Nesivine
Nesivine Uses, Dosage, Side Effects, Food Interaction and all others data.
Nesivine is a direct-acting sympathomimetic which has vasoconstrictor effect on mucosal blood vessels when applied topically and in turn reduces oedema of the nasal mucosa.
Nesivine is an adrenergic α1- and α2-agonist and a direct-acting sympathomimetic drug. By stimulating adrenergic receptors, oxymetazoline causes vasoconstriction of dilated arterioles and reduces blood flow. In a radioligand competition study, oxymetazoline displayed higher affinity at α1A-adrenoceptors compared to α2B-adrenoceptors, but with higher potency at α2B-adrenoceptors. When sprayed intranasally, oxymetazoline relieved relief nasal congestion and improved nasal airflow in patients with acute coryzal rhinitis for up to 12 hours following a single dose.
An early in vitro study demonstrated oxymetazoline to exert anti-oxidant actions, where it inhibited microsomal lipid peroxidation and mediated hydroxyl radical scavenging activity. This suggests that oxymetazoline has a beneficial effect against oxidants, which play a role in tissue damage in inflammation.
| Trade Name | Nesivine |
| Availability | Prescription only |
| Generic | Oxymetazoline |
| Oxymetazoline Other Names | Oximetazolinum, Oxymetazolina, Oxymetazoline, Oxymétazoline, Oxymetazolinum, Oxymethazoline, Oxymetozoline |
| Related Drugs | doxycycline, metronidazole topical, ivermectin topical, minocycline topical, brimonidine topical, Vibramycin |
| Type | |
| Formula | C16H24N2O |
| Weight | Average: 260.3746 Monoisotopic: 260.1888634 |
| Protein binding | In vitro, oxymetazoline is 56.7% to 57.5% bound to human plasma proteins. |
| Groups | Approved, Investigational |
| Therapeutic Class | Nasal Anti-histamine preparations, Nasal Decongestants & Other Nasal Preparations |
| Manufacturer | |
| Available Country | Belgium |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Nesivine Hydrochloride is applied topically to relieve nasal congestion associated with acute or chronic rhinitis, common cold, sinusitis, and hay fever or other allergies. It is also used as nasal decongestant in otitis media.
Nesivine is also used to associated treatment for these conditions: Acquired Blepharoptosis, Allergic Rhinitis (AR), Nasal Congestion, Postoperative Hemorrhages, Rhinorrhoea, Sinus Congestion, Acute Rhinitis, Persistent facial erythema, Airway visualization
How Nesivine works
Nesivine binds to α1- and α2-adrenoceptors, which are Gq-protein-coupled receptors that promote vascular smooth muscle contraction by increasing intracellular calcium levels in response to ligand activation.
Rosacea is a condition characterized by transient and persistent facial erythema. By stimulating α1A-adrenoceptors and causing vasoconstriction, oxymetazoline is believed to diminish the symptoms of erythema. In blepharoptosis, it is hypothesized that oxymetazoline works by stimulating α-adrenergic receptors on the Müller muscle that elevates the upper eyelid, causing muscle contraction. Nesivine is used in combination with tetracaine for local anesthesia in dentistry. Such combination use adds beneficial effects: the vasoconstrictor counteracts the local anesthetic agent's vasodilatory action, thereby constricting dilated arterioles and reducing blood flow to the application area. Nesivine relieves nasal congestion by vasoconstricting the respiratory microvasculature, in both resistance and capacitance blood vessels on the human nasal mucosa, leading to decreased nasal mucosal blood flow, edema, and airflow resistance.
Dosage
Nesivine dosage
Adults and children 6 years of age and older: 2-3 drops or sprays in each nostril twice daily for 3-5 days.
Children of age 2-6 years: 2-3 drops in each nostril twice daily for 3-5 days. Sprays are generally unsuitable for young children because of the small size of their nostrils. The drug is not recommended in children under the age of 2 years.
The nasal spray can be used with the patient in the upright position. Sprays are generally unsuitable for young children because of the small size of their nostril. A treatment course should not normally exceed three to five days, and on no account should it be continued for longer than two weeks because of the risk of developing "rhinitis medicamentosa".
Side Effects
Transient burning, dryness of the nasal mucosa, sneezing, Nervousness, dizziness, headache, Hypertension, palpitation or reflex bradycardia.
Toxicity
In rats, the oral LD50 is 680 ug/kg and the subcutaneous LD50 is 1630 ug/kg. In mice, the oral LD50 is 4700 ug/kg, the intraperitoneal LD50 is 48 mg/kg, and the subcutaneous LD50 is 34 mg/kg.
Case reports have documented unintended overdose in both children and adults: overdose has led to dizziness, chest pain, headaches, myocardial infarction, stroke, visual disturbances, arrhythmia, hypertension, or hypotension. Accidental ingestion of topical solutions of imidazoline derivatives, including oxymetazoline, in children has resulted in serious adverse events requiring hospitalization, such as nausea, vomiting, lethargy, tachycardia, decreased respiration, bradycardia, hypotension, hypertension, sedation, somnolence, mydriasis, stupor, hypothermia, drooling, and coma. Possible rebound nasal congestion, irritation of nasal mucosa, and adverse systemic effects (particularly in children), including serious cardiovascular adverse events, have been reported with overdosage as well as prolonged or too frequent intranasal use of oxymetazoline. Overdose should be responded with close monitoring, supportive care, and symptomatic treatment.
Precaution
- Prolonged use may result in rebound congestion.
- Since oxymetazoline has systemic adverse effects, it should be used with caution in patients with
- Hypertension, cardiovascular disease or hyperthyroidism or in those receiving MAO inhibitors.
Interaction
Monoamine oxidase inhibitors (MAOIs): Concomitant use of oxymetazoline and MAOI can result in hypertensive reaction.
Tricyclic antidepressants (TCAs): TCAs may increase the effects of oxymetazoline on blood pressure.
Food Interaction
No interactions found.Volume of Distribution
There is limited information on the volume of distribution of oxymetazoline.
Elimination Route
Imidazole derivatives such as oxymetazoline are readily absorbed across mucosal membranes, especially in children. In adult subjects with erythema associated with rosacea, the mean ± standard deviation (SD) Cmax was 60.5 ± 53.9 pg/mL and the AUC from time 0 to 24 hours (AUC0-24hr) was 895 ±798 pg x hr/mL following topical administration of first-dose oxymetazoline. Following once-daily topical applications for 28 days, the mean ± SD Cmax was 66.4 ± 67.1 pg/mL and the AUC0-24hr was 1050 ± 992 pg x hr/mL. Following twice-daily applications for 28 days, the mean ± SD Cmax was 68.8 ± 61.1 pg/mL and the AUC0-24hr was 1530 ± 922 pg x hr/mL.
Following single-drop ocular administration of oxymetazoline in healthy adult subjects, the mean ± SD Cmax was 30.5 ± 12.7 pg/mL and the area under the concentration-time curve (AUCinf) was 468 ± 214 pg x hr/mL. The median Tmax was 2 hours, ranging from 0.5 to 12 hours.
Following nasal administration of an 0.6 mL combination product containing tetracaine and oxymetazoline in adult subjects, the maximum concentrations of oxymetazoline were reached within approximately 10 minutes. The mean Cmax was 1.78 ng/mL and the AUC0-inf value was 4.24 ng x h/mL, with a median Tmax of 5 minutes.
Half Life
Following ocular administration in healthy adults, the mean terminal half-life was 8.3 hours, ranging from 5.6 to 13.9 hours.
The terminal half-life of oxymetazoline following nasal administration of the combination product containing tetracaine and oxymetazoline in adult subjects is approximately 5.2 hours.
Clearance
There is limited information on the clearance rate of oxymetazoline.
Elimination Route
While the excretion of oxymetazoline following nasal, topical, or ophthalmic administration of oxymetazoline has not been fully characterized in humans, it is believed that the predominant route of elimination at clinically relevant concentrations of oxymetazoline is renal excretion.
Pregnancy & Breastfeeding use
Pregnancy: Safe use of oxymetazoline during pregnancy has not been established; it should be avoided by pregnant women.
Nursing Mother: It is not known whether oxymetazoline is secreted in human breast milk; caution is advised.
Contraindication
Contraindicated in patients hypersensitive to Oxymetazoine Hydrochloride.
Acute Overdose
Following a proper application, systemic action is unlikely. If, however, some of the drops are swallowed, systemic effect can be produced. Symptoms include rapid, irregular heartbeat, headache, dizziness, increased sweating, nervousness. Such symptoms are more likely to be seen in young children.
Innovators Monograph
You find simplified version here Nesivine
Nesivine contains Oxymetazoline see full prescribing information from innovator Nesivine Monograph, Nesivine MSDS, Nesivine FDA label
FAQ
What is Nesivine used for?
Nesivine is used for the temporary relief of nasal (of the nose) congestion or stuffiness caused by hay fever or other allergies, colds, or sinus trouble.
How safe is Nesivine?
Nesivine is safe to use topical nasal Nesivine with or without benzalkonium chloride for 10 days in patients with vasomotor rhinitis.
How does Nesivine work?
Nesivine works by narrowing the blood vessels in the nasal passages.
What are the common side effects of Nesivine?
Common side effects of Nesivine are include:
- burning
- stinging
- increased nasal discharge
- dryness inside the nose
- sneezing
- nervousness
- nausea
- dizziness
- headache
- difficulty falling asleep or staying asleep
Is Nesivine safe during pregnancy?
If you're suffering from a cold or allergies during pregnancy, nasal sprays are most likely safe to use. Nesivine, one of the most common active ingredients used in nasal spray decongestants, is generally considered safe to use during pregnancy.
Is Nesivine safe during breastfeeding?
No information exists on the use of Nesivine specifically during breastfeeding, very little should reach the infant through breastmilk because of the local administration and limited absorption into the maternal bloodstream.
Can I drink alcohol with Nesivine?
No interactions were found between Alcohol and Nesivine nasal.
How long does Nesivine stay in my system?
Effects on α receptors from systemically absorbed Nesivine hydrochloride may persist for up to 7 hours after a single dose. The elimination half-life in humans is 5–8 hours.
How often can I take Nesivine?
Nesivine comes as a solution to spray into the nose. It is usually used every 10 to 12 hours as needed, but not more often than twice in a 24-hour period.
How long can I take Nesivine?
Do not use Nesivine nasal spray for longer than 3 days.
Who should not take Nesivine?
Tell your doctor if you have or have ever had high blood pressure, diabetes, difficulty urinating due to an enlarged prostate gland, or thyroid or heart disease. tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding.
Is Nesivine safe for heart patients?
Most topical nasal decongestants also carry the warning against use by patients with heart disease and high blood pressure, due to the possibility that some of the chemical might be absorbed and reach blood levels that would endanger their health.
What happens if I miss a dose?
Use the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose.
What happens if I overdose?
Seek emergency medical attention if anyone has accidentally swallowed the medication. Keep Nesivine nasal out of the reach of children. Certain nasal medications can cause serious medical problems in a young child who accidentally sucks on or swallows medicine from the nasal spray bottle.
Is Nesivine bad for my health?
Nesivine may also cause some other unwanted effects if used for long: Temporary burning, stinging, and dryness in the nose. Runny nose and sneezing. Slow/fast/pounding heartbeat.
Does Nesivine raise blood sugar?
Since these nasal sprays are less fully absorbed into the bloodstream than are the oral agents, they should have less effect on blood sugar levels.
Why are Nesivine bad for my heart?
Nesivine can also abnormally stimulate the heart and blood vessels throughout the body.
Does high blood pressure cause insomnia?
Hypertension and insomnia are very common and often coexist.
