Pharmacology - Definitions

Question 1

Adrenergic bronchodilators

Answer 1

Relaxation of smooth airway muscle in the presence of a reversible obstructions.

Clinical indications: asthma, COPD, bronchitis, emphysema, bronchiectasis

Question 1

Anticholinergic bronchodilator

Answer 1

Blocks parasympathetic nerve fibers which allow dilation of smooth muscle in airways

Question 2

Pharmacokinetics

Answer 2

Study of what body does to a drug. Recall ADME

Question 3

Xanthines

Manages, Mechanism of action, Side effects, examples

Answer 3

Used to manage:
Apnea of prematurity (first line choice)
Asthma after as a last-ditch effort
COPD

Also know as methylxanthines (b/c methyl groups)

Exact mechanism of action is unknown

Effects:
Stimulate CNS, stimulate cardiac muscle, diuresis, bronchial, uterine, and vascular smooth muscle relaxation, peripheral and coronary vasodilation, cerebral constriction.

Ex Theophylline, Caffeine, and Theobromine

Question 4

Pharmacodynamics

Answer 4

Study of drug effect on the body; the mechanism of action, desirable, adverse and toxic effects.

Question 5

ADME

Answer 5

Absorption
Distribution
Metabolism
Elimination

Question 6

Absorption

Answer 6

Rate at which drug leaves it site of administration, and the extent to which adsorption occurs

Factors affecting: Administration route, Administered with fluids/food, Dosage, Integrity of body surface, Physical-Chemical properties of drug, Acidity of stomach

Question 7

Distribution

Answer 7

Transport of drug in the body by the bloodstream to its site of action

Factors affecting: Cardiac output and regional blood flow, plasma protein binding, blood brain barrier, tissue affinity, placental/breast milk transfer

Question 8

Metabolism (biotransformation)

Answer 8

Biologic transformation of a drug into an inactive metabolite, a more soluble compound, or a more potent metabolite

Factors affecting:Presence of disease state, age, body mass and gender, enzyme inhibition/induction

Question 9

Elimination

Answer 9

Ability of the body to rid itself of a drug

Factors affecting: Kidney function, Disease states, age, urine pH

Question 10

Therapeutic Index (Window)

Answer 10

Ration between median toxic dose/ median effective does

Higher the number, the safer the drug

Lower numbers require monitoring of serum levels (Therapeutic drug monitoring)

Question 12

3 Major mechanisms of drug action are:

Answer 12

NOTE: Other cards to go over each of these
Drug-Receptor interaction
Drug-Enzyme Interaction
Anti-metabolite effect

Question 13

Drug-Receptor interaction:

4 mechanisms for transmembrane signaling

Answer 13

1. Lipid-soluble drugs cross cell membrane and act on intracellular receptors to initiate drug response
2. Drug attaches to extracellular portion of a protein in receptor and activates an enzyme system
3. Drug attaches to a surface receptor which regulates the opening of an ion channel
4. Drug attaches to transmembrane receptor that is coupled to an intracellular enzyme by a G-protein

Question 14

Drug-Receptor interaction:

Agonist Drug

Answer 14

Drug that mimics effects (efficacy) of endogenous substance by binding with receptors (affinity)

Question 15

Drug-Receptor interaction:

Antagonists Drug

Answer 15

Drug that binds to a receptor (affinity) but blocks, inhibits or counteracts effect (zero efficacy) of given agonist, natural or other drug.

Question 16

Drug-Receptor interaction:

Tachyphylaxis

Answer 16

Also known as desensitization.
rapid decrease in response to an agonist after prolonged exposure
Short period of time

Question 17

Drug-Receptor interaction: Synergism

Answer 17

Synergism (1+1=2)

2 drugs, same target, different mechanisms of action, effect that are greater than if the drugs were given alone

Question 18

Drug-Receptor interaction:Additivity

Answer 18

Additivity (1+1=3)

2 drugs, same receptor, combined effect is a linear sum of the two drugs effects, up to a maximal effect

Question 19

Drug-Receptor interaction: Potentiation

Answer 19

Potentiation (0+1=2)

A special case of synergism where one drug has no effect but can increase the activity of the other drug

Question 20

Drug-Receptor interaction: Antagonism

Answer 20

Antagonism (1+1=0)
Antibiotic combination in which the activity of one antibiotic interferes with the activity of the other (block receptor site, enzymatic inactivation), resulting in less activity with the combination than with the individual drug.

Question 21

Drug-Enzyme interaction

Answer 21

Drug modifies function of enzyme. The drug binds with the enzyme instead of the normal substrate inhibits (competitive inhibitor) certain biology reactions.

Question 22

Anti-metabolite effect

Answer 22

Metabolic reactions produce metabolites

Anti-metabolites are drugs that resemble these
metabolites but do not produce the usual
physiological response.

Therefore the effect is that anti-metabolites can block normal enzymatic action or produce substances with unique biological properties that cannot be used for further biological reactions. (Non-competitive inhibitor)

Question 23

Short-acting beta2-agonist (SABA)

Answer 23

Quick acting bronchodilator. Relieves acute reversible symptoms

Question 24

Long-acting beta2-agonist (LABA)

Answer 24

Maintenance of bronchodilation and control of bronchospasm and nocturnal symptoms. Reduces the frequency of exacerbation

Question 25

Short-Acting-anti-cholinergic (SAAC)

Answer 25

Used as relievers in patients unable to tolerate beta2 bronchodilators. Rarely used in asthma therapy.

Question 26

Long-Acting-Anti-Cholinergic (LAAC)

Answer 26

Used as relievers in patients unable to tolerate beta2 bronchodilators. Rarely used in asthma therapy.

Question 27

Inhaled Corticosteroids (ICS)

Answer 27

Reduces severity of exacerbation.

When combined with LABA improves lung function and improves health status compared to each drug alone

When combined with LAAC does not show improvement in exacerbation rates, but did improve lung function and health status.

Question 28

Mild Asthma

Answer 28

2 attacks per week or more. Less than once a day. Overnight: more than two attacks in a month. During attack you probably have to stop what you are doing and lung function 80% or over pre bronchodilator.

Question 29

Moderate Asthma

Answer 29

Daily symptoms (coughing and wheezing). Sometimes symptoms last several days.Disrupts normal activities. Night exacerbation once a week or more. 60-80% lung function pre bronchodilator.

Question 30

Moderate Severe Asthma

Answer 30

Daily symptoms (coughing and wheezing) more than once a day. Activity’s are disrupted, Sleep disrupted. Less 60% lung function pre bronchodilator.

Question 31

Severe Asthma

Answer 31

Daily symptoms (coughing and wheezing) more than once a day. Activity’s are disrupted, Sleep disrupted. Less 60% lung function pre bronchodilator.BUT less than 60% lung function POST bronchodilator.