LIDOCAINE

Drugs in Pregnancy and Lactation.

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Name: LIDOCAINE
Class: Local Anesthetic/Cardiac Drug
Risk Factor:    BM

Fetal Risk Summary

Lidocaine is a local anesthetic that is also used for the treatment of cardiac ventricular arrhythmias. The majority of the information on the drug in pregnancy derives from its use as a local anesthetic during labor and delivery. Reproduction studies have revealed no evidence of fetal harm in pregnant rats at doses up to 6.6 times the human dose (1).

The drug rapidly crosses the placenta to the fetus, appearing in the fetal circulation within a few minutes after administration to the mother. Cord:maternal serum ratios range between 0.50 and 0.70 after IV and epidural anesthesia (2,3,4,5,6,7,8,9,10,11 and 12). In 25 women just before delivery, a dose of 2–3 mg/kg was given by IV infusion at a rate of 100 mg/minute (2). The mean cord:maternal serum ratio in 9 patients who received 3 mg/kg was 0.55. A mean ratio of 1.32 was observed in nonacidotic newborns following local infiltration of the perineum for episiotomy (13). A similarly elevated ratio was measured in an acidotic newborn (14). The infant had umbilical venous/arterial pH values of 7.23/7.08 and a lidocaine cord:maternal serum ratio of 1.32 following epidural anesthesia. Because lidocaine is a weak base, the high ratio may have been caused by ion trapping (14).

Both the fetus and the newborn are capable of metabolizing lidocaine (8,9). The elimination half-life of lidocaine in the newborn following maternal epidural anesthesia averaged 3 hours (8). After local perineal infiltration for episiotomy, lidocaine was found in neonatal urine for at least 48 hours after delivery (13).

A number of studies have examined the effect of lidocaine on the newborn. In one report, offspring of mothers receiving continuous lumbar epidural blocks had significantly lower scores on tests of muscle strength and tone than did controls (15). Results of other tests of neurobehavior did not differ from those of controls. In contrast, four other studies failed to find adverse effects on neonatal neurobehavior following lidocaine epidural administration (10,11 and 12,16). Continuous infusion epidural analgesia with lidocaine has been used without effect on the fetus or newborn (17).

Lidocaine may produce central nervous system depression in the newborn with high serum levels. Of eight infants with lidocaine levels greater than 2.5 ΅g/mL, four had Apgar scores of 6 or less (3). Three infants with levels above 3.0 ΅g/mL were mildly depressed at birth (3). A 1973 study observed fetal tachycardia (3 cases) and bradycardia (3 cases) after paracervical block with lidocaine in 12 laboring women (18). The authors were unable to determine whether these effects were a direct effect of the drug. Accidental direct injection into the fetal scalp during local infiltration for episiotomy led to apnea, hypotonia, and fixed, dilated pupils 15 minutes after birth in one infant (19). Lidocaine-induced seizures occurred at 1 hour. The lidocaine concentration in the infant's serum at 2 hours was 14 ΅g/mL. The heart rate was 180 bpm. Following successful treatment, physical and neurologic examinations at 3 days and again at 7 months were normal.

Lidocaine is the treatment of choice for ventricular arrhythmias (20,21). A 1984 report described the use of therapeutic lidocaine doses (100 mg IV injection followed by 4 mg/minute infusion) in a woman who was successfully resuscitated after a cardiac arrest at 18 weeks' gestation (22). A normal infant was delivered at 38 weeks' gestation. Neurologic development was normal at 17 months of age, but growth was below the 10th percentile.

The Collaborative Perinatal Project monitored 50,282 mother-child pairs, 293 of which had exposure to lidocaine during the 1st trimester (23, pp. 358–363). No evidence of an association with large classes of malformations was found. Greater than expected risks were found for anomalies of the respiratory tract (3 cases), tumors (2 cases), and inguinal hernias (8 cases), but the statistical significance is unknown and independent confirmation is required (23, pp. 358–363, 477). For use anytime during pregnancy, 947 exposures were recorded (23, pp. 440, 493). From these data, no evidence of an association with large categories of major or minor malformations or to individual defects was found.

Breast Feeding Summary

Small amounts of lidocaine are excreted into breast milk (24). A 37-year-old, lactating woman was treated with intravenous lidocaine for acute onset ventricular arrhythmia secondary to chronic mitral valve prolapse. The woman had been nursing her 10-month-old infant up to the time of treatment. She was treated with lidocaine, 75 mg over 1 minute, followed by a continuous infusion of 2 mg/minute (23 ΅g/kg/minute). A second 50-mg dose was given 5 minutes after the first bolus dose. The woman's serum lidocaine level 5 hours after initiation of therapy was 2 ΅g/mL. The drug concentration in a milk sample, obtained 2 hours later when therapy was stopped, was 0.8 ΅g/mL (40% of maternal serum). Although the infant was not allowed to nurse during and immediately following the mother's therapy, the potential for harm of the infant from exposure to lidocaine in breast milk is probably very low. The American Academy of Pediatrics considers lidocaine to be compatible with breast feeding (25).

References

  1. Product information. Xylocaine. Astrazeneca, 2000.
  2. Shnider SM, Way EL. The kinetics of transfer of lidocaine (Xylocaine) across the human placenta. Anesthesiology 1968;29:944–50.
  3. Shnider SM, Way EL. Plasma levels of lidocaine (Xylocaine) in mother and newborn following obstetrical conduction anesthesia: clinical applications. Anesthesiology 1968;29:951–8.
  4. Lurie AO, Weiss JB. Blood concentrations of mepivacaine and lidocaine in mother and baby after epidural anesthesia. Am J Obstet Gynecol 1970;106:850–6.
  5. Petrie RH, Paul WL, Miller FC, Arce JJ, Paul RH, Nakamura RM, Hon EH. Placental transfer of lidocaine following paracervical block. Am J Obstet Gynecol 1974;120:791–801.
  6. Zador G, Lindmark G, Nilsson BA. Pudendal block in normal vaginal deliveries. Acta Obstet Gynecol Scand 1974;Suppl 34:51–64.
  7. Blankenbaker WL, DiFazio CA, Berry FA Jr. Lidocaine and its metabolites in the newborn. Anesthesiology 1975;42:325–30.
  8. Brown WU Jr, Bell GC, Lurie AO, Weiss JB, Scanlon JW, Alper MH. Newborn blood levels of lidocaine and mepivacaine in the first postnatal day following maternal epidural anesthesia. Anesthesiology 1975;42:698–707.
  9. Kuhnert BR, Knapp DR, Kuhnert PM, Prochaska AL. Maternal, fetal, and neonatal metabolism of lidocaine. Clin Pharmacol Ther 1979;26:213–20.
  10. Abboud TK, Sarkis F, Blikian A, Varakian L. Lack of adverse neurobehavioral effects of lidocaine. Anesthesiology 1982;57(Suppl):A404.
  11. Kileff M, James FM III, Dewan D, Floyd H, DiFazio C. Neonatal neurobehavioral responses after epidural anesthesia for cesarean section with lidocaine and bupivacaine. Anesthesiology 1982;57(Suppl):A403.
  12. Abboud TK, David S, Costandi J, Nagappala S, Haroutunian S, Yeh SY. Comparative maternal, fetal and neonatal effects of lidocaine versus lidocaine with epinephrine in the parturient. Anesthesiology 1984;61(Suppl):A405.
  13. Philipson EH, Kuhnert BR, Syracuse CD. Maternal, fetal, and neonatal lidocaine levels following local perineal infiltration. Am J Obstet Gynecol 1984;149:403–7.
  14. Brown WU Jr, Bell GC, Alper MH. Acidosis, local anesthetics, and the newborn. Obstet Gynecol 1976;48:27–30.
  15. Scanlon JW, Brown WU Jr, Weiss JB, Alper MH. Neurobehavioral responses of newborn infants after maternal epidural anesthesia. Anesthesiology 1974;40:121–8.
  16. Abboud TK, Williams V, Miller F, Henriksen EH, Doan T, Van Dorsen JP, Earl S. Comparative fetal, maternal, and neonatal responses following epidural analgesia with bupivacaine, chloroprocaine, and lidocaine. Anesthesiology 1981;55(Suppl):A315.
  17. Chestnut DH, Bates JN, Choi WW. Continuous infusion epidural analgesia with lidocaine: efficacy and influence during the second stage of labor. Obstet Gynecol 1987;69:323–7.
  18. Liston WA, Adjepon-Yamoah KK, Scott DB. Foetal and maternal lignocaine levels after paracervical block. Br J Anaesth 1973;45:750–4.
  19. Kim WY, Pomerance JJ, Miller AA. Lidocaine intoxication in a newborn following local anesthesia for episiotomy. Pediatrics 1979;64:643–5.
  20. Tamari I, Eldar M, Rabinowitz B, Neufeld HN. Medical treatment of cardiovascular disorders during pregnancy. Am Heart J 1982;104:1357–63.
  21. Rotmensch HH, Elkayam U, Frishman W. Antiarrhythmic drug therapy during pregnancy. Ann Intern Med 1983;98:487–97.
  22. Stokes IM, Evans J, Stone M. Myocardial infarction and cardiac arrest in the second trimester followed by assisted vaginal delivery under epidural analgesia at 38 weeks gestation. Case report. Br J Obstet Gynaecol 1984;91:197–8.
  23. Heinonen OP, Slone D, Shapiro S. Birth Defects and Drugs in Pregnancy. Littleton, MA:Publishing Sciences Group, 1977.
  24. Zeisler JA, Gaarder TD, De Mesquita SA. Lidocaine excretion in breast milk. Drug Intell Clin Pharm 1986;20:691–3.
  25. Committee on Drugs, American Academy of Pediatrics. The transfer of drugs and other chemicals into human milk. Pediatrics 1994;93:137–50.

Index

Q&A about Lidocaine

skibum_u...
Can you become allergic to lidocaine all of a sudden?
I was just perscribed lidocaine and was allergic to it - well - I felt dizzy, nausous, diarra, just icky. I also have this feeling when I go to the dentist. I have been ok with the dentist until 8 years ago when I passed out in the dentist office. And ever since then I am terrified about going to the dentist because of that. Was that a allergic reaction and can you become allergic to lidocaine and the dentist "caine"?
The mom
You can be allergic to just about anything, but you don't describe the usual allergic reaction. The dentist uses the same local anesthetic the doctors do, except their preps usually contain epinephrine as well- to restrict bleeding and extend the effectiveness. Epinephrine is the "fight or flight" chemical your body produces when you are stressed or frightened, and can cause all sorts of odd feelings- including the gut. To find out if you are truly allergic to it you would need to be specifically tested by an allergist. If you suspect you are, that would be a good thing to do, because allergies to medications that are injected can be quite deadly. They can show up all of a sudden, and can go from one mild to one life threatening reaction without warning. And since lidocaine is such a common local anesthetic, you would certainly need to know and have a medicalert tag to the effect. But what I think is you are dealing with an overstressed body in fear of the dentist, and the epinephrine isn't helping matters any. That's what it really sounds like. Still, get tested and find out for certain. Then if it's safe, you can always ask the dentist for a bit of a sedative first, which will help control the other reactions.

Note- you aren't supposed to swallow the mouthwash. You are supposed to swish in in your mouth and spit it out- not swallow it. You feel slighty icky because you just slightly anesthetized your esophogus, stomach and everything else. While it won't hurt you- it's not intended to be swallowed in much quantity.
mark g
Why does lidocaine sometimes not work?
I've had this problem a couple times at the dentist (different dentists). The dentist will numb the area he is going to work on with lidocaine (or some other ...caine) and the stuff just wont take. He then uses more and it still doesn't work. He then tries another type of anesthetic and it still doesn't work. I either have to suffer through some pain or wait and come back a different day (it worked the next time I came back). I'm only 29, don't smoke, don't do drugs and rarely drink. It this common or could it be something I'm doing that causes it not to work?
LaLa
Sometimes the anaesthetic won't take if there is an infection present, or if your nerves aren't exactly where they should be, or even if you're really anxious it can affect the freezing. I don't think it's anything that you did. It just happens. I'll be back. I remember reading about this. I'll see if I can find it. =)

Okay - I found a site that may be able to answer some of your questions. Check this out:

http://www.dentalfearcentral.org/difficu...
MsLuLupR...
Im allergic to lidocaine. Will that affect me getting an epidural if I need one?
When I was younger, I had an allergic reaction to lidocaine. I went to get a filling in my molar and my throat started to like close up and I could breath normally. Now that Im getting closer to my due date, Im getting very nervous about this. I dont plan on getting an epidural, but if I really do need it, I want to know if it would be safe to get it because of my allergic reaction.
MonTana Tiggs (Smokey)
Tell them Now so they can prepare- OK The need to know this - it's possible they can test you -topically to see if there is still a positive reaction or at the least a blood test

They can use a substitue like "sensorcaine" (i have had many epidurals for pain) or xylocaine

Do yourself a favor and INFORM then now ok

Congratulations!
momabee
I have aloe with Lidocaine. Can I use it on my dogs allergic rash?
She was running through some plants and now has a rash. She's already had her Benadril, given to at the vet, but the rash is itchy. Will the Lidocaine hurt her?
;)
Benedryl would work better.
missy
What are the dangers of administering Lidocaine to infants for a sore throat?
My son was given this in an ER and our pediatrician just told me it can cause an infant to choke to death because the musclesof the throat would be too relaxed to swallow for a child as young as 8 months.
momx4
i WOULDN'T GIVE IT TO HIM! i WOULD TRUST YOUR FAMILY DOC BEFORE I WOULD TRUST AN ER DOC!
bonzaibb
How to make a lidocaine injection ?
I just purchased an emergency kit for suturing it contains 99.9% pure Lidocaine powder

How would I prepare that for injection purposes.

Before you say see a Dr I travel to places where there are no Dr.'s .. Backpacking ect...
terra
I think it should come with a vial of sterile water or saline to mix it with and instructions for how much to dilute it with. I don't think lido is necessarily rx, you can get the spray at the pharmacy, its otc.
Jennifer O
Has anybody used SSD with Lidocaine cream for tattoo healing?
I got a new tattoo on Sat. night, a "side piece" it is multiple stars that wrap from my ribs to hip. the spot is very sensitive, and it is hurting, all the time. i know i am probably being a big baby, but i have cream that i was given for a third degree burn, that has a numbing agent in it, and i am wondering if i could use that to heal and protect the tatoo, but it will also give me a bit of pain relief for the next couple days. Has anybody ever heard of using SSD (SILVER SULFADIAZINE) with Lidocaine cream to heal and help a tattoo?
lotus4yo...
Nope, don't think I would try that. I've never heard of Silvadene being used for anything but a serious burn. It can discolor your skin a little, too.

Neosporin is okay for the first couple days. (They do make one with lidocaine, I believe.) There is something better, though; I just don't know where you'd find it if your tattoo person didn't have it. I think it's called "emu" something. It's all natural - aloe vera, emu oil, and a couple other kinds of oils. After the first few days use any kind of cream/lotion that is unscented and has SPF. (Sun will fade your tattoo.)
shark
How do you extract lidocaine?
I want to extract lidocaine from some stinging nettles or perhaps an aloe vera leaf. It would be great if someone could give me a proven extraction method. If not, it would also be helpful if someone could tell me whether lidocaine is polar or non-polar soluble. Thanks for your help!!!
Felix
there is no easy way to do it..
estrange...
Which nitrogen on Lidocaine structure is most basic?
there are two nitrogen in the lidocaine structure, one is with the amine group and one is with the amide group. i think that the N of the amine group will be most basic because its electrons will readily accept a proton if reacted with an acid. (strong base + strong acid = rxn completion). please explain further and verify if my theory is correct. thank you very much!
Chad
Amines are much more basic than amides. This is due in part to the resonance structure of the amide in which the free electron pair of the nitrogen can be delocalized leaving a formal positive change on the amide nitrogen and negative on the amide oxygen.

_ +

O=C-N <--> O-C=N

You are also correct that the amine's nitrogen will react with a strong acid while the amide nitrogen will not be protonated. The amine nitrogen is not a "strong base" though. It is simply a more basic site than the amide nitrogen and will thus react with strong acid.