PHARMACOKINETICS 1 Flashcards

1
Q

A KEY DETERMINANT OF THE EFFECTIVENESS AND USEFULNESS OF A DRUG DEPENDS ON ACHIEVING THE CORRECT ………..

A

CONCENTRATION

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2
Q

WHAT ARE THE THINGS THAT AFFECT DRUG CONCENTRATION

A

MECHANISM OF ACTION OF THE DRUG
THE DRUG TARGET
THE PHYSICOCHEMICAL PROPERTIES OF THE DRUG
BODILY PROCESSES

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3
Q

WHAT BODILY PROCESS AFFECTING DRUG CONC

A

ABSORPTION
DRISTRIBUTION
METABOLISM
EXCRETION

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4
Q

WHAT CAN BE SAID ABOUT THE CONCENTRATION OF A DRUG THROUGHOUT THE BODY

A

THE CONCENTRATION WILL REACH A CONSTANT BUT THIS CONSTANT WILL BE DIFFERENT ACROSS BODILY COMPARTMENTS

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5
Q

WHAT DIFFERENT BODY COMPARTMENTS ARE THERE

A
PLASMA
ISF
LYMPH
FAT
IC FLUID
TRANSCELLULAR FLUID
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6
Q

HOW DO DRUGS MOVE BETWEEN COMPARTMENTS

A

VIA BARRIERS

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7
Q

HOW CAN DRUGS MOVE ACROSS BARRIERS

A

DIFFUSION THROUGH THE BILAYER
DIFFUSION THROUGH CHANNELS
CARRIERS
PINOCYTOSIS

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8
Q

WHAT IS THE PARTITION CO-EFFICIENT

A

THIS IS A MEASURE OF LIPID SOLUBILITY

IE THE HIGHER THE CO-EFFICIENT THE MORE EASILY DIFFUSIBLE IN LIPIDS

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9
Q

NON POLAR MOLECULES DISSOLVE ………………… IN LIPIDS AND PENETRATE CELL ……………………… FREELY. THIS MEASURE THAT THERE IS AN ………………….. RATE OF GUT ABSORPTION AS WELL AS PENETRATION INTO BRAIN AND TISSUES AS WELL AS ……………………… EXRETION.

A

FREELY
MEMBRANES
INCREASED
RENAL

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10
Q

DIFFUSION IS ……………………. TO THE SIZE OF THE DRUG

A

PROPORTIONAL

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11
Q

WHAT ARE THE ROUTES OF ADMINISTRATION

A
ORAL/RECTAL
PERCUTANEOUS
INTRAVENOUS
INTRAMUSCULAR
INTRATHECAL
INHALATION
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12
Q

WHAT IS THE FASTEST ROUTE OF ADMINISTRATION

A

INTRAVENOUS

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13
Q

WHERE IS THE MORE COMMON SITE OF ADMINISTRATION FOR BIOLOGICS AND WHY

A

INTRAMUSCULAR

TO ESCAPE METABOLISM

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14
Q

WHAT IS INTRATHECAL

A

DIRECTLY IN CSF

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15
Q

WHAT IS BIOAVAILABILITY

A

FREE CONC OF DRUG IN PLASMA/THE AMOUNT OF DRUG TAKEN

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16
Q

WHAT FORM DO DRUGS COME AS USUALLY

A

SALTS FROM WEAK ACIDS AND BASES

17
Q

WHAT IS PKA

A

A DISSOCIATION CONSTANT THAT DESCRIBES THE RATIO OF DISSOCIATED TO NON DISSOCIATED FORM OF ACID AT DIFFERENT PH

18
Q

WHAT IS THE FORMULA FOR AN ACID

A

HA ——- H+ + A-

19
Q

THE NON DISSOCIATED FORM OF ACID (HA) IS WHAT

A

NON POLAR (THEREFORE WOULD DIFFUSE EASILY)

20
Q

THE DISSOCIATED FORM OF ACID (H+ + A-) IS WHAT

A

POLAR (THEREFORE WILL NOT DIFFUSE AS EASILY)

21
Q

HOW TO WE CALCULATE PKA

A

PKA= PH + LOG([HA]/[A-])

22
Q

IF THE PKA WAS 3 WHAT DOES THIS ACTUALLY TELL US

A

3 TIMES MORE OF THE DRUG DIGESTED WILL BE IN UNDISSOCIATED FORM THAT DISSOCIATED FORM AND THEREFORE WILL DIFFUSE WELL

23
Q

WEAK ACIDS IN AN ACIDIC ENVIRONMENTS (IE LOW PH) TEND TO …………………. PKA. IF PKA IS ……………. THEN MORE OF THE DRUG WILL BE IN ………………….. FORM

A

DECREASE
LOWER
NON DISSOCIATED

24
Q

WHAT HAPPENS TO WEAK ACIDS IN MORE ALKALINE ENVIRONMENTS

A

THE PKA INCREASES
MORE OF THE DRUG WILL BE IN DISSOCIATED FORM AND THEREFORE CANNOT DIFFUSE WELL BETWEEN COMPARTMENTS
THE CONCENTRATION WILL THEN BUILD IN THAT COMPARTMENT (TRAPPED)

25
Q

EXPLAIN ONE WAY IN WHICH MORE ALKALINE ENVIRONMENTS FOR DRUGS CAN BE DANGEROUS AND ONE WAY IN WHICH IT CAN BE HELPFUL

A

ACCUMULATION OF DRUGS IN A COMPARTMENT CAN CAUSE TOXICITY

ALKALINISATION OF THE URINE MEANS HIGHER DISSOCIATED FORM FOR DRUG EXCRETION IN THE CASE OF POISONING

26
Q

HOW CAN YOU ALKALINISE URINE FOR USE IN TREATMENT OF POISONING

A

NAHCO3

27
Q

WHEN CONSIDERING TRANSPORTERS AS A MEANS OF DIFFUSION WHAT CAN AFFECT DRUG CONCENTRATION

A

GENETIC VARIATION/POLYMORPHISMS IN TRANSPORTERS

28
Q

WHAT IS AN EXAMPLE OF A POLYMORPHISM IN A TRANSPORTER THAT AFFECTS DRUG CONCENTRATION

A

OCT1 TRANSPORTER ARE ASSOCIATED WITH DIFFERENT RESPONSES TO METFORMIN IN HEALTHY HUMANS AFFECTING ABILITY TO MAINTAIN BLOOD SUGAR LEVELS

29
Q

WHAT IS METFORMIN USED FOR

A

TREATMENT OF DIABETES TYPE 2