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James Med chem Mod 6
mod 6
30
Chemistry
Graduate
12/01/2016

Additional Chemistry Flashcards

 


 

Cards

Term

stomach pH

 

 

 

Intestine pH

Definition

stomach pH: 2-6

 

 

 

Intestine pH: 6-8

Term
Most rx absorption in
Definition
small intestine
Term
Passive must be
Definition

less than 4 angstroms

 

less than 200 molecular weight

Term
Log S is the solubility in water
Definition
Log S greater than -4 is soluble in water
Term
SLC
Definition
SOLUTE CARRIER PROTEIND (UPTAKE AND EFFLUX)
Term
ABC
Definition
ATP BINDING CASSETTE PROTEINS(efflux)
Term
slc FAMILY
Definition

OAT [ORGANIC ANION TRANSPORTER]

OATP [ORGANIC ANION TRANSPORTER PROTEIN]

OCT[ORGANIC CATION TRANSPORTERS]

MATE [MULTIDRUG AND TOXIN EXTRUSION] 

Term
OATP FOUND WHERE
Definition

ON APICAL SIDE OF ENTEROCYTE

 

[INHIBITOR: GRAPEFRUIT,Ornge juice]

 

[SUBSTRATE: FEXOFENADINE]

Term
OAT1 [FOUND WHERE]
Definition

IN KIDNEY TUBULES

 

UPTAKE OF GLYCINE CONJUGATES FROM BLOOD INTO KIDNEY

 

Term
WHAT DRUG INHIBITS OAT1
Definition

PROBENECID

 

 

[OAT1 Substrate: P-aminohippurate]

Term
OCT (ORGANIC CATION TRANSPORTER)[WHERE FIND]
Definition

TAKES UP DRUG FROM BLOOD INTO HEPATOCYTE(LIVER)

 

[Substrate: METFORMIN]

 

[Inhibitor: Cimetidine]

Term

 

MATE [FIND WHERE]

 

 

Definition

LIVER AND KIDNEY

 

TAKES CATIONS OUT[EFFLUX]

SLC

 

[from hepatocyte to bile, kidney to urine]

 

ex:metformin

Term
MATE INHIBITOR
Definition

CIMETIDINE

 

[also an OCT inhibitor]

Term
ABC REQUIRE________
Definition
ATP
Term
MATE DISCOVERED FIRST IN
Definition

CANCER CELLS

[TOO MUCH EFFLUX PROTEIN CAUSES MULTI DRUG RESISTANCE] 

Term
MDR1 (MULTI DRUG RESISTANCE PROTEIN 1)
Definition

AKA p glycoprotein[usually passive lipophilic dif]

 

EFFLUX PROTEIN 

(IN INTESTINE)

 

LIMITS DRUG ABSORPTION IN ENTEROCYTES

Term
MDR1 RECOGNIZES______ AND _____ DRUGS
Definition

NEUTRAL AND WEAKLY CATIONIC

 

[SUBSTRATES ARE BULKY]

Term

MDR1 SUBSTRATES 

(BULKY ISH)

Definition

LABETOLOL

LOPERAMIDE

 

Term
MDR1 INHIBITOR
Definition

VERAPAMIL

 

[USUALLY USED AS A TEST TO SEE WHATOTHER DRUGS BIN P GLYCOPROTEIN]

Term
ANION EFFLUX PROTEINS (2)
Definition

MRP2 =MULTI DRUG RESISTANT PROTEIN 2

BCRP= BREAST CANCER RESISTANT PROTEIN

Term

mrp2 (MULTI-DRUG RESISTANCE PROTEIN 2)

 

(FOUND WHERE)

Definition

LIVER, BRAIN, INTESTINE,KIDNEY (*bilk mneumonic)

 

 

Term

mrp2 (MULTI-DRUG RESISTANCE PROTEIN 2)

 

SUBSTRATES<<

Definition

INDINAVIR

CISPLATIN

ACETAMINOPHEN GLUCURONIDE

Term

bcrp (BREAST CANCER RESISTANCE PROTEIN)

 

FOUIND WHERE????(*PILB mnuemonic)

Definition

PLACENTA

INTESTINE

LIVER 

BREAST

Term

bcrp (BREAST CANCER RESISTANCE PROTEIN)

SUBSTRATES......

 

 

 

 

 

effluxed several cancer drugs(first found in mdr breast cancer cells)

Definition

estrone sulfate

 

methotrexate

Term
ABC FAMILY ?
Definition

MDR1

MRP2

BCRP

Term
SLC FAMILY?
Definition

OAT

OATP

OCT

MATE(EFFLUX)

Term
LIPID SOLUBLE DRUGS(5)
Definition

JANITOR    (*mops p  MNEUMONIC)

 

Morphine

Ondansetron

Prednisone

Simvastatin

Pentobarbital (most of barbiturates)

Term
UPTAKE transporters (*OOO mnuemonic)
Definition

OAT1
OATP 

OCT

Term

Paracellular drugs (water soluble)

 (MAA*)

Definition

Metfromin

Acetaminophen

Aspirin

Term
Efflux Transporters(MMMB*)
Definition

MATE

MDR1

MRP2

BCRP

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