Diprophylline

254.24

254.24

207-526-1

756753|40844|14305

DTXSID6022975

CRYSTALS FROM ALCOHOL|WHITE AMORPHOUS SOLID

R - Respiratory system

2939590000

98.9

-1.8

White Powder

1.6±0.1 g/cm3

158 °C

589.6°C at 760 mmHg

310.4±32.9 °C

1.689

H2O: 33 g/100 mL (25 ºC)

Hygroscopic, Refrigerator, Under Inert Atmosphere

9.57E-15mmHg at 25°C

LD50 in mice (mg/kg): 3400 orally; 1430 s.c. (Al'tshuler)

EXTREME BITTER TASTE

(1% AQ SOLN) 6.6 TO 7.3

152.6 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

NONH for all modes of transport

3

22-36/37/38

36-36/37-26

XH5100000

Xn,Xi

IS STABLE IN GASTRIC JUICE

P301 + P312 + P330

H302

|Danger|H302: Harmful if swallowed [Warning Acute toxicity, oral]|P260, P264, P270, P301+P312, P307+P311, P314, P321, P330, P405, and P501

LD50=1954 mg/kg (orally in mice)

METHYLXANTHINES CAN ALSO ANTAGONIZE EFFECTS OF HYPOPROTHROMBINEMIA CAUSED BY COUMARIN DERIV... /METHYLXANTHINES/|XANTHINES CAN MARKEDLY POTENTIATE CARDIAC INOTROPIC RESPONSES TO BETA-ADRENERGIC AGONISTS & TO GLUCAGON. /XANTHINES/

84%

For relief of acute bronchial asthma and for reversible bronchospasm associated with chronic bronchitis and emphysema.

Bronchodilator Agents; Phosphodiesterase Inhibitors; Vasodilator Agents|THEOPHYLLINE PREPN...ARE USED TO RELAX BRONCHIAL SMOOTH MUSCLE & TO STIMULATE MYOCARDIUM. ... THEOPHYLLINE COMPD...PLAY IMPORTANT ROLE IN MGMNT OF ASTHMATIC PT. THEY ARE USEFUL AS PROPHYLACTIC DRUGS & ARE VALUABLE ADJUNCTS IN TREATMENT OF PROLONGED ATTACKS & IN MGMNT OF STATUS ASTHMATICUS. /THEOPHYLLINE COMPD/|PERIPHERAL VASODILATOR & BRONCHODILATOR ACTIONS CHARACTERISTIC OF THEOPHYLLINE DERIV. IT IS EFFECTIVE ORALLY BUT HAS NOT BEEN SHOWN TO BE SUPERIOR TO THEOPHYLLINE SODIUM GLYCINATE. IT ALSO HAS TYPICAL DIURETIC & MYOCARDIAL STIMULANT EFFECTS.|...CAN BE USED INTRAMUSCULARLY WITHOUT PRODUCING LOCAL PAIN BECAUSE IT IS NEUTRAL SOL DERIV.|For more Therapeutic Uses (Complete) data for DYPHYLLINE (11 total), please visit the HSDB record page.

IT IS NOT RECOMMENDED FOR USE IN CORONARY DISEASE OR ANGINA PECTORIS UNTIL IT CAN BE SHOWN THAT INCR CORONARY BLOOD FLOW PRECEDES RATHER THAN FOLLOWS MYOCARDIAL STIMULATION.|METHYLXANTHINES CAN ALSO STIMULATE RELEASE OF CATECHOLAMINES FROM ADRENAL MEDULLA & LARGE INCR IN URINARY EXCRETION OF EPINEPHRINE OCCUR... /METHYLXANTHINES/

Dyphylline, a xanthine derivative, is a bronchodilator used for relief of acute bronchial asthma and for reversible bronchospasm associated with chronic bronchitis and emphysema. Dyphylline is a xanthine derivative with pharmacologic actions similar to theophylline and other members of this class of drugs. Its primary action is that of bronchodilation, but it also exhibits peripheral vasodilatory and other smooth muscle relaxant activity to a lesser degree.

Agents that cause an increase in the expansion of a bronchus or bronchial tubes. (See all compounds classified as Bronchodilator Agents.)|Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases. (See all compounds classified as Phosphodiesterase Inhibitors.)|Drugs used to cause dilation of the blood vessels. (See all compounds classified as Vasodilator Agents.)

Dyphylline exerts its bronchodilatory effects directly and, unlike the­ophylline, is excreted unchanged by the kidneys without being metabolized by the liver. Approximately 88% of a single oral dose can be recovered from the urine unchanged.|...RAPID RATE OF DISPOSITION.|IT MAY BE MORE CONSISTENTLY ABSORBED FROM GI TRACT & LESS IRRITATING THAN THEOPHYLLINE & AMINOPHYLLINE.|SINGLE DYPHYLLINE DOSE WAS GIVEN TO 5 NORMAL VOLUNTEERS. DOSES OF 19-27 MG/KG RESULTED IN PEAK SERUM CONCN OF 19.3-23.5 MUG/ML & WERE TOLERATED WELL BY 4 SUBJECTS. 1 HAD SEVERE HEADACHE AFTER 28 MG/KG DOSE ASSOC WITH 36.4 MUG/ML; WAS NOT METABOLIZED TO THEOPHYLLINE.|IN 5 NORMAL VOLUNTEERS MEAN T/2 WAS 1.8 HR; MEAN TOTAL BODY CLEARANCE RATE & MEAN RENAL CLEARANCE RATE WERE 333 & 276 ML/MIN, RESPECTIVELY. MEAN VOL OF DISTRIBUTION WAS 0.8 L/KG. IN URINE 83% OF DOSE WAS EXCRETED UNCHANGED & THEOPHYLLINE WAS NOT DETECTED.|For more Absorption, Distribution and Excretion (Complete) data for DYPHYLLINE (6 total), please visit the HSDB record page.

Hepatic|IN BODY XANTHINES ARE ONLY PARTIALLY DEMETHYLATED & OXIDIZED. THEY ARE LARGELY EXCRETED AS METHYLURIC ACIDS OR AS METHYLXANTHINES. /XANTHINES/

2 hours (range 1.8 - 2.1 hours)

The bronchodilatory action of dyphylline, as with other xanthines, is thought to be mediated through competitive inhibition of phosphodiesterase with a resulting increase in cyclic AMP producing relaxation of bronchial smooth muscle as well as antagonism of adenosine receptors.|THEIR MOST IMPORTANT ACTION...IS THEIR ABILITY TO RELAX SMOOTH MUSCLES OF BRONCHI... THEOPHYLLINE IS MOST EFFECTIVE... /THEOPHYLLINE/|ACTION OF XANTHINES ON MOTOR ACTIVITY OF GI TRACT... DILUTE SOLN INCR, & HIGH CONCN DEPRESS, TONE & STRENGTH OF CONTRACTION OF ISOLATED INTESTINAL STRIPS. /XANTHINES/|...ACTION SEEMS TO RESULT FROM INCR IN CONCN OF FACTOR V (AC-GLOBULIN) IN PLASMA WHICH, IN TURN, MAY BE CAUSED BY INCR IN PLASMA CONCN OF FREE FATTY ACIDS PRODUCED...THERE ARE ALSO INCR IN CONCN OF CIRCULATING PROTHROMBIN & FIBRINOGEN. /XANTHINES/|...ACCOMPANYING DECR IN VENOUS FILLING PRESSURE, WHICH IS CAUSED @ LEAST PARTLY BY MORE COMPLETE EMPTYING OF HEART. /THEOPHYLLINE/

PARENTERALLY ADMIN THEOPHYLLINE...INCR RATE & DEPTH OF RESP... AFTER ADMIN OF LARGE AMT OF...THEOPHYLLINE, ENTIRE CNS, INCL SPINAL CORD, IS STIMULATED. REFLEX EXCITABILITY IS INCR, & LOWER MOTOR CENTERS MAY BE DIRECTLY EXCITED. /THEOPHYLLINE/|THEOPHYLLINE...CAN BE QUITE TOXIC & HAS OCCASIONALLY PROVED FATAL. /THEOPHYLLINE/|GREAT CARE...MUST BE EXERCISED WHEN /SALTS OF XANTHINES/...ARE ADMIN /IV/... ESP IN PT WITH SEVERE MYOCARDIAL DAMAGE, FOR HIGH LOCAL CONCN MAY RESULT IN PPT OF FREE ALKALOIDS WHEN SALTS ARE EXPOSED TO PH OF BLOOD. ...SHARP, USUALLY TRANSIENT, FALL IN BLOOD PRESSURE...WHEN INJECTION IS TOO RAPID. /XANTHINE SALTS/

Dihydroxypropyltheophylline

TABLETS (200 MG), ELIXIR (100 MG/15 ML), & AMPULS (500 MG/2 ML) ARE AVAIL.|ORAL: ELIXIR 100 MG/15 ML; TABLETS 200 MG; TABLETS (TIMED-RELEASE) 400 MG. ... ELIXIR 160 MG/15 ML; TABLETS 200 & 400 MG. INJECTION: SOLN 250 MG/ML IN 2 & 10 ML CONTAINERS.

1H-Purine-2,6-dione, 7-(2,3-dihydroxypropyl)-3,7-dihydro-1,3-dimethyl-: ACTIVE

QUALITATIVE DETERMINATION /XANTHINE GROUP ALKALOIDS/.

SIMPLE RAPID HIGH-PRESSURE LIQUID CHROMATOGRAPHIC METHOD FOR DETERMINATION OF DYPHYLLINE.|DETERMINED ON A C18-REVERSE PHASE MUBONDAPAK COLUMN WITH A MOBILE PHASE ACETONITRILE 9% (VOL/VOL) IN WATER & WITH BETA-HYDROXYETHYLTHEOPHYLLINE AS INTERNAL STD.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals