Nasotrac
Nasotrac Uses, Dosage, Side Effects, Food Interaction and all others data.
Benzalkonium chloride is a quaternary ammonium antiseptic and disinfectant. It is also used as an antimicrobial preservative for pharmaceutical products. It is also used for the disinfection of rigid contact lenses.
Benzalkonium chloride solutions are generally categorized as biocidal agents with relative long durations of action. Their spectrum of activity has been demonstrated against bacteria, to some viruses, fungi, and protozoa , although bacterial spores are treated as being resistant to the agent. Additionally, the agent generally shows more activity against gram-positive than gram-negative bacteria . Finally, solutions of benzalkonium chloride are bacteriostatic or bactericidal based on their concentration. Bacteriostatic agents act to prevent further growth of bacterial organisms that are present while bactericidal agents function to kill bacteria that are present . In general, the activity of the agent is not largely affected by pH, but such activity does increase substantially at higher temperatures and prolonged exposure times.
Xylometazoline is a sympathomimetic agent with marked alphaadrenergic activity, and is intended for use in the nose. It constricts the nasal blood vessels, thereby decongesting the mucosa of the nose and neighboring regions of the pharynx. This enables patients suffering from colds to breathe more easily through the nose. The effect of Xylometazoline begins within a few minutes and persists for several hours. Xylometazoline is generally well tolerated and does not impair the function of ciliated epithelium. Systemic absorption may occur following nasal application of Xylometazoline.
Xylometazoline is a sympathomimetic agent that causes vasoconstriction of the nasal mucosa. In one study comprising subjects with nasal congestion associated with the common cold, the median time of onset of subjective relief of nasal congestion was about 1.7 minutes and the time of subjective peak relief of nasal congestion was 30 minutes. Previous studies reported rebound swelling, rebound nasal congestion, rhinitis medicamentosa, and shorter duration of decongestant effect from the long-term use of xylometazoline in healthy volunteers, suggesting that the drug is most effective if used temporarily.
An early in vitro study demonstrated xylometazoline to exert anti-oxidant actions, where it inhibited microsomal lipid peroxidation and mediated hydroxyl radical scavenging activity. This suggests that xylometazoline has a beneficial effect against oxidants, which play a role in tissue damage in inflammation.
Trade Name | Nasotrac |
Generic | Benzalkonium + Xylometazoline |
Weight | 0.02% |
Type | Nasal Drops |
Therapeutic Class | |
Manufacturer | Albia Biocare |
Available Country | India |
Last Updated: | September 19, 2023 at 7:00 am |
![Nasotrac Nasotrac](https://www.medicinesfaq.com/media/png/nasotrac.png)
Uses
Higher concentrations of Benzalkonium chloride is used as an antiseptic and disinfectant. This is also widely used as a preservative in eye-drops.
For the symptomatic relief of nasal congestion, perennial allergic rhinitis (including hay fever), sinusitis.
Nasotrac is also used to associated treatment for these conditions: Diaper Dermatitis, Dry Eye Syndrome (DES), Eye and eyelid infections, Gingivitis, Hemorrhoids, Infantile Eczema, Mouth irritation, Pruritus Ani, Tonsillitis, Throat inflammation, Antisepsis, Disinfection therapy, Eye disinfection, Eye lubrication, Hand Hygiene, Skin disinfection, Wound treatmentAllergic Rhinitis (AR), Nasal Congestion, Seasonal Allergic Rhinitis
How Nasotrac works
Although not entirely elucidated, the bactericidal action of benzalkonium chloride is believed to be due to the disruption of intermolecular interactions. Such disruption can cause the dissociation of cellular membrane lipid bilayers of bacteria, resulting in compromised cellular permeability control and the leakage of important cellular contents. Additionally, other important molecular complexes like enzymes which control the maintenance of a great range of respiratory and metabolic cellular activities, are also susceptible to such deactivation. Consequently, a variety of critical intermolecular interactions and tertiary structures in very highly specific biochemical systems that allow bacterial agents to function normally can be readily disrupted or deactivated by cationic surfactants like benzalkonium chloride. .
Nasal congestion is caused by various etiologies, such as rhinosinusitis and allergic or non-allergic rhinitis, leading to congestion of the venous sinusoids lining the nasal mucosa. Activation of α-adrenergic receptors leads to vasoconstriction of the blood vessels of the nasal mucosa and resumption of nasal airflow. As the most abundantly expressed in the human nasal mucosa, α1A- and α2B-adrenoceptors may play the most important role in vasoconstriction of the human nasal mucosa. Xylometazoline is a more selective agonist at α2B-adrenoceptors, with affinity at α1A-, α2A-, α2C-, α1B-, and α1D-adrenoceptors. Xylometazoline decreases nasal resistance during inspiration and expiration and increases the volume of nasal airflow. Compared to oxymetazoline, another imidazoline nasal decongestant, xylometazoline had a slightly faster onset of action although they had a similar duration of action. In one study, subjects with nasal congestion reported relief of earache and sore throat in addition to nasal decongestion: it is speculated that oxymetazoline mediates this effect by causing vasoconstriction of the nasal mucosa that contains the venous sinuses and nasal decongestion allows breathing through the nose, providing relief from sore throat caused by mouth breathing that dries and irritates the throat.
Dosage
Nasotrac dosage
- Tincture of benzalkonium chloride 1:750 is used for the preoperative disinfection of unbroken skin or treatment of superficial injuries.
- For preoperative disinfection of mucous membranes and denuded skin, benzalkonium chloride solution in concentrations of 1:10000 to 1:2000 is used.
- For irrigation of the eye, a solution of 1:10000 to 1:5000 is used.
- For urinary bladder and urethral irrigation, a solution 1:5000 to 1:20000 is used.
- For vaginal douche and irrigation, benzalkonium chloride solution 1:5000 to 1:20000.
Adults: 2 or 3 drops of Xylometazoline Adult formula (0.1%) two to three times daily. This adult formula should not be used for children under the age of 12 years.Children under 12 years: 1 or 2 drops of the Xylometazoline children's formula (0.05%) in each nostril once or twice daily. Not to be used in infants less than 3 months.
Side Effects
Repeated application may cause hypersensitivity reactions. May cause nausea and vomiting if ingested.
The following side effects have occasionally been encountered: a burning sensation in the nose and throat, local irritation, nausea, headache, and dryness of the nasal mucosa. Systemic cardiovascular effects have occurred, and this should be kept in mind when giving Xylometazoline to people with cardiovascular disease.
Toxicity
An oral dose of 100-400 mg/kg or a parenteral dose of 5-15 mg/kg is believed to be fatal in humans .
A potential concern for larger concentrations of benzalkonium chloride to possibly cause corneal damage when implemented as an excipient ingredient in aqueous eye products is an issue that should be discussed between potential patents and their health care providers . Since decreased regular blinking and tear generation in patients experiencing dry eyes due to any number of eye conditions can result in reduced dilution of applied eye drops containing the benzalkonium chloride preservative , alternative options including benzalkonium chloride-free products should be considered.
Additionally, benzalkonium chloride has been reported to cause punctate keratopathy and/or toxic ulcerative keratopathy. In addition, benzalkonium chloride may cause eye irritation and is known to discolour soft contact lenses . There may also be the possibility of benzalkonium chloride containing eye drops to cause some stinging and pain .
There is the possibility of ototoxicity occurring when benzalkonium chloride containing ear drops are applied to the ear .
Benzalkonium chloride used as a preservative in nebulised solutions of anti-asthma drugs has been reported to cause dose-related bronchoconstriction especially in asthmatic patients and has been associated with the precipitation of respiratory arrest .
Despite the fairly widespread cutaneous use of benzalkonium chloride, only limited human evidence of sensitization in relatively small populations of individuals have been reported . Nevertheless, the main adverse effect for topical formulations of benzalkonium chloride is usually the warning 'may cause local irritation' .
The oral LD50 is 230 mg/kg in rats and 75 mg/kg in mice. The subcutaneous LD50 is 90 mg/kg in rats and 53 mg/kg in mice. The intraperitoneal LD50 is 43 mg/kg in rats.
Xylometazoline poisoning is documented in three pediatric patients who were exposed to a drug concentration 40 times above the adequate dosage for children due to a compounding error: these patients experienced bradypnea and sinus bradycardia with supraventricular extrasystoles and were managed with fluid management.
Precaution
Each Xylometazoline pack should be used by one person only to prevent any cross-infection. Patients are advised not to take decongestants for more than seven consecutive days.
Interaction
Disinfectants containing quaternary ammonium salts should not be used for skin preparation before injections of viscoelastic solutions. Hyaluronic acid will precipitate in the presence of these salts.
No drug interactions have been reported.
Volume of Distribution
When applied as a topical antibacterial, antiseptic, disinfectant, or sanitizer it is believed that molecules of benzalkonium chloride are poorly absorbed (perhaps due to their large, positively charged nature ), especially considering expectations for such topical applications to keep their biocidal agents available for action at the topical level and to not be absorbed significantly beyond it.
When benzalkonium chloride is implemented as an excipient preservative ingredient in various eye, nose, and ear aqueous products, such products will always have other active pharmacological agents whose volume of distribution will be of greater importance. In these cases the excipients will only ever be present at the minimal levels necessary to maintain the integrity of the product substance.
Moreover, Benzalkonium chloride is currently listed as a Category III ingredient by the United States Food and Drug Administration . Ingredients are listed in the FDA Category III when the data available about them are insufficient to classify as safe and effective, requiring further testing to determine more formal details about elements like human pharmacokinetic studies, and studies on the ingredients' absorption, distribution, metabolism, and excretion.
No information is available on xylometazoline pharmacokinetics.
Elimination Route
Percutaneous absorption is considered to be insignificant .
In one study, benzalkonium chloride absorption was evaluated in women using tampons containing the agent. Venous blood samples were drawn 15 minutes before the tampon application and then again at 15 min, 1 h, 3 h, and 24 h after application. Benzalkonium chloride was not detected in any of the blood samples at any time tested.
Similarly, in another study, benzalkonium chloride absorption was tested in women using tampons containing the agent. Venous blood and breast milk samples were taken 15 minutes before application and 3 h and 24 h after tampon administration. Benzalkonium chloride was not found in any of the subjects' samples. .
Moreover, in a study where benzalkonium chloride solution was placed on the corneal surface of rabbit subjects, at various intervals after administration, the rabbits' eyes would be washed with 1 mL saline and the following tissues and fluids were removed: bulbar and palpebral conjunctiva, aqueous humour, corneal epithelium, endothelium and stroma, iris-ciliary body, lens, vitreous, retina, and choroid. Plasma samples were obtained with direct cardiac punctures. After administration of one drop, benzalkonium chloride was found in the corneal epithelium, endothelium, and stroma, and in the bulbar and palpebral conjunctivae. Benzalkonium chloride loss from ocular tissues was such that about one-third to two thirds of its concentration (depending on the tissue) at 30 min remained after 24 hr; measurable values existed for as long as 120 hr. The administration of multiple drops led to continued accumulation of benzalkonium chloride. .
No information is available on xylometazoline pharmacokinetics.
Half Life
No information is available on xylometazoline pharmacokinetics.
Clearance
No information is available on xylometazoline pharmacokinetics.
Elimination Route
Administered benzalkonium chloride is likely eliminated largely in faeces, similar to other quaternary ammonium compounds .
No information is available on xylometazoline pharmacokinetics.
Pregnancy & Breastfeeding use
No foetal toxicity or fertility studies have been carried out in animals. In view of its potential systemic vasoconstrictor effect, it is advisable to take the precaution of not using Xylometazoline during pregnancy
Contraindication
Incompatible with soaps and other anionic surfactants, citrates, iodides, nitrates, permanganates, salicylates, silver salts, tartrates, and zinc oxide and sulfate.
Xylometazoline nasal drops is contraindicated in patients with trans-sphenoidal hypophysectomy or surgery exposing the dura mater. It is also contraindicated in patients who are hypersensitive to Xylometazoline.
Storage Condition
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Protect from heat. For reasons of hygiene, do not use the bottle more than 28 days after opening it.
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