479-18-5Cn1c(=O)c2c(ncn2CC(O)CO)n(C)c1=OKSCFJBIXMNOVSH-UHFFFAOYSA-NDyphylline 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.
479-18-5DTXSID6022975CHEMBL1752CHEBI:4728-1.9
-1.25
CRYSTALS FROM ALCOHOL
WHITE AMORPHOUS SOLID
FREELY SOL IN WATER; 1 G IN 3 ML H2O @ 25 °C
SOL IN ALC: 2 G/100 ML; IN CHLOROFORM: 1 G/100 ML
1.43e+01 g/L
>38.1 [ug/mL] (The mean of the results at pH 7.4)
Breast Feeding; Lactation; Milk, Human; Anti-Asthmatic Agents; Bronchodilator Agents
FDA approved drugs -> Active ingredient
FDA approved drugs -> Active ingredient
Pharmaceuticals
155-157
158 °C
161.5 °C
안전 정보는 참고용이며, 공급업체의 물질안전보건자료(SDS), 관련 법규 및 전문가 평가를 대체하지 않습니다.
Warning
H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]
P261, P264, P270, P271, P301+P317, P304+P340, P317, P330, and P501 (click each P-code to see the statement)
Aggregated GHS information provided per 61 reports by companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
Danger
H302: Harmful if swallowed [Warning Acute toxicity, oral]
Acute Tox. 4 (100%)
Acute toxicity (Oral) - Category 4
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/
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/
R - Respiratory system
QR - Respiratory system
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.
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/
Hepatic
IN BODY XANTHINES ARE ONLY PARTIALLY DEMETHYLATED & OXIDIZED. THEY ARE LARGELY EXCRETED AS METHYLURIC ACIDS OR AS METHYLXANTHINES. /XANTHINES/
불러오는 중…
152.6 Ų [M+H]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]
151.82 Ų [M+H]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]
white to light yellow crystal powder
Drug Induced Liver Injury Rank (DILIrank 2.0)
Dyphylline
vNo-DILI-concern
0
No match
DOI:10.1016/j.drudis.2016.02.015
Agents that cause an increase in the expansion of a bronchus or bronchial tubes.
Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases.
Drugs used to cause dilation of the blood vessels.
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.
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.
개요Dyphylline is the N-7 dihydroxypropyl derivative of theophylline and is not a theophylline salt. Dyphylline does not get metabolized to theophylline in vivo, and even though it contains 70% theophylline by molecular weight ratio, the equivalent amount to theophylline is not known. Dosing must be accomplished independently by monitoring dyphylline blood levels. Dyphylline has a diminished bronchodilator effect compared to theophylline, but it may have lower and less serious side effects. Dosage forms available are an elixir and tablets.
용도PDE inhibitor, bronchodilator, vasodilator
정의ChEBI: 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.