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Minocycline (Mucosal-Local)

Primary: OR900

Commonly used brand name(s): Arestin.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).


Antibacterial (dental) —


General considerations
A 9-month, two-center study in a small number of patients found a slight increase in the numbers of minocycline-resistant bacteria in single-site plaque samples taken before and after treatment with minocycline.{01} However, the clinical significance of these findings is not known.{01}

A phase three, 56-day study found no changes in the presence of minocycline-resistant bacteria, Candida albicans, or Staphylococcus aureus in the gastrointestinal tract.{01}


Periodontitis (treatment adjunct)—Minocycline periodontal system is indicated as an adjunct to scaling and root planing to reduce pocket depth in adults with periodontitis.{01}

Acceptance not established
The safety and efficacy of minocycline periodontal system for use in acutely abscessed periodontal pockets have not been established.{01} Therefore, use is not recommended.{01} Minocycline periodontal system has not been clinically tested for use in the regeneration of alveolar bone, either in preparation for, or in conjunction with, the placement of endosseous (dental) implants or in the treatment of failing implants.{01} It also has not been clinically tested in immunocompromised patients, such as those immunocompromised by chemotherapy, diabetes, infection with human immunodeficiency virus (HIV), or radiation therapy.{01}


Physicochemical characteristics:

Chemical group—
    A broad-spectrum semisynthetic tetracycline.{01}
Molecular weight—
    Minocycline hydrochloride: 493.94{01}

Mechanism of action/Effect:

Minocycline is a member of the tetracycline class of antibiotics, which are broad-spectrum bacteriostatic agents that act by inhibiting protein synthesis{01} by blocking the binding of aminoacyl-tRNA (transfer RNA) to the mRNA (messenger RNA)-ribosome complex. Reversible binding occurs primarily at the 30 S ribosomal subunit of susceptible organisms. Bacterial cell wall synthesis is not inhibited.{03}

In vitro testing has shown that Porphyromonas gingivalis, Prevotella intermedia , Fusobacterium nucleatum, Eikenella corrodens, and Actinobacillus actinomycetemcomitans , which are associated with periodontal disease, are susceptible to minocycline at concentrations £ 8 mcg per mL (mcg/mL).{01}

No overgrowth of opportunistic organisms, such as yeast, was observed.{01} However, therapy may result in the overgrowth of nonsusceptible organisms, including fungi, as is true with other antibiotic preparations.{01}

Peak serum concentration:

Gingival fluid—1000 times less than that of saliva following a mean dose of 46.2 mg.{01}

Duration of action:

The minimum inhibitory concentrations (MICs) of common periodontal pathogens are maintained for at least 14 days.{02}

Precautions to Consider


Dietary administration of minocycline in long-term tumorigenicity studies in rats resulted in evidence of thyroid tumor production. Minocycline has also been found to produce thyroid hyperplasia in rats and dogs. In addition, there has been evidence of oncogenic activity (development of adrenal and pituitary tumors) in rats studied with a related antibiotic, oxytetracycline.{01}

Minocycline demonstrated no potential to cause genetic toxicity in the following mutagenicity assays: bacterial reverse mutation assay (Ames Test), an in vitro mammalian gene cell mutation test (L5178Y/TK+/- mouse lymphoma assay), an in vitro mammalian chromosome aberration test, and an in vivo micronucleus assay conducted in ICR mice.{01}

Fertility and general reproduction studies have provided evidence that minocycline impairs fertility in male rats.{01}

Studies have not been done in humans.{01} However, it has been demonstrated in animals that tetracyclines, such as minocycline, cross the placenta.{01} Use of tetracyclines is not recommended during the last half of pregnancy since they may cause permanent discoloration of teeth, enamel hypoplasia, and inhibition of skeletal growth in the fetus.{01} Permanent discoloration of teeth is more common during long-term use of tetracyclines, but also has been observed following repeated short-term courses.{01} Before use during pregnancy, or if pregnancy occurs during treatment with minocycline, the patient should be informed of the potential risks.{01}

In animal studies, tetracyclines have been found to cause fetotoxicity, often related to retardation of skeletal development. Also, tetracyclines administered early in pregnancy have been found to cause embryotoxicity.{01}

FDA Pregnancy Category D.{01}


Tetracyclines are distributed into human breast milk. Use of minocycline is not recommended in nursing mothers because of the risk of permanent discoloration of teeth and enamel hypoplasia in the infant. Because of the potential for serious adverse reactions in nursing infants from tetracyclines, a decision should be made whether to discontinue nursing or discontinue the medication, taking into account the importance of the medication to the mother.{01}


In infants and children up to 8 years of age, tetracyclines may cause permanent discoloration of teeth and enamel hypoplasia.{01} Therefore, use of minocycline is not recommended.{01} Safety and efficacy have not been established in children 8 years of age or older.{01}


No information is available on the relationship of age to the effects of minocycline in geriatric patients.

Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).

Risk-benefit should be considered when the following medical problems exist
Candidiasis, oral, history of or predisposition to{01}    (caution is recommended;{01} safety and efficacy in treatment of periodontitis in patients with coexisting oral candidiasis have not been established{01})

Sensitivity to minocycline or other tetracyclines{01}

Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Incidence more frequent
—greater than 5%     
Dental pain {01}
gingivitis {01}(bleeding from gums; redness or swelling of gums)
infection {01}(chills; fever)
stomatitis {01}(pain, redness, and swelling in the mouth)
tooth caries {01}(toothache)
tooth disorder {01}

Incidence less frequent
—5% or less    
Dental infection {01}(bad taste in mouth; discharge from gums; foul breath odor; redness or swelling of gums)
mouth ulceration {01}(painful sores in the mouth)
mucous membrane disorder {01}

Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent
—greater than 5%     
Headache {01}

Incidence less frequent
—5% or less    
Dyspepsia (acid or sour stomach; belching; heartburn; indigestion; stomach discomfort, upset, or pain){01}
flu-like syndrome {01}(abdominal pain; chills; cough; headache; pain in joints or muscles; runny nose; sneezing; sore throat)
pain {01}
pharyngitis (sore throat){01}
photosensitivity {01}(increased sensitivity to sunlight)

Note: If skin erythema occurs as a result of a photosensitivity reaction, treatment should be discontinued.{01}

Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Minocycline (Dental).
In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before receiving this medication
»   Conditions affecting use, especially:
Sensitivity to minocycline or other tetracyclines

Pregnancy—In animals, tetracyclines cross the placenta and appear in fetal tissues ;tetracyclines have been found to cause fetotoxicity, often related to retardation of skeletal development; tetracyclines administered early in pregnancy have been found to cause embryotoxicity; use of tetracyclines is not recommended during the last half of pregnancy since they may cause permanent discoloration of teeth, enamel hypoplasia, and inhibition of skeletal growth

Breast-feeding— Tetracyclines are distributed into breast milk; use is not recommended because of the risk of permanent discoloration of teeth and enamel hypoplasia in the infant

Proper use of this medication
Avoiding actions that may dislodge the medication
Not chewing hard, crunchy, or sticky foods for 1 week after treatment

Not brushing near treated areas; waiting 12 hours after the procedure before brushing other teeth

Not using interproximal cleaning devices for 10 days after treatment

Not probing or picking at treated areas with the tongue, toothpicks, or fingers
» Proper dosing

Precautions while receiving this medication
» Checking with dentist as soon as possible if pain, swelling, or other problems occur in treated areas

Importance of not missing dental appointments

» Avoiding excessive sunlight or artificial ultraviolent light after receiving minocycline; wearing protective clothing and applying sun block; checking with dentist or doctor if a severe reaction occurs

Signs of potential side effects, especially dental pain, gingivitis, infection, stomatitis, tooth caries, tooth disorder, dental infection, mouth ulceration, and mucous membrane disorder

General Dosing Information
Minocycline powder is composed of bioadhesive microspheres microencapsulated in a bioresorbable polymer, Poly (glycolide-co-dl-lactide [PGLA]).{01}{02} Upon subgingival administration into periodontal pockets, the microspheres activate and adhere to tissue when they come into contact with moisture.{02} This product requires administration by an oral health care professional.{01} Administration is accomplished by inserting the unit-dose cartridge into the specially designed handle.{04} The tip of the cartridge is then inserted into the base of the periodontal pocket, and the thumb ring on the handle mechanism is pressed to expel the powder while gradually withdrawing the tip from the base of the pocket.{01}{04} The handle mechanism should be sterilized between patients.{01}

Each specially designed unit-dose cartridge contains 1 mg of minocycline (enough minocycline for one periodontal pocket) and requires no preparation before administration.{01}

Local anesthesia is not required.{01} Periodontal dressings and adhesives also are not required.{01} And because the microspheres are bioresorbable, they do not have to be removed.{01}

The effects of prolonged treatment (longer than 6 months) have not been studied.{01}

Mucosal-Local Dosage Forms

Note: Strength and dose of minocycline periodontal system are expressed in terms of the base.{01}

Usual Adult Dose
Periodontitis (treatment adjunct)
Subgingival, dosing is dependent on the size, shape, and number of periodontal pockets being treated. {01}

Usual pediatric dose
Infants and children up to 8 years of age—Use is not recommended because minocycline may cause permanent discoloration of teeth and enamel hypoplasia.{01}

Children 8 years of age or older—Safety and efficacy have not been established.{01}

Strength(s) usually available

1 mg (base) (Rx) [Arestin{01}]

Packaging and storage:
Store at 20 to 25 °C (68 to 77 °F), and 60% relative humidity (RH), excursions permitted to 15 and 30 ºC (59 and 86 ºF).{01}

Avoid exposure to excessive heat.{01}

Preparation of dosage form:
Remove the disposable cartridge from its pouch and connect it to the handle mechanism.{01}

Developed: 08/02/2001
Revised: 03/06/2002

  1. Product Information: Arestin™, minocycline. OraPharma, Warminster, PA (PI issued 02/2001) reviewed 5/2001.
  1. Arestin: effective and easy to administer. Accessed on May 16, 2001. Available at
  1. Hardman JG, Limbird LE, Molinoff PB, Ruddon RW, Goodman Gilman A, editors. Goodman and Gilman's the pharmacological basis of therapeutics. 9th ed. New York: McGraw-Hill, 1996: 1123-53.
  1. Manufacturer comment, 08/20/2001.
  1. Nomenclature and Labeling Expert Committee Meeting, 12/11/2001.