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      [HydrochlorothiazideÀÇ ÈÇб¸Á¶Á¤º¸] [HydrochlorothiazideÀÇ ¹°¼ºÁ¤º¸] CAS number  /58-93-5 ATC code  /C03 AA03 PubChem  /3639 Formula  /C 7 H 8 Cl N 3 O 4 S 2 Mol. mass  /297.742 Bioavailability  /Variably absorbed from GI tract Metabolism  / ? Excretion  /Primarily excreted unchanged in urine Pregnancy cat.  /
B (D if used to treat pregnancy-induced hypertension) Legal status  /
℞ Prescription only   Routes  /Oral (capsules, tablets, oral solution)  
     
         
  
   
    Mechanism of Action 
    
      Bisoprolol¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸  Bisoprolol selectively blocks catecholamine stimulation of beta(1)-adrenergic receptors in the heart and vascular smooth muscle. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. Bisoprolol can also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles, causing bronchospasm.Hydrochlorothiazide¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸  As a diuretic, hydrochlorothiazide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like hydrochlorothiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of hydrochlorothiazide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle. 
     
   
  
   
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      Bisoprolol¿¡ ´ëÇÑ Pharmacology Á¤º¸  Bisoprolol is a competitive, beta(1)-selective (cardioselective) adrenergic antagonist. Bisoprolol is used to treat hypertension, arrhythmias, coronary heart disease, glaucoma, and is also used to reduce non-fatal cardiac events in patients with heart failure. Activation of beta(1)-receptors (located mainly in the heart) by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Drugs such as Bisoprolol that block these receptors therefore have the reverse effect: they lower the heart rate and blood pressure and hence are used in conditions when the heart itself is deprived of oxygen. They are routinely prescribed in patients with ischemic heart disease. In addition, beta(1)-selective blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. Bisoprolol is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane stabilizing activity.Hydrochlorothiazide¿¡ ´ëÇÑ Pharmacology Á¤º¸  Thiazides such as hydrochlorothiazide promote water loss from the body (diuretics). They inhibit Na+ /Cl-  reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue. 
     
   
  
   
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Bisoprolol FumarateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á  
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    Toxicity 
    
      Bisoprolol¿¡ ´ëÇÑ Toxicity Á¤º¸  Oral, mouse: LD50  = 100 mg/kg; Skin, rabbit: LD50  = 200 mg/kg; Skin, rat: LD50  = 500 mg/kg. Symptoms of overdose include congestive heart failure (marked by sudden weight gain, swelling of the legs, feet, and ankles, fatigue, and shortness of breath), difficult or labored breathing, low blood pressure, low blood sugar, and slow heartbeat.Hydrochlorothiazide¿¡ ´ëÇÑ Toxicity Á¤º¸  The most common signs and symptoms observed are those caused by electrolyte depletion (hypokalemia, hypochloremia, hyponatremia) and dehydration resulting from excessive diuresis. If digitalis has also been administered, hypokalemia may accentuate cardiac arrhythmias. The oral LD50 of hydrochlorothiazide is greater than 10 g/kg in the mouse and rat. 
     
   
  
   
    Drug Interactions 
    
      Bisoprolol¿¡ ´ëÇÑ Drug_Interactions Á¤º¸  Acetohexamide	The beta-blocker decreases the symptoms of hypoglycemiaChlorpropamide	The beta-blocker decreases the symptoms of hypoglycemiaClonidine	Increased hypertension when clonidine stoppedDihydroergotamine	Ischemia with risk of gangreneDihydroergotoxine	Ischemia with risk of gangreneDisopyramide	The beta-blocker increases toxicity of disopyramideEpinephrine	Hypertension, then bradycardiaErgonovine	Ischemia with risk of gangreneErgotamine	Ischemia with risk of gangreneFenoterol	AntagonismFormoterol	AntagonismGliclazide	The beta-blocker decreases the symptoms of hypoglycemiaGlipizide	The beta-blocker decreases the symptoms of hypoglycemiaGlisoxepide	The beta-blocker decreases the symptoms of hypoglycemiaGlibenclamide	The beta-blocker decreases the symptoms of hypoglycemiaGlycodiazine	The beta-blocker decreases the symptoms of hypoglycemiaIbuprofen	Risk of inhibition of renal prostaglandinsIndomethacin	Risk of inhibition of renal prostaglandinsInsulin	The beta-blocker decreases the symptoms of hypoglycemiaInsulin-aspart	The beta-blocker decreases the symptoms of hypoglycemiaInsulin-detemir	The beta-blocker decreases the symptoms of hypoglycemiaInsulin-glargine	The beta-blocker decreases the symptoms of hypoglycemiaInsulin-glulisine	The beta-blocker decreases the symptoms of hypoglycemiaInsulin-lispro	The beta-blocker decreases the symptoms of hypoglycemiaIsoproterenol	AntagonismLidocaine	The beta-blocker increases the effect and toxicity of lidocaineMethysergide	Ischemia with risk of gangreneOrciprenaline	AntagonismPirbuterol	AntagonismPiroxicam	Risk of inhibition of renal prostaglandinsPrazosin	Risk of hypotension at the beginning of therapyProcaterol	AntagonismRepaglinide	The beta-blocker decreases the symptoms of hypoglycemiaRifampin	Rifampin decreases the effect of the metabolized beta-blockerSalbutamol	AntagonismSalmeterol	AntagonismTerbutaline	AntagonismTolazamide	The beta-blocker decreases the symptoms of hypoglycemiaTolbutamide	The beta-blocker decreases the symptoms of hypoglycemiaVerapamil	Increased effect of both drugsHydrochlorothiazide¿¡ ´ëÇÑ Drug_Interactions Á¤º¸  Amantadine	The diuretic increases the adverse effect of amantadineDeslanoside	Possible electrolyte variations and arrhythmiasDigitoxin	Possible electrolyte variations and arrhythmiasDigoxin	Possible electrolyte variations and arrhythmiasLithium	The thiazide diuretic increases serum levels of lithiumDofetilide	Increased risk of cardiotoxicity and arrhythmiasDiazoxide	Significant hyperglycemic effect 
     
   
  
   
    CYP450  Drug Interaction 
    
      [CYP450 TableÁ÷Á¢Á¶È¸]  
     
   
  
   
    Drug Target 
    
      
      [Drug Target]  
     
   
  
   
    Description 
    
      Bisoprolol¿¡ ´ëÇÑ Description Á¤º¸  A cardioselective beta-1-adrenergic blocker. It is effective in the management of hypertension and angina pectoris. [PubChem]Fumarate¿¡ ´ëÇÑ Description Á¤º¸  Not AvailableHydrochlorothiazide¿¡ ´ëÇÑ Description Á¤º¸  A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It has been used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism. [PubChem] 
     
   
  
   
    Drug Category 
    
      Bisoprolol¿¡ ´ëÇÑ Drug_Category Á¤º¸  Adrenergic AgentsAdrenergic beta-AntagonistsAntihypertensive AgentsSympatholyticsFumarate¿¡ ´ëÇÑ Drug_Category Á¤º¸  Not AvailableHydrochlorothiazide¿¡ ´ëÇÑ Drug_Category Á¤º¸  Antihypertensive AgentsDiureticsSodium Chloride Symporter Inhibitors 
     
   
  
   
    Smiles String Canonical 
    
      Bisoprolol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸  CC(C)NCC(O)COC1=CC=C(COCCOC(C)C)C=C1Fumarate¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸  [O-]C(=O)C=CC([O-])=OHydrochlorothiazide¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸  NS(=O)(=O)C1=C(Cl)C=C2NCNS(=O)(=O)C2=C1 
     
   
  
   
    Smiles String Isomeric 
    
      Bisoprolol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸  CC(C)NC[C@@H](O)COC1=CC=C(COCCOC(C)C)C=C1Fumarate¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸  [O-]C(=O)\C=C\C([O-])=OHydrochlorothiazide¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸  NS(=O)(=O)C1=C(Cl)C=C2NCNS(=O)(=O)C2=C1 
     
   
  
   
    InChI Identifier 
    
      Bisoprolol¿¡ ´ëÇÑ InChI_Identifier Á¤º¸  InChI=1/C18H31NO4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4/h5-8,14-15,17,19-20H,9-13H2,1-4H3Fumarate¿¡ ´ëÇÑ InChI_Identifier Á¤º¸  InChI=1/C4H4O4/c5-3(6)1-2-4(7)8/h1-2H,(H,5,6)(H,7,8)/p-2/b2-1+/fC4H2O4/q-2Hydrochlorothiazide¿¡ ´ëÇÑ InChI_Identifier Á¤º¸  InChI=1/C7H8ClN3O4S2/c8-4-1-5-7(2-6(4)16(9,12)13)17(14,15)11-3-10-5/h1-2,10-11H,3H2,(H2,9,12,13)/f/h9H2 
     
   
  
   
    Chemical IUPAC Name 
    
      Bisoprolol¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸  1-(propan-2-ylamino)-3-[4-(2-propan-2-yloxyethoxymethyl)phenoxy]propan-2-olFumarate¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸  but-2-enedioic acidHydrochlorothiazide¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸  6-chloro-1,1-dioxo-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine-7-sulfonamide 
     
   
  
   
    Drug-Induced Toxicity Related Proteins 
    
      BISOPROLOL   ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸Replated Protein  :CYP2D6Drug  :Bisoprolol Toxicity  :Increased beta-blockade. [¹Ù·Î°¡±â]  
     
   
    
 
	  
	   
	
	  
       
	    
	      
	        
            
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