Keloid and Hypertrophic Scar Medication

Updated: May 29, 2020
  • Author: Brian Berman, MD, PhD; Chief Editor: Dirk M Elston, MD  more...
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Medication

Medication Summary

The goals of pharmacotherapy are to reduce morbidity and prevent complications.

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Corticosteroids

Class Summary

These agents have profound and varied metabolic effects. They possess anti-inflammatory and immunosuppressive properties. The most commonly used corticosteroid is triamcinolone acetonide  (TAC).

Triamcinolone (Aristospan, Kenalog-10)

Triamcinolone decreases inflammation by suppressing the migration of polymorphonuclear leukocytes and reversing capillary permeability. It is approved by US Food and Drug Administration (FDA) for use in keloids.

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Immunomodulators

Class Summary

This is a family of glycoproteins produced mainly by eukaryotic cells when induced by viral and nonviral triggers. Antiviral properties include induction of 2'-5' A synthetase, ribonuclease L, and protein kinase P1. Antiproliferative properties include induction of 2'-5' A synthetase, inhibition of growth factors, enhancement of p53, and down-regulation of c-myc, c-fos, and certain c-ras. Immunoregulatory properties include induction of class I and II MHC antigens, increase of natural killer cells, and inhibition of the production of TH-2 cytokines.

Interferon alfa-2b (Intron-A)

This is a protein product manufactured by recombinant DNA technology. Its mechanism of antitumor activity is not clearly understood; however, direct antiproliferative effects against malignant cells and modulation of host immune response may play important roles. Its immunomodulatory effects include suppression of tumor cell proliferation, enhancement of macrophage phagocytic activity, and augmentation of lymphocyte cytotoxicity. It is not approved by the FDA for use in hypertrophic scars and keloids.

Interferon beta 1a (Avonex, Rebif)

This is a protein product manufactured by recombinant DNA technology. Its mechanism of antitumor activity is not clearly understood; however, direct antiproliferative effects against malignant cells and modulation of host immune response may play important roles. Its immunomodulatory effects include suppression of tumor cell proliferation, enhancement of macrophage phagocytic activity, and augmentation of lymphocyte cytotoxicity. It is not approved by the FDA for use in hypertrophic scars and keloids.

Interferon alfa-n3 (Alferon N)

Interferon alfa is a protein product either manufactured from a single-species recombinant DNA process or obtained from pooled units of donated human leukocytes that have been induced by incomplete infection with a murine virus.

The mechanisms by which interferon alfa exerts antiviral activity are not understood clearly. However, modulation of the host immune response may play an important role.

Peginterferon alfa 2b (PEG Intron, PegIntron Redipen, Sylatron)

PEG-IFN consists of IFN alfa-2b attached to a single 12-kd PEG chain. It is excreted by the kidneys. PEG-IFN has sustained absorption, a slower rate of clearance, and a longer half-life than unmodified IFN, which permits more convenient once-weekly dosing and significantly improves quality of life for patients.

Pegylated interferon alfa-2a (Pegasys)

PEG-IFN alfa-2a consists of IFN alfa-2a attached to a 40-kd branched PEG molecule. PEG-IFN has sustained absorption, a slower rate of clearance, and a longer half-life than unmodified IFN, which permits more convenient once-weekly dosing and significantly improves quality of life for patients.

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Calcium Channel Blockers

Class Summary

Treatment of keloids and hypertrophic scars with verapamil has shown a reduction in vascularity, pliability, height, and width of the lesions.

Verapamil (Isoptin, Calan, Verelan PM)

Verapamil blocks the synthesis and secretion of extracellular matrix molecules and increases fibrinase. It is not approved by the FDA for use in hypertrophic scars and keloids.

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Antineoplastic Agents

Class Summary

These agents inhibit cell growth and proliferation.

Bleomycin

Injections cause necrosis of keratinocytes. It is not approved by the FDA for use in hypertrophic scars and keloids.

Fluorouracil topical (Adrucil)

Fluorouracil is a pyrimidine analog that inhibits fibroblastic proliferation in tissue culture and is believed to reduce postoperative scarring by decreasing fibroblast proliferation. It is not approved by the FDA for use in hypertrophic scars and keloids.

Doxorubicin (Adriamycin)

Doxorubicin irreversibly inactivates prolyl 4-hydroxylase in human skin fibroblasts and inhibits collagen alpha-chain assembly.  It is not approved by the FDA for use in hypertrophic scars and keloids.

Tamoxifen

Tamoxifen competitively binds to estrogen receptors, producing a nuclear complex that decreases DNA synthesis and inhibits estrogen effects.

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Retinoid-like Agents

Class Summary

These agents decrease normal tonofilament and keratohyalin synthesis, increase the production of mucoid substances and the epidermal cell growth rate, and inhibit DNA synthesis in vitro.

Tretinoin topical (Retin-A, Retin-A Micro, Renova)

Although the exact mechanism of action is unknown, retinoids decrease the cohesiveness of abnormal hyperproliferative keratinocytes, modulate keratinocyte differentiation, and have anti-inflammatory properties. It is not approved by the FDA for use in hypertrophic scars and keloids.

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Immunosuppressants

Class Summary

These agents inhibit immune processes that promote inflammation.

Tacrolimus ointment (Protopic)

Tacrolimus suppresses release of cytokines from T cells. It also inhibits transcription for genes that encode interleukin 3 (IL-3), IL-4, IL-5, granulocyte-macrophage colony-stimulating factor (GM-CSF), and tumor necrosis factor–alpha (TNF-alpha), all of which are involved in the early stages of T-cell activation.

Additionally, tacrolimus may inhibit release of preformed mediators from skin mast cells and basophils and may down-regulate expression of high-affinity IgE receptor (FCeRI) on Langerhans cells. It is not approved by the FDA for use in hypertrophic scars and keloids.

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Topical Skin Products

Class Summary

The agent imiquimod has been reported to show some efficacy. However, the mechanism of action of imiquimod cream in treating keratosis is unknown.

Imiquimod (Aldara, Zyclara)

Imiquimod is an immune response modifier currently approved for the treatment of genital and perianal warts. It is capable of inducing IFN-alpha, TNF-alpha, IL-1, IL-6, and IL-8. Studies using 5% cream in mice showed significant induction of IFN-alpha at the application site occurring as early as 2 hours after treatment. At 4 hours after application, increases in IFN-alpha mRNA levels were found, indicating an increase in transcription. It is not approved by the FDA for use in hypertrophic scars and keloids.

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