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À¯´Ï¾ÈÁ¡¾È¾× [Chlorpheniramine Maleate , Dipotassium glycyrrhizinate , Sodium chondroitin sulfate , Sulfamethoxazole]
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| µ¶¼ºÁ¤º¸ |
Chlorpheniramine¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Potassium¿¡ ´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 |
Chlorpheniramine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
Sulfamethoxazole¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Sulfonamides inhibit bacterial dihydrofolate synthetase, causing interference in the conversion of p-aminobenzoic acid (PABA) into folic acid. As folic acid is a coenzyme responsible for the transport of one-carbon fragments from one molecule to another, it is an essential component of bacterial development. Pyrimethamine and trimethoprim inhibit dihydrofolate reductase, the immediate next step, and therefore act synergistically with the sulfonamides.
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| Pharmacology |
Chlorpheniramine¿¡ ´ëÇÑ Pharmacology Á¤º¸ In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Chlorpheniramine, is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.
Sulfamethoxazole¿¡ ´ëÇÑ Pharmacology Á¤º¸ Sulfamethoxazole is a sulfonamide drug that inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA). Sulfamethoxazole is normally given in combination with Trimethoprim (a dihydrofolate reductase inhibitor). Studies have shown that bacterial resistance develops more slowly with the combination of the two drugs than with either Trimethoprim or Sulfamethoxazole alone.
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| Protein Binding |
Chlorpheniramine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 72%
Sulfamethoxazole¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 70%
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| Half-life |
Chlorpheniramine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 21-27 hours
Sulfamethoxazole¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 10 hours
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| Absorption |
Chlorpheniramine¿¡ ´ëÇÑ Absorption Á¤º¸ Well absorbed in the gastrointestinal tract.
Sulfamethoxazole¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed following oral administration.
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| Pharmacokinetics |
SulfamethoxazoleÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- »ýü³»ÀÌ¿ë·ü : °æ±¸ : 90%
- ºÐÆ÷ : ŹÝÅë°ú, ³úô¼ö¾×À¸·Î ¿ëÀÌÇÏ°Ô È®»ê
- ´Ü¹é°áÇÕ : 70%
- ´ë»ç : ÀÏÂ÷ÀûÀ¸·Î °£´ë»ç, 10-20%´Â Ç÷¾×¿¡¼ N-acetylationµÈ´Ù.
- ¹Ý°¨±â : 9-12 ½Ã°£, ½ÅÀå¾Ö½Ã ¿¬Àå
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 3-4 ½Ã°£ À̳»
- ¼Ò½Ç : 20%´Â ¹Ìº¯Èü·Î, ³ª¸ÓÁö´Â ´ë»çü·Î ½Å¹è¼³
Chlorpheniramine MaleateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ´Ü¹é°áÇÕ : 69-72%
- ´ë»ç : °£´ë»ç
- ¹Ý°¨±â : 20-24 ½Ã°£
- ¼Ò½Ç : ´ë»çü, ¾à¹°(3-4%)ÀÌ ½Å¹è¼³µÇ¸ç, 48½Ã°£³»¿¡ ÀüüÀÇ 35%°¡ ¼Ò½ÇµÈ´Ù.
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| Biotransformation |
Chlorpheniramine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic via Cytochrome P450 (CYP450) enzymes.
Sulfamethoxazole¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. The metabolism of sulfamethoxazole occurs predominately by N4-acetylation, although the glucuronide conjugate has been identified.
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| Toxicity |
Chlorpheniramine¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50 = 306 mg/kg in humans, mild reproductive toxin to women of childbearing age.
Sulfamethoxazole¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
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| Drug Interactions |
Chlorpheniramine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Donepezil Possible antagonism of actionGalantamine Possible antagonism of actionRivastigmine Possible antagonism of actionEthotoin The antihistamine increases the effect of hydantoinFosphenytoin The antihistamine increases the effect of hydantoinMephenytoin The antihistamine increases the effect of hydantoinPhenytoin The antihistamine increases the effect of hydantoin
Sulfamethoxazole¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Sulfamethoxazole¿¡ ´ëÇÑ P450 table Chlorpheniramine¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 2D6
Beta Blockers:
S-metoprolol
propafenone
timolol
Antidepressants:
amitriptyline
clomipramine
desipramine
imipramine
paroxetine
Antipsychotics:
haloperidol
risperidone
thioridazine
aripiprazole
codeine
dextromethorphan
duloxetine
flecainide
mexiletine
ondansetron
tamoxifen
tramadol
venlafaxine
INHIBITORS
CYP 2D6
amiodarone
buproprion
**chlorpheniramine**
cimetidine
clomipramine
duloxetine
fluoxetine
haloperidol
methadone
mibefradil
paroxetine
quinidine
ritonavir
INDUCERS
CYP 2D6
N/A
SUBSTRATES
CYP 2C9
NSAIDs:
diclofenac
ibuprofen
piroxicam
Oral Hypoglycemic Agents:
tolbutamide
glipizide
Angiotensin II Blockers:
NOT candesartan
irbesartan
losartan
NOT valsartan
celecoxib
fluvastatin naproxen
phenytoin
**sulfamethoxazole**
tamoxifen
tolbutamide
torsemide
warfarin
INHIBITORS
CYP 2C9
amiodarone
fluconazole
isoniazid
INDUCERS
CYP 2C9
rifampin
secobarbital
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| Drug Target |
[Drug Target]
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| Description |
Chlorpheniramine¿¡ ´ëÇÑ Description Á¤º¸ A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than promethazine. [PubChem]
Sulfamethoxazole¿¡ ´ëÇÑ Description Á¤º¸ A bacteriostatic antibacterial agent that interferes with folic acid synthesis in susceptible bacteria. Its broad spectrum of activity has been limited by the development of resistance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p208)
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| Dosage Form |
Chlorpheniramine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Syrup OralTablet OralTablet, extended release Oral
Sulfamethoxazole¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Chlorpheniramine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Allergic AgentsAntihistaminesAntipruriticsHistamine H1 Antagonists
Sulfamethoxazole¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Infective AgentsAnti-InfectivesSulfonamides
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| Smiles String Canonical |
Chlorpheniramine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)CCC(C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Sulfamethoxazole¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC1=CC(NS(=O)(=O)C2=CC=C(N)C=C2)=NO1
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| Smiles String Isomeric |
Chlorpheniramine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)CC[C@H](C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Sulfamethoxazole¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC1=CC(NS(=O)(=O)C2=CC=C(N)C=C2)=NO1
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| InChI Identifier |
Chlorpheniramine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C16H19ClN2/c1-19(2)12-10-15(16-5-3-4-11-18-16)13-6-8-14(17)9-7-13/h3-9,11,15H,10,12H2,1-2H3
Sulfamethoxazole¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C10H11N3O3S/c1-7-6-10(12-16-7)13-17(14,15)9-4-2-8(11)3-5-9/h2-6H,11H2,1H3,(H,12,13)/f/h13H
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| Chemical IUPAC Name |
Chlorpheniramine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine
Sulfamethoxazole¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 4-amino-N-(5-methyl-1,2-oxazol-3-yl)benzenesulfonamide
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| Drug-Induced Toxicity Related Proteins |
MALEATE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Intercellular adhesion molecule 1 Drug:maleate Toxicity:hepatic injury. [¹Ù·Î°¡±â] SULFAMETHOXAZOLE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Myeloperoxidase Drug:sulfamethoxazole Toxicity:agranulocytosis. [¹Ù·Î°¡±â] Replated Protein:Myeloperoxidase Drug:sulfamethoxazole Toxicity:lupus. [¹Ù·Î°¡±â]
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