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Farmacologie > CURS 5 SIMPATICOMIMETICE > Flashcards

CURS 5 SIMPATICOMIMETICE Flashcards

1
Q
  • ce sunt catecolaminele?

- ce fel de grupare prezinta? Trece de barierele fiziologice?

A
  • Mediatori ai ai SNV

- Grupare catecol, traverseaza foarte greu barierele.

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2
Q
  • Care sunt?
  • Cine le produce?
  • Pe ce receptori actioneaza fiecare?
A
  • Adrenalina: de MSR, pe alfa1,2 si beta1,2,3
  • Noradrenalina:neuronul postggl are SN periferic, neuroni cerebrali, si MSR, pe alfa1,2 si beta1, mai slab pe beta2
  • Dopamina: pe D1-D5»beta»alfa
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3
Q

Reactia sintezei

A

Fenilalanina - Tirozina - L-dihidroxifenilalanina - dopamina - NA - A

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4
Q

Posibilitatile NA dupa eliberare in fanta

A
  • difuzarea in circulatia generala unde va fi degradata de MAO sau COMT
  • inactive in spatiul sinpatic de COMT
  • recaptare
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5
Q

Receptorul alfa1

  • unde se afla
  • cum actioneaza (tabel)
A

-alfa1A : Neocortex, hipocamp, cord, rinichi, musculatura neteda, limfocite, macrofage
-alfa1B: idem + ficati si splina
actioneaza prin cresterea IP3 si DAG

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6
Q

Receptorul alfa2:

  • unde se afla
  • cum actioneaza (tabel)
A

-alfa2A: plachete, cortex, musculatura neteda vasculara, adipocite, cel. juxtaglomerulare renale, terminatii nervoase presinaptice, postsinaptic in SNC
-alfa2B: idem doar ca fara plachete
-alfa2C: idem 2B
actioneaza prin scaderea AMPc, activeaza canalele de K, le bloccheaza pe cele de Ca

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7
Q

Receptorul beta1

  • unde se afla
  • cum actioneaza (tabel)
A

Presinaptic: terminatii nervoase presinaptice, celule juxtagl renale
Postsinaptic: cord creier adipocite limfocite T, macrofage
Creste AMPc

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8
Q

Receptorii beta2 si beta3

  • unde se afla
  • cum actioneaza (tabel)
A

-beta2: cel. musculare netede, ficat, cord, muschi scheletic, limfocite. mastocite
-beta3:adipocite
Cresc AMPc

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9
Q

Receptorul D1

  • unde se afla
  • cum actioneaza (tabel)
A

Cel efectoare in special m neteda a patului vascular renal, creiet, limfocite T
Creste AMPc

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10
Q

Receptorul D2

  • unde se afla
  • cum actioneaza (tabel)
A

Cel efectoare in special m neteda a patului vascular renal, terminatii presinaptice
Scade AMPc, activeaza K si Ca

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11
Q

Receptorii D3 D4 D5

  • unde se afla
  • cum actioneaza (tabel)
A

D3:Creier - scade AMPc
D4:Creier, aparat cardio-vasc - scade AMPc
D5: idem D1 - creste AMPc

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12
Q

Farmacodinamie catecolamine

-Globi oculari

A
  • alfa1 : midriaza si favorizarea drenarii umorii

- beta2 si D2 : relaxarea muschiului ciliar

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13
Q

Farmacodinamie catecolamine

-Cord

A
  • alfa1 : initrop +

- beta1 : inotrp si dromotrop +, creste consumul de oxigen, astfel eficienta cordului este diminuata

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14
Q

Farmacodinamie catecolamine

-vase sanguine

A

ADRENALINA:
-doze mici: vasodilatatie si scaderea presiunii (beta2)
-doze medii: creste TA si scade rezistenta periferica + creste frecventa si debitul (alfa1)
-doze mari, creste TA, creste rezist periferica si bradicardie prin riposta vagala
NORADRENALINA
-creste TA, rezistenta periferica + bradicardie la orice dozaj

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15
Q

Farmacodinamie catecolamine

-vasele coronare?

A

efect coronarodilatator, iar pe vasele viscerelor, vasodilatatie medie

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16
Q

Farmacodinamie catecolamine

-musculatura neteda gastrointestinala

A

-alfa 2 si beta2: relaxare musc. neteda a tubului digestiv
-alfa1: contractia sfincterelor
NU influenteaza secretia gastro-intestinala

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17
Q

Farmacodinamie catecolamine

-musculatura tract genito-urinar

A
  • beta2: relaxarea peretelui vezicii
  • alfa1: contractia sfincterului vezical, musculaturii uterine
  • alfa1: stimulata ejacularea
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18
Q

Farmacodinamie catecolamine

  • bronsii
  • m. pilomotori
  • trombocite
  • SNC
A
  • beta2: bronhodilatatie medie
  • alfa1: erectia firelor de par, transpiratie palmare
  • stimularea agregarii plachetare
  • creste atentia, nervozitatea, tremor, anxietate, insomnie
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19
Q

Farmacodinamie catecolamine

-conditii fiziologice metabolism

A
  • hiperglicemie
  • inhiba sinteza de insuline
  • hiperlactacidemie
  • hiperkaliemie
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20
Q

Farmacodinamie catecolamine

-in concentratii mari, metabolism

A
  • acidoza metabolica

- hiperlipemie

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21
Q

Farmacodinamie catecolamine

  • la niv. renal
  • metabolism bazal
A
  • beta1 stimuleaza renina iar alfa2 o inhiba

- efect calorigen, NA are un rol important in apararea fata de frig

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22
Q

Farmacodinamie catecolamine

-glande exo/endocrine

A
  • inhiba secretia salivara de apa si K si a secretiei exocrine pancreatice
  • creste sinteza de melatonina
  • det eliberarea de prostaglandine
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23
Q

Reglarea presinaptica

A 
-Autoreceptori:
prin alfa2: inhiba NA
prin beta1: elibereaza NA
prin D2: inhiba NA, Dopamina
-Terminatiile nervilor adrenergici pot regla si alti heteroreceptori, spre ex pt Ach, prostaglandine
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24
Q

Reglare postsinaptica

A
  • desensibilizarea adrenoreceptorilor ( tahifilaxie)
  • sechestrarea receptorilor in membrana
  • scaderea sintezei de R
  • inactivarea R prin fosforilare
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25
Q

Clasificare stimulante alfa, beta, D

A
  • actiune directa: A, NA, dopamina, ibopamina

- actiune indirecta: Efedrina

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26
Q

Adrenalina

indicatii

A
  • soc anafilactic
  • hemoragii difuze
  • glaucom
  • resuscitare in stop
  • asociere cu anestezice locale
  • criza de astm
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27
Q

Adrenalina

efecte adverse

A
  • anxietate, paloare, palpitatii

- cresterea TA (cu complicatii)

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28
Q

Adrenalina

contraindicatii

A
  • angina, tahiaritmii, HTA
  • risc de AVC
  • hipertiroidii
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29
Q

Cu cine nu asociem Adrenalina

A
  • preparate cu calciu

- anestezice locale cand e vorba de extremitati

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30
Q

Noradrenalina

indicatii

A
  • sangerari difuze de la suprafata pielii sau mucoaselor

- asociere cu anestezice locale

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31
Q

Dopamina

mecanism actiune

A

-agonist al R dopaminergici, prin D1 det. vasodilatatie, iar prin D2 inhiba NA si dopamina
-agonist beta (doze medii)
agonist alfa (doze mari)

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32
Q

Dopamina

  • indicatii
  • efecte adverse
A
  • soc cardiogen

- greata, varsaturi, dureri anginoase

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33
Q

Dopamina

-contraindicatii

A
  • hipo/hipertensiunea arteriala, tulburari de ritm, de conducere, angina
  • scleroze cerebrale
  • glaucom
  • migrena
  • manii, schizofrenii
34
Q

Efedrina

mecanism

A
  • in primul rand elibereaza NA

- agonist al alfa1,2 si beta1,2

35
Q

Efedrina

-efecte farmacodinamice

A
  • inotrop, dromotrop pozitiv
  • vasoconstrictie
  • scade permeabilitatea capilara
  • bronhodilatatie
  • efecte psihoanaleptice si anorexigene
36
Q

Efedrina

-indicatii

A
  • bloc AV
  • hipotensiune
  • astm criza
  • reduce edemul mucoasei nazale si conjunctivale
37
Q

Efedrina

-efecte adverse

A
  • tahiaritmii
  • HTA
  • tahifilaxie
  • anorexie, dependenta
38
Q

Efedrina

-contraindicatii

A

-HTA, tahiaritmii, angina
-psihoze endogene
OBS: Cocaina reduce efectele Efedrinei. De ce?

39
Q

Clasificare stimulate ale R alfa

A
  • administrare sistemica: Etliefrina, Fenilefrina, Metoxamina, Midodrina, Metaraminol
  • administrare locala: Nafazolina Tetrizolina Oximetazolina, Xylometazolina
40
Q

Etilefrina

  • mecanism
  • efecte
  • indicatii
A
  • agonist alfa1 si 2
  • creste presiunea arteriala
  • hTA (tratament de fond)
41
Q

Fenilefrina

  • mecanism
  • efecte
A
  • agonist alfa1»»>alfa2, in plus elibereaza NA

- creste TA, bradicardie prin reflex vagal, midriaza scurta, reduce edem nazal si conjunctival

42
Q

Fenilefrina

-Indicatii

A
  • rinite/conjunctivite
  • hTA
  • midriaza de diagnostic
  • tahicardii paroxistice supraventriculare
  • se asociaza cu anestezice locale
  • DIAGNOSTICUL SDR CBH
43
Q

Fenilefrina

  • efecte adverse
  • contraindicatii
A
  • tahifilaxie, cresterea TA, tahicardie

- HTA, tahiaritmii, angina

44
Q

Midodrine

  • mecanism
  • indicatii
A
  • agonist alfa1 selectiv

- HTA ortostatica

45
Q

Metoxamina

  • mecanism
  • efecte
  • indicatii
A
  • agonist alfa1 selectiv
  • creste TA de lunga durata si bradicardie prin reflex
  • hTA
46
Q

Metaraminol

-efecte

A

-puternic efect de crestere a TA
-bradicardie reflexa
-creste tonusul venos/scade fluxul sanguin renal si cerebral
-vasoconstrictie pulmonara
Indicatie: hTA

47
Q

Nafazolina

-mecanism

A
  • agonist alfa1 si 2

- elibereaza NA

48
Q

Nafazolina

  • efecte
  • indicatii
A
  • reduce edemul nazal/conjunctiv

- rinite/conjunctivite

49
Q

Nafazolina

-efecte adverse

A
  • tahifilaxie
  • atrofia mucoasei nazale
  • copii sub 3 ani : hTA
  • adulti:HTA si cresterea conductivitatii in tesutul excitoconductor
50
Q

Tetrizolina, Oximetazolina, Xylometazolina

  • mecanism?
  • indicatii?
A
  • agonist alfa1 si 2

- rinite nespecifice sau alergice

51
Q

Stimulante semiselective beta1 si 2

A
  • cu actiune semiselectiva si de scurta durata: Isoprenalina, Orciprenalina, Etilnorepinefrina
  • Actiune predominanta pe beta-vasculari: Bufenina, Bamethan
52
Q

Stimulante selective beta1

A

Dobutamina, Prenalterol

53
Q

Stimulante selective beta2

A

durata medie si efect rapid: Salbutamol, Terbutalina, Fenoterol, Clenbuterol, Pirbuterol, Procaterol

  • durata lunga si efect tardiv: Salmeterol, Formoterol
  • durata superlunga: Bambuterol
  • Indicate in travaliul prematur: Salbutamol, Ritodrine, Isoetharina, Isoxuprina
54
Q

Isoprenalina

  • efecte
  • indicatii
A
  • cronotrop/inotrop pozitiv si puternic bronhodilatator

- resuscitarea stopului din IMA cu asistola sau BAV total, astm bronsic, doar initial ca alternativa

55
Q

Isoprenalina

  • efecte adverse
  • dezavantaje
A
  • greata, varsaturi, cefalee, palpitatii

- durata de actiune scurta si stimulare puternica beta1 cardiaci

56
Q

Orciprenalina

  • mecanism
  • efecte
  • indicatii
A
  • mai mult pe beta2 decat beta1
  • puternic bronhodilatator, slab crono/inotrop pozitiv
  • astm
57
Q

Bufenina si Bamethan

  • mecanism
  • efecte
  • indicatii
A
  • agonist beta1 si 2
  • puternic bronhodilatator si vasodilatator
  • claudicatie intermitenta, sindrom Raynaud
58
Q

Dobutamina

-efecte

A
  • inotrop pozitiv accentuat
  • prezinta tahifilaxie
  • poate induce aritmii
  • reduce edemul mucoaselor
59
Q

Dobutamina

  • mecanism
  • indicatii
A
  • agonist beta1

- soc cardiogen, insuf cardiaca congestiva

60
Q

Prenalterol

  • mecanism
  • indicatii
A
  • agonist beta1

- unele forme de IC

61
Q

Stimulante selective beta2

-efecte

A
  • bronhodilatator
  • imunosupresor
  • antiinflamator
  • la concentratii scazute deschide canalele de K, Ca-dependente din celulele musculare netede din caile respiratorii
  • fenomen de stabilizare membranara
  • stimuleaza efectul de autoepurare bronsica mucocicliara
62
Q

Stimulante selective beta2

-efecte adverse

A
  • tremor
  • anxietate, nervozitate, agitatie, cefalee
  • palpitatii
  • hiperpotasemie
63
Q

Alti eliebratori de catecolamine, exemple

A

Hidroxi/met/amfetamina, Fenmetrazina, Pemolin, Fenilpropanolamina, Metilfenidat, MDMA, Amantadina

64
Q

Alti eliebratori de catecolamine

-efecte SNC

A
  • efecte psihoanaleptice si anorexigene, determina dependenta
  • stimuleaza SRAA
  • inhiba MAO
  • inhiba recaptarea de catecolamine
65
Q

Alti eliebratori de catecolamine

-efecte periferice

A
  • cresterea TA

- inotrop/cronotrop/dromotrop pozitiv

66
Q

Alti eliebratori de catecolamine

-efecte adverse

A
  • greata varsaturi constipatie/diaree
  • HTA, tahiartimtii, cefalee
  • psihoze endogene
  • dependenta
  • tulburari ale gandirii
67
Q

Alti eliebratori de catecolamine

-contraindicatii

A
  • psihoze
  • Tourette
  • HTA, tahiaritmii
  • leziuni ateroatoase coronariene
  • glaucom
68
Q

Amfetamina

-indicatii

A
  • narcolepsie
  • sindrom hiperkinetic
  • enurezis
  • adjuvant in parkinson
  • adjuvant in crizele de epilepsie petit mal
  • stimularea performantelor psihomotorii
69
Q

Fenmetrazina

-indicatie

A

-anorexigen

70
Q

Hidroxiamfetamina

-indicatie

A

-sindrom Horner cu leziune preggl

71
Q

Ecstasy-efecte

A

-euforie, halucinatii, comportament stereotipic

72
Q

Amantadina

-mecanisme

A
  • agonist neselectiv R dopaminergici
  • eliberator dopamina
  • antagonist al R NMDA
  • inhibarea proteinei M2 de la nivelul capsidei virale => este impiedicata asamblarea si eliberarea de noi virioni
73
Q

Amantadina

-indicatii

A
  • antiviral

- boala parkinson

74
Q

Cocaina

-efecte farmacodinamice

A
  • midriaza, tahiaritmii, cresteri tensionale
  • perforatie de sept nazal
  • dependenta puternica si rapida
75
Q

Cocaina

  • mecanism
  • utilizari
A
  • inhiba recaptarea noradrenalinei

- nemedical: efect euforizant/ medical: anestezic local de suprafata in ORL/oftalmo

76
Q

Tiramina

  • mecanism
  • efecte
A

-blocarea recaptarii NA
-eliberarea NA
-efecte similare cu NA
Rezulta din metabolismul normal al tirozinei rapid metabolizata prin MAO

77
Q

inhibitori ai dopa-decarboxilazei

A

Benserazida, Carbidopa

78
Q

inhibitori MAO-B

A

Selegiline, Rasagiline, Lazabemide, Mofegiline

79
Q

inhibitori COMT

A

Tolcapone, Nitecapone, Entacapone

80
Q

Agonisti ai R-dopaminergici

A
  • Ergopeptine: Bromocriptina, Lisuride, Pergolide

- Deriv neergopeptinici: Piribedil, Ropinirole, Apomorfina

81
Q

inhibitori neselectivi ai MAO

A

Hidrazine: Fenelzina, Isocarboxazid
Nehidrazine: Tranycypromine, Dextroamfetamina

82
Q

inhibitori selectivi ai MAO

A

Moclobemide, Brofaromine, Toloxatone

Farmacologie (10 decks)

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