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| Related FDA Approved Drug |
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Bisoprolol and thiazides / C07BB07
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 [HydrochlorothiazideÀÇ ¹°¼ºÁ¤º¸] CAS number/58-93-5 ATC code/C03AA03 PubChem/3639 Formula/C7H8ClN3O4S2 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)
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| 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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| Pharmacology |
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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| Absorption |
Bisoprolol¿¡ ´ëÇÑ Absorption Á¤º¸ 80%
Hydrochlorothiazide¿¡ ´ëÇÑ Absorption Á¤º¸ 50-60%
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| Pharmacokinetics |
HydrochlorothiazideÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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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.
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| 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 drugs
Hydrochlorothiazide¿¡ ´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
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Drug Target |
[Drug Target]
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| 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 Available
Hydrochlorothiazide¿¡ ´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]
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| Drug Category |
Bisoprolol¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic AgentsAdrenergic beta-AntagonistsAntihypertensive AgentsSympatholytics
Fumarate¿¡ ´ëÇÑ Drug_Category Á¤º¸ Not Available
Hydrochlorothiazide¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antihypertensive AgentsDiureticsSodium Chloride Symporter Inhibitors
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| Smiles String Canonical |
Bisoprolol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(C)NCC(O)COC1=CC=C(COCCOC(C)C)C=C1
Fumarate¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ [O-]C(=O)C=CC([O-])=O
Hydrochlorothiazide¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ NS(=O)(=O)C1=C(Cl)C=C2NCNS(=O)(=O)C2=C1
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| Smiles String Isomeric |
Bisoprolol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(C)NC[C@@H](O)COC1=CC=C(COCCOC(C)C)C=C1
Fumarate¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ [O-]C(=O)\C=C\C([O-])=O
Hydrochlorothiazide¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ NS(=O)(=O)C1=C(Cl)C=C2NCNS(=O)(=O)C2=C1
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| 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,9-13H2,1-4H3
Fumarate¿¡ ´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-2
Hydrochlorothiazide¿¡ ´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
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| Chemical IUPAC Name |
Bisoprolol¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 1-(propan-2-ylamino)-3-[4-(2-propan-2-yloxyethoxymethyl)phenoxy]propan-2-ol
Fumarate¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ but-2-enedioic acid
Hydrochlorothiazide¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 6-chloro-1,1-dioxo-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine-7-sulfonamide
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| Drug-Induced Toxicity Related Proteins |
BISOPROLOL ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:CYP2D6 Drug:Bisoprolol Toxicity:Increased beta-blockade. [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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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.
¹Ýµå½Ã Á¦Á¶¡¤¼öÀÔ»ç, ÆÇ¸Å»ç, ÀÇ»ç, ¾à»ç¿¡°Ô ÃÖÁ¾ÀûÀ¸·Î È®ÀÎÇϽñ⠹ٶø´Ï´Ù.
ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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