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Pronunciation |
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(tet
ra SYE
kleen) |

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U.S. Brand
Names |
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Achromycin® Ophthalmic;
Achromycin® Topical; Sumycin® Oral; Topicycline®
Topical |

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Generic
Available |
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Yes |

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Canadian Brand
Names |
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Apo®-Tetra; Novo-Tetra;
Nu-Tetra |

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Synonyms |
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TCN; Tetracycline Hydrochloride |

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Pharmacological Index |
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Antibiotic, Ophthalmic; Antibiotic, Tetracycline Derivative; Antibiotic,
Topical |

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Use |
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Dental: Treatment of periodontitis associated with presence of
Actinobacillus actinomycetemcomitans (AA). As adjunctive therapy in
recurrent aphthous ulcers
Medical: 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; used concomitantly with metronidazole, bismuth
subsalicylate and an H2-antagonist for the treatment of duodenal
ulcer disease induced by H. pylori |

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Pregnancy Risk
Factor |
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D/B (topical) |

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Pregnancy/Breast-Feeding
Implications |
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Breast-feeding/lactation: Excreted in breast milk; avoid use if possible in
lactating mothers |

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Contraindications |
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Hypersensitivity to tetracycline or any component; do not administer to
children less than or equal to 8 years of age |

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Warnings/Precautions |
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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) and in pregnancy; 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 |

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Adverse
Reactions |
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>10%: Gastrointestinal: Discoloration of teeth and enamel hypoplasia
(young children)
1% to 10%:
Dermatologic: Photosensitivity
Gastrointestinal: Nausea, diarrhea
<1%: Pericarditis, increased intracranial pressure, bulging fontanels in
infants, pseudotumor cerebri, dermatologic effects, pruritus, pigmentation of
nails, exfoliative dermatitis, diabetes insipidus syndrome, vomiting,
esophagitis, anorexia, abdominal cramps, antibiotic-associated pseudomembranous
colitis, staphylococcal enterocolitis, hepatotoxicity, thrombophlebitis,
paresthesia, acute renal failure, azotemia, renal damage, superinfections,
anaphylaxis, hypersensitivity reactions, candidal superinfection
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Overdosage/Toxicology |
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Symptoms of overdose include nausea, anorexia, diarrhea; following GI
decontamination
Supportive care only |

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Drug
Interactions |
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Decreased effect: Calcium-, magnesium-, or aluminum-containing antacids, oral
contraceptives, iron, zinc, sodium bicarbonate, penicillins, cimetidine may
decrease tetracycline absorption
Although no clinical evidence exists, may bind with bismuth or calcium
carbonate, an excipient in bismuth subsalicylate, during treatment for H.
pylori
Increased toxicity: Methoxyflurane anesthesia when concurrent with
tetracycline may cause fatal nephrotoxicity; warfarin with tetracyclines may
result in increased anticoagulation; tetracyclines may rarely increase digoxin
serum levels |

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

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Mechanism of
Action |
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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 |

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Pharmacodynamics/Kinetics |
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Absorption: Oral: 75%
Distribution: Small amount appears in bile
Relative diffusion of antimicrobial agents from blood into cerebrospinal
fluid (CSF): Good only with inflammation (exceeds usual MICs)
Ratio of CSF to blood level (%): Inflamed meninges: 25
Protein binding: 20% to 60%
Half-life:
Normal renal function: 8-11 hours
End-stage renal disease: 57-108 hours
Time to peak serum concentration: Oral: Within 2-4 hours
Elimination: Primary route is the kidney, with 60% of a dose excreted as
unchanged drug in the urine; concentrated by liver in bile and feces in
biologically active form |

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Usual Dosage |
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Children >8 years: Oral: 25-50 mg/kg/day in divided doses every 6 hours
Children >8 years and Adults:
Ophthalmic:
Ointment: Instill every 2-12 hours
Suspension: Instill 1-2 drops 2-4 times/day or more often as needed
Topical: Apply to affected areas 1-4 times/day
Adults: Oral: 250-500 mg/dose every 6 hours
Helicobacter pylori: Clinically effective treatment regimens include
triple therapy with amoxicillin or tetracycline, metronidazole, and bismuth
subsalicylate; amoxicillin, metronidazole, and H2-receptor
antagonist; or double therapy with amoxicillin and omeprazole. Adult dose: 850
mg 3 times/day to 500 mg 4 times/day
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
nor via continuous arteriovenous or venovenous hemofiltration (CAVH/CAVHD); no
supplemental dosage necessary
Dosing adjustment in hepatic impairment: Avoid use or maximum dose is
1 g/day |

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Dietary
Considerations |
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Food: Dairy products decrease effect of tetracycline |

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

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Test
Interactions |
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False-negative urine glucose with
Clinistix® |

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Mental Health: Effects
on Mental Status |
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None reported |

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Mental Health:
Effects on Psychiatric
Treatment |
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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 |

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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |

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Dental Health:
Effects on Dental Treatment |
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Opportunistic "superinfection" with Candida albicans; tetracyclines
are not recommended for use during pregnancy or in children less than or equal
to 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. |

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Patient
Information |
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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.
Pregnancy/breast-feeding precautions: Do not get pregnant while
taking this medication - effectiveness of oral contraceptives may be reduced;
use appropriate barrier contraceptive measures. Breast-feeding is not
recommended.
Ophthalmic: Sit down, tilt head back, instill solution or drops inside lower
eyelid, and roll eyeball in all directions. Close eye and apply gentle pressure
to inner corner of eye for 30 seconds. Do not touch tip of applicator to eye or
any contaminated surface. May experience temporary stinging or blurred vision.
Inform prescriber if condition worsens or does not improve in 3-4 days.
Topical: Wash area and pat dry (unless contraindicated). Avoid getting in
mouth or eyes. You may experience temporary stinging or burning which will
resolve quickly. Treated skin may turn yellow; this will wash off. May stain
clothing (permanent). Report rash. Inform prescriber if condition worsens or
does not improve in a few days. |

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Nursing
Implications |
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Do not administer I.M. injection I.V., or I.V. injection I.M. (specific
products available for each). I.V. should be infused over at least 2
hours |

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Dosage Forms |
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Capsule, as hydrochloride: 100 mg, 250 mg, 500 mg
Ointment:
Ophthalmic: 1% [10 mg/mL] (3.5 g)
Topical, as hydrochloride: 3% [30 mg/mL] (14.2 g, 30 g)
Solution, topical: 2.2 mg/mL (70 mL)
Suspension:
Ophthalmic: 1% [10 mg/mL] (0.5 mL, 1 mL, 4 mL)
Oral, as hydrochloride: 125 mg/5 mL (60 mL, 480 mL)
Tablet, as hydrochloride: 250 mg, 500 mg |

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

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