1 / 21

ANTIINFLAMATOARELE NESTEROIDIENE

ANTIINFLAMATOARELE NESTEROIDIENE. FARMACOLOGIE CLINICA. AINS - GENERALITATI. medicatie simptomatica reduc semnele + simptomele inflamatiei, dar nu inlatura cauza. AINS - MECANISM DE ACTIUNE (1). FOSFOLIPIDE. fosfolipaza. ACID ARAHIDONIC. AINS. COX 1, 2. PROSTAGLANDINE.

driscoll-mooney
Download Presentation

ANTIINFLAMATOARELE NESTEROIDIENE

An Image/Link below is provided (as is) to download presentation Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author. Content is provided to you AS IS for your information and personal use only. Download presentation by click this link. While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server. During download, if you can't get a presentation, the file might be deleted by the publisher.

E N D

Presentation Transcript

  1. ANTIINFLAMATOARELENESTEROIDIENE FARMACOLOGIE CLINICA

  2. AINS - GENERALITATI • medicatie simptomatica • reduc semnele + simptomele inflamatiei, dar nu inlatura cauza

  3. AINS - MECANISM DE ACTIUNE (1) FOSFOLIPIDE fosfolipaza ACID ARAHIDONIC AINS COX 1, 2 PROSTAGLANDINE

  4. AINS - MECANISM DE ACTIUNE (2) ACID ARAHIDONIC COX 2 indusa COX 1 constitutiva INFLAMATIE DURERE FEBRA protectie g-I agregarea plachetelor mentine FPR

  5. AINS - MECANISM DE ACTIUNE (3) • prin inhibarea COX2, AINS pot proteja contra unor tumori si a b. Alzheimer • in unele f. de cancer exista o hiperactivitate a genei COX2 si concentratii crescute in sange inhibarea apoptozei elib. de radicali liberi stim. neoformarii vaselor in tumori

  6. AINS - STRUCTURA CHIMICA (1) • ACIZI CARBOXILICI • a. si esteri salicilici: ASPIRINA, DIFLUNISAL • a. acetici: • acizi fenilacetici: DICLOFENAC, ACLOFENAC • acizi carbo- si heterociclici: INDOMETACIN, SULINDAC • a. propionici: KETOPROFEN, IBUPROFEN, NAPROXEN • a. fenamici: ACID FLUFENAMIC, ACID MEFENAMIC

  7. AINS - STRUCTURA CHIMICA (2) • ACIZI ENOLICI • pirazolidine: OXIFENBUTAZONA, FENILBUTAZONA • oxicami: PIROXICAM, TENOXICAM, MELOXICAM • COMPONENTE NONACIDE • NABUMETON

  8. AINS - CLASIFICARE • CLASICE • aspirina, indometacin, diclofenac, piroxicam • COX 2 SELECTIVE • meloxicam (movalis), nimesulid (aulin) • COX 2 SPECIFICE • celecoxib (celebrex), rofecoxib (vioxx)

  9. AINS - FARMACOCINETICA (1) • parametri farmacocinetici • absorbtie • biodisponibilitate • distributie in organism • timp de injumatatire (T 1/2)

  10. AINS - FARMACOCINETICA (2) • absorbtia • completa (majoritatea) • biodisponibilitatea • difuzeaza mai lent in fluidul sinovial, unde nivelul conc. este mult mai stabil intervalul dozarii este mai lung decat T1/2 plasmatica • se leaga in procent mare de prot. plasmatice, cant. de drog liber (comp. activa)= relativ mica • fractia nelegata nu e dependenta de doza, exceptii: naproxen, fenilbutazona, salicilat. • legarea scade la varstinici, PR

  11. AINS - FARMACOCINETICA (3)

  12. AINS - FARMACOCINETICA (4) • clearance-ul AINS = metabolizare hepatica, rezultand metaboliti inactivi, ce sunt excretati prin urina • alte AINS (aspirina, sulindac, nabumeton) sunt convertite in metab. activi ce produc efectele terapeutice • farmacocinetica unor AINS poate fi afectata de b. hepatice, renale si de varsta inaintata

  13. AINS - REACTII ADVERSE (1) • gastrointestinale (10%): indigestie, reflux GE, eroziuni, ulcer peptic, hemoragii g-I • hepatice: crestere a transaminazelor, colestaza • renale: crestere tranzitorie a creatininei, hiponatremie, hiperkaliemie, IRA, nefropatie analgezica

  14. AINS - REACTII ADVERSE (2) • hematologice: trombocitopenie, neutropenie, aplazie a liniei rosii, a. hemolitica • cutanate: fotosensibilitate, eritem multimorf, urticarie, necroliza epidermica toxica • respiratorii: bronhospasm, pneumonita • SNC: cefalee, ameteli, meningita aseptica

  15. INTERACTIUNI MEDICAMENTOASEAINS CE AFECTEAZA ALTE DROGURI • anticoagulante orale: creste ef. anticoagulant • litiu: risc de toxicitate • ADO: risc de hipoglicemii • metotrexat: risc de toxicitate • digoxin: la varste inaintate, scade eliminarea, risc de toxicitate • aminoglicozide: afectare a functiei renale • BB, IECA, diuretice: scade ef. hipotensor

  16. INTERACTIUNI MEDICAMENTOASEDROGURI CE AFECTEAZA AINS • antiacide: cele cu Al reduc absorbtia, dar bicarbonatul de Na o creste • probenecid: scade metab. si clearance-ul renal • colestiramina: scade absorbtia • metoclopramid: creste absorbtia aspirinei

  17. AINS - INDICATII • spondilartropatii seronegative • PR, reumatisme abarticulare • criza de guta • stari inflamatorii- dureroase postoperator, dupa extractii dentare • inflamatii in sfera pelvina • dismenoree

  18. AINS - INDICATII • conjunctivita alergica, keratoconjunctivita, ulcer cornean • migrene • mialgii, boala artrozica • in aplicatii topice: afectare dureroasa a tes. cel. subcutanat, fascii, tendoane, enteze, ligamente, capsule, burse, tromboze varicoase, degeraturi

  19. CONTRAINDICATII, PRECAUTII • astm bronsic • UGD, sangerari GI • supresie medulara, imunosupresie • coagulopatii • sarcina, alaptare • varstnici • IC, HTA • afectiuni hepatice, renale • porfirie • hipersensibilitate le med, polipi nazali, urticarie

  20. PRESCRIERE PRACTICA • raspuns individual • durata 7-10 zile • AINS nu se asociaza intre ele • forme de prezentare: cp, sup, f, ungv. • prep. combinate: arthrotec (diclofenac+misoprostol)

  21. PRESCRIERE PRACTICA-DOZE AINS DOZA

More Related