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Flashcards in Pharmacology principles Deck (22):
1

Minimum effective concentration

Concentration of the drug needed for the drug to have an effect on the body. (critical concentration)

2

Maximum tolerated concentration

The maximum concentration of a drug that can be tolerated by the body without any adverse effects

3

Clearence

Volume of plasma cleared of the drug per unit of time

4

First order kinetics

The rate of elimination is directly proportional to drug concentration

5

Zero order kinetics

The rate of elimination is not proportional to drug concentration.

6

Rate of elimination is a product of?

Plasma concentration and clearence

7

Steady state

Rate of elimination=rate of administration

8

IV dosing to steady state graph

Smooth curve up and plateauing when it reaches steady state.

9

Oral dosing to steady state graph

Fluctuates around steady state because you are not constantly being given the drug.

10

Volume of distribution

The volume into which a drug appears to be distributed with a concentration equal to that of plasma

11

Polar metabolites are more readily excreted. True or false.

True

12

Phase 1 metabolism

Adding a chemically reactive handle via oxidation, reduction or hydrolysis. Making the drug more polar.

13

Phase 2 metabolism

Adds an endogenous compound increasing the polarity e.g. glucorindation

14

CYP450 mono-oxygenases

Family of haem proteins located in the endoplasmic reticulum of liver hepatocytes. They mediate phase 1 reactions.

15

In CYP3A4, what do the 3,A and 4 represent?

3- gene family
A- gene subfamily
4- individual gene.

16

What do phase 2 reactions usually result in, where do they occur and give an example?

They usually result in inactive products. It occurs in the liver and an example is glucorindation. This is the adding of glucuronic acid to electron rich atoms on the substrate.

17

Renal excretion via filtration

Only unbound drugs can pass through the glomerulus. Have to have a molecular weight of less than 20,000.
Clearance by filtration= glomerular filtration rate x fraction of unbound drug

18

Two transporters that transport drugs into the nephron

Organic anion transporter and organic cation transporter.

19

Pro's and cons of OAT or OCT

Pro's- protein bound drugs can be excreted.
Con's- They are saturable. Substances may compete with each other

20

Give examples of what the organic anion transporter may excrete

Acidic drugs e.g. penicillin, uric acid, thiazides

21

Give examples of what the organic cation transporter may excrete

Basic drugs e.g. morphine

22

Factors that influence reabsorbtion

Lipid solubility- higher the lipid solubility- more reabsorption
Polarity- more polar, more likely it it to be excreted
Urinary flow rate
Urinary pH- more acidic- basic drugs will be excreted. More basic- acidic drugs will be excreted