1. Absorption Flashcards

1
Q

what is PHARMACOKINETICS the STUDY OF

A

what the BODY DOES TO A DRUG

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2
Q

only SMALL PORTION of the DRUG reaches the SITE OF ACTION. what happens to the rest?

A

either METABOLISED or ELIMINATED

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3
Q

drug by ORAL ADMINISTRATION passage to SYSTEMIC CIRCULATION:

A

drug in solution
released in INTENSTINES lumen, passes intestines wall to the LIVER
(to systemic circulation)

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4
Q

drug by ORAL ADMINISTRATION passage to SYSTEMIC CIRCULATION:

A

DIRECTLY to Systemic Circulation

  • BYPASSES other organs etc
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5
Q

an understanding of PHARMACOKINETICS should help us to:

A
  • design DOSAGE Regimens
  • PERSONALISE/STRATIFT DOSAGE Regimen based on PATIENT’S CHARACTERISTICS
  • DETERMINE what is wrong when a patient FAILS to RESPOND to TREATMENT
  • find out why a Drug has CAUSED TOXICITY
  • Understand the MECHANISMS of DRUG INTERACTIONS
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6
Q

ROUTE of DRUG ADMINISTRATIONS:
(dependent on DRUG and TARGET AREA)

A
  • ORAL
  • SUBLINGUAL
  • RECTAL
  • other Epithelal surfaces:
    SKIN, CORNEA, VAGINA, NASAL MUCOSA
  • INJECTION
  • INHALATION
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7
Q

what is TOPICAL ADMINISTRATION

A

ON TO the SKIN

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8
Q

what is SYSTEMIC ADMINISTRATION

A

INTO the BODY

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9
Q

what is SYSTEMIC ADMINISTRATION: ENTERAL administration

A

GI TRACT ROUTE

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10
Q

what is SYSTEMIC ADMINISTRATION: PARENTAL administration

A

NON-GI TRACT ROUTE

eg. injection, inhalation

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11
Q

ORAL administration: what is Fa

A

Fraction of the dose AVAILABLE FOR ABSORPTION

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12
Q

ORAL administration: what is Fg

A

Fraction of the dose ESCAPING INTESTINAL METABOLISM
(ability to permeate intestinal wall)

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13
Q

ORAL administration: what is Fh

A

Fraction of the dose ESCAPING HEPATIC FIRST PASS METABOLISM
(penetration through first pass metabolism)

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14
Q

what is FIRST PASS METABOLISM

A

The degree of metabolic breakdown of an orally administered drug that occurs in the INTESTINE or LIVER BEFORE it reaches the SYSTEMIC CIRCULATION

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15
Q

How is PENETRATION and Cmax (max plama conc.) after INTRAVENOUS ADMINISTRATION

A

IMMEDIATE

Cmax at 0 Hours

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16
Q

what is HALF LIFE of a drug

A

Time taken for DRUG CONC to DECLINE by HALF

17
Q

how to CALCULATE FRACTIONAL BIOAVAILABILTY (F)

A

= AUC (ORAL) / AUC (IV)

AUC - area under the curve

18
Q

what is Drug BIOAVAILABILITY

A

FRACTION of the administered DOSE that ENTERS the SYSTEMIC CIRCULATION and so reaches SITE OF ACTION

19
Q

why can ABSORPTION be DELAYED

A

due to FOOD
- causes DECREASED GASTRIC EMPTYING RATE

20
Q

Why might you have DECREASED ABSORPTION:

A
  • drug UNSTABLE in Gastric Fluids
  • DECREASED SOLUBILITY due to CHANGES in pH
  • INCREASED FIRST PASS METABOLISM
    (GI Enzymes / Transporters can be INDUCED by Food / Concomitant Drugs)
21
Q

why might there be INCREASED or DECREASED FIRST PASS METABOLISM

A

INDUCTION or INHIBITION of GI ENZYMES or TRANSPORTERS

by FOOD or CONCOMITANT (accompanying) DRUGS

22
Q

why might you have INCREASED ABSORPTION

A
  • INCREASED SOLUBILISATION of poorly soluble drug due to CHANGES in pH
  • DECREASED FIRST PASS METABOLISM
    (Inhibition of GI Enzymes/Transporters by Food or Concomitant drugs)
23
Q

what can cause CHANGES in DRUG SOLUBILITY

A

PH CHANGES

24
Q

ORAL ADMINISTRATION is a RESULT of Multiple Processes:

A

Fa, Fh, Fg