Aniline Derivatives (Drugs)

PARACETAMOL
1. Brand name: BIOGESIC

- This combination product contains 2 medications, acetaminophen and an
antihistamine. Acetaminophen helps to reduce fever and/or mild to moderate pain (such as headache,
backache, aches/pains due to muscle strain, cold, or flu).
Derivative from aniline- acetanilide
 Aniline is found to possess a derivative which is the acetanilide that possess a analgesic and antipyretic
property. Acetanilide is formed by the addition of secondary amide group to aniline.
 Despite acetanilide being effective, a need for a less toxic aniline derivative started because of side
effects of acetnilide like cyanosis. It found out that Phenacietin or N-(4-Ethoxyphenyl)ethanamide has
fewer side effects and therefore Joseph von Mering improved on phenacetin producing paracetamol.
 Metabolism of Acetaminophen (Biogesic)
- it first undergoes sulphation (binding to a sulphate molecule) and glucuronidation (binding to a
glucuronide molecule) before being eliminated from the body by the liver
aniline acetanilide Phenacetin Acetaminophen
Benzocaine
1. Brand name: Orajel
- Orajel is the brand name of the topical numbing medicine benzocaine. It's used to reduce pain caused by
teething, cold sores, canker sores, and toothaches. The drug is in class of medicines known as local
anesthetics. It works by blocking nerve signals in the body
Derivative from aniline- Benzocaine
 Benzocaine- is an ester local anesthetic commonly used as a topical pain reliever or in cough drops. It is
the active ingredient in many over-the-counter anesthetic ointments.
 Benzocaine is a compound made from the organic acid PABA (para-aminobenzoic acid) and ethanol.
The process in which this ester is created is known as Fischer esterification.
Bacrim and
Septra
sulfamethoxazole trimethoprim
1. Brand name: Bactrim
- Bactrim (sulfamethoxazole and trimethoprim) DS is a combination of two antibiotics used to treat

urinary tract infections, acute otitis media, bronchitis, Shigellosis, Pneumocystis pneumonia, traveler's
diarrhea, methicillin-resistant Staphylococcus aureus (MRSA).
2. Brand anme: SEPTRA
- (trimethoprim and sulfamethoxazole) is a combination of two antibiotics used to treat ear infections,
urinary tract infections, bronchitis, traveler's diarrhea, methicillin-resistant Staphylococcus aureus (MRSA)
and Pneumocystis carinii pneumonia.
 Sulfa-containing drugs include: sulfonamide antibiotics, including sulfamethoxazole-trimethoprim

(Bactrim and Septra)
 Sulfa drugs were discovered in the early 1900’s and found to be active anti-bacterial agents.
Sulfanilamide inhibits the formation of folic acid in bacteria, thus preventing its further growth.
Sulfanilamide is easily synthesized from aniline in four steps.
Derivative from aniline- sulfanamide

Nomifensine (Nomifensine)
1. Brand name: Merital
- Merital Tablet works by inhibiting the uptake of norepinephrine and serotonin in adrenergic and serotonergic
neurons; calming the nerves in the brain .

- used for Depression, Anxiety, Insomnia, Alcohol withdrawal symptoms and other conditions.
Why Nomifensine causes haemolytic anemia? The importance of Drug metabolism.
 Nomifensine possess an aniline group, which is a substituent in drugs frequently associated with blood
and liver toxicities.
 In an examination of the metabolism of nomifensine in vivo, the observed metabolites included
alterations of the phenyl ring, including conjugates suggesting the existence of a catechol intermediate
metabolite.
 These represent two possibilities of structural elements in nomifensine that could underlie the toxicity
of the drug.
 We hypothesized that the tetrahydroisoquinoline structure of nomifensine could be the chemical group
responsible for toxicity, as metabolism to the dihydroisoquinolinium ion would represent a bioactivation
pathway analogous to the formation of other iminium ion metabolites.
PROCAINE
1. Brand name: Novocaine
- It is a local anesthetic medication that is used to numb a particular part of the body. It is most commonly used
in dental procedures to numb the area around a tooth.
 Procaine is a benzoate ester, formally the result of esterification of 4-aminobenzoic acid with 2-
diethylaminoethanol.
 Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase
through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the
urine.
Benzocaine and Glycerin Oral Spray
1. Brand name: Cepacol
- It is used to treat mouth sores, ease mouth and throat pain and treat canker sores.
- The action of benzocaine in Cepacol® Lozenges works on the nerve receptors in your throat so they are
temporarily unable to register sensations of pain, which is why your throat feels numb. Numbing action is a fast
and effective way to relieve sore throat pain.
 Benzocaine is the derivative of p-aminobenzoic acid and can be synthesized via the Fischer esterification
reaction.

Aniline Derivatives (Drugs)

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PARACETAMOL

1. Brand name: BIOGESIC

Derivative from aniline- acetanilide

aniline acetanilide Phenacetin Acetaminophen

1. Brand name: Orajel

Derivative from aniline- Benzocaine

1. Brand name: Bactrim

- Bactrim (sulfamethoxazole and trimethoprim) DS is a combination of two antibiotics used to treat

2. Brand anme: SEPTRA

 Sulfa-containing drugs include: sulfonamide antibiotics, including sulfamethoxazole-trimethoprim

Derivative from aniline- sulfanamide

1. Brand name: Merital

neurons; calming the nerves in the brain .

1. Brand name: Novocaine

1. Brand name: Cepacol

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