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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5282_Библиотеки_им_академика_М_И_Перельмана
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145
Non-steroidal Anti-inflammatory Agents
Paracetamol
Structure:
O
N
H
OH
H
3
C
Chemical name: N-(4-Hydroxyphenyl)-ethanamide.
Uses: In the treatment of fever, headache and lower back pain.
Contraindication: Contraindicated in a patient with liver impairment.
Formulations: Tablet, Suspension and Suppository.
Brand names: Crocin, Metacin and Febrinil.
12.1 MORPHINE ANALOGUES (OPIOID/NARCOTIC
ANALGESICS)
Morphine analogs are prepared from morphine by several chemical processes. All these
drugs are habit-forming.
They are classified as follows:
(a) Opioid µ Receptor Agonist
(i) Natural opium alkaloids
Morphine
Codeine
(ii) Semi-synthetic agonist
Pholcodine
Diacetylmorphine (Heroin)
(iii) Synthetic agonist
Pethidine
Methadone
Fentanyl
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A Textbook of Pharmaceutical
Chemistry
(b) K-agonist Agents
Nalorphine
Pentazocine
Butorphanol
(c) Morphine Antagonist
Naloxone
Naltrexone
Morphine
Structure:
Chemical name: (4R, 4aR, 7S, 7Ar, 12Bs)-3-methyl-2, 3, 4, 4a, 7, 7a-hexhydro-1H-4, 12-
methanobenzofuro [3, 2-e] isoquinoline-7, 9-diol.
Uses: To treat severe and acute pain in operative and postoperative patient.
It is also used to treat pain due to myocardial infarction, labor and in cancer patient.
Adverse effect: Constipation.
Formulations: Tablet and Injectable.
Brand names: Morcontin, Rilimore and Oramorph.
147
Non-steroidal Anti-inflammatory Agents
Codeine
Structure:
Chemical name: 3-Methylmorphine.
Uses: To treat severe pain, as a cough reliever and for diarrheal treatment.
Formulations: Syrup and Injectable.
Brand names: Codeine and Korex.
Fentanyl
Structure:
N N
O
Chemical name: N-[1-(2-Phenylethyl)-4-piperidinyl)-N-phenylpropanamide.
Uses: Intravenous fentanyl is useful for anesthesia and analgesia.
Formulations: Injectable, Transdermal patch and Lozenge.
Brand names: Fent and Durogesic.
148
A Textbook of Pharmaceutical
Chemistry
Pentazocine
Structure:
OH
N
Chemical name: 2-Dimethylallyl-5,9-dimethyl-2’-hydroxybenzomorphan.
Uses: To treat severe pain.
Formulations: Tablet and Injectable.
Brand names: Fortwin and Fortstar.
Naloxone
Structure:
OH
N
O
HO
O
Chemical name: 17-allyl-4, 5α-epoxy-3, 14-dihydroxymorphinan-6-one.
Uses: As an antidote in opioid poisoning. It is used to prevent abuse.
Formulation: Injectable.
Brand names: Nalox, NEX and Narcan.
General Information
149
Chapter
Anti-infective Agents
Anti-infective is a broad term and these agents are used in the treatment of infections caused
by different types of organisms such as fungi, bacteria, viruses etc.
13.1 ANTIFUNGAL AGENTS
Fungus is a parasite. Fungus is a different kingdom of living things, different from plants and
animals. The yeast moulds and mushrooms are types of fungi. The fungus infection results in
mycotic illnesses, the majority of which involve superficial invasion of skin of the mucous
membranes of body orifices.
Fungal diseases are generally called as mycoses. These mycotic infections are classified as:
1. Dermatophytoses (Skin Infections)
It is caused by various trichophyton, microsporum and epidermophyton species. These
include superficial infections of keratinized tissues like stratum corneum, hair, nail etc. Topical
antifungal agents are effective in such cases. Systemic antifungal agents may also be given with
one of the topical antifungal agents to treat deeper infections.
2. Candidiasis
Candidiasis affects mainly the skin and mucous membrane. It is caused by Candida albicans.
These infections mainly develop in the mouth, vagina etc.
3. Systemic Fungal Infection
It involves fungal infections of bones, viscera, lungs and meninges.
Many fungal infections occur either on skin or on nails, hair. At such places, the drug cannot
build up its therapeutic concentration required to exhibit antifungal activity. To cover such a
broad range of systemic fungal infections, very few antifungal agents are available. These include
polyene class of antibiotics like amphotericin B, imidazoles like ketoconazole, Miconazole and
clotrimazole etc.
13
150
A Textbook of Pharmaceutical
Chemistry
Antifungal agents are used to treat the fungal infections. An antifungalmedication is a
pharmaceutical fungicide or fungistatic used to treat and prevent mycoses such as athlete’s foot,
ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and
others.
Classification
(a) Azoles
(i) Imidazole
Topical
Clotriamazole
Econazole
Miconazole
Systemic
Ketoconazole
(ii) Triazoles
Fluconazole
Itraconazole
(b) Antibiotics
(i) Polyene antibiotics
Amphotericin-B
Nystatin
(ii) Benzofuran
Griseofulvin
(c) Allylamine
Terbinafine
(d) Topical agents
Tolnaftate
Benzoic acid
151
Anti-infective
Agents
Undecylenic acid
Sodium thiosulfate
Amphotericin-B
Uses: It is used in the treatment of fungal infection and in Leishmaniasis.
Formulations: Dry powder and Ear drops.
Brand names: Mycol, Fungizone, Otic, and Mysteclin-F.
Griseofulvin
Structure:
O
O
C
l
O
O
O
O
Chemical name: (2S,6’R)-7-Chloro-2’,4,6-trimethoxy-6’-methyl-33H,4’H-spiro-[1-
benzofuran-2,1’-cyclohex[2]ene]-3,4’-dione.
Uses: It is used orally for dermatophytosis. It is ineffective topically.
Formulations: Ointment and Tablet.
Brand names: Grisoral, Grisovin-FP, Crivicin, and Grison-250.
Econazolenitrate
Structure:
Cl
Cl
N
N
O
Cl
N
OHO
O
152
A Textbook of Pharmaceutical
Chemistry
Chemical name: (RS)-1-{2-[4-Chlorophenyl)-methoxy]-2-(2,4-dichlorophenyl)ethyl}-1H-
imidazole.
Uses: It is used as an antifungal agent.
Formulations: Ointment and Cream.
Brand names: Ecoderm, Econazole, and Ecostatin.
Miconazole
Structure:
Cl
Cl
O
N
N
ClCl
Chemical name: (RS)-1-(2-(2,4-Dichlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl)-1H-
imidazole.
Uses: It is used externally for the treatment of athlete’s foot (fungal infection that affects the
skin on the feet), ringworm and jock itch. Internal application is used for oral or vaginal thrush.
Formulations: Ointment, Cream, Gel, Lotion, and Solution.
Brand names: Zole and Daktarin.
Fluconazole
Structure:
F
F
N
HO
N
N
N
N
N
153
Anti-infective
Agents
Chemical name: 2-(2,4-Difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)propan-2-ol.
Uses: It is used as an antifungal agent.
Formulations: Ointment, Cream, Eyedrop, and Capsule.
Brand names: Zocon, Fluzon, and Syscan.
Ketoconazole
Structure:
Chemical name: 1-[4-(4-{[(2R,4S)-rel-2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-
1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1yl]-ethan-1-one.
Uses: It is used as an antifungal agent.
Topical Antifungal
Topical preparation of ketoconazole is usually prescribed for fungal infections of the skin
and mucous membranes such as athlete's foot, ringworm and candidiasis.
Systemic Antifungal
Ketoconazole has activity against many kinds of fungi that may cause systemic infection in
human e.g., Candida, Histoplasma.
Brand names: Ketovae and Danruf.
Formulations: Ointment, Cream, Shampoo, Tablet and Lotion.
Itraconazole
Uses: It is used as an antifungal agent.Itraconazole has a broader spectrum of activity than
fluconazole. In particular it is active against aspergillus, which fluconazole is not. It is also used
in blastomycosis.
Formulations: Ointment and Capsule.
Brand names: Itaspor and Flucover.
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A Textbook of Pharmaceutical
Chemistry
Tolnaftate
Structure:
N
O
S
Chemical name: O-2-Naphthyl methyl-3(-methylphenyl)-thiocarbamate.
Uses: It is used as an antifungal agent.Tolnaftate has been found to be slightly less effective
than azoles when used to treat Tinea pedis (athlete’s foot). It is however, useful when dealing
with ringworm infections.
Formulations: Ointment, Cream, and Lotion.
Brand names: Tolnaderm and Tinaderm.
Naftifine
Structure:
N
Chemical name: (2E)-N-methyl-N-(1-naphthylmethyl)-3-phenylprop-2-en-1-amine.
Uses: It is used as an antifungal agent. In the topical treatment of Tinea pedis, Tinea cruris
and Tinea corporis.
Naftifine has triple action: antifungal, antibacterial and anti-inflammatory.
Formulations: Ointment, Cream, and Lotion.
Brand name: Exoderil.
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