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828 Dosage > ADMET > Flashcards

ADMET Flashcards

1
Q

Disposition

A

-Distribution and elimination (Metabolism and Excretion)

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1
Q

ADMET

A

-Absorption
-disposition (Distribution and elimination (Metabolism and Excretion)
-Toxicity

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2
Q

elimination

A

-removal of drug via metabolism and excretion

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3
Q

Toxicity

A

result of exposure

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4
Q

Plasma vs Time curves

A

can determine each phase of ADMET

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5
Q

Pharmacokinetic view

A

dresser (person) vs drawers (organs)

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6
Q

Sampling sites (exposure)

A

-blood, plasma, serum
-urine

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7
Q

Sites of delivery

A

-arterial
-venous
-SC,IM
-pulmonary
-oral

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8
Q

Elimination site

A

-gut metabolism
-exhalation
-hepatic metabolism
-fecal excretion
-renal excretion

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9
Q

Drug distribution

A

-dependent on physiochemical properties
-lipophillic vs hydrophillic

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10
Q

Lipophilic drugs

A

-partition into fatty tissues

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11
Q

Hydrophillic drugs

A

-partition into tissues where endothelium is permissive

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12
Q

Pharmacokinetic Process

A

-defined by concentration vs time profiles
-compartments represent kinetically similar tissues
-reversible or irreversible
-linear or nonlinear
-fast and slow processes tend to disappear

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13
Q

Differences in blood perfusion rates after drug distribution

A

-dictate organ distribution levels

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14
Q

Distribution Limitations

A

-perfusion rate
-permeability rate
-convection
-diffusion

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15
Q

Perfusion rate

A

-blood flow to tissues

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16
Q

Permeability rate

A

-membrane permeability

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17
Q

convection

A

-mechanism of transvascular transport
-pressure gradient

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18
Q

Diffusion

A

concentration gradient

19
Q

Typical Plasma vs time curve

A

-increase to peak during absorption (Cmax, Tmax)
-decrease through the rest of the phases

20
Q

AUC

A

area under curve

21
Q

Tmax

A

time to reach maximum blood concentration

22
Q

Cmax

A

maximum blood concentration of dosage form

23
Q

Bioavailability

A

rate and extent of drug absorption

24
Q

Absolute bioavailability

A

AUC of given dosge form compared to AUC of same dose injected intravenously

25
Q

Relative bioavailability

A

AUC of given dosage form compared to arbitrary reference standard

26
Q

Bioequivalence

A

does NOT mean the therapeutic effect of the two dosage froms are equivalent

27
Q

Paracelsus

A

“everything is poison actually it’s just the dose”

28
Q

Paraclesian theory

A

chemical may have no effect, beneficial effect or toxic effect

29
Q

dose-response relationship

A

-most important factor in pharmacology and toxicology

30
Q

Dose

A

-amount of chemical
-local concentration of chemical at response site

31
Q

dose-receptor concentration

A

function of ADME

32
Q

Absorption rate (Kabs) defined by

A

-drug properties
-excipient/drug composition
-physiological barriers between GI tract and systemic circulation

33
Q

Absorption rate controlled by

A

-formulation parameters that are optimized to provide a Cmax and Tmax associated with safe and efficacious response = therapy is realized

34
Q

Influences of efficacy and safety

A

-duration of drug plasma concentration in the therapeutic window (Cmax and T max)
-duration of chronic therapy

35
Q

Potential Worsening of disease

A

Prolonged exposure to subtherapeutic doses or ineffective drugs

36
Q

Therapeutic window

A

-concentration of drug between the minimum effective level and the minimum toxic level

37
Q

MTC

A

minimum toxic level

38
Q

MEC

A

minimum effective level

39
Q

True (A) or False (B): BIOAVAILABILITY is the fraction of an
administered dose that reaches the systemic circulation
intact.

A

True

40
Q

True (A) or False (B): Dosage forms are designed to convey
performance by balancing the composition of the excipients,
the drug’s physicochemical properties and to overcome the
physiological barriers required for a safe and efficacious
response.

A

True

41
Q

True (A) or False (B): When blinding clinical trials, it is often
important to mask the ORGANOLEPTIC properties of the
comparator and the drug being tested. These senses include
sight, smell, taste, touch, and sound.

A

True

42
Q

True (A) or False (B): The STOMACH has a significantly
increased surface area due to villi, folds of Keckring, and
microvilli.

A

FALSE, intestine

43
Q

Which is NOT included in the acronym of ADMET?

A

Dissolution

44
Q

True (a) or False (f): The microenvironmental pH at the membrane surface may
be different than the lumen based on the fact that the mucus and the glycocalyx
have buffering effects.

A

True

45
Q

True (a) or False (b): Drug levels observed in the therapeutic window can be
governed in part by transporters and metabolism, based on the compound being
studied. Therefore, transporters and enzymes do not play an important role in
drug product performance.

A

FALSE

46
Q

All of the following can reduce the bioavailability of an orally administered drug
EXCEPT:
a) Poor dissolution in the GI tract
b) Poor penetration of the blood-brain barrier Ans
c) Chemical degradation in the GI tract
d) Poor solubility in the GI fluids
e) Poor absorption across the GI mucosa

A

828 Dosage (27 decks)

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