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Semester 3 > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

What is a Drug?

A

Any Substance that , when administered to a living organism brings about functional changes as a consequence of interactions at the molecular level

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2
Q

What is Pharmacokinetics?

A

The Absorption , Distribution , Metabolism , Elimination of Drugs

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3
Q

What is the Pharmacological effect , action and Mechanism of Action of NorEpi on Cardiac tissue?

A

Pharmacological Effect

The observed event which has been produced by the drug ( Tachycardia)

Pharmacological Action

The functional modification that leads to that effect( Increased frequency of spontaneous depolarization of the SA node)

The Mechanism of Action

The molecular modification that causes that action ( Cardiac beta receptors)

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4
Q

What are the Two Permeation processes for the movement of Drugs?

A

Diffusional Transport ( Cell Membrane)

Bulk Flow Transport ( Intercellular Pores)

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5
Q

What is the most frequent process for the movement of drugs across the cell membrane?

A

Lipid Diffusion

Proportional to the Concentration Gradeint and the Area of Diffusion

Inversely Proportional to the Thickness of the Membrane

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6
Q

How is Lipid Diffusion mainly determined?

A

Oil/Water Partition Coefficient

Passive Process

Nonselective Process

Most Drugs around 100 to 1500D

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7
Q

What are the Characteristics of Aqueous Diffusion of a drug across the Cell Membrane?

A

Occurs through protein channels ( 7 Angstrom wide)

Maximum MW of 100

Proportional to protein channels and concentration gradient

Passive Process

Nonselective Process

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8
Q

What is the Oil/Water partition coefficient?

A

Index of the Relative Solubility of the drug in lipid and water

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9
Q

What do Ionized and Nonionized Molecules readily associate with in the cell?

A

Ionized: Water (Hydrophillic)

Nonionized: Lipid Soluble ( Lipophilic)

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10
Q

What quantitative difference is required between pH and pK to ensure the molecule is Ionized?

A

Above 3 = 99.99% Ionized

Weak Acid

pKa - pH

pK higher then pH ensures non ionized ( Lots of Protons)

Weak Base

pH-pK

pK lower then pH ensures non ionized

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11
Q

What is the Ion Trapping Mechanism?

A

Aspirin (pKa of 3.5)

In the Gastric Lumen: 1.5 pH = NI

In the Cell: 7 pH = Ionized and Trapped

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12
Q

What does the Ion Trapping Mechanism Ensure?

A

A concentration gradient of the nonionized form will remain high

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13
Q

What is the clinical importance of the Ion trapping mechanism?

A

Can accelerate the elimination of drugs from the kidneys

Acidic Drugs can be trapped in the tubular lumen by making urine alkaline (Basic= Ionized)

Basic Drugs can be trapped in the tubular lumen by making the urine acidic ( Acidic=Ionized)

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14
Q

What are characteristics of Facilated Diffusion?

A

Protein Carrier

Passive

Selective

Saturable

Subject to Inhibition

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15
Q

What are the Characteristics of Active Transport of a Drug across a cell membrane?

A

Protein Carrier

Active

Selective

Saturable

Subject to Inhibition

Against Concentration Gradient

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16
Q

What are the four mechanism carrier mediated drug transport?

A

GI Tract

Biliary Tract

Renal Tubule

Blood Brain Barrier

17
Q

What size molecules of drugs will enter with endocytosis and exocytosis?

A

100,000 Daltons

Active Transport

NonSpecific: Physicochemical Character

Specific: Receptor Mediated

18
Q

What drug molecules transport through Bulk Flow through Intercellular Pores?

A

Pressure Gradient

Passive Process

Nonselective Process

Drugs with Molecular Size of 15000-16000 Daltons

Through Capillary Pores

Any higher then that

19
Q

What is first order kinetics and how does it relate to the processing of drugs?

A

A process is called first order when a constant fraction ( or percentage) of what must be processed , is processed per unit time

20
Q

What compartment model is the human body assumed to be?

A

One Compartment Model

Drug is Instantly and Uniformly Distributed

21
Q

What is Drug Absorption?

A

the process by which the unchanged drugs proceeds from the site of administration to the site of measurement within the body

22
Q

What is Bioavailability and how is it influenced?

A

The fraction of a drug dose reaching unchanged the systemic circulation when administered by any route

The Route of Administration

23
Q

What is Cmax , Tmax and AUC?

A

Peak Concentration(Cmax): the maximum drug concentration reached in plasma after administration of a given dose ( related to ADME)

Time to Peak Concentration (Tmax): the time to maximum drug concetration in plasma. Inversely proportional to the rate of drug absorption

Area Under the Curve(AUC): the total amount of drug that reaches the systemic circulation and relfects absorption , distribution and elimination factors of a drug

24
Q

What are the Advantages and Disadvantages of Oral Drug Administration?

A

Advantage

Hastened and Delayed

Safest , Cheapest and Easiest

Disadvantages

GI upset

Digestive secretion

First Pass Effect

25
Q

What are the Factors that affect Oral Drug Administration?

A
26
Q

How can Gastric Emptying be hastened and delayed?

A
27
Q

What is Presystemic Elimination?

A

The fraction of the drug that is eliminated during the first pass through the liver

28
Q

What are the Advantages and Disadvantages of Sublingual/Buccal Drug Administration?

A
29
Q

What is the Advantages and Disadvantages of Rectal Drug Administration?

A

Advantages

Avoid the First Pass Effect

Do not need to be awake

Seizures

Disadvantages

Lower oral absorption then most cases

Influenced by degree of rectum content

Can Irritate the Mucosa

30
Q

What are the Advantages of Cutaneous Drug Administration(Topical)?

A

Advantages

Drug Concentration is locally high

Systemic adverse effects are minimal

Disadvantages

Systemic adverse effects can occur if the skin is damages

31
Q

What is the Advantage and Disadvantages of Transdermal Administration?

A

Advantages

First Pass effect is avoided

Dont need to be Awake

Repeated administration are minimized

Disadvantages

Few drugs can be absorbed this way

Semester 3 (6 decks)

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