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Diltiazem hydrochloride for injection

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

Approval date: April 15, 2009

Modified on May 07, 2016

Please read the instructions carefully and use under the guidance of a physician

[Drug name] Common name: Diltiazem hydrochloride for injection
English name: Diltiazem Hydrochloride for Injection
Phonetic script: Zhusheyong Yansuan Di'erliuzhuo

[Ingredients]

The active ingredient of this product is diltiazem hydrochloride, and its chemical name is: 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: mannitol.

[Character] This product is white or almost white loose block or powder.

[Specifications] (1) 10mg; (2) 50mg

【Dosage】

Dissolve diltiazem hydrochloride (10mg or 50mg) for injection with 5ml or more of normal saline or glucose injection, and use it as follows:

1. supraventricular tachycardia

A single intravenous injection, usually an adult dose of 10 mg diltiazem hydrochloride slowly intravenously about 3 minutes, and can be appropriately increased or decreased according to age and symptoms.

2. Emergency treatment of abnormal hypertension during surgery

A single intravenous injection is usually a slow intravenous injection of 10 mg of diltiazem hydrochloride to an adult within about 1 minute, which can be appropriately increased or decreased according to the age and symptoms of the patient.

For intravenous drip, diltiazem hydrochloride is usually administered intravenously to an adult at a rate of 5 to 15 μg / kg / min. When the blood pressure drops to the target value, adjust the drip rate while monitoring the blood pressure.

3. Hypertension Emergencies

Diltiazem hydrochloride is usually administered intravenously to an adult at a rate of 5 to 15 μg / kg / min. When the blood pressure drops to the target value, adjust the drip rate while monitoring the blood pressure.

4. Unstable angina

Generally, an adult intravenously injects diltiazem hydrochloride at a rate of 1 to 5 μg / kg / min. It should start with a small dose and then increase or decrease according to the condition. The maximum dosage is 5 μg / kg / min.

【Adverse reactions】

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%)

① Occasionally complete atrioventricular block, severe bradycardia (initial symptoms: bradycardia, dizziness, mild headache, etc.) may sometimes lead to cardiac arrest, and you should fully prepare for these symptoms before starting medication. If abnormality occurs, the drug should be stopped immediately and the following treatments should be performed: complete atrioventricular block, severe bradycardia: give atropine sulfate, isoprenaline, etc. and / or use a pacemaker. Cardiac cessation: Perform cardiac massage and give catecholamines such as epinephrine for cardiac resuscitation.

② 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 should be given (such as discontinuation) and appropriate treatment.

The incidence rate is 0.1% ~ <5%. Adverse reactions are:

Bradycardia, atrioventricular block, hypotension, atrioventricular junction rhythm, preconstriction, sinus arrest, facial fever, facial flushing, elevated GOT, GPT, LDH, etc.

Incidence: <0.1% Adverse reactions are:

Sinoatrial block, bundle branch block, palpitations, dizziness, paroxysmal tachycardia, headache, nausea, vomiting, increased AI-P, decreased urine output, increased serum creatinine and BUN, rash, itching, Local redness at the injection site.

Oral preparations are still visible, but the frequency is unknown.

[Taboo]

1. Patients with severe hypotension or cardiogenic shock.

2. Ⅱ and Ⅲ 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】

1.Use with caution for the following patients

Patients with congestive heart failure

Patients with cardiomyopathy

Patients with acute myocardial infarction

Bradycardia, 1 degree atrioventricular block

Patients with hypotension

Patients with atrial fibrillation and atrial flutter with WPW syndrome and LGL syndrome

Patients using β-blockers

Patients with severe liver and kidney dysfunction

2. Important notes

Continuous monitoring of ECG and blood pressure

When using this medicine, sometimes complete atrioventricular block, severe bradycardia, or even cardiac arrest may occur, so you need to pay full attention to the following points (see [Adverse Reactions]).

① It is limited to the minimum dosage necessary for treatment or the shortest medication time required for intravenous drip.

② Fully observe the state of the patient during or after the medication, and pay attention to the early detection of the above symptoms.

③ 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 with calcium channel blockers. Before intravenous diltiazem, it is important to identify the wide QRS complex as supraventricular or ventricular.

For patients with severe angina pectoris that lasts 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 period, which can cause Ⅱ and Ⅲ degree AV block in patients with sinus rhythm. 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 hydrochloride 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 who are taking drugs that 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. Use caution

When mixed with other chemicals, if the pH exceeds 8, diltiazem hydrochloride may precipitate.

[Medication 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.

[Child medication]

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

[Medicine for the elderly]

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.

【medicine interactions】

Precautions for combined medication

[Drug 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]

Pharmacological action

By inhibiting the influx of calcium ions into peripheral blood vessels, coronary smooth muscle cells and atrioventricular node cells, it has the effect of expanding blood vessels and prolonging atrioventricular node conduction, thereby producing effects on hypertension, arrhythmia and angina pectoris.

1. Effect on blood pressure

(1) Elevated hypertension can be reduced during anesthesia and awake, but the effect is enhanced 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 canine supraventricular tachycardia.

(2) It can inhibit supraventricular tachycardia in rabbits caused by atrial electrical stimulation.

3. Effect on myocardial ischemia

(1) Improve the supply and demand balance of myocardial oxygen.

① Dilate the coronary arterial trunk and collaterals of dogs and increase blood flow in the ischemic area of myocardium.

② Inhibit coronary artery spasm in pigs and humans.

(2) Myocardial protection

By inhibiting excessive calcium ions from entering ischemic cardiomyocytes in dogs and cats, heart function is maintained, energy metabolism is improved, and the area of the ischemic area is reduced.

4. Clinical effect

(1) supraventricular tachycardia

A double-blind trial with placebo as a control drug proved that the 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) Hypertension emergency

The effective rate for hypertensive emergencies such as malignant hypertension, hypertensive encephalopathy, dissection aneurysms, and acute left heart failure was 100.0% (28/28).

(4) unstable angina

The results of randomized single-blind clinical trials confirmed that this drug is effective for unstable angina pectoris, with an effective rate (more than moderate improvement) of 80.0% (32/40).

Toxicology research

Large doses of intravenous diltiazem in dogs can 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】

Plasma drug concentration

The single elimination of diltiazem has a half-life of about 1.9 hours.

Intravenous administration of the drug in a steady state for 5 to 6 hours.

[Storage] Sealed and kept in a cool and dark place.

[Packaging] Low Borosilicate Glass Controlled Injection Bottle

(1) 10mg: 1 stick / box; 6 sticks / box; 8 sticks / box; 10 sticks / box

(2) 50mg: 1 stick / box; 6 sticks / box; 8 sticks / box; 10 sticks / box

[Validity] 24 months

[Executive Standard] WS1- (X-015) -2010Z-2015

[Approval number] (1) 10mg: National Medicine Standard H20093456

(2) 50mg: National Medicine Standard H20093455

【manufacturer】