This monograph discusses the use of the lidocaine; hydrocortisone products. Clinicians may wish to consult the individual monographs of hydrocortisone or lidocaine for more information about each specific agent.
Lidocaine and hydrocortisone are combined and used topically and rectally for the relief of inflammation, pain, and pruritus associated with minor skin irritations, hemorrhoids, and anal fissures. Lidocaine is a topical amide local anesthetic that provides relief of pain and itching; hydrocortisone is a corticosteroid that has antiinflammatory, antipruritic, and vasoconstrictive properties. Several different formulations are available, including creams, gels, and lotions; these combinations are for prescription use only. Lidocaine and hydrocortisone were initially marketed for use before 1962, which is when Congress passed the amended Federal Food, Drug, and Cosmetic Act requiring that the FDA establish both safety and efficacy for all subsequently approved drugs. Lidocaine; Hydrocortisone lidocaine is an unapproved marketed drug that has not been formally evaluated by the FDA.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Topical Administration
Cream/Ointment/Lotion Formulations
-Lotion is for topical use only. Do not apply in the mouth, ears, or eyes.
-Wash hands before and after application.
-Apply as a thin film to the cleansed affected area.
Rectal Administration
Topical Rectal Administration:
-For topical use to the perianal area only. Do not apply in the mouth, ears, or eyes.
-Wash hands before and after application.
-Apply as a thin film to the cleansed affected area.
Rectal Administration (products with applicators):
-For rectal and perianal use only. Do not apply in the mouth, ears, eyes, or to other areas.
-Wash hands before and after application.
-Remove cap and foil seal and screw the applicator tip firmly onto the end of the tube. Do not over tighten.
-While holding the tube, squeeze the tube to fill the applicator until a small amount of cream shows and lubricate the end of the tip with cream.
-Gently insert applicator tip with attached tube into anal area. Squeeze the body of the tube as it is moved around the areas of discomfort, and lastly, around and in the anal opening.
-Do not completely insert the applicator and tube into the anus or insert deep into the rectum. Do not insert a loose applicator tip into the anus or rectum.
-Once application is completed, the tube and applicator tip should be gently removed from the area and disposed.
This monograph discusses the use of the lidocaine; hydrocortisone. Clinicians may wish to consult the individual monographs of lidocaine or hydrocortisone for more information about each specific agent.
After topical or rectal administration of lidocaine; hydrocortisone, there may be skin irritation (i.e., transient stinging or burning from open areas of skin), transient skin hypopigmentation, or erythema of the skin. Topical hydrocortisone may also produce pruritus, maceration of the skin, acneiform rash, perioral dermatitis and allergic contact dermatitis, folliculitis, miliaria, hypertrichosis, secondary infection, skin hypopigmentation, xerosis, and striae. Prolonged use of topical corticosteroids may result in skin atrophy as well as atrophy of subcutaneous tissues; skin atrophy may occur even with short-term use on intertriginous or flexor areas, or on the face.
Systemic absorption of topical lidocaine; hydrocortisone is assumed minimal but theoretically could cause systemic adverse reactions, especially if applied to a large surface area or with the use of occlusive dressings. Rectal administration may increase systemic absorption. Systemic absorption of topical corticosteroids can produce reversible hypothalamic-pituitary-adrenal (HPA) suppression with possible adrenocortical insufficiency after stopping treatment. In some patients, systemic absorption can produce manifestations of Cushing's syndrome. Manifestations of adrenocortical insufficiency in children include linear growth inhibition, delayed weight gain, low plasma cortisol concentrations, increased intracranial pressure, and absence of response to ACTH stimulation. Clinical signs of increased intracranial pressure include bulging fontanelles, headache, and bilateral papilledema. Recovery of HPA axis function is generally prompt and complete upon discontinuation of the topical corticosteroid. Infrequently, signs and symptoms of corticosteroid withdrawal may occur, requiring supplemental systemic corticosteroids.
Systemic absorption of topical steroids has produced hyperglycemia and glycosuria in some patients. Lidocaine; hydrocortisone should be used with caution in patients with diabetes mellitus.
Systemic adverse reactions related to local anesthetic actions following appropriate use of lidocaine; hydrocortisone products are unlikely. However, rarely systemic toxicity may be possible. Signs of CNS toxicity may start at plasma concentrations of lidocaine as low as 1000 ng/mL, although CNS toxicity is typically observed around 5000 ng/mL. Lidocaine induced CNS toxicity usually presents with symptoms of a CNS stimulation such as confusion, dizziness, tinnitus, blurred vision, tremor, and/or seizures. Local anesthetic CNS toxicity appear to occur before cardiotoxic effects. Depression of cardiac excitability and contractility may cause AV block, ventricular arrhythmias, or cardiac arrest. Examples of other possible adverse cardiovascular effects include angina, QT prolongation, PR prolongation, atrial fibrillation, sinus bradycardia, hypotension, palpitations, syncope, and cardiovascular collapse. General supportive physiologic measures such as oxygen therapy, assisted ventilation, and IV fluids are usually used in patients who develop toxicity.
Methemoglobinemia has been reported with local anesthetic use. Signs and symptoms of methemoglobinemia may occur immediately or may be delayed some hours after local anesthetic exposure and are characterized by cyanotic skin discoloration and abnormal coloration of the blood. Other symptoms may include headache, rapid heart rate, shortness of breath, dizziness, and drowsiness. Since methemoglobin concentrations may continue to rise, immediately discontinue lidocaine; hydrocortisone to avoid serious central nervous system and cardiovascular adverse events including seizures, coma, arrhythmias, and death. Depending on the severity of symptoms, patients may require supportive care, such as oxygen therapy and hydration. More severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
This monograph discusses the use of the lidocaine; hydrocortisone. Clinicians may wish to consult the individual monographs of lidocaine or hydrocortisone for more information about each specific agent.
Lidocaine; hydrocortisone is contraindicated in patients who are allergic to or have a known or suspected hypersensitivity to hydrocortisone (corticosteroid hypersensitivity), hypersensitivity to lidocaine (amide local anesthetic hypersensitivity) or any ingredient or excipient in these products. True corticosteroid hypersensitivity reactions are rare. While a hypersensitivity reaction could be to a specific salt of the corticosteroid (i.e., hydrocortisone sodium succinate), patients who have demonstrated a prior hypersensitivity reaction to hydrocortisone should receive any form of hydrocortisone with extreme caution. It is possible, though also rare, that such patients will display cross-hypersensitivity to other corticosteroids; there have been reports that a cross-sensitivity between hydrocortisone and methylprednisolone may exist. It is advisable that patients who have a hypersensitivity reaction to any corticosteroid undergo skin testing, which, although not a conclusive predictor, may help to determine if hypersensitivity to another corticosteroid exists. Such patients should be carefully monitored during and following the administration of any corticosteroid.
Systemic absorption of topical corticosteroids can aggravate Cushing's syndrome and should be avoided in patients with Cushing's syndrome. Prolonged administration of pharmacological doses of topical preparations of corticosteroids may result in systemic absorption which can produce hypothalamic-pituitary-adrenal (HPA) suppression and/or manifestations of Cushing's syndrome in some patients. Conditions that increase systemic absorption of topical corticosteroids or lidocaine include use over large surface areas, prolonged use, use in areas where the epidermal barrier is disrupted (i.e., skin abrasion or skin atrophy or thinning), and the use of an occlusive dressing. Patients receiving large doses of lidocaine; hydrocortisone applied to a large surface area should be evaluated periodically for evidence of HPA axis suppression by using urinary free cortisol and ACTH stimulation tests. If these effects are noted, an attempt should be made to withdraw the drug, to reduce the frequency of application, or to substitute a less potent corticosteroid.
Lidocaine; hydrocortisone should be used with caution in patients with diabetes mellitus. Systemic absorption of topical steroids has produced hyperglycemia and glycosuria in some patients.
In the presence of a dermatological infection, the use of an appropriate antifungal or antibacterial agent should be instituted. If a favorable response does not occur promptly, the corticosteroid should be discontinued until the infection has been adequately controlled. Lidocaine; hydrocortisone is contraindicated for treating tuberculosis, fungal infection lesions, viral infection of the skin (i.e., vaccinia, varicella or acute herpes infection).
Lidocaine; hydrocortisone is for topical or rectal administration only; accidental exposure or ingestion should be avoided due to the potential for toxicity. Avoid ocular exposure and exposure to mucous membranes. Inadvertent ophthalmic administration may cause severe ocular irritation and loss of eye surface sensation reducing protective reflexes and resulting in corneal irritation and possibly abrasion. If eye contact occurs, rinse out the eye immediately with saline or water and protect the eye surface until sensation is restored. Also avoid otic administration. Lidocaine-induced ototoxicity has been observed in animals when instilled in the middle ear; any situation where lidocaine penetrates beyond the tympanic membrane into the middle ear is contraindicated.
According to the manufacturer, lidocaine; hydrocortisone should be used cautiously in geriatric patients or very ill patients. Repeated doses of topical lidocaine may cause a significant increase in blood concentrations with each successive dose. These increases may be poorly tolerated, particularly by the elderly or acutely ill. Geriatric patients may also be more likely to experience skin atrophy secondary to corticosteroid use.
According to the manufacturers, lidocaine; hydrocortisone should be used cautiously in those with impaired liver function and those with significant hepatic disease. Conditions that reduce hepatic blood flow such as hepatic disease may reduce hepatic metabolism of lidocaine and lead to drug accumulation, increasing the risk of developing systemic toxicity.
The safety and clinical efficacy of lidocaine; hydrocortisone products have not been established in neonates, infants, children or adolescents. Repeated doses of topical or rectal lidocaine may cause an increase in blood concentrations with each successive dose and these increases may be poorly tolerated, particularly by young or debilitated pediatric patients. Pediatric patients may also absorb larger amounts of topical corticosteroids due to a larger skin surface area to body weight ratio, and therefore are more susceptible to developing systemic toxicity. Hypothalamic-pituitary-adrenal (HPA) axis suppression, Cushing's syndrome, and increased intracranial pressure have been reported in pediatric patients receiving topical corticosteroids. Chronic corticosteroid therapy in children may interfere with growth and development, resulting in growth inhibition.
Lidocaine; hydrocortisone is classified in FDA pregnancy risk category C. There are no adequate and well-controlled studies in pregnant women. According to the manufacturer, lidocaine; hydrocortisone should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. Do not use extensively, in large amounts, or for prolonged periods of time in pregnant women.
According to the manufacturer, lidocaine; hydrocortisone should be used with caution in breast-feeding women. Lidocaine is excreted into breast milk; however, the clinical significance of this is unknown. An alternative, should corticosteroid treatment be needed, would be to use topical hydrocortisone products that do not contain lidocaine. While the American Academy of Pediatrics does not comment on the use of hydrocortisone during breast-feeding, it does consider other corticosteroids (prednisone and prednisolone) to be usually compatible with breast-feeding. It is not known whether topical administration of hydrocortisone could result in sufficient systemic absorption to produce detectable quantities in breast milk; however, increased blood pressure has been reported in an infant whose mother applied a topical corticosteroid ointment directly to the nipples. If applied topically, care should be used to ensure the infant will not come into direct contact with the area of application. Most authorities recommend caution when prescribing topical corticosteroids to breast-feeding women. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.
Methemoglobinemia has been reported with local anesthetic use. Although all patients are at risk for methemoglobinemia, patients with glucose-6-phosphate dehydrogenase deficiency (G6PD deficiency), preexisting (congenital or idiopathic) methemoglobinemia, cardiac or pulmonary compromise (cardiac disease or pulmonary disease), those younger than 6 months, and those with concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing methemoglobinemia. Monitor such patients closely for signs and symptoms of methemoglobinemia if a local anesthetic must be used. Signs of methemoglobinemia may occur immediately or may be delayed hours after exposure. Immediately discontinue the local anesthetic to avoid serious central nervous system and cardiovascular adverse events, as methemoglobin concentrations may continue to rise. Patients may require supportive care such as oxygen therapy and hydration. More severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
For the treatment of mild pain and pruritus due to pruritic eczema, skin abrasion, minor burns, insect bites or stings, and similar conditions of the skin and mucous membranes.:
NOTE: These products have not been evaluated by the FDA for safety and clinical efficacy for the conditions listed.
Topical dosage:
Adults: Apply topically to the affected area(s) twice daily. Patients should be instructed to consult their health care provider if condition worsens or does not respond to repeated courses of lidocaine; hydrocortisone.
For the treatment of itching, pain, soreness and discomfort due to hemorrhoids, anal fissures, pruritus ani and similar conditions of the anal area:
Rectal Topical dosage:
Adults: Dependent on product selected, 1 applicatorful rectally twice daily OR applied topically to the affected area surrounding the rectum 2 to 3 times per day. Follow the directions on the product label. These products have not been evaluated by the FDA for safety and clinical efficacy for the conditions listed; they are not for prolonged use. Topical anesthetics or anti-inflammatory products are included in the initial management of acute anal fissures as they provide symptomatic relief of pain and bleeding with few side effects.
Maximum Dosage Limits:
-Adults
3 applications/day topically; 2 applications/day rectally.
-Geriatric
3 applications/day topically; 2 applications/day rectally.
-Adolescents
Safety and efficacy have not been established.
-Children
Safety and efficacy have not been established.
-Infants
Safety and efficacy have not been established.
-Neonates
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available. Use cautiously in patients with hepatic disease; repeated doses of topically applied lidocaine may result in drug accumulation in patients with hepatic impairment.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
Adapalene; Benzoyl Peroxide: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
Benzoyl Peroxide: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
Benzoyl Peroxide; Clindamycin: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
Benzoyl Peroxide; Erythromycin: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
Benzoyl Peroxide; Sulfur: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
Calamine; Pramoxine: (Moderate) Caution is advised if combining local anesthetics. The toxic effects of local anesthetics are additive. 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. 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. Patients who are receiving other drugs that can cause methemoglobin formation, such as prilocaine, are at greater risk for developing methemoglobinemia.
Clindamycin; Adapalene; Benzoyl Peroxide: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
Dibucaine: (Moderate) Caution is advised if combining local anesthetics. The toxic effects of local anesthetics are additive. 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. 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. Patients who are receiving other drugs that can cause methemoglobin formation, such as prilocaine, are at greater risk for developing methemoglobinemia.
Ethyl Chloride: (Moderate) Caution is advised if combining local anesthetics. The toxic effects of local anesthetics are additive. 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. 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. Patients who are receiving other drugs that can cause methemoglobin formation, such as prilocaine, are at greater risk for developing methemoglobinemia.
Hydrocortisone; Pramoxine: (Moderate) Caution is advised if combining local anesthetics. The toxic effects of local anesthetics are additive. 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. 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. Patients who are receiving other drugs that can cause methemoglobin formation, such as prilocaine, are at greater risk for developing methemoglobinemia.
Menthol; Pramoxine: (Moderate) Caution is advised if combining local anesthetics. The toxic effects of local anesthetics are additive. 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. 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. Patients who are receiving other drugs that can cause methemoglobin formation, such as prilocaine, are at greater risk for developing methemoglobinemia.
Pramoxine: (Moderate) Caution is advised if combining local anesthetics. The toxic effects of local anesthetics are additive. 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. 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. Patients who are receiving other drugs that can cause methemoglobin formation, such as prilocaine, are at greater risk for developing methemoglobinemia.
Pramoxine; Zinc Acetate: (Moderate) Caution is advised if combining local anesthetics. The toxic effects of local anesthetics are additive. 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. 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. Patients who are receiving other drugs that can cause methemoglobin formation, such as prilocaine, are at greater risk for developing methemoglobinemia.
Tretinoin; Benzoyl Peroxide: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
Lidocaine; hydrocortisone topical or rectal products are used to reduce local pain, inflammation, and pruritus.
-Lidocaine: Lidocaine is a local amide anesthetic that interferes with the transmission of impulses along sensory nerve fibers to relieve pain, itching, and irritation. Local anesthetics block both the initiation and conduction of nerve impulses from sensory nerves by decreasing the permeability of the neuronal membrane to sodium ions. This reversibly stabilizes the membrane and inhibits depolarization, resulting in the failure of a propagated action potential and subsequent conduction blockade.
-Hydrocortisone: Hydrocortisone is a corticosteroid that exhibits anti-inflammatory, antipruritic, and vasoconstrictive properties. The exact mechanism of anti-inflammatory activity is unclear for topical steroids. However, there is some evidence that a correlation exists between vasoconstrictor potency and therapeutic efficacy. Corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins (lipocortins). These proteins may control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid, which is released from membrane phospholipids by phospholipase A2. Early anti-inflammatory effects of topical corticosteroids include the inhibition of macrophage and leukocyte movement and activity in the inflamed area by reversing vascular dilation and permeability. Later inflammatory processes such as capillary production, collagen deposition, and keloid (scar) formation also are inhibited by corticosteroids. Clinically, these actions correspond to decreased edema, erythema, pruritus, plaque formation and scaling of the affected skin.
Lidocaine; hydrocortisone products are administered topically or rectally. The amount of systemic absorption from these routes is unclear.
-Lidocaine: Any systemically absorbed lidocaine crosses the blood-brain and placental barriers, presumably through passive diffusion. It is rapidly metabolized by the liver and its metabolites are excreted by the kidneys. More than 98% of an absorbed dose can be recovered in the urine as metabolites or parent drug. Less than 10% of lidocaine is excreted unchanged in adults.
-Hydrocortisone: Any systemically absorbed hydrocortisone is bound to some plasma proteins. It is metabolized by the liver to inactive metabolites. These inactive metabolites, as well as a small portion of unchanged drug, are excreted by the kidneys in the urine. Some metabolites are also excreted into the bile.
-Route-Specific Pharmacokinetics
Topical Route
-Lidocaine: Following topical administration to the mucous membranes, the rate and extent of systemic absorption of lidocaine depends on the site of application, duration of exposure, concentration, and total dosage. It is not known if topical lidocaine is metabolized in the skin. The onset of action of lidocaine ointment is 3 to 5 minutes.
-Hydrocortisone: The extent of percutaneous absorption of topical steroids is determined by many factors including the vehicle, the integrity of the epidermal barrier, and the use of occlusive dressings. Hydrocortisone is absorbed through normal intact skin. Inflammation or inflammatory disease processes in the skin can increase percutaneous absorption. Occlusive dressings substantially increase percutaneous absorption of steroids. Topical preparations distribute throughout the area of application and are usually metabolized in the skin. If absorbed systemically, topical corticosteroids follow the same pharmacokinetic pathways of systemic corticosteroids.
Other Route(s)
Rectal route
Specific information on the systemic absorption of lidocaine; hydrocortisone after topical application to the rectal area is unknown. The rate and extent of absorption of lidocaine depends on the site of application, duration of exposure, concentration, and total dosage.