Minoxidil Topical Solution USP 2% w/v and 5% w/v
For the use only of Registered Medical Practitioners or a Hospital or a laboratory
QUALITATIVE & QUANTITATIVE COMPOSITION:
Regaine 2%
Each ml of Minoxidil Topical Solution USP 2% contains:
Minoxidil IP…………………………..20mg
Ethanol (95%) IP equivalent to Ethanol (Absolute Alcohol) IP……………60% v/v
No perfume added.
Regaine 5%
Each ml of Minoxidil Topical Solution USP 5% contains:
Minoxidil IP…………………………..50mg
Ethanol (95%) IP equivalent to Ethanol (Absolute Alcohol) IP............ 30% v/v
No perfume added.
FOR EXTERNAL USE ONLY
WARNING: To be sold by retail on the prescription of a Dermatologist only.
Chemically, minoxidil is 2, 4-diamino-6-piperidinopyrimidine. REGAINE® solution is a minoxidil USP 2% w/v and 5% w/v solution containing propylene glycol and alcohol in an aqueous base. REGAINE® solution is available in 60 mL bottle.
CLINICAL PARTICULARS
Therapeutic Indications
Treatment of alopecia androgenetica (male pattern baldness).
Dosage and Administration
REGAINE® solution is for external use only. It should be used as directed by the treating physician. The recommended dose is 1 mL per application. 1 mL of REGAINE® solution should be applied twice per day to the scalp, beginning at the centre of the affected area. This dose should be used regardless of the size of the affected area. The total daily dose should not exceed 2 mL. After applying REGAINE® solution, hands should be washed thoroughly. The REGAINE® solution should not be applied to any other area of the body.
REGAINE® solution should be applied when the hair and scalp are thoroughly dry. Do not use a hairdryer to speed the drying of the solution, because blowing air on the scalp may decrease the effectiveness of the drug. REGAINE® solution should not be mixed with other hair oil.
Increased hair growth has not been associated with increased systemic absorption of REGAINE® solution. The onset of hair growth stimulation requires twice daily applications of REGAINE® solution for 4 or more months, and is variable among patients. Upon discontinuation of REGAINE® solution, new hair growth has been anecdotally reported to stop and restoration of pretreatment appearance to occur within 3 to 4 months. 5% minoxidil solution is not recommended for use in females.
CONTRAINDICATIONS
REGAINE® solution is contraindicated in patients with hypersensitivity to minoxidil, propylene glycol or to any of its ingredients.
REGAINE® solution should not be used in patients with history of underlying coronary artery disease, cardiac arrhythmias, congestive heart failure or valvular heart disease. Patients with hypertension, including those under treatment with antihypertensive agents, should be monitored closely and their medication adjusted if necessary. REGAINE® solution should be used with caution in patients with any other cardiovascular disease.
WARNINGS
Although the following systemic effects have not been associated with the use of minoxidil solution, there is some absorption of minoxidil from the skin and the potential exists for systemic effects such as tachycardia, angina, edema or potentiating of the orthostatic hypotension produced by guanethidine. Patients should be observed periodically for any systemic effects of minoxidil.
In the event of systemic side effects, discontinue use of the drug.
If required, fluid retention and edema can be managed with diuretic treatment. Tachycardia and angina can be controlled by administration of beta-adrenergic blocking drugs or other sympathetic nervous system suppressants. Patients should discontinue use of minoxidil solution and contact their physician in the event of systemic effects and/or severe dermatologic reactions.
PRECAUTIONS
Minoxidil solution may cause burning and irritation of the eye. In the event of accidental contact with sensitive surfaces (eye, abraded skin, mucous membranes), the area should be bathed with copious amounts of cool tap water.
Minoxidil solution is for external use only. Accidental ingestion of minoxidil solution could lead to serious adverse effects. The effects of minoxidil solution in patients with concomitant
dermal diseases, or in those using topical corticosteroids or other dermatologic preparations are unknown. It has not been clearly determined whether occlusion, after administration of the solution, will increase the absorption of minoxidil. As is the case with other topically applied drugs, decreased integrity of the epidermal barrier caused by inflammation or disease processes in the skin, may increase percutaneous absorption of minoxidil.
ADVERSE REACTIONS
The most frequently encountered adverse effects in clinical trials with minoxidil solution were minor dermatologic reactions. Local irritation was the most common adverse reaction reported, including scaling, erythema/flushing, dermatitis, dry skin, hypertrichosis (in areas other than where minoxidil solution was applied), burning sensation and rash.
Infrequent adverse reactions including allergic reactions (sensitivity, hives, generalized erythema and facial swelling); dizziness; tingling sensation; headache; weakness; neuritis; edema; eye irritation; altered taste; ear infection (otitis externa);and visual disturbances have been reported. Rarely reported adverse reactions included alopecia, hair abnormalities, chest pain, blood pressure changes, pulse changes, hepatitis, and kidney stones.
DRUG INTERACTIONS
Currently, there are no known drug Interactions associated with the use of minoxidil solution. There exists the possibility of potentiating orthostatic hypotension in patients currently taking guanethidine, although it has not been clinically demonstrated.
USE IN SPECIFIC POPULATIONS
Pregnancy and Lactation
The safety for use of minoxidil solution in pregnancy and lactation has not been established. Orally administered minoxidil has been shown to reduce the conception rate in rats and to show evidence of increased fetal resorption in rabbits when administered at 5 times the human oral dose. There was no evidence of teratogenic effects in rats and rabbits.
Minoxidil solution should not be used by pregnant or nursing women.
Pediatric Use
Safety and effectiveness of minoxidil solution in patients under 18 years of age has not been established.
Geriatric Use
Studies involving subjects over the age of 65 years have not been performed hence the safety and effectiveness of minoxidil solution in these patients has not been established.
CLINICAL PHARMACOLOGY
Pharmacodynamics
When applied topically, minoxidil solution has been shown to stimulate hair growth, in individuals with alopecia androgenetica (male pattern baldness). Although the exact mechanism of action of minoxidil in the treatment of alopecia androgenetica is not known, there may be more than one mechanism by which minoxidil stimulates hair growth which includes:
Vasodilatation of the microcirculation around the hair follicles which may stimulate hair growth.
Direct stimulation of the hair follicle cells to enter into a proliferative phase- resting phase (telogen) follicles being stimulated to pass into active phase (anagen) follicles.
Alteration of the effect of androgens on genetically predetermined hair follicles by inhibiting the capacity of androgens to affect the hair follicles.
There is no evidence of new follicle formation. The new hair arises from existing quiescent terminal hair follicles and from remaining vellus hair follicles. When applied topically, minoxidil has shown conversion of vellus to terminal hair.
Pharmacokinetics
Following topical application of minoxidil solution, minoxidil is poorly absorbed from normal intact skin, with an average of 1.4% (range 0.3 to 4.5%) of the total applied dose reaching the systemic circulation. The effects of concomitant dermal diseases, or occlusion, on absorption are unknown. Serum minoxidil levels resulting from topical administration are governed by the drug's percutaneous absorption rate; increases in surface area of application do not result in proportionate increases in the serum minoxidil level. Steady state is achieved by the end of the third dosing interval (36 hours) when the drug is administered twice daily. Approximately 95% of the systemically absorbed minoxidil from topical dosing is eliminated within 4 days. The metabolic biotransformation of minoxidil absorbed following topical application has not been fully determined.
SYMPTOMS & TREATMENT OF OVERDOSAGE
Overdosage with minoxidil may result from systemic absorption if the medication is applied excessively, no more rapid or better results will be obtained and this will increase the chances of side effects. Accidental ingestion of minoxidil solution may produce systemic effects related to the vasodilatory action of minoxidil. Signs and symptoms of drug overdosage would most likely include cardiovascular effects associated with fluid retention, lowered blood pressure and tachycardia. Fluid retention can be managed with appropriate diuretic therapy.
Tachycardia can be controlled by administration of a beta- adrenergic blocking agent.
If exaggerated hypotension is encountered, it is most likely to occur in association with residual sympathetic nervous system blockade from previous therapy (guanethidine-like effects or alpha adrenergic blockade). The recommended treatment is i.v. administration of normal saline. Sympathomimetic drugs, such as norepinephrine or epinephrine, should be avoided because of their excessive cardiac-stimulating action. Phenylephrine, angiotensin II, vasopressin and dopamine, which reverse the effects of orally administered minoxidil, should only be used if inadequate perfusion of a vital organ is evident.
PHARMACEUTICAL FORM:
REGAINE® is available in concentrations of 2% and 5% in 60 mL bottle.
PHARMACEUTICAL PARTICULARS:
List of Excipients:
Ethanol, Propylene Glycol & Purified Water
Incompatibilities
None known
Shelf Life:
See on outer pack.
Storage and Handling:
Preserve in tight container.
Store below 25°C, Protected from light.
Keep out of reach of children.
Avoid contact with eyes.
Do not take orally.
Nature of Container:
High Density Polyethylene container
Instructions for use/handling:
Dropper Applicator
Remove large outer cap of Regaine® bottle, then remove the inner cap.
Insert the dropper applicator in to the bottle and squeeze the rubber bulb. Release the bulb allowing the dropper to fill to the 1mL line.
Place the tip of the dropper near the part of the scalp you want to treat and gently squeeze the bulb to gradually release the solution. To prevent the solution from running off the scalp, apply a small amount at a time.
Pump-Spray Applicator
(Works best for the large area of baldness)
Remove large outer cap of Regaine® bottle, then remove the Inner cap.
Insert the pump spray applicator in to the bottle and screw on firmly.
Aim the applicator towards the center of the bald area, press the pump once and spread Regaine® with finger tips to cover all bald area. Repeat 6 times (approx. 1mL).
Manufactured by:
Encube Ethicals Pvt. Ltd.,
Plot No. C1, Madkaim Ind. Estate, Madkaim, Post Mardol, Ponda, Goa - 403 404, India.
Marketed by:
JNTL Consumer Health (India) Pvt. Ltd,
Office No. 16, Ground Floor, Admin Block,
L.B.S. Marg, Mulund (West),
Mumbai 400 080.
DATE OF REVISION OF THE TEXT
27 December 2022
Reference: Company Core Data Sheet (CCDS) dated 11 July 2017