The xanthine derivative diprophylline, also marketed under the trade names Dilor and Lufyllin, has bronchodilator and vasodilator properties. Respiratory conditions such as bronchitis, heart dyspnea, and asthma are treated with it. It functions as a phosphodiesterase inhibitor and antagonist of adenosine receptors.

Absorption, Distribution and Excretion
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.

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

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Biological Half-Life
2 hours (range 1.8 - 2.1 hours)

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Because of the relatively high levels in milk and a previous report with theophylline, occasional stimulant effects in infants should be anticipated in breastfed infants. No severe adverse reactions are expected. Amounts in milk can be minimized by avoiding breastfeeding for 3 to 4 hours after a dose.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

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Protein Binding
84%

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Interactions
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/

[1]. Xanthine derivatives as antagonists at A1 and A2 adenosine receptors. Naunyn Schmiedebergs Arch Pharmacol. 1985 Sep;330(3):212-21.

[2]. In-vitro evaluation of sustained-release dyphylline tablets. Drug Development and Industrial Pharmacy. Volume 17, 1991 - Issue 2.

Dyphylline is an oxopurine that is theophylline bearing a 2,3-dihydroxypropyl group at the 7 position. It has broncho- and vasodilator properties, and is used in the treatment of asthma, cardiac dyspnea, and bronchitis. It is also an ingredient in preparations that have been promoted for coughs. It has a role as a bronchodilator agent, a vasodilator agent, an EC 3.1.4.* (phosphoric diester hydrolase) inhibitor and a muscle relaxant. It is an oxopurine and a member of propane-1,2-diols.
Dyphylline is a theophylline derivative with broncho- and vasodilator properties. It is typically used in the management of asthma, cardiac dyspnea, and bronchitis.
Dyphylline has been reported in Haplophyllum patavinum and Haplophyllum tuberculatum with data available.
Dyphylline is a xanthine derivative. Dyphilline exerts bronchodilator effects and to a lesser extent vasodilator and diuretic properties. Dyphilline probably acts as a competitive inhibitor of phosphodiesterase which leads to an increase in intracellular cAMP. This results in relaxation of bronchial smooth muscle and other smooth muscles. Dyphylline may also antagonize adenosine receptors. Dyphylline is used in the treatment of acute bronchial asthma, chronic bronchitis and emphysema.
A THEOPHYLLINE derivative with broncho- and vasodilator properties. It is used in the treatment of asthma, cardiac dyspnea, and bronchitis.

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

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Mechanism of Action
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/

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Therapeutic Uses
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.

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Drug Warnings
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/

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Pharmacodynamics
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.

C10H14N4O4

254.24

254.101

479-18-5

3182

White to off-white solid powder

1.6±0.1 g/cm3

589.6±60.0 °C at 760 mmHg

161-162 °C(lit.)

310.4±32.9 °C

0.0±1.7 mmHg at 25°C

1.689

-1.1

2

5

3

18

364

0

KSCFJBIXMNOVSH-UHFFFAOYSA-N

InChI=1S/C10H14N4O4/c1-12-8-7(9(17)13(2)10(12)18)14(5-11-8)3-6(16)4-15/h5-6,15-16H,3-4H2,1-2H3

7-(2,3-dihydroxypropyl)-1,3-dimethylpurine-2,6-dione

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility in Formulation 1: ≥ 3 mg/mL (11.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 3 mg/mL (11.80 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 3 mg/mL (11.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 100 mg/mL (393.33 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)