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| {{drugbox |
| | #REDIRECT [[Diltiazem#Pharmacology]] |
| |IUPAC_name = [2-(2-dimethylaminoethyl)-5-(4-methoxyphenyl)<br>-3-oxo-6-thia-2-azabicyclo[5.4.0]undeca-7,9,<br>11-trien-4-yl]ethanoate
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| |CAS_number = 42399-41-7
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| | ATC_prefix=C08
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| | ATC_suffix=DB01
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| | PubChem=39186
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| | DrugBank=APRD00473
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| | C=22 | H=26 | N=2 | O=4 | S=1
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| |molecular_weight = 414.519 [[gram|g]]/[[Mole (unit)|mol]]
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| |bioavailability = 40%
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| |metabolism = [[Liver|Hepatic]]
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| |elimination_half-life = 3-4.5 [[hour]]s
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| |excretion = [[Kidney|Renal]]<br>[[Bile|Biliary]]<br>[[Mammary gland|Lactic]] (in lactiferous females)
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| |pregnancy_category = D: ([[United States of America|USA]])
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| |legal_status =
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| |routes_of_administration = [[Mouth|Oral]]
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| }}
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| {{SI}}
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| {{WikiDoc Cardiology Network Infobox}}
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| {{CMG}}
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| __NOTOC__
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| ==Overview==
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| '''Diltiazem''' is a member of the group of drugs known as [[benzothiazepine]]s, which are a class of [[calcium channel blocker]]s, used in the treatment of [[hypertension]], [[angina pectoris]], and some types of [[arrhythmia]]. It is a class 3 anti-anginal drug, and a class IV antidysrhythmic. It incites very minimal reflex sympathetic changes.
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| Diltiazem is a potent [[vasodilator]], increasing blood flow and variably decreasing the heart rate via strong depression of A-V node conduction. Its pharmacolgical activity is somewhat similar to [[verapamil]].
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| Diltiazem is metabolized by and acts as an inhibitor of the [[CYP3A4]] enzyme.
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| Diltiazem is relatively contraindicated in the presence of [[sick sinus syndrome]], [[atrioventricular node]] conduction disturbances, [[bradycardia]], impaired [[left ventricle]] function, [[peripheral artery occlusive disease]], [[chronic obstructive pulmonary disease]], and [[Prinzmetal's angina]].
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| ==Brand names==
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| *Cardizem
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| *Cartia XT
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| *Tiazac
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| *Tiazac XC
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| *Tiamate
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| *Tildiem in particular in Europe
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| *Adizem
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| *Viazem
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| *Dilatam
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| *Dilzem
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| *Angiozem
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| *Dilatem
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| *Dilcardia
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| *Diltelan
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| *Diltime
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| *Dyalec
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| *Filazem
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| *Tildiem
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| *Vasmulax
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| *Zandil
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| *Zemtrial
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| ==Therapeutic effects==
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| Potent vasodilator of coronary vessels.
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| Vasodilator of peripheral vessels. This reduces peripheral resistance and afterload.
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| Negative inotropic effect. Diltiazem causes a modest decrease in contractility and reduces myocardium oxygen consumption.
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| Negative chronotropic effect. Diltiazem causes a modest lowering of heart rate. This effect is due to slowing of the SA node. It results in reduced myocardium oxygen consumption.
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| Negative dromotropic effect. By slowing conduction through the AV node, diltiazem increases the time needed for each beat. This results in reduced myocardium oxygen consumption.
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| ==Nontherapeutic effects and toxicities==
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| *Reflex sympathetic response. Caused by the peripheral dilatation of vessels and the resulting drop in BP; the response works to counteract the [[inotropic]], [[chronotropic]] and [[dromotropic]] effects of diltiazem.
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| *[[Hypotension]]
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| *[[Bradycardia]]
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| *[[Dizziness]]
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| *[[Flushing]]
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| ==Indications==
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| Stable (exercise-induced) Angina. Diltiazem increases coronary blood flow and decreases myocardial oxygen consumption, secondary to decreased peripheral resistance, heart rate, and contractility.
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| Variant Angina. Diltiazem is effective due to its direct effects on coronary dilatation.
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| Unstable (preinfarction, crescendo) Angina. Diltiazem may be particularly effective if the underlying mechanism is vasospasm.
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| Supraventricular tachycardias. Diltiazem appears to be as effective as [[verapamil]] in treating reentrant [[supraventricular tachycardia]].
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| [[Atrial fibrillation]] or [[Atrial flutter|flutter]].
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| [[Hypertension]]. Because of its vasodilatatory effects, diltiazem is useful for treating [[hypertension]]. [[Calcium channel blocker]]s are well-tolerated, and especially effective in treating low-renin hypertension.
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| ==Contraindications and precautions==
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| CHF. Patients with reduced ventricular function may not be able to counteract the inotropic and chronotropic effects of diltiazem, the result being an even higher compromise of function.
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| SA node or AV conduction disturbances. Use of diltiazem should be avoided in patients with SA or AV nodal abnormalities, because of its negative chronotropic and dromotropic effects
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| Low blood pressure. Patients with systolic blood pressures below 90 mm Hg should not be treated with diltiazem.
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| [[Wolff-Parkinson-White syndrome]]. Diltiazem may paradoxically increase ventricular rate in patients with WPW syndrome because of accessory conduction pathways.
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| ==Drug interactions==
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| '''[[Beta blocker]]s'''
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| Intravenous diltiazem should never be used concurrently with a beta-blocker as AV node block may result.
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| '''[[Quinidine]]'''
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| [[Quinidine]] should not be used concurrently with [[calcium channel blocker]]s because of reduced clearance of both drugs and potential pharmacodynamic effects at the SA and AV nodes.
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| '''Miscellaneous'''
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| Inhibition of hepatic enzymes. Diltiazem and [[verapamil]] inhibit hepatic cytochromes CYP3A4, CYP2C9 and CYP2D6, possibly resulting in drug interactions.
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| ==Potential future indications==
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| Recent research has shown that diltiazem is able to reduce [[cocaine]] cravings in drug addicted rats.[http://www.sciencedaily.com/releases/2008/02/080227155016.htm] This is believed to be due to the effects of calcium blockers on [[dopamine]]rgic and [[glutamate]]rgic signalling in the brain.
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| Diltiazem is also being used to aid in the treatment of anal fissures and hemhorroids. However, it is not taken orally. It is made into a cream form using either vaseline or Phlogel. Phlogel absorbs the diltiazem into the problem area better than the vaseline base. It has excellent success rates.
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| {{Calcium channel blockers}}
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| [[Category:Calcium channel blockers]]
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| [[de:Diltiazem]]
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| [[it:Diltiazem]]
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| [[hu:Diltiazem]]
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| [[ja:ジルチアゼム]]
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| [[pl:Diltiazem]]
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| [[uk:Дилтіазем]]
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| [[zh:地尔硫䓬]]
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