Lysine aspirin

Aspirin desensitization is useful in diseases where low-level antiplatelet action is needed and in the care of patients with aspirin sensitivity and intractable nasal polyps. Lysine aspirin availability in Europe allows desensitization by inhalation at... 

In the third stndy, 27 patients with stable chronic asthma in whom inhalation of lysine aspirin cansed a 20% fall in FEVi were challenged with increasing doses of oral cele-coxib (from 10 to 200 mg/day) they do not develop bronch-oconstriction or other extrapulmonary reactions (68). 

Jang AS. Severe reaction to lysine aspirin. Allergy 2000 55(ll) 1092-3. 

Diagnosis of aspirin-induced asthma requires a detailed medical history. The definitive diagnosis is made by aspirin provocation tests, which may be done via different routes. An oral provocation test is used commonly where threshold doses of aspirin induce a positive reaction measured by a drop in forced expiratory volume in 1 second (FEVi) and/or the presence of symptoms. A nasal provocation test is done by the application of one dose of lysine-aspirin, and aspirin sensitivity is manifested with clinical symptoms of watery discharge and a significant fall in inspiratory nasal flow. When lysine-aspirin bronchoprovocation was compared with oral aspirin provocation, both methods were equally sensitive. ... 

Aspirin and oral salicylates Aloxiprin, Aspirin, Benorilate, Choline salicylate, Diflunisal, Etheniamide, Lysine aspirin. Magnesium salicylate, Salsalate, Sodium salicylate... 

A study in 11 patients with chronic heart failure found that both aspirin 75 mg daily and aspirin 300 mg daily for 14 days reduced the venodilatory effects produced by a single 20-mg intravenous dose of furosemide (as measured by the forearm venous capacitance). Six patients with cirrhosis and ascites had a reduced diuretic response to intravenous furosemide 40 mg when a single 450-mg dose of lysine aspirin was given before the injection. ... 

No clinically significant pharmacokinetic interaction appears to occur between aspirin, lysine aspirin and sodium salicylate and lithium. 

No change in serum lithium levels was seen in 7 patients taking lithium when they were given aspirin 975 mg four times daily for 6 days. Another report states that aspirin 600 mg four times daily had no effect on the absorption or renal excretion of single doses of lithium carbonate given to 6 healthy subjects. Further reports describe no change in serum lithium levels with lysine aspirin, intravenous aspirin, or intravenous sodium salicylate. However, lithium clearance was slightly reduced by 22% by intravenous sodium salicylate, and a study in one healthy subject found a 32% increase in mean serum-lithium levels from 0.41 to 0.54 mmol/L after 5 days of oral aspirin treatment (975 mg four times daily for 2 days, then 650 mg four times daily for 3 days). ... 

D Alka-Seltzer (Bayer) Aspirin (Bayer 1899) Aspisol (Bayer as dl-lysine salt)... 

The hydrolysis of acetylsalicylic acid (aspirin) has also been described, and it involves the rapid acetylation of Lys199 [123], This reactive site also involves Trp214 and has been called the U-site [124], Drugs that inhibit the hydrolysis of substituted acetylsalicylic acids by HSA and decrease the fluorescence intensity of Trp214 are referred to as U-type drugs (e.g., sulfinpyrazone and warfarin). Because U-type drugs also bind to the site know as site I (which overlaps with subdomain IIA), the U-site and I-site are believed to overlap. Lysine residues also appear to be involved in the /3-lactamase activity of HSA [125],... 

Aspirin (acetylsalicylic acid, Figure 7.9) is a derivative of salicyclic acid, which was first used in 1875 as an antipyretic and antirheumatic. The usual dose for mild pain is 300-600 mg orally. In the treatment of rheumatic diseases, larger doses, 5-8 g daily, are often required. Aspirin is rapidly hydrolysed in the plasma, liver and eiythrocytes to salicylate, which is responsible for some, but not all, of the analgesic activity. Both aspirin and salicylate are excreted in the urine. Excretion is facilitated by alkalinisation of the urine. Metabolism is normally very rapid, but the liver enzymes responsible for metabolism are easily saturated and after multiple doses the terminal half-life may increase from the normal 2-3 h to 10 h. A soluble salt, lysine acetylsalicylic acid, with similar pharmacological properties to aspirin, has been used by parenteral administration for postoperative pain. Aspirin in low doses (80-160 mg daily) is widely used in patients with cardiovascular disease to reduce the incidence of myocardial infarction and strokes. The prophylaxis against thromboembolic disease by low-dose aspirin is due to inhibition of COX-1-generated thromboxane A2 production. Because platelets do not form new enzymes, and COX-1 is irreversibly inhibited by aspirin, inhibition of platelet function lasts for the lifetime of a platelet (8-10 days). 

Garagiola, U., Dacatra, U., Braconaro, F., Porretti, E., Pisetti, A., and Azzolini, V. lontophoretic administration of pirprofen or lysine soluble aspirin in the treatment of rheumatic diseases. Clin. Ther. 70 553, 1988. 

Aarons L, Hopkins K, Rowland M, Brossel S, Thiercelin JF. Route of administration and sex differences in the pharmacokinetics of aspirin, administered as its lysine salt. Pharm Res 1989 6 660-6. 

Lysine acetylsalicylate is a soluble form of salicylate developed for intravenous administration in acute pain. Its mode of action and scope of adverse effects are similar to those of aspirin (1), although it has a faster onset of action (2) and causes less gastrointestinal bleeding (3). 

Majluf-Cruz A, Chavez-Ochoa AR, Majluf-Cruz K, Coria-Ramirez E, Pineda Del AguUa I, Trevino-Perez S, Matias-Aguilar L, Lopez-Armenia JC, Corona de la Pena N. Effect of combined administration of clopidogrel and lysine acetylsalicylate versus clopidogrel and aspirin on platelet aggregation and activated GPIIb/IIIa expression in healthy volunteers. Platelets 2006 17(2) 105-7. 

Gurfinkel EP, Altman R, Scazziota A, HeguUen R, Mautner B. Fast Platelet suppression by lysine acetylsahcy-late in chronic stable coronary patients. Potential chnical impact over regular aspirin for coronary syndromes. Chn Cardiol 2000 23(9) 697-700. 

Other natural sources of salicylates are listed in Table 1. There are separate monographs on acetylsali-cylic acid (aspirin), benorilate, diflunisal, lysine acetyl-salicylate, and salsalate. Methyl salicylate is covered under Gaultheria procumbens in the monograph on the Ericaceae. 

The analgesic efficacy of tramadol can be further enhanced by adding injectable lysine acetyl salicylate (aspirin) after orthopedic surgery with no significant increase in adverse effects (26). 

BOX 26.1 The water-soluble d, L-lysine salt of aspirine a success story based on luck and serendipity... 

With the objective of preparing water-soluble salts of aspirin (which is known to be badly soluble in water and anyway rapidly hydrolyzed), the chemists of TEquilibre Biologique prepared and patented some aspirin salts of the basic amino-acids lysine and arginine which were provided by AEC (French patent 1 295 304, May 7th, 1956). The salts proved to be water-soluble, but the laboratory procedure used for their preparation yielded slightly hygroscopic salts which partly decomposed to acetic acid and free salicylic acid. The industrial development was therefore precluded for some years. 

The combination of a modified preparation procedure yielding a very anhydrous lyophilized salt (French Demande 2 115 060, August 11, 1972) on one hand, and working under controlled atmosphere on the other hand, allowed the industrial production of the racemic lysine salt. This compound is a white crystalline powder which is freely soluble in water, odorless and tasteless. It allowed for the first time to prepare injectable preparations of aspirin. 

A number of new copper complexes have also been found to have antiinflammatory activity. Copper(II)(j8-oxo-2-thiophenepropionitrile) is effective in treating rat polyarthritis [175]. The copper complex of glycyl-L-histidyl-L-lysine, Cu(II)(GHL), is claimed to have anti-inflammatory activity and increase the rate of wound healing [176, 177] consistent with earlier reports of increased gastric wound healing rates associated with Cu(II)(aspirinate)4 and Cu(II)(tryptophanate)2 treatment [178]. Copper(II)(L-histidinate)2, Cu(II)-... 

A study in patients about to undergo surgery found that pretreatment with aspirin 1 g (given as intravenous lysine acetylsalicylate) one minute before induetion redueed the dosage of thiopental by 34%, from 5.3 to 3.5 mg/kg. Initially thiopental 2 mg/kg was given followed by increments of 25 mg until the eyelash reflex was abolished. The same study also found that oral probenecid 1 g given one hour before anaesthesia reduced the thiopental dosage by 23%, from 5.3 to 4.1 mg/kg. 

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