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| Mechanism of Action |
Diltiazem¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, dilitiazem, like verapamil, inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue.
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| Pharmacology |
Diltiazem¿¡ ´ëÇÑ Pharmacology Á¤º¸ Diltiazem, a benzothiazepine 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. Diltiazem is similar to other peripheral vasodilators. Diltiazem 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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| Protein Binding |
Diltiazem¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 70%-80%
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| Half-life |
Diltiazem¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 3.0 - 4.5 hours
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| Absorption |
Diltiazem¿¡ ´ëÇÑ Absorption Á¤º¸ Diltiazem is well absorbed from the gastrointestinal tract but undergoes substantial hepatic first-pass effect.
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| Pharmacokinetics |
Diltiazem HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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| Biotransformation |
Diltiazem¿¡ ´ëÇÑ Biotransformation Á¤º¸ Diltiazem is metabolized by and acts as an inhibitor of the CYP3A4 enzyme.
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| Toxicity |
Diltiazem¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=740mg/kg (orally in mice)
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| Drug Interactions |
Diltiazem¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amiodarone Increased risk of cardiotoxicity and arrhythmiasAmlodipine Increases the effect and toxicity of amlodipineAprepitant This CYP3A4 inhibitor increases the effect and toxicity of aprepitantAtazanavir Atazanavir increases the effect and toxicity of diltiazemAtenolol Increased risk of bradycardiaAtorvastatin Increases the effect and toxicity of atorvastatinBuspirone The calcium channel blocker increases the effect and toxicity of buspironeCarbamazepine Increases the effect of carbamazepineCerivastatin Increases the effect and toxicity of the statinCilostazol Increases the effect of cilostazolCisapride Increases the levels of cisaprideCyclosporine Increases the effect and toxicity of cyclosporineDihydroquinidine barbiturate Increases the effect and toxicity of quinidineLovastatin Increases the effect and toxicity of the statinMesoridazine Increased risk of cardiotoxicity and arrhythmiasMetoprolol Increased risk of bradycardiaMidazolam The calcium channel blocker increases the effect and toxicity of the benzodiazepineMoricizine Increased effect/toxicity of moricizinePindolol Increased risk of bradycardiaPropranolol Increased risk of bradycardiaQuinidine Increases the effect and toxicity of quinidineQuinidine barbiturate Increases the effect and toxicity of quinidineQuinupristin This combination presents an increased risk of toxicityRanolazine Increased levels of ranolazine- risk of toxicityRifampin Rifampin decreases levels of diltiazemRitonavir Ritonavir increases diltiazem levelsSimvastatin Increases the effect and toicity of simvastatinSirolimus Increases the effect and toxicity of sirolimusTacrolimus Increases levels of tacrolimusTerfenadine Increased risk of cardiotoxicity and arrhythmiasThioridazine Increased risk of cardiotoxicity and arrhythmiasTriazolam The calcium channel blocker increases the effect and toxicity of the benzodiazepine
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Diltiazem¿¡ ´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
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 |
Diltiazem¿¡ ´ëÇÑ Description Á¤º¸ A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of the calcium ion in membrane functions. It is also teratogenic. [PubChem]
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| Dosage Form |
Diltiazem¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule, extended release OralLiquid IntravenousSolution IntravenousTablet OralTablet, extended release Oral
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| Drug Category |
Diltiazem¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antihypertensive AgentsCalcium Channel BlockersCalcium-channel blocking agentsCardiovascular AgentsVasodilator Agents
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| Smiles String Canonical |
Diltiazem¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC=C(C=C1)C1SC2=CC=CC=C2N(CCN(C)C)C(=O)C1OC(C)=O
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| Smiles String Isomeric |
Diltiazem¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC=C(C=C1)[C@@H]1SC2=CC=CC=C2N(CCN(C)C)C(=O)[C@@H]1OC(C)=O
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| InChI Identifier |
Diltiazem¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C22H26N2O4S/c1-15(25)28-20-21(16-9-11-17(27-4)12-10-16)29-19-8-6-5-7-18(19)24(22(20)26)14-13-23(2)3/h5-12,20-21H,13-14H2,1-4H3/t20-,21+/m1/s1
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| Chemical IUPAC Name |
Diltiazem¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ [(2S,3S)-5-(2-dimethylaminoethyl)-2-(4-methoxyphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] acetate
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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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