ADME Excretion Flashcards

1
Q

What is Excretion?

A

Removal of the drug (and metabolites) from the body

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2
Q

Where does Excretion primarily occur?

A

The kidneys.

altho a small amount of excretion can occur from the lungs, sweat, saliva etc.

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3
Q

What is Tonal Renal Excretion of a drug?

A

the glomerular filtration, active tubular secretion and tubular re-absorption

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4
Q

what does Glomerular filtration depend on?

A

depends on systemic BP and renal blood flow

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5
Q

Glomerular filtration is a ____ process?

A

Passive

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6
Q

What factors sifnificantly affect a drugs likely hood of being filtered?

A

Molecular size, charge, and protein binding.

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7
Q

Drugs that are very small < 7,000 Da will be?

A

freely filtered weather charged or uncharged

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8
Q

Drugs that are larger (7,000-70,000Da) will be?

A

filtered according to their mass. Drugs larger than 70,000 are less likely to be filtered through the normal glomerulus esp if they carry charge (repelled by neg charge basal cell membrane proteins)

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9
Q

Where does active tubular secretion occur?

A

Proximal Convoluted tubules

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10
Q

In active tubular Secretion…

A

drugs are moved against a concentration gradient using energy dependent. allows a higher concentration to be achieved in the filtrate.

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11
Q

Active tubular secretion allows…

A

ionized drugs and protein-bound drugs to more

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12
Q

Active tubular secretion is subject to?

A

saturation and inhibition

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13
Q

Organic Cation transporters OCT’s move…

A

organic bases

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14
Q

Organic Anion transporters OAT move…

A

Organic acids

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15
Q

Where does tubular rebsorption take place?

A

passive diffusion occurs in the proximal and distal convoluted tubules. Lipid soluable / nonionized drugs have the greatest chance of moving back into circulation

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16
Q

H20-soluble, ionized, polar drugs are…

A

excreted in the urine

17
Q

Acidification of the urine will cause?

A

withe ammonium chloride or methionine.

will cause BASIC drugs to be ionized and enhance their excretion

18
Q

Alkalinization of the Urine…

A

with Sodium bicarb or potassium citrate will cause weak

ACIDS to be ionized and enhance their excretion.

19
Q

What is Hepatic Excretion?

A

typically an active transport of drugs and/or conjugates from the hepatic sinusoids to the BILE canaliculi

20
Q

What type of drugs are more easily excreted in the bile?

A

lipid soluble drugs with MW> 300 and polar group are more easily excreted.

21
Q

what is Enterohepatic circulation?

A

conjugates excreted in the bile can be hydrolyzed in the intestine and the free radicals reabsorbed, prolonging the drugs residence in the body

22
Q

What type of drugs will be trapped in the milk?

A

some weak basic drugs will be ion trapped in the milk (pH ~ 6.7)