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Farmacologie > CURS 8 AUTACOIZI-incomplet > Flashcards

CURS 8 AUTACOIZI-incomplet Flashcards

1
Q

Ce sunt autacoizii

A

substante care se elibereaza local si asigura homeostazia si/sau reactia tesuturilor/organelor

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2
Q

Din ce categorie fac parte autacoizii

A

Mesageri primari

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3
Q

Clasificarea autacoizilor

A
  • Aminge biologic active
  • Lipide biologic active
  • Polipeptide biologic active
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4
Q

Mecanism actiune Histamina

A

Agonist receptori histaminergici

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5
Q

Distributie si transmitere H1

A
  • musculatura neteda, endoteliu, creier

- creste IP3 si DAG

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6
Q

Distributie si transmitere H2

A
  • mucoasa gastrica, muschi cardiac, mastocite, creier

- creste AMPc

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7
Q

Distributie si transmitere H3

A
  • plex mezenteric

- det. scaderea histaminei din neuronii histaminergici

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8
Q

Efecte Histamina cord

A
  • scade TA creste frecvente
  • Efect aritmogen
  • dilatatia si scaderea rezistentei vaselor coronare
  • hipotensiune, edem, hemoconcentratie
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9
Q

Efecte histamina bronhii

A

-bronhoconstrictie

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10
Q

Efecte histamina tract GI

A
  • stimuleaza m. neteda

- stimuleaza secretia gastrica

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11
Q

Efecte histamina terminatii nervoase/MDS

A
  • poate induce durere si prurit

- descarcari ale MDS

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12
Q

La ce se refera “Triplul raspuns”

A

Injectare intradermina de H => rasp din partea
-m. netede microcirculatorii
-endoteliu capilar/venular
-terminatii nervoase senzitive
Consta in edem roseata vasodilatatie brusca

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13
Q

Indicatii Histamina

A

Diagnosticare:

  • capacitatea secretiei gastrice
  • feocromocitomul
  • hiperreactivitate bronsica - PERICULOS
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14
Q

Efecte adverse Histamina

A
  • bronhoconstrictie
  • hipotensiune
  • dereglaj gastro-intestinal
  • astenie
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15
Q

Factori care elibereaza histamina

A
  • fizici: traumatisme, arsuri
  • chimici: opiacee, chinina, Peniciline, cefalosporine, aminoglicozide, hidralazina, curarizante, barbiturice, bradikinina
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16
Q

3 agonisti ai R-H

A

Betahistidina, Betazole, Impromidina

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17
Q

Indicatie Betahistidina

A

Sindrom Meniere

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18
Q

Mecanism Cromoglicat de sodiu

A
  • inhiba histamina si leucotrienele din mastocite
  • altereaza functia canalelor de Cl
  • blocarea influxului transmembranar de Ca
  • inhiba SELECTIV anafilaxia pulmonara
  • creste AMPc
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19
Q

Cromoglicat de sodiu farmacocinetica

A
  • slab absorbit gastro-intestinal
  • se ia prin inhalatie/aerosoli
  • 1-2h inaite de contactul cu alergeni
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20
Q

Cromoglicat de sodiu indicatii

A

In scop profilactic: astm, rinita, conjunctivita alergica

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21
Q

inhibitori ai eliberarii de histamina

A 
Cromoglicat de sodiu
Nedocromil
Amlexanox
Lodoxamida
Pemirolast
Reprinast
Metilxantine
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22
Q

Nedocromil particularitati?

A

Aceleasi actiuni ca si cromoglicat de sodiu dar cu intensitate mult mai mare + important efect de inhibare a tusei
Reduce necesarul de glucocorticoizi sistemici daca sunt adm in asociere

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23
Q

Antagonisti fiziologici histamina

A

A/NA

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24
Q

Exemple antagonisti competitivi R-H1 Generatia I

A

Etanolamine ( Carbinoxamina, Difenhidramina, Doxylamina, dimenhydrinate )
Imidazoline (Antazoline )
Etilamindiamine (Tripelenamine, Pyrilamina )
Etilendiamine ( Cloropiramina )
Deriv. piperazinici ( Hydroxizin, Ciclizine, Mecyclizin)
Alchilamine ( Clorfeniramin, Brompheniramin )
Deriv. fenotiazinici ( Prometazina, Proclorperazina,
Tetilperazina, Alimemazina)

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25
Q

Exemple antagonisti competitivi R-H1 Generatia II

A

Deriv. piperidinici (Loratadina, Terfenadina, Astemizol )
piperazinici (Cetirizina )
fenotiazinici (Mequitazina )

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26
Q

Exemple antagonisti competitivi R-H2

A

Cimetidina
Ranitidia
Nizatidina
Famotidina

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27
Q

Cromoglicat de Na - efecte adverse

A

miozite, artralgii, inflitrate pulmonare cu eozinofile, disurie, greata, gust neplacut, gastro-enterite

28
Q

Alte antihistaminice de tip anti-H1

A

Ciproheptadina, Clemastina, Phenindamine, Clorfenoxamina, Dimetinden, Bamipine

29
Q

Efecte biologice antihistaminice de tip anti-H1

A
  • antialergice
  • antiemetic
  • anticolinergic
  • alfa1-blocant
  • antiserotoninergic
  • antiparkinsonian
  • sedativ
  • anestezic local
  • antiinflamator
30
Q

cine are efect sedativ?

A

deriv. piperazinici, fenotiazinici, etanolamine, etilendiamine

31
Q

cine are efect antiemetic?

A

deriv. piperazinici, fenotiazinici, etanolamine

32
Q

cine are efect anticolinergic?

A

deriv. fenotiazinici, etanolamine, alchilamine, etilendiamine

33
Q

cine are efect antiparkinsonian?

A

etanolamine, etilendiamina

34
Q

cine are efect alfa1-blocant?

A

deriv. fenotiazinici, alchilamine

35
Q

cine are efect antiseroninerigic?

A

Ciproheptadina

36
Q

cine are efect de anestezic local?

A

deriv. piperidinici

37
Q

cine are efect antiinflamator?

A

Generatia a IIa

38
Q

efect Hidroxizin?

A

inhiba histamina, substanta P, serotonina si prostaglandine

39
Q

Farmacocinetica antihistaminice de tip H1?

A

Deriv piperazinici si piperidinici nu se adm cu sucuri de grapefruit =>tahiaritmii severe si fibrilatie atriala

40
Q

Efecte adverse antihistaminice de tip H1?

A
  • sedare - cine?
  • ef. antimuscarinice
  • stimularea apetitului - cine?
  • torsada varfurilor - cine?
41
Q

Indicatii antihistaminici de tip H1

A
  • alergii
  • antiemetice ( deriv piperazinici, fenotiazine, etanolamine)
  • sdr Meniere: Proclorperazina
  • greata si varsaturi in sarcina: Doxylamina
  • anxiolitice: etanolamine etilendiamine, fenotiazine, piperazine
  • boli psihice: Clorpromazina
  • stimularea apetitului: Ciproheptadina
  • Parkinson: Difenhidramina + etanolamine
  • Sdr cistitei interstitiale: Hidroxizin
42
Q

Antihistaminice de tip H2 - mecanism

A

antagonisti competitivi H2

Nizatidina mai inhiba acetilcolinesteraza

43
Q

Antihistaminice de tip H2- farmacodinamie

A
  • inhiba secretia gastrica bazala de HCl
44
Q

Antihistaminice de tip H2 - farmacocinetica

A

Cimetidina este un inhibitor enzimatic al metabolizaii medicamentelor

45
Q

Antihistaminice de tip H2- Indicatii

A
  • boala peptica
  • Sdr Zollinger Ellison
  • reflux gastro-esofagian
  • prevenire gastrite
  • disepsia neulceroasa
46
Q

Efecte adverse - Cimetidina

A

SNC- stari confuzionale, delir, halucinatii

  • endocrine: ginecomastie, scaderea spermatogenezei, a libidoului, galactoree
  • hematologice: granulocitopenie, anemie plastica
  • hepatic: cresterea transaminazelor, icter colestatic, hepatite acute
47
Q

Efecte adverse - Nizatidina

A

cefalee, efect prokinetic cresterea tranzitorie transaminazelor, cronotrop/inotrop negativ

48
Q

Efecte adverse - Ranitidina

A

cresterea transaminazelor, icter colestatic, hepatite acute

49
Q

Efecte adverse - Famotidina

A

cefalee, cresterea tranzitorie a transaminazelor

50
Q

Efecte serotonina

A
  • Cardiov: vasoconstrictie si agregare plachetara
  • Respirator : bronhoconstrictie si hiperventilatie reflexa
  • Tract GI: stimuleaza peristaltismul
  • SNC: halucinatii, transmite durerea, somnolenta, stimuleaza emeza, modif ale dispozitie si comportamentului
51
Q

Agonisti neselectivi ai h-HT1D si 5-HT1B

  • care sunt?
  • indicatii
A
  • Sumatriptan, Naratriptan, Rizatriptan, Zolmitriptan

- Criza de migrena, cefalee vasculara

52
Q

Agonisti neselectivi ai h-HT1D si 5-HT1B

  • efecte adverse
  • contraindindicatii
A
  • parestezii, dureri anginoase, tahicardii

- angina pectorala, leziuni aretomatoase coronariene

53
Q

Agonisti selectivi ai HT4 ( elibereaza si acetilcolina la nivel enteric)

  • care sunt?
  • efecte
A
  • Cisaprid, Norcisaprid

- stimuleaza peristaltismul, relaxeaza pilorul, contracta cardia

54
Q

Agonisti selectivi ai HT4

  • indicatii
  • efecte adverse
A
  • prokinetic

- diaree, crampe, cefalee, aritmii

55
Q

Agonist partial 5HT4:

  • care e?
  • indicatie
A
  • Tegaserod

- colon iritabil

56
Q

Agonisti selectivi 5HT1A

  • care sunt?
  • efecte?
  • farmacocinetica
A
  • Buspiron, Isapiron, Gepiron, Tandopiron
  • Anxiolitice fara efecte sedative
  • supuse efectului primului pasaj
57
Q

Agonisti selectivi 5HT1A

  • Efecte adverse
  • contraindicatii
A
  • tahicardii, nervozitate, parestezii, mioza, stari de confuzie, tulburari GI
  • tulburari de ritm
  • Nu determina adictie
58
Q

Antagonisti ai 5HT2A si 5HT2C

  • care sunt?
  • indicatii?
  • efecte adverse
A
  • Trazodone, Nefazodone, Mirtazapine
  • Depresii
  • somnolenta, ameteli, greata, Mirtazapine da si stimularea apetitului cu crestere ponderala
59
Q

Antagonisti 5HT3

  • care sunt?
  • efecte?
  • indicatii?
A

-Ondansetron, Granisetron, Dolansetron, Tropisetron, Alosetron, Cilansetron
-antiemetic, antidepresiv
-electie pt varsaturile induse de citostatice
Alosetron e indicat in colon iritabil

60
Q

Antagonisti 5HT3

  • efecte adverse?
  • contraindicatii?
A

-cefalee, constipatie/diaree, crampe, aritmii
-sarcina
Trebuie redusa doza in caz de insuf hepatica

61
Q

Ritanserine

  • efecte
  • indicatii
A
  • modifica timpul de sangerare, reduce formarea tromboxanului, altereaza functia plachetara
  • antiagregant
62
Q

Ketanserine

  • efecte
  • indicatii
A
  • antagonizeaza agregarea plachetara, vasodilatatie

- HTA, vasospasm

63
Q

Ciproheptadina

  • efecte?
  • indicatii?
A
  • antialergic, sedativ, crestere ponderal

- antialergic, stimularea apetitului, tumori carcinoide, sindrom dumping post-gastrectomie

64
Q

Ciproheptadina

  • efecte adverse?
  • contraindicatii?
A
  • cefalee, somnolenta, confuzie

- glaucom, conducatori, retentie

65
Q

Inhibitori selectivi ai recaptarii de serotonina

  • care sunt?
  • indicatii?
A
  • Fluoxetine, Sertraline, Paroxetine, Fluvoxamine, Ctalopram si Escitalopram
  • Depresie
66
Q

Inhibitori ai recaptarii serotoninei si NA

  • care sunt?
  • indicatii?
A
  • Venlafaxine si Bupropion

- Depresii

67
Q

Stimulatori de serotonina

  • care sunt?
  • indicatii?
  • efecte adverse?
A
  • Dexfenfluramina si Fenfluramina
  • Tratamentul obezitatii
  • insomnie, cefalee, fibroplazie endocardica si retroperitoneala, hipertensiune pulmonara

Farmacologie (10 decks)

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