OTRIVIN 0.05% NASAL DROPS

Indications

• Nasal congestion due to rhinosinusitis
• Allergic rhinitis
• Non-allergic rhinitis
• Common cold-related nasal congestion

Dosage

Adults: For adults, the typical dose is 0.1% to

Mechanism of action

Xylometazoline acts primarily as an agonist at α_2B-adrenergic receptors, with additional activity at α_1A-, α_2A-, α_2C-, α_1B-, and α_1D-adrenergic receptors. This agonistic action leads to vasoconstriction of the blood vessels in the nasal mucosa, decreasing nasal resistance during breathing and enhancing airflow. The drug's vasoconstrictive properties also contribute to symptomatic relief of associated conditions, such as earache and sore throat, which may arise from mouth breathing due to nasal congestion.

Pharmacodynamics

Xylometazoline is effective in reducing nasal congestion, with a median onset of relief approximately 1.7 minutes after administration and peak relief at around 30 minutes. Its vasoconstrictive effect can lead to rebound swelling and congestion if used long-term, with potential for rhinitis medicamentosa. The drug also exhibits antioxidant properties, which may protect against oxidative stress associated with inflammation in the nasal passages.

Pharmacokinetics

Xylometazoline is rapidly absorbed when administered nasally, although specific pharmacokinetic parameters such as half-life and bioavailability are not well-documented. Its effects are relatively short-lived, necessitating careful management of dosing to avoid rebound congestion. Regular use past the recommended duration can lead to diminished efficacy and increased risk of adverse effects.

Adverse effects

• Rebound congestion
• Nasal mucosa irritation
• Dryness of the nasal mucosa
• Headache
• Nausea

Interactions

• volatile halogenated anesthetics + xylometazoline: Unknown (additive effect)

Precautions

• Use with caution in patients with cardiovascular disease
• Use with caution in patients with hypertension
• Use with caution in patients with hyperthyroidism
• Avoid prolonged use to prevent rebound congestion

Pregnancy

Use during pregnancy only if clearly needed, as safety in pregnancy has not been established.

Breast-feeding

Use with caution, as it is not known whether xylometazoline is excreted in human milk.

Storage

Store below 30°C. Protect from light.

Formulations

• Nasal spray
• Nasal drops

Indications

• Nasopharyngitis (common cold)
• Sinusitis (acute)
• Nasal congestion

Dosage

Children: For children aged 12-17 years, the recommended dosage is 2-3 drops of a 0.1% solution or 1 spray into each nostril 1-3 times a day as required, with a maximum duration of use of 7 days. Caution is advised for children under 12 years, as use is generally not recommended in younger children.

Adults: For adults, the usual dosage is 0.1% solution, administered as 1 spray into each nostril up to 3 times a day as required, with a maximum duration of use of 7 days.

Mechanism of action

Xylometazoline acts as an alpha-adrenergic agonist, stimulating alpha-1 adrenergic receptors on vascular smooth muscle, leading to vasoconstriction. This action reduces blood flow to the nasal mucosa, decreasing swelling and congestion. The onset of action is rapid, providing quick relief from nasal obstruction.

Pharmacodynamics

The pharmacodynamic effects of xylometazoline include significant vasoconstriction of nasal mucosa blood vessels, which leads to decreased nasal congestion. This effect can last for several hours, making it effective for acute conditions. However, prolonged use may lead to rebound congestion due to tolerance development.

Pharmacokinetics

Xylometazoline is administered intranasally, allowing for localized effects with minimal systemic absorption. Peak plasma concentrations are typically reached shortly after administration, although due to its local action, systemic effects are usually minimal. The metabolism and elimination pathways are not well characterized but are believed to involve hepatic metabolism and renal excretion.

Contra-indications

• Hypersensitivity to xylometazoline or any of its excipients
• Severe cardiovascular disease
• Closed-angle glaucoma
• Children under 6 years of age

Adverse effects

• Cardiovascular effects
• Headache
• Hypersensitivity reactions
• Nasal dryness
• Nausea
• Paresthesia
• Visual impairment
• Rebound congestion (rhinitis medicamentosa) with prolonged use
• Agitated psychosis, ataxia, hallucinations, and rare fatalities in infants and children under 6 years

Interactions

• Other sympathomimetics
• Vasoconstrictors

Precautions

• Use with caution in patients with diabetes mellitus
• Hypertension
• Hyperthyroidism
• Prolonged use should be avoided to prevent rebound congestion

Pregnancy

Manufacturer advises avoiding use during pregnancy due to insufficient data on safety.

Breast-feeding

Manufacturer advises caution as no information is available regarding the safety of xylometazoline during breastfeeding.

Storage

Store below 25°C. Do not freeze. Keep the container tightly closed.

Formulations

• {'name': 'Otrivine', 'type': 'Nasal spray', 'strength': '0.1%', 'volume': '15 ml'}
• {'name': 'Sudafed Sinus-Ease', 'type': 'Nasal drops', 'strength': '1 mg per 1 ml', 'volume': '10 ml'}

Mechanism of action

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, α_1A- and α_2B-adrenoceptors may play the most important role in vasoconstriction of the human nasal mucosa. Xylometazoline is a more selective agonist at α_2B-adrenoceptors, with affinity at α_1A-, α_2A-, α_2C-, α_1B-, and α_1D-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.

Pharmacodynamics

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.