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Ãâó: ±¹¸³µ¶¼º°úÇпø µ¶¼º¹°ÁúÁ¤º¸DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do |
| Mechanism of Action |
Enalapril¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Enalaprilat, the active metabolite of enalapril, competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Inhibition of ACE results in decreased plasma angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and stimulation of baroreceptor reflex mechanisms, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Enalaprilat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin.
Nitrendipine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Nitrendipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
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| Pharmacology |
Enalapril¿¡ ´ëÇÑ Pharmacology Á¤º¸ Enalapril, an angiotensin-converting enzyme (ACE) inhibitor, is a prodrug which, when hydrolyzed by estarases to its active Enalaprilat, is used to treat hypertension and heart failure, to reduce proteinuria and renal disease in patients with nephropathies, and to prevent stroke, myocardial infarction, and cardiac death in high-risk patients. Enalapril and enalaprilat inhibit angiotensin-converting enzyme (ACE) in human subjects and animals. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex.
Nitrendipine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Nitrendipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nitrendipine is similar to other peripheral vasodilators. Nitrendipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
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| Absorption |
Enalapril¿¡ ´ëÇÑ Absorption Á¤º¸ 60%
Nitrendipine¿¡ ´ëÇÑ Absorption Á¤º¸ Not Available
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| Pharmacokinetics |
Enalapril maleateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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- ÀÛ¿ë¹ßÇö½Ã°£ : ¡1 ½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 12-24 ½Ã°£
- Èí¼ö : 55-75%
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- Enalapril : 0.5-1.5 ½Ã°£ À̳»
- Enalaprilat (Ȱ¼ºÇü) : 3-4.5 ½Ã°£ À̳»
- ´Ü¹é°áÇÕ : 50-60%
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- ¿ïÇ÷¼º½ÉºÎÀü ȯÀÚ : 3.4-5.8 ½Ã°£
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- ¼ºÀÎ : 35-38 ½Ã°£
- ¼Ò½Ç : ÁÖ·Î (60-80%) ´¢¸¦ ÅëÇØ, ¼Ò·®Àº ´ëº¯À¸·Î ¹è¼³µÊ
NitrendipineÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£ : 2½Ã°£ À̳»
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 1-2½Ã°£ À̳»
- Èí¼ö : Àß Èí¼öµÊ. Èí¼öÀ² : ¾à 88%
- »ýü³»ÀÌ¿ë·ü : ¾à 23%
- ºÐÆ÷ : ºÐÆ÷¿ëÀû : 6 L/kg
- ´Ü¹é°áÇÕ : 97-99%. ºñȰ¼ºÇü ´ë»çüµéµµ ´Ü¹é°áÇÕÀ²ÀÌ ³ôÀ½
- ´ë»ç : °£ ÃÊȸÅë°úÈ¿°ú Å. ºñȰ¼ºÇü ´ë»çüµé·Î °£¿¡¼ ´ëºÎºÐ ´ë»çµÊ
- ¹Ý°¨±â : 2-24 ½Ã°£ (Æò±Õ 12½Ã°£)
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| Toxicity |
Enalapril¿¡ ´ëÇÑ Toxicity Á¤º¸ Hypotension
Nitrendipine¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
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| Drug Interactions |
Enalapril¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amiloride Increased risk of hyperkaliemiaDrospirenone Increased risk of hyperkaliemiaRifampin Rifampin reduces the efefct of enalapril Spironolactone Increased risk of hyperkaliemiaTizanidine Tizanidine increases the risk of hypotension with the ACE inhibitorTriamterene Increased risk of hyperkaliemiaLithium The ACE inhibitor increases serum levels of lithiumPotassium Increased risk of hyperkaliemia
Nitrendipine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Methotrexate The penicillin increases the effect and toxicity of methotrexateAnisindione The IV penicillin increases the anticoagulant effectDicumarol The IV penicillin increases the anticoagulant effectAcenocoumarol The IV penicillin increases the anticoagulant effectWarfarin The IV penicillin increases the anticoagulant effectEthinyl Estradiol This anti-infectious agent could decreases the effect of the oral contraceptiveMestranol This anti-infectious agent could decreases the effect of the oral contraceptiveDoxycycline Possible antagonism of actionDemeclocycline Possible antagonism of actionTetracycline Possible antagonism of actionRolitetracycline Possible antagonism of actionOxytetracycline Possible antagonism of actionMinocycline Possible antagonism of actionMethacycline Possible antagonism of action
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Nitrendipine¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 3A4/3A5/3A7
Macrolide antibiotics:
clarithromycin
erythromycin
NOT azithromycin
telithromycin
Anti-arrhythmics:
quinidine
Benzodiazepines:
alprazolam
diazepam
midazolam
triazolam
Immune Modulators:
cyclosporine
tacrolimus (FK506)
HIV Protease Inhibitors:
indinavir
ritonavir
saquinavir
Prokinetic:
cisapride
Antihistamines:
astemizole
chlorpheniramine
Calcium Channel Blockers:
amlodipine
diltiazem
felodipine
nifedipine
nisoldipine
**nitrendipine**
verapamil
HMG CoA Reductase Inhibitors:
atorvastatin
cerivastatin
lovastatin
NOT pravastatin
simvastatin
aripiprazole
buspirone
gleevec
haloperidol (in part)
methadone
pimozide
quinine
NOT rosuvastatin
sildenafil
tamoxifen
trazodone
vincristine
INHIBITORS
CYP 3A4/3A5/3A7
HIV Protease Inhibitors:
indinavir
nelfinavir
ritonavir
amiodarone
NOT azithromycin
cimetidine
clarithromycin
diltiazem
erythromycin
fluvoxamine
grapefruit juice
itraconazole
ketoconazole
mibefradil
nefazodone
troleandomycin
verapamil
INDUCERS
CYP 3A4/3A5/3A7
carbamazepine
phenobarbital
phenytoin
rifabutin
rifampin
St. John's wort
troglitazone
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| Drug Target |
[Drug Target]
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| Description |
Enalapril¿¡ ´ëÇÑ Description Á¤º¸ One of the angiotensin-converting enzyme inhibitors that is used to treat hypertension. [PubChem]
Nitrendipine¿¡ ´ëÇÑ Description Á¤º¸ A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive. [PubChem]
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| Dosage Form |
Enalapril¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid IntravenousTablet Oral
Nitrendipine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Not Available
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| Drug Category |
Enalapril¿¡ ´ëÇÑ Drug_Category Á¤º¸ Angiotensin-converting Enzyme InhibitorsAntihypertensive Agents
Nitrendipine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antihypertensive AgentsCalcium Channel BlockersVasodilator Agents
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| Smiles String Canonical |
Enalapril¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCOC(=O)C(CCC1=CC=CC=C1)NC(C)C(=O)N1CCCC1C(O)=O
Nitrendipine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCOC(=O)C1=C(C)NC(C)=C(C1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OC
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| Smiles String Isomeric |
Enalapril¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CCOC(=O)[C@@H](CCC1=CC=CC=C1)N[C@@H](C)C(=O)N1CCC[C@H]1C(O)=O
Nitrendipine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CCOC(=O)C1=C(C)NC(C)=C([C@H]1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OC
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| InChI Identifier |
Enalapril¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C20H28N2O5/c1-3-27-20(26)16(12-11-15-8-5-4-6-9-15)21-14(2)18(23)22-13-7-10-17(22)19(24)25/h4-6,8-9,14,16-17,21H,3,7,10-13H2,1-2H3,(H,24,25)/t14-,16+,17-/m0/s1/f/h24H
Nitrendipine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H20N2O6/c1-5-26-18(22)15-11(3)19-10(2)14(17(21)25-4)16(15)12-7-6-8-13(9-12)20(23)24/h6-9,16,19H,5H2,1-4H3
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| Chemical IUPAC Name |
Enalapril¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (2S)-1-[(2S)-2-[[(2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]pyrrolidine-2-carboxylic acid
Nitrendipine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ O3-ethyl O5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
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| Drug-Induced Toxicity Related Proteins |
ENALAPRIL ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:CYP3A Drug:Enalapril Toxicity:idiosyncratic hepatotoxicity. [¹Ù·Î°¡±â] ENALAPRIL MALEATE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Angiotensin-converting enzyme(ACE) Drug:Enalapril maleate Toxicity:blood-pressure reduction and reduction in left ventricular mass. [¹Ù·Î°¡±â] Replated Protein:B2 bradykinin receptor Drug:Enalapril maleate Toxicity:cough. [¹Ù·Î°¡±â] 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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ÃÖ±ÙÁ¤º¸¼öÁ¤ÀÏ 2021-12-09
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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
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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