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PHARM > Exam 1 > Flashcards

Exam 1 Flashcards

(59 cards)

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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

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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
potency
dosage of drug needed to produce a response
26
Selectivity of a drug
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
Properties of Ideal drug
``` Effectiveness Safety Selectivity Reversible action Predictability Ease of administration Freedom from drug interactions Low cost Chemical stability Possession of simple generic name ```
28
Basic principles of drug action
Drugs modify existing function within the body No drug has a single action Drug response determined by drug's interaction within the body
29
Solubility
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
Affinity
The attraction of the drug to the receptor
31
High affinity
drug molecules binds to receptors at a low drug concentration You will have a lower drug dose
32
Low affinity
drug molecules bind to receptors at a high drug concentration need a higher drug dose
33
Phases of Pharmacokinetics
absorption Distribution Biotransformation (metabolism) Excretion
34
Absorption
The movement of the drug from the site of administration into the bloodstream There is no absorption with IV drugs
35
Distribution
The movement of the drug through the bloodstream and eventually into the cells
36
Biotransformation (metabolism)
transforming the medicine Converting the drug from one substance into another Changing from lipophilic molecule to a hydrophilic molecule Happens in the liver
37
Bioavailability
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
Factors affecting distribution
Blood flow Protein binding Blood brain barrier Placental membranes
39
3 ways that drugs cross the cell membrane
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
Factors affecting metabolism
``` First pass effect- Age Pregnancy Drug metabolizing enzymes Nutritional status Competition between drugs Disease Genetics ```
41
Factors affecting excretion
Renal clearance pH dependent ionization Competition for active tubular transport Age
42
Pharmacodynamics
Action of a particular drug within the body and the study of how those actions occur How the drug affects the body
43
Steady State
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
Variables that influence the dose of a drug
Potency and efficacy Maintenance and loading doses Therapeutic index
45
Therapeutic index
The difference between an effective dose and a toxic dose
46
Unpredicted Adverse Responses
idiosyncratic response allergic reactions anaphylactic reaction
47
Transduction
Injured tissue releases chemicals that propagate pain messages (become neurotransmitters) Neurotransmitters stimulate nociceptors
48
Transmission
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
Modulation
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
Opioid Angoist Effects
``` Analgesia Sedation Mental clouding Euphoria Respiratory depression Miosis Decreased GI movement Depression of cough reflex Orthostatic hypotension Can stimulate vomiting reflex ```
51
Opioid Kinetics
Absorption-- good oral and large first pass effect Metabolism-- hepatic Elimination-- renal and feces (morphine) Onset- 15-30 mins Duration 3-7 hours
52
Opioid cautions
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
Opioid adverse effects
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
Opioid Drug interactions
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
Pure Food and Drug Act
First federal law to protect the public from mislabeled and unlabeled drugs
56
Sherley Amendment
Prohibited the use of fraudulent therapeutic claims
57
Food Drug and Cosmetic Act
Prevented marketing new drugs before they were properly tested
58
Durham-Humphrey Amendment
related to prescription of drugs and refills
59
Controlled Substances Act
Increased research into prevention of and treatment for drug abuse

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