proquazone

Action and Spectrum

Actions and Spectrum: 

Actions: 

Proquazon is a non-steroidal anti-inflammatory drug that has been investigated for use in treating osteoarthritis and rheumatoid arthritis. Proquazon’s molecular mode of action involves blocking the synthesis of proteoglycan core proteins and glucosamine secondary biosynthesis. 

Spectrum: 

Unlike the majority of other non-steroidal anti-inflammatory drugs (NSAIDs), proquazone does not contain a free acid group in its structural makeup. It is recommended for use in the treatment of musculoskeletal disorders, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute inflammatory problems, and acute pain states such as dysmenorrhea, headache, and postoperative pain.

Drug Interaction

Adverse Reaction

Frequency defined 

Diarrhea (>30%) 

Black Box Warning

N/A

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Peptic ulcer 
• Allergic to NSAIDS 

Cautions 

• Renal impairment 
• GI disorders 
• 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: 

Thus far, clinical investigations have indicated that proquazone, at dosages of roughly 900 mg/day, causes a high rate of gastrointestinal problems, including diarrhea (30% of patients). Proquazone’s overall tolerability was determined to be equivalent compared with that of other NSAIDs examined in the majority of comparative studies, despite the fact that these effects were often low to moderate in severity and temporary in nature.

Proquazone did not cause a higher rate of therapy withdrawal because of adverse reactions than the other NSAIDs that were examined. Proquazone dosages as low as 300 to 450 mg/day appear to retain efficacy while significantly enhancing tolerability, according to preliminary experience. 

Therefore, proquazone appears to be as potent as other NSAIDs for treating osteoarthritis and rheumatoid arthritis as of right now. To completely assess the effectiveness and tolerance of this drug, particularly at the reduced daily dosages now advised, more research is necessary. Additionally, it is unclear whether this agent actually has considerable “disease-modifying” potential. 

Pharmacodynamics: 

In a number of animal model studies of chronic and acute illnesses, proquazone, a non-steroidal anti-inflammatory medication (NSAID) with antipyretic and analgesic qualities, shows anti-inflammatory benefits. In experiments involving carrageenin-induced paw edema and adjuvant-induced arthritis, its potency is comparable to diclofenac but less than indomethacin. In both animal and human pain models, proquazone has demonstrated efficacy similar to or exceeding that of indomethacin and other NSAIDs designed for ‘non-narcotic-type’ analgesia. Notably, in human trials, a single dose of proquazone 600mg was found to be a more effective analgesic compared to phenylbutazone 400mg, naproxen 500mg, diclofenac 100mg, and marginally superior to indomethacin 100mg. 

Proquazone is a potent inhibitor of prostaglandin production, showing activity similar to that of diclofenac and indomethacin and more significant than that of naproxen, according to both in vivo and in vitro investigations. Additionally, it inhibits platelet aggregation induced by collagen, arachidonic acid, and ADP. Preliminary findings in patients with rheumatoid arthritis indicate that daily doses of proquazone ranging from 600 to 900 mg may impact synovial fluid concentrations by increasing complement components (C3 and C4) and reducing the levels of immunoglobulins IgG, IgM, and IgA, suggesting an immunological mechanism. However, in various animal models, proquazone, akin to indomethacin and phenylbutazone, did not influence cell-mediated or humoral immune mechanisms. While animal studies generally suggest that proquazone has a lower ulcerogenic potential compared to other NSAIDs, a study involving healthy volunteers showed that proquazone (600 and 900 mg/day) and aspirin (3600 mg/day) produced a similar extent of fecal blood loss. 

Pharmacokinetics: 

Absorption 

The bioavailability is 7% 

The time to reach peak plasma levels: 1.5 hours 

Distribution 

Protein binding: > 98% 

The volume of distribution is 0.52 L/kg 

Metabolism 

Via Liver 

Elimination and Excretion 

The half-life is 1.27 hours 

The major portion of the drug and its metabolites are excreted from the body within the first 24 hours by a mix of biliary (30 - 43%) and urine (46 - 51%) excretion.

Adminstartion

Administration: 

Proquazone is administered orally, and the typical dose varies depending on the condition being treated. For the relief of pain and inflammation in conditions like rheumatoid arthritis, the usual dosage is determined based on individual patient needs but often falls between 600 and 900 mg per day.

It’s crucial to follow the prescribed administration and dosage guidelines provided by healthcare professionals to ensure higher therapeutic benefits while reducing the chances of potential adverse effects associated with the medication. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: proquazone 

Pronounced: pro-KWAY-zone 

Why do we use proquazone? 

The typical dosage of Proquazone consistently provided clinically significant pain relief, enhanced grip strength, and decreased the number of affected joints in placebo-controlled trials involving patients with rheumatoid arthritis. In comparative studies, the standard dose of Proquazone demonstrated efficacy comparable to that of NSAIDs such as aspirin, diclofenac, indomethacin, ibuprofen, and naproxen in individuals with rheumatoid arthritis. Initial findings from long-term trials (lasting 12 months or more) suggest that the usual dose of Proquazone sustains its effectiveness and may potentially halt the progression of bone erosions. However, this promising result requires confirmation through well-controlled trials involving a larger patient population.