0516-MAD-01 Madopar HBS Roche Capsules 125 mg 125 Capsules Italy 250 Tablets Roche 100/25 017077 100/25 () 025352 200/50 009796 Levodopa + benserazide 1. 1.1 / ATC : N04BA Madopar levodopa benserazide 1.2 : Madopar Madopar 125 Madopar Madopar 250 : Madopar HBS (Hydrodynamically Balanced System ) Madopar 125 1.3 1.4 Madopar levodopa benserazide() 4 1 Madopar 125 = levodopa 100 + benserazide 25 1
Madopar 250 = levodopa 200 + benserazide 50 100/25 hypromellose hydrogenated vegetable oil calcium hydrogen phosphate mannitol talc povidon magnesium stearate gelatin titanium dioxide (E171) yellow iron oxide (E172) indigo carmine (E132) 100/25 () microcrystalline cellulose talc povidon magnesium stearate gelatin iron oxide red (E172) titanium dioxide (E171) indigo carmine (E132) Printing ink: shellac, dehydrated alcohol, isopropyl alcohol, butyl alcohol, propylene glycol, purified water, strong ammonia solution, potassium hydroxide, black iron oxide (E172) 200/50 mannitol calcium hydrogen phosphate microcrystalline cellulose pregelatinised maize starch crospovidone ethylcellulose colloidal anhydrous silica docusate sodium magnesium stearate red iron oxide ci 77491 2. 2.1 Madopar HBS ( peak dose dyskinesia end of dose deterioration ) 2.2 Madopar Madopar HBS Madopar Madopar 30 1 Madopar 2
Madopar 125 3-4 300-800 levodopa 75-200 benserazide 3 4-6 3-6 1 125 Madopar ( 3 ) Madopar HBS Madopar 2.2.1 2.1 Madopar Madopar (on-off phenomena) Madopar HBS Madopar Madopar HBS Madopar 2-3 50% Madopar HBS Madopar HBS Madopar Madopar HBS 2-3 Madopar HBS 250 Madopar HBS ( ) Madopar HBS Madopar 2.3 Madopar HBS levodopa benserazide 3
Madopar (MAO) MAO-B selegiline rasagiline MAO-A moclobemide MAO-A MAO-B MAO Madopar ( 2.4.5 ) Madopar Madopar 25 () Madopar ( 2.5.1 2.5.2 ) Madopar 2.4 2.4.1 levodopa Madopar levodopa halothane Madopar halothane Madopar 12-48 Madopar / Madopar Madopar neuroleptic malignant-like syndrome ( serum creatinine phosphokinase ) Madopar Levodopa levodopa ( ) ( 2.4.3 ) 4
Madopar Madopar 2.4.2 2.4.3 levodopa ( ) ( ) ( 2.4.1 ) 2.4.4 2.4.5 trihexyphenidyl Madopar levodopa trihexyphenidyl Madopar HBS levodopa Madopar HBS levodopa 32% levodopa AUC 30-50% Metoclopramide levodopa Domperidone levodopa reserpine Madopar MAO Madopar MAO Madopar 2 ( 2.3 ) MAO-B selegiline rasagiline MAO-A moclobemide Madopar 5
levodopa MAO-A MAO-B MAO Madopar ( 2.3 ) Madopar ( epinephrine norepinephrine isoproterenol amphetamine) levodopa amantadine selegiline bromocriptine Madopar COMT Madopar Madopar levodopa Levodopa catecholamines Madopar Coombs tests D2 levodopa-benserazide Levodopa halothane : Madopar halothane 12-48 / 2.4.1 ( ). 2.5 2.5.1 Madopar ( 2.3 3.3.4 3.3.5 ) 2.5.2 benserazide Madopar 2.5.3 2.3 6
2.5.4 Levodopa benserazide 10% levodopa levodopa Madopar 2.5.5 Levodopa levodopa 2.6 2.6.1 levodopa Madopar ((choreiform)(athetotic)) freezing episodes on-off Madopar Madopar Madopar 7
gamma-glutamyltransferase Madopar 2.6.1.1 2.6.1 2.7 Madopar 2.6.1 () Madopar Madopar HBS 3. 3.1 3.1.1 Dopamine dopamine Levodopa (INN) L-DOPA (3,4-dihydroxy L-phenylalanine) dopamine Levodopa (dopamine ) dopamine - dopamine - levodopa (CNS), aromatic L-amino acid decarboxylase dopamine levodopa dopamine levodopa dopamine levodopa levodopa benserazide 8
Madopar 4 1 levodopa 3.2 3.2.1 Levodopa Madopar 1 levodopa Madopar Levodopa (AUC) (50-200 levodopa) levodopa Madopar levodopa 30% levodopa 15% Madopar HBS Madopar 3 levodopa 20-30% - Madopar HBS Madopar ( ) Madopar HBS Madopar 50-70% levodopa Madopar HBS (5 ) 3.2.2 Levodopa - 57 Levodopa AUC 12% levodopa benserazide - 3.2.3 Levodopa ( O- ) ( ) Levodopa dopamine homovanillic acid dihydroxyphenylacetic acid Levodopa catechol-o- 9
methyltransferase 3-O-methyldopa 15 Madopar benserazide levodopa levodopa 3-O-methyldopa catecholamines (dopamine noradrenaline) phenolcarboxylic acids (homovanillic acid dihydroxyphenylacetic acid) Benserazide trihydroxybenzylhydrazine 3.2.4 levodopa levodopa 1.5 (65-78 )( 25%) 3.2.5 levodopa 430 / Benserazide (64%) (24%) 3.2.5 levodopa (65-78 ) levodopa AUC (34-64 ) 25% 3.3 3.3.1 Madopar 3.3.2 Ames Madopar levodopa benserazide 3.3.3 Madopar 10
3.3.4 (400 / [600 / 250 / ] [120 / 150 / ]) ( ) / ( ) 3.3.5 4. 4.1 100/25 30 C 200/50 30 C 100/25 30 C 5. 200/50 2~1000 009796 100/25 6~1000 025352 100/25 16-1000 017077 2015 11 CDS 7.0 01.16-MAD-3B01 11
F. Hoffmann-La Roche Ltd. Grenzacherstrasse 124, CH-4070 Basel, Switzerland Roche S.p.A. Via Morelli 2, 20090, Segrate (MI), Italy. F. Hoffmann-La Roche Ltd. : Wurmisweg, CH-4303, Kaiseraugst, Switzerland. 3 134 9 (02) 27153111 Madopar 12