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Doc: is it safe to use my Nasal spray in the long run?


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Many of us suffer from Allergic Rhinitis (sinus) and use intra nasal steroid sprays on a daily basis.


How safe are these to use for the long term? Are there any risks? How about for my children? Do such steroid sprays affect their growth and well being?


Well, let's delve deeper into this topic, shall we?



Q: What are the different types of Nasal Sprays available?


Well, there are many types available on the market, both on and off-prescription, with a wide selection available to you.


Nasal sprays are useful dosage forms that yield medical benefits by allowing our patients to place / spray medications inside the nasal cavity, directly where they are needed.


There are four types of nonprescription nasal sprays in common use—corticosteroids, nasal decongestants, sodium chloride, and cromolyn sodium.

these are generally:


1. Intranasal corticosteroids (INCS)

2. Anti-histamine

3. Decongestants eg Oxymetazoline

4. Cromolyn sodium


and various combinations of the above. In Singapore, patients need a prescription to obtain INCS.


Many patients use topical nasal decongestant drops or sprays eg AFRIN for acute respiratory infections or the common cold.

Image of an Oxymetazoline nasal spray courtesy of Afrin website


It is important to note that such decongestant sprays / drops are NOT used for more than 3 days duration. Prolonged use may result in rebound rhinitis and other unwanted side effects.


Oxymetazoline AFRIN comes as a solution (liquid) 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.


Do not use more or less of it or use it more often than prescribed by your doctor or directed on the label.


If you use oxymetazoline nasal spray for more often or for longer than the recommended period of time, your congestion may get worse or may improve but come back. Do not use oxymetazoline nasal spray for longer than 3 days.


Most commonly used in Singapore, are the Intranasal corticosteroids (INCS)


Q: What are intranasal corticosteroids (INCS) ?

Intranasal corticosteroids (INCS) sprays are accepted as safe and effective first-line therapy for allergic rhinitis. Several intranasal corticosteroids are available: beclomethasone dipropionate, budesonide, flunisolide, fluticasone propionate, mometasone furoate, and triamcinolone acetonide.


All are efficacious in treating seasonal allergic rhinitis and as prophylaxis for perennial allergic rhinitis. In general, they relieve nasal congestion and itching, rhinorrhea, and sneezing that occur in the early and late phases of allergic response, with studies showing almost complete prevention of late-phase symptoms.


The rationale for topical intranasal corticosteroids (INCS) in the treatment of allergic rhinitis is that adequate drug concentrations can be achieved at receptor sites in the nasal mucosa. This leads to symptom control and reduces the risk of systemic adverse effects. Adverse reactions usually are limited to the nasal mucosa, such as dryness, burning and stinging, and sneezing, together with headache and epistaxis in 5-10% of patients regardless of formulation or compound.


Differences among agents are limited to potency, patient preference, dosing regimens, and delivery, device and vehicle.


Q: How do I select the intranasal corticosteroid (INCS) spray for myself?

Intranasal corticosteroids (INCS) can be categorised based on their generation. The older, first generation INCSs (beclomethasone dipropionate, triamcinolone acetonide, flunisolide, budesonide) have a significantly higher systemic bioavailability than the second generation INCSs (ciclesonide, fluticasone furoate, fluticasone propionate, mometasone furoate)


Characteristics of the nasal mucosa can also alter your selection of INCS. The presence, or absence, of nasal secretions affects how the INCS is absorbed. Movement of nasal cilia can become impaired if the sol layer of mucous is too thin, or too thick. This affects the permeability of the steroid, as muco-ciliary clearance is altered, and duration of contact between the steroid and nasal mucosa is decreased. To counteract this, selection of an INCS that alters the viscosity within the nose, can increase contact time and overall diffusion of the steroid. For example, in a “dry” congested nose, ciclesonide is favoured. Ciclesonide is a hypotonic solution, resulting in rapid diffusion water molecules into the nasal mucosa of a dry nose. The difference in osmolarity increases the viscosity within the nose, thus increasing contact time.


Nasonex:

Image of Nasonex Allergy intranasal corticosteroid nasal spray from Nasonex website


A similar principle can be seen for a “wet” congested nose. In this case, mometasone furoate and budesonide (Rhinocort Turbuhaler) are recommended. Mometasone furoate (Nasonex) contains the highest concentration of microcrystalline cellulose and carboxy-methylcellulose sodium for aqueous INCS. These are thixotropic agents, which dry and increase viscosity within the nasal cavity. Rhinocort Turbuhaler also dries the nose, secondary to its dry powered formulation, but as of February 2020 has been discontinued by the manufacturer. Both steroids increase viscosity, while decreasing moisture within the nasal cavity.


Fluticasone : Flixonase & Avamys

Photo of Avamys nasal spray


Although fluticasone is the backbone of both fluticasone furoate (FF - Avamys) and fluticasone propionate (FP - Flixonase), one should be cognisant that their efficacies are not equivalent. The two molecules are relatively similar in structure, only differing in the esters attached to the 17α-OH group. Esterified furoate and propionic acid are found at this location for fluticasone furoate and fluticasone propionate, respectively. When metabolised, fluticasone is not released from the ester substituent, which affects target receptor binding. The ester side-chain of fluticasone furoate is much larger than that of fluticasone propionate. This structural difference allows fluticasone furoate to bind to the glucocorticoid receptor with a higher affinity. Valotis et al. report that fluticasone furoate has a relative receptor affinity ratio (in comparison to dexamethasone) of 2989, while fluticasone propionate has an affinity of 1775. Clinically, this results in superior efficacy for fluticasone furoate (Avamys) INCS.


Dymista Spray:

Image of Dymista nasal spray from Dymista website


Fluticasone propionate-azelastine (Dymista) is unique. Produced in 2012, it combines the therapeutic effects of a corticosteroid and an antihistamine. Fluticasone-azelastine is effective in treating severe seasonal allergic rhinitis refractory to steroid or antihistamine treatment alone. The combination spray results in an incremental improvement of around 1 over and above FP on the Total Nasal Symptom Score (TNSS), and doubles the small reduction seen on the Total Ocular Symptom Score (TOSS) with FP alone. Dymista achieved a reduction of TNSS to one or less in 12% of patients, versus 9.5% for FP, and had 35% of patients achieve a 50% reduction in TNSS by day 7, versus day 9 for INCS alone and day 11 for azelastine. The bioavailability of the fluticasone component is low, but is 44–61% higher than monotherapy FP. This is a negligible difference as the bioavailability of monotherapy FP is < 0.5%. Adverse effects are rare (< 5%), and have a similar side effect profile to other INCSs . Given the cost-benefit ratio, it generally should be reserved as a second line therapy after failure of another INCS.


Q: What are the possible side effects of steroid nasal sprays?

Steroid nasal sprays do not usually cause any significant side effects if used correctly and at normal doses.


Side effects can include:

  • a stinging or burning sensation in the nose

  • dryness and crustiness in the nose

  • a dry, irritated throat

  • an unpleasant taste in the mouth

  • itchiness, redness and swelling in the nose

  • nosebleeds

If you're taking a high dose for a long time, there's also a small chance you could get some of the side effects of steroid tablets, such as increased appetite, mood changes and difficulty sleeping.


Conclusion:


In the final selection of your INCS, you may want to consult / discuss with your GP or ENT Specialist. They may be able to take a deeper discussion and also see any possible drug interactions with your other medications.


You can also book an appointment with us at Euan's ENT Surgery & Clinic to consult Dr Euan and find out more about which nasal spray may be suitable for you.


Have a healthy and happy weekend ahead :-)


Here are some useful references you may want to look up for more information on INCS

References:

1. Ezer N, Belga S, Daneman N, et al. Inhaled and intranasal ciclesonide for the treatment of covid-19 in adult outpatients: CONTAIN phase II randomised controlled trial. Bmj 2021;375:e068060. doi: 10.1136/bmj-2021-068060 [published Online First: 2021/11/04]

2. Lipworth BJ, Chan R, Carr T. Corticosteroid Protection Against COVID-19: Begin with the Nose. J Allergy Clin Immunol Pract 2021;9(11):3941-43. doi: 10.1016/j.jaip.2021.08.025 [published Online First: 2021/10/14]

3. Strauss R, Jawhari N, Attaway AH, et al. Intranasal Corticosteroids Are Associated with Better Outcomes in Coronavirus Disease 2019. J Allergy Clin Immunol Pract 2021;9(11):3934-40 e9. doi: 10.1016/j.jaip.2021.08.007 [published Online First: 2021/08/27]

4. Lee DK, Fardon TC, Bates CE, et al. Airway and systemic effects of hydrofluoroalkane formulations of high-dose ciclesonide and fluticasone in moderate persistent asthma. Chest 2005;127(3):851-60. doi: 10.1378/chest.127.3.851 [published Online First: 2005/03/15]

5. Lipworth BJ, Kaliner MA, LaForce CF, et al. Effect of ciclesonide and fluticasone on hypothalamic-pituitary-adrenal axis function in adults with mild-to-moderate persistent asthma. Annals of Allergy, Asthma and Immunology 2005;94(4):465-72.

6. Yu LM, Bafadhel M, Dorward J, et al. Inhaled budesonide for COVID-19 in people at high risk of complications in the community in the UK (PRINCIPLE): a randomised, controlled, open-label, adaptive platform trial. Lancet 2021;398(10303):843-55. doi: 10.1016/S0140-6736(21)01744-X [published Online First: 2021/08/14]

7. Daley-Yates P, Brealey N, Thomas S, et al. Therapeutic index of inhaled corticosteroids in asthma: A dose-response comparison on airway hyperresponsiveness and adrenal axis suppression. Br J Clin Pharmacol 2020 doi: 10.1111/bcp.14406 [published Online First: 2020/06/03]

8. Wilson AM, Lipworth BJ. Dose-response evaluation of the therapeutic index for inhaled budesonide in patients with mild-to-moderate asthma. Am J Med 2000;108(4):269-75. doi: 10.1016/s0002-9343(99)00435-0 [published Online First: 2000/10/03]

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