacokinetics and Pharmacodynamics
Effects on systems
Side effects

Drug interaction / metabolism

Drug use in Adults, paediatric, pregnant patient
RSI, Primary principles

Diseases that alter muscle relaxant action

Myasthenia gravis
Myasthenic syndromes
Myotonia

Familial periodic paralysis

UMN and LMN disease
Burns

INTRA OPERATIVE PERIOD

Maintenance
O2, N2O + Inhalational agent
Muscle relaxant

Analgesics
Fluids : Crystalloids ; colloids, blood
Role of Monitoring

Reversal agents : Anticholinestrase drugs

Act by inhibiting the enzyme acetylcholinestarase

acetylcholinestrase
Ach ---------------------------> Choline + Acetic acid
Classification : Mechanism by which inhibition of acetyl cholinestrase
1. Reversible inhibition : Edrophonium

2. Formation of carbanyl esters : Physostigmin, Neostigmin, Pyridostymin

3. Irreversible inactivation : Organophosphorous, Ecothiophate, Parathion,

malathion.

Structure Activity Relationship

Pharmakokinetics

Pharmacological effect on all systems

Clinical uses
Over dosage, muscarinic and nicotinic symptoms
Drug interactions

Synthetic cholinergic agonists

Methacholine ; carbachol ; bethanacol

Cholinomimetic alkaloids

Pilocarpine ; muscarine ; arecoline

POST OPERATIVE PERIOD

Fluids
Pain
PONV

CONCLUSION
Pharmacology and Anaesthesia
In detail about each drug (uses ; side effects, drug
interaction)

Any Questions ?