Cetirizine Research Articles

The Role of Cetirizine in the Changing Landscape of IV Antihistamines: A Narrative Review.

Since 1955, the only available H1 antihistamines for intravenous administration have been first-generation formulations and, of those, only intravenously administered (IV) diphenhydramine is still approved in the USA. Orally administered cetirizine hydrochloride, a second-generation H1 antihistamine, has been safely used over-the-counter for many years. In 2019, IV cetirizine was approved for the treatment of acute urticaria. In light of this approval, this narrative review discusses the changing landscape of IV antihistamines for the treatment of histamine-mediated conditions. Specifically, IV antihistamines will be discussed as a treatment option for acute urticaria and angioedema, as premedication to prevent infusion reactions related to anticancer agents and other biologics, and as an adjunct treatment for anaphylaxis and other allergic reactions. Before the development of IV cetirizine, randomized controlled trials of IV antihistamines for these indications were lacking. Three randomized controlled trials have been conducted with IV cetirizine versus IV diphenhydramine in the ambulatory care setting. A phase 3 trial of IV cetirizine 10 mg versus IV diphenhydramine 50 mg was conducted in 262 adults who presented to the urgent care/emergency department with acute urticaria requiring antihistamines. For the primary efficacy endpoint, defined as change from baseline in a 2-h patient-rated pruritus score, non-inferiority of IV cetirizine to IV diphenhydramine was demonstrated (score − 1.6 vs − 1.5, respectively; 95% CI − 0.1, 0.3). Compared with IV diphenhydramine, IV cetirizine demonstrated fewer adverse effects including less sedation, a significantly shorter length of stay in the treatment center, and fewer returns to the treatment center at 24 and 48 h. Similar findings were demonstrated in another phase 2 acute urticaria trial and in a phase 2 trial assessing IV cetirizine for pretreatment for infusion reactions in the oncology/immunology setting. IV cetirizine is associated with similar patient outcomes, fewer adverse effects, and increased treatment center efficiency than IV diphenhydramine.

Utilization of amphiphilic antihistamines drugs to enhance micellization of anionic surfactant and improve the binding and solubility of Itraconazole drug

Many salt-based medicines are used in pharmaceutical formulations as active components. Excipients performance can be improved by using these medicines. The use of amphiphilic antihistamine medications (diphenhydramine hydrochloride (DPC) and cetirizine hydrochloride (CTZ)) to improve sodium dodecylbenzene sulfonate (SDBS) micellization is demonstrated in this work. DPC/CTZ considerably lowered the critical micelle concentration (CMC) of SDBS in aqueous media by measuring conductivity. SDBS micelles demonstrated a greater electrostatic interaction with CTZ than DPC micelles, based on counterion binding (βc and B) and binding constant (Kb) values. The DPC/CTZ mean ion occupancy (i0) per SDBS micelle was also calculated using the UV spectroscopy experiment. For SDBS micelles, we observed that DPC and CTZ had i0 values of 1.700 and 2.622, respectively. The electrostatic interaction between the medication and the surfactants was shown to be controlling the i0 levels. The medicine Itraconazole (ITZ), which is poorly water-soluble, was found to be more soluble in SDBS micelles containing CTZ than in DPC combinations. At 0.002 mol L-1 in the aqueous medium, the greatest i0 values of ITZ were 185 in SDBS + DPC and 203 in SDBS + CTZ. The CMC and the binding behaviour of drug-micelles were found to be critical determinants in controlling ITZ drug solubilization. Finally, we concluded that the above formulation might be used in the pharmaceutical industry to improve multi-drug delivery systems.

Carbamazepine removal from aqueous solution by synthesized reduced graphene oxide-nano zero valent iron (Fe0-rGO) composite: theory, process optimization, and coexisting drugs effects.

Synthesized Fe0-rGO nanocomposite with ratio of 1/1 (w/w) was prepared and has been used as adsorbent for the removal of Carbamazepine (CBZ) from aqueous solution. The adsorbent was characterized by various techniques such as Fourier-transform infrared spectroscopy (FTIR), energy-dispersive X-ray spectroscopy (EDX), X-ray diffraction (XRD), and Field Emission Scanning Electron Microscopy (FE-SEM) analyses. Linear experiments were performed to compare the best fitting isotherms and kinetics. The Freundlich isotherm (R2>0.90) and pseudo second order kinetic (R2>0.99) fitted well the experimental data. On the basis of the Langmuir isotherm, the maximum adsorption capacity of Fe0-rGO for CBZ was up to 50 mg g-1 at 30 °C. The pH, adsorbent dose, and initial concentration of CBZ were observed to be the leading parameters that affected the removal of CBZ considering the analysis of variance (ANOVA; p<0.05). The optimum process value of variables obtained by numerical optimization corresponds to pH 3.07, an adsorbent dose of 36.2 mg, an initial CBZ concentration of 5 mg L-1 and at 30.15 °C. The results of optimum conditions reveal that a maximum of 94% removal efficiency can be achieved; whereas, this phenomenon was independent of temperature (p-value>0.05). Moreover, Fe0-rGO can be used to remove diclofenac (DIC) and cetirizine (CTZ) simultaneously. To sum up, the Fe0-rGO is a promising adsorbent not only for the efficient removal of CBZ but also for the reduction of coexisting drugs in aqueous solution.

Eczema Herpeticum in an Infant

A 3-month-old otherwise healthy girl with known eczema presented to the Department of Pediatrics with acute onset of a facial rash and fever of 39 °C. On examination, the infant was systemically well and stable hemodynamically. She had confluent areas of skin crusting and weeping over the entire face, with disseminated monomorphic, umbilicated, vesiculopapular lesions (Figure 1, A). Facial edema and cervical lymphadenopathy were also present. Despite therapy with oral cefaclor (30 mg/kg/d, 3 times daily) and cetirizine hydrochloride liquid drops (0.25 mg/kg/d, twice daily) for 3 consecutive days, eczema lesions worsened.

Plasma and urine pharmacokinetics of hydroxyzine and cetirizine following repeated oral administrations to exercised horses.

Hydroxyzine and cetirizine are first- and second-generation oral antihistamine drugs, respectively, used to treat allergic reactions in horses. Cetirizine is also a metabolite of hydroxyzine, which may lead to complexities in regulating their use in equine sporting events. The aim of the research was to be able to provide detection times (DT) from pharmacokinetic studies in thoroughbred horses to better inform trainers, and their veterinary surgeons, prescribing these substances for treatment of Thoroughbred racehorses. Six and two horses were given 9 repeated administrations of hydroxyzine HCl (500mg BID) or cetirizine HCl (190mg BID), respectively. Plasma and urine hydroxyzine and cetirizine concentrations were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS). A holistic non-linear mixed effects PK model was developed that described both plasma and urine concentrations of hydroxyzine and cetirizine, either from administration of each individually or cetirizine as a metabolite of hydroxyzine. Using the parameters obtained from this PK model in conjunction with methodology developed by Toutain afforded possible screening limits (SL) that can regulate for a DT of 4days in either plasma or urine. Hydroxyzine and cetirizine concentration prediction intervals for the 80th , 95th and 99th percentiles of a virtual horse population were performed in order to assess the statistical protection of the DT. However, it is down to the individual racing authorities to apply their own risk management.

Development of silica molecularly imprinted polymer on carbon dots as a fluorescence probe for selective and sensitive determination of cetirizine in saliva and urine

A fluorescence probe based on carbon dots (CDs) coated with silica molecularly imprinted polymer (MIPs) was synthesized for selective and sensitive determination of cetirizine (CTZ). Green source carbon dots were firstly derived from orange peels through a microwave method, and had the merits of eco-friendly and low toxicity. Then a thin silica film was formed on the surface of CDs by reverse microemulsion technique, and molecularly imprinted polymer coated on silica–carbon dots. In this scene, CTZ, 3-aminopropyltriethoxysilane (APTES) and tetraethoxysilane (TEOS) were employed as a template, a functional monomer and cross linker, respectively. The obtained CDs-MIPs can selectively bind CTZ through the specific interaction between recognition sites and template, and obey photoinduced electron transfer fluorescence quenching mechanism. Fluorescence dropped linearly in the range of 0.5–500 ng mL−1, under the optimal conditions, with a detection limit of 0.41 ng mL−1. Furthermore, the proposed method was successfully intended for the determination of trace CTZ in human saliva and urine samples without the interference of other molecules and ions. And recoveries ranged from 95.8% to 99.8% with relative standard deviation less than 3.0%.

An overview of recent developments of carbon-based sensors for the analysis of drug molecules

This review summarizes some recent developments in the fabrication of modified sensors and biosensors using carbon-based materials. The great potential of carbon-based electrodes as sensing platforms is exciting due to their unique electrical and chemical properties, high accessibility and high biocompatibility. Carbon-based materials are particularly interesting due to almost infinite possibility of their functionalization with a wide variety of organic molecules, biologically important compounds and pharmaceuticals. This review is specifically focused on recent developments in the utilization of various carbon-based electrodes in sensing devices for the electrochemical investigation of drug molecules. Various voltammetric techniques considered in this effort include linear sweep voltammetry (LSV), cyclic voltammetry (CV), differential pulse voltammetry (DPV), square wave voltammetry (SWV), and square wave adsorptive stripping voltammetry (SWAdSV). The carbon-based electrode materials considered in this review comprise carbon paste, carbon nanotubes, graphite, graphene, and glassy carbon. The analytes chosen are some routinely used drugs such as paracetamol (PC), diclofenac sodium (DCF), 5-fluorouracil (5-FU), cetirizine (CTZ) and salbutamol (SAL). All here reported sensing electrodes produced very good results in electrochemical investigations of these drug molecules.

Stability Indicating Simultaneous Estimation of Cetirizine Hydrochloride and Phenylephrine Hydrochloride in Combined tablet formulation by using HPTLC- Densitometric method

The new simple, precise, rapid, selective, high performance thin layer chromatography method has been developed for simultaneous estimation of cetirizine hydrochloride and phenylephrine hydrochloride in its combined solid dosage form. The HPTLC method was performed on precoated silica gel G60 F254 plates with, Toluene: Methanol: Ammonia (8: 2: 1, v/v/v) as optimum mobile phase. The plates were developed in 6.00× 0.30mm at room temperature. The developed plates were scanned and quantified at their absorption at 224 nm for CET and PHE respectively. The drugs were satisfactorily resolved with Rf = 0.36± 0.001 for CET and 0.65±0.004 for PHE. Calibration plot was linear between 100-600 ng/ spot for CET and 200-1200 ng/ spot for PHE. This HPTLC method is sensitive, economical, less time consuming than other chromatographic procedures. It can become important tool for analysis of combined solid dosage from. In addition to this results acid exposure, base exposure, oxidative exposure, neutral exposure, photolysis and dry heat exposure is carried out.

Optimization, in vitro release and toxicity evaluation of novel pH sensitive itaconic acid-g-poly(acrylamide)/sterculia gum semi-interpenetrating networks.

In recent era, pH sensitive polymeric carriers that combines the materials engineering and medicine is gaining researcher's attention as they maximizes drug concentration at site of absorption and reduces side effects for e.g. orally administered cetirizine HCl (CTZ HCl) upsets the stomach and furthermore shows high intestinal absorption. Thus, development of pH sensitive hydrogels with sufficient mechanical strength will be good candidate to address this issue. Here, we developed pH sensitive itaconic acid-g-poly(acrylamide)/sterculia gum (IA-g-poly(AM)/sterculia gum) semi-interpenetrating network (semi-IPN) by free radical polymerization technique for intestinal delivery of CTZ HCL. Optimized formulation (I5) with 6% w/w IA showed negligible swelling at pH1.2, and maximum swelling at pH7.4. Solid state characterization of optimized formulation showed successful development of semi-IPN structure and incorporation of drug without any noticeable drug-carrier interaction. In vitro release study showed biphasic pH dependent release of CTZ HCl, where initial burst release was observed at acidic pH followed by sustained release at basic pH. Acute oral toxicity and histopathological studies confirmed the non-toxic nature of IA-g-poly(AM)/sterculia gum. Conclusively, developed biocompatible semi-IPN hydrogels with sufficient pH sensitivity and mechanical strength could serve as a potential carrier for intestinal delivery of CTZ HCL to maximize its absorption and reduce side effects.

Voltammetric analysis of antihistamine drug cetirizine and paracetamol at poly(L-Leucine) layered carbon nanotube paste electrode

In the present effort, a highly responsive electrochemical sensor made up of a carbon nanotube paste electrode modified with a thin layer of electrochemically polymerized L-Leucine was employed for the determination of cetirizine (CTZ) in the presence of paracetamol. In contrast to bare carbon nanotube paste electrode (BCNTPE), a noticeable shift in the peak potential along with an enhancement in the peak current was observed for the electro‒oxidation of CTZ on the modified electrode surface, which can be associated to the extended microscopic active surface area of the modified electrode. The surface of both unmodified and modified electrode surfaces were characterized using field emission scanning electron microscopy (FE-SEM) and electrochemical impedance spectroscopy (EIS) studies. The influence of experimental circumstances on the response of electrode, such as number of sweeping segments in the polymerization process, accumulation potential, accumulation time, and the pH were examined. Under the optimized experimental conditions, the calibration plot was achieved in the concentration range from 5 μM to 50 μM of CTZ with a regression co-efficient of 0.996. The evaluated detection limit for CTZ was achieved as 0.17 μM. The proposed electrode and method were effectively utilized to analyze CTZ in pharmaceutical, blood serum and urine sample with a recovery of 96.49‒99.85 %.

Alteration of Serum Liver Enzymes Level Caused by Cetirizine Hydrochloride in Exercise Performers

Background: Players regularly use cetirizine HCL for the prevention and treatment of various symptoms of allergy while playing in unfamiliar environments. &#x0D; Objective: This research study was carried out to examine the effect of cetirizine HCL on liver function (ALT, ALP and AST) among the players.&#x0D; Methods: A descriptive study was carried out at Gomal University, Dera Ismail Khan from January 2019 to June 2019.Twenty male subjects 10 players using cetirizine HCL (one tablet of 10mg/day) as experimental group and 10 players not using cetirizine HCL as control group was selected voluntarily as participants of the study. Five ml blood was taken from all subjects after three hours of administration of cetirizine HCL for the assessment of ALT, ALP and AST. The results obtained through liver functions test (LFTs) were analyzed through a statistical package for social sciences (SPSS, Version 24).&#x0D; Results: Significant difference was found in both groups (CG and EXG) in term of ALT (P = 000, 0.05&gt;.000). There was significant difference between in both groups (CG and EXG) in term of ALP (P = 000, 0.05&gt;.000). A significant difference was found between in both groups (CG and EXG) in term of AST (P = .001, 0.05&gt;.000).&#x0D; Conclusion: on the basis of finding, the researcher concluded that Cetirizine HCL (Tablet 10mg) produced a significant rise in liver enzymes and hence disturbing the normal functioning of liver.

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Simultaneous Determination of Chloroquine and Pyrimethamine with Cetirizine in an Active Form and Human Serum by RP-HPLC.

A simple, accurate and precise RP-HPLC method was developed for the simultaneous determination of chloroquine, pyrimethamine and cetirizine hydrochloride concentrations in bulk drug and human serum. The assay was performed using a mobile phase of methanol: water (70:30) at pH of 2.8±0.05 on the Purospher C-18 column with UV detection at 230nm and rosuvastatin used as an internal standard. The retention times observed for chloroquine, pyrimethamine and cetirizine hydrochloride were 3.5, 2.5 and 5.5minutes, respectively. The method was found to be specific for the assayed drugs showing a linear response in the concentration range of 1-100μg mL-1 with coefficients of determination values of (r=0.999). The method was developed and validated according to ICH guidelines. The method was used to monitor the serum samples and was found to be sensitive for therapeutic purposes, showing the potential to be a useful tool for routine analysis in laboratories.

Design and Development of Cetirizine HCL Oral Disintegrating Mini-Tablet for to Enhances Patient Compliance

Design and Development of Cetirizine HCL Oral Disintegrating Mini-Tablet for to Enhances Patient Compliance

Poly (DL-valine) electro-polymerized carbon nanotube paste sensor for determination of antihistamine drug cetirizine

Poly (DL-valine) modified multiwalled carbon nanotube paste sensor (PVLMCNTPS) was prepared by electro-polymerization route. PVLMCNTPS and bare multiwalled carbon nanotube paste sensor (BMCNTPS) morphologies and sensing properties for cetirizine (CTZ) were confirmed through a field emission scanning electron microscope (FE-SEM) and electrochemical studies, respectively. In contrast to BMCNTPS, PVLMCNTPS surface composite creates an electrocatalytic impact on the oxidation of CTZ. PVLMCNTPS properties were optimized using parameters such as accumulation time, number of polymerization cycles, solution pH, and scan rate. The optimized PVLMCNTPS was applied for the determination of cetirizine in 0.1 M phosphate buffer solution (PBS) of pH 7.0, using cyclic voltammetry (CV). It is shown that PVLMCNTPS provided analytical linearity from 2.0 to 80 µM, with a detection limit of 0.11 µM for CTZ determination. PVLMCNTPS is found highly selective for CTZ in presence of some interfering organic molecules. The stable and selective PVLMCNTPS was applied for CTZ determination in pharmaceutical pills with satisfactory results.

Investigation the effect of sodium carboxymethylcellulose as polycounterion on cetirizine hydrochloride–sodium dodecyl sulphate mixed micelle

The aim of this research was to investigate the binding properties of sodium carboxymethylcellulose (NaCMCu) as polycounterions on mixed micelles of drug surfactants. Mixed micellization behavior of cetirizine hydrochloride (CTZ) and sodium dodecyl sulphate (SDS) was investigated in the absence and presence of NaCMCu using electrical conductivity, surface tension, fluorescence measurements, dynamic light scattering and UV measurements. The critical micelle concentration (CMC) in the aqueous and NaCMCu medium of CTZ + SDS mixed micelle was lower than the single micelle of CTZ and SDS. The presence of electrostatic interaction between NaCMCu and CTZ + SDS could increase the stability of mixed micelle from αSDS 1.0–0.0. The results showed that CTZ + SDS monomers could bind to the NaCMCu chains and form free mixed micelles in the solution, whereas no SDS / NaCMCu micelle-like complexes were found due to repulsive interaction. NaCMCu significantly decreased the CMC of CTZ. The values of counterion binding (B) from Corrin–Harkins approach and binding constant (Kb) indicated that the CTZ micelles bound to electrostatic interaction by –COO¯ ions of NaCMCu. UV absorbance data given a significant parameter, mean ion occupancy per micelle (i0) which estimated the occupancy per micelle of polycounterions for αSDS 1.0–0.0. However, the turbidity data and micellar size showed that the amount of NaCMCu increased, and the mixed micellar size also increased. Eventually, this system demonstrated that polyelectrolyte was used as an organic counterion to improve the micellar properties of amphiphilic drugs for the formulation of pharmaceutical medicinal products.

Can ocean warming alter sub-lethal effects of antiepileptic and antihistaminic pharmaceuticals in marine bivalves?

The negative effects induced in marine organisms by Climate Change related abiotic factors consequences, namely ocean warming, are well-known. However, few works studied the combined impacts of ocean warming and contaminants, as pharmaceutical drugs. Carbamazepine (CBZ) and cetirizine (CTZ) occur in the marine environment, showing negative effects in marine organisms. This study aimed to evaluate the impacts of ocean warming on the effects of CBZ and CTZ, when acting individually and combined (drug vs drug), in the edible clam Ruditapes philippinarum. For that, drugs concentration, bioconcentration factors and biochemical parameters, related with clam’s metabolic capacity and oxidative stress, were evaluated after 28 days exposure to environmentally relevant scenarios of these stressors. The results showed limited impacts of the drugs (single and combined) at control and warming condition. Indeed, it appeared that warming improved the oxidative status of contaminated clams (higher reduced to oxidized glutathione ratio, lower lipid peroxidation and protein carbonylation levels), especially when both drugs were combined. This may result from clam’s defence mechanisms activation and reduced metabolic capacity that, respectively, increased elimination and limited production of reactive oxygen species. At low stress levels, defence mechanisms were not activated which resulted into oxidative stress. The present findings highlighted that under higher stress levels clams may be able to activate defence strategies that were sufficient to avoid cellular damages and loss of redox homeostasis. Nevertheless, low concentrations were tested in the present study and the observed responses may greatly change under increased pollution levels or temperatures. Further research on this topic is needed since marine heat waves are increasing in frequency and intensity and pollution levels of some pharmaceuticals are also increasing in coastal systems.

Intravenous Cetirizine for Acute Urticaria

Intravenous (IV) diphenhydramine has long been a staple for treating patients with acute urticaria in urgent care settings, but it causes substantial

Selective oxidation of H1-antihistamines by unactivated peroxymonosulfate (PMS): Influence of inorganic anions and organic compounds

The rapid and selective peroxymonosulfate (PMS) induced transformation of H1-antihistamines cetirizine (CET) and diphenhydramine (DPH) can be influenced by the presence of common organic and inorganic water constituents. Presence of HCO3– and/or CO32–, which often exhibit powerful inhibition on the advanced oxidation processes (AOPs), can enhance the PMS mediated transformation of CET/DPH. The observed promotion is demonstrated by the changed solution pH through detailed kinetic studies. The impact of halide ions is remarkable, with I– inhibiting the process through consumption of PMS, while Cl– increases slightly the transformation kinetics through the formation and subsequent reactions of HOCl. The CET/DPH degradation in the Br–/PMS system is influenced by the generation of reactive species such as HOBr which leads to different reaction pathways as compared to PMS alone. The results demonstrated the performance of PMS can be tailored through varying the experimental parameters. In addition, the presence of model organic constituents found in water, e.g., humic acid, phenol, pyridine or sorbate, has a minimal effect on the PMS mediated oxidation processes, highlighting the strong application potential of PMS in water treatment.