Lidocaine and Hydrocortisone
Lidocaine and Hydrocortisone Uses, Dosage, Side Effects, Food Interaction and all others data.
Hydrocortisone binds to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Specifically glucocorticoids induce lipocortin-1 (annexin-1) synthesis, which then binds to cell membranes preventing the phospholipase A2 from coming into contact with its substrate arachidonic acid. This leads to diminished eicosanoid production. The cyclooxygenase (both COX-1 and COX-2) expression is also suppressed, potentiating the effect. In other words, the two main products in inflammation Prostaglandins and Leukotrienes are inhibited by the action of Glucocorticoids. Glucocorticoids also stimulate the lipocortin-1 escaping to the extracellular space, where it binds to the leukocyte membrane receptors and inhibits various inflammatory events: epithelial adhesion, emigration, chemotaxis, phagocytosis, respiratory burst and the release of various inflammatory mediators (lysosomal enzymes, cytokines, tissue plasminogen activator, chemokines etc.) from neutrophils, macrophages and mastocytes. Additionally the immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.
Hydrocortisone is the most important human glucocorticoid. It is essential for life and regulates or supports a variety of important cardiovascular, metabolic, immunologic and homeostatic functions. Topical hydrocortisone is used for its anti-inflammatory or immunosuppressive properties to treat inflammation due to corticosteroid-responsive dermatoses. Glucocorticoids are a class of steroid hormones characterised by an ability to bind with the cortisol receptor and trigger a variety of important cardiovascular, metabolic, immunologic and homeostatic effects. Glucocorticoids are distinguished from mineralocorticoids and sex steroids by having different receptors, target cells, and effects. Technically, the term corticosteroid refers to both glucocorticoids and mineralocorticoids, but is often used as a synonym for glucocorticoid. Glucocorticoids suppress cell-mediated immunity. They act by inhibiting genes that code for the cytokines IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-8 and TNF-alpha, the most important of which is the IL-2. Reduced cytokine production limits T cell proliferation. Glucocorticoids also suppress humoral immunity, causing B cells to express lower amounts of IL-2 and IL-2 receptors. This diminishes both B cell clonal expansion and antibody synthesis. The diminished amounts of IL-2 also leads to fewer T lymphocyte cells being activated.
Trade Name | Lidocaine and Hydrocortisone |
Generic | Lidocaine hydrochloride + hydrocortisone acetate |
Type | Cream, Rectal Gel, Rectal Cream |
Therapeutic Class | |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Hydrocortisone Acetate is used for:
- Primary irritant dermatitis
- Contact allergic dermatitis
- Eczema: atopic, infantile, discoid, stasis
- Seborrheic dermatitis
- Lichen simplex and pruritus ani
- Flexural psoriasis
- Skin irritations, itching and rashes, for example those caused by insect bites, minor thermal burns, sunburn, etc
Lidocaine and Hydrocortisone is also used to associated treatment for these conditions: Acute, Inflammatory Superficial Cutaneous Lesions caused by susceptible bacteria, Adrenal cortical hypofunctions, Anal Fissures, Anal inflammation, Androgenital syndrome, Conjunctivitis, Conjunctivitis allergic, Corneal Inflammation, Dermatitis infected, Diaper Dermatitis, Eczema infected, Episcleritis, Hemorrhoids, Iridocyclitis, Iritis, Ocular Inflammation, Ocular Irritation, Postoperative pain, Proctitis, Pruritus, Pruritus Ani, Radiation Induced Proctitis, Rheumatoid Arthritis, Scleritis, Skin Infections, Skin Irritation, Superficial ocular bacterial infections caused by susceptible bacteria, Thyroiditis, Ulcerative Colitis, Anal eczema, Bacterial blepharitis, Corneal clouding, Corticosteroid responsive Dermatosis of the anal region, Corticosteroid-responsive dermatoses, Cryptitis, Localized uninfected hemorrhoids, Mild Anal Fissures, Pruritus associated with bowel movements, Skin and skin-structure infections caused by susceptible bacteria, Postoperative Eye Care
How Lidocaine and Hydrocortisone works
Hydrocortisone binds to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Specifically glucocorticoids induce lipocortin-1 (annexin-1) synthesis, which then binds to cell membranes preventing the phospholipase A2 from coming into contact with its substrate arachidonic acid. This leads to diminished eicosanoid production. The cyclooxygenase (both COX-1 and COX-2) expression is also suppressed, potentiating the effect. In other words, the two main products in inflammation Prostaglandins and Leukotrienes are inhibited by the action of Glucocorticoids. Glucocorticoids also stimulate the lipocortin-1 escaping to the extracellular space, where it binds to the leukocyte membrane receptors and inhibits various inflammatory events: epithelial adhesion, emigration, chemotaxis, phagocytosis, respiratory burst and the release of various inflammatory mediators (lysosomal enzymes, cytokines, tissue plasminogen activator, chemokines etc.) from neutrophils, macrophages and mastocytes. Additionally the immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.
Dosage
Lidocaine and Hydrocortisone dosage
Hydrocortisone cream should be applied in a thin smear to the affected area one to two times per day or as directed by the physician. The recommended duration of treatment is usually two weeks. For rectal use apply to the irritated anorectal tissue in the morning and at evening and after each bowel movement for two to six days.
Side Effects
Hydrocortisone Acetate 1% cream is usually well-tolerated, but if signs of hypersensitivity appear, application should be stopped.
Toxicity
Side effects include inhibition of bone formation, suppression of calcium absorption and delayed wound healing
Precaution
In infants and children, long-term continuous topical therapy should be avoided where possible, as adrenal suppression can occur. As with all corticosteroids, prolonged application to the face is undesirable.
Elimination Route
Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption.
Half Life
6-8 hours
Elimination Route
Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.
Pregnancy & Breastfeeding use
There is inadequate evidence for safety in human pregnancy. It is recommended that topical corticosteroids should not be used extensively during pregnancy. It is highly unlikely that sufficiently high blood levels of Hydrocortisone are achieved during topical therapy to reach breast milk.
Contraindication
Contraindicated in infections (bacterial; viral; fungal), skin ulcers, hypersensitivity to the preparation
Acute Overdose
Acute overdosage is very unlikely to occur, however, in the case of chronic overdosage or misuse, the features of hypercorticism may appear and in this situation topical steroids should be discontinued
Storage Condition
Store in a cool and dry place, away from light. Keep out of reach of children.
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