Oracea

Generic Name: Doxycycline
Class: Skin and Mucous Membrane Agents, Miscellaneous
Chemical Name: 4 - (Dimethylamino) - 1,4,4a,5,5a,6,11,12a - octahydro - 3,5,10,12,12a - pentahydroxy - 6 - methyl - 1,11 - dioxo - 2 - naphthacenecarboxamide monohydrate
Molecular Formula: C₂₂H₂₄N₂O₈•H₂0
CAS Number: 17086-28-1

Introduction

Semisynthetic tetracycline antibiotic.¹

Available as 40-mg capsules (Oracea) containing 2 types of doxycycline beads (i.e., 30 mg as immediate-release beads and 10 mg as delayed-release beads).¹

Uses for Oracea

Rosacea

Treatment of inflammatory lesions (papules and pustules) associated with rosacea (acne rosacea).¹

Safety and efficacy not established for treatment of the erythematous, telangiectatic, or ocular components of rosacea.¹

The 40-mg capsules of doxycycline (Oracea) are not indicated for the treatment or prevention of bacterial infections or to reduce the number of or eliminate organisms associated with bacterial disease.¹ (See Selection and Use of Anti-infectives under Cautions).

Oracea Dosage and Administration

Administration

Oral Administration

Administer orally in the morning, on an empty stomach, at least 1 hour before or 2 hours after a meal.¹

Give with adequate amounts of fluid to reduce risk of esophageal irritation and ulceration.¹

Dosage

Adults

Rosacea

Oral

40 mg once daily in the morning.¹

Prescribing Limits

Adults

Oral

Efficacy of the 40-mg capsules of doxycycline (Oracea) not established beyond 16 weeks and safety not established beyond 9 months of therapy.¹

Exceeding the dosage of doxycycline recommended for rosacea may increase the incidence of adverse effects (e.g., development of drug-resistant bacteria).¹

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time.¹

Renal Impairment

Dosage adjustment not required.⁹

Geriatric Patients

No specific dosage recommendations at this time.¹

Cautions for Oracea

Contraindications

• 
  

  Known hypersensitivity to doxycycline or other tetracyclines.¹

  
  

Warnings/Precautions

Warnings

Fetal/Neonatal Morbidity

Animal studies indicate possible fetal toxicity (e.g., retardation of skeletal development) and embryotoxicity.¹

Use not recommended in pregnant women.¹ Avoid pregnancy during therapy.¹ If pregnancy occurs, immediately discontinue and apprise of potential fetal hazard.¹

Use not recommended for individuals of either gender who are attempting to conceive a child.¹

Dental and Bone Effects

Avoid use during tooth development (the last half of pregnancy, infancy, childhood up to 8 years of age); potential for permanent tooth discoloration and enamel hypoplasia.¹

Tetracyclines form a stable calcium complex in any bone-forming tissue.¹ Reversible decrease in fibula growth rate has occurred in premature infants receiving oral tetracyclines.¹

Superinfection/Clostridium difficile-associated Colitis

Treatment with anti-infectives may permit overgrowth of clostridia.^{1 5 6 7 8} Consider Clostridium difficile-associated diarrhea and colitis (antibiotic-associated pseudomembranous colitis) if diarrhea develops and manage accordingly.^{1 5 6 7 8}

Some mild cases of C. difficile-associated diarrhea and colitis may respond to discontinuance alone.^{1 5 6 7 8} Manage moderate to severe cases with fluid, electrolyte, protein supplementation, and appropriate anti-infective therapy (e.g., oral metronidazole or vancomycin) as clinically indicated.^{1 5 6 7 8}

Renal Effects

Tetracyclines have antianabolic effects and may increase BUN concentrations.¹ This effect usually is not clinically important in patients with normal renal function; however, high serum tetracycline concentrations may result in azotemia, hyperphosphatemia, and acidosis in patients with impaired renal function.¹ (See Renal Impairment under Cautions.)

Sensitivity Reactions

Photosensitivity Reactions

Possible photosensitivity reaction (e.g., exaggerated sunburn reaction).¹

Avoid unnecessary exposure to sunlight or artificial UV light (sunlamps, solariums).¹

General Precautions

Superinfection/Candidiasis

Doxycycline may result in overgrowth of nonsusceptible organisms, including fungi.¹ If superinfection occurs, discontinue doxycycline and initiate appropriate therapy.¹

Tetracyclines may increase the incidence of vaginal candidiasis.¹ Use with caution in patients with a history of or predisposition to candidiasis.¹

Selection and Use of Anti-infectives

To reduce development of drug-resistant bacteria and maintain effectiveness of other antibacterials, use the 40-mg capsules of doxycycline (Oracea) only for the treatment of rosacea.¹

Doxycycline 40-mg capsules are not to be used for the treatment or prevention of bacterial infections or to reduce or eliminate organisms associated with bacterial disease.¹ The dosage regimen used for the treatment of rosacea results in doxycycline plasma concentrations that are too low for the treatment of bacterial infections.¹

Autoimmune Syndromes

Tetracyclines have been associated with autoimmune syndromes (e.g., lupus-like syndrome, autoimmune hepatitis, vasculitis, serum sickness).¹

If symptoms suggestive of an autoimmune syndrome develop (e.g., fever, rash, arthralgia, malaise), immediately discontinue use of tetracyclines and perform appropriate tests (liver function tests, ANA, CBC) to evaluate the patient.¹

Tissue Hyperpigmentation

Tetracyclines are known to cause hyperpigmentation in many organs (e.g., nails, bone, skin, eyes, thyroid, visceral tissue, oral cavity, sclerae, and heart valves).¹

Nervous System Effects

Tetracyclines have been reported to cause bulging fontanels in infants and benign intracranial hypertension (pseudotumor cerebri) in adults.¹ These effects usually resolve when the drug is discontinued.¹

Laboratory Monitoring

Periodically assess organ system function (including hematopoietic, renal, and hepatic function).¹ Perform appropriate tests for autoimmune syndromes if indicated.¹

Specific Populations

Pregnancy

Category D.¹ (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Lactation

Distributed into milk.¹ Discontinue nursing or the drug.¹

Pediatric Use

Safety and efficacy not established; use not recommended.¹

Possible permanent tooth discoloration in children <8 years of age.¹ (See Dental and Bone Effects under Cautions.) Do not use in infants or children <8 years of age.¹

Renal Impairment

Serum half-life of doxycycline is not altered in patients with severe renal impairment;¹ renal impairment does not appear to result in excessive accumulation of doxycycline.¹⁰ (See Renal Effects under Cautions.)

Excessive drug accumulation and possible liver toxicity may occur if usual dosages of some tetracyclines are used in patients with renal impairment.¹ Dosage adjustment of tetracyclines may be necessary in patients with renal impairment; serum tetracycline concentrations should be monitored in patients receiving long-term therapy.¹

Common Adverse Effects

Nasopharyngitis,¹ hypertension,¹ sinusitis,¹ increased AST,¹ upper respiratory tract infection,⁴ headache,⁴ diarrhea.⁴

Interactions for Oracea

Specific Drugs and Laboratory Tests

Drug	Interaction	Comments
Antacids (aluminum-, calcium- or magnesium- containing)	Decreased absorption of doxycycline1	Give antacids containing aluminum, calcium, or magnesium 1–2 hours before or after doxycycline9
Anticoagulants, oral	Decreased plasma prothrombin activity1	Monitor PT carefully; adjust anticoagulant dosage as needed1
Anticonvulsants (carbamazepine, barbiturates, phenytoin)	Possible decreased doxycycline half-life1
Bismuth subsalicylate	Decreased absorption of doxycycline1	If concomitant use cannot be avoided, give doxycycline at least 2-3 hours before bismuth subsalicylate9
Hormonal contraceptives	Decreased effectiveness of oral contraceptive1	Use of a second form of contraceptive during treatment with doxycycline is advised1
Iron-containing preparations	Decreased absorption of doxycycline1	Give doxycycline 2 hours before or 3 hours after iron-containing preparations9
Methoxyflurane (no longer commercially available in the US)	Fatal renal toxicity1
Penicillins	Decreased efficacy of penicillins1	Avoid concomitant use1
Proton-pump inhibitors	Decreased absorption of doxycycline1
Retinoids, oral (e.g., acitretin, isotretinoin)	Additive adverse CNS effect of pseudotumor cerebri (benign intracranial hypertension)1	Avoid concomitant use1
Urinary catecholamine assay	Possible false elevation secondary to interference with fluorescence test1

Oracea Pharmacokinetics

Absorption

Bioavailability

Oracea is not bioequivalent to other commercially available doxycycline preparations.¹

Food

Decreased rate and extent of absorption when administered with a high-fat, high-protein meal including dairy products.¹

Special Populations

Bioavailability is reported to be reduced at high pH; may be clinically important in patients with gastrectomy, gastric bypass surgery, or those who otherwise are achlorhydric.¹

Distribution

Extent

Crosses the placenta and is distributed into milk.¹

Plasma Protein Binding

>90%.¹

Elimination

Metabolism

Major metabolites not identified.¹

Elimination Route

Excreted in urine (29–55% by 72 hours) and feces as unchanged drug.¹

Half-life

21 hours.¹

Special Populations

No significant difference in serum half-life of patients with normal and severely impaired renal function.¹ Hemodialysis does not alter the serum half-life.¹

Stability

Storage

Oral

Capsules

Tight, light-resistant containers at 15–30°C.¹

ActionsActions

• 
  

  Semisynthetic tetracycline antibiotic; also has anti-inflammatory and immunomodulatory effects.^{1 2 3}

  
  


• 
  

  Mechanism(s) by which doxycycline reduces inflammatory lesions (papules and pustules) in patients with rosacea not known.² Effects may result at least in part from the anti-inflammatory and antiangiogenic actions of the drug.²

  
  


• 
  

  The plasma concentrations of doxycycline achieved during therapy with the 40-mg capsules (Oracea) are less than the concentration required to treat bacterial diseases.¹

  
  


• 
  

  Causes no long-term effects on bacterial flora of the oral cavity, skin, intestinal tract, or vagina.¹

  
  

Advice to Patients

• 
  

  Importance of taking dose in the morning, on an empty stomach (at least 1 hour before or 2 hours after a meal) and drinking sufficient amounts of fluid to reduce the risk of esophageal irritation and ulceration.¹ Importance of not lying down immediately following the dose.⁹

  
  


• 
  

  Importance of avoiding exposure to direct sunlight or UV light while taking doxycycline.¹ When exposure cannot be avoided, importance of wearing protective clothing.¹ Importance of discontinuing the drug and informing clinician at the first sign of skin erythema.¹

  
  


• 
  

  Importance of taking only as prescribed; increasing dosage above 40 mg daily may increase the likelihood that bacteria will develop resistance and will not be treatable by other antibacterial drugs in the future.¹

  
  


• 
  

  Importance of women using alternative nonhormonal contraceptive measures because of the potential interaction with hormonal contraceptives.¹

  
  


• 
  

  Advise patients that autoimmune syndromes have been observed with doxycycline; importance of discontinuing the drug and informing clinician if arthralgia, fever, rash, or malaise occurs.¹

  
  


• 
  

  Advise patients that doxycycline therapy can cause discoloration of skin, scars, teeth, or gums.¹

  
  


• 
  

  Importance of providing patient a copy of manufacturer's patient information.¹

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant diseases.¹

  
  


• 
  

  Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed; necessity for clinicians to advise women to avoid pregnancy during therapy, advise pregnant women of risk to the fetus, and advise males to utilize effective contraception during therapy.¹

  
  


• 
  

  Importance of informing patients of other important precautionary information. (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Doxycycline

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Capsules (containing beads)	40 mg (immediate-release 30 mg with delayed-release 10 mg)	Oracea	CollaGenex

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions August 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. CollaGenex. Oracea (doxycycline, USP) capsules 40 mg prescribing information. Newtown, PA; 2006 May 26.

2. Sapadin AN, Fleischmajer R. Tetracyclines: nonantibiotic properties and their clinical implications. J Am Acad Dermatol. 2006; 54:258-65. [PubMed 16443056]

3. Anon. Low-dose doxycycline (Oracea) for rosacea. Med Lett Drugs Ther. 2007; 49:5-6.

4. Del Rosso JQ, Webster GF, Jackson M et al. Two randomized phase III clinical trials evaluating anti-inflammatory dose doxycycline (40-mg doxycycline, USP capsules) administered once daily for treatment of rosacea. J Am Acad Dermatol. 2007; 56:791-802. [PubMed 17367893]

5. Johnson S, Gerding DN. Clostridium difficile-associated diarrhea. Clin Infect Dis. 1998; 26:1027-36. [IDIS 407733] [PubMed 9597221]

6. Gerding DN, Johnson S, Peterson LR et al for the Society for Healthcare Epidemiology of America. Position paper on Clostridium difficile-associated diarrhea and colitis. Infect Control Hosp Epidemiol. 1995; 16:459-77. [PubMed 7594392]

7. Fekety R for the American College of Gastroenterology Practice Parameters Committee. Guidelines for the diagnosis and management of Clostridium difficile-associated diarrhea and colitis. Am J Gastroenterol. 1997; 92:739-50. [IDIS 386628] [PubMed 9149180]

8. American Society of Health-System Pharmacists Commission on Therapeutics. ASHP therapeutic position statement on the preferential use of metronidazole for the treatment of Clostridium difficile-associated disease. Am J Health-Syst Pharm. 1998; 55:1407-11. [IDIS 407213] [PubMed 9659970]

9. Collagenex, Newtown, PA: Personal communication.

10. Pfizer. Vibramycin calcium (doxycycline calcium) oral suspension syrup, Vibramycin hyclate (doxycycline hyclate) capsules, Vibramycin monohydrate (doxycycline monohydrate) for oral suspension, Vibra-tabs (doxycycline hyclate) film coated tablets prescribing information. New York, NY. 2003 Sep.

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