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farmaco > curs 3 > Flashcards

curs 3 Flashcards

1
Q

unde sunt sintetizati si depozitati neurotransmitatorii

A

sintetizati- terminatii axonale buton presinaptic
depozitati- vezicule sinaptice

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2
Q

ce se intampla in mom declansarii unui impuls nv

A
  1. depolarizare mb presinaptica
  2. deschidere canale Ca
  3. creste conc Ca intracelul
  4. activare calmodulina care activ o proteinkinaza calciu/ calmodulin dependenta
  5. fosforilare proteine asociate cu vezicule depozit ex sinaptotagmina
  6. initiere proces alipire vezicule de mb presinapt
  7. eliberare neurotransmitator in fanta sinaptica
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3
Q

cum se elibereaza neurotransmitator in fanta sinaptica

A

prin exocitoza/ difuziune

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4
Q

ce se intampla dupa eliberare neurotransmitator in fanta sinaptica

A
  1. declansare RC specific- inhibitor/ excitator
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5
Q

cum se face inactivarea neurotransmitatorului eliberat in fanta sinaptica

A
  • recaptare in term presinaptica cu depozitare in vezicule sinaptice= metabolizare intraneuronala
  • metabolizare in fanta sinaptica
  • difuziune extrasinaptica
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6
Q

prin ce componenta difera SN vegetativ de SN somatic

A

componenta eferenta
2 neuroni legati prin sinapse ganglionare in afara SNC

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7
Q

componenta eferenta din SN somatic?

A

fibre eferente cu orig in SNC
inerveaza cel musc striate printr o sinapsa periferica neuromusculara

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8
Q

origine fibre nv preggl sistem simpatic

A

radacini ventrale corpi neuronali T1-L3

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9
Q

origine fibre nv preggl sistem parasimpatic

A

nuclei nv cranieni 3, 7, 9, 10
neuroni mv spinala S2-S4

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10
Q

structura acetilcolina

A

ester hidrosolubil al acid acetic si colina
- struct cuaternara de amoniu

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11
Q

unde este sintetizata Ach

A

buton neuronal presinaptic colinergic

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12
Q

cum se sintetizeaza Ach

A

sub influenta:
- colinacetiltransferaza din colina
- acid acetic din acetil coA mitocondriala

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13
Q

unde se depoziteaza Ach

A

vezicule terminatii colinergice presinaptice

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14
Q

enzime care hidrolizeaza Ach

A

SPECIFIC:
- acetilcolinesteraza
NESPECIFIC: (actioneaza si pe alte molec cu struct esterica)
- pseudocolinesteraza
- butirilcolinesteraza

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15
Q

ce rezulta din hidroliza Ach

A
  • acid acetic
  • colina- recaptata in buton presinaptic pt sinteza noi molec Ach
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16
Q

chimie fixare Ach pe receptori postsinaptici

A

are o:
- extremitate cationica- fixare pe sediu anionic receptor
- extremitate esterofila- fixare pe sediu esterofil receptor

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17
Q

receptorii colinergici difera in ceea ce priveste…..

A

structura sterica situs receptor

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18
Q

tipuri de receptori colinergici

A
  • muscarinici- agonist muscarina
  • nicotinici- agonist nicotina
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19
Q

ce sunt receptorii muscarinici

A

receptori in serpentina cuplati cu proteina G
- 5 tipuri care difera in fct de a 3 a ansa intracelulara

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20
Q

receptori muscarinici cu efecte stimulante

A

M1, M3, M5
* se cupleaza cu prot Gq
* fixare Ach-> stim fosfolipaza C-> activare IP3+ DAG-> cresc conc Ca2+

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21
Q

receptori muscarinici cu efecte inhibitorii

A

M2 si M4
* cuplare cu prot Gi
* fixare Ach-> scade cant de AMPc intracelular

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22
Q

localizare receptori muscarinici

A
  • in principal- sinapse PS terminale( neuroefectorii)
  • SNC
  • ggl simp+ psimp
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23
Q

struct chimica receptori nicotinici

A

canale ionice pt sodiu din 5 subunitati polipeptidice (2 pt α, 3 pt β, γ, δ)
* fiecare subunit- 4 segmente transmb
* situs receptor ach- mereu pe α=> cuplare 2 molec ach simultan pe receptor

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24
Q

tipuri receptori nicotinici

A
  • ganglonari Nn
  • musculari Nm
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25
Q

localizare recept nicotinici Nn

A
  • ggl simp+ psim
  • SNC
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26
Q

localizare recept nicotinici Nm

A

jonctiune neuromusculara
(placa motorie muschi striati)

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27
Q

ce fel de receptori muscarinici se gasesc in tub digestiv

A

M1+ M3

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28
Q

ce fel de receptori muscarinici se gasesc in gl exocrine

A

M3

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29
Q

ce fel de receptori muscarinici se afla in ochi

A

M3

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30
Q

ce receptori muscarinici se gasesc la nivel cardiovascular

A

M2 inima ig?
M3 vasculari

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31
Q

efecte Ach pe tub digestiv

A
  • fav peristaltism GI
  • creste secretii gastrice, biliare, pancreas, bila, intestin
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32
Q

ce receptori muscarinici se gasesc la nivel arbore traheobronsic

A

M3

33
Q

efecte Ach pe arbore traheobronsic

A

-bronhoconstrictie
-crestere secretie traheobronsica

34
Q

efecte Ach pe vezica biliara+ uretere

A
  • relaxare sfinctere
    -eliminare secretii biliare+ urina
35
Q

efecte Ach la niv gl exocrine

A

crestere secretie lacrimala, salivara, sudorala

36
Q

efecte Ach la nivel ocular

A
  • mioza ( contractie sfincter iris)
  • contractie m ciliar
  • bombare cristalin
  • fixare vedere pt aproape
  • scade presiune intraoculara
  • poate aparea hiperemie conjunctivala tranzitorie
37
Q

efecte Ach la nivel cardiovasc

A

mimeaza actiune nv vag:
- deprima fct cardiace
- scade frecventa
- scade excitabilitate
- scade viteza conducere atrio-ventric
- scade contractilitate

38
Q

efecte Ach la nivel vascular

A
  • vasodilatatie
  • eliberare monoxid azot cel endoteliu vasc=> crestere conc GMP ciclic intracel
39
Q

stimulare receptori Nn

A

efecte in general antagoniste- depinde de localizare?

40
Q

efect stim receptori Nn ggl psimp

A

eliberare Ach
efecte psimp

41
Q

efect stim receptori Nn din ggl simpatici

A

elib NA in sinapse simp terminale
efecte simpatice

42
Q

efecte stim receptroi Nn din gl medulosuprarenala

A

eliberare adrenalina in circulatie
efecte simpatice

43
Q

efecte stim receptori Nm

A

contractia musc striata

44
Q

unde exista si receptori muscarinici si nicotinici

A

SNC
muscarinici- M1 si M4

45
Q

efect stim colinergica SNC

A

efecte excitatorii
pot aparea convulsii la doze toxice de Ach

46
Q

tipuri de medicamente agoniste sistem colinergic

A
  • parasimpatomimetice- efect asem crestere tonus SN psimp si vag
  • nicotinice- pe Nn din ggl si SNC
47
Q

ce sunt parasimpaticomimetice indirecte

A

agonisti care actioneaza indirect
- det crestere disponibil de Ach fanta sinaptica=> stim psimp

48
Q

tipuri medicamente antagoniste sist colinergic

A
  • parasimpatolitice- muscarinici
  • ganglioplegice- Nn din ganglioni
  • curarizante
49
Q

de cate feluri pot fi curarizantele

A
  • depolarizante- agonist pe Nm- intai stim placa motorie, apoi paralizie
  • anti depolarizante- antagonist pe Nm- produc de la inceput paralizie neuromusculara
50
Q

dc Ach nu este avantajoasa ca medicament

A

actiune intensa, brutala, neselctiva si de scurta durata

51
Q

avantaje compusi sinteza Ach

A
  • absorbtie dupa adm orala
  • durata de actiune mai lunga
  • efecte predominant muscarinice
52
Q

ce compusi de sinteza ai ach se folosesc in clinica

A
  • metacolina
  • carbacol
  • betanecol
53
Q

indicatii carbacol

A

tratament glaucom- instilatii conjunctivale

54
Q

indicatii metacolina

A

vasodilatator in afectiuni vasculospastice
-cale orala

55
Q

indicatii betanecol

A

stim motilitate tub dig/ vezica urinara in atonii postop
- adm orala/ inj

56
Q

utilizare betanecol in stomatologie

A

creste secr salivara bolnavi xerostomie

57
Q

parasimpaticomimetice

A
  • metacolina
  • carbacol
  • betanecol
  • pilocarpina
  • cevimelina
58
Q

mod actiune pilocarpina

A

act pe recept M din gl exocrine si ochi

59
Q

indicatii pilocarpina

A
  • glaucom- solutie oftalmica 0,5-4%
  • xerostomie
  • antidot intoxicatie atropina
60
Q

pilocarpina ca tratament glaucom

A

sol oftalmica 0,5-4% instilatii conjunctivale
* fav drenare umoare apoasa
* scade presiune intraoc
* dezavantaj- scurta durata, aplic la 3-6 ore

61
Q

pilocarpina ca tratament xerostomie

A

adm orala 5-10 mg de 3 ori/zi
* crestere secretii parotide, submandib, subling
* putine r adverse cardiovasc
* poate determina hipersudoratie, frisoane, greata, ameteala

62
Q

actiune cevimelina

A

stim selectiv recept M1 si M3=> m putine reactii adverse decat pilocarpina
- efecte similare pilocarpina

63
Q

indicatii cevimelina

A

xerostomie
doze 30 mg de 3 ori/ zi

64
Q

la ce fel de pac trb sa ai grija cand adm parasimpatomimetice in tratament xerostomie

A

astmatici
intoleranti
tratamente care pot interactiona cu actiuni tip parasimpatomimetic

65
Q

actiune anticolinesterazice

A

inhiba acetilcolinesteraza(= enzima care degradeaza Ach)
=> efecte stim receptori muscarinici si nicotinici

66
Q

tipuri de anticolinesterazice

A

reversibile
ireversibile

67
Q

actiune anticolinesterazice reversibile

A

durata limitata actiune( 2-6 ore)
- legarea de enzima form complex lent hidrolizabil

68
Q

medicamente anticolinesterazice reversibile

A
  • ezerina (fiziostigmina)
  • neostigmina
  • tacrina
  • donepezil
69
Q

utilizari ezerina

A

local, intraocular pt glaucom

70
Q

utilizari neostigmina

A

stim musc neteda G-I su vezicala in:
- atonii digestive+ vezicale postop

stim musc striata
- miastenia gravis

antidot intoxicatii cu subst blocante placa motorie ( curarizante antidepolarizante)

71
Q

indicatii tacrina si donepezil

A

tratament Alzheimer
-patrund in SNC si cresc nivel Ach sinapse

72
Q

mod actiune anticolinesterazice ireversibile

A

form leg covalenta cu acetilcolinesteraza=> inactivare un timp ft lung, chiar sute de ore
disparitie efect- prin sinteza molecule noi Ach

73
Q

anticolinesterazice ireversibile

A

compusi organofosforici
- insecticide- paration, malation
- gaze toxice lupta- tabun, sarin, soman

74
Q

intoxicatie acuta cu organofosforice

A
  • acumulare excesiva Ach
  • efecte muscarinice+ colinergice intense= CRIZA COLINERGICA
  • liposolub mare-> absorbtie rapida aproape completa pe orice cale de adm
75
Q

simtpome intoxicatie organofosforice

A
  • hipersudoratie, hipersalivatie, hiperlacrimatie
  • bronhoree
  • greturi, varsaturi, diaree, colivi
  • hipotensiune cu bradicardie
  • mioza
  • fasciculatii musculare, chiar convulsii care pot evolua spre paralizie musc striata
  • confuzie mintala pana la coma
76
Q

tratament intoxicatie cu organofosforice

A

atropina in doze ft mari
- inj iv de 2 mg odata la 5-10 min pana la aparitie midriaza

  • adm de reactivatori colinesteraza- oxime
  • spalare tegumente, indepartare haine, spalaturi gastrice
  • aspiratie traheobronsica
  • respiratie asistata
  • tratament simptomatic cu anticonvulsivante, sedative
77
Q

reactivatori de colinesteraza

A

OXIME
- pralidoxima
- obidoxima

78
Q

ce sunt parasimpaticolitice

A

antagonisti competitivi receptori muscarinici

79
Q
A

farmaco (27 decks)

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