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SEDATIVE-HIPNOTICE. Clasificare: Sedative hipnotice barbiturice Sedative hipnotice nebarbiturice. SEDATIVE HIPNOTICE BARBITURICE Acizi slabi, derivati ai acidului barbituric/tiobarbituric; Farmacocinetica: Barbituricele liposolubile; Barbituricele < liposolubile;

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slide2
Clasificare:
  • Sedative hipnotice barbiturice
  • Sedative hipnotice nebarbiturice
slide3
SEDATIVE HIPNOTICE BARBITURICE

Acizi slabi, derivati ai acidului barbituric/tiobarbituric;

Farmacocinetica:

  • Barbituricele liposolubile;
  • Barbituricele < liposolubile;
  • Metabolizarea: hepatica → metaboliti inactivi
slide4
Actiune farmacodinamica:

1. Sedative (doze mici);

2. Hipnotice (doze mari);

3. Narcotice: Tiopental (i.v.);

4. Anticonvulsivante: Fenobarbital;

5. Inductor enzimatic: Fenobarbital.

slide7
Utilizari terapeutice.
  • stari de hiperexcitabilitate, tireotoxicoza;
  • insomnii: - Ciclobarbitalul

- Fenobarbitalul

  • epilepsie: - Fenobarbitalul
slide8
Principii de administrare:
  • doza minima eficace;
  • administrare intermitenta;
  • durata administrarii: maximum 4 saptamani;
  • nu se intrerupe brusc tratamentul:

risc de revenire (rebound) a insomniei.

slide10
Efecte adverse:
  • agitatie psihomotorie (la batrani);
  • obisnuinta si dependenta;
  • intoxicatia acuta (supradozaj).

Tratamentul intoxicatiei acute:

- spalatura gastrica;

- Manitol, alcalinizante (perfuzie i.v.);

- respiratie asistata.

slide11
Barbiturice. Contraindicatii:

- porfirie;

- insuficienta respiratorie severa;

- soferi;

- sindrom depresiv;

- sarcina.

slide12
II. SEDATIVE HIPNOTICE NEBARBITURICE

DERIVATI DE BENZODIAZEPINA

slide13
Actiune farmacodinamica:

- anxiolitica

- sedativa-hipnotica;

- miorelaxanta;

- anticonvulsivanta.

Utilizari terapeutice:

- insomnie anxioasa.

slide14
ZOLPIDEM si ZOPICLONA

Actiune farmacodinamica:

- sedativa;

- hipnotica;

- anxiolitica;

- anticonvulsivanta (Zopiclona);

- miorelaxanta.

Utilizari terapeutice: insomnii

slide15
Zolpidem si Zopiclona

Efecte adverse:

- Zopiclona: gust amar si metalic;

- toleranta si dependenta, nesemnificative.

Administrare: 1 cpr seara

slide17
Clasificare:
  • Derivati de benzodiazepina:

DIAZEPAM, CLORDIAZEPOXID, OXAZEPAM,

MEDAZEPAM, LORAZEPAM, BROMAZEPAM,

CLOBAZAM, TOFISOPAM, etc….

B. Derivati de difenilmetan: HIDROXIZIN

C. Carbamati ai propandiolului: MEPROBAMAT

D. Derivat de azaspirodecandiona: BUSPIRONA

slide18
BENZODIAZEPINELE:

Farmacocinetica:

  • absorbtie buna din intestin;
  • fixare foarte buna pe proteine plasmatice;
  • difuzeaza bine in creier;
  • traverseaza placenta;
  • metabolizare hepatica → metabolit activ;
  • eliminare renala.
slide19
BENZODIAZEPINELE:

Actiune farmacodinamica:

- anxiolitica;

- sedativa;

- hipnogena;

- miorelaxanta;

- anticonvulsivanta (Diazepam);

- anestezica generala (Midazolam).

Potenteaza deprimantele SNC, alcoolul etilic → NU se asociaza !!!

slide21
BENZODIAZEPINELE:

Utilizari terapeutice:

- sindrom anxios;

- stari de neliniste, anxietate;

- contracturi musculare;

- preanestezie;

- medicatie adjuvanta.

slide23
BENZODIAZEPINE

Principii de administrare:

  • initial, doze mici;
  • in anxietate acuta: BDZ cu actiune rapida;
  • in anxietate cronica: BDZ cu efect prelungit;
  • tratamentul nu se intrupe brusc;
  • la virstnici doze reduse (Oxazepam, Lorazepam).
slide25
TRANCHILIZANTE NEBENZODIAZEPINICE

1.HIDROXIZINA

2. MEPROBAMAT

3. BUSPIRONA

slide26
BUSPIRONA

Caracteristici farmacodinamice:

  • efect anxiolitic puternic: anxiolitic selectiv;
  • efect sedativ slab;

NUeste miorelaxant/anticonvulsivant !

Administrare: oral, cpr.

slide27
TRANCHILIZANTE MAJORE

(NEUROLEPTICELE)

slide28
NEUROLEPTICELE SEDATIVE

Clasificare:

  • Neuroleptice fenotiazinice:

CLORPROMAZINA, LEVOMEPROMAZINA,

TIORIDAZINA, PERICIAZINA

2. Neuroleptice tioxantenice:

CLORPROTIXEN, CLOPENTIXOL,

FLUPENTIXOL

3. Neuroleptice butirofenonice:

FLUANISONA

slide29
NEUROLEPTICE FENOTIAZINICE

CLORPROMAZINA

Actiune farmacodinamica:

- antipsihotica;

- sedativa;

- deprima SNV;

- antivomitiva;

- hipotermizant;

- manifestari de tip extrapiramidal;

- efecte endocrine.

slide30
Clorpromazina

Mecanism de actiune:

Blocheaza:

- receptorii dopaminergici D2

- receptorii adrenergici α1 si β

- receptorii serotoninergici 5-HT2

- receptorii histaminergici H1

slide31
Clorpromazina

Utilizari terapeutice:

- psihoze;

- varsaturi;

- sughit rebel;

- preanestezie;

- stari de hiperexcitabilitate.

slide32
Clorpromazina

Efecte adverse:

- somnolenta;

- hTA ortostatica;

- manifestari extrapiramidale

Administrare: Clordelazin dj.

Plegomazin f. (i.m./i.v.)

slide33
NEUROLEPTICE TIOXANTENICE

-CLORPROTIXEN

- CLOPENTIXOL

- FLUPENTIXOLantipsihotic polivalent

slide34
NEUROLEPTICE INCISIVE

“antideficitare” sau “dezinhibitorii”

Clasificare:

  • Fenotiazine: Flufenazina
  • Tioxantene: Tiotixen
  • Butiroferone: HALOPERIDOL, Pimozid, Penfluridol
  • Diverse: Sulpirida, Tiaprida
slide35
HALOPERIDOL
  • neuroleptic incisiv cu potenta mare

Actiune farmacodinamica:

- antipsihotica marcata;

- antivomitiva puternica;

- sedativa moderata.

Utilizari terapeutice:

  • psihoze acute si cronice;
  • agitatie psiho-motorie;
  • in anesteziologie
  • varsaturi
slide36
Haloperidol

Efecte adverse:

  • manifestari extrapiramidale intense
  • hTA ortostatica;
  • tulburari de vedere;
  • hipertermie.

Administrare: cpr., f. (i.m., i.v., s.c.)

Haloperidol decanoat f. (i.m.)

slide37
Contraindicatii:

- Parkinson;

- scleroza in plagi;

- epilepsie;

- afectiuni hepatice grave;

- sarcina

- CONSUMUL DE ALCOOL !!!