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Module 1 > Medicinal Chemistry > Flashcards

Medicinal Chemistry Flashcards

1
Q

The biotransformation of drugs in the body
* Important in the elimination of drugs from the body
* Converts drugs to hydrophilic, inactive and nontoxic

A

Metabolism

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2
Q

2 Phases of Metabolism

A

Functionalization & Conjugation

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3
Q

Phase 1 Metabolism is also known as

A

Functionalization

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4
Q

Phase 2 Metabolism is also known as

A

Conjugation

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5
Q

What are the reaction in Phase 1 metabolism

A

Oxidation, Reduction, Hydrolysis

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6
Q

Most common phase I reaction

A

Oxidation

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7
Q

functional group that undergone Oxidation reaction

A

Undergone by Olefins, Alcohols, Aldehydes & Aromatic moieties

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8
Q

What type of reaction?

Carbonyl compounds → Alcohol derivatives
* Nitro and Azo compounds → Amine derivatives
ex. Chloral hydrate → Trichloroethanol
*Prednisone – Ketone reduction → Prednisolone

A

Reduction

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9
Q

Reaction that commonly undergone by lactams, esters and amides

A

Hydrolysis

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10
Q

What type of reaction?
Aspirin → Salicylic acid + Acetic acid

A

Hydrolysis

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11
Q

Mechanism of Phase II Metabolism

A

Attach small. Ionizable, endogenous compounds to the functional handles

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12
Q

Reactions under Phase II Metabolism

A

Reactions: Glucuronidation, Sulfation, Glycine & Glutamine conjugation, Glutathione, Acetylation, Methylation

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13
Q

Purpose of PII Metab

A

Purpose:
1. Form excretable & inactive metabolites
2. Terminate/Attenuate activity
3. Detoxify

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14
Q

Glucuronidation enzyme

A

Coenzyme: Uridine-5’-diphospho-α-D-glucuronic acid
(UDPGA)

Transferase enzyme (TE): Glucuronyltransferase

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15
Q

Caution for Glucuronidation

A

Not yet developed in neonates

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16
Q

Sulfation enzymes

A

Coenzyme: 3 phosphoadenosine-5 phosphosulfate (PAPS)

TE: Sulfotransferase

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17
Q

Major process of metabolism happened in Neonates

A

Sulfation

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18
Q

Mechanism of Sulfation

A

Yields water soluble and inactive conjugates

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19
Q

The first mammalian metabolite discovered from glycine conjugation

A

Hippuric acid

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20
Q

Amino acids that are present in Glutathione

A

Cysteine, Glycine, Glutamine

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21
Q

Metabolism process which termination of activity & detoxification

A

Acetylation

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22
Q

Acetylation enzyme

A

N-acetyltransferase

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23
Q

Acetyl group supplier

A

Acetyl-CoA

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24
Q

Europeans, Caucasians, Egyptians (Low dose) are examples of

A

Slow acetylators

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25
Q

Eskimos & Asians (High dose) are examples of

A

Fast acetylators

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26
Q

When orally administered drugs are extensively metabolized before reaching the systemic circulation

A

First-Pass Metabolism / Pre-systemic metabolism

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27
Q

Drugs with extensive first pass effect

A

Isoproterenol
Lidocaine
Morphine
Meperidine
Nitroglycerin
Pentazocine
Propoxyphene
Propranolol
Salicylamide
Grape Fruit

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28
Q

ENZYME INHIBITORS
“SICKFACES.COM”

↑ enzyme activity
↑ drug metabolism
↓ drug effect

A

Sodium valproate
Isoniazid
Cimetidine
Ketoconazole
Fluconazole
Alcohol (Acute)
Ciprofloxacin
Erythromycin
Sulfonamide
Chloramphenicol
Omeprazole
Metronidazole

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29
Q

ENZYME INDUCERS
“GPPPRS CAM”

↓ enzyme activity
↓ drug metabolism
↑ drug effect

A

Griseofulvin
Phenobarbital (Barbiturates) Phenytoin
Phenylbutazone
Rifampicin
Sulfonylurea Carbamazepine
Alcohol (chronic) Meprobamate
St. John’s wort
Valencia oranges

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30
Q

application of agent to living tissue to prevent infection

A

Antisepsis

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31
Q

destruction or reduction in the number
of microorganisms

A

Decontamination

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32
Q

chemical or physical tx on inanimate surfaces

A

Disinfection

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33
Q

reduction of microbial load on inanimate
surface to a level acceptable for public health purposes

A

Sanitization

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34
Q

kill or remove all types of microorganisms

A

Sterilization

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35
Q

kills nonsporulating microorganisms by hot
water @ 65C-100C

A

Pasteurization

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36
Q

anti-infective agents used locally

A

Germicides

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37
Q

Suffix used for “kill”

A

-Cidal

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38
Q

Suffix used for “prevent growth”

A

-static

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39
Q

True or False?

↑ # of C - ↑ antibacterial activity up to C8 only

A

True

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40
Q

True or False?

↑ 9C – nonpolar ↓ water solubility, ↓ antibacterial activity

A

True

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41
Q

state the Isomeric alcohol potency decreases in the order

A

Primary > Secondary > Tertiary

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42
Q

MOA of Alcohol

A

Protein denaturation/precipitation

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43
Q

most widely abused of all recreational drugs

A

Alcohol

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44
Q

Percentage of commercial alcohol

A

95%

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45
Q

Ethanol to Acetaldehyde Enzyme:

A

alcohol dehydrogenase

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46
Q

Acetaldehyde to Acetic acid Enzyme:

A

aldehyde dehydrogenase

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47
Q

Used as an antidote for methanol poisoning and Inhibits alcohol dehydrogenase

A

Fomepizole

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48
Q

inhibits aldehyde dehydrogenase and used as a deterrent for alcohol addiction

A

Disulfiram

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49
Q

Type of alcohol that has 95% alcohol

A

Absolute alcohol

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50
Q

Type of alcohol that has 99% alcohol, prepared by azeotropic distillation

A

Dehydrated alcohol

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51
Q

Type of alcohol that has 49-50% alcohol

A

Diluted alcohol

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52
Q

Type of alcohol that has EtOH rendered unfit for use in beverages by the addition of subs.

A

Denatured alcohol

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53
Q

Type of alcohol that contains added wood alcohol and benzene unsuitable for internal or
external use

A

Completely denatured alcohol

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54
Q

Type of alcohol that treated with subs. so that its use is permitted for specialized purpose
ex. Iodine in alcohol

A

Specially denatured alcohol

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55
Q

also known as 2-propanol

A

Isopropyl alcohol

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56
Q

Isopropyl alcohol is also a substitute for?

A

Ethanol

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57
Q

True or False:

Isopropyl alcohol is prepared by sulphuric acid catalyzed hydration of propylene

A

True

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58
Q

Molecular formula for Ethylene alcohol

A

C2H4O

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59
Q

MOA of Ethylene alcohol

A

MOA: alkylation of bacterial protein by nucleophilic opening
of oxide ring

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60
Q

It is used to sterilize (gas sterilant) temperature sensitive pharmaceuticals and equipment that can’t be autoclaved

A

Ethylene alcohol

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61
Q

Product of 10% ethylene oxide + 90% CO2

A

Carboxide

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62
Q

aka: Methanal, HCHO

A

Formaldehyde

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63
Q

MOA of Formaldehyde

A

MOA: direct and nonspecific alkylation of nucleophilic functional groups of proteins

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64
Q

It is used as embalming fluid, disinfectant

A

Formaldehyde

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65
Q

aka: Glutarol

A

Glutaraldehyde

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66
Q

sterilizing solution for equipment and phcals that cannot be autoclaved

A

Glutaraldehyde

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67
Q

Cidex®

A

Glutaraldehyde

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68
Q

aka: Carbolic acid, C6H5OH

A

Phenol, USP

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69
Q

He discovered Phenol

A

Joseph Lister

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70
Q

True or False:

Substitution at ortho position increases bacterial activity

A

False.

Substitution at [para] position increases bacterial activity

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71
Q

Microorganism that Phenols can kill?

A

a strain of Salmonella typhi

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72
Q

Phenol coefficient formula

A

Dilution of a disinfectant/Dilution of phenol

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73
Q

phenol with 10% water

A

Liquefied phenol

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74
Q

aka: PC-MX, Metasep
antibacterial & antifungal

A

p-chloro-m-xylenol

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75
Q

aka: pHisoHex
in soaps, lotions, shampoos

A

Hexachlorophene

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76
Q

aka: Methylphenol
From coal tar or petroleum by alkaline extraction

A

Cresol

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77
Q

aka: Isospropyl m-cresol
Antifungal property

A

Thymol

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78
Q

from oil of Thymus vulgaris (Thyme)

A

Thymol

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79
Q

aka: 4-allyl-2-methoxyphenol
from clove oil
has dental analgesic “toothache drops”, used in mouthwashes

A

Eugenol

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80
Q

aka: m-dihydroxybenzene
keratolytic agent

A

Resorcinol

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81
Q

it is often used in throat lozenges

A

Hexylresorcinol

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82
Q

It is effective against anaerobic bacteria

A

Oxidizing agents

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83
Q

MOA of Oxidizing agents

A

MOA: liberation of oxygen in the tissues (peroxides)

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84
Q

Used for cleansing contaminated wounds
& Transient action (rapid action, short duration)

A

Hydrogen Peroxide (H2O2)

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85
Q

complex of urea and H2O2

A

Carbamide Peroxide

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86
Q

Vanoxide, Panoxyl
most effective topical OTC agent for acne

A

Hydrous Benzoyl Peroxide

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87
Q

oldest germicide in use today

A

Iodine (I2)

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88
Q

Iodine (I2) is Iodination of what aromatic residues

A

(phenylalanyl & tyrosyl)

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89
Q

Official iodine preparations in the USP: 2% in H2O with NaI

A

Iodine solution

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90
Q

Official iodine preparations in the USP: 5% I2 in H2O with KI

A

Strong Iodine Solution (Lugol’s)

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91
Q

Official iodine preparations in the USP: 2% in 50% alcohol with NaI

A

Iodine Tincture

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92
Q

It is admixed to increase the solubility of I2 and to reduce its volatility

A

Inorganic iodide salts

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93
Q

It is the complexes of iodine and non-ionic surfactants and also removed irritant properties

A

Iodophors

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94
Q

Example of Iodophors

A

Povidone-Iodine (Betadine, [PVP]-Iodine)

A complex with the non-ionic surfactant polymer,
polyvinylpyrrolidone

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95
Q

It is used for disinfection of water supplies

A

Chlorine (Cl2)

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96
Q

MOA of Cl2

A

MOA: chlorination of amide nitrogen atoms in proteins, oxidation of sulfhydryl groups

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97
Q

It is the active germicidal species formed when Cl2 is dissolved in water

A

Hypochlorous acid (HClO)

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98
Q

quaternary ammonium compounds that ionize in water and exhibit surface active properties

inactivated by soaps and other anion detergents & tissue constituents, blood, serum, and pus tend to reduce the effectiveness of these substances

A

Cationic surfactant

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99
Q

MOA of Cationic Surfactants

A

MOA: adsorb onto the surface of the bacterial cell, at which they cause lysis

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100
Q

new generic name of Merthiolate

A

Benzalkonium chloride (Merthiolate, Zephiran)

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101
Q

used to control diaper rash in infants caused by Candida albicans

A

Methylbenzethonium Chloride (Diaparene)

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102
Q

antiseptic in mouthwash and lozenges

A

Cetylpyridinium chloride

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103
Q

FDA approved for the Tx of gingivitis

A

Cetylpyridinium chloride

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104
Q

It is classified under biguanides
It is not a cationic surfactant but share many physical, chemical and antimicrobial properties
Also used in oral surgery, mouthwash, and irrigation

A

Chlorhexidine gluconate (Hibiclens)

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105
Q

It is added to prevent microbial contamination
* Ideal preservative
* Effective at low concentrations
* Nontoxic, compatible with other constituents of the preparation
* Stable for the shelf life of the preparation

A

Preservatives

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106
Q

esters of p-hydroxybenzoic acid have
antifungal properties

A

Parabens

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107
Q

aka: Methyl-p-hydroxybenzoate
Effective against molds

A

Methylparaben

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108
Q

aka: Propyl-p-hydroxybenzoate
Effective against yeast

A

Propylparaben

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109
Q

Preferred preservatives for drugs in oil
or lipophilic bases

A

Butylparaben & Ethyl paraben

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110
Q

camphor like aroma
a bacteriostatic agent in pharmaceuticals for injection, ophthalmic use, and intranasal administration

A

Chlorobutanol

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111
Q

aka: phenylcarbinol, phenylmethanol
from oil of jasmine
preservative in vials of injectable drugs

A

Benzyl alcohol

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112
Q

a/e of Benzyl alcohol

A

gasping syndrome

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113
Q

Naturally from gum benzoin and in peru and tolu balsams

effective as a preservative in food and pharmaceutical products at low pH

A

Benzoic acid

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114
Q

Use of Sodium propionate

A

Antifungal

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115
Q

Antifungal preservative in preserve syrups, elixirs, ointments, and lotions containing components such as sugars

A

Sorbic acid

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116
Q

True or False:

Anionic dyes are active against gram (+) and fungi but gram (-) are generally resistant

A

False

Cationic dyes are active against gram (+) and fungi but gram (-) are generally resistant

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117
Q

2 Triphenylmethane dyes

A

Gentian Violet & Basic Fuschin

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118
Q

aka: Crystal violet, methyl violet, methyl-
rosaline chloride

Pessaries for that tx of yeast infections
(1-3%)

also used as anthelminthic for strongyloides
(liquid form)

A

Gentian Violet

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119
Q

mixture of chlorides of rosaniline
and p-rosaniline

A

Basic Fuschin

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120
Q

aka Castellani’s paint

A

carbol fuschin

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121
Q

Tx of fungi, ringworm & athlete’s foot

A

Basic Fuschin

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122
Q

Only Thiazine dye

A

Methylene blue

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123
Q

Antidote for cyanide poisoning

A

Methylene blue

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124
Q

Antiseptic property in Tx of
cystitis and urethritis

A

Methylene blue

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125
Q

a/e of Methylene blue

A

a/e: blue-green color of stool

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126
Q

at one time very popular antiseptic for skin and ocular infections because it is nonirritating and non-staining

A

Nitromersol

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127
Q

preservative of vaccines, antitoxins, and immune sera

A

Thimerosal

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128
Q

old generic name of Merthiolate

A

Thimerosal

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129
Q

classification of drugs that are capable of eliminating parasitic worms or helminths

A

Anthelmentics

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130
Q

What are the Helmentics?

A

Cestodes (tapeworms), Trematodes (flukes),
Nematodes (roundworms)

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131
Q

Name all the Antihelmentics for Nematodes

A

Piperazine
Pyrantel Pamoate
Thiabendazole
Mebendazole
Albendazole
Ivermectin
Diethylcarbamazine (DEC)

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132
Q

Tx of pinworm roundworm

A

Piperazine

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133
Q

Tx of pinworm, roundworm (ascaris)

A

Pyrantel Pamoate

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134
Q

broad spectrum anthelminthic (whip, pin, round, hook)

A

Thiabendazole, Mebendazole & Abendazole

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135
Q

Tx of onchocerciasis (river blindness) – Oncocerca volvulus

A

Ivermectin

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136
Q

Tx of Filiariasis

A

Diethylcarbamazine (DEC)

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137
Q

MOA of Piperazine

A

MOA: block response of ascaris muscle to Ach → leading to placid paralysis

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138
Q

MOA of Pyrantel Pamoate

A

MOA: depolarizing Nm blocking agent → spastic paralysis

should not be used with piperazine (opposite effects)

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139
Q

MOA of Thiabendazole

A

MOA: inhibit fumarate reductase / antimitotic /
antimicrotubule

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140
Q

MOA of Mebendazole

A

MOA: irreversibly blocks glucose uptake → depleted glucose/ antimitotic/ antimicrotubule

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141
Q

MOA of Albendazole

A

MOA: antimitotic/ antimicrotubule

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142
Q

It came from Streptomyces avermitilis

A

Ivermectin

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143
Q

MOA of Ivermectin

A

MOA: stimulating gaba → blocked interneuron-motor neuron transmission

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144
Q

Name all the Antihelmentics for Trematodes

A

Praziquantel
Niridazole
Oxamniquine
Bithionol

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145
Q

MOA of Praziquantel

A

MOA: increase Ca2+ membrane permeability → loss of Ca → contraction → paralysis → phagocytosis (DEATH)

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146
Q

Broad spectrum drug for Antihelmentics for Trematodes

A

Praziquantel

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147
Q

Agent of choice for blood flukes (schistosomes)

A

Praziquantel

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148
Q

It is used for schistosomiasis

A

Niridazole

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149
Q

MOA of Oxamniquine

A

MOA: inhibit DNA, RNA, Protein synthesis

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150
Q

Tx of Schistosoma mansoni

A

Oxamniquine

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151
Q

Agent of choice for liver fluke (Fasciola hepatica) and lung fluke (Paragonimus westermani)

A

Bithionol

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152
Q

Only anthelmentics for Cestodes

A

Niclosamide

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153
Q

MOA of Niclosamide

A

MOA: inhibit Oxidative phosphorylation

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154
Q

Protozoal infections are:

A

malaria, amoebiasis, giardiasis, trichomoniasis, toxoplasmosis, P carinii pneumonia

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155
Q

___________ are effective against both intestinal & extraintestinal forms of the disease

A

Emetine, Dehydroemetine, Metronidazole & Tinidazole

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156
Q

These are alkaloids from Ipepac

A

Emetine and Dehydroemetine

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157
Q

MOA of Emetine and Dehydroemetine

A

MOA: inhibit protein synthesis by preventing protein elongation (protoplasmic poison)

158
Q

Limited use of Emetine & Dehydroemetine is due to

A

toxic effects (GI, cardiovascular,
neuromascular)

159
Q

Uses of Emetine & Dehydroemetine

A

for balatidial dysentery, fascioliasis,
paragonimiasis

160
Q

Agent used for the tx of amoeba, giardiasis, trichomonas, anaerobic bacterial infections

A

Metronidazole (Flagyl, Protostat)

161
Q

MOA of Metronidazole

A

MOA: covalent binding of reactive intermediate from the reduction of 5-nitro group to the DNA → lethal effect

162
Q

a/e of Metronidazole

A

a/e: disulfiram like effect (if taken with alcohol)

163
Q

Amebicides that are effective only against intestinal form:

A

8-hydroxyquinoline
Iodoquinol
Diloxane

164
Q

MOA of 8-hydroxyquinoline

A

MOA: chelation of metal ions

165
Q

It is a derivative of 8-hydroxyquinoline

A

Iodoquinol

166
Q

Use of Iodoquinol

A

For acute and chronic intestinal amebiasis

167
Q

Agent used for the tx of asymptomatic carriers of E. histolytica

A

Diloxanide

168
Q

It is from the discovery of α-dichloroacetamides

A

Diloxanide

169
Q

Tx for Amoebiasis

Hint: 8 DIME

A

8-hydroxyquinoline
Diloxanide
Iodoquinol
Metronidazole
Emetine

170
Q

Tx for Pneumocytisis carinii pneumonia

Hint: CAP

A

Cotrimoxazole
Atovaquone
Pentamidine isethionate

171
Q

Drug of choice for PCP (Pneumocytisis carinii pneumonia)

A

Cotrimoxazole

172
Q

Combination of Sulfamethoxazole + Trimethoprim

A

Cotrimoxazole

173
Q

Prophylaxis for African trypanosomiasis (rapidly distributed to tissues where it is stored)

A

Pentamidine Isethionate

174
Q

Analog of Ubiquinone, a component of mitochondrial electron transport chain

A

Atovaquone

175
Q

MOA of Atovaquone

A

MOA: Interfere with the electron transport chain as it is antimetabolite for ubiquinone

176
Q

Tx for Trypanomosomiasis

Hint: BS MEN

A

Benznidazole
Suramin
Melarsoprol
Eflornithine
Nifurtimox

177
Q

Tx of African sleeping sickness

A

Eflornithine

178
Q

MOA of Eflornithine

A

MOA: irreversible inactivation of Ornithine decarboxylase

179
Q

Tx of South American trypanosomiasis (T. cruzi)

A

Nifurtimox

180
Q

Tx of Chagas disease

A

Benznidazole

181
Q

Drug of Choice or later stages of both forms of African trypanosomiasis

A

Melarsoprol

182
Q

Bisurea derivative containing six sulfonic acid groups

183
Q

It is used as long-term prophylactic agent for trypanosomiasis (due to high protein-binding, effect can last up to 3 months)

184
Q

Most effective therapy and treatment for Toxoplasmosis

A

Sulfadiazine + Pyrimethamine

185
Q

Tx of Leishmaniasis

A

Sodium Stibogluconate

186
Q

aka Sodium antimony gluconate

A

Sodium Stibogluconate

187
Q

MOA of Na Stibogluconate

A

MOA: inhibit phosphofructokinase

188
Q

Term for agents that control the mite Sacroptes scabei

A

Scabicides

189
Q

Term for agents that used to eliminate head, body, and crab lice

A

Pediculicides

190
Q

2 Scabicides

A

Benzyl Benzoate & Crotamiton

191
Q

from Peru balsam, also from benzyl alcohol + benzoyl chloride

A

Benzyl Benzoate

192
Q

Antipruritic (local anesthetic action), a colorless, odorless oily liquid and a 10% lotion/cream for scabies

A

Crotamiton

193
Q

2 scabicides & pediculicides

A

Permethrin & Lindane

194
Q

MOA of Permethrin

A

MOA: acts on nerve cell membranes → disrupt Na+ channel conductance → paralysis

195
Q

A synthetic pyrethrin

A

Permethrin

196
Q

___% lotion of Permethrin is used for the tx of lice

197
Q

___% cream of Permethrin is used for the treatment of scabies

198
Q

MOA of Lindane

A

MOA: direct contact poison, fumigant effect, stomach poison

199
Q

It is composed of chlorinated benzene (benzene hexachloride)

200
Q

Antineoplastic agent that can cause Nephrotoxic & acoustic n. Damage

A

Cisplatin & Carboplatin

201
Q

Antineoplastic agent that can cause Peripheral neuropathy toxicity

A

Vincristine

202
Q

Antineoplastic agent that can cause Cardiotoxicity

A

Doxorubicin

203
Q

Antineoplastic agent that can cause Pulmonary fibrosis

204
Q

Antineoplastic agent that can cause Hemorrhagic cystitis

A

Cyclophosphamide

205
Q

Antineoplastic agent that can cause Myelosuppression

A

Methotrexate, 5-Fluorouracil & 6-mercaptopurine

206
Q

MOA of Tyrosine Kinase Inhibitors

A

inhibits tyrosine kinase and prevents phosphorylation of kinase substrate by ATP

207
Q

Give some Tyrosine Kinase Inhibitors

Hint: ends with -tinib

A

Erlotinib, Imatinib

208
Q

Tyrosine Kinase inhibitors that inhibits EGFR

209
Q

Tyrosine Kinase inhibitors that inhibits BCR-ABL kinase

210
Q

Classification of Targeted Therapy agents

A
  1. Monoclonal antibodies
  2. Tyrosine kinase inhibitors
211
Q

This targeted therapy class target growth factor receptor and inhibit cell growth

A

Monoclonal antibodies

212
Q

Examples of Monoclonal antibodies

Hint: ends with -mab

A

Trastuzumab, Bevacizumab

213
Q

This monoclonal antibodies inhibit the HER-2/neu

A

Trastuzumab

214
Q

This monoclonal antibody inhibits human vascular endothelial growth factor (VEGF), preventing angiogenesis

A

Bevacizumab

215
Q

Hormonal therapy: Glucocorticoid receptor agonist

A

Prednisone

216
Q

Hormonal therapy: Selective Estrogen Receptor Modulator used for premenopausal px w/ HR (+) breast cancer

217
Q

Hormonal therapy: Selective Estrogen Receptor Down regulator

A

Fulverstant

218
Q

Hormonal therapy: Aromatase inhibitors used for postmenopausal px with HR (+) breast cancer

A

Anastrozole, Letrozole & Exemestane

219
Q

Cell cycle specific agents for G1-phase specific

A

L-asparaginase & Prednisone

220
Q

Source of L-asparaginase

221
Q

MOA of L-asparaginase

A

MOA: hydrolyzes asparagine to aspartic acid and ammonia,
thus depriving the tumor cells of asparagine, which is needed for protein synthesis

222
Q

Class under S-phase specific of cell cycle specific agents

A
  1. Camptothecin derivatives
  2. Hydroxyurea
  3. Antimetabolite
223
Q

MOA of Camptothecin derivatives (S-phase specific CCSA)

A

Inhibit Topoisomerase I

224
Q

Camptothecin derivatives drugs

A

Topotecan, Irinotecan

225
Q

Side effects of Camptothecin derivatives

A

S/E (Irinotecan): cholinergic diarrhea (mgt: Atropine or
Loperamide)

226
Q

MOA of Hydroxyurea

A

MOA: inhibits ribo-nucleotide reductase (RNR - conversion of
ribo- to deoxyribonucleotides)

227
Q

MOA of Antimetabolite

A

MOA: inhibit enzymes necessary for folic acid, DNA or RNA
synthesis

228
Q

What are the Antimetabolites?

A

Folic acid analogues
Pyrimidine analogues
Purine analogues

229
Q

Antimetabolite Folic acid analogues are:

A

Methotrexate & Pemetrexed

230
Q

Methotrexate toxicity

A

Myelosuppression

231
Q

Methotrexate toxicity antidote

A

Leucovorin/ Folinic acid

232
Q

Pyrimidine analogues are:

A

5–fluorouracil, Capecitabine, Cytarabine, Gemcitabine, 5-Azacytidine

233
Q

Purine analogues are:

A

6-Mercaptopurine, Fludarabine, Cladribine, Pentostatin

234
Q

Cell Cycle Specific agents under G2-phase specific are:

A
  1. Bleomycine
  2. Epipodophyllotoxins
235
Q

Source of Bleomycin

A

S. Verticulus

236
Q

MOA of Bleomycin

A

MOA: binds to DNA, generates free radicals

237
Q

Bleomycin toxicity

A

pulmonary toxicity (pulmonary fibrosis)

238
Q

semisynthetic derivatives of podophyllotoxin, isolated from
mayapple root

A

Epipodophyllotoxins

239
Q

MOA of Epipodophyllotoxins

A

MOA: inhibits Topoisomerase II

240
Q

Epipodophyllotoxins Drugs are:

A

Etoposide, Teniposide

241
Q

Cell cycle specific agent class under M phase are:

A
  1. Taxanes
  2. Vinca alkaloids
242
Q

Isolated from the bark of pacific yew tree (Taxus brevifolia)

243
Q

MOA of Taxanes

A

MOA: stabilize microtubules, inhibit depolymerization

244
Q

Taxane drugs are:

Hint: ends with -taxel

A

Paclitaxel, Docetaxel

245
Q

Source of Vinca alkaloids

A

source: Catharanthus roseus leaves

246
Q

MOA of Vinca alkaloids

A

MOA: inhibit tubulin polymerization and microtubule
formation

247
Q

Drugs under Vinca alkaloids are:

A

Vincristine, Vinblastine, Vinorelbine

248
Q

MOAs of Antibacterial agents

A
  1. Inhibition of cell wall synthesis
  2. Inhibition of protein synthesis
  3. Inhibition of cell metabolism
  4. Inhibition of nucleic acid transcription and replication
  5. Interactions with plasma membrane
249
Q

Beta-Lactam Antibiotics are:

A

Penicillins, Cephalosporins, Monobactams, Carbapanems

250
Q

He discovered Penicillin

A

Alexander Fleming

251
Q

Old name of Penicillin

A

Penicillium notatum

252
Q

New name of Penicillin

A

Penicillium chrysogenum

253
Q

Process usued by Florey & Chain to isolate Penicillin

A

By freeze drying/ Lyophilization

254
Q

Properties of Penicillin

A

Betalactam & Thiazolidine ring
Nucleus: 6- Aminopenicillanic acid (6-APA)
Precursor: Cysteine & Valine
Shape: half- open book

255
Q

Penicillin Structure-activity relationship (SAR)

A
  1. Addition of electron withdrawing group – acid stability
  2. Addition of bulky groups – penicillin’s resistant
  3. Addition of amino group – increase spectrum activity
256
Q

MOA of Penicillin

A

Irreversibly inhibits transpeptidase by covalently binding to
the serine residue of the active site thus inhibiting cell wall synthesis

257
Q

Classification of Penicillin

A
  1. Narrow spectrum penicillins / Natural penicillins
  2. Penicillinase-resistant penicillins / Antistaphylococcal penicillins
  3. Broad spectrum penicillins / Aminopenicillins
  4. Extended spectrum penicillins / Antipseudomonal penicillins
258
Q

Narrow spectrum penicillins / Natural penicillins:

aka Benzyl penicillin
given IV
depot forms: Benzathine penicillin & Procaine penicillin
DOC: Syphilis

A

Penicillin G

*remember that PenG is only given IV.

259
Q

Narrow spectrum penicillins / Natural penicillins:

aka Phenoxymethyl penicillin
given PO

A

Penicillin V

260
Q

Penicillinase-resistant penicillins / Antistaphylococcal
penicillins drugs

Hint: MNOCD

A

Methicillin, Nafcilli, Oxacillin, Cloxacillin, Dicloxacillin

261
Q

Penicillinase-resistant penicillins / Antistaphylococcal
penicillins:

Prototype
s/e: Interstitial nephritis
emergence of MRSA

A

Methicillin

262
Q

Penicillinase-resistant penicillins / Antistaphylococcal
penicillins:

It can be given to px with renal problems

263
Q

Penicillinase-resistant penicillins / Antistaphylococcal
penicillins:

It contains 3-phenyl & 5-methyl

A

Oxacillin, Cloxacillin, Dicloxacillin

Dicloxacillin – best absorbed

264
Q

Broad spectrum penicillins / Aminopenicillins:

given IV
Prodrugs: Bacampicillin, Hetacillin, Ciclacillin + Sulbactam = Unasyn

DOC: Listeria monocytogenes

A

Ampicillin

265
Q

Broad spectrum penicillins / Aminopenicillins:

+ clavulanic acid = Co-Amoxiclav

commonly used in respiratory infections

A

Ampicillin

266
Q

Broad spectrum penicillins / Aminopenicillins drugs are:

A

Ampicillin, Amoxicillin

267
Q

Extended spectrum penicillins / Antipseudomonal
penicillins drugs are:

A

Carbenicillin, Ticarcillin, Piperacillin, Azlocillin, Mezlocillin

268
Q

Carboxypenicillins are?

  • Carboxyl at the α-position
A

Carbenicillin, Ticarcillin

269
Q

Ureidopenicillins are?

  • Urea at the α-position
A

Piperacillin, Azlocillin, Mezlocillin

Piperacillin – most potent

270
Q

The first cephalosporin

A

Cephalosporin C

271
Q

Old name for Cephalosporin

A

Cephalosporium acremonium

272
Q

New name for Cephalosporin

A

Acremonium chrysogenum

273
Q

Properties of Cephalosporins

A

Contains an unstable bicyclic system
Beta-lactam & Dihydrothiazine
Nucleus: 7-Aminocephalosporanic acid (7-ACA)
Precursors: Cysteine & Valein
Better acid stability & resistance to B-lactamase

274
Q

MOA of Cephalosporins

A

Irreversibly inhibits transpeptidase by covalently binding to
the serine residue of the active site thus inhibiting cell wall synthesis

275
Q

1st Gen Cephalosporins are:

A

Cefalexin
Cefadroxil
Cefazolin
Cephalotin
Cephradine

276
Q

2nd Gen Cephalosporins are:

A

Cefaclor
Cefoxitin
Cefuroxime
Cefonicid
Cefamandole
Cefpodoxime
Cefprozil
Cefotetan
Loracarbacef

277
Q

3rd Gen Cephalosporins are:

A

Cefoperazone
Ceftriaxone
Ceftibuten
Cefdinir
Cefixime
Cefotaxime
Moxalactam
Ceftidoxime
Cefditoren

278
Q

4th Gen Cephalosporins

A

Cefepime
Cefpirome

279
Q

Clinical use of Cefalexin

A

used for UTI in pregnant

280
Q

Clinical use of Cefazoline

A

pre-surgical prophylaxis

281
Q

Clinical use of Ceftriaxone

A

New DOC: Typhoid fever

282
Q

Cephalosporins used for antipseudomonal activity

A

Cefoperazone, Cefotaxime, Ceftazidime, Ceftriaxone, Moxalactam

283
Q

Side effects/ Adverse effects of Cephalosporins

A

Hypersensitivity
Disulfiram-like reaction & Hypoprothrombinemia

284
Q

N-Methyl-5-thiotetrazole (MTT) containing cephalosporins:

A

Cefamandole, Cefotetan, Moxalactam, Cefoperazone

285
Q

Properties of Carbapenems

A

Differ from penicillin in that the sulfur atom has been replaced by carbon atom

Broad spectrum of activity, including P. aeruginosa

286
Q

Carbapenem drugs are:

A

Thienamycin, Imipenem, Meropenem, Ertapenem

287
Q

Carbapenems:

It is isolated from Streptomyces cattleya and inactivated by Renal dehydropeptidase-I

A

Thienamycin

288
Q

Carbapenems:

N-formimidoylthienamycin

+ Cilastin (renal dehydropeptidase inhibitor) = Tienam

289
Q

Carbapenems:

2nd generation carbapenem
Resistant to dehydropeptidases & B-lactamases

290
Q

Carbapenems:

Benzoic acid contributes to high protein binding and prolongs the half-life of the drug

291
Q

Properties of Monobactam

A

Monocyclic B-lactams
Inactive against gram positive. Moderate activity against a narrow group of gram-negative bacteria, including P. aeruginosa.

292
Q

Only Monobactam drug:

It is isolated from Chromobacterium violaceum

293
Q

Antibacterial agent:

Sources: Streptomyces garyphalus, S. orchidaceus, S. lavendulus

A

Cycloserine

294
Q

MOA of Cycloserine

A

MOA: Prevent the formation of D-ala-D-ala (inhibits L-alanine racemase & D-ala, D-ala ligase)

295
Q

Use: Second-line drug for tuberculosis

A

Cycloserine

296
Q

Antibacterial agent:

It is a polypeptide from Bacillus subtilis, isolated from a fracture fragment from Margaret Tracy

A

Bacitracin

297
Q

MOA of Bacitracin

A

MOA: Binds to the lipid carrier

298
Q

Use: + Polymyxin B for the topical treatment of skin infections.

A

Bacitracin

299
Q

Side effects of Bacitracin

A

s/e: nephrotoxic & hematotoxic

300
Q

Caution for Bacitracin

A

Avoid Zinc.

Action is enhanced by zinc

301
Q

Antibacterial agent:

A glycopeptide from Streptomyces orientalis

A

Vancomycin

302
Q

MOA of Vancomycin

A

MOA: Inhibits transglycosidation, inhibits synthesis of mucopeptide polymer

303
Q

Drug of choice for MRSA (IV), C. difficile induced Pseudomembranous colitis (PO)

A

Vancomycin

304
Q

Side effect of Vancomycin

A

s/e: red-man syndrome (remedy: slow infusion)

305
Q

Antibacterial agent:

A glycopeptide from Actinoplanes teichomyceticus

A

Teicoplanin

306
Q

MOA of Teicoplanin

A

MOA: long alkyl chain anchors the antibiotic to the outer surface of the cell membrane

307
Q

Agent used for the treatment of gram-positive infections

A

Teicoplanin

308
Q

Antibacterial agent:
Synthetic derivative of Phosphoric acid

A

Fosfomycin

309
Q

MOA of Fosfomycin

A

MOA: inhibits UDP-N-acetyl glucosamine enolpyruvyl transferase

310
Q

Use of Fosfomycin

A

tx: UTI cause by E. coli

311
Q

Agents used for Inhibition of cell wall synthesis:

A

BETALACTAM
CYCLOSERINE
BACITRACIN
VANCOMYCIN
TEICOPLANIN
FOSFOMYCIN

312
Q

Agents used for Interactions with Plasma Membrane

A

POLYMYXINS
GRAMICIDIN A
DAPTOMYCIN

313
Q

Agents used for Inhibition of Protein Synthesis

A

AMINOGLYCOSIDES
TETRACYCLINES
MACROLIDES
LINCOSAMIDES
CHLORAMPHENICOL
STREPTOGRAMINS
LINEZOLID

314
Q

Agents used for Inhibition of DNA Replication

A

QUINOLONES
NITROFURANS

315
Q

Agents used for Inhibition of Cell Metabolism

A

SULFONAMIDES
SULFONES

316
Q

Interactions with Plasma Membrane:

Cation polypeptides that has the side effects of Nephrotoxic and neurotoxic

A

Polymyxins

317
Q

MOA of Polymyxins

A

MOA: bind to phospholipids on the cell membrane of gram-
negative bacteria

318
Q

Type of Polymyxins that is + Bacitracin for skin infections and + Dexamethasone & Neomycin for eye infections

A

Polymyxin B

319
Q

Also known as Polymyxin E

320
Q

Source of Colistin

A

Aerobacillus colistinus

321
Q

Use of Colistin

A

For refractory urinary tract infections & gram-negative
infections

322
Q

Source of Gramicidin A

A

Source: Bacillus brevis

323
Q

MOA of Gramicidin A

A

MOA: acts as ionophore allowing the loss of K+ ions

324
Q

A cyclic lipopeptide from Streptomyces roseosporus

A

Daptomycin

325
Q

Use of Daptomycin

A

Use: reserve agent for SSTIs

326
Q

It is an inhibition of Protein Synthesis Antimicrobial that has the properties of the following:

Properties

Amino sugars joined by a glycosidic linkage
derived from Streptomyces spp (mycin) or Micromonospora
spp. (micin)
given IV (except: neomycin)
+ penicillins = synergism
for the treatment of serious infections caused by gram-
negative bacilli

A

Aminoglycosides

327
Q

MOA of Aminoglycosides

A

Mechanism of action (MOA)

Bind to 30s ribosomal subunit to prevent the reading of the
mRNA

328
Q

Drugs under Aminoglycosides

A

Gentamicin
Tobramycin
Amikacin
Neomycin
Kanamycin
Streptomycin

329
Q

Aminoglycosides from Micromonospora purpurea

A

Gentamicin

330
Q

Aminoglycosides from Streptomyces tenebravius

A

Tobramycin

331
Q

Aminoglycosides that is semi synthetically derived from Kanamycin and first prepared in Japan

332
Q

Aminoglycosides from Streptomyces fradiae

333
Q

Aminoglycosides from Streptomyces kanamyceticus

334
Q

Aminoglycosides from Streptomyces griseus

A

Streptomycin

335
Q

1st aminoglycoside discovered and 1st effective agent used against tuberculosis

A

Streptomycin

336
Q

Side effects of Aminoglycosides

A

Allergic reactions
Ototoxicity
most ototoxic: KAN
most vestibulotoxic: SG
Nephrotoxicity
most nephrotoxic: NTG
Neuromuscular paralysis

337
Q

Drug choice for Lime Disease and Rickettsia

A

Tetracyclines

338
Q

Properties of Tetracyclines

A

Consists for 4 fused rings with a system of conjugated
double bonds.
Broadest spectrum of the antibiotics
Have activity against gram positive & negative, spirochetes &
atypical bacteria

339
Q

Chlortetracycline is from:

A

Streptomyces aureofaciens

340
Q

MOA of Tetracyclines

A

Mechanism of action (MOA)

Binds to the 30s subunit of ribosomes which prevents
aminoacyl-tRNA from binding to the mRNA ribosome complex

341
Q

Short Acting Class of Tetracyclines

A

Tetracycline, Oxytetracycline

342
Q

Intermediate Acting Class of Tetracycline

A

Metacycline , Demeclocycline

343
Q

Long Acting Class of Tetracycline

A

Doxycycline
Minocycline

344
Q

Very Long Acting Class of Tetracycline

A

Tigecycline

345
Q

Interactions of Tetracyclines

A

Products containing metals
Dairy products and drugs containing divalent and trivalent
metals
Decreased absorption of tetracycline due to chelation

346
Q

Antagonism reaction with Tetracycline

A

Penicillins

347
Q

Side effects / Adverse reaction of Tetracycline

A

Photosensitivity
Fanconi-like syndrome
taking expired tetracycline
Tooth discoloration & stunting of growth
Contraindicated to pregnant women & young children

348
Q

Properties of Macrolides

A

Properties
Common chemical characteristics:
14-membrane lactone ring
Ketone group
Glycosidically linked amino sugar

349
Q

MOA of Macrolides

A

Mechanism of action (MOA): Binds to the 50s ribosomal subunit, inhibiting translocation.

350
Q

Drugs under Macrolides

A

Erythromycin
Clarithromycin
Azithromycin
Roxithromycin

351
Q

Macrolides from Streptomyces erythraeus, from Iloilo

A

Erythromycin

352
Q

lipid soluble, acid stable prodrug with better
oral absorption; s/e: Cholestatic jaundice

A

Estolate (ester salt from Erythromycin)

353
Q

Macrolide that substitutes for penicillin in allergic patients and a motilin agonist

A

Erythromycin

354
Q

Drug choice for Legionnaire’s disease

A

Erythromycin

355
Q

Macrolide which is used for the treatment of ulcers causes by H. pylori

A

Clarithromycin

356
Q

Methylated erythromycin and more stable in gastric acid and has improved oral absorption

A

Clarithromycin

357
Q

Dehydrate Azithromycin is

358
Q

Monohydrate Azithromycin is

359
Q

This Macrolide contains a 15-membered macrocycle with N-methyl group, Extensive tissue distribution and food decreases absorption

A

Azithromycin

360
Q

Semisynthetic macrolide derived from erythromycin (+N- oxime side chain)

A

Roxithromycin

361
Q

Sulfur containing antibiotics

A

Lincosamides

362
Q

MOA of Lincosamides

A

Binds to 50s ribosomal subunit (same with macrolides)

363
Q

Drugs under Lincosamides

A

Lincomycin & Clindamycin

364
Q

Lincosamide that is from Streptomyces lincolnensis

A

Lincomycin

365
Q

Lincosamide that is also known as 7-chloro-7-deoxy derivative of lincomycin

A

Clindamycin

366
Q

Potent drug for anaerobic bacteria

A

Clindamycin

367
Q

Drug of choice for Clindamycin A/E: Clostridium difficile induced pseudomembranous colitis

A

Vancomycin, Metronidazole

368
Q

Source of Chloramphenicol

A

Streptomyces venezuelae

369
Q

Source of Chloramphenicol

A

Streptomyces venezuelae

370
Q

MOA of Chloramphenicol

A

MOA: Binds to 50s subunit, inhibiting peptidyl transferase

371
Q

Old drug choice for Typhoid Fever

A

Chloramphenicol

372
Q

New drug of choice for Typhoid fever

A

Ceftriaxone

373
Q

Chloramphenicol a/e

A

Aplastic anemia, Gray baby syndrome

374
Q

Chloramphenicol a/e

A

Aplastic anemia, Gray baby syndrome

375
Q

Chloramphenicol toxicophore

A

Nitro group

376
Q

MOA of Streptogramins

A

MOA: Binds to different regions of the 50s subunit and form a complex with it

377
Q

Drugs under Streptogramins

A

Pritinamycin
Quinupristin
Daflopristin

378
Q

Streptogramins from Streptomyces pristinaespiralis

A

Pritinamycin

379
Q

Streptogramins that inhibits peptide chain elongation

A

Quinupristin

380
Q

Streptogramins that interferes with the transfer of the peptide chain from one tRNA to the next

A

Daflopristin

381
Q

classified under oxazolidinones, synthetic antibiotics

382
Q

MOA of Linezolid

A

MOA: Binds to 50s preventing the formation of the 70s complex

383
Q

Drug of choice for Vancomycin-resistant Staphylococcus aureus (VRSA)

384
Q

patterned after Nalidixic acid (NegGram) o synthetic antibacterial agent

A

Quinolones

385
Q

MOA of Quinolones

A

inhibits DNA Gyrase Topoisomerase

386
Q

Drugs under 1st gen Quinolones
Activity: Moderate gram (-) act

A

Nalidixic acid, Cinoxacin

387
Q

Drugs under 2nd gen Quinolones
Activity: Improved act against gram (-), has act against G (+) & Atypical microorganism

A

Ciprofloxacin, Lomefloxacin, Ofloxacin, Norfloxacin, Enofloxacin

388
Q

Drugs under 3rd gen Quinolones
Activity: Retained gram (-) act, improved gram (+) & atypical act

A

Gatifloxacin, Gemifloxacin, Sparfloxacin, Moxifloxacin, Levofloxacin

389
Q

Drugs under 4th gen Quinolones
Activity:

A

Retained gram (-), gram (+), atypical microorganism, also for anaerobic microorganism

390
Q

Quinolones Structure Activity Relationship (SAR)

A

Nucleus: 1,4 dihydro-4-oxo-3 pyridine carboxylic acid
- At 2, addition of groups greatly reduces or abolishes activity
- At 5,6,7,8, may be substituted with good effects
- At 6, + F increases antibacterial activity
- Fluoroquinolones – broad spectrum (+, -)
- At 7, + Piperazine provides activity against Pseudomonas aeruginosa
- At 1, small alkyl substitution provides greater potency
- At 8, + Halogen, side effect is photosensitivity
- Highest – Lomefloxacin
- Lowest – Sparfloxacin

391
Q

Quinolone interactions are:

A

Enzyme inhibitor
Products containing divalent and trivalent metals

392
Q

Derivatives of 5-nitro-2-furaldehyde

A

Nitrofurans

Module 1 (4 decks)

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