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Pharamcology > Week 2 > Flashcards

Week 2 Flashcards

1
Q

Metabolism of drugs occur primarily in the ____ and usually makes the drug more _______.
In some cases the more polar the drug metabolite may be excreted in the ____ into the small intestine and then stool

A

liver
polar
bile

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2
Q

What are the two phases of drug metabolism and what is the major in phase 1 ______ and what is the primary enzyme in phase 2______ and what is there biological function

A

cytochrome P-450
Glucuronyl transferase
function is to ad more polar groups to make it more water soluble

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3
Q

cytochrome P-450 is actually a family closely related enzymes called _____ or ____

A

isozymes or isoforms

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4
Q

where is cytochrome P-450 found in the body

A

in the ER inside liver cells

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5
Q

in phase II gluucuronyl transferase adds a molecule of ______ however this molecule can also be sometimes added ______

A

glucuronic acid

ionic sulfate

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6
Q

codeine and heroin are both metabolized into the ______ drug ______

A

active

morphine

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7
Q

_____ and ____ are cholesterol drugs and these forms become active

A

simvastatin

atorvastatin

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8
Q

______(—–) an otc antihistamine is actives into prescription _____(—-)

A

Loratidine(claritin)

Desloratidine(clarinex)

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9
Q

the in active form of a drug can then become active by metabolism is called ______

A

pro-drugs

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10
Q

in how many half lives does the drug have no clinical potency

A

4-5 half-lives

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11
Q

Two drugs that can increase their half life by storage in lipids are ____ and ____

A

THC

sodium pentothal

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12
Q

the rate of drug excretion front he body depends on what two factors

A
  1. rate of drug metabolism (mostly by liver)

2. rate of excretion by kidneys or in intestinal bile.

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13
Q

relatively non-polar drugs are reabsorbed in _

A

nephrons

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14
Q

most drugs are inactivated on the first pass of the blood through the liver and this is refereed to as the ____ _____ _____

A

first pass effect

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15
Q

drugs with half lives of ___-____ usual provide once a day dosing

A

10-24 hours

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16
Q

sedatives with narrow therapeutic range

A

barbiturates

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17
Q

sedatives with large therapeutic range:

A

benzodiazepines (valium, xanax)

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18
Q

the reason new borns should be given a lower does than normal is because x4

A
  1. lower level of liver enzymes
  2. less renal function
    3,lower serum albumen
  3. less developed BBB
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19
Q

patients with _____ disease will have a decreased excretion of the drug and the potentially increased drug activity

A

liver

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20
Q

______(especially older than 80) have decreased _____ and ____ function resulting in slower drug excretion.

A

liver & renal

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21
Q

LD50

A

lethal does for 50% of the population

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22
Q

ED50

A

effective does for 50% of the population

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23
Q

LD50/ED50

A 
therapeutic index (TI)
(the bigger the number the safer)
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24
Q

what are 3 drugs with small TI

A 
coumadin
digoxin (TI=2)
phenytoin (Dilantin) (TI=3)
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25
how many half lives may it take for a drug to reach equilibrium blood level
4 half-lives
26
bioavailabilty in pill form may be influenced by X5
1. empty stomach or with food 2. whether the drug is taken with +2 or +3 ions 3. gelatin capsule or tablet form 4. size of drug crystals 5. presence of constipation or diarrhea in the patient
27
_________ are the details of processes by which a drug produces its effect.
pharmacodynamics
28
a drug usually binds to a receptor and the receptor may be a ____ and ______
channel protein | enzyme
29
if the drug activates the receptor it is referred to as a
agonist
30
if the drugs prevents activation of the receptor it is referred to as an ______ or _______
antagonist or blocker
31
in some cases a drug may bind tot he receptor and gives partial activation, it is referred to as a
partial agonist
32
_____ (-----) is a partial agonist which binds to the nicotine receptor but doesn't give the strong effect of nicotine and helps taper a person off
Varenicline(Chantix)
33
ibuprofen and aleve inhibit ____ ______ the enzyme that make inflammatory molecules
prostaglandin cyclooxygenase
34
_______ is an opiate antagonists to help people get off the addiction
Buprenorphine
35
drug may bind on the ____ of a membrane protein and activate the protein to catalyze a reaction on the ___ (second messenger). thus the drug never enters the cell
outside | inside
36
a drug may bind to a membrane ____ and wither open or close the channel
protein
37
drug may bind to a membrane protein which then activates a __ protein in the inside which then activates a second protein membrane bound protein
G
38
Drugs may pass through membrane, pass into the ___ and activate synthesis of new proteins
nucleus | EX. steroids
39
what occurs in phase 1 phase 2 phase 3
phase 1-drug may be metabolized faster than it can bind to receptors phase 2-the physiological response increases in proportion to the number of receptors bound by the drug phase 3-reduced effects are obtained until no further increase in effect and this is refereed to as the PLATEAU EFFECT
40
some drugs may inherently activate the receptor more effective than other drugs and these drugs are more ___ oxycodone is more ____ than _____
efficacious | efficacious than codeine
41
morphine is more potent than ______- | just because is more potent does not mean that it is more efficacious
meperidine (demerol)
42
_______ _______ occurs when the number of drug receptors decreases with time upon repeated stimulation thus decreasing the effect of the drug. what is an example of this
Pharmacodynamic tolerance | ex. morphine and other opiates
43
_____ ______ results from the increases synthesis of cytochrome p-450 and /or glucuronyl transferase what is an example of this
metabolic tolerance | barbiturates, tegretol (anti-seizure med and mood stabilizer used for bipolar)
44
______ dependence is when the a user experiences physical observable withdraw symptoms such as ______ ____ (DT's) during alcohol withdraw. Symptoms include _____, ____ and uncontrollable _____
``` physical delirium tremens hallucinations confusion shaking ```
45
_____ dependence is when no physically observed symptoms are evident, but compulsion to obtain the drug still exists
phsychological
46
if two drugs are taken together and there effects add up together then this is referred to as a ______ effect
additive
47
if two drugs are taken together and the effect is greater than the sum of the two drugs then this effect is referred to as a
synergistic effect
48
codeine, prozac, and metoprolol (lopressor) are all inactivated by the same isozyme of _____. Thus is a patent is given more than one one of these drugs the isozyme may become saturated thus the effects of both drugs is increased and prolonged
cytochrome P-450 (2D6)
49
_______ juice acts to inhibit CYP3A4
grapefruit
50
the production of more cytochrome P-450 by the liver is refereed to as ____ ______
enzyme induction
51
regular use of alcohol can cause induction of ____ _____ isozymes which can result in faster drug metabolism, on the other hand excessive consumption of alcohol can cause cirrhosis of the _____ resulting in ______ and ______. Thus a slower metabolism of the drug
cytochrome P-450 liver liver tissue death liver enzyme levels drop
52
the most commonly used drugs that exist primarily bound to serum albumen include ______, ______, _____ and _______
coumadin, sulfonamides, digoxin, and Dilantin
53
drugs act on the autonomic nervous system by........ | inhibition of the electrical conduction down the axon produces ______ either local or general
acting on the electrical conduction in the axon itself. anesthesia
54
What are three general inhalation anesthetics
ether chloroform sevoflurane
55
ether
-very flammable, post-op vomitting, lung damage. Not used in the US
56
Chloroform
non-flammable, but heart arrhytmias. prolonged exposure can cause liver damage. Not used in the US
57
Sevoflurane
fluorinated ether. non-flammable, very low incidence of liver damage.
58
modifying neurotransmisssions at synapses. this can produce a much more specific pharmacological action. a. ) stimulate receptors at the synapse-1. b. )inhibit synapse receptor-2. c. ) stimulate and inhibit 3. d. )increase or decrease the life of the neurotransmitter in the synapse
1. agonist 2. antagonsit, blocker 3. mixed agonist/antagonist
59
_______ is the neurotransmitter at the ganglia of both the sympathetic and parasympathetic.
acetylcholine (ACh)
60
the receptors at the ganglia are called _____ ____. these receptors are activated by the binding of ____ and _____
nicotinic receptors | nicotine and ACh
61
ACh is also the neurotransmitter released by the __-_____ parasympathetic neuron. It binds to receptors called ____ receptors
post-ganglionic | muscarinic receptors
62
Drugs which activate the post-ganlionic parasympathetic are referred to as ____ _____
cholinergic agonists
63
Drugs which inactivate the post-ganlionic parasympathetic are referred to as ____
cholinergic antagonists or anticholinergics
64
the action of acetylcholine is terminated by the enzyme
acetylcholinesterase.
65
the post ganglionic sympathetic neurotransmitter is
norepinephrine (NE)
66
what are the 4 types of adrenergic receptors
a1, a2,b1,b2
67
how is the activity of NE commonly terminated
reabsorption into the afferent neuron
68
what are the two enzymes that inactivate NE in the afferent neuron.
monoamine oxidase (MAO) and catechol orthomethyl transferase (COMT)
69
the second important sympathetic neurotransmitter is _________
epinephrine (adrenaline)
70
what is epinephrine released by in the body.
adrenal medulla
71
the receptors that epinephrine bind to is _____ however epinephrine can be inactivated by _____
``` adrenergic Monoamine oxidase (MAO) ```
72
what are in B1 x2
heart rate | kidneys
73
what are in B2 x4
1. Bronchi 2. uterus 3. blood glucose, 4. arterioles in heart, lung, skeletal muscle
74
what are in a1 x5
1. peripheral arterioles (skin) 2. eye 3. genitals 4. veins 5. visercal arterioles (Gi tract)
75
epinephrine can act on how many receptors
all 4
76
norepinephrine can act on how many receptors
all except B2
77
_____(------) is used after post partum or post-op to stimulate contraction of the detrusor muscle and relaxation of the bladder sphincter to help one go pee
Bethanecol (Urecholine)
78
______ ______ increase acetylcholine activity by blocking inactivation of ACh. Several types of insecticides and nerve gas act as ______ _____. Continued stimulation of ACh receptors can cause profuse salivation, dedication, urination, bronchoconstriction. Ach is also the transmitter at the neuromuscular junction and continuous stimulation of those receptors can cause muscular and respiratory paralysis which can be fatal
Cholinesterase inhibitors | Cholinesterase inhibitors

Pharamcology (12 decks)

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