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[Drugbank ÀÇ ¼ººÐÁ¤º¸¿¶÷] [Colistin][Tetracycline]
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(tetracycline. ÀӽŠ2±â¿Í 3±â¿¡ Åõ¿© ±Ý±â )
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| Mechanism of Action |
Colistin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Colistin is a surface active agent which penetrates into and disrupts the bacterial cell membrane. Colistin is polycationic and has both hydrophobic and lipophilic moieties. It interacts with the bacterial cytoplasmic membrane, changing its permeability. This effect is bactericidal. There is also evidence that polymyxins enter the cell and precipitate cytoplasmic components, primarily ribosomes.
Tetracycline¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Tetracycline passively diffuses through porin channels in the bacterial membrane and reversibly binds to the 30S ribosomal subunit, preventing binding of tRNA to the mRNA-ribosome complex, and thus interfering with protein synthesis.
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| Pharmacology |
Colistin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Colistin is a polymyxin antibiotic agent. Polymyxins are cationic polypeptides that disrupt the bacterial cell membrane through a detergentlike mechanism. With the development of less toxic agents, such as extended-spectrum penicillins and cephalosporins, parenteral polymyxin use was largely abandoned, except for the treatment of multidrug-resistant pulmonary infections in patients with cystic fibrosis. More recently, however, the emergence of multidrug-resistant gram-negative bacteria, such as Pseudomonas aeruginosa and Acinetobacter baumannii, and the lack of new antimicrobial agents have led to the revived use of the polymyxins.
Tetracycline¿¡ ´ëÇÑ Pharmacology Á¤º¸ Tetracycline is a short-acting antibiotic semisynthetically produced from chlortetracycline, which is derived from Streptomyces aureofaciens. Tetracycline inhibits cell growth by inhibiting translation. It binds to the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. This binding is reversible in nature.
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| Metabolism |
Colistin¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
Tetracycline¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
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| Protein Binding |
Colistin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
Tetracycline¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Tetracyclines bind to plasma proteins to varying degrees
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| Half-life |
Colistin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 5 hours
Tetracycline¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 6-11 hours
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| Absorption |
Colistin¿¡ ´ëÇÑ Absorption Á¤º¸ Very poor absorption from gastrointestinal tract.
Tetracycline¿¡ ´ëÇÑ Absorption Á¤º¸ Bioavailability is less than 40% when administered via intramuscular injection, 100% intravenously, and 60-80% orally (fasting adults). Food and/or milk reduce GI absorption of oral preparations of tetracycline by 50% or more.
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| Pharmacokinetics |
Colistin sodium methanesulfonateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : °æ±¸ :
- ¼ºÀÎ : ¼Ò·®ÀÌ À§Àå°ü¿¡¼ Èí¼ö
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- ¹«´¢Áõ : 48-72 ½Ã°£
- ¼Ò½Ç : 65-75%°¡ ¹Ìº¯Èü·Î ½Å¹è¼³
Tetracycline HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : °æ±¸ : 75%
- ºÐÆ÷ : ¼Ò·®ÀÌ ´ãÁóºÐºñ
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- ³úô¼ö¾× ´ë Ç÷¾×ÀÇ ³óµµºñ : 25%
- ´Ü¹é°áÇÕ : 20-60%
- ¹Ý°¨±â :
- Á¤»ó ½Å±â´É : 8-11 ½Ã°£
- ¸»±â ½ÅºÎÀü : 57-108 ½Ã°£
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : °æ±¸ : 2-4 ½Ã°£ À̳»
- ¼Ò½Ç : ÁÖ·Î ½Å¹è¼³ (60%°¡ ¹Ìº¯Èü·Î ½Å¹è¼³)
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| Biotransformation |
Colistin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Not Available
Tetracycline¿¡ ´ëÇÑ Biotransformation Á¤º¸ Not metabolized
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| Toxicity |
Colistin¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral LD50 in rats is 5450 mg/kg. Overdosage with colistimethate can cause neuromuscular blockade characterized by paresthesia, lethargy, confusion, dizziness, ataxia, nystagmus, disorders of speech and apnea. Respiratory muscle paralysis may lead to apnea, respiratory arrest and death.
Tetracycline¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=808mg/kg (orally in mice)
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| Drug Interactions |
Colistin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
Tetracycline¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Tetracycline¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid milk, calcium containing dairy products, iron, antacids, or aluminium salts 2 hours before or 6 hours after using antacids while on this medication.Take on empty stomach: 1 hour before or 2 hours after meals.Take with a full glass of water.
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| Drug Target |
[Drug Target]
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| Description |
Colistin¿¡ ´ëÇÑ Description Á¤º¸ Cyclic polypeptide antibiotic from Bacillus colistinus. It is composed of Polymyxins E1 and E2 (or Colistins A, B, and C) which act as detergents on cell membranes. Colistin is less toxic than Polymyxin B, but otherwise similar; the methanesulfonate is used orally. [PubChem]
Tetracycline¿¡ ´ëÇÑ Description Á¤º¸ A naphthacene antibiotic that inhibits amino acyl TRNA binding during protein synthesis. [PubChem]
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| Dosage Form |
Colistin¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Powder, for solution Intravenous
Tetracycline¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule OralOintment OphthalmicTablet Oral
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| Drug Category |
Colistin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Bacterial Agents
Tetracycline¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Bacterial AgentsAntiprotozoalsProtein Synthesis InhibitorsTetracyclines
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| Smiles String Canonical |
Colistin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCC(C)CCCC(=O)NC(CCN)C(=O)NC(C(C)O)C(=O)NC(CCN)C(=O)NC1CCNC(=O)C(NC(=O)C(CCN)NC(=O)C(CCN)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CCN)NC1=O)C(C)O
Tetracycline¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)C1C2CC3C(C(=O)C2(O)C(=O)C(C1=O)=C(N)O)=C(O)C1=C(C=CC=C1O)C3(C)O
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| Smiles String Isomeric |
Colistin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC[C@@H](C)CCCC(=O)N[C@@H](CCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@@H](NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O
Tetracycline¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)[C@H]1[C@@H]2C[C@@H]3C(C(=O)[C@@]2(O)C(=O)\C(C1=O)=C(\N)O)=C(O)C1=C(C=CC=C1O)[C@@]3(C)O
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| InChI Identifier |
Colistin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C52H98N16O13/c1-9-29(6)11-10-12-40(71)59-32(13-19-53)47(76)68-42(31(8)70)52(81)64-35(16-22-56)44(73)63-37-18-24-58-51(80)41(30(7)69)67-48(77)36(17-23-57)61-43(72)33(14-20-54)62-49(78)38(25-27(2)3)66-50(79)39(26-28(4)5)65-45(74)34(15-21-55)60-46(37)75/h27-39,41-42,69-70H,9-26,53-57H2,1-8H3,(H,58,80)(H,59,71)(H,60,75)(H,61,72)(H,62,78)(H,63,73)(H,64,81)(H,65,74)(H,66,79)(H,67,77)(H,68,76)/t29?,30-,31-,32+,33+,34+,35+,36+,37+,38+,39-,41+,42+/m1/s1/f/h58-68H
Tetracycline¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C22H24N2O8/c1-21(31)8-5-4-6-11(25)12(8)16(26)13-9(21)7-10-15(24(2)3)17(27)14(20(23)30)19(29)22(10,32)18(13)28/h4-6,9-10,15,25-26,30-32H,7,23H2,1-3H3/b20-14-
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| Chemical IUPAC Name |
Colistin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ N-[(2S)-4-amino-1-[[(2S,3R)-1-[[(2S)-4-amino-1-oxo-1-[[(3S,6S,9S,12S,15R,18S,21S)-6,9,18-tris(2-aminoethyl)-3-(1-hydroxyethyl)-12,15-bis(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxobutan-2-yl]-5-methylheptanamide
Tetracycline¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (2Z)-2-(amino-hydroxymethylidene)-4-dimethylamino-6,10,11,12a-tetrahydroxy-6-methyl-4,4a,5,5a-tetrahydrotetracene-1,3,12-trione
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. TETRACYCLINE[GGT Increase][Composite Activity](Score) NA(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA[SGOT Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA[SGPT Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA[LDH Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA[GGT Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA
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