Liprikaine

Liprikain Kremi (% 2.5 lidokain ve% 2.5 prilokain ötektik karışımı), aşağıdakiler için topikal bir anestezik olarak endikedir:

- normal bozulmamış cilt lokal analjezi için.

- genital mukoza zarları yüzeysel minör cerrahi ve infiltrasyon anestezisi için ön tedavi olarak.

Liprikain (lidokain ve prilokain) Hayvan çalışmalarında gözlenen ototoksik etkiler nedeniyle timpanik membranın ötesine orta kulağa nüfuz etme veya göç mümkün olduğunda krem herhangi bir klinik durumda önerilmez (bkz UYARILAR).

Adult Patients - Intact Skin

A thick layer of Liprikaine (lidocaine and prilocaine) Cream is applied to intact skin and covered with an occlusive dressing (see Instruction For Application).

Minor Dermal Procedures: For minor procedures such as intravenous cannulation and venipuncture, apply 2.5 grams of Liprikaine (lidocaine and prilocaine) Cream (1/2 the 5 g tube) over 20 to 25 cm² of skin surface for at least 1 hour. In controlled clinical trials using Liprikaine (lidocaine and prilocaine) Cream, two sites were usually prepared in case there was a technical problem with cannulation or venipuncture at the first site.

Major Dermal Procedures: For more painful dermatological procedures involving a larger skin area such as split thickness skin graft harvesting, apply 2 grams of Liprikaine (lidocaine and prilocaine) Cream per 10 cm² of skin and allow to remain in contact with the skin for at least 2 hours.

Adult Male Genital Skin: As an adjunct prior to local anesthetic infiltration, apply a thick layer of Liprikaine (lidocaine and prilocaine) Cream (1 g/10 cm²) to the skin surface for 15 minutes. Local anesthetic infiltration should be performed immediately after removal of Liprikaine (lidocaine and prilocaine) Cream.

Dermal analgesia can be expected to increase for up to 3 hours under occlusive dressing and persist for 1 to 2 hours after removal of the cream. The amount of lidocaine and prilocaine absorbed during the period of application can be estimated from the information in Table 2, ** footnote, in Individualization of Dose.

Adult Female Patients - Genital Mucous Membranes

For minor procedures on the female external genitalia, such as removal of condylomata acuminata, as well as for use as pretreatment for anesthetic infiltration, apply a thick layer (5-10 grams) of Liprikaine (lidocaine and prilocaine) Cream for 5 to 10 minutes.

a href="/script/main/art.asp?articlekey=24885">Occlusion is not necessary for absorption, but may be helpful to keep the cream in place. Patients should be lying down during the Liprikaine (lidocaine and prilocaine) Cream application, especially if no occlusion is used. The procedure or the local anesthetic infiltration should be performed immediately after the removal of Liprikaine (lidocaine and prilocaine) Cream.

Pediatric Patients - Intact Skin

The following are the maximum recommended doses, application areas and application times for Liprikaine (lidocaine and prilocaine) Cream based on a child's age and weight:

Please note: If a patient greater than 3 months old does not meet the minimum weight requirement, the maximum total dose of Liprikaine (lidocaine and prilocaine) Cream should be restricted to that which corresponds to the patient's weight. (see Instruction For Application).

Practitioners should carefully instruct caregivers to avoid application of excessive amounts of Liprikaine Cream (see PRECAUTIONS).

When applying Liprikaine (lidocaine and prilocaine) Cream to the skin of young children, care must be taken to maintain careful observation of the child to prevent accidental ingestion of Liprikaine (lidocaine and prilocaine) Cream or the occlusive dressing. A secondary protective covering to prevent inadvertent disruption of the application site may be useful.

Liprikaine (lidocaine and prilocaine) Cream should not be used in neonates with a gestational age less than 37 weeks nor in infants under the age of 12 months who are receiving treatment with methemoglobin-inducing agents (see Methemoglobinemia subsection of WARNINGS).

When Liprikaine Cream (lidocaine 2.5% and prilocaine 2.5%) is used concomitantly with other products containing local anesthetic agents, the amount absorbed from all formulations must be considered (see Individualization of Dose). The amount absorbed in the case of Liprikaine (lidocaine and prilocaine) Cream is determined by the area over which it is applied and the duration of application under occlusion (see Table 2, ** footnote, in Individualization of Dose).

Although the incidence of systemic adverse reactions with Liprikaine (lidocaine and prilocaine) Cream is very low, caution should be exercised, particularly when applying it over large areas and leaving it on for longer than 2 hours. The incidence of systemic adverse reactions can be expected to be directly proportional to the area and time of exposure (see Individualization of Dose).

Instruction For Application

To measure 1 gram of Liprikaine (lidocaine and prilocaine) , the Cream should be gently squeezed out of the tube as a narrow strip that is 1.5 inches (3.8 cm) long and 0.2 inches (5 mm) wide. The strip of Liprikaine (lidocaine and prilocaine) cream should be contained within the lines of the diagram shown below.

≈1 g strip
1.5 X 0.2 inches

Use the number of strips that equals your dose, like the examples in the table below.

Dosing Information

1 gram = 1 strip
2 grams = 2 strips
2.5 grams = 2.5 strips

For adult and pediatric patients, apply ONLY as prescribed by your physician.

If your child is below the age of 3 months or small for their age, please inform your doctor before applying Liprikaine (lidocaine and prilocaine) Cream, which can be harmful, if applied over too much skin at one time in young children.

When applying Liprikaine (lidocaine and prilocaine) to the intact skin of young children, it is important that they be carefully observed by an adult in order to prevent the accidental ingestion of or eye contact with Liprikaine Cream.

Liprikaine® (lidocaine and prilocaine) Cream must be applied to intact skin at least 1 hour before the start of a routine procedure and for 2 hours before the start of a painful procedure. A protective covering of the Cream is not necessary for absorption but may be helpful to keep the cream in place.

If using a protective covering, your doctor will remove it, wipe off the Liprikaine® (lidocaine and prilocaine) Cream, clean the entire area with an antiseptic solution before the procedure. The duration of effective skin anesthesia will be at least 1 hour after removal of the protective covering.

PRECAUTIONS

1. Do not apply near eyes or on open wounds.
2. Keep out of reach of children.
3. If your child becomes very dizzy, excessively sleepy, or develops duskiness of the face or lips after applying Liprikaine (lidocaine and prilocaine) Cream, remove the cream and contact the child's physician at once.

Liprikaine Cream (lidocaine 2.5% and prilocaine 2.5%) is contraindicated in patients with a known history of sensitivity to local anesthetics of the amide type or to any other component of the product.

WARNINGS

Application of Liprikaine (lidocaine and prilocaine) Cream to larger areas or for longer times than those recommended could result in sufficient absorption of lidocaine and prilocaine resulting in serious adverse effects (see Individualization of Dose).

Patients treated with class III anti-arrhythmic drugs (eg, amiodarone, bretylium, sotalol, dofetilide) should be under close surveillance and ECG monitoring considered, because cardiac effects may be additive.

Studies in laboratory animals (guinea pigs) have shown that Liprikaine (lidocaine and prilocaine) Cream has an ototoxic effect when instilled into the middle ear. In these same studies, animals exposed to Liprikaine (lidocaine and prilocaine) Cream only in the external auditory canal, showed no abnormality. Liprikaine (lidocaine and prilocaine) Cream should not be used in any clinical situation when its penetration or migration beyond the tympanic membrane into the middle ear is possible.

Methemoglobinemia: Liprikaine (lidocaine and prilocaine) Cream should not be used in those rare patients with congenital or idiopathic methemoglobinemia and in infants under the age of twelve months who are receiving treatment with methemoglobin-inducing agents.

Very young patients or patients with glucose-6-phosphate dehydrogenase deficiencies are more susceptible to methemoglobinemia.

Patients taking drugs associated with drug-induced methemoglobinemia such as sulfonamides, acetaminophen, acetanilid, aniline dyes, benzocaine, chloroquine, dapsone, naphthalene, nitrates and nitrites, nitrofurantoin, nitroglycerin, nitroprusside, pamaquine, para-aminosalicylic acid, phenacetin, phenobarbital, phenytoin, primaquine, quinine, are also at greater risk for developing methemoglobinemia.

There have been reports of significant methemoglobinemia (20-30%) in infants and children following excessive applications of Liprikaine (lidocaine and prilocaine) Cream. These cases involved the use of large doses, larger than recommended areas of application, or infants under the age of 3 months who did not have fully mature enzyme systems. In addition, a few of these cases involved the concomitant administration of methemoglobin-inducing agents. Most patients recovered spontaneously after removal of the cream. Treatment with IV methylene blue may be effective if required.

Physicians are cautioned to make sure that parents or other caregivers understand the need for careful application of Liprikaine (lidocaine and prilocaine) Cream, to ensure that the doses and areas of application recommended in Table 2 are not exceeded (especially in children under the age of 3 months) and to limit the period of application to the minimum required to achieve the desired anesthesia.

Neonates and infants up to 3 months of age should be monitored for Met-Hb levels before, during, and after the application of Liprikaine (lidocaine and prilocaine) Cream, provided the test results can be obtained quickly.

PRECAUTIONS

General

Repeated doses of Liprikaine Cream may increase blood levels of lidocaine and prilocaine. Liprikaine (lidocaine and prilocaine) Cream should be used with caution in patients who may be more sensitive to the systemic effects of lidocaine and prilocaine including acutely ill, debilitated, or elderly patients.

Liprikaine (lidocaine and prilocaine) Cream should not be applied to open wounds.

Care should be taken not to allow Liprikaine (lidocaine and prilocaine) Cream to come in contact with the eye because animal studies have demonstrated severe eye irritation. Also the loss of protective reflexes can permit corneal irritation and potential abrasion. Absorption of Liprikaine (lidocaine and prilocaine) Cream in conjunctival tissues has not been determined. If eye contact occurs, immediately wash out the eye with water or saline and protect the eye until sensation returns.

Patients allergic to paraaminobenzoic acid derivatives (procaine, tetracaine, benzocaine, etc.) have not shown cross sensitivity to lidocaine and/or prilocaine; however, Liprikaine (lidocaine and prilocaine) Cream should be used with caution in patients with a history of drug sensitivities, especially if the etiologic agent is uncertain.

Patients with severe hepatic disease, because of their inability to metabolize local anesthetics normally, are at greater risk of developing toxic plasma concentrations of lidocaine and prilocaine.

Lidocaine and prilocaine have been shown to inhibit viral and bacterial growth. The effect of Liprikaine (lidocaine and prilocaine) Cream on intradermal injections of livevaccines has not been determined.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis: Long-term studies in animals designed to evaluate the carcinogenic potential of lidocaine and prilocaine have not been conducted.

Metabolites of prilocaine have been shown to be carcinogenic in laboratory animals. In the animal studies reported below, doses or blood levels are compared with the Single Dermal Administration (SDA) of 60 g of Liprikaine (lidocaine and prilocaine) Cream to 400 cm² for 3 hours to a small person (50 kg). The typical application of Liprikaine (lidocaine and prilocaine) Cream for one or two treatments for venipuncture sites (2.5 or 5 g) would be 1/24 or 1/12 of that dose in an adult or about the same mg/kg dose in an infant.

Chronic oral toxicity studies of ortho-toluidine, a metabolite of prilocaine, in mice (450 to 7200 mg/m²; 60 to 960 times SDA) and rats (900 to 4,800 mg/m²; 60 to 320 times SDA) have shown that ortho-toluidine is a carcinogen in both species. The tumors included hepatocarcinomas/adenomas in female mice, multiple occurrences of hemangiosarcomas/hemangiomas in both sexes of mice, sarcomas of multiple organs, transitional-cell carcinomas/papillomas of urinary bladder in both sexes of rats, subcutaneous fibromas/fibrosarcomas and mesotheliomas in male rats, and mammary gland fibroadenomas/adenomas in female rats. The lowest dose tested (450 mg/m² in mice, 900 mg/m² in rats, 60 times SDA) was carcinogenic in both species. Thus the no-effect dose must be less than 60 times SDA. The animal studies were conducted at 150 to 2,400 mg/kg in mice and at 150 to 800 mg/kg in rats. The dosages have been converted to mg/m² for the SDA calculations above.

Mutagenesis: The mutagenic potential of lidocaine HCl has been tested in a bacterial reverse (Ames) assay in Salmonella, an in vitro chromosomal aberration assay using human lymphocytes and in an in vivo micronucleus test in mice. There was no indication of mutagenicity or structural damage to chromosomes in these tests.

Ortho-toluidine, a metabolite of prilocaine, at a concentration of 0.5 µg/mL was genotoxic in Escherichia coliDNA repair and phage-induction assays. Urine concentrates from rats treated with ortho-toluidine (300 mg/kg orally; 300 times SDA) were mutagenic when examined in Salmonella typhimurium in the presence of metabolic activation. Several other tests on ortho-toluidine, including reverse mutations in five different Salmonella typhimurium strains in the presence or absence of metabolic activation and a study to detect single strand breaks in DNA of V79 Chinese hamster cells, were negative.

Impairment of Fertility: See Use in Pregnancy.

Use in Pregnancy: Teratogenic Effects: Pregnancy Category B.

Reproduction studies with lidocaine have been performed in rats and have revealed no evidence of harm to the fetus (30 mg/kg subcutaneously; 22 times SDA). Reproduction studies with prilocaine have been performed in rats and have revealed no evidence of impaired fertility or harm to the fetus (300 mg/kg intramuscularly; 188 times SDA). There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, Liprikaine (lidocaine and prilocaine) Cream should be used during pregnancy only if clearly needed.

Reproduction studies have been performed in rats receiving subcutaneous administration of an aqueous mixture containing lidocaine HCl and prilocaine HCl at 1:1 (w/w). At 40 mg/kg each, a dose equivalent to 29 times SDA lidocaine and 25 times SDA prilocaine, no teratogenic, embryotoxic or fetotoxic effects were observed.

Labor and Delivery: Neither lidocaine nor prilocaine are contraindicated in labor and delivery. Should Liprikaine (lidocaine and prilocaine) Cream be used concomitantly with other products containing lidocaine and/or prilocaine, cumulative doses from all formulations must be considered.

Nursing Mothers: Lidocaine, and probably prilocaine, are excreted in human milk. Therefore, caution should be exercised when Liprikaine (lidocaine and prilocaine) Cream is administered to a nursing mother since the milk: plasma ratio of lidocaine is 0.4 and is not determined for prilocaine.

Pediatric Use: Controlled studies of Liprikaine (lidocaine and prilocaine) Cream in children under the age of seven years have shown less overall benefit than in older children or adults. These results illustrate the importance of emotional and psychological support of younger children undergoing medical or surgical procedures.

Liprikaine (lidocaine and prilocaine) Cream should be used with care in patients with conditions or therapy associated with methemoglobinemia (see Methemoglobinemia subsection of WARNINGS).

When using Liprikaine (lidocaine and prilocaine) Cream in young children, especially infants under the age of 3 months, care must be taken to insure that the caregiver understands the need to limit the dose and area of application, and to prevent accidental ingestion (see DOSAGE AND ADMINISTRATION and Methemoglobinemia).

In neonates (minimum gestation age: 37 weeks) and children weighing less than 20 kg, the area and duration of application should be limited (see TABLE 2 in Individualization of Dose).

Studies have not demonstrated the efficacy of Liprikaine (lidocaine and prilocaine) Cream for heel lancing in neonates.

Geriatric Use: Of the total number of patients in clinical studies of Liprikaine (lidocaine and prilocaine) Cream, 180 were age 65 to 74 and 138 were 75 and over. No overall differences in safety or efficacy were observed between these patients and younger patients. Other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

Plasma levels of lidocaine and prilocaine in geriatric and non-geriatric patients following application of a thick layer of Liprikaine (lidocaine and prilocaine) Cream are very low and well below potentially toxic levels. However, there are no sufficient data to evaluate quantitative differences in systemic plasma levels of lidocaine and prilocaine between geriatric and non-geriatric patients following application of Liprikaine (lidocaine and prilocaine) Cream.

Consideration should be given for those elderly patients who have enhanced sensitivity to systemic absorption. (See PRECAUTIONS.)

After intravenous dosing, the elimination half-life of lidocaine is significantly longer in elderly patients (2.5 hours) than in younger patients (1.5 hours). (See CLINICAL PHARMACOLOGY.)

Localized Reactions: During or immediately after treatment with Liprikaine (lidocaine and prilocaine) Cream on intact skin, the skin at the site of treatment may develop erythema or edema or may be the locus of abnormal sensation. Rare cases of discrete purpuric or petechial reactions at the application site have been reported. Rare cases of hyperpigmentation following the use of Liprikaine (lidocaine and prilocaine) Cream have been reported. The relationship to Liprikaine (lidocaine and prilocaine) Cream or the underlying procedure has not been established. In clinical studies on intact skin involving over 1,300 Liprikaine (lidocaine and prilocaine) Cream-treated subjects, one or more such local reactions were noted in 56% of patients, and were generally mild and transient, resolving spontaneously within 1 or 2 hours. There were no serious reactions that were ascribed to Liprikaine (lidocaine and prilocaine) Cream.

Two recent reports describe blistering on the foreskin in neonates about to undergo circumcision. Both neonates received 1.0 g of Liprikaine (lidocaine and prilocaine) Cream.

In patients treated with Liprikaine (lidocaine and prilocaine) Cream on intact skin, local effects observed in the trials included: paleness (pallor or blanching) 37%, redness (erythema) 30%, alterations in temperature sensations 7%, edema 6%, itching 2% and rash, less than 1%.

In clinical studies on genital mucous membranes involving 378 Liprikaine (lidocaine and prilocaine) Cream-treated patients, one or more application site reactions, usually mild and transient, were noted in 41% of patients. The most common application site reactions were redness (21%), burning sensation (17%) and edema (10%).

Allergic Reactions: Allergic and anaphylactoid reactions associated with lidocaine or prilocaine can occur. They are characterized by urticaria, angioedema, bronchospasm, and shock. If they occur they should be managed by conventional means. The detection of sensitivity by skin testing is of doubtful value.

Systemic (Dose Related) Reactions: Systemic adverse reactions following appropriate use of Liprikaine (lidocaine and prilocaine) Cream are unlikely due to the small dose absorbed (see Pharmacokinetics subsection of CLINICAL PHARMACOLOGY). Systemic adverse effects of lidocaine and/or prilocaine are similar in nature to those observed with other amide local anesthetic agents including CNS excitation and/or depression (light-headedness, nervousness, apprehension, euphoria, confusion, dizziness, drowsiness, tinnitus, blurred or double vision, vomiting, sensations of heat, cold or numbness, twitching, tremors, convulsions, unconsciousness, respiratory depression and arrest). Excitatory CNS reactions may be brief or not occur at all, in which case the first manifestation may be drowsiness merging into unconsciousness. Cardiovascular manifestations may include bradycardia, hypotension and cardiovascular collapse leading to arrest.

Peak blood levels following a 60 g application to 400 cm² of intact skin for 3 hours are 0.05 to 0.16 µg/mL for lidocaine and 0.02 to 0.10 µg/mL for prilocaine. Toxic levels of lidocaine ( > 5 µg/mL) and/or prilocaine ( > 6 µg/mL) cause decreases in cardiac output, total peripheral resistance and mean arterial pressure. These changes may be attributable to direct depressant effects of these local anesthetic agents on the cardiovascular system. In the absence of massive topical overdose or oral ingestion, evaluation should include evaluation of other etiologies for the clinical effects or overdosage from other sources of lidocaine, prilocaine or other local anesthetics. Consult the package inserts for parenteral Xylocaine (lidocaine HCl) or Citanest (prilocaine HCl) for further information for the management of overdose.

Liprikain Kremi, su emülsiyonunda bir yağ olarak formüle edilen% 2.5 lidokain ve% 2.5 prilokainin ötektik bir karışımıdır. Bu ötektik karışımda, her iki anestezik oda sıcaklığında sıvıdır (bkz AÇIKLAMA) ve hem prilokain hem de lidokainin penetrasyonu ve müteakip sistemik emilimi, kristal formundaki her bileşen% 2.5 topikal krem olarak ayrı ayrı uygulanırsa görülecek olanın üzerine çıkarılır.

Emilim: Liprikaine (lidokain ve prilokain) Kreminden sistematik olarak emilen lidokain ve prilokain miktarı, hem uygulama süresi hem de uygulandığı alanla doğrudan ilişkilidir. İki farmakokinetik çalışmada, 400 cm'ye 60 g Liprikain (lidokain ve prilokain) Krem (1.5 g lidokain ve 1.5 g prilokain) uygulandı² lateral uylukta bozulmamış cilt ve daha sonra tıkayıcı bir pansuman ile kaplanır. Denekler daha sonra deneklerin yarısının 3 saat sonra tıkayıcı pansuman ve artık krema çıkarıldığı, geri kalanı ise pansumanı 24 saat boyunca yerinde bıraktığı şekilde randomize edildi. Bu çalışmaların sonuçları aşağıda özetlenmiştir.

TABLO 1: Lidokain ve Prilokainin Liprikaine (lidokain ve prilokain) Kreminden Emilmesi: Normal Gönüllüler (N = 16)

60 g Liprikain (lidokain ve prilokain) Krem 400 cm'nin üzerine uygulandığında² 24 saat boyunca, lidokainin pik kan seviyeleri sistemik toksik seviyenin yaklaşık 1 / 20'sidir. Benzer şekilde, maksimum prilokain seviyesi toksik seviyenin yaklaşık 1 / 36'sıdır. Farmakokinetik bir çalışmada, 20 yetişkin erkek hastada 15 dakika boyunca 0.5 g ila 3.3 g arasında değişen dozlarda Liprikaine (lidokain ve prilokain) Krem penil cilde uygulandı. Liprikain (lidokain ve prilokain) sonrasında lidokain ve prilokainin plazma konsantrasyonları Bu çalışmada krem uygulaması sürekli düşüktü (lidokain için 2.5-16 ng / mL ve prilokain için 2.5-7 ng / mL). Liprikaine (lidokain ve prilokain) Kreminin kırık veya iltihaplı cilde veya 2.000 cm'ye uygulanması² veya her iki anestezinin daha fazlasının emildiği cildin daha fazlası, duyarlı bireylerde sistemik bir farmakolojik yanıt üretebilecek daha yüksek plazma seviyelerine neden olabilir.

Genital mukoza zarlarına uygulanan Liprikain (lidokain ve prilokain) Kreminin emilimi iki açık etiketli klinik çalışmada incelenmiştir. Yirmi dokuz hastaya vajinal forniklerde 10 ila 60 dakika uygulanan 10 g Liprikain (lidokain ve prilokain) Krem verildi. Liprikaine sonrası lidokain ve prilokainin plazma konsantrasyonları (lidokain ve prilokain) Bu çalışmalarda krem uygulaması lidokain için 148 ila 641 ng / mL ve prilokain için 40 ila 346 ng / mL ve maksimum konsantrasyona ulaşma süresi arasındaydı (tmax) lidokain için 21 ila 125 dakika ve prilokain için 21 ila 95 dakika arasında değişmektedir. Bu seviyeler, sistemik toksisiteye (lidokain ve prilokain için yaklaşık 5000 ng / mL) yol açması beklenen konsantrasyonların oldukça altındadır.

Dağıtım: Her ilaç intravenöz olarak uygulandığında, kararlı durum dağılım hacmi lidokain için 1.1 ila 2.1 L / kg'dır (ortalama 1.5, Â ± 0.3 SD, n = 13) ve 0.7 ila 4.4 L / kg'dır (ortalama 2.6, Â ± 1.3 SD, n = 13) prilokain için. Prilokain için daha büyük dağılım hacmi, eşit miktarda prilokain ve lidokain uygulandığında gözlenen daha düşük plazma prilokain konsantrasyonlarını üretir. Liprikain (lidokain ve prilokain) Kreminin uygulanmasıyla üretilen konsantrasyonlarda lidokain, başta alfa-1-asit glikoprotein olmak üzere plazma proteinlerine yaklaşık% 70 oranında bağlanır. Çok daha yüksek plazma konsantrasyonlarında (1 ila 4 ug / mL serbest baz) lidokainin plazma proteinlerine bağlanması konsantrasyona bağlıdır. Prilokain plazma proteinlerine% 55 bağlanır. Hem lidokain hem de prilokain, muhtemelen pasif difüzyonla plasental ve kan beyin bariyerini geçer.

Metabolizma: Lidokain veya prilokainin deride metabolize olup olmadığı bilinmemektedir. Lidokain, her ikisi de lidokain benzeri fakat daha az güçlü farmakolojik aktiviteye sahip olan monoetilglisinksilidid (MEGX) ve glisinksilidid (GX) dahil olmak üzere bir dizi metabolite karaciğer tarafından hızla metabolize edilir. 2,6-ksilidin metaboliti farmakolojik aktiviteye sahip değildir. İntravenöz uygulamayı takiben, serumdaki MEGX ve GX konsantrasyonları sırasıyla lidokain konsantrasyonlarının sırasıyla% 11 ila 36 ve% 5 ila 11'i arasında değişir. Prilokain, karaciğer ve böbreklerde, çeşitli metabolitlerin aralarına göre metabolize edilir orto-toluidin ve N-n-propilalanin. Plazma esterazları tarafından metabolize edilmez. Orto-toluidin metabolitinin çeşitli hayvan modellerinde kanserojen olduğu gösterilmiştir (bkz ÖNLEMLERİN kanserojenez alt bölümü). Ayrıca, orto-toluidin, 8 mg / kg'a yaklaşan sistemik prilokain dozlarını takiben methemoglobinemi üretebilir (bkz REKLAM REAKSİYONLARI). Çok genç hastalar, glikoz-6-fosfat dehidrojenaz eksiklikleri olan hastalar ve antimalaryaller ve sülfonamidler gibi oksitleyici ilaçlar alan hastalar methemoglobinemiye daha duyarlıdır (bkz ÖNLEMLERİN methemoglobinemi alt bölümü).

Eliminasyon: IV uygulamasını takiben lidokainin plazmadan terminal eliminasyon yarılanma ömrü yaklaşık 65 ila 150 dakikadır (ortalama 110, Â ± 24 SD, n = 13). Emilen bir lidokain dozunun% 98'inden fazlası idrarda metabolitler veya ana ilaç olarak geri kazanılabilir. Sistemik klerens 10 ila 20 mL / dak / kg'dır (ortalama 13, Â ± 3 SD, n = 13). Prilokainin eliminasyon yarılanma ömrü yaklaşık 10 ila 150 dakikadır (ortalama 70, Â ± 48 SD, n = 13). Sistemik klerens 18 ila 64 mL / dak / kg'dır (ortalama 38, Â ± 15 SD, n = 13). İntravenöz çalışmalar sırasında lidokainin eliminasyon yarılanma ömrü yaşlı hastalarda (2.5 saat) genç hastalara (1.5 saat) göre istatistiksel olarak anlamlı derecede daha uzundu. Yaşlı hastalarda prilokainin intravenöz farmakokinetiği üzerine bir çalışma mevcut değildir.

Pediatri : Bazı farmakokinetik (PK) verileri bebeklerde (1 aydan <2 yaşına kadar) ve çocuklarda (2 ila <12 yaş arası) mevcuttur. Bir PK çalışması 9 tam dönem yenidoğanda (ortalama yaş: 7 gün ve ortalama gebelik yaşı: 38.8 hafta) gerçekleştirildi. Çalışma sonuçları, yenidoğanların, önceki pediatrik PK çalışmalarında ve klinik çalışmalarda bulunanlarla karşılaştırılabilir plazma lidokain ve prilokain konsantrasyonlarına ve kan methemoglobin konsantrasyonlarına sahip olduğunu göstermektedir. Methemoglobin oluşumunda bir artış eğilimi vardı. Bununla birlikte, test sınırlamaları ve yenidoğanlardan toplanabilecek çok az miktarda kan nedeniyle, yukarıda bildirilen konsantrasyonlarda büyük farklılıklar bulunmuştur.

Özel Nüfuslar : Spesifik PK çalışması yapılmamıştır. Yarılanma ömrü kardiyak veya hepatik disfonksiyonda artabilir. Prilokain'in yarı ömrü hepatik veya böbrek fonksiyon bozukluğunda da artabilir, çünkü bu organların her ikisi de prilokain metabolizmasına katılır.