|
| Primary information |
|---|
| ID | 10187 |
| 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 | Neosporin |
| Company | Pfizer |
| Brand Description | Pfizer |
| Prescribed For | Neosporin ointment is an antibiotic combination which works by killing sensitive bacteria on the skin or in wounds.Thus, treating and preventing infection due to minor cuts, scrapes, and burns. |
| Chemical Name | NA |
| Formulation | Each gram contains: neomycin sulfate equivalent to 3.5 mg neomycin base, polymyxin B sulfate equivalent to 10,000 polymyxin B units, bacitracin zinc equivalent to 400 bacitracin units, and white petrolatum, q.s. |
| Physical Appearance | Ointment |
| Route of Administration | External use only |
| Recommended Dosage | Apply the ointment every 3 or 4 hours for 7 to 10 days depending on the severity of the infection. |
| Contraindication | Individuals who have shown hypersensitivity to any of its components |
| Side Effects | Rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue; skin irritation, pain, burning, cracking, redness, or peeling not present before using Neosporin ointment; worsening or recurrence of wound symptoms. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |