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PHARM > Exam 1 > Flashcards

Exam 1 Flashcards

1
Q

Bioavailability

A

Rate and extent to which the active ingredients are absorbed and made available at the site of action

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2
Q

Preclinical testing

A

The chemist has and idea and puts it together and gives it to animals
Testing for toxicity
Looking to see if there are any useful effects to it
Takes 6 to 7 years

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3
Q

Phase I

A

Done only on healthy volunteers that have nothing wrong with them
Looking for how the drug is working in the body
Determining safety
Usually only on 20 to 80 people
Takes 1 to 2 years

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4
Q

Phase II

A

Population 100 to 300 patients who actually have the disease
Looking at the dosage to figure out what is effective for these patients
Start to look at a lot more side effects of the medication on these patients
Takes about 2 years

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5
Q

Phase III

A 
1000-3000 patients 
Looking for long term side effects 
3 to 4 years 
Nurses are involved in this process 
This is done in a double blind study
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6
Q

FDA reporting/ NDA

A

Report from the three phases waiting for their approval and can take 1 to 2 years
Once you get the new drug application you can start to market the drug

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7
Q

Phase IV

A

Point at which drugs are given to elderly patients and children

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8
Q

Orphan drugs

A

A drug that has been abandoned because it may have been too expensive to develop

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9
Q

Off label prescribing

A

Given to treat something else than what it was made for

There are laws that say you can prescribe off label but if you market it for that then you have to go back to phase II

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10
Q

Legend drugs

A

Prescription drugs

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11
Q

black box warning

A

highlight the most serious warnings

Not only indicates adverse reactions but what patients should not be taking that drug

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12
Q

Schedule I

A

non medical use for the drug (street drugs) highest potential for abuse

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13
Q

Schedule II

A

High abuse potential but there is a medical reason for it
These drugs cannot have refills
Can lead to severe psychological and physical dependence
needs warning label
ex: narcotics

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14
Q

Schedule III

A

Less potential for abuse
can get refills– up to 4
Prescription expires in about 6 months time
Differs state to state

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15
Q

Schedule IV

A

Lower abuse potential

ex: sedatives

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16
Q

Schedule V

A

a lot of drugs that you can buy OTC

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17
Q

Category X

A

Studies in animals or humans have demonstrated fetal abnormalities and or there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience and the risks involved in use of the drug in pregnant woman clearly outweigh potential benefits

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18
Q

affinity

A

Propensity of a drug to bind or attach itself to a given receptor site

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19
Q

Agonist

A

Drug that combines with receptors and initiates sequence of biochemical and physiologic changes
Possesses both affinity and efficacy

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20
Q

Antagonist

A

Agent designed to inhibit or counteract effects produced by other drugs or undesired effects caused by cellular components during illness

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21
Q

competitive antagonist

A

Agent with affinity for same receptor site as an agonist
Concentration of agonist tends to overome inhibition
Competitive inhibition responses usually reversible

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22
Q

Efficacy

A

ability of drug to initiate biologic activity as result of binding to given receptor

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23
Q

noncompetitive antagonist

A

agent that combines with different parts of receptor mechanism and inactivates receptor so that agonist can’t be effective regardless of its concentration
effects considered to be irreversible or nearly irreversible

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24
Q

partial agonist

A

agent that has affinity and some efficacy but may antagonize action of other drugs that have greater efficacy
diminished response compared with that elicited by the agonist

25
Q

potency

A

dosage of drug needed to produce a response

26
Q

Selectivity of a drug

A

The size of the drug molecule
The shape of the drug
The electrical charge of the molecule (want drugs to have no charge in order to cross the cell membrane)
The more selective the drug the less side effects

27
Q

Properties of Ideal drug

A 
Effectiveness
Safety 
Selectivity 
Reversible action 
Predictability 
Ease of administration 
Freedom from drug interactions
Low cost
Chemical stability 
Possession of simple generic name
28
Q

Basic principles of drug action

A

Drugs modify existing function within the body
No drug has a single action
Drug response determined by drug’s interaction within the body

29
Q

Solubility

A

Measuring how well an amount of a given substance will dissolve in a liquid
Drugs need to dissolve in the stomach or GI tract in order to be absorbed
Drugs need to be lipophilic

30
Q

Affinity

A

The attraction of the drug to the receptor

31
Q

High affinity

A

drug molecules binds to receptors at a low drug concentration
You will have a lower drug dose

32
Q

Low affinity

A

drug molecules bind to receptors at a high drug concentration
need a higher drug dose

33
Q

Phases of Pharmacokinetics

A

absorption
Distribution
Biotransformation (metabolism)
Excretion

34
Q

Absorption

A

The movement of the drug from the site of administration into the bloodstream
There is no absorption with IV drugs

35
Q

Distribution

A

The movement of the drug through the bloodstream and eventually into the cells

36
Q

Biotransformation (metabolism)

A

transforming the medicine
Converting the drug from one substance into another
Changing from lipophilic molecule to a hydrophilic molecule
Happens in the liver

37
Q

Bioavailability

A

The fraction of a drug that is absorbed into the circulation after administration
Other routes are compared to IV route
A bioavailability of 1 means that all of the given drug is available in the blood stream

38
Q

Factors affecting distribution

A

Blood flow
Protein binding
Blood brain barrier
Placental membranes

39
Q

3 ways that drugs cross the cell membrane

A

Pass between the spaces or channels between the molecules in the membrane
Pass through the membrane with the help of a transport system
Penetrate the membrane directly

40
Q

Factors affecting metabolism

A 
First pass effect- 
Age
Pregnancy 
Drug metabolizing enzymes 
Nutritional status
Competition between drugs 
Disease 
Genetics
41
Q

Factors affecting excretion

A

Renal clearance
pH dependent ionization
Competition for active tubular transport
Age

42
Q

Pharmacodynamics

A

Action of a particular drug within the body and the study of how those actions occur
How the drug affects the body

43
Q

Steady State

A

The point at which the amount of drug being administered and the amount being eliminated balance off are equal
At four to five half lives steady state is achieved
Increasing the dose has no effect on how quickly steady state can be achieved

44
Q

Variables that influence the dose of a drug

A

Potency and efficacy
Maintenance and loading doses
Therapeutic index

45
Q

Therapeutic index

A

The difference between an effective dose and a toxic dose

46
Q

Unpredicted Adverse Responses

A

idiosyncratic response
allergic reactions
anaphylactic reaction

47
Q

Transduction

A

Injured tissue releases chemicals that propagate pain messages (become neurotransmitters)

Neurotransmitters stimulate nociceptors

48
Q

Transmission

A

afferent neurons
Carry signals to CNS and pain begins in nociceptors in afferent neurons and gets carried to CNS
Pain stimuli enters spinal cord int he dorsal horn
Substance P a peptide in the dorsal horn is released in response to the pain – acts as a neurotransmitter has a role in interpreting pain and has a role in regulating self produced endogenous analgesic response

49
Q

Modulation

A

Pain message is inhibited through this phase
Descending from brain to spinal cord we produce another set of neurotransmitters that will impede pain impulse
Neurotransmitters include serotonin norepinephrine neurotensin GABA our own endogenous opioids
Within the spinal cord – kappa and mu
endogenous opioids can block these receptors and exogenous works here

50
Q

Opioid Angoist Effects

A 
Analgesia
Sedation 
Mental clouding 
Euphoria 
Respiratory depression 
Miosis 
Decreased GI movement 
Depression of cough reflex 
Orthostatic hypotension 
Can stimulate vomiting reflex
51
Q

Opioid Kinetics

A

Absorption– good oral and large first pass effect
Metabolism– hepatic
Elimination– renal and feces (morphine)
Onset- 15-30 mins
Duration 3-7 hours

52
Q

Opioid cautions

A

Contraindicated resp depression pts receiving other CNS depressants and head injury
Dose reduction may be necessary in elderly due to altered pharmacokinetic properties
Drug addict

53
Q

Opioid adverse effects

A

CNS: mood changes lethargy euphoria pupillary constriction
respiratory: decrease RR respiratory arrest and apnea
CV: hypotension bradycardia cardiac arrest coma and shock
GI: N/V constipation
GU: urinary retention
Histamine release: puritis and uticaria

54
Q

Opioid Drug interactions

A

Possible with any other hepatic ally cleared drug– will increase opioid level or increased other drug level, H2 blockers barbiturates and warfarin
Potentiation of sedation and respiratory depression
Caution with other CNS depressant drugs including alcohol

55
Q

Pure Food and Drug Act

A

First federal law to protect the public from mislabeled and unlabeled drugs

56
Q

Sherley Amendment

A

Prohibited the use of fraudulent therapeutic claims

57
Q

Food Drug and Cosmetic Act

A

Prevented marketing new drugs before they were properly tested

58
Q

Durham-Humphrey Amendment

A

related to prescription of drugs and refills

59
Q

Controlled Substances Act

A

Increased research into prevention of and treatment for drug abuse

PHARM (4 decks)

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