Rifampicina
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Transcript of Rifampicina
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Departamento de Farmacología Toxicología y Farmacodependencia
Facultad de FarmaciaUniversidad de Costa Rica
Farmacología III
Rifampicina
Dra. Beatriz Badilla B.II ciclo 2009
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RifampicinaEstructura química
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RifampicinaMecanismo de acción
Unión a la subunidad polimerasa de RNA dependiente de ADN
de los microorganismos formando un Complejo estable.
Impide la iniciación de la síntesis de ARN
Bactericida
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RifampicinaFarmacocinética
Absorción oral: Buena. Retrasada o reducida por alimentos
Distribución: Altamente lipofílica (BHE) Tmax: 3 a 4 horas
T ½ : 9.8 horas. Aumentada por disfunción hepática
Unión a proteínas: 80%
Metabolismo: Hepático. Circulación enterohepática
Categoría C
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Eliminación
Metabolitos en bilisHeces 60-65%Orina 30-35% (inalterados)
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Rifampicina. Espectro de actividad
Gram (+)St.pneumonie
St. grupo ABCGStaph. aureus (MS) (MR)
Staph. epidermidisListeria monocitogenes
Gram (-)N. meningitiidisM. catarrhalisH. influenzae
Legionella pneumophila
OtrosChlamydophyla sp
Gilbert D. et al.The Sanford Guide 39th Ed. 2009, p71
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RifampicinaUso clínico
Tratamiento combinado de TB
PROFILAXIS de meningitis por H. influenzae tipo B
Contactos familiares cercanos y otros
600 mg c/24 h por 4 dosis*Niños 20 mg/kg vo c/24 h x4 días
NO EN EMBARAZO
X
Gilbert D. et al.The Sanford Guide 39th Ed. 2009, p9
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RifampicinaUso clínico
PROFILAXIS de enfermedad meningocóccica *
Contactos familiares cercanos y otros600 mg c/12 h por 4 dosisNiños> 1 mes 10 mg/kg c/12 h x 2 días (4 dosis)Niños< 1 mes 5 mg/kg c/12 h x 2 días (4 dosis)
NO EN EMBARAZO*Cipro500 mg vo stat
Ceftriaxona 250 mg IM x 1 dosis
X
Gilbert D. et al. The Sanford Guide 39th Ed. 2009, p8
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RifampicinaUso clínico
Endocarditis infecciosaStaph aureus
Vancomicina+ Rifampicina
Válvula prostética
Marcapasos
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INTERACCIONES
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Gilbert D. et al. The Sanford Guide 39th Ed. 2009, p198
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Departamento de Farmacología Toxicología y Farmacodependencia
Facultad de FarmaciaUniversidad de Costa Rica
Farmacología III
Metronidazol
Dra. Beatriz Badilla B.II ciclo 2009
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Fermentación oxidativa de cetoácidos
Donación de electrones hacia otros aceptores
Metronidazol
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Espectro de actividad
Bacteroides fragilisClostridium difficili
Clostridium no difficilePeptostreptococcus sp.
Helicobacter pyloriInfecciones intra-abdominales
Infeciones en SNCColitis pseudomenbranosa
Infec. sitémicas por anaerobiosVaginosis bacterial
Enf. de Crohn
Usos
Gilbert D. The Sanford Guide 39th ed. 2009. p71
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Apendicectomía:No perforada MND 500 mg IV statPerforada MND 500 mg iv stat y c/8h x 5d.
Cirugía colorectalMND 500 mg IV+ Cefazolina 1-2 g IV
Usos en profilaxis
Herida abdominal penetrante:MND 500 mg IV stat y c/8h x 5d
.
X
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Violación sexualMND 2g VO statAZITRO 1 g VOCEFTRIAXONA 125 mg IM
Usos en profilaxis
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Farmacocinética
Abs. Oral: BuenaTópica: 10v menos que oral
U. A prot.: < 20%Metabolismo: hepático
T1/2: 6—8 h (se prolonga en disf. Hep.Pico máximo oral: 1-2 h
Excreción: renal (20-40% sin cambio)Ajuste de dosis en I.renal
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Precauciones
Insuficiencia hepáticaDiscrasias sanguíneas
Historia de convulsiones
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Reacciones adversas
>10% SNC: cefalea , nauseas
GI: nausea, vómito, diarrea, anorexia<1%
Convulsiones, ataxia,orina oscura, sabor metálico,neuropatía, pancreatitis
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Interacciones
WarfarinaLitioCiclosporina Fenobarbital
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Efecto tipo disulfirán
No tomar alcohol dentro de 72 horasDespues de ss tx
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Tetraciclinas
Departamento de Farmacología Toxicología y Farmacodependencia
Facultad de FarmaciaUniversidad de Costa Rica
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Tetraciclinas
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Tetraciclinas. Mecanismo de Acción
BACTERIOSTÁTICOS
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TetraciclinasFarmacocinética
TetraciclinaOxytetraciclinaClortetraciclinaDemeclocicline
MetaciclinaLimeciclina
Rolitetraciclina
DoxyciclinaMinociclina Aminometilciclinas
Tigeciclina(Glycilciclinas)
Agwuh & MacGowan. Pharmacokinetics and Pharmacodynamics of theTetracyclines including glycyclynes.
J.Antimicrobial Chemotherapu¡y (2006) 58, 256-265
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Tetraciclinas. Farmacocinética
Categoría D
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Agwuh & MacGowan. Pharmacokinetics and Pharmacodynamics of theTetracyclines including glycyclynes.
J.Antimicrobial Chemotherapu¡y (2006) 58, 256-265
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TetraciclinasEspectro de actividad
Gram (+)St. Grupo ABCGSt. pneumonieStap. aureus MSStap. aureus CA-MRSA
Gram (-)N. meningitidisM. catarrhalisE. ColiH.influenzaeLegionellaV. choleraeF. tularensisBrucella
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TetraciclinasEspectro de actividad
OtrosChl. trachomatisChlamydia sp
RickettsiasCoxelia burnetiiEhrlichia sp
Borrelia burdorferi Borrelia recurrentis
Ureaplasma urealiticumMycoplasma pneumonie
RickettsiaChlamydia
Mycoplasma
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Tetraciclinas. Uso clínico
Chl. trachomatis
Rickettsias
Borrelia burdorferi
Coxelia burnetii
Ehrlichia sp
Linfogranuloma venéreo
F.de las Montañas Rocosas
Enfermedad de Lyme
Fiebre Q
Ehrliquiosis (CR)
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Vibrio choleraeDoxicilina 300 mg/día x 3 días(adultos)Tetraciclina 400 mg qid x 3 días
FQ 100 mg/dNiños TMP-SMX
DosisTetraciclina 250-500 mgc/6 h
Doxicilina 100 mg c/12 horas por 24 horas100 mg c/24 horas
Tetraciclinas. Uso clínico
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www.bioterrorism.slu.edu. BMJ
Bioterrorismo
Doxy: 100 mg bid X 60 d(incluye mujeres embarazadas)
Antrax cutáneo ( inhalación)
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Thielman N and Guerrant R. N Engl J Med 2004;350:38-47
Antimicrobial Recommendations for Infections with Specific Pathogens
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Tetraciclinas Uso clínico
-Acné vulgaris (Propionibacterun acnes) Minociclina .Doxiciclina
-Neumonía adquirida en la comunidad-Neumonía atípica ( M.pneumonie) TETRA o DOXI
-ITU por U. urealiticumTETRA o DOXI Eritro o Macrol 1ª Alt.
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-Borrelia burgdorferi Enf. de Lyme TETRA O DOXI
-Tularemia 3º elección TETRA o DOXI
Tetraciclinas Uso clínico
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>85%adolescentes
2M /añoVisitas
$1 B/añoCosto total
$100 M /año OTC
Propionibacterium acnes
ACNÉ ACNÉ
James. Acne. NEJM 352:14, 2006
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James W. N Engl J Med 2005;352:1463-1472
Mild Acne
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James W. N Engl J Med 2005;352:1463-1472
Classification of Acne
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James W. N Engl J Med 2005;352:1463-1472
Medications for the Treatment of Acne
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James W. N Engl J Med 2005;352:1463-1472
Medications for the Treatment of Acne
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Rodriguez-Cavallini,Vargas Dengo. Etiología bacteriana y susceptibilidad a antibióticos en pacientes con acné.Rev. Biomed 2004;15:101-106
n= 46
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Rodriguez-Cavallini,Vargas Dengo. Etiología bacteriana y susceptibilidad a antibióticos en pacientes con acné.Rev. Biomed 2004;15:101-106
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AbsorciónAbsorción
AluminioCalcio
MagnesioHierro
Sucralfato
Tetraciclinas Interacciones
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Tetraciclinas Interacciones
BarbituratosFenitoína
Carbamazepina
T ½Tetra-doxi
BarbituratosFenitoína
Carbamazepina
T ½Tetra-doxi
Tetra-doxi Efecto
WarfarinaDigoxina
Tetra-doxi Efecto
WarfarinaDigoxina
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Efectos Secundarios
Sanford p. 86
Categoría D