Xylorex
Xylorex Uses, Dosage, Side Effects, Food Interaction and all others data.
Ipratropium Bromide is a quaternary ammonium compound with anticholinergic properties. It appears to inhibit vagal reflexes by antagonising the action of acetylcholine (the transmitter agent released from the vagus nerve). Anticholinergics prevent the increase in intracellular concentration of cyclic guanosine monophosphate (cyclic GMP) caused by interaction of acetylcholine with the muscarinic receptor on bronchial smooth muscle.
Ipratropium is a short-acting agent that inhibits the parasympathetic nervous system at the level of the airway which then produces bronchodilatation. The effect of this agent starts after 1-2 hours and it is known to last only from 4 to 6 hours. As part of the effect, ipratropium relaxes the bronchial airways which reverse the narrowing that accounts for wheezy breathing, chest tightness, cough and abnormal gas exchange.
In clinical trials where ipratropium was used in the initial management of status asthmaticus, it was demonstrated a clear benefit in pulmonary function in children and adults. However, the continuous use of ipratropium after an acute asthmatic attack is not proven to be significantly advantageous nor the prophylactic administration of this agent.
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 | Xylorex |
| Generic | Ipratropium + Xylometazoline |
| Type | Nasal Spray |
| Therapeutic Class | |
| Manufacturer | Ajanta Pharma Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Ipratropium Nebuliser Solution is used for a bronchodilator for maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease, including chronic bronchitis and emphysema.
For the symptomatic relief of nasal congestion, perennial allergic rhinitis (including hay fever), sinusitis.
Xylorex is also used to associated treatment for these conditions: Acute Exacerbation of Asthma, Asthma, Bronchospasm, Chronic Obstructive Pulmonary Disease (COPD), Nasal Congestion Associated With the Common Cold, Non-Allergic Rhinitis, Perennial Allergic Rhinitis (PAR), RhinitisAllergic Rhinitis (AR), Nasal Congestion, Seasonal Allergic Rhinitis
How Xylorex works
Ipratropium acts as an antagonist of the muscarinic acetylcholine receptor. This effect produces the inhibition of the parasympathetic nervous system in the airways and hence, inhibit their function. The function of the parasympathetic system in the airway is to generate bronchial secretions and constriction and hence, the inhibition of this action can lead to bronchodilation and fewer secretions.
At the cellular level, the diameter of the airways is controlled by the release of acetylcholine into the muscle cells causing them to contract and producing a narrow airway. Thus administration of ipratropium stops the activity of acetylcholine in the smooth muscle preventing the contraction and producing relaxed airways.
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
Xylorex dosage
Children over 3 years: The usual dose is 0.4-2.0 ml Ipratropium Bromide Solution (100-500 micrograms) up to three times daily.
Adults (including elderly and adolescents) over 12 years of age: The usual dose is 0.4-2.0 ml Ipratropium Bromide Solution (100-500 micrograms) up to four times daily.
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
Allergic-type reactions such as skin rash, angio-oedema of the tongue, lips and face, urticaria (including giant urticaria), laryngospasm and anaphylactic reactions have been reported, with positive rechallenge in some cases.
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
The reported LD50 in mice after oral administration of ipratropium is 1500 mg/kg. However, overdosage is not very likely due to the poor absorption of ipratropium.
Ipratropium was not shown to present carcinogenesis, teratogenesis not mutagenesis potential and it did not present effects on fertility. The only effect after high administration of ipratropium was a reduction in the conception rate.
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
Ipratropium Bromide should be used with caution in patients predisposed to narrow-angle glaucoma, or with prostatic hyperplasia or bladder-neck obstruction.
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
No drug interactions have been reported.
Volume of Distribution
Ipratropium has a volume of distributions of 4.6 L/kg and hence, it is known to be highly distributed in the tissues.
No information is available on xylometazoline pharmacokinetics.
Elimination Route
Ipratropium is a topically active but poorly absorbed agent. The lack of absorption potential in the mucosal surfaces is associated with the presence of a charge in the 5-valent nitrogen. The molecule itself presents very large topic effectiveness however, it does not produce detectable blood levels nor systemic effects.
Serum levels of ipratropium after oral or inhaled administration are very low, corresponding to only 1-2% of the administered dose. These low levels peak after 1-2 hours and it presents a low bioavailability of 2%.
No information is available on xylometazoline pharmacokinetics.
Half Life
Ipratropium presents a short half-life of about 1.6 hours.
No information is available on xylometazoline pharmacokinetics.
Clearance
The average clearance rate of ipratropium is of 2.3 L/min with a renal clearance of 0.9 L/min.
No information is available on xylometazoline pharmacokinetics.
Elimination Route
About 80-100% of the administered dose of ipratropium is excreted in the urine leaving less than 20% of the dose to be eliminated through the feces. From the urine eliminated portion, almost all the drug is found unchanged.
However, when ipratropium is orally administered, due to its low absorption, most of the dose is recovered in the feces with a very minimal amount found in the urine.
No information is available on xylometazoline pharmacokinetics.
Pregnancy & Breastfeeding use
The safety of Ipratropium Bromide during human pregnancy has not been established. The benefits of using Ipratropium Bromide during a confirmed or suspected pregnancy must be weighed against possible hazards to the unborn child. It is not known whether Ipratropium Bromide is excreted into breast milk.
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
Ipratropium Bromide solution should not be taken by patients with known hypersensitivity to atropine or its derivatives or to any other component of the product.
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
Should be stored in cool and dry place
Protect from heat. For reasons of hygiene, do not use the bottle more than 28 days after opening it.
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