Doxycycline is metabolized in the liver and gastrointestinal tract and concentrated in bile [FDA label], [F3055]. Major metabolic pathways of doxycycline have not been identified, however, enzyme inducers have been found to decrease the half-life of doxycycline [F3055].
来源:DrugBank
代谢
/DOXYCYCLINE/ 以无活性的结合物形式或在可能是螯合物形式从粪便中排出（高达90%）。
/DOXYCYCLINE/ IS EXCRETED IN FECES (UP TO 90%) AS INACTIVE CONJUGATE OR PERHAPS AS CHELATE.
Although it was previously suggested that doxycycline is partially metabolized in the liver, recent studies indicate that the drug is not metabolized but is partially deactivated in the intestine by chelate formation.
Doxycycline has been associated with rare instances of hepatic injury, generally arising within 1 to 2 weeks of starting therapy, sometimes with a history of previous administration of the agent without injury. The pattern of injury ranges from hepatocellular to cholestatic and is probably most commonly mixed. The onset is often abrupt and can be accompanied by signs of hypersensitivity, such as fever, rash and eosinophilia (DRESS syndrome). Recovery is usually rapid and usually complete within 4 to 6 weeks. However, instances of severe and prolonged cholestatic liver injury have been reported with oral doxycycline. The autoimmune-like hepatitis that has been described with minocycline has not been linked to doxycycline, despite similarities in chemical structure and similar indications and uses, perhaps because it is used less frequency in a low dose, long term regimen. High dose intravenous doxycycline can cause acute fatty liver typical of that caused by intravenous tetracycline, particularly in susceptible patients such as pregnant women. This type of injury is, however, quite rare. Nevertheless, for these reasons, the duration and dose of parenteral doxycycline therapy should be minimized.
Tetracyclines, such as doxycycline, are readily absorbed and are bound to plasma proteins by varying degrees. Doxycycline is almost completely absorbed after oral administration. This drug is highly lipid soluble and has a low affinity for calcium binding [FDA label]. Absorption is not significantly affected by the concomitant ingestion of food or milk [F3052]. Peak serum levels of approximately 2.6 mcg/ml are reached at 2 hours following a 200 mg tablet oral dose [F3052].
Mainly the urine and feces as active and unchanged drug [FDA label]. Between 40% and 60% of an administered dose can be accounted for in the urine by 92 hours, and approximately 30% can be accounted for in the feces [F3055].
来源:DrugBank
吸收、分配和排泄
分布容积
多西环素容易扩散到大多数身体组织、体液和/或空腔中，分布容积已测量为0.7升/千克。
Doxycycline diffuses readily into most body tissues, fluid and/or cavities and the volume of distribution has been measured as 0.7 L/kg [F3052].
The excretion of doxycycline by the kidney is about 40% over 72 hours in individuals with normal kidney function (creatinine clearance approximately 75 mL/min). This rate may fall as low as 1-5% over 72 hours in individuals with severe renal insufficiency (creatinine clearance below 10 mL/min). Some clinical studies have shown no major difference in serum half-life of doxycycline (range 18-22 hours) in patients with normal and severely impaired renal function. Hemodialysis does not affect serum half-life of doxycycline [FDA label].
RELATIVE INSENSITIVITY OF DOXYCYCLINE PHARMACOKINETICS TO RENAL INSUFFICIENCY HAS ... BEEN DEMONSTRATED IN HUMANS & APPEARS TO BE ASSOC WITH INCR FECAL EXCRETION OWING TO DIFFUSION OF DRUG INTO LUMEN OF SMALL INTESTINE. ... RENAL CLEARANCE OF ACTIVE ANTIBIOTIC IS ... 20 ... ML/MIN FOR DOXYCYCLINE ... .
申请人：Fraunhofer-Gesellschaft zur Förderung der
angewandten Forschung e.V.
公开号：EP3646852A1
公开（公告）日：2020-05-06
The present invention generally relates to controlled release of tetracycline antibiotics. Specifically, it relates to a complex comprising a tetracycline compound (TC) or a pharmaceutically acceptable salt, hydrate or solvate thereof and a divalent metal carboxylate; a pharmaceutical preparation comprising the complex, methods for manufacturing the complex and the pharmaceutical preparation, and a complex or a pharmaceutical preparation for use in a method for treatment of the human or animal body, in particular for therapy and/or prophylaxis of a bacterial infection; and/or wherein antibiotic activity is maintained over a prolonged period of time; and/or for the therapy and/or prophylaxis of an acute, chronic or recurrent periodontal disease.
The present application relates to a method of treating an inflammatory skin condition by administering a pharmaceutical composition comprising a reduced dose of minocycline to a subject in need thereof, wherein said administration provides an effective plasma or interstitial fluid concentration of minocycline for treating the inflammatory skin condition.
COMPOSITIONS AND METHODS FOR TREATING AN INFECTION
申请人：CMPD LICENSING, LLC
公开号：US20170239277A1
公开（公告）日：2017-08-24
The present application relates to compounded compositions, methods of making compounded compositions, and methods of using compounded compositions. For example, disclosed herein are compounded compositions and methods of making compounded compositions comprising one or more anti-infective agents such as mupirocin and doxcycline.
METHODS FOR TREATING INFLAMMATORY SKIN CONDITIONS
申请人：DR. REDDY'S LABORATORIES LTD.
公开号：US20190209500A1
公开（公告）日：2019-07-11
The present application relates to a method of treating an inflammatory skin condition by administering a pharmaceutical composition comprising a reduced dose of minocycline to a subject in need thereof, wherein said administration provides an effective plasma or interstitial fluid concentration of minocycline for treating the inflammatory skin condition.
