SEDACION EN PACIENTES CON ERC Francisco José de la Prada Alvarez Servicio de Nefrología Hospital...

SEDACION EN PACIENTES SEDACION EN PACIENTES CON ERCCON ERC

Francisco José de la Prada AlvarezFrancisco José de la Prada Alvarez

Servicio de NefrologíaServicio de Nefrología

Hospital Universitario Son DuretaHospital Universitario Son Dureta

Ansiedad.Ansiedad.

DolorDolor

DelirioDelirio

DisneaDisnea

ParálisisParálisis

FármacoFármaco SedaciónSedación HiponósisHiponósis AmnesiaAmnesia AnalgesiaAnalgesia

Benzodia-Benzodia-cepinascepinas

++ ++ ++ --

HaloperidolHaloperidol ++ +*+* +*+* --

KetaminaKetamina -- -- ++ ++

OpioidesOpioides -- -- -- ++

PropofolPropofol +**+** ++ +*+* --

*mínimo efecto*mínimo efecto

**solo a bajas dosis**solo a bajas dosis

Analgésicos:Analgésicos:– Fentanilo.Fentanilo.– Hidromorphina.Hidromorphina.– Sulfato de morfina.Sulfato de morfina.

Anestésicos:Anestésicos:– Ketamina.Ketamina.– Propofol.Propofol.

Neurolépticos:Neurolépticos:– Haloperidol.Haloperidol.

Sedantes-Hipnóticos:Sedantes-Hipnóticos:– Benzodiacepinas:Benzodiacepinas:

DiacepamDiacepam

LorazepamLorazepam

MidazolamMidazolam

– Barbitúricos:Barbitúricos:TiopentalTiopental

MethohexitalMethohexital

Jacobi, J, Fraser, GL, Coursin, DB, et al. Clinical practice guidelines for the sustained use of sedatives and analgesics in the critically ill adult. Crit Care Med 2002; 30:119

BenzodiacepinasBenzodiacepinas

Mecanismo de acción:Mecanismo de acción:– Unión a receptores específicos del complejo del receptor de Unión a receptores específicos del complejo del receptor de

GABA en el SNC, favoreciendo la unión y el efecto de este GABA en el SNC, favoreciendo la unión y el efecto de este neurotransmisor inhibitorio de la excitabilidad neuronal. neurotransmisor inhibitorio de la excitabilidad neuronal. (incrementa la permeabilidad al Cl de la membrana neuronal, (incrementa la permeabilidad al Cl de la membrana neuronal, hiperpolarizando la membrana, estabilizandola y haciéndola hiperpolarizando la membrana, estabilizandola y haciéndola menos excitable.menos excitable.

Acciones:Acciones:– Sedantes a bajas dosis.Sedantes a bajas dosis.– A altas dosis: A altas dosis:

AnticonvulsivantesAnticonvulsivantesSedantes.Sedantes.Amnésicos.Amnésicos.Depresores cardio y respiratorio.Depresores cardio y respiratorio.

Principal problema: Principal problema: – Tolerancia.Tolerancia.

BenzodiacepinasBenzodiacepinas

Todos tienen la misma eficacia a dosis Todos tienen la misma eficacia a dosis equipotentes. Las diferencias dependen de la equipotentes. Las diferencias dependen de la afinidad por el receptor, lipofilia y la cinética de afinidad por el receptor, lipofilia y la cinética de eliminación.eliminación.Afinidad:Afinidad:– Lorazepam: mayor afinidad y mayor potenciaLorazepam: mayor afinidad y mayor potencia– Midazolam y Diazepam: menos afinidad y potenciaMidazolam y Diazepam: menos afinidad y potencia

Lipofilia:Lipofilia:– Midazolam y Diazepam: los más lipofílicos (pasan Midazolam y Diazepam: los más lipofílicos (pasan

BHE, rápido inicio de acción, acumulación en los BHE, rápido inicio de acción, acumulación en los tejidos grasos)tejidos grasos)

Cinética de eliminación:Cinética de eliminación:

BenzodiacepinasBenzodiacepinasDiazepamDiazepam Reducción oxidativa (Se Reducción oxidativa (Se

afecta por edad, afecta por edad, disfunción hepática e disfunción hepática e interacciones interacciones farmacológicas)farmacológicas)

Gran volumen de distribución.Gran volumen de distribución.

Bajo metabolismo hepático.Bajo metabolismo hepático.

Metabolitos activos (diametildiazepam Metabolitos activos (diametildiazepam y oxazepam) que se elimina via renal.y oxazepam) que se elimina via renal.

Propilenglicol Propilenglicol (hiperosmolaridad y (hiperosmolaridad y acidosis metabólica con osmol gap acidosis metabólica con osmol gap elevado)elevado)

MidazolamMidazolam Reducción oxidativa (Se Reducción oxidativa (Se afecta por edad, afecta por edad, disfunción hepática e disfunción hepática e interacciones interacciones farmacológicas)farmacológicas)

Corta vida media. Corta vida media.

Gran volumen de distribuciónGran volumen de distribución

Metabolito activo (alfa-Metabolito activo (alfa-hidroximidazolam)hidroximidazolam)

LorazepamLorazepam GlucoroconjugaciónGlucoroconjugación Bajo metabolismo hepático.Bajo metabolismo hepático.

Metabolitos inactivos.Metabolitos inactivos.

Propilenglicol (hiperosmolaridad y Propilenglicol (hiperosmolaridad y acidosis metabólica con osmol gap acidosis metabólica con osmol gap elevado).elevado).

Se afecta por la ERC.Se afecta por la ERC.

N03AE-Benzodiacepinas

NOMBRE GENÉRICO

PRESENTACIÓN VÍA NOMBRE COMERCIAL

Clobazam Comp 10 mgComp 20 mg

OROR

Noiafren

Clonazepam Amp 1 mg/2 mlComp 0,5 mgComp 2 mgGts 2,5 mg/ml (1)

IM, IVOROROR

Rivotril

Diazepam Amp 10 mg/2 mlComp 5 mgComp 10 mg Microenema 5 mg

IM, IV

REC

Valium, Diazepam Stesolid

Nota 1: 1 gota=0,1 mg

DiazepamDiazepamDOSING: ADULTSDOSING: ADULTS — Note: — Note: Oral absorption is more reliable than I.M.Oral absorption is more reliable than I.M.Anticonvulsant (acute treatment): Rectal gel: 0.2 mg/kg. Note: Dosage Anticonvulsant (acute treatment): Rectal gel: 0.2 mg/kg. Note: Dosage should be rounded upward to the next available dose, 2.5, 5, 7.5, 10, 12.5, should be rounded upward to the next available dose, 2.5, 5, 7.5, 10, 12.5, 15, 17.5, and 20 mg/dose; dose may be repeated in 4-12 hours if needed; 15, 17.5, and 20 mg/dose; dose may be repeated in 4-12 hours if needed; do not use for more than 5 episodes per month or more than one episode do not use for more than 5 episodes per month or more than one episode every 5 days.every 5 days.Anxiety/sedation/skeletal muscle relaxation:– Oral: 2-10 mg 2-4 times/day

– I.M., I.V.: 2-10 mg, may repeat in 3-4 hours if needed

Sedation in the ICU patient: I.V.: 0.03-0.1 mg/kg every 30 minutes to 6 Sedation in the ICU patient: I.V.: 0.03-0.1 mg/kg every 30 minutes to 6 hourshoursStatus epilepticus: I.V.: 5-10 mg every 10-20 minutes, up to 30 mg in an 8-Status epilepticus: I.V.: 5-10 mg every 10-20 minutes, up to 30 mg in an 8-hour period; may repeat in 2-4 hours if necessaryhour period; may repeat in 2-4 hours if necessaryRapid tranquilization of agitated patient (administer every 30-60 minutes): Oral: 5-10 mg; average total dose for tranquilization: 20-60 mg

DiazepamDiazepamDOSING: PEDIATRICDOSING: PEDIATRIC Conscious sedation for procedures:Conscious sedation for procedures: Oral: Oral: Children: 0.2-0.3 mg/kg (maximum dose: 10 mg) 45-60 minutes prior to procedure Children: 0.2-0.3 mg/kg (maximum dose: 10 mg) 45-60 minutes prior to procedure Adolescents: 10 mg Adolescents: 10 mg I.V.: Adolescents: 5 mg; may repeat with 2.5 mg if needed I.V.: Adolescents: 5 mg; may repeat with 2.5 mg if neededFebrile seizure prophylaxis: Oral: Children: 1 mg/kg/day divided every 8 hours; initiate therapy at first sign of fever Febrile seizure prophylaxis: Oral: Children: 1 mg/kg/day divided every 8 hours; initiate therapy at first sign of fever and continue for 24 hours after fever is goneand continue for 24 hours after fever is goneSedation or muscle relaxation or anxiety:Sedation or muscle relaxation or anxiety: Oral: Children: 0.12-0.8 mg/kg/day in divided doses every 6-8 hours Oral: Children: 0.12-0.8 mg/kg/day in divided doses every 6-8 hours I.M., I.V.: Children: 0.04-0.3 mg/kg/dose every 2-4 hours to a maximum of 0.6 mg/kg within an 8-hour period if I.M., I.V.: Children: 0.04-0.3 mg/kg/dose every 2-4 hours to a maximum of 0.6 mg/kg within an 8-hour period if neededneededStatus epilepticus:Status epilepticus: I.V.: I.V.: Infants >30 days and Children <5 years: 0.05-0.3 mg/kg/dose given over 3-5 minutes, every 15-30 minutes to a Infants >30 days and Children <5 years: 0.05-0.3 mg/kg/dose given over 3-5 minutes, every 15-30 minutes to a maximum total dose of 5 mg or 0.2-0.5 mg/dose every 2-5 minutes to a maximum total dose of 5 mg; repeat in 2-maximum total dose of 5 mg or 0.2-0.5 mg/dose every 2-5 minutes to a maximum total dose of 5 mg; repeat in 2-4 hours as needed4 hours as needed Children 5 years: 0.05-0.3 mg/kg/dose given over 3-5 minutes, every 15-30 minutes to a maximum total dose of Children 5 years: 0.05-0.3 mg/kg/dose given over 3-5 minutes, every 15-30 minutes to a maximum total dose of 10 mg or 1 mg/dose every 2-5 minutes to a maximum of 10 mg; repeat in 2-4 hours as needed10 mg or 1 mg/dose every 2-5 minutes to a maximum of 10 mg; repeat in 2-4 hours as needed Rectal: 0.5 mg/kg/dose then 0.25 mg/kg/dose in 10 minutes if needed (prepare dose using parenteral Rectal: 0.5 mg/kg/dose then 0.25 mg/kg/dose in 10 minutes if needed (prepare dose using parenteral formulation)formulation)Anticonvulsant (acute treatment): Rectal gel:Anticonvulsant (acute treatment): Rectal gel: Children <2 years: Safety and efficacy have not been studied Children <2 years: Safety and efficacy have not been studied Children 2-5 years: 0.5 mg/kg Children 2-5 years: 0.5 mg/kg Children 6-11 years: 0.3 mg/kg Children 6-11 years: 0.3 mg/kg Children 12 years: Refer to adult dosing. Children 12 years: Refer to adult dosing. Note: Dosage should be rounded upward to the next available dose, 2.5, 5, 7.5, 10, 12.5, 15, 17.5, and 20 Note: Dosage should be rounded upward to the next available dose, 2.5, 5, 7.5, 10, 12.5, 15, 17.5, and 20 mg/dose; dose may be repeated in 4-12 hours if needed; do not use for more than 5 episodes per month or more mg/dose; dose may be repeated in 4-12 hours if needed; do not use for more than 5 episodes per month or more than one episode every 5 days.than one episode every 5 days.Muscle spasm associated with tetanus: I.V., I.M.:Muscle spasm associated with tetanus: I.V., I.M.: Infants >30 days: 1-2 mg/dose every 3-4 hours as needed Infants >30 days: 1-2 mg/dose every 3-4 hours as needed Children 5 years: 5-10 mg/dose every 3-4 hours as needed Children 5 years: 5-10 mg/dose every 3-4 hours as needed

DiazepamDiazepam

DOSING: ELDERLYDOSING: ELDERLY– Oral absorption is more reliable than I.M..Oral absorption is more reliable than I.M..

Oral: Oral: – Initial:Initial:– Anxiety: 1-2 mg 1-2 times/day; increase gradually Anxiety: 1-2 mg 1-2 times/day; increase gradually

as needed, rarely need to use >10 mg/day.as needed, rarely need to use >10 mg/day.

– Skeletal muscle relaxant: 2-5 mg 2-4 times/daySkeletal muscle relaxant: 2-5 mg 2-4 times/day

Rectal gel: Due to the increased half-life in Rectal gel: Due to the increased half-life in elderly and debilitated patients, elderly and debilitated patients, consider consider reducing dose.reducing dose.

DiazepamDiazepamPHARMACODYNAMICS / KINETICSPHARMACODYNAMICS / KINETICS I.VI.V.: Status epilepticus:.: Status epilepticus: Onset of action: Almost immediateOnset of action: Almost immediate Duration: 20-30 minutes Duration: 20-30 minutes

Absorption: Oral: 85% to 100%, more reliable than I.M.Absorption: Oral: 85% to 100%, more reliable than I.M.Food: Food: Diazepam serum levels may be increased if taken with food.Diazepam serum levels may be increased if taken with food. Diazepam effect/toxicity may be increased by grapefruit juice; avoid Diazepam effect/toxicity may be increased by grapefruit juice; avoid concurrent use.concurrent use.

Protein binding: 98%.Protein binding: 98%.

Metabolism: Hepatic.Metabolism: Hepatic.Half-life elimination: Half-life elimination: – Parent drug: Adults: Parent drug: Adults: 20-50 hours20-50 hours;;– increased half-life in neonates, elderly, and those with severe hepatic increased half-life in neonates, elderly, and those with severe hepatic

disorders; disorders; – Active major metabolite (desmethyldiazepam): 50-100 hoursActive major metabolite (desmethyldiazepam): 50-100 hours; may be ; may be

prolonged in neonatesprolonged in neonates

DiazepamDiazepam

Rango terapéutico:Rango terapéutico: – Diazepam: 0.2-1.5 mcg/mL Diazepam: 0.2-1.5 mcg/mL

(SI: 0.7-5.3 µmol/L); (SI: 0.7-5.3 µmol/L);

– N-desmethyldiazepam (nordiazepam): 0.1-0.5 N-desmethyldiazepam (nordiazepam): 0.1-0.5 mcg/mL mcg/mL

(SI: 0.35-1.8 µmol/L)(SI: 0.35-1.8 µmol/L)

DiazepamDiazepam

Sobredosis:Sobredosis:– SintomasSintomas: somnolencia, confusion, coma, : somnolencia, confusion, coma,

reflejos hipotónicos, disnea, hipotension, reflejos hipotónicos, disnea, hipotension, alteración de la coordinación. alteración de la coordinación.

– Tratamiento de soporteTratamiento de soporte. Rara vez se requiere . Rara vez se requiere ventilación mecánica.ventilación mecánica.

– Flumazenil (AnexateFlumazenil (Anexate): bloquea ): bloquea selectivamenten la unión de la selectivamenten la unión de la benzodiacepinas a los receptores del SNC, benzodiacepinas a los receptores del SNC, revirtiendo la depresión del SNC, revirtiendo la depresión del SNC, pero no la pero no la depresión respiratoria.depresión respiratoria.

DiazepamDiazepam

Embarazo:Embarazo: – Teratogenico.Teratogenico.– Atraviesa la placenta. Atraviesa la placenta. – Se han descrito hipotonía, hipotermia, Se han descrito hipotonía, hipotermia,

sintomas de abstinencia dificultad respiratoria sintomas de abstinencia dificultad respiratoria y para la alimentación en neonatos cuyas y para la alimentación en neonatos cuyas madres toman BZDP.madres toman BZDP.

Contraindicados en la lactancia.Contraindicados en la lactancia.

BenzodiacepinasBenzodiacepinasDosis de carga

Dosis de mantenimiento

FG > 50 ml/min

FG 10-50 ml/min

FG < 10 ml/min

Dosis suplemtaria tras HD

DPCA TSCR

Diaze-pam

5-20 5-20 mg IV mg IV bolusbolus

5-20 5-20 mg/2-4 mg/2-4 horas IVhoras IV

100%100% 100%100% 100%100% NingunaNinguna DesconDesconocidaocida

100%100%

Loraze-pam

1-4 mg 1-4 mg IV IV bolusbolus

0,5-10 0,5-10 mg/hora mg/hora IVIV

100%100% 100%100% 100%100% NingunaNinguna DesconoDesconocidacida

Dosis Dosis FG 10-FG 10-50 50 ml/minml/min

Midazo-lam


2-5 2-5 mg/hora mg/hora IVIV

100%100% 100%100% 50%50% No No aplicableaplicable

No No aplicableaplicable

No No aplicableaplicable

DiazepamDiazepam

INYECCION IV: SIINYECCION IV: SI– Administrar en venas de gran calibre o bien a través del equipo de Administrar en venas de gran calibre o bien a través del equipo de

suerosuero. . En general la ampolla debe administrarse directamente, sin En general la ampolla debe administrarse directamente, sin diluir y muy lentamente (*). diluir y muy lentamente (*). Se recomienda no sobrepasar la Se recomienda no sobrepasar la velocidad de 5 mg por minuto en adultos; en niños debe administrarse velocidad de 5 mg por minuto en adultos; en niños debe administrarse en al menos 3 minutosen al menos 3 minutos. La administración demasiado rápida puede . La administración demasiado rápida puede causar hipotensión y depresión respiratoria severa. causar hipotensión y depresión respiratoria severa.

– (*) (*) En caso de diluir la ampolla debe realizarse en una En caso de diluir la ampolla debe realizarse en una proporción de 1 proporción de 1 ml de Valium y 1 ml de agua p.i. o SF. ml de Valium y 1 ml de agua p.i. o SF. (Si diluimos en proporciones (Si diluimos en proporciones más altas, ejemplo la ampolla de 2 ml de Valium en 10 ml-50 ml de SF, más altas, ejemplo la ampolla de 2 ml de Valium en 10 ml-50 ml de SF, se produce precipitación: La jeringa tiene un aspecto turbio y lechoso y se produce precipitación: La jeringa tiene un aspecto turbio y lechoso y no es recomendable administrarla).no es recomendable administrarla).

INFUSION INTERMITENTEINFUSION INTERMITENTE:: SI SI– Una ampolla de 2 ml debe diluirse en Una ampolla de 2 ml debe diluirse en al menos 50-100 ml de SF óal menos 50-100 ml de SF ó

SG5%SG5% y administrar en 15-30 minutos. y administrar en 15-30 minutos. INFUSION CONTINUA: NO RECOMENDADOINFUSION CONTINUA: NO RECOMENDADO– Disponemos de pocos datos sobre esta vía de administración, aunque Disponemos de pocos datos sobre esta vía de administración, aunque

puede estar indicada cuando se pautan dosis altas y continuas de puede estar indicada cuando se pautan dosis altas y continuas de Diazepam (Ej.: Tétanos).Diazepam (Ej.: Tétanos).

DiazepamDiazepam

INYECCION IMINYECCION IM:: SI SI– Inyección intramuscular profunda. Inyección intramuscular profunda. La absorción es La absorción es

lenta y algo errática,lenta y algo errática, por lo que se recomienda pasar por lo que se recomienda pasar a la vía oral siempre que sea posible.a la vía oral siempre que sea posible.

SUEROS COMPATIBLESSUEROS COMPATIBLES: SF, SG5%.: SF, SG5%.

OBSERVACIONESOBSERVACIONES: : – Evitar extravasación o administración intraarterial. Evitar extravasación o administración intraarterial. – Diazepam se une a algunos componentes de los Diazepam se une a algunos componentes de los

plásticos del material usado en su administración y plásticos del material usado en su administración y no no es recomendable guardarlo preparado en jeringas.es recomendable guardarlo preparado en jeringas.

N03AE-Benzodiacepinas

NOMBRE GENÉRICO


Clobazam Comp 10 mgComp 20 mg

OROR

Noiafren

Clonazepam Amp 1 mg/2 mlComp 0,5 mgComp 2 mgGts 2,5 mg/ml (1)

IM, IVOROROR

Rivotril

Diazepam Amp 10 mg/2 mlComp 5 mgComp 10 mg Microenema 5 mg

IM, IV

REC

Valium, Diazepam

Stesolid

Nota 1: 1 gota=0,1 mg

N05C-Hipnóticos y sedantes

NOMBRE GENÉRICO


Clometiazol (1) Caps 192 mg OR Distraneurine

Flurazepam (2) Caps 30 mg OR Dormodor

Hidrato de cloral Jbe 50 mg/mlEnema 100 mg/ml

ORREC

Hidrato de Cloral FM

Lorazepam (3) Comp 1 mg OR Orfidal

Lormetazepam Comp 2 mg OR Loramet , Noctamid

Midazolam Amp 15 mg/3 ml IM,IV Dormicum

Zolpidem (4) Comp 10 mg OR Stilnox

Nota 2: Flunitrazepam (Rohipnol ) se considera equivalente terapéutico de Flurazepam. Nota 3: Bromazepam (Lexatin) se considera equivalente terapéutico de Lorazepam. Nota 4: Zopiclona (Limovan) y Midazolam comp (Dormicum comp ) se consideran equivalentes terapéuticos del Zolpidem. Consultar programa de equivalencias.

MidazolamMidazolamDOSING: ADULTSDOSING: ADULTS La dosis debe ser individualizada segun la edad del paciente, las patologías La dosis debe ser individualizada segun la edad del paciente, las patologías subyacentes y las medicaciones concurrentes. Debe reducirse la dosis un subyacentes y las medicaciones concurrentes. Debe reducirse la dosis un 30% si se administran ´narcóticos u otros depresores del SNC. Debe haber 30% si se administran ´narcóticos u otros depresores del SNC. Debe haber disponible equipo de resucitación respiratoria.disponible equipo de resucitación respiratoria.

Conscious sedationConscious sedation: : I.V.: Initial: 0.5-2 mg slow I.V. over at least 2 minutes; I.V.: Initial: 0.5-2 mg slow I.V. over at least 2 minutes; slowly titrate to effect by repeating doses every 2-3 minutes if needed; usual slowly titrate to effect by repeating doses every 2-3 minutes if needed; usual total dose: 2.5-5 mg; use decreased doses in elderly.total dose: 2.5-5 mg; use decreased doses in elderly. Initial: Some patients respond to doses as low as 1 mg; no more than 2.5 Initial: Some patients respond to doses as low as 1 mg; no more than 2.5 mg should be administered over a period of 2 minutes. Additional doses of mg should be administered over a period of 2 minutes. Additional doses of midazolam may be administered after a 2-minute waiting period and midazolam may be administered after a 2-minute waiting period and evaluation of sedation after each dose increment. evaluation of sedation after each dose increment. A total dose >5 mg is A total dose >5 mg is generally not needed.generally not needed. If narcotics or other CNS depressants are If narcotics or other CNS depressants are administered concomitantly, the midazolam dose should be reduced by administered concomitantly, the midazolam dose should be reduced by 30%. 30%. Maintenance: 25% of dose used to reach sedative effect Maintenance: 25% of dose used to reach sedative effect

MidazolamMidazolamDOSIS: ADULTOSDOSIS: ADULTOS

Preoperative sedation:Preoperative sedation: I.M.: 0.07-0.08 mg/kg 30-60 minutes prior to surgery/procedure; usual dose: 5 mg; I.M.: 0.07-0.08 mg/kg 30-60 minutes prior to surgery/procedure; usual dose: 5 mg; Note: Reduce dose in patients with COPD, high-risk patients, patients 60 years of Note: Reduce dose in patients with COPD, high-risk patients, patients 60 years of age, and patients receiving other narcotics or CNS depressantsage, and patients receiving other narcotics or CNS depressants I.V.: 0.02-0.04 mg/kg; repeat every 5 minutes as needed to desired effect or up to I.V.: 0.02-0.04 mg/kg; repeat every 5 minutes as needed to desired effect or up to 0.1-0.2 mg/kg0.1-0.2 mg/kg Intranasal (not an approved route): 0.2 mg/kg (up to 0.4 mg/kg in some studies); Intranasal (not an approved route): 0.2 mg/kg (up to 0.4 mg/kg in some studies); administer 30-45 minutes prior to surgery/procedureadminister 30-45 minutes prior to surgery/procedure

Anesthesia: I.V.:Anesthesia: I.V.: Induction: Induction: Unpremedicated patients: 0.3-0.35 mg/kg (up to 0.6 mg/kg in resistant cases) Unpremedicated patients: 0.3-0.35 mg/kg (up to 0.6 mg/kg in resistant cases) Premedicated patients: 0.15-0.35 mg/kg Premedicated patients: 0.15-0.35 mg/kg Maintenance: 0.05-0.3 mg/kg as needed, or continuous infusion 0.25-1.5 Maintenance: 0.05-0.3 mg/kg as needed, or continuous infusion 0.25-1.5 mcg/kg/minutemcg/kg/minute

Sedation in mechanically-ventilated patients: I.V. continuous infusion: 100 mg in 250 Sedation in mechanically-ventilated patients: I.V. continuous infusion: 100 mg in 250 mL D5W or NS (if patient is fluid-restricted, may concentrate up to a maximum of 0.5 mL D5W or NS (if patient is fluid-restricted, may concentrate up to a maximum of 0.5 mg/mL); initial dose: 0.02-0.08 mg/kg (~1 mg to 5 mg in 70 kg adult) initially and mg/mL); initial dose: 0.02-0.08 mg/kg (~1 mg to 5 mg in 70 kg adult) initially and either repeated at 5-15 minute intervals until adequate sedation is achieved or either repeated at 5-15 minute intervals until adequate sedation is achieved or continuous infusion rates of 0.04-0.2 mg/kg/hour and titrate to reach desired level of continuous infusion rates of 0.04-0.2 mg/kg/hour and titrate to reach desired level of sedationsedation

MidazolamMidazolam

ANCIANOS.ANCIANOS. – La dosis debe ser individualizada segun la edad del paciente, La dosis debe ser individualizada segun la edad del paciente,

las patologías subyacentes y las medicaciones concurrentes.las patologías subyacentes y las medicaciones concurrentes.– Debe reducirse la dosis un 30% si se administran narcóticos u Debe reducirse la dosis un 30% si se administran narcóticos u

otros depresores del SNC. otros depresores del SNC. – Debe haber disponible equipo de resucitación respiratoria.Debe haber disponible equipo de resucitación respiratoria.

I.V.: Conscious sedation: I.V.: Conscious sedation: – Initial: Initial: 0.5 mg slow I.V.; give no more than 1.5 mg in a 2-minute 0.5 mg slow I.V.; give no more than 1.5 mg in a 2-minute

period.period. – If additional titration is needed, give no more than 1 mg over 2 If additional titration is needed, give no more than 1 mg over 2

minutes, waiting another 2 or more minutes to evaluate sedative minutes, waiting another 2 or more minutes to evaluate sedative effect. effect.

– A total dose >3.5 mg is rarely necessary.A total dose >3.5 mg is rarely necessary.

MidazolamMidazolamDOSING: PEDIATRICDOSING: PEDIATRIC Notes: The dose of midazolam needs to be individualized based on the patient's age, underlying diseases, and Notes: The dose of midazolam needs to be individualized based on the patient's age, underlying diseases, and concurrent medications. Decrease dose (by ~30%) if narcotics or other CNS depressants are administered concurrent medications. Decrease dose (by ~30%) if narcotics or other CNS depressants are administered concomitantly. Personnel and equipment needed for standard respiratory resuscitation should be immediately concomitantly. Personnel and equipment needed for standard respiratory resuscitation should be immediately available during midazolam administration. Children <6 years may require higher doses and closer monitoring available during midazolam administration. Children <6 years may require higher doses and closer monitoring than older children; calculate dose on ideal body weightthan older children; calculate dose on ideal body weightConscious sedation for procedures or preoperative sedation:Conscious sedation for procedures or preoperative sedation: Oral: 0.25-0.5 mg/kg as a single dose preprocedure, up to a maximum of 20 mg; administer 30-40 minutes prior Oral: 0.25-0.5 mg/kg as a single dose preprocedure, up to a maximum of 20 mg; administer 30-40 minutes prior to procedure. Children <6 years, or less cooperative patients may require as much as 1 mg/kg as a single dose; to procedure. Children <6 years, or less cooperative patients may require as much as 1 mg/kg as a single dose; 0.25 mg/kg may suffice for children 6-16 years of age.0.25 mg/kg may suffice for children 6-16 years of age. Intranasal (not an approved route): 0.2 mg/kg (up to 0.4 mg/kg in some studies), administered 30-45 minutes Intranasal (not an approved route): 0.2 mg/kg (up to 0.4 mg/kg in some studies), administered 30-45 minutes prior to procedureprior to procedure I.M.: 0.1-0.15 mg/kg 30-60 minutes before surgery or procedure; range 0.05-0.15 mg/kg; doses up to 0.5 mg/kg I.M.: 0.1-0.15 mg/kg 30-60 minutes before surgery or procedure; range 0.05-0.15 mg/kg; doses up to 0.5 mg/kg have been used in more anxious patients; maximum total dose: 10 mghave been used in more anxious patients; maximum total dose: 10 mg I.V.: I.V.: Infants <6 months: Limited information is available in nonintubated infants; dosing recommendations not clear; Infants <6 months: Limited information is available in nonintubated infants; dosing recommendations not clear; infants <6 months are at higher risk for airway obstruction and hypoventilation; titrate dose in small increments to infants <6 months are at higher risk for airway obstruction and hypoventilation; titrate dose in small increments to desired effect; monitor carefullydesired effect; monitor carefully Infants 6 months to Children 5 years: Initial: 0.05-0.1 mg/kg; titrate dose carefully; total dose of 0.6 mg/kg may Infants 6 months to Children 5 years: Initial: 0.05-0.1 mg/kg; titrate dose carefully; total dose of 0.6 mg/kg may be required; usual maximum total dose: 6 mgbe required; usual maximum total dose: 6 mg Children 6-12 years: Initial: 0.025-0.05 mg/kg; titrate dose carefully; total doses of 0.4 mg/kg may be required; Children 6-12 years: Initial: 0.025-0.05 mg/kg; titrate dose carefully; total doses of 0.4 mg/kg may be required; usual maximum total dose: 10 mgusual maximum total dose: 10 mg Children 12-16 years: Dose as adults; usual maximum total dose: 10 mg Children 12-16 years: Dose as adults; usual maximum total dose: 10 mgConscious sedation during mechanical ventilation: I.V.: Children: Loading dose: 0.05-0.2 mg/kg, followed by initial Conscious sedation during mechanical ventilation: I.V.: Children: Loading dose: 0.05-0.2 mg/kg, followed by initial continuous infusion: 1-2 mcg/kg/minute; titrate to the desired effect; usual range: 0.4-6 mcg/kg/minutecontinuous infusion: 1-2 mcg/kg/minute; titrate to the desired effect; usual range: 0.4-6 mcg/kg/minuteStatus epilepticus refractory to standard therapy (unlabeled use): I.V.: Infants >2 months and Children: Loading Status epilepticus refractory to standard therapy (unlabeled use): I.V.: Infants >2 months and Children: Loading dose: 0.15 mg/kg followed by a continuous infusion of 1 mcg/kg/minute; titrate dose upward every 5 minutes until dose: 0.15 mg/kg followed by a continuous infusion of 1 mcg/kg/minute; titrate dose upward every 5 minutes until clinical seizure activity is controlled; mean infusion rate required in 24 children was 2.3 mcg/kg/minute with a clinical seizure activity is controlled; mean infusion rate required in 24 children was 2.3 mcg/kg/minute with a range of 1-18 mcg/kg/minute.range of 1-18 mcg/kg/minute.

MidazolamMidazolam

ADVERSE REACTIONS SIGNIFICANTADVERSE REACTIONS SIGNIFICANT — —>10%: Respiratory: Decreased tidal volume and/or respiratory rate >10%: Respiratory: Decreased tidal volume and/or respiratory rate decrease, apnea (3% children)decrease, apnea (3% children)1% to 10%:1% to 10%: Cardiovascular: Cardiovascular: HypotensionHypotension (3% children) (3% children) Central nervous system: Drowsiness (1%), Central nervous system: Drowsiness (1%), oversedationoversedation, , headache (1%), seizure-like activity (1% children)headache (1%), seizure-like activity (1% children) Gastrointestinal: Nausea (3%), vomiting (3%) Gastrointestinal: Nausea (3%), vomiting (3%) Local: Pain and local reactions at injection site (4% I.M., 5% I.V.; Local: Pain and local reactions at injection site (4% I.M., 5% I.V.; severity less than diazepam)severity less than diazepam) Ocular: Nystagmus (1% children) Ocular: Nystagmus (1% children) Respiratory: Cough (1%) Respiratory: Cough (1%) Miscellaneous: Physical and psychological dependence with Miscellaneous: Physical and psychological dependence with prolonged use, hiccups (4%, 1% children), paradoxical reaction (2% prolonged use, hiccups (4%, 1% children), paradoxical reaction (2% children)children)<1% (Limited to important or life-threatening): Agitation, amnesia, <1% (Limited to important or life-threatening): Agitation, amnesia, bigeminy, bronchospasm, emergence delirium, euphoria, bigeminy, bronchospasm, emergence delirium, euphoria, hallucinations, laryngospasm, rashhallucinations, laryngospasm, rash

MidazolamMidazolam

CONTRAINDICATIONS.CONTRAINDICATIONS.HypersensitivityHypersensitivity to midazolam or any component to midazolam or any component of the formulation, including benzyl alcohol of the formulation, including benzyl alcohol (cross-sensitivity with other benzodiazepines (cross-sensitivity with other benzodiazepines may exist); may exist); parenteral form is not for parenteral form is not for intrathecal or epidural intrathecal or epidural injection; injection; narrow-angle glaucoma; narrow-angle glaucoma; concurrent use of potent inhibitors of CYP3A4 concurrent use of potent inhibitors of CYP3A4 (amprenavir, atazanavir, or ritonavir);(amprenavir, atazanavir, or ritonavir); pregnancypregnancy

MidazolamMidazolamDRUG INTERACTIONSDRUG INTERACTIONS — Substrate of CYP2B6 (minor), 3A4 (major); Inhibits — Substrate of CYP2B6 (minor), 3A4 (major); Inhibits CYP2C8 (weak), 2C9 (weak), 3A4 (weak)CYP2C8 (weak), 2C9 (weak), 3A4 (weak)CNS depressantsCNS depressants: Sedative effects and/or respiratory depression may be additive : Sedative effects and/or respiratory depression may be additive with CNS depressants; includes ethanol, barbiturates, narcotic analgesics, and other with CNS depressants; includes ethanol, barbiturates, narcotic analgesics, and other sedative agents; monitor for increased effect. If narcotics or other CNS depressants sedative agents; monitor for increased effect. If narcotics or other CNS depressants are administered concomitantly, the midazolam dose should be reduced by 30% if are administered concomitantly, the midazolam dose should be reduced by 30% if <65 years of age, or by at least 50% if >65 years of age.<65 years of age, or by at least 50% if >65 years of age.CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of midazolam. CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of midazolam. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.phenobarbital, phenytoin, and rifamycins.CYP3A4 inhibitors: May increase the levels/effects of midazolam. Example inhibitors CYP3A4 inhibitors: May increase the levels/effects of midazolam. Example inhibitors include azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, include azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, telithromycin, and verapamil.telithromycin, and verapamil.Levodopa: Therapeutic effects may be diminished in some patients following the Levodopa: Therapeutic effects may be diminished in some patients following the addition of a benzodiazepine; limited/inconsistent dataaddition of a benzodiazepine; limited/inconsistent dataOral contraceptives: May decrease the clearance of some benzodiazepines (those Oral contraceptives: May decrease the clearance of some benzodiazepines (those which undergo oxidative metabolism); monitor for increased benzodiazepine effectwhich undergo oxidative metabolism); monitor for increased benzodiazepine effectSaquinavir: A 56% reduction in clearance and a doubling of midazolam's half-life Saquinavir: A 56% reduction in clearance and a doubling of midazolam's half-life were seen with concurrent administration with saquinavir.were seen with concurrent administration with saquinavir.Theophylline: May partially antagonize some of the effects of benzodiazepines; Theophylline: May partially antagonize some of the effects of benzodiazepines; monitor for decreased response; may require higher doses for sedationmonitor for decreased response; may require higher doses for sedation

MidazolamMidazolam

EMBARAZO.EMBARAZO.– Contraindicado.Contraindicado.

LACTANCIA.LACTANCIA.– ContraindicadoContraindicado

MidazolamMidazolam

Sobredosis:Sobredosis:– SintomasSintomas: depresion respiratoria, hipotension, : depresion respiratoria, hipotension,

coma, estupor, confusion y apneacoma, estupor, confusion y apnea– Tratamiento de soporteTratamiento de soporte. Rara vez se requiere . Rara vez se requiere

ventilación mecánica.ventilación mecánica.– Flumazenil (AnexateFlumazenil (Anexate): bloquea ): bloquea

selectivamenten la unión de la selectivamenten la unión de la benzodiacepinas a los receptores del SNC; benzodiacepinas a los receptores del SNC; puede no revertirse la reaccion respiratoria a puede no revertirse la reaccion respiratoria a la hipoxia.la hipoxia.

MidazolamMidazolam

PHARMACODYNAMICS / KINETICSPHARMACODYNAMICS / KINETICS Onset of action: I.M.: Sedation: ~15 minutes; I.V.: 1-5 minutesOnset of action: I.M.: Sedation: ~15 minutes; I.V.: 1-5 minutesPeak effect: I.M.: 0.5-1 hourPeak effect: I.M.: 0.5-1 hourDuration: I.M.: Up to 6 hours; Mean: 2 hoursDuration: I.M.: Up to 6 hours; Mean: 2 hours

Distribution: Distribution: VdVd: 0.8-2.5 L/kg; increased with congestive heart failure : 0.8-2.5 L/kg; increased with congestive heart failure (CHF) and (CHF) and chronic renal failurechronic renal failure

Protein binding: 95%Protein binding: 95%Metabolism: Extensively hepatic via CYP3A4Metabolism: Extensively hepatic via CYP3A4Bioavailability: Mean: 45%Bioavailability: Mean: 45%

Half-life elimination: 1-4 hours; prolonged with cirrhosis, congestive Half-life elimination: 1-4 hours; prolonged with cirrhosis, congestive heart failure, obesity, and elderlyheart failure, obesity, and elderlyExcretion: Urine (as glucuronide conjugated metabolites); feces Excretion: Urine (as glucuronide conjugated metabolites); feces (~2% to 10%)(~2% to 10%)

MidazolamMidazolam

Proteger de la luz. Conservar entre 15 y 30 ºCProteger de la luz. Conservar entre 15 y 30 ºC

INYECCION IV DIRECTAINYECCION IV DIRECTA:: SI SI– Administrar en forma de inyección IV lentaAdministrar en forma de inyección IV lenta. Esta vía de administración . Esta vía de administración

se utiliza en la sedación anterior al inicio de la intervención diagnostica se utiliza en la sedación anterior al inicio de la intervención diagnostica o quirúrgica administrando 5-10 minutos antes una dosis de 0,05 mg/kg. o quirúrgica administrando 5-10 minutos antes una dosis de 0,05 mg/kg. La dosis de mantenimiento es un 25% de la dosis inicial. En la La dosis de mantenimiento es un 25% de la dosis inicial. En la inducción a la anestesia, también se inyecta por vía IV lenta en 20-30 inducción a la anestesia, también se inyecta por vía IV lenta en 20-30 segundos y la dosis habitual es de 0,3 mg/kg de peso.segundos y la dosis habitual es de 0,3 mg/kg de peso.

INFUSION INTERMITENTE: NO RECOMENDABLEINFUSION INTERMITENTE: NO RECOMENDABLE– No se recomienda el uso de esta vía para las indicaciones terapéuticas No se recomienda el uso de esta vía para las indicaciones terapéuticas

del Midazolam.del Midazolam.

INFUSION CONTINUA: NO RECOMENDABLEINFUSION CONTINUA: NO RECOMENDABLE– No se recomienda el uso de esta vía para las indicaciones terapéuticas No se recomienda el uso de esta vía para las indicaciones terapéuticas

del Midazolam.del Midazolam.

MidazolamMidazolam

INYECCION IMINYECCION IM:: SI SI– Administrar en forma de inyección IM profunda en una zona de gran Administrar en forma de inyección IM profunda en una zona de gran

masa muscularmasa muscular. Esta vía de administración se utiliza en la . Esta vía de administración se utiliza en la sedación sedación preoperatoriapreoperatoria. La dosis suele ser de 0,07-0,1 mg/kg administrada 30-60 . La dosis suele ser de 0,07-0,1 mg/kg administrada 30-60 minutos antes de la intervención.minutos antes de la intervención.

SUEROS COMPATIBLESSUEROS COMPATIBLES: SF, SG5%: SF, SG5%

Las soluciones de 1 ampolla en 500 ml son estables a temperatura Las soluciones de 1 ampolla en 500 ml son estables a temperatura ambiente 24 horas. ambiente 24 horas.

OBSERVACIONESOBSERVACIONES::– La solución de la ampolla de midazolam es estable hasta un máximo de La solución de la ampolla de midazolam es estable hasta un máximo de

1 hora a temperatura ambiente cuando se mezcla en la misma jeringa 1 hora a temperatura ambiente cuando se mezcla en la misma jeringa con: Atropina sulfato, Escopolamina bromhidrato, Morfina sulfato o con: Atropina sulfato, Escopolamina bromhidrato, Morfina sulfato o Meperidina.Meperidina.

– Injection: Injection: Sodium content of 1 mL: 0.14 mEq Sodium content of 1 mL: 0.14 mEq

BenzodiacepinasBenzodiacepinasDosis de carga

Dosis de mantenimiento

FG > 50 ml/min

FG 10-50 ml/min

FG < 10 ml/min

Dosis suplemtaria tras HD

DPCA TSCR

Diaze-pam

5-20 5-20 mg IV mg IV bolusbolus

5-20 5-20 mg/2-4 mg/2-4 horashoras


100%100%

Loraze-pam


0,5-10 0,5-10 mg/horamg/hora


Dosis Dosis FG 10-FG 10-50 50 ml/minml/min

Midazo-lam


2-5 2-5 mg/horamg/hora

100%100% 100%100% 50%50% DesconDesconocidaocida

DesconDesconocidaocida

DesconDesconocidaocida

N05C-Hipnóticos y sedantes

NOMBRE GENÉRICO


Clometiazol (1) Caps 192 mg OR Distraneurine

Flurazepam (2) Caps 30 mg OR Dormodor

Hidrato de cloral Jbe 50 mg/mlEnema 100 mg/ml

ORREC

Hidrato de Cloral FM

Lorazepam (3) Comp 1 mg OR Orfidal

Lormetazepam Comp 2 mg OR Loramet , Noctamid

Midazolam Amp 15 mg/3 ml IM,IV Dormicum

Zolpidem (4) Comp 10 mg OR Stilnox

Nota 2: Flunitrazepam (Rohipnol ) se considera equivalente terapéutico de Flurazepam. Nota 3: Bromazepam (Lexatin) se considera equivalente terapéutico de Lorazepam. Nota 4: Zopiclona (Limovan) y Midazolam comp (Dormicum comp ) se consideran equivalentes terapéuticos del Zolpidem. Consultar programa de equivalencias.

OpioidesOpioides

Todos tienen similares propiedades analgésicas Todos tienen similares propiedades analgésicas y sedantes en dosis equipotentes.y sedantes en dosis equipotentes.Carecen de efectos amnésicos.Carecen de efectos amnésicos.Su principal problema es la Su principal problema es la tolerancia.tolerancia.Pueden usarse:Pueden usarse:– Sulfato de morfina.Sulfato de morfina.– Fentanilo.Fentanilo.– Hidromorphona.Hidromorphona.

Alfentanilo y sulfentanilo no aportan ventajas Alfentanilo y sulfentanilo no aportan ventajas (salvo su vida media ultracorta) y son más (salvo su vida media ultracorta) y son más caros.caros.

NeurolepticosNeurolepticos

Su principal indicación es el Su principal indicación es el Delirio. Delirio. Haloperidol:Haloperidol:– Potente acción neuroleptica.Potente acción neuroleptica.– Mínima actividad anticolinérgica.Mínima actividad anticolinérgica.

Mecanismo de acción:Mecanismo de acción:– Butirofenona. Antipsicótica.Butirofenona. Antipsicótica.– Bloquea los receptores dopaminérgicos D1 y D2 mesolímbicos Bloquea los receptores dopaminérgicos D1 y D2 mesolímbicos

en el cerebro.en el cerebro.– Disminuye la libreación de hormonas hipotalámicas e Disminuye la libreación de hormonas hipotalámicas e

hipofisiariashipofisiarias– Parece que deprime el sistema reticular activador ascendente Parece que deprime el sistema reticular activador ascendente

afectando al metabolismo basal, la temperatura corporal el tono afectando al metabolismo basal, la temperatura corporal el tono vasomotor y la emesis.vasomotor y la emesis.

N05AD-Butirofenonas

NOMBRE GENÉRICO


Haloperidol Amp 5 mg/1 mlGts 2 mg/ml (2)Comp 10 mg

IMOROR

Haloperidol

(2): 1 gota=0,1 mg.

HaloperidolHaloperidolDOSING: ADULTSDOSING: ADULTS Psychosis:Psychosis: Oral: 0.5-5 mg 2-3 times/day; usual maximum: 30 mg/day Oral: 0.5-5 mg 2-3 times/day; usual maximum: 30 mg/day I.M. (as lactate): 2-5 mg every 4-8 hours as needed I.M. (as lactate): 2-5 mg every 4-8 hours as needed I.M. (as decanoate): Initial: 10-20 times the daily oral dose administered at I.M. (as decanoate): Initial: 10-20 times the daily oral dose administered at 4-week intervals. Maintenance dose: 10-15 times initial oral dose; used to 4-week intervals. Maintenance dose: 10-15 times initial oral dose; used to stabilize psychiatric symptoms.stabilize psychiatric symptoms.

Delirium in the intensive care unit Delirium in the intensive care unit (unlabeled use, unlabeled route):(unlabeled use, unlabeled route): I.V.: 2-10 mg; may repeat bolus doses every 20-30 minutes until calm I.V.: 2-10 mg; may repeat bolus doses every 20-30 minutes until calm achieved then administer 25% of the maximum dose every 6 hours; achieved then administer 25% of the maximum dose every 6 hours; monitor ECG and QTc intervalmonitor ECG and QTc interval Intermittent I.V.: 0.03-0.15 mg/kg every 30 minutes to 6 hours Intermittent I.V.: 0.03-0.15 mg/kg every 30 minutes to 6 hours Oral: Agitation: 5-10 mg Oral: Agitation: 5-10 mg Continuous I.V. infusion (100 mg/100 mL D5W): Rates of 3-25 mg/hour Continuous I.V. infusion (100 mg/100 mL D5W): Rates of 3-25 mg/hour have been used.have been used.

Rapid tranquilization of severely-agitated patient (Rapid tranquilization of severely-agitated patient (unlabeled useunlabeled use; ; administer every 30-60 minutes):administer every 30-60 minutes): Oral: 5-10 mg Oral: 5-10 mg I.M.: 5 mg I.M.: 5 mg Average total dose (oral or I.M.) for tranquilization: 10-20 mg Average total dose (oral or I.M.) for tranquilization: 10-20 mg

HaloperidolHaloperidol

DOSING: PEDIATRICDOSING: PEDIATRIC

Sedation/psychotic disorders: Oral:Sedation/psychotic disorders: Oral: Children: 3-12 years (15-40 kg): Initial: 0.05 mg/kg/day or 0.25-0.5 Children: 3-12 years (15-40 kg): Initial: 0.05 mg/kg/day or 0.25-0.5 mg/day given in 2-3 divided doses; increase by 0.25-0.5 mg every mg/day given in 2-3 divided doses; increase by 0.25-0.5 mg every 5-7 days; maximum: 0.15 mg/kg/day5-7 days; maximum: 0.15 mg/kg/day Usual maintenance: Usual maintenance: Agitation or hyperkinesia: 0.01-0.03 mg/kg/day once daily Agitation or hyperkinesia: 0.01-0.03 mg/kg/day once daily Nonpsychotic disorders: 0.05-0.075 mg/kg/day in 2-3 divided Nonpsychotic disorders: 0.05-0.075 mg/kg/day in 2-3 divided dosesdoses Psychotic disorders: 0.05-0.15 mg/kg/day in 2-3 divided doses Psychotic disorders: 0.05-0.15 mg/kg/day in 2-3 divided doses Children 6-12 years: Sedation/psychotic disorders: I.M. (as Children 6-12 years: Sedation/psychotic disorders: I.M. (as lactate): 1-3 mg/dose every 4-8 hours to a maximum of 0.15 lactate): 1-3 mg/dose every 4-8 hours to a maximum of 0.15 mg/kg/day; change over to oral therapy as soon as able.mg/kg/day; change over to oral therapy as soon as able.


DOSING: ELDERLYDOSING: ELDERLY — — – Nonpsychotic patients, Nonpsychotic patients, dementia behaviordementia behavior: Initial: : Initial:

Oral: 0.25-0.5 mg 1-2 times/day; increase dose at 4- Oral: 0.25-0.5 mg 1-2 times/day; increase dose at 4- to 7-day intervals by 0.25-0.5 mg/day. Increase to 7-day intervals by 0.25-0.5 mg/day. Increase dosing intervals (twice daily, 3 times/day, etc) as dosing intervals (twice daily, 3 times/day, etc) as necessary to control response or side effects.necessary to control response or side effects.


NIVELES DE REFERENCIANIVELES DE REFERENCIA

Therapeutic: 5-20 ng/mLTherapeutic: 5-20 ng/mL (SI: 10-40 (SI: 10-40 nmol/L) (psychotic disorders - less for nmol/L) (psychotic disorders - less for Tourette's and mania)Tourette's and mania)

Toxic: >42 ng/mLToxic: >42 ng/mL (SI: >84 nmol/L) (SI: >84 nmol/L)


SOBREDOSIS.SOBREDOSIS.– Síntomas: sueño profundo, distonía, Síntomas: sueño profundo, distonía,

agitación, arritmias y sintomas agitación, arritmias y sintomas extrapiramidales.extrapiramidales.

– Tratamiento: medidas de soporte.Tratamiento: medidas de soporte.– Arritmias cardíacas criticas: Lidocaina.Arritmias cardíacas criticas: Lidocaina.– Sintomas extrapiramidales: Agentes Sintomas extrapiramidales: Agentes

anticolinérgicos. Benztropine mesylate I.V. 1-anticolinérgicos. Benztropine mesylate I.V. 1-2 mg (adult). Efectivo en 2-5 minutes.2 mg (adult). Efectivo en 2-5 minutes.


PHARMACODYNAMICS / KINETICSPHARMACODYNAMICS / KINETICS– Onset of action: Sedation: I.V.: ~1 hourOnset of action: Sedation: I.V.: ~1 hour– Time to peak, serum: 20 minutesTime to peak, serum: 20 minutes– Duration: Decanoate: ~3 weeksDuration: Decanoate: ~3 weeks

– Protein binding: 90%Protein binding: 90%

– Metabolism: Hepatic to inactive compoundsMetabolism: Hepatic to inactive compounds– Bioavailability: Oral: 60%Bioavailability: Oral: 60%– Half-life elimination: 20 hoursHalf-life elimination: 20 hours

– Excretion: UrineExcretion: Urine (33% to 40% as metabolites) within (33% to 40% as metabolites) within 5 days; feces (15%)5 days; feces (15%)


EMBARAZO:EMBARAZO: – No recomendado.No recomendado.

LACTANCIALACTANCIA– No recomendado. No recomendado.


Efectos secundarios:Efectos secundarios:– Taquicardia ventricular.Taquicardia ventricular.

Asociado a dosis inicial elevada.Asociado a dosis inicial elevada.

Evitar en pacientes con riesgo de arritmias: Evitar en pacientes con riesgo de arritmias: QTc largo,QTc largo, disfunción hepática, alteraciones electrolíticas y disfunción hepática, alteraciones electrolíticas y miocardiopatia dilatada.miocardiopatia dilatada.

– Reacciones distónicas, parkinsonismoReacciones distónicas, parkinsonismo (más (más frecuentes por via oral), diskinesia tardia, akatisia, frecuentes por via oral), diskinesia tardia, akatisia, sindrome neuropleptico maligno.sindrome neuropleptico maligno.

– Hipotension arterial si hipovolemia.Hipotension arterial si hipovolemia.– No depresión respiratoria.No depresión respiratoria.


ADMINISTRACION:ADMINISTRACION:INYECCION IV DIRECTAINYECCION IV DIRECTA: SI: SIAdministrar la dosis prescrita en forma de inyección IV lenta, en al Administrar la dosis prescrita en forma de inyección IV lenta, en al menos 1 minuto por cada dosis de 5 mg. Se puede administrar sin menos 1 minuto por cada dosis de 5 mg. Se puede administrar sin diluir o diluido en 10-50 ml de SF o SG5%,diluir o diluido en 10-50 ml de SF o SG5%,

INFUSION INTERMITENTEINFUSION INTERMITENTE: SI: SIDiluir la dosis en 50-100 ml de SG5% y administrar en 30 minutos.Diluir la dosis en 50-100 ml de SG5% y administrar en 30 minutos.

INFUSION CONTINUAINFUSION CONTINUA: SI : SI Diluir la dosis en 500 ml de SG5%.Diluir la dosis en 500 ml de SG5%.

INYECCION IMINYECCION IM: SI: SISe recomienda no administrar más de 3 ml por inyección.Se recomienda no administrar más de 3 ml por inyección.


SUEROS COMPATIBLESSUEROS COMPATIBLES: : SG5%. A concentraciones altas (1mg/ml) SG5%. A concentraciones altas (1mg/ml) es incompatible con SF.es incompatible con SF.

OBSERVACIONES:OBSERVACIONES:Si la agitación es aguda se recomienda administrar de 1 a 2 ampollas.Si la agitación es aguda se recomienda administrar de 1 a 2 ampollas.Proteger de la luz. Conservar entre 15 y 30 refrigerar.Proteger de la luz. Conservar entre 15 y 30 refrigerar.


0.5-2 mg si agitación leve.0.5-2 mg si agitación leve.

2-5 mg si agitación moderada.2-5 mg si agitación moderada.

10-20 mg si agitación severa.10-20 mg si agitación severa.

Infusión contínua a 10 mg/h con incrementos de 5 mg/hora cada 30 minutos.Infusión contínua a 10 mg/h con incrementos de 5 mg/hora cada 30 minutos.

Dosis Dosis de de cargacarga

Dosis de Dosis de mantenimantenimientomiento

FG > 50 FG > 50 ml/minml/min

FG 10-50 FG 10-50 ml/minml/min

FG < 10 FG < 10 ml/minml/min

Dosis Dosis suplemesuplementaria ntaria tras HDtras HD

DPCADPCA TSCRTSCR

HaloperidolHaloperidol 2 -10 2 -10 mg IV mg IV en en bolus, bolus, duplicanduplican-dose -dose cada 20 cada 20 - 30 - 30 minutosminutos

50-100% 50-100% dosis dosis total de total de caga en caga en dosis dosis divididas divididas en 24 en 24 horashoras

100%100% 100%100% 100%100% NingunaNinguna NingunaNinguna Dosis de Dosis de FG 10-FG 10-50%50%


Olanzapine.Olanzapine.– Antipsicótico oral de 2ª generación.Antipsicótico oral de 2ª generación.– No se ha detectado arritmias ni prolongación No se ha detectado arritmias ni prolongación

del QT.del QT.

N05AX-Antipsicóticos atípicos

NOMBRE GENÉRICO


Clotiapina Comp 40 mg OR Etumina

Clozapina Comp 100 mg OR Leponex

Olanzapina Comp 5 mgComp 10 mgVial 10 mg/ 2ml

ORORIM

Zyprexa

Risperidona Comp 1 mgComp 3 mgComp 6 mgSol 1 mg/ml 30 ml

OROROROR

Risperdal

Nota 1: 1 gota=1 mg.Nota 2: 1 gota=0,1 mg.Nota 3: 1 gota=1 mg.Nota 4: 1 gota= 1 mg.

PropofolPropofol

Anestésico.Anestésico.

Hipnótico y sedante.Hipnótico y sedante.

Metabolismo hepático Metabolismo hepático (Glucoroconjugación).(Glucoroconjugación).

Eliminacion renal de metabolitos inactivos.Eliminacion renal de metabolitos inactivos.

Acúmulo en tejidos grasos (posibilidad de Acúmulo en tejidos grasos (posibilidad de sedación prolongada).T1/2 31 horas.sedación prolongada).T1/2 31 horas.

PropofolPropofolDOSING: ADULTSDOSING: ADULTS — Dosage must be individualized based on total body weight and titrated to the desired — Dosage must be individualized based on total body weight and titrated to the desired clinical effect. Wait at least 3-5 minutes between dosage adjustments to clinically assess drug effects. Smaller clinical effect. Wait at least 3-5 minutes between dosage adjustments to clinically assess drug effects. Smaller doses are required when used with narcotics. The following are general dosing guidelines (see "Symbols and doses are required when used with narcotics. The following are general dosing guidelines (see "Symbols and Abbreviations Used in This Handbook" in front section of this book for explanation of ASA classes):Abbreviations Used in This Handbook" in front section of this book for explanation of ASA classes):

Induction:Induction: General anesthesia: General anesthesia: ASA I or II, <55 years: I.V.: 2-2.5 mg/kg (~40 mg every 10 seconds until onset of induction) ASA I or II, <55 years: I.V.: 2-2.5 mg/kg (~40 mg every 10 seconds until onset of induction) Debilitated, ASA III or IV, hypovolemic: Refer to elderly dosing. Debilitated, ASA III or IV, hypovolemic: Refer to elderly dosing. Cardiac anesthesia: I.V.: 0.5-1.5 mg/kg (~20 mg every 10 seconds until onset of induction) Cardiac anesthesia: I.V.: 0.5-1.5 mg/kg (~20 mg every 10 seconds until onset of induction) Neurosurgical patients: I.V.: 1-2 mg/kg (~20 mg every 10 seconds until onset of induction) Neurosurgical patients: I.V.: 1-2 mg/kg (~20 mg every 10 seconds until onset of induction)Maintenance:Maintenance: ASA I or II, <55 years: ASA I or II, <55 years: I.V. infusion: Initial: 150-200 mcg/kg/minute for 10-15 minutes; decrease by 30% to 50% during first 30 minutes I.V. infusion: Initial: 150-200 mcg/kg/minute for 10-15 minutes; decrease by 30% to 50% during first 30 minutes of maintenance; usual infusion rate: 100-200 mcg/kg/minute (6-12 mg/kg/hour)of maintenance; usual infusion rate: 100-200 mcg/kg/minute (6-12 mg/kg/hour) I.V. intermittent bolus: 20-50 mg increments as needed I.V. intermittent bolus: 20-50 mg increments as needed Debilitated, ASA III or IV, hypovolemic: I.V. Infusion: Refer to elderly dosing. Debilitated, ASA III or IV, hypovolemic: I.V. Infusion: Refer to elderly dosing. Cardiac anesthesia: I.V. infusion: Cardiac anesthesia: I.V. infusion: Low-dose propofol with primary opioid: 50-100 mcg/kg/minute (see manufacturer's labeling) Low-dose propofol with primary opioid: 50-100 mcg/kg/minute (see manufacturer's labeling) Primary propofol with secondary opioid: 100-150 mcg/kg/minute Primary propofol with secondary opioid: 100-150 mcg/kg/minute Neurosurgical patients: I.V. infusion: 100-200 mcg/kg/minute (6-12 mg/kg/hour) Neurosurgical patients: I.V. infusion: 100-200 mcg/kg/minute (6-12 mg/kg/hour)Monitored anesthesia care sedation:Monitored anesthesia care sedation: Initiation: Initiation: ASA I or II, <55 years: Slow I.V. infusion: 100-150 mcg/kg/minute for 3-5 minutes or slow injection: 0.5 mg/kg ASA I or II, <55 years: Slow I.V. infusion: 100-150 mcg/kg/minute for 3-5 minutes or slow injection: 0.5 mg/kg over 3-5 minutesover 3-5 minutes Debilitated, neurosurgical, or ASA III or IV patients: Use similar doses to healthy adults; avoid rapid I.V. boluses Debilitated, neurosurgical, or ASA III or IV patients: Use similar doses to healthy adults; avoid rapid I.V. boluses Maintenance: Maintenance: ASA I or II, <55 years: I.V. infusion using variable rates (preferred over intermittent boluses): 25-75 ASA I or II, <55 years: I.V. infusion using variable rates (preferred over intermittent boluses): 25-75 mcg/kg/minute or incremental bolus doses: 10 mg or 20 mgmcg/kg/minute or incremental bolus doses: 10 mg or 20 mg Debilitated, neurosurgical, or ASA III or IV patients: Use 80% of healthy adult dose; do not use rapid bolus Debilitated, neurosurgical, or ASA III or IV patients: Use 80% of healthy adult dose; do not use rapid bolus doses (single or repeated)doses (single or repeated)

PropofolPropofol

DOSING: ADULTSDOSING: ADULTS — Dosage must be individualized based on — Dosage must be individualized based on total body weight and titrated to the desired clinical effect. Wait at total body weight and titrated to the desired clinical effect. Wait at least 3-5 minutes between dosage adjustments to clinically assess least 3-5 minutes between dosage adjustments to clinically assess drug effects. Smaller doses are required when used with narcotics.drug effects. Smaller doses are required when used with narcotics.

ICU sedation in intubated mechanically-ventilated patients: Avoid ICU sedation in intubated mechanically-ventilated patients: Avoid rapid bolus injection; individualize dose and titrate to responserapid bolus injection; individualize dose and titrate to response Continuous infusion: Initial: 0.3 mg/kg/hour (5 mcg/kg/min); Continuous infusion: Initial: 0.3 mg/kg/hour (5 mcg/kg/min); increase by 0.3-0.6 mg/kg/hour (5-10 mcg/kg/min) every 5-10 increase by 0.3-0.6 mg/kg/hour (5-10 mcg/kg/min) every 5-10 minutes until desired sedation level is achieved; usual maintenance: minutes until desired sedation level is achieved; usual maintenance: 0.3-4.8 mg/kg/hour (5-80 mcg/kg/min) or higher. Elderly, debilitated, 0.3-4.8 mg/kg/hour (5-80 mcg/kg/min) or higher. Elderly, debilitated, or ASA III or IV patients: Refer to elderly dosing. Some clinicians or ASA III or IV patients: Refer to elderly dosing. Some clinicians recommend daily interruption of infusion to perform clinical recommend daily interruption of infusion to perform clinical evaluation.evaluation.

PropofolPropofol

DOSING: PEDIATRICDOSING: PEDIATRIC — Dosage must be individualized based on — Dosage must be individualized based on total body weight and titrated to the desired clinical effect; wait at total body weight and titrated to the desired clinical effect; wait at least 3-5 minutes between dosage adjustments to clinically assess least 3-5 minutes between dosage adjustments to clinically assess drug effects; smaller doses are required when used with narcotics; drug effects; smaller doses are required when used with narcotics; the following are general dosing guidelines (see "Symbols and the following are general dosing guidelines (see "Symbols and Abbreviations Used in This Handbook" in front section of this book Abbreviations Used in This Handbook" in front section of this book for explanation of ASA classes):for explanation of ASA classes):

General anesthesia:General anesthesia:Induction: I.V.: Children 3-16 years, ASA I or II: 2.5-3.5 mg/kg over Induction: I.V.: Children 3-16 years, ASA I or II: 2.5-3.5 mg/kg over 20-30 seconds; use a lower dose for children ASA III or IV20-30 seconds; use a lower dose for children ASA III or IVMaintenance: I.V. infusion: Children 2 months to 16 years, ASA I or Maintenance: I.V. infusion: Children 2 months to 16 years, ASA I or II: Initial: 200-300 mcg/kg/minute; decrease dose after 30 minutes if II: Initial: 200-300 mcg/kg/minute; decrease dose after 30 minutes if clinical signs of light anesthesia are absent; usual infusion rate: 125-clinical signs of light anesthesia are absent; usual infusion rate: 125-150 mcg/kg/minute (range: 125-300 mcg/kg/minute; 7.5-18 150 mcg/kg/minute (range: 125-300 mcg/kg/minute; 7.5-18 mg/kg/hour); children 5 years may require larger infusion rates mg/kg/hour); children 5 years may require larger infusion rates compared to older children.compared to older children.

PropofolPropofolDOSING: ELDERLYDOSING: ELDERLY General anesthesia:General anesthesia: Induction: Elderly, debilitated, ASA III or IV, hypovolemic: I.V.: 1-1.5 mg/kg Induction: Elderly, debilitated, ASA III or IV, hypovolemic: I.V.: 1-1.5 mg/kg (~20 mg every 10 seconds until onset of induction)(~20 mg every 10 seconds until onset of induction) Maintenance: Elderly, debilitated, ASA III or IV, hypovolemic: I.V. infusion: Maintenance: Elderly, debilitated, ASA III or IV, hypovolemic: I.V. infusion: 50-100 mcg/kg/minute (3-6 mg/kg/hour)50-100 mcg/kg/minute (3-6 mg/kg/hour)Monitored anesthesia care sedation:Monitored anesthesia care sedation: Initiation: Elderly, debilitated, ASA III or IV, neurosurgical: I.V.: Use doses Initiation: Elderly, debilitated, ASA III or IV, neurosurgical: I.V.: Use doses similar to healthy adults; avoid rapid I.V. bolusessimilar to healthy adults; avoid rapid I.V. boluses Maintenance: Elderly, debilitated, ASA III or IV, neurosurgical: I.V.: Use Maintenance: Elderly, debilitated, ASA III or IV, neurosurgical: I.V.: Use 80% of healthy adult dose; do not use rapid bolus doses (single or 80% of healthy adult dose; do not use rapid bolus doses (single or repeated)repeated)ICU sedation in intubated mechanically-ventilated patients: Avoid rapid ICU sedation in intubated mechanically-ventilated patients: Avoid rapid bolus injection; individualize dose and titrate to response: Continuous bolus injection; individualize dose and titrate to response: Continuous infusion: Elderly, debilitated, ASA III or IV: Reduce dose by 80%; reduce infusion: Elderly, debilitated, ASA III or IV: Reduce dose by 80%; reduce dose after adequate sedation established and adjust to response (ie, dose after adequate sedation established and adjust to response (ie, evaluate frequently to use minimum dose for sedation).evaluate frequently to use minimum dose for sedation).

PropofolPropofol

Principal efecto secundario: Principal efecto secundario: HipoTAHipoTAOtros: bradicardia, arritmias, efectos neurológicos Otros: bradicardia, arritmias, efectos neurológicos (procovulsivante, mioclonías, movimiento (procovulsivante, mioclonías, movimiento coreoatetósicos, meningismo), acidosis respiratoria coreoatetósicos, meningismo), acidosis respiratoria (aumento de producción de CO2), pancreatitis, (aumento de producción de CO2), pancreatitis, hipertrigliceridemia, anafilaxis y coloración verdosa de la hipertrigliceridemia, anafilaxis y coloración verdosa de la orina.orina.Acidosis láctica, insuficiencia renal aguda y Acidosis láctica, insuficiencia renal aguda y rabdomiolisis.rabdomiolisis.La administración contínua más de 24-48 horas se La administración contínua más de 24-48 horas se relaciona con serias complicaciones.relaciona con serias complicaciones.La solución contiene 1,1 kcal/ml, principalmente en La solución contiene 1,1 kcal/ml, principalmente en forma de lípidos.forma de lípidos.Frecuente contaminación bacteriana.Frecuente contaminación bacteriana.

PropofolPropofolDRUG INTERACTIONSDRUG INTERACTIONS — Substrate of CYP1A2 (minor), 2A6 — Substrate of CYP1A2 (minor), 2A6 (minor), 2B6 (major), 2C9 (major), 2C19 (minor), 2D6 (minor), 2E1 (minor), 2B6 (major), 2C9 (major), 2C19 (minor), 2D6 (minor), 2E1 (minor), 3A4 (minor); Inhibits CYP1A2 (moderate), 2C9 (weak), (minor), 3A4 (minor); Inhibits CYP1A2 (moderate), 2C9 (weak), 2C19 (moderate), 2D6 (weak), 2E1 (weak), 3A4 (strong)2C19 (moderate), 2D6 (weak), 2E1 (weak), 3A4 (strong)

CNS depressantsCNS depressants:: Additive CNS depression and respiratory Additive CNS depression and respiratory depression may necessitate dosage reduction when used with depression may necessitate dosage reduction when used with anesthetics, benzodiazepines, opiates, ethanol, phenothiazines.anesthetics, benzodiazepines, opiates, ethanol, phenothiazines.CYP1A2 substrates: Propofol may increase the levels/effects of CYP1A2 substrates: Propofol may increase the levels/effects of CYP1A2 substrates. Example substrates include aminophylline, CYP1A2 substrates. Example substrates include aminophylline, fluvoxamine, mexiletine, mirtazapine, ropinirole, theophylline, and fluvoxamine, mexiletine, mirtazapine, ropinirole, theophylline, and trifluoperazine.trifluoperazine.CYP2B6 inhibitors: May increase the levels/effects of propofol. CYP2B6 inhibitors: May increase the levels/effects of propofol. Example inhibitors include desipramine, paroxetine, and sertraline.Example inhibitors include desipramine, paroxetine, and sertraline.CYP2C9 Inhibitors may increase the levels/effects of propofol. CYP2C9 Inhibitors may increase the levels/effects of propofol. Example inhibitors include delavirdine, fluconazole, gemfibrozil, Example inhibitors include delavirdine, fluconazole, gemfibrozil, ketoconazole, nicardipine, NSAIDs, sulfonamides and tolbutamide.ketoconazole, nicardipine, NSAIDs, sulfonamides and tolbutamide.

PropofolPropofolDRUG INTERACTIONSDRUG INTERACTIONS — Substrate of CYP1A2 (minor), 2A6 (minor), 2B6 — Substrate of CYP1A2 (minor), 2A6 (minor), 2B6 (major), 2C9 (major), 2C19 (minor), 2D6 (minor), 2E1 (minor), 3A4 (minor); (major), 2C9 (major), 2C19 (minor), 2D6 (minor), 2E1 (minor), 3A4 (minor); Inhibits CYP1A2 (moderate), 2C9 (weak), 2C19 (moderate), 2D6 (weak), Inhibits CYP1A2 (moderate), 2C9 (weak), 2C19 (moderate), 2D6 (weak), 2E1 (weak), 3A4 (strong)2E1 (weak), 3A4 (strong)

CYP2C19 substrates: Propofol may increase the levels/effects of CYP2C19 CYP2C19 substrates: Propofol may increase the levels/effects of CYP2C19 substrates. Example substrates include citalopram, diazepam, substrates. Example substrates include citalopram, diazepam, methsuximide, phenytoin, propranolol, and sertraline.methsuximide, phenytoin, propranolol, and sertraline.CYP3A4 substrates: Propofol may increase the levels/effects of CYP3A4 CYP3A4 substrates: Propofol may increase the levels/effects of CYP3A4 substrates. Example substrates include benzodiazepines, calcium channel substrates. Example substrates include benzodiazepines, calcium channel blockers, mirtazapine, nateglinide, nefazodone, tacrolimus, and venlafaxine. blockers, mirtazapine, nateglinide, nefazodone, tacrolimus, and venlafaxine. Selected benzodiazepines (midazolam and triazolam), cisapride, ergot Selected benzodiazepines (midazolam and triazolam), cisapride, ergot alkaloids, selected HMG-CoA reductase inhibitors (lovastatin and alkaloids, selected HMG-CoA reductase inhibitors (lovastatin and simvastatin), and pimozide are generally contraindicated with strong simvastatin), and pimozide are generally contraindicated with strong CYP3A4 inhibitors.CYP3A4 inhibitors.Narcotics:Narcotics: Concomitant use may lead to increased sedative or anesthetic Concomitant use may lead to increased sedative or anesthetic effects of propofol, more pronounced decreases in systolic, diastolic, and effects of propofol, more pronounced decreases in systolic, diastolic, and mean arterial pressures and cardiac output. Lower doses of propofol may mean arterial pressures and cardiac output. Lower doses of propofol may be needed. In addition, fentanyl may cause serious bradycardia when used be needed. In addition, fentanyl may cause serious bradycardia when used with propofol in pediatric patients.with propofol in pediatric patients.VecuroniumVecuronium: Propofol may potentiate the neuromuscular blockade of : Propofol may potentiate the neuromuscular blockade of vecuronium.vecuronium.

PropofolPropofol

EMBARAZO.EMBARAZO.– No recomendado. Cruza la barrera No recomendado. Cruza la barrera

placentaria causando depresión neonatal.placentaria causando depresión neonatal.

LACTANCIALACTANCIA– No recomendado.No recomendado.

PropofolPropofolPHARMACODYNAMICS / KINETICSPHARMACODYNAMICS / KINETICS

– Onset of action: Anesthetic: Bolus infusion (dose dependent): 9-51 Onset of action: Anesthetic: Bolus infusion (dose dependent): 9-51 seconds (average 30 seconds)seconds (average 30 seconds)

– Duration (dose and rate dependent): 3-10 minutesDuration (dose and rate dependent): 3-10 minutes– Distribution: Vd: 2-10 L/kg; highly lipophilicDistribution: Vd: 2-10 L/kg; highly lipophilic

– Protein binding: 97% to 99%Protein binding: 97% to 99%– Metabolism: Hepatic to water-soluble sulfate and glucuronide Metabolism: Hepatic to water-soluble sulfate and glucuronide

conjugatesconjugates– Half-life elimination: Biphasic: Initial: 40 minutes; Terminal: 4-7 hours Half-life elimination: Biphasic: Initial: 40 minutes; Terminal: 4-7 hours

(up to 1-3 days)(up to 1-3 days)

– Excretion: Urine (~88% as metabolites, 40% as glucuronide metabolite); Excretion: Urine (~88% as metabolites, 40% as glucuronide metabolite); feces (<2%)feces (<2%) Clearance: 20-30 mL/kg/minute; total body clearance exceeds liver Clearance: 20-30 mL/kg/minute; total body clearance exceeds liver blood flow.blood flow.

– Food: EDTA, an ingredient of propofol emulsion, Food: EDTA, an ingredient of propofol emulsion, may lead to may lead to decreased zinc levels in patients on prolonged therapy (>5 days) decreased zinc levels in patients on prolonged therapy (>5 days) or those predisposed to deficiency (burns, diarrhea, and/or major or those predisposed to deficiency (burns, diarrhea, and/or major sepsis).sepsis).

PropofolPropofolADMINISTRACION:ADMINISTRACION:

INYECCION IV DIRECTAINYECCION IV DIRECTA: SI: SIInyección en bolus repetidos, se pueden administrar incrementos de 25 mg (2,5 ml) a 50 mg (5 Inyección en bolus repetidos, se pueden administrar incrementos de 25 mg (2,5 ml) a 50 mg (5 ml) de acuerdo con las necesidades clínicas. La velocidad de administración es de 2-4 ml cada ml) de acuerdo con las necesidades clínicas. La velocidad de administración es de 2-4 ml cada 10 segundos.10 segundos.

INFUSION INTERMITENTEINFUSION INTERMITENTE: SI: SIDiluir la dosis prescrita con SG5% sin exceder de la concentración de 2 mg/ml (como mínimo Diluir la dosis prescrita con SG5% sin exceder de la concentración de 2 mg/ml (como mínimo deben utilizarse 4 ml de SG5% para diluir 1 ml de Propofol). Usualmente la velocidad de infusión deben utilizarse 4 ml de SG5% para diluir 1 ml de Propofol). Usualmente la velocidad de infusión es de 4 a 12 mg/kg/h. En sedación UCI 1-4 mg/Kg/h.es de 4 a 12 mg/kg/h. En sedación UCI 1-4 mg/Kg/h.También puede ser utilizada sin diluir, en infusión controlada por bombas u otros sistemas. También puede ser utilizada sin diluir, en infusión controlada por bombas u otros sistemas.

INFUSION CONTINUAINFUSION CONTINUA: SI : SI Diluir la dosis prescrita con SG5% sin exceder de la concentración de 2 mg/ml (como mínimo Diluir la dosis prescrita con SG5% sin exceder de la concentración de 2 mg/ml (como mínimo deben utilizarse 4 ml de SG5% para diluir 1 ml de Propofol). Usualmente la velocidad de infusión deben utilizarse 4 ml de SG5% para diluir 1 ml de Propofol). Usualmente la velocidad de infusión es de 0,1-0,2 mg/kg/minuto.es de 0,1-0,2 mg/kg/minuto.También puede ser utilizada sin diluir, en infusión controlada por bombas u otros sistemas. También puede ser utilizada sin diluir, en infusión controlada por bombas u otros sistemas.

Velocidad de administración de propofol en infusión IV (ml/h o microgotas/min) cuando se Velocidad de administración de propofol en infusión IV (ml/h o microgotas/min) cuando se emplea la solución del 1 % ( 10 mg/ml sin diluir).emplea la solución del 1 % ( 10 mg/ml sin diluir).

INYECCION IMINYECCION IM: NO: NO

PropofolPropofol

SUEROS COMPATIBLESSUEROS COMPATIBLES: Unicamente SG5%. Una vez diluido en : Unicamente SG5%. Una vez diluido en SG5%, las soluciones son estables 6 horas a temperatura SG5%, las soluciones son estables 6 horas a temperatura ambiente. ambiente.

OBSERVACIONES:OBSERVACIONES:– Conservar por debajo de 25° C. Conservar por debajo de 25° C. – Se trata de una emulsión de color blanco. Es importante no Se trata de una emulsión de color blanco. Es importante no

guardar en nevera y evitar su congelación.guardar en nevera y evitar su congelación.– Agitar los envases antes de usar. Si la ampolla presenta Agitar los envases antes de usar. Si la ampolla presenta

partículas o decoloración debe desecharse. partículas o decoloración debe desecharse.

PropofolPropofol

Dosis de Dosis de cargacarga

Dosis Dosis de de mantenimantenimientomiento

FG > FG > 50 50 ml/minml/min

FG 10-FG 10-50 50 ml/minml/min

FG < FG < 10 10 ml/minml/min

Dosis Dosis suplemesuplementaria ntaria tras HDtras HD

DPCADPCA TSCRTSCR

PropofolPropofol 0,5 0,5 mg/kg/h.mg/kg/h.

Aumentar Aumentar 0,3-0,6 0,3-0,6 mg/kg/h mg/kg/h cada 5-10 cada 5-10 min.min.

0,5-3 0,5-3 mg/g/hmg/g/h

100%100% 100%100% 100%100% DesconoDescono-cido-cido

Desco-Desco-nocidonocido

Dosis Dosis de FG de FG 10-50%10-50%

Propofol Amp 200 mg/20 ml IV Lipuro 1% Braun Diprivan

SEDACION EN PACIENTES CON ERC Francisco José de la Prada Alvarez Servicio de Nefrología Hospital...

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