Prescription Drug Information: Doxycycline Hyclate

DOXYCYCLINE HYCLATE- doxycycline hyclate tablet
Pharmasource Meds, LLC

To reduce the development of drug-resistant bacteria and maintain the effectiveness of Doxycycline and other antibacterial drugs, Doxycycline should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

DESCRIPTION

Doxycycline hyclate is an antibacterial drug synthetically derived from oxytetracycline. The chemical designation for doxycyclin is 4-(Dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,5,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-2-naphthacene-carboxamide monohydrate.

Doxycycline hyclate is yellow to light yellow powder. It is freely soluble in water and methanol, sparingly soluble in alcohol; practically insoluble in chloroform and in ether. It dissolves in aqueous solution of alkali hydroxides and carbonates.

Doxycycline has a high degree of lipoid solubility and a low affinity for calcium binding. It is highly stable in normal human serum. Doxycycline will not degrade into an epianhydro form. The structural formula is as follows:

Doxycycline hyclate tablets
(click image for full-size original)

Each film-coated tablet for oral administration contains doxycycline hyclate equivalent to 100 mg of doxycycline (anhydrous). Inactive ingredients are: anhydrous lactose, croscarmellose sodium, colloidal silicon dioxide, hypromellose, iron oxide yellow , iron oxide red, microcrystalline cellulose, magnesium stearate, polyethylene glycol, pregelatinised starch and titanium dioxide.

CLINICAL PHARMACOLOGY

Tetracyclines are readily absorbed and are bound to plasma proteins in varying degree. They are concentrated by the liver in the bile and excreted in the urine and feces at high concentrations and in a biologically active form. Doxycycline is virtually completely absorbed after oral administration.

Following a 200 mg dose, normal adult volunteers averaged peak serum levels of 2.6 mcg/mL of doxycycline at 2 hours, decreasing to 1.45 mcg/mL at 24 hours. Excretion of doxycycline by the kidney is about 40%/72 hours in individuals with normal function (creatinine clearance about 75 mL/min). This percentage excretion may fall as low as 1 to 5%/72 hours in individuals with severe renal insufficiency (creatinine clearance below 10 mL/min). Studies have shown no significant difference in serum half-life of doxycycline (range 18 to 22 hours) in individuals with normal and severely impaired renal function.

Hemodialysis does not alter serum half-life.

Results of animal studies indicate that tetracyclines cross the placenta and are found in fetal tissues.

Population pharmacokinetic analysis of sparse concentration-time data of doxycycline following standard of care intravenous and oral dosing in 44 pediatric patients (2 years to 18 years of age) showed that allometrically-scaled clearance (CL) of doxycycline in pediatric patients ≥2 to ≤8 years of age (median [range] 3.58 [2.27 to 10.82] L/h/70 kg, N =11) did not differ significantly from pediatric patients >8 to 18 years of age (3.27 [1.11 to 8.12] L/h/70 kg, N=33). For pediatric patients weighing ≤45 kg, body weight normalized doxycycline CL in those ≥2 to ≤8 years of age (median [range] 0.071 [0 .041 to 0.202] L/kg/h, N=10) did not differ significantly from those >8 to 18 years of age (0.081 [0.035 to 0.126] L/kg/h, N=8). In pediatric patients weighing >45 kg, no clinically significant differences in body weight normalized doxycycline CL were observed between those ≥2 to ≤8 years (0.050 L/kg/h, N=l) and those >8 to 18 years of age (0.044 [0.014 to 0.121] L/kg/h, N=25). No clinically significant difference in CL between oral and IV dosing was observed in the small cohort of pediatric patients who received the oral (N=19) or IV (N=2l) formulation alone.

Microbiology

Mechanism of action

Doxycycline inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit.

Doxycycline has bacteriostatic activity against a broad range of Gram-positive and Gram-negative bacteria.

Resistance

Cross resistance with other tetracyclines is common.

Antimicrobial Activity

Doxycycline has been shown to be active against most isolates of the following microorganisms, both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section of the package insert for doxycycline hyclate tablets.

Gram-Negative Bacteria

Acinetobacter species

Bartonella bacilliformis

Brucella species

Klebsiella species

Klebsiella granulomatis

Campylobacter fetus

Enterobacter aerogenes

Escherichia coli

Francisella tularensis

Haemophilus ducreyi

Haemophilus influenzae

Neisseria gonorrhoeae

Shigella species

Vibrio cholerae

Yersinia pestis

Gram-Positive Bacteria

Bacillus anthracis

Listeria monocytogenes

Streptococcus pneumoniae

Anaerobic Bacteria

Clostridium species

Fusobacterium fusiforme

Propionibacterium acnes

Other Bacteria

Nocardiae and other aerobic Actinomyces species

Borrelia recurrentis

Chlamydophila psittaci

Chlamydia trachomatis

Mycoplasma pneumoniae

Rickettsiae

Treponema pallidum

Treponema pallidum subspecies pertenue

Ureaplasma urealyticum

Parasites

Balantidium coli

Entamoeba species

Plasmodium falciparum *

* Doxycycline has been found to be active against the asexual erythrocytic forms of Plasmodium falciparum , but not against the gametocytes of P. falciparum. The precise mechanism of action of the drug is not known.

Susceptibility Testing

For specific information regarding susceptibility test interpretive criteria and associated test methods and quality control standards recognized by FDA for this drug, please see: https://www.fda.gov/STIC.

INDICATIONS AND USAGE

To reduce the development of drug-resistant bacteria and maintain effectiveness of doxycycline hyclate tablets and other antibacterial drugs, doxycycline hyclate tablets should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.

Treatment

Doxycycline hyclate tablets are indicated for the treatment of following infections:

  • Rocky Mountain spotted fever, typhus fever and the typhus group, Q fever, rickettsialpox, and tick fevers caused by Rickettsiae.
  • Respiratory tract infections caused by Mycoplasma pneumoniae.
  • Lymphogranuloma venereum caused by Chlamydia trachomatis.
  • Psittacosis (ornithosis) caused by Chlamydophila psittaci.
  • Trachoma caused by Chlamydia trachomatis , although the infectious agent is not always eliminated, as judged by immunofluorescence.
  • Inclusion conjunctivitis caused by Chlamydia trachomatis.
  • Uncomplicated urethral, endocervical, or rectal infections in adults caused by Chlamydia trachomatis.
  • Nongonococcal urethritis caused by Ureaplasma urealyticum.
  • Relapsing fever due to Borrelia recurrentis.

Doxycycline hyclate tablets are also indicated for the treatment of infections caused by the following gram-negative microorganisms:

  • Chancroid caused by Haemophilus ducreyi.
  • Plague due to Yersinia pestis.
  • Tularemia due to Francisella tularensis.
  • Cholera caused by Vibrio cholerae.
  • Campylobacter fetus infections caused by Campylobacter fetus.
  • Brucellosis due to Brucella species (in conjunction with streptomycin).
  • Bartonellosis due to Bartonella bacilliformis.
  • Granuloma inguinale caused by Klebsiella granulomatis.

Because many strains of the following groups of microorganisms have been shown to be resistant to doxycycline, culture and susceptibility testing are recommended.

Doxycycline hyclate tablets are indicated for treatment of infections caused by the following gram-negative bacteria, when bacteriologic testing indicates appropriate susceptibility to the drug:

  • Escherichia coli.
  • Enterobacter aerogenes.
  • Shigella species .
  • Acinetobacter species.
  • Respiratory tract infections caused by Haemophilus influenzae.
  • Respiratory tract and urinary tract infections caused by Klebsiella species.

Doxycycline hyclate tablets are indicated for treatment of infections caused by the following gram-positive microorganisms when bacteriologic testing indicates appropriate susceptibility to the drug:

  • Upper respiratory infections caused by Streptococcus pneumoniae.
  • Anthrax due to Bacillus anthracis , including inhalational anthrax (post-exposure): to reduce the incidence or progression of disease following exposure to aerosolized Bacillus anthracis.

When penicillin is contraindicated, doxycycline hyclate tablets are an alternative drug in the treatment of the following infections:

  • Uncomplicated gonorrhea caused by Neisseria gonorrhoeae.
  • Syphilis caused by Treponema pallidum.
  • Yaws caused by Treponema pallidum subspecies pertenue.
  • Listeriosis due to Listeria monocytogenes.
  • Vincent’s infection caused by Fusobacterium fusiforme.
  • Actinomycosis caused by Actinomyces israelii.
  • Infections caused by Clostridium species.

In acute intestinal amebiasis, doxycycline may be a useful adjunct to amebicides.

In severe acne, doxycycline may be useful adjunctive therapy.

Prophylaxis:

Doxycycline hyclate tablets are indicated for the prophylaxis of malaria due to Plasmodium falciparum in short- term travelers (<4 months) to areas with chloroquine and/or pyrimethamine-sulfadoxine resistant strains. ( See DOSAGE AND ADMINISTRATION section and Information for Patients subsection of the PRECAUTIONS section) .

Page 1 of 3 1 2 3

RxDrugLabels.com provides trustworthy package insert and label information about marketed prescription drugs as submitted by manufacturers to the U.S. Food and Drug Administration. Package information is not reviewed or updated separately by RxDrugLabels.com. Every individual prescription drug label and package insert entry contains a unique identifier which can be used to secure further details directly from the U.S. National Institutes of Health and/or the FDA.

As a leading independent provider of trustworthy medication information, we source our database directly from the FDA's central repository of drug labels and package inserts under the Structured Product Labeling standard. RxDrugLabels.com provides the full prescription-only subset of the FDA's repository. Medication information provided here is not intended as a substitute for direct consultation with a qualified health professional.

Terms of Use | Copyright © 2024. All Rights Reserved.