Product Information
Registration Status: ActiveCANDID-B CREAM is approved to be sold in Singapore with effective from 1990-02-21. It is marketed by UNI DRUG HOUSE, with the registration number of SIN03941P.
This product contains Beclomethasone Dipropionate 0.025% w/w, and Clotrimazole 1% w/w in the form of CREAM. It is approved for TOPICAL use.
This product is manufactured by GLENMARK PHARMACEUTICALS LTD in INDIA.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Beclomethasone dipropionate is a prodrug of the free form, beclomethasone (beclomethasone-17-monopropionate). An anti-inflammatory, synthetic corticosteroid, it is used topically as an anti-inflammatory agent and in aerosol form for the treatment of asthma and allergic rhinitis (seasonal and perennial). Beclometasone dipropionate is also being investigated for oral treatment in mild-to-moderate Crohn's disease of ileal or ileal-right colonic localisation and for "topical" use mild-to-moderate graft versus host disease. It is marketed under several brand names such as Qnasl (US) and Rivanase AQ (Canada).
Indication
Used in the maintenance treatment of asthma as prophylactic therapy in patients 5 years of age and older, and in treating symptoms for allergic rhinitis (seasonal or perennial) in patients 12 years of age and older. Also being investigated for oral treatment in mild-to-moderate Crohn's disease of ileal or ileal-right colonic localisation and for "topical" use mild-to-moderate graft versus host disease.
Mechanism of Action
Unbound corticosteroids cross cell membranes and bind with high affinity to specific cytoplasmic receptors. The result includes inhibition of leukocyte infiltration at the site of inflammation, interference in the function of mediators of inflammatory response, suppression of humoral immune responses, and reduction in edema or scar tissue. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. For the investigated use in the treatment of GvHD or Crohn's, beclometasone acts by binding to interleukin-13 to inhibit cytokines, which in turn inhibits inflammatory chemicals downstream.
Pharmacokinetics
- Absorption
- Mean peak plasma concentration was 88pg/ml at 0.5 hour.
- Distribution
- The steady state volume of distribution for beclomethasone dipropionate is 20 L, and for it's active metabolite, beclomethasone-17-monopropionate, it is much larger at 424 L.
- Metabolism
- Metabolism mediated via esterase enzymes that are found in most tissues. Undergoes rapid and extensive conversion to beclomenthasone-17-monopropionate (17-BMP) during absorption
- Elimination
Clearance
High plasma clearance after intravenous administration (150 and 120 L/hour).
Toxicity
The acute toxicity of beclometasone dipropionate is low. The only harmful effect that follows inhalation of large amounts of the drug over a short period of time is suppression of hypothalamic-pituitary-adrenal (HPA) function. Chronic: The excessive use of beclometasone dipropionate over a long period could lead to adrenal suppression.
Active Ingredient/Synonyms
(11β,16β)-9-chloro-11-hydroxy-16-methyl-17,21-bis(1-oxopropoxy)pregna-1,4-diene-3,20-dione | 9-chloro-11β-hydroxy-16β-methylpregna-1,4-diene-3,20-dione 17,21-dipropionate | 9-chloro-16β-methyl-11β,17,21-trihydroxypregna-1,4-diene-3,20-dione 17,21-dipropionate | beclometasone 17,21-dipropionate | Beclometasone dipropionate | Beclomethasone dipropionate |
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.