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¿ÀÅ¥·ÐÁ¡¾È¾× OCULON EYE DROPS[Phenylephrine HCl , Prednisolone acetate , Sulfacetamide sodium]
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650203250[A08502261]
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| 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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- ÇÇÇÏÁÖ»ç : 1½Ã°£
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Prednisolone acetateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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Sulfacetamide sodiumÀÇ 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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º» ¼öÁ¤ÀÏ Á¤º¸´Â Çã°¡Á¤º¸ ÀÌ¿ÜÀÇ ±âŸÁ¤º¸ ¼öÁ¤ÀÏÀ» ÀǹÌÇϹǷÎ, Çã°¡Á¤º¸¼öÁ¤ÀÏÀº º»¹®¿¡ Ç¥±âµÈ ³¯Â¥¸¦ ÂüÁ¶ÇϽñ⠹ٶø´Ï´Ù.
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Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´Â
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¹Ýµå½Ã Á¦Á¶¡¤¼öÀÔ»ç, ÆÇ¸Å»ç, ÀÇ»ç, ¾à»ç¿¡°Ô ÃÖÁ¾ÀûÀ¸·Î È®ÀÎÇϽñ⠹ٶø´Ï´Ù.
ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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