Rosacea Medication

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

Topical metronidazole is commonly used as a first-line agent. Topical azelaic acid, sulfacetamide products, and topical acne medications are also commonly used. Retinoids are advocated by some authorities.^{[15, 16, 17]}

In addition to the agents listed below, anecdotal evidence indicates effective treatment of rosacea with medications that reduce flushing, including beta-blockers, clonidine, naloxone, ondansetron, and selective serotonin reuptake inhibitors.

Oral contraceptive therapy has been helpful in patients who provide historical information of worsening rosacea with their hormonal cycle.

Dapsone has been used in severe, refractory rosacea, and dapsone has been particularly beneficial for patients who cannot take isotretinoin.^[18]

Class Summary

These agents inhibit immune reactions resulting from diverse stimuli.^[19]

Tacrolimus ointment (Protopic)

Reduces itching and inflammation by suppressing release of cytokines from T cells. Also inhibits transcription of genes encoding IL-3, IL-4, IL-5, GM-CSF, and TNF-alpha, all of which are involved in early stages of T-cell activation. Additionally, may inhibit release of preformed mediators from skin mast cells and basophils, and may down-regulate expression of FCeRI on Langerhans cells. Can be used in patients as young as 2 y. Drugs of this class are more expensive than topical corticosteroids. Available as ointment in concentrations of 0.03% and 0.1%. Indicated only after other treatment options have failed.

Class Summary

Since the 1950s, oral antibiotics have been prescribed off label for treatment because microorganisms were thought to be the underlying cause of disease. In current practice, experts do not believe bacterial infection plays a part in the pathogenesis of rosacea; however, the observed clinical benefits of oral antibiotics have allowed this treatment option to remain in favor for both physicians and patients. Since 2006, nonantibiotic dosing of doxycycline has become first-line treatment for many clinicians. In many cases, oral and topical antibiotics are used in combination; the oral treatment is eventually withdrawn and the topical treatment is used alone as maintenance therapy.^[18]

In patients who require a systemic antibiotic, evidence suggests that the newer regimen of 40 mg of doxycycline is as effective as the older regimen of 100 mg of doxycycline^[20] For many patients, this could represent a significant cost reduction.

Metronidazole gel 0.75% or 1% (MetroGel, Noritate, Flagyl, Protostat)

Imidazole ring–based antibiotic active against various anaerobic bacteria and protozoa.

Oral metronidazole has been shown to be beneficial against papules and pustules of acne rosacea.

Topical applications are helpful for mild disease and as an adjuvant to systemic therapy.

Erythromycin (E.E.S., E-Mycin, Eryc, Ery-Tab) tab or 2% topical solution

Inhibits bacterial growth, possibly by blocking dissociation of peptidyl tRNA from ribosomes, causing RNA-dependent protein synthesis to arrest. For treatment of staphylococcal and streptococcal infections.

In children, age, weight, and severity of infection determine proper dosage. When bid dosing is desired, half-total daily dose may be taken q12h. For more severe infections, double the dose.

Can be used when tetracyclines are not tolerated or are contraindicated.

Used for the treatment of ocular rosacea.

Fusidic acid (Fucithalmic)

Ophthalmic susp as 10 mg/g (1%) (0.2 g) unit-dose, without preservative; 3 g and 5 g in multidose contains benzalkonium chloride.

For the treatment of ocular rosacea. Topical antibacterial that inhibits bacterial protein synthesis, causing bacterial death. Rosacea may respond to topical fusidic acid for at least 3 mo.

Clindamycin topical

Semisynthetic antibiotic produced by 7(S)-chloro substitution of 7(R)-hydroxyl group of parent compound lincomycin. Inhibits bacterial growth, possibly by blocking dissociation of peptidyl tRNA from ribosomes, causing RNA-dependent protein synthesis to arrest. Widely distributes in body without penetration of CNS. Protein bound and excreted by liver and kidneys.

Upon application to skin, drug is converted to active component, which inhibits the microorganism.

Available as topical solution, lotion, or gel for external use. Solution contains equivalent of 10 mg/mL clindamycin.

Effective against mild-to-moderate papulopustular rosacea.

Tetracycline (Sumycin)

Inhibits bacterial protein synthesis by binding with 30S and possibly 50S ribosomal subunit(s). Has anti-inflammatory activity. Improvement is evident within 2-4 mo after commencement of therapy.

Minocycline (Dynacin, Minocin, Solodyn)

Treats infections caused by susceptible gram-negative and gram-positive organisms, in addition to infections caused by susceptible P acnes. The extended-release tablet (Solodyn) has a variety of doses ranging from 45 mg up to 135 mg and can be administered once daily.

Doxycycline (Oracea, Bio-Tab, Doryx, Periostat, Vibramycin)

Broad-spectrum, synthetically derived, bacteriostatic antibiotic in tetracycline class. Almost completely absorbed, concentrates in bile, and is excreted in urine and feces as a biologically active metabolite in high concentrations.

Inhibits protein synthesis and, thus, bacterial growth by binding to 30S and possibly 50S ribosomal subunits of susceptible bacteria. May block dissociation of peptidyl tRNA from ribosomes, causing RNA-dependent protein synthesis to arrest.

Clarithromycin (Biaxin)

Semisynthetic macrolide antibiotic that reversibly binds to P site of 50S ribosomal subunit of susceptible organisms and may inhibit RNA-dependent protein synthesis by stimulating dissociation of peptidyl tRNA from ribosomes, causing bacterial growth inhibition.

Class Summary

These agents decrease the cohesiveness of abnormal hyperproliferative keratinocytes and may reduce the potential for malignant degeneration. They modulate keratinocyte differentiation, and they have been shown to reduce the risk of skin cancer formation in patients who have undergone renal transplantation.

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

Structurally related to vitamin A. May be helpful for recalcitrant disease, but recurrence is common. Long-term, low-dose therapy may be suitable for selected patients.

May cause skin irritation in some patients. Has been linked to promotion of angiogenesis; however, has not demonstrated increased telangiectasias.

Inhibits microcomedo formation and eliminates lesions. Makes keratinocytes in sebaceous follicles less adherent and easier to remove. Available as 0.025%, 0.05%, and 0.1% creams. Available also as 0.01% and 0.025% gels.

Isotretinoin (Accutane)

Oral agent that treats serious dermatologic conditions. Synthetic 13-cis isomer of naturally occurring tretinoin (trans -retinoic acid). May be helpful for recalcitrant disease, but recurrence is common. Long-term, low-dose therapy may be suitable for selected patients.

A US Food and Drug Administration–mandated registry is now in place for all individuals prescribing, dispensing, or taking isotretinoin. For more information on this registry, see iPLEDGE. This registry aims to further decrease the risk of pregnancy and other unwanted and potentially dangerous adverse effects during a course of isotretinoin therapy.

Class Summary

These agents are relatively contraindicated, except as a short course in rosacea fulminans.

Prednisolone (AK-Pred, Delta-Cortef, Articulose-50, Econopred)

Moderately high doses may be helpful in rosacea fulminans. Decreases inflammation by suppressing migration of PMN leukocytes and reducing capillary permeability. Use in combination with isotretinoin. Rosacea fulminans is treated with moderately high doses of prednisolone (30-60 mg/d) followed by oral isotretinoin.

Class Summary

Potassium-sparing diuretics can be used to reduce morbidity.

Spironolactone (Aldactone)

Competes with aldosterone for receptor sites in distal renal tubules, increasing water excretion while retaining potassium and hydrogen ions.

Aldosterone inhibitors help block the renin-angiotensin system and help prevent potassium loss in distal tubules. The body conserves potassium, and less oral potassium supplementation is needed.

Class Summary

Some products in this category can be effective in patients with papules, pustules, and the phymatous and glandular types of rosacea.

Benzoyl peroxide (Benoxyl, Benzac, Oxy-5, Fostex)

Free-radical oxygen is released upon administration and oxidizes bacterial proteins in sebaceous follicles, decreasing quantity of irritating free fatty acids and of anaerobic bacteria. Converted on skin into benzoic acid, which has keratolytic and comedolytic effects. However, can be quite irritating in patients with barrier dysfunction and can cause further erythema. Available over the counter and by prescription.

Available in 2.5%, 5%, and 10% gels, lotions, creams, or washes.

Azelaic acid (Azelex, Finacea)

Available in 2 strengths azelaic acid 15% gel (Finacea) or azelaic acid 20% cream (Azelex). Effective against mild-to-moderate papulopustular rosacea. Can be used twice daily as initial treatment. May reduce production of ROS by neutrophils. Some patients report transient burning or stinging.

Sodium sulfacetamide and sulfur (Plexion, Clenia, Rosanil wash, Rosula gel or wash, Rosac cream, Sulfacet-R lotion, Clarifoam EF)

Contains 5% sulfur and 10% sodium sulfacetamide. Used topically for acne rosacea. Sodium sulfacetamide has antibacterial properties, whereas sulfur is considered an antiseptic with keratolytic action.