Benzodiacepinas

Estructura Química y Farmacodinamia

Estructura química

• Las benzodiacepinas tienen un sistema de anillos heterocíclicos típicos, que es una fusión entre los LOS Neisseria anillos benceno y diazepina.
• Hay una variedad de medicamentos en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum la clase de las benzodiacepinas, que varían según el grupo secundario adjunto.
• Los LOS Neisseria diferentes grupos laterales afectan la afinidad de unión y la interacción con los LOS Neisseria receptores GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS.

Mecanismo de acción

• Las benzodiacepinas se unen a la subunidad gamma del receptor Receptor Receptors are proteins located either on the surface of or within a cell that can bind to signaling molecules known as ligands (e.g., hormones) and cause some type of response within the cell. Receptors GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS_A → mejoran la actividad de unión de GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS al AL Amyloidosis bolsillo entre las subunidades α y 𝛃 del receptor Receptor Receptors are proteins located either on the surface of or within a cell that can bind to signaling molecules known as ligands (e.g., hormones) and cause some type of response within the cell. Receptors GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS_A
• ↑ Frecuencia de apertura del canal de cloruro → ↑ entrada de cloruro → inhibe el potencial de acción
• El flumazenil Flumazenil A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses. Benzodiazepines es un antagonista competitivo de las benzodiacepinas en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum el receptor Receptor Receptors are proteins located either on the surface of or within a cell that can bind to signaling molecules known as ligands (e.g., hormones) and cause some type of response within the cell. Receptors GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS_A.

Efectos fisiológicos

GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS:

• GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS es el principal neurotransmisor inhibidor en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum el SNC
• Las neuronas que usan GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS como transmisor, contienen una enzima llamada descarboxilasa del ácido glutámico, que convierte el aminoácido glutamato en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS.

Receptores GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS:

• Los LOS Neisseria receptores GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS_A y GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS_C son receptores ionotrópicos.
• Los LOS Neisseria receptores GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS_B son receptores acoplados a proteína G o metabotrópicos.
• Los LOS Neisseria receptores GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS_A y GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS_B modulan la actividad inhibidora del SNC.
• Los LOS Neisseria receptores GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS_C se encuentran en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum las células retinianas del ojo; se desconoce su función exacta.
• Los LOS Neisseria receptores GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS_A son estructuras pentaméricas y constan de:
  • 2 subunidades α (alfa)
  • 2 subunidades 𝛃 (beta)
  • 1 subunidad γ (gamma).
• Localización y efectos del receptor Receptor Receptors are proteins located either on the surface of or within a cell that can bind to signaling molecules known as ligands (e.g., hormones) and cause some type of response within the cell. Receptors GABA GABA The most common inhibitory neurotransmitter in the central nervous system. Receptors and Neurotransmitters of the CNS_A:
  • Corteza cerebral → confusión, amnesia
  • Tálamo → desinhibición, sedación, inhibición motora
  • Estructuras límbicas → ansiolisis, sedación

Efectos terapéuticos de las benzodiacepinas:

• Ansiolítico
• Relajante del músculo esquelético
• Sedante:
  • Mitigan la agitación
  • Disminuyen la actividad
  • Producen sensación de calma
• Anticonvulsivantes: medicamento que controla las convulsiones
• Hipnótico:
  • Induce la somnolencia, y promueve el inicio y mantenimiento del sueño
  • ↓ Sueño de movimientos oculares rápidos (REM, por sus siglas en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum inglés; cuando ocurre el sueño)
• Anestesia

Farmacocinética

Absorción

Las benzodiacepinas lipofílicas tienen una absorción más rápida.

Distribución

• Las benzodiacepinas y los LOS Neisseria metabolitos están altamente unidos a proteínas.
• Amplia distribución:
  • Ingresan al AL Amyloidosis SNC (la solubilidad en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum lípidos también aumentan su tasa)
  • Cruzan la placenta Placenta A highly vascularized mammalian fetal-maternal organ and major site of transport of oxygen, nutrients, and fetal waste products. It includes a fetal portion (chorionic villi) derived from trophoblasts and a maternal portion (decidua) derived from the uterine endometrium. The placenta produces an array of steroid, protein and peptide hormones (placental hormones). Placenta, Umbilical Cord, and Amniotic Cavity

Metabolismo

• Hepático
• Isoenzimas involucradas del citocromo P450:
  • CYP3A4 CYP3A4 Class 3 Antiarrhythmic Drugs (Potassium Channel Blockers)
  • CYP2C19
• Algunos metabolitos pueden ser activos → mayor duración del efecto terapéutico
• Los LOS Neisseria metabolitos están conjugados → glucurónidos

Excreción

La eliminación se produce a través del riñón ( los LOS Neisseria glucurónidos se excretan en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum la orina).

Tabla comparativa de la farmacocinética

La siguiente tabla destaca a las benzodiacepinas y aborda las propiedades de cada una. Con respecto a la farmacocinética, es importante prestar atención al AL Amyloidosis inicio de acción, el metabolismo y la eliminación.

Indicaciones

Las benzodiacepinas son depresores del SNC. Por lo tanto, son clínicamente útiles para situaciones en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum las que puede ser necesario un agente sedante. La siguiente tabla aborda los LOS Neisseria agentes individuales y sus indicaciones. Estas son las indicaciones generales de las benzodiacepinas:

• Trastornos convulsivos: útil en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum el tratamiento de convulsiones prolongadas en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum situaciones de emergencia
• Abstinencia alcohólica: alivia los LOS Neisseria síntomas de abstinencia y previene las convulsiones por abstinencia
• Trastornos de ansiedad:
  • Trastorno de pánico
  • Trastorno de ansiedad generalizada
• Insomnio: útil a corto plazo, pero no se recomienda administrarlo durante más de un mes para esta indicación
• Inducción de la anestesia

Efectos Secundarios y Contraindicaciones

Descripción general

Hay algunos puntos de alta importancia a los LOS Neisseria que se debe prestar atención al AL Amyloidosis considerar las benzodiacepinas:

• Esta clase de medicamentos deben utilizarse con precaución en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum pacientes de edad avanzada y en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum aquellos con daño hepático o renal.
  • Los LOS Neisseria principales metabolitos activos, como el nordiazepam y el N-Desalkylflurazepam, tienen vidas medias prolongadas y se acumulan con el tiempo.
  • Por lo tanto, en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum pacientes de edad avanzada o en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum pacientes con insuficiencia hepática/renal, la acumulación de metabolitos activos puede producir sobresedación y amnesia anterógrada.
• Los LOS Neisseria efectos hipnóticos dan como resultado un efecto rebote del aumento del sueño REM, que se produce con la interrupción de las benzodiacepinas. Este es especialmente el caso de agentes de acción más corta como el triazolam Triazolam A short-acting benzodiazepine used in the treatment of insomnia. Its use at lower doses with appropriate care and labeling has been reaffirmed by the fda and most other countries. Benzodiazepines.
• Todas las benzodiacepinas deben usarse cuidadosamente con opioides.

Efectos secundarios

• Cardiovasculares: hipotensión
• Musculoesqueléticos: debilidad muscular
• Neurológicos/psiquiátricos
  • Amnesia
  • Somnolencia
  • Mareo
  • Sedación
  • Euforia
  • Ataxia Ataxia Impairment of the ability to perform smoothly coordinated voluntary movements. This condition may affect the limbs, trunk, eyes, pharynx, larynx, and other structures. Ataxia may result from impaired sensory or motor function. Sensory ataxia may result from posterior column injury or peripheral nerve diseases. Motor ataxia may be associated with cerebellar diseases; cerebral cortex diseases; thalamic diseases; basal ganglia diseases; injury to the red nucleus; and other conditions. Ataxia-telangiectasia
• Respiratorios: depresión respiratoria
• Dermatológicos: erupción cutánea
• Genitourinarios: dificultad para la micción

Advertencias

• Criterios de Beers: aumento del riesgo de delirium Delirium Delirium is a medical condition characterized by acute disturbances in attention and awareness. Symptoms may fluctuate during the course of a day and involve memory deficits and disorientation. Delirium, sedación y caídas en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum las personas de edad avanzada
• Potencial de abuso: puede causar euforia con riesgo de dependencia y abstinencia del medicamento
• Sustancias controladas por la FDA C-IV
• Advertencia de recuadro negro: el uso concomitante de benzodiacepinas y opioides puede provocar sedación profunda, depresión respiratoria, coma Coma Coma is defined as a deep state of unarousable unresponsiveness, characterized by a score of 3 points on the GCS. A comatose state can be caused by a multitude of conditions, making the precise epidemiology and prognosis of coma difficult to determine. Coma o el fallecimiento.

Contraindicaciones

• Edad:
  • Pediátricos < 6 meses: diazepam Diazepam A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of gamma-aminobutyric acid activity. Benzodiazepines oral
  • Lactantes prematuros: inyección de lorazepam Lorazepam A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. Benzodiazepines debido al AL Amyloidosis contenido de alcohol bencílico
• Insuficiencia hepática grave ( clonazepam Clonazepam An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of gamma-aminobutyric acid receptor responses. Benzodiazepines y diazepam Diazepam A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of gamma-aminobutyric acid activity. Benzodiazepines)
• Miastenia gravis
• Respiratorias:
  • Apnea del sueño
  • Enfermedad pulmonar obstructiva crónica (EPOC)
  • Bronquitis
• Oftálmicas:
  • Glaucoma Glaucoma Glaucoma is an optic neuropathy characterized by typical visual field defects and optic nerve atrophy seen as optic disc cupping on examination. The acute form of glaucoma is a medical emergency. Glaucoma is often, but not always, caused by increased intraocular pressure (IOP). Glaucoma de ángulo estrecho
  • Glaucoma Glaucoma Glaucoma is an optic neuropathy characterized by typical visual field defects and optic nerve atrophy seen as optic disc cupping on examination. The acute form of glaucoma is a medical emergency. Glaucoma is often, but not always, caused by increased intraocular pressure (IOP). Glaucoma de ángulo abierto no tratado

Interacciones medicamentosas

• Se debe evitar otros depresores y sedantes del SNC (e.g., opioides, barbitúricos, etanol)
• Los LOS Neisseria inhibidores potentes de CYP3A4 CYP3A4 Class 3 Antiarrhythmic Drugs (Potassium Channel Blockers) o CYP2C19 están contraindicados (e.g., itraconazol, ketoconazol) → ↑ niveles de benzodiacepinas
• Inductores potentes de CYP3A4 CYP3A4 Class 3 Antiarrhythmic Drugs (Potassium Channel Blockers) o CYP2C19 → ↓ niveles de benzodiacepinas

Sobredosis

Estos medicamentos rara vez provocan una sobredosis de forma aislada. Cuando se combinan con otras clases de medicamentos, como el alcohol y los LOS Neisseria opiáceos, existe un riesgo mucho mayor de toxicidad.

• Síntomas de sobredosis:
  • Dificultad para hablar y somnolencia
  • Hipotensión
  • Depresión respiratoria
  • Coma Coma Coma is defined as a deep state of unarousable unresponsiveness, characterized by a score of 3 points on the GCS. A comatose state can be caused by a multitude of conditions, making the precise epidemiology and prognosis of coma difficult to determine. Coma
  • Paro cardiorespiratorio
• Tratamiento:
  • Agente de reversión: flumazenil Flumazenil A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses. Benzodiazepines
    • Antagonista de las benzodiacepinas
    • Se debe considerar la posibilidad de convulsiones en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum pacientes con terapia a largo plazo.
  • Terapia de soporte
    • Mantener la vía aérea e intubar, si es necesario.
    • Líquidos intravenosos para la hipotensión; vasopresores si el paciente no responde a los LOS Neisseria líquidos
    • La bradicardia debe tratarse con terapia farmacológica (e.g., atropina).

Relevancia Clínica

Los LOS Neisseria siguientes son usos terapéuticos de las benzodiacepinas:

• Trastornos de ansiedad: trastornos mentales que (combinados) son el tipo de trastorno psiquiátrico más prevalente en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum Estados Unidos. Los LOS Neisseria trastornos de ansiedad se caracterizan por una preocupación y un miedo excesivo. Los LOS Neisseria ejemplos incluyen trastorno de ansiedad por separación, mutismo selectivo, fobias específicas, trastorno de ansiedad social, trastorno de pánico, agorafobia, trastorno de ansiedad generalizada, trastorno de ansiedad inducido por sustancias o medicamentos y trastorno de ansiedad debido a otra afección médica.
• Trastornos de pánico: implica ataques de pánico recurrentes e inesperados (sin una señal o desencadenante). Los LOS Neisseria ataques de pánico son estallidos repentinos de miedo o malestar intenso que culminan en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum minutos y pueden estar asociados con síntomas de sudoración, palpitaciones, miedo, náuseas y dificultad para respirar.
• Abstinencia alcohólica: conjunto de síntomas que se manifiestan tras el cese brusco del consumo de etanol cuando se ha HA Hemolytic anemia (HA) is the term given to a large group of anemias that are caused by the premature destruction/hemolysis of circulating red blood cells (RBCs). Hemolysis can occur within (intravascular hemolysis) or outside the blood vessels (extravascular hemolysis). Hemolytic Anemia ingerido regularmente durante un período prolongado de tiempo. Los LOS Neisseria síntomas de la abstinencia alcohólica consisten en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum hiperactividad autonómica, alucinaciones, ansiedad, agitación y temblores. También pueden surgir complicaciones mortales, como convulsiones, delirium Delirium Delirium is a medical condition characterized by acute disturbances in attention and awareness. Symptoms may fluctuate during the course of a day and involve memory deficits and disorientation. Delirium y síndrome de Wernicke-Korsakoff.