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Medication Safety Issues
Sound-alike/look-alike issues:
Tetracycline may be confused with tetradecyl sulfate
Achromycin may be confused with actinomycin, Adriamycin PFS®
Pronunciation
(tet ra SYE kleen)
Index Terms
Generic Available
Yes: Capsule
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
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 who 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
D
Pregnancy Considerations
Tetracyclines cross the placenta, enter fetal circulation, and may cause permanent discoloration of teeth if used during the second or third trimester. Maternal hepatic toxicity has been associated with the use of tetracycline during pregnancy, especially in patients with azotemia or pyelonephritis. Because use during pregnancy may cause fetal harm, tetracycline is classified as pregnancy category D.
Lactation
Enters breast milk/not recommended (AAP rates “compatible”)
Breast-Feeding Considerations
Tetracyclines are excreted in breast milk. Tetracycline binds to calcium. The calcium in the maternal milk will decrease the amount of tetracycline absorbed by the breast-feeding infant. Because of this “negligible absorption by the neonate,” the AAP considers tetracycline to be “usually compatible with breast-feeding.” Nondose-related effects could include modification of bowel flora.
Contraindications
Hypersensitivity to tetracycline or any component of the formulation; do not administer to children ?8 years of age; pregnancy
Warnings/Precautions
Concerns related to adverse effects:
• Increased BUN: May be associated with increases in BUN secondary to antianabolic effects; use caution in patients with renal impairment.
• Nephropathy: Outdated drug can cause nephropathy.
• Photosensitivity: May cause photosensitivity; discontinue if skin erythema occurs. Use skin protection and avoid prolonged exposure to sunlight; do not use tanning equipment.
• Pseudotumor cerebri: Has been (rarely) reported with tetracycline use; usually resolves with discontinuation.
• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.
Disease-related concerns:
• Hepatic impairment: Hepatotoxicity has been reported rarely; risk may be increased in patients with pre-existing hepatic or renal impairment.
• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment recommended.
Special populations:
• Pediatrics: May cause tissue hyperpigmentation, enamel hypoplasia, or permanent tooth discoloration; use of tetracyclines should be avoided during tooth development (children ?8 years of age) unless other drugs are not likely to be effective or are contraindicated. However, recommended in treatment of anthrax exposure.
• Pregnancy: Do not use during pregnancy. In addition to affecting tooth development, tetracycline use has been associated with retardation of skeletal development and reduced bone growth.
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
Metabolism/Transport Effects
Substrate of CYP3A4 (major); Inhibits CYP3A4 (moderate)
Drug Interactions
Antacids: May decrease the absorption of Tetracycline Derivatives. Risk D: Consider therapy modification
Atovaquone: Tetracycline may decrease the serum concentration of Atovaquone. Risk C: Monitor therapy
Bile Acid Sequestrants: May decrease the absorption of Tetracycline Derivatives. Risk D: Consider therapy modification
Bismuth: May decrease the absorption of Tetracycline Derivatives. Risk D: Consider therapy modification
Bismuth Subsalicylate: May decrease the absorption of Tetracycline Derivatives. Risk D: Consider therapy modification
Coumarin Derivatives: Tetracycline Derivatives may enhance the anticoagulant effect of Coumarin Derivatives. Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Substrates: CYP3A4 Inhibitors (Moderate) may decrease the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
Eplerenone: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Eplerenone. Management: A lower starting dose of eplerenone (25 mg once daily) is recommended in patients with hypertension who are also taking drugs that are moderate inhibitors of CYP3A4. Risk D: Consider therapy modification
Herbs (CYP3A4 Inducers): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
Iron Salts: May decrease the absorption of Tetracycline Derivatives. Only a concern with orally administered products. Exceptions: Ferric Gluconate; Iron Dextran Complex; Iron Sucrose. Risk D: Consider therapy modification
Magnesium Salts: May decrease the absorption of Tetracycline Derivatives. Only applicable to oral preparations of each agent. Risk D: Consider therapy modification
Maraviroc: CYP3A4 Inhibitors may increase the serum concentration of Maraviroc. Risk D: Consider therapy modification
Penicillins: Tetracycline Derivatives may diminish the therapeutic effect of Penicillins. Risk D: Consider therapy modification
Pimecrolimus: CYP3A4 Inhibitors (Moderate) may decrease the metabolism of Pimecrolimus. Risk C: Monitor therapy
Quinapril: May decrease the absorption of Tetracycline Derivatives. Risk D: Consider therapy modification
Ranolazine: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ranolazine. Risk X: Avoid combination
Retinoic Acid Derivatives: Tetracycline Derivatives may enhance the adverse/toxic effect of Retinoic Acid Derivatives. The development of pseudotumor cerebri is of particular concern. Exceptions: Adapalene; Alitretinoin; Tretinoin (Topical). Risk X: Avoid combination
Salmeterol: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Salmeterol. Risk C: Monitor therapy
Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Risk D: Consider therapy modification
Zinc Salts: May decrease the absorption of Tetracycline Derivatives. Only a concern when both products are administered orally. Exceptions: Zinc Chloride. Risk D: Consider therapy modification
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)
Storage
Outdated tetracyclines have caused a Fanconi-like syndrome (nausea, vomiting, acidosis, proteinuria, glycosuria, aminoaciduria, polydipsia, polyuria, hypokalemia). 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
Usual dosage range:
Children >8 years: Oral: 25-50 mg/kg/day in divided doses every 6 hours
Adults: Oral: 250-500 mg/dose every 6 hours
Indication-specific dosing:
Adults: Oral:
Acne: 250-500 twice daily
Chronic bronchitis, acute exacerbation: 500 mg 4 times/day
Erlichiosis: 500 mg 4 times/day for 7-14 days
Peptic ulcer disease: Eradication of Helicobacter pylori: 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)
Periodontitis: 250 mg every 6 hours until improvement (usually 10 days)
Vibrio cholerae:
500 mg 4 times/day for 3 days
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: Use caution; no dosing adjustment required
Dental Usual Dosing
Periodontitis: Adults: Oral: 250 mg every 6 hours until improvement (usually 10 days)
Administration: Oral
Oral should be given 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. Administer around-the-clock to promote less variation in peak and trough serum levels.
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
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 or persistent 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.
Geriatric Considerations
The role of tetracycline has decreased because of the emergence of resistant organisms. Doxycycline is the tetracycline of choice when one is indicated because of its better GI absorption, less interactions with divalent cations, longer half-life, and the fact that the majority is cleared by nonrenal mechanisms.
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
Nursing: Physical Assessment/Monitoring
Assess results of culture and sensitivity tests and patient's allergy history prior to beginning therapy. Assess potential interactions with other pharmacological agents and herbal products patient may be using (eg, may decrease levels/effects of penicillins and CYP3A4 inducers, increase levels/effects of warfarin and CYP3A4 substrates). Assess results of laboratory tests, therapeutic effectiveness (resolution of infection), and adverse reactions (eg, nausea, diarrhea, pericarditis, photosensitivity, rash, opportunistic infection, hypersensitivity) at beginning of and periodically throughout therapy. Caution patients with diabetes to monitor glucose levels closely (may cause false-positive urine glucose with Clinitest®). Assess knowledge/teach patient appropriate use, interventions to reduce side effects, and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, as hydrochloride: 250 mg, 500 mg
Pricing: U.S. (www.drugstore.com)
Capsules (Tetracycline HCl)
250 mg (100): $12.99
500 mg (100): $19.99
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
Lexi-Comp.com
Last full review/revision August 2008
Content last modified August 2008
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