Doxycycline bioavailability

Doxycycline tends to be more active against some bacteria than other tetracyclines. This is probably due to its slower excretion rather than to enhanced oral absorption. Doxycycline is used in cases where cost is unimportant. It is a very lipophilic drug that shows a high bioavailability, being almost completely absorbed after oral administration to different animal species except chickens (250, 251). 

A lead compound bearing a ferrocenyl moiety at position N(l) was identified. This derivative is more active than Ciprofloxacin and Doxycycline. The activity is remarkably constant regardless of the level of resistance to CQ of the strains. Contrary to other antibiotics, no delayed-death effect was noted. Isobologram analysis showed that this compound exerts an antagonist effect with the main quinoline-containing antimalarials. In vitro results have to be confirmed in vivo to check the bioavailability of the molecule and its potential interest as a new antimalarial [113],... 

Doxycycline can cause nausea, vomiting, and diarrhea. The bioavailability of doxycycline is reduced if coadministered with multivalent ions such as iron or magnesium. However, unlike tetracycline, it can be administered with food and dairy products. In addition, patients taking tetracyclines may experience photosensitivity, especially if they are fair skinned. Patients taking tetracyclines should avoid prolonged exposure to sunlight. 

Drug interactions The bioavailability of tetracyclines is significantly deaeased when administered with antacids containing aluminum, calcium, or magnesium, with iron-containing products, or with food. Food or dairy products do not affect the bioavailability of doxycycline or minocycyline. 

As tetracyclines have moderate to high lipophilic properties, the poor bioavailability associated with oral administration is somewhat surprising. Papich and Riviere suggest that causes may be multifactorial. As zwitterions, they are mainly ionized at pHs within GIT liquor. Moreover, feed reduces bioavailability, and tetracyclines chelate with polyvalent cations. Oxytetracycline absorption has been shown, experimentally, to be reduced by feed, dairy products, Ca +, Mg +, Al +, and Fe + ions and antacids. Even though doxycycline has a similar structure, affinity for metals is different from that of oxytetracycline with greater affinity for zinc and less for calcium. 

Supplementation of feed for piglets with zinc can drastically reduce bioavailability of doxycycline. 

Deppermann K-M, Lode H, HofQ en G, Tschink G, Kalz C, Koeppe P. Influence of ranitidine, pirenzepine, and aluminum magnesium hydroxide on the bioavailability of various antibiotics, including amoxicillin, cephalexin, doxycycline and amoxicillin-clavulanic acid. Antmdcrob Agents Chemodier( 9Z9) 33,1901-1907. 

Cimetidine reduces the absorption of tetracycline but does not appear to affect its serum levels. Ranitidine seems not to affect the bioavailability of doxycycline. Information about other tetracyclines and H2-receptor antagonists is lacking, but there would seem to be no reason to suspect that they will interact. 

In 10 healthy subjects, the bioavailability of doxycycline 200 mg was not altered by three 150-mg doses of ranitidine. 

A study in 8 healthy subjects found that dimeticone 2.25 g did not alter the bioavailability of a single 200-mg dose of doxycycline. ... 

An active substance, although initially released from its dosage form (and dissolved), may become unavailable for absorption due to reactimis with other medicines or food components [4]. An example is the formation of insoluble complexes of tetracycline with calcium or aluminium ions from antacids or milk products. Interaction (chelation or binding) with iron ions leads to a reduced absorption for a variety of active substances such as doxycycline, penicillamine, methyldopa and ciprofloxacin. The absorption of active substances showing pH-dependent dissolution behaviour may be influenced by medicines that influence the gastric pH, such as H2-antagonists, proton pump inhibitors and antacids. Antimycotic active substances such as ketoconazole or itraconazole dissolve better in acidic fluids. Therefore their bioavailability may be increased by the concomitant use of an acidic drink like cola, whereas the concomitant use of antacids or proton pump inhibitors is likely to reduce the bioavailability. Concomitant use of milk may increase the dissolution of acidic active substances, whereas fats from food may increase the bioavailability of lipophilic active substances like albendazole and griseofulvin. 

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