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Pronunciation |
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(doks
i SYE
kleen) |
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U.S. Brand
Names |
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Bio-Tab® Oral; Doryx® Oral;
Doxychel® Injection; Doxychel® Oral; Doxy® Oral;
Monodox® Oral; Periostat™; Vibramycin® Injection;
Vibramycin® Oral; Vibra-Tabs® |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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Apo®-Doxy; Apo®-Doxy Tabs;
Doxycin; Doxytec; Novo-Doxylin; Nu-Doxycycline |
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Synonyms |
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Doxycycline Hyclate; Doxycycline Monohydrate |
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Pharmacological Index |
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Antibiotic, Tetracycline Derivative |
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Use |
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Dental: Treatment of periodontitis associated with presence of
Actinobacillus actinomycetemcomitans (AA)
Periostat® capsules are indicated for use as an adjunct
to scaling and root planing to promote attachment level gain and to reduce
pocket depth in adult periodontitis
Medical: Principally in the treatment of infections caused by susceptible
Rickettsia, Chlamydia, and Mycoplasma along with uncommon
susceptible gram-negative and gram-positive organisms; alternative to mefloquine
for malaria prophylaxis; treatment for syphilis in penicillin-allergic patients;
often active against vancomycin-resistant enterococci; used for
community-acquired pneumonia and other common infections due to susceptible
organisms; sclerosing agent for pleural effusions |
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Pregnancy Risk
Factor |
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D |
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Contraindications |
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Hypersensitivity to doxycycline, tetracycline or any component; children
<8 years of age; severe hepatic dysfunction |
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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; prolonged use may result in
superinfection; photosensitivity reaction may occur with this drug; avoid
prolonged exposure to sunlight or tanning equipment. Do not administer to
children less than or equal to 8 years of age. |
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Adverse
Reactions |
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>10%: Miscellaneous: Discoloration of teeth in children
1% to 10%: Gastrointestinal: Esophagitis
<1%: Increased intracranial pressure, bulging fontanels in infants, rash,
photosensitivity, nausea, diarrhea, neutropenia, eosinophilia, hepatotoxicity,
phlebitis |
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Overdosage/Toxicology |
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Symptoms of overdose include nausea, anorexia, diarrhea
Following GI decontamination, supportive care only; fluid support may be
required for hypotension |
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Drug
Interactions |
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CYP3A3/4 enzyme substrate
Iron and bismuth subsalicylate may decrease doxycycline bioavailability
Barbiturates, phenytoin, and carbamazepine decrease doxycycline's half-life
Increased effect of warfarin |
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Stability |
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Tetracyclines form toxic products when outdated or when exposed to light,
heat, or humidity; reconstituted solution is stable for 72 hours (refrigerated);
for I.V. infusion in NS or D5W solution, complete infusion should be
completed within 12 hours; discard remaining solution |
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Mechanism of
Action |
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Inhibits 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: Almost completely from the GI tract; absorption can be reduced by
food or milk by 20%
Distribution: Widely distributed into body tissues and fluids including
synovial, pleural, prostatic, seminal fluids, and bronchial secretions; saliva,
aqueous humor, and CSF penetration is poor; readily crosses placenta and appears
in breast milk
Protein binding: 90%
Metabolism: Not metabolized in the liver, instead is partially inactivated in
the GI tract by chelate formation
Half-life: 12-15 hours (usually increases to 22-24 hours with multiple
dosing)
End-stage renal disease: 18-25 hours
Time to peak serum concentration: Within 1.5-4 hours
Elimination: In urine (23%) and feces (30%) |
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Usual Dosage |
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Oral, I.V.:
Children >8 years (>45 kg) and Adults: 100-200 mg/day in 1-2 divided
doses
Acute gonococcal infection: 200 mg immediately, then 100 mg at bedtime on the
first day followed by 100 mg twice daily for 3 days OR 300 mg
immediately followed by 300 mg in 1 hour
Primary and secondary syphilis: 300 mg/day in divided doses for greater than
or equal to 10 days
Uncomplicated chlamydial infections: 100 mg twice daily for greater than or
equal to 7 days
Endometritis, salpingitis, parametritis, or peritonitis: 100 mg I.V. twice
daily with cefoxitin 2 g every 6 hours for 4 days and for greater than or equal
to 48 hours after patient improves; then continue with oral therapy 100 mg twice
daily to complete a 10- to 14-day course of therapy
Sclerosing agent for pleural effusion injection: 500 mg as a single dose in
30-50 mL of NS or SWI
Dosing adjustment in renal impairment: Clcr <10
mL/minute: 100 mg every 24 hours
Dialysis: Not dialyzable; 0% to 5% by hemo- and peritoneal methods or by
continuous arteriovenous or venovenous hemofiltration (CAVH/CAVHD); no
supplemental dosage necessary |
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Dietary
Considerations |
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Administration with iron, calcium, milk or other dairy products may decrease
doxycycline absorption. May decrease absorption of calcium, iron, magnesium,
zinc, and amino acids, |
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Test
Interactions |
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False-negative urine glucose using Clinistix®,
Tes-Tape® |
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Mental Health: Effects
on Mental Status |
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Tetracyclines have been reported to cause memory disturbance, mood
stabilizing and antidepressant effects |
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Mental Health:
Effects on Psychiatric
Treatment |
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May cause neutropenia; use caution with clozapine and carbamazepine;
barbiturates and carbamazepine increase the clearance of
doxycycline |
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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 as directed, for the entire prescription, even if you are feeling
better. Avoid alcohol and maintain adequate hydration (2-3 L/day of fluids
unless instructed to restrict fluid intake). You may be very sensitive to
sunlight; use sunblock, wear protective clothing and eyewear, or avoid exposure
to direct sunlight. You may experience lightheadedness, dizziness, or drowsiness
(use caution when driving or engaging in tasks that require alertness until
response to drug is known); nausea or vomiting (small frequent meals, frequent
mouth care, sucking lozenges, or chewing gum may help); or diarrhea (buttermilk,
boiled milk, or yogurt may help). If diabetic, drug may cause false tests with
Clinitest® urine glucose monitoring; use of glucose
oxidase methods (Clinistix®) or serum glucose monitoring
is preferable. Report skin rash or itching, easy bruising or bleeding, yellowing
of skin or eyes, pale stool or dark urine, unhealed sores of mouth, itching or
vaginal discharge, fever or chills, or unusual cough.
Pregnancy/breast-feeding precautions: Do not get pregnant while taking this
medication - Oral contraceptives effectiveness may be reduced; use appropriate
barrier contraceptive measures. Breast-feeding is not
recommended. |
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Nursing
Implications |
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Avoid extravasation |
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Dosage Forms |
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Capsule, as hyclate:
Doxychel®, Vibramycin®: 50 mg
Doxy®, Doxychel®,
Vibramycin®: 100 mg
Periostat®: 20 mg
Capsule, as monohydrate (Monodox®): 50 mg, 100 mg
Capsule, coated pellets, as hyclate (Doryx®): 100 mg
Gel, for subgingival application: Atridox™: 50 mg in
each 500 mg of blended formulation; 2-syringe system contains doxycycline
syringe (50 mg) and delivery system syringe (450 mg) along with a blunt cannula
Powder for injection, as hyclate (Doxy®,
Doxychel®, Vibramycin® IV): 100 mg,
200 mg
Powder for oral suspension, as monohydrate (raspberry flavor)
(Vibramycin®): 25 mg/5 mL (60 mL)
Syrup, as calcium (raspberry-apple flavor)
(Vibramycin®): 50 mg/5 mL (30 mL, 473 mL)
Tablet, as hyclate
Doxychel®: 50 mg
Bio-Tab®, Doxychel®,
Vibra-Tabs®: 100 mg |
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References |
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Böcker R, Mühlberg W, Platt D, et
al,
"Serum Level, Half-Life and Apparent Volume of Distribution of Doxycycline in Geriatric Patients,"
Eur J Clin Pharmacol, 1986, 30(1):105-8.
Bryant SG, Fisher S, and Kluge RM,
"Increased Frequency of Doxycycline Side Effects," Pharmacotherapy, 1987,
7(4):125-9.
Centers for Disease Control and Prevention,
"1998 Guidelines for Treatment of Sexually Transmitted Diseases," MMWR Morb
Mortal Wkly Rep, 1998, 47(RR-1):1-111.
Daunt N, Brodribb TR, and Dickey JD,
"Oesophageal Ulceration Due to Doxycycline," Br J Radiol, 1985,
58(696):1209-11.
Francke EL and Neu HC, "Chloramphenicol and Tetracyclines," Med Clin North
Am, 1987, 71(6):155-68.
Joshi N and Miller DQ, "Doxycycline Revisited," Arch Int Med, 1997,
157(13):1421-8.
Ljungberg B and Nilsson-Ehle I,
"Pharmacokinetics of Antimicrobial Agents in the Elderly," Rev Infect
Dis, 1987, 9(2):250-64.
Rams TE and Slots J, "Antibiotics in Periodontal Therapy: An Update,"
Compendium, 1992, 13(12):1130, 1132, 1134.
Smilack JD, Wilson WR, and Cockerill FR 3d,
"Tetracyclines, Chloramphenicol, Erythromycin, Clindamycin, and Metronidazole,"
Mayo Clin Proc, 1991, 66(12):1270-80.
Wilson WR and Cockerill FR 3d,
"Tetracyclines, Chloramphenicol, Erythromycin, and Clindamycin," Mayo Clin
Proc, 1987, 62(10):906-15.
Wyler DJ, "Malaria: Overview and Update," Clin Infect Dis, 1993,
16(4):449-56. |
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