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pharm > exam 1: Lecture 1 > Flashcards

exam 1: Lecture 1 Flashcards

1
Q

what is a drug?

A

drug is any chemical agent that affects the protoplasm of the cell

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2
Q

pharmacodynamics vs pharmacokinetics?

A

pharmacodynamics is how the drugs affects the body (working with receptors)

kinetics is how the drugs moves within the body (how its metabolism, absorbed, eliminated etc)

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3
Q

what is voltage gated ion channels?

A

it changes the membrane potential, causes channel to open up and ions movements out or in

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4
Q

what are the three types of voltage gated ion channels?

A

Na+, Ca+, K+

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5
Q

where are voltage gated Na+ channel seen?

A

Na+ are seen in nerve cells, cardiac cells and skeletal cells

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6
Q

what medication blocks Na+ channels from exerting its forces?

A

lidocaine

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7
Q

what is Ca+ channels used for?

A

regulates vascular tone

used for BP regulation

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8
Q

what rx are some calcium channel blockers?

A

verapamil, diltiazem

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9
Q

what are K+ channels used for?

A

helps to restore membrane potential after depolarization duh!!

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10
Q

what is an rx that interacts with voltage gated K+ channels?

A

Topiramate (anti seizure medication)

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11
Q

what is a ligand gated ion channel?

A

its when a ligand binds to the channel and causes confirmational change

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12
Q

what are TWO examples of LIGAND gated channels?

A

nicotinic aCH receptors and GABA receptors!

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13
Q

what happens in a nicotinic aCH receptor?

A

(Nicotinic=sodium, n=na)

the ligand is the ACH

ACH binds to the nicotinic receptor and it causes NA channel to open up

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14
Q

what happens in a GABA receptor?

A

(g looks like c = gaba and cl)

GABA binds to gaba receptors and it OPENS CL channel, CL rushes INTO the cells = hyperpolarization

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15
Q

what rx binds to GABA receptors

A

benzodiazepine binds to gaba and causes hyperpolarization of nervous cells which causes depression

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16
Q

what are G protein coupled receptors?

A

this is when a receptor is coupled to INTRAcellular G protein so when the ligand binds to the receptor, G protein is freed intracellular and exerts a downstream effect!

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17
Q

what are two examples of G protein coupled receptors (GPCR)?

A

muscarinic receptor and catecholamine receptors

rememeber: 30% of drugs on market work through GPCR

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18
Q

what is muscarinic and catecholamine receptors?

A

(muscarinic means relating to parasympathic shit)
MR are postsynaptic aCH receptor that are found in the parasympathetic system

CR are receptors for noepi, epi and doapmine

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19
Q

what time of protein is G-protein and what subunits does it have?

A

heterotrimer - it has alpha subunit (Gs, Gi, Gq) beta and gamma

the alpha has three diff parts
the beta and gamma helps localize alpha subunits to the receptor

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20
Q

how does Gs stimulate and Gi inhbit?

A

Gs stimulates by activating the adenylyl cyclase. It converts ATP into cAMP and has downstream affects

Gi inhibits aCH and turns off productions of cAMP. without cAMP we cannot have downstream affects

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21
Q

what is an ex of Gq? and explain mechanism

A

PLC-DAG/IP3-Ca2+
activates phospholipase C, diacylgylcerol, inositol triphosphae which releases Ca+ which activates other proteins OR causes smooth muscles contractions

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22
Q

what is RTK?

A

for RTK, there is extracellular, transcellular and cytosolic domain which has alot of tyrosine residues

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23
Q

explain the events of RTK?

A

ligand binds to RTK, casues dimerization, casues phospholation of tyrosine residues –> exerts downstream effects

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24
Q

what are examples of RTK and whats an example receptor of RTK?

A

ex; growth factors, VEGF, insulin

Receptor: JAK-STAT receptor (ligand casues activation of JAK and phosphorlaytion of STAT –> gene transcription)

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25
Q

expalin the mechanisim of intracellular receptors

A

ligand will MIGRATE through cell and bind to receptor on the nucleus or cytosol–> casues dimerization and go tot he DNA –> casues expression or turns off genes

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26
Q

what are ex that will bind to intracelluar receptors?

A

glucocorticoids, thyroid hormones, estrogen, vit B (lipid soluble shit)

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27
Q

what is an agonist? anatagonist?

A

agonist is a drug that binds to a receptor and MIMIKS the NORMAL response

ex: aCH agonist will elicit the same response as ach

antagonist is a drug that BLOCKS/REDUCE the action of the agonist

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28
Q

whats a orthosteric?

A

binds to where the native ligand binds

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29
Q

whats allosteric agonist? whats an example?

A

agonist binds to a DIFF place from the native ligand

EX: Benzo binding to GABA receptor
(remember; on GABA , Cl channels opens and CL goes into which causes hyperpolization)

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30
Q

whats partial and inverse agonist? what are ex as inverse agonist?

A

partial agonist is drugs that dont elicit the maximun repsonse as native ligand

inverse agonist is drug that DECREASES normal response by turning cell OFF
EX: parkinson drugs or antihistamine

31
Q

whats allosteric antagonist?

A

drug that interacts with a DIFF place on the receptor

32
Q

what is chemical antagonist (whats an ex of a drug) and what are two ex?

A

chemical antagonist is a drug that binds to the ligand in the BLOODSTREAM
ex) bevacizumab inhibits VEGF)

two ex are competitive and non competitive antagonist

33
Q

what is competiive antagonist?

A

competitive antagonist is when the antagonist binds to the receptor and BLOCKS the agonist from exerting its effects

high dose of agonist will overcome the comp antagonist

high dose of antagonist will prevent agonist from binding to receptor

34
Q

what is noncompetitive antagonist? what type of bond is it? whats an ex?

A

noncompetitive antagonist is when antagonist binds to diff part of the receptor (covalent bond) and NO AMT of agonist will overcome the antagonist since it changes the shape!

ex: asprin. no amount of arachidonic acid can overcome antagonist which is why people who take asprin needs to be off of it to regenerates platelets

35
Q

what is EC50?

A

the concentration of drug that will reach 50% of maximum effect of drug

it is a measure of potency!!!

36
Q

what is potency of a drug?

A

potency of a drug is the amount of drug needed to get to HALF MAXIMAL response

think about EC50 which is a measure of potency

37
Q

is having a small EC50 = high potency or low potency of drug?

A

small EC50 correlates to HIGH potency of drug since it requires small amt of concentration to reach to 50% of maximun repsosne!

38
Q

what is efficacy?

A

efficacy is quantify of cellular response

its the ABILITY of a drug to bind to receptor and elicit some response

39
Q

what is loading dose of a drug?

A

loading dose of a drug is the initial higher dose of drug that may be given at the begining of a course of tx before dropping down to maintance dose

think of biologics

40
Q

if the graph shifts DOWN/UP, are you changing efficacy or potency?

A

efficacy - ability of drug to bind to receptor
(R/L is potency)

41
Q

what is the therapeutic window?

A

the window of a drug is the RANGE of the drug’s dose that is SAFE enough without having toxic effect

So, rx with SMALL window must be carefully administered to avoid toxicity

42
Q

what is median effective dose ED50?

A

the conc/dose of drug that can produce a biological desired outcome (response) in 50% of population

43
Q

what is median toxic dose TD50?

A

how much of the drug that can produce toxic effect on 50% of the population

44
Q

what is median lethal dose LD50?

A

how much of the drug needed to cause death to 50% of lab animal (obv not humans lol)

45
Q

what is the therapeutic index?

A

TD50 or LD50 / ED50
its the quantitative measure of drug safety. Small index is BAD :(
Large index is GOOD :) –> (hard to make mistake)

46
Q

what is absorption of drug?

A

how a drug is administered via PO, IM, IV etc

47
Q

what is the first pass effect/elimination?

A

first pass effect/elimination is the idea of drug metabolism where the conc of drug decreases when it reaches the systemic circulation

48
Q

what is bioavailability? does IV dose have 100% bioavailability? what about PO?

A

the proportion of drug or substance that enters the circulation system when introduced to the body and able to have an active effect

(IV dose has 100% bioavailability - it can enter circulation with 100% effect)

(PO has less than 100% bioavailability since it goes through so much like gut, mesenteric vein, liver, IVC)

49
Q

what is distrubution of drug?

A

when the drug is in the bloodstream, itll go to diff compartments in the body depending on a number of things: blood, solubility, proteins etc

50
Q

how does high albumin affect distribution?

A

if you have high protein bound drugs, there is decrease in amt of free drugs in the blood which can go to tissue –> decreases distribution

51
Q

what effect does unbound form of drugs do? more free drugs!

A

UNBOUND form of the drug (when the drug is not bound to albumin) has greater distribution – it can go to other parts and diffuse in the cell membrane

52
Q

what is volume of distribution Vd?

A

Vd estimate how WIDESPREAD a drug can be distributed to all diff body compartments

53
Q

explain what happens if someone has liver diseases and its affect on drugs distribution?

A

if someone has liver diseases/CKD, they cannot produce albumin so theres alot of free drugs in the blood stream which can go into tissue –> may lead to toxicity

54
Q

what is large Vd and small Vd?

A

large Vd = most drugs goes into third space like connective/adipose tissue

small Vd = most drugs stays in the bloodstream

55
Q

what is decreased and increased Vd?

A

decreased Vd = more plasma protein binding, drugs do not move around

increased Vd = more free drugs that can move around to tissue due to low albumin/proteins

56
Q

what is metabolism?

A

taking a substance and transforming into a water soluble or polar compound SO THAT it can easily be excreted by the kidneys

57
Q

the liver can change toxic, prodrug (inactive), and active drug into what?

A

toxic to non toxic metabolite
prodrug to active drug
active drug to inactive drug

58
Q

what is the CYP450?

A

rate limiting enzyme on the liver that forms or breaks various molecules –> can takes a active drug turn into inactive etc

59
Q

what are the two phases of biotransformation?

A

phase 1 - exposes or adds a function group to parent compounds such as -OH, -SH, -NH2

phase 2 - conjugation rx to make it water soluble so it can be excreted via 6 things

60
Q

what are the 6 conjugation for phase 2 reactions?

A

MAAGGS

methylation
acetylation
AA conjugation
glucuronidation
GSH conjugation
sulfonation

61
Q

what will happen if pt takes warfarin and also takes a drug that is a CYP450 inducer? think how the inducer will affect warfarin (anti clotting) metabolism

A

CYP450 will take warfarin and change it to inactive form of warfarin

we will have more inactive form and less active form = BAD = pt will clot more since warfarin is anti-clotting rx

62
Q

what will happen if u have CYP405 inhibitor? think using warfarin

A

CYP450 will increase active form of warfarin since it wont change to inactive = pt will bleed more since its anti-clotting

63
Q

does cigarette smoke and charcoal broiled food induce or inhibit 1A2? how?

A

induce 1A2

smoker + oral contraception can lead to unplanned preg bc it induced 1A2 which metabolizes estrogen

64
Q

how does cimetidine affect CYP450? explain what will happen if you take warfarin and cimetidine tg?

A

cimetidine inhibits CYP450 / 2b+3A

cimetidine will inhibit the enzyme so warfarin wont be created into inactive. more active warfarin present so more prone to bleeding

65
Q

whats the effects of erythromycin and keto?

A

potent inhibitor of P450 enzymes

66
Q

what does the drug pass through in the kidney before elimination?

A

passes through glomerular filtration, tubular secretion and tubular reabsorption

67
Q

why is elimination so imp

A

if metabolites dont get excreted properly, it can build up in the pt and kill them

68
Q

what is drug clearance? where do drugs get metabolized and excreted?

A

drug clearance is the rate of elimination of a drug in proportion to its concentration

its metabolized in the liver and excreted in the kidneys OR live, kidney skin etc

69
Q

what is first order elimination ?

A

it is the rate of elimination directly proportional to the concentration

70
Q

does concentration change clearnace?

A

concentration does not change the clearance. the enzyme metabolizing the drug can metabolized alot of conc and it still will NOT change clearance

71
Q

what is zero order/non linear?

A

this is when the enzyme that is metabolizing the drug becomes SATURATED. This changed the rate of clearance depending of the dose

72
Q

relationship between rate of clearance and dose of drug?

A

rate of clearance decreases with higher dose of drug

73
Q
A

pharm (13 decks)

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