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LOCAL ANESTHETICS,IV SEDATION AND PAIN MANAGEMENT

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Title: LOCAL ANESTHETICS,IV SEDATION AND PAIN MANAGEMENT


1
LOCAL ANESTHETICS,IV SEDATION AND PAIN MANAGEMENT
  • MORAYA ALQAHTANI,MD

2
Local Anesthetichistory
  • Cocaine-1800
  • Niemann-1859
  • 1884-1st use in clinical practice
  • 1904-procaine
  • 1925-dibucaine
  • 1932-tetracaine
  • 1942-Licocaine
  • Mepivicaine,prilocaine,bupivicaine,etidocaine.
  • ropivicaine

3
neurophysiology
4
Nerve structure
5
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6
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7
pharmacokinetics
  • Weak bases
  • Lipid soluble
  • Pka8-9 at physiological pH
  • Lipophilic portion-hydrophilic portion
  • and intermediate link

8
pharmacokinetics
  • Degree of ionization.
  • Both are involved in the blockage of the nerve
  • They act by blocking Na channel
  • Duration of esters are shorter

9
pharmacokinetics
  • Vasoconstrictor activity at low doses
  • Vasodilatation at higher doses
  • MetabolismEsters by plasma cholinesterase ?PAMA
  • Amides metabolized in
    the liver

10
pharmacokinetics
  • Vasoconstrictor activity at low doses
  • Vasodilatation at higher doses
  • MetabolismEsters by plasma cholinesterase ?PAMA
  • Amides metabolized in
    the liver

11
pharmacokinetics
  • Clearanceamide mainly hepatic,
  • widely distributed compared to esters
  • More stable
  • Minimal allergic reaction

12
Pharmacological factors
  • Lipid solubility
  • Absorption and distribution
  • pharmacological factors
  • Physical factorsage,hepatic,renal,inflammation

13
  • pharmacological factors
  • injection site
  • dosage
  • presence of epinephrine ,carbonation
  • protein binding
  • chemical properties

14
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15
Classification of LA
16
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17
LA
  • Preparation
  • - topical ointments,cream,lotion,spray
  • -Injection
  • EMLAEutotic Mixture of Local Anesthetics
  • 2.5 prilocaine
  • 2.5 lidocaine

18
TOXICITY
19
Toxicity
  • Allergic reaction
  • Local toxicity
  • Systemic toxicity

20
Allergic reaction
  • Rare condused with adverse effects
  • More with esters-PABA
  • Delayed type
  • No cross sensitivity
  • prevention proper Hx PE
  • skin test- 20-30
    false positive

21
Local toxicity
  • Direct trauma
  • Intraneuronal injection
  • Rare
  • preventable

22
Systemic toxicity
  • CNS
  • CVS
  • Methemoglobinemia

23
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24
CVS
  • Conduction
  • Contractility
  • Peripheral effect
  • CVS more resistant than CNS
  • Bupivicaine more cardiac toxicity
  • Ropivicaine less cardiac toxicity
  • Lidocaine anti arrhythmic drug

25
CNS
  • Concentration dependant
  • Low concentration
  • CNSincreases with hypoxia,acidosis ,pregnancy
  • Adverse effect
  • drowsiness,light headiness
  • slurred speech,restlessness,
  • vertigo,tinnitus, muscle twitching,
  • tremors,convulsion, coma,

26
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27
  • IV Sedation

28
Practical consideration
  • Quite environment
  • Repeated cuff blood pressure measurement should
    be avoided
  • Monitors should be muted apart from alarm.

29
Requirements of analgesia
  • 1.Continuous IV access.
  • 2.Continuous monitoring with both ECG and pulse
    oximeter.
  • 3.Both the practitioner and the assistant should
    have recently certified in CPR.
  • 4.Resuscitation equipments should be available
    (crash cart).
  • 5.Possibility to transfer for full critical care
    facilities e.g. Other hospital, ICU, OR.

30
Steps to Sedoanalgesia
  • 1.Premedication with BDZ
  • 2.Adequate local or regional anesthesia
  • 3.IV sedation e.g. Midazolam
  • 4.Adjuvant analgesia with narcotics only if
    local/regional anesthetic is ineffective.

31
IV Anesthetics
  • Neuroleptanesthesia
  • Neuroleptic drugs   
  • Phenothiazines e.g.
    Chlorpromazine.
  • Butyrophenones e.g. Haloperidol,
    Droperidol.
  • Rarely used in anesthesia because of hypotension
  • droperidol fentanyl (Innovar )

32
IV Anesthetics
  • Butyrophenones result in significant
  •          Sedation.
  •          Tranquility.
  •          Immobility
  • Antiemesis

33
IV Anesthetics
  • Their side effects include
  •    An extrapyramidal syndrome with
    face and neck
    dyskinesia.
  •    Oculogyric crises.
  •    Torticollis.
  •    Agitation
  • Hallucination

34
IV Anesthetics
  • Droperidol (like other Butyrophenones) affect
    GABA receptors and alters the balance of dopamine
    and acetylcholine in certain brain sites.
  •  Neuroleptanesthesia is contraindicated in
    patients receiving Mono Amine Oxidase Inhibitors,
    abusing drugs or alcohol and those with
    Parkinsons disease.

35
Benzodiazepines
  • Diazepam (valium) 1959
  • Lorazepam (ativan) 1971
  • Midazolam (versed) 1976

36
pharmacokinetics
  • Small molecule
  • Lipid soluble
  • Metabolized in the liver
  • Habitual use of alcohol
  • Lorazepam has higher
  • affinity to receptors

37
Benzodiazepines
  • Action mediated through GABA
  • Mainly on CNS ,minimal action on PNS
  • Cells become hyperpolarized resistant to
    exitation
  • Function is blood level dependant
  • 20 anxiolytic
  • 30-50 sedation
  • 60 loss of consciousness
  • Tolerance

38
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39
Benzodiazepines
  • Hypnotic
  • Sedative
  • Anxiolytic
  • Amnestic
  • Anticonvulsantincreases seizure threshold
  • Muscle relaxant

40
Benzodiazepines
  • Uses Sedation,Induction,maintainance
  • Contraindication
  •      Hypersensitivity, myasthenia gravis, COPD,
    acute narrow angle glaucoma.
  • Safety has not been established in children and
    pregnant females

41
Benzodiazepines
  • Side effects
  • high safety margin
  • free allergic reaction
  • inactive non toxic metabolite
  • respiratory problem
  • venous irritation,thrombophlebitis
  • unpredictable interval of amnesia
  • Rx  Flumazenil (Anexate) 0.2 mg IV over 15 sec.
    Then 0.1mg IV q60 sec. To effect (max. 1mg).

42
Benzodiazepines
  • Dosage
  • midazolam
  •  IM 0.07 mg/kg (5mg) 30 60 min.prior (50 of
    dose if gt60 years)
  •         I.V. sedation titrate with small doses
    (2mg initial followed by 1mg q2 min to effect)
    (max.dose 0.1mg/kg) (reduce dose by 30 if
    premedicated and by 50 if gt60yo).

43
  • Diazepam (Valium ) IM/PO premedication 5-10
    mg. 1 to 2 h prior (reduce dose by 50 if gt60yo).
  •         IV sedation 5 - 10 mg IV q3h. (Reduce by
    50 if gt60yo).
  • Lorazepam (ativan)
  • PO/SL premedication 50mcg/kg
    (maximum 4mg) 1-2 hour prior (50 of dose if more
    than 60 yo)

44
  • OPOIDS

45
Classification
  • Natural
  • Semisynthetics
  • synthetics

46
Natural opoids
  • Morphine
  • Codeine
  • Papaverine
  • Semisynthetic
  • Heroin -dihydromorphone

47
Synthetic opoids
  • Levorphenols
  • -Methadone
  • -pentazocine
  • Phenypiperidine
  • -meperidine
  • -fentanyl

48
opoids
  • Inhibit the action of opoid neurotransmitters
  • Analgesic effect differences
  • -access to the receptor
  • -binding affinity
  • -lipophility,ionization
  • -distribution,clearance

49
OPOIDS
  • In general most of them
  • respiratory depression
  • bradycardia except demerol
  • anti tussive
  • sleep
  • nausea,vomiting,constipation
  • hypersensitivity
  • Overdose naloxone 0.4 mg IV q 2min

50
opoids
  • Morphine
  • Pharmacology Onset of action 2 to 5 min.
  • Duration of
    action 4-5 hrs.
  • IndicationAnalgesia, induction of anesthesia.
  • Contraindication
  • Hypersensitivity, MAO inhibitors within 14 days
    (hpertensive crises, tachyarrethmias).
  •  Dosage 0.1-0.2 mg/kg IV/IM/SC q3h.

51
opoids
  • Hydromorphone
  • -7-8 times stronger than morphine
  • -rapid distribution
  • -good in renal failure patient
  • -dose2-4 mg po

52
Demerol
  • Pharmacology Onset of action 2 to 5 min. via IV


    duration of action 2-4 hrs.
  •  absorbed slowly
  •  7 to 10 times less potent than morphine
  • 60 bound to protien 
  • Dosageup to 1.8 mg/kg IM/SC/IV q2h.

53
Fentanyl
  • Demorol family -100x morphine
  • High lipid solubility
  • Metabolized in the liver , excreted by bile or
    kidney
  • Poor hypnotic and sedative activity at low doses
  • No histamine release

54
katamine
  • Cataleptic, analgesic, and dissociative
    anesthetic agent.
  • Onset of action 30 sec. For IV ,12-25 min for IM
    dosing. 
  • Dosageinduction 2.0 mg/kg IV over 60 sec or 10
    mg/kg IM (adults and children).
  • Maintenance of anesthesia 50 of induction dose
    IV or IM, as anesthesia is lost.

55
katamine
  • ContraindicationHypersensitivity,
    pregnancy,uncontrolled HTN
  • Adverse effectHR,BP,RR, pleasant dreams 5,
    unpleasant dreams 2, hallucinations 1,
    confusion 3 (give BDZ with it to prevent bad
    trips).

56
Other IV anestheticspropofol
  • Most resent 1977
  • High lipid solubility
  • Alkylphenols
  • Viscous milky white substance
  • 1 of propofol
  • 1soy bean oil
  • 2.25 glycerol
  • 1.2 pure egg

57
Propofol
  • Metabolized in the liver
  • Iactive metabolite ,98 protein bound
  • Hypnotic,analgesic,induction
  • Titratable level of sedation
  • Dose sedation 10-50 micgm/kg/min
  • induction 0.1-1 mg/kg over 3 min
  • Side effectsrespiratory depression

58
PAIN MANAGEMENT
59
  • Definition
  • Effect of pain
  • -Neuroendocrine system
  • -CVS
  • -Resp
  • -GIT
  • -GUT
  • -immunity

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61
NSAIDs
  • Limited use for acute PO pain
  • Mechanism of action
  • Prostaglandins -?fever ,pain,vasodilatation

62
Classification
63
Mechanism of action
64
pharmacokinetics
  • Rapidly absorped
  • Metabolized in the liver,inactive metabolites
  • High protein bound
  • Action dose dependent

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66
Side effects
  • Gastropathy
  • Hemostasis
  • nephrotoxocity

67
Ketorolactromethaminne(Toradol)
  • Pyrolle acetic acid
  • High analgesic potency
  • 2mg of toradol 1mg og morphine 6-10mg of
    demerol
  • Dose 60mg IM followed by 30 mg IM q 6h
  • 50 in renal problem

68
Toradol
  • Most sufficient for sever pain
  • 0.3 incidence of PU
  • Bleeding with long term use
  • Increases bleeding time

69
Nausea and Vomiting
  • History of PO emesis
  • Female
  • Obesity
  • Pain
  • Type of surgery
  • Anesthetic drugs
  • Gastric distension

70
Treatment
  • Prophylactic antiemetic droperidol 10 to 20
    micgm/kg
  • Ondansetron 4 to 8 mg IV
  • Metoclopramide (10 to 20 mg IV)
  • Transdermal scopolamine
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