When systemic therapy is used for acne, oral and topical agents are often given simultaneously. The objective, if possible, is to discontinue or taper the oral agent based on the clinical response. A risk-benefit calculation is particularly important whenever you are treating a benign condition, such as acne
Compared with topical therapy,
systemic therapy has a more rapid onset of clearing, which may enhance patient compliance. However, whenever systemic drugs are administered, the potential dangers- including side effects, drug allergy/intolerance, drug interactions, and fetal exposure in women who are or may become pregnant-must be carefully considered.
ANTIBIOTICS
Oral antibiotics are used in the management of moderate- to-severe acne and acne-like disorders, such as rosacea. The tetracyclines are the usual drug of choice; of the tetracyclines, minocycline is considered the gold standard. Both the tetracyclines and the less frequently used erythromycin preparations inhibit the growth of Propionibacterium acnes, which decreases free fatty acid production and pustule formation.
TETRACYCLINES
The tetracylines are the workhorses in systemic acne therapy. They have the disadvantage of staining teeth in children under age 9, and in fact, they may temporarily stain the teeth of older patients, particularly those with orthodontic braces.
DOXYCYCLINE
Somewhat less expensive and probably less effective than minocycline, doxycycline is well absorbed and may be taken with food. Its main disadvantage is its phototoxic potential-the highest of the tetracyclines. Patients should be advised regarding sun protection.
ERYTHROMYCIN
This drug is a useful alternative when tetracycline fails or is not tolerated, when the patient is younger than 10 years old, or when the patient is pregnant. Although it is always best to avoid, whenever possible, the use of systemic drugs in a woman who is pregnant, trying to become pregnant, or breast-feeding, in exceptional circumstances, erythromycin can be given.
HORMONAL TREATMENT
Oral contraceptives or systemic antiandrogens (such as spironolactone) are used in women in whom hormonal treatment may be an effective alternative or adjuvant to antibiotics and oral retinoids. Hormonal treatment is an option when conventional topical and systemic therapies are not working or when an androgenic endocrine abnormality is found.
ORAL CONTRACEPTIVES
By suppressing gonadotropins, reducing ovarian androgen secretion, and increasing sex hormone-binding globulin levels, oral contraceptives decrease serum testosterone concentrations. Oral contraceptives may be used in women older than 15 years who have no known contraindications to this form of therapy. They are often prescribed to prevent pregnancy in patients who are given 13-cis-retinoic acid.
SPIRONOLACTONE
A steroidal androgen receptor blocker, spironolactone is effective for hormonal acne and hirsutism. It is generally given concomitantly with oral contraceptives. Spironolactone may cause menstrual irregularities (usually metrorrhagia). Normal menses may resume with a reduction of the dosage. Spironolactone may also feminize a male fetus, which is another reason it should be administered with oral contraceptives.
FLUTAMIDE
A weak inhibitor of testosterone synthesis, flutamide is a nonsteroidal androgen receptor blocker approved for the treatment of prostate cancer. Although it is infrequently used, flutamide may prove to be effective in treating hormonal acne coexisting with hirsutism.
CYPROTERONE
An acetate steroidal androgen receptor blocker and potent progestin, cyproterone acts as a competitive inhibitor
of testosterone and dehydroepiandrosterone at the level of androgen receptors. Diane-35, an oral contraceptive that is very effective in the treatment of acne but not available in the United States, contains a combination of cyproterone acetate and ethinyl estradiol. Apparently, an association with liver tumors in beagles has prevented its approval by the Food and Drug Administration for use in the United States.
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