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z md1 gi block > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

1 drug that is an antacid

A

magnesium hydroxide

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1
Q

where is the chemoreceptor trigger zone

A

in the medulla, but outside of the BBB

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1
Q

forumla to work out the volume of distribution

A

amount in body/conc in plasma

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1
Q

describe the difference in renal excretion and metabolism of drugs of a newborn compared to normal

A

renal clearance is 20% of adults deficient in phase 2 conjugation therefore increased conc in blood and increased half life

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2
Q

what is zero order elimination

A

you saturate the elimination process at a certain concentration, and therefore with more drug administered.. you get increasing concentration with no steady state achieved

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3
Q

drug distribution is driven by what

A

circulation

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3
Q

why is the peak concentration higher in a slow distributing drug with iv administration

A

because it stays in the blood for longer

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3
Q

what are the causes of interpatient variability

A

age genetic factors idiosyncratic reactions disease drug-drug interaction

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4
Q

which drugs are used for motion sickness as well as nausea and vomiting

A

H1 receptor anatagonists and muscurinic receptor antagonists

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4
Q

most drugs are eliminated at a rate that is…

A

proportional to the conc in plasma

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6
Q

2 drugs that are proton pump inhibitors

A

omeprazole esomeprazole

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7
Q

definition of constipation

A

infrequent defection less than 3x per week, often with straining, with hard, uncomfortable stools

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8
Q

side effects of H1 receptor antagonists used for vomiting/nausea

A

extremely sedative

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8
Q

what is the name of the opoid that causes constipation

A

loperamide

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8
Q

what things in the body act as drug reservoirs

A

plasma proteins cells fat - leads to slow distribution

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9
Q

major problem with using CNS D2 anatagonists

A

can cause extrapyramidal side effects - worst case scenario = tardive dyskinesia

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10
Q

action of proton pump inhibitors

A

decreases gastric acid secretion by inhibiting the proton pump in the parietal cells

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10
Q

why are prostaglandin E analogues not regularly used

A

can induce abortion but increasing the motility of the uterus

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11
Q

what are 2 bulking agents used for constipation

A

bran psyllium

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12
Q

major lifestyle factors that lead to constipation

A
  • inadequate dietary fibre - inappropriate fluid intake - inappropriate bowel habits - inadequate activity and exercise - DRUGS - spinal injury - dementia - depression
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13
Q

forumla for renal clearance

A

GFR + TS - TR

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15
Q

how do prostaglandin E analogues treat PUD

A

increased mucous secretion and mucosal blood flow and decreases gastric acid secretion

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16
Q

2 major actions of metoclopramide

A
  • anti-emetic - increases gastric motility
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16
Q

how do you calculate bioavailability

A

area under the curve for oral absorption / area under the curve for iv adminstration x 100

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17
Q

for a drug with oral absorption with first order elimination, the rate of change of drug in the body is related to

A

absorption rate and elimination rate

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18
Q

what factors affect drug distribution

A

molecular size - small can cross vascular endothelium ability to bind to plasma proteins - unbound can cross vascular endothelium lipid solubility - can pass into cell membranes

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18
Q

when you change first order kinetics of a drug to a log vs time graph - what three things can you calculate

A
  • VD - half life - clearance
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19
Q

what is first pass metabolism

A

metabolism of a drug when it passes through the liver

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20
Q

when are the only times that drug-drug interactions are important

A

when drug B has a narrow therapeutic index conc-response curve to B should be steep

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21
Q

what is bioavailability

A

the proportion of active drug which enters systemic circulation

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21
Q

describe the effects of disease on drugs

A

can effect: - absorption (gastric stasis, malabsorption) - metabolism (liver cirrhosis) - excretion (renal failure)

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22
Q

what side effects do prostaglandin E analogues have

A
  • abortion - colic and diarrhoea by stimulating the bowel
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22
Q

what are the features of a drug that follows first order kinetics

A
  • rapid rise - drug has half life - peak conc related to dose and volume of distrubtion
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23
Q

How do antacids work

A

neutralise the gastric acid (dont decrease production)

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24
Q

what are the features of a drug with first order kinetics using low term iv infusion

A
  • at steady state, the rate of infusion = rate of elimination - concentration at the steady state is proportional to infusion rate - pattern of accumulation reflect multiple dosing
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25
Q

what is the difference between metabolism and excretion

A

metabolism - chemical changes excretion - physical expulsion

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27
Q

1 drug that is a prostaglandin E analogue

A

misoprostol

28
Q

actions of the 3 steps in renal excretion

A
  • glomerular filtration (takes drugs out of blood) - tubular secretion (takes drugs out of blood) - tubular reabsorption (puts drugs back into blood)
29
Q

how do cytoprotective agents treat PUD

A

coat the ulcer site and therefore heals ulcers by stopping the acid from getting to them

30
Q

drug that is a 5HT3 receptor antagonist

A

ondansetron

30
Q

action of faecal softeners and lubcricants

A

detergents - enhance mixture of water into faeces –> makes faeces softer

30
Q

for a first order kinetic drug - what is the formula for the rate of elimination

A

-KX (K = elimination rate constant, X = amount of drug in body)

32
Q

what do spasmolytics do

A

blocks muscurinic receptors on the muscle –> stops the increased gut motility - reduces pain associated with ulcers

33
Q

action of H2 receptor antagonists in treating peptic ulcer disease

A

decrease gastric acid secretion by blocking effects of histamine on parietal cells

34
Q

action of osmotic saline laxatives

A

slowly absorbed ions which cause osmotic fluid retention –> colonic stimulation by distention due to increased fluid volume

35
Q

1 drug that is a H2 receptor antagonist used for treating PUD

A

Ranitidine

35
Q

drug that is a faecal softener

A

docusate

36
Q

describe the difference in renal excretion and metabolism of drugs in the elderly

A

renal function decreases from age 20 deficient in cytochrome p450 causes increased half life and conc in blood of drug

37
Q

what is the volume of distribution

A

the volume of body water in which a drug appears to be dissolved in after it has distributed throughout the body

38
Q

2 drugs used as dopamine D2 receptor antagonists

A

metoclopramide prochlorperazine

39
Q

what is the lipid solubility of acidic and basic drugs in different pHs

A

low pH - acidic drugs lipid soluble and basic not high pH - acidic drugs not lipid soluble and basic are

40
Q

where is the vomiting centre

A

in the dorsolateral reticular formation of the floor of the 4th ventricle

41
Q

1 drug that is a H1 receptor antagonists

A

promethazine

43
Q

receptors that involve the circulating substances stimulating the chemoreceptor trigger zone that stimulates vomiting

A

D2 receptors and 5HT3 receptors

45
Q

how long is the course of treatment of peptic ulcer disease using proton pump inhibitors

A

~8 weeks

46
Q

what are pharmacokinetic drug-drug interactions

A

drug A modifies conc of drug B at its receptor

48
Q

1 drug that is a muscarinic receptor antagonists used for nausea/vomiting/motion sickness

A

hyoscine hydrobromide

49
Q

difference between phase 1 and phase 2 drug metabolism

A

1 - creates a chemical functional group on the drug (cytocrome p450) 2 - conjugation of water soluble molecule to the functional group on the drug

51
Q

what are the main classes of drugs used for peptic ulcer disease

A
  • proton pump inhibitors - H2 receptor antagonists - antacids - cytoprotective agents - spasmolytics - Prostaglandin E Analogues
51
Q

side effects of antacids

A
  • constipation/diarrhoea - cause rebound gastric acid secretion - can tend to effect some prescription drugs - systemic drugs can cause alkalosis, kidney damage and worsen existing HT - Mg can cause coma in kids
52
Q

action of stimulant laxatives

A

precise mode of action not known - may stimulate colonic myenteric nerve plexuses, irritate intestinal mucosa or by direct sensory nerve ending irritation –> increase motility

53
Q

what is the renal clearance

A

the amount of blood from which drug is removed by the kidneys per time

55
Q

side effects of 5HT3 R anatagonists

A

very minor - maybe headache and constipation

57
Q

how do bulking agents help for constipation

A

indigestible vegetable fibres - causes greater faecal water retention –> greater volume of intestinal contents –> increased stimulation of reflex bowel activity

58
Q

what are pharmacodynamic drug-drug interactions

A

drug A modifies effect of drug B without affecting its conc

59
Q

features of oral administration with first order elimination

A
  • peak no as high as with IV (due to some elimination during absorption
61
Q

drug that is a osmotic saline laxative

A

magnesium sulphate

63
Q

what is the disadvantage of lipid soluble drugs

A

high lipid solubility will lead to sequestration in lipid (sit in the fat)

64
Q

all drug elimination depends on

A

concentration of drug in the blood

66
Q

receptors for motion sickness

A

muscurinic receptors and H1 receptors

67
Q

how does metoclopramide increase gastric motility

A
  • through acting on 5HT4 –> releases ACh in the nerve plexuses in the gut –> speeds up the movement of the gut - D2 anatagonism –> dis-inhibition
69
Q

what are the 4 types of laxatives

A
  • bulking agents - faecal softeners and lubricants - osmotic laxatives - stimulant laxatives
70
Q

drug metabolism involves

A

a chemical change to a drug by enzymes making is more water soluble for excretion

71
Q

why do you give a loading dose

A

if you have a drug with a long half life, it is going to take a long time to reach a steady state concentration. Therefore to get the patient to experience the effect of the drug sooner you give a loading dose

73
Q

where does drug metabolism occur

A

mostly in the liver

74
Q

what can drug reservoirs do

A
  • prolong action (release from store as conc falls) - can quickly terminate action (if stored drug has high capacity) - can lead to slow distribution (if capacity of store is great)
76
Q

drug that is a neurokinin-1 receptor antagonists

A

aprepitant

77
Q

3 actions on receptors that metoclopramide does

A
  • D2 antagonist - weak 5HT3 anatagonist - 5HT4 agonist
78
Q

drugs that are stimulant laxatives

A

bisacodyl Senna

79
Q

what are the maximal values for GFR and renal clearance

A

GFR = 125 ml/min renal clearance = 800ml/min

80
Q

what is ADME

A
  • administration and absorption - distribution - elimination - metabolism - excretion
81
Q

what are the features of a drug with first order kinetics using short term iv infusion

A
  • rate of accumulation decreases as conc increases - peak not as high as for iv bolus - after infusion over, get elimination only
82
Q

side effect of bulking agents

A

flatulence

83
Q

what is the major precaution when taking stimulant and osmotic laxatives

A

pt can become dehyrated and loose electrolytes

84
Q

action of deactivated charcoal

A

gastrointestinal decontaminant - also used to remove poisons from the GI tract

86
Q

what factors of a drug make it good for local administration

A
  • poorly absorbed - conc so low that if it were to be absorbed - conc will be too low for systemic effect
87
Q

what factors determine the volume of distribution

A
  • if the drug binds to plasma proteins (greater conc in plasma - VD is small) - if the drug binds to tissues/taken up by cells (VD is large)
88
Q

how many half lives does a drug go through when giving multiple doses to get to 99% of the drug conc at a steady state

A

7 half lives

89
Q

1 drug that is a spasmolytic

A

hyoscine butylbromide

90
Q

what affects bioavailability

A

how much drug is absorbed how much drug undergoes first pass hepatic metabolism and local metabolism

91
Q

how does the rebound effect of antacids work

A

antacids stimulate gastrin release –> need to take more and more antacid to neutralise the excessive stimulation of HCL production by gastrin

92
Q

what is simethicone

A

agent used for the treatment of flatulence - changes the surface tension of the small air bubbles –> coalescence into big, air bubbles –> easily passed

z md1 gi block (18 decks)

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