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M4: Pharmacology-Pharmacokinetics > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

Process involved (LADME)

A

Pharmacokinetics
Transport
Liberation
Absorption
Distribution
Metabolism
Excretion

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2
Q

▪️ movement through the cell membrane
▪️ basic requirement: drug must be in aqueous solution except in pinocytosis where drug is in missile form

A

Transportation

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3
Q

Two types of mechanism of transport in Pharmacokinetics

A
  1. Passive Diffusion
  2. Carrier-mediated Transport
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4
Q

▪️ dominant, most common; slowest; no enery requirement
▪️ along concentration gradient (high to low)
▪️ governed by Fick’s Law Diffusion

A

Passive diffusion

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5
Q

“LUNA”

A

Lipophilic
Unionized
Non-Polar
Absorbed

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6
Q

“HIPE”

A

Hydrophilic
Ionized
Polar
Excreted

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7
Q

▪️ selectivity/ specificity- carriers recognize specific molecules
▪️ subject to competition, inhibition or antagonism
▪️ Michaelis-Menten Kinetics/ non-linear kinetics/ capacity limited

A

Carrier-Mediated Transport

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8
Q

Drug that crosses the BBB because of large neutral AA transporter (LNAAT)

A

Levodopa

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9
Q

Elimination is DEPENDENT on drug concentration

A

First Order

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10
Q

▪️Drug clearance is on a constant rate
▪️INDEPENDENT on drug concentration

A

Zero Order

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11
Q

Energy requiring; against concentration gradient (uphill); fastest

A

Active Transport

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12
Q

No energy requirement; along concentration gradient; passive diffusion with carrier

A

Facilitated Diffusion

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13
Q

Drug passes through water filled pores; only paracellular transport mechanism

A

Convective Transport / Bulk Flow

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14
Q

Important for movement or transport of large ions

A

Ion-Pair Transport

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15
Q

▪️ release of drug from the dosage form
▪️ end product: drug in aqueous form/sol’n
▪️ highly modifiable

A

Liberation

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16
Q

▪️Physiologic: rate and extent of drug disappearance from the site of administration
▪️Pharmacokinetic: rate and extent of drug entry into the systemic circulation

A

Absorption

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17
Q

Is the measure of rate and extent of drug entry into the systemic circulation / pharmacokinetic absorption

A

Bioavailability [BA] or [F]

18
Q

2 Methods of Bioavailability

A
  1. Cumulative Urinary Excretion Data
  2. Drug Plasma Concentration vs Time Graph
19
Q

Maximum plasma concentration; measures both rate and extent of absorption; most variable

A

Cmax

20
Q

Time it takes to reach Cmax; measures rate only; least important

A

Tmax

21
Q

Area under the curve; measures extent only; most important

A

AUC

22
Q

Types of BA

▪️ same dose, different routes

A

Absolute Bioavailability

23
Q

Types of BA

▪️ use when comparing a generic drug to a reference standard
▪️ same dose, same route particularly PO

A

Relative Bioavailability

24
Q

Main site of drug absorption

A

Small intestine

25
Q

Time it takes the stomach to empty its contents into the small intestine

Normal: 2-3 hours

A

Gastric Emptying Time (GET)

26
Q

Faster Emptying, Faster Absorption, Lower

A

Lower GET

27
Q

What Factors Increasing GET (slower absorption)

A

▪️high fat / protein meal, happy meal
▪️ stress
▪️ strenuous exercise (heavy)
▪️ gastric ulcers
▪️ lying on the LEFT side
▪️ anticholinergics, opioid, morphine, nalbuphine

28
Q

What Factors Decreasing GET (faster absorption)

A

▪️ extreme temperature of food
▪️ mild exercise
▪️ DM
▪️ lying on the RIGHT side
▪️ cholinomimetics
▪️ prokinetics: domperidone metoclopramide

29
Q

▪️ SAME API, salt / ester / complex and dosage form and strength
▪️ DIFFERENT in excipients used such as flavorants and colorings

A

Pharmaceutical Equivalents

30
Q

▪️SAME API
▪️DIFFERENT salt/ester/complex, dosage form & strength

A

Pharmaceutical Alternative

31
Q

▪️SAME API in the same dosage form and route of administration
▪️ Similar bioavailability

A

Therapeutic Equivalents

32
Q

▪️SAME drug class
▪️DIFFERENT API

A

Therapeutic Alternatives

33
Q

Reversible transfer of a drug from the systemic circulation to the site of action and to the other compartment

A

Distribution

34
Q

Pharmacokinetic Parameters:

Hypothetical value of body fluid required to dissolve a given amount of drug concentration equal to that of plasma concentration

A

Volume of distribution (Vd)

35
Q

Drugs that undergo extensive protein binding (WNMS)

A

Warfarin
NSAIDs (Phenylbutazone)
Midazolam
Sulfa drugs

36
Q

▪️Biotransformation
▪️Primary Goal: to convert drugs into an inactive / less active non-toxic / less toxic polar, water soluble

A

Metabolism

37
Q

Initially inactive

A

Prodrug

38
Q

Aka Pre-systemic metabolism

A

First Pass Effect

39
Q

▪️Final loss drug from the body
▪️Requirement: polar, water soluble

A

Excretion

40
Q

▪️Main excretory organ
▪️Requirement: Polar; Low MW <400-600

A

Kidneys

41
Q

▪️Slow Acetylators
▪️Fast Acetylators

A

▪️Caucasians
▪️Asians

M4: Pharmacology-Pharmacokinetics (50 decks)

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