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PubMed1981

Utility of chloranil in assay of naphazoline, clemizole, penicillin G sodium, and piperazine.

A simple and sensitive spectrophotometric method is described for the assay of naphazoline, clemizole, penicillin G sodium, and piperazine. The method was based on the formation of a charge transfer complex between these drugs as n-donors and chloranil, the pi-acceptor. Conformity to Beer's law enabled the assay of dosage forms of these drugs. Compared with official methods, the results obtained were of equal accuracy. A more detailed investigation of th naphazoline-chloranil complex was made with respect to its composition, association constant, and free energy change.

Benzimidazoles↗
PubMed1983

High-performance liquid chromatographic stability-indicating assay for naphazoline and tetrahydrozoline in ophthalmic preparations.

A high-performance liquid chromatographic (HPLC) analysis for tetrahydrozoline and naphazoline in ophthalmic solutions is presented. The analysis allows a more reproducible, direct stability-indicating assay than the colorimetric methods generally employed. The HPLC system is so designed that a variety of ophthalmic solutions containing either naphazoline or tetrahydrozoline can be analyzed concomitantly.

Chromatography, High Pressure Liquid↗
PubMed1995

Synthesis and identification of the primary degradation product in a commercial ophthalmic formulation using NMR, MS, and a stability-indicating HPLC method for antazoline and naphazoline.

HPLC analysis of an anti-infective ophthalmic solution (Albalon-A), containing the active drugs naphazoline and antazoline, revealed a degradation peak of unknown identity. To elucidate the identity of the degradant, the active drugs were each hydrolyzed by refluxing at high pH, and their respective hydrolysis products were isolated and spectrally characterized by NMR, FT-IR, and MS for conclusive structure elucidation. The degradant's identity was confirmed by HPLC-MS analysis of Albalon-A ophthalmic solution to be the antazoline hydrolysis product N-[(N-benzylanilino)acetyl]ethylenediamine (IV). A stability-indicating HPLC method was then developed which was able to resolve IV from the active drugs. This HPLC method was then validated for quantitating the active drugs and IV. Validation studies demonstrated linear UV response at 280 nm, recovery > 98%, good reproducibility, and a detection limit of 2 micrograms/mL IV. Overall, the data demonstrated that the HPLC method was quantitative and specific for antazoline, naphazoline, and IV. Analysis of an expired stabilitry lot of the ophthalmic solution indicated the concentration of IV was 0.002% (w/v).

Antazoline↗
PubMed1991

Inhibition by glibenclamide of the effects of cromakalim on responses of rat vas deferens to naphazoline.

Cromakalim has been shown to inhibit naphazoline-induced contractions and spontaneous activity induced by exposure to naphazoline in the rat isolated vas deferens. Glibenclamide 10(-6) M blocked both these effects of cromakalim. Our data add to the list of data derived mainly from experiments on vascular smooth muscle; they suggest that the same glibenclamide-sensitive K+ channel is present in vascular and non-vascular smooth muscle and that it may be involved in the relaxant actions of cromakalim.

Animals↗
PubMed2004

Hemorrhagic stroke after naphazoline exposition: case report.

Ten percent of all strokes are due to spontaneous cerebral hemorrhages. They are associated to drugs (licit and illicit) in 9.5% of all cases in young adults. This is a case report of a 44-year-old man, without previous morbidities, who presented a sudden onset headache and arterial hypertension 24 hours after use of naphazoline as nasal decongestant. Cranial tomography showed right thalamus hemorrhage. Cerebral angiography showed no aneurisms, vascular malformations or vasculitis. No other risk factors were found during investigation in this patient and the stroke was attributed to naphazoline exposition.

Adult↗
PubMed1983

Oxymetazoline ophthalmic solution versus naphazoline solution in non-infectious conjunctivitis.

A double-blind, randomized study was carried out in 38 adult patients with non-infectious conjunctivitis to compare the efficacy and tolerance of oxymetazoline (0.025%) ophthalmic solution with that of naphazoline (0.04%) solution. Treatment was continued for 7 to 8 days and severity of symptoms was recorded before, during and at the end of therapy. At the end of the study period, 11 (69%) of 16 patients treated with oxymetazoline demonstrated a good to excellent response to therapy compared with 8 (53%) of 15 patients in the naphazoline-treated group. A statistically significant difference favouring oxymetazoline was observed in duration of action and the mean number of applications needed. No adverse reactions were reported in either treatment group.

Adult↗
PubMed1998

Two examples of rapid and simple drug analysis in pharmaceutical formulations using capillary electrophoresis: naphazoline, dexamethasone and benzalkonium in nose drops and nystatin in an oily suspension.

Capillary electrophoresis is a versatile tool in pharmaceutical analysis. In the course of a revision of the "Standardrezepturen", a German formula of standard dispensings for preparation in pharmacies, this technique has been applied to drug analysis in pharmaceutical formulations. The present paper deals with two different examples. First, naphazoline, dexamethasone and the preservative benzalkonium are quantified in nose drops without any sample preparation. Second, the antifungal antibiotic nystatin is quantified using nonaqueous capillary electrophoresis in methanol after sample preparation from an oily suspension.

Administration, Intranasal↗
PubMed2006

Evaluation, in vitro, of the radioprotection of DNA from gamma-rays by naphazoline.

Design of compounds that can protect efficiently against gamma-rays irradiation is a great challenge. An ionizing event can cause variety of DNA damage scenarios leading to mutagenesis, cell death. 2-(1-Naphthylmethyl)-2-imidazoline (naphazoline, NP) is a drug belonging to the vasoregulator class, which was shown to be a very interesting compound in radioprotection. In order to highlight the NP radioprotective activity, a comparison of its ability to protect DNA against either gamma-irradiation or radicals generated by Fenton's reaction was made. Results show that NP inhibits efficiently the generation of DNA single-strand breaks and that NP is a potent radioprotector and also an hydroxyl radical scavenger.

DNA↗
PubMed2005

A fluorescence optosensor for analyzing naphazoline in pharmaceutical preparations. Comparison with other sensors.

We have developed an optical sensor for determining and quantifying naphazoline (NPZ) based on its inherent fluorescence property. We have placed a non-ionic-exchanger solid support (Amberlite XAD-7) in a flow cell in the light path of the excitation beam and the fluorescence signal for NPZ is continuously monitored at lambda(exc/nm)=294/306 nm. The response time for this sensor is acceptably fast, 80s, obtaining a detection limit of 2.6 ng mL(-1) with standard deviations of 2.0% at 125 ng mL(-1). This device has been satisfactorily applied to two commercial formulations and its selectivity has been demonstrated with an interference study. The advantages have been compared with the only published sensor for determining NPZ in pharmaceutical preparations and with other analytical methods in the literature.

Adrenergic alpha-Agonists↗
PubMed2003

Simultaneous determination of naphazoline, diphenhydramine and phenylephrine in nasal solutions by capillary electrophoresis.

A capillary zone electrophoresis (CZE) method has been developed to separate and quantitate naphazoline (NAPH), dyphenhydramine (DIP) and phenylephrine (PHE) in nasal solutions. Samples were diluted 1:25 in ultrapure water and injected at the anodic end. A central composite design has been used to optimise the experimental conditions for a complete and fast separation of the active ingredients studied. Critical parameters such as voltage, pH and buffer concentration have been studied to evaluate how they affect responses such as resolution and migration times. Separation was performed on a silica capillary with 75 microm I.D. and 70 cm total length at an applied voltage of 17.7 kV with a phosphate run buffer of pH 3.72 and 0.063 mol l(-1). Calibration curves were prepared for NAPH, DIP and PHE. For each analyte, the correlation coefficients were >0.999 (n=15). The RSD% of six replicate injections for each analyte were reasonably good. The method was applied to the quantitation of the three components in a commercial dosage form. The proposed method has the advantage of needing a very simple sample pretreatment and being faster than a typical HPLC chromatographic method.

Administration, Intranasal↗
PubMed2003

[Cardiac arrest and secondary pulmonary oedema following accidental intramucosal injection of naphazoline in an adult].

During neurosurgery for hypophysary adenoma under general anaesthesia in a prone position, a 34 year-old-women received accidental 6 ml intramucosal injection of lidocaine with naphazoline. The patient presented a severe bradycardia associated with a major increase in arterial blood pression followed by a brief cardiac arrest. She also presented a prolonged awakening and a pulmonary oedema, which lead to mechanical ventilation. The patient rapidly recovered a normal clinical state.

Adenoma↗
PubMed1999

Phototoxicity of naphazoline. Evidence that hydrated electrons, nitrogen-centered radicals, and OH radicals trigger DNA damage: a combined photocleavage and laser flash photolysis study.

The potential phototoxic activity of naphazoline (NP), 2-(1-naphthylmethyl)imidazoline, was investigated by studying its photoreactivity toward DNA. Photocleavage studies combined with laser flash photolysis experiments provide clear evidence that the transient species produced under NP photolysis react with DNA, thereby promoting its breakage under both aerobic and anaerobic conditions. Hydrated electrons and nitrogen-centered radicals are involved in the photodamage under anaerobic conditions. Hydroxyl radicals generated by Haber-Weiss reaction seem to initiate the photocleavage observed under aerobic conditions. A photodynamic mechanism involving the participation of singlet oxygen does not seem to play a crucial role in the photoinduced DNA breakage. The interaction between the NP and the biopolymer is also investigated by using both steady state and time-resolved spectroscopy.

Algorithms↗
PubMed2001

Prolonged awakening and pulmonary edema after general anesthesia and naphazoline application in an infant.

IMPLICATIONS: Naphazoline intoxication by intrabronchial overdose caused prolonged unconsciousness of an 18-mo-old child after general anesthesia for tracheal rigid bronchoscopy. The leading symptoms were side effects involving the cardiovascular, pulmonary, and central nervous systems. Intensive care unit admission with the need for mechanical ventilation was necessary. Recovery was uneventful.

Adrenergic alpha-Agonists↗
PubMed1976

Effects of diphenhydramine, naphazoline and m-amino-alpha(1-aminoethyl)benzyl alcohol dihydrochloride on the nasal mucosa determined by impedance method: a simple method for evaluation of nasal decongestant.

A simple, new method was devised for evaluating nasal decongestants. In anesthetized dogs, two needle electrodes were inserted bilaterally into the superficial mucosa of the nasal wings. An impedance plethysmorgraphy provided with a DC output was used to measure impedance between the two electrodes. When 1% histamine solution was sprayed into a nostril focusing on the inside mucosa of a nasal wing, impedance decreased markedly and thereafter recovered to a control level within 1-1.5 h. Comparable responses were obtained when the same solution was sprayed into the opposite nostril. The drugs to be tested were administered intravenously or topically between these two histamine application. Intravenous administrations of diphenhydramine (0.5 mg/kg) and m-amino-alpha)1-aminoethyl) benzyl alcohol dihydrochloride (0.1 mg/kg) inhibited the histamine effect completely. Pretreatment with naphazoline administered topically also inhibited impedance changes cause by histamine application. Local appliations of acetycholine (10%) and bradykinin (0.1%) did not change nasal impedance significantly in any instances.

Acetylcholine↗
PubMed1975

Antazoline phosphate and naphazoline hydrochloride, singly and in combination for the treatment of allergic conjunctivitis-a controlled, double-blind clinical trial.

A controlled, double-blind comparison of naphalzoline hydrochloride 0.05%, antazoline phosphate 0.5%, a combination of both components and a placebo was performed on 51 ragweed sensitive patients presenting allergic conjunctivitis. Evaluation of response at various times after instillation of medication for lacrimation, conjunctival inflammation, pruritus, photophobia and pain showed naphazoline hydrochloride, antazoline phosphate and the combination product superior to placebo. The combination product was statistically significantly superior for conjunctival inflammation and photophobia. The need for post-challenge treatment with epinephrine hydrochloride was significantly less in those eyes treated with the combination product. demonstrating prophylactic efficacy.

Adolescent↗
PubMed1991

[The effect of bioadhesiveness of viscous solutions with naphazoline hydrochloride on the elimination of the drug from the eye of swine].

Solutions of sodium carboxymethylamylopectine, tragant, hydroxyethylcellulose, polyvinylalcohol, polyacrylic ester D 339, polyacrylic ester D 340 and polyacrylic acid, all of the same viscosity and with the same concentration of naphazoline hydrochloride, were applied on the isolated eye of pig. After sink the eye in a solution of sodium chloride the elimination of the drug from the eye was investigated. The results were compared with the bioadhesion of the viscous solutions measured ex vivo on the intestine of pigs. There were correlations between the eliminated mass after 5 min, after 30 min and the bioadhesion. Furthermore the calculated initial elimination constant was indirect proportional to the bioadhesion. The elimination of the drug between 5 and 30 min was independent on the bioadhesion.

Adhesiveness↗
PubMed1994

High-performance liquid chromatographic determination of benzalkonium and naphazoline or tetrahydrozoline in nasal and ophthalmic solutions.

A high-performance liquid chromatographic method is described for the determination of benzalkonium chloride homologues and naphazoline nitrate or tetrahydrozoline hydrochloride in ophthalmic and nasal solutions. The technique involves a one-step dilution (1:5) for sample preparation and direct injection onto a 5 mm RP C-8 column. The mobile phase is acetonitrile-diluted acetic acid (80:20, v/v) with 6 mM tetramethylammonium bromide. Detection is carried out at 260 nm with a diode array. The method is rapid, specific, reproducible and is especially useful for quality control procedures.

Benzalkonium Compounds↗