DRUG NAME

Generic name: Doxofylline Injection

Brand name: 安思平

INGREDIENT

The main content of this product is Doxofylline and the chemical name is 1,3-dimethyl-7- (1,3-dioxocyclopentyl-2-yl)methyl-3,7-dihydro-1H-purine-2,6-dione. The chemical structure formula is as follows: C₁₁H₁₄N₄O₄ and the molecular weight is 266.256.

DESCRIPTION

This product is colorless and transparent liquid.

INDICATIONS

Bronchial asthma, asthmatic chronic bronchitis and other bronchial spasm due to breathing difficulties.

FORMAT

0.1g/10ml

DOSAGE AND ADMINISTRATION

Adults dosage: 200mg per time every 12 hours. The drug should be diluted to 40ml by 25% glucose injection with slow intravenous drip. Administration time for adults should be more than 20 minutes.Treatment course is usually 5-10 days or follow doctor's order.

There is another way of administration that is 300mg this product be diluted to 100ml 5% glucose injection or saline injection with slow intravenous drip once a day.

ADVERSE REACTION

With xanthine derivatives involved ,some adverse reaction such as nausea, vomit, epigastric ache, headache, insomnia, irritability, tachycardia, extrasystoles, tachypnea, hyperglycemia and albuminuria could appear. With over-dose administration, some adverse reaction such as serious arrhythmia ，clonospasm etc. could appear which are early toxic symptoms and should suspend administration. Doctor should evaluate and monitor the plasmatic levels. After all the toxic symptoms completely disappear, can continue use this product.

CONTRAINDICATION

1. This product is forbidden for patients who are allergic to theophylline or xanthine derivatives.

2. This product is forbidden for patients with acute myocardial infarction.

CAUTIONS

1. Patients with heart diseases, hypertension, chronic pulmonary heart disease, hyperthyroidism, liver disease, gastrointestinal ulceration, renal insufficiency or co-infection should use it with caution.

2. It is recommended not to drink caffeine-containing beverages and eat caffeine-containing food when using this product.

3. Since large individual differences in theophylline drugs, its necessary to select optimal dosage and administration method of this product depending on individual conditions change and monitor the levels of plasma concentration.

4. When increasing the dosage, attention should be paid to monitoring the blood drug concentration (the treatment is effective within the range of 10 μg/ml. The toxic concentration is above 20μg/ml).

5. The speed of intravenous drip should not be too fast，generally administration time should be more than 45 minutes.

6. This product will be precipitated in low temperature ，please check it carefully before use . Do not use this product if it is turbid.

7. When the temperature is low ,make the product as room temperature before use it .

PREGNANT OR LACTATING WOMEN USE

Pregnant or lactating women are not recommended for using this product.

PEDIATRIC USE

No effectiveness or safety data for pediatric use

GERIATRIC USE

The clearance rate of this product for geriatrics may be different ,so its necessary to monitor the levels of plasma concentration.

DRUG INTERACTIONS

Doxofylline should not be used simultaneously with other xanthine drugs; Be cautious when using ephedrine or other epinephrine drugs together.

Erythrotoxin, acetoideomycin, lincomycin, clindamycin, allopurinol, cimetidine, propranolol and flu vaccines, etc. may weaken the hepatic clearance of xanthine drugs which increases blood concentration.

OVER DOSE

With over-dose administration, some adverse reaction such as serious arrhythmia ，clonospasm etc. could appear which are early toxic symptoms and should suspend administration. Doctor should evaluate and monitor the plasmatic levels. After all the toxic symptoms completely disappear, can continue use this product.

PHARMACOLOGY AND TOXICOLOGY

Doxofylline is derivant of methylxanthine .It is a kind of bronchodilators and effects on bronchus directly to relax the bronchial smooth muscle.It inhibits asthma by inhibiting the action of phosphodiesterase in the smooth muscle cells and relax the smooth muscle.

PHARMACOKINETICS

Patients with chronic bronchitis are given with Doxofylline 100mg dosage by I.V.(administration time :more than 10 minutes) and related results (data) are as follows：1)Peak time (t_max) of plasma drug is about 0.10 hours;2)Peak of plasma concentration (C_max) is about 2.5 ug/ml.;3) Elimination half-life (t_1/2) is about1.83 hours; 4）The medicine is widely distributed in various body fluids and organs；5）Total clearance is (683.6+_197.8)ml/minute. Eating can make peak concentration(C_max) reduces and delay t_max , in this case it should be necessary to increase the dosage.

STORAGE

Sealed storage 

PACKING

Ampoule: 10ml, 3 ampoules /box

VALIDITY

36 months