Arquist 250 mikrogram/dos Inhalationsspray, suspension

Sverige - svenska - Läkemedelsverket (Medical Products Agency)

Bipacksedel Bipacksedel (PIL)

21-06-2018

Produktens egenskaper Produktens egenskaper (SPC)

20-04-2018

Aktiva substanser:
flutikasonpropionat
Tillgänglig från:
Cipla Europe NV,
ATC-kod:
R03BA05
INN (International namn):
fluticasone propionate
Dos:
250 mikrogram/dos
Läkemedelsform:
Inhalationsspray, suspension
Sammansättning:
flutikasonpropionat 250 mikrog Aktiv substans
Receptbelagda typ:
Receptbelagt
Produktsammanfattning:
Förpacknings: Inhalator, 120 doser; Inhalator, 2 x 120 doser; Inhalator, 3 x 120 doser; Inhalator, 10 x 120 doser (sjukhusförpackning)
Bemyndigande status:
Godkänd
Godkännandenummer:
53660
Tillstånd datum:
2016-12-22

Dokument på andra språk

Bipacksedel Bipacksedel - engelska

01-03-2021

Produktens egenskaper Produktens egenskaper - engelska

30-11-2020

Offentlig bedömningsrapport Offentlig bedömningsrapport - engelska

06-03-2017

Läs hela dokumentet

Package leaflet: Information for the patient

Arquist 125 microgram per actuation pressurised inhalation, suspension

Arquist 250 microgram per actuation pressurised inhalation, suspension

fluticasone propionate

Read all of this leaflet carefully before you start using this medicine because it contains important

information for you.

Keep this leaflet. You may need to read it again.

If you have any further questions, ask your doctor, pharmacist or nurse.

This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even

if their signs of illness are the same as yours.

If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side

effects not listed in this leaflet. See section 4.

What is in this leaflet

What Arquist is and what it is used for

What you need to know before you use Arquist

How to use Arquist

Possible side effects

How to store Arquist

Contents of the pack and other information

1.

What Arquist is and what it is used for

This medicine contains the active substance fluticasone propionate which belongs to a group of medicines

called corticosteroids. Arquist works by reducing inflammation in the lungs. This helps to prevent asthma

attacks in people who need regular treatment. It takes 4-7 days for this medicine to work and it is very

important that you use it regularly also when you do not have symptoms.

Arquist is used for the regular treatment of asthma in adult and adolescents over 12 years of age.

2.

What you need to know before you use Arquist

Do not use Arquist

if you are allergic to fluticasone propionate or any of the other ingredients of this medicine (listed in

section 6).

Warnings and precautions

Stop using Arquist immediately

if you experience difficulty in breathing with immediate increase in wheezing just after taking a dose of

this medicine.

In this case, immediately use a short-acting bronchodilator inhaler.

Talk to your doctor, pharmacist or nurse before using Arquist

if you have ever been treated for tuberculosis (TB), viral, bacterial or fungal infections;

if you have a history of diabetes mellitus (because fluticasone may increase your blood sugar level);

if you have used high doses of this medicine for a long period of time and notice any of the following.

weight gain and a rounded (moon shaped) face (these could be signs of Cushing’s Syndrome);

vague symptoms such as tummy ache, sickness, diarrhoea, headache or drowsiness (adrenal

supression, acute adrenal crisis). This is more likely during an infection such as viral infection or

stomach upset;

thinning of the bones;

eyeproblems (cataract and glaucoma);

slowing of growth (mainly occurs in children and adolescents).

If you are not sure if any of the above applies to you, talk to your doctor, nurse or pharmacist before using

Arquist.

Contact your doctor if you experience blurred vision or other visual disturbances.

Do not use Arquist to relieve acute symptoms of asthma or a sudden asthma attacks. In this case you must

use a short-acting bronchodilator i. e. short-acting inhaled beta-2- agonist.

Children

Arquist is not intended for children below 12 years of age.

Other medicines and Arquist

Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines,

including medicines obtained without a prescription. In particular tell your doctor or pharmacist if you are

taking any of the following:

medicines used to treat different types of infections such as ritonavir, ketoconazole, clarithromycin,

telithromycin, atazanavir, indinavir, nelfinavir or saquinavir;

steroid tablets together with your Arquist inhaler or if you have just finished taking steroid tablets. You

should carry a steroid warning card as there is a possibility of impaired adrenal function, especially during

stressful circumstances (such as a serious accident or if you have surgery) and your doctor may decide to

give you extra steroid medicines during such a time

.

some medicines may increase the effects of Arquist and your doctor may wish to monitor you carefully if

you are taking these medicines (including some medicines for HIV: ritonavir, cobicistat)

If you are not sure if any of the above applies to you, talk to your doctor or pharmacist before using Arquist.

Pregnancy, breast-feeding and fertility

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.

Driving and using machines

Arquist is not likely to affect your ablility to drive or use any tools or machines.

3.

How to use Arquist

Arquist comes in two different strengths for oral inhalation use only.Your doctor will decide which strength

you need. Always use Arquist exactly as your doctor has told you. Check with your doctor, nurse or

pharmacist if you are not sure.

Using this medicine

Arquist may be used with the Volumatic spacer device by patients who find it difficult to release a puff

(actuation) of medicine just after they start to breathe in.

The starting dose needs to be appropriate considering the severity of the disease. Your doctor will work

with you to decrease your dose to the lowest dose that effectively controls your asthma.

Adults and adolescent patients over 12 years of age

The recommended dose is 125 micrograms to 500 micrograms twice daily.

Use in children

Arquist is not intended for children below 12 years of age.

If you are using high doses of an inhaled steroid for a long time you may sometimes need extra steroids, for

example during stressful circumstances such as a road traffic accident or before an operation.Your doctor

may decide to give you extra steroid medicines during this time.

Instructions for use

Your doctor, nurse or pharmacist should show you how to use your inhaler. They should check how you use

it from time to time. Not using the Arquist properly or as prescribed, may mean that the medicine will not

help your asthma as it should.

The medicine is contained in a pressurised canister in a plastic casing with a mouthpiece. To prevent your

inhaler from blocking, it is important to clean it at least once a week.

Testing your inhaler

When you use the inhaler for the first time, you should test if it works properly.

1

Remove the mouthpiece cover by gently squeezing the sides with your thumb and forefinger and pull

apart.

2

To make sure that it works, shake the inhaler well, point the mouthpiece away from you and press

the canister to release four puffs into the air. If you have not used the inhaler for a week or more,

release two puffs of medicine into the air.

How to use your inhaler

It is important to start to breathe as slowly as possible just before using your inhaler.

You should either stand up or sit upright when using your inhaler.

Remove the mouthpiece cover. Check inside and outside to make sure that the mouthpiece is clean

and free of objects (figure A).

Shake the inhaler 4 or 5 times to ensure that any loose objects are removed and that the contents of the

inhaler are evenly mixed (figure B).

Hold the inhaler upright with your thumb on the base, below the mouthpiece. Breathe out for as long

as is comfortable (figure C). Do not breathe in again yet.

Place the mouthpiece in your mouth between your teeth. Close your lips around it.

Do not bite (figure D).

Breathe in through your mouth. Just after starting to breathe in, press down on the top of the canister

to release a puff of medicine. Do this while still breathing in steadily and deeply (figure D).

Hold your breath, take the inhaler from your mouth and your finger from the top of the inhaler.

Continue holding your breath for a few seconds, or as long as comfortable (figure E).

If your doctor has told you to take two puffs, wait about half a minute before you take another puff by

repeating steps 3 to 7.

Afterwards, rinse your mouth with water and spit it out.This is to avoid side effects related to your

mouth or throat. You can also brush your teeth.

After using your inhaler always replace the mouthpiece cover straight away to keep out dust. Replace

the cover by firmly pushing and clicking into position.

Practise in front of a mirror for the first few times. If you see ‘mist’ coming from the top of your inhaler or

the sides of your mouth, you should start again.

Adolescents or people with weak hands may find it easier to hold the inhaler with both hands. Put the two

forefingers on top of the inhaler and both thumbs on the bottom below the mouthpiece.Your doctor, nurse or

pharmacist will advise you how to do this.

Cleaning your Inhaler

To prevent your inhaler from blocking, it is important to clean it at least once a week.

To clean your inhaler:

Remove the mouthpiece cover.

Do not remove the metal canister from the plastic casing at any time.

Wipe the inside and outside of the mouthpiece and the plastic casing with a

dry cloth or tissue

Replace the mouthpiece cover.

Do not put the metal canister in water.

If you use more Arquist than you should

If you use more than you should, talk to your doctor as soon as possible.

It is important that you take your dose as stated on the pharmacist’s label or as advised by your doctor. Do

not increase or decrease your dose without seeking medical advice.

If you forget to use Arquist

Take the next dose when it is due.

Do not take a double dose to make up for the forgotten dose.

If you stop using Arquist

Do not stop treatment even if you feel better unless your doctor told you to do so. If you have been on high

doses of steroids for a long time, you must not stop taking your medicine suddenly without talking to your

doctor, as this could make your asthma worse. Suddenly stopping treatment can also make you feel unwell

and may cause symptoms such as vomiting, drowsiness, nausea, headache, tiredness, loss of appetite, low

blood sugar level and fitting (having convulsions).

If you have any further questions on the use of this medicine ask your doctor, nurse or pharmacist.

4.

Possible side effects

Like all medicines, this medicine can cause side effects, although not everybody gets them.

If you notice any of the following serious side effects, stop using this medicine and talk to your doctor

straight away.

If you have an allergic reaction (rarely) or severe allergic reactions (very rarely). The signs include skin

rashes, redness, itching or weals like nettle rash or hives and swelling of your face, lips, mouth, tongue or

throat, which may cause difficulty in swallowing or breathing, itchy rash, feeling faint and light headed

and collapse respectively;

If your breathing or wheezing gets worse straight after using your inhaler.

Other side effects include:

Very common:

may affect more than 1 in 10 people

thrush in the mouth and throat

Common:

may affect up to 1 in 10 people

blood clot (hematoma);

hoarseness of voice;

pneumonia (infection of the lung) in COPD patients.

Tell your doctor if you have any of the following while taking Arquist they could be symptoms of a

lung infection:

fever or chills

increased mucus production, change in mucus colour

increased cough or increased breathing difficulties

Very rare:

may affect up to 1 in 10,000 people

sleeping problems or feeling worried, over-excited and irritable (these effects mainly occur in

children);

level of sugar (glucose) in your blood may increase;

using high doses of Arquist for a long period of time can cause : adrenal supression, adrenal crisis,

Cushing’s syndrome

,

thinning of your bones, eye problems and slowing of growth in young people

(see section 2 “Warnings and precautions”).

Your doctor will help stop this happening by making sure you use the lowest dose of steroid which controls

your symptoms.

Not known:

frequency cannot be estimated from the available data

depression;

feeling restless or nervous (these effects mainly occur in children).

blurred vision

Reporting of side effects

If you get any side effects, talk to your doctor or, pharmacist or nurse. This includes any possible side effects

not listed in this leaflet. You can also report side effects directly via <to be completed nationally>. By

reporting side effects you can help provide more information on the safety of this medicine.

5.

How to store Arquist

Keep this medicine out of the sight and reach of children.

Do not use Arquist after the expiry date, which is stated on the label and carton after ‘EXP’. The expiry date

refers to the last day of that month.

The canister contains a pressurised liquid. Do not expose to temperatures higher than 50

C. Do not pierce the

canister. Do not freeze. Protect from frost and direct sunlight.

If the inhaler gets very cold, take the metal canister out of the plastic case and warm it in your hands for a

few minutes before use. Never use anything else to warm it up.

The metal canister is pressurised. Do not puncture, break or burn it even when apparently empty.

Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to

throw away medicines you no longer use. These measures will help protect the environment.

If you are told to stop taking this medicine, return the inhaler to your pharmacist to be thrown away in an

appropriate manner.

6.

Contents of the pack and other information

What Arquist contains

The active substance is fluticasone propionate. One metered dose (ex-valve) contains 125 or 250

micrograms of fluticasone propionate respectively. This is equivalent to a delivered dose (ex-actuator) of

110 microgram or 227 microgram fluticasone propionate respectively.

The other ingredient is norflurane (HFA 134a).

What Arquist looks like and contents of the pack

Arquist is a white suspension inside the aluminium alloy canister sealed with a

metering valve, actuator and dust cap.

Each canister contains 120 metered actuations of either 125 or 250 micrograms of fluticasone propionate.

Pack sizes:

Single pack - Each single pack contain a canister with 120 actuations.

Multipack - Bundle pack of 2 or 3 single packs.

Hospital pack - Bundle pack of 10 single packs.

Not all pack sizes may be marketed.

Marketing Authorisation Holder and Manufacturer

Marketing Authorisation Holder

[To be completed nationally]

Manufacturer

Cipla Europe NV

De Keyserlei,

58-60 Box 19

Antwerpen 2018

Belgium

This medicinal product is authorised in the Member States of the EEA under the following names:

<{Name of the Member State}> <{Name of the medicinal product}>

<{Name of the Member State}> <{Name of the medicinal product}>

This leaflet was last revised in 2021-02-08

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SUMMARY OF PRODUCT CHARACTERISTICS

1.

NAME OF THE MEDICINAL PRODUCT

Arquist 125 microgram per actuation pressurised inhalation, suspension

Arquist 250 microgram per actuation pressurised inhalation, suspension

2.

QUALITATIVE AND QUANTITATIVE COMPOSITION

metered

dose

(ex-valve)

contains

micrograms

fluticasone

propionate

respectively. This is equivalent to a delivered dose (ex-actuator) of 110 microgram or 227

microgram fluticasone propionate respectively.

For the full list of excipients, see section 6.1.

3.

PHARMACEUTICAL FORM

Pressurised inhalation, suspension

An inhaler comprising an aluminium alloy canister sealed with a metering valve, actuator and dust

cap.

4.

CLINICAL PARTICULARS

4.1Therapeutic indications

Arquist is indicated for the regular treatment of asthma.

Arquist is indicated in adult and adolescent patients over 12 years of age.

4.2Posology and method of administration

Arquist is for oral inhalation use only.

Patients should be made aware Arquist should be taken regularly even when they are asymptomatic.

If patients find that relief with short-acting bronchodilator treatment becomes less effective or they

need more inhalations than usual, medical attention must be sought.

Adult and adolescent patients over 12 years of age:

125 micrograms to 500 micrograms twice daily. The dose may be adjusted until control is achieved

or reduced to the minimum effective dose, according to the individual response. Where the control

of symptoms is maintained with the lowest strength of Arquist (125 microgram/actuation), the next

step could include a swap to a different inhaled fluticasone product available in a lower strength

(50 micrograms/actuation). The onset of therapeutic effect is within 4 to 7 days.

For patients with severe asthma and during asthma exacerbations, as an alternative to oral

corticosteroid therapy, a temporary increase in dose may be needed (up to 2000 micrograms daily

in adult patients). The treatment effect should be monitored and for maintenance therapy the lowest

effective dose should be used.

Arquist may be used with a Volumatic spacer device by patients who find it difficult to synchronise

inspiration with aerosol actuation.

Special patient groups:

There is no need to adjust the dose in elderly patients or in patients with

renal impairment. There

is no experience in patients with hepatic impairment

.

Paediatric population

The efficacy and safety of Arquist has not been established in children (< 12 years of age).

Alternative products indicated for children should be used.

Method of administration:

It is important to instruct the patient about correct inhalation technique (see package leaflet and

instructions for use).

Instructions for use

Patients should be instructed in the proper use of their inhaler (see patient information leaflet)

During inhalation, the patient should preferably sit or stand. The inhaler has been designed for use

in a vertical position.

Testing the inhaler

Before using for the first time patients should remove the mouthpiece cover by gently squeezing

the sides of the cover, shake the inhaler well, hold the inhaler between fingers and thumb with

their thumb on the base, below the mouthpiece and release puffs into the air.

The inhaler should be shaken immediately before releasing each puff. If the inhaler has not been

used for a week or more the mouthpiece cover should be removed, the patient should shake the

inhaler well and should release two puffs into the air.

Use of the inhaler

On each occasion on which the inhaler is used the following instructions should be followed:

Remove the dustcap form the mouthpiece cover.

Shake the inhaler 4 or 5 times to ensure that any loose objects are removed and that the

contents of the inhaler are evenly mixed.

Hold the inhaler upright (the arrow on the base of the cantainer should be pointing upwards),

breathe out as far as is comfortable, and as slowely and deeply as possible and then close the

lips over the mouthpiece.

Breathe in slowly and deeply, through the mouth and immediately after starting to breathe in

press down firmly on the top of the inhaler to release one actuation (puff) and continue to

breathe in steadily and deeply.

Hold your breath for as long as is comfortable, for few

seconds if possible, then remove the mouthpiece from the mouth and breathe out slowly.

If a second inhaltion is required you should wait at least half a minute and repeat steps 3 and

4 above.

Replace the dustcap after use.

Cleaning (also detailed in patient information leaflet):

Your inhaler should be cleaned at least once a week.

Remove the mouthpiece cover.

Do not remove the metal canister from the plastic casing at any time.

Wipe the inside and outside of the mouthpiece and the plastic casing with a

dry cloth or

tissue

Replace the mouthpiece cover.

Do not put the metal canister in water.

4.3Contraindications

Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.

4.4Special warnings and precautions for use

The management of asthma should follow a stepwise programme, and patient response should be

monitored clinically and by lung function tests.

Before starting treatment, any bronchoconstriction should be treated, as otherwise the efficacy

could be lesser than expected

.

Patients' inhaler technique should be checked regularly to make sure

that inhaler actuation is synchronised with inspiration to ensure optimum delivery to the lungs.

During inhalation, the patient should preferably sit or stand. The inhaler has been designed for use

in a vertical position.

Fluticasone HFA Inhaler is not designed to relieve acute symptoms for which an inhaled short-

acting bronchodilator is required. Patients should be advised to have such rescue medication

available.

Increasing use of short-acting inhaled β

-agonists to relieve symptoms indicates deterioration of

asthma control. Under these conditions, the patient’s therapy plan should be reassessed.

Sudden

progressive

deterioration

asthma

control

potentially

life-threatening

consideration should be given to increasing corticosteroid dosage. In patients considered at risk,

daily peak flow monitoring may be instituted.

Lack of response or severe exacerbations of asthma should be treated by increasing the dose of

inhaled fluticasone propionate and, if necessary, by giving a systemic steroid and/or an antibiotic

if there is an infection.

Systemic effects of inhaled corticosteroids may occur, particularly at high doses prescribed for

prolonged periods. These effects are much less likely to occur than with oral corticosteroids (see

section 4.9). Possible systemic effects include Cushing's syndrome, Cushingoid features, adrenal

suppression, growth retardation in children and adolescents, decrease in bone mineral density,

cataract and glaucoma and more rarely, a range of psychological or behavioural effects including

psychomotor hyperactivity, sleep disorders, anxiety, depression or aggression (particularly in

children). It is important therefore that the dose of inhaled corticosteroid is reviewed regularly and

reduced to the lowest dose at which effective control of asthma is maintained (see section 4.8).

Certain individuals can show greater susceptibility to the effects of inhaled corticosteroid than do

most patients

.

Prolonged treatment with high doses of inhaled corticosteroids may result in adrenal suppression

and acute adrenal crisis. In very rare cases, adrenal suppression and acute adrenal crisis has occurred

at doses of between 500 and 1000 micrograms of fluticasone propionate

.

Situations, which could

potentially trigger acute adrenal crisis, include trauma, surgery, infection or any rapid reduction in

dosage. Presenting symptoms are typically vague and may include anorexia, abdominal pain,

weight

loss,

tiredness,

headache,

nausea,

vomiting,

decreased

level

consciousness,

hypoglycaemia, and seizures. The possibility of residual impaired adrenal response should always

be considered in emergency (medical or surgical) and elective situations likely to produce stress,

and appropriate corticosteroid treatment considered (see section 4.9).

As systemic absorption is largely through the lungs, the use of Volumatic spacer plus metered dose

inhaler may increase drug delivery to the lungs. It should be noted that this could potentially lead

to an increase in the risk of systemic adverse effects.

Treatment with Fluticasone HFA Inhaler should not be stopped abruptly due to the risk of

exacerbations. Tapering of the dose should be done under medical supervision

.

with

inhaled

corticosteroids,

special

care

necessary

patients

with

pulmonary

tuberculosis, viral, bacterial and fungal infections.

There have been very rare reports of increases in blood glucose levels, (see section 4.8). This should

be considered when prescribing to patients with a history of diabetes mellitus.

As with other inhalation therapy, paradoxical bronchospasm may occur with an immediate increase

in wheezing after dosing. Fluticasone HFA Inhaler should be discontinued immediately, the patient

assessed and alternative therapy instituted if necessary. In this case the patient should immediately

use a short-acting bronchodilator inhaler.

During post-marketing use, there have been reports of clinically significant drug interactions in

patients receiving fluticasone propionate and ritonavir, resulting in systemic corticosteroid effects

including Cushing’s syndrome and adrenal suppression. Therefore, concomitant use of fluticasone

propionate and ritonavir

should be avoided, unless the potential benefit to the patient outweighs the

risk of systemic corticosteroid side-effects. There is also an increased risk of systemic side effects

when combining fluticasone propionate with other potent CYP3A inhibitors (see section 4.5).

For the transfer of patients being treated with oral corticosteroids:

Adrenal function and adrenal reserve usually remain within the normal range on recommended

doses of fluticasone propionate therapy.

The benefits of inhaled fluticasone propionate should

minimise the need for oral steroids. However, the possibility of adverse effects in patients, resulting

from prior or intermittent administration of oral steroids,

may persist for some time. The extent of

adrenal impairment may require specialist advice

before elective procedures. The possibility of

residual impaired adrenal response should always be considered in emergency (medical or surgical)

and elective situations likely to produce stress, and appropriate corticosteroid treatment considered

(see section 4.9).

Because of the possibility of impaired adrenal response, patients transferring from oral steroid

therapy to inhaled fluticasone propionate therapy should be treated with special care, and

adrenocortical function regularly monitored.

Following introduction of inhaled fluticasone propionate, withdrawal of systemic therapy should

be gradual and patients encouraged to carry a steroid warning card indicating the possible need for

additional therapy in times of stress.

For patients dependent on oral corticosteroids, fluticasone propionate should be administered

concomitantly with systemic steroid therapy for 10 days

.

Thereafter, gradual withdrawal of the

systemic steroid is commenced at a rate of 2.5 mg of prednisolone (or equivalent) per month, to the

lowest possible level.

Some patients feel unwell in a non-specific way during the withdrawal phase despite maintenance

or even improvement of the respiratory function. They should be encouraged to persevere with

inhaled fluticasone propionate and to continue withdrawal of systemic steroid, unless there are

objective signs of adrenal insufficiency.

Replacement of systemic steroid treatment with inhaled therapy sometimes unmasks allergies such

as allergic rhinitis or eczema previously controlled by the systemic drug. These allergies should be

symptomatically treated with antihistamine and/or topical preparations, including topical steroids.

An increase in the incidence of pneumonia, including pneumonia requiring hospitalisation, has been

observed in patients with COPD receiving inhaled corticosteroids. There is some evidence of an

increased risk of pneumonia with increasing steroid dose but this has not been demonstrated

conclusively across all studies.

There is no conclusive clinical evidence for intra-class differences in the magnitude of the

pneumonia risk among inhaled corticosteroid products.

Physicians should remain vigilant for the possible development of pneumonia in patients with

COPD

clinical

features

such

infections

overlap

with

symptoms

COPD

exacerbations.

Risk factors for pneumonia in patients with COPD include current smoking, older age, low body

mass index (BMI) and severe COPD.

Arquist should not be used for rapid relief of bronchospasm.

Visual disturbance

Visual disturbance may be reported with systemic and topical corticosteroid use. If a patient

presents with symptoms such as blurred vision or other visual disturbances, the patient should be

considered for referral to an ophthalmologist for evaluation of possible causes which may include

cataract, glaucoma or rare diseases such as central serous chorioretinopathy (CSCR) which have

been reported after use of systemic and topical corticosteroids.

4.5Interaction with other medicinal products and other forms of interaction

Under normal circumstances, low plasma concentrations of fluticasone propionate are achieved

after inhaled dosing, due to extensive first pass metabolism and high systemic clearance mediated

by cytochrome P450 3A4 in the gut and liver. Hence, clinically significant drug interactions

mediated by fluticasone propionate are unlikely.

In an interaction study in healthy subjects with intranasal fluticasone propionate, ritonavir (a highly

potent cytochrome P450 3A4 inhibitor) 100 mg b.i.d. increased the fluticasone propionate plasma

concentrations several hundred fold, resulting in markedly reduced serum cortisol concentrations.

Information about this interaction is lacking for inhaled fluticasone propionate, but a marked

increase in fluticasone propionate plasma levels is expected. Cases of Cushing's syndrome and

adrenal suppression have been reported. Co-treatment with CYP3A inhibitors, including cobicistat-

containing products, is expected to increase the risk of systemic side-effects. The combination

should be avoided unless the benefit outweighs the increased risk of systemic corticosteroid side-

effects, in which case patients should be monitored for systemic corticosteroid side-effects.

In a small study in healthy volunteers, the slightly less potent CYP3A inhibitor ketoconazole

increased the exposure of fluticasone propionate after a single inhalation by 150%. This resulted in

a greater reduction of plasma cortisol as compared with fluticasone propionate alone. Co-treatment

with

other

potent

CYP3A

inhibitors,

such

itraconazole,

clarithromycin,

telithromycin,

atazanavir, indinavir, nelfinavir or saquinavir is also expected to increase the systemic fluticasone

propionate exposure and the risk of systemic side-effects. Caution is recommended and long-term

treatment with such drugs should, if possible, be avoided.

4.6Fertility, pregnancy and lactation

Fertility

There are no clinical data on human fertility. Animal studies indicates no effects of fluticasone

propionate on male or female fertility.

Pregnancy

There are limited data in pregnant women. Administration of fluticasone propionate during

pregnancy should only be considered if the expected benefit to the mother is greater than any

possible risk to the fetus. The dose of inhaled corticosteroid should be titrated to the lowest dose at

which effective control is maintained.

Results from a retrospective epidemiological study did not find an increased risk of major

congenital malformations (MCMs) following exposure to fluticasone propionate when compared

to other inhaled corticosteroids, during the first trimester of pregnancy.

Reproductive

studies

animals

have

shown

only

those

effects

characteristic

glucocorticosteroids at systemic exposures in excess of those seen at the recommended inhaled

therapeutic dose.

Breast-feeding

The excretion of fluticasone propionate in human breast milk has not been investigated. When

measurable plasma levels were obtained in lactating laboratory rats following subcutaneous

administration there was evidence of fluticasone propionate in the breast milk. However, plasma

levels in humans after inhalation at recommended doses are likely to be low.

The benefit of therapy with fluticasone propionate for the woman and the benefit of breastfeeding

for the child must be weighed against the potential hazards to the baby.

4.7Effects on ability to drive and use machines

Fluticasone propionate is unlikely to produce an effect.

4.8Undesirable effects

Adverse events are listed below by system organ class and frequency. Frequencies are defined as:

very common (

1/10), common (

1/100 and <1/10), uncommon (

1/1000 and <1/100), rare (

1/10,000 and <1/1000), very rare (<1/10,000) including isolated reports

and not known (cannot be

estimated from the available data). Very common, common and uncommon events were generally

determined from clinical trial data. Rare and very rare events were generally determined from

spontaneous data.

System Organ Class

Adverse Event

Frequency

Candidiasis of the mouth and

throat

Very Common

Infections and infestations

pneumonia (in patients with

COPD)

Common

Hypersensitivity reactions with

the following manifestations:

Immune system disorders

Cutaneous hypersensitivity

reactions

Uncommon

System Organ Class

Adverse Event

Frequency

Angioedema (mainly facial and

oropharyngeal oedema)

Very Rare

Respiratory symptoms

(dyspnoea and/or

bronchospasm)

Very Rare

Anaphylactic reactions

Very Rare

Endocrine disorders

Cushing's syndrome,

Cushingoid features, adrenal

suppression, growth retardation

in children and adolescents,

decreased bone mineral density

Very Rare

Eye disorders

Cataract, glaucoma

Very Rare

Vision, blurred (see section 4.4)

Not known

Metabolism and nutrition

disorders

Hyperglycaemia (see section

4.4)

Very Rare

Anxiety, sleep disorders,

behavioural changes, including

hyperactivity and irritability

(predominantly in children)

Very Rare

Psychiatric disorders

Depression, aggression

(predominantly in children)

Not known

Respiratory, thoracic and

mediastinal disorders

Hoarseness/dysphonia

Common

Skin and subcutaneous tissue

disorders

Hematoma (or effusion)

Common

Hoarseness and candidiasis of the mouth and throat (thrush) occurs in some patients. Such patients

may find it helpful to rinse out their mouth with water after using the inhaler. Symptomatic

candidiasis can be treated with topical anti-fungal therapy whilst still continuing with Fluticasone

HFA Inhaler.

Possible systemic effects include Cushing's syndrome, Cushingoid features, adrenal suppression,

growth retardation, decreased bone mineral density, cataract, glaucoma (see section 4.4).

As with other inhalation therapy, paradoxical bronchospasm may occur (see section 4.4).

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is

important. It allows continued 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 listed in Appendix V.

4.9Overdose

Acute:

Inhalation of the drug in doses in excess of those approved

may lead to temporary

suppression of adrenal function. This does not necessitate emergency action being taken. In these

patients treatment with fluticasone propionate by inhalation should be continued at a dose sufficient

to control asthma adrenal function recovers in a few days and can be verified by measuring plasma

cortisol.

Chronic:

higher

than

approved

doses

continued

over

prolonged

periods,

significant

adrenocortical suppression is possible. There have been very rare reports of acute adrenal crisis

occurring in children exposed to higher than approved doses (typically 1000 micrograms daily and

above),

over

prolonged

periods

(several

months

years);

observed

features

included

hypoglycaemia and sequelae of decreased consciousness and/or convulsions. Situations which

could potentially trigger acute adrenal crisis include exposure to trauma, surgery infection or any

rapid reduction in dosage

.

Monitoring of adrenal reserve may be indicated. Treatment with inhaled

fluticasone propionate should be continued at a dose sufficient to control asthma.

5.

PHARMACOLOGICAL PROPERTIES

5.1Pharmacodynamic properties

Pharmacotherapeutic group: Glucocorticoids, ATC code: R03BA05

Fluticasone propionate is a glucocorticoid with anti-inflammatory effects

.

Fluticasone propionate

given by inhalation at recommended doses has a potent glucocorticoid anti-inflammatory action

within the lungs, resulting in a reduction of both symptoms and exacerbations of asthma, with a

lower incidence and severity of adverse effects than those observed when corticosteroids are

administered systemically. Full effect is achieved after 4-7 days of treatment. The majority of

particles are less than 5 micrometers.

5.2Pharmacokinetic properties

Absorption

In healthy subjects the mean systemic bioavailability of Fluticasone HFA Inhaler is 5-11% of the

nominal dose, depending on the inhalation device used

.

In patients with asthma (FEV 1 < 75%

predicted) the mean systemic absolute bioavailability is reduced as compared to healthy volunteers.

Systemic absorption occurs mainly through the lungs and has been shown to be linearly related to

dose over the dose range 500 to 2000 micrograms. Absorption is initially rapid then prolonged.

Absolute oral bioavailability is negligible (<1%) due to a combination of incomplete absorption

from the GI tract and extensive first-pass metabolism.

Distribution

After an intravenous dose, fluticasone propionate is extensively distributed in the body. Plasma

clearance is high (approximately 1150 ml/min) and volume of distribution at steady state is large

(approximately 300 L). The binding of fluticasone to plasma proteins is 91%.

Biotransformation

Fluticasone is metabolized by the enzyme CYP3A4 to an inactive major carboxyacid metabolite.

Elimination

87-100% of an oral dose is excreted in the faeces, up to 75% as parent compound. Other metabolites

with unknown structure have also been identified in faeces. The terminal half-life is about 8 hours

.

5.3Preclinical safety data

Administration

corticosteroids

pregnant

animals

cause

abnormalities

fetal

development, including cleft palate and intra-uterine growth retardation. There may therefore be a

very small risk of such effects in the human fetus. It should be noted, however, that the fetal changes

in animals occur after relatively high systemic exposure.

Toxicology has shown only those class effects typical of potent corticosteroids, and these only at

doses greatly in excess of that proposed for therapeutic use. No novel effects or effects on fertility

were identified in repeat dose toxicity tests, reproductive studies or teratology studies. Fluticasone

propionate is devoid of mutagenic activity in vitro and in vivo and showed no tumorigenic potential

in rodents. It is both non-irritant and non-sensitising in animal models.

The non-CFC propellant, HFA 134a, has been shown to have no toxic effect at very high vapour

concentrations, far in excess of those likely to be experienced by patients, in a wide range of animal

species exposed daily for periods of two years.

The use of HFA 134a as a propellant has not altered the toxicity profile of fluticasone propionate

compared to that using the conventional CFC propellant.

6.

PHARMACEUTICAL PARTICULARS

6.1List of excipients

Norflurane (HFA 134a)

6.2Incompatibilities

Not applicable

6.3Shelf life

2 years

6.4Special precautions for storage

The canister contains a pressurized liquid. Do not expose to temperatures higher than 50

C. Do not

pierce the canister. Do not freeze. Protect from frost and direct sunlight.

As with most medicines in pressurised canisters, the therapeutic effect of this medication may

decrease when the canister is cold.

If the inhaler gets very cold, take the metal canister out of the plastic case and warm it in your hands

for a few minutes before use. Never use anything else to warm it up.

The canister should not be punctured, broken or burnt even when apparently empty.

Replace the mouthpiece cover firmly and snap into position.

6.5Nature and contents of container

An inhaler comprising an aluminium alloy canister sealed with a metering valve, actuator and dust

cap.

Each canister contains 120 metered actuations of either 125 or 250 micrograms of fluticasone

propionate.

Pack sizes:

Single pack - Each single pack contain a canister with 120 actuations.

Multipack - Bundle pack of 2 or 3 single packs.

Hospital pack - Bundle pack of 10 single packs.

Not all pack sizes may be marketed.

6.6Special precautions for disposal and other handling

The aerosol spray is inhaled through the mouth into the lungs. After shaking the inhaler the patient

should exhale, the mouthpiece should be placed in the mouth and the lips closed around it. The

actuator is depressed to release a spray, which must coincide with inspiration of breath.

For detailed instructions for use refer to the package leaflet in every pack.

7.

MARKETING AUTHORISATION HOLDER

Cipla (EU) Limited,

Hillbrow House,

Hillbrow Road,

Esher Surrey,

KT10 9NW,

United Kingdom.

8.

MARKETING AUTHORISATION NUMBER(S)

<[To be completed nationally]>

9.

DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION

<[To be completed nationally]>

10.

DATE OF REVISION OF THE TEXT

2020-11-19

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