Active ingredients: Fluocinolone (fluocinolone acetonide), Clonazoline (clonazoline hydrochloride)
Locrinolyn 0.01% + 0.02% nasal spray, solution
Why is Locrinolyn used? What is it for?
What is Locrinolyn and what is it for
Locrinolyn contains two active ingredients: fluocinolone acetonide and clonazoline hydrochloride. Fluocinolone acetonide belongs to a group of medicines called "corticosteroids" and works against inflammation (anti-inflammatory) and allergies (anti-allergic); it is specific for local use. Clonazoline hydrochloride belongs to a group of medicines called "nasal decongestants" and works by decreasing the size of the blood vessels at the place of application (vasoconstrictor).
Locrinolyn is used for the local treatment of inflammatory allergic and vasomotor diseases of the nasal and paranasal cavities, such as:
- common cold and inflammation of the inner lining of the nose with phlegm (catarrhal rhinitis)
- inflammation of the inner wall of the nose due to allergy and excessive sensitivity problems (allergic and vasomotor rhinitis)
- accumulation of phlegm in the ear (tubal phlegm)
- inflammation of the nose and bony cavities near the nose with phlegm (catarrhal sinusitis and rhinosinusitis)
- inflammation of the nose and bony cavities near the nose due to allergy and excessive sensitivity problems (sinusitis and allergic and vasomotor rhinosinusitis)
- inflammation of the nose and bony cavities near the nose with drop-shaped nodules inside the nose (rhinitis, sinusitis and polyposis ethmoiditis)
- respiratory disorders due to deviation of the nose bone (nasal septum) or to the increase in volume (hypertrophy) of the fleshy formations contained inside the nostrils (turbinates).
Contraindications When Locrinolyn should not be used
Do not use Locrinolyn
- if you are allergic to the active substances or any of the other ingredients of this medicine (listed in section 6)
- if you are allergic to medicines of the same class as fluocinolone acetonide and clonazoline hydrochloride
- if you have a skin disease characterized by reddish-brown lesions and plaques (cutaneous tuberculosis), infections caused by the Herpes simplex virus and other diseases caused by viruses localized on the skin (smallpox, chicken pox, etc.)
- if you are a child under the age of 12.
Precautions for use What you need to know before taking Locrinolyn
What you need to know before you use Locrinolyn
Using Locrinolyn for long periods can cause allergic reactions and irritation. In these cases, contact your doctor who will stop the treatment and prescribe a suitable therapy.
Talk to your doctor if:
- you have an infection caused by microbes or fungi (mycotic). In this case your doctor may associate a specific treatment with Locrinolyn. If you do not get a result quickly, your doctor may advise you to stop using Locrinolyn until when it does not recover from the infection
- develop an "infection affecting the whole organism (systemic) or an" infection caused by non-sensitive microbes. In this case, your doctor will recommend appropriate therapy
- have heart or blood vessel disease (cardiovascular), and especially if you have high blood pressure (you are hypertensive). In this case the doctor will evaluate from time to time whether the use of Locrinolyn is appropriate.
Prolonged use of preparations containing medicines that constrict blood vessels (vasoconstrictors) can alter the normal function of the inner wall (mucous membrane) of the nose and nearby bony cavities (sinuses), leading to a reduction or loss of the effectiveness of the medicine (addiction).
Repeating the applications of Locrinolyn for long periods can be harmful.
Use Locrinolyn as directed in the package leaflet or as prescribed by your doctor. Only use the dose of medicine recommended by your doctor; the use of higher or lower doses can cause worsening of symptoms.
Avoid contact with eyes.
Interactions Which drugs or foods can modify the effect of Locrinolyn
Other medicines and Locrinolyn
Tell your doctor or pharmacist if you are using, have recently used or might use any other medicines.
Locrinolyn should be used with caution in patients being treated with a class of medicines used to treat depression (MAO inhibitors), to avoid sudden crises due to high blood pressure (hypertensive crisis).
Clonazoline, one of the two active ingredients of Locrinolyn, can enhance the effect of sedative medicines on the nervous system
Warnings It is important to know that:
Warnings and Precautions
Talk to your doctor or pharmacist before using Locrinolyn.
Children
The use of Locrinolyn is contraindicated in children under 12 years of age.
Pregnancy and breastfeeding
If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before using this medicine.
Pregnancy
During pregnancy, your doctor will prescribe Locrinolyn only in cases of real need and under his direct control.
Feeding time
If you are breast-feeding, your doctor will consider whether to discontinue breast-feeding or treatment with Locrinolyn.
While breastfeeding, your doctor will prescribe Locrinolyn only in cases of real need and under your direct control.
Driving and using machines
Clonazoline, one of the two active ingredients of Locrinolyn, can perform a sedative action and therefore the possibility of modifying the reaction times cannot be excluded.
Therefore use the medicine with caution if you drive or use machines.
Locrinolyn contains
- propylene glycol which can cause skin irritation
- benzalkonium chloride (BAC) which can cause the bronchial volume to shrink (bronchospasm). BAC contained as a preservative in Locrinolyn especially when used for long periods, can cause swelling of the inner wall of the nose (nasal mucosa). If such a reaction (persistent nasal congestion) is suspected, a BAC-free nasal medicine should be used if possible. If such nasal medications without BAC are not available, another pharmaceutical form should be considered.
Dose, Method and Time of Administration How to use Locrinolyn: Posology
How to use Locrinolyn
Always use this medicine exactly as your doctor or pharmacist has told you. If in doubt, consult your doctor or pharmacist.
The recommended dose is:
- Adults: 1-2 sprays per nostril 2-3 times a day.
- Teenagers (12-18 years old): 1 spray per nostril 1-2 times a day.
Use in children
The use of Locrinolyn is contraindicated in children under 12 years of age
If you forget to use Locrinolyn
Do not use a double dose to make up for a forgotten dose.
If you stop taking Locrinolyn
If you have any further questions on the use of this medicine, ask your doctor or pharmacist.
Overdose What to do if you have taken too much Locrinolyn
If you use more Locrinolyn than you should
Any overdose of Locrinolyn can produce sedation.
The excessive or prolonged use of corticosteroids for local use, medicines belonging to the same family as Locrinolyn, can cause a reduced activity of some glands of the body (pituitary and adrenal glands, causing secondary hypoadrenalism) and manifestations of hypercorticism (increased production of hormones adrenal cortex) including:
- a disease characterized by "excessive production of a hormone called cortisol (Cushing's syndrome)
- decreased muscle strength (asthenia)
- weakness (adynamia)
- high blood pressure (arterial hypertension)
- changes in heart rhythm (heart rhythm disturbances)
- decreased potassium in the blood (hypokalaemia)
- increase of acids in the blood (metabolic acidosis).
If you accidentally take an overdose of Locrinolyn, notify your doctor immediately or go to the nearest hospital.
Side Effects What are the side effects of Locrinolyn
Possible side effects
Like all medicines, this medicine can cause side effects, although not everybody gets them.
Occasionally they can occur:
- burning sensation
- itch
- irritation and dryness of the inner walls of the nose (nasal mucous membranes)
In case of very prolonged treatments, reduction (atrophy) of the internal walls of the nose (nasal mucous membranes) may occur. Side effects that may affect the whole body (systemic) are very rare, as the active ingredients are contained in the medicine in very low doses. These effects can occur with corticosteroids administered inside the nose (intranasal), in particularly when prescribed in high doses for prolonged periods, and may include growth retardation in children and adolescents.
Reporting of side effects
If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. You can also report side effects directly via the national reporting system at www.agenziafarmaco.it/it/responsabili. By reporting side effects you can help provide more information on the safety of this medicine.
Expiry and Retention
Do not store above 30 ° C.
After first opening the bottle and inserting the dispenser, the medicine should be used within 3 months. After this date, any excess medicine should be discarded.
Keep this medicine out of the sight and reach of children.
Do not use this medicine after the expiry date which is stated on the carton after "Expiry". The expiry date refers to the last day of that month.
Do not throw any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. This will help protect the environment.
Contents of the pack and other information
What Locrinolyn contains
- The active ingredients are fluocinolone acetonide and clonazoline hydrochloride. 100 ml of solution contain 10 mg of fluocinolone acetonide and 20 mg of clonazoline hydrochloride. One spray contains 0.006 mg of fluocinolone acetonide and 0.012 mg of clonazoline hydrochloride.
- The other ingredients are citric acid, benzalkonium chloride, polyethylene glycol 4000, propylene glycol, purified water.
What Locrinolyn looks like and contents of the pack
Locrinolyn comes in the form of a nasal spray, solution.
The contents of the package are a 20 ml bottle with dispenser.
Source Package Leaflet: AIFA (Italian Medicines Agency). Content published in January 2016. The information present may not be up-to-date.
To have access to the most up-to-date version, it is advisable to access the AIFA (Italian Medicines Agency) website. Disclaimer and useful information.
01.0 NAME OF THE MEDICINAL PRODUCT
LOCRINOLYN 0.01% + 0.02% NASAL SPRAY, SOLUTION
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
100 ml of solution contain 10 mg of fluocinolone acetonide and 20 mg of clonazoline hydrochloride.
One spray contains 0.006 mg of fluocinolone acetonide and 0.012 mg of clonazoline hydrochloride.
Excipients with known effects:
100 ml of solution contain 0.02 g of benzalkonium chloride, 3 g of propylene glycol.
For the full list of excipients, see section 6.1.
03.0 PHARMACEUTICAL FORM
Nasal spray, solution.
04.0 CLINICAL INFORMATION
04.1 Therapeutic indications
Local treatment of allergic and vasomotor inflammatory diseases of the nasal and paranasal cavities, such as: common cold and catarrhal rhinitis in general, allergic and vasomotor rhinitis, tubal catarrh, catarrhal sinusitis and rhinosinusitis, allergic and vasomotor sinusitis and rhinosinusitis, rhinitis, sinusitis and polypous ethmoiditis , respiratory disorders from deviation of the nasal septum or from hypertrophy of the turbinates.
04.2 Posology and method of administration
Dosage
Adults: 1-2 sprays per nostril, 2-3 times a day.
Teenagers (ages 12-18): 1 spray per nostril, 1-2 times a day.
Pediatric population
Locrinolyn is contraindicated in children below 12 years of age (see section 4.3).
04.3 Contraindications
Hypersensitivity to the active substances or to any of the excipients listed in section 6.1 or to other closely related substances from a chemical point of view.
Infections from cutaneous tuberculosis and Herpes Simplex, as well as from viral diseases with skin localization (smallpox, chicken pox, etc.).
Children under the age of 12.
04.4 Special warnings and appropriate precautions for use
The use, especially if prolonged, of products for local use, can give rise to sensitization phenomena or irritation. In this case it is necessary to interrupt the treatment and institute a suitable therapy.
In the presence of a "possible microbial or fungal component, it is advisable to associate a specific treatment with Locrinolyn.
In case of development of systemic infection, appropriate coverage therapy should be instituted; likewise in the case of the development of non-sensitive microorganisms.
If a response is not obtained quickly, discontinue corticosteroid treatment until the infection is adequately controlled.
In patients with cardiovascular diseases, and especially in hypertensive patients, the use of nasal decongestants must be subjected to the judgment of the physician from time to time.
The prolonged use of preparations containing vasoconstrictors can alter the normal function of the mucous membrane of the nose and paranasal sinuses, also inducing addiction to the drug.
Repeating the applications of Locrinolyn nasal spray for long periods can be harmful.
Any of the undesirable effects described for systemic corticosteroids, including hypoadrenalism, can also occur with locally used corticosteroids.
Systemic effects may occur with intranasal corticosteroids, particularly when prescribed in high doses for prolonged periods. These effects are less likely to occur than with oral corticosteroid treatment and may vary in individual patients and between different corticosteroid preparations. Possible systemic effects include Cushing's syndrome, Cushingoid aspect, adrenal suppression, growth retardation in children and adolescents, decreased bone mineral density, cataracts, glaucoma and, more rarely, a range of psychological or behavioral effects including psychomotor hyperactivity, disturbances sleep, anxiety, depression or aggression (particularly in children).
Regular monitoring of the height of children receiving prolonged intranasal corticosteroid treatment is recommended (see section 4.8).
Avoid contact with eyes.
Locrinolyn contains propylene glycol which can cause skin irritation.
Locrinolyn contains benzalkonium chloride which can cause bronchospasm. Benzalkonium chloride (BAC) contained as a preservative in Locrinolyn, especially when used for long periods, can cause swelling of the nasal mucosa. If such a reaction (persistent nasal congestion) is suspected, a BAC-free nasal medicine should be used if possible. If such nasal medications without BAC are not available, another pharmaceutical form should be considered.
04.5 Interactions with other medicinal products and other forms of interaction
Concomitant treatment with CYP3A inhibitors, including cobicistat-containing medicines, is thought to increase the risk of systemic side effects. The combination should be avoided unless the benefit outweighs the increased risk of systemic side effects due to corticosteroids, in which case patients should be monitored for the absence of systemic side effects due to corticosteroids.
Locrinolyn should be used with caution in patients treated with MAO inhibitors, to avoid sudden hypertensive crises.
Clonazoline can potentiate the effect of sedative drugs on the CNS.
04.6 Pregnancy and breastfeeding
During pregnancy and breastfeeding, the medicine should be administered in cases of real need, under the direct supervision of the doctor.
Pregnancy
The safety of corticosteroids for local use has not been established in pregnant women and, therefore, during pregnancy, the use of drugs belonging to this class should be limited to cases where the expected benefit justifies the potential risk to the fetus. In any case, in pregnant women, these drugs should not be used intensively at high doses and for long periods of time.
Feeding time
As it is not known whether local administration of corticosteroids can result in sufficient systemic absorption to produce measurable concentrations in breast milk, a decision must be made whether to discontinue breastfeeding or to discontinue therapy given the importance of the drug to the mother.
04.7 Effects on ability to drive and use machines
Clonazoline can have a sedative action; therefore the possibility of modifying the reaction times cannot be excluded.
Therefore, patients who have to wait while driving or using machines should use the medicine with caution.
04.8 Undesirable effects
Occasionally there may be: burning sensations, itching, irritation and dryness of the mucous membrane.
Very prolonged treatments can produce mucosal atrophy.
Systemic effects are extremely rare in consideration of the low doses of the active ingredients used.
Systemic effects may occur with intranasal corticosteroids, particularly when prescribed in high doses for prolonged periods. These can include growth retardation in children and adolescents.
Reporting of suspected adverse reactions
Reporting of suspected adverse reactions occurring after authorization of the medicinal product is important as it allows continuous monitoring of the benefit / risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system. "address www.agenziafarmaco.gov.it/it/responsabili.
04.9 Overdose
Symptoms
Any overdose can produce sedation.
Excessive or prolonged use of corticosteroids for local use can depress the adrenal pituitary function, causing secondary hypoadrenalism and manifestations of hypercorticism including Cushing's syndrome, in particular asthenia, adynamia, arterial hypertension, heart rhythm disturbances, hypokalemia, metabolic acidosis.
Treatment
& EGRAVE; appropriate symptomatic treatment indicated. Symptoms of acute hypercorticism are usually reversible. If necessary, treat the electrolyte imbalance. In the case of chronic toxicity, slow elimination of the corticosteroid is recommended.
05.0 PHARMACOLOGICAL PROPERTIES
05.1 Pharmacodynamic properties
Pharmacotherapeutic group: decongestants and other nasal preparations for topical use - corticosteroids - various combinations.
ATC code R01AD99.
Fluocinolone acetonide is a fluorinated steroid, with a remarkable anti-inflammatory, anti-allergic and anti-reactive action also at the level of the rhinosinusal mucous membranes. In the experimental inflammation tests, fluocinolone acetonide showed a significantly higher activity than hydrocortisone and most topical steroids. Fluocinolone acetonide is also very active in the vasoconstriction test. Optimal active concentrations are between 0.01. and 0.025%.
Clonazoline is an imidazole derivative with an intense peripheral vasoconstrictive and local decongestant action, with little systemic effect and practically no rebound effect.
05.2 Pharmacokinetic properties
Applied on the nasal mucosa, the action of fluocinolone acetonide is carried out locally: a transcutaneous absorption of steroid doses capable of depressing the pituitary-adrenal axis can occur only for quantities considerably higher than the therapeutic ones. The local activity / systemic activity ratio for fluocinolone acetonide is 10 to 20 times higher than that of hydrocortisone and other locally used steroids.
The presence of the vasoconstrictor further reduces the possibility of absorption.
Pharmacological experimentation indicates that the combination maintains the properties of the individual components and that the vasoconstrictor effect of clonazoline is increased and prolonged over time.
05.3 Preclinical safety data
Fluocinolone acetonide has very poor toxicity: oral LD50 in mice 3 g / kg. Oral doses of 0.05-0.125 mg / kg / day in dogs and 0.125-0.500 mg / kg / day in monkeys for 3 months produced no hormonal effects (adrenal hypotrophy) other than those expected. Good local tolerability (0.5 ml of 0.01% solution in the conjunctival sac of rabbit).
The fluocinolone acetonide / clonazoline combination shows oral LD50 in mice of 267 mg / kg.
Chronic oral toxicity tests in rats and dogs show only cortisone-type pharmacological effects, not influenced by the presence of clonazoline.
Preclinical data suggest that benzalkonium chloride is capable of producing a toxic effect - concentration and time dependent - on the vibrating cilia of the epithelium of the nasal mucosa, including irreversible immobility and can induce histopathological changes of the nasal mucosa.
06.0 PHARMACEUTICAL INFORMATION
06.1 Excipients
Citric acid
Benzalkonium chloride
Polyethylene glycol 4000
Propylene glycol
Purified water.
06.2 Incompatibility
None known.
06.3 Period of validity
3 years.
After first opening the bottle and inserting the dispenser, the medicine should be used within 3 months. After this date, any excess medicine should be discarded.
06.4 Special precautions for storage
Do not store above 30 ° C.
06.5 Nature of the immediate packaging and contents of the package
Glass bottle fitted with a sealed aluminum screw cap. 20 ml bottle with dispenser.
06.6 Instructions for use and handling
No special instructions.
Unused medicine and wastes derived from this medicine must be disposed of in accordance with local regulations.
07.0 MARKETING AUTHORIZATION HOLDER
RECORDATI Chemical and Pharmaceutical Industries S.p.A. - Via M. Civitali, 1 - 20148 Milan.
08.0 MARKETING AUTHORIZATION NUMBER
Locrinolyn 0.01% + 0.02% nasal spray, solution - bottle with dispenser 20 ml A.I.C. n. 039636016
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION
Date of first authorization: January 16, 1965
Date of most recent renewal: May 31, 2010
10.0 DATE OF REVISION OF THE TEXT
27/03/2017
