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Lecture 4 Flashcards

1
Q

What is the fraction of administered drug that reaches systemic circulation following administration by any route?

A

Bioavailability

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2
Q

What are three things that influence bioavailability?

A

1st pass hepatic metabolism
Solubility
Stability

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3
Q

Where is drug concentration measured?

A

In the plasma

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4
Q

What three things affect drug distribution into the tissue?

A

o Blood Flow
o Capillary permeability (ex- BBB)
o Drug structure (hydrophobic, hydrophillic)

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5
Q

What is volume of distribution?

A

Dose/ concentration of drug in plasma

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6
Q

What does a high volume of distribution mean?

A

Drugs distribute really well into the tissues

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7
Q

When a drug is bound to a protein is it active?

A

No, it is inactive

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8
Q

What is an example of a major protein that acidic drugs can bind to?

A

Albumin

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9
Q

What route of administration avoids the blood brain barrier?

A

Intrathecal route

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10
Q

What type substances diffuse easily across the blood brain barrier?

A

Lipid-soluble

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11
Q

What is the fastest equilibrium b/w mother and fetus?

A

40 minutes

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12
Q

What material move easily across the placenta?

A

Lipid-soluble

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13
Q

Where does most drug elimination take place?

A

Kidney

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14
Q

What is the disappearance of a drug when it is changed chemically into another compound?

A

Metabolism

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15
Q

What type of drugs can kidneys not eliminate?

A

lipophilic drugs

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16
Q

What ability have neonates not fully developed?

A

Conjugation

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17
Q

What is responsible for conjugating biliruben?

A

UDP-glucuronyl transferase

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18
Q

What competitively inhibits p450 enzyme?

A

Ketaconazole (binds to this instead of medication it should metabolize)

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19
Q

What drug permanently inactivates p450?

A

secobarbitol alkylates

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20
Q

These drugs do what to P450? Cimetidine, ciprofloxacin, erythromycin, ketoconazole, OCPs, quinidine, ETOH

A

Inhibit

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21
Q

These drugs do what to P450? Barbituates, phenytoin, steroids, isoniazid, rifampin, ETOH

A

Induce (increase metabolization)

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22
Q

What type drugs move easily across membranes?

A

Hydrophobic

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23
Q

What protein do acidic drugs bind to?

A

Albumin

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24
Q

What protein do basic drugs bind to?

A

Alpha 1-acid glycoprotein

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25
When you don't want a drug to act on the brain should you use a water-soluble drug or a lipid-soluble drug?
Water-soluble as it can't pass the BBB (ionized molecules also can't pass this barrier)
26
What is the name of a drug that is administered in an inactive form and is then activated by metabolism?
Prodrugs
27
Phase I of drug metabolism involved the ______ system.
Cytochrome P450 system
28
Whatare are P450 isozymes located?
In most cells but mainly liver and intestinal tract
29
What are the primary families in the P450 system?
CYP1, CYP2, and CYP3 families
30
What is involved in phase II of drug metabolism?
Conjugation with 2nd endogenous substrate
31
Monoamine oxidase (MAO) involved the oxidation of catecholamines and tyramine. Does it use the P450 pathway?
No, it utilizes a different pathway
32
Small doses of what drug help treat jaundice as they upregulate the expression of UDPGT.
Phenobarbital
33
Proximal tubular secretion involved in renal elimination of a drug is a _____ process
active
34
Where are all of these eliminated? PCN, cephalosporins, salicylates, thiazides, “loop” diuretics, sulfonamides, lactic acid, uric acid
Proximal tubular secretions
35
What type of drugs can't be reabsorbed?
Ionized drugs
36
What should you do to enhance the elimination of weak bases?
Acidify the urine with ammonium chloride
37
What should you do the enhance the elimination of weak acids?
Alkalinize the urine with sodium bicarbonate
38
What are 5 routes of elimination
``` Renal Biliary secretion and enterohepatic cycling Exhalation Sweat Secretion into breast milk ```
39
What is is the time it takes for the plasma concentration or the amount of drug in the body to be reduced by 50%
half life
40
What makes up total body clearance?
Cl renal + Cl hepatic + CL other
41
What is non-linear kinetics where a constant amount of drug is metabolized per unit time
zero-order kinetics
42
What is drugs catalyzed by enzymes and follows Michaelis-Menten kinetics
1st order kinetics
43
In first order kinetics, the rate of metabolism is directly proportional to the ______
concentration of free drug
44
What is when drug levels in blood when input= output?
Steady-state drug levels
45
Steady state is about how may 1/2 lives?
4-5
46
A loading dose is administered to achieve what?
Rapid plasma level
47
Foods containing pyridoxine (vit B6) increases the metabolism of what drug?
levodopa in patient's with Parkinson's
48
_______ can alter the urinary pH making the urine more alkaline thus increasing the proportion of non-ionized drug thus increasing reabsorption of the drug systemically.
Fruit juices
49
A premature infant is considered less than how many weeks?
Less than 36 week gestational age
50
A neonate is less than ____ days
30
51
Gastric pH is _____ for the first two years of life.
Alkaline (improves absorption of weakly basic drugs and decreases absorption of weakly acidic drugs)
52
Neonates in the first 24 hours of life have what?
Decrease gastric emptying increased gastroesophageal reflux irregular peristalsis increased absorption size of duodenum
53
Rectal absorption avoids what effect?
1st pass effect (drug absorbed by the hemorrhoidal veins which aren't part of the portal circulation)
54
Peds have lower ________ _________ __________ creating larger volume of distribution and increased free drug concentrations.
Plasma protein binding
55
What drug could lead to gray baby syndrome?
Chloramphenicol
56
When does GFR approach adult rates?
2 years
57
When do tubular secretion and absorption reach adult rates?
5-7 months
58
Injections are limited to how mLs in peds?
2 mL
59
Elderly patients have decreased what affect?
First pass effect
60
elderly have higher ___________ of these drugs- digoxin, warfarin, theophylline)
bioavailability
61
Elderly will have an increased rate of absorption of ______ medications due to loss of subQ fat.
topical
62
Are serum albumin levels altered in the majority of elderly?
No, unless they are severely malnourished or have advanced chronic disease
63
What is the preferred drug pathway for geriatric patients?
Phase II (conjugation)
64
After age 40, GFR decreases ____ to _____ % for every decade of life.
6-10%
65
Why may geriatric patients have an artificially lowered BUN?
Inadequate protein intake
66
Why may geriatric patients have an artificially lowered creatinine and not altered renal clearance?
Diminished muscle mass
67
What type of antibiotics have poor absorption from the GI tract so they must be administered via a parenteral route?
Aminoglycosidae antibiotics
68
What weight should be used for dosing of aminoglycoside antibiotics?
IBW or adjusted body weight
69
almost all of the clearance of aminoglycoside antibiotics occurs where?
Renal
70
What drugs inactive aminoglycosides invitro (clinically significant in patients w/ renal failure)
Extended-spectrum penicillin
71
What is the normal 1/2 life for aminoglycoside antibiotics? what about for a dialysis patient?
2-3 hours | dialysis- 30-60 hours
72
What is an aminoglycoside antibiotic that is given orally?
Neomycin (Gi infections)
73
When do you want to take a peak sample?
1 hour after the end of the infusion
74
When do you want to take a trough sample?
1/2 before next dose
75
What drug is poorly absorbed orally but is useful in the treatment of C. difficile w/ the PO route.
Vancomycin
76
When is the only time vancomycin will get into the meningeal system?
With inflamed meninges
77
Clearance of vancomycin approximates what clearance?
Creatinine
78
Vancomycin may increase levels/ effects of what drugs?
Aminoglycosides
79
This drug is a P450 inducer, highly protein bound, has slow absorption from the oral route and goes into zero order kinetics?
Phenytoin
80
In an acute setting how often should levels of phenytoin be monitored?
2-3 days after therapy initiation and another 3-5 days after
81
Stable patients should have their phenytoin levels monitored how often?
At 3-12 month intervals
82
What are some signs of phenytoin toxicity?
``` Drowsiness fatigue lateral nystagmus ataxia, slurred speech sever confusion seizures, death ```
83
What is a more soluble ester of phenytoin and can be administered IM?
Fosphenytoin (doesn't use propylene glycol)
84
What is the diluent in phenytoin IV that has cardiac depressant properties?
Propylene glycol (anti- freeze)

Pharm (29 decks)

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