|
| Primary information |
|---|
| ID | 10190 |
| Therapeutic ID | Th1024 |
| Protein Name | Gramicidin D |
| Sequence | >Th1024_Gramicidin_D
VGALAVVVWLWLWLWX
|
| Molecular Weight | 1811.253 |
| Chemical Formula | C96H135N19O16 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | 229 |
| Half-life | NA |
| Description | Gramcidin D is a heterogeneous mixture of three antibiotic compounds, gramicidins A, B and C, making up 80%, 6%, and 14% respectively all of which are obtained from the soil bacterial species Bacillus brevis and called collectively gramicidin D. Gramcidins are 15 residue peptides with alternating D and L amino acids. The peptides assemble inside of the hydrophobic interior of the cellular lipid bilayer to form an alpha helix. The helix itself is not long enough to span the membrane but it dimerizes to form the elongated channel needed to span the whole membrane. Gramicidin D is used primarily as a topical antibiotic and is one of the three constituents of consumer antibiotic polysporin ophthalmic solution. |
| Indication/Disease | For treatment of skin lesions, surface wounds and eye infections |
| Pharmacodynamics | Gramicidin is particularly effective against gram-positive bacteria because the drug is highly hemolytic, it cannot be administered internally and so is used only on the skin as a lotion or ointment. It is used primarily in the treatment of infected surface wounds, and in eye, nose, and throat infections. It is normally given with two other antibiotics (neomycin and polymixin B) as an ophthalmic solution |
| Mechanism of Action | Gramicidin D binds and inserts itself into bacterial membranes (preference to gram-positive cell membranes) resulting in membrane disruption and permeabilization (it acts as a channel). This leads to loss of intracellular solutes (e.g., K+ and amino acids); dissipation of the transmembrane potential; inhibition of respiration; a reduction in ATP pools; and inhibition of DNA, RNA, and protein synthesis, which leads to cell death. |
| Toxicity | NA |
| Metabolism | NA |
| Absorption | NA |
| NA |
| Clearance | NA |
| Categories | Amino Acids, Peptides, and Proteins, Anti-Bacterial Agents, Anti-Infective Agents, Anti-Infective Agents, Local, Membrane Proteins, P-glycoprotein inhibitors, P-glycoprotein substrates, Peptides, Peptides, Cyclic, Pore Forming Cytotoxic Proteins, Proteins, Throat Preparations |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | NA |
| Brand Name | Sofradex |
| Company | Sanofi |
| Brand Description | Sanofi |
| Prescribed For | Used in the eye(s) to treat Inflammation in the eye when prevention of bacterial infection is also needed. Signs include sore, red or swollen eyes. It is used in the ear(s) to treat Inflammation of the ear canal (otitis externa) |
| Chemical Name | NA |
| Formulation | Each bottle contains 0.5% w/v of Framycetin Sulphate, Dexamethasone Sodium Metasulphobenzoate (equivalent to 0.050% w/v of Dexamethasone) and 0.005% w/v of Gramicidin. The other ingredients are citric acid, sodium citrate, lithium chloride, phenylethyl al |
| Physical Appearance | Sterile, clear, bright, colourless, aqueous solution |
| Route of Administration | Auricular and Ocular use. |
| Recommended Dosage | One or two drops applied to each affected eye up to six times daily or more frequently if required. Two or three drops instilled into the ear three or four times daily. |
| Contraindication | If glaucoma is present or herpetic keratitis (e.g. dendritic ulcer) is considered a possibility. Otitis Externa should not be treated when the eardrum is perforated because of the risk of ototoxicity. Hypersensitivity to framycetin sulphate, dexamethasone sodium metasulphobenzoate, gramicidin or to any of the excipients. |
| Side Effects | Stop using Sofradex if: You get any kind of skin problem, such as a rash or itching around your eyes or irritation burning, stinging, itching or swelling, your eyes have problems focussing or develop a blind spot. You may have increased pressure in the eye, you have difficulty seeing at night or notice that your eyesight is cloudy and fuzzy, or you see halos around lights. These could be signs of cataracts. This may occur after using the medicine for a long time |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |