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Åäºñ·ÕÁ¡¾È¾× TOBILONG EYE DROP[Allantoin , Chlorpheniramine Maleate , Chondroitin Sodium Sulfate , Dipotassium glycyrrhizinate , Neostigmine
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15ML/CASE
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| Pharmacokinetics |
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
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°í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
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| µ¶¼ºÁ¤º¸ |
Chlorpheniramine¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Magnesium¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Potassium¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Pyridoxine¿¡ ´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.
Neostigmine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Neostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors. It does not cross the blood-brain barrier.
Potassium¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Potassium is the major cation (positive ion) inside animal cells, while sodium is the major cation outside animal cells. The concentration differences of these charged particles causes a difference in electric potential between the inside and outside of cells, known as the membrane potential. The balance between potassium and sodium is maintained by ion pumps in the cell membrane. The cell membrane potential created by potassium and sodium ions allows the cell generate an action potential?”a "spike" of electrical discharge. The ability of cells to produce electrical discharge is critical for body functions such as neurotransmission, muscle contraction, and heart function. Potassium is also an essential mineral needed to regulate water balance, blood pressure and levels of acidity.
magnesium¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Not Available
Pyridoxine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Vitamin B6 is the collective term for a group of three related compounds, pyridoxine (PN), pyridoxal (PL) and pyridoxamine (PM), and their phosphorylated derivatives, pyridoxine 5'-phosphate (PNP), pyridoxal 5'-phosphate (PLP) and pyridoxamine 5'-phosphate (PMP). Although all six of these compounds should technically be referred to as vitamin B6, the term vitamin B6 is commonly used interchangeably with just one of them, pyridoxine. Vitamin B6, principally in the form of the coenzyme pyridoxal 5'-phosphate, is involved in a wide range of biochemical reactions, including the metabolism of amino acids and glycogen, the synthesis of nucleic acids, hemogloblin, sphingomyelin and other sphingolipids, and the synthesis of the neurotransmitters serotonin, dopamine, norepinephrine and gamma-aminobutyric acid (GABA).
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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.
Neostigmine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Neostigmine is a cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike physostigmine, does not cross the blood-brain barrier.
Potassium¿¡ ´ëÇÑ Pharmacology Á¤º¸ Not Available
Pyridoxine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Vitamin B6 (pyridoxine) is a water-soluble vitamin used in the prophylaxis and treatment of vitamin B6 deficiency and peripheral neuropathy in those receiving isoniazid (isonicotinic acid hydrazide, INH). Vitamin B6 has been found to lower systolic and diastolic blood pressure in a small group of subjects with essential hypertension. Hypertension is another risk factor for atherosclerosis and coronary heart disease. Another study showed pyridoxine hydrochloride to inhibit ADP- or epinephrine-induced platelet aggregation and to lower total cholesterol levels and increase HDL-cholesterol levels, again in a small group of subjects. Vitamin B6, in the form of pyridoxal 5'-phosphate, was found to protect vascular endothelial cells in culture from injury by activated platelets. Endothelial injury and dysfunction are critical initiating events in the pathogenesis of atherosclerosis. Human studies have demonstrated that vitamin B6 deficiency affects cellular and humoral responses of the immune system. Vitamin B6 deficiency results in altered lymphocyte differentiation and maturation, reduced delayed-type hypersensitivity (DTH) responses, impaired antibody production, decreased lymphocyte proliferation and decreased interleukin (IL)-2 production, among other immunologic activities.
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| Protein Binding |
Chlorpheniramine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 72%
Neostigmine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Protein binding to human serum albumin ranges from 15 to 25 percent.
Pyridoxine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 22%
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| Half-life |
Chlorpheniramine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 21-27 hours
Neostigmine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ The half-life ranged from 42 to 60 minutes with a mean half-life of 52 minutes.
Pyridoxine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 15-20 days
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| Absorption |
Chlorpheniramine¿¡ ´ëÇÑ Absorption Á¤º¸ Well absorbed in the gastrointestinal tract.
Neostigmine¿¡ ´ëÇÑ Absorption Á¤º¸ Neostigmine bromide is poorly absorbed from the gastrointestinal tract following oral administration
Potassium¿¡ ´ëÇÑ Absorption Á¤º¸ Not Available
Pyridoxine¿¡ ´ëÇÑ Absorption Á¤º¸ The B vitamins are readily absorbed from the gastrointestinal tract, except in malabsorption syndromes. Pyridoxine is absorbed mainly in the jejunum.
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| Pharmacokinetics |
Pyridoxine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : À§Àå°üÀ¸·ÎºÎÅÍ Àß Èí¼öµÈ´Ù.
- ´ë»ç : °£¿¡¼ 4-pyridoxic acid·Î ´ë»çµÈ´Ù.
- ¹Ý°¨±â : 15-20ÀÏ
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : °æ±¸ : 1.25 ½Ã°£
- ¼Ò½Ç : 4-pyridoxic acid·Î ½Å¹è¼³µÇ¸ç, ¼Ò·® (¾à 2%)Àº ´ãÁóÀ» ÅëÇØ ¹è¼³µÈ´Ù.
Neostigmine MethylsulfateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£ :
- °æ±¸ : 45-75ºÐ
- ±ÙÀ°ÁÖ»ç : 20-30ºÐ
- Á¤¸ÆÁÖ»ç : 4-8ºÐ
- ÀÛ¿ëÁö¼Ó½Ã°£ : °æ±¸, ±ÙÀ°ÁÖ»ç, Á¤¸ÆÁÖ»ç : 2-4 ½Ã°£
- Èí¼ö : °æ±¸ : Àß Èí¼öµÇÁö ¾ÊÀ½ (2% À̳»)
- ´Ü¹é°áÇÕ : 15-25%
- ´ë»ç : Cholinesterase¿¡ ÀÇÇØ °¡¼öºÐÇØ, °£¿¡¼ ´ë»çµÊ
- ¹Ý°¨±â : Á¤»ó ½Å±â´É : 0.5-2.1 ½Ã°£ (¸»±â½ÅÁúȯ¿¡¼´Â ¿¬ÀåµÊ)
- ¼Ò½Ç : 24½Ã°£ À̳»¿¡´Â 80%°¡ ½Å¹è¼³µÊ (¾à 50%´Â ¹Ìº¯Èü·Î, 30%´Â ´ë»çü·Î)
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.
Neostigmine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Neostigmine undergoes hydrolysis by cholinesterase and is also metabolized by microsomal enzymes in the liver.
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| Toxicity |
Chlorpheniramine¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50 = 306 mg/kg in humans, mild reproductive toxin to women of childbearing age.
Neostigmine¿¡ ´ëÇÑ Toxicity Á¤º¸ Overdosage of Neostigmine can cause cholinergic crisis, which is characterized by increasing muscle weakness, and through involvement of the muscles of respiration, may result in death. The LD 50 of neostigmine methylsulfate in mice is 0.3 ¡¾ 0.02 mg/kg intravenously, 0.54 ¡¾ 0.03 mg/kg subcutaneously, and 0.395 ¡¾ 0.025 mg/kg intramuscularly; in rats the LD 50 is 0.315 ¡¾ 0.019 mg/kg intravenously, 0.445 ¡¾ 0.032 mg/kg subcutaneously, and 0.423 ¡¾ 0.032 mg/kg intramuscularly.
Potassium¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
Pyridoxine¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral Rat LD50 = 4 gm/kg. Toxic effects include convulsions, dyspnea, hypermotility, diarrhea, ataxia and muscle weakness.
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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
Neostigmine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
Potassium¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amiloride Increased risk of hyperkaliemiaBenazepril Increased risk of hyperkaliemiaCandesartan Increased risk of hyperkaliemiaCaptopril Increased risk of hyperkaliemiaCilazapril Increased risk of hyperkaliemiaDrospirenone Increased risk of hyperkaliemiaEnalapril Increased risk of hyperkaliemiaEplerenone This association presents an increased risk of hyperkaliemiaEprosartan Increased risk of hyperkaliemiaForasartan Increased risk of hyperkaliemiaFosinopril Increased risk of hyperkaliemiaIrbesartan Increased risk of hyperkaliemiaLisinopril Increased risk of hyperkaliemiaLosartan Increased risk of hyperkaliemiaMoexipril Increased risk of hyperkaliemiaPerindopril Increased risk of hyperkaliemiaPolystyrene sulfonate Antagonism of actionQuinapril Increased risk of hyperkaliemiaRamipril Increased risk of hyperkaliemiaSaprisartan Increased risk of hyperkaliemiaSpirapril Increased risk of hyperkaliemiaSpironolactone Increased risk of hyperkaliemiaTasosartan Increased risk of hyperkaliemiaTelmisartan Increased risk of hyperkaliemiaTrandolapril Increased risk of hyperkaliemiaTriamterene Increased risk of hyperkaliemiaValsartan Increased risk of hyperkaliemia
magnesium¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alendronate Formation of non-absorbable complexesCiprofloxacin Formation of non-absorbable complexesClodronate Formation of non-absorbable complexesDemeclocycline Formation of non-absorbable complexesDoxycycline Formation of non-absorbable complexesEnoxacin Formation of non-absorbable complexesEtidronic acid Formation of non-absorbable complexesGatifloxacin Formation of non-absorbable complexesGemifloxacin Formation of non-absorbable complexesGrepafloxacin Formation of non-absorbable complexesIbandronate Formation of non-absorbable complexesLevofloxacin Formation of non-absorbable complexesLomefloxacin Formation of non-absorbable complexesMethacycline Formation of non-absorbable complexesMinocycline Formation of non-absorbable complexesMoxifloxacin Formation of non-absorbable complexesNorfloxacin Formation of non-absorbable complexesOfloxacin Formation of non-absorbable complexesOxytetracycline Formation of non-absorbable complexesPefloxacin Formation of non-absorbable complexesRisedronate Formation of non-absorbable complexesTrovafloxacin Formation of non-absorbable complexesTetracycline Formation of non-absorbable complexesTemafloxacin Formation of non-absorbable complexesAmprenavir The antiacid decreases the absorption of amprenavirChloroquine The antiacid decreases the absorption of chloroquineAtazanavir This gastric pH modifier decreases the levels/effects of atazanavirDelavirdine The antiacid decreases the absorption of delavirdineDihydroquinidine barbiturate The antiacid decreases the absorption of quinidineFosamprenavir The antiacid decreases the absorption of amprenavirIndinavir The antiacid decreases the absorption of indinavirQuinidine The antiacid decreases the absorption of quindineQuinidine barbiturate The antiacid decreases the absorption of quinidinePolystyrene sulfonate Risk of alkalosis in renal impairmentRosuvastatin The antiacid decreases the absorption of rosuvastatin
Pyridoxine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] 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
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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]
Neostigmine¿¡ ´ëÇÑ Description Á¤º¸ A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike physostigmine, does not cross the blood-brain barrier. [PubChem]
Potassium¿¡ ´ëÇÑ Description Á¤º¸ Potassium is the major cation (positive ion) inside animal cells, while sodium is the major cation outside animal cells. The concentration differences of these charged particles causes a difference in electric potential between the inside and outside of cells, known as the membrane potential. The balance between potassium and sodium is maintained by ion pumps in the cell membrane. The cell membrane potential created by potassium and sodium ions allows the cell generate an action potential?”a "spike" of electrical discharge. The ability of cells to produce electrical discharge is critical for body functions such as neurotransmission, muscle contraction, and heart function. Potassium is also an essential mineral needed to regulate water balance, blood pressure and levels of acidity.
magnesium¿¡ ´ëÇÑ Description Á¤º¸ Magnesium hydroxide is used primarily in "Milk of Magnesia", a white aqueous, mildly alkaline suspension of magnesium hydroxide formulated at about 8%w/v. Milk of magnesia is primarily used to alleviate constipation, but can also be used to relieve indigestion and heartburn. When taken internally by mouth as a laxative, the osmotic force of the magnesia suspension acts to draw fluids from the body and to retain those already within the lumen of the intestine, serving to distend the bowel, thus stimulating nerves within the colon wall, inducing peristalsis and resulting in evacuation of colonic contents.
Pyridoxine¿¡ ´ëÇÑ Description Á¤º¸ The 4-methanol form of vitamin B 6 which is converted to pyridoxal phosphate which is a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. Although pyridoxine and Vitamin B 6 are still frequently used as synonyms, especially by medical researchers, this practice is erroneous and sometimes misleading (EE Snell; Ann NY Acad Sci, vol 585 pg 1, 1990). [PubChem]
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| Dosage Form |
Chlorpheniramine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Syrup OralTablet OralTablet, extended release Oral
Neostigmine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid IntramuscularLiquid IntravenousTablet Oral
Potassium¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Aerosol OralCapsule OralCapsule, extended release OralElixir OralLiquid IntravenousLiquid OralLiquid SublingualPowder OralPowder, for solution OralSolution IntravenousSolution OralSolution / drops OralTablet OralTablet, extended release Oral
magnesium¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Aerosol OralCapsule OralLiquid IntramuscularLiquid IntravenousLiquid OralOintment TopicalPellet OralPowder OralSolution IntramuscularSolution IntravenousSolution OralSolution / drops OralSuspension OralSyrup OralTablet Oral
Pyridoxine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid IntramuscularSolution IntramuscularSolution / drops OralTablet Oral
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| Drug Category |
Chlorpheniramine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Allergic AgentsAntihistaminesAntipruriticsHistamine H1 Antagonists
Neostigmine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Cholinesterase InhibitorsParasympathomimetics
magnesium¿¡ ´ëÇÑ Drug_Category Á¤º¸ Not Available
Pyridoxine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-inflammatory AgentsEssential VitaminVitamin B ComplexVitamins (Vitamin B Complex)
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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
Neostigmine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)C(=O)OC1=CC(=CC=C1)[N+](C)(C)C
Potassium¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ Not Available
magnesium¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ [Mg++]
Pyridoxine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC1=NC=C(CO)C(CO)=C1O
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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
Neostigmine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)C(=O)OC1=CC(=CC=C1)[N+](C)(C)C
Potassium¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ Not Available
magnesium¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ [Mg++]
Pyridoxine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC1=NC=C(CO)C(CO)=C1O
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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
Neostigmine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C12H19N2O2/c1-13(2)12(15)16-11-8-6-7-10(9-11)14(3,4)5/h6-9H,1-5H3/q+1
Potassium¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ Not Available
magnesium¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/Mg/q+2
Pyridoxine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C8H11NO3/c1-5-8(12)7(4-11)6(3-10)2-9-5/h2,10-12H,3-4H2,1H3
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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
Neostigmine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ [3-(dimethylcarbamoyloxy)phenyl]-trimethylazanium
Potassium¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ Not Available
magnesium¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ magnesium(+2) cation
Pyridoxine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 4,5-bis(hydroxymethyl)-2-methylpyridin-3-ol
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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]
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