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Pharm 507 > Pharmacokinetics I > Flashcards

Pharmacokinetics I Flashcards

1
Q

Xenobiotic

A

Anything that enters the body

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2
Q

Drug

A

Brings about change in biological function through its chemical actions

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3
Q

Prodrug

A

Inactive form of a drug, converted to an active form in the body

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4
Q

Pharmacodynamics

A

Action of drug ON the body

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5
Q

Drug disposition

A

Qualitative; how the body handles the drug

How it’s absorbed, distributed, metabolized, eliminated

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6
Q

Pharmacokinetics

A

Quantitative description of drug disposition

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7
Q

First pass metabolism occurs where?

A

Liver

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8
Q

“A” in ADME

A

Absorption: transport drugs from site of admin to circulation

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9
Q

“D” in ADME

A

Distribution: delivery of drug via blood to tissues, drug must have adequate concentration at site of action to produce effect

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10
Q

“M” in ADME

A

Metabolism: parental compound converts to metabolite, compound made more amendable for excretion, occurs in liver, typically inactive metabolites but pharmacologically active

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11
Q

“E” in ADME

A

Excretion: via kidney or intestine

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12
Q

Most critical step for bioavailability?

A

Absorption

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13
Q

Factors that determine absorption

A

1) property of the drug (size, acid/base, lipophilic/hydrophobic)
2) vehicle/formulation
3) route of admin and conditions at route of admin

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14
Q

Route of admin most critically effects…

A

Rate of drug absorption

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15
Q

What does route of drug admin influence?

A

Extent and speed drug is absorbed
1st pass metabolism or not
Efficacy and therapeutic effect

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16
Q

Drug Route Administration - Enteral/Enteric

A

Oral - per os, PO
Buccal/sublingual - BU/SL
Rectal - REC

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17
Q

Oral Route of Admin characteristics & issues

A 
Enteral
Most common
Safest
Large SA
Intestine is site of absorption

Issues: slow & subject to liver first-pass metabolism

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18
Q

Buccal/Sublingual Route Admin: characteristics

A

Enteral
Small area, HIGH vascularization
Rapid absorption to VENOUS blood
Bypass liver first pass liver metabolism

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19
Q

Route of admin: rectal

A 
Enteral
Performed if oral is precluded
Suppository, foam, or liquid form
Drug placement isn’t well controlled
Absorbed 50% hepatic portal vein (proximal- first pass metabolism) and 50% to venous blood (distal- bypasses first pass metabolism)
20
Q

Drug Amin Routes - parenteral

A 
!! Bypass first pass metabolism !!
Subcutaneous (SC)
Intramuscular (IM)
Intravenous (IV)
Intrathecal (IT)
Inhalation
Intranasal
21
Q

Subcutaneous Injection

A

Poor blood flow
Sustained, slow release
Small volumes of drugs

22
Q

Intramuscular Injection

A

High blood flow = prompt absorption

Large volumes, prolonged release

23
Q

Intravenous Injection

A

Instant delivery - 100% absorption

Prone to adverse effects

24
Q

Intrathecal Injection

A

Subarachnoid space of spine
Bypasses BBB
Rapid effect on meninges or cerebrospinal axis
Used for spinal anesthesia

25
Q

Inhalation

A

Action on bronchioles, rapid access to circulation
High vascularization
Inhalation anesthetics, asthma inhalants

26
Q

Intranasal

A

Parenteral
Acts on nasal mucosa
Future drugs via vaccines

27
Q

Topical Drug Admin

A

Ophthalmic drops

Dermal

28
Q

Ophthalmic drops

A

Instillation into eye for local effect

29
Q

Dermal

A

Topical
Local acting
Systemic absorption - oily vehicles, transdermal patches, Iontophoretic and phonophoretic delivery

30
Q

Transdermal Iontophoretic Delivery

A

Delivery of ionic molecules into tissues by electric current

(-) charged drug driven into skin from cathode to anode

31
Q

Route of Drug Admin (quickest to slowest)

A 
IV
Inhalation
SL
IM
SC
REC
PO
Transdermal
32
Q

Bioavailability

A

Fraction (F) of the dose of unchanged drug that reaches systemic circulation by any route

  • IV dose drugs have 100% bioavailability
  • other admin route <100%
33
Q

Bioavailability depends on:

A

Chemical form of drug
Rate of absorption
Contact time with absorbing surface
Enzymes and efflux transporters

34
Q

Drug Movement Across Biological Membranes

A

A - enter circulation
D - traverse within the body, critical concentration needed at site of action
M - drug moves into liver
E - drug/metabolites must be eliminated

35
Q

Mechanisms by which drugs are transported after admin

A

Passive Transfer - bulk flow/filtration, passive diffusion

Carrier-Mediated Transport - facilitated diffusion, active transport, receptor-mediated endocytosis

36
Q

Bulk Flow/Filtration

A

Passage of compounds through intercellular pores

Drug flows through intercellular clefts or fenestra

37
Q

Filtration/Bulk Flow Drug Size

A

MW < 300-500 daltons

38
Q

Filtration/Bulk Flow Drug Types

A

Ionic, lipophilic, hydrophilic, etc.

39
Q

Examples of Bulk Flow/Filtration

A

Peripheral capillaries

Glomerular filtration in kidney

40
Q

Passive Diffusion

A

Passage of drugs by dissolving into and diffusing across lipid membranes through intercellular cleft

MOST IMPORTANT TRANSPORT PROCESS, most common route of transport for enteral route

41
Q

Properties of molecules that cross by passive diffusion

A

1) uncharged, non-ionized
2) lipid soluble (lipophilic, hydrophobic)
- non-polar groups increase solubility (CH2, CH3, aromatic rings)
- polar groups decrease lipid solubility (OH, COOH, NH, sulfates, ionized groups)
3) correlation of absorption and lipophilicity

42
Q

Lipophilicity

A

Measured by distribution in an immiscible mix of organic-aqueous solvent

43
Q

Passive Diffusion of Non/ionic Drugs

A

Small MW organic acids or bases that exist as ionized and non-ionized forms (non-ionized can diffuse, ionized cannot)
Classified as acids or bases based on the uncharged (neutral) form of drug

44
Q

Charged & Uncharged Forms of Acidic Drugs

A

Acidic drug is neutral molecule which can reversible dissociate into an anion (conj. base) to yield a proton donor

45
Q

Charged and Uncharged Forms of Basic Drugs

A

Basic drug is a neutral molecule which can form a cation (conj. acid) by combining with a proton (proton acceptor)

Pharm 507 (6 decks)

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