ACTICLATE CAP
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ACTICLATE CAP (ACTICLATE CAP).
Inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, blocking aminoacyl-tRNA binding.
| Metabolism | Primarily hepatic; metabolites include 4-epimino derivatives; not significantly metabolized via CYP450. |
| Excretion | Renal (60-70% as unchanged drug), fecal (20-30% as metabolites); minor biliary elimination |
| Half-life | Terminal elimination half-life 6-10 hours; prolonged in renal impairment (up to 22 hours in anuria) |
| Protein binding | 90-95% bound to serum proteins, primarily albumin |
| Volume of Distribution | 0.75 L/kg (50-70 L in adults); distributes well into tissues including bone, teeth, and synovial fluid |
| Bioavailability | Oral: 90-100% (capsule); food or dairy reduces absorption by up to 50% |
| Onset of Action | Oral: 1-2 hours; IV: immediate |
| Duration of Action | Oral: 12-24 hours; IV: 12-24 hours; clinically, bacteriostatic effect persists beyond serum levels |
350 mg orally once daily, increased to 350 mg twice daily if no response after 2 weeks.
| Dosage form | CAPSULE |
| Renal impairment | eGFR 30-59 mL/min: 350 mg once daily; eGFR <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B or C: 175 mg once daily. |
| Pediatric use | Not established for children <12 years; for ≥12 years, same as adult dosing. |
| Geriatric use | Initiate at 175 mg once daily; titrate cautiously based on renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ACTICLATE CAP (ACTICLATE CAP).
| Breastfeeding | Tetracyclines are excreted in breast milk but absorption by the infant is limited due to chelation with milk calcium; M/P ratio for doxycycline is approximately 0.3-0.4. Theoretical risk of tooth staining and bone inhibition, but clinical significance is low with short-term use; caution with prolonged therapy. |
| Teratogenic Risk | First trimester: Category D; tetracyclines can cause fetal harm including inhibited bone growth and discoloration of teeth (yellow-gray-brown). Second and third trimesters: Known to cause permanent tooth discoloration (enamel hypoplasia) and reversible inhibition of bone growth; use contraindicated after 15 weeks gestation. |
■ FDA Black Box Warning
Photosensitivity: severe sunburn can occur with sun exposure; discontinue if photosensitivity occurs. Tooth development: use during tooth development (last half of pregnancy, infancy, childhood to age 8) may cause permanent tooth discoloration. Bone growth: may retard bone growth in premature infants. Renal toxicity: may cause azotemia, hyperphosphatemia, and acidosis. Avoid in renal impairment.
| Serious Effects |
Hypersensitivity to tetracyclines, pregnancy, breastfeeding, children under 8 years, renal impairment, and concurrent use with oral retinoids.
| Precautions | Photosensitivity, tooth discoloration, bone growth retardation, renal impairment, hepatotoxicity, increased intracranial pressure, superinfection, and use in pregnancy/lactation. |
| Food/Dietary | Avoid food and beverages for at least 1 hour before and after administration, as they can reduce the efficacy of activated charcoal. Do not mix with milk or ice cream, as they decrease binding capacity. Administer with water or a non-carbonated, non-alcoholic drink. |
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| Fetal Monitoring | Monitor liver function, renal function, and complete blood count periodically in the mother. For the fetus/infant: assess for potential effects on skeletal and dental development if exposed in utero or during breastfeeding; no specific fetal monitoring required but consider ultrasound for bone growth if prolonged exposure. |
| Fertility Effects | Tetracyclines have no direct effect on fertility; however, infection treated with this drug may impact reproductive health if untreated. No known impact on spermatogenesis or oogenesis. |
| Clinical Pearls | ACTICLATE CAP is a high-dose activated charcoal formulation used for acute poisoning or overdose. Administer within 1 hour of ingestion for optimal efficacy. Do not use in patients with impaired consciousness unless the airway is protected. Monitor for vomiting and ensure rapid administration via nasogastric tube if necessary. Not effective for alcohols, metals, or caustics. |
| Patient Advice | Take ACTICLATE CAP only if directed by a healthcare professional after a poisoning or overdose. · This medication is not for regular use; it is a one-time emergency treatment. · Avoid taking this with food or drinks; take on an empty stomach for best absorption of toxins. · You may experience black stools or vomiting; this is normal. · Seek immediate medical attention if you have trouble swallowing, severe vomiting, or signs of bowel obstruction. |