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Chlorpheniramine¿¡ ´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.
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.
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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.
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.
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| Metabolism |
Chlorpheniramine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)Cytochrome P450 2D6 (CYP2D6)
Phenylephrine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Monoamine oxidase type A (MAO-A)
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| Protein Binding |
Chlorpheniramine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 72%
Phenylephrine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 95% binding-plasma proteins
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| Half-life |
Chlorpheniramine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 21-27 hours
Phenylephrine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2.1 to 3.4 hours
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| Absorption |
Chlorpheniramine¿¡ ´ëÇÑ Absorption Á¤º¸ Well absorbed in the gastrointestinal tract.
Phenylephrine¿¡ ´ëÇÑ Absorption Á¤º¸ Reduced bioavailability (compared to pseudoephedrine) following oral administration due to significant first-pass metabolism.
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| Pharmacokinetics |
Phenylephrine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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- ´ë»ç : Phenolic Æ÷ÇÕü·Î ´ë»çµÊ. Monoamine oxidase¿¡ ÀÇÇØ °£°ú Àå¿¡¼ ´ë»çµÊ.
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- ¼Ò½Ç : ½Å¹è¼³ (90%)
Chlorpheniramine MaleateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ´Ü¹é°áÇÕ : 69-72%
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| Biotransformation |
Chlorpheniramine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic via Cytochrome P450 (CYP450) enzymes.
Phenylephrine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Oral phenylephrine is extensively metabolised by monoamine oxidase, an enzyme which is present in the stomach and 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.
Phenylephrine¿¡ ´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
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
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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.
Phenylephrine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.
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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]
Phenylephrine¿¡ ´ëÇÑ Description Á¤º¸ An alpha-adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent. [PubChem]
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| Dosage Form |
Chlorpheniramine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Syrup OralTablet OralTablet, extended release Oral
Phenylephrine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid IntramuscularLiquid IntravenousLiquid OphthalmicOintment TopicalSolution IntravenousSolution / drops OphthalmicStrip OralTablet Oral
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| Drug Category |
Chlorpheniramine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Allergic AgentsAntihistaminesAntipruriticsHistamine H1 Antagonists
Phenylephrine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic alpha-AgonistsCardiotonic AgentsMydriaticsNasal DecongestantsSympathomimeticsVasoconstrictor Agents
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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
Phenylephrine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CNCC(O)C1=CC(O)=CC=C1
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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
Phenylephrine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CNC[C@H](O)C1=CC(O)=CC=C1
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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
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
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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
Phenylephrine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-[(1R)-1-hydroxy-2-methylaminoethyl]phenol
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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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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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µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
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
Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù. ÀÚ¼¼ÇÑ ³»¿ëÀº ¡°Ã¥ÀÓÀÇ ÇÑ°è ¹× ¹ýÀû°íÁö¡±¸¦ ÂüÁ¶ÇØ ÁֽʽÿÀ.
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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