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Diflunisal

Outline Pharmacokinetics Clinical application Precaution Adverse reaction
Diflunisal
Diflunisal structure
CAS No.
22494-42-4
Chemical Name:
Diflunisal
Synonyms
mk647;Adomal;MK 647;Dolisal;Dolobid;Dolobil;Dolobis;Flustar;Difludol;Flovacil
CBNumber:
CB9674965
Molecular Formula:
C13H8F2O3
Formula Weight:
250.2
MOL File:
22494-42-4.mol

Diflunisal Properties

Melting point:
207-209?C
Density 
1.3505 (estimate)
storage temp. 
Refrigerator
solubility 
Practically insoluble in water, soluble in ethanol (96 per cent). It dissolves in dilute solutions of alkali hydroxides.
pka
pKa 3.3 (H2O I=0.1) (Uncertain)
form 
neat
CAS DataBase Reference
22494-42-4(CAS DataBase Reference)
NIST Chemistry Reference
Diflunisal(22494-42-4)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  Xn,Xi
Risk Statements  22-36/37/38-63
Safety Statements  22-26-36
WGK Germany  3
RTECS  DV2030000
Hazard Note  Irritant
Toxicity LD50 orally in female mice: 439 mg/kg (Stone)
Symbol(GHS):
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning P264, P270, P301+P312, P330, P501
H315 Causes skin irritation Skin corrosion/irritation Category 2 Warning P264, P280, P302+P352, P321,P332+P313, P362
H319 Causes serious eye irritation Serious eye damage/eye irritation Category 2A Warning P264, P280, P305+P351+P338,P337+P313P
H335 May cause respiratory irritation Specific target organ toxicity, single exposure;Respiratory tract irritation Category 3 Warning
H361 Suspected of damaging fertility or the unborn child Reproductive toxicity Category 2 Warning P201, P202, P281, P308+P313, P405,P501
Precautionary statements:
P261 Avoid breathing dust/fume/gas/mist/vapours/spray.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P281 Use personal protective equipment as required.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Diflunisal price More Price(7)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich D3281 Diflunisal analytical standard 22494-42-4 5g $43.8 2018-11-20 Buy
Sigma-Aldrich 1197506 Diflunisal United States Pharmacopeia (USP) Reference Standard 22494-42-4 200mg $338.1 2018-11-20 Buy
Cayman Chemical 19187 Diflunisal ≥98% 22494-42-4 5g $35 2018-11-13 Buy
Cayman Chemical 19187 Diflunisal ≥98% 22494-42-4 10g $67 2018-11-13 Buy
Sigma-Aldrich D1750000 Diflunisal European Pharmacopoeia (EP) Reference Standard 22494-42-4 d1750000 $179 2018-11-23 Buy

Diflunisal Chemical Properties,Uses,Production

Outline

Diflunisal, a nonsteroidal anti-inflammatory analgesic, is the most promising alternative to aspirin.It is used clinically for the treatment of rheumatoid arthritis, rheumatoid arthritis, osteoarthritis, sprain, strain and analgesia. Researches have indicated that diflunisal and ibuprofen are effective in the treatment of rheumatoid arthritis and degenerative arthritis. It has also been observed that diflunisal is superior to ibuprofen in improving the grip strength and relieving joint pain and tenderness of rheumatoid arthritis and degenerative arthritis in patients with rheumatoid arthritis. At the same time, diflunisal can decrease and alleviate the rheumatoid factor titre in patients with rheumatoid arthritis and stiffness,The analgesic effect of diflunisal is 7.5 to 13 times as high as aspirin.Its antipyretic effect is 1.4 times as high as aspirin, and its therapeutic effect is about 3 times as strong as aspirin. Therefore, it is suitable for treating rheumatoid arthritis, osteoarthritis, muscle sprain, strain, meniscus surgery, orthopedic and oral surgery, and primary pain caused by dysmenorrhea. It is worthy of clinical application.Diflunisal is selected from more than 500 salicylic acid derivatives by American company Merck Sharp & Do hme using the flunisal as the leading compound in 1975. It was launched in 1975. Now it is one of the Merck Co's annual sales of over 100 million US dollars. And it has been listed in more than 70 countries, such as Britain, the United States, Japan, Italy, France and other countries. It has also been recorded by the United States Pharmacopoeia and the British Pharmacopoeia. In China, the tablets and capsules of diflunisal have been approved for production.

Pharmacokinetics

This product is well absorbed in oral administration, and the blood concentration 2 ~ 3H after taking will reach the peak.The half-life is proportional to the dosage, about 8 to 12h, and the binding rate of plasma protein is 90%. Oral administration of 125mg should be 3 ~ 4d and 500mg should be 7 to 9d. .The elimination of half-life of 125mg is 7 to 8h, and 500mg is 15h.Its binding rate with plasma protein in normal human body is up to 98% ~ 99%.The content of breast milk in lactating women is 2% ~ 7% of the blood concentration.It is not metabolized into salicylic acid in the body.80% to 95% of the drugs will be discharged from the urine in the form of 2 soluble glucoside complexes within 72-96h.

Clinical application

This product can inhibit the synthesis of prostaglandin with analgesic, anti-inflammatory and antipyretic effects. It is used to relieve the moderate pain in bone and rheumatoid arthritis.It is also used to relieve pain and joint, muscle sprain and cancer pain after meniscus and orthopedic surgery. The drug will take effect 1h after taking and the effect lasts for 8 ~ 12h.It can also be used to treat osteoarthritis and rheumatoid arthritis etc.

Precaution

  1. The combined use with hydrochlorothiazine, indomethacin, and paracetamol can increase the plasma concentration of these drugs. 
  2. Long-term application can cause renal function damage and drug accumulation, so the patients with renal insufficiency should be careful in application with reduced doses.
  3. This drug is forbidden for patients with cardiac insufficiency, hypertension, edema, peptic ulcer and bleeding as well as for pregnant women and breast-feeding women.
  4. It is forbidden for those who are allergic to this product and acetyl salicylic acid.
  5. Used with anticoagulants, it can prolong the time of coagulation 

Adverse reaction

  1. Digestive system: anorexia, nausea, abdominal pain, abdominal distention, diarrhea, and constipation.
  2. Nervous system: vertigo, headache, fatigue, insomnia, lethargy, etc.
  3. Others: rare rash, edema, rhinitis, tinnitus, transient visual impairment, etc.

Chemical Properties

White Solid

Uses

Salicylate; non-selective cyclo-oxygenase inhibitor; antipyretic; analgesic; anti- inflammatory.

brand name

Dolobid (Merck).

General Description

Diflunisal (Dolobid), is a longer acting and more potent drugthan aspirin because of its hydrophobic, 2,4-difluorophenylgroup attached to the 5-position of the salicyclic acid. In alarge-scale comparative study with aspirin, it was also bettertolerated with less GI complications than aspirin. It ismarketed in tablet form for treating mild to moderate postoperativepain as well as RA and OA.
Diflunisal is highly protein bound. Its metabolism is subjectto a dose-dependent, saturable, and capacity-limitedglucuronide formation. This unusual pharmacokineticprofile is a result of an enterohepatic circulation and the reabsorptionof 65% of the drug and its glucuronides, followedby cleavage of its unstable, acyl glucuronide back tothe active drug. Thus, diflunisal usage in patients with renalimpairment should be closely monitored.

Safety Profile

Poison by ingestion, subcutaneous, and intraperitoneal routes. Human systemic effects by ingestion: tolerance, and cholestatic jaundce (due to the stoppage of the flow of bile), agranulocytosis, increased body temperature. An experimental teratogen. Other experimental reproductive effects. An analgesic and anti-inflammatory agent. When heated to decomposition it emits toxic fumes of F-. See also FLUORIDES.

Diflunisal Preparation Products And Raw materials

Raw materials

Preparation Products


Diflunisal Suppliers

Global( 127)Suppliers
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