Sadaqat Ali
 Definition
 How local anesthetic work
 Moa
 Classification
 Pharmacokinetics
 Clinical uses
 Lidocaine
 Diylocini...
DEFINITION:
Local anesthesia is defined as a loss
of sensation in a circumscribed area of the
body caused by depression of...
 Altering the basic potential of nerve membrane
 Altering the threshold
 Decreasing the rate of depolarization
 Prolon...
 Local anesthetics inhibit depolarization of the
nerve membrane by interfering with both Na+ and
K+ currents.
 The actio...
 Esters:
Cocaine, Procaine. Chloroprocaine , Tetracaine.
 Amides:
Lidocaine, Mepivacaine, Prilocaine, Articaine,
Popivac...
 Following injection into the area of nerve fibers to be
blocked, local anesthetics are absorbed into blood.
 Ester-link...
Absorption of local anesthetics is affected by
following factors:
– dosage,
– site of injection
– drug-tissue-binding and
...
 Analgesia
 Regional anesthesia
 Prevention and treatment of cardiac arrhythmias
 Prevention/management: increased int...
 CNS
Low doses: tremors and oral numbness,
with possible dizziness, confusion and
agitation (exception = cocaine)
Mod. do...
 Cardiovascular:
vasodilation (exception = cocaine)
- less often, myocardial depression
- ventricular contraction possibl...
 Hypersensitivity:
local dermatitis with some topical; rare
systemic allergic response with injected
esters (due to metab...
 Smooth Muscle
• Depress contractions in the intact bowel
• Relax vascular and bronchial smooth muscle
• May increase the...
 Cocaine, an ester of benzoic acid and
methylecognine, occurs in abundance in the
leaves of the coca shrub.
 Cocaine produces anesthesia by inhibiting
excitation of nerve endings or by blocking
conduction in peripheral nerves. Th...
 This is a result of its blockade of norepinephrine
reuptake in the autonomic nervous system.
Cocaine binds differentiall...
 PHARMACOKNIETICS
 Absorption
Cocaine is absorbed from all sites of application,
including mucous membranes and gastroin...
 Indication
For the introduction of local (topical) anesthesia of
accessible mucous membranes of the oral,
laryngeal and ...
 A local anesthetic and cardiac depressant used as
an anti arrhythmia agent.
 Its actions are more intense and its effec...
 Mechanism of action
Lidocaine stabilizes the neuronal membrane by
inhibiting the ionic fluxes required for the initiatio...
 With sufficient blockage the membrane of the
postsynaptic neuron will not depolarize and will
thus fail to transmit an a...
 Absorption
information derived from diverse formulations,
concentrations and usages reveals that lidocaine
is completely...
 Route of elimination
Lidocaine and its metabolites are excreted by the
kidneys.
 Half life
109 minutes
 Toxicity
convu...
 Indication
For production of local or regional anesthesia by
infiltration techniques such as
percutaneous injection and
...
 Dyclonine is an oral anesthetic found in Sucrets,
an over the counter throat lozenge.
 It is also found in some varieti...
 Mechanism of action
Local anesthetics block both the initiation and
conduction of nerve impulses by decreasing the
neuro...
 Absorption
Readily absorbed through mucous membranes
into the systemic circulation.
 Half life
Approximately 30 to 60 m...
 Indication
Used to provide topical anesthesia of accessible mucous
membranes prior to examination, endoscopy or
instrume...
 Topical application:
Lidocaine (ointment)
 SC injections
 Topical application
Anesthesia of mucous membrane of nose, mouth
throat can be produced by direct application of salts o...
 It is the injection of local anesthetic directly into
the tissue without taking into consideration the
course of nerve
...
 Is produced by SC injection of a solution of LA in
order to anesthetize the region distal to the
injection.
Nerve block
...
 Nerve blocked
 Trigeminal nerve is blocked
 Anesthetic Cartridges + syringes
 Intervertibral space
 CSF withdrawal
 Injection procedure
 Goodman and Gilman’s the pharmacological
Basis of therapeutics 12th Edition Chapter no
20
 www.drugbank.com
 www.link....
Local anesthetics and techniques of anesthesia
Local anesthetics and techniques of anesthesia
Local anesthetics and techniques of anesthesia
Local anesthetics and techniques of anesthesia
Local anesthetics and techniques of anesthesia
Local anesthetics and techniques of anesthesia
Local anesthetics and techniques of anesthesia
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Local anesthetics and techniques of anesthesia

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Local anesthetics and techniques of anesthesia

  1. 1. Sadaqat Ali
  2. 2.  Definition  How local anesthetic work  Moa  Classification  Pharmacokinetics  Clinical uses  Lidocaine  Diylocinine  Spinal cord anesthesia
  3. 3. DEFINITION: Local anesthesia is defined as a loss of sensation in a circumscribed area of the body caused by depression of excitation in nerve endings or an inhibition of the conduction process in peripheral nerves LOSS OF SENSATION WITHOUT INDUCING LOSS OF CONSCIOUSNESS.
  4. 4.  Altering the basic potential of nerve membrane  Altering the threshold  Decreasing the rate of depolarization  Prolonging the rate of repolarization
  5. 5.  Local anesthetics inhibit depolarization of the nerve membrane by interfering with both Na+ and K+ currents.  The action potential is not propagated because the threshold level is never attained.  Local anesthetics act at the cell membrane to prevent the generation and the conduction of nerve impulses
  6. 6.  Esters: Cocaine, Procaine. Chloroprocaine , Tetracaine.  Amides: Lidocaine, Mepivacaine, Prilocaine, Articaine, Popivacaine, Etidocaine.  Ketones: Dyclonine.  Quinoline: Centbucridine
  7. 7.  Following injection into the area of nerve fibers to be blocked, local anesthetics are absorbed into blood.  Ester-linked local anesthetics are quickly hydrolyzed by butyrylcholinesterase in blood.  Amide-linked local anesthetics can be widely distributed via circulation. Amide- linked local anesthetics are hydrolyzed by liver microsomal enzymes.  Thus, half lifes of these drugs are significantly longer and toxicity is more likely to occur in patients with impaired liver function.
  8. 8. Absorption of local anesthetics is affected by following factors: – dosage, – site of injection – drug-tissue-binding and – Presence of vaso-constricting drugs
  9. 9.  Analgesia  Regional anesthesia  Prevention and treatment of cardiac arrhythmias  Prevention/management: increased intracranial pressure  Treatment of grand mal seizure
  10. 10.  CNS Low doses: tremors and oral numbness, with possible dizziness, confusion and agitation (exception = cocaine) Mod. doses: convulsions (immediately preceded by muscle twitching); prevented by injection of anti-convulsant High doses: possible respiratory depression
  11. 11.  Cardiovascular: vasodilation (exception = cocaine) - less often, myocardial depression - ventricular contraction possibly leading to reduced cardiac output, in the worst case, ventricular arrhythmias and cardiac arrest unintentional high plasma levels of LAs, but can occur with normal IV doses of bupivacaine
  12. 12.  Hypersensitivity: local dermatitis with some topical; rare systemic allergic response with injected esters (due to metabolite)
  13. 13.  Smooth Muscle • Depress contractions in the intact bowel • Relax vascular and bronchial smooth muscle • May increase the resting tone • Decrease the contractions of isolated human uterine muscle.
  14. 14.  Cocaine, an ester of benzoic acid and methylecognine, occurs in abundance in the leaves of the coca shrub.
  15. 15.  Cocaine produces anesthesia by inhibiting excitation of nerve endings or by blocking conduction in peripheral nerves. This is achieved by reversibly binding to and inactivating sodium channels. Sodium influx through these channels is necessary for the depolarization of nerve cell membranes and subsequent propagation of impulses along the course of the nerve. Cocaine is the only local anesthetic with vasoconstrictive properties.
  16. 16.  This is a result of its blockade of norepinephrine reuptake in the autonomic nervous system. Cocaine binds differentially to the dopamine, serotonin, and norepinephrine transport proteins and directly prevents the re-uptake of dopamine, serotonin, and norepinephrine into pre-synaptic neurons. Its effect on dopamine levels is most responsible for the addictive property of cocaine.
  17. 17.  PHARMACOKNIETICS  Absorption Cocaine is absorbed from all sites of application, including mucous membranes and gastrointestinal mucosa. By oral or intra-nasal route, 60 to 80% of cocaine is absorbed.  Metabolism Hepatic. Cocaine is metabolized to benzoylecgonine and ecgonine methyl ester, which are both excreted in the urine.
  18. 18.  Indication For the introduction of local (topical) anesthesia of accessible mucous membranes of the oral, laryngeal and nasal cavities.
  19. 19.  A local anesthetic and cardiac depressant used as an anti arrhythmia agent.  Its actions are more intense and its effects more prolonged than those of procaine.  its duration of action is shorter than that of bupivacaine or prilocaine.
  20. 20.  Mechanism of action Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action. Lidocaine alters signal conduction in neurons by blocking the fast voltage gated sodium (Na+) channels in the neuronal cell membrane that are responsible for signal propagation.
  21. 21.  With sufficient blockage the membrane of the postsynaptic neuron will not depolarize and will thus fail to transmit an action potential. This creates the anesthetic effect by not merely preventing pain signals from propagating to the brain but by aborting their birth in the first place.
  22. 22.  Absorption information derived from diverse formulations, concentrations and usages reveals that lidocaine is completely absorbed following parenteral administration, its rate of absorption depending, for example, upon various factors such as the site of administration and the presence or absence of a vasoconstrictor agent.  Metabolism Primarily hepatic.
  23. 23.  Route of elimination Lidocaine and its metabolites are excreted by the kidneys.  Half life 109 minutes  Toxicity convulsions, hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest
  24. 24.  Indication For production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks.
  25. 25.  Dyclonine is an oral anesthetic found in Sucrets, an over the counter throat lozenge.  It is also found in some varieties of the Cepacol sore throat spray.
  26. 26.  Mechanism of action Local anesthetics block both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions. This reversibly stabilizes the membrane and inhibits depolarization, resulting in the failure of a propagated action potential and subsequent conduction blockade.
  27. 27.  Absorption Readily absorbed through mucous membranes into the systemic circulation.  Half life Approximately 30 to 60 minutes.  Toxicity cardiovascular system depression, CNS toxicity, and methemoglobinemia
  28. 28.  Indication Used to provide topical anesthesia of accessible mucous membranes prior to examination, endoscopy or instrumentation, or other procedures involving the esophagus, larynx, mouth, pharynx or throat, respiratory tract or trachea, urinary tract, or vagina. Also used to suppress the gag reflex and/or other laryngeal and esophageal reflexes to facilitate dental examination or procedures (including oral surgery), endoscopy, or intubation. Also used for relief of canker sores, cold sores or fever blister.
  29. 29.  Topical application: Lidocaine (ointment)  SC injections
  30. 30.  Topical application Anesthesia of mucous membrane of nose, mouth throat can be produced by direct application of salts of many local anesthetics or by suspension of poorly soluble drugs like tetracain 2 % or lidocain2 %
  31. 31.  It is the injection of local anesthetic directly into the tissue without taking into consideration the course of nerve  Lidocain  Procain  Bupivacaine
  32. 32.  Is produced by SC injection of a solution of LA in order to anesthetize the region distal to the injection. Nerve block injection of a LA into or about individual peripheral nerve or peripheral plexuses.
  33. 33.  Nerve blocked  Trigeminal nerve is blocked  Anesthetic Cartridges + syringes
  34. 34.  Intervertibral space  CSF withdrawal  Injection procedure
  35. 35.  Goodman and Gilman’s the pharmacological Basis of therapeutics 12th Edition Chapter no 20  www.drugbank.com  www.link.springer.com
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