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| Mechanism of Action |
Erythromycin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Erythromycin acts by penetrating the bacterial cell membrane and reversibly binding to the 50 S subunit of bacterial ribosomes or near the ¡°P¡± or donor site so that binding of tRNA (transfer RNA) to the donor site is blocked. Translocation of peptides from the ¡°A¡± or acceptor site to the ¡°P¡± or donor site is prevented, and subsequent protein synthesis is inhibited. Erythromycin is effective only against actively dividing organisms. The exact mechanism by which erythmromycin reduces lesions of acne vulgaris is not fully known: however, the effect appears to be due in part to the antibacterial activity of the drug.
Isotretinoin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Isotretinoin noticeably reduces the production of sebum and shrinks the sebaceous glands. It stabilises keratinization and prevents comedones from forming. The exact mechanism of action is unknown, however it is known that it alters DNA transcription.
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| Pharmacology |
Erythromycin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Erythromycin is produced by a strain of Streptomyces erythraeus and belongs to the macrolide group of antibiotics. After absorption, erythromycin diffuses readily into most body fluids. In the absence of meningeal inflammation, low concentrations are normally achieved in the spinal fluid, but the passage of the drug across the blood-brain barrier increases in meningitis. Erythromycin is excreted in breast milk. The drug crosses the placental barrier, but fetal plasma levels are low. Erythromycin is not removed by peritoneal dialysis or hemodialysis.
Isotretinoin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Isotretinoin, a retinoid, is indicated in the treatment of severe recalcitrant nodular acne. Nodules are inflammatory lesions with a diameter of 5 mm or greater. The nodules may become suppurative or hemorrhagic. "Severe," by definition, means "many" as opposed to "few or several" nodules. Clinical improvement in nodular acne patients occurs in association with a reduction in sebum secretion. The decrease in sebum secretion is temporary and is related to the dose and duration of treatment with Accutane, and reflects a reduction in sebaceous gland size and an inhibition of sebaceous gland differentiation.
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| Protein Binding |
Erythromycin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Erythromycin is largely bound to plasma proteins, and the freely dissociating bound fraction after administration of erythromycin base represents 90% of the total erythromycin absorbed.
Isotretinoin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 99.9%
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| Half-life |
Erythromycin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 1.5 hours
Isotretinoin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 17-50 hours
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| Absorption |
Erythromycin¿¡ ´ëÇÑ Absorption Á¤º¸ Orally administered erythromycin base and its salts are readily absorbed in the microbiologically active form. Topical application of the ophthalmic ointment to the eye may result in absorption into the cornea and aqueous humor.
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| Pharmacokinetics |
IsotretinoinÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : À½½Ä¹°À̳ª ¿ìÀ¯¿¡ ÀÇÇØ Èí¼ö°¡ Áõ°¡ÇÑ´Ù.
- »ýü³»ÀÌ¿ë·ü : °æ±¸ : 23-25%
- ºÐÆ÷ : ÅÂ¹Ý Åë°ú, À¯Áó ºÐºñ
- ´Ü¹é°áÇÕ : 99.9%
- ´ë»ç : °£´ë»ç
- ÁÖ È°¼ºÇü ´ë»çü´Â 4-oxo-isotretinoinÀÌ¸ç ±âŸ tretinoin, 4-oxo-tretinoin µîÀÇ ´ë»çü°¡ Á¸ÀçÇÑ´Ù.
- Åõ¿© 6½Ã°£ ÀÌÈÄ¿¡´Â 4-oxo-isotretinoinÀÇ Ç÷Áß³óµµ°¡ isotretinoinÀÇ Ç÷Á߳󵵺¸´Ù ³ô´Ù.
- ¹Ý°¨±â :
- Isotretinoin : 10-20 ½Ã°£
- 4-oxo-isotretinoin : 17-50 ½Ã°£ (Æò±Õ 25½Ã°£)
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ :
- Isotretinoin : ¾à 3½Ã°£
- 4-oxo-isotretin
ErythromycinÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö :
- ´Ù¾çÇÏÁö¸¸ base Çüź¸´Ù ¿°ÀÇ ÇüŰ¡ ´õ Àß Èí¼öµÈ´Ù.
- ÀϹÝÀûÀ¸·Î À½½Ä¹° Á¸Àç½Ã Èí¼ö°¡ Áö¿¬µÇ³ª ethylsuccinate¿°Àº ½ÄÁ÷ÈÄ¿¡ º¹¿ëÇϸé Èí¼ö°¡ Áõ°¡µÈ´Ù.
- Èí¼ö·üÀÇ Â÷ÀÌ·Î erythromycin ethylsuccinate 200 mg´Â erythromycin base 125 m¿Í µ¿µîÇÑ Ç÷Á߳󵵸¦ ³ªÅ¸³½´Ù.
- »ýü³»ÀÌ¿ë·ü : °æ±¸ : 18-45%
- ºÐÆ÷ :
- ŹÝÅë°ú, À¯ÁóºÐºñ
- ³úô¼ö¾×À¸·ÎÀÇ ºÐÆ÷´Â ¿°ÁõÀÌ ÀÖ´Â °æ¿ì¿¡µµ ¹Ì¹ÌÇÏ´Ù.
- ³úô¼ö¾× ´ë Ç÷¾×ÀÇ ³óµµ ºñ (%) :
- Á¤»ó ³ú¸· : 1-12
- °¨¿°µÈ ³ú¸· : 7-25
- ´Ü¹é°áÇÕ : 75-90%
- ´ë»ç : °£¿¡¼ demethylation
- ¹Ý°¨±â : 1.5-2 ½Ã°£
- ¸»±â ½ÅºÎÀüȯÀÚ : 5-6 ½Ã°£
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ :
- base : 4½Ã°£
- Ethylsuccinate ¿° : 0.5-2.5 ½Ã°£
- ¼Ò½Ç : ´ëºÎºÐ ´ãÁó¹è¼³µÇ°í, 2-15%°¡ ¹Ìº¯Èü·Î ½Å¹è¼³
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| Biotransformation |
Erythromycin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Extensively metabolized - after oral administration, less than 5% of the administered dose can be recovered in the active form in the urine.
Isotretinoin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Not Available
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| Toxicity |
Erythromycin¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include diarrhea, nausea, stomach cramps, and vomiting.
Isotretinoin¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
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| Drug Interactions |
Erythromycin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alfentanil The macrolide increases the effect and toxicity of alfentanilAlprazolam The macrolide increases the effect of the benzodiazepineAminophylline The macrolide increases the effect and toxicity of theophyllineAmiodarone Increased risk of cardiotoxicity and arrhythmiasAnisindione The macrolide increases anticoagulant effectAprepitant This CYP3A4 inhibitor increases effect and toxicity of aprepitantAstemizole Increased risk of cardiotoxicity and arrhythmiasAtorvastatin The macrolide possibly increases the statin toxicityBretylium Increased risk of cardiotoxicity and arryhthmiasBromocriptine Erythromycin increases serum levels of bromocriptineBuspirone The macrolide increases the effect and toxicity of buspironeCabergoline Erythromycin increases serum levels and toxicity of cabergolineCarbamazepine The macrolide increases the effect of carbamazepineCerivastatin The macrolide possibly increases the statin toxicityCilostazol Erythromycin increases the effect of cilostazolCinacalcet This macrolide increases the serum levels and toxicity of cinacalcetCisapride Increased risk of cardiotoxicity and arrhythmiasCitalopram Possible serotoninergic syndrome with this combinationClozapine Erythromycin increases the effect of clozapineColchicine Severe colchicine toxicity can occurCyclosporine The macrolide increases the effect of cyclosporineDiazepam The macrolide increases the effect of the benzodiazepineDicumarol The macrolide increases anticoagulant effectDigoxin The macrolide increases the effect of digoxin in 10% of patientsDihydroergotamine Possible ergotism and severe ischemia with this combinationDihydroergotoxine Possible ergotism and severe ischemia with this combinationDyphylline The macrolide increases the effect and toxicity of theophyllineDisopyramide Increased risk of cardiotoxicity and arrhythmiasDivalproex sodium Erythromycin increases the effect of valproic acidDocetaxel The agent increases the serum levels and toxicity of docetaxelDofetilide Increased risk of cardiotoxicity and arrhythmiasEletriptan The macrolide increases the effect and toxicity of eletriptanEplerenone This CYP3A4 inhibitor increases the effect and toxicity of eplerenoneErgotamine Possible ergotism and severe ischemia with this combinationErlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinibImatinib The macrolide increases levels of imatinibFelodipine Erythromycin increases the effect of felodipineFluoxetine Possible serotoninergic syndrome with this combinationGefitinib This CYP3A4 inhibitor increases levels/toxicity of gefitinibGrepafloxacin Increased risk of cardiotoxicity and arrhythmiasItraconazole The macrolide increases the effect and toxicity of itraconazoleLevofloxacin Increased risk of cardiotoxicity and arrhythmiasMesoridazine Increased risk of cardiotoxicity and arrhythmiasMethylergonovine Possible ergotism and severe ischemia with this combinationLovastatin The macrolide possibly increases the statin toxicityMethylprednisolone The macrolide increases the effect of corticosteroidMethysergide Possible ergotism and severe ischemia with this combinationMidazolam The macrolide increases the efect of the benzodiazepineMoxifloxacin Increased risk of cardiotoxicity and arrhythmiasOxtriphylline The macrolide increases the effect and toxicity of theophyllinePimozide Increased risk of cardiotoxicity and arrhythmiasQuetiapine This macrolide increases the effect/toxicity of quetiapineQuinidine Increased risk of cardiotoxicity and arrhythmiasQuinidine barbiturate Increased risk of cardiotoxicity and arrhythmiasQuinupristin This combination presents an increased risk of toxicityRanolazine Increased levels of ranolazine - risk of toxicityRepaglinide This macrolide increases effect of repaglinideRifabutin The rifamycin decreases the effect of the macrolideRifampin The rifamycin decreases the effect of the macrolideRitonavir Increased toxicity of both agentsSertraline Possible serotoninergic syndrome with this combinationSibutramine Erythromycin increases the effect and toxicity of sibutramineSildenafil The macrolide increases the effect and toxicity of sildenafilSimvastatin The macrolide possibly increases the statin toxicitySirolimus The macrolide increases sirolimus levelsSotalol Increased risk of cardiotoxicity and arrhythmiasSparfloxacin Increased risk of cardiotoxicity and arrhythmiasTacrolimus Erythromycin increases the effect and toxicity of tacrolimusTerfenadine Increased risk of cardiotoxicity and arrhythmiasTheophylline The macrolide increases the effect and toxicity of theophyllineThioridazine Increased risk of cardiotoxicity and arrhythmiasVerapamil Increased risk of cardiotoxicity and arrhythmiasTriazolam The macrolide increases the effect of the benzodiazepineVardenafil The macrolide increases the effect and toxicity of vardenafilVinblastine Erythromycin increases vinblastine toxicityWarfarin The macrolide increases anticoagulant effectZafirlukast Erythromycin decreases the effect of zafirlukastErgonovine Possible ergotism and severe ischemia with this combinationEverolimus The macrolide increases everolimus levels/toxicityLincomycin Possible antagonism of action with this combinationAcenocoumarol The macrolide increases anticoagulant effect
Isotretinoin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Anisindione Retinoids decreases the anticoagulant effectDicumarol Retinoids decreases the anticoagulant effectAcenocoumarol Retinoids decreases the anticoagulant effectWarfarin Retinoids decreases the anticoagulant effectCarbamazepine Isotretinoine decreases the effect of carbamazepineDemeclocycline Increased risk of intracranial hypertensionDoxycycline Increased risk of intracranial hypertensionMinocycline Increased risk of intracranial hypertensionMethacycline Increased risk of intracranial hypertensionOxytetracycline Increased risk of intracranial hypertensionTetracycline Increased risk of intracranial hypertensionRolitetracycline Increased risk of intracranial hypertension
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Erythromycin¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 3A4/3A5/3A7
Macrolide antibiotics:
clarithromycin
**erythromycin**
NOT azithromycin
telithromycin
Anti-arrhythmics:
quinidine
Benzodiazepines:
alprazolam
diazepam
midazolam
triazolam
Immune Modulators:
cyclosporine
tacrolimus (FK506)
HIV Protease Inhibitors:
indinavir
ritonavir
saquinavir
Prokinetic:
cisapride
Antihistamines:
astemizole
chlorpheniramine
Calcium Channel Blockers:
amlodipine
diltiazem
felodipine
nifedipine
nisoldipine
nitrendipine
verapamil
HMG CoA Reductase Inhibitors:
atorvastatin
cerivastatin
lovastatin
NOT pravastatin
simvastatin
aripiprazole
buspirone
gleevec
haloperidol (in part)
methadone
pimozide
quinine
NOT rosuvastatin
sildenafil
tamoxifen
trazodone
vincristine
INHIBITORS
CYP 3A4/3A5/3A7
HIV Protease Inhibitors:
indinavir
nelfinavir
ritonavir
amiodarone
NOT azithromycin
cimetidine
clarithromycin
diltiazem
**erythromycin**
fluvoxamine
grapefruit juice
itraconazole
ketoconazole
mibefradil
nefazodone
troleandomycin
verapamil
INDUCERS
CYP 3A4/3A5/3A7
carbamazepine
phenobarbital
phenytoin
rifabutin
rifampin
St. John's wort
troglitazone
SUBSTRATES
CYP 3A4/3A5/3A7
Macrolide antibiotics:
clarithromycin
**erythromycin**
NOT azithromycin
telithromycin
Anti-arrhythmics:
quinidine
Benzodiazepines:
alprazolam
diazepam
midazolam
triazolam
Immune Modulators:
cyclosporine
tacrolimus (FK506)
HIV Protease Inhibitors:
indinavir
ritonavir
saquinavir
Prokinetic:
cisapride
Antihistamines:
astemizole
chlorpheniramine
Calcium Channel Blockers:
amlodipine
diltiazem
felodipine
nifedipine
nisoldipine
nitrendipine
verapamil
HMG CoA Reductase Inhibitors:
atorvastatin
cerivastatin
lovastatin
NOT pravastatin
simvastatin
aripiprazole
buspirone
gleevec
haloperidol (in part)
methadone
pimozide
quinine
NOT rosuvastatin
sildenafil
tamoxifen
trazodone
vincristine
INHIBITORS
CYP 3A4/3A5/3A7
HIV Protease Inhibitors:
indinavir
nelfinavir
ritonavir
amiodarone
NOT azithromycin
cimetidine
clarithromycin
diltiazem
**erythromycin**
fluvoxamine
grapefruit juice
itraconazole
ketoconazole
mibefradil
nefazodone
troleandomycin
verapamil
INDUCERS
CYP 3A4/3A5/3A7
carbamazepine
phenobarbital
phenytoin
rifabutin
rifampin
St. John's wort
troglitazone
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| Drug Target |
[Drug Target]
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| Description |
Erythromycin¿¡ ´ëÇÑ Description Á¤º¸ Erythromycin is a bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins. [PubChem]
Isotretinoin¿¡ ´ëÇÑ Description Á¤º¸ Isotretinoin is a medication used for the treatment of severe acne. It is sometimes used in prevention of certain skin cancers. It is a retinoid, meaning it derives from vitamin A and is found in small quantities naturally in the body. Isotretinoin binds to and activates nuclear retinoic acid receptors (RAR), thereby regulating cell proliferation and differentiation. This agent also exhibits immunomodulatory and anti-inflammatory responses and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.
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| Dosage Form |
Erythromycin¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule, coated OralLiquid DentalLiquid OralOintment OphthalmicPowder IntravenousPowder OralPowder, for solution IntravenousPowder, for solution OralPowder, for suspension OralSuspension OralTablet Oral
Isotretinoin¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule Oral
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| Drug Category |
Erythromycin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Bacterial Agents
Isotretinoin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-acne AgentsAntineoplastic AgentsKeratolytic AgentsSkin and Mucous Membrane Agents
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| Smiles String Canonical |
Erythromycin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCC1OC(=O)C(C)C(OC2CC(C)(OC)C(O)C(C)O2)C(C)C(OC2OC(C)CC(C2O)N(C)C)C(C)(O)CC(C)C(=O)C(C)C(O)C1(C)O
Isotretinoin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC(O)=O
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| Smiles String Isomeric |
Erythromycin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@H]2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@@H]([C@H]2O)N(C)C)[C@](C)(O)C[C@@H](C)C(=O)[C@H](C)[C@@H](O)[C@]1(C)O
Isotretinoin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(\C=C\C1=C(C)CCCC1(C)C)=C/C=C/C(C)=C/C(O)=O
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| InChI Identifier |
Erythromycin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C37H67NO13/c1-14-25-37(10,45)30(41)20(4)27(39)18(2)16-35(8,44)32(51-34-28(40)24(38(11)12)15-19(3)47-34)21(5)29(22(6)33(43)49-25)50-26-17-36(9,46-13)31(42)23(7)48-26/h18-26,28-32,34,40-42,44-45H,14-17H2,1-13H3/t18-,19-,20+,21+,22-,23+,24+,25-,26+,28-,29+,30-,31+,32-,34+,35-,36-,37-/m1/s1
Isotretinoin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C20H28O2/c1-15(8-6-9-16(2)14-19(21)22)11-12-18-17(3)10-7-13-20(18,4)5/h6,8-9,11-12,14H,7,10,13H2,1-5H3,(H,21,22)/f/h21H
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| Chemical IUPAC Name |
Erythromycin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-[(2S,3R,4S,6R)-4-dimethylamino-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,7,9,11,13-hexamethyl-1-oxacyclotetradecane-2,10-dione
Isotretinoin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexenyl)nona-2,4,6,8-tetraenoic acid
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| Drug-Induced Toxicity Related Proteins |
ERYTHROMYCIN ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Misshapen-like kinase(Mink) Drug:Erythromycin Toxicity:torsade de pointes. [¹Ù·Î°¡±â] Replated Protein:Potassium voltage-gated channel subfamily KQT member 1 (KvLQT1) Drug:Erythromycin Toxicity:torsade de pointes. [¹Ù·Î°¡±â] Replated Protein:Intercellular adhesion molecule 1 Drug:erythromycin Toxicity:pathogenesis of infusion phlebitis. [¹Ù·Î°¡±â] Replated Protein:HERG Drug:Erythromycin Toxicity:torsade de pointes. [¹Ù·Î°¡±â] Replated Protein:Alanine aminotransferase Drug:erythromycin Toxicity:adverse gastrointestinal effects. [¹Ù·Î°¡±â]
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