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Doxycycline is an antibiotic that is used in the treatment of a number of types of infections caused by bacteria and protozoa.
Common side effects include diarrhea, nausea, vomiting, a red rash, and an increased risk of a sunburn.
Doxycycline was patented in 1957 and came into commercial use in 1967.
Contents
1 Medical use
1.1 Antibacterial
1.2 Antimalarial
1.3 Antihelminthic
1.4 Spectrum of susceptibility
2 Adverse effects
2.1 Interactions
2.2 Pregnancy and lactation
3 Pharmacology
4 Chemistry
5 History
6 Society and culture
7 Research
7.1 Research reagent
8 References
9 External links
Medical use
Generic 100 mg doxycycline capsules Doxycycline package
In addition to the general indications for all members of the tetracycline antibiotics group, doxycycline is frequently used to treat Lyme disease, chronic prostatitis, sinusitis, pelvic inflammatory disease,
In Canada, in 2004, doxycycline was considered a first-line treatment for chlamydia and non-gonococcal urethritis and with cefixime for uncomplicated gonorrhea.
Antibacterial
Moraxella catarrhalis, Brucella melitensis, Chlamydia pneumoniae, and Mycoplasma pneumoniae are generally susceptible to doxycycline, while some Haemophilus spp., Mycoplasma hominis, and Pseudomonas aeruginosa have developed resistance to varying degrees.
It is used in the treatment and prophylaxis of anthrax and Leptospirosis.
Doxycycline is indicated for treatment of:
Rocky Mountain spotted fever, typhus fever and the typhus group, Q fever, rickettsialpox, and tick fevers caused by Rickettsia
Respiratory tract infections caused by Mycoplasma pneumoniae
Lymphogranuloma venereum, trachoma, inclusion conjunctivitis, and uncomplicated urethral, endocervical, or rectal infections in adults caused by Chlamydia trachomatis
Psittacosis
Nongonococcal urethritis caused by Ureaplasma urealyticum
Relapsing fever due to Borrelia recurrentis
Chancroid caused by Haemophilus ducreyi
Plague due to Yersinia pestis
Tularemia
Cholera
Campylobacter fetus infections
Brucellosis caused by Brucella species (in conjunction with streptomycin)
Bartonellosis
Granuloma inguinale ( Klebsiella species)
Lyme disease
When bacteriologic testing indicates appropriate susceptibility to the drug, doxycycline may be used to treat these infections caused by Gram-negative bacteria :
Escherichia coli infections
Enterobacter aerogenes (formerly Aerobacter aerogenes ) infections
Shigella species infections
Acinetobacter species (formerly Mima species and Herellea species) infections
Respiratory tract infections caused by Haemophilus influenzae
Respiratory tract and urinary tract infections caused by Klebsiella species
Some Gram-positive bacteria have developed resistance to doxycycline. Up to 44% of Streptococcus pyogenes and up to 74% of S. faecalis specimens have developed resistance to the tetracycline group of antibiotics. When bacteriologic testing indicates appropriate susceptibility to the drug, doxycycline may be used to treat these infections caused by Gram-positive bacteria :
Upper respiratory infections caused by Streptococcus pneumoniae (formerly Diplococcus pneumoniae )
Skin and soft tissue infections caused by Staphylococcus aureus, including methicillin-resistant Staphylococcus aureus infections
Anthrax caused by Bacillus anthracis infection
When penicillin is contraindicated, doxycycline can be used to treat:
Syphilis caused by Treponema pallidum
Yaws caused by Treponema pertenue
Listeriosis due to Listeria monocytogenes
Vincent’s infection caused by Fusobacterium fusiforme
Actinomycosis caused by Actinomyces israelii
Infections caused by Clostridium species
Doxycycline may also be used as adjunctive therapy for severe acne.
The first-line treatment for brucellosis is a combination of doxycycline and streptomycin and the second-line is a combination of doxycycline and rifampicin (rifampin).
Antimalarial
It is used to prevent malaria.
The World Health Organization Guidelines states that the combination of doxycycline with either artesunate or quinine may be used for the treatment of uncomplicated malaria due to Plasmodium falciparum or following intravenous treatment of severe malaria.
Antihelminthic
Doxycycline kills the symbiotic Wolbachia bacteria in the reproductive tracts of parasitic filarial nematodes, making the nematodes sterile, and thus reducing transmission of diseases such as onchocerciasis and elephantiasis.
Spectrum of susceptibility
Doxycycline has been used successfully to treat sexually transmitted, respiratory, and ophthalmic infections. Representative pathogenic genera include Chlamydia, Streptococcus, Ureaplasma, Mycoplasma, and others. The following represents MIC susceptibility data for a few medically significant microorganisms.
Chlamydia psittaci : 0.03 μ g/mL
Mycoplasma pneumoniae : 0.016 μ g/mL — 2 μ g/mL
Streptococcus pneumoniae : 0.06 μ g/mL — 32 μ g/mL
Adverse effects
Cautions and side effects are similar to those of other members of the tetracycline antibiotic group.
An erythematous rash in sun-exposed parts of the body has been reported to occur in 7.3–21.2% of persons taking doxycycline for malaria prophylaxis. One study examined the tolerability of various malaria prophylactic regimens and found doxycycline did not cause a significantly higher percentage of all skin events (photosensitivity not specified) when compared with other antimalarials. The rash resolves upon discontinuation of the drug.
Unlike some other members of the tetracycline group, it may be used in those with renal impairment.
Interactions
The combination of doxycycline with dairy, antacids, calcium supplements, iron products, and laxatives containing magnesium is not inherently dangerous, but any of these foods and supplements may decrease doxycycline’s effectiveness.
Breakfast was observed to reduce doxycycline absorption significantly. Absorption of tetracycline occurs in the stomach and the upper small intestine. Absorption of tetracyclines has been reported to be impaired by milk products, aluminum hydroxide gels, sodium bicarbonate, calcium and magnesium salts, laxatives containing magnesium and iron preparations. The mechanisms responsible for decreased absorption appear to be chelation and an increase in gastric pH…. In view of these results, it is advisable to instruct the patients to take doxycycline on an empty stomach.
Previously, doxycycline was believed to impair the effectiveness of many types of hormonal contraception due to CYP450 induction. Recent research has shown no significant loss of effectiveness in oral contraceptives while using most tetracycline antibiotics (including doxycycline), although many physicians still recommend the use of barrier contraception for people taking the drug to prevent unwanted pregnancy.
Pregnancy and lactation
Doxycycline is categorized by the FDA as a class D drug in pregnancy. Doxycycline crosses into breastmilk.
Pharmacology
See also: Tetracycline antibiotics § Mechanism of action
Doxycycline, like other tetracycline antibiotics, is bacteriostatic. It works by preventing bacteria from reproducing through the inhibition of protein synthesis.
Doxycycline–metal ion complexes are unstable at acid pH, therefore more doxycycline enters the duodenum for absorption than the earlier tetracycline compounds. In addition, food has less effect on absorption than on absorption of earlier drugs with doxycycline serum concentrations being reduced by about 20% by test meals compared with 50% for tetracycline.
Chemistry
Expired tetracyclines or tetracyclines allowed to stand at a pH less than 2 are reported to be nephrotoxic due to the formation of a degradation product, anhydro-4-epitetracycline
History
After penicillin revolutionized the treatment of bacterial infections in WWII, many chemical companies moved into the field of discovering antibiotics by bioprospecting. American Cyanamid was one of these, and in the late 1940s chemists there discovered chlortetracycline, the first member of the tetracycline class of antibiotics.
As its patent grew near to expiring in the early 1970s, the patent became the subject of lawsuit between Pfizer and International Rectifier
In January 2013, the FDA reported shortages of some, but not all, forms of doxycyline “caused by increased demand and manufacturing issues”.
Society and culture
Doxycycline is available worldwide under many brand names.
Research
Tet-ON inducible shRNA system
At subantimicrobial doses, doxycycline is an inhibitor of matrix metalloproteases, and has been used in various experimental systems for this purpose, such as for recalcitrant recurrent corneal erosions.
Doxycycline has been used successfully in the treatment of one patient with lymphangioleiomyomatosis, an otherwise progressive and fatal disease.
In chronic obstructive pulmonary disease, doxycycline has been shown to improve lung functions in patients with stable symptoms.
Doxycycline is also used in “tet-on” ( gene expression activated by doxycycline) and “tet-off” (gene expression inactivated by doxycycline) tetracycline-controlled transcriptional activation to regulate transgene expression in organisms and cell cultures.
Other experimental applications include:
Macular degeneration
Vancomycin-resistant enterococcus
Infected animal bite wounds ( Pasteurella multocida, Pasteurella pneumotropica )
Rheumatoid arthritis instead of minocycline (both of which have demonstrated modest efficacy for this disease)
Chronic inflammatory lung diseases ( panbronchiolitis, asthma, cystic fibrosis, bronchitis ).
Sarcoidosis
Idiopathic pulmonary fibrosis
Research reagent
Doxycycline and other members of the tetracycline class of antibiotics are often used as research reagents in in vitro and in vivo biomedical research experiments involving bacteria as well in experiments in eukaryotic cells and organisms with inducible protein expression systems using tetracycline-controlled transcriptional activation. The mechanism of action for the antibacterial effect of tetracyclines relies on disrupting protein translation in bacteria, thereby damaging the ability of microbes to grow and repair; however protein translation is also disrupted in eukaryotic mitochondria impairing metabolism and leading to effects that can confound experimental results.

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