Extent of Absorption

More documents

Recommendations

Info

• The activity of drug metabolizing enzymes is dependent on numerous factors • Species • Age (activity is generally lower in very young and aged animals) • Sex (activity is generally higher in males than in females) • Genetics (remember slow versus fast acetylators) • Organ (activity of many enzymes is highest in the liver) • General health status (e.g., hepatic injury decreases metabolic activity in the liver) • Diet (remember how fasting decreases the amount of glutathione available for GST) • Previous exposure to other compounds ٨١
• Induction – an increase in the activity of one or more enzymes as a result of previous exposure of the organism to compounds that serve as substrates for the enzyme(s) • Classic example of an inducer is phenobarbital, , which induces the activity of cytochrome P-450 enzymes • Induction may involve either increases in the synthesis of enzymatic protein, or increases in activation of proenzymes. • Induction may result in increases in the amount of cellular protein, hypertrophy (increases in size) of the cells, and increases in weight of the affected organs (especially liver). • One effect of induction of microsomal enzymes is an increase in the amount of smooth endoplasmic reticulum in a cell. This can be seen microscopically. ٨٢
Page 1 and 2:
Extent of Absorption The extent of
Page 3 and 4:
٢٠
Page 5 and 6:
Calculation of Bioavailability The
Page 7 and 8:
2. Distribution Distribution is the
Page 9 and 10:
The rate of distribution is indicat
Page 11 and 12:
4. Effect of pH The pH of the blood
Page 13 and 14: Lipid-soluble compounds frequently
Page 15 and 16: The parameter used to reflect the e
Page 17 and 18: when a chemical shows a more extens
Page 19 and 20: Elimination The parameter most comm
Page 21 and 22: The mechanisms of elimination depen
Page 23 and 24: If a chemical undergoes metabolic a
Page 25 and 26: The best measure of the ability of
Page 27 and 28: It is measured from the total amoun
Page 29 and 30: Measurement of dose/AUC for an oral
Page 31 and 32: Summary of Toxicokinetic Parameters
Page 33 and 34: • Example - If you know that 3 mg
Page 35 and 36: • Clearance (Cl( Cl) • A ratio
Page 37 and 38: • Half-life life (t 1/2 1/2 ) •
Page 39 and 40: • Classical toxicokinetics • On
Page 41 and 42: • Two compartment model • The e
Page 43 and 44: Chronic Administration The kinetic
Page 45 and 46: ٦٢
Page 47 and 48: Because the plasma and therefore ti
Page 49 and 50: In simple mathematical terms this m
Page 51 and 52: • Example: Cholinesterase is an e
Page 53 and 54: • Types of Biotransformation Reac
Page 55 and 56: • Anything that affects the activ
Page 57 and 58: • Phase II reactions • Involve
Page 59 and 60: • Acetylation • Replacement of
Page 61 and 62: • Significance of Biotransformati
Page 63: • Another good example - metaboli
Page 67 and 68: • Inhibition - a decrease in the
Page 69 and 70: Factors affecting metabolism 1. Age
Page 71 and 72: 4. Excretion • Excretion • The
show all

Extent of Absorption

You also want an ePaper? Increase the reach of your titles

Delete template?

Save as template?