PPT-Claire

Question 1

What is a zero order reaction?

Answer 1

If drug is processed by zero order kinetics then change in concentration with time is a fixed amount per time, independent of concentration

Question 2

What is a first order reaction?

Answer 2

The change in concentration at any time is proportional to the concentration present at that time.

Question 3

What is clearance?

Answer 3

Ability of organs to eliminate drugs from blood stream

Question 4

What is bio transformation?

Answer 4

Drug metabolism occurring in 2 phases

Question 5

What is preconjugation reaction?

Answer 5

Non synthetic reaction that may be active or inactive involving oxidation, reduction and hydrolysis producing a molecule for conjugation reaction.
Enzyme catalysed reactions

Question 6

What is conjugation reaction?

Answer 6

An endogenous ligand is conjugated to a polar functional group

Question 7

What are the four steps involved in the CYP (cytochrome P450) reaction?

Answer 7

The drug substrate binds to the oxidised form of P450
The drug P450 complex is reduced by CYP reductase, using electrons donated by the reduced form of NADP
The drug reduced form of P450 interacts with oxygen
The oxidig sed drug and water are produced

Question 8

What does glucoronidation increase?

Answer 8

Polarity and water solubility which increases the rate of biliary or urinary excretion

Question 9

What other types of conjugations occur?

Answer 9

Acetylation, methylation, glycine, glucathione etc

Question 10

Where does drug excretion occur?

Answer 10

Renal, biliary and lungs

Question 11

Renal excretion is governed by what?

Answer 11

GFR, tubular secretion and tubular reabsorption

Question 12

What is half time?

Answer 12

Time it takes for the plasma concentration of a drug to decrease by half

Question 13

What is a steady state concentration?

Answer 13

The time during which the concentration remains stable or consistent when the drug is given repeatedly or continuously

Question 14

Define agonist and antagonist

Answer 14

Agonist binds to receptor and activates it to produce a biological response
Agonist binds to receptor but no response

Question 15

What are the different receptor types?

Answer 15

7 transmembrane,
Transmembrane ion channels
Enzymes linked transmembrane receptors
Intracellular receptors

Question 16

In terms of the drugs receptor interaction, what is meant by selectivity?

Answer 16

Degree of complimentary co relation between drug and receptor

Question 17

What is drug efficacy?

Answer 17

ability of drug to procduce a pharmological response after making the drug receptor complex

Question 18

What is the mechanism of action of a GPCR?

Answer 18

When an external signalling molecule binds to a GPCR, causing a conformational change in the GPCR.
This change triggers the interaction between the GPCR and a nearby G protein

Question 19

What are the two major families of ion channel receptors?

Answer 19

LGIC, VGIC

Question 20

What are the enzyme linked receptor families?

Answer 20

Intrinsic enzyme linked receptors.
Protein kinase or guanyl cyclase domain
JAK-STAT-kinase binding receptor

Question 21

What are the different types of agonism?

Answer 21

Summation
Additive
Synergystic

Question 22

On a dose response curve, what is meant by the threshold?

Answer 22

Dose below which the are no adverse effects from exposure to chemical

Question 23

What is the Kd of a drug?

Answer 23

The dissociation constant of a drug receptor complex at which half maximal response is produced

Question 24

What is the potency of a drug?

Answer 24

It is the amount of drug required to produce a certain response

Question 25

What are the two types of dose response curves?

Answer 25

Graded and quantal

Question 26

What is a ligand?

Answer 26

Any molecule which attaches selectively to particular receptors or sites

Question 27

What is StAR?

Answer 27

Steroidogenic acute regulatory protein takes free cholesterol into the mitochondria

Question 28

What are the different routes of drug administration?

Answer 28

Enteral, patenteral, inhalation, intrathecal, iv

Question 29

What is distribution?

Answer 29

The transfer of the drug from the general circulation into the different organs of the body

Question 30

What are the mechanisms by which a drug crosses a membrane? 

Answer 30

Passive diffusion, facilitated diffusion, active transport and pinocytosis

Question 31

What law regulated passive diffusion?

Answer 31

Ficks law

Question 32

Absorption of an orally administered drug is dependent on? 

Answer 32

Disintegration, dissolution and diffusion

Question 33

Where does absorption occur?

Answer 33

Stomach and intestines

Question 34

What is bioavailability?

Answer 34

Fraction of dose which reaches systemic circulation

Question 35

What affects the bioavailability of a drug?

Answer 35

First pass effect

Question 36

What do drugs bind to?

Answer 36

Plasma and tissue proteins

Question 37

When does drug displacement occur?

Answer 37

When there is competition for binding sites