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Diltiazem powder, with the molecular formula C22H26N2O4S, is a calcium ion antagonist used clinically for hypertension and angina pectoris in coronary heart disease. It is an organic compound belonging to the class of benzothiazepine calcium channel blockers, mostly existing in the form of hydrochloride salts. The chemical formula of its hydrochloride salt is C22H27ClN2O4S, with a molecular weight of 450.979. It is a white or off white crystalline or crystalline powder, odorless. As a representative drug of non dihydropyridine calcium channel blockers, it can selectively act on L-type calcium channels, inhibit the influx of calcium ions into cells, and thus exert pharmacological effects such as vasodilation, lowering blood pressure, and reducing myocardial oxygen consumption.
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C.F |
C22H26N2O4S |
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E.M |
414.16 |
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M.W |
414.52 |
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m/z |
414.16 (100.0%), 415.16 (23.8%), 416.16 (4.5%), 416.17 (2.7%), 417.16 (1.1%) |
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E.A |
C, 63.75; H, 6.32; N, 6.76; O, 15.44; S, 7.73 |
Extensive clinical studies have been conducted on its effectiveness in Japan, Europe, and the United States. Clinically, it is mainly used to treat cardiovascular diseases such as hypertension, coronary heart disease, angina pectoris, and arrhythmia. In addition, diltiazem also has pharmacological effects such as improving myocardial blood supply and inhibiting platelet aggregation, and has certain therapeutic effects on preventing and treating cardiovascular complications such as stroke and myocardial infarction.Diltiazem powder acts on the vascular smooth muscle and atrioventricular nodes of coronary and peripheral blood vessels, inhibiting the influx of calcium ions into cells and exhibiting vasodilation and prolonging atrioventricular node conduction time, thus effectively treating hypertension, arrhythmia, and angina.
Currently, diltiazem and other atrioventricular node blockers are used as first-line drugs for controlling ventricular rates in most patients. The mechanism of its treatment for arrhythmia is: by inhibiting the influx of calcium ions, the slope of the four phase automatic depolarization is reduced, which inhibits the sinus node and the autonomic inhibition of the atrioventricular node conductivity, but has no significant inhibitory effect on the atrioventricular bypass; Inhibition of supraventricular rapid arrhythmia caused by atrial electrical stimulation; In addition, there are vasodilators and mild negative inotropic effects.
Compared with thiazide diuretics and beta receptor antagonists, there was no significant difference in overall mortality and incidence of major cardiovascular events between diltiazem and thiazide diuretics. As a representative drug of non dihydropyridine calcum channel blockers, diltiazem can bind to slow calcum channels at action potential 2, preventing calcum ions from flowing into cells and causing significant dilation of coronary arteries and peripheral blood vessels. Diltiazem can also block potassium ion efflux and sodium ion influx, prolonging the effective refractory period of the atrioventricular node.
It has a strong dilating effect on arterial blood vessels, reduces peripheral vascular resistance, and produces a significant hypotensive effect, which can eliminate coronary artery spasm, increase coronary artery blood supply, and improve myocardial blood supply. In addition, it has a certain inhibitory effect on vascular active substances such as catecholamines, acetylcholine, histamine, and platelets. Diltiazem is a selective non dihydropyridine calcium channel blocker.
In addition, compared to diuretics, beta blockers, or a combination of diuretics and beta blockers, diltiazem is equally effective in preventing and treating stroke, myocardial infarction, and other cardiovascular deaths. Diltiazem is more effective than dihydropyridine calcum antagonists in reducing cardiovascular complications. Its possible mechanism is its ability to reverse left ventricular hypertrophy; Compared with dihydropyridine calcium antagonists, diltiazem has lower sympathetic excitability and does not have complications such as leg swelling and flushing that are common with dihydropyridine calcum antagonists.
It has a wide range of applications and significant therapeutic effects in the treatment of cardiovascular diseases. By inhibiting the influx of calcum ions into peripheral blood vessels, coronary smooth muscle cells, and atrioventricular node cells, it can dilate blood vessels and relax the smooth muscle of surrounding arteries, reducing peripheral vascular resistance and exerting its antihypertensive effect. It can be clinically used for various types of hypertension, especially for patients with hypertension emergencies complicated by arrhythmia and angina pectoris. Calcium channel blockade has a preventive and therapeutic effect on ischemic acute renal failure and has a certain protective effect on the kidneys in hypertensive patients.
Beyond the aforementioned core uses in cardiovascular disease treatment, diltiazem also has extended clinical applications in related diseases and special scenarios, further expanding its therapeutic value. It is clinically used as an adjuvant treatment for Raynaud's phenomenon, especially secondary Raynaud's phenomenon caused by connective tissue diseases or vascular lesions. By dilating peripheral small arteries and improving microcirculation, diltiazem can relieve the spasm of digital arteries, reduce symptoms such as numbness, pain, and discoloration of fingers and toes induced by cold or emotional excitement, and improve the quality of life of patients.
For patients with pulmonary hypertension, especially those with mild to moderate pulmonary arterial hypertension combined with coronary heart disease or arrhythmia, diltiazem can dilate pulmonary blood vessels, reduce pulmonary vascular resistance, alleviate pulmonary congestion and dyspnea, and improve cardiac function, serving as a supplementary treatment option under strict clinical monitoring.
When used in combination with drugs that affect cardiac contraction and/or conduction, there may be a synergistic effect, and the dosage of diltiazem powder used must be carefully determined. Diltiazem is biotransformation by cytochrome P450 oxidase in the body, and its combination with other drugs that undergo the same biotransformation pathway can lead to competitive inhibition of metabolism. Therefore, caution should be exercised when using multiple drugs for treatment. When adding or discontinuing diltiazem, other drugs with the same metabolic pathway, especially those with low therapeutic index, need to adjust their dosage to maintain a reasonable blood drug concentration.
1. Diltiazem can enhance the effect of beta blockers and is beneficial for individuals with normal heart function. But it may also lead to hypotension, left heart failure, and atrioventricular block. Elderly patients, those with left heart dysfunction, and those with aortic stenosis are particularly prone to this condition. Diltiazem can also increase the plasma concentration of beta blockers metabolized by liver enzymes by about 30% to 40%. If used together, the patient's cardiac function should be carefully monitored and the dosage of medication adjusted.
2. It has a synergistic effect with antiarrhythmic drugs, such as amiodarone hydrochloride, metoprolol hydrochloride, etc. Combined use can further slow down sinus heart rate and worsen atrioventricular block. When used in combination with quinidine, it may also enhance quinidine toxicity. Therefore, electrocardiogram and patient reactions should be monitored, and if there are abnormalities, medication should be reduced or stopped.
3. Anesthetics have inhibitory effects on myocardial contraction, conduction, and autonomy, as well as vasodilatory effects. They have a synergistic effect with calcium channel blockers, so the dosage should be carefully determined when used together.
4. Nitrates have the effect of enhancing blood pressure. When used in combination, blood pressure should be measured and the dosage should be adjusted appropriately.
5. Ximitiding can inhibit cytochrome P450, increase the blood concentration and area under the curve of diltiazem, so the dosage of diltiazem needs to be adjusted. Although ranitidine can also increase the blood concentration of diltiazem, it is not significant.
6. Apurin hydrochloride and diltiazem can mutually affect common metabolic enzymes, causing an increase in blood drug concentration. When used in combination, it should be reduced or discontinued.
7. HIV protease inhibitors, such as ritonavir, saquinavir, etc., can inhibit the metabolism of diltiazem and increase the blood concentration of diltiazem. When used simultaneously, the dosage of diltiazem should be reduced or discontinued.
8. Diltiazem can significantly increase the peak blood concentration of afzosin and enhance its antihypertensive effect. Calcium channel blockers should be avoided from being used in combination with alfuzosin as much as possible.
9. Diltiazem can inhibit the metabolic enzymes of dihydropyridine calcium channel blockers such as nifedipine, causing an increase in the blood concentration of dihydropyridine calcium channel blockers. Therefore, clinical symptoms should be observed when using it simultaneously, and the dosage should be reduced or discontinued.
10. Diltiazem can inhibit the metabolic enzyme of theophylline, delay theophylline metabolism, and enhance the effect of theophylline. During clinical application, clinical symptoms should be observed regularly, and if abnormalities are found, the dosage of theophylline should be reduced or the medication should be stopped.
11. Diltiazem powder can inhibit the metabolic enzymes of immunosuppressive drugs such as tacrolimus, leading to an increase in blood drug concentration. When used in combination, if abnormalities are found, the dosage of immunosuppressive drugs should be reduced or stopped.
12. Diltiazem can inhibit the metabolism of carbamazepine and increase its blood concentration. When used in combination, attention should be paid to the symptoms of carbamazepine poisoning, such as drowsiness, nausea, vomiting, dizziness, etc., and the blood concentration of carbamazepine should be regularly tested. If abnormalities are found, the dosage should be reduced or stopped.
13. Diltiazem can inhibit the metabolism of sodium phenytoin, increase the blood concentration of sodium phenytoin, and cause symptoms such as movement disorders and dizziness. When using in combination, attention should be paid to observing clinical symptoms, and if abnormalities are found, medication should be reduced or stopped.
14. Diltiazem can inhibit the metabolism of triazolam and midazolam, increase their blood drug concentration, and enhance their effects. Therefore, if used in combination, triazolam or midazolam should be started from a small dose and clinical symptoms should be observed regularly. If abnormalities are found, the dosage should be reduced or stopped.
15. Diltiazem can enhance the effect of muscle relaxants. When used in combination, the dosage should be reduced or discontinued.
16. Diltiazem can enhance the cholesterol lowering effect of simvastatin, but increases the risk of muscle disease and rhabdomyolysis. If used in combination, patients should be closely monitored for muscle pain or weakness symptoms, and serum creatine kinase (CK) values should be regularly checked. Once CK values show a significant increase and suspicion or diagnosis of myopathy or rhabdomyolysis occurs, medication should be discontinued.
17. Fentanyl is metabolized by cytochrome P450, and diltiazem can prolong the half-life of fentanyl. If used in combination, fentanyl toxicity should be monitored.
18.The combination of diltiazem and aspirin can further inhibit ADP induced platelet aggregation and prolong bleeding time.
19. Co administration with nonsteroidal anti-inflammatory drugs or oral anticoagulants increases the risk of gastrointestinal bleeding.
20. Rifampicin can induce the metabolic enzymes of diltiazem, leading to a decrease in the blood concentration of diltiazem. When using it simultaneously, clinical symptoms should be observed, and if necessary, the dose of diltiazem should be increased.
21. Ephedra contains ephedrine and pseudoephedrine, which can reduce the efficacy of antihypertensive drugs. Hypertensive patients treated with diltiazem should avoid taking ephedra preparations simultaneously.
22. Diltiazem can increase the blood concentration of digoxin by 20%, but there are also reports that it does not affect it. Although the results are contradictory, the blood concentration of digoxin should be monitored when starting to use digtiazem, adjusting the dosage, or stopping use to avoid excessive or insufficient digoxin.
adverse reaction
Diltiazem powder is a non dihydropyridine calcium channel blocker widely used to treat hypertension, angina pectoris, and certain arrhythmias. Although its therapeutic effect is significant, it may be accompanied by a series of adverse reactions during use.
Cardiovascular system adverse reactions
As a calcium channel blocker, Diltiazem has a particularly significant impact on the cardiovascular system. Common adverse reactions include:
Bradycardia: Drugs slow down the conduction velocity of the sinoatrial node and atrioventricular node by inhibiting the influx of calcium ions, resulting in a decrease in heart rate. Severe bradycardia may cause dizziness, fatigue, and even fainting.
Arrhythmia: including atrioventricular block, junctional rhythm, and premature ventricular contractions. These reactions occur in about 1% or less of patients and may be life-threatening, requiring close monitoring.
Aggravated angina: In some patients, Diltiazem may induce or exacerbate angina due to coronary artery spasm or increased myocardial oxygen consumption.
Hypotension: Medications lower blood pressure by dilating blood vessels, but excessive hypotension may lead to dizziness, darkening of the eyes, or fainting, especially when standing or suddenly standing up.
Peripheral edema: due to vasodilation and fluid retention, patients may have lower limb or ankle edema, usually mild to moderate.
Adverse reactions to the digestive system
Diltiazem may cause various digestive system symptoms, including:
Constipation: Medications slow down intestinal peristalsis by inhibiting the influx of calcium ions into the intestinal smooth muscle, leading to constipation. This is one of the most common digestive system adverse reactions of Diltiazem.
Nausea, vomiting, and diarrhea: These symptoms may occur alone or simultaneously, usually related to direct stimulation of the gastrointestinal mucosa by medication or changes in gastrointestinal motility.
Abnormal liver function: A very small number of patients may experience elevated serum transaminase levels, indicating liver cell damage. Patients with long-term medication or liver dysfunction need to regularly monitor their liver function.
Other symptoms include dry mouth, abnormal taste, loss of appetite, and abdominal discomfort, which are usually mild and tolerable.
Skin and allergic reactions
Diltiazem may cause skin and allergic reactions, including:
Mild rash and itching: This is the most common skin reaction, usually manifested as scattered erythema or papules, accompanied by mild itching.
Severe skin reactions, such as Stevens Johnson syndrome and toxic epidermal necrolysis (TEN). These reactions, although rare, can be life-threatening, manifested as widespread erythema, blisters, and skin peeling.
Vascular edema: Medication may cause swelling in the face, lips, tongue, or throat, leading to difficulty breathing or swallowing, requiring urgent treatment.
Other system adverse reactions
Respiratory system: Diltiazem may cause respiratory symptoms such as difficulty breathing, nasal congestion, and pharyngitis. These reactions may be related to the relaxation effect of drugs on bronchial smooth muscle or the stimulation of respiratory mucosa.
Eye: A small number of patients may experience blurred vision or eye pain, which may be related to the effects of medication on eye blood vessels or nerves.
Musculoskeletal system: Long term medication may cause muscle pain or joint pain, which may be related to the direct effect or metabolic changes of the drug on muscle or joint tissue.
Urinary system: very few patients may have frequent urination or urinary retention, which may be related to the effect of drugs on bladder smooth muscle.
FAQ
What is the use of diltiazem powder?
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Diltiazem is used alone or together with other medicines to treat angina (severe chest pain) or hypertension (high blood pressure). High blood pressure adds to the workload of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly.
How to use diltiazem for fissures?
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Apply a small amount on your finger (approximately 2.5cm) and place the cream just inside the anus. A finger covering, such as cling film or a disposable glove may be used to apply the ointment. Wash hands after use and dispose of finger covering appropriately.
Can diltiazem be sprinkled?
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Long-acting capsules (24 hour):
Check with your pharmacist about how to take this drug. Some products may be opened and sprinkled on a spoonful of applesauce. Some products must be swallowed whole. Check with your pharmacist to see if you can open this product.
How long should I use diltiazem?
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How long to take it for. If you're taking diltiazem for high blood pressure or angina, you'll usually take it long term, even for the rest of your life. Talk to your doctor if you want to stop taking diltiazem. Stopping may cause your blood pressure to rise and this may increase your risk of a heart attack or stroke.
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