Pharmacology lecture 6

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What is enterohepatic recirculation?
Where drugs hat have been eliminated in the bile can be reabsorbed in the GI tract
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Drugs with.................... and/or........... degree of................ to.......... .............. will tend to stay in systemic circulation
high Mr, high, binding, plasma proteins
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What are the two main binding proteins?
Albumin, Alpha 1 acid glycoprotein
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Where is albumin produced?
Liver
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What does albumin bind?
acidic drugs
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What does albumin cause?
DECREASE in malnutrition and cirrhosis
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What are the normal ranges of albumin in the blood?
3.5-5 g/dL
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Where is alpha 1 acid glycoprotein produced?
Liver
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What does alpha 1 acid glycoprotein bind?
Basic drugs
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What are the normal ranges of alpha 1 acid glycoprotein in the blood?
0.4-1.1 mg/ml
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If there are LARGE amounts of drug binding proteins in the blood...
LOWER DISTRIBUTION because more protein bound to drug
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If there are SMALL amounts of drug binding proteins in the blood...
more DRUG to TISSUE because less bound to protein
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What are the Phase I drug metabolising enzymes?
Cytochrome P450 family
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What are the Phase II drug metabolising enzymes?
UDP-glucuronosyltransferases
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What is the goal of drug metabolising enzymes?
Make a drug more water-soluble to be excreted in the urine (metabolite)
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What do prodrugs contain?
They contain an ester group which are hydrolysed in vivo
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How do you calculate volume of distribution?
Vd = total amount of drug in body/ drug blood plasma concentration (time 0)
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Ke =
gradient of the log-transformed concentration-time profile (elimination rate constant)
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How do you eliminate volatile gases?
Exhalation
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How do you eliminate water-soluble drugs?
Urine/bile
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How do you eliminate lipid-soluble drugs?
change to water-soluble then out via urine/bile
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What is the half-life?
time it takes for concentration of a compound to reach 50% of its current value
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Half life =
0.693/Ke
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How do you calculate total clearance?
Total Cl = Hepatic Cl + Renal Cl + other Cl
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What is clearance?
volume of plasma cleared of compound per unit of time
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Clearance: IV dosing
Cl= IV dose/IV AUC
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Clearance
Cl = Dose x F / Oral AUC
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Other cards in this set

Card 2

Front

Drugs with.................... and/or........... degree of................ to.......... .............. will tend to stay in systemic circulation

Back

high Mr, high, binding, plasma proteins

Card 3

Front

What are the two main binding proteins?

Back

Preview of the front of card 3

Card 4

Front

Where is albumin produced?

Back

Preview of the front of card 4

Card 5

Front

What does albumin bind?

Back

Preview of the front of card 5
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