Download Hydroquinone (Topical)

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Hydroquinone (Topical)
Sub-sections

Introduction

Uses

Dosage and Administration

Cautions

Acute Toxicity
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Pharmacology

Pharmacokinetics

Chemistry and Stability

Preparations
Drug Nomenclature
Generic Name: Hydroquinone
CAS Number: 123-31-9
Synonyms: Hydroquinol; Quinol
Synonyms: Active 4; Clairissime clear complexion lotion; Clarite 4;
Continuum unifying lotion i (combination product); Continuum unifying lotion
ii (combination product); Creme blanchissante - crm 2%; Drula fade cream
extra-medicated (combination product); Drula fade cream mediummedicated (combination product); Drula fade cream normal-medicated
(combination product); Drula fade cream superforte medicated (combination
product); Eldopaque crm 2%; Eldopaque forte crm 4%; Eldoquin; Eldoquin
forte; Esoterica facial cream (combination product); Esoterica regular
cream; Esoterica sunscreen fade cream (combination product); Esoterica
unscented; Glyquin xm (combination product); Lustra; Lustra-af
(combination product); Neostrata canada hq plus cream (combination
product); Neostrata hq plus lightening cream (combination product);
Nuderm sunfader (combination product); Palmer's skin success fade creamfor dry skn; Palmer's skin success fade cream-for oily sk; Palmer's skin
success fade cream-normal skin; Seequin 2 ids; Seequin 4 ids; Solaquin
forte; Sunbalance (combination product); Ultraquin 4% hydroquinone cream
with sunscreens (combination product); Vantex skin bleaching crm w
sunscreen 2%
Introduction
Hydroquinone, which is structurally related to monobenzone, is a
depigmenting agent.
Uses
Hyperpigmentation
Hydroquinone is applied topically to gradually reduce hyperpigmentation in
conditions such as freckling (ephelides), inactive chloasma, generalized and
senile lentigo, and other unwanted areas of melanin hyperpigmentation. The
drug also has been used to reduce hyperpigmentation caused by
photosensitization associated with inflammation or with the use of certain
perfumes. Depigmentation produced by hydroquinone varies among patients
in completeness, time of onset, and duration. Although hydroquinone rarely
completely reduces hyperpigmentation and some patients exhibit no
response to the drug, most clinicians consider hydroquinone to be useful in
some patients with hyperpigmentation in which a large excess of melanin is
not being produced. The results of one study indicate that a topical
hydrophilic ointment containing 5% hydroquinone, 0.1% dexamethasone,
and 0.1% tretinoin is more effective and depigments chloasma more rapidly
than does topical hydroquinone alone; however, further studies are needed
to fully assess the safety and efficacy of this combination.
Other Uses
Hydroquinone, in concentrations of less than 1%, is used as an antioxidant
in topical preparations.
Dosage and Administration
Administration
Preparations containing 2–4% hydroquinone are applied topically.
Hydroquinone should not be administered orally.
Dosage
To depigment hyperpigmented skin, a thin layer of hydroquinone cream or
solution should be applied uniformly and rubbed into the pigmented area
twice daily, in the morning and evening. Application of the drug should be
limited to an area equal to that of the face and neck or hands and arms.
Exposure to sunlight should be minimized during treatment (See Cautions:
Precautions and Contraindications); the opaque base in some hydroquinone
preparations (Eldopaque®, Eldopaque Forte®) may provide sufficient
protection from sunlight. If no depigmentation is evident after 2 months of
hydroquinone treatment, the drug should be discontinued. When the desired
degree of depigmentation is obtained, hydroquinone should be applied only
as often as needed to maintain depigmentation.
Cautions
Adverse Effects
Mild skin irritation and sensitization, including burning, stinging, and allergic
dermatitis, have occurred following topical application of hydroquinone and
reportedly occur more frequently with 4% than with 2% concentrations of
the drug. Topical corticosteroids may be used to reduce irritation and
sensitization. Dryness and fissuring of paranasal and infraorbital areas has
also been reported. Chronic use (up to 8 years) of 5% hydroquinone creams
has been reported to produce ochronosis and colloid milium.
Precautions and Contraindications
Hydroquinone is a skin bleaching agent that may produce unwanted
cosmetic effects if not used as directed. The physician should be thoroughly
familiar with the use, adverse effects, and precautions and contraindications
of hydroquinone before prescribing or dispensing the drug. Hydroquinone
should not be used for the prevention of sunburn.
Hydroquinone should not be applied near the eyes; to cut, abraded, or
sunburned skin; after shaving or using a depilatory agent; or over miliaria
rubra (prickly heat). One manufacturer recommends that small amounts of
the commercially available 2 or 4% hydroquinone preparations be applied to
an area of unbroken skin about 25 mm in diameter prior to depigmentation
therapy with the drug to assess the risk of irritation or allergic reactions. The
test site is examined after 24 hours; minor redness is not a contraindication,
but if itching, vesicle formation, or excessive inflammation occurs, treatment
with the drug is not advised. Alternatively, some clinicians recommend use
of an extemporaneously prepared 1% hydroquinone in petrolatum ointment
to test for allergy. If rash or irritation develops during hydroquinone therapy,
treatment should be discontinued, the drug washed off, and a physician
consulted.
Since minimal exposure to sunlight may reverse the bleaching effect of
hydroquinone, unnecessary exposure to sunlight should be avoided during
and after therapy. If hydroquinone preparations which do not contain
sunscreen agents are used during the daytime, sunscreen agents and/or
protective clothing should be used to minimize exposure and prevent
repigmentation of treated areas; alternatively, these preparations should be
used only at night (and the usual preventive measures employed during the
daytime), or daytime use of preparations containing sunscreen agents may
be considered. After reduction of hyperpigmentation and during maintenance
therapy, use of sunscreen agents and/or protective clothing should continue.
Some commercially available topical formulations of hydroquinone contain
sulfites that may cause allergic-type reactions, including anaphylaxis and
life-threatening or less severe asthmatic episodes, in certain susceptible
individuals. The overall prevalence of sulfite sensitivity in the general
population is unknown but probably low; such sensitivity appears to occur
more frequently in asthmatic than in nonasthmatic individuals.
Hydroquinone is contraindicated in patients with a history of sensitivity or
allergic reaction to the drug or any ingredients in the commercially available
preparations.
Pediatric Precautions
Safety and efficacy of hydroquinone in children younger than 12 years of age
have not been established.
Pregnancy, Fertility, and Lactation
Pregnancy
Reproductive studies in animals have not been performed with topical
hydroquinone. It is not known whether hydroquinone can cause fetal harm
when used topically by pregnant women. Topical hydroquinone should be
used during pregnancy only when clearly needed.
Fertility
The effect of hydroquinone on fertility is not known.
Lactation
Since it is not known if topical hydroquinone is absorbed or distributed into
human milk, the drug should be used with caution in nursing women.
Acute Toxicity
Adults ingesting 300–500 mg of hydroquinone daily for 3–5 months have
reported no toxic adverse effects. However, single oral doses of 5–12 g of
hydroquinone have produced symptoms similar to those following phenol
overdosage, including tremors, seizures, and, occasionally, severe hemolytic
anemia.
Systemic overdosage of hydroquinone, like phenol, should be treated with
measures intended to reduce absorption of the drug, including
administration of activated charcoal and gastric lavage, and supportive
therapy.
Pharmacology
Following topical application in animals, hydroquinone increases the
excretion of melanin from melanocytes; the same action is thought to be
responsible for the depigmenting effect of the drug in humans. Some
pharmacologists believe that hydroquinone may also prevent melanin
production. Unlike monobenzone, hydroquinone reportedly does not cause
destruction of melanocytes or permanent depigmentation. Depigmentation
may take 1–4 months to occur while existing melanin is lost with the normal
sloughing of the stratum corneum and excretion of new melanin is increased
by hydroquinone. Hyperpigmented skin appears to fade more rapidly and
completely than does normal skin and exposure to sunlight reduces the
depigmenting effect of the drug. Depigmentation usually persists for 2–6
months following discontinuance of hydroquinone treatment.
Pharmacokinetics
Information on the absorption, distribution, and elimination of hydroquinone
is not available.
Chemistry and Stability
Chemistry
Hydroquinone is structurally related to monobenzone. Hydroquinone occurs
as fine, white needles. The drug is freely soluble in water and in alcohol and
has a pKa of 9.96.
Stability
Commercially available hydroquinone preparations should be stored in lightresistant containers. Hydroquinone darkens upon exposure to light and air
and is incompatible with alkalis, ferric salts, and oxidizing agents.
Preparations
Excipients in commercially available drug preparations may have clinically
important effects in some individuals; consult specific product labeling for
details.
Hydroquinone
Dosage
Brand
Routes Forms Strengths Names
Bulk
Manufacturer
Powder*
Topical Cream
1.5%
Esoterica®
Medicis
Sensitive Skin
(with
parabens and
sodium
bisulfite)
2%
Eldopaque®
(with sodium
metabisulfite
in an opaque
base)
Valeant
Eldoquin®
Valeant
(with sodium
metabisulfite)
Esoterica®
Medicis
Regular (with
parabens,
propylene
glycol, and
sodium
bisulfite)
4%
Eldopaque
Valeant
Dosage
Brand
Routes Forms Strengths Names
Manufacturer
Forte® (with
propylene
glycol and
sodium
metabisulfite
in an opaque
base)
Eldoquin
Valeant
®
Forte (with
propylene
glycol
propylparaben
and sodium
metabisulfite)
Generic
Ethex, Glades
Name:
Hydroquinone
Cream
Melpaque® HP Stratus
(with sodium
metabisulfite
in an opaque
talc base)
Melquin® HP
Stratus
(with
propylparaben
and sodium
metabisulfite)
Solution 3%
Melanex®
Neutrogena
(with SD
alcohol 40
45% isopropyl
alcohol 4%
and propylene
glycol)
Melquin®-3
(with SD
alcohol 45%
Stratus
Dosage
Brand
Routes Forms Strengths Names
Manufacturer
isopropyl
alcohol 4%
and propylene
glycol)
Generic
Glades
Name:
Hydroquinone
Solution
(with SD
alcohol 45%
isopropyl
alcohol 4%
and propylene
glycol)
* available from one or more manufacturer, distributor, and/or repackager
by generic (nonproprietary) name
Hydroquinone Combinations
Dosage
Routes Forms Strengths
Topical Cream
Brand
Names
Manufacturer
2% with
Solaquin®
Valeant
Dioxybenzone (with sodium
3%,
metabisulfite)
Oxybenzone
2%, and
Padimate O
5%
2% with
Oxybenzone
2.5% and
Padimate O
3.3%
Esoterica®
Facial (with
parabens
propylene
glycol and
sodium
bisulfite)
Medicis
Dosage
Routes Forms Strengths
Brand
Names
Esoterica®
Sunscreen
(with
parabens
propylene
glycol and
sodium
bisulfite)
Manufacturer
Medicis
4% with
Nuquin® HP
Stratus
Dioxybenzone (with sodium
3%, and
metabisulfite)
Oxybenzone
2%
4% with
Dioxybenzone
3%,
Oxybenzone
2%, and
Padimate O
8%
Hydroquinone Ethex, Glades
with
Sunscreens
(with sodium
metabisulfite)
Solaquin
Valeant
®
Forte (with
propylene
glycol and
sodium
metabisulfite)
Viquin Forte® Valeant
(with
propylene
glycol and
sodium
metabisulfite)
Gel
4% with
Nuquin® HP
Stratus
Dioxybenzone (with alcohol
3%
and sodium
metabisulfite)
4% with
Generic
Dioxybenzone Name:
Glades
Dosage
Routes Forms Strengths
3%, and
Padimate O
5%
Brand
Names
Manufacturer
Hydroquinone
Forte Gel
(with sodium
metabisulfite)
Solaquin
Valeant
Forte® (with
propylene
glycol and
sodium
metabisulfite)
AHFS Drug Information. © Copyright, 1959-2013, Selected Revisions
December 1, 2003. American Society of Health-System Pharmacists, Inc.,
7272 Wisconsin Avenue, Bethesda, Maryland 20814.
AHFS Drug Information © American Society of Health-System Pharmacists 2013
MedicinesComplete © The Pharmaceutical Press 2014