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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
Q

What is the function of phase II of drug metabolism?

A

adds an endogenous compound increasing polarity

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26
Q

What are the cytochrome P450 enzymes?

A

haem proteins in the endoplasmic reticulum of liver

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27
Q

What phase of drug metabolism d othe CYP enzymes mediate?

A

oxidation reactions in phase I

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28
Q

What happens in the monooxygenase P450 cycle?

A

one atom of xygen is added to the drug to yield the hydroxyl product and second oxygen combines iwth protons to form water

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29
Q

What is glucuronidation?

A

common reaction involving the transfer of glucuronic acid to electron-rich atoms of the substrate

30
Q

What endogenous substances are subject to lgucuronidation?

A

bilirubin; adrenal corticosteroids

31
Q

What is paracetamol normally metabolised to?

A

a glucuronate and a sulphate

32
Q

What happens if the processes are saturated in paracetamol overdose?

A

toxic metabolite N-acetyl-p-benxoquinone-imine is produced

33
Q

How can HAPBQI be inactivated?

A

conjugated with glutathione

34
Q

What is given for paracetmol overdose?

A

N-acetylcysteine

35
Q

What is the function of N-acetlycysteine?

A

increases the syntehsis of glutathione permitting inreased conjugation and elimination of NAPBQI

36
Q

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?

A

conc. in glomerular filtrate will be less than palsma conc.

37
Q

Where are organic anion transporter and organic cation transporters found?

A

proximal tubule

38
Q

What is the function of organic anion transporter?

A

handles acidic drugs

39
Q

What is the function of the organic cation transporter?

A

handles basic drugs

40
Q

What is the most effective mechanism for drug elimination by the kidney?

A

excretion by tubular secretion

41
Q

What factors influence kidney reabsorption of drugs?

A

lipi solubility; polarity; urinary flow rate; urinary pH

42
Q

What is therapeutic ratio equal to?

A

maximum tolerated conc./minimum effective conc.

43
Q

What is the quantal dose response relationship?

A

the fraction of the population that responds to a give ndose of drug against the drug dose

44
Q

What is ED50?

A

median effective dose- dose of therapeutic effect in 50% population

45
Q

What is TD50?

A

dose of toxic effect for 50% of the population

46
Q

What is LD50?

A

dose of lethal effect for 50% of the populatio

47
Q

What is pharmacodynamic drug interaction?

A

drug A modified the pharmacological effect of drug b without altering its conc. in tissue fluid

48
Q

What is a pharmacokinetic drug interaction?

A

drug A modifies the conc. of drug B taht reaches its site of action

49
Q

What is the effect of fluconazole on warfarin?

A

potentiates

50
Q

What happens to enzymes with competitive inhibitors?

A

higher Km, sam Vmax

51
Q

What happens to enzymes with non-competitive inhibitors?

A

same Km , lower Vmax

52
Q

What happens with enzyme induction?

A

same Km, higher Vmax

53
Q

What should be watched with when giving drugs to neonates?

A

inefficient renal filtration; relative enzyme deficienies; inadequate detoxyifying systems

54
Q

What dosing does knowledge of volume of distribution allow?

A

calculation of a loading dose

55
Q

How is elimination affected with first order kinetics if doubling the oral dose?

A

doubling the rate of elimination

56
Q

What happens to average steady state plasma concentration if the oral dose is doubled?

A

doubles average stead ystate palsma

57
Q

What happens to the duration of drug action if the oral dose is doubled?

A

prolongs duration of drug action by one half-life

58
Q

What happens in Wiskott-Aldrich syndrome?

A

cannot produce IgM in response to capsular polysaccharide antigens of bacteria

59
Q

What are the symptoms of wiskott-aldrich syndrome?

A

lots of bacterial infection; eczema; thrombocytopenia; bloody diarrhoea

60
Q

Where is the PKD1 gene?

A

chromosome 16

61
Q

What happens when a drug induces enzyme and why?

A

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
Q

Why does furosemide cause gout?

A

both uric acid and furosemide are transported by OATs

63
Q

What phosphodiesterase is inihibited by viagra?

A

5

64
Q

Why is furosemide actively secreted in the proximal tubule not at the glomerulus?

A

extensively bound to protein

65
Q

Why is furosemide not toxic to the whole body if the triple transporter is found all over the body?

A

actively secreted into the proximal tubule- found in much higher concentrations in the tubule

66
Q

What happens to furosemide in nephrotic syndrome?

A

lose efficacy- as so bound to protein, protein enters tubule drug isn’t active

67
Q

How many days before surgery should warfarin be stopped? Why?

A

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
Q

What other treatment is for chorea/tics aside from tetrabenazine?

A

clonidine

69
Q

What antiemetic is used to treat N&V in pregnnant?

A

cyclizine

70
Q

What is the action of ephedrine?

A

mimics the effet of sympathetic stimulation- stimulates alpha and beta receptors

Transition Block (35 decks)

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