Description :
Not applicable.
1. DRUG NAME
ALOPEXY 2 PER CENT, solution for cutaneous application
2. QUALITATIVE AND QUANTITATIVE COMPOSITION
Minoxidil ................................................................................................................................................ 2 g
Per 100 ml of solution for cutaneous application.
Notable excipient: propylene glycol
For full list of excipients, see section 6.1.
3. PHARMACEUTICAL FORM
Solution for cutaneous application.
4. CLINICAL DATA
4.1 Therapeutic indications
This drug is indicated for moderate hair loss (androgenetic alopecia) in adult men and women. It promotes hair growth and stabilizes hair loss.
4.2. Dosage and administration
Dermal route.
FOR ADULTS ONLY.
Apply a 1 ml dose to the scalp twice a day, starting from the center of the area to be treated.
The daily dose should not exceed 2 ml.
Spread the product with your fingertips to cover the entire area to be treated.
Before and after applying the solution, wash hands thoroughly.
Apply to perfectly dry hair and scalp.
Using the pipette
A pipette is used to accurately dispense 1 ml of solution over the entire treatment area.
Using the pump with applicator:
Remove the cap from the bottle and unscrew the plug.
Screw the dosing pump onto the bottle.
To apply: direct the pump towards the center of the area to be treated, squeeze once and spread the product with the fingertips to cover the entire area.
Repeat 6 times to apply a dose of 1 ml.
4.3. Contraindications
Hypersensitivity to minoxidil or to any of the other ingredients of the solution.
4.4 Special warnings and precautions for use
Special warnings
Before using topical minoxidil, patients should ensure that their scalp is normal and healthy.
Increased percutaneous absorption of minoxidil, which may lead to systemic effects, is possible in cases of:
- dermatosis or lesions of the scalp,
- concomitant application of retinoic acid, anthralin or any other irritant topical,
- increasing the dose and/or frequency of application: it is essential to follow the dosage and administration instructions.
Similarly, although extensive use of minoxidil solution has not revealed any systemic effects, it cannot be ruled out that greater absorption due to individual variability or unusual sensitivity may cause systemic effects. Patients should be warned accordingly.
In the event of systemic effects (drop in blood pressure, tachycardia, signs of fluid retention, chest pain) or severe dermatological reactions, treatment should be discontinued.
In subjects with a history of heart disease, the benefit of treatment must be weighed up. They should be particularly warned of potential adverse effects, so that treatment can be discontinued as soon as any of them appear, and a doctor notified.
Do not apply minoxidil:
- in cases of sudden hair loss, or hair loss resulting from illness or medication,
- on any other part of the body.
Precautions for use
Accidental ingestion may cause severe adverse reactions (see section 4.9).
In the event of accidental contact with the eye, damaged skin or mucous membranes, the solution (containing ethyl alcohol) may cause a burning sensation and irritation: rinse thoroughly with running water.
Sun exposure is not recommended when applying minoxidil.
This product contains propylene glycol and may cause skin irritation.
4.5. Interactions with other drugs and other forms of interaction
The data available to date do not suggest the existence of clinically significant interactions.
4.6. Pregnancy and breast-feeding
Pregnancy
Animal studies have not demonstrated any teratogenic effect. In the absence of teratogenic effects in animals, a malformative effect in humans is not expected. Indeed, to date, substances responsible for malformations in humans have been shown to be teratogenic in animals in well-conducted studies in two species.
Clinically, there are currently no sufficiently relevant data to assess a possible malformative or fetotoxic effect of minoxidil when administered during pregnancy.
Consequently, as a precautionary measure, minoxidil should not be used during pregnancy.
Breast-feeding
Systemically administered minoxidil is excreted in breast milk; it should therefore be avoided by nursing mothers.
4.7. Effects on ability to drive and use machines
Not applicable.
4.8. Undesirable effects
- Most often minor skin reactions: local irritation with, in particular, desquamation, erythema, dermatitis, dry skin, hypertrichosis (at a distance), burning sensation and pruritus (in particular due to the presence of alcohol).
- More rarely: allergy (sensitivity, rhinitis, rash, generalized erythema, facial edema), dizziness, tingling, headache, weakness, neuritis, edema, taste alteration, ear infection (especially otitis externa), visual disturbances, eye irritation.
- Alopecia, irregular hair growth, chest pain, changes in blood pressure and pulse may also occur.
Liver abnormalities may occur.
- Due to the presence of propylene glycol, contact eczema may occur.
It should be noted, however, that these medical events, and in particular those which have been most rarely reported, have not been formally attributable to treatment.
4.9. Overdose
Accidental ingestion may cause systemic effects due to the vasodilatory action of minoxidil (5 ml solution contains 100 mg minoxidil, the maximum dose used for oral administration in adults treated for hypertension). Signs and symptoms of possible overdosage would be cardiovascular, with a drop in blood pressure, tachycardia and fluid retention. Fluid retention can be treated with appropriate diuretic therapy, while tachycardia and angina can be treated with beta-blockers or other sympathetic nervous system inhibitors. Symptomatic hypotension may be treated by intravenous administration of isotonic sodium chloride solution. The use of sympathomimetics, such as noradrenaline and adrenaline, should be avoided because of excessive cardiac stimulation.
5. PHARMACOLOGICAL PROPERTIES
5.1. Pharmacodynamic properties
Pharmacotherapeutic class:
OTHER DERMATOLOGICAL DRUGS
ATC code: D11AX01
Efficacy and safety in subjects under 18 and over 65 years of age have not been studied.
Applied topically, minoxidil stimulates keratinocyte growth in vitro and in vivo, and hair growth in certain subjects with androgenetic alopecia.
The onset of this phenomenon occurs after around 4 months (or more) of product use, and varies from subject to subject.
When treatment is stopped, regrowth ceases, and a return to the initial state can be expected within 3 or 4 months.
The precise mechanism of action is not known. Topical application of minoxidil in controlled clinical trials in normotensive or hypertensive patients has not led to the observation of systemic manifestations linked to minoxidil absorption.
5.2. Pharmacokinetic properties
Minoxidil is poorly absorbed when applied topically: an average of 1.4% (ranging from 0.3 to 4.5%) of the applied dose reaches the systemic circulation. Thus, for a dose of 1 ml of 2% solution (equivalent to 20 mg minoxidil applied to the skin), the amount of minoxidil absorbed corresponds to around 0.28 mg.
By way of comparison, when minoxidil is administered orally (in the treatment of certain types of hypertension), it is virtually completely absorbed from the gastrointestinal tract. It has also been shown that the smallest I.V. dose of minoxidil to induce clinically significant hemodynamic effects in patients with mild to moderate hypertension is 6.86 mg.
Results from pharmacokinetic studies indicate that the three main factors increasing absorption of topical minoxidil are
- quantitative increase in applied dose
- increased frequency of application,
- decrease in the barrier function of the epidermal stratum corneum.
This increase is rapidly limited by a saturation effect.
Absorption of minoxidil after topical application is unaffected by gender, UV exposure, simultaneous application of a moisturizing product, occlusion (hair prosthesis), solvent evaporation (hair dryer) or application surface.
Serum minoxidil levels following topical administration are dependent on the rate of percutaneous absorption. After discontinuation of topical application, approximately 95% of absorbed minoxidil is eliminated within 4 days.
The biotransformation of absorbed minoxidil after topical application is not fully understood.
5.3. Preclinical safety data
Not available.
6. PHARMACEUTICAL DATA
6.1. List of excipients
γ-Cyclodextrin, 96% ethanol, propylene glycol, purified water.
6.2 Incompatibilities
Not applicable.
6.3. Shelf life
- Bottle packaging (brown glass): 3 years
- Bottle packaging (PET): 2 years.
6.4. Special storage precautions
No special storage precautions.
6.5. Nature and contents of packaging
- 15 ml, 30 ml or 60 ml bottle (brown glass) with or without pipette (Polystyrene/polyethylene) graduated to 1 ml. Boxes of 1 or 3.
- 60 ml bottle (PET) with pipette (Polystyrene/polyethylene) graduated to 1 ml and metering pump with applicator. Boxes of 1 or 3.
6.6. Special precautions for disposal and handling
No special requirements.
7. MARKETING AUTHORIZATION HOLDER
PIERRE FABRE DERMATOLOGIE
45, PLACE ABEL GANCE
92100 BOULOGNE
8. MARKETING AUTHORIZATION NUMBER(S)
- 330 924-1: 15 ml bottle (brown glass) with pipette (polystyrene/polyethylene).
- 330 228-5: 30 ml bottle (brown glass) with pipette (polystyrene/polyethylene).
- 330 925-8: 60 ml bottle (brown glass) with pipette (polystyrene/polyethylene).
- 332 175-6: 2 bottles (brown glass) of 60 ml + 1 bottle (brown glass of 15 ml).
- 335 273-9: 60 ml bottle (brown glass) box of 3.
- 362 991-6: 60 ml bottle (PET) with pipette (Polystyrene/polyethylene) and metering pump with applicator. Box of 1.
- 364 307-5: 60 ml bottle (PET) with pipette (Polystyrene/polyethylene) and metering pump with applicator. Box of 3.
9. DATE OF FIRST AUTHORIZATION/RENEWAL OF AUTHORIZATION
[to be completed by the holder]
10. DATE OF TEXT UPDATE
[to be completed by the holder]
11. DOSIMETRY
Not applicable.
12. INSTRUCTIONS FOR THE PREPARATION OF RADIOPHARMACEUTICALS
Description :
Not applicable.
1. DRUG NAME
ALOPEXY 2 PER CENT, solution for cutaneous application
2. QUALITATIVE AND QUANTITATIVE COMPOSITION
Minoxidil ................................................................................................................................................ 2 g
Per 100 ml of solution for cutaneous application.
Notable excipient: propylene glycol
For full list of excipients, see section 6.1.
3. PHARMACEUTICAL FORM
Solution for cutaneous application.
4. CLINICAL DATA
4.1 Therapeutic indications
This drug is indicated for moderate hair loss (androgenetic alopecia) in adult men and women. It promotes hair growth and stabilizes hair loss.
4.2. Dosage and administration
Dermal route.
FOR ADULTS ONLY.
Apply a 1 ml dose to the scalp twice a day, starting from the center of the area to be treated.
The daily dose should not exceed 2 ml.
Spread the product with your fingertips to cover the entire area to be treated.
Before and after applying the solution, wash hands thoroughly.
Apply to perfectly dry hair and scalp.
Using the pipette
A pipette is used to accurately dispense 1 ml of solution over the entire treatment area.
Using the pump with applicator:
Remove the cap from the bottle and unscrew the plug.
Screw the dosing pump onto the bottle.
To apply: direct the pump towards the center of the area to be treated, squeeze once and spread the product with the fingertips to cover the entire area.
Repeat 6 times to apply a dose of 1 ml.
4.3. Contraindications
Hypersensitivity to minoxidil or to any of the other ingredients of the solution.
4.4. special warnings and precautions for use
Special warnings
Before using topical minoxidil, patients should ensure that their scalp is normal and healthy.
Increased percutaneous absorption of minoxidil, which may lead to systemic effects, is possible in cases of:
- dermatosis or lesions of the scalp,
- concomitant application of retinoic acid, anthralin or any other irritant topical,
- increasing the dose and/or frequency of application: it is essential to follow the dosage and administration instructions.
Similarly, although extensive use of minoxidil solution has not revealed any systemic effects, it cannot be ruled out that greater absorption due to individual variability or unusual sensitivity may cause systemic effects. Patients should be warned accordingly.
In the event of systemic effects (drop in blood pressure, tachycardia, signs of fluid retention, chest pain) or severe dermatological reactions, treatment should be discontinued.
In subjects with a history of heart disease, the benefit of treatment must be weighed up. They should be particularly warned of potential adverse effects, so that treatment can be discontinued as soon as any of them appear, and a doctor notified.
Do not apply minoxidil:
- in cases of sudden hair loss, or hair loss resulting from illness or medication,
- on any other part of the body.
Precautions for use
Accidental ingestion may cause severe adverse reactions (see section 4.9).
In the event of accidental contact with the eye, damaged skin or mucous membranes, the solution (containing ethyl alcohol) may cause a burning sensation and irritation: rinse thoroughly with running water.
Sun exposure is not recommended when applying minoxidil.
This product contains propylene glycol and may cause skin irritation.
4.5. Interactions with other drugs and other forms of interaction
The data available to date do not suggest the existence of clinically significant interactions.
4.6. Pregnancy and breast-feeding
Pregnancy
Animal studies have not demonstrated any teratogenic effect. In the absence of teratogenic effects in animals, a malformative effect in humans is not expected. Indeed, to date, substances responsible for malformations in humans have been shown to be teratogenic in animals in well-conducted studies in two species.
Clinically, there are currently no sufficiently relevant data to assess a possible malformative or fetotoxic effect of minoxidil when administered during pregnancy.
Consequently, as a precautionary measure, minoxidil should not be used during pregnancy.
Breast-feeding
Systemically administered minoxidil is excreted in breast milk; it should therefore be avoided by nursing mothers.
4.7. Effects on ability to drive and use machines
Not applicable.
4.8. Undesirable effects
- Most often minor skin reactions: local irritation with, in particular, desquamation, erythema, dermatitis, dry skin, hypertrichosis (at a distance), burning sensation and pruritus (in particular due to the presence of alcohol).
- More rarely: allergy (sensitivity, rhinitis, rash, generalized erythema, facial edema), dizziness, tingling, headache, weakness, neuritis, edema, taste alteration, ear infection (especially otitis externa), visual disturbances, eye irritation.
- Alopecia, irregular hair growth, chest pain, changes in blood pressure and pulse may also occur.
Liver abnormalities may occur.
- Due to the presence of propylene glycol, contact eczema may occur.
It should be noted, however, that these medical events, and in particular those which have been most rarely reported, have not been formally attributable to treatment.
4.9. Overdose
Accidental ingestion may cause systemic effects due to the vasodilatory action of minoxidil (5 ml solution contains 100 mg minoxidil, the maximum dose used for oral administration in adults treated for hypertension). Signs and symptoms of possible overdosage would be cardiovascular, with a drop in blood pressure, tachycardia and fluid retention. Fluid retention can be treated with appropriate diuretic therapy, while tachycardia and angina can be treated with beta-blockers or other sympathetic nervous system inhibitors. Symptomatic hypotension may be treated by intravenous administration of isotonic sodium chloride solution. The use of sympathomimetics, such as noradrenaline and adrenaline, should be avoided because of excessive cardiac stimulation.
5. PHARMACOLOGICAL PROPERTIES
5.1. Pharmacodynamic properties
Pharmacotherapeutic class:
OTHER DERMATOLOGICAL DRUGS
ATC code: D11AX01
Efficacy and safety in subjects under 18 and over 65 years of age have not been studied.
Applied topically, minoxidil stimulates keratinocyte growth in vitro and in vivo, and hair growth in certain subjects with androgenetic alopecia.
The onset of this phenomenon occurs after around 4 months (or more) of product use, and varies from subject to subject.
When treatment is stopped, regrowth ceases, and a return to the initial state can be expected within 3 or 4 months.
The precise mechanism of action is not known. Topical application of minoxidil in controlled clinical trials in normotensive or hypertensive patients has not led to the observation of systemic manifestations linked to minoxidil absorption.
5.2. Pharmacokinetic properties
Minoxidil is poorly absorbed when applied topically: an average of 1.4% (ranging from 0.3 to 4.5%) of the applied dose reaches the systemic circulation. Thus, for a dose of 1 ml of 2% solution (equivalent to 20 mg minoxidil applied to the skin), the amount of minoxidil absorbed corresponds to around 0.28 mg.
By way of comparison, when minoxidil is administered orally (in the treatment of certain types of hypertension), it is virtually completely absorbed from the gastrointestinal tract. It has also been shown that the smallest I.V. dose of minoxidil to induce clinically significant hemodynamic effects in patients with mild to moderate hypertension is 6.86 mg.
Results from pharmacokinetic studies indicate that the three main factors increasing absorption of topical minoxidil are
- quantitative increase in applied dose
- increased frequency of application,
- decrease in the barrier function of the epidermal stratum corneum.
This increase is rapidly limited by a saturation effect.
Absorption of minoxidil after topical application is unaffected by gender, UV exposure, simultaneous application of a moisturizing product, occlusion (hair prosthesis), solvent evaporation (hair dryer) or application surface.
Serum minoxidil levels following topical administration are dependent on the rate of percutaneous absorption. After discontinuation of topical application, approximately 95% of absorbed minoxidil is eliminated within 4 days.
The biotransformation of absorbed minoxidil after topical application is not fully understood.
5.3. Preclinical safety data
Not available.
6. PHARMACEUTICAL DATA
6.1. List of excipients
γ-Cyclodextrin, 96% ethanol, propylene glycol, purified water.
6.2 Incompatibilities
Not applicable.
6.3. Shelf life
- Bottle packaging (brown glass): 3 years
- Bottle packaging (PET): 2 years.
6.4. Special storage precautions
No special storage precautions.
6.5. Nature and contents of packaging
- 15 ml, 30 ml or 60 ml bottle (brown glass) with or without pipette (Polystyrene/polyethylene) graduated to 1 ml. Boxes of 1 or 3.
- 60 ml bottle (PET) with pipette (Polystyrene/polyethylene) graduated to 1 ml and metering pump with applicator. Boxes of 1 or 3.
6.6. Special precautions for disposal and handling
No special requirements.
7. MARKETING AUTHORIZATION HOLDER
PIERRE FABRE DERMATOLOGIE
45, PLACE ABEL GANCE
92100 BOULOGNE
8. MARKETING AUTHORIZATION NUMBER(S)
- 330 924-1: 15 ml bottle (brown glass) with pipette (polystyrene/polyethylene).
- 330 228-5: 30 ml bottle (brown glass) with pipette (polystyrene/polyethylene).
- 330 925-8: 60 ml bottle (brown glass) with pipette (polystyrene/polyethylene).
- 332 175-6: 2 bottles (brown glass) of 60 ml + 1 bottle (brown glass of 15 ml).
- 335 273-9: 60 ml bottle (brown glass) box of 3.
- 362 991-6: 60 ml bottle (PET) with pipette (Polystyrene/polyethylene) and metering pump with applicator. Box of 1.
- 364 307-5: 60 ml bottle (PET) with pipette (Polystyrene/polyethylene) and metering pump with applicator. Box of 3.
9. DATE OF FIRST AUTHORIZATION/RENEWAL OF AUTHORIZATION
[to be completed by the holder]
10. DATE OF TEXT UPDATE
Français
English
