2. Lidocaine
Lidocaine, the first amino amide-type local
anesthetic, was first synthesized under the name
Xylocaine by Swedish chemist Nils Löfgren in 1943.
3. Indications
Rapid acting local anesthetic for procedures ranging
from infiltration to regional nerve block
Antiarrhythmic in the treatment of vent. arrhythmias
Treatment of status epilepticus (INVESTIGATIONAL)
Treatment of pain
Operative
Neuropathic pain
4. Pharmacology
Half life: 90-120 min.
Time to steady state: 8-10 hours
Distribution: Lipo-philic, widely distributed into body
Protein binding: 60-80 %
Metabolism:
90% metabolite in the liver,
10 % unchanged drug excreted by kidney.
Mao & Chen, 2000
5. Pharmacology
Active metabolites:
Active metabolites: 90% in the liver
monoethylglycinexylidide(MEDX), half life 2
hrs, 60-80% as potent as lidocaine
glycinexylidine(GX), half life 10 hrs
Half-life of lidocaine is approximately 90–120 min.
hepatic impairment (average 343 min.) or
Congestive heart failure (average 136 min.)
6. Mechanism of action:
Intravenous lidocaine is analgesic, antihyperalgesic, and
antiinflammatory.
These properties are mediated by a variety of
mechanisms, including sodium channel
blockade,as well as inhibition of G protein–coupled
receptors and N-methyl-D-aspartate receptors. * *
In sub-anesthetic dose, it blocks spontaneous ectopic
discharge of the injured nerve without blocking
normal nerve conduction*
* * Acta Anaesthesiol Scand.2006 * * Int Anesthesiol Clin. 2003 * Mao & Chen, 2000
8. Contraindications for the use of lidocaine
• Heart block, second or third degree (without pacemaker)
• Severe sinoatrial block (without pacemaker)
• Serious adverse drug reaction to amide local anaesthetics
• Concurrent treatment with
quinidine, flecainide, disopyramide, procainamide (Class I
agents)
• Prior use of Amiodarone hydrochloride
• Hypotension not due to Arrhythmia
• Bradycardia
• Accelerated idioventricular rhythm
• Pacemaker
• Porphyria, especially acute porphyria (AIP);
9.
10. Sodium Channel
• The sodium channel is a voltage gated channel (Nav)
is grouped into 9 classifications dependant upon there
location and action.
• The therapeutic goal would be to develop one that
could specifically block the four channels (1.3, 1.7, 1.8
and 1.9) that have been shown to be in use for the
proliferation of neuropathic and other pain signals.
11. Sodium Channels role in neuropathic pain
A Theory suggests that the fast
activation, inactivation and rapid re-priming kinetics
and persistent current component of The sodium
channel 1.3 contribute to the development of
spontaneous ectopic discharges and sustained firing
characteristics of injured sensory nerves, leading to
neuropatheic pain.
Rogers M, et al.2006
12. Its mode of action is the attenuation of peripheral
nociceptors sensitisation and CNS
hyperexcitability, it achieves this by stablaising the
open state of the sodium channel, this will lead to
the sodium channel effectively being deactivated.
Rogers M, et al., Semin Cell Dev Biol (2006)
13. Lidocaine
Bartlett et al. 1961
First study suggesting there is a role for systemic
lidocaine for relief of post-op pain
Boas et al. 1982
Clinical role for lidocaine for treatment of
peripheral and central pain
14. Inhibition of Postoperative Pain by Continuous Low-
Dose intravenous Infusion of Lidocaine
Jean Cassuto, Anesthesia and Analgesia
low-dose continuous infusion of lidocaine is devoid of
side effects and can be used to decrease the severity
of postoperative pain,
thus reducing the need for potent morphinomimetic
drugs in the postoperative period
15. Treatment of Postoperative Paralytic ileus by
Intravenous Lidocaine Infusion
Gunnar Rimback, Md, Anesth Analg,1990
lidocaine or saline placebo.
Thirty patients scheduled for elective cholecystectomy were studied
Continuous IV infusion of lidocaine during the first
postoperative day after cholecystectomy can reduce
the need for narcotics and shorten the period of
postoperative colonic inhibition in patients
undergoing major abdominal surgery.
Secondary to the inhibition of peritoneal irritation
followed by reduced activation of inhibitory
gastrointestinal reflexes.
16. Intravenous Lidocaine Infusion Facilitates Acute
Rehabilitation after Laparoscopic Colectomy
Abdourahamane Kaba, M.D.,*Anesthesiology 2007
45 patients enrolled
Conclusions:
Intravenous lidocaine improves postoperative
analgesia, fatigue, and bowel function after
laparoscopic colectomy.
These benefits are associated with a significant
reduction in hospital stay.
17. Perioperative Intravenous Lidocaine Has Preventive
Effects on Postoperative Pain and Morphine
Consumption After Major Abdominal Surgery
Wolfgang Koppert, Germany ,Anesth Analg 2004
A prospective, randomized, and double-blinded study of 40 patients undergoing major
abdominal surgery
The perioperative administration of systemic lidocaine
is most effective in surgery associated with the
development of pronounced central
hyperalgesia, i.e., intestinal and bowel surgery.
The pain experience after these types of surgery can be
attenuated by lidocaine in a clinically relevant
manner.
18. Intravenous Lidocaine for Ambulatory
Anesthesia
Christopher L. Wu, MD ,Inter Anes Research Society,Dec. 2009
Using 1.5–3 mg kg h
lidocaine significantly reduced the incidence of
nausea and vomiting (32% vs 52%),
Marginally reduced pain scores ,
Decreased duration of postoperative ileus (8.4 h)
and hospital stay (0.84 days).
19. Systemic Lidocaine Shortens Length of
Hospital Stay After Colorectal Surgery
A Double-blinded, Randomized, Placebo-controlled Trial
Susanne Herroeder, MD Annals of Surgery, August 2007
60 patients of ASA physical status I to III, between 18
and 75 years of age, scheduled for elective colorectal
surgery
20. Study Drug Administration
Patients in the lidocaine group received 1.5 mg/kg
lidocaine intravenously as a loading dose before
induction of general anesthesia.
Immediately after tracheal intubation, a continuous
systemic lidocaine infusion (2 mg/min) was initiated
and terminated 4 hours after skin closure.
Patients in the control group were treated likewise
using NaCl 0.9% in a double-blinded fashion.
21. Outcome Measures
The primary outcome measure
• length of hospital stay.
Secondary outcome measures
• Length of PACU stay,
• Time until return of bowel function,
• Postoperative pain and opioid consumption,
• Plasma levels of several pro- and anti-
inflammatory interleukins .
27. Conclusions:
Systemic lidocaine may thus provide a convenient
and inexpensive approach to improve outcome for
patients not suitable for epidural anesthesia.
28. Comparison of the effects of thoracic epidural
analgesia and i.v. infusion with lidocaine on cytokine
response, postoperative pain and bowel function in
patients undergoing colonic surgery
C. P. Kuo ,British Journal of Anaesthesia Sept, 2006
Conclusions
The TEA lidocaine had better pain relief, lower
opioid consumption, earlier return of bowel function
and lesser production of cytokines than IV lidocaine
during 72 h after colonic surgery; IV group was better
than the control group.
29. Systemic administration of local anesthetics
to relieve neuropathic pain : a systemic
review and meta-analysis
Tremont-Lukats, 2005
30.
31. conclude
“Lidocaine and mexiletine produced no major adverse
events in controlled clinical trials, were superior to
placebo to relieve neuropathic pain, and were as
effective as other analgesics used for this condition.”
Tremont-Lukats, 2005
32. The Analgesic Response to Intravenous
Lidocaine in the Treatment of Neuropathic Pain
F. Michael Ferrante, Anesth A nalg 1996
13 patients were enrolled in the study,with neuropathic
pain for at least 6 months .
Lidocaine was administered IV at a rate of 8.35 mg/min
over 60 min.
In conclusion,
the results of this study suggest that the analgesic
response to IV lidocaine is best characterized by a
precipitous ‘break in pain” over a narrow dosage and
concentration range.
33. Topical Lidocaine Patch Relieves a Variety of
Neuropathic Pain Conditions
Devers, Clinical Journal of Pain: Sept 2000
Results:
Moderate or better pain relief was reported by 13 of the
16 participants (81%).
Patients had a mean duration of patch use of 6.2 weeks
with continued relief.
34. Chronic pain treatment with intravenous
lidocaine
Petersen P, Neurol Res., Sep,1986
18 patients with severe chronic pain states due
neurological diseases.
After the infusion of lidocaine 14 patients (78%)
had significant pain relief ranging from 2 hours to
25 days.
35. Efficacy of 5-Day Infusion Continuous Lidocaine for the
Treatment of Refractory C R P S
Robert . schwartzman, md,pain medicine, 2009
The majority of patients demonstrated a significant
decrease in pain parameters and other symptoms
and signs of CRPS. The pain reduction lasted an
average of 3 months.
Lidocaine may be particularly effective for thermal
and mechanical allodynia. Less clinically significant
effects were documented on the motor aspects of
the syndrome.
36. Diabetic Polyneuropathy (DPN)
Viola et al., Journal of Diabetes and Complications, 2006
15 pat. with intractable painful DPN
Double-blind, placebo-controlled crossover trial
Two doses: 5mg/kg and 7.5mg/kg vs. saline
Infusion during 4h and every 4 weeks
Both doses ↓↓ severity of pain
Dose-response effect !
Reduction present at 14 and 28 days after
Decrease in qualitative nature of pain up to 28d
37. Guidelines
Pre infusion assessment and preperation
Lidocaine test
Lidocaine infusion
Home infusion
38. Pre infusion assessment
Complete history and physical examination
Quantitative pain assessment
Any history of allergy from lidocaine
Any history of Heart or liver diseases
ECG
Ferrini& Paice, 2004
39. Patient preperation
Patients are required to have nothing by mouth for
4 hours prior to the procedures
Written consent
Vital signs are monitored including heart
rhythm, heart rate, blood pressure and oxygen
saturation
40. Lidocaine test Dose: 1-3 mg/kg (average 100 mg)
Concentration:
8 mg/ml IV over 20-30 min. OR
40 mg/ml SC over 30-60 min (2-3 ml/hr)
Monitor pain relief, vital signs and side effects q15
min.
50% of the dose in elderly patients >70 year, patients
with heart or liver disease
Ferrini& Paice, 2004
41. Lidocaine infusion
If pain relief > 50% and no side effects
Dose 0.5 -2 mg/kg/hr IV OR SC
Monitor pain, V/S and side effect after 15 min then
60 min then q 8 hr then prn
Titrate up based on pain relief
If any side effects occurred, stop infusion, reassess
after 30-60 min then resume with 20% Or last safe
dose
42. Home infusion
Patient must have a stable caregiver situation, with
24-hour supervision by a competent adult
Patient must consent to being visited by a registered
nurse 2–7 times a week
Patient/caregiver should be provided with a
lidocaine patient information sheet
43. Home Massages
• Lidocaine infusion is safe and effective
intervention for operative and chronic pain
• Lidocaine infusion has narrow therapeutic
index. So, it needs clear guidelines to
demonstrate how we use it safely
Editor's Notes
Animated spinning picture(Intermediate)Tip: Some shape effects on this slide are created with the Combine Shapes commands. To access this command, you must add it to the Quick Access Toolbar, located above the File tab. To customize the Quick Access Toolbar, do the following:Click the arrow next to the Quick Access Toolbar, and then under CustomizeQuickAccessToolbar click MoreCommands.In the PowerPointOptions dialog box, in the Choose commands from list, select All Commands. In the list of commands, click CombineShapes, and then click Add.To reproduce the shape effect on this slide, do the following:On the Home tab, in the Slides group, click Layout, and then click Blank.Also on the Home tab, in the Drawing group, click Shapes, and then under Basic Shapes click Oval (first row).On the slide, drag to draw an oval.Select the oval. Under DrawingTools, on the Format tab, in the Size group, enter 6” in the Height box and 6” in the Width box.Also on the Format shape, in the ShapeStyles group, click ShapeOutline, and then click NoOutline.On the Home tab, in the Drawing group, click Shapes, and then under BasicShapes click Pie (second row).On the slide, drag to draw a pie.Select the pie. Drag the yellow diamond adjustment handle to create a wedge shape.Under DrawingTools, on the Format tab, in the Size group, enter 5.7” in the Height box and 5.7” in the Width box.Press and hold CTRL, select the oval, and then select the pie. On the Home tab, in the Drawing group, click Arrange, point to Align, and then do the following:Click Align to Slide.Click Align Center.Click Align Middle.Press and hold CTRL, and then select the oval and then the pie shape. On the Quick Access Toolbar, click Combine Shapes, and then click ShapeSubtract.Select the new shape. Under DrawingTools, on the Format tab, in the ShapeStyle group, click the FormatShape dialog box launcher. In the FormatShape dialog box, click Fill in the left pane, in the Fill pane, click Pictureor texture fill, and then click the button next to Texture and click RecycledPaper (third row). Also in the FormatShape dialog box, click PictureColor in the left pane, in the PictureColor pane, under Recolor, click the button next to Presets, and then click Grayscale (first row). Also in the FormatShape dialog box, click PictureCorrections in the left pane, in the PictureCorrections pane, under Brightness and Contrast, in the Contrast box, enter 20%. Also in the FormatShape dialog box, click Shadow in the left pane, in the Shadow pane, click the Presets button, and then under Outer, click Offset Diagonal Bottom Left.Also in the Shadow pane, in the Blur box, enter 10 pt. To reproduce the picture effects on this slide, do the following:On the Insert tab, in the Images group, click Picture. In the Insert Picture dialog box, select a picture and then click Insert.Select the picture. Under PictureTools, on the Format tab, in the Size group, click the Size and Position dialog box launcher. In the Format Picture dialog box, resize or crop the image so that the height is set to 5.8” and the widthis set to 5.8”. To crop the picture, click Crop in the left pane, and in the right pane, under Crop position, enter values into the Height, Width, Left, and Top boxes. To resize the picture, click Size in the left pane, and in the right pane, under Size and rotate, enter values into the Height and Width boxes.Under Picture Tools, on the Format tab, in the Size group, click the down arrow under Crop, and then click Crop to Shape. Under Basic Shapes, click Oval (first row, first option from the left).Also under PictureTools, on the Format tab, in the Arrange group, click SendBackward.To reproduce the other shapes on this slide, do the following:Also on the Home tab, in the Drawing group, click Shapes, and then under BasicShapes click Oval (first row). On the slide, drag to draw an oval.Select the oval. Under DrawingsTools, on the Format tab, in the Size group, enter 0.17” in the Height box and 0.17” in the Width box. Also on the Format tab, in the ShapeStyles group, click ShapeFill, and then under ThemeColors, click Black, Text 1, Lighter 25% (fourth row). Also on the Format tab, in the ShapeStyles group, click ShapeOutline, and then click No Line. On the Home tab, in the Drawing group, click Shapes, and then under BasicShapes click Donut.On the slide, drag to draw a donut.Select the donut. Under Drawing Tools, on the Format tab in the Size group, enter 0.25” in the Height box and 0.25” in the Width box.Also on the Format tab, in the ShapeStyles group, click the FormatShape dialog box launcher. In the FormatShape dialog box, click Fill in the left pane, in the Fill pane, click Gradientfill, and then click the button next to Preset colors and click Silver (fifth row). Also in the FormatShape dialog box, click LineColor in the left pane, in the LineColor pane, click No line.Also in the FormatShape dialog box, click 3-DFormat in the left pane, in the 3-DFormat pane, under Bevel, click the button next to Top, and then click Circle (first row).Press and hold CTRL, and then select the freeform shape, the picture, the small circle, and the donut. On the Home tab, in the Drawing group, click Arrange, point to Align, and the do the following:Click Align to Slide.Click Align Center.Click Align Middle.Also on the Home tab, in the Drawing group, click Shapes, and then under BasicShapes click Oval.On the slide, drag to draw an oval.Select the oval. Under DrawingTools, on the Format tab, in the Size group, enter 0.65” in the Height box and 0.65” in the Width box. Also on the Format tab, in the ShapeStyles group, click the FormatShape dialog box launcher. In the FormatShape dialog box, click Fill in the left pane, in the Fill pane, click Picture or texture fill, and then click the button next to Texture and then click Recycled Paper (fourth row). Select the freeform shape. On the Home tab, in the Clipboard group, click Format Painter, and then click the new oval. Position this circle over the top edge of the freeform shape. On the Home tab, in the Drawing group, click Arrange, and then do the following:Under OrderObjects, click Send to Back.Point to Align, and then click Align Center.To reproduce the animation effects on this slide, do the following:Select the picture. On the Animations tab, in the AdvancedAnimation group, click AddAnimation, and then under EmphasisEffects, click Spin.Also on the Animations tab, in the Animation group, click the Show Additional Effects Options dialog box launcher. In the Spin dialog box, on the Effect tab, do the following:In the Smoothstart box, enter 5 sec.In the Smooth end box, enter 5 sec.Also in the Spin dialog box, click the Timing tab, and then do the following:In the Start list, select WithPrevious.In the Duration box, enter 20 sec.Select the small oval at the top edge of the freeform shape. On the Animations tab, in the AdvancedAnimation group, click AddAnimation, under Motion Paths, click Shapes.On the slide, drag the bottom, left, and right sides of the motion path so that it matches the inside edge of the freeform shape.Also on the Animations tab, in the Animation group, click the Show Additional Effects Options dialog box launcher. In the Circle dialog box, on the Effect tab, do the following:In the Smoothstart box, enter 5 sec.In the Smooth end box, enter 5 sec.Also in the Spin dialog box, click the Timing tab, and then do the following:In the Start list, select WithPrevious.In the Duration box, enter 20 sec.To reproduce the background effects on this slide, do the following:On the Design tab, in the Background group, click BackgroundStyles, and then click Style9.
A bolus injection of lidocaine 1.5 mg/kg followed by a continuous infusion of 1.5 mg /kg/ h led to lidocaine plasma levels of approximately 2 mic mL
Performed between Dec. 2003 and Nov. 2004. Sixty patients, ASA I or II, aged 40–80 yr, and Undergoing elective surgery for colon cancer were recruited
