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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

1

1

2

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 ?