DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

as monotherapy or in combination with other medications, such as
topical corticosteroids, for the treatment of localized plaque psoriasis.
Topical corticosteroids improve the efficacy of therapy and
reduce the side effects of burning, itching, and skin irritation that are
commonly associated with tazarotene.
Alitretinoin
Alitretinoin (PANRETIN) is a retinoid that binds all types of retinoid
receptors and is applied two to four times daily to cutaneous
lesions of Kaposi sarcoma. Alitretinoin should not be applied concurrently
with insect repellants containing diethyltoluamide
(DEET, N,N-diethyl-m-toluamide) because it may increase DEET
absorption.
Bexarotene
Topical bexarotene (TARGRETIN) is approved for early-stage (IA and
IB) cutaneous T-cell lymphoma. Its application is titrated up from
every other day to two to four times daily over several weeks to
improve patient tolerance. Its mechanism of action may involve
downregulation of survivin and upregulation of caspase-3, leading to
apoptosis of malignant cells (Sami and Harper, 2007). Patients using
bexarotene should avoid products containing DEET due to an
increased risk for DEET toxicity.
Systemic Retinoids
Systemic retinoids are approved for the treatment of
acne, psoriasis, and cutaneous T-cell lymphoma
(Table 65–5). Off-label uses include ichthyosis,
Darier’s disease, pityriasis rubra pilaris, rosacea,
hidradenitis suppurativa, chemoprevention of malignancy,
lichen sclerosus, subacute lupus erythematosus,
and discoid lupus erythematosus. All systemic retinoids
are contraindicated in women who are pregnant, contemplating
pregnancy, or breast-feeding. Relative
contraindications include leukopenia, alcoholism,
hyperlipidemia, hypercholesterolemia, hypothyroidism,
and significant hepatic or renal disease.
Toxicity and Monitoring. Acute retinoid toxicities may
include mucocutaneous or laboratory abnormalities;
bony changes may occur after chronic use at high doses.
Mucocutaneous side effects may include cheilitis, xerosis,
blepharoconjunctivitis, cutaneous photosensitivity,
Table 65–5
Systemic Retinoids
RECEPTOR
STANDARD
DRUG STRUCTURE SPECIFICITY DOSING RANGE t 1/2
Isotretinoin H
H
No clear receptor 0.5-2 mg/kg/day 10-20 hours
H
affinity
H
H
H
O
O
H
Etretinate O
RAR-, 0.25-1 mg/kg/day 80-160 days
H H
RAR-,
O RAR-
H H H H
O
Acitretin O RAR-, 0.5-1 mg/kg/day 50 hours
H
H
RAR-,
O
H
RAR-
H H H H
O
Bexarotene RXR-, 300 mg/m 2 /day 7-9 hours
RXR-,
RXR-
O H
O