Page 1089 - Basic _ Clinical Pharmacology ( PDFDrive )

CHAPTER 61 Dermatologic Pharmacology 1075

cytokines and mediators from mast cells in vitro after stimula- LINDANE (HEXACHLOROCYCLOHEXANE)
tion by antigen-IgE complexes. Tacrolimus is available as 0.03%
and 0.1% ointments, and pimecrolimus is available as a 1% The gamma isomer of hexachlorocyclohexane was commonly
cream. Both are indicated for short-term and intermittent long- called gamma benzene hexachloride, a misnomer, since no ben-
term therapy for mild to moderate atopic dermatitis. Tacrolimus zene ring is present in this compound. Percutaneous absorption
0.03% ointment and pimecrolimus 1% cream are approved for studies using a solution of lindane in acetone have shown that
use in children older than 2 years of age, although all strengths almost 10% of a dose applied to the forearm is absorbed, to be
are approved for adult use. Recommended dosing of both agents subsequently excreted in the urine over a 5-day period. After
is twice-daily application to affected skin until clearing is noted. absorption, lindane is concentrated in fatty tissues, including the
Neither medication should be used with occlusive dressings. The brain.
most common side effect of both drugs is a burning sensation in Lindane is available as a 1% shampoo or lotion. For pedicu-
the applied area that improves with continued use. The US Food losis capitis or pubis, 30 mL of shampoo is applied to dry hair
and Drug Administration (FDA) mandates a black box warning on the scalp or genital area for 4 minutes and then rinsed off.
regarding the long-term safety of topical tacrolimus and pimecro- No additional application is indicated unless living lice are
limus because of animal tumorigenicity data. present 1 week after treatment. Then reapplication may be
required.
Recent concerns about the toxicity of lindane have altered
■ ECTOPARASITICIDES treatment guidelines for its use in scabies; the current recom-
mendation calls for a single 60 mL application to the entire body
PERMETHRIN from the neck down, left on for 8–12 hours, and then washed off.
Patients should be retreated only if active mites can be demon-
Permethrin is toxic to Pediculus humanus, Pthirus pubis, and strated, and never within 1 week of initial treatment.
Sarcoptes scabiei. Less than 2% of an applied dose is absorbed per- Concerns about neurotoxicity and hematotoxicity have resulted
cutaneously. Residual drug persists up to 10 days following appli- in warnings that lindane should be used with caution in infants,
cation. Resistance to permethrin is becoming more widespread. children, and pregnant women. The current USA package insert
It is recommended that permethrin 1% cream rinse (Nix) be recommends that it not be used as a scabicide in premature infants
applied undiluted to affected areas of pediculosis for 10 minutes and in patients with known seizure disorders. Local irritation may
and then rinsed off with warm water. For the treatment of occur, and contact with the eyes and mucous membranes should
scabies, a single application of 5% cream (Elimite, Acticin) is be avoided.
applied to the body from the neck down, left on for 8–14 hours,
and then washed off. Adverse reactions to permethrin include
transient burning, stinging, and pruritus. Cross-sensitization to CROTAMITON
pyrethrins or chrysanthemums has been alleged but inadequately
documented. Crotamiton, N-ethyl-o-crotonotoluidide, is a scabicide with some
antipruritic properties; its mechanism of action is not known.
Studies on percutaneous absorption have revealed detectable levels
SPINOSAD of crotamiton in the urine following a single application on the
forearm.
Spinosad (Natroba) suspension is approved for the topical treat- Crotamiton (Eurax) is available as a 10% cream or lotion. Sug-
ment of head lice in patients 4 years of age and older. Spinosad gested guidelines for scabies treatment call for two applications
is derived from the fermentation of a soil Actinomyces bacterium to the entire body from the chin down at 24-hour intervals, with
and is toxic to P humanus with no appreciable absorption from a cleansing bath 48 hours after the last application. Crotamiton
topical application. It is recommended that the 0.9% suspension is an effective agent that can be used as an alternative to lindane.
be applied to the hair and scalp for 10 minutes and then rinsed Allergic contact dermatitis and primary irritation may occur,
out. A repeat treatment may be applied 1 week later if live lice necessitating discontinuance of therapy. Application to acutely
are present. inflamed skin or to the eyes or mucous membranes should be
avoided.
IVERMECTIN
SULFUR
Ivermectin (Sklice) 0.5% lotion is approved for head lice treat-
ment in patients 6 months of age and older. Ivermectin is toxic Sulfur has a long history as a scabicide. Although it is nonirritat-
to P humanus, resulting in paralysis and death of the parasite. ing, it has an unpleasant odor, is staining, and is thus disagreeable
The pharmacology of ivermectin is discussed in Chapter 53. The to use. It has been replaced by more aesthetic and effective scabi-
lotion should be applied to the hair and scalp and rinsed out after cides in recent years, but it remains a possible alternative drug for
10 minutes. Ivermectin is for single use only and should not be use in infants and pregnant women. The usual formulation is 5%
repeated without health care provider recommendation. precipitated sulfur in petrolatum.