Cellular regulation Flashcards
Unit 1
1
Q
define pharmacology
A
the study of medicines
2
Q
what is the purpose of pharmacology?
A
to cure, relieve symptoms and improve quality of life
3
Q
define pharmacotherapeutics
A
utilization of medicines (drugs) to heal or manage patient care
4
Q
what are the 3 categories of pharmacotherapeutics?
A
(1) drug/medication (2) biologics (3) natural health products
5
Q
define drug/medicine
A
a chemical agent, typically synthetically produced
e.g. ibuprofen
6
Q
define biologic
A
medication that is naturally produced in animal cells
e.g. antibodies, blood products, hormones
7
Q
define natural health product
A
medications that are naturally occuring and typically used as adjunct treatment
(e.g. vitamin minerals, dietary supplements)
8
Q
what is the general body that regulates pharmacotherapeutics?
A
Health Canada
9
Q
what is Health Canada responsible for regarding pharmacotherapeutics?
A
evaluating/monitoring safety, efficacy, quality and advertising of pharmacotherapeutics
10
Q
what is the Canadian pharmaceutical association responsible for?
A
publishing the compendium of pharmaceuticals and specialties
11
Q
define the CPS
A
Compilation of drug information and all adverse effects reported
12
Q
define placebo effect
A
a “neutral” substance said to have an effect, which may lead to an actual effect
13
Q
what does the Declaration of Helsinki state?
A
Encourages against the use of placebo drugs in clincial trials unless there is no better clinical trial control
comparative substance should be the primary treatment used at the time
14
Q
what are the 3 types of drug names?
A
- Generic
- Brand/trade
- Chemical
15
Q
define generic name
A
describes the drug without a proprietary affiliation
16
Q
how many generic names can a drug have?
A
1
17
Q
define brand/trade name
A
the name provided to a drug by the manufacturing company
18
Q
how many brand/trade names can a drug have?
A
many per one generic drug
depends on how many companies make it
19
Q
define chemical name
A
drug name as assigned by the IUPAC based on its chemical composition
e.g. potassium chloride
20
Q
what are the main differences between brand and generic drugs?
A
- cost
- prescribing - they are interchangeable
- bioequivalence
21
Q
describe the difference in bioequivalence between brand/trade and generic drugs
A
active ingredients are the same in both but filler ingredients may differ, changing the efficacy or effectiveness of a drug
22
Q
define prototype drug
A
selection of a single drug from a drug class to serve as a reference drug within a particular class
23
Q
what are the 2 types of drug class nomenclature?
A
- therapeutic drug class
- pharmacological drug class
24
Q
define therapeutic drug class nomeclature
A
The name specifies a treatment/a therapy of a particular disease/disorder
e.g. antihypertensive, anticoagulant, antiinflammatory
25
define pharmacological drug class nomenclature
The name describes the molecular/receptor activity: ‘mechanism of action’ (how it works)
| e.g. beta blocker, calcium channel blocker
26
what is the criteria of schedule I drugs?
* controlled drugs that need a prescription from health care professionals
* narrowly used drugs that require more education or monitoring for use
| e.g. narcotics, opiods
27
what is the criteria of schedule II drugs?
* Available only from a pharmacist
* Must be retained in an area with no public access
* Does not need prescription
| e.g. Tylenol I, II or III
28
what is the criteria of schedule III drugs?
* Available via open access in a pharmacy or pharmacy area (OTC)
* Drugs restricted to specific population criteria (i.e. age)
| e.g. non medical cannabis
29
what is the criteria of unscheduled drugs?
can be sold in any store without professional supervision
| e.g. Advil, Tums, Reactine
30
what are the 6 rights of medication administration?
1. right patient
2. right drug
3. right dosage
4. right route
5. right time
6. right documentation
31
define drug formulation
the way the drug ingredients are prepared to be administered in a specific form
| e.g. solid, liquid, injectable
32
define drug route for administration
the way the drug is taken into the body
## Footnote
specified by formulation
33
what factors does the route of administration depend on?
1. medical situation
2. drug kinetics
3. drug formulation availability
4. clinical setting
34
define oral administration
ingested through the mouth in liquid, tablet/pill or powder form
35
define enteric coated tablets
tablets/pills that are coated to withstand the conditions in the stomach and dissolve further down the GI tract in the jejunum or duodenum
36
define enteral feed
feeding a pateitn via a tube into the GI tract
37
what is a nasojejunal tube?
a tube that enters via the nasal cavity to reach an end destination: the jejunum of the small intestine
38
what challenges do we consider for oral administration?
1. Drugs have to maneuver an acidic environment
2. Administration is peristalsis dependant
3. First pass metabolism has a great effect
39
does oral administration provide a local or systemic effect?
systemic
40
define sublingual administration
a pill is dissolved under the tongue, bypassing the GI system and 1st pass metabolism
41
does sublingual administration provide a local or systemic effect?
systemic
42
when should sublingual administration **not** be used?
for drugs that need to be administered often to avoid causing damage to oral mucosa
43
define intranasal (insufflation) administration
drug is administered into the nasal cavity
44
does intranasal administration provide a local or systemic effect?
can be either deending on formulation and molecular composition of the drug
| e.g. local effect - nasal spray or systemic effect - flu vaccine
45
define inhalation administration
drug is inhaled into the lungs
46
does inhalation administration provide a local or systemic effect?
can be either depending on the drug
| e.g. local effect - ashtma inhaler or systemic effect - anesthesia
47
define endotrachal administration
drugs administered via a tube going in through the mouth, into the lungs
48
in which occasions would we use an endotracheal tube?
in ER/ICU situations
49
define topical administration
drug is applied directly to a surface
50
does topical administration provide a local or systemic effect?
has and is intended to have a local effect
51
define transdermal administration
administration of a drug through the dermis
| e.g. through a patch
52
does transdermal administration provide a local or systemic effect?
systemic effect is desired
53
define rectal administration
the drug is inserted into the rectum in a suppository
54
does rectal administration provide a local or systemic effect?
can be either depending on drug composition
| e.g. local effect - glycerine or systemic effect - morphine
55
define parenternal administration
drug administration involving a needle
56
define intravenous administration
drug administered via a needle catheter inserted into a vein
57
does intravenous administration provide a local or systemic effect?
immediate systemic effect
58
what is are associated risk with IV?
* risk of infection - insertion site needs to be monitored frequently
* patient discomfort
59
define intramuscular administration
drug administered through a needle injection into muscle tissue
60
which forms does intramuscular injection take?
aqueous or depot preparation
61
which IM preparation has faster effects?
aqueous
62
does intramuscular administration provide a local or systemic effect?
systemic
63
what sites is IM administration done at?
1. deltoid site
2. ventrogluteal site
3. rectus femoris and vastus laterus site
64
define subcutaneous administration
drug administered via a needle injection into adipose tissue of hypodermis
65
does subcutaneous administration provide a local or systemic effect?
systemic
66
define implanted port administration
a type of central line that starts under the skin on the chest and connects to a catheter that is threaded into a large vein near or inside the heart
67
what considerations need to be made with implanted port administration?
1. what type of port it is
2. A&p of where it leads to
3. what to assess or how to care for it
4. which drugs can be administered via port
5. how to maintain its patency
68
define vaginal administration
drugs inserted into vagina to make a local action
69
define intraosseous administration
drug is administered through a needle going directly into bone
70
define epidural administration
drug is injected into epidural space of spine
71
define spinal administration
drug is injected into CSF
72
what are the 4 phases of pharmacokinetics?
1. absorption
2. distribution
3. metabolism
4. excretion
73
define absorption
process of moving a drug from the site of administration to the bloodstream
74
what factors affect absorption?
1. administration route
2. molecular characteristics
75
define plasma concentration
how much drug is in the systemic circulation
76
define bioavailability
systemic circulation's drug concentration
77
define first pass metabolism
process of which drugs enter the liver and undergo biotransformation (metabolized), reducing bioavailability
78
which drugs do we consider to have extensive 1st pass metabolism?
1. morphine
2. meperidine
3. diazepam
4. midazolam
5. lidocaine
6. propranolol
7. ETOH
79
define therapeutic range
plasma drug concentration between the minimum effective concentration and the toxic concentration
80
define onset of action
time at which plasma drug concentration reaches the minimum effective concentration within the therapeutic range
81
define minimum effective concentration
amount of drug required to produce a therapeutic effect
82
define duration of action
time spent in the therapeutic range
83
define termination of action
time at which plasma drug concentration drops back to the minimum effective concentration, dropping lower until conc. is no longer in the therapeutic range
84
define loading dose
a higher amount of drug, often given once or twice, that is administered to prime the bloodstream with a level sufficient to quickly induce a therapeutic response
85
define ED50
the dose that elicited a therapeutic response in 50% of patients
| median therapeutic dose
86
define TD50
the dose that elicited a toxic response in 50% of patients
87
define LD50
the dose that was lethal to 50% of lab subjects
88
define therapeutic index
the ratio between TD50:ED50
89
what do we consider narrow TI meds?
1. digoxin
2. warfarin
3. phenytoin
4. tacrolimus
90
what does a low TI tell us about the risk of a drug?
the lower the TI, the higher the risk of adverse effects (overdose)
91
define steady state level
drugs are administered continously to maintain a plasma conc. level within the therapeutic range
| e.g. IV drip
92
define distribution
transport of drug molecules through the body to target tissue
93
what main factors affect distribution?
1. blood flow to the tissue
2. size of the tissue
3. molecular characteristics
4. plasma protein binding
94
define plasma protein binding (PPB)
binding of drug molecules to plasma proteins during distribution
95
acidic drugs have a high affinity for which plasma protein?
albumin
96
basic drugs have a high affinity for which plasma protein?
Alpha-1-acid glycoprotein
97
what are the characteristics of binding?
1. competitive
2. reversible
3. saturable
98
what considerations do we take with drug-to-drug interactions in regards to binding?
drugs can compete for a protein and one with stronger affinity can displace a currently bound drug, resulting in more free, active molecules circulating
99
what drugs do we consider as extensively bound drugs?
| greater than 90% bound
* warfarin
* ibuprofen
* naproxen
* furosemide
* digitoxin
* diazepam
* midazolam
100
define volume of distribution
estimates how extensively a drug is distributed into tissues
101
what does a higher Vd indicate?
more drug molecules reach tissues and bind to receptors, also increasing risk of side effects
102
define metabolism
an enzymatic chemical conversion to prepare the drug/substance for excretion
103
what is the primary metabolizing organ?
the liver
104
define prodrug
an active metabolite that was biotransformed from an inactive drug
| inactive drug -> active metabolite
105
define "travel unchanged" drugs
drugs that are never metabolized
106
what processes occur during phase I metabolism?
hydrolysis, reduction, oxidation
107
what is the main enzyme group responsible for oxidation during phase I metabolism?
Cytochrome p450 enzyme group
108
which CYP450 enzyme group is most active?
CYP3A4/5 is the most active, responsible for the bulk of drug metabolism
109
define inducer
a drug that increases the rate of enzyme activity, causing faster metabolism
| e.g. tobacco is an inducer for Tylenol
110
define inhibiter
a drug that decreases the rate of enzyme activity, causing slower metabolism
| e.g. some antibiotics are inhibitors of Tylenol
111
what process occurs during phase II metabolism?
conjugation
112
define conjugation
ionization of a substance
113
define excretion
elimination of drugs from the body
114
what are the molecular characteristics of molecules that are easier to excrete?
1. hydrophilic
2. ionized
3. small
115
what is the primary organ of excretion?
kidneys
116
what are the main factors affecting renal excretion?
1. molecular characteristics
2. cardiac output
3. renal function
117
define GFR
a calculation used to test kidney function by measuring creatinine levels
| high creatinine = bad kidney fxn
118
define clearance
rate of elimination of a drug in an hour
119
define 1st order elimination kinetics
elimination is proportionate to the drug serum concentration
| more drug = faster clearance
120
define zero order elimination kinetics
rate of elimination or clearance is constant regardless of plasma drug conc.
| e.g. ETOH, aspirin
121
what are the Cytochrome p450 enzyme groups?
* 3a4/5
* 2a4
* 2b6
* 2c8/9, 2c19
* 2d6
* 2e1
* 1a2
122
what enzymes carry out metabolism in the liver?
hepatic microsomal enzymes
123
define ionized
neutral atoms or molecules converted to electrically charged ones
124
what is the acid-to-acid or base-to-base rule?
molecules retain their ionization state when in the same environment - e.g. acidic molecules stay acidic in the stomach bc its acidic
125
which molecules have an easier time entering a cell: hydrophilic or lipophilic?
lipophilic molecules
126
what molecules are required to make ATP?
Na+, K+ and Ca 2+
127
what is the ADME general rule?
* Lipophilic, nonionized and small molecules = easy absorption and distribution
* Hydrophilic, ionized molecules = easy excretion
128
what percentage of blood flow goes to bone marrow?
5%
129
what percentage of blood flow goes the brain?
18%
130
what percentage of blood flow goes to the heart?
5%
131
what percentage of blood flow goes to the liver?
25%
132
what percentage of blood flow goes to the kidneys?
20%
133
what percentage of blood flow goes to the muscles?
20%
134
what percentage of blood flow goes to the skin?
7%
135
what is the equation for calculating Vd?
Drug dose / measured drug plasma concentration
136
what is the equation for calculating clearance?
CrCl = [(140 – age) x (lean body weight)] / (serum creatinine) x 72
x0.85 for females
