1.subst anest Flashcards by Epsi M

Structura anest locale

aminoesteri sau amide

radical aromatic (comp anionica H^-) confera caracter lipofil = traverseaza membr axonala pt act directa

gr. aminica tertiara (comp cationica B⁺) - blocheaza transmiterea sinaptica neuronala
- real. mediul alcalin=> fav. puterea anest

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alfa1 glicoprot (AGP)

transporta si subst medicamentoase:

Beta-blocante (propanolol)

Blocante de Ca (verapamil)

Antiaritmice (chinidina)

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Lidocaina(xilina) = acetamida

pH=6,5

cu vasoconstr pH=3,5

conservant=metilparaben sau metabisulfit de Na (la cele cu adrenalina)

efect = 2x procaina

instalare = 2-5 min

durata = 20-45 min

toxic=2x procaina

ef vasodilatator < procaina ;

>mepi / prilo

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Lidocaina - farmacocinetica si metabolism

se leaga de prot.plasm 70%

trece bariera hemato-encefalica difuziune pasiva

metabolizare hep 90%; restul - elim renala

per ½ = 90 min (se poate dubla/tripla in afect hep)

manif sistemice lidocaina nelegata>6μg/ml

acidoza influent mom aparitiei ef sistemice

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Lidocaina - adm

xilina 2%= 20mg clorhidrat de lidocaina in 1,8 ml sol

asoc cu adrenalina 1:100.000 - 0,01 mg clorhidrat de adrenalina

doza uzuala= 20-100mg lidocaina, 1-5ml sol 2%

doza max xilina 2% simpla=3,2 mg/kg-corp; max 400mg = 10 fiole de 2 ml

doza max xilina 2% cu adrenalina 1:100.000=7mg/kg-corp, max 400mg/zi

copii> 4ani- doza max= 2-7mg/kg-corp

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Lidocaina - C.I. precautii

hipersensibilitatea anest amidice

Semne Neurotoxicitate centrala:

agitatie, anxietate, ameteala
tinitus, tulb de vedere, tremuraturi
stari depresive, somnolente

Cu precautie la pac cu afect hep.severe

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Lidocaina-la gravide

ef teratogen- cls B

temporizare adm in I trimestru (organogeneza)

rar hipotens sarcina la adm in trim III

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Lidocaina-la gravide

ef teratogen- cls B

temporizare adm in I trimestru (organogeneza)

rar hipotens sarcina la adm in trim III

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Lidocaina - interact medicamentoase

IMAO (antidepresive triciclice) => HTA severa persistenta

Fenotiazinele, butirofenonele - reduc/anuleaza ef vasoconstr. al adren

medicatia vasopresoare(pt. hipotens de cauza obstreticala) si medicatia ocitocica ergotaminica- pot induce HTA persistenta sau AVC

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Lidocaina - R.adverse si supradozaj

Manif SNC=excitate-inhibitie corticala

ameteala

caldura, confuzie, convulsii

euforie

frig, fotofobie, greata

nervozitate, parestezii

somnolenta, stop cardio-resp, stare de inconstienta

tinitus, tremuraturi

vedere dubla, voma

Somnolenta=semn de nivel plasm >>

Manif cardiovasc= cardiodepresor cu bradicardie, hipotens;

in cazuri severe: colaps si stop

Manif alergice=rare; urticarie, edem, r.anafilactoide

Atit ter - oxigenoterapie

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Mepivacaina = amidica

in EU- sol 3% fara vasoconstr

In SUA- sol 2% cu adren 1:100.000

rar sol 2% cu 36µg noradren sau cu 1:20.000 neocorbefrin

Nu este disponibila pt anest topica

potenta medie= 2 (fata de procaina)

toxic=1,5-2 x procaina

instalare=2-3 min

durata=20-40min la niv pulpei (20-plexala, 40-tronculara perif)

45-90min- la niv p.moi

ef. vasodilatator slab

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Mepivacaina - farmacocinetica si metabolism

ef vasodilatator redus

ag.vasoconstr nu prelungesc durata anest.

se absoarbe rapid si aproape complet

se leaga 60-78% de prot plasm

metabolizare lenta si completa prin demetilare la niv hepatic

per ½=2-3 ore (adult),

8-9 ore (copil mic)

eliminare in ~ 30 ore

traverseaza usor bariera hemato-encefalica si feto-placentara

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Mepivacaina - farmacocinetica si metabolism

ag.vasoconstr nu prelungesc durata anest.

se leaga 60-70% de prot plasm

metabolizare lenta si completa prin demetilare la niv hepatic

per ½=2-3 ore(adult), 8-9 ore(copilmic)

eliminare in ~ 30 ore

traverseaza usor bariera hemato-encefalica si feto-placentara

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Mepivacaina - adm

mepi 3% = 30 mg clorhidrat de mepivacaina in 1 ml sol

dz max = 4mg/kg-corp, MAX 300mg = 5,5 carpule

copii>4 ani cu G=20kg -

dz max=3mg/kgcorp (0,1 ml/kgcorp)

doza terapeutica max = ½ doza max acceptata

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Mepivacaina - C.I.(in ritm) si precautii

hipersensibilitate tip amidic

risc de aritmii la pac sub anest gen.

risc de neurotixicitate centrala

CI = blocuri de ram gr II/III; bradicardie severa

insuf cardiaca severa

hipotens art. severa

epilepsie necontrolata

Prudenta=insuf hep, insuf renala, angina pectorala, tulb de coag, hipoxie, hiperkaliemie, acidoza, anteced de hipertermie maligna

poate influenta capac de a conduce vehicule (se va evita 4-6ore)

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Mepivacaina - la gravide

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ef teratogen cls.C

Nu se va fol in I trimestru

(decat daca beneficiu>>Risc deoarece 30% trece bar.feto plac)

Mepivacaina - interact medicm

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precautie la adm concomitenta cu Aprindina - Antiaritmic cls I (struct chim ~ Mepi)

↑ Risc hemoragic : antitrombotice, anticoag, AINS

Mepivacaina - R.adverse si supradozaj

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Manif SNC= agitatie, cefalee, logoree, nervozitate, tremor, nistagmus

Manif cardiovasc=ef inotrop (-) si hipotens; doze mari=>bloc atrio-ventr, bradicardie, aritmii ventr, vasodilatatie, colaps

Manif resp= tahipnee, urmata de apnee

Manif alergice: f rare; eruptii cutanate, prurit, edem; r.anafilact

Atit ter= clinostatism, 112, oxigenoterapie; convulsii- diazepam 10-20mg i.m.

Articaina

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are gr.amidica si gr.esterica

Indicata doar loco-reg pt stoma

Nu e disponibila pt anest topica

sol 4% disponibila doar cu adrenalina

potenta=4-5 (fata de procaina); (2 fata de lidocaina)

toxic=1-1,5 x procaina

instalare=2-3 min

durata= 45 min pt 1:200.000

75 min pt 1:100.000

ARTICAINA - farmacocinetica si met.

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peak plasm la 30min de la inj.

per ½ = 100-110 min

se leaga 90% de prot plasm

este hidroliz rapid de colinesterazele plasm, restul met hep

elim in 12-24 ore renal 95% metaboliti; 2-5% nemetaboliz

Articaina - adm

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carpule = 1.7ml

1 ml sol clorhidrat de articaina 4% cu adrenalina 1:200.000= 40 mg articaina si 0,005 mg adrenalina

1: 100.000- 40 mg articaina si 0,01 mg adrenalina
dz. max=7mg/kg corp, MAX 500mg = 7 carpule

CI - copii< 4ani

dz max=7mg/kg corp - copii>4ani cu G>20kg

Articaina - CI si precautii

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hipersensibilitate

CI: bronhospasm in antec

deficit de colinesteraza

bloc AV gr.II/III

bradicardie marcata

insuf cardiaca congestiva acuta

hipotens severa

porfirie acuta rec.

epilepsie fara trat

glaucom cu unghi inch

hipertiroidism netratat

aritmii grave(tahicardie paroxist)

I.m. recent 3-6 luni

bypass coronarian rec 3 luni

feocromocitom

Articaina - la gravide

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ef teratogen - cls C

trece bariera feto-placentara (chiar daca se leaga 95%)

Se evita in I trimestru

Medicamente care intensifica ef. simpaticomimetic al vasoconstr

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antidepresivele triciclice (Imira,Amitrip)

IMAO nespecifici (Fenel,Tranilc)

si specifici A (Clor, Moclo)

specifici B (Sele)

Articaina Precautie la Medicm Simpaticolitice

Guanetidina ( antihipertensiv de rezerva)- Ismelin

Risc ↑ T.A. articaina cu urm medicm:

β blocante (Propranolol, Pindolol, Timolol, Sotalol, Carteolol) ## Footnote **aritmii-halotan**

Articaina - R.adverse si supradozaj

Manif SNC=frecvent ameteli, cefalee, parestezii. doze mari=initial excitatie psihomotorie- agitatie,nervozitate,stupor pana la pierderea constientei, coma, spasme musc, convulsii Manif cardio-vasc=tahicardie, bradicardie, hipotens, insuf cardiaca, soc. Manif resp: tahipnee urmata de bradipnee si apoi apnee Manif gastro-int=greata, varsaturi Manif alergice=f rara; rash, prurit, urticarie; r.anafilact la astmatici=\>wheezing sau criza astm Ef adverse tardive= necroza locala; tulb sens pe tr nerv(se remit in 8 sapt); methemoglobinemie ( cei cu methem..subclinica) Atit ter- clinostatism, diazepam 10-20 mg i.m. oxigen (in spasme/convulsii) in hipotens/tahicar/bradi - clinosta - trendelemburg- adm adrenalina 0,25-1 ml i.m. (0,025-0,1 mg adrenalina)

Prilocaina - amino-amidic

folosita in SUA ef \< asupra cardiovasc risc \< methemoglobinemie ef teratogen cls C dz max=6 mg/kgcorp, max 400mg Citanest - prilocaina 3% cu felipresina

Bupivacaina - amino amidic

fol in anest epidurala si uneori BMF instalare=2-10 min durata=90 min akinezie multe ore **_cardiotoxic \>\>, SNC toxic_** ef teratogen - cls C dz max=9-18 mg pt BMF- sol 0,5% cu sau fara adren Marcaine, Sensorcaine, Vivacaine

Ag vasoconstr

adrenalina noradrenalina felipresina levonordefrinul fenilefrina

Dezavantaje noradrenalina

vasoconstr periferica intensa bradicardie (reflex compensator vag) HTA marcata vasoconstr la locul inj \< risc/beneficiu=9 \>adren

Secr catecolamine endogene

in repaus = 7 µg/min in stres= 280 µg/min inj.anest ↑secr catecol endo de 2x neinstalarea anest ↑ 50x

Inj intravasc 0,015 mg xilina

↑ ritm cardiac ↑ TA sistolice cu 50 mmHG extrasistole ventr

Dz max adrenalina

0,2mg/sedinta 0,002mg/kg-corp = 200µg/kg-corp max 7 carpule (1:100.000/1:200.000) 0,0005mg/kg-corp= 0,04mg/sedinta - afect cardio necontrolate- max 3,5 carpule ( 1:200.000)

Catecolamine - CI si precautii

peak plasm=10-20 min Adren: ↑ TA sistolina si tahicardie rasp local exagerat - pac cu HTA sau vasculopatii perif aritmii - in anest gen se evita in I trimestru; la diabetici, bronhospasm in antec; alergici; astmatici NU se adm in trim III - risc declansare travaliu ef.teratogen cls C

Levonordefrin

non-catecolaminic adjuvant pt Mepi 3% potenta 15% (1/6-fata de adren) stimulare directa rec α si β ef stimulator SNC, cord \< adren ef tox ~ dar intens in doze mari=\>HTA, tahicardie ventr, crize anginoase - la pac coronarieni doza max 1mg/sedinta 1:20.000

Felipresina

noncatecol analog ADH/vasopresina risc redus pt cardiovasc; tox\< CI la gravide; la cei cu risc hemoragic\>\> asoc cu prilocaina 3% dilutie 0,03 UI Japonia, Germania dz max =0,27 UI/sedinta (9ml sol 0,03 UI)

Fenilefrina

agonist α1 selectiv; β1 neglijabil cel mai stabil cel mai slab vasocontr din stoma 5% din potenta adren durata \> adren in comb cu prilo 4% dilutie 1:2500 dz max=4mg/sedinta (10 ml sol ) dz max =1,6mg la cardiovasc ef tox \<\< cefalee; rar aritmii ventr

1.subst anest Flashcards

(38 cards)