Product Information
Registration Status: ActiveCANESTEN PLUS ANTIFUNGAL CREAM is approved to be sold in Singapore with effective from 2015-11-27. It is marketed by BAYER (SOUTH EAST ASIA) PTE LTD, with the registration number of SIN14898P.
This product contains Hydrocortisone 1g/100g, and Clotrimazole 1g/100g in the form of CREAM. It is approved for TOPICAL use.
This product is manufactured by Kern Pharma in SPAIN.
It is a Pharmacy Only Medicine that can be obtained from a pharmacist at a retail pharmacy.
Description
The main glucocorticoid secreted by the adrenal cortex. Its synthetic counterpart is used, either as an injection or topically, in the treatment of inflammation, allergy, collagen diseases, asthma, adrenocortical deficiency, shock, and some neoplastic conditions. [PubChem]
Indication
For the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. Also used to treat endocrine (hormonal) disorders (adrenal insufficiency, Addisons disease). It is also used to treat many immune and allergic disorders, such as arthritis, lupus, severe psoriasis, severe asthma, ulcerative colitis, and Crohn's disease.
Mechanism of Action
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.
Pharmacokinetics
- Absorption
- Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption.
- Distribution
- Metabolism
- Primarily hepatic via CYP3A4
- Elimination
Toxicity
Side effects include inhibition of bone formation, suppression of calcium absorption and delayed wound healing
Active Ingredient/Synonyms
(11alpha,14beta)-11,17,21-trihydroxypregn-4-ene-3,20-dione | (11beta)-11,17,21-Trihydroxypregn-4-ene-3,20-dione | 11beta-hydrocortisone | 11beta,17alpha,21-Trihydroxy-4-pregnene-3,20-dione | 11β-hydrocortisone | 17-Hydroxycorticosterone | 4-Pregnen-11beta,17alpha,21-triol-3,20-dione | Cortisol | Hidrocortisona | Hydrocortisone | Hydrocortisonum | Kendall's compound F | Reichstein's substance M | Hydrocortisone |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.
Description
An imidazole derivative with a broad spectrum of antimycotic activity. It inhibits biosynthesis of the sterol ergostol, an important component of fungal cell membranes. Its action leads to increased membrane permeability and apparent disruption of enzyme systems bound to the membrane. [PubChem]
Indication
For the local treatment of oropharyngeal candidiasis and vaginal yeast infections, also used in fungal infections of the skin such as ringworm, athlete's foot, and jock itch.
Mechanism of Action
Clotrimazole interacts with yeast 14-α demethylase, a cytochrome P-450 enzyme that converts lanosterol to ergosterol, an essential component of the membrane. In this way, clotrimazole inhibits ergosterol synthesis, resulting in increased cellular permeability. Clotrimazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms and the uptake of purine, impair triglyceride and/or phospholipid biosynthesis, and inhibit the movement of calcium and potassium ions across the cell membrane by blocking the ion transport pathway known as the Gardos channel.
Pharmacokinetics
- Absorption
- Poorly and erratically absorbed orally, minimal vaginal or topical absorption.
- Distribution
- Metabolism
- Hepatic (metabolized to inactive metabolites)
- Elimination
Toxicity
Symptoms of overdose include erythema, stinging, blistering, peeling, edema, pruritus, urticaria, burning, and general irritation of the skin, and cramps.
Active Ingredient/Synonyms
1-((2-Chlorophenyl)diphenylmethyl)-1H-imidazole | 1-(alpha-(2-Chlorophenyl)benzhydryl)imidazole | 1-(O-Chloro-alpha,alpha-diphenylbenzyl)imidazole | 1-(o-Chloro-α,α-diphenylbenzyl)imidazole | 1-(o-Chlorotrityl)imidazole | 1-(α-(2-Chlorophenyl)benzhydryl)imidazole | Clotrimazole | Lotrimin (tn) | Mycelex (tn) | Clotrimazole |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.