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Profiles of Drug Substances,... 2020A comprehensive profile of piroxicam including the nomenclatures, formulae, elemental composition, appearance, uses and applications. The methods which were utilized for...
A comprehensive profile of piroxicam including the nomenclatures, formulae, elemental composition, appearance, uses and applications. The methods which were utilized for the preparation of the drug substance and their respective schemes are outlined. The physical characteristics of the drug including the ionization constant, solubility, x-ray powder diffraction pattern, differential scanning calorimetry, thermal behavior and spectroscopic studies are described. The methods which were used for the analysis of the drug substance in bulk drug and/or in pharmaceutical formulations including the compendial, spectrophotometric, electrochemical and the chromatographic methods are reported. The stability, toxicity, pharmacokinetics, bioavailability, drug evaluation, comparison, in addition to compiled reviews on the drug substance are involved. Finally, more than four hundred and fifty references are listed at the end of this profile.
Topics: Biological Availability; Drug Compounding; Drug Stability; Piroxicam; Solubility; X-Ray Diffraction
PubMed: 32164968
DOI: 10.1016/bs.podrm.2019.10.007 -
Central Nervous System Agents in... 2017The use of central nervous system (CNS) acting drugs in the management of neuro degenerative and psychiatric problems cannot be overemphasized. Therefore, the chemical... (Review)
Review
BACKGROUND
The use of central nervous system (CNS) acting drugs in the management of neuro degenerative and psychiatric problems cannot be overemphasized. Therefore, the chemical structure of piroxicam can be modified to yield new CNS stimulants and depressants that can be of great benefit to man and animals.
METHODOLOGY
Acetylcholine has Methyl - Oxygen-Oxygen (M-O-O) and Nitrogen (N) functional groups which are structurally related to Sulphur-Oxygen-Oxygen (S-O-O) and Nitrogen (N) of piroxicam that are either methylated or hydrogenated. Each arecoline and nicotine has M-O-O in addition to methylated nitrogen and pyridine ring respectively, making them structurally related to piroxicam. Therefore, when Sulphur of piroxicam is replaced by methyl group, it may likely have muscarinic effects expressed by glandular secretion, gut sedation and vasodepression. Whereas the nitrogen group may be responsible for cholinergic effect in gaglia and striated muscle. Because of the carboxylic functional group (COOH), piroxicam may display depressant effect. Hence C = O, C = N and C = C in piroxicam may change due to biofield treatement.
CONCLUSION
The conversion of piroxicam to central nervous system (CNS) acting drugs may be by desulphation, methylation, dehydrogenation, carboxylation and carbonylation. The would-be synthesized CNS drugs from piroxicam, should have low molecular weight, lipid solubility and low PH.
Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Central Nervous System Agents; Humans; Nervous System Diseases; Piroxicam; Structure-Activity Relationship
PubMed: 27439371
DOI: 10.2174/1871524916666160719102335 -
Central Nervous System Agents in... 2017Piroxicam has been reported to be convertible to Central Nervous System (CNS) acting agents. It has serious depressant effects at high doses. (Review)
Review
BACKGROUND
Piroxicam has been reported to be convertible to Central Nervous System (CNS) acting agents. It has serious depressant effects at high doses.
OBJECTIVE
In view of this, structures of piroxicam metabolites were assessed for possible conversion to CNS depressants.
METHODS
Literature search was carried out with intent to identifying piroxicam metabolites and the possibility of converting them to CNS acting depressants.
RESULTS
Piroxicam is convertible to hydroxymethylated metabolite which may be converted to barbiturates such as thiopentone and thiamylal. Whereas cyclodehydrated metabolite may be converted to acetylcyclodehydrated compound that may be in turn converted to acetylacetone and cyclohexamide. However, carboxybenzothiazine metabolite may be converted to carboxamide compound, benzolactone which is convertible to phenazone. Carboxybenzothiazine is also convertible to 2-aminopyridine mepyramine and triplenamine. Conversion of carboxybenzothiazine to gamma aminobutyric acid and phenothiazines such as chlorpromazine, thioridazine, fluphenazine and perphenazine is highly possible.
CONCLUSION
Structurally, barbituric compounds, carboxamide, cyclodehydrated, benzothiazine and carboxybenzothiazine metabolites may act via dopamine and adrenergic receptors causing depression of CNS activities. Piroxicam metabolites may also act via histamine, melatonin and potassium channel receptors causing CNS depression.
Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Central Nervous System Depressants; Depression; Humans; Piroxicam
PubMed: 27834137
DOI: 10.2174/1871524917666161111093759 -
Molecules (Basel, Switzerland) Apr 2021Piroxicam (PRX) is a commonly prescribed nonsteroidal anti-inflammatory drug. Its efficacy, however, is partially limited by its low water solubility. In recent years,...
Piroxicam (PRX) is a commonly prescribed nonsteroidal anti-inflammatory drug. Its efficacy, however, is partially limited by its low water solubility. In recent years, different studies have tackled this problem and have suggested delivering PRX through solid dispersions. All these strategies, however, involve the use of potentially harmful solvents for the loading procedure. Since piroxicam is soluble in supercritical CO (scCO), the present study aims, for the first time, to adsorb PRX onto mesoporous silica using scCO, which is known to be a safer and greener technique compared to the organic solvent-based ones. For comparison, PRX is also loaded by adsorption from solution and incipient wetness impregnation using ethanol as solvent. Two different commercial mesoporous silicas are used (SBA-15 and Grace Syloid XDP), which differ in porosity order and surface silanol population. Physico-chemical analyses show that the most promising results are obtained through scCO, which yields the amorphization of PRX, whereas some crystallization occurs in the case of adsorption from solution and IWI. The highest loading of PRX by scCO is obtained in SBA-15 (15 wt.%), where molecule distribution appears homogeneous, with very limited pore blocking.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Ethanol; Humans; Inflammation; Piroxicam; Silicon Dioxide; Solubility; Water
PubMed: 33922927
DOI: 10.3390/molecules26092500 -
Drug Intelligence & Clinical Pharmacy Dec 1988
Topics: Aged; Agranulocytosis; Arthritis; Female; Humans; Piroxicam
PubMed: 3243167
DOI: 10.1177/106002808802201216 -
Journal of the American Academy of... Dec 1986Eleven patients had piroxicam-induced photosensitivity when first seen. Six were photopatch-tested to piroxicam (2%, 5%, 20% concentrations); all tests were positive....
Eleven patients had piroxicam-induced photosensitivity when first seen. Six were photopatch-tested to piroxicam (2%, 5%, 20% concentrations); all tests were positive. This same group were patch test-positive to thimerosal. Three of the eleven patients became persistent light reactors. Two additional patients developed persistent hand dermatitis.
Topics: Adult; Aged; Aged, 80 and over; Arthritis, Rheumatoid; Drug Eruptions; Female; Humans; Male; Middle Aged; Osteoarthritis; Patch Tests; Photosensitivity Disorders; Piroxicam
PubMed: 2948973
DOI: 10.1016/s0190-9622(86)70296-x -
Acta Obstetricia Et Gynecologica... 1986Piroxicam, a potent inhibitor of prostaglandins, is effective and well-tolerated in the treatment of primary dysmenorrhea. A single 40 mg dose has been shown to rapidly... (Review)
Review
Piroxicam, a potent inhibitor of prostaglandins, is effective and well-tolerated in the treatment of primary dysmenorrhea. A single 40 mg dose has been shown to rapidly reduce the uterine hypercontractility of primary dysmenorrhea. In clinical trials vs placebo, piroxicam in a dose of 40 mg once daily for two days followed by 20 mg once daily thereafter demonstrated superior efficacy. In more than 1,400 piroxicam-treated menstrual cycles and more than 200 placebo-controlled cycles, a similar incidence of side effects-7% and 8.4% respectively-was observed.
Topics: Dysmenorrhea; Female; Humans; Piroxicam
PubMed: 3548205
DOI: 10.3109/00016348509157060 -
Die Pharmazie May 2015Piroxicam is a potent, nonsteroidal, anti-inflammatory agent (NSAID) which also exhibits antipyretic activity. The antiviral effect of piroxicam against herpes simplex...
Piroxicam is a potent, nonsteroidal, anti-inflammatory agent (NSAID) which also exhibits antipyretic activity. The antiviral effect of piroxicam against herpes simplex virus type 1 (HSV-1) was examined in vitro on RC-37 monkey kidney cells using a plaque reduction assay. Piroxicam was dissolved in ethanol or dimethylsulfoxide (DMSO) and the 50% inhibitory concentration (IC50) was determined at 4 μg/ml and 75 μg/ml, respectively. The IC50 for the standard antiherpetic drug acyclovir was determined at 1.6 μM. At non-cytotoxic concentrations of these piroxicam solutions, plaque formation was significantly reduced by 62.4% for ethanolic piroxicam and 72.8% for piroxicam in DMSO. The mode of antiviral action of these drugs was assessed by time-on-addition assays. No antiviral effect was observed when cells were incubated with piroxicam prior to infection with HSV-1 or when HSV-1 infected cells were treated with dissolved piroxicam. Herpesvirus infection was, however, significantly inhibited when HSV-1 was incubated with piroxicam prior to the infection of cells. These results indicate that piroxicam affected the virus before adsorption, but not after penetration into the host cell, suggesting that piroxicam exerts a direct antiviral effect on HSV-1. Free herpesvirus was sensitive to piroxicam in a concentration-dependent manner and the inhibition of HSV-1 appears to occur before entering the cell but not after penetration of the virus into the cell. Considering the lipophilic nature of piroxicam, which enables it to penetrate the skin, it might be suitable for topical treatment of herpetic infections.
Topics: Acyclovir; Animals; Antiviral Agents; Cell Line; Cell Survival; Chlorocebus aethiops; Herpes Simplex; Herpesvirus 1, Human; Piroxicam; Viral Plaque Assay
PubMed: 26062303
DOI: No ID Found -
The British Journal of Clinical Practice Apr 1988
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European Journal of Rheumatology and... 1987Patient acceptance of medications often depends upon individual and cultural preferences for particular dosage forms. A variety of dosage forms also provides the patient... (Clinical Trial)
Clinical Trial
Patient acceptance of medications often depends upon individual and cultural preferences for particular dosage forms. A variety of dosage forms also provides the patient and the physician with greater convenience and flexibility. Thus, multiple formulations increase the clinical utility of a drug. In addition to the capsule, dosage forms of piroxicam now available or in an advanced stage of clinical development include a suppository, dispersible tablet, topical gel, and parenteral formulation. (Ed.: The parenteral and topical formulations were launched after the symposium was held, and are now available). The piroxicam suppository offers an alternative to the oral route of administration. Pharmacokinetic studies demonstrate that the 20-mg suppository is bioequivalent to the 20-mg capsule, and clinical studies have shown that it is equal to the capsule in efficacy and toleration. Piroxicam is the only non-steroidal anti-inflammatory drug (NSAID) that is available as a dispersible tablet. This dosage form is also well tolerated by patients and equally effective as the capsule. Intramuscular administration of piroxicam is in development. All these dosage forms offer the convenience of once-a day administration. Piroxicam topical gel (0.5%) has been demonstrated to have anti-inflammatory activity in several animal models. In double-blind clinical trials involving patients with osteoarthritis of the knee, the topical gel was found to be significantly more effective than placebo and well tolerated.
Topics: Administration, Topical; Animals; Arthritis; Clinical Trials as Topic; Dogs; Gels; Humans; Injections, Intramuscular; Piroxicam; Suppositories; Tablets
PubMed: 3305038
DOI: No ID Found