'Diflunisal' is a
genericA generic drug is a drug which isproduced and distributed without patent protection. The generic drug may still have a patent on the formulation but not on the active ingredient....
NSAID (non-steroidal anti-inflammatory drug). It was developed by Merck Sharp & Dohme in 1971 after showing promise in a research project studying more potent chemical analogs of
aspirinAspirin , also known as acetylsalicylic acid , is a salicylate drug, often used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication....
.
It was first sold under the brand name
Dolobid, marketed by
Merck & Co.Merck & Co., Inc. , also known as Merck Sharp & Dohme or MSD outside the USA and Canada, is one of the largest pharmaceutical companies in the world. The headquarters of the company is located in Whitehouse Station, New Jersey, an unincorporated area in Readington Township...
, but generic versions are now widely available. It is available in 250 mg and 500 mg tablets.
Like all NSAIDs, Diflunisal acts by inhibiting the production of
prostaglandinA prostaglandin is any member of a group of lipid compounds that are derived enzymatically from fatty acids and have important functions in the animal body. Every prostaglandin contains 20 carbon atoms, including a 5-carbon ring....
, a hormone which is involved in inflammation and pain.
'Diflunisal' is a
genericA generic drug is a drug which isproduced and distributed without patent protection. The generic drug may still have a patent on the formulation but not on the active ingredient....
NSAID (non-steroidal anti-inflammatory drug). It was developed by Merck Sharp & Dohme in 1971 after showing promise in a research project studying more potent chemical analogs of
aspirinAspirin , also known as acetylsalicylic acid , is a salicylate drug, often used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication....
.
It was first sold under the brand name
Dolobid, marketed by
Merck & Co.Merck & Co., Inc. , also known as Merck Sharp & Dohme or MSD outside the USA and Canada, is one of the largest pharmaceutical companies in the world. The headquarters of the company is located in Whitehouse Station, New Jersey, an unincorporated area in Readington Township...
, but generic versions are now widely available. It is available in 250 mg and 500 mg tablets.
Mechanism
Like all NSAIDs, Diflunisal acts by inhibiting the production of
prostaglandinA prostaglandin is any member of a group of lipid compounds that are derived enzymatically from fatty acids and have important functions in the animal body. Every prostaglandin contains 20 carbon atoms, including a 5-carbon ring....
, a hormone which is involved in inflammation and pain. There is also an
antipyreticAntipyretics are drugs that reduce body temperature in situations such as fever. However, they will not affect the normal body temperature if one does not have a fever....
effect, but this is not a recommended use of the drug. Though diflunisal has an onset of 1 hour, and maximum analgesia at 2 to 3 hours, the diflunisal plasma levels will not be steady until repeated doesages are achieved. The long plasma half-life is a distinctive feature of diflunisal in comparison to similar drugs. To increase the rate at which the diflunisal plasma levels become steady, a loading dose is usually used. It is primarily used to treat symptoms of
arthritisArthritis is a group of conditions involving damage to the joints of the body....
, and for acute pain following oral surgery, especially removal of wisdom teeth.
Side Effects
The inhibition of prostaglandins also has the effect of decreasing the protection given to the stomach from its own acid. Like all NSAIDS, this leads to an increased risk of stomach ulcers, and their complications, with long-term use.
Overdose
Deaths that have occurred from diflunisal usually involved mixed drugs and or extremely high dosage. The oral
LD50In toxicology, the median lethal dose, LD50 , LC50 or LCt50 of a toxic substance or radiation is the dose required to kill half the members of a tested population...
is 500 mg/kg. Symptoms of overdose include coma,
tachycardiaTachycardia comes from the Greek words tachys and kardia . Tachycardia typically refers to a heart rate that exceeds the normal range for a resting heartrate...
, stupor, and vomiting. The lowest dose without the presence of other medicines which caused death was 15 grams. Mixed with other medicines, a death at 7.5 grams has also occurred. Diflunisal usually comes in 250 or 500 mg, thus it is relatively hard to overdose by accident.
Abuse
This medication is unlikely to be abused: it has no effects in common with recreational drugs. However, a few people with psychological disturbances are susceptible to abusing medication of any kind.
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Indicated for:
- Pain, mild-moderate
- Osteoarthritis
- Rheumatoid arthritis
- Injury to tendons
- Inflammation
Do not cut/crush/chew. Monitor blood pressure. Use lowest effective dose for shortest duration. |
| Side effects An adverse drug reaction is an expression that describes harm associated with the use of given medications at a normal dose. The meaning of this expression differs from the meaning of "side effect", as this last expression might also imply that the effects can be beneficial...
:
Cardiovascular:
- Irregular heart beat (!)
- This medication may increase risk of serious and potentially fatal cardiovascular thrombotic events, MI, and stroke (!)
- Risk may increase with duration of use (!)
- Increased risk for Cardiovascular disease history (!)
- Contraindicated for Heart Bypass peri-op pain (!)
EarThe ear is the organ that detects sound. The vertebrate ear shows a common biology from fish to humans, with variations in structure according to order and species. It not only acts as a receiver for sound, but plays a major role in the sense of balance and body position...
, noseAnatomically, a nose is a protuberance in vertebrates that houses the nostrils, or nares, which admit and expel air for respiration in conjunction with the mouth....
, and throatIn anatomy, the throat is the anterior part of the neck, in front of the vertebral column. It consists of the pharynx and larynx. An important feature of the throat is the epiglottis, a flap which separates the esophagus from the trachea and prevents inhalation of food or drink.The throat...
:
EyeEyes are organs that detect light, and send electrical impulses along the optic nerve to the visual and other areas of the brain. Complex optical systems with resolving power have come in ten fundamentally different forms, and 96% of animal species possess a complex optical system...
:
Gastrointestinal:
- Increased risk of serious GI adverse events including bleeding, ulceration, and stomach or intestine perforation which can be fatal: may occur at any time during use and without warning. Elderly at greater risk for serious GI events (!)
- Abdominal pain and cramps
- Constipation
- Gas & Flatulence
- Diarrhea
- Nausea & Vomiting
- Dyspepsia
Central Nervous SystemThe central nervous system is the part of the nervous system that functions to coordinate the activity of all parts of the bodies of bilaterian animals—that is, all animals more advanced than sponges or jellyfish. In vertebrates, the central nervous system is enclosed in the meninges. It contains...
:
- Drowsiness
- Dizziness
- Headache
- Insomnia
- Fatigue
- Somnolence
Psychiatric:
SkinThe skin is the outer covering of the body. In humans, it is the largest organ of the integumentary system made up of multiple layers of mesodermal tissue, and guards the underlying muscles, bones, ligaments and internal organs. Skin of a different nature exists in amphibians, reptiles, birds...
:
- Swelling of the feet, ankles, lower legs, and hands (!)
- Yellowing of skin (!)
- Rash
- Ecchymosis
ContraindicationIn medicine, a contraindication is a condition or factor that increases the risks involved in using a particular drug, carrying out a medical procedure, or engaging in a particular activity....
s:
- Hypersensitivity to aspirin/NSAID-induced asthma or urticaria
- Aspirin triad
- Pregnancy 3rd trimester
- CABG surgery (peri-op pain)
CautionCaution may refer to:* A precautionary statement describing a potential hazard* police caution, an alternative to prosecution for a criminal offence in some countries such as the United Kingdom and Australia...
s:
- Cardiovascular disease
- Cardiac risk factors
- Hypertension
- Congestive Heart Failure
- Elderly or debilitated
- Impaired liver function
- Impaired kidney function
- Dehydration
- Fluid retention
- GI bleed history/PUD
- Asthma
- Coagulopathy
- Smoker
- Corticosteriod use
- Anticoagulant use
- Alcohol use
- Diuretic use
- ACE Inhibitor use
Precautions:
- If symptoms labeled, (!), appear, stop usage immediately and contact your doctor.
- Overdose is possible and deaths have occurred.
- Do not take while on other pain medications.
- Do not take while pregnant or breast feeding.
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