Introduction To Pharmacology ** Not Complete - Start With Page 10 To Finish, Sympathetic Receptors

Front 1

a drug that is on a "fast track" because it's not studied (e.g. hiv drugs)

Back 1

orphan drug

Front 2

chemical agents used in the diagnosis, treatment, prevention of disease and the prevention of pregnancy

Back 2

drug

Front 3

study of drugs and their actions on the body

Back 3

pharmacology

Front 4

precise description of a drug's chemical composition and molecular structure

Back 4

chemical name

Front 5

3 ways to classify a drug

Back 5

1) body system
2) class of agent
3) mechanism of action

Front 6

Bacteria produces ____ which breaks clots

Back 6

TPA
(tissue plasminogen activator)

Front 7

A protein involved in the breakdown of blood clots

Back 7

TPA
(tissue plasminogen)

Front 8

Oral medications must pass through the _____ before entering the bloodstream

Back 8

wall of the gut & blood vessel walls

Front 9

What is the first pass effect?

Back 9

When ingesting oral medications, the liver may destroy the medication because blood from the GI tract passes through the liver before entering any other organs

Front 10

Where would you administer a drug if it is to be given "PR"?

Back 10

rectally

Front 11

Where would you administer an intra-articular medication?

Back 11

into a joint

Front 12

What do you call the amount of time required for the plasma concentration of a drug to decrease by 50% after discontinuance of the drug

Back 12

Half-life (t 1/2)

Front 13

What is half-life (t 1/2)?

Back 13

the amount of time required for the plasma concentration of a drug to decrease by 50% after discontinuance of the drug

Front 14

reflects the rapid decline in plasma drugs concentration as a drug is a distributed

Back 14

Distribution half-life (t 1/2 alpha)

Front 15

What is the distribution half-life (t 1/2 alpha)?

Back 15

reflects the rapid decline in plasma drugs concentration as a drug is a distributed

Front 16

getting rid of the medication from our body; often much slower, reflecting the metabolism and excretion of the drug

Back 16

Elimination half-life (t 1/2 beta)

Front 17

What is the elimination half-life (t 1/2 beta)?

Back 17

getting rid of the medication from our body; often much slower, reflecting the metabolism and excretion of the drug

Front 18

What is a Loading Dose?

Back 18

the initial dose of drug that is higher than subsequent doses for the purposes of rapidly achieving a therapeutic serum level of the drug

Front 19

What is the initial dose of drug that is higher than subsequent doses for the purposes of rapidly achieving a therapeutic serum level of the drug?

Back 19

Loading Dose

Front 20

What is a Maintenance Dose?

Back 20

the dose(s) of drug that maintains a certain plasma concentration of the drug in the therapeutic range

Front 21

What is the dose(s) of drug that maintains a certain plasma concentration of the drug in the therapeutic range?

Back 21

Maintenance Dose

Front 22

What is a drug's onset?

Back 22

amount of time it takes a drug to begin working

Front 23

What do you call the amount of time it takes a drug to begin working?

Back 23

Onset

Front 24

What is a drug's duration?

Back 24

length of time it takes for a drug to become therapeutic

Front 25

What is length of time it takes for a drug to become therapeutic?

Back 25

Duration

Front 26

What is therapeutic level?

Back 26

amount of drug needed to produce a desired response with minimal adverse effects

Front 27

What is pharmacodynamics?

Back 27

effects of drugs on the body and biochemical and physiological mechanisms of action of drugs
“Pharmacodynamics is the study of the biochemical and physiological effects of drugs on the body”

Front 28

What is - Pharmacokinetics?

Back 28

study of drug concentrations in body fluids and tissues
“… determination of the fate of substances administered externally”
o Absorption
o Distribution
o Metabolism
o Elimination

Front 29

What is drug absorption?

Back 29

- Movement of a drug across one or more phospholipid bilayers into a compartment

Front 30

What type of drug transport has the following characteristics? Requires no energy, has a concentration gradient, high to low solute concentration

Back 30

passive diffusion

Front 31

What is passive diffusion?

Back 31

 Requires no energy; only requires a concentration gradient
 High solute concentration to Low solute concentration
 Rapid for: lipophilic, nonionic and small molecules
** FASTER FOR FAT/LIPIDS, NOT CHARGED AND SMALL
 Slow for: hydrophilic, ionic and large molecules
** SLOWER FOR WATER, CHARGED (POLAR) AND LARGE

Front 32

What type of drug transport requires a transport protein to get large molecules "through"?

Back 32

facilitated diffusion

Front 33

What are the 4 factors that affect drug absorption?

Back 33

 Ionization state (the more charge it has, the harder it is to move)
 Molecular weight (big molecules more slower than smaller molecules)
 Solubility (lipophilicity)
 Formulation

Front 34

Water soluble things can NOT cross the _______

Back 34

blood-brain barrier

Front 35

In order for a drug to work it CAN/CAN NOT (choose) be bound to anything.

Back 35

can not

Front 36

When a medication/drug binds to the surface of a cell, it's called a ____

Back 36

ligand

Front 37

The most common place of drug binding is in the _____

Back 37

plasma protein

Front 38

Drugs bind to ____

Back 38

plasma

Front 39

The function of a protein is determined by its ____

Back 39

shape

Front 40

The shape of a protein determines its ____

Back 40

function

Front 41

The shape of a protein is determined by the _____

Back 41

arrangement of amino acid chains

Front 42

Three BIG factors in the blood that will have an affect on a medication's success are ____

Back 42

blood pH, blood Na+ concentration, and blood temperature

Front 43

What is negatively charged; likes to stick to positively charged drugs;?

Back 43

albumin

Front 44

What is positively charge; likes to stick to negatively charged drugs;?

Back 44

IMMUNOGLOBINS

Front 45

If you want to alter the shape of a protein, then change its _____

Back 45

environment (e.g. pH, temp, Na+ concentration)

Front 46

What is it called when certain drugs re-present them selves down the road, well after administration?

Back 46

depot storage

Front 47

What is another name for drug metabolism?

Back 47

biotransformation

Front 48

Drugs must be _____ before they can be eliminated or excreted

Back 48

metabolized

Front 49

Metabolism refers to the process of making a drug more _____ and _______ so that it can be eliminated

Back 49

POLAR and WATER SOLUBLE (hydrophilic)

Front 50

What is a prodrug?

Back 50

A prodrug is a pharmacological substance (drug) that is administered in an inactive (or significantly less active) form. Once administered, the prodrug is metabolised in vivo into an active metabolite.

Front 51

Phase I of drug metabolism typically involves ______ which also includes use of a ______ haemoprotein

Back 51

oxidation

Cytochrome P450

Front 52

What happens during Phase II of drug metabolism?

Back 52

a polar group is attached to the drug, increasing its polarity

Front 53

What are the 3 routes of excretion for drug elimination?

Back 53

o Urine
o Feces
o Expired air

Front 54

The "head" of a phospholipid (phosphate head) is _____ and the "tail" (free fatty acid tail) is _____

Back 54

hydrophillic

hydrophobic

Front 55

Which vitamins are fat soluble?

Back 55

A,D,E,K

Front 56

Vitamins A,D,E and K are ____

Back 56

fat soluble

Front 57

Which vitamins are water soluble?

Back 57

B,C

Front 58

Vitamins B and C are____

Back 58

water soluble

Front 59

Most drugs bind to ____ where they initiate a series of biochemical reactions that alter the cell’s physiology

Back 59

receptors

Front 60

When you STIMULATE a STIMULATING process, the net result is ______

Back 60

stimulation

Front 61

When you STIMULATE a INHIBITORY process, the net result is ______

Back 61

inhibition

Front 62

When you INHIBIT a STIMULATING process, the net result is ______

Back 62

inhibition

Front 63

When you INHIBIT an INHIBITING process, the net result is ______

Back 63

stimulation

Front 64

What is AFFINITY?

Back 64

the strength of binding between a drug and its receptor; a high affinity drug is less likely to dissociate from its receptor

Front 65

How do you measure affinity?

Back 65

Dissociation Constant (KD)

“The dissociation constant is commonly used to describe the affinity between a ligand (L) (such as a drug) and a protein (P) i.e. how tightly a ligand binds to a particular protein”

Front 66

What is a LIGAND GATED CHANNEL?

Back 66

channel that opens or closes in response to an external chemical/receptor interaction

Front 67

What do you call a channel that opens or closes in response to an external chemical/receptor interaction?

Back 67

Ligand Gated

Front 68

What is a VOLTAGE GATED CHANNEL?

Back 68

channel that opens or closes in response to electrical charge of the membrane

Front 69

What do you call a channel that opens or closes in response to electrical charge of the membrane?

Back 69

Voltage Gated

Front 70

The inside of a "cell at rest" is _____ charged at ______ mV.

Back 70

Negatively;

-90mV

Front 71

The primary cation in the ICF is _____

Back 71

K+

Front 72

The primary cation in the ECF is ____

Back 72

Na+

Front 73

The inside of the cell (negatively charged) leaks ____ which is positively charged which therefore keeps it at a constantly negative state (-90mV)

Back 73

K+

Front 74

What is depolarization?

Back 74

decrease in the absolute value of a cell's membrane potential. Thus, changes in membrane voltage in which the membrane potential becomes less positive or less negative are both depolarizations.

Front 75

Pacemaker cells are impermeable to ______. Rather, they ARE permeable to ______

Back 75

Sodium

Calcium

Front 76

What is repolarization?

Back 76

the change in membrane potential that returns the membrane potential to a negative value after the depolarization phase of an action potential has just previously changed the membrane potential to a positive value. Repolarization results from the movement of positively charged potassium ions out of the cell.

Front 77

What is hyperpolarization?

Back 77

any change in a cell's membrane potential that makes it more polarized. That is, hyperpolarization is an increase in the absolute value of a cell's membrane potential. Thus, any change of membrane voltage in which the membrane potential moves farther from zero, in either a positive or negative direction, is a hyperpolarization.

Front 78

What is ATPase?

Back 78

enzyme that works to manage levels of sodium & potassium in the cell

"ATPases are a class of enzymes that catalyze the decomposition of adenosine triphosphate (ATP) into adenosine diphosphate (ADP) and a free phosphate ion"

Front 79

What is the function of the Sodium-Potassium Exchange Pump?

Back 79

handles exchange of sodium & potassium against their concentration gradients to get the cell back to its normal state (K+ inside; Na+ outside)

"Active transport is responsible for the well-established observation that cells contain relatively high concentrations of potassium ions but low concentrations of sodium ions. The mechanism responsible for this is the sodium-potassium pump which moves these two ions in opposite directions across the plasma membrane."

Front 80

What is the absolute refractory period?

Back 80

o Point at which the cell is depolarized and is about to repolarize
o Nothing else can happen at this point;
o Once it gets below threshold again, it’s no longer in the refractory period and can depolarize again

Front 81

What type of receptors are almost always stimulatory & extremely quick?

Back 81

Nicotinic

Front 82

What are nicotinic receptors?

Back 82

are almost always stimulatory; extremely quick (fire and shut down)
“The nicotinic AChRs are ligand-gated ion channels that form pores in cells’ plasma membranes, mediating fast signal transmission at synapses.”

Front 83

What type of receptors are G-protein coupled receptors that mediate a slow metabolic response via second messenger cascades

Back 83

Muscarinic

Front 84

What are muscarinic receptors?

Back 84

G-protein coupled receptors that mediate a slow metabolic response via second messenger cascades

Front 85

What are RECEPTOR AGONISTS?

Back 85

Drugs alter the physiology of a cell by binding to plasma membrane or intracellular receptors:

Front 86

What is a STRONG AGONIST?

Back 86

causes maximal effects even though it may only occupy a small fraction of receptors on a cell

Front 87

What type of agonist causes maximal effects even though it may only occupy a small fraction of receptors on a cell?

Back 87

strong agnoist

Front 88

What is a WEAK AGONIST?

Back 88

must be bound to many more receptors than a strong agonist to produce the same effect

Front 89

What type of agonist must be bound to many more receptors than a strong agonist to produce the same effect

Back 89

weak agonist

Front 90

What is a PARTIAL AGONIST?

Back 90

drug which fails to produce maximal effects, even when all the receptors are occupied by the partial agonist (may have antagonistic properties)
 Are known for causing withdrawl

Front 91

What type of agonist is a drug which fails to produce maximal effects, even when all the receptors are occupied by the partial agonist (may have antagonistic properties)
 Are known for causing withdrawl

Back 91

partial agonist

Front 92

What are receptor antagonists?

Back 92

Drugs which inhibit or block responses caused by agonists:

Front 93

What is a competitive antagonist?

Back 93

• Competes with agonists for binding sites
• The drug with the higher affinity wins
• During the time that a receptor is occupied by an antagonist, agonists cannot bind to the receptor
• e.g. Narcan
• Are reversible

Front 94

What is a non-competitive agonist?

Back 94

• Binds to a site other than the agonist-binding site (receptor)
• Induces a change in receptor shape such that the agonist no longer “recognizes” the receptor
• Are almost always poisons
• Are not reversible

Front 95

Define EFFICACY

Back 95

o Degree to which a drug is able to produce maximal effects

Front 96

The degree to which a drug is able to produce maximal effects is called ____

Back 96

efficacy

Front 97

the amount of drug required to produce 50% of the maximal response the drug is capable of producing is called ____

Back 97

potency

Front 98

Define potency

Back 98

the amount of drug required to produce 50% of the maximal response the drug is capable of producing

Front 99

What is the EFFECTIVE CONCENTRATION (EC50) of a drug?

Back 99

the concentration of a drug which induces a specified clinical effect in 50% of the population

Front 100

What is the concentration of a drug which induces a specified clinical effect in 50% of the population?

Back 100

effective concentration (EC50)

Front 101

What is the LETHAL DOSE (LD50)?

Back 101

the concentration of a drug which causes death in 50% of the population

Front 102

What is the MINIMUM LETHAL DOSE (MLD)?

Back 102

minimum dose reported to cause death in a population; is usually lower than LD50

Front 103

Define bioavailabiity

Back 103

percentage of a drug that actually reaches target organ(s) to produce an affect

"“the fraction of an administered dose of unchanged drug that reaches the systemic circulation. By definition, when a medication is administered intravenously, its bioavailability is 100%. However, when a medication is administered via other routes (such as orally), its bioavailability decreases (due to incomplete absorption and first-pass metabolism). Bioavailability is one of the essential tools in pharmacokinetics, as bioavailability must be considered when calculating dosages for non-intravenous routes of administration.”

Front 104

What is the percentage of a drug that actually reaches target organ(s) to produce an affect?

Back 104

bioavailability

Front 105

What is the ADDITIVE EFFECT?

Back 105

the response elicited by combined drugs is EQUAL TO the combined response of each individual drug

1 + 1 = 2

Front 106

What is SYNERGISM?

Back 106

the response elicited by combined drugs is GREATER than the combined response of each individual drug

1 + 1 = 5

Front 107

What is POTENTATION?

Back 107

drug which has no effect enhances the effect of a second drug

0 + 1 = 2

Front 108

What is ANTAGONISM (in regard to drug effects)?

Back 108

drug inhibits the effect of another drug or agonist; usually, the antagonist has no inherent activity;

1 + 1 = 0

Front 109

Define DRUG TOLERANCE

Back 109

o Represents a decreased response to a drug
o The dose must increase to achieve the same effect

Front 110

What are the 3 types of drug tolerance?

Back 110

 METABOLIC – drug is metabolized more quickly after chronic use
 CELLULAR – decreased number of drug receptors (downregulation)
 BEHAVIORAL –

Front 111

Define DEPENDENCE

Back 111

o Occurs when a patient needs the drug to “function normally”

Front 112

What is WITHDRAWAL?

Back 112

o Occurs when a drug is no longer administered to a dependent patient
o Symptoms are often the opposite of the effects achieved by the drug

Front 113

What are the 2 division of the ANS?

Back 113

Sypmapthetic and Parasympathetic systems

Front 114

The sympathetic system is also called ____

Back 114

adrenergic

Front 115

The parasympathetic system is also called _____

Back 115

cholinergic

Front 116

What are the 2 chemicals of the sympathetic system?

Back 116

NE & E

(both agonists, both catecholamines)

Front 117

What is the main chemical in the parasympathetic system?

Back 117

ACh

Front 118

What are the degrading enzymes for NE & E?

Back 118

MAO and COMT

Front 119

Sympathetic receptors have _____ pre-synaptic ganglia and ___ post-synaptic ganglia

Back 119

short

long

Front 120

Parasympathetic receptors have _____ pre-synaptic ganglia and ___ post-synaptic ganglia

Back 120

long

short

Front 121

How is NE made/converted?

Back 121

Amino acid (tyrosine) gets converted to DOPA (water soluble) which gets converted to Dopamine and is altered to become Norepinephrine

Front 122

What nerve does the parasympathetic system leverage?

Back 122

vagus

Front 123

What is the parasympathetic system stimulated by?

Back 123

nicotinic receptors

Front 124

What are the 2 divisions of the PNS?

Back 124

Autonomic and Somatic Nervous Systems

Front 125

What is INFLAMMATION?

Back 125

- General process that happens in response to injury at the cellular level
- Is not always bad; e.g. pain signals that something is wrong so that you can fix it
- Swelling acts as a splint; WBC’s rush to the site to attempt to rid foreign bodies
Inflammation can also cause problems (e.g. in the lungs/asthma)

Front 126

What are CORTICOSTEROIDS?

Back 126

Class of steroid hormones that aid in regulation of inflammation

Front 127

What breaks down ACh?

Back 127

AChE (acetylcholinesterase)

Front 128

What are nicotinic ACh receptors?

Back 128

Na+ ion channels
o ALWAYS stimulatory
 Found in:
• CNS & ANS
• Sensory / Motor Nerves
• Skeletal Muscle

Front 129

What are muscarinic ACh receptors?

Back 129

G protein linked receptors

Front 130

Define M1 muscarinic receptors.

Back 130

o M1 Stimulatory (increased cGMP)
 Found in:
• Bronchial smooth muscle (causes constriction)
• Gut smooth muscle (causes peristalsis)

Front 131

Define M2 muscarinic receptors

Back 131

Inhibitory –
 Increasing outward flow of K+ so that it hyperpolarizes
 Slows down the heart
 Decreased cGMP
 Found in:
• Heart (Vagus)