Hydroquinone

D11A - Other dermatological preparations ATC D11AX11 Small molecule approved 2002 Topical Natural product

JFDA label: Fediquin Cream

Mechanism of Action

Produces reversible depigmentation of the skin by suppression of melanocyte metabolic processes, in particular the inhibition of the enzymatic oxidation of tyrosine to DOPA (3,4-dihydroxyphenylalanine); sun exposure reverses this effect and will cause repigmentation.

Indications

Approved

Skin bleaching

Contraindications

Source: Lexicomp

Hypersensitivity to hydroquinone or any component of the formulation Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Skin and subcutaneous tissue disorders (6)

Not Known Allergic skin reaction · dermatitis · erythema · inflammation · stinging of the skin · xeroderma

General disorders and administration site conditions (1)

Not Known Local irritation

Dosing

Source: Lexicomp

Skin bleaching: Topical: Apply a thin layer to the affected areas and rub in well twice daily, in the morning and at bedtime Discontinue use if no improvement is seen after 2 to 3 months of treatment.

Skin bleaching: Children ≥12 years and Adolescents: Refer to adult dosing.

Refer to adult dosing.

There are no dosage adjustments provided in the manufacturer's labeling.

Warnings & Precautions

Source: Lexicomp

Appropriate use

Limit application to area no larger than face and neck or hands and arms.

Pregnancy & Lactation

Pregnancy

FDA category C

Animal reproduction studies have not been conducted with topical administration; the amount of systemic absorption is unknown.

Lactation

It is not known if hydroquinone is excreted in breast milk. The manufacturer recommends that caution be exercised when administering hydroquinone to nursing women

Chemistry & Properties

Formula	C6H6O2
Molecular weight	110.11 g/mol
IUPAC name	benzene-1,4-diol
CAS	123-31-9
PubChem CID	785
InChIKey	`QIGBRXMKCJKVMJ-UHFFFAOYSA-N`
logP	1.1 (XLogP 0.6)
Polar surface area	40.46 Å²
H-bond acceptors / donors	2 / 2
Drug-likeness (QED)	0.49
Lipinski violations	0

SMILES

Oc1ccc(O)cc1

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability	70.0%
Half-life	1.765 h
Volume of distribution	0.937 L/kg
Protein binding	24.2%
BBB penetrant	No

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Inhibitor	—
CYP2C8	Inhibitor	—
CYP2D6	Substrate	—

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (6)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Tretoquin	Cream 0.025 %, 2 %	30 g tube	Arab Center for Pharmaceuticals & Chemicals	3.800
Jolite Cream	Cream 4.00 %	30 GM/1 TUB	JERASH PHARMACEUTICALS LTD.CO/JORDAN	3.820
Fediquin Cream	Cream 4 %	30 g tube	Pharma International Company/ Jordan	4.950
philaquin with AHA Gel	Gel 2.0 %WW, 10 %WW	30 gm	Philadelphia Pharmaceuticals	5.000
Eldoquin Cream	Cream 4 %	28.35 grams	Khoury Drug Store	6.460
Triderma	Cream 0.05 %, 4 %, 0.01 %	30 g tube	PELLA PHARMACEUTICALS CO.LTD/JORDAN	11.510