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| Off-label Usage |
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| Related FDA Approved Drug |
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| µ¶¼ºÁ¤º¸ |
Chlorpheniramine¿¡ ´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.
L-asparagine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Asparagine, a non-essential amino acid is important in the metabolism of toxic ammonia in the body through the action of asparagine synthase which attaches ammonia to aspartic acid in an amidation reaction. Asparagine is also used as a structural component in many proteins.
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.
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.
L-asparagine¿¡ ´ëÇÑ Pharmacology Á¤º¸ A non-essential amino acid. Asparagine is critical for the production of the body's proteins, enzymes and muscle tissue. Supplements of this amino acid are claimed to balance nervous system function.
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.
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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| Metabolism |
Chlorpheniramine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)Cytochrome P450 2D6 (CYP2D6)
L-asparagine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
Neostigmine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cholinesterase
Pyridoxine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Methylenetetrahydrofolate reductase
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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
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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| 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.
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
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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| Food Interaction |
Chlorpheniramine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with food.Avoid alcohol.
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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]
L-asparagine¿¡ ´ëÇÑ Description Á¤º¸ A non-essential amino acid that is involved in the metabolic control of cell functions in nerve and brain tissue. It is biosynthesized from aspartic acid and ammonia by asparagine synthetase. (From Concise Encyclopedia Biochemistry and Molecular Biology, 3rd ed)
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]
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
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
L-asparagine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Dietary supplementMicronutrientNon-Essential Amino Acids
Neostigmine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Cholinesterase InhibitorsParasympathomimetics
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
L-asparagine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ NC(CC(N)=O)C(O)=O
Neostigmine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)C(=O)OC1=CC(=CC=C1)[N+](C)(C)C
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
L-asparagine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ N[C@@H](CC(N)=O)C(O)=O
Neostigmine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)C(=O)OC1=CC(=CC=C1)[N+](C)(C)C
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
L-asparagine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C4H8N2O3/c5-2(4(8)9)1-3(6)7/h2H,1,5H2,(H2,6,7)(H,8,9)/t2-/m0/s1/f/h8H,6H2
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
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
L-asparagine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (2S)-2,4-diamino-4-oxobutanoic acid
Neostigmine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ [3-(dimethylcarbamoyloxy)phenyl]-trimethylazanium
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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