Product Information
Registration Status: ActivePROCTOSEDYL OINTMENT is approved to be sold in Singapore with effective from 1988-08-06. It is marketed by SANOFI-AVENTIS SINGAPORE PTE LTD, with the registration number of SIN01718P.
This product contains Dibucaine 0.5% w/w,Esculoside 1% w/w,Hydrocortisone 0.5% w/w, and Neomycin B 1% w/w in the form of OINTMENT. It is approved for TOPICAL use.
This product is manufactured by HANDOK Inc. in KOREA, and in REPUBLIC OF.
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
A local anesthetic of the amide type now generally used for surface anesthesia. It is one of the most potent and toxic of the long-acting local anesthetics and its parenteral use is restricted to spinal anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1006)
Indication
For production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks.
Mechanism of Action
Local anesthetics block both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions through sodium channel inhibition. This reversibly stabilizes the membrane and inhibits depolarization, resulting in the failure of a propagated action potential and subsequent conduction blockade.
Pharmacokinetics
- Absorption
- In general, ionized forms (salts) of local anesthetics are not readily absorbed through intact skin. However, both nonionized (bases) and ionized forms of local anesthetics are readily absorbed through traumatized or abraded skin into the systemic circulation.
- Distribution
- Metabolism
- Primarily hepatic.
- Elimination
Toxicity
Subcutaneous LD50 in rat is 27 mg/kg. Symptoms of overdose include convulsions, hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest.
Active Ingredient/Synonyms
2-Butoxy-N-(2-(diethylamino)ethyl)cinchoninamide | 2-Butoxy-N-(alpha-diethylaminoethyl)cinchoninamide | 2-Butoxy-N-(beta-diethylaminoethyl)cinchoninamide | 2-Butoxy-N-[2-(diethylamino)ethyl]-4-quinolinecarboxamide | 2-Butoxy-quinoline-4-carboxylic acid (2-diethylamino-ethyl)-amide | 2-Butoxyquinoline-4-carboxylic acid diethylaminoethylamide | 2-N-Butoxy-N-(2-diethylaminoethyl)cinchoninamide | alpha-Butyloxycinchonic acid-gamma-diethylethylenediamine | alpha-Butyloxycinchoninic acid diethylethylenediamide | CINCHOCAINE | Cinchocainum | Cincocainio | Dibucaine | Dibucaine base | N-(2-(Diethylamino)ethyl)-2-butoxycinchoninamide | Cinchocaine |
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
Esculin is found in barley. Vitamin C2 is generally considered a bioflavanoid, related to vitamin P esculin is a glucoside that naturally occurs in the horse chestnut (Aesculus hippocastanum), California Buckeye (Aesculus californica) and in daphnin (the dark green resin of Daphne mezereum). Esculin belongs to the family of Glycosyl Compounds. These are carbohydrate derivatives in which a sugar group is bonded through its anmoeric carbonA to another group via a C-, S-,N-,O-, or Se- glycosidic bond.
Indication
As medication, esculin is sometimes used as a vasoprotective agent. Esculin is also used in a microbiology laboratory to aid in the identification of bacterial species (especially Enterococci and Listeria). In fact, all strains of Group D Streptococci hydrolyze æsculin in 40% bile.
Mechanism of Action
The main activities of Esculine focus on capillary protection, as it improves capillary permeability and fragility. It is reported to inhibit catabolic enzymes such as hyaluronidase and collagenase, thus preserving the integrity of the perivascular connective tissue. Esculine also showed good antioxidant properties, protecting triglycerides against auto-oxidation at high temperatures . The antioxidant property might as well explain some of the anti-inflammatory activity of the product, making it a suitable product for after sun treatments, for example.
Pharmacokinetics
- Absorption
- Rarely, absorbed into the blood stream if used as a combination with other ingredients in suppository form. But, Applying cream or ointment form to open wound or skin may lead this drug to absorb and circulate into blood stream.
- Distribution
- Metabolism
- After oral administration of esculin (100 mg/kg) for rats, plasma, urine, feces and bile samples were collected to screen metabolites. As a result, a total of 19 metabolites (10 phase I metabolites and 9 phase II metabolites) were found and identified. It was also found that after oral administration of esculin, the esculin could be metabolized to esculetin in vivo via deglycosylation, and esculetin was found in all biological samples.
- Elimination
Toxicity
Organism : Mouse Test type : LD50 Route: Intraperitoneal Reported dose: 1900mg/kg No reported effects known other than LD50
Active Ingredient/Synonyms
6-(beta-D-Glucopyranosyloxy)-7-hydroxy-2H-1-benzopyran-2-one | 6-(beta-D-Glucopyranosyloxy)-7-hydroxy-cumarin | 6,7-Dihydroxycoumarin 6-glucoside | 6,7-Dihydroxycoumarin-6-O-glucoside | Aesculin | Aesculinum | Esculetin 6-O-glucoside | esculetin 6-β-D-glucoside | Esculina | Esculoside | Esculin |
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
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
A component of neomycin that is produced by Streptomyces fradiae. On hydrolysis it yields neamine and neobiosamine B. (From Merck Index, 11th ed)
Indication
For the treatment of bacterial blepharitis, bacterial bonjunctivitis, corneal injuries, corneal ulcers and meibomianitis. For the prophylaxis of ocular infections following foreign body removal
Mechanism of Action
Framycetin binds to specific 30S-subunit proteins and 16S rRNA, four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes.
Active Ingredient/Synonyms
Fradiomycin B | Framicetina | Framycetin | Framycétine | Framycetinum | Neomycin B | Framycetin |
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.