Drug Interaction:
Interacting drugs- summary
Local anesthetics +
Sedatives
if employed to reduce patient apphrension during dental procedures, use reduced doses, since loacl anesthetics used in combination with CNS depressants may have additive effects. Give young children minimal dose of each agent
Sulfonamides
the para- aminobenzoic acid metabolite of procaine,chloroprocaine and tetracaine inhibits the action of sulfonamides. Therefore do not use procaine, or tetracaine in any condition in which a sulfonamide drug is employed
Cimetidine/ranitidine
Decreased clearance with cimetidine and ranitidine.
Lignocaine/mepivacine
Potentiates lignocaine and mepivacaine. Prior use of chlorprocaine may interfere with susequent use of bupivacaine
Indication:
HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to use
EXPAREL® safely and effectively. See full prescribing information for EXPAREL. EXPAREL (bupivacaine liposome injectable suspension)
Initial U.S. Approval: 1972
New Drugs Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
S-Bupivacaine Hcl Injection 28-04-2011
2mg/5mg/7.5mg per ml
For Surgical Anesthesia in adults for Epidural (incuding Caesarian
Section) intrathecal ,Peripheral Nerve block.
Infiltration block Caudal epidural lumbar anaethesia
Adverse Reaction:
Cardiac arrest.
CNS excitation may be followed by depression
. Hypotension, bradycardia, arrhythmias and arrest, methhaemoglobinaemia.
Hypersensitivity. Prolonged block.
Dermatologic-
cutaneous lesions, urticaria, pruritus, erythema, angioneurotic edema, sneezing, syncope, excessive sweating, elevated temperature
CNS-
restlessness, anxiety dizziness, tinnitus, blurred vision, nausea, vomiting, chills, pupil constriction or trmors may occur.
Cardiovascular-
myocardial depression, hypotension, decreased cardiac output, herat block, syncope, bradycardia ventricular arrhythmias
Respiratory-
respiratory impairment or paralysis, dueto level of anesthesia (spinal ) extending to upper thoraic and cervical segments
Miscellaneous-
occasional intentional penetration of the subarachoid space by the catheter may occur.
Contra-Indications:
Hypersens to local anaesthetics of amide type.IV regional anaesthesia.
Special precautions:
Pregnancy, severe hepatic disease.
CVS disease.
Dosage- use the lowest dosage that results in effective anesthesia to avoid high plasma levels and serious adverse effects.
Inflammation or sepsis- use local anesthetic procedures with caution when there is inflammation or sepsis. in the region of the proposed injection.
CNS toxicity- monitor cardiovascular and respiratory vital signs and state of consciousness after each injection.
Special risks patients- debilated persons, acuely ill patients , children, obstertic delivery patients and patients with increased intra-abdominal pressure .
Malignant hyperthermia- many drugs used during ansthesia are considered potential triggering agents for familial malignant hyperthermia.
Vasoconstrictors- use sloutions containg vasoconstrictors with caution and in carefully circumscribed quantities in areas of body supplied by end arteries or having otherwise compromised blood supply (eg. digits, nose, external ear, penis) Intravenous regional anesthesia- cardiac arrest and death are reported with the use of bupivacaine for IV anesthesia. Bupivacaine is not recommended for this technique
Warnings-
Hypersenstivity reactions- including anaphylaxis may occurv in small segment of the population allergic to para-aminobenzoic acid derivatives (eg procaine, tetracaine, benzocaine)
Renal function impairment- use mepivacaine with caution in patients with renal disease. Hepatic function impairment- becausee amide-type local anesthetics are metabolised primarily in the liver, patients with hepatic disease, especially severe hepatic disease, may be more susceptible to potential toxicity
Elderly- repeated doses may cause accumulation of the drug or or its metabolites or slow metabolic degradation
Pregnancy- safety for use in pregnant women other than those in labor has not been established
Lactation- safety for use in nursing mother has not ben established.
Children- due to lack of clinical experience the administration of bupivacaine to children < 12 years of age is not recommended. Safety and efficacy of tetracaine in children have not been established
Dosages/ Overdosage Etc:
Indication-
Infiltration block Caudal epidural lumbar anaethesia
See literature
Dosage-
smallest dose and concentration to produce desired result should be administered
Patient Information:
1. When appropiate inform patients in advance that they may experience temporary loss of sensation, and motor activity, usually in the lower halfof the body, following proper administration of caudal or epidural anaesthesia
Pharmacology/ Pharmacokinetics:
Pharmacology-
These agents prevent generation and conduction of nerve impluses by inhibiting ionic fluxes, increasing electrical excitation threshold.slowing nerve impulse propagation and reducing rate of rise of action potential
Pharmcokinetics-
The onset of local anesthesia is dependent on the dissociation constant (pKa) lipid solubility, pH at the injection site protein binding and molecular size.
Pregnancy and lactation:
Pregnancy-
Safety for use in pregnant women other than those in labor has not been established
Lactation-
Safety for use in nursing mother has not ben established.
Children-
Due to lack of clinical experience the administration of bupivacaine to children < 12 years of age is not recommended. Safety and efficacy of tetracaine in children have not been established