Tetracycline

Pronunciation

(tet ra SYE kleen)

U.S. Brand Names

Sumycin®

Synonyms

Achromycin; TCN; Tetracycline Hydrochloride

Generic Available

Yes: Capsule

Canadian Brand Names

Apo-Tetra®; Novo-Tetra; Nu-Tetra

Use

Treatment of susceptible bacterial infections of both gram-positive and gram-negative organisms; also infections due to Mycoplasma , Chlamydia , and Rickettsia ; indicated for acne, exacerbations of chronic bronchitis, and treatment of gonorrhea and syphilis in patients that are allergic to penicillin; as part of a multidrug regimen for H. pylori eradication to reduce the risk of duodenal ulcer recurrence

Use - Dental

Treatment of periodontitis associated with presence of Actinobacillus actinomycetemcomitans (AA); as adjunctive therapy in recurrent aphthous ulcers

Pregnancy Risk Factor

Pregnancy Implications

Tetracyclines cross the placenta and enter fetal circulation; may cause permanent discoloration of teeth if used during the last half of pregnancy.

Lactation

Enters breast milk/not recommended (AAP rates "compatible")

Contraindications

Hypersensitivity to tetracycline or any component of the formulation; do not administer to children

8 years of age; pregnancy

Warnings/Precautions

Use of tetracyclines during tooth development may cause permanent discoloration of the teeth and enamel, hypoplasia and retardation of skeletal development and bone growth with risk being the greatest for children <4 years and those receiving high doses; use with caution in patients with renal or hepatic impairment (eg, elderly); dosage modification required in patients with renal impairment since it may increase BUN as an antianabolic agent; pseudotumor cerebri has been reported with tetracycline use (usually resolves with discontinuation); outdated drug can cause nephropathy; superinfection possible; use protective measure to avoid photosensitivity

Adverse Reactions

Frequency not defined.

Cardiovascular: Pericarditis

Central nervous system: Intracranial pressure increased, bulging fontanels in infants, pseudotumor cerebri, paresthesia

Dermatologic: Photosensitivity, pruritus, pigmentation of nails, exfoliative dermatitis

Endocrine & metabolic: Diabetes insipidus syndrome

Gastrointestinal: Discoloration of teeth and enamel hypoplasia (young children), nausea, diarrhea, vomiting, esophagitis, anorexia, abdominal cramps, antibiotic-associated pseudomembranous colitis, staphylococcal enterocolitis, pancreatitis

Hematologic: Thrombophlebitis

Hepatic: Hepatotoxicity

Renal: Acute renal failure, azotemia, renal damage

Miscellaneous: Superinfection, anaphylaxis, hypersensitivity reactions, candidal superinfection

Overdosage/Toxicology

Symptoms of overdose include nausea, anorexia, and diarrhea. Treatment is supportive.

Drug Interactions

Substrate of CYP3A4 (major); Inhibits CYP3A4 (moderate)

Antacids: May decrease tetracycline absorption; separate doses.

Calcium supplements (oral): May decrease tetracycline absorption; separate doses.

CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of tetracycline. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.

CYP3A4 substrates: Tetracycline may increase the levels/effects of CYP3A4 substrates. Example substrates include benzodiazepines, calcium channel blockers, cyclosporine, mirtazapine, nateglinide, nefazodone, sildenafil (and other PDE-5 inhibitors), tacrolimus, and venlafaxine. Selected benzodiazepines (midazolam and triazolam), cisapride, ergot alkaloids, selected HMG-CoA reductase inhibitors (lovastatin and simvastatin), and pimozide are generally contraindicated with strong CYP3A4 inhibitors.

Didanosine: May decrease tetracycline absorption; separate doses.

Digoxin: Tetracyclines may rarely increase digoxin serum levels.

Iron: May decrease tetracycline absorption; separate doses.

Methoxyflurane anesthesia when concurrent with tetracycline may cause fatal nephrotoxicity.

Oral contraceptives: Anecdotal reports suggesting decreased contraceptive efficacy with tetracyclines have been refuted by more rigorous scientific and clinical data.

Quinapril: May decrease tetracycline absorption; separate doses.

Warfarin with tetracyclines may result in increased anticoagulation.

Ethanol/Nutrition/Herb Interactions

Food: Tetracycline serum concentrations may be decreased if taken with dairy products.

Herb/Nutraceutical: Avoid dong quai, St John's wort (may also cause photosensitization)

Stability

Outdated tetracyclines have caused a Fanconi-like syndrome; protect oral dosage forms from light

Mechanism of Action

Inhibits bacterial protein synthesis by binding with the 30S and possibly the 50S ribosomal subunit(s) of susceptible bacteria; may also cause alterations in the cytoplasmic membrane

Pharmacodynamics/Kinetics

Absorption: Oral: 75%

Distribution: Small amount appears in bile

Relative diffusion from blood into CSF: Good only with inflammation (exceeds usual MICs)

CSF:blood level ratio: Inflamed meninges: 25%

Protein binding: ~65%

Half-life elimination: Normal renal function: 8-11 hours; End-stage renal disease: 57-108 hours

Time to peak, serum: Oral: 2-4 hours

Excretion: Urine (60% as unchanged drug); feces (as active form)

Dosage

Oral:

Children >8 years: 25-50 mg/kg/day in divided doses every 6 hours

Adults: 250-500 mg/dose every 6 hours

Helicobacter pylori eradication: 500 mg 2-4 times/day depending on regimen; requires combination therapy with at least one other antibiotic and an acid-suppressing agent (proton pump inhibitor or H2 blocker)

Dosing interval in renal impairment:

Clcr 50-80 mL/minute: Administer every 8-12 hours

Clcr 10-50 mL/minute: Administer every 12-24 hours

Clcr<10 mL/minute: Administer every 24 hours

Dialysis: Slightly dialyzable (5% to 20%) via hemo- and peritoneal dialysis or via continuous arteriovenous or venovenous hemofiltration; no supplemental dosage necessary

Dosing adjustment in hepatic impairment: Avoid use or maximum dose is 1 g/day

Administration

Should be administered on an empty stomach (ie, 1 hour prior to, or 2 hours after meals) to increase total absorption. Administer at least 1-2 hours prior to, or 4 hours after antacid because aluminum and magnesium cations may chelate with tetracycline and reduce its total absorption.

Monitoring Parameters

Renal, hepatic, and hematologic function test, temperature, WBC, cultures and sensitivity, appetite, mental status

Test Interactions

False-negative urine glucose with Clinistix®

Patient Education

Take this medication exactly as directed. Take all of the prescription even if you see an improvement in your condition. Do not use more or more often than recommended. Preferable to take on an empty stomach, 1 hour before or 2 hours after meals. Take at regularly scheduled times, around-the-clock. Avoid antacids, iron, or dairy products within 2 hours of taking tetracycline. You may experience photosensitivity (use sunscreen, wear protective clothing and eyewear, and avoid direct sunlight); dizziness or lightheadedness (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or nausea/vomiting (small, frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help). Report rash or intense itching, yellowing of skin or eyes, fever or chills, blackened stool, vaginal itching or discharge, foul-smelling stools, excessive thirst or urination, acute headache, unresolved diarrhea, respiratory difficulty, condition does not improve, or worsening of condition. Pregnancy/breast-feeding precautions: Do not get pregnant while taking this medication. Use appropriate barrier contraceptive measures. Breast-feeding is not recommended.

Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Esophagitis, superinfections, and candidal superinfection. Opportunistic "superinfection" with Candida albicans ; tetracyclines are not recommended for use during pregnancy or in children

8 years of age since they have been reported to cause enamel hypoplasia and permanent teeth discoloration. The use of tetracyclines should only be used in these patients if other agents are contraindicated or alternative antimicrobials will not eradicate the organism. Long-term use associated with oral candidiasis.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

None reported

Mental Health: Effects on Psychiatric Treatment

Tetracycline may decrease lithium clearance resulting in an increase in serum lithium levels and potential lithium toxicity although the clinical significance is likely minimal; monitor serum lithium levels

Dosage Forms

Capsule, as hydrochloride: 250 mg, 500 mg

Suspension, oral, as hydrochloride (Sumycin®): 125 mg/5 mL (480 mL) [contains sodium benzoate and sodium metabisulfite; fruit flavor]

Tablet, as hydrochloride (Sumycin®): 250 mg, 500 mg

References

American Academy of Pediatrics. Committee on Drugs. "Requiem for Tetracyclines," Pediatrics , 1975, 55(1):142-3.

"American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals Into Human Milk," Pediatrics , 2001, 108(3):776-89.

Coronado BE, Opal SM, and Yoburn DC, "Antibiotic-Induced D-Lactic Acidosis," Ann Intern Med , 1995, 122(11):839-42.

Cuddihy J, "Case Report of Benign Intra-cranial Hypertension Secondary to Tetracycline," Ir Med J , 1994, 87(3):90.

Fox SA, Berenyi MR, and Straus B, "Tetracycline Toxicity Presenting as a Multisystem Disease," Mt Sinai J Med , 1976, 43(2):129-35.

Gardner K, Cox T, and Digre KB, "Idiopathic Intracranial Hypertension Associated With Tetracycline Use in Fraternal Twins: Case Reports and Review," Neurology , 1995, 45(1):6-10.

Gordon JM and Walker CB, "Current Status of Systemic Antibiotic Usage in Destructive Periodontal Disease," J Periodontol , 1993, 64(8 Suppl):760-71.

Lee AG, "Pseudotumor Cerebri After Treatment With Tetracycline and Isotretinoin for Acne," Cutis , 1995, 55(3):165-8.

Maroon JC and Mealy J Jr, "Benign Intracranial Hypertension. Sequel to Tetracycline Therapy in a Child," JAMA , 1979, 216(9):1479-80.

Rams TE and Slots J, "Antibiotics in Periodontal Therapy: An Update," Compendium , 1992, 13(12):1130, 1132, 1134.

Sargent E, "Tetracycline for Seal Finger," JAMA , 1980, 244(5):437.

Seymour RA and Heasman PA, "Pharmacological Control of Periodontal Disease. II. Antimicrobial Agents," J Dent , 1995, 23(1):5-14

Seymour RA and Heasman PA, "Tetracyclines in the Management of Periodontal Diseases. A Review," J Clin Periodontol , 1995, 22(1):22-35.

Smilack JD, Wilson WR, and Cockerill FR 3d, "Tetracyclines, Chloramphenicol, Erythromycin, Clindamycin, and Metronidazole," Mayo Clin Proc , 1991, 66(12):1270-80.

Walters BN and Gubbay SS, "Tetracycline and Benign Intracranial Hypertension: Report of Five Cases," Br Med J (Clin Res Ed) , 1981, 282(6257):19-20.

Wandstrat TL and Phillips J, "Pseudotumor Cerebri Responsive to Acetazolamide," Ann Pharmacother , 1995, 29(3):318.

Yoshikawa TT, "Antimicrobial Therapy for the Elderly Patient," J Am Geriatr Soc , 1990, 38(12):1353-72.

International Brand Names

Apo-Tetra® (CA); Bactocyline® (BD); Ciclobiotico® (PT); Economycin® (GB); Infex® (BR); Novo-Tetra (CA); Nu-Tetra (CA); Pervasol® (AR); Tancilina® (AR); Teracilin® (BD); Tetra-Atlantis® (MX); Tetrabiotico® (EC); Tetraciclina® (BR, CL); Tetraciclina L.CH.® (CL); Tetrana® (TH); Tetrin® (ID)

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