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ÆçÇÉÁö¼ÓÁ¤5mg(Æç·ÎµðÇÉ) FELPIN SR TAB. 5MG[Felodipine]
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µå·°ÀÎÆ÷¿¡¼´Â ÀǾàǰ ÀÎÅÍ³Ý ÆÇ¸Å¸¦ ÇÏÁö ¾Ê½À´Ï´Ù. |
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643201180[A06703831]
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1. °íÇ÷¾Ð
Æç·ÎµðÇÉÀ¸·Î¼ ÃÊȸ·®À¸·Î 1ÀÏ 1ȸ 5§·À», À¯Áö·®À¸·Î 1ÀÏ 5‐10§·À» ¾ÆÄ§¿¡ °æ±¸Åõ¿©ÇÑ´Ù. 1ÀÏ ÃÖ´ë 20§·À» ÃʰúÇÏÁö ¾Ê´Â´Ù. ÀÌ ¾àÀº ¥â‐Â÷´ÜÁ¦ ¶Ç´Â ÀÌ´¢Á¦¿Í º´¿ëÅõ¿©ÇÒ ¼ö ÀÖÀ¸¸ç ´Ù¸¥ Ç÷¾Ð°ÇÏÁ¦°¡ ºÎÀûÀýÇÑ °æ¿ì¿¡´Â ÀÌ ¾à ´Üµ¶¿ä¹ýÀ¸·Î¼ Åõ¿©ÇÒ ¼ö ÀÖ´Ù. Åõ¿©¿ë·®Àº ȯÀÚÀÇ Ä¡·á¹ÝÀÀ¿¡ µû¶ó Á¶ÀýÇÑ´Ù.
2.¾ÈÁ¤Çü Çù½ÉÁõ
ÃÊȸ·®À¸·Î 1ÀÏ 1ȸ 5§·À» Åõ¿©Çϸç Çʿ信 µû¶ó 10§·À¸·Î Áõ·®ÇÒ ¼ö ÀÖ´Ù.ÀÌ ¾àÀº ¥â‐Â÷´ÜÁ¦¿¡ ÀÇÇÏ¿© ÃæºÐÇÑ È¿°ú°¡ ³ªÅ¸³ªÁö ¾Ê´Â °æ¿ì¿¡ º´¿ëÅõ¿©ÇÒ ¼ö ÀÖ´Ù. Åõ¿©¿ë·®Àº ȯÀÚÀÇ Ä¡·á¹ÝÀÀ¿¡ µû¶ó Á¶ÀýÇÑ´Ù.
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4. ½ÅÀå¾Ö ȯÀÚ
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5. °£Àå¾Ö ȯÀÚ
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2) ½ÉÀμº ¼ï ȯÀÚ(ÀúÇ÷¾Ð¿¡ ÀÇÇØ Áõ»óÀÌ ¾Ç鵃 ¼ö ÀÖ´Ù.)
3) ÀÌ ¾à¿¡ °ú¹ÎÁõÀÇ º´·ÂÀÌ Àִ ȯÀÚ
4) ´ëµ¿¸ÆÆÇ.½Â¸ðÆÇÇùÂøÁõ ȯÀÚ(Ç÷°üÈ®ÀåÀÛ¿ë¿¡ ÀÇÇØ °úµµ ÇÑ Ç÷¾Ð°Çϰ¡ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.)
5) ÁßÁõÀÇ °£±â´ÉÀå¾Ö ȯÀÚ
6) ½ÉÀå´ë»ó(ÓÛßÁ)±â´ÉºÎÀü ȯÀÚ
7) ±Þ¼º ½É±Ù°æ»ö ȯÀÚ
8) ºÒ¾ÈÁ¤¼º Çù½ÉÁõ ȯÀÚ
9) ÀÌ ¾àÀº À¯´çÀ» ÇÔÀ¯Çϰí ÀÖÀ¸¹Ç·Î, °¥¶ôÅä¿À½º ºÒ³»¼º(galactose intolerance), Lapp À¯´çºÐÇØÈ¿¼Ò °áÇÌÁõ(Lapp lactase deficiency) ¶Ç´Â Æ÷µµ´ç-°¥¶ôÅä¿À½º Èí¼öÀå¾Ö(glucose-galactose malabsorption) µîÀÇ À¯ÀüÀûÀÎ ¹®Á¦°¡ Àִ ȯÀÚ¿¡°Ô´Â Åõ¿©ÇÏ¸é ¾È µÈ´Ù.(À¯´çÇÔÀ¯ Á¦Á¦¿¡ ÇÑÇÔ)
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5) ÁßÁõÀÇ ½ÅºÎÀü ȯÀÚ(CFR<30ml/min)
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ÀÌ ¾àÀº CYP3A4ÀÇ ±âÁúÀÌ´Ù. CYP3A4¸¦ ÀúÇØÇϰųª À¯µµÇÏ´Â ¾àÁ¦´Â ÀÌ ¾àÀÇ Ç÷Àå ³óµµ¿¡ À¯ÀÇÇÑ ¿µÇâÀ» ÁֹǷΠº´¿ëÅõ¿©¸¦ ÇÇÇϵµ·Ï ÇÑ´Ù.
1) ´Ù¸¥ Ç÷¾Ð°ÇÏÁ¦¿Í º´¿ë Åõ¿©ÇÏ´Â °æ¿ì¿¡´Â »óÈ£ÀÛ¿ëÀÌ Áõ°¡µÉ ¼ö ÀÖÀ¸¹Ç·Î ½ÅÁßÈ÷ Åõ¿©ÇÑ´Ù.
2) ¸ÞÅäÇÁ·Î·ÑÀ» º´¿ë Åõ¿©ÇÏ´Â °æ¿ì¿¡´Â ¸ÞÅäÇÁ·Î·ÑÀÇ Ç÷Áß³óµµ°¡ »ó½ÂµÉ ¼ö ÀÖ´Ù.
3) µð°î½Å°ú º´¿ë Åõ¿©ÇÏ´Â °æ¿ì¿¡´Â µð°î½ÅÀÇ Ç÷Àå³óµµ°¡ »ó½ÂµÉ ¼ö ÀÖ´Ù.
4) ¿¡¸®½º·Î¸¶À̽Å, ÀÌÆ®¶óÄÚ³ªÁ¹, ÄÉÅäÄÚ³ªÁ¹, HIV ÇÁ·ÎÅ×¾ÆÁ¦ ÀúÇØÁ¦µîÀÇ °·ÂÇÑ CYP3A4 ÀúÇØÁ¦¿Í º´¿ëÅõ¿©´Â ÇÇÇÏ´Â °ÍÀÌ ÁÁ´Ù. ÀÌÆ®¶óÄÚ³ªÁ¹ÀÇ °æ¿ì ÀÌ ¾àÀÇ Cmax°¡ 8¹è, AUC°¡ 6¹è Áõ°¡ÇÏ¿© ¾à¹°ÀÇ ÀÌ»ó¹ÝÀÀ(¿¹ : ´Ù¸®ºÎÁ¾) ¹ßÇöÀ²À» Áõ°¡½ÃŲ´Ù. ¿¡¸®½º·Î¸¶À̽Űú º´¿ëÅõ¿©½Ã Æç·ÎµðÇÉÀÇ Cmax¿Í AUC´Â ¾à 2.5¹è Áõ°¡ÇÑ´Ù.
5) ½Ã¸ÞƼµò°ú º´¿ëÅõ¿©ÇÏ´Â °æ¿ì, Æç·ÎµðÇÉÀÇ Cmax¿Í AUC°¡ ¾à 55% Áõ°¡Çß´Ù.
6) Æä´ÏÅäÀÎ, Ä«¸£¹Ù¸¶Á¦ÇÉ, ¸®ÆÊÇǽÅ, Æä³ë¹Ù¸£ºñÅ» ¹× ¼¼ÀÎÆ® Á¸½º ¿ÍÆ®¿Í °°Àº È¿¼Ò (½ÃÅäÅ©·Ò P450)À¯µµ¾à¹°°ú º´¿ëÅõ¿©ÇÏ´Â °æ¿ì¿¡´Â ÀÌ ¾àÀÇ ´ë»ç°¡ Áõ°¡µÇ¾î Ç÷Àå³óµµ¸¦ °¨¼Ò½Ãų ¼ö ÀÖ´Ù. Ä«¹Ù¸¶Á¦ÇÉ, Æä´ÏÅäÀÎ ¹× Æä³ë¹Ù¸£ºñÅ»°ú ÀÌ ¾àÀ» º´¿ëÅõ¿©½Ã ÀÌ ¾àÀÇ AUC´Â 93%, Cmax´Â 82% °¨¼ÒÇß´Ù. CYP3A4 À¯µµÁ¦¿Í º´¿ëÇÏÁö ¾Êµµ·Ï ÇÑ´Ù.
7) ¸®ÆÊÇǽŰú º´¿ëÅõ¿©ÇÏ´Â °æ¿ì¿¡´Â ´Ù¸¥ Ä®½·±æÇ×Á¦(´ÏÆäµðÇÉ µî)ÀÇ ÀÛ¿ëÀ» °¨¼Ò½ÃÄ×´Ù´Â º¸°í°¡ ÀÖÀ¸¹Ç·Î ½ÅÁßÈ÷ Åõ¿©ÇÑ´Ù.
8) »çÀÌÅäÅ©·Ò P-450 3A4 È¿¼Ò¸¦ ¹æÇØÇÏ´Â ¾à¹°°ú º´¿ëÅõ¿©ÇÏ´Â °æ¿ì¿¡´Â ÀÌ ¾àÀÇ ÀÛ¿ëÀÌ Áõ°¡µÉ ¼ö ÀÖÀ¸¹Ç·Î ÀÌ ¾àÀÇ ¿ë·®À» °¨·®ÇÏ´Â µî ½ÅÁßÈ÷ Åõ¿©ÇÑ´Ù.
9) ÀÌ ¾à°ú ÀÚ¸ù(grapefruit)ÁÖ½º¿Í ÇÔ²² Åõ¿©ÇÏ´Â °æ¿ì¿¡´Â ÀÌ ¾à°ú ÁÖ½ºÀÇ Çö󺸳ëÀÌµå ¼ººÐ°úÀÇ »óÈ£ÀÛ¿ë¿¡ ÀÇÇØ Cmax¿Í AUC°¡ µÎ ¹è Áõ°¡Çß´Ù. µû¶ó¼ ÀÌ ¾à°ú ÀÚ¸ù ÁÖ½º¸¦ ÇÔ²² º¹¿ëÇÏÁö ¾Ê´Â´Ù.
10) »çÀÌŬ·Î½ºÆ÷¸°°ú º´¿ëÅõ¿©ÇÏ´Â °æ¿ì¿¡´Â ¿î¹Ý È¿¼Ò P-glycoproteinÀ» ÀúÇØÇϹǷΠÀÌ ¾àÀÇ Ç÷Àå ³óµµ°¡ Áõ°¡ÇÑ´Ù. Cmax´Â 150%±îÁö Áõ°¡Çϰí AUC´Â 60% Áõ°¡ÇÑ´Ù. ÀÌ ¾àÀÌ »çÀÌŬ·Î½ºÆ÷¸°ÀÇ ¾àµ¿Çп¡ ¹ÌÄ¡´Â ¿µÇâÀº Å©Áö ¾Ê´Ù.
11) ÀÌ ¾àÀÇ Ç÷Àå ´Ü¹é °áÇÕ·üÀº ³ôÀ¸³ª ¿ÍÆÄ¸°°ú °°ÀÌ ±¤¹üÀ§ÇÏ°Ô °áÇÕÇÏ´Â ´Ù¸¥ ¾à¹°ÀÇ ¹Ì°áÇÕ ºÐȹ¿¡´Â ¿µÇâÀ» ¹ÌÄ¡Áö ¾Ê´Â °ÍÀ¸·Î º¸ÀδÙ.
12) ÀÌ ¾àÀº Ÿũ·Î¸®¹«½ºÀÇ ³óµµ¸¦ ³ôÀÏ ¼ö ÀÖ´Ù. µÎ ¾àÀ» º´¿ë½Ã tacrolimusÀÇ Ç÷û ³óµµ¸¦ ¸ð´ÏÅÍÇÏ¿© ¿ë·®À» Á¶ÀýÇÑ´Ù.
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Á¦Ç°±Ô°Ý: /Á¦Ç°¼ö·®: 0/Á¦Çü:
Æû¸ñ±âÁØÄÚµå: 200500847 /´ëÇ¥ÄÚµå: 8806432011803/Ç¥ÁØÄÚµå: 8806432011803
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643201180[A06703831]
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| Mechanism of Action |
Felodipine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Felodipine is a calcium channel blocker. It reversibly competes with nitrendipine and/or other calcium channel blockers for dihydropyridine binding sites, blocks voltage-dependent calcium currents in vascular smooth muscle and cultured rabbit atrial cells, and blocks potassium-induced contracture of the rat portal vein. By blocking the calcium channels, felodipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes and results in a decrease of peripheral vascular resistance.
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| Pharmacology |
Felodipine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Felodipine, 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. Felodipine is similar to other peripheral vasodilators. Felodipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes blocking the calcium channels. 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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| Metabolism |
Felodipine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)
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| Protein Binding |
Felodipine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 99%
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| Half-life |
Felodipine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 14.1 hours
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| Absorption |
Felodipine¿¡ ´ëÇÑ Absorption Á¤º¸ 15%
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| Pharmacokinetics |
FelodipineÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£ : 2-5½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 16-24½Ã°£
- Èí¼ö : 100% ( absolute : ÃÊȸÅë°úÈ¿°ú·Î ÀÎÇÏ¿© 20%)
- ´Ü¹é°áÇÕ : 99% ÀÌ»ó
- ´ë»ç : °£¿¡¼ 99% ÀÌ»ó
- ¹Ý°¨±â : 11-16½Ã°£
- ¼Ò½Ç : ´ë»çü·Î¼ ´¢¸¦ ÅëÇØ ¹è¼³µÈ´Ù.
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| Biotransformation |
Felodipine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic
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| Toxicity |
Felodipine¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include excessive peripheral vasodilation with marked hypotension and possibly bradycardia. Oral rat LD50 is 1050 mg/kg.
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| Drug Interactions |
Felodipine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amobarbital The barbiturate decreases the effect of felodipineAprobarbital The barbiturate decreases the effect of felodipineButabarbital The barbiturate decreases the effect of felodipineButalbital The barbiturate decreases the effect of felodipineButethal The barbiturate decreases the effect of felodipineCarbamazepine Carbamazepine decreases the effect of felodipineDihydroquinidine barbiturate The barbiturate decreases the effect of felodipineHeptabarbital The barbiturate decreases the effect of felodipineHexobarbital The barbiturate decreases the effect of felodipineMethohexital The barbiturate decreases the effect of felodipineMethylphenobarbital The barbiturate decreases the effect of felodipinePentobarbital The barbiturate decreases the effect of felodipinePhenobarbital The barbiturate decreases the effect of felodipinePrimidone The barbiturate decreases the effect of felodipineQuinidine barbiturate The barbiturate decreases the effect of felodipineSecobarbital The barbiturate decreases the effect of felodipineTalbutal The barbiturate decreases the effect of felodipineErythromycin Erythromycin increases the effect of felodipineJosamycin Erythromycin increases the effect of felodipineEthotoin The hydantoin decreases the effect of felodipineFosphenytoin The hydantoin decreases the effect of felodipineMephenytoin The hydantoin decreases the effect of felodipinePhenytoin The hydantoin decreases the effect of felodipineQuinupristin This combination presents an increased risk of toxicityItraconazole Itraconazole increases effect/toxicity of felodipineNelfinavir Nelfinavir increases the effect and toxicity of felodipineOxcarbazepine Oxcarbazepine decreases the levels of felodipineTacrolimus Felodipine increases tacrolimus levels
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Felodipine¿¡ ´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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| Food Interaction |
Felodipine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Grapefruit and grapefruit juice should be avoided throughout treatment as grapefruit can significantly increase serum levels of this product.
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| Drug Target |
[Drug Target]
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| Description |
Felodipine¿¡ ´ëÇÑ Description Á¤º¸ A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. [PubChem]
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| Drug Category |
Felodipine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Arrhythmia AgentsAntiarrhythmic AgentsAntihypertensive AgentsCalcium Channel BlockersDihydropyridinesVasodilator Agents
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| Smiles String Canonical |
Felodipine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCOC(=O)C1=C(C)NC(C)=C(C1C1=C(Cl)C(Cl)=CC=C1)C(=O)OC
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| Smiles String Isomeric |
Felodipine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CCOC(=O)C1=C(C)NC(C)=C([C@H]1C1=C(Cl)C(Cl)=CC=C1)C(=O)OC
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| InChI Identifier |
Felodipine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H19Cl2NO4/c1-5-25-18(23)14-10(3)21-9(2)13(17(22)24-4)15(14)11-7-6-8-12(19)16(11)20/h6-8,15,21H,5H2,1-4H3
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| Chemical IUPAC Name |
Felodipine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ O3-ethyl O5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
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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.
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. FELODIPINE[GGT Increase][Composite Activity](Score) I(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.6[SGOT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.3[SGPT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.3[LDH Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.3[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.3
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