In vivo release of diltiazem occurs throughout the gastrointestinal tract, with controlled release still occurring for up to 24 hours after administration, as determined by radio-labeled methods. As the once daily dose of Dilacor XR was increased, departures from linearity were noted. Ranitidine produced smaller, nonsignificant increases. The effect may be mediated by cimetidine's known inhibition of hepatic cytochrome P-450, the enzyme system responsible for the first-pass metabolism of diltiazem. Patients currently receiving diltiazem therapy should be carefully monitored for a change in pharmacological effect when initiating and discontinuing therapy with cimetidine. An adjustment in the diltiazem dose may be warranted.
Anesthetics: The depression of cardiac contractility, conductivity, and automaticity as well as the vascular dilation associated with anesthetics may be potentiated by calcium channel blockers. When used concomitantly, anesthetics and calcium blockers should be titrated carefully. Several literature reports have identified cases of diltiazem hydrochloride overdose, some with multiple drug ingestion, with both fatal and non-fatal outcomes. The reported events affected multiple body systems including the cardiovascular system bradycardia, complete heart block, asystole, cardiac failure, arrhythmia, atrial fibrillation, palpitations, hypotension, ischemia, ECG changes respiratory system respiratory failure, hypoxia, dyspnea, pulmonary edema central nervous system loss of consciousness, convulsions, dizziness, confusion, agitation gastrointestinal system nausea, vomiting skin and appendages increased sweating and other systems hypotonia, iliac artery thrombosis, metabolic acidosis, increased blood glucose. The administration of ipecac to induce vomiting and activated charcoal to reduce drug absorption have been advocated as initial means of intervention.
Store at room temperature away from moisture and heat. Tell your doctor all medications you use. Cartia XT should be used only when prescribed during pregnancy. This drug passes into breast milk and may have undesirable effects on a nursing infant. Consult your doctor before breastfeeding. Cardiac Conduction: Diltiazem hydrochloride prolongs AV node refractory periods without significantly prolonging sinus node recovery time, except in patients with sick sinus syndrome. In domestic controlled trials in patients with atrial fibrillation or atrial flutter, bolus administration of diltiazem hydrochloride injection was effective in reducing heart rate by at least 20% in 95% of patients. Diltiazem hydrochloride injection rarely converts atrial fibrillation or atrial flutter to normal sinus rhythm. Following administration of one or two intravenous bolus doses of diltiazem hydrochloride injection, response usually occurs within 3 minutes and maximal heart rate reduction generally occurs in 2 to 7 minutes. Heart rate reduction may last from 1 to 3 hours. If hypotension occurs, it is generally short-lived, but may last from 1 to 3 hours.
Cartia XT is available in form. As with all drugs, care should be exercised when treating patients with multiple medications. Diltiazem hydrochloride undergoes biotransformation by cytochrome P-450 mixed function oxidase. Co-administration of diltiazem hydrochloride with other agents which follow the same route of biotransformation may result in the competitive inhibition of metabolism. Diltiazem hydrochloride extended-release capsules should be taken on an empty stomach. Patients should be cautioned that the diltiazem hydrochloride extended-release capsules should not be opened, chewed or crushed, and should be swallowed whole.
This medication can slow down the removal of other medications from your body, which may affect how they work. Statins: Diltiazem has been shown to increase significantly the AUC of some statins. The risk of myopathy and rhabdomyolysis with statins metabolized by CYP3A4 may be increased with concomitant use of diltiazem. When possible, use a non-CYP3A4-metabolized statin together with diltiazem; otherwise, dose adjustments for both diltiazem and the statin should be considered along with close monitoring for signs and symptoms of any statin related adverse events. Concomitant administration of diltiazem with carbamazepine has been reported to result in elevated plasma levels of carbamazepine, resulting in toxicity in some cases. In short-term, double-blind, placebo-controlled clinical trials diltiazem hydrochloride extended-release capsules, USP demonstrated a dose-related antihypertensive response among patients with mild to moderate hypertension. In one parallel-group study of 198 patients Diltiazem hydrochloride extended-release capsules, USP was given for four weeks. Symptoms associated with the arrhythmia were improved in conjunction with decreased heart rate or conversion to normal sinus rhythm following administration of diltiazem hydrochloride injection. Concomitant Use with Other Cardiovascular Agents. Dermatological events see may be transient and may disappear despite continued use of diltiazem hydrochloride tablets. Sublingual Nitroglycerin NTG: May be taken as required to abort acute anginal attacks during diltiazem hydrochloride therapy.
Diltiazem is excreted in human milk. One report suggests that concentrations in breast milk may approximate serum levels. Because of the potential for serious adverse reactions in nursing infants from diltiazem, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Keep refrigerated until use. In another clinical trial that followed a dose-escalation design, diltiazem hydrochloride extended-release capsules, USP also reduced blood pressure in a linear dose-related manner. What other drugs will affect diltiazem? Worsening of heart failure has been reported in patients with impairment of ventricular function. Experience with the use of diltiazem in combination with beta-blockers in patients with impaired ventricular function is limited. Enhanced effects and increased toxicity of buspirone may be possible during concomitant administration with diltiazem. Subsequent dose adjustments may be necessary during coadministration, and should be based on clinical assessment. The usual dosage range studied in clinical trials was 180 mg to 480 mg once daily. If you have trouble swallowing a diltiazem capsule whole, ask your doctor or pharmacist if it is safe for you to open the capsule and sprinkle the medicine into a spoonful of applesauce to make swallowing easier. Swallow this mixture right away without chewing. Do not save the mixture for later use. Discard the empty capsule. Like other calcium antagonists, diltiazem decreases sinoatrial and atrioventricular conduction in isolated tissues and has a negative inotropic effect in isolated preparations. In the intact animal, prolongation of the AH interval can be seen at higher doses. Dosage needs to be adjusted by titration to individual patient needs. When used as monotherapy, usual starting doses are 120 to 240 mg once daily. Maximum antihypertensive effect is usually observed by 14 days of chronic therapy; therefore, dosage adjustments should be scheduled accordingly. The usual dosage range studied in clinical trials was 120 to 540 mg once daily. Current clinical experience with 540 mg dose is limited; however, the dose may be increased to 540 mg once daily. Diltiazem hydrochloride is a calcium ion cellular influx inhibitor slow channel blocker. Do not crush, chew, break, or open an extended-release tablet or capsule. Swallow it whole. Breaking or opening the pill may cause too much of the drug to be released at one time.
RxList is part of the WebMD Health Network. The opinions expressed in the WebMD User Reviews are solely those of the User, who may or may not have medical or scientific training, and do not represent the opinions of WebMD. These member reviews have not been reviewed by a WebMD physician or any member of the WebMD editorial staff for accuracy, balance, objectivity, or any other purpose except for compliance with our Terms and Conditions. Our Cartia XT diltiazem hydrochloride Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication. Diltiazem Hydrochloride Tablets, USP are available containing 30 mg, 60 mg, 90 mg or 120 mg of diltiazem hydrochloride, USP. Bradycardia frequently responded favorably to atropine, as did heart block, although cardiac pacing was also frequently utilized to treat heart block. Fluids and vasopressors were used to maintain blood pressure, and in cases of cardiac failure, inotropic agents were administered. Anesthetics: The depression of cardiac contractility, conductivity, and automaticity as well as the vascular dilation associated with anesthetics may be potentiated by calcium channel blockers. When used concomitantly, anesthetics and calcium channel blockers should be titrated carefully. No dose adjustment is necessary. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit. As with all drugs, care should be exercised when treating patients with multiple medications. Diltiazem is both a substrate and an inhibitor of the cytochrome P-450 3A4 enzyme system. Other drugs that are specific substrates, inhibitors, or inducers of this enzyme system may have a significant impact on the efficacy of and side effect profile of diltiazem. The presence of food did not affect the ability of Dilacor XR to maintain a controlled release of the drug and did not impact its sustained release properties over 24-hours after administration. However, simultaneous administration of Dilacor XR with a high-fat breakfast resulted in increases in AUC of 13% and 19%, and in C max by 37% and 51%, respectively. Overdosage experience is limited. In the event of overdosage or an exaggerated response, appropriate supportive measures should be employed.
There were seven reports with a fatal outcome; although the amount of diltiazem ingested was unknown, multiple drug ingestions were confirmed in six of the seven reports. Beta-Blockers: Controlled and uncontrolled domestic studies suggest that concomitant use of diltiazem hydrochloride and beta-blockers is usually well-tolerated, but available data are not sufficient to predict the effects of concomitant treatment in patients with left ventricular dysfunction or cardiac conduction abnormalities. Administration of diltiazem hydrochloride concomitantly with propranolol in five normal volunteers resulted in increased propranolol levels in all subjects and the bioavailability of propranolol was increased approximately 50%. If combination therapy is initiated or withdrawn in conjunction with propranolol, an adjustment in the propranolol dose may be warranted. Patients who have demonstrated hypersensitivity to the drug. As with all drugs, care should be exercised when treating patients with multiple medications. Diltiazem is both a substrate and an inhibitor of the cytochrome P450 3A4 enzyme system. Other drugs that are specific substrates, inhibitors, or inducers of this enzyme system may have a significant impact on the efficacy and side effect profile of diltiazem. High-Degree AV Block: Treat as for bradycardia above. Total radioactivity measurement following short IV administration in healthy volunteers suggests the presence of other unidentified metabolites, which attain higher concentrations than those of diltiazem and are more slowly eliminated; half-life of total radioactivity is about 20 hours compared to 2 to 5 hours for diltiazem. It may take up to 2 weeks before you get the full benefit of this drug. Tell your doctor if your condition persists or worsens for example, your routine remain high or increase. Diltiazem is well absorbed from the gastrointestinal tract and is subject to an extensive first-pass effect, giving an absolute bioavailability compared to intravenous administration of about 40%. Diltiazem undergoes extensive metabolism in which only 2% to 4% of the unchanged drug appears in the urine. Drugs that induce or inhibit hepatic microsomal enzymes may alter diltiazem disposition. P-450, the enzyme system responsible for the first-pass metabolism of diltiazem. Patients currently receiving diltiazem therapy should be carefully monitored for a change in pharmacological effect when initiating and discontinuing therapy with cimetidine. An adjustment in the diltiazem dose may be warranted. Jago Research AG, Zollikon, Switzerland, is a patented controlled-release system incorporated in the tablets. Controlled absorption of diltiazem begins within 1 hour, with maximum plasma concentrations being achieved 4 to 6 hours after administration. The apparent steady-state half-life of diltiazem following once daily administration of Dilacor XR capsules ranges from 5 to 10 hours. This prolongation of half-life is attributed to continued absorption of diltiazem rather than to alterations in its elimination.
Do not consider WebMD User-generated content as medical advice. Never delay or disregard seeking professional medical advice from your doctor or other qualified healthcare provider because of something you have read on WebMD. You should always speak with your doctor before you start, stop, or change any prescribed part of your care plan or treatment. WebMD understands that reading individual, real-life experiences can be a helpful resource but it is never a substitute for professional medical advice, diagnosis, or treatment from a qualified health care provider. If you think you may have a medical emergency, call your doctor or dial 911 immediately. Intravenous diltiazem hydrochloride 20 mg prolongs AH conduction time and AV node functional and effective refractory periods by approximately 20%. In a study involving single oral doses of diltiazem hydrochloride 300 mg in six normal volunteers, the average maximum PR prolongation was 14% with no instances of greater than first-degree AV block. In the same study, there was no significant change in 20 mg single dose pravastatin AUC and C max during diltiazem co-administration. The therapeutic effects of diltiazem are believed to be related to its ability to inhibit the cellular influx of calcium ions during membrane depolarization of cardiac and vascular smooth muscle. The toxic dose in man is not known. To contact the physician who prescribed Cardizem LA or any other physician immediately if they experience possible adverse reactions, including bradycardia, arrhythmias, symptoms indicative of hypotension or heart failure, hepatic and skin reactions. This characteristic also makes them more suitable for angina than short-acting dihydropyridines. Non-dihydropyridines, of which there are only two currently used clinically, comprise the other two classes of CCBs. Verapamil phenylalkylamine class is relatively selective for the myocardium, and is less effective as a systemic vasodilator drug. This drug has a very important role in treating angina by reducing myocardial oxygen demand and reversing coronary vasospasm and arrhythmias. Diltiazem benzothiazepine class is intermediate between verapamil and dihydropyridines in its selectivity for vascular calcium channels. By having both cardiac depressant and vasodilator actions, diltiazem is able to reduce arterial pressure without producing the same degree of reflex cardiac stimulation caused by dihydropyridines. Acute Hepatic Injury: Mild elevations of serum transaminases with and without concomitant elevation in alkaline phosphatase and bilirubin have been observed in clinical studies. Such elevations were usually transient and frequently resolved even with continued diltiazem treatment. In rare instances, significant elevations in alkaline phoshatase, LDH, SGOT, SGPT, and other phenomena consistent with acute hepatic injury have been noted. These reactions tended to occur early after therapy initiation 1 to 6 weeks and have been reversible upon discontinuation of drug therapy. The relationship to diltiazem is uncertain in some cases, but probable in some others. Diltiazem is excreted in human milk. Talk to your doctor or about lifestyle changes that might benefit you.
This list is not complete and other drugs may interact with diltiazem. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor. Initiate dosing at 180 to 240 mg once daily, although some patients may respond to lower doses. Titrate according to blood pressure to a maximum of 540 mg daily. Maximum antihypertensive effect is usually observed by 14 days of chronic therapy. Dilacor XR capsules should be taken on an empty stomach. Patients should be cautioned that the Dilacor XR capsules should not be opened, chewed or crushed, and should be swallowed whole. Abnormal dreams, amnesia, depression, gait abnormality, hallucinations, insomnia, nervousness, paresthesia, personality change, somnolence, tinnitus, tremor. If possible, it is recommended that diltiazem hydrochloride not be co-infused in the same intravenous line. To consult their physician if they become pregnant while taking Diltiazem Hydrochloride Extended-Release Tablets or plan to become pregnant. Diltiazem produces its antihypertensive effect primarily by relaxation of vascular smooth muscle and the resultant decrease in peripheral vascular resistance. The magnitude of blood pressure reduction is related to the degree of hypertension: thus hypertensive individuals experience an antihypertensive effect, whereas there is only a modest fall in blood pressure in normotensives. Diltiazem hydrochloride injection was tested for compatibility with three commonly used intravenous fluids at a maximal concentration of 1 mg diltiazem hydrochloride per milliliter. In a 10-subject randomized, open label, 4-way cross-over study, coadministration of diltiazem 120 mg BID diltiazem SR for 2 weeks with a single 20 mg dose of lovastatin resulted in 3- to 4-fold increase in mean lovastatin AUC and C max versus lovastatin alone. In the same study, there was no significant change in 20 mg single dose pravastatin AUC and C max during diltiazem coadministration. Diltiazem plasma levels were not significantly affected by lovastatin or pravastatin. Although diltiazem hydrochloride extended-release capsules utilize a slowly disintegrating matrix, caution should still be used in patients with preexisting severe gastrointestinal narrowing pathologic or iatrogenic. There have been no reports of obstructive symptoms in patients with known strictures in association with the ingestion of diltiazem hydrochloride extended-release capsules. The therapeutic benefits of diltiazem hydrochloride are believed to be related to its ability to inhibit the influx of calcium ions during membrane depolarization of cardiac and vascular smooth muscles. Mechanism of Action: Hypertension.
Long-acting forms of diltiazem may be used to treat high blood pressure. If your doctor prescribes diltiazem to treat high blood pressure, check with your pharmacist to make sure you are getting the correct form of diltiazem. The effectiveness of intravenous calcium administration to reverse the pharmacological effects of diltiazem overdose has been inconsistent. In a few reported cases, overdose with calcium channel blockers associated with hypotension and bradycardia that was initially refractory to atropine became more responsive to atropine after the patients received intravenous calcium. In some cases intravenous calcium has been administered 1 g calcium chloride or 3 g calcium gluconate over 5 minutes, and repeated every 10 to 20 minutes as necessary. Calcium gluconate has also been administered as a continuous infusion at a rate of 2 g per hour for 10 hours. Infusions of calcium for 24 hours or more may be required. Patients should be monitored for signs of hypercalcemia. Adverse events occurring in 1% or more of patients receiving diltiazem hydrochloride extended-release capsule once daily dosing. Cardizem LA is indicated to improve exercise tolerance in patients with chronic stable angina. The two primary metabolites of diltiazem are desacetyldiltiazem and desmethyldiltiazem. The desacetyl metabolite is approximately 25% to 50% as potent a coronary vasodilator as diltiazem and is present in plasma at concentrations of 10% to 20% of parent diltiazem. However, recent studies employing sensitive and specific analytical methods have confirmed the existence of several sequential metabolic pathways of diltiazem. As many as nine diltiazem metabolites have been identified in the urine of humans. Total radioactivity measurements following single intravenous dose administration in healthy volunteers suggest the presence of other unidentified metabolites. These metabolites are more slowly excreted with a half-life of total radioactivity of approximately 20 hours and attain concentrations in excess of diltiazem. Diltiazem works by relaxing blood vessels and increasing the supply of blood and oxygen to the heart. Do not share this medication with others. Paroxysmal Supraventricular Tachycardia. Rapid conversion of paroxysmal supraventricular tachycardias PSVT to sinus rhythm. This includes AV nodal reentrant tachycardias and reciprocating tachycardias associated with an extranodal accessory pathway such as the WPW syndrome or short PR syndrome. Unless otherwise contraindicated, appropriate vagal maneuvers should be attempted prior to administration of diltiazem hydrochloride injection. Store at room temperature away from light and moisture. not store in the bathroom. Keep all away from children and pets. Your pharmacist can provide more information about diltiazem. Extended-release tablets with 120 mg, 180 mg, 240 mg, 300 mg, 360 mg, or 420 mg diltiazem hydrochloride per tablet. Cardizem LA Tablets are white, capsule-shaped, and debossed with "B" on one side and the diltiazem content mg on the other. BEFORE ACCESSING OR USING THIS SITE. Ask your pharmacist about using those products safely. Cardizem LA is formulated as a once-a-day extended-release tablet for oral administration containing 120 mg, 180 mg, 240 mg, 300 mg, 360 mg or 420 mg of diltiazem hydrochloride.
Cardiac Conduction. Diltiazem hydrochloride prolongs AV node refractory periods without significantly prolonging sinus node recovery time, except in patients with sick sinus syndrome. Category C: Reproduction studies have been conducted in mice, rats, and rabbits. Administration of doses ranging from 4 to 6 times depending on species the upper limit of the optimum dosage range in clinical trials 480 mg once daily. Nervous system: Abnormal dreams, amnesia, depression, extrapyramidal symptoms, gait abnormality, hallucinations, insomnia, nervousness, personality change, somnolence, tremor. Diltiazem is called a channel blocker. It works by relaxing vessels in the body and so can flow more easily. The opinions expressed in WebMD User-generated content areas like communities, reviews, ratings, or blogs are solely those of the User, who may or may not have medical or scientific training. These opinions do not represent the opinions of WebMD. User-generated content areas are not reviewed by a WebMD physician or any member of the WebMD editorial staff for accuracy, balance, objectivity, or any other reason except for compliance with our Terms and Conditions. The following post-marketing reactions have been reported infrequently in patients receiving diltiazem: acute generalized exanthematous pustulosis, allergic reactions, alopecia, angioedema including facial or periorbital edema erythema multiforme, extrapyramidal symptoms, gingival hyperplasia, hemolytic anemia, increased bleeding time, leukopenia, photosensitivity including lichenoid keratosis and hyperpigmentation at sun-exposed skin areas purpura, retinopathy, myopathy, and thrombocytopenia. Caution should be exercised when using this combination.
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Due to extensive metabolism, plasma concentrations after a standard dose of diltiazem can vary over tenfold, which significantly limits their value in evaluating cases of overdosage. Diltiazem-associated prolongation of the AH interval is not more pronounced in patients with first-degree heart block. In patients with sick sinus syndrome, diltiazem significantly prolongs sinus cycle length up to 50% in some cases. Intravenous diltiazem in doses of 20 mg prolongs AH conduction time and AV node functional and effective refractory periods approximately 20%. The use of intravenous diltiazem for control of ventricular response in patients with supraventricular arrhythmias should be undertaken with caution when the patient is compromised hemodynamically. In addition, caution should be used in patients taking other drugs that decrease peripheral resistance, intravascular volume, myocardial contractility or conduction.
TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. While a dose of diltiazem hydrochloride extended-release capsules USP Once-a-day dosage given once-daily may produce an antihypertensive effect similar to the same total daily dose given in divided doses, individual dose adjustment may be needed. Take Diltiazem Hydrochloride Extended-Release Tablets once a day at approximately the same time. Do not chew or crush the tablet. Patients with atrial fibrillation or atrial flutter associated with an accessory bypass tract such as in WPW syndrome or short PR syndrome.
Some doctors have also prescribed diltiazem to prevent migraines, though the evidence supporting its use among people with migraines is not universally accepted. Following single intravenous injection of diltiazem hydrochloride, however, plasma concentrations of N-mono-desmethyldiltiazem and desacetyldiltiazem, two principal metabolites found in plasma after oral administration, are typically not detected. These metabolites are observed, however, following 24 hour constant rate intravenous infusion. Total radioactivity measurement following short IV administration in healthy volunteers suggests the presence of other unidentified metabolites which attain higher concentrations than those of diltiazem and are more slowly eliminated; half-life of total radioactivity is about 20 hours compared to 2 to 5 hours for diltiazem.
Other medications can affect the removal of diltiazem from your body, which may affect how this medication works. Examples include cimetidine, quinidine, St. John's wort, azole antifungals such as ketoconazole, macrolide antibiotics such as erythromycin, rifamycins including rifabutin and rifampin. If you are being treated for high blood pressure, keep using this medication even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life. Cardiovascular: AV block third degree bundle branch block, ECG abnormality, palpitations, syncope, tachycardia, ventricular extrasystoles.