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                    ¿ÀÅ¥·ÐÁ¡¾È¾×  OCULON EYE DROPS[Phenylephrine HCl , Prednisolone acetate , Sulfacetamide sodium]  
                    
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    Acetamide¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â 
  Ãâó: ±¹¸³µ¶¼º°úÇпø µ¶¼º¹°ÁúÁ¤º¸DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do  | 
   
  
   
    | Mechanism of Action | 
    
       Phenylephrine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Phenylephrine produces its ophthalmic and systemic actions by acting on alpha 1 adrenergic receptors in the pupillary dilator muscle and the vascular smooth musle, resulting in contraction of the dilator muscle and contraction of the smooth muscle in the arterioles of the conjunctiva and peripheral vasoconstriction. Phenylephrine decreases nasal congestion by acting on alpha 1 adrenergic receptors in the arterioles of the nasal mucosa to produce constriction.
  Prednisolone¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Glucocorticoids such as Prednisolone can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of glucocorticoids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Prednisolone reduces inflammatory reaction by limiting the capillary dilatation and permeability of the vascular structures. These compounds restrict the accumulation of polymorphonuclear leukocytes and macrophages and reduce the release of vasoactive kinins. Recent research suggests that corticosteroids may inhibit the release of arachidonic acid from phospholipids, thereby reducing the formation of prostaglandins. Prednisolone is a glucocorticoid receptor agonist. On binding, the corticoreceptor-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 an increase or decrease in expression of specific target genes, including suppression of IL2 (interleukin 2) expression.
  Sulfacetamide¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Sulfacetamide is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), an essential component for bacterial growth (according to the Woods-Fildes theory). The inhibited reaction is necessary in these organisms for the synthesis of folic acid. 
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    | Pharmacology | 
     
       Phenylephrine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Phenylephrine is a powerful vasoconstrictor. It is used as a mydriatic, nasal decongestant, and cardiotonic agent. Phenylephrine is a postsynaptic alpha-receptor stimulant with little effect on the beta receptors of the heart. Parenteral administration of Phenylephrine causes a rise in systolic and diastolic pressures, cardiac output is slightly decreased and peripheral resistance is considerably increased, most vascular beds are constricted; renal, splanchnic, cutaneous, and limb blood flows are reduced but coronary blood flow is increased. Pulmonary vessels are constricted, and pulmonary arterial pressure is raised. This alpha receptor sympathetic agonist is also used locally because its vasoconstrictor and mydriatic action.
  Prednisolone¿¡ ´ëÇÑ Pharmacology Á¤º¸ Prednisolone is a synthetic glucocorticoid used as antiinflammatory or immunosuppressive agent. Prednisolone is indicated in the treatment of various conditions, including congenital adrenal hyperplasia, psoriatic arthritis, systemic lupus erythematosus, bullous dermatitis herpetiformis, seasonal or perennial allergic rhinitis, allergic corneal marginal ulcers, symptomatic sarcoidosis, idiopathic thrombocytopenic purpura in adults, leukemias and lymphomas in adults, and ulcerative colitis. Glucocorticoids are adrenocortical steroids and cause profound and varied metabolic effects. In addition, they modify the body's immune responses to diverse stimuli.
  Sulfacetamide¿¡ ´ëÇÑ Pharmacology Á¤º¸ Sulfacetamide is a sulfonamide antibiotic. The sulfonamides are synthetic bacteriostatic antibiotics with a wide spectrum against most gram-positive and many gram-negative organisms. However, many strains of an individual species may be resistant. Sulfonamides inhibit multiplication of bacteria by acting as competitive inhibitors of p-aminobenzoic acid in the folic acid metabolism cycle. Bacterial sensitivity is the same for the various sulfonamides, and resistance to one sulfonamide indicates resistance to all. Most sulfonamides are readily absorbed orally. However, parenteral administration is difficult, since the soluble sulfonamide salts are highly alkaline and irritating to the tissues. The sulfonamides are widely distributed throughout all tissues. High levels are achieved in pleural, peritoneal, synovial, and ocular fluids. Although these drugs are no longer used to treat meningitis, CSF levels are high in meningeal infections. Their antibacterial action is inhibited by pus. 
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    | Metabolism | 
    
       Phenylephrine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Monoamine oxidase type A (MAO-A)
  Prednisolone¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4) 
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    | Protein Binding | 
    
       Phenylephrine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 95% binding-plasma proteins
  Prednisolone¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Very high (>90%)
  Sulfacetamide¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available 
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    | Half-life | 
    
       Phenylephrine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2.1 to 3.4 hours
  Prednisolone¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2-3 hours
  Sulfacetamide¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 7-12.8 hours 
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    | Absorption | 
    
       Phenylephrine¿¡ ´ëÇÑ Absorption Á¤º¸ Reduced bioavailability (compared to pseudoephedrine) following oral administration due to significant first-pass metabolism.
  Prednisolone¿¡ ´ëÇÑ Absorption Á¤º¸ Readily absorbed by gastrointestinal tract, peak plasma concentration is reached 1-2 hours after administration. 
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    | Pharmacokinetics | 
    
       Phenylephrine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á 
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    | Biotransformation | 
    
       Phenylephrine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Oral phenylephrine is extensively metabolised by monoamine oxidase, an enzyme which is present in the stomach and liver.
  Prednisolone¿¡ ´ëÇÑ Biotransformation Á¤º¸ Excreted in the urine as either free or glucoconjugate.
  Sulfacetamide¿¡ ´ëÇÑ Biotransformation Á¤º¸ Not Available 
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    | Toxicity | 
    
       Phenylephrine¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
  Prednisolone¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=500 mg/kg (oral, rat), short-term side effects include high blood glucose levels and fluid retention. Long term side effects include Cushing's syndrome, weight gain, osteoporosis, glaucoma, type II diabetes and adrenal suppression.
  Sulfacetamide¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral LD50 Mouse : 16500 mg/kg. Side effects include moderate to severe erythema (redness) and moderate edema (raised kin), nausea, vomiting, headache, dizziness, and tiredness. Higher exposure causes unconsciousness. 
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    | Drug Interactions | 
    
       Phenylephrine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alseroxylon	Increased arterial pressureIsocarboxazid	Increased arterial pressureDeserpidine	Increased arterial pressureGuanethidine	The agent decreases the effect of guanethidineRasagiline	Increased arterial pressureMethyldopa	Increased arterial pressureMidodrine	Increased arterial pressurePargyline	Increased arterial pressurePhenelzine	Increased arterial pressureReserpine	Increased arterial pressureTranylcypromine	Increased arterial pressureOxytocin	Possible marked increase of arterial pressureMethylergonovine	Possible marked increase of arterial pressureLinezolid	Possible increase of arterial pressureErgonovine	Possible marked increase of arterial pressureTrimipramine	The tricyclic increases the sympathomimetic effectProtriptyline	The tricyclic increases the sympathomimetic effectNortriptyline	The tricyclic increases the sympathomimetic effectClomipramine	The tricyclic increases the sympathomimetic effectAmitriptyline	The tricyclic increases the sympathomimetic effectAmoxapine	The tricyclic increases the sympathomimetic effectDesipramine	The tricyclic increases the sympathomimetic effectDoxepin	The tricyclic increases the sympathomimetic effectImipramine	The tricyclic increases the sympathomimetic effectMoclobemide	Moclobemide increases the sympathomimetic effect
  Prednisolone¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Ambenonium	The corticosteroid decreases the effect of anticholinesterasesEdrophonium	The corticosteroid decreases the effect of anticholinesterasesNeostigmine	The corticosteroid decreases the effect of anticholinesterasesPyridostigmine	The corticosteroid decreases the effect of anticholinesterasesWarfarin	The corticosteroid alters the anticoagulant effectAcenocoumarol	The corticosteroid alters the anticoagulant effectDicumarol	The corticosteroid alters the anticoagulant effectAnisindione	The corticosteroid alters the anticoagulant effectMidodrine	Increased arterial pressureAspirin	The corticosteroid decreases the effect of salicylatesBismuth Subsalicylate	The corticosteroid decreases the effect of salicylatesSalicylate-magnesium	The corticosteroid decreases the effect of salicylatesSalicylate-sodium	The corticosteroid decreases the effect of salicylatesSalsalate	The corticosteroid decreases the effect of salicylatesTrisalicylate-choline	The corticosteroid decreases the effect of salicylatesTalbutal	The barbiturate decreases the effect of the corticosteroidSecobarbital	The barbiturate decreases the effect of the corticosteroidQuinidine barbiturate	The barbiturate decreases the effect of the corticosteroidPrimidone	The barbiturate decreases the effect of the corticosteroidPhenobarbital	The barbiturate decreases the effect of the corticosteroidPentobarbital	The barbiturate decreases the effect of the corticosteroidMethylphenobarbital	The barbiturate decreases the effect of the corticosteroidMethohexital	The barbiturate decreases the effect of the corticosteroidHexobarbital	The barbiturate decreases the effect of the corticosteroidHeptabarbital	The barbiturate decreases the effect of the corticosteroidDihydroquinidine barbiturate	The barbiturate decreases the effect of the corticosteroidButethal	The barbiturate decreases the effect of the corticosteroidButalbital	The barbiturate decreases the effect of the corticosteroidButabarbital	The barbiturate decreases the effect of the corticosteroidAprobarbital	The barbiturate decreases the effect of the corticosteroidAmobarbital	The barbiturate decreases the effect of the corticosteroidChlorotrianisene	The estrogenic agent increases the effect of the corticosteroidClomifene	The estrogenic agent increases the effect of the corticosteroidDiethylstilbestrol	The estrogenic agent increases the effect of the corticosteroidEstradiol	The estrogenic agent increases the effect of the corticosteroidEstriol	The estrogenic agent increases the effect of the corticosteroidConjugated Estrogens	The estrogenic agent increases the effect of the corticosteroidEstrone	The estrogenic agent increases the effect of the corticosteroidEstropipate	The estrogenic agent increases the effect of the corticosteroidEthinyl Estradiol	The estrogenic agent increases the effect of the corticosteroidMestranol	The estrogenic agent increases the effect of the corticosteroidQuinestrol	The estrogenic agent increases the effect of the corticosteroidEthotoin	The enzyme inducer decreases the effect of the corticosteroidFosphenytoin	The enzyme inducer decreases the effect of the corticosteroidMephenytoin	The enzyme inducer decreases the effect of the corticosteroidPhenytoin	The enzyme inducer decreases the effect of the corticosteroidRifampin	The enzyme inducer decreases the effect of the corticosteroidItraconazole	The imidazole increases the effect and toxicity of the corticosteroidKetoconazole	The imidazole increases the effect and toxicity of the corticosteroid
  Sulfacetamide¿¡ ´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 | 
    
       Phenylephrine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.
  Prednisolone¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with food to reduce gastric irritation.Avoid alcohol. Avoid caffeine. 
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    | Drug Target | 
    
      
      [Drug Target]
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    | Description | 
    
       Phenylephrine¿¡ ´ëÇÑ Description Á¤º¸ An alpha-adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent. [PubChem]
  Prednisolone¿¡ ´ëÇÑ Description Á¤º¸ A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states. [PubChem]
  Sulfacetamide¿¡ ´ëÇÑ Description Á¤º¸ An anti-infective agent that is used topically to treat skin infections and orally for urinary tract infections. [PubChem] 
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    | Dosage Form | 
    
       Phenylephrine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid	IntramuscularLiquid	IntravenousLiquid	OphthalmicOintment	TopicalSolution	IntravenousSolution / drops	OphthalmicStrip	OralTablet	Oral
  Prednisolone¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid	OralSolution	OralSolution / drops	OphthalmicSuspension	OphthalmicTablet	Oral
  Sulfacetamide¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid	OphthalmicOintment	OphthalmicSolution / drops	Ophthalmic 
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    | Drug Category | 
    
       Phenylephrine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic alpha-AgonistsCardiotonic AgentsMydriaticsNasal DecongestantsSympathomimeticsVasoconstrictor Agents
  Prednisolone¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic AgentsAnti-inflammatory AgentsAntineoplastic AgentsAntineoplastic Agents, HormonalGlucocorticoids
  Sulfacetamide¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Bacterial AgentsAnti-Infective Agents, LocalAnti-Infective Agents, Urinary 
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    | Smiles String Canonical | 
    
       Phenylephrine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CNCC(O)C1=CC(O)=CC=C1
  Prednisolone¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC12CC(O)C3C(CCC4=CC(=O)C=CC34C)C1CCC2(O)C(=O)CO
  Sulfacetamide¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(=O)NS(=O)(=O)C1=CC=C(N)C=C1 
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    | Smiles String Isomeric | 
    
       Phenylephrine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CNC[C@H](O)C1=CC(O)=CC=C1
  Prednisolone¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ C[C@]12C[C@H](O)[C@H]3[C@@H](CCC4=CC(=O)C=C[C@]34C)[C@@H]1CC[C@]2(O)C(=O)CO
  Sulfacetamide¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(=O)NS(=O)(=O)C1=CC=C(N)C=C1 
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    | InChI Identifier | 
    
       Phenylephrine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C9H13NO2/c1-10-6-9(12)7-3-2-4-8(11)5-7/h2-5,9-12H,6H2,1H3/t9-/m0/s1
  Prednisolone¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C21H28O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h5,7,9,14-16,18,22,24,26H,3-4,6,8,10-11H2,1-2H3/t14-,15-,16-,18+,19-,20-,21-/m0/s1
  Sulfacetamide¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C8H10N2O3S/c1-6(11)10-14(12,13)8-4-2-7(9)3-5-8/h2-5H,9H2,1H3,(H,10,11)/f/h10H 
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    | Chemical IUPAC Name | 
    
       Phenylephrine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-[(1R)-1-hydroxy-2-methylaminoethyl]phenol
  Prednisolone¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
  Sulfacetamide¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ N-(4-aminophenyl)sulfonylacetamide 
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    | Drug-Induced Toxicity Related Proteins | 
    
      PREDNISOLONE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:DNA topoisomerase 1 Drug:prednisolone Toxicity:appearance of apoptotic cells.  [¹Ù·Î°¡±â] 
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                ÃÖ±ÙÁ¤º¸¼öÁ¤ÀÏ 2015-01-21
              
 
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                          ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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