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Question 1

CYP1A2 Substrate

Answer 1

in vitro: Phenacetin, Coffein

in vivo: Coffein, Theophyllin

Question 2

CYP3A4 Substrate

Answer 2

in vitro: Midazolam, Testosteron, Dextrometorphan; Erythromycin

in vivo: Midazolam

Question 3

CYP2B6 Substrate

Answer 3

in vitro: Bupropion, Efavirenz

(in vivo: Efavirenz)

Question 4

CYP2C9 Substrate

Answer 4

in vitro: S-Wafarin, Tolbutamid, Diclofenac

in vivo: Losartan

Question 5

CYP2C19 substrates

Answer 5

in vitro: S-Mephenytoin, Omeprazol

in vivo: Clopidogrel

Question 6

CYP2D6 Substrate

Answer 6

in vitro: Dextromethorphan, Metoprolol, Tamoxifen (bzw. N-DesmethylTAM), Debrisoquin

in vivo: Dextromethorphan Metoprolol

Codein

Question 7

CYP2A6 Substrate

Answer 7

in vitro: Cumarin, Nikotin

(in vivo: Nikotin)

Question 8

CYP2E1 Substrate

Answer 8

in vitro: Chlorzoxazone

(in vivo: Chlorzoxazone)

Acetaminophen

Question 9

CYP2C8 Substrate

Answer 9

in vitro: Taxol (Paclitaxcel)

in vivo: Repaglinid
Cerivastatin

Question 10

CYP1A2 Inhibitoren

Answer 10

in vitro: Furafyllin (nicht-kompetitiv)

in vivo: Fluvoxamin (kompetitiv)

Question 11

CYP3A4 Inhibitoren

Answer 11

in vitro: Ketoconazol

in vivo: Clarithromycin, Ritonavir; Itraconazol

Grapefruitsaft, Mibefradil

Question 12

CYP2B6 Inhibitoren

Answer 12

Ticolpidin

Question 13

CYP2C9 Inhibitoren

Answer 13

in vitro: Sulfaphenazol

in vivo: Fluconazol

Question 14

CYP2C19 Inhibitoren

Answer 14

in vitro: Omeprazol (kompetitiv)

in vivo: Omeprazol
(kompetitiv)

Question 15

CYP2D6 Inhibitoren

Answer 15

Paroxetin, Quinidine, (Chinidin)

Question 16

CYP2A6 Inhibitoren

Answer 16

in vitro: Methoxsalen, Trancylpromin (kompetitiv, stereoselektiv)

(in vivo: Trancylpromin)

Question 17

CYP2E1 Inhibitoren

Answer 17

in vitro: Fomepizol (kompetitiv)

in vivo: Fomepizol

Question 18

CYP2C8 Inhibitoren

Answer 18

in vitro: Montelukast

in vivo: Gemfibrozil (Prodrug!)

Question 19

CYP1A2 Induktoren

Answer 19

Rifampicin, Kohlgemüse, gegrilltes Fleisch, Rauchen, Barbiturate, Carbamazepin

Question 20

CYP3A4 Induktoren

Answer 20

Rifampicin, Hyperforin, Efavirenz

Question 21

CYP2B6 Induktoren

Answer 21

Efavirenz, Rifampicin

Question 22

CYP2C9 Induktoren

Answer 22

Rifampicin, Hyperforin, Barbiturate, Carbamazepin

Question 23

CYP2C19 Induktoren

Answer 23

Rifampicin, Hyperforin, Carbamazepin

Question 24

CYP2D6 Induktoren

Answer 24

keine

Question 25

CYP2A6 Induktoren

Answer 25

Rifampicin

Question 26

CYP2E1 Induktoren

Answer 26

Ethanol, Aceton, andere Lösungsmittel

Question 27

CYP2C8 Induktoren

Answer 27

Rifampicin, Hyperforin

Question 28

CYP1A2 Metabolismus von...

Answer 28

Planarer polyaromatischer Amide und Amine

Question 29

CYP3A4 Metabolismus von...

Answer 29

Lipophilen Molekülen unterschiedlicher Struktur

Question 30

CYP2B6 Metabolismus von...

Answer 30

Neutralen bzw. schwach basischen, meist nicht planaren lipophilen Molekülen, welche 1-2 H-Brücken akzeptieren

Question 31

CYP2C9 Metabolismus von...

Answer 31

Sauren lipophilen Molekülen, welche H-Brücken akzeptieren können

Question 32

CYP2C19 Metabolismus von...

Answer 32

Neutralen Substanzen bzw. schwachen Basen wie Amiden, die mind. 2 H-Brücken akzeptieren

Question 33

CYP2D6 Metabolismus von...

Answer 33

Basischen Substanzen, welche ein protonierbares N-Atom aufweisen

Question 34

CYP1A2 Klinisches Beispiel

Answer 34

Theophyllin: Asthma

Question 35

CYP3A4 Klinisches Beispiel

Answer 35

Ritonavir: pharmakokinetisches Boostering (Cobicistat)

Question 36

CYP2B6 Klinisches Beispiel

Answer 36

Efavirenz (Stocrin®): Autoinduktion

Question 37

CYP2C9 Klinisches Beispiel

Answer 37

Wafarin (enge therapeutische Breite)

Question 38

CYP2C19 Klinisches Beispiel

Answer 38

Clopidogrel Prodrug

Question 39

CYP2D6 Klinisches Beispiel

Answer 39

Codein (Giftung)

Question 40

CYP1A2 Metabolismus Phenacetin

Answer 40

Acetaminophen

Question 41

CYP1A2 Metabolismus Coffein

Answer 41

Paraxanthin

Question 42

CYP2B6 Metabolismus Bupropion

Answer 42

Hydroxybupropion

Question 43

CYP2C9 Metabolismus S-Warfarin

Answer 43

7-Hydroxywarfarin

Question 44

CYP2D6 Metabolismus Codein

Answer 44

Morphin (Nebenweg)

Question 45

CYP2E1 Metabolismus Acetaminophen

Answer 45

Acetaminophen -> N-Acetyl-p-benzochinonimin (Giftung)

Question 46

UGT Name & Reaktion

Answer 46

Uridin-Diphosphat-Glukuronosyltransferasen Glucuronidierung

Question 47

SULT Name & Reaktion

Answer 47

Sulfotransferasen Sulfatierung

Question 48

NAT Name & Reaktion

Answer 48

N-Acetyltransferasen Acetylierung

Question 49

MT Name & Reaktion

Answer 49

Methyltransferasen Methylierung

Question 50

GST Name & Reaktion

Answer 50

Glutathion-S-Transferasen Glutathionkonjugation

Question 51

MT katalysiert...

Answer 51

N-, O- und S-Methylierung von Substraten

Question 52

GST katalysiert...

Answer 52

Übertragung von des Tripeptids Glutathion (GSH) auf elektrophile Substanzen

Question 53

UGT Co-Faktor

Answer 53

UDP-Glukuronsäure (UDPGA) (durch Nukleosid-Transporter vermittelt)

Question 54

SULT Co-Faktor

Answer 54

3'Phosphoadenosin-5'Phosphosultat (PAPS) (Sulfatgruppendonator)

Question 55

NAT Co-Faktor

Answer 55

Coenzym A (Acetylgruppendonator)

Question 56

MT Co-Faktor

Answer 56

S-Adenosylmethionin(SAM)(Methylgruppendonator)

Question 57

GST Co-Faktor

Answer 57

Glutathion (GSH) (Tripeptid)

Question 58

UGT Isoformen

Answer 58

UGT1A1, UGT2B7 (wichtigste Bedeutung, überlappendes Substratspektrum)

Question 59

SULT Isoformen

Answer 59

SULT1A1 (wichtigste Bedeutung)

Question 60

NAT Isoformen

Answer 60

NAT1 und NAT2 (überlappendes Spektrum)

Question 61

MT Isoformen

Answer 61

TPMT, COMT, HNMT

Question 61

GST Isoformen

Answer 61

Viele Isoformen

Question 62

UGT Substrate

Answer 62

UGT1A: SN-38 -> SN38G UGT2B: Morphin, Bilirubin

Question 63

NAT Substrate

Answer 63

NAT2: Isoniazid, Sulfasalazin, Sulfapyridin Coffein

Question 64

MT Substrate

Answer 64

6-Mercaptopurin (Azathioprin) (TPMT) Katecholamin (COMT)

Question 65

GST Substrate

Answer 65

NAPQI