Pharmacology Lecture - 1

Question 1

1. ____ is the area of pharmacology concerned with the undesirable effects of chemicals and biologics on cellular functions.
2. _____ describes the effects of the BODY on drugs (absorption, distribution, excretion) and
3. _____ describes the action of DRUGS on the body such as the mechanism of action and therapeutic and toxic effects.

Answer 1

1. toxicology
2. pharmacokinetics
3. pharmacodynamics
   (drug on body)

Question 2

Aspirin blocks formation of _____ (can cause vasoconstriction in the coronaries)

What are the two major drugs in thrombosis?

Thrombolytics are also useful in ____

Answer 2

PROSTAGLANDINS

1. major drugs in thrombosis = HEPARIN & WARFARIN

heparin  anti-coagulant

Warfarin  outpatient management of thrombosis

STROKES

Question 3

Which are examples of active immunization & which are passive

  1  - inactivated bacteria
  2  - inactivated virus	
 3   - bacterial polysaccharide
  4  - immunoglobulins
  5  - recombinant antibodies*

Answer 3

Active immunization

- inactivated bacteria
- inactivated virus	
- bacterial polysaccharide

Passive immunization

- immunoglobulins
- recombinant antibodies*

Question 4

What is the most widely used stem cell therapy?

Answer 4

BONE MARROW TRANSPLANT

Question 5

What is fick’s law of diffusion of drugs in the body? (equation)

Answer 5

[C1-C2 x (Permeability Coefficient) x Area ]
/ Thickness

Predicts the rate of movement of molecules across a barrier.

The concentration gradient (C1-C2) and permeability coefficient for the drug and the thickness of the barrier impact a drug’s diffusion

Question 6

What type of diffusion do ionized drugs used?

Answer 6

AQEUOUS
- ionized vs. non-ionized drug components are determined by pH

• henderson - hasselbach equation

Question 7

What are the determinants of distribution of drugs?

Answer 7

1. Size of target site
2. Blood flow
3. Solubility
4. Binding

APPARENT volume of distribution & PHYSICAL volume

Question 8

_____ order elimination implies that the rate of elimination is proportional to the concentration.

The higher the concentration of drug
the greater what?

Answer 8

First Order

the greater amount of drug is eliminated per unit time.
- curved line (hyperbola)

Question 9

_____ order elimination implies that the rate of elimination is constant regardless of the concentration

Answer 9

Zero Order ELimination

• straight line

Question 10

What is multicomponent distribution?

What type of mathematical model does this process represent?

Answer 10

Many drugs undergo an initial DISTRIBUTION phase followed by a SLOW ELIMINATION phase.

Mathematically this process can be modeled by means of a two compartment model.

(alpha = distribution
beta = elimination)

Question 11

What is single compartment distribution?

Answer 11

A few drugs may behave as they are distributed to only one compartment (vascular compartment).

Others have more complex distributions that require more than two compartments for construction of accurate models.

Question 12

_____ is a protein that can make a signal which propagates a physiologic response once a drug binds

Answer 12

Receptor

Question 13

Where are the following receptors found and name examples:

1. Type I
2. Type II
3. Type III

Answer 13

1. Type I - plasma membrane
   * Ach & NE
2. Type II - Cytoplasm
   * steroid hormones
3. Type III - Nucleus
   * Anti-cancer drugs

Question 14

A drug capable of fully activating the effector system when it binds to the receptor.

Answer 14

Agonist

Question 15

Define an antagonist

Answer 15

STRUCTURALLY similarity to agonist and interaction with receptor but does not cause same molecular change in receptor, therefore inhibits interaction of agonist with receptor.

Question 16

What are the sequence of events following a drug-receptor interaction?

Answer 16

1. ACh + receptor
2. Na influx
3. Action potential
4. Increased free Ca
5. Contraction

Question 17

What is pharmacodynamic tolerance or desensitization? (ex)

What is pharmacodynamic sensitization? (ex)

Answer 17

Down- regulation

• repeated administration of catecholamines decreasing number of alpha-receptors.

Up-regulation:
-thyroid hormone increasing number of beta-receptors in myocardium.

Question 18

Antibodies to acetylcholine receptors in the motor-end plate describes _____

Decreased number of receptors for plasma LDL describes ____

Answer 18

1. Myasthenia Gravis

2. Familial hypercholesterolemia

Question 19

What is competitive antagonism?

What drug for opiod overdose?

Drug Antidote to benzodiapens?

What is non-competitive antagonism

Answer 19

REVERSIBLE competition for agonist receptor binding sites WITHOUT inducing a biological response

1. Naloxone to opiod overdose
2. Flumazenil antidote to benzodiazepines
3. IRREVERSIBLE binding with receptor preventing agonist binding to receptor, such as DFP which combines with acetylcholinesterase to prevent acetylcholine from binding to acetylcholinesterase.

Question 20

State which describes the following (chemical equivalence, biological, or therapeutic)

1. related to pharmacokinetics involving bioavailability
2. related to amount of drug per tablet
3. related to clinical response that will provide same efficacy and toxicity (hopefully lack of toxicity)

Answer 20

1. Biological
2. Chemical
3. Therapeutic

Clinical implications: most of the generic drugs are comparable in their safety and efficacy profile with the branded products. Very few exceptions.