What Are the Side Effects of Diltiazem?

Diltiazem hydrochloride for injection, 1. supraventricular tachycardia 2. emergency treatment of abnormal hypertension during surgery 3. hypertension emergency 4. unstable angina pectoris

Diltiazem hydrochloride for injection, 1. supraventricular tachycardia 2. emergency treatment of abnormal hypertension during surgery 3. hypertension emergency 4. unstable angina pectoris

Drug Name

Diltiazem hydrochloride for injection

Drug type

Occupational injury medical insurance

Use classification

Calcium antagonists

Diltiazem hydrochloride for injection

Chemical name: cis-(+)-5-[(2-dimethylamino) ethyl] -2- (4-methoxyphenyl) -3-acetoxy-2,3-dihydro-1, 5-Benzothiazepine-4 (5H) -one hydrochloride.
Chemical Structure:

Molecular formula: C ₂₂ H ₂₆ N ₂ O ₄ S · HCl
Molecular weight: 450.99
Excipients: D-mannitol.

Diltiazem hydrochloride for injection

This product is white lumps or porous solid, and tasteless. This product is soluble in water.

Indications for diltiazem hydrochloride for injection

1. supraventricular tachycardia 2. emergency treatment of abnormal hypertension during surgery 3. hypertension emergency 4. unstable angina pectoris

Diltiazem hydrochloride for injection

(1) 10mg; (2) 50mg

Dosage and dosage of diltiazem hydrochloride for injection

Dissolve diltiazem hydrochloride (10mg or 50mg) for injection with 5ml or more of normal saline or glucose injection, and use it as follows:
1. A single intravenous injection of supraventricular tachycardia, usually an adult dose of 10 mg diltiazem hydrochloride slowly intravenously for about 3 minutes, and can be increased or decreased appropriately according to age and symptoms.
2. A single intravenous injection of emergency treatment for abnormal hypertension during surgery, usually a slow intravenous injection of 10 mg of diltiazem hydrochloride to an adult within about 1 minute, and can be appropriately increased or decreased according to the age and symptoms of the patient.
Intravenous infusion, diltiazem hydrochloride is usually administered intravenously to an adult at a rate of 5 to 15 g / kg / min. When the blood pressure drops to the target value, adjust the drip rate while monitoring the blood pressure.
3. Hypertensive emergencies usually include intravenous diltiazem hydrochloride at a rate of 5 to 15 g / kg / min. When the blood pressure drops to the target value, adjust the drip rate while monitoring the blood pressure.
4. Unstable angina pectoris is usually administered intravenously to diltiazem hydrochloride at a rate of 1 to 5 g / kg / min. It should start with a small dose and then increase or decrease according to the condition.

Adverse reactions of diltiazem hydrochloride for injection

There were 266 (4.1%) adverse reactions in 6,543 treated patients. Common adverse reactions were bradycardia (1.1%), hypotension (0.7%), first degree atrioventricular block (0.4%), second degree atrioventricular block (0.3%), and atrioventricular junction rhythm ( 0.3%) and so on.
(1) Serious adverse reactions (occasional: 0.1% to <5%, rare: <0.1%)
Occasionally complete atrioventricular block, severe bradycardia (initial symptoms: bradycardia, dizziness, mild headache, etc.) may sometimes lead to cardiac arrest. You need to be fully prepared for these symptoms before starting medication. If abnormalities occur, the drug should be stopped immediately and the following treatments should be performed: complete atrioventricular block, severe bradycardia: give atropine sulfate, isoproterenol, etc. and / or use cardiac pacing. Cardiac cessation: Perform cardiac massage and give catecholamines such as epinephrine for cardiac resuscitation.
Rarely, congestive heart failure. Once it occurs, the medication should be stopped and appropriate treatment should be performed.
(2) Other adverse reactions If adverse reactions occur, appropriate treatment (such as discontinuation of the drug) should be given and appropriate treatment should be performed.
The incidence rate is 0.1% ~ <5%. Adverse reactions are:
Bradycardia, atrioventricular block, hypotension, atrioventricular junction rhythm, preconstriction, sinus arrest, facial fever, facial flushing, headache, nausea, elevated GOT, GPT, LDH, etc.
Incidence: <0.1% Adverse reactions are:
Sinoatrial block, bundle branch block, palpitations, dizziness, paroxysmal tachycardia, headache, nausea, vomiting, increased AL-P, decreased urine output, increased serum creatinine and BUN, rash, itching, Local redness at the injection site.
The frequency of adverse reactions is unknown: photosensitivity (oral preparations), phlebitis.

Diltiazem hydrochloride for injection contraindications

1. Patients with severe hypotension or cardiogenic shock.
2. and degree atrioventricular block or sick sinus syndrome (sustained 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. Those who are allergic to any of the ingredients in the drug.
6. Women who are pregnant or likely to become pregnant.

Precautions for diltiazem hydrochloride for injection

1. The following patients should be used with caution in patients with congestive heart failure, patients with cardiomyopathy, patients with acute myocardial infarction, bradycardia in patients with 1 degree atrioventricular block, and patients with hypotension with WPW syndrome and LGL syndrome. Patients with -blockers with severe liver and kidney dysfunction 2. Important considerations Continuous monitoring of ECG and blood pressure The use of this drug may sometimes lead to complete atrioventricular block, severe bradycardia, or even cardiac arrest. Pay full attention to the following points (refer to [Adverse Reactions]).
It is limited to the minimum dosage necessary for treatment or the shortest medication time required for intravenous drip.
Fully observe the state of the patient during or after the medication, and pay attention to the early detection of the above symptoms.
Make full preparations for the above symptoms when taking the medicine. If abnormality is found, stop using the medicine immediately and take appropriate measures.
Other antiarrhythmic drugs (dasulopine phosphate) in combination with terfenadine have been reported to cause prolonged QT intervals and ventricular arrhythmias.
Intravenous diltiazem and intravenous beta-blockers should be avoided at the same time or within a similar period (within a few hours).
Patients with ventricular tachycardia, patients with wide QRS tachycardia (QRS 0.12s) may experience hemodynamic deterioration and ventricular fibrillation when using calcium channel blockers. Before intravenous diltiazem, it is important to identify the wide QRS complex as supraventricular or ventricular.
For severe episodes of angina pectoris that last more than 15 minutes, it is necessary to consider other treatment methods (PTCA, CABG, etc.).
In rare cases, diltiazem can prolong atrioventricular node conduction and refractory periods and cause and degree atrioventricular block in patients with sinus heart rate. The combined use of diltiazem and drugs that affect cardiac conduction can cause additive side effects. If high AV block occurs during sinus rhythm, the drug should be discontinued immediately and supportive care should be taken.
Although in vitro experiments show that diltiazem has a negative inotropic effect, blood flow to healthy people with normal ventricular function and patients with severe cardiomyopathy (such as severe congestive heart failure, acute MI, and hypertrophic cardiomyopathy) The results of kinetic studies showed no decrease in heart index and no negative effect on cardiac contraction. Patients with acute myocardial infarction and X-ray diagnosed pulmonary congestion cannot take diltiazem orally. Patients with impaired ventricular function have limited experience with diltiazem for injection, and care should be taken in these patients.
Intravenous diltiazem can cause orthostatic hypotension. Hemodynamically deficient supraventricular tachycardia should be treated with diltiazem intravenously. In addition, patients taking drugs that can reduce peripheral impedance, vascular volume, myocardial contractility, or myocardial conduction should also use this product with caution.
Very few patients take diltiazem orally to increase alkaline phosphatase, LDH, SGOT, SGPT and other enzymes, and other phenomena related to acute liver damage can be seen. Therefore, intravenous diltiazem is also at risk of acute liver damage.
Ventricular premature beats may occur when PSVT is converted to sinus rhythm. These ventricular premature beats are usually transient and benign and have no clinical significance. Similar ventricular syndromes can occur when electroconversion, other medications, and spontaneous conversion of PSVT to sinus heart rate.
Oral diltiazem has occasionally been reported with erythema polymorpha and / or exfoliative dermatitis. Therefore, intravenous administration of this product also has the possibility of skin reactions, and should be discontinued if skin reactions occur.
3. When using with other chemicals, if the pH exceeds 8, diltiazem hydrochloride may precipitate.

Diltiazem hydrochloride for injection for pregnant and lactating women

1. Women who are pregnant or likely to become pregnant should not use it.
2. Breastfeeding women should avoid using it as much as possible. When it is necessary for clinical use, breastfeeding should be stopped.

Diltiazem hydrochloride for injection for children

This experiment was not performed and there are no reliable references.

Diltiazem hydrochloride for injection

Generally, the elderly patients have lower physiological functions. When using, they should start with a low dose, and carefully observe the symptoms of the patients when they are administered.

Diltiazem hydrochloride for injection drug interactions

Diltiazem hydrochloride for injection overdose

Symptoms: Drug overdose can cause bradycardia, complete atrioventricular block, heart failure, and hypotension.
Disposal: When overdose occurs, medication should be stopped and the following treatments should be performed:
(1) Bradycardia and complete atrioventricular block:
Give atropine sulfate, isoprenaline, etc. and / or use cardiac pacing.
(2) Heart failure and hypotension:
Give a cardiotonic agent, a booster, an infusion, etc. and / or use a cardiac assisted circulation device.

Pharmacology and toxicology of diltiazem hydrochloride for injection

Pharmacological effects can inhibit the influx of calcium ions into peripheral blood vessels, coronary smooth muscle cells and atrioventricular node cells, thereby expanding the blood vessels and prolonging atrioventricular node conduction, thereby producing effects on hypertension, arrhythmia and angina pectoris.
1. Effect on blood pressure (1) It can reduce elevated hypertension during anesthesia and awake, but the effect is strengthened under anesthesia. It has no significant effect on blood pressure in normal rats and has a strong antihypertensive effect on hypertensive rats.
(2) Can reduce peripheral vascular resistance and myocardial oxygen consumption in dogs, and increase cardiac output.
(3) It does not reduce blood flow to the brain, coronary arteries, and kidneys while reducing blood pressure in dogs and monkeys, and has a sodium-releasing and diuretic effect.
2. Effect on arrhythmia (1) It can prolong atrioventricular node conduction time, effective refractory period and functional refractory period, and is effective for dogs with supraventricular tachycardia.
(2) It can inhibit supraventricular tachycardia in rabbits caused by atrial electrical stimulation.
3. Effect on myocardial ischemia (1) Improve myocardial oxygen supply and demand balance.
Dilate the coronary arterial trunk and collaterals of dogs and increase blood flow in the ischemic area of myocardium.
Inhibit coronary artery spasm in pigs and humans.
(2) Cardioprotective effect Maintains cardiac function, improves energy metabolism, and reduces ischemic area by inhibiting excessive calcium ions from entering ischemic cardiomyocytes in dogs and cats.
4. Clinical efficacy (1) Double-blind trial of supraventricular tachycardia using placebo as a control, the results prove that this drug is suitable for paroxysmal supraventricular tachycardia, rapid atrial fibrillation and atrial flutter . The effective rates were 86.4% (184/213) and 87.2% (130/149).
(2) Emergency treatment of abnormal hypertension during surgery A single-blind clinical trial using nitroglycerin (injection) as a control drug has proven that this drug is effective for emergency treatment of abnormal hypertension during surgery, with an effective rate of 94.0% (315 / 335).
(3) The effective rate of hypertensive emergency to hypertensive emergency such as malignant hypertension, hypertensive encephalopathy, dissecting aneurysm, and acute left heart failure is 100.0% (28/28).
(4) The results of a randomized single-blind clinical trial of unstable angina pectoris confirm that the drug is effective for unstable angina pectoris, with an effective rate (more than moderate improvement) of 80.0% (32/40).
Toxicity study. High-dose intravenous injection of diltiazem and diltiazem hydrochloride in dogs may show significant bradycardia and changes in atrioventricular conduction.
In subacute and chronic toxicity studies in dogs and rats, high-dose oral diltiazem can cause liver damage. In a subacute liver toxicity study, oral administration of 125 mg / kg diltiazem in rats can cause histological changes in the liver, which can be restored after drug withdrawal; oral administration of 20 mg / kg diltiazem in dogs can cause liver changes. Can resume after continued medication.

Pharmacokinetics of diltiazem hydrochloride for injection

Plasma drug concentration · The single-dose diltiazem elimination half-life is about 1.9 hours.
· Intravenous injection of blood drug concentration reached steady state for 5-6 hours.

Storage of diltiazem hydrochloride for injection

Sealed and stored below 20 ° C.

Diltiazem Hydrochloride for Injection Packaging

Xilin bottle (1) 10mg: 5 bottles / box; 10 bottles / box (2) 50mg: 1 bottle / box; 10 bottles / box

Diltiazem hydrochloride for injection

36 months

Diltiazem hydrochloride for injection

Import drug registration standard JX200100130

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