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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
Q

how many half lives may it take for a drug to reach equilibrium blood level

A

4 half-lives

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26
Q

bioavailabilty in pill form may be influenced by X5

A
  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
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27
Q

_________ are the details of processes by which a drug produces its effect.

A

pharmacodynamics

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28
Q

a drug usually binds to a receptor and the receptor may be a ____ and ______

A

channel protein

enzyme

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29
Q

if the drug activates the receptor it is referred to as a

A

agonist

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30
Q

if the drugs prevents activation of the receptor it is referred to as an ______ or _______

A

antagonist or blocker

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31
Q

in some cases a drug may bind tot he receptor and gives partial activation, it is referred to as a

A

partial agonist

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32
Q

_____ (—–) 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

A

Varenicline(Chantix)

33
Q

ibuprofen and aleve inhibit ____ ______ the enzyme that make inflammatory molecules

A

prostaglandin cyclooxygenase

34
Q

_______ is an opiate antagonists to help people get off the addiction

A

Buprenorphine

35
Q

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

A

outside

inside

36
Q

a drug may bind to a membrane ____ and wither open or close the channel

A

protein

37
Q

drug may bind to a membrane protein which then activates a __ protein in the inside which then activates a second protein membrane bound protein

A

G

38
Q

Drugs may pass through membrane, pass into the ___ and activate synthesis of new proteins

A

nucleus

EX. steroids

39
Q

what occurs in phase 1
phase 2
phase 3

A

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
Q

some drugs may inherently activate the receptor more effective than other drugs and these drugs are more ___
oxycodone is more ____ than _____

A

efficacious

efficacious than codeine

41
Q

morphine is more potent than ______-

just because is more potent does not mean that it is more efficacious

A

meperidine (demerol)

42
Q

_______ _______ 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

A

Pharmacodynamic tolerance

ex. morphine and other opiates

43
Q

_____ ______ results from the increases synthesis of cytochrome p-450 and /or glucuronyl transferase what is an example of this

A

metabolic tolerance

barbiturates, tegretol (anti-seizure med and mood stabilizer used for bipolar)

44
Q

______ dependence is when the a user experiences physical observable withdraw symptoms such as ______ ____ (DT’s) during alcohol withdraw. Symptoms include _____, ____ and uncontrollable _____

A 
physical
delirium tremens 
hallucinations
confusion
shaking
45
Q

_____ dependence is when no physically observed symptoms are evident, but compulsion to obtain the drug still exists

A

phsychological

46
Q

if two drugs are taken together and there effects add up together then this is referred to as a ______ effect

A

additive

47
Q

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

A

synergistic effect

48
Q

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

A

cytochrome P-450 (2D6)

49
Q

_______ juice acts to inhibit CYP3A4

A

grapefruit

50
Q

the production of more cytochrome P-450 by the liver is refereed to as ____ ______

A

enzyme induction

51
Q

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

A

cytochrome P-450
liver
liver tissue death
liver enzyme levels drop

52
Q

the most commonly used drugs that exist primarily bound to serum albumen include ______, ______, _____ and _______

A

coumadin, sulfonamides, digoxin, and Dilantin

53
Q

drugs act on the autonomic nervous system by……..

inhibition of the electrical conduction down the axon produces ______ either local or general

A

acting on the electrical conduction in the axon itself.

anesthesia

54
Q

What are three general inhalation anesthetics

A

ether
chloroform
sevoflurane

55
Q

ether

A

-very flammable, post-op vomitting, lung damage. Not used in the US

56
Q

Chloroform

A

non-flammable, but heart arrhytmias. prolonged exposure can cause liver damage. Not used in the US

57
Q

Sevoflurane

A

fluorinated ether. non-flammable, very low incidence of liver damage.

58
Q

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

A
  1. agonist
  2. antagonsit, blocker
  3. mixed agonist/antagonist
59
Q

_______ is the neurotransmitter at the ganglia of both the sympathetic and parasympathetic.

A

acetylcholine (ACh)

60
Q

the receptors at the ganglia are called _____ ____. these receptors are activated by the binding of ____ and _____

A

nicotinic receptors

nicotine and ACh

61
Q

ACh is also the neurotransmitter released by the __-_____ parasympathetic neuron. It binds to receptors called ____ receptors

A

post-ganglionic

muscarinic receptors

62
Q

Drugs which activate the post-ganlionic parasympathetic are referred to as ____ _____

A

cholinergic agonists

63
Q

Drugs which inactivate the post-ganlionic parasympathetic are referred to as ____

A

cholinergic antagonists or anticholinergics

64
Q

the action of acetylcholine is terminated by the enzyme

A

acetylcholinesterase.

65
Q

the post ganglionic sympathetic neurotransmitter is

A

norepinephrine (NE)

66
Q

what are the 4 types of adrenergic receptors

A

a1, a2,b1,b2

67
Q

how is the activity of NE commonly terminated

A

reabsorption into the afferent neuron

68
Q

what are the two enzymes that inactivate NE in the afferent neuron.

A

monoamine oxidase (MAO) and catechol orthomethyl transferase (COMT)

69
Q

the second important sympathetic neurotransmitter is _________

A

epinephrine (adrenaline)

70
Q

what is epinephrine released by in the body.

A

adrenal medulla

71
Q

the receptors that epinephrine bind to is _____ however epinephrine can be inactivated by _____

A 
adrenergic
Monoamine oxidase (MAO)
72
Q

what are in B1 x2

A

heart rate

kidneys

73
Q

what are in B2 x4

A
  1. Bronchi
  2. uterus
  3. blood glucose,
  4. arterioles in heart, lung, skeletal muscle
74
Q

what are in a1 x5

A
  1. peripheral arterioles (skin)
  2. eye
  3. genitals
  4. veins
  5. visercal arterioles (Gi tract)
75
Q

epinephrine can act on how many receptors

A

all 4

76
Q

norepinephrine can act on how many receptors

A

all except B2

77
Q

_____(——) 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

A

Bethanecol (Urecholine)

78
Q

______ ______ 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

A

Cholinesterase inhibitors

Cholinesterase inhibitors

Pharamcology (12 decks)

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