Documenti di Didattica
Documenti di Professioni
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Ácido Araquidónico
COX-1
5-Lipooxigenasa
Ciclooxigenasa
COX-2
5-HETE
12-Lipooxigenasa 15-Lipooxigenasa
TXB2
Tromboxano
LT A4 Sintetasa
PROSTANOIDES
LT C4 LT B4
SNC
LT D4 PGI2 Endotelio
Riñón
LT E4 Plaquetas
Bronquios
Piel
Macrófagos
PGD2 PGF2
Bronquios Neutrófilos
Eosinófilos
Fosfolípidos de membrana
AG /
AC
Fosfolipasa A2
Ácido Araquidónico
O2
5-Lipooxigenasa
5-HETE
H2O
LTA4 -Hidrolasa
LT A4
Glutation
LT B4 LT C4 Bronquios
Ac. Glutámico Glutamil transpeptidasa Piel
Macrófagos
LT D4
Bronquios Neutrófilos
Glicina Cisteinil-glicina dipeptidasa
Eosinófilos
LT E4
LEUCOTRIENOS
Leucotrieno B4 (LTB4) y
Cisteinil leucotrienos (LTC4, LTD4 y LTE4).
LEUCOTRIENOS
Cisteinil - Leucotrienos ( CysLT )
MONTELUKAST
Es el único antileucotrieno cuyo uso es aprobado en niños desde los seis años de edad. Se
administra una vez al día, vía oral, con la ventaja que su biodisponibilidad no es afectada por
los alimentos en los adultos y mínimamente afectado en los niños.
No inhibe las isoenzimas CYP2C9 y CYP3A4 del citocromo P450 con lo que presenta muchas
menos interacciones con otros fármacos.
ANTILEUCOTRIENOS
Farmacocinética:
Concentraciones plasmáticas máximas entre las 2.5- 4 horas.
Actúa solamente sobre los receptores CysLT1, no antagonizando las contracciones del músculo
liso producidas por la acetilcolina, la histamina, la serotonina o las prostaglandinas.
Eliminado, conjuntamente con sus metabolitos, casi exclusivamente por vía biliar.
ANTILEUCOTRIENOS
MONTELUKAST
La dosis recomendada:
Adultos: 10 mg / día
Niños 6-12 años: 5 mg/ día
Menores de 6 años: 4 mg/ día
INDICACIONES DEL MONTELUKAST
MONTELUKAST
Method:
Randomized, double blind, placebo-controlled crossover trial with washout period,
conducted from May 2002 to February 2006. The study involved 25 patients, 2-16 years old
with dermatitis, receiving montelukast.
Conclusion:
This study showed that montelukast reduces itching, sleep disturbance, disease extent and
severity, blood eosinophil count and serum IgE.
OTRAS EVIDENCIAS CLINICAS:
MONTELUKAST en DERMATITIS ATOPICA
Author(s), Method Duration Subjects Intervention Outcomes Results
Date Measured
Pei, A.Y. Randomized 12 weeks 15 subjects Montelukast 5mg OD Impact of eczema on Statistically significant
(2001)52 double-blind age 6-16 yr vs. placebo daily living (subjective) improvement in severity
placebo-controlled mod-severe AD Disease extent, severity of AD in patients on
crossover study (objective) active treatment
compared with placebo
(p<0.05)
Yanase,D and Randomized 8 weeks 8 subjects Montelukast 10mg OD Clinical severity scores Improvement in:
David-Bajar, K. double-blind, adult (male and vs. placebo (6 signs of AD) • Scaling/dryness
(2001)53 placebocontrolled, female) Continuous adjunctive (p=0.003)
crossover study with AD treatment: emollients, • Lichenification
antihistamines, weak (p=0.009)
topical corticosteroids • Induration (p=0.016)
• Erythema (p=0.024)
• Erosions (p=0.027)
Capella, GL. Randomized 6 weeks 20 males Montelukast 10 mg OD SCORAD index Significant reduction in
(2001)31 double-blind Age range: 18-28 n=10) vs. placebo (n=10) (objective and disease activity
study yr. Severe AD No other treatment for subjective criteria). (measured by SCORAD
(SCORAD index) AD index) in the montelukast
allowed. group compared with
placebo group. (p<0.02)
HIPERTROFIA de ADENOIDES
Montelukast in Adenoid Hypertrophy: Its Effect
on Size and Symptoms
Farshid Shokouhi, Ahmad Meymaneh Jahromi, Mohamad Reza Majidi, Maryam Salehi
Methods: 60 children between the ages of 4–12 years with >75% choanal
obstruction on primary nasal endoscopy were recruited in this randomized, placebo-
controlled trial divided into two groups. The study group was treated with
montelukast 5 mg daily for 12 weeks while the control group received matching
placebo for the same period of time.
Results: Adenoid size decreased in 76% of the study group compared with 3% of
the placebo group after 12 weeks.
Conclusion: Montelukast chewable tablets achieved a significant reduction in
adenoid size and improved the related clinical symptoms of AH and can therefore be
considered an effective alternative to surgical treatment in children with adenoid
hypertrophy.
APNEA OBSTRUCTIVA DEL SUEÑO (OSA)
Montelukast for Children With Obstructive Sleep
Apnea: A Double-blind, Placebo-Controlled Study
Aviv D. Goldbart, MD, MSc; Sari Greenberg-Dotan, PhD,
Asher Tal, MD
Conclusion:
There is increasing evidence that even mild OSA may be associated with significant cognitive,
behavioral, and vascular morbidity. This sequel may have a major impact on quality of life and
health care costs. The results of this study supported the introduction of a leukotriene modifier as a
novel, safe, therapeutic alternative for the treatment of children with a non-severe form of OSA.
Montelukast potentially efficacious in children with non-
severe obstructive sleep apnea in the short term
Joanna E MacLean
Method: Tympanometry and spectral gradient acoustic reflectometry were used to confirm the effusion of otitis media in
patients between 2 and 12 years of age. Patients were treated with amoxicillin for 10 days and montelukast sodium or placebo
for 30 days in a random, double-blind manner. Sixty patients completed the study: 31 received placebo and 29 received
montelukast sodium. At a 4-week follow-up visit, 5 ears (16%) were free of effusion in the placebo group and 17 (58%) in the
montelukast sodium group.
Conclusions:
The difference was significant. The efficacy of montelukast sodium in clearing the effusion was 58%.
PMID: 15248005
Improvement of otitis media with effusion after treatment of asthma with leukotriene
antagonists in children with co-existing disease.
Balatsouras DG , Eliopoulos P , Rallis E , Sterpi P , Korres S , Ferekidis E Department of Otolaryngology, Tzanion General
Hospital, Piraeus, Greece. Drugs Under Experimental and Clinical Research [2005, 31 Suppl:7-10]
Objective:
The aim of this study was to evaluate the impact of leukotriene inhibitor therapy for asthma on the clinical course of OME in children with co-existing
disease.
Method: Comparative study. Fifty children with bilateral OME and asthma, divided equally into two groups, were studied. The children in the first group
were treated with budesonide and terbutaline inhalers together with the leukotriene inhibitor montelukast, whereas the children in the second group were
treated with the inhalers alone. Duration of treatment was 30 days. Pneumatic otoscopy, tympanometry and pure-tone audiometry were performed at the
beginning and at the end of treatment.
Results: Fifteen (60%) of the children receiving inhalers and montelukast and nine (36%) of those receiving only inhalers were found free of OME after 30
days of therapy.
Conclusion: Thus, it may be concluded that a statistically significant beneficial effect on the clinical course of OME resulted from the addition of
montelukast to the treatment of children with co-existing asthma and OME.
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