Axivate
Axivate Uses, Dosage, Side Effects, Food Interaction and all others data.
Axivate is a synthetic trifluorinated corticosteroid with potent anti-inflammatory activity. Like other corticosteroids Axivate is found to have a wide range of actions on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (e.g.- histamine, eicosanoids, leukotrienes, cytokines) involved in inflammation.
Systemically, in vitro experiments show fluticasone furoate activates glucocorticoid receptors, inhibits nuclear factor kappa b, and inhibits lung eosinophilia in rats.
| Trade Name | Axivate |
| Generic | Fluticasone Furoate |
| Fluticasone Furoate Other Names | Fluticasone furoate, Fluticasonum furoas, Furoate de fluticasone, Furoato de fluticasona |
| Type | Cream |
| Formula | C27H29F3O6S |
| Weight | Average: 538.576 Monoisotopic: 538.163693965 |
| Protein binding | Fluticasone furoate is >99% protein bound in serum and may be as high as 99.6%. |
| Groups | Approved |
| Therapeutic Class | Nasal Steroid Preparations |
| Manufacturer | Aurz Pharmaceuticals Pvt Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Axivate nasal spray is used for the treatment of the symptoms of seasonal and perennial allergic rhinitis in patients aged 2 years and older.
Axivate is also used to associated treatment for these conditions: Asthma, Bacterial Sinusitis, Chronic Obstructive Pulmonary Disease (COPD), Chronic Sinusitis, Perennial Allergic Rhinitis (PAR), Seasonal Allergic Rhinitis
How Axivate works
Fluticasone furoate works through an unknown mechanism to affect the action of various cell types and mediators of inflammation. In vitro experiments show fluticasone furoate activating glucocorticoid receptors, inhibiting nuclear factor kappa b, and inhibiting lung eosinophilia in rats.
Dosage
Axivate dosage
Adults & Children over 12 years: 2 sprays in each nostril once a day. In some cases 2 sprays into each nostril twice daily, not exceeding 4 sprays.
Children under 12 years (2-11 Years): 1 spray in each nostril once a day. Patients should use Axivate nasal spray at regular intervals as directed since its effectiveness depends on its regular use.
Children (under 2 years of age): There are no data to recommend use of Axivate Nasal Spray for the treatment of seasonal or perennial allergic rhinitis in children under 2 years of age.
How to use the Nasal Spray
- Shake the bottle gently and remove the dust cover.
- Hold the spray with your forefinger and middle finger on either side of the nozzle and your thumb underneath the bottle. If using for the first time or if you have not used it for a week or more, press the nasal applicator several times until a fine mist comes out from the container.
- Gently blow the nose to clear the nostrils.
- Close one nostril and carefully insert the nasal applicator into the open nostril. Tilt your head forward slightly and keep the spray upright. Breathe in through your nose and while breathing in, press the white collar of nasal applicator firmly down once to release a spray.
- Breathe out through your mouth.
- Repeat the above steps in the same/other nostril for consecutive doses.
Side Effects
Eosinophilic conditions, adrenal insufficiency, growth retardation, Cushing's syndrome, decreased bone density, cataract, glaucoma. Rarely, psychological effects.
Toxicity
Fluticasone furoate administered nasally may be associated with adrenal suppression or an increase in QTc interval though the association has not been well demonstrated in studies. Fluticasone furoate requires no dosage adjustment in renal impairment but must be used in caution in hepatic impairment due to the elimination mechanisms. Fluticasone furoate is not associated with carcinogenicity, mutagenicity, or impairment of fertility. There are no well controlled studies in pregnancy or lactation though animal studies have shown teratogenicity and hypoadrenalism in the offspring of treated mothers and other corticosteroids are known to be excreted in breast milk. Generally, there are no reported adverse effects with fluticasone in pregnancy. Pediatric patients should be given the lowest possible dose and monitored for reduction in growth velocity. There is insufficient evidence to determine whether geriatric patients respond differently to other patients. Systemic exposure may be 27-49% higher in Japanese, Korean, and Chinese patients compared to Caucasian patients. Caution should be exercised in these patients and the benefit and risk should be assessed before deciding on a treatment.
Precaution
Patients taking Axivate nasal spray should be periodically monitored for signs of adverse effects on the nasal mucosa such as epistaxis, nasal ulceration and impaired wound healing. Avoid using the drug in patients with recent nasal ulcers, nasal surgery, or nasal trauma. Closely monitor patients with a history of increased intraocular pressure, glaucoma and hypersensitivity reactions (including anaphylaxis, angioedema, rash, and urticaria). Besides, potential worsening of existing fungal, bacterial, viral, or parasitic infections or ocular herpes simplex, hypercorticism and growth retardation may occur after the administration of Axivate nasal spray.
Interaction
Potent inhibitors of cytochrome P450 3A4 (CYP3A4) may increase exposure to Axivate. Coadministration of ritonavir is not recommended. Use caution with coadministration of other potent CYP3A4 inhibitors, such as ketoconazole.
Special instruction: Patients should be instructed that the device must be primed: before first use, and if the cap is left off or if the device does not seem to be working or if the nasal spray has not been used for 30 days or more. In order to prime the device, the nasal spray needs to be shaken vigorously for about 10 seconds with the cap on. The patient must then press the button firmly all the way in, approximately 6 times until a fine mist is seen. Once primed, the patient must shake the nasal spray vigorously each time before use.
Food Interaction
No interactions found.Volume of Distribution
608L at steady state for intravenous administration of fluticasone furoate. Other reports suggest the mean volume of distribution at steady state is 661L. A study of 24 healthy Caucasian males showed a volume of distribution at steady state of 704L following intravenous administration.
Elimination Route
Intranasal exposure of fluticasone furoate results in patients swallowing a larger portion of the dose. However, absorption is poor and metabolism is high, therefore there is negligible systemic exposure with a nasal bioavailability of 0.50% and oral bioavialability of 1.26%. Inhaled bioavailability is 13.9%. A study of 24 healthy Caucasian males showed an inhaled bioavailability of 6.3-18.4%.
Half Life
15.1 hours for intranasal fluticasone furoate and 24 hours for the inhaled formulation. A study of 24 healthy Caucasian males showed a half life of 13.6 hours following intravenous administration and 17.3-23.9 hours followed inhalation.
Clearance
57.8L/h for fluticasone furoate. A study of 24 healthy Caucasian males showed a clearance of 71.8L/h following intravenous administration.
Elimination Route
Fluticasone furoate is eliminated ≥90% in the feces and 1-2% in the urine.
Pregnancy & Breastfeeding use
Pregnancy: Plasma Axivate concentrations were typically non-quantifiable and therefore potential for reproductive toxicity is expected to be very low.
Lactation: The excretion of Axivate into human breast milk has not been investigated.
Contraindication
Axivate nasal spray is contraindicated in patients with a hypersensitivity to any of its ingredients.
Special Warning
Pediatric use: The safety and effectiveness of Axivate in children younger than 2 years have not been established.
Geriatric use: In general, dose selection for the elderly patient should be cautious, keeping in mind the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Use in hepatic impairment: Use Axivate with caution in patients with severe hepatic impairment.
Use in renal impairment: No dosage adjustment is required in patients with renal impairment.
Storage Condition
- Store at a temperature not exceeding 30 °C.
- Do not refrigerate.
- Protect from light and moisture.
- Keep out of the reach of children.
Innovators Monograph
You find simplified version here Axivate
Axivate contains Fluticasone Furoate see full prescribing information from innovator Axivate Monograph, Axivate MSDS, Axivate FDA label
FAQ
What is Axivate used for?
Axivate is used to treat seasonal and year-round allergy symptoms such as stuffy/runny nose, itching, and sneezing. It may also reduce other symptoms of seasonal allergies such as red, itchy, and watery eyes. It is also available as an inhaled corticosteroid to help prevent and control symptoms of asthma.
How safe is Axivate?
Axivate was well tolerated. The incidence of most AEs was similar to that observed with placebo, with the exception of epistaxis, which was more frequently reported on active treatment.
How does Axivate work?
Axivate works on your immune system to reduce the symptoms of inflammatory conditions and allergic reactions such as swelling, redness and itching. The nasal spray reduces swelling and mucus in your nose. It can take a little longer to work than antihistamine nasal sprays but the effects last for longer.
What are the common side effects of Axivate?
Common side effects of Axivate are include:
- throat irritation.
- dryness of the nose.
- nasal passage irritation.
- headache.
- nosebleed.
Is Axivate safe during pregnancy?
Axivate is safe if they are used at the recommended therapeutic dose after a proper medical evaluation.
Is Axivate safe during breastfeeding?
Expert opinion considers inhaled, nasal and oral corticosteroids acceptable to use during breastfeeding.
Can I drink alcohol with Axivate?
Yes, you can drink alcohol while taking Axivate.
How long does Axivate take to work?
You will not notice an immediate improvement in your symptoms when you first start using Axivate nasal spray. This is because it takes a few days for Axivate to take full effect. Tell your doctor if you feel no better after using the spray for 7 days.
How long does Axivate stay in my system?
Most inhaled steroids have a beneficial effect for 12 hours. The exceptions are Arnuity Ellipta, Asmanex, and Trelegy Ellipa, which last for 24 hours.
When should be taken of Axivate?
The same total daily dose, 1 spray in each nostril administered twice daily (e.g., 8 a.m. and 8 p.m.) is also effective. After the first few days, patients may be able to reduce their dose to 1 spray in each nostril once daily for maintenance therapy.
How long can I take Axivate?
This is usually between 1 and 3 months. If you are prescribed fluticasone nasal spray, your doctor may advise you to use it for longer. If you are using Axivate drops to shrink nasal polyps, your doctor will tell you how long to use them for. It will usually be for several weeks.
How much Axivate can I take in a day?
Adults, The recommended starting dosage in adults is 2 sprays (50 mcg of Axivate each) in each nostril once daily (total daily dose, 200 mcg). The same total daily dose, 1 spray in each nostril administered twice daily (e.g., 8 a.m. and 8 p.m.) is also effective.
Who should not take Axivate?
You should not use Axivate nasal if you are allergic to it. Axivate can weaken your immune system, making it easier for you to get an infection or worsening an infection you already have or recently had.
What happens if I miss a dose?
If you are using this product on a regular schedule and miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Use your next dose at the regular time. Do not double the dose to catch up.
What happen if I overdose on Axivate?
If you take too much Axivate, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away. If Axivate is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur.
What happen If I stop taking Axivate?
If you suddenly stop taking the drug, you may also have withdrawal symptoms (such as weakness, weight loss, nausea, muscle pain, headache, tiredness, dizziness). To help prevent withdrawal, your doctor may slowly lower the dose of your old medication after you begin using Axivate.
Can Axivate cause heart problems?
Axivate often contain vasoconstrictors that narrow your blood vessels, which can cause heart problems with long-term, frequent use.
Can Axivate affects my liver?
Long term use of these chemical sprays can also damage the liver and other vital organs.
Is Axivate bad for my kidneys?
Axivate Allergy Relief has a well-established safety profile. Axivate Allergy Relief is not associated with Higher blood pressure and is not contraindicated in patients with hypertension, heart disease, diabetes, liver disease, or kidney disease.
Can Axivate make me gain weight?
Axivate are generally not associated with weight gain.
Is Axivate safe to use everyday?
Use Axivate every day as full effectiveness is usually achieved after 3 or 4 days of continuous use.
