Intro PDA Exam 2 – Flashcards

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question
How structure affects movement of the drug from point A to point B?
answer

ADME

Absorption

Distribution

Metabolism

Excretion

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What is the main organ most drugs have to go through?
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Liver
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Isomer
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Different compoiunds with the same molecular formula
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Aliphatic
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Alkanes

Alkenes

Alkynes

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In order for oxidation to occur, alkanes need what?
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An enzyme
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Rxns of Alkenes
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Halogenation

Hydrogenation

Oxidation

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Dienes
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Two double bonds
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w-oxidation
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Oxidation occurs on the last Carbon
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w-1 oxidation
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Oxidation occurs on the next to last carbon
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CH3CH2CH2OH
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Primary Alcohol
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[image]
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Secondary Alcohol
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[image]
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Tertiary Alcohol
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When oxidized primary alcohols form?
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Aldehydes and Carboxylic Acids
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When oxidized secondary alcohols form?
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Ketones
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[image]
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Ketone
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[image]
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Aldehyde
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[image]
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Carboxylic Acid
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[image]
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Ether
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[image]
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Ester
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[image]
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Amide
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When oxidized tertiary alcohols form?
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No Rxn
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Rate dehydration of alcohols from slowest to fastest
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Primary<Secondary<Tertiary
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Isolated Diene
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double bonds seperated by two single bonds
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[image]
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Isolated Diene
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Conjugated Diene
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Double bonds seperated by one single bond
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[image]
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Conjugated Diene
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Conjugated diene have ____ energy; more _____
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lower; stable
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Isolated diene has _____ energy; more ____
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higher; reactive
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[image]
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Phenol
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Electron Donating Groups
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-OH, -OR, -SH, -SR, -NR, -R1, -R2, -R3
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What do electron donating groups do to the aromatic ring?
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Activate
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If the R is electron donating, what can occur and where?
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Oxidation can occur

It occurs in the para position

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Electron Withdrawing Groups
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Halogens (F, Br, Cl, I)

COOH, aldehydes, ketones, ester

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T or F: Oxidation can occur when the R group is an electron withdrawing group
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False
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Five Acidic Functional Groups
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  1. Carboxylic Acid
  2. Sulfonic Acid
  3. Phosphoric Acid
  4. Sulfonamide
  5. Active methylene group
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[image]
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Sulfonic Acid
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[image]
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Phosphoric Acid
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[image]
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Sulfonamide
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Acids have a _____ pKa
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High
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Bases have a _____ pKa
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Low
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What is used to mease the stregth of an acid?
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pKa
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Are Amines basic or acidic?
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Basic
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T or F: Quaternary amines are not basic
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True
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Rules to determine if a drug is basic:
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  1. A nitrogen MUST be present
  2. Is there a strong electorn withdrawing gp attached to N? if yes NOT BASIC
  3. Does N carry a positive charge? if yes NOT BASIC
  4. If e's of N contribute to the aromaticity of a ring NOT BASIC
  5. If N is flanked by two e withdrawing gps NOT BASIC, but H is acidic
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Neutral Drug
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The drug does not contain any acidic grps and basic nitrogens
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Amphoteric Drugs
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The drug contains both an acidic grp and a basic Nitrogen
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Zwitterionic Drug
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A charged species
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How does a drug know where to go?
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  • Shape of drug
  • Affinity for receptor
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What happens to salt when it is placed in H20?
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Salt will undergo hydrolysis and the solution will becom ebasic
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3 Rxns of Carboxylic Acids
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  1. Ionization
  2. Neutralization
  3. Esterfication
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Esters undergo what type of rxn?
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Hydrolysis
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Diastereomeers
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these are the stereoisomers which are not mirror images
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Henderson- Hasselbach Equation
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PH= pKa + Log [cong. base]/[acid]
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Oxidation
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Removing a H
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Reduction
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Adding a H
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[image]
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Azo Group
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Reduction of azo groups will ALWAYS form ???
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Primary amines
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When determining the # of stereoisomers what equation would you use?
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2n

n= # of chiral centers

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Which configuration has coutner-clockwise rotation?
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S- configuration
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Which configuration has clockwise rotation?
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R- configuration
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Acids are proton _____
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Donors
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Bases are proton ______
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Acceptors
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Equation for % ionization;of acids
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100


1+10(pka-ph)

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What is the primary purpose for metabolism
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to facilitate elimination from the body
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In order for a drug to go thru phase 2 which groups must be present?
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-OH, -NH2, -COOH, -SH

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Oxidative N-dealkylation
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removal of an akyl group from a nitrogen
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Desulfuration
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removal of a sulfur
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Types of phase 1
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Oxidative

Reductive

Hydrolytic

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O-Glucuronic Acid Conjugation
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Adding glucuronic acid to an Oxygen
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Sulfate Conjugation
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Adding sulfur to a functional group
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Amino Acid Conjugation
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Adding an amino acid to a functional group

;

*can only happen on Carboxylic Acid*

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S- Methylation
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Adding a methyl group to a sulfur
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Types of Phase 2 Rxns
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Glucuronic Acid Conjugation (O, N, S)

Sulfate Conjugation

Amino Acid Conjugation

Methylation ( O, N, S)

Acetylation

Glutathione Conjugation

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