ACTISITE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ACTISITE (ACTISITE).
Tetracycline antibiotic that inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, preventing aminoacyl-tRNA from binding to the A site.
| Metabolism | Not significantly metabolized; primarily excreted unchanged in urine and feces. |
| Excretion | Primarily eliminated by phagocytic degradation at the application site; minimal systemic absorption, negligible renal or biliary excretion. |
| Half-life | Not applicable due to local degradation; systemic half-life is negligible as tetracycline hydrochloride is not absorbed. |
| Protein binding | Not applicable (no systemic absorption); if systemically present, tetracycline is 50-60% bound to plasma proteins. |
| Volume of Distribution | Not applicable due to lack of systemic absorption; if systemic, tetracycline Vd is 1.3-1.6 L/kg. |
| Bioavailability | Negligible systemic bioavailability (<0.1%) when applied topically; not administered orally or intravenously for periodontal use. |
| Onset of Action | Therapeutic effect on periodontal pockets observed within 2-3 days following subgingival application. |
| Duration of Action | Sustained release over 7-10 days; clinical improvement maintained for up to 12 weeks post-treatment. |
| Molecular Weight | Tetracycline hydrochloride: 480.9 Da per molecule (tetracycline: 444.4 Da as base) |
Topical application of tetracycline hydrochloride 10 mg/g periodontal fiber. Inserted into periodontal pocket and left in place for 10 days.
| Dosage form | FIBER, EXTENDED RELEASE |
| Renal impairment | Not systemically absorbed; no renal adjustment required. |
| Liver impairment | Not systemically absorbed; no hepatic adjustment required. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment; use standard adult dosing with caution for age-related comorbidities. |
| 1st trimester | Contains tetracycline hydrochloride, which is contraindicated in pregnancy due to risk of fetal skeletal and dental abnormalities, hepatotoxicity, and inhibition of bone growth. Avoid use. |
| 2nd trimester | Same risks as t1. Contraindicated. |
| 3rd trimester | Consult provider for 3rd trimester safety assessment. |
Clinical note
Comprehensive clinical and safety monograph for ACTISITE (ACTISITE).
| Placental transfer | Tetracyclines cross the placenta readily; fetal serum levels reach 60-75% of maternal levels. |
| Breastfeeding | Excreted in breast milk; may cause dental discoloration and bone growth inhibition in infants. Avoid use in breastfeeding mothers. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
PregnancyBreastfeedingHypersensitivity to tetracyclines or any componentSevere renal impairment (if systemic absorption is a concern, though Actisite is topical, systemic effects are minimal but caution advised)
| Precautions | Photosensitivity, Superinfection with resistant organisms, Use in renal impairment may require dose adjustment, Not recommended in children under 8 years due to permanent tooth discoloration |
| Food/Dietary | No direct food interactions. Avoid eating on the treated side to prevent dislodgement of the fiber. Maintain soft diet to minimize trauma. Avoid alcohol-based mouthwashes. |
Loading safety data…
| L5 - Contraindicated |
| Teratogenic Risk | FDA Pregnancy Category C. No adequate studies in pregnant women. In animal studies, tetracycline hydrochloride (active component) caused fetal toxicity (skeletal malformations, reduced fetal weight) at doses 1-2 times the human dose. First trimester: potential for teratogenicity (neural tube defects, cardiovascular anomalies). Second and third trimesters: risk of permanent tooth discoloration (yellow-gray-brown) and enamel hypoplasia in the fetus; also potential for inhibition of fetal bone growth and maternal hepatotoxicity. Use only if potential benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal liver function tests (especially in prolonged therapy), renal function, and signs of superinfection. For fetus, monitor for potential growth restriction and signs of congenital anomalies if exposure occurs during first trimester. For pregnant women, perform periodic complete blood counts (CBC) and assess for photosensitivity. Avoid use after 4 months' gestation due to fetal tooth and bone effects. |
| Fertility Effects | In animal studies, tetracycline has been associated with reduced fertility in male rats (decreased spermatogenesis) at high doses. Human data limited; no significant impact on female fertility reported. Use with caution in patients planning conception. |
| Clinical Pearls |
| ACTISITE (tetracycline hydrochloride) periodontal fiber is a controlled-release local antibiotic for adjunctive treatment of chronic periodontitis. Insert fiber into periodontal pocket to deliver drug over 10 days. Ensure pocket depth is ≥5mm. Do not use with metallic or synthetic fibers. Fiber must be secured with cyanoacrylate adhesive. Monitor for foreign body sensation, pain, or infection. Removal at 10 days is mandatory to avoid excessive tissue reaction. Not for acute abscesses. |
| Patient Advice | Do not brush or floss the treated area while the fiber is in place. · Avoid chewing hard or sticky foods on the treated side. · You may feel a mild foreign body sensation; report severe pain or swelling. · The fiber must be removed after 10 days; do not leave it longer. · Complete the full course of prescribed oral hygiene and antibiotics if given. |