imidazole salicylate

Action and Spectrum

Actions and Spectrum: 

Actions: 

The non-steroidal anti-inflammatory medication imidazole salicylate has a restricted ability to block prostaglandin production. 

Spectrum: 

Using a chemiluminescence (CL) experiment, the effects of IS (imidazole salicylate), an organic salt made from imidazole and salicylic acid, on polymorphonuclear leukocytes’ (PMNs’) respiratory burst were investigated. The study evaluated the effects of 1 to 4 μg/ml of IS on the lucigenin- and luminol-amplified CL reactions of PMNs, which were induced by either phorbol myristate acetate (PMA) or N-formyl-methionyl-leucyl-phenylalanine (FMLP).

While PMA-stimulated PMNs did not exhibit any discernible effects, the luminol-amplified CL reaction of PMNs triggered with FMLP demonstrated a significant decrease in the presence of IS. Furthermore, IS dramatically reduced the lucigenin-amplified CL reaction of PMA-stimulated PMNs.

Furthermore, in the presence of IS, the xanthine/xanthine oxidase system’s CL response was completely eliminated. These results suggest that IS acts as a superoxide anion scavenger and may influence PMN respiratory burst-mediated interactions with the plasma membrane. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Tremor 

Increased output of urine 

Edema 

Hypotension 

Hypersensitivity reactions 

Raised LFTs 

Angina 

Headache 

MI 

Flushing 

Fatigue 

Nausea 

Dizziness 

Diarrhea 

Paresthesia 

Bloating 

Respiratory disorders 

Myalgia 

Gingival hyperplasia 

Changes in the CBP 

Irritability 

Drowsiness 

Tachycardia 

Asthenia 

Palpitation 

Black Box Warning

Black Box Warning: 

 N/A 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Unstable angina 
• Pregnancy 
• Lactation 

Cautions 

• Renal impairment 
• Hepatic impairment 
• Drug interactions 
• Pregnancy  
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the administration of the drug during pregnancy. 

Breastfeeding warnings:  

No data is available regarding the excretion of drug in breast milk. 

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

ITF-182, also known as imidazole salicylate, is a nonsteroidal anti-inflammatory medication (NSAID) with modest inhibition on prostaglandin production and an inhibitory effect on Tromboxane A2 synthesis without interfering with the cyclo-oxygenase pathway. Treatment options for musculoskeletal injuries and osteoarthrosis include imidazole salicylate.

Furthermore, there is no chance that it will prevent renal prostaglandin synthesis when administered to individuals with decompensated cirrhosis. Good stomach tolerability made imidazole salicylate a suitable therapeutic option for rheumatic disorders in the elderly. Patients who are sensitive to aspirin can also safely use this medication. 

Pharmacodynamics: 

Thirty-seven orthopedists and traumatologists participated in a postmarketing survey with 700 patients of both sexes, ages ranging from 7 to 87. Evaluating imidazole salicylate’s efficacy and tolerance was the goal.

Among the participants, 233 patients with traumatic pathologies were given imidazole salicylate tablets (twice to thrice daily), gel (twice to thrice daily) for ten days, or a combination of both gel and tablets. Four hundred sixty-seven individuals with osteoarthritis received 750 mg tablets (thrice daily) for a maximum of one month. 

Both groups saw acceptable results from the treatment, which improved joint function and markedly decreased the level of pain and edoema. Notably, only a small number of GI side effects (with an incidence of less than 1%) were recorded; no hitherto undisclosed adverse events were found. 

Pharmacokinetics: 

Absorption 

Imidazole (single dosage) produced values of 138% according to the relative bioavailability assessments, while multiple dosing (final dose) produced values of 113%. For salicylic acid, the equivalent values were 128% for multiple doses (final dose) and 148% for a single dose. These results shed light on the degree of salicylic acid and imidazole protein binding, as well as differences in the relative bioavailability of each compound at various dosage levels. 

Distribution 

Salicylic acid showed a higher binding capability, about 80-85%, while imidazole showed a range of 5-15% for protein binding.  

Metabolism 

It is metabolized in the liver and expelled together with its byproducts, which are mainly urine. 

Elimination and Excretion 

For imidazole (oral administration), the t1/2 beta was found at 2.98 +/- 1.13 h for a single dose and 1.86 +/- 0.78 h for a multiple-dose (final dose); for salicylic acid, the t1/2 beta was found at 6.46 +/- 3.79 h for a single dose and 6.40 +/- 3.36 h for a multiple-dose (last dose). 

Adminstartion

Administration: 

The administration of imidazole salicylate varies according to the patient’s health. For traumatic diseases, the gel may be applied twice to three times daily for ten days, tablets may be taken at the same frequency, or a mix of gel and tablets may be utilized. For osteoarthritis, 750 mg tablets are commonly administered three times daily for up to one month.

The administration seeks to enhance joint function and reduce discomfort and edoema. The absence of precise information regarding the duration and dosage highlights the need for medical supervision in order to customize the treatment to meet the needs of each patient. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: imidazole salicylate 

Pronounced: ih-MID-uh-zohl sal-i-si-late 

Why do we use imidazole salicylate? 

Because of its anti-inflammatory qualities, imidazole salicylate is frequently used to treat a variety of illnesses, including fever, inflammatory respiratory tract diseases, and otorhinolaryngeal disorders. Since it is a non-steroidal anti-inflammatory medicine (NSAID), its ability to reduce prostaglandin formation is somewhat limited.

Its effectiveness and tolerability in a variety of patient populations, including those with osteoarthritis and traumatic pathologies, have been examined in clinical studies and surveys.

The findings show positive results, such as a notable decrease in the severity of pain and edoema and an increase in joint function. Since imidazole salicylate does not impede renal responsiveness to furosemide or kidney prostaglandin formation, it is thought to be appropriate for people with decompensated cirrhosis.