Phenothiazines and butyrophenones may reduce or reverse the pressor effect of epinephrine. Concurrent use of these agents should generally be avoided.
In situations when concurrent therapy is necessary, careful patient monitoring is essential. Concurrent administration of vasopressor drugs for the treatment of hypotension related to obstetric blocks and ergot-type oxytocic drugs may cause severe, persistent hypertension or cerebrovascular accidents.
Thus, the use of this enzyme determination, without isoenzyme separation, as a diagnostic test for the presence of acute myocardial infarction may be compromised by the intramuscular injection of Lidocaine HCl. Carcinogenesis, Mutagenesis, Impairment of Fertility Studies of Lidocaine HCl in animals to evaluate the carcinogenic and mutagenic potential or the effect on fertility have not been conducted.
Reproduction studies have been performed in rats at doses up to 6. There are, however, no adequate and well-controlled studies in pregnant women. Animal reproduction studies are not always predictive of human response. General consideration should be given to this fact before administering Lidocaine HCl to women of childbearing potential, especially during early pregnancy when maximum organogenesis takes place.
Labor and Delivery Local anesthetics rapidly cross the placenta and when used for epidural, paracervical, pudendal or caudal block anesthesia, can cause varying degrees of maternal, fetal and neonatal toxicity. The potential for toxicity depends upon the procedure performed, the type and amount of drug used, and the technique of drug administration. Adverse reactions in the parturient, fetus and neonate involve alterations of the central nervous system, peripheral vascular tone and cardiac function.
Maternal hypotension has resulted from regional anesthesia. Local anesthetics produce vasodilation by blocking sympathetic nerves. The fetal heart rate also should be monitored continuously, and electronic fetal monitoring is highly advisable.
Epidural, spinal, paracervical, or pudendal anesthesia may alter the forces of parturition through changes in uterine contractility or maternal expulsive efforts. In one study, paracervical block anesthesia was associated with a decrease in the mean duration of first stage labor and facilitation of cervical dilation. The use of obstetrical anesthesia may increase the need for forceps assistance. The use of some local anesthetic drug products during labor and delivery may be followed by diminished muscle strength and tone for the first day or two of life.
The long-term significance of these observations is unknown. Fetal bradycardia may occur in 20 to 30 percent of patients receiving paracervical nerve block anesthesia with the amide-type local anesthetics and may be associated with fetal acidosis.
Fetal heart rate should always be monitored during paracervical anesthesia. The physician should weigh the possible advantages against risks when considering a paracervical block in prematurity, toxemia of pregnancy, and fetal distress.
Careful adherence to recommended dosage is of the utmost importance in obstetrical paracervical block. Failure to achieve adequate analgesia with recommended doses should arouse suspicion of intravascular or fetal intracranial injection.
Cases compatible with unintended fetal intracranial injection of local anesthetic solution have been reported following intended paracervical or pudendal block or both. Babies so affected present with unexplained neonatal depression at birth, which correlates with high local anesthetic serum levels, and often manifest seizures within six hours.
Prompt use of supportive measures combined with forced urinary excretion of the local anesthetic has been used successfully to manage this complication.
Case reports of maternal convulsions and cardiovascular collapse following use of some local anesthetics for paracervical block in early pregnancy as anesthesia for elective abortion suggest that systemic absorption under these circumstances may be rapid. The recommended maximum dose of each drug should not be exceeded. Injection should be made slowly and with frequent aspiration. Allow a 5- minute interval between sides. Nursing Mothers It is not known whether this drug is excreted in human milk.
Because many drugs are excreted in human milk, caution should be exercised when Lidocaine HCl is administered to a nursing woman. Adverse Reactions Systemic Adverse experiences following the administration of Lidocaine HCl are similar in nature to those observed with other amide local anesthetic agents.
These adverse experiences are, in general, dose- related and may result from high plasma levels caused by excessive dosage, rapid absorption or inadvertent intravascular injection, or may result from a hypersensitivity, idiosyncrasy or diminished tolerance on the part of the patient.
Serious adverse experiences are generally systemic in nature. Moderate Anti-retroviral protease inhibitors can inhibit hepatic cytochrome P 3A4, an isoenzyme that is partially responsible for the metabolism of lidocaine. The concurrent use of systemic lidocaine and anti-retroviral protease inhibitors should be carefully monitored due to the potential for serious toxicity.
In theory, coadministration of anagrelide with substrates of CYP1A2, including lidocaine, could lead to increases in the serum concentrations of lidocaine and, thus, adverse effects. Patients receiving anagrelide and lidocaine concomitantly should be monitored for increased toxicity of lidocaine.
Moderate Monitor for decreased efficacy of lidocaine if coadministration of systemic lidocaine with apalutamide is necessary; higher doses of lidocaine may be required. Major Use caution if lidocaine and aprepitant, fosaprepitant are used concurrently and monitor for an increase in lidocaine-related adverse effects, including QT prolongation and torsade de pointes TdP , for several days after administration of a multi-day aprepitant regimen. This interaction is not expected with topical preparations of lidocaine.
Lidocaine is a CYP3A4 substrate. As a single mg or 40 mg oral dose, the inhibitory effect of aprepitant on CYP3A4 is weak, with the AUC of midazolam increased by 1. After administration, fosaprepitant is rapidly converted to aprepitant and shares many of the same drug interactions. However, as a single mg intravenous dose, fosaprepitant only weakly inhibits CYP3A4 for a duration of 2 days; there is no evidence of CYP3A4 induction.
Fosaprepitant mg IV as a single dose increased the AUC of midazolam given on days 1 and 4 by approximately 1. Less than a 2-fold increase in the midazolam AUC is not considered clinically important. Moderate Use articaine and lidocaine together with caution. Moderate Caution and therapeutic drug concentrations monitoring, if available, is recommended during coadministration of systemic lidocaine with cobicistat.
Lidocaine is a substrate for CYP3A4; cobicistat is an inhibitor of this enzyme. Concurrent use may result in elevated lidocaine plasma concentration. Moderate Local anesthetics can prolong and enhance the effects of neuromuscular blockers. Monitoring of neuromuscular function is recommended. Moderate Lidocaine is a substrate for the cytochrome P isoenzymes 1A2 and 3A4. Barbiturates may enhance lidocaine clearance by inducing cytochrome P enzymes. In the case of phenobarbital, enhanced lidocaine clearance may persist for several days after phenobarbital is discontinued.
Increased lidocaine clearance, however, appears to be of minor clinical significance since IV lidocaine is usually titrated to response. Moderate Caution is advised if combining topical local anesthetics. The toxic effects of local anesthetics are additive. In addition, rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine-containing products. Clinicians should closely monitor patients for the development of methemoglobinemia when a combination local anesthetic is used during a procedure.
If a patient becomes cyanotic or if elevated methemoglobin concentrations are suspected, immediately institute treatment to counteract methemoglobinemia such as administration of methylene blue as oxygen delivery is ineffective throughout the body until the condition is reversed. Major Caution is advised if amide local anesthetics are used concurrently with benzonatate.
Moderate Concomitant use of systemic lidocaine and bexarotene may decrease lidocaine plasma concentrations. Higher lidocaine doses may be required; titrate to effect. If lidocaine dose adjustments are made, re-adjust the dose upon completion of boceprevir treatment.
Although this interaction has not been studied, predictions about the interaction can be made based on the metabolic pathway of lidocaine. Lidocaine is partially metabolized by the hepatic isoenzyme CYP3A4; boceprevir inhibits this isoenzyme. Coadministration may result in elevated lidocaine plasma concentrations. Moderate Bosentan is an inducer of CYP3A4 enzymes, and may decrease plasma concentrations of drugs metabolized by these enzymes.
Caution is recommended when administering bosentan to patients receiving lidocaine as lidocaine is a CYP3A4 substrate. Moderate Monitor for decreased efficacy of lidocaine if coadministration with brigatinib is necessary. Major Avoid use of other local anesthetics for 96 hours after liposomal bupivacaine administration.
Liposomal bupivacaine administration may follow lidocaine administration after a delay of 20 minutes or more. Use lidocaine and other formulations of bupivacaine together with caution. Moderate Partial neuromuscular blockade has been reported with capreomycin after the administration of large intravenous doses or rapid intravenous infusion.
Lidocaine could potentiate the neuromuscular blocking effect of capreomycin by impairing transmission of impulses at the motor nerve terminals. If these drugs are used in combination, monitor patients for increased adverse effects. Moderate Concomitant use of systemic lidocaine and carbamazepine may decrease lidocaine plasma concentrations.
Moderate Monitor for lidocaine toxicity if coadministration with ceritinib is necessary. Concomitant treatment CYP3A4 inhibitors has the potential to increase lidocaine plasma levels by decreasing lidocaine clearance and prolonging the elimination half-life. Moderate Concomitant use of systemic lidocaine and chloramphenicol may increase lidocaine plasma concentrations by decreasing lidocaine clearance and therefore prolonging the elimination half-life. Moderate Use chloroprocaine and lidocaine together with caution.
Moderate Caution is advised if combining local anesthetics. A major cause of adverse reactions appears to be excessive plasma concentrations, which may be due to accidental intravascular administration, slow metabolic degradation, or overdosage. In addition to additive toxic effects, rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine-containing products.
Patients who are receiving other drugs that can cause methemoglobin formation, such as prilocaine, are at greater risk for developing methemoglobinemia. Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine: Moderate Concomitant use of systemic lidocaine and cimetidine may increase lidocaine plasma concentrations. Moderate Concomitant use of systemic lidocaine and ciprofloxacin may increase lidocaine plasma concentrations by decreasing lidocaine clearance and therefore prolonging the elimination half-life.
Moderate Concomitant use of systemic lidocaine and citalopram may increase lidocaine plasma concentrations by decreasing lidocaine clearance and therefore prolonging the elimination half-life. Cobicistat; Elvitegravir; Emtricitabine; Tenofovir Alafenamide: Moderate Colesevelam may decrease the absorption of lidocaine.
To minimize potential for interactions, consider administering lidocaine at least 1 hour before or at least 4 hours after colesevelam. Theoretically, similar pharmacokinetic effects could be seen with lidocaine. Treatment with lidocaine may be initiated no sooner than 1 week after completion of conivaptan therapy. Moderate Monitor for lidocaine-related adverse reactions and toxicities if coadministration with crizotinib is necessary.
Moderate Concomitant use of systemic lidocaine and cyclosporine may increase lidocaine plasma concentrations by decreasing lidocaine clearance and therefore prolonging the elimination half-life.
Moderate Concomitant use of systemic lidocaine and dabrafenib may decrease lidocaine plasma concentrations. Concomitant use may cause an increase in lidocaine concentrations, which could increase efficacy or toxicity. If lidocaine and dalfopristin; quinupristin is used concurrently, careful plasma lidocaine concentration monitoring is needed.
Patients receiving lidocaine should be closely monitored for toxicity if danazol is added to therapy. Major Darunavir can inhibit CYP3A4, an isoenzyme partially responsible for the metabolism of lidocaine. The concurrent use of systemic lidocaine and darunavir should be carefully monitored due to the potential for serious toxicity. Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir: Major Concomitant use of systemic lidocaine and deferasirox may alter lidocaine plasma concentrations; avoid concurrent use.
If use together is necessary, monitor patients closely for lidocaine toxicity and therapeutic efficacy. Moderate Delavirdine is a potent inhibitor of the CYP3A4 and increased plasma concentrations of drugs extensively metabolized by this enzyme, such as lidocaine, should be expected with concurrent use of delavirdine.
Moderate Concomitant use of systemic lidocaine and dexamethasone may decrease lidocaine plasma concentrations. Major Avoid concurrent use of quinidine with other antiarrhythmics with Class I activities, such as lidocaine. Concurrent use may result in additive or antagonistic cardiac effects and additive toxicity. Moderate Concomitant use of systemic lidocaine and diltiazem may increase lidocaine plasma concentrations by decreasing lidocaine clearance and therefore prolonging the elimination half-life.
Major The effects of concomitant administration of disopyramide with other antiarrhythmics could potentially be synergistic or antagonistic, and adverse cardiac effects could potentially be additive. Class IA antiarrhythmic agents are associated with proarrhythmias e. It may also be used to produce local anesthesia by injection of the solution close to the nerves whose conduction is to be cut off, or into the epidural space near the spinal cord, or by administering the solution into a vein in a limb that has been isolated from the circulation by means of a tourniquet bandage that stops the flow of blood from vessel by applying pressure.
Speak to your doctor if one of these applies to you before you are given this medicine. Lidocaine solution for injection is not recommended for use in neonates less than a month old. Other medicines and Lidocaine solution for injection Please tell your doctor or pharmacist if you are taking or have recently taken any other medicines. A large number of drugs can interact with Lidocaine Hydrochloride which can significantly alter their effects.
If adrenaline epinephrine is to be added to your lidocaine injection, you should also tell your doctor if you suffer from high blood pressure, shortage of blood supply to the brain, an overactive thyroid gland or if you are taking antidepressant drugs.
If you are about to receive a strong anesthetic to put you to sleep, you should tell your doctor if you have already received an injection of lidocaine containing adrenaline epinephrine.
If you are already taking one of these medicines, speak to your doctor before you receive Lidocaine Hydrochloride. Concomitant use of both fluvoxamine and a CYP3A4 inhibitor such as erythromycin can further increase lidocaine concentrations.
Because lidocaine possesses a narrow therapeutic window, doses of lidocaine may need to be adjusted accordingly. Conversely, reduced serum lidocaine concentrations may result from drugs that may stimulate the hepatic metabolism of lidocaine e. Narcotics are probably proconvulsants and this would support the evidence that lidocaine reduces the seizure threshold to fentanyl in man.
Opioid-antiemetic combination sometimes used for sedation in children could reduce the convulsant threshold to lidocaine and increase the CNS depressant effect. AAG concentrations may be reduced by oestrogens leading to a higher free fraction of lidocaine in women than in men and the free fraction is further increased during pregnancy and in women taking oral contraceptives or HRT.
Lidocaine given by epidural or paracervical block, especially in large doses, or by local perineal infiltration prior to delivery crosses rapidly into the foetal circulation. Elevated lidocaine levels may persist in the newborn for at least 48 hours after delivery. Foetal bradycardia or neonatal bradycardia, hypotonia or respiratory depression may occur. Lactation Small amounts of Lidocaine are secreted into breast milk and the possibility of an allergic reaction in the infant, albeit remote, should be borne in mind when using Lidocaine in nursing mothers.
Following regional blockade as when lidocaine is injected intrathecally or extradurally, hypotension, hypoventilation, Horners Syndrome and hypoglycaemia may be seen. The degree of these effects will depend on the dose and the height of the block. Urinary retention may occur following sacral or lumbar epidural block. It should not outlast the duration of the block. Apnoea and hemiparesis may occur following stellate ganglion block.
The probable cause is a direct injection of lidocaine into the vertebral or carotid arteries. Nervous system reactions may be excitatory and or depressant. Signs of CNS stimulation may be brief, or may not occur at all, so that the first signs of toxicity may be confusion and drowsiness, followed by coma and respiratory failure. Neurological complications of spinal anaesthesia include transient neurological symptoms such as pain of the lower back, buttock and legs.
These symptoms usually develop within twenty-four hours of anaesthesia and resolve within a few days.
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