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¸ðµà·ÎƽÁ¤ [Amiloride HCl , Hydrochlorothiazide]
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Àü¹®ÀǾàǰ | ¹Ì»ý»ê
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µå·°ÀÎÆ÷¿¡¼´Â ÀǾàǰ ÀÎÅÍ³Ý ÆÇ¸Å¸¦ ÇÏÁö ¾Ê½À´Ï´Ù. |
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½ÅÀå¾Ö, °£Àå¾Ö½Ã ¿ë·®Á¶Àý |
À¯·áÁ¤º¸ÀÔ´Ï´Ù.
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| Pharmacokinetics |
À¯·áÁ¤º¸ÀÔ´Ï´Ù.
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| º´¿ë±Ý±â ¹× ¿¬·É´ë±Ý±â ±Ù°ÅÁ¶È¸ |
[º´¿ë±Ý±â ¹× ¿¬·É´ë±Ý±â ±Ù°ÅÁ¶È¸]
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| º¸°ü»ó ÁÖÀÇ |
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| Á¶Á¦½Ã ÁÖÀÇ |
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| Ç׸ñ |
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
º´¿ë±Ý±â :
°í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
[»óÈ£ÀÛ¿ë/º´¿ë±Ý±â°Ë»ö]
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[¿¬·É´ë±Ý±â»ó¼¼°Ë»ö]
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| µ¶¼ºÁ¤º¸ |
Amiloride¿¡ ´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 |
Amiloride¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Amiloride works by inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys by binding to the amiloride-sensitive sodium channels. This promotes the loss of sodium and water from the body, but without depleting potassium. Amiloride exerts its potassium sparing effect through the inhibition of sodium reabsorption at the distal convoluted tubule, cortical collecting tubule and collecting duct; this decreases the net negative potential of the tubular lumen and reduces both potassium and hydrogen secretion and their subsequent excretion. Amiloride is not an aldosterone antagonist and its effects are seen even in the absence of aldosterone.
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 |
Amiloride¿¡ ´ëÇÑ Pharmacology Á¤º¸ Amiloride, an antikaliuretic-diuretic agent, is a pyrazine-carbonyl-guanidine that is unrelated chemically to other known antikaliuretic or diuretic agents. It is an antihypertensive, potassium-sparing diuretic that was first approved for use in 1967 and helps to treat hypertension and congestive heart failure. The drug is often used in conjunction with thiazide or loop diuretics. Due to its potassium-sparing capacities, hyperkalemia (high blood potassium levels) are occasionally observed in patients taking amiloride. The risk is high in concurrent use of ACE inhibitors or spironolactone. Patients are also advised not to use potassium-containing salt replacements.
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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| Metabolism |
Amiloride¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
Hydrochlorothiazide¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
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| Absorption |
Amiloride¿¡ ´ëÇÑ Absorption Á¤º¸ Readily absorbed following oral administration.
Hydrochlorothiazide¿¡ ´ëÇÑ Absorption Á¤º¸ 50-60%
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| Pharmacokinetics |
Amiloride HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö: °æ±¸ : 15~25%
- ÀÛ¿ë¹ßÇö½Ã°£ : 2½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 24½Ã°£
- ºÐÆ÷ : Vd : 350~380 L
- ´Ü¹é°áÇÕ : 23%
- ´ë»ç : Ȱ¼ºÇü ´ë»çü´Â ¾ø´Ù.
- ¹Ý°¨±â
- Á¤»ó ½Å±â´É : 6~9½Ã°£
- ¸»±â ½ÅÁúȯ : 8~144½Ã°£
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 6~10½Ã°£
- ¼Ò½Ç : ¹Ìº¯Èü·Î ´¢¿Í º¯¿¡ µ¿µî·®ÀÌ ¹è¼³µÈ´Ù.
HydrochlorothiazideÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÌ´¢È¿°ú ¹ßÇö½Ã°£ : °æ±¸ : 2½Ã°£ À̳»
- ÃÖ´ëÈ¿°ú ¹ßÇö½Ã°£ : 4½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 6-12½Ã°£
- Èí¼ö : °æ±¸ : 60-80%
- ¼Ò½Ç : ¹Ìº¯Èü·Î ½Å¹è¼³µÈ´Ù.
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| Toxicity |
Amiloride¿¡ ´ëÇÑ Toxicity Á¤º¸ No data are available in regard to overdosage in humans. The oral LD50 of amiloride hydrochloride (calculated as the base) is 56 mg/kg in mice and 36 to 85 mg/kg in rats, depending on the strain. The most likely signs and symptoms to be expected with overdosage are dehydration and electrolyte imbalance.
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 |
Amiloride¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Benazepril Increased risk of hyperkaliemiaCandesartan Increased risk of hyperkaliemiaCaptopril Increased risk of hyperkaliemiaEnalapril Increased risk of hyperkaliemiaEplerenone The association presents an ncreased risk of hyperkaliemiaEprosartan Increased risk of hyperkaliemiaFosinopril Increased risk of hyperkaliemiaIrbesartan Increased risk of hyperkaliemiaLisinopril Increased risk of hyperkaliemiaLosartan Increased risk of hyperkaliemiaMoexipril Increased risk of hyperkaliemiaQuinapril Increased risk of hyperkaliemiaQuinidine Decreases the antiarrhythmic effect of quinidineRamipril Increased risk of hyperkaliemiaTelmisartan Increased risk of hyperkaliemiaTrandolapril Increased risk of hyperkaliemiaValsartan Increased risk of hyperkaliemiaCilazapril Increased risk of hyperkaliemiaDihydroquinidine barbiturate Decreases the antiarrhythmic effect of quinidineForasartan Increased risk of hyperkaliemiaPerindopril Increased risk of hyperkaliemiaPolystyrene sulfonate Antagonism of actionPotassium Increased risk of hyperkaliemiaQuinidine barbiturate Decreases the antiarrhythmic effect of quinidineSaprisartan Increased risk of hyperkaliemiaSpirapril Increased risk of hyperkaliemiaTasosartan Increased risk of hyperkaliemia
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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| Food Interaction |
Amiloride¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid drastic changes in dietary habit.Avoid salt substitutes containing potassium.Take with food to reduce irritation.Avoid natural licorice.
Hydrochlorothiazide¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Avoid excess salt/sodium unless otherwise instructed by your physician.Take with food.Increase potassium intake; add a banana or orange juice; unless instructed otherwise.Avoid natural licorice.Do not take calcium, aluminum, magnesium or Iron supplements within 2 hours of taking this medication.
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| Drug Target |
[Drug Target]
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| Description |
Amiloride¿¡ ´ëÇÑ Description Á¤º¸ A pyrazine compound inhibiting sodium reabsorption through sodium channels in renal epithelial cells. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with diuretics to spare potassium loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705)
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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| Dosage Form |
Amiloride¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Amiloride¿¡ ´ëÇÑ Drug_Category Á¤º¸ DiureticsSodium channel blockers
Hydrochlorothiazide¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antihypertensive AgentsDiureticsSodium Chloride Symporter Inhibitors
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| Smiles String Canonical |
Amiloride¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ NC(N)=NC(=O)C1=C(N)N=C(N)C(Cl)=N1
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 |
Amiloride¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ N\C(N)=N/C(=O)C1=C(N)N=C(N)C(Cl)=N1
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 |
Amiloride¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C6H8ClN7O/c7-2-4(9)13-3(8)1(12-2)5(15)14-6(10)11/h(H4,8,9,13)(H4,10,11,14,15)/f/h8-11H2
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 |
Amiloride¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide
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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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
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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