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Farmacologie > CURS 5 SIMPATICOMIMETICE > Flashcards

CURS 5 SIMPATICOMIMETICE Flashcards

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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
Clasificare stimulante alfa, beta, D
- actiune directa: A, NA, dopamina, ibopamina | - actiune indirecta: Efedrina
26
Adrenalina | indicatii
- soc anafilactic - hemoragii difuze - glaucom - resuscitare in stop - asociere cu anestezice locale - criza de astm
27
Adrenalina | efecte adverse
- anxietate, paloare, palpitatii | - cresterea TA (cu complicatii)
28
Adrenalina | contraindicatii
- angina, tahiaritmii, HTA - risc de AVC - hipertiroidii
29
Cu cine nu asociem Adrenalina
- preparate cu calciu | - anestezice locale cand e vorba de extremitati
30
Noradrenalina | indicatii
- sangerari difuze de la suprafata pielii sau mucoaselor | - asociere cu anestezice locale
31
Dopamina | mecanism actiune
-agonist al R dopaminergici, prin D1 det. vasodilatatie, iar prin D2 inhiba NA si dopamina -agonist beta (doze medii) agonist alfa (doze mari)
32
Dopamina - indicatii - efecte adverse
- soc cardiogen | - greata, varsaturi, dureri anginoase
33
Dopamina | -contraindicatii
- hipo/hipertensiunea arteriala, tulburari de ritm, de conducere, angina - scleroze cerebrale - glaucom - migrena - manii, schizofrenii
34
Efedrina | mecanism
- in primul rand elibereaza NA | - agonist al alfa1,2 si beta1,2
35
Efedrina | -efecte farmacodinamice
- inotrop, dromotrop pozitiv - vasoconstrictie - scade permeabilitatea capilara - bronhodilatatie - efecte psihoanaleptice si anorexigene
36
Efedrina | -indicatii
- bloc AV - hipotensiune - astm criza - reduce edemul mucoasei nazale si conjunctivale
37
Efedrina | -efecte adverse
- tahiaritmii - HTA - tahifilaxie - anorexie, dependenta
38
Efedrina | -contraindicatii
-HTA, tahiaritmii, angina -psihoze endogene OBS: Cocaina reduce efectele Efedrinei. De ce?
39
Clasificare stimulate ale R alfa
- administrare sistemica: Etliefrina, Fenilefrina, Metoxamina, Midodrina, Metaraminol - administrare locala: Nafazolina Tetrizolina Oximetazolina, Xylometazolina
40
Etilefrina - mecanism - efecte - indicatii
- agonist alfa1 si 2 - creste presiunea arteriala - hTA (tratament de fond)
41
Fenilefrina - mecanism - efecte
- agonist alfa1>>>>>alfa2, in plus elibereaza NA | - creste TA, bradicardie prin reflex vagal, midriaza scurta, reduce edem nazal si conjunctival
42
Fenilefrina | -Indicatii
- rinite/conjunctivite - hTA - midriaza de diagnostic - tahicardii paroxistice supraventriculare - se asociaza cu anestezice locale - DIAGNOSTICUL SDR CBH
43
Fenilefrina - efecte adverse - contraindicatii
- tahifilaxie, cresterea TA, tahicardie | - HTA, tahiaritmii, angina
44
Midodrine - mecanism - indicatii
- agonist alfa1 selectiv | - HTA ortostatica
45
Metoxamina - mecanism - efecte - indicatii
- agonist alfa1 selectiv - creste TA de lunga durata si bradicardie prin reflex - hTA
46
Metaraminol | -efecte
-puternic efect de crestere a TA -bradicardie reflexa -creste tonusul venos/scade fluxul sanguin renal si cerebral -vasoconstrictie pulmonara Indicatie: hTA
47
Nafazolina | -mecanism
- agonist alfa1 si 2 | - elibereaza NA
48
Nafazolina - efecte - indicatii
- reduce edemul nazal/conjunctiv | - rinite/conjunctivite
49
Nafazolina | -efecte adverse
- tahifilaxie - atrofia mucoasei nazale - copii sub 3 ani : hTA - adulti:HTA si cresterea conductivitatii in tesutul excitoconductor
50
Tetrizolina, Oximetazolina, Xylometazolina - mecanism? - indicatii?
- agonist alfa1 si 2 | - rinite nespecifice sau alergice
51
Stimulante semiselective beta1 si 2
- cu actiune semiselectiva si de scurta durata: Isoprenalina, Orciprenalina, Etilnorepinefrina - Actiune predominanta pe beta-vasculari: Bufenina, Bamethan
52
Stimulante selective beta1
Dobutamina, Prenalterol
53
Stimulante selective beta2
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
Isoprenalina - efecte - indicatii
- cronotrop/inotrop pozitiv si puternic bronhodilatator | - resuscitarea stopului din IMA cu asistola sau BAV total, astm bronsic, doar initial ca alternativa
55
Isoprenalina - efecte adverse - dezavantaje
- greata, varsaturi, cefalee, palpitatii | - durata de actiune scurta si stimulare puternica beta1 cardiaci
56
Orciprenalina - mecanism - efecte - indicatii
- mai mult pe beta2 decat beta1 - puternic bronhodilatator, slab crono/inotrop pozitiv - astm
57
Bufenina si Bamethan - mecanism - efecte - indicatii
- agonist beta1 si 2 - puternic bronhodilatator si vasodilatator - claudicatie intermitenta, sindrom Raynaud
58
Dobutamina | -efecte
- inotrop pozitiv accentuat - prezinta tahifilaxie - poate induce aritmii - reduce edemul mucoaselor
59
Dobutamina - mecanism - indicatii
- agonist beta1 | - soc cardiogen, insuf cardiaca congestiva
60
Prenalterol - mecanism - indicatii
- agonist beta1 | - unele forme de IC
61
Stimulante selective beta2 | -efecte
- 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
Stimulante selective beta2 | -efecte adverse
- tremor - anxietate, nervozitate, agitatie, cefalee - palpitatii - hiperpotasemie
63
Alti eliebratori de catecolamine, exemple
Hidroxi/met/amfetamina, Fenmetrazina, Pemolin, Fenilpropanolamina, Metilfenidat, MDMA, Amantadina
64
Alti eliebratori de catecolamine | -efecte SNC
- efecte psihoanaleptice si anorexigene, determina dependenta - stimuleaza SRAA - inhiba MAO - inhiba recaptarea de catecolamine
65
Alti eliebratori de catecolamine | -efecte periferice
- cresterea TA | - inotrop/cronotrop/dromotrop pozitiv
66
Alti eliebratori de catecolamine | -efecte adverse
- greata varsaturi constipatie/diaree - HTA, tahiartimtii, cefalee - psihoze endogene - dependenta - tulburari ale gandirii
67
Alti eliebratori de catecolamine | -contraindicatii
- psihoze - Tourette - HTA, tahiaritmii - leziuni ateroatoase coronariene - glaucom
68
Amfetamina | -indicatii
- narcolepsie - sindrom hiperkinetic - enurezis - adjuvant in parkinson - adjuvant in crizele de epilepsie petit mal - stimularea performantelor psihomotorii
69
Fenmetrazina | -indicatie
-anorexigen
70
Hidroxiamfetamina | -indicatie
-sindrom Horner cu leziune preggl
71
Ecstasy-efecte
-euforie, halucinatii, comportament stereotipic
72
Amantadina | -mecanisme
- 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
Amantadina | -indicatii
- antiviral | - boala parkinson
74
Cocaina | -efecte farmacodinamice
- midriaza, tahiaritmii, cresteri tensionale - perforatie de sept nazal - dependenta puternica si rapida
75
Cocaina - mecanism - utilizari
- inhiba recaptarea noradrenalinei | - nemedical: efect euforizant/ medical: anestezic local de suprafata in ORL/oftalmo
76
Tiramina - mecanism - efecte
-blocarea recaptarii NA -eliberarea NA -efecte similare cu NA Rezulta din metabolismul normal al tirozinei rapid metabolizata prin MAO
77
inhibitori ai dopa-decarboxilazei
Benserazida, Carbidopa
78
inhibitori MAO-B
Selegiline, Rasagiline, Lazabemide, Mofegiline
79
inhibitori COMT
Tolcapone, Nitecapone, Entacapone
80
Agonisti ai R-dopaminergici
- Ergopeptine: Bromocriptina, Lisuride, Pergolide | - Deriv neergopeptinici: Piribedil, Ropinirole, Apomorfina
81
inhibitori neselectivi ai MAO
Hidrazine: Fenelzina, Isocarboxazid Nehidrazine: Tranycypromine, Dextroamfetamina
82
inhibitori selectivi ai MAO
Moclobemide, Brofaromine, Toloxatone

Farmacologie (10 decks)

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