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Look Up > Drugs > Doxycycline
Doxycycline
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Test Interactions
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(doks i SYE kleen)

U.S. Brand Names
Bio-Tab® Oral; Doryx® Oral; Doxychel® Injection; Doxychel® Oral; Doxy® Oral; Monodox® Oral; Periostat™; Vibramycin® Injection; Vibramycin® Oral; Vibra-Tabs®

Generic Available

Yes


Canadian Brand Names
Apo®-Doxy; Apo®-Doxy Tabs; Doxycin; Doxytec; Novo-Doxylin; Nu-Doxycycline

Synonyms
Doxycycline Hyclate; Doxycycline Monohydrate

Pharmacological Index

Antibiotic, Tetracycline Derivative


Use

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


Pregnancy Risk Factor

D


Contraindications

Hypersensitivity to doxycycline, tetracycline or any component; children <8 years of age; severe hepatic dysfunction


Warnings/Precautions

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.


Adverse Reactions

>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


Overdosage/Toxicology

Symptoms of overdose include nausea, anorexia, diarrhea

Following GI decontamination, supportive care only; fluid support may be required for hypotension


Drug Interactions

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


Stability

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


Mechanism of Action

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


Pharmacodynamics/Kinetics

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%)


Usual Dosage

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


Dietary Considerations

Administration with iron, calcium, milk or other dairy products may decrease doxycycline absorption. May decrease absorption of calcium, iron, magnesium, zinc, and amino acids,


Test Interactions

False-negative urine glucose using Clinistix®, Tes-Tape®


Mental Health: Effects on Mental Status

Tetracyclines have been reported to cause memory disturbance, mood stabilizing and antidepressant effects


Mental Health: Effects on Psychiatric Treatment

May cause neutropenia; use caution with clozapine and carbamazepine; barbiturates and carbamazepine increase the clearance of doxycycline


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

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.


Patient Information

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.


Nursing Implications

Avoid extravasation


Dosage Forms

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


References

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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