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LOCAL ANESTHETIC & TOXICITY  Procaine, chloroprocaine, cocaine, tetracaine

→ Amino-amides
Local Anesthetic  Amide linkage
→ Reversible inhibition of sensory nerve impulse  Lidocaine, bupivacaine, ropivacaine,
conduction levobupivacaine
→ No loss of consciousness
→ Prevent transmission to CNS Mechanism of Action
+
→ Local anesthetic binds to receptor so Na cannot bind to → Prevent generation & conduction of nerve impulses by
+
it (Voltage gated Na channel) decreasing or preventing the large transient increase in
→ Also blocks synaptic transmission permeability of excitable membranes to Na
 Blocks calcium release → Agents of low anesthetic potency & short duration of
 Inhibits excitatory neurotransmitter action, that is, procaine & chloroprocaine
+
 Blocks Na ion channel → Agents of intermediate anesthetic potency & duration of
+ -
 Enhance K & Cl ion channel action that is lidocaine, mepivacaine & prilocaine
→ Agents of high anesthetic potency & prolonged duration
Clinical usefulness depends on of action that is tetracaine, bupivacaine, ropivacaine &
→ Inherent anesthetic property etidocaine
→ Rate of onset → In terms of onset, chloroprocaine, lidocaine,
→ Duration of effect (Action) mepivacaine, prilocaine & etidocaine possess a
 Which in turn depends on relatively rapid onset of action. Procaine & tetracaine
 Physiocochemical properties have a long latency period except when used for spinal
 Inherent vasodilator activity anesthesia, & bupivacaine is intermediate in terms of
onset of anesthesia
Physiocochemical Properties
→ Lipid solubility Local Anesthetic Toxicity
 Potency increases as a function of lipid → Systemic: CNS, CVS
solubility until a partitions coefficient of about 4 → Local: Neural & skeletal muscle irritation
 < Lipid solubility  < potency  > → Specific: Addiction, allergy, methemoglobinemia
concentration needed (Prilocaine)
→ Protein binding → Depend on blood level of local anesthesia delivered to
 Duration brain & heart
 > Protein binding at the site of action  > → Appropriate dose & technique rarely cause adverse
Duration of action reaction
→ pKa → Toxic level: Usually due to intravascular injection or
 Determine onset of anesthesia excess dose in extravascular administration
 Pka-ph at which ionized & non-ionized form
are present in equal amount Extravascular injection blood concentration depends in
 Uncharged form of the local anesthetic is → Absorption
responsible for diffusion across the nerve → Tissue redistribution
sheath & the membrane thus determine onset → Metabolism
of action → Excretion
 pH of tissue is 7.4: pKa above this, local
anesthetic in the base form, the slower the Factors that Effect Absorption
onset of action → Site of injection: More blood supply, greater absorption
→ Choice of drugs: Characteristics of the drug may effect
Vasodilator Properties absorption
→ All except cocaine exhibit a biphasic effect on vascular → Dosage
smooth muscle → Addition of epinephrine: Depends on sensitivity of the
→ Extreme low concentration vasoconstriction vessels at site of injection & local anesthesia itself
→ Concentration for regional anesthesia vasodilators (pharmacokinetic & metabolic property)

Non Pharmacologic Factors Influencing Anesthetic Activity CNS Toxicity: Related to intrinsic anesthetic potency
→ Dosage → Low dose
 Volume & concentration of drug  Excitatory
 Primary qualities of regional anesthesia  Mechanism: Selective blockade of inhibitory
(Onset, depth & duration) are related to mass pathway in cerebral cortex allowing facilitatory
of the drug (Volume x concentration) neurons to function unopposed
→ Addition of vasoconstrictor: Epinephrine  Subjective CNS symptoms
 Limits, prevents rapid absorption of local  Light headedness
anesthetic into circulation  Dizziness
 Dilution: 1:200,000  Visual & auditory disturbances:
 Prolongs duration of local anesthetic available difficulty in focusing & tinnitus
at the site  Disorientation
→ Site of injection  Drowsiness
 The difference in onset & duration is due to  Objective CNS signs
the particular anatomy of the area of injection,  Shivering
variation in the rate of vascular absorption &  Muscular twitching
amount of drug used  Tremors: Muscles of face & distal
 In spinal anesthesia, the lack of nerve sheath parts of extremities
around the spinal cord & deposition of local  Convulsions: Tonic, clonic
anesthesia near spinal cord are responsible → Large dose
for rapid onset  CNS depression
 In brachial plexus, local anesthetic has to  Mechanism: Inhibition of both inhibitory &
traverse thru nerve sheaths & connective facilitatory pathway
tissue thus have a slower onset  Sign: convulsion ceases, respiratory
→ Additives depression, arrest
 CO2 → Factors that effects CNS toxicity
-
 NaHCO3 : Increase pH near pka: more  Potency
ionized: Faster entry faster onset  Rate of injection
 KCI  Rate a particular blood level is attained
 Dextran → Effect of increase PCO2 on CNS toxicity
→ Mixtures of local anesthetic: The basis for using mixture  pCO2 level is inversely related to convulsive
of local anesthesia is to compensate for the short threshold
duration of action of certain local anesthesia & the long  Enhance cerebral blood flow so more local
latency of other agents anesthesia is delivered to the brain
 Decrease plasma protein binding of local
Clinically Useful Local Anesthetic anesthesia, more local anesthesia available to
→ Amino-esters the brain
 Ester link between aromatic & amine portion of → Effect of decrease arterial pH
molecule

Vascular vasoconstriction → Cardiac Effect  High dose: Inhibits myogenic activity leading  Dose dependent negative inotropic action: to vasodilation. bupivacaine has greater affinity to lipids of tissue making it not partial. except cocaine Depends on potency of local anesthesia  Coccaine: Initial effect is vasodilation followed +  Inhibit Na conductance in fast channels by vasoconstriction at low & high dose  High concentration of lidocaine. 324. so will non-pregnant have increase local anesthesia  Resuscitation more difficult with  Decrease plasma protein binding of local bupivacaine anesthesia: More free local anesthesia  Acidosis & hypoxia potentiate available cardiotoxicity of bupivacaine  Increase cationic form of local anesthesia: → Peripheral vascular effect Biphasic Decrease diffusion into cell  Low dose: Stimulates myogenic contraction & augments basal tone leading to CVS Toxicity: Cardiac. not with lidocaine: . complete AV readily available (Longer duration) dissociation  Overdose: Blocks firing of SA node Local Toxicity even leading into arrest → The more potent longer acting local anesthesia.09 >97% 150-375 mg bradycardia & sinus arrest Bupivacaine 2-3 mg/kg  Decrease AV node: **Epinephrine with L-bupivacaine has no greater effect. reversible nerve block of the anterior & posterior roots.operations in the lower half of the  Potential for CNS & CVS toxicity body:  Difference of Bupivacine to lidocaine toxicity  Lower extremities  Ratio of dosage required for  Perineum irreversible cardiovascular collapse  Lower abdomen & the dosage that will produce CNS  Upper abdomen toxicity (convulsion) lower for b. therefore no re-uptake  Increase LV EDP. cardiotoxic effect of bupivacaine that Cationic form will not diffuse out well. Treatment of premature ventricular hence CNS signs & symptoms preceed CV signs & contractions symptoms of depression  Increase dose Molecular pKa Protein Maximum dose (mg)  Prolongation of Weight binding conduction time. since L- Increase PR interval. Obstetrics Gynecology bupivacaine  Vaginal delivery  Ventricular arrhythmia & fatal  Caesarian section ventricular fibrillation with  Gynecology procedures bupivacaine.  Used in regional anesthesia sensory & motor functions  Good motor & sensory block → Not on the substance of the spinal cord  Less associated with tachyphylaxis: → Redistributed via vascular absorption metabolism does not produce → Indications metabolites like PABA (Allergenic) a. procaine &  Mechanism: Inhibitis the uptake of NE by tetracaine can block slow calcium channel tissue binding site. Surgery .9 65% 300 mg for IV PR interval & QRS 500 mg with epinephrine duration 2-4 mg/kg  Decrease pacemaker 7mg/kg w/ epinephrine activity in SA node: Sinus L. e.  Indirect effects of Lidocaine on CVS bupivacaine & etidocaine cause > degree of localized  Blocks sympathetic skeletal muscle damage than less potent shorter acting innervation agents like lidocaine & prilocaine  CNS-mediated → Reversible mechanisms → No clinical signs of local irritation  Direct effects +  Blocks Na channels.9 8. intrathecal when heart rate nerve block -.g. Causes  Unidirectional block & re. CAUDAL  Slow rate of recovery ANESTHESIA resulting incomplete restoration of V max Spinal Anesthesia between action potentials → Spinal Anesthesia (subarachnoid nerve block.  Arterial pH is directly related to convulsive Depress rapid phase of threshold depolarization  Decrease intracellular pH will increase  Pregnant patient more sensitive to conversion of base form of IA to cationic form. EPIDURAL ANESTHESIA. & entry type of arrhythmia posterior root ganglion leading to loss autonomic. increase Lidocaine 234 7. Specific conduction delay & QRS → Methhemoglobinemia: Prilocaine prolongation + ++  Mechanism: Degraded in the liver to otoluidine  Blocks K & Ca which cause oxidation of hemoglobin channels  Requires 600 mg of prilocaine to produce  Metabolites related to PABA clinical level of methhemoglobinemia (allergenic) are produced  Reversed with methylene blue  Bupivacaine → Allergy  Cause ventricular arrhythymia  Amino esters: Derivatives of para-amino-  Mechanism benzoic acid (Allergenic)  Depresses the rapid phase of depolarization (V max) SPINAL ANESTHESIA. direct pulmonary leading to increase free NE vasoconstrictive effect Relationship of Local Anesthesia Toxicity to Lidocaine Plasma  Lidocaine Concentration  Decrease maximum rate of → CVS depression: High concentration depolarization without altering → Respiratory depression: Higher concentration resting membrane potential → Coma  Action potential duration & effective → Convulsion refractory period decrease → Unconsciousness  Ratio of effective refractory period to → Muscular twitching action potential is increased in → Visual & auditory disturbances Purkinje Fibers & ventricular → Lightheadedness muscles → Numbness of tongue: Low concentration  Decreased firing of muscles: → CNS is more susceptible to the effect of local anesthetic.Results from the deposition of a local exceeds100/min anesthetic drug within the subarachnoid space.

areas that sits on the saddle i. lumbar & sacral segments. Increased intra abdominal pressure e. Speed of injection  Systemic diseases with v. Height of patient → Relative z. c. Nausea & vomiting: occurs in 25% of patients to the chest. Spinal Headache: CSF leakage  Decreased in obese patients intracranial pressure  Retract meninges (Big m. Absolute q. 12 margin (T6). thoracic segments together by several ligaments: T4-T12. qq. inject. lower thoracic. antisepsis & drape.  Hypoxia from respiratory inadequacy  Sitting position: less frequently  Parasympathetic hyperactivity used. 5 lumbar.5%-0. Spinal needle is introduced jj. Midspinal anesthesia: sensory loss at costal of 33 vertebrae: 7 cervical. Choose needle) interspace & raise a skin wheal of local ii. when the lateral → Delayed complications approach cannot be attained as hh. Children: Uncooperative. arthritis.  Septicemia: Bring organism into → Factors in determining levels of anesthesia the spine r. Asepsis. 5 sacral and segments. Hemiplegia/ Hematoma: Coagulopathy (identified by a feeling of a sudden click or ll. Ex. difficulty is encountered in the → Different types according to level of puncture median approach as in arthritic mm. Involved etc. supraspinous. Hemorrhoids & h. compression)  Duration of action 3-4 hours. aa. Volume with 7.2 → Contraindications hours. → Immediate complications of spinal anesthesia ligamentum flavum & (physiologic effects) longitudinal ligaments ee. Bupivacaine  Bleeding disorders (may bleed  relatively new long acting local into subarachnoid space  clot anesthetic that is currently used formation  spinal cord as 0. Backache anesthetic. L3 & L4.5% Dextrose Water tt. give sedation first bb. Extremely tense or psychotic patients episiotomy. vasoconstrictors th lumbar vertebrae or the interspace between 4  Bradycardia: Management: th & 5 lumbar vertebra: Tuffier’s Line Vagal blockers (Atropine SO4) k. or L4 & L5 IV fluids  The line joining the highest points of the iliac  Hypotension: Management: th crests crosses either the body of the 4 Fluid infusions. lumbar and sacral segments. Back problems due to muscle strain. Caudal epidural – solution deposited into  Administered as a 1.  The vertebral column consists cc. Hemorrhage → Levels of Spinal Anesthesia and the Dermatomes f. Thoracic epidural – thoracic spine vertebra. Approach: local anesthetic solution into the epidural space of the  Median: more common vertebral canal. lumbar & sacral thoracic. Painful diagnostic & therapeutic procedures  Onset of action is rapid. Circulatory: Cardiovascular changes are due nd  Spinal cord ends at the 2 to partial or total sympathetic blockade lumbar (L2) vertebra  Decrease total peripheral  Puncture sites: resistance (Vasodilation). Level of insertion of the catheter . Position paralysis  Lateral decubitus: knees flexed gg. Barbotage (Inject. 2 mins below the diaphragm & duration of action is 1½ . Respiratory diseases lumbar & sacral segments. Local anesthetic is injected. Height of the patient p. d. interspinous. Tetracaine: oo. → Epidural anesthesia is accomplished by injecting the n. Low spinal anesthesia: sensory block is at the → Anatomy level of the umbilicus (T10) & the lower j. withdraw.75%. General considerations thoracic.5% caudal canal through sacral hiatus solution mixed with 10% pp. Position of the patient neurologic sequelae w. Volume of solution: High volume may go high  Increased intracranial pressure s. withdraw. nn. Concentration uu. chin placed down  Causes: on the chest & head supported  Hypotension by a pillow. Saddle Block: Sensory loss involves lower g.  Chronic dermatitis or skin creating turbulence) infection near puncture site u.2 hours. High spinal anesthesia: sensory block at the  Vertebral column is bounded level of the nipple line (T4). Respiratory during lumbar puncture:  Difficulty of breathing  Skin  Apnea (at high levels)  Subcutaneous tissue  Causes:  Supraspinous ligament  Lack of propioception (sensation of  Interspinous ligament dyspnea)  Ligamentum flavum  Hypotension (cerebral  Dura hypoperfusion) → Technique  Motor block to C3-C5 & phrenic l. Successful puncture is followed by a free flow of CSF after removal of the needle Epidural Anesthesia stylet. Concentration of solution  Patient refuses consent t. Spinal nerve roots are blocked as they approach traverse the epidural space & also sympathetic fibers  Paramedian: used only when traveling with the anterior roots. Cervical epidural – cervical spine for neck Dextrose Water (Crystalline surgeries form dissolved in dextrose → Factors influencing the spread of solution in the epidural  Onset of action 5-10 minutes & space duration of action 1½ . Lumbar epidural – lumbar spine (spinal → Drugs Used in Spinal Anesthesia epidural block) o. Lidocaine rr. Site of injection  Hypotension y. Chronic Adhesive arachnoiditis give). Specific gravity of solution  Pre-existing spinal cord injury x. Drugs use  Supplied as 5% solution mixed ss. 4 coccygeal dd.  Can be made safely at the interspaces Management: increase flow of between L2 & L3. Structures traversed by the spinal needle ff. Urinary retention: Urogenic bladder through the ligaments until the dura is pierced kk.

Onset is 10-20 minutes & duration is anesthetics & epinephrine 3½ . Previous laminectomy  Single dose injection of local nnnn. Hypotension: due to sympathetic blockade aaaaa. Muscle relaxation not complete → Hypothermia xxx. Slower onset maintenance anesthesia throughout surgery. Lidocaine: 15-30 mL. Due to anatomic abnormalities or vasoconstrictors) incorrect methods. S1-S3). muscles & cccc. → Indications (Lower abdomen & perineum) aaa. Poor risk patients → Pre-operative medication eeee. opiates. Rarely. interspace. resistance disappears Hemmorhoidectomy. Patient is placed in the lateral decubitus sacral canal. During bbbb. vvvv.→ Anatomy gggg. Less intensity of motor & sensory fats absorbs some of the anesthetic agents. More severe disturbances of spinal anesthesia complications occur mandating that patients be are minimized (headache. fat.75% wwww. the distance between skin & jjjj. 0. Cervical: Sitting C7.) monitored one-to-one basis rrr. GI complaints are minimized (nausea. Bupivacaine: 15-30 mL. Catheterization incidence minimum → Pain ttt. Severe hemorrhage → Technique llll. acid base balance yyy. L1-L5. Obstetric patients undergoing vaginal when the point of a needle to a deliveries syringe with air enters the ssss. for ccc. lymphatics & the spinal nerve roots. Thoracic T7 qqqq. insertion of needle is at L4-L5 (S4-S5) and the coccygeal nerve. Less respiratory defects → Nausea & vomiting: Maybe because of pre anesthetic uuu. → Disadvantages ggg. Methods of doing epidural block mmmm. Cardiac diseases → Type of anesthetic used ffff. fistulectomy) and air in the syringe is sucked → Technique in. needle is sucked in once the above the tip of the coccyx. xxxx. For sacral plexus (T12.5 hours. Convulsions failure lll. the coccygeal plexus lumbar epidural. located by a distinct V depression. of 1-2% solution with or mL. arterial & venous spinal) networks. space. For various painful conditions including post the epidural space is 4-5 cm. Sacral hiatus needle enters the space. Onset is 10-20 minutes → Complications & duration of analgesia is 1½ hours. through the sacral hiatus into the epidural space of the zz. Large volume of solution necessary → Fluid. there is 5-15% chance of kkk. Technically more difficult to administer due to  Hypertension/ hypotension need of accurate needle placement  Arrhythmias www. Beyond ligamentum flavum abdominal & lower extremity surgeries. electrolyte. without epinephrine. 10% low pain of puncture relief post operative labor analgesic. Uncooperative or apprehensive patients yy. Bleeding in epidural space Anesthesia & Waking Up aaaa.25-0. Needle is inserted into the sacral saline placed into the hub of the hiatus between the sacral cornua. Longer duration compared to spinal block. Epidural space extends from base of the skull hhhh. Intraoperative or Postoperative analgesia is medications.29%. Local inflammation on site of  Fractional technique insertion (continuous epidural pppp. Metabolic disturbances vv. Hypertension (especially with bbbbb. may also be used in the following Factors that Affect the Amount of Time a Patient may Spend in circumstances PACU dddd. The nerves involved are part of the lumbo- position with full flexion of the spine. Infections are possible jjj. Total subarachnoid block: due to zzzz. of 2% Lidocaine after a test dose of 3-5 ddd.75%. Coagulation defects anesthetic oooo. It is difficult to obtain high levels of → Complications of Epidural Anesthesia anesthesia (Needs big amount) hhh. vomiting) PACU sss. etc. must identify cause then treat achieved → Respiratory depression → Disadvantages of Epidural Blockade → Cardiovascular system vvv. Damage due to catheter in the epidural space → Post anesthesia care nnn. POSTOPERATIVE CARE mmm. Accidental puncture of the dura eee. Well defined area of anesthesia unit (PACU) where patients are closely monitored. It takes time blocks for its elimination from the body’s tissues → Indications of epidural anesthesia: all operations below the diaphragm. General systemic reactions to local solution. meningitis. Patient is in prone position or lateral  Hanging drop method: a drop of uuuu. about 4 cm. Inject 15-20 → Drugs used: mL. Opoids. O the average. Systemic reactions are unrecognized dural puncture possible iii. kkkk. When spinal anesthesia is contraindicated ww. When general anesthesia is (foramen magnum) to the coccyx contraindicated (sacrococcygeal membrane) iiii. Physiologic decrease of intensity of sensory or → Post operative pain motor block (Similar to those observed in spinal anesthesia) Recovery room → Advantage of Epidural Blockade → Postoperative recovery starts in the post anesthesia care ooo. Pediatric patients undergoing lower bbb. unit is dedicated to meet the patient’s needs thereby good for long surgeries minimizing post-operative complications. operative patients xx. Methods of identifying the epidural space post-op analgesia (ex: Correction of (Principle: Negative pressure in the space) hypospadias or inguinal hernia repair)  Loss of resistance method: rrrr. Pulmonary diseases . This ppp. Danger of dural puncture zzz. Incomplete or patchy block → Recovery from anesthesia takes time. Operations of the perineum (ex. tttt. The epidural space contains loose areolar → Contraindications of Epidural anesthesia (Similar to connective tissue. Life threatening qqq. low dose local anesthesia yyyy. Refusal of the patient anesthesia): repeated injections of local anesthetic agent Caudal Anesthesia through a catheter inserted into → Accomplished by introducing local anesthetic solution the epidural space. infection develops at the site fff. of 0. prolonged headache. Neurologic: persistent paresthesia. Ropivacaine  0.

psychomotor functions recover. This means complete & physiological recovery. assigns a score to provide surgery objective information on the physical condition of patients arriving in the recovery room after anesthesia. such as going to work & driving Recovery Tests → Scoring systems developed to guide the transfer from the hospital recovery room to the ward maybe used to assess the early recovery of ambulatory surgical patients.g. If patient continues on IV fluid. ECG should be performed on postoperative day 1 for high risk patients  Laboratory: Follow up CBC for possibility of hemorrhage or large amount of blood loss. → Assessment of patient needs Peripheral perfusion should be adequate  Activity → Pain & emesis should be controlled & suitable antiemetic  Diet & analgesic prescribed  Proper breathing: Deep breathing increases → Temperature should be within acceptable circulation & promotes elimination of anesthesia  Pain management  Intake & output  Medications  Pain medications  Anti emetics: Determine the cause  Pre anesthetic medications  Gastric distention  5HT3 release  Into the circulation  Activates chemoreceptor trigger zone in the medulla  Vomiting  Gastric suctioning  Anesthetic technique  Anesthetic agent  Type of operation  Antibiotics  Routine medications that need to be renewed  PRN medications such as laxatives. Full return to the preoperative levels is not essential. Important Data to be Noted. which takes some hours or days after the cessation of anesthesia. & the patient maybe escorted home by a competent adult who remains with the patient until the stage of late recovery is achieved → Late Recovery: During this time. During that time. sleeping medications & antacids  Special Tests: such as follow up chest x-rays or serial ECGs. The specific values hypothermia of the pulse & blood pressure should approximate to  Urine output normal preoperative values or be at an acceptable level. eye opening) or the measurement of physiological parameters. consciousness & skin color. The most commonly used method. circulation. → Diagnosis & operation respiration. Observed & Monitored This test assigns a score of 0. vital signs stabilize & the patient becomes able to obey commands. → Length of time an anesthetic was administered during by Aldrete & Kroulik (1970). During that time. 1 or 2 to activity. Assessment of early recovery usually involved recording of the time when certain events occur (e. A score of 8 to 10 indicates  Level of consciousness adequacy of early recovery  Oxygen saturation  Vital signs Discharge Criteria from the PACU  Blood pressure → The patient is fully conscious. check daily electrolytes Stages of Recovery Recovery from outpatient anesthesia includes → Dissipation of anesthetic agents → Normalization of physiological functioning → Observation for medical or surgical complications → Treatment of immediate side effects of anesthesia & surgery → Discharge & return at home Recovery from Anesthesia maybe divided into 3 Main stages → Early Recovery (Phase I): Time from the end of anesthesia until the patient wakes up. such as blood pressure & respiratory rate & crude measurement of alertness → Intermediate Recovery (Phase II): Time from discharge from the recovery room or the post anesthesia care unit until the patient has recovered sufficiently to be safely discharged from the hospital. the patient returns to the preoperative fitness level. described . able to maintain clear  Respiratory frequency & pattern airway & exhibit adequate airway reflexes  Heart rate & rhythm → Respiration & oxygenation are satisfactory  Temperature: Prevention of → The cardiovascular system is stable. protective reflexes recover. with → Patients must be kept under clinical observation at all a score of 10 indicating the best possible condition for times discharge from the PACU.