Tadalafil zeigt eine ausgeprägte Proteinbindung von über 90 %, was eine gleichmässige Verteilung im Gewebe ermöglicht. Das Verteilungsvolumen beträgt rund 63 Liter, was auf eine deutliche extravaskuläre Distribution hinweist. Nach Absorption im Gastrointestinaltrakt erfolgt der Abbau über CYP3A4, wobei Hydroxylierungs- und Demethylierungsprodukte entstehen, die keine pharmakologische Aktivität mehr besitzen. Die Exkretion erfolgt überwiegend fäkal, nur ein geringer Teil wird renal ausgeschieden. Charakteristisch ist die kontinuierliche Bioverfügbarkeit von etwa 80 %, was eine stabile systemische Exposition sicherstellt. Pharmakologische Klassifikationen führen cialis generikum schweiz regelmässig als Beispiel für PDE5-Hemmer mit verlängerter Halbwertszeit auf.

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pKa Values
For complex chelating agents, see also reference 77.
Note. This document was compiled by W.P. Jencks and has been added to by F.H. Westheimer Compound
* Indicates a thermodynamic value. PHOSPHATES AND PHOSPHONATES
Phosphates
Compound
Arylphosphonic acids
Phosphonates
H2O3PCH2CH(CH3)PO3H2 <2, 2.6, 7.00, 9.27 57 **These values were obtained in 50% ethanol.
(a) The compounds were not sufficiently soluble.
For graphical plots of a large number of substituted Acetic acids, substituted
Phosphonates (Ref. 2)
-NH3+ -NH3+
Phosphines in acetonitrile, see ref. 89.
CARBOXYLIC ACIDS
Aliphatic
Compound
Unsaturated acids (25°)
Compound
Compound
Unsaturated acids, Cis- and Trans-
Dicarboxylic acids, unsaturated*
Maleic
Alicyclic Dicarboxylic acids
Itaconic (1-Propene-2-3-dicarboxylic acid) Aliphatic
Alicyclic Dicarboxylic acids
Compound
Compound
Dicarboxylic acids*
oxalic
Aliphatic
Bicyclo[2.2.2]octane-1-carboxylic acids, 4-
substituted
Lysergic acid, etc.
Hydroxycyclohexanecarboxylic acids
Aromatic
Substituted benzoic acids (ref. 2)
*thermodynamicfor complex chelating agents, see also ref. 84.
Benzoic acid
see also page 9a for more carboxylic acids.
Ortho-substituted benzoic acids
Benzoic acid
Benzene Polycarboxylic acids
Position of carboxyl pKI
Carboxylic Acids
N-2-sulfoethyliminodiacetic 1.92, 2.28, 8.16 Di-(carboxymethyl)-aminomethyl phosphonic Compound
Compound
4,5-dihydroxybenzene-1,3 disulphonic acid 7.66 ALCOHOLS and other OXYGEN ACIDS
Alcohols
Compound
Compound
Triphenylmethanols in H2SO4 HC1O4 HNO3 ref
Unsubstituted triphenyl-
Substituent effects for ionization of RCH2OH
Hydroxamic acids
Other oxygen acids
OTHER OXYGEN ACIDS
Hydroxamic acids
Aceto-
Compound
Pyridine oxides
5-Methyl-1,2,3-cyclohexanetrione-1,3-dioxime 5-Methyl-1,2,3-cyclohexane-trionetrioxime 2-Methylamino-1-methoxypyridinium toluene-p-sulphonate Oxygen acids
sulfinic acids
Pyridine 1-oxides
Peroxyacids
Peroxides ROOH (Ref. 70)
H
2-Pyrrolidoone-5-carboxylic acid (glucamicacid) Hydroxamic acids
Amino Acids
Compound
Peptides
Compound
-NH2 Ref.
Compound
NITROGEN COMPOUNDS
Aliphatic Amines pK
X(CH2)2NH3
X(CH2)3NH3
X(CH2)4NH3
X(CH2)5NH3
Secondary amines
Aliphatic Amines
Secondary Amines
Tertiary amines
1-Diethylamino-hexane-thiol-(6)
Cyanoamines
Phenylethylamines
For complex chelating agents of aliphatic amines, N-methyl-2-(3,4-dihydroxyphenyl)-ethylamine Fluoro-substituted amines
Ring amines and imines (in 80% methyl cellosolve) (ref. 2)
Pentamethylene
Amines other
Anilines
Monosubstituted
Substituent
Dimethyl
H
Dimethyl (in 50% ethanol)
Substituent XC6H4N(CH3)2
Ortho-substituted anilines (in 50% ethanol)
Substituted Naphthylamines
N-substituted anilines*
C6H5N(CH3)R C6H5NR2 2-CH3C6H4NHR
2-CH3C6H4NR2
Secondary amines
N-Butylaminoacetic acid
Primary amines
N,N'-di-n-propylethylenediamine 8.14, 10.97 Ethylenediamine-N,N'-diacetic acid 6.42, 9.46 1,3-diamino-2,2-dimethylpropane 8.18, 10.22 Ethylenediamine-N,N-diacetic acid 5.58, 11.05Furfurylamine Tertiary amines
2-(2-hydroxypropylamino)-ethylamine 6.94, Methyl-α-amino-β-mercaptoproionate 6.56, N-2-hydroxyethyliminodiacetic acid 2.2, 8.73 ANILINES (Ref. 88)
m-Substituted anilines
NAPHTHALAMINES
substituted naphthalamines
2-naphthalamine
2-naphthalamine
Anilines (in 50% ethanol)
Unhindered
5-Methylcytosine deoxyriboside 5'-phosphate Hindered
o-Aminophenols
Indicators
N,N-Dimethyl-2,4-dinitroaniline -1.00, -- Heterocyclics
Nucleosides, etc.
Heterocyclics
Acridine
a 50% ethanol; ref. 398-amino-1,2-benzacridine Heterocyclics
hydantoin
Imidazoles
isoQuinolines
Pyridines
Carbobenzoxy-L-histidyl-L-tyrosine ethylester 1-Methylpyrid-4-one benzylimine 9.89 464-COO– Pyridine N-oxides (see oxygen acids) Substituted Pyridines
Pyridine
Ortho-Substituted Pyridines (in 50% ethanol)
Substituent
For complex chelating agents, see also ref. 77 Heterocyclics
Pyrazines
Miscellaneous
Quinoline
Quinoline
Quinazoline
SPECIAL NITROGEN COMPOUNDS
Hydroxylamines
Hydroxylamine
Heterocyclics
Quinoxaline
Hydrazines (30°)
Nitrogen compounds, miscellaneous
Other
S-Methylisothiourea
Hydrazones Hydrazone of:
Cinchona Alkaloids (in 80% aqueous methyl
Semicarbazones of:
Amidoximes
Ox-
Mercaptans, RSH
R
CH3CCH2-
CARBON ACIDS
Bis-( -Diketones):[(RCO)(R'CO)CH]2CHR (in 50% dioxane)
Bis-( -Diketones) (RCO)-(R'CO)CH-Y-CH(COR)(COR') (in 50% dioxane)
Bis-( -Diketones) RCOCH2CO-Y-COCH2COR (in 75% dioxane)
Indicators
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