- March 15, 2022
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Brand Name :
Cardizem, Cardizem CD, Cardizem LA, matzim LA, tiadylt ER, tiazac, Dilt-CD, diltia-XT, Dilzem, Dilatrate
Synonyms :
diltiazem
Class :
Anti-anginal agents, Calcium channel blockers, Anti arrhythmic
Dosage Forms & Strengths
Extended-release Capsule/tablet
120mg
180mg
240mg
300mg
360mg
420mg
Injectable solution
5mg/ml
Powder for injection
100mg
Tablet
30mg
60mg
90mg
120mg
Immediate release
:
Initial dose: 30mg orally every 6 hours, increasing gradually every 1 to 2 days
Maintenance dose: 180-360mg orally divided every 6-8 hours. Do not exceed 360mg/day
Extended-release tablets
Initial dose: 180mg orally once a day, increasing gradually every 7 to 14 days
Maintenance dose: 360mg orally every day
Extended-release capsules
Initial dose: 120-180mg orally once a day, increasing gradually every 7 to 14 days
Maintenance dose: 540mg orally every day
Extended-release coated capsules
Initial dose: 120-180mg orally once a day, increasing gradually every 7 to 14 days
Maintenance dose: 480mg orally every day
Extended-release capsules:
Initial dose: 120-240mg orally once a day, increasing the dose as needed
Maintenance dose: 120 to 540mg orally once every day
Maximum dose:540mg/day
Extended-release coated capsules
Initial dose: 120-180mg orally once a day; increase the dose as needed
Maintenance dose: 240 to 360mg orally every day
Maximum dose: 480mg/day
Extended-release tablets
Initial dose: 180 to 240mg orally once a day; increase the dose as needed
Maintenance dose: 540mg orally every day
supraventricular tachycardia (SVT)
Bolus injection:
Initial dose: 0.25mg/kg intravenous bolus administration for 2 minutes
Second dose of 0.35mg/kg intravenous can be administered
Continuous infusion:
It should begin immediately after a bolus injection of 0.35mg/kg intravenous or 0.25mg/kg intravenous administered over 2 minutes
Initial rate of infusion:10mg/hr intravenous
Maintenance rate of infusion: Can increase 5mg/hr increments up to 15mg/hr
Maximum duration:24 hours
Bolus injection:
Initial dose: 0.25mg/kg intravenous bolus administration for 2 minutes. The second dose of 0.35mg/kg intravenous can be administered after 15 mins
Continuous infusion:
It should begin immediately after a bolus injection of 0.35mg/kg intravenous or 0.25mg/kg intravenous administered over 2 minutes
Initial rate of infusion:10mg/hr intravenous
Maintenance rate of infusion: Can increase 5mg/hr increments up to 15mg/hr
Maximum duration:24 hours
Dosage Forms & Strengths
Extended-release Capsule/tablet
120mg
180mg
240mg
300mg
360mg
420mg
Injectable solution
5mg/ml
Powder for injection
100mg
Tablet
30mg
60mg
90mg
120mg
1.5-2mg/kg/day orally divided every 8 hours. Do not exceed 6mg/kg/day
Refer adult dosing
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may increase the hypotensive effect of antihypertensives
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of calcium channel blockers
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
diltiazem: they may diminish the serum concentration of CYP3A4 Inducers
diltiazem: they may diminish the serum concentration of CYP3A4 Inducers
diltiazem: they may diminish the serum concentration of CYP3A4 Inducers
diltiazem: they may diminish the serum concentration of CYP3A4 Inducers
diltiazem: they may diminish the serum concentration of CYP3A4 Inducers
may enhance the serum concentration when combined
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 substrates
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
diltiazem can impact the hepatic/intestinal enzyme CYP3A4 metabolism, leading to an elevation in the level or potency of intranasal midazolam
it may enhance the effects when combined with lofexidine by pharmacodynamic synergism
the effect of diltiazem is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of diltiazem
may enhance the risk of hypoglycemia when combined with Diltiazem
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
It may diminish the effect when combined with griseofulvin by CYP3A4 metabolism
it may diminish the therapeutic efficacy when combined with castor oil
nafcillin will decrease the effect of action of diltiazem by affecting enzyme CYP3A4 metabolism.
increases serum level of cabazitaxel by affecting the enzyme CYP3A4
may enhance the serum levels and adverse effects of docetaxel
it increases the effect or level of palbociclib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
Mechanism of action
It is a calcium channel blocker that works by inhibiting the influx of calcium ions into smooth muscle cells, leading to the relaxation of the smooth muscle in the walls of blood vessels. This results in a decrease in blood vessel tone and an increase in blood flow, which can help to lower blood pressure and improve symptoms of angina. Additionally, diltiazem may also have some anti-arrhythmic effects, which can help to stabilize the heart rhythm in certain conditions
Spectrum
It has a broad spectrum of activity and is used to treat various cardiovascular conditions
Hypertension: It is an antihypertensive agent to lower high blood pressure
Angina Pectoris: It is used to treat angina (chest pain) caused by coronary artery disease by dilating the coronary vessels and improving blood flow to the heart
Supraventricular Tachycardia: It is used to slow down the heart rate and convert certain types of supraventricular tachycardia (SVT) to a normal heart rhythm
Atrial fibrillation and Atrial Flutter: It is used as adjunctive therapy to help prevent atrial fibrillation and flutter
Chronic stable angina: It is used as a first-line therapy for chronic stable angina
Raynaud’s phenomenon: It is used to improve blood flow in patients with Raynaud’s phenomenon
Chronic heart failure: It is used as an adjunctive therapy to help improve symptoms of chronic heart failure
Frequency defined:
>10%
Headache
Edema
1-10%
AV block
Bradyarrhythmia
Hypotension
Vomiting
Extrasystoles
Drug-induced gingival hyperplasia
Diarrhea
Bronchitis
Dyspnea
Dizziness
Peripheral edema
Headache
Nausea
Vasodilation
Flushing
Myalgia
Constipation
Sinus congestion
congestion
<1%
Toxic epidermal necrolysis
Photosensitivity
Syncope
Increased alkaline phosphatase
Thrombocytopenia
Hemolytic anemia
Extrapyramidal symptoms
Contraindications
Hypersensitivity: It should not be used in patients with known hypersensitivity to the drug or its components
Cardiogenic shock: It should not be used in patients with cardiogenic shock, as it may worsen this condition
Second- or third-degree atrioventricular block: It should not be used in patients with second or third-degree atrioventricular block, as it may worsen this condition
Sick sinus syndrome: It should not be used in patients with sick sinus syndrome, as it may worsen this condition.
Severe hepatic impairment: It should be used with caution in patients with severe hepatic impairment, as it may accumulate in the body and cause toxicity.
Severe renal impairment: It should be used with caution in patients with severe renal impairment, as it may accumulate in the body and cause toxicity
Caution
Heart failure: It should be used with caution in patients with heart failure, as it may sometimes worsen this condition.
Aortic stenosis should be used with caution in patients with aortic stenosis, as it may sometimes worsen this condition.
Low blood pressure (hypotension): It may cause low blood pressure, particularly in patients who are also taking other medications that lower blood pressure.
Bradycardia: It may cause a slowing of the heart rate (bradycardia), particularly in patients who are also taking other medications that slow the heart rate.
Liver and kidney function: It should be used with caution in patients with liver or kidney disease, as it may accumulate in the body and cause toxicity in these patients.
Interactions: It may interact with other medications, including calcium channel blockers, beta-blockers, digoxin, and warfarin. It is essential to inform your healthcare provider of all medications and supplements you are taking before starting diltiazem.
diltiazem may cause swelling of the feet and ankles.
diltiazem may cause a headache as a side effect.
diltiazem may cause drowsiness and fatigue, so it’s essential to be careful when driving or doing activities that require alertness.
Pregnancy consideration: It should be used with caution in pregnancy, as it may cause harm to the fetus
Lactation: It should be used with caution in lactating women, as it may be present in breast milk and cause harm to the nursing infant
Pregnancy category:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology
Inhibits extracellular calcium ion influx across membranes of myocardial cells and vascular smooth muscle cells, resulting in inhibition of cardiac and vascular smooth muscle contraction and thereby dilating primary coronary and systemic arteries; no effect on serum calcium concentrations; substantial inhibitory effects on cardiac conduction system, acting principally at AV node, with some effects at the sinus node.
Pharmacodynamics
It is a calcium channel blocker primarily used to treat hypertension (high blood pressure) and angina (chest pain). It works by relaxing the smooth muscle cells in the walls of the blood vessels, which in turn causes the vessels to widen (dilate) and decreases blood pressure. Diltiazem also slows the heart rate by decreasing the conductivity of the electrical impulses in the heart. Additionally, it also reduces myocardial contractility, which decreases myocardial oxygen consumption. This can be helpful in angina and heart failure patients
Pharmacokinetics
Absorption:
It is a calcium channel blocker taken orally, with a bioavailability of 40%. The onset of action for hypertension is 30-60 minutes for the immediate-release (IR) form and 3 minutes for the intravenous (IV) form. The duration of action for supraventricular tachycardia (SVT) is 1-3 hours for an IV bolus and 0.5-10 hours following discontinuation of a continuous IV infusion. The peak serum time for the IR form is 2-4 hours, while the extended-release (ER) capsule and tablet have peak serum times of 10-14 hours and 11-18 hours, respectively
Distribution:
It is highly protein bound, with 70-80% of the drug bound to proteins in the bloodstream. The volume of distribution (Vd) is 3-13 L/kg
Metabolism
It is metabolized via the hepatic enzymes CYP3A4, desacetyldiltiazem, and N-monodesmethyldiltiazem as the primary metabolites. The half-life of diltiazem is 3-4.5 hours for the IR form, 6-9 hours for the ER tablet, and 5-10 hours for the ER capsule
Elimination/excretion:
The clearance of the drug is 11.8 mL/min/kg, and it is excreted in the urine (2-4% as unchanged; 6-7% as metabolites) and faeces
Administration
Intravenous administration
When administering diltiazem via an intravenous (IV) bolus, it should be given over 2 minutes, with a continuous electrocardiogram (ECG) and blood pressure (BP) monitoring. The response to the bolus may take several minutes to reach maximum effect, and the response may persist for several hours after the infusion is discontinued.
It should be done using an infusion pump when administering diltiazem via a continuous IV infusion. The infusion should be given for up to 24 hours as it is not recommended. It is essential to continuously monitor the patient’s vital signs and clinical response during the infusion and adjust the infusion rate accordingly. Consultation with a healthcare professional is recommended when administering diltiazem via IV
Storage
Patient information leaflet
Generic Name: diltiazem
Pronounced: [ dil-TYE-a-zem ]
Why do we use diltiazem?
diltiazem is a medication that belongs to a class of drugs called calcium channel blockers. It is used to treat several cardiovascular conditions, including:
Hypertension: It is an antihypertensive agent to lower high blood pressure.
Angina Pectoris: It is used to treat angina (chest pain) caused by coronary artery disease by dilating the coronary vessels and improving blood flow to the heart.
Supraventricular Tachycardia is used to slow down the heart rate and convert certain types of supraventricular tachycardia (SVT) to a normal heart rhythm.
Atrial fibrillation and Atrial Flutter: It is used as adjunctive therapy to help prevent atrial fibrillation and flutter
Chronic stable angina is used as a first-line therapy for chronic stable angina.
Raynaud’s phenomenon: It is used to improve blood flow in patients with Raynaud’s phenomenon.
Chronic heart failure: It is used as an adjunctive therapy to help improve symptoms of chronic heart failure.
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