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Farmacologie > CURS 3 PARASIMPATICOMIMETICE > Flashcards

CURS 3 PARASIMPATICOMIMETICE Flashcards

1
Q

Sinteza Ach

  • Unde?
  • Din ce?
  • Sub actiunea cui?
A
  • in citoplasma neuronului terminal
  • din colina si acetil-coenzima A
  • colin-acetiltransferaza (CAT)
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2
Q

Cum e transportata colina?

A

Activ cu participarea Na+

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3
Q

Cu cine se cupleaza Ach in fanta sinaptica si care-s cele 2 etape?

A

Cu AchE (acetilcolinesteraza)

  • prima etapa: complexul Ach-AchE e scindat in colina si enzima acetilata
  • a doua: enzima acetilata elibereaza acetilcolinesteraza si acetat
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4
Q

Timp de actiune Ach

A

De ordinul milisecundelor

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5
Q

Cele 2 profiluri ale Ach si cu cine se cupleaza fiecare.

A

Profil metilic ( R muscarinici) si carbonilic ( R nicotinici )

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6
Q

Ce tip de grupare are Ach in structura? + detalii

A

Grupare de tip onium ( N cu toate valentele ocupate pozitiv) + nu traverseaza bariere. Este o molecula mare si polara => nu poate fi administrata oral

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7
Q

INTERACTIUNEA ACH-R MUSCARINICI

  • Capatul cationic
  • oxigen esteric
  • hidroxil atasat C nr 3
  • grup metil atasat C nr 2
A

-zona anionica (situs de afinitate)
-grupare incarcata +
-grupare incarcata +
-regiunea hidrofoba
(ultimele 3 fac situsul de activitate )

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8
Q

Mecanism de actiune M pe cardiac, ggl vegetativi + muschi, celule glandulare

A
  • hiperpolarizare =>scade frecventa
  • depolarizare => creste peristaltismul si tonusul muscular
  • cresc ionii de Ca2+ =>hipersecretie glandulara
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9
Q

M1 - localizare, proteina G, transmitere post-R, efecte

A
  • Cortex cerebra, hipocamp, stomac, neuroni postggl
  • Gq/11
  • Activeaza IP3 si DAG
  • Functie cognitiva si memorizare, stimulare secretie gastrica acida
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10
Q

M2 - localizare, proteina G, transmitere post-R, efecte

A
  • Miocard, m. neted, SNC
  • Gi/o
  • Activeaza canalele de K+, inhiba adenilat ciclaza
  • Frecventa cardiaca, temperatura, analgezie, control motor
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11
Q

M3 - localizare, proteina G, transmitere post-R, efecte

A
  • Cel glandelor exocrine, vase, SNC
  • Gq/11
  • IP3 si DAG
  • Motilitate gastro-int, secretii glandulare, bronhoconstrictie
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12
Q

M4 - localizare, proteina G, transmitere post-R, efecte

A
  • SNC
  • Gi/o
  • Scade AMPc
  • Analgezie, poate regla eliberarea DA
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13
Q

M5 - localizare, proteina G, transmitere post-R, efecte

A
  • SNC
  • Gi/o
  • IP3 si DAG
  • Mediaza eliberarea de DA, regleaaza dilatatia vaselor cerebrale
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14
Q

INTERACTIUNEA ACH-R NICOTINICI

A
  • Legarea Ach la una/doua subunitati alfa ale R-N det o crestere moderata a nr de canale de Na+ in pozitia deschis
  • Mai multe molecule => fenomenul de stabilizare membranara =>blocarea canalelor in pozitia deschis deci oprirea influxului nervos (blocarea repolarizarii membranare )
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15
Q

Nm

A

=De placa terminala

  • La niv jonctiunii neuromusc
  • Deschiderea Na+/K+ si depolarizare
  • fasciculatii fine ale m urmata de miorelaxare
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16
Q

Nn

A

=Neuronal

  • La niv. neuronilor postggl si unele situsuri presinaptice colinergice
  • Deschiderea Na+/K+ si depolarizare
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17
Q

Ach- efecte farmacodinamice la nivel cardio vascular

A

-inotrop, dromotrop, cronotrop negativ (M2)

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18
Q

Ach- efecte farmacodinamice la nivelul musculaturii netede

A
  • glob ocular:mioza si contractia m. ciliar
  • digestiv: efect prokinetic si tonus crescut
  • bronsic: bronhoconstrictie
  • genito-urinar: contractia detrusorului
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19
Q

Ach- efecte farmacodinamice la nivel glandular + exemple de glande exocrine

A
  • hipersecretie

- lacrimale, sebacee, sudoripare, pancreatice, bronsice, salivare, gastro-intestinale

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20
Q

Ach- efecte farmacodinamice la nivel MSR

A

-stimuleaza secretia de A/NA

21
Q

Efecte adverse parasimpaticomimetice

A
  • hipersalivatie/ transpiratii abundente
  • greata/varsaturi
  • dureri abdominale/diaree
  • bronhispasm
  • scaderea TA
22
Q

Contraindicatii parasimpaticomimetice

A
  • astm bronsic/BPOC
  • hipertiroidie
  • epilepsie
  • leziuni ateromatoase stenozante coronariene severe
  • ulcer peptic
23
Q

AGONISTI NESELECTIVI AI R M SI N (Actiune directa)

-Exemple esteri sintetici ai colinei

A

Metacolina, Carbacol, Betanecol

24
Q

AGONISTI NESELECTIVI AI R M SI N (Actiune directa)

-Exemple alcaloizi cu actiune semiselectiva pe M

A

Pilocarpina
Muscarina
Arecolina

25
Q

AGONISTI NESELECTIVI AI R M SI N (Actiune directa)

-Exemple alcaloizi cu actiune semiselectiva pe N

A

Lobelina
Nicotina
Difenilmetilpiperazinium

26
Q

AGONISTI SLECTIVI AI R. M (Actiune directa)

A
  • M1: Xanomeline, Cevimeline
  • M2: Oxotremorine
  • M3: Aceclidine
27
Q

Indicatii Ach

A
  • Oftalmo: prevenirea cresterii prestiunii intraoculare postoperator
  • Cardio: detectarea spasmului coronarian in angina pectorala
28
Q

Indicatii Carbacol

A

Glaucom

29
Q

Indicatii betanecol

A
  • glaucom acut sau cronic

- pareze postoperatorii ale tubului digestiv

30
Q

Indicatii Pilocarpina

A
  • glaucom
  • Xerostomie (de ex in Sdr Sjogren)
  • Antidot in intoxicatia acuta cu Atropina
31
Q

Indicatii Xanomeline, Cevimeline, Aceclidina

A

Xerostomie

32
Q

Parasimpaticomimetic NATURAL cu actiune indirecta

A

Fisostigmina

33
Q

Exemple inhibitori reversibili ai AchE

A 
Edrofonium
Neostigmina
Piridostigmina
Distigmina
Clorura de ambenoniu (NU este hidrolizata de colinesteraze)
Demecarium
Tacrine
Donepezil
Rivastigmine
34
Q

Exemple organofosforate medicamente

A

Ecotiofat

Metrifonat

35
Q

Exemple organofosforate insecticide

A

Paration

Malation

36
Q

Exemple organofosforate gaze toxice

A

Sarin
Tabun
Soman

37
Q

Indicatii Fisostigmina

A
  • glaucom

- Alzheimer (cat exista neuroni colinergici)

38
Q

Indicatii Edrofonium

A
  • Diagnostic miastenia gravis

- Detectare terapie inadecvante cu alte anticolinesterazice

39
Q

Indicatii Neostigmina

A
  • Miastenia gravis
  • ileus paralitic, retentie urinara
  • decurarizare
  • intoxicatie acuta cu atropina
40
Q

Indicatii Piridostigmina

A
  • Miastenia gravis
  • Ileus paralitic. retentie urinara
  • decurarizare
41
Q

Indicatii Distigmina

A
  • Miastenia gravis

- ileus paralitic, retentie urinara

42
Q

Indicatii Clorura de ambenoniu

A

miastenia gravis

43
Q

Indicatii demecarium

A

glaucom

44
Q

Tratament Alzheimer

A

tacrine
donepezil
rivastigmine
galantamina

45
Q

Indicatii Ecotiofat

A

glaucom

46
Q

Indicatii metrifonat

A

antihelmintic

47
Q

Simptomatologie intoxicatie cu organofosforate

A

grata, varsaturi, dureri abdominale colicative, mioza, incontinenta vezicala,, hipersecretie bronsica si edem pulmonar, hipersecretie lacrimala si salivara, fasciculatii musculare, tahicardie, cresteri de tensiune, anxietate, tremor, confuzie, convulsii

48
Q

Antidot intoxicatie cu organofosforate

A
  • Atropina
  • Pralidoxima si Obidoxima (reactivatoare de colinesteraza, inainte de etapa de imbatranire cand legaturile sunt inca scindabile)
  • colinesteraza umana purificata

Farmacologie (10 decks)

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