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Dermatologic Toxicities of Chemotherapeutic Agents

Manouchkathe Cassagnol, PharmD Assistant Clinical Professor of Clinical Pharmacy Practice, College of Pharmacy and Allied Health Professions, St. John’s University, Queens, New York;
Clinical Coordinator of Internal Medicine Pharmacotherapy,
Department of Pharmacy, Long Island Jewish Medical Center, New Hyde Park, New York   Henry Cohen, MS, PharmD, FCCM, BCPP, CGP Associate Professor of Pharmacy Practice,
Arnold & Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, New York;
Chief Pharmacotherapy Officer, Director of Pharmacy Residency Programs (PGY-1 & PGY-2),
Kingsbrook Jewish Medical Center, Department of Pharmacy Services, Brooklyn, New York

2/20/2008

US Pharm. 2008;33(1):10-18.

ABSTRACT: Despite advancements in chemotherapy treatments, dermatologic complications continue to be associated with chemotherapeutic agents. These adverse effects include alopecia, hyperpigmentation, nail changes, palmar-plantar erythrodysesthesia, extravasation, and radiation reactions. This article reviews the general dermatologic adverse effects of chemotherapeutic agents and discusses their pharmacologic and nonpharmacologic management.

Chemotherapy has been proven efficacious for the treatment of cancer; however, these treatments are often associated with serious toxicities. Chemotherapeutic agents generally target rapidly dividing cells and consequently are toxic to organ systems with high metabolic rates, such as bone marrow, hair, nails, skin, and the gastrointestinal mucosa. Adverse effects associated with chemotherapy such as myelosuppression, chemotherapy-induced emesis, diarrhea, mucositis, and stomatitis are well appreciated in the literature. However, there is a paucity of data and guidelines for the management of dermatologic toxicities. Despite much advancement in chemotherapy, dermatologic complications continue to be associated with both older and newer chemotherapeutic agents. The dermatologic toxicities may be the most psychologically detrimental and have been shown to have a major negative impact on quality of life, specifically when treating women's cancers.1 Dermatologic toxicities of chemotherapy often include alopecia, pigment and nail changes, palmar-plantar erythrodysesthesia (PPE), chemotherapy-induced extravasation (CIE), radiation recall, and photosensitivity.

Chemotherapy-Induced Alopecia

Terminal hair follicles with the most rapid hair matrix formation, such as those on the scalp, are affected more than slower growing hair such as eyebrows, eyelashes, axillary, and pubic hair.2 Hair growth occurs in three separate phases during the hair life cycle: the anagen, telogen, and catagen phases. During the anagen phase, hair undergoes mitotic changes and rapid cell growth. In the telogen phase, hair is dormant and mitotic activity is arrested. The telogen phase lasts from three to six months. In the final catagen phase, the hair root is separated from the hair bulb, pigment storage is terminated, and the club-shaped root end is pushed out from the bulb. Less than 1% of hair is in the catagen phase at any time.2,3 Chemotherapy-induced alopecia frequently occurs during the anagen phase, which results in suppression of cell production and thinner, more brittle hair. This affect is typically seen within two to three weeks of therapy and resolves within two to three months of discontinuation of treatment, often noted with a change of hair color and texture.4,5 Another mechanism by which chemotherapy can induce alopecia involves the transition between anagen and telogen. Hair breakage is caused by the hair being prematurely forced into the telogen phase. Examples of chemotherapeutic agents that are associated with hair loss are listed in TABLE 1.




Minoxidil: Topical minoxidil 2% is the only pharmacologic agent that has been studied in the treatment of chemotherapy-induced alopecia. Minoxidil is a pyrimidine N-oxide used as an antihypertensive agent when administered orally and for male-pattern baldness when used topically. Minoxidil modifies hair cycle dynamics, by prolonging the anagen phase as demonstrated in the animal model. 6 Minoxidil 2% was ineffective for the treatment of chemotherapy-induced alopecia in past studies.5,7 However, a randomized, placebo-controlled study of 43 female cancer patients receiving doxorubicin-based chemotherapy investigated the use of topical minoxidil 2% applied twice daily starting 24 hours before the first course of chemotherapy. 8 Minoxidil 2% did not prevent alopecia; however, it significantly decreased the duration of alopecia.8 Clinicians may use topical minoxidil prophylactically to reduce the length of time that patients are exposed to this aesthetically displeasing effect of chemotherapy.

Scalp Tourniquets: Scalp tourniquets temporarily occlude, by pressure, superficial blood vessels that supply the scalp, which can minimize drug contact with hair follicles. 9 The scalp tourniquet is inflated 10 mm Hg above the patient's systolic blood pressure to occlude superficial scalp circulation. The tourniquet should be applied when plasma drug levels are highest, e.g., during the last 10 minutes of infusion and for 10 minutes after it is stopped. Scalp tourniquets are not recommended for use in leukemias or lymphomas, due to the risk of metastases. The most common adverse effect is scalp numbness. A randomized, controlled study investigating the use of tourniquets found that they were ineffective in treating chemotherapy-induced alopecia.10

Scalp Hypothermia: Scalp hypothermia prevents chemotherapy-induced alopecia by two mechanisms: 1) it causes vasoconstriction and reduces the blood flow to hair follicles during peak plasma concentrations of the chemotherapeutic agents, thus reducing cellular uptake; and 2) it reduces biochemical activity, which makes hair follicles less susceptible to the damage of chemotherapeutic agents. 11 Scalp cooling procedures are done by use of an ice or cold gel cap. The most common adverse effects are headaches, complaints of coldness, and/or uncomfortable sensations. Scalp cooling is contraindicated in cases of cold sensitivity, cold agglutinin disease, cryoglobulinemia, cryofibrinogenemia, and hematological malignancies. Cancers with a high prevalence of scalp metastases (i.e., leukemia and lymphoma), carry a risk of cancer recurrence on the scalp, when using cooling methods to prevent hair loss.12,13† This is due to a reduction of drug delivery to the scalp, which allows cancer cells to thrive.

Several randomized controlled studies have shown that scalp cooling resulting in a reduction of alopecia is both statistically and clinically significant.14-17 No distinct method of scalp cooling has been described; however, a cooling time of approximately 90 minutes postinfusion has been suggested.17 Liver dysfunction or the presence of liver metastasis was related to less benefit in several nonrandomized trials.18-20 Although more efficacious, scalp cooling is associated with more adverse effects than scalp tourniquets. Prior to using scalp tourniquets or scalp hypothermia therapy, careful screening must be conducted by clinicians to prevent any long-term adverse effects.

Chemotherapy-Induced Hyperpigmentation and Nail Changes
Pigment Changes: Hyperpigmentation is a common cutaneous adverse effect of cancer chemotherapeutic agents. Hyperpigmentation can occur locally at the site of infusion or diffusely.2 The nails, mucous membranes, and teeth have all been reported sites of discoloration.2 Some of the mechanisms of chemotherapy-induced hyperpigmentation that have been postulated include: 1) drug deposition in certain areas that subsequently lead to increased pigmentation; 2) direct skin toxicity caused by secretion of drug in sweat with accumulation of drug on the skin; 3) endocrinologic abnormalities with increased adrenocorticotrophic hormone and melanocyte-stimulating hormone causing hyperpigmentation as a result of suppressed adrenal function; 4) depletion of tyrosinase inhibitors resulting in increased pigmentation; and 5) direct toxic effects on epidermal melanocytes stimulating increased melanin production.17 Some hyperpigmentation may be irreversible, but often resolves after discontinuation of the chemotherapeutic agent. The pigment changes are mainly a cosmetic concern as they have not been associated with any negative clinical sequelae. There is no treatment available for this adverse effect. Patients should be counseled about the risk of developing pigment changes when starting the chemotherapeutic agents listed in TABLE 2 .




Nail Changes: The nail plate is made up of the hard keratin cover of the dorsal portion of the distal phalanx and as it grows the distal part of the nail matrix generates the deeper layers of the plate.21 The epithelium of the nail matrix is made up of rapidly proliferating cells that differentiate and keratinize to generate the nail plate, making it susceptible to the toxicities of chemotherapy.22 Nail changes seen with the use of chemotherapy are both cosmetically displeasing (nail discoloration) and can result in onycholysis (separation of the nail plate from the nail bed)--which can be painful and may lead to infection.21 Taxanes (e.g., docetaxel and paclitaxel) are most notorious for causing onycholysis.22 These nail changes have been attributed to a cessation of mitotic activity in the nail matrix, which produces a horizontal depression of the nail plate or complete separation of the nail plate from the nail bed (Figure 1).23 After several weeks of chemotherapy, Beau's lines (darkened horizontal lines) or Mees' lines (horizontal white lines) appear on the nail bed. Beau's and Mees' lines move with normal nail growth and disappear within six months. 23,24 Chemotherapeutic agents that cause nail changes include 5-fluorouracil, bleomycin, cyclophosphamide, daunorubicin, docetaxel, doxorubicin, epirubicin, hydroxyurea, and paclitaxel.2

Treatment: No current pharmacological therapies are available for the treatment of chemotherapy-induced nail changes and only one nonpharmacological therapy is available. The Elasto-Gel (84400 APT Cedex, Akromed, France) frozen glove (FG) is a glycerin-containing glove with thermal properties, allowing its use in hot or cold therapies.25 The FG causes vasoconstriction of the blood vessels that supply the hand, which then minimizes the amount of chemotherapy reaching the nail matrix. In a phase II, multicenter, matched case-control study, patients wore the frozen FG for 90 minutes starting 15 minutes prior to receiving chemotherapy. Overall, skin toxicity was reduced by approximately 50% with the use of the FG.25 Persons who should not receive FG therapy include those with Raynaud's phenomenon, distal metastases, ungual pathology, arteriopathy, cold intolerance, or peripheral neuropathy. 25 Excluding any contraindications, one can initiate FG therapy, especially with the use of taxanes for cancer therapy.

Chemotherapy-Induced Palmar-Plantar Erythrodysesthesia (PPE)
PPE, also termed hand-foot syndrome or chemotherapy-associated acral erythema, is a common adverse effect of 5-fluorouracil, capecitabine, and liposomal doxorubicin. 26 Chemotherapeutic agents that have sustained blood levels are more likely to cause this reaction.26 PPE typically presents with dysesthesia and tingling in the hands and feet, which usually appear 2 to 12 days after the administration of chemotherapy. These symptoms may progress, three to four days later, into symmetrical edema and erythema of the palms and soles. Erythematous plaques with violaceous and edematous patches in the palms, soles, and other high-pressure areas are usually mild and resolve in one to two weeks. However, PPE may evolve into blistering desquamation, crusting, ulceration, and epidermal necrosis.27 PPE results from the rupture of small capillaries in the palms of the hands and soles of the feet with increased pressure from walking or use, leading to the extravasation of chemotherapy which creates an inflammatory reaction.26 The treatment of PPE depends on the severity of ulceration; however, there is a paucity of data discussing the management of capecitabine and 5-fluorouracil-induced PPE. Guidelines for the management of doxorubicin-induced PPE include dose reduction and delay of chemotherapy ( TABLE 3).



Nonpharmacologic Treatment: A nonpharmacological method of preventing PPE is hypothermia treatment. In a retrospective study, regional cooling was performed by applying ice packs around the patients' wrist and ankles during chemotherapy and 24 hours postchemotherapy treatment.28 Patients were also instructed to avoid direct sunlight, hot foods and liquids, hot water contact, and undue friction to the hands and feet for 72 hours postchemotherapy. The regional cooling protocol was found to be effective in significantly reducing the frequency and severity of PPE.28 The greatest obstacle in this method of treatment would be patient compliance with the protocol.

Pharmacologic Treatment: The pharmacologic agents used to prevent and treat PPE include pyridoxine, dexamethasone, amifostine, celecoxib, Bag Balm, and dimethyl sulfoxide (DMSO).29-33

Pyridoxine: Pyridoxine (vitamin B6) has been investigated because of the similarities between PPE and acrodynia (chronic mercury poisoning that results in irritability, photophobia, pink discoloration of hands and feet, and polyneuritis).28 In a phase I, observational study investigating the use of pyridoxine in 23 cancer patients with solid tumors, pyridoxine 50 mg orally three times daily was given on days 2 to 21 of each cycle in patients taking cisplatin and paclitaxel. No cases of grade 3/4 PPE were observed and grade 1/2 PPE occurred in four of 18 patients.29 Randomized, placebo-controlled trials that would provide more robust findings are lacking. However, pyridoxine is inexpensive and relatively nontoxic, therefore, supplemental pyridoxine 150 to 200 mg daily can be recommended to patients on chemotherapy for prevention of PPE.

Dexamethasone: Corticosteroids have been investigated for the management of PPE due to their anti-inflammatory properties. Kollmannsberger et al studied high-dose dexamethasone 8 mg twice daily in combination with pyridoxine 100 mg twice daily given on days 1 through 5 of each cycle. Only 12 of the 27 patients studied had grade 3 or higher PPE.30 Drake et al conducted a randomized, placebo-controlled trial in which the use of dexamethasone alone prevented further delay of chemotherapy or dose reduction when compared to patients who did not receive dexamethasone.31 Therefore, dexamethasone 8 mg twice daily, with or without pyridoxine or an equivalently dosed corticosteroid, may be used in patients to reduce the frequency and severity of PPE. However, the many adverse effects of corticosteroids (e.g., hyperglycemia, psychosis, electrolyte imbalances, hypertension) may limit its use.

Amifostine: Amifostine, a cytoprotective adjuvant used in cancer chemotherapy, has been reported to reduce the incidence of grade 3/4 PPE.32 In a crossover study of 22 patients with solid tumors, intravenous amifostine 500 mg was administered on days 1, 3 or 4, and 8 during treatment with pegylated liposomal doxorubicin.32 Although in this study and in clinical trials amifostine did not interfere with the clinical efficacy of chemotherapy, it is not recommended to be used in patients receiving chemotherapy or radiotherapy for other malignancies in which chemotherapy or radiotherapy can produce a significant survival benefit or cure (e.g., certain malignancies of germ cell origin), due to the risk of the reduced antitumor efficacy of chemotherapy.33 Other serious adverse effects of amifostine include hypotension, hypersensitivity reactions with anaphylaxis, and hypocalcemia.33 Due to its many toxicities and limited efficacy data, amifostine should only be reserved for patients who are refractory to all other therapies and can tolerate treatment.

Celecoxib: Celecoxib, a COX-2 inhibitor known to attenuate the inflammatory response, has also been studied in the prevention of capecitabine-induced PPE. A retrospective study comparing the incidences of hand-foot syndrome in 67 patients with metastatic colorectal cancer was undertaken. The study found that celecoxib given at 400 mg twice daily reduced the incidence and frequency of capecitabine-induced PPE.34 The drawback is that chronic use of celecoxib at high doses increases the risk of serious adverse cardiovascular thrombotic events, in patients who may already have underlying hypercoagulability. In the Prevention of Sporadic Colorectal Adenomas with Celecoxib trial, the relative risk for the composite endpoint of cardiovascular death, mycardial infarction, or stroke was 3.4 (95% CI, 1.4 to 8.5) for celecoxib 400 mg twice daily and 2.5 (95% CI, 1.0 to 6.4) for the celecoxib 200 mg twice daily compared to placebo.35 Although there is data that suggest positive outcomes, further studies should be conducted before using such a high-risk medication in this subset of patients.

Topical Treatments: Topical agents used to treat PPE include emollients, aloe vera lotion, and moisturizing creams such as Bag Balm, a topical petroleum-lanolin-based ointment with the antiseptic ingredient 8-hydroxyquinoline sulfate, to maintain skin integrity.28 In a nonrandomized trial of 39 cancer patients, Bag Balm was evaluated for its effects on PPE.36 Bag Balm was applied three times daily to the affected areas at the first signs and symptoms of PPE; this therapy was associated with an improvement in skin appearance and resulted in no delays or reduction of chemotherapy.36 This study did not mention the use of concomitant therapies (e.g., routine wound care and topical antibiotics); therefore, one cannot definitively conclude that the use of Bag Balm alone is effective. Due to its low toxicity, Bag Balm may be recommended in patients with the initial signs and symptoms of PPE.

Dimethyl Sulfoxide: Dimethyl sulfoxide (DMSO), a potent free-radical scavenger, has been investigated for the treatment of PPE. In a small observational study, 99% DMSO applied four times daily to the affected areas for 14 days resulted in symptom resolution over one to three weeks.37 Large randomized trials are lacking in investigating DMSO for the treatment of PPE. However, the initial findings in this pilot study do show promising results, making DMSO a drug that may be considered for use in the treatment of PPE.




Chemotherapy-Induced Extravasation
Extravasation occurs when there is an inadvertent leaking of intravenous fluid during medication administration which, in turn, leads to tissue damage.23 The accidental extravasation of intravenous drug occurs in approximately 0.1% to 6% in patient receiving chemotherapy.23,38,39 Risk factors for extravasation include the size and type of vein chosen for administration of drug, recent venipuncture, and limited vein selection.39 Steps that can be taken to minimize the incidence of extravasation include the use of the forearm as the preferred site of infusion, performing only one venipuncture, taping the needle in place, and testing the IV site.24 Extravasation results in local reactions ranging from local irritation to severe tissue necrosis of the skin, surrounding vasculature, and supporting structures.40 More severe reactions are seen with vesicants (i.e., cisplatin, dactinomycin, daunorubicin, idarubicin, mechlorethamine, mithramycin, mitomycin-C, mitoxantrone, paclitaxel, vinblastine, vincristine, and vinorelbine) as compared to irritants (i.e., carmustine , dacarbazine, etoposide, and streptozocine).2 Vesicants are highly reactive chemicals that combine with proteins, DNA, and other cellular components, which result in cellular changes immediately after exposure. Irritants produce irritation after exposure to tissue but do not combine with proteins and tissue DNA.2 Treatment modalities for extravasation include immediate discontinuation of chemotherapy and cooling of the site (TABLE 4). To reduce the morbidity associated with extravasation, it is vital that clinicians focus on prevention and develop expertise in its management.

Radiation Recall and Sensitivity
Radiation reactions can be subdivided into four categories: radiation enhancement, radiation recall, photosensitivity reaction, and sunburn reactivation.1 Radiation reactions are varied and range from a maculopapular rash to a generalized exfoliative, ulcerative dermatitis. Enhanced radiation effects that occur with chemotherapy may be caused by an agent's ability to interfere with enzyme-mediated radiation repair. Chemotherapy agents are known to inhibit some of the enzymes and synthetic mechanisms needed to repair tissue. 24 Enhancement reactions may occur when chemotherapy is given concomitantly with radiation or within one week of radiation.24 In contrast, the recall phenomenon may develop over several weeks to years after radiation therapy, when a chemotherapy agent causes an inflammatory reaction in tissues previously treated with radiation.2,24 Chemotherapy may also interact with ultraviolet (UV) light to produce similar effects. Reactivation of sunburn is a variation of the recall phenomenon and is most commonly associated with methotrexate.24 Chemotherapy agents that have reactions to radiation or UV light are listed in TABLE 5. Patients should be counseled on the appropriate use of sunscreens and cautioned to avoid unnecessary sun exposure.2




Conclusion

Dermatological toxicities associated with chemotherapy are common. However, the dearth of information available makes the management of these dermatological toxicities difficult. Clinicians should become more cognizant of the dermatological adverse effects of oncology drugs and radiation in order to minimize the morbidity associated with these devastating toxicities.

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