Hydroquinone

Drug class: Antineoplastic Agents

Usage of Hydroquinone

Hyperpigmentation

Used to reduce hyperpigmentation in conditions such as freckling (ephelides), inactive chloasma, melasma, generalized and senile lentigo, and other unwanted areas of melanin hyperpigmentation.

Used for gradual treatment of ultraviolet-induced dyschromia and skin discoloration resulting from the use of oral contraceptives, pregnancy, hormone replacement therapy, or skin trauma.

Most clinicians consider hydroquinone to be useful in some patients with hyperpigmentation in which a large excess of melanin is not being produced.

Has been used to reduce hyperpigmentation caused by photosensitization associated with inflammation or with the use of certain perfumes.

Used in combination with fluocinolone and tretinoin for short-term and intermittent long-term treatment of moderate to severe melasma.

Relate drugs

How to use Hydroquinone

General

  • Depigmentation varies among patients in completeness, time of onset, and duration; rarely completely reduces hyperpigmentation and some patients exhibit no response to the drug.
  • May require 1–4 months for depigmentation effects to occur. Following discontinuance of hydroquinone, depigmentation effects usually persist for 2–6 months.
  • Avoid unnecessary exposure to sunlight during and after therapy.
  • Prior to initiating therapy, assess the risk of irritation or allergic reactions by applying a small amount of hydroquinone preparation to an area of unbroken skin. After 24 hours, examine test site; discontinue treatment if itching, vesicle formation, or excessive inflammation occurs; however, minor redness is not a contraindication for further treatment.

    • Administration

    Topical Administration

    Apply topically to the skin as a cream, gel, emulsion, or solution. (See Sensitivity Reactions under Cautions.)

    Limit application to an area equal to that of the face and neck or hands and arms.

    For dermatologic use only; avoid contact with eyes. If such contact occurs, flush the affected eye(s) with copious amounts of water and contact a clinician.

    Not for oral administration.

    Apply hydroquinone cream, gel, emulsion, or solution (with or without sunscreens) uniformly to pigmented area and rub into skin. Do not rub cream containing opaque sunblocking agents (e.g., talc) into the skin.

    If hydroquinone preparations without sunscreen agents are applied during the daytime, use sunscreen agents and/or protective clothing to minimize exposure and prevent repigmentation of treated areas; alternatively, apply these preparations only at night.

    Gently wash face and neck with mild soap, rinse, and pat dry before applying fixed-combination hydroquinone, fluocinolone, and tretinoin cream to affected area(s).

    Apply a small amount of fixed-combination hydroquinone, fluocinolone, and tretinoin cream to affected area(s), including about ½ inch of normal skin surrounding each lesion. Rub lightly and uniformly into the skin. Do not use occlusive dressing.

    Dosage

    When the desired degree of depigmentation is obtained, apply only as often as needed to maintain depigmentation.

    Pediatric Patients

    Hyperpigmentation Topical

    Adolescents >12 years of age: Apply hydroquinone cream, emulsion, gel, or solution (with or without sunscreens) uniformly to pigmented area(s) and rub in well twice daily, in the morning and evening.

    If improvement does not occur after 2 months of treatment, discontinue the drug.

    Adults

    Hyperpigmentation Topical

    Hydroquinone cream, emulsion, gel, or solution (with or without sunscreens): Apply uniformly to pigmented area(s) and rub in well twice daily, in the morning and evening or as directed by a clinician.

    Hydroquinone cream with opaque sunblock: Apply uniformly to the pigmented area(s) twice daily, in the morning and evening; do not rub into affected area(s).

    If improvement does not occur after 2 months of treatment, discontinue the drug.

    Melasma Topical

    Fixed-combination hydroquinone, fluocinolone, and tretinoin cream: Apply a thin layer uniformly to the affected area(s) once daily, in the evening, at least 30 minutes before bedtime. Continue daily for as long as the melasma lesions persist. Discontinue treatment when melasma resolves.

    If melasma reoccurs, repeat treatment until condition resolves.

    Prescribing Limits

    Pediatric Patients

    Hyperpigmentation Topical

    Adolescents >12 years of age: Maximum 2 months of therapy if no improvement is seen.

    Adults

    Hyperpigmentation Topical

    Maximum 2 months of therapy if no improvement is seen.

    Melasma Topical

    Fixed-combination hydroquinone, fluocinolone, and tretinoin cream has been safely administered for cumulative ≥180 days.

    Special Populations

    Geriatric Patients

    Clinical studies of 4% hydroquinone cream did not include sufficient number of patients ≥65 years of age to determine whether they respond differently from younger patients. In general, dosage selection for geriatric patients should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy.

    Warnings

    Contraindications

  • History of sensitivity or allergic reaction to hydroquinone or any ingredient in the formulation.

    • Warnings/Precautions

    Warnings

    Cosmetic Effects

    May produce undesired cosmetic effects (e.g., excessive skin bleaching) if not used as directed. Clinician should be familiar with the use, adverse effects, precautions, and contraindications before prescribing or dispensing the drug.

    Exposure to Sunlight or Ultraviolet Light

    Exposure to sunlight or ultraviolet light may cause repigmentation of bleached areas. Avoid unnecessary exposure to sunlight during and after therapy.

    Sunscreen agents and/or protective clothing recommended if preparations which do not contain sunscreen are applied during the daytime. Preparations containing sunscreen may provide sufficient protection from sunlight.

    After reduction of hyperpigmentation and during maintenance therapy, continue the use of sunscreen agents and/or protective clothing.

    Sensitivity Reactions

    Sulfite Sensitivity

    Some formulations contain sulfites, which may cause allergic-type reactions (including anaphylaxis and life-threatening or less severe asthmatic episodes) in certain susceptible individuals.

    Other Sensitivity Reactions

    Contact dermatitis reported. If contact dermatitis occurs, discontinue immediately and contact a clinician.

    Major Toxicities

    Rarely, ochronosis (gradual blue-black darkening of the skin) and colloid milium reported with chronic use (up to 8 years) of 5% hydroquinone cream. If affected skin changes to a blue-black color, discontinue immediately and contact a clinician.

    General Precautions

    Topical Use

    For external use only. Notfor topical application in the eyes, ears, or mouth; to cut, abraded, or sunburned skin; after shaving or using a depilatory agent; or over miliaria rubra (prickly heat).

    Dermatologic Effects

    Possible local skin irritation (e.g., burning, stinging, mild erythema). Dryness and fissuring of paranasal and infraorbital areas reported.

    Use of Fixed Combinations

    When hydroquinone is used in fixed combination with topical sunscreens (e.g., dioxybenzone, oxybenzone, and padimate), fluocinolone, or retinoids (e.g., tretinoin), consider the cautions, precautions, and contraindications associated with these agents.

    Specific Populations

    Pregnancy

    Category C.

    Lactation

    Not known if topical hydroquinone is distributed into milk. Caution advised if topical hydroquinone is used.

    Pediatric Use

    Safety and efficacy of hydroquinone preparations not established in children <12 years of age.

    Safety and efficacy of the fixed-combination hydroquinone, fluocinolone, and tretinoin cream not established in pediatric patients of any age.

    Common Adverse Effects

    Mild skin irritation and sensitization (e.g., burning, erythema, stinging).

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