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Transition Block > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What is pharmacokinetics?

A

mathematical analysis of all drug disposition factors

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2
Q

What is concentration equal to?

A

mass/volume

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3
Q

What is ke?

A

elimination rate constant- the fraction of the amount of drug in the body that is eliminated per unit time

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4
Q

What is A equal to?

A

amoutn of drug in the body

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5
Q

What is rate of elimination equal to?

A

Ke x A

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6
Q

What is first-order kinetics

A

rate of elimination is directly proportional to drug concentration

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7
Q

What type of graph is seen with drug concentration over ttime with first-order kinetics?

A

exponential

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8
Q

What is the relationip of half life and Ke?

A

inversely related

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9
Q

What is Ct?

A

concentration at a later time

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10
Q

How is Ke, T1/2 and Cp affected in first order kinetics?

A

dose adminitered changed Cp but no Ke or t1/2

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11
Q

What is clearance?

A

volume of plasma cleared of drug in unit time or a constant relating the rate of elimination to plasma concentration

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12
Q

What type of order kinetics does clearnace apply to?

A

drugs which exhibit first order kinetcs

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13
Q

What is clearnace used for clinically?

A

determines the maintenance dose rate

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14
Q

What is rate of elimination equal to?

A

clearance x Concentration of drug in plasam

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15
Q

What determines the time to reach steady state of drug concentration in teh plasma with Iv drugs?

A

half life, not infusion rate - reached after approximately 5 half-lifes

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16
Q

What is bioavailability?

A

fraction of the drug administered that enters the ssytemic circulation

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17
Q

What is the volume of distibtuion?

A

volume into which a drug appears to be distributed with a concentration equal to that of plasma

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18
Q

What is a loading dose?

A

initial high dose of a drug given at the beginning of a course of treatment before stepping down to a lower maintence dose

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19
Q

What is zero-order kinetics?

A

eliminated at a constant rate rather than proportional to their concentration

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20
Q

Why does phenytoin demonstrate zero-order kinetics?

A

range of therapeutic concentrations of phenytoin is above Km of the metabolising enzymes- saturated

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21
Q

What is the function of drug metabolism?

A

convert parent drugs to more polar metabolites that arent readily reabsorbed from the kidneys; convert to less active metabolites

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22
Q

What is phase I of drug metabolism?

A

oxidation; reduction and hydrolysis

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23
Q

What is phase II of drug metabolism?

A

conjugation

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24
Q

What is the function of phase I of drug metabolism?

A

make drug more polar, adds a hadnle to permit conjugation

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25
What is the function of phase II of drug metabolism?
adds an endogenous compound increasing polarity
26
What are the cytochrome P450 enzymes?
haem proteins in the endoplasmic reticulum of liver
27
What phase of drug metabolism d othe CYP enzymes mediate?
oxidation reactions in phase I
28
What happens in the monooxygenase P450 cycle?
one atom of xygen is added to the drug to yield the hydroxyl product and second oxygen combines iwth protons to form water
29
What is glucuronidation?
common reaction involving the transfer of glucuronic acid to electron-rich atoms of the substrate
30
What endogenous substances are subject to lgucuronidation?
bilirubin; adrenal corticosteroids
31
What is paracetamol normally metabolised to?
a glucuronate and a sulphate
32
What happens if the processes are saturated in paracetamol overdose?
toxic metabolite N-acetyl-p-benxoquinone-imine is produced
33
How can HAPBQI be inactivated?
conjugated with glutathione
34
What is given for paracetmol overdose?
N-acetylcysteine
35
What is the function of N-acetlycysteine?
increases the syntehsis of glutathione permitting inreased conjugation and elimination of NAPBQI
36
What is seen with concentrations a drug in the glomerular filtrate compared to the the plasma concentration if a drug binds to a plasma protein?
conc. in glomerular filtrate will be less than palsma conc.
37
Where are organic anion transporter and organic cation transporters found?
proximal tubule
38
What is the function of organic anion transporter?
handles acidic drugs
39
What is the function of the organic cation transporter?
handles basic drugs
40
What is the most effective mechanism for drug elimination by the kidney?
excretion by tubular secretion
41
What factors influence kidney reabsorption of drugs?
lipi solubility; polarity; urinary flow rate; urinary pH
42
What is therapeutic ratio equal to?
maximum tolerated conc./minimum effective conc.
43
What is the quantal dose response relationship?
the fraction of the population that responds to a give ndose of drug against the drug dose
44
What is ED50?
median effective dose- dose of therapeutic effect in 50% population
45
What is TD50?
dose of toxic effect for 50% of the population
46
What is LD50?
dose of lethal effect for 50% of the populatio
47
What is pharmacodynamic drug interaction?
drug A modified the pharmacological effect of drug b without altering its conc. in tissue fluid
48
What is a pharmacokinetic drug interaction?
drug A modifies the conc. of drug B taht reaches its site of action
49
What is the effect of fluconazole on warfarin?
potentiates
50
What happens to enzymes with competitive inhibitors?
higher Km, sam Vmax
51
What happens to enzymes with non-competitive inhibitors?
same Km , lower Vmax
52
What happens with enzyme induction?
same Km, higher Vmax
53
What should be watched with when giving drugs to neonates?
inefficient renal filtration; relative enzyme deficienies; inadequate detoxyifying systems
54
What dosing does knowledge of volume of distribution allow?
calculation of a loading dose
55
How is elimination affected with first order kinetics if doubling the oral dose?
doubling the rate of elimination
56
What happens to average steady state plasma concentration if the oral dose is doubled?
doubles average stead ystate palsma
57
What happens to the duration of drug action if the oral dose is doubled?
prolongs duration of drug action by one half-life
58
What happens in Wiskott-Aldrich syndrome?
cannot produce IgM in response to capsular polysaccharide antigens of bacteria
59
What are the symptoms of wiskott-aldrich syndrome?
lots of bacterial infection; eczema; thrombocytopenia; bloody diarrhoea
60
Where is the PKD1 gene?
chromosome 16
61
What happens when a drug induces enzyme and why?
increasing number of enzymes- have the same Km as aren't changing the inherent nature of hte ezyme but you have more, so maximum velocity of the reaction will be higher- higher Vmax
62
Why does furosemide cause gout?
both uric acid and furosemide are transported by OATs
63
What phosphodiesterase is inihibited by viagra?
5
64
Why is furosemide actively secreted in the proximal tubule not at the glomerulus?
extensively bound to protein
65
Why is furosemide not toxic to the whole body if the triple transporter is found all over the body?
actively secreted into the proximal tubule- found in much higher concentrations in the tubule
66
What happens to furosemide in nephrotic syndrome?
lose efficacy- as so bound to protein, protein enters tubule drug isn't active
67
How many days before surgery should warfarin be stopped? Why?
5 days- half-life of warfarin is long (generally 24 hours)- rule for elimination is 5 half-lives, takes body about 2-5 days to make new clotting factors after vit K gamma-carboxylation
68
What other treatment is for chorea/tics aside from tetrabenazine?
clonidine
69
What antiemetic is used to treat N&V in pregnnant?
cyclizine
70
What is the action of ephedrine?
mimics the effet of sympathetic stimulation- stimulates alpha and beta receptors

Transition Block (35 decks)

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