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Brand names,
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Analogs
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Brand Names Mixture
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Chemical_Formula
C22H26N2O4S
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RX_link
http://www.rxlist.com/cgi/generic/diltiaz.htm
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
H. Kugita et al., U.S. Pat. 3,562,257 (1971)
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Molecular Weight
414.519 g/mol
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Melting Point
231oC
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H2O Solubility
465 mg/L
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State
Solid
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LogP
3.141
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Dosage Forms
Solution
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Indication
For the treatment of Hypertension
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Pharmacology
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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Absorption
Diltiazem is well absorbed from the gastrointestinal tract but undergoes substantial hepatic first-pass effect.
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side effects and Toxicity
LD50=740mg/kg (orally in mice)
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Patient Information
PATIENT INFORMATION
Take this medicine exactly as directed even if you feel well and do not notice any signs of chest pain.
Do not take more of this medicine and do not take it more often than your doctor ordered.
Do not miss any doses.
Diltiazem is a calcium channel blocking agents. For the calcium channel blocking agents, the following should be considered:
-Tell your doctor if you have ever had any unusual or allergic reaction to amlodipine, bepridil, diltiazem, felodipine, flunarizine, isradipine, nicardipine, nifedipine, nimodipine, or verapamil. Also tell your health care professional if you are allergic to any other substances, such as foods, preservatives, or dyes.
-Calcium channel blocking agents have not been studied in pregnant women. However, studies in animals have shown that large doses of calcium channel blocking agents cause birth defects, prolonged pregnancy, poor bone development in the offspring, and stillbirth.
-Although bepridil, diltiazem, nifedipine, verapamil, and possibly other calcium channel blocking agents, pass into breast milk, they have not been reported to cause problems in nursing babies.
-Although there is no specific information comparing use of this medicine in children with use in other age groups, it is not expected to cause different side effects or problems in children than it does in adults.
-Elderly people may be especially sensitive to the effects of calcium channel blocking agents. This may increase the chance of side effects during treatment. A lower starting dose may be required.
-The presence of other medical problems may affect the use of the calcium channel blocking agents. Make sure you tell your doctor if you have any other medical problems, especially
Follow Rxlist link and drugs.com link and other links for detailed information.
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Organisms Affected
Humans and other mammals