Diltiazem Hydrochloride for Injection

Pharmacology: It acts on the smooth muscle of the coronary and peripheral blood vessels and the atrioventricular node, inhibiting the influx of Ca2 into the cells, and exhibits vasodilation and prolongs the conduction time of the atrioventricular node, thus being effective for hypertension, arrhythmia, and angina pectoris. 1. Effect on blood pressure 1) It can reduce hypertension under anesthesia and without anesthesia, but the effect is stronger under anesthesia than without anesthesia, and it has a stronger antihypertensive effect on blood pressure higher than normal blood pressure (rat). 2) While reducing blood pressure, it reduces peripheral vascular resistance and myocardial oxygen consumption, and increases cardiac output (dog). 3) It lowers blood pressure without reducing blood flow to the brain, coronary arteries, and kidneys. It also exhibits a sodium diuretic effect (dog, monkey). 2. Effect on arrhythmia 1) It prolongs the conduction time, effective refractory period, and functional refractory period of the atrioventricular node, and exhibits an effect on supraventricular tachyarrhythmia (dog). 2) It inhibits supraventricular tachyarrhythmia caused by atrial electrical stimulation (rabbit). 3. Effects on myocardial ischemia 1) Improve the balance of myocardial oxygen supply and demand ① Dilate the main trunk and side branches of the coronary artery, increase blood flow to the ischemic part of the myocardium (dog). ② Inhibit coronary artery spasm (pig, human). 2) Myocardial protection When myocardial ischemia occurs, it inhibits excessive influx of Ca2 into cells, maintains cardiac function and myocardial energy metabolism, and reduces the infarct focus (dog, cat). Toxicology: When diltiazem hydrochloride is orally administered to mice, its LD50 is 640-740 mg/kg; the LD50 of intravenous injection is 58-61 mg/kg. When diltiazem hydrochloride is orally administered to rats, its LD50 is 585 mg/kg; the LD50 of intravenous injection is 58-61 mg/kg. In reproductive toxicity tests, when mice, rats and rabbits were orally administered diltiazem that is 5-10 times the human dose, embryonic and fetal death was observed. In some studies, it has been reported that these doses can cause bone abnormalities. In perinatal and postnatal studies, individual pups were found to have reduced weight and reduced survival rates in the early stages. It was found that administration of >20 times the human oral dose increased the incidence of stillbirth. The mutation test of this product was negative.

The main ingredient of this product is diltiazem hydrochloride.

This product is white loose lumps and powder.

Supraventricular tachycardia; emergency management of abnormally high blood pressure during surgery; hypertensive emergencies; unstable angina.

Intravenous injection: The adult dosage is 10 mg for the first time. Dissolve and dilute it to 1% concentration with sodium chloride injection or glucose injection before use, and inject slowly within 3 minutes. Alternatively, calculate the dose based on 0.15-0.25 mg/kg body weight, and repeat after 15 minutes. It can also be administered by intravenous drip at 5-15 μg/kg body weight per minute.

266 (4.1%) of the 6,543 treated patients experienced adverse reactions. Common adverse reactions were: bradycardia (1.1%), hypotension (0.7%), first-degree atrioventricular block (0.4%), second-degree atrioventricular block (0.3%), atrioventricular junctional rhythm (0.3%), etc. 1. Serious adverse reactions (occasionally: 0.1-<5%, rarely: <0.1%) ① Occasionally, complete atrioventricular block, severe bradycardia (initial symptoms: bradycardia, dizziness, mild headache, etc.), sometimes leading to cardiac arrest, and full preparation for the treatment of these symptoms should be made before starting medication. If abnormalities occur, medication should be stopped immediately and the following treatments should be performed: Complete atrioventricular block, severe bradycardia: administer atropine sulfate, isoproterenol, etc. and/or use a pacemaker. Cardiac arrest: perform cardiac massage, administer catecholamines such as epinephrine for cardiac resuscitation. ② Congestive heart failure is extremely rare. Once it occurs, the drug should be stopped and appropriate treatment should be carried out. 2. Other adverse reactions If adverse reactions occur, appropriate treatment (such as discontinuation of the drug) should be given and appropriate treatment should be carried out. Adverse reactions with an incidence of 0.1-5% include: bradycardia, atrioventricular block, hypotension, atrioventricular junctional rhythm, premature contraction, sinus arrest, facial fever, facial flushing, GOT, GPT, LDH increase, etc. Adverse reactions with an incidence of <0.1% include: sinoatrial block, bundle branch block, palpitations, dizziness, paroxysmal tachycardia, headache, nausea, vomiting, increased AL-P, decreased urine volume, increased serum creatinine and BUN, rash, itching, local redness at the injection site, etc. Oral preparations can still cause photosensitivity reactions, but the frequency of occurrence is unknown.

1. Patients with severe hypotension or cardiogenic shock. 2. II and III degree atrioventricular block or sick sinus syndrome (persistent sinus bradycardia (heart rate less than 50 beats/min), sinus arrest and sinoatrial block, etc.). 3. Patients with severe congestive heart failure. 4. Patients with severe cardiomyopathy. 5. Patients who are allergic to any of the ingredients in the drug. 6. Pregnant or potentially pregnant women. 7. Avoid administering intravenous diltiazem and intravenous beta-blockers at the same time or at a close time (within a few hours). 8. Patients with ventricular tachycardia, wide QRS tachycardia.

Precautions for children: The safety of the drug for children has not been confirmed. Precautions for pregnancy and lactation: Women who are pregnant or may become pregnant are prohibited from taking this product.

Drugs with antihypertensive effects (antihypertensive drugs, nitrates, etc.) enhance the antihypertensive effect. Measure blood pressure and adjust the dosage. Additive effects (enhanced antihypertensive effect) of beta-blockers (bisoprolol fumarate, propranolol hydrochloride, atenolol, etc.) may cause bradycardia, atrioventricular conduction stagnation, sinoatrial block, etc. Monitor the electrocardiogram and reduce or stop the medication when abnormalities are found. Additive effects (inhibition of sinus rhythm and conduction, negative inotropic effect, antihypertensive effect) are enhanced. Pay special attention to the combined use of these three drugs (diltiazem hydrochloride, beta-blockers and digitalis preparations). Rauwolfia preparations (reserve, etc.) and digitalis preparations (digoxin, methyldigoxin) may cause bradycardia and atrioventricular conduction block. Due to the increase in the blood concentration of digitalis preparations, digitalis poisoning symptoms (nausea, vomiting, headache, dizziness, visual abnormalities, etc.) including arrhythmias may occur. Monitor the electrocardiogram and observe regularly for symptoms of digitalis poisoning. If necessary, measure the blood concentration of digitalis preparations. Reduce the dosage or stop the medication if abnormalities are found. The additive effect (inhibition of sinus rhythm and conduction) is enhanced. Pay special attention to the combined use of these three drugs (diltiazem hydrochloride, β-blockers and digitalis preparations). Diltiazem hydrochloride can increase the blood concentration of digitalis. Antiarrhythmic drugs (amiodarone hydrochloride, mexiletine hydrochloride, etc.) may cause bradycardia, atrioventricular block, sinus arrest, etc. Monitor the electrocardiogram and reduce the dosage or stop the medication if abnormalities are found. The additive effect (inhibition of sinus rhythm and conduction) is enhanced. Symptoms caused by the increase in the blood concentrations of the two drugs may occur with apristinine hydrochloride (bradycardia, atrioventricular block, sinus arrest, tremor, dizziness or mild headache, etc.). Monitor the electrocardiogram, observe clinical symptoms regularly, and reduce or stop the medication if abnormalities are found. This combination of drugs can affect the common metabolic enzyme (cytochrome P450), resulting in an increase in the blood concentration of both drugs. Dihydropyridine Ca2 antagonists (nifedipine, amlodipine besylate, etc.) sometimes cause symptoms caused by increased blood concentrations of dihydropyridine Ca2 antagonists (enhanced antihypertensive effect, etc.). Observe clinical symptoms regularly, and reduce or stop the medication if abnormalities are found. Because diltiazem hydrochloride inhibits the metabolic enzymes (cytochrome P450) of these drugs, the blood concentrations of these drugs increase. Triazolam (sleep induction agent) sometimes causes symptoms caused by increased blood concentrations of triazolam (prolonged sleep time, etc.). Start with a small dose, observe clinical symptoms regularly, and reduce or stop the medication if abnormalities are found. Midazolam (sedative, hypnotic induction agent) sometimes causes symptoms caused by increased blood concentrations of midazolam (enhanced sedative, hypnotic effect, etc.). Observe clinical symptoms regularly, and reduce or stop the medication if abnormalities are found. Carbamazepine (anti-epileptic drug, drug for the treatment of manic states) may cause symptoms (drowsiness, nausea, vomiting, dizziness, etc.) caused by increased blood concentrations of carbamazepine. Observe clinical symptoms regularly, and reduce or stop the medication if abnormalities are found. Selegiline hydrochloride (a drug for the treatment of Parkinson's disease) The effects and toxicity of selegiline hydrochloride may be enhanced. Observe clinical symptoms regularly, and reduce or stop the medication if abnormalities are found. Theophylline (bronchodilator) may cause symptoms (nausea, vomiting, headache, insomnia, etc.) caused by increased blood concentrations of theophylline. Observe clinical symptoms regularly, and reduce or stop the medication if abnormalities are found. Cilostazol (antiplatelet drug) may enhance the effects of cilostazol. Observe clinical symptoms regularly, and reduce or stop the medication if abnormalities are found. Vinorelbine tartrate (anti-tumor drug) may enhance the effects of vinorelbine tartrate. Observe clinical symptoms regularly, and reduce or stop the medication if abnormalities are found. Cyclosporine (immunosuppressant) may cause symptoms (such as renal dysfunction, etc.) due to increased blood concentration of cyclosporine. Regularly observe clinical symptoms, monitor blood concentration of cyclosporine, and reduce or stop the medication if abnormalities are found. Tacrolimus (immunosuppressant) may cause various symptoms (such as renal dysfunction, etc.) due to increased blood concentration of tacrolimus. Regularly observe clinical symptoms, monitor blood concentration of tacrolimus, and reduce or stop the medication if abnormalities are found. Phenytoin (anti-epileptic drug) may cause various symptoms (such as ataxia, dizziness, nystagmus, etc.) due to increased blood concentration of phenytoin. Regularly observe clinical symptoms, and reduce or stop the use of phenytoin if abnormalities are found. In addition, it may weaken the effect of diltiazem hydrochloride. Diltiazem hydrochloride inhibits the metabolic enzyme (cytochrome P450) of phenytoin, resulting in increased blood concentration of phenytoin. At the same time, phenytoin accelerates the metabolism of diltiazem, resulting in a decrease in the blood concentration of diltiazem. Cimetidine HIV protease inhibitors (ritonavir, saquinavir, etc.) may cause symptoms due to increased blood concentrations of diltiazem (enhanced antihypertensive effect, bradycardia, etc.). Monitor blood pressure and electrocardiogram, and reduce or stop the medication if abnormalities are found. These drugs inhibit the metabolic enzymes (cytochrome P450) of diltiazem, resulting in increased blood concentrations of diltiazem. The effect of rifampicin on diltiazem may be weakened. Observe clinical symptoms regularly, and if possible, monitor the blood concentration of diltiazem. If abnormalities are found, take appropriate measures such as changing the medication or increasing the dosage of this drug. Rifampicin induces the metabolic enzymes (cytochrome P450) of diltiazem, resulting in a decrease in the blood concentration of diltiazem. Anesthetic drugs (isoflurane, enflurane, halothane, etc.) may cause bradycardia, atrioventricular block, sinus arrest, etc. Monitor the electrocardiogram and reduce or stop the medication if abnormalities are found. Additive effects (inhibition of sinus rhythm and cardiac conduction) are enhanced. Muscle relaxants (pancuronium, vecuronium, etc.) enhance the effects of muscle relaxants. Pay attention to the muscle relaxant effect and reduce or stop the medication if abnormalities are found. Diltiazem hydrochloride inhibits the release of acetylcholine from the presynaptic membrane of nerve endings at the neuromuscular junction.

Keep in a dark, airtight, cool place.

10mg

24 months

Wuhan Pusheng Pharmaceutical Co., Ltd.

• Founded in:

  1998-05-11

• Address:

  No. 1, Miaoshan Sunshine Avenue, Jiangxia District, Wuhan

• Tax NO.:

  91420000707090425F

• Registered Funds:

  23.141141 million yuan

• Email:

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