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Anesthetics
   Priestly discovered first inhalation anesthetic nitrous oxide
•   Loss of sensation
•   Insensibility to the vital organs
•   Loss of consciousness is reversible
•   Temporary insensibility to pain or feeling in the body

Characteristics of anesthetic agent

•   Should give enough relaxation time
•   Inert, potent, non-flammable, non-irritating
•   Should not have toxic effect
•   Stable to light and heat
•   Economical
•   Analgesic action and muscle relaxation
•   Should not induce vomiting
•   Should not reduce blood pressure
•   Should not have any adverse effect with the administration of other drugs.
.




Classification of anesthetics
  1. General anesthetics
  2. Local anesthetics




General anesthetics are further classified into
  a. Volatile general anesthetics
  b. Non-volatile anesthetics
Some of Volatile general anesthetics

Ether

• Anesthetic ether is 96-98% diethyl ether
• Colourless volatile liquid with pungent smell
• Soluble in organic solvents like alcohol, chloroform, etc.
• Prepared by williamson’s synthesis
• Stored in well-closed, light resistant bottles
• Inflammable.
• When exposed in air it forms peroxides or acetic
  aldehydes
• Stabilizers like sodium pyrogallate are added
• Stored in internally copper plated containers.
Advantages                             .




•   Induces surgical anesthetics without pre- anesthetics medication
•   Safe
•   Produces muscular relaxation
•   Does not modify blood pressure
•   Economical and stable
•   Administered without a complicated process



Disadvantages

•   Induction is slow
•   Boils at low temperature
•   Inflammable
•   Vapours are irritating to mucous membrane
•   Nausea and vomiting appear
•   Slow recovery
•   Ether convulsions may occur in children
Derivatives of ether were found to be less irritating than
                                    .



  ether

Methyl-n-propyl ether
• Powerful than ethyl ether
• Less adverse side effects
Vinyl ether
• Colourless liquid
• Miscible with alcohol, ether and chloroform
• Stored in well closed container
• Stored in cool, dark place
Advantages
• More potent
• Speedy recovery
• Useful in Dental procedures
• Used in minor operations for short duration
Disadvantages
• Damages liver
• Inflammable
Chloroform
                               .




• Powerful volatile liquid
• Prepared from bleaching powder and ethyl alcohol
• Colourless volatile liquid
• 1-2% of ethanol is added to prevent the formation of
  poisonous phosgene gas
• Should be protected from light
Advantages
• Induction is prompt
• Vapours are not flammable
• Used in obstetrical anesthetics
Disadvantages
• Toxic
• Liver and cardiac toxicity
• Due to its toxicity chloroform is no longer used
.




Halothane


• Fluorinated volatile liquid
• Structure similar to chloroform
• Heavy colourless liquid
• Non-flammable
• Sweet fruity odour
• Miscible with chloroform, ether, etc.
• Stored in air tight containers at low temperature
• Should be protected from light
• Stable in presence of alkalis
Advantages                               .




•   Not flammable
•   Does not irritate the respiratory passage
•   Nice pleasant odour
•   Potent anesthetics
•   Post operative vomiting is low
•   Relaxes bronchial muscle
•   Safe
•   Used as anesthetic during plastic surgery

Disadvantages
•   Causes cardiovascular depression
•   Depresses respiration
•   Poor analgesic
•   Expensive
•   Has to be given through a special apparatus
•   Hepatic damage
•   Used for intro-abdominal operation
Trichloroethylene
                                            .


•   Colourless
•   Characteristic odour
•   Thymol is added as preservative
•   Immiscible in water
•   Miscible with alcohol, chloroform, ether, etc
•   Stored in air tight and light resistant containers
•   Kept in cool places

Advantages
• Potent
• Rapid onset of action
• Recommended for short procedures such as dental extractions, etc.
• Used for migraine pain, angina pectoris and child birth

Disadvantages
• Poor muscular relaxation
• May be hepatotoxic and tachypnoea
• Breaks down in the presence of soda lime to give highly toxic products
.




                         Ethyl chloride
• Non- irritating
• Highly volatile
• Inflammable
• At ordinary temperature and pressure it is a gas
• Pleasant characteristic odour
• Miscible with organic solvents like alcohol and ether
• Slightly miscible in water
• Stored in air tight containers
• When sprayed on skin it evaporates rapidly and cools the skin
.




Advantages
• Used as local anesthetic for minor operations such as incision, etc
• As general anesthetic it induces anesthetic within 1 or 2 minutes
• Quick induction




Disadvantages
• May damage liver
• Induce cardiac arrhythmias or cardiac arrest
• Poor muscle relaxation
• Low safety
• Difficult to maintain steady depth of anesthetic
.


                                  Nitrous oxide
•   Colourless inorganic, non-irritating
•   Sweet taste
•   Non-flammable
•   Available in steel cylinders
•   Known as laughing gas

Advantages
• Safest anesthetic
• Non-flammable
• Non-irritating
• Rapid induction nad rapid recovery
• Pronounced analgesic action
• Does not induce post-operative nausea and vomiting
• Used in painful procedures like cleaning and changing burn wounds

Disadvantages
• Not potent anesthetic
• Pre-anesthetic medication has to be given
• Produce violent excitation
• Hypoxia
• Increases cardiac irregularities
.




                           Cyclopropane
• Colorless sweet smelling gas
• Available in metal cylinders in compressed form
• Kept in cool place

Advantages
• Potent anesthetic
•   Has fast induction
•   Rapid and smooth recovery
•   Maintains blood pressure and cardiac contracitility
•   Used in hemorrhagic agent
•   Does not produce irritation of respiratory passage
•   Good muscle relaxant
•   Produces quite breathing
•   Supplies enough oxygen
•   Does not produce visceral damage
.




Disadvantages
•   Induction is done carefully
•   Produce cardiac irregularities
•   Depresses respiratory center
•   Increases capillary oozing
•   Anesthetic mixture of cyclopropane and oxygen is explosive
Non-volatile anesthetics
Thiopental sodium

•   Yellowish white hygroscopic powder
•   Characteristic odour and bitter taste
•   Soluble in water
•   Solution is freshly prepared before using it in injection form
•   Stored in sealed containers
•   It is a derivative of barbituric acid and malonic ester
•   Patient passes through the stages of hypnosis and deep sleep to
    anesthesia
•   First consciousness is lost and then reflex activity and finally
    medullary centres are lost.
•   Used in minor operations such as fracture, dental surgerics, etc
•   Anti-convulsant
.




Advantages
• Non-explosive
• Easy to administer
• Induction is rapid and without any unpleasant feeling
• Tendency of nausea and vomiting is very less
• Does not effect respiration
• No post-anesthetic complications

Disadvantages
•   Needs constant supervision to avoid overdostage
•   Depresses vasomotor centre and myocardium
•   Poor analgesic
•   Does not produce muscular relaxation
Local anesthetics

Characteristics of local anesthetics

•   Non-irritant
•   Should not be painful
•   Low toxicity
•   Stable
•   Should not damage nerve cells
•   Sterilization of drugs should be easy
•   Should not damage nerve cells
The Esters
Cocaine
•   It is alkaloid obtained from leaces of Erthroxylon Coca
•   It is methyl benzoyl ester of Ecgonine which is a tropane derivative
•   Basic in nature
•   Levorotatory
•   White Crystalline powder
•   Sparingly soluble in water
•   Hygroscopic in nature
Advantages
•   Useful in surgery of nose, throat and eye
•   Local anaesthtic action
•   Stimulates central nervous system
Disadvantages
•   Drug is addiction
•   Dilates pupil
•   Raises blood pressure
•   Produces euphoria and fatigue
•   Poisonous in nature
.




Benzocaine
•   Ester derivative
•   White crystalline powder
•   Stored in air tight containers
•   Light resistant containers
•   Soluble in water
•   Low toxicity
•   Available under the name anesthetic
•   Useful as dusting
•   Used in throat lozenges
•   Useful in relieving pain of gastric ulcer
•   Used in ointment form and is a surface anesthetic
The amides
Lignocaine


•   Crystalline solid
•   Sparingly soluble in water
•   Used as hydrochloric salt
•   Very stable
•   Stored in room temperature
•   Resistance to hydrolysis
•   Used topically as surface anesthetic and ointment
•   Available in injection form as spinal nerve block injections
•   Quick onset of action
•   Good analgesic agent
•   Used for dental analgesia
•   Used in cardiac arrhythmias
•   Used for patients who are allergic to procaine
•   Toxicity is similar to that of other local anesthetics
•   May cause drowsiness

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Anesthetics

  • 1. Anesthetics  Priestly discovered first inhalation anesthetic nitrous oxide • Loss of sensation • Insensibility to the vital organs • Loss of consciousness is reversible • Temporary insensibility to pain or feeling in the body Characteristics of anesthetic agent • Should give enough relaxation time • Inert, potent, non-flammable, non-irritating • Should not have toxic effect • Stable to light and heat • Economical • Analgesic action and muscle relaxation • Should not induce vomiting • Should not reduce blood pressure • Should not have any adverse effect with the administration of other drugs.
  • 2. . Classification of anesthetics 1. General anesthetics 2. Local anesthetics General anesthetics are further classified into a. Volatile general anesthetics b. Non-volatile anesthetics
  • 3. Some of Volatile general anesthetics Ether • Anesthetic ether is 96-98% diethyl ether • Colourless volatile liquid with pungent smell • Soluble in organic solvents like alcohol, chloroform, etc. • Prepared by williamson’s synthesis • Stored in well-closed, light resistant bottles • Inflammable. • When exposed in air it forms peroxides or acetic aldehydes • Stabilizers like sodium pyrogallate are added • Stored in internally copper plated containers.
  • 4. Advantages . • Induces surgical anesthetics without pre- anesthetics medication • Safe • Produces muscular relaxation • Does not modify blood pressure • Economical and stable • Administered without a complicated process Disadvantages • Induction is slow • Boils at low temperature • Inflammable • Vapours are irritating to mucous membrane • Nausea and vomiting appear • Slow recovery • Ether convulsions may occur in children
  • 5. Derivatives of ether were found to be less irritating than . ether Methyl-n-propyl ether • Powerful than ethyl ether • Less adverse side effects Vinyl ether • Colourless liquid • Miscible with alcohol, ether and chloroform • Stored in well closed container • Stored in cool, dark place Advantages • More potent • Speedy recovery • Useful in Dental procedures • Used in minor operations for short duration Disadvantages • Damages liver • Inflammable
  • 6. Chloroform . • Powerful volatile liquid • Prepared from bleaching powder and ethyl alcohol • Colourless volatile liquid • 1-2% of ethanol is added to prevent the formation of poisonous phosgene gas • Should be protected from light Advantages • Induction is prompt • Vapours are not flammable • Used in obstetrical anesthetics Disadvantages • Toxic • Liver and cardiac toxicity • Due to its toxicity chloroform is no longer used
  • 7. . Halothane • Fluorinated volatile liquid • Structure similar to chloroform • Heavy colourless liquid • Non-flammable • Sweet fruity odour • Miscible with chloroform, ether, etc. • Stored in air tight containers at low temperature • Should be protected from light • Stable in presence of alkalis
  • 8. Advantages . • Not flammable • Does not irritate the respiratory passage • Nice pleasant odour • Potent anesthetics • Post operative vomiting is low • Relaxes bronchial muscle • Safe • Used as anesthetic during plastic surgery Disadvantages • Causes cardiovascular depression • Depresses respiration • Poor analgesic • Expensive • Has to be given through a special apparatus • Hepatic damage • Used for intro-abdominal operation
  • 9. Trichloroethylene . • Colourless • Characteristic odour • Thymol is added as preservative • Immiscible in water • Miscible with alcohol, chloroform, ether, etc • Stored in air tight and light resistant containers • Kept in cool places Advantages • Potent • Rapid onset of action • Recommended for short procedures such as dental extractions, etc. • Used for migraine pain, angina pectoris and child birth Disadvantages • Poor muscular relaxation • May be hepatotoxic and tachypnoea • Breaks down in the presence of soda lime to give highly toxic products
  • 10. . Ethyl chloride • Non- irritating • Highly volatile • Inflammable • At ordinary temperature and pressure it is a gas • Pleasant characteristic odour • Miscible with organic solvents like alcohol and ether • Slightly miscible in water • Stored in air tight containers • When sprayed on skin it evaporates rapidly and cools the skin
  • 11. . Advantages • Used as local anesthetic for minor operations such as incision, etc • As general anesthetic it induces anesthetic within 1 or 2 minutes • Quick induction Disadvantages • May damage liver • Induce cardiac arrhythmias or cardiac arrest • Poor muscle relaxation • Low safety • Difficult to maintain steady depth of anesthetic
  • 12. . Nitrous oxide • Colourless inorganic, non-irritating • Sweet taste • Non-flammable • Available in steel cylinders • Known as laughing gas Advantages • Safest anesthetic • Non-flammable • Non-irritating • Rapid induction nad rapid recovery • Pronounced analgesic action • Does not induce post-operative nausea and vomiting • Used in painful procedures like cleaning and changing burn wounds Disadvantages • Not potent anesthetic • Pre-anesthetic medication has to be given • Produce violent excitation • Hypoxia • Increases cardiac irregularities
  • 13. . Cyclopropane • Colorless sweet smelling gas • Available in metal cylinders in compressed form • Kept in cool place Advantages • Potent anesthetic • Has fast induction • Rapid and smooth recovery • Maintains blood pressure and cardiac contracitility • Used in hemorrhagic agent • Does not produce irritation of respiratory passage • Good muscle relaxant • Produces quite breathing • Supplies enough oxygen • Does not produce visceral damage
  • 14. . Disadvantages • Induction is done carefully • Produce cardiac irregularities • Depresses respiratory center • Increases capillary oozing • Anesthetic mixture of cyclopropane and oxygen is explosive
  • 15. Non-volatile anesthetics Thiopental sodium • Yellowish white hygroscopic powder • Characteristic odour and bitter taste • Soluble in water • Solution is freshly prepared before using it in injection form • Stored in sealed containers • It is a derivative of barbituric acid and malonic ester • Patient passes through the stages of hypnosis and deep sleep to anesthesia • First consciousness is lost and then reflex activity and finally medullary centres are lost. • Used in minor operations such as fracture, dental surgerics, etc • Anti-convulsant
  • 16. . Advantages • Non-explosive • Easy to administer • Induction is rapid and without any unpleasant feeling • Tendency of nausea and vomiting is very less • Does not effect respiration • No post-anesthetic complications Disadvantages • Needs constant supervision to avoid overdostage • Depresses vasomotor centre and myocardium • Poor analgesic • Does not produce muscular relaxation
  • 17. Local anesthetics Characteristics of local anesthetics • Non-irritant • Should not be painful • Low toxicity • Stable • Should not damage nerve cells • Sterilization of drugs should be easy • Should not damage nerve cells
  • 18. The Esters Cocaine • It is alkaloid obtained from leaces of Erthroxylon Coca • It is methyl benzoyl ester of Ecgonine which is a tropane derivative • Basic in nature • Levorotatory • White Crystalline powder • Sparingly soluble in water • Hygroscopic in nature Advantages • Useful in surgery of nose, throat and eye • Local anaesthtic action • Stimulates central nervous system Disadvantages • Drug is addiction • Dilates pupil • Raises blood pressure • Produces euphoria and fatigue • Poisonous in nature
  • 19. . Benzocaine • Ester derivative • White crystalline powder • Stored in air tight containers • Light resistant containers • Soluble in water • Low toxicity • Available under the name anesthetic • Useful as dusting • Used in throat lozenges • Useful in relieving pain of gastric ulcer • Used in ointment form and is a surface anesthetic
  • 20. The amides Lignocaine • Crystalline solid • Sparingly soluble in water • Used as hydrochloric salt • Very stable • Stored in room temperature • Resistance to hydrolysis • Used topically as surface anesthetic and ointment • Available in injection form as spinal nerve block injections • Quick onset of action • Good analgesic agent • Used for dental analgesia • Used in cardiac arrhythmias • Used for patients who are allergic to procaine • Toxicity is similar to that of other local anesthetics • May cause drowsiness