PMID- 838428
OWN - NLM
STAT- MEDLINE
DCOM- 19770428
LR  - 20131121
IS  - 0015-8178 (Print)
IS  - 0015-8178 (Linking)
VI  - 95
IP  - 3
DP  - 1977 Jan 20
TI  - [Antiphiogistic drugs. Sudies on the pharmocokinetics of anti-inflammatory 
      agents].
PG  - 177-81
AB  - The kinetic behaviour of radioactively labeled acetylsalicylic acid (ASA), 
      phenylbutazone (PBZ), indometacin and dexamethasone in rabbits with knee joints 
      experimentally inflamed can be summarized as follows: 1. Under control 
      (non-inflammation) conditions as well as during inflammation, subthreshold doses 
      of 14C-ASA intravenously (i.v.) administered were eliminated from the blood in a 
      fast and slow biphasis process. The changes of the concentration in the perfusion 
      fluid were very similar compared to the changes in the blood. However, they were 
      enhanced during experimentally induced synovitis. 2. Subthreshold does of 
      3H-phenylbutazone i.v. administered were eliminated from the blood like 14C-ASA 
      in a biphasic process. During an experimentally produced inflammation of the 
      joints, the blood level decreased rapidly. The concentration of radioactivity in 
      the perfusion fluid was very low. 3. In constrast, 3H-indometacin injected like 
      ASA and PBZ in subtherapeutic dosage diappeared from the blood in a threephasic 
      process. The uptake into both the normal and the inflamed synovial space was 
      biphasic. Under both conditions the perfusion fluid contained low concentrations 
      of the drug. 4. 3H-dexamethasone (subtherapeutic dosage) displayed a biphasis 
      fall of concentration in the blood: a fast first phase and a slower second phase. 
      With inflammation of the kneejoint, the elimination was characterized by a 
      three-phase slope and was significantly faster compared with control animals. 
      While the alterations of ASA and indometacin level in the perfusion fluid were 
      corresponding to the decrease of the blood concentration, the uptake of 
      dexamethasone into the synovial space did not show any change. 5. Under control 
      conditions. 3H-dexamethasone (subthreshold doses) injected intraariculary was 
      rapidly detectalbe in the blood. However, systemic absorption was considerably 
      faster under inflammation conditions; the blood level was lower than following 
      administration of 3H-dexamethasone into the normal knee-joint, the distribution 
      from which was not uniform. After pretreating the animals with high does of 
      hydrocortisonacetate, the i.v. application of 3H-dexamethasone was followed by a 
      delayed first phase of the biphasis process of elimination. 6. Autoradiographic 
      studies revealed 14C-ASA to be accumulated in the synovial fluid under normal 
      conditions and in the periaricular connective tissue under inflammation 
      conditions.
FAU - Havemann, D
AU  - Havemann D
LA  - ger
PT  - English Abstract
PT  - Journal Article
TT  - Antiphlogistische Pharmaka. Untersuchungen zur Pharmakokinetik 
      anti-inflammatorischer Substanzen.
PL  - Germany
TA  - Fortschr Med
JT  - Fortschritte der Medizin
JID - 2984763R
RN  - 0 (Anti-Inflammatory Agents)
RN  - 7S5I7G3JQL (Dexamethasone)
RN  - GN5P7K3T8S (Phenylbutazone)
RN  - R16CO5Y76E (Aspirin)
RN  - XXE1CET956 (Indomethacin)
SB  - IM
MH  - Animals
MH  - Anti-Inflammatory Agents/administration & dosage/blood/*pharmacology
MH  - Aspirin/pharmacology
MH  - Dexamethasone/pharmacology
MH  - Indomethacin/pharmacology
MH  - Injections, Intra-Articular
MH  - Phenylbutazone/pharmacology
MH  - Rabbits
MH  - Synovitis/drug therapy
EDAT- 1977/01/20 00:00
MHDA- 1977/01/20 00:01
CRDT- 1977/01/20 00:00
PHST- 1977/01/20 00:00 [pubmed]
PHST- 1977/01/20 00:01 [medline]
PHST- 1977/01/20 00:00 [entrez]
PST - ppublish
SO  - Fortschr Med. 1977 Jan 20;95(3):177-81.