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Farida
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PT
PT TANABE
TANABE INDONESIA
INDONESIA
Drug Information
INDICATIONS
- Allergic Rhinitis
- Urticaria
DOSAGE and
ADMINISTRATION
Lymphocyte
TALION
(Inhibition of
IL-5 Production
Cytokine
Production
IL-5
, IL4
TALION
(H-1 Antagonism)
TALION
(Inhibition of Eosinophil
Infiltration)
Microvasculature,
Sensory Nerve
Eosinophil
Eosinophil Infiltration
Allergic
Symptoms
Allergic Rhinitis
Urticaria, etc.
Vasodilation,
Enhanced Vasopermiability,
Excitement of Nerve
TALION
FAST ACTION
Desloratadine
3 hours
(Aerius)
TALION
Cetirizine
Levocetirizine
Fexofenadine
(Ryzen)
1 hours
(Xyzal)
2.6 hours
(Telfast))
Loratadine
(Claritin)
0.0
0.5
1.0
1.5
2.0
2.5
3.0
3.5
4.0
4.5
(Hours)
TALION
Non Sedating Antihistamine
H1
occupation
rate in brain
PET
images
(subjects: 8 normal 8
adults)
PET
placebo
Bepotastine
Diphenhydramine
MRI-T1
p< 0.001
56.4%
14.7%
Bepotastine
Diphenhydramine
TALION
was
confirmed
to be classified as NON 20%
SEDATING
Antihistamine
CONGA
defined
by CONGA (Consensus Group on New Generation Antihistamine :
H1-RO less than 20%)
Tashiro M, et al : British Journal Clinical Pharmacology, 65(8), 2008
TALION
High Selectivity to Histamine H1 Receptor
H1
-9
-8
-7
-6
H3
Bzd
1
H1
-9
-8
-7
-6
Bzd
H3
1
-9
-8
-7
-6
H3
1
H1:Histamine H1,
2
5-HT
5-HT
5-HT
Triludan
Bzd
H3
1
5-HT
:Adrenergic ,
D2L:Dopamine D2L,
H1
-9
-8
-7
-6
2:Adrenergic 2,
600nM
H1
-9
-8
-7
-6
Triludan
Terfenadine
52nM
H1
1:Adrenergic 1,
L
Fexofenadine
TALION
101nM
Bzd
Bzd
H3
1
5-HT
H3:Histamine H3,
-9
-8
-7
-6
H3
5-HT2: Serotonin 2,
1
M:Muscarinic,
Bzd:Benzodiazepine
5-HT
D
L
Zaditen
Ketotifen
2.2nM
Cetirizine
(253nM
Zyrtec
Alesion
Epinastine
3.6nM
Wheal areas
150
100
50
0
50%
TALION 10 mg
1%
0 1
10 12
15
Placeb
o
20
25
(hours)
Mean
n=10
Anti-inflammatory Actions
of
TALION
Rate of Suppression of
IL-5
Production
(%)
100
**
80
Ketotifen
Cetirizine
60
TALION
TALION
( Zyrtec)
Zyrtec)
**
40
20
(Zaditen
(Zaditen))
**
**
**
MeanS.E.
n36
**
Paired t test
** p<0.01
20
0.1
10
Drug Concentration
100 (M)
(O. Kamimura et al.: Biolo ical & Pharmaceutical Bulletin 21 4 411 1998
TALION
Not have Drug-to-Drug Interaction
Drug Interaction
- Erythromycin, Cimetidine, Ketokonazole
- CNS depressant, Alcohol CNS depressant effect may be enhanced
- Amiodarone --> increase Loratadine serum concentration
Desloratadine
Bepotastine
TALION
No Report
Drug
Interaction
No Drug
Interation
Cetirizine
Levocetirizine
Fexofenadine
TALION
Not have Drug-to-Food Interaction
10%
Twice daily
Once daily
(Remicut)
Loratadine
After meal
(Claritin)
(Azeptine)
Epinastine
Cetirizine
(Alesion)
(Zy
(Zyrtec)
rtec)
Olopatadine
Tendency
Twice daily
Once daily
No description
Tendency, 10%
Once daily
Before bedtime
Twice daily
(Allelock)
(Allegra)
Once
Once daily
No description
Not influenced
Twice daily
No description
32
Metabolism
2)
At dosages of 10 mg
: little metabolites were detected in plasma and urine
At dosages of 20 mg or more : metabolites detected in urine 1% of the original dosages
Excretion
3)
(%)
100
80
60
40
20
0
(hours)
02 4
10
24
Time
1 R. Ohashi et al.: Pharmacokinetics 12 (5), 417, 1997
2 T. Kadosaka et al.: J Clin Therap Med 13 (5), 1155, 1997
3) H. Yokota et al.: J Clin Therap Med 13 (5), 1137, 1997
Shelf Life :
3 years
Packaging :
TALION
CLINICAL STUDIES
Bepotastine Downregulates
The Production of Th1 & Th2 Chemokines :
Its Beneficial Effect on Acute and Chronic Atopic Skin Lesions
(Kobayashi, et al.: Skin Pharmacol Physiol 2009; 22 : 45-48)
Substance-P
Serotonin
Leukotriene
Serotonin
Substance-P
VH = Vehicle
BB = Bepotastine Besilate
Leukotriene
*P<0.05 when compared
with VH
Methods
;
;
434 pts
10
20
Chronic urticaria
n=250)
Eczema/dermatitis
n=103
Prurigo
n=41
30
40
50
60
49.6
70
26.8
32.0
31.1
80
90
12.0
22.3
10.4
1.2
10.7
3.9
19.5
53.7
9.8
37.5
9.8
7.3
100
22.5
25.0
15.0
Remarkably
Improved
Moderately
Improved
Slightly
Improved
Not
changed
Aggravate
d
(Y. Ishibashi et al.: J Clin Therap Med 13 (5) 1199, 1997/13 (5) 1237, 1997/13 (5) 1287, 1997/13 (5) 1383, 1997)
Kriteria Penilaian
Kriteria Penilaian
Methods
10
20
30
40
50
60
62.0
70
80
25.4
Moderately
Improved
Slightly
Improved
Not changed
90
100
9.9
n=71
1.4
1.4
Worsening
In general, the global improvement rate at 12 week treatment would be the final global
improvement rate.
Y. Ishibashi et al.: J Clin Therap Med 13 5 ,1337,1997
Skin Disease
Results/Clinical Study
(Long-term Treatment Study-2)
1 week n=63
2 weeks n=71
4 weeks n=68
10
20
30
20.6
40
50
60
70
41.3
100
11.1
1.6
43.7
28.2
47.1
6 weeks n=63
8 weeks n=64
16.2
1.5 1.5
17.5
38.1
37.5
12 weeks n=60
90
25.4
10 weeks n=57
80
10.9
3.1
35.1
8.8
3.5
26.7
10.0
Moderately
Improved
Slightly
Improved
Not changed
Aggravated
Clinical Studies
(Double-blind placebo-controlled comparative study)
Subjects : Chronic Urticaria
TALION group: 55 cases , Placebo group : 54 cases
Methods The double blind comparative study was carried out using 10mg (b.i.d) of TALION and
Placebo (b.I.d.) for one week. Degrees of itching and of eruption (wheal/erythema) were
judged based on the patients diaries.
Score of itching : The higher score between day and night was adopted
Score
Excruciating itching
(not allowing housework or job.)
Considerable itching
(irritated and hard to concentrate
on housework or my work.)
Feeling itchy
(not so concerned, but sometimes
scratching myself unconsciously.)
Score
Degree of Eruption
(Dermal Symptom)
Severe in appearance
(swelling is recognized and
redness is distinct from the
surrounding area)
No symptoms
Severe in appearance
(Swelling is recognized and redness can be
distinguished from the surrounding area)
No symptoms
( M. Kawashima et al.: J Clin. Therapy Med 18 (4), 501, 2002)
2.5
2.70
2.0
TAON
-1.42
1.5
*
2.56
2.33
Placebo
-0.41
2.30
2.0
Placebo
- 0.14
Itching
3.0
2.75
2.5
2.70
TAON
-1.31
1.5
1.02
1.0
0.5
Day 3
1.5
TAON
-1.62
1.13
2.30
0.0
Day 1
TALION group n = 55
Placebo group n = 54
*
Placebo
-0.47
Day 3
TAON
-1.49
1.0
0.84
0.5
0.5
0.0
Day 1
Placebo
-0.14
2.0
2.33
1.83
1.0
0.0
2.56
Eruption
2.0
1.0
0.5
2.5
1.89
1.5
1.33
Eruption
Score
s
2.75
2.5
Score
s
Itching
3.0
Scores
Scores
0.0
Day 1
Day 7
Day 1
Day 7
THANK YOU
Almost satisfied
45.4%
0%
20%
44.1%)
40%
60%
Dissatisfied
10.5%)
80%
100%
Incidence of
Adverse reaction
Special Surveillance
for child patients
1.1% (14/1,316)
58
(ng/mL)
Plasma Concentration
80
CCr = 51 70 mL/min
M/S = 66.3
M = 61
60
N = 55.1
T1/2 = 3 hours
Moderate to severe impairment n=6
CCr = 6 50 mL/min
40
20
0
0
12
18
24
hours
Plasma Concentration
(ng/mL)
120
at the 1st
administration
at the 3rd
103.8
100
82.9
day
MeanS.D.
n=10
80
60
40
17
20
15
(hours)
12
18
24