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Local Anesthetic
history
Cocaine-1800
Niemann-1859
1884-1st use in clinical practice
1904-procaine
1925-dibucaine
1932-tetracaine
1942-Licocaine
Mepivicaine,prilocaine,bupivicaine,etidocaine.
ropivicaine
neurophysiology
Nerve structure
pharmacokinetics
Weak bases
Lipid soluble
Pka:8-9 at physiological pH
Lipophilic portion-hydrophilic portion
and intermediate link
pharmacokinetics
Degree of ionization.
Both are involved in the blockage of the nerve
They act by blocking Na channel
Duration of esters are shorter
pharmacokinetics
Vasoconstrictor activity at low doses
Vasodilatation at higher doses
Metabolism:Esters by plasma cholinesterase
PAMA
Amides metabolized in the liver
pharmacokinetics
Vasoconstrictor activity at low doses
Vasodilatation at higher doses
Metabolism:Esters by plasma cholinesterase
PAMA
Amides metabolized in the liver
pharmacokinetics
Clearance:amide mainly hepatic,
widely distributed compared to esters
More stable
Minimal allergic reaction
Pharmacological factors
Lipid solubility
Absorption and distribution:
pharmacological factors
Physical factors:age,hepatic,renal,inflammation
pharmacological factors
*injection site
*dosage
*presence of epinephrine ,carbonation
*protein binding
*chemical properties
Classification of LA
Short acting
Intermediate
acting
Long acting
Procaine
60-90 min
Chloroprocaine
30-60 min
Mepivicaine
Prilocaine
Lidocaine
Tetracaine
Bupivicaine
20-24
20-24
90-200
80-600
Etidocaine
DRUG
Maximum
Plain(mg)
Maximum
Epinephrine(mg)
Chloroprocaine
800
1000
Lidocaine
300
500
Mepivacaine
300
500
Prilocaine
500
600
Bupivacaine
175
225
Etidocaine
300
400
LA
Preparation:
- topical :ointments,cream,lotion,spray
-Injection
EMLA:Eutotic Mixture of Local Anesthetics
2.5% prilocaine
2.5% lidocaine
TOXICITY
Toxicity
Allergic reaction
Local toxicity
Systemic toxicity
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
Local toxicity
Direct trauma
Intraneuronal injection
Rare
preventable
Systemic toxicity
CNS
CVS
Methemoglobinemia
CVS
Conduction
Contractility
Peripheral effect
CNS
Concentration dependant
Low concentration
CNS:increases with hypoxia,acidosis ,pregnancy
Adverse effect:
drowsiness,light headiness
slurred speech,restlessness,
vertigo,tinnitus, muscle twitching,
tremors,convulsion, coma,
IV Sedation
Practical consideration
Quite environment
Repeated cuff blood pressure measurement should
be avoided
Monitors should be muted apart from alarm.
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.
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.
IV Anesthetics
Neuroleptanesthesia
Neuroleptic drugs :
Phenothiazines e.g. Chlorpromazine.
IV Anesthetics
Butyrophenones result in significant:
Sedation.
Tranquility.
Immobility
Antiemesis
IV Anesthetics
Their side effects include:
An extrapyramidal syndrome with
face and neck dyskinesia.
Oculogyric crises.
Torticollis.
Agitation
Hallucination
IV Anesthetics
Droperidol (like other Butyrophenones) affect
GABA receptors and alters the balance of
dopamine and acetylcholine in certain brain sites.
Benzodiazepines
Diazepam (valium)
1959
Lorazepam (ativan)
1971
Midazolam (versed)
1976
pharmacokinetics
Small molecule
Lipid soluble
Metabolized in the liver
Habitual use of alcohol
Lorazepam has higher
affinity to receptors
Benzodiazepines
Short acting
Midazolam
6-11ml/kg/min
Intermediate
acting
Lorazepam
0.8-1.8ml/kg/min
Long acting
Diazepam
0.2-0.5ml/kg/min
Benzodiazepines
Hypnotic
Sedative
Anxiolytic
Amnestic
Anticonvulsant:increases seizure threshold
Muscle relaxant
Benzodiazepines
Uses Sedation,Induction,maintainance
Contraindication:
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).
Benzodiazepines
Dosage:
midazolam:
IM 0.07 mg/kg (5mg) 30 60 min.prior (50% of
dose if >60 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 >60yo).
Lorazepam (ativan):
PO/SL premedication: 50mcg/kg (maximum
4mg) 1-2 hour prior (50% of dose if more than 60
yo)
OPOIDS
Classification
Natural
Semisynthetics
synthetics
Natural opoids
Morphine
Codeine
Papaverine
Semisynthetic
Heroin
-dihydromorphone
Synthetic opoids
Levorphenols:
-Methadone
-pentazocine
Phenypiperidine
-meperidine
-fentanyl
opoids
Inhibit the action of opoid neurotransmitters
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
opoids
Morphine:
Pharmacology: Onset of action 2 to 5 min.
Duration of action 4-5 hrs.
Indication:Analgesia, induction of anesthesia.
Contraindication:
Hypersensitivity, MAO inhibitors within 14 days
(hpertensive crises, tachyarrethmias).
Dosage: 0.1-0.2 mg/kg IV/IM/SC q3h.
opoids
Hydromorphone :
-7-8 times stronger than morphine
-rapid distribution
-good in renal failure patient
-dose:2-4 mg po
Demerol
Pharmacology: Onset of action 2 to 5 min. via IV
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
katamine
Cataleptic, analgesic, and dissociative anesthetic
agent.
Onset of action 30 sec. For IV ,12-25 min for IM
dosing.
Dosage:induction 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.
katamine
Contraindication:Hypersensitivity,
pregnancy,uncontrolled HTN
Other IV anesthetics
propofol
Propofol
PAIN MANAGEMENT
Definition
Effect of pain
-Neuroendocrine system
-CVS
-Resp
-GIT
-GUT
-immunity
NSAIDs
Limited use for acute PO pain
Mechanism of action
Classification
Mechanism of action
pharmacokinetics
Rapidly absorped
Metabolized in the liver,inactive metabolites
High protein bound
Action dose dependent
Side effects
Gastropathy
Hemostasis
nephrotoxocity
Ketorolactromethaminne
(Toradol)
Pyrolle acetic acid
High analgesic potency
Toradol
Most sufficient for sever pain
0.3% incidence of PU
Bleeding with long term use
Increases bleeding time
History of PO emesis
Female
Obesity
Pain
Type of surgery
Anesthetic drugs
Gastric distension
Treatment
Prophylactic antiemetic droperidol 10 to 20
micgm/kg
Ondansetron 4 to 8 mg IV
Metoclopramide (10 to 20 mg IV)
Transdermal scopolamine