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195
Antibiotics
Carbenicillin
Pivampicillin
(iv) Carboxy penicillins
Carbenicillin
Ticarcillin
Penicillin-G (Benzyl Penicillin)
Structure:
N
S
H
O
H
N
O
O
OH
Chemical name: (2S, 5R, 6R)-3, 3-Dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-
azabicyclo-[3.2.0]-heptane-2-carboxylic acid
Uses: It is used in the treatment of infections caused by gram-positive bacteria.
Formulations: Tablet, dry powder and Injectable.
Brand name: Benzyl penicillin dry powder.
Cloxacillin
Structure:
N
S
H
O
H
N
O
O
OH
N
O
Cl
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Chemistry
Chemical name: (2S, 5R, 6R)-6-{[3-(2-chlorophenyl)-5-methyl-oxazole-4-
carbonyl]amino}-3, 3-dimethyl-7-oxo-4-thia-1-azabicyclo-[3.2.0]-heptane-2-carboxylic acid
Uses: As an antibiotic.
Formulations: Capsule and Injectable.
Brand names: Klox and Bioclox.
Ampicillin
Structure:
N
S
H
O
H
N
O
O
OH
H
2
N
H
Chemical name: (2S, 5R, 6R)-6-([2R)-2-amino-2-phenylacetyl]amino)-3, 3-dimethyl-7-
oxo-4-thia-1-azabicyclo-[3.2.0]-heptane-2-carboxylic acid
Uses: To prevent and treat several bacterial infections, such as respiratory tract infections,
urinary tract infections, meningitis, etc
Brand names: Ampilin and Roscillim.
Formulations: Capsule and Injectable.
Amoxicillin
Structure:
N
S
H
O
H
N
O
O
OH
NH
2
HO
197
Antibiotics
Chemical name: (2S, 5R, 6R)-6-([2R)-2-amino-2-(4-hydroxyphenyl)-acetyl]amino}-3, 3-
dimethyl-7-oxo-4-thia-1-azabicyclo-[3.2.0]-heptane-2-carboxylic acid
Uses: Used in the treatment of various infections including acute otitis media, streptococcal
pharyngitis, pneumonia, skin infections and urinary tract infections.
Formulations: Capsule, Injectable and Dry syrup.
Brand names: Amoxil, Synamox, Augmentin and Amonate (Amoxicillin + Clavulanic acid
combination).
14.4 CEPHALOSPORINS
Cephalosporins are a class of β-lactam antibiotics derived from the fungus Acremonium
(Cephalosporium). It is composed of the β-lactam ring and cephem ring structures.
N
S
R
1
O
O
H
H
N
O
O
R
2
H
(a) First-generation Cephalosporins
(i) Oral cephalosporins
Cephalexin
Cefadroxil
(ii) Parenteral cephalosporins
Cefazolin
(b) Second-generation Cephalosporins
(i) Oral cephalosporins
Cefaclor
Cefuroxime axetil
Cefprozil
(ii) Parenteral cephalosporins
Cefuroxime
Cefoxitin
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Chemistry
(c) Third-generation Cephalosporins
(i) Oral cephalosporins
Cefixime
Cefpodoxime Proxetil
Ceftibuten
(ii) Parenteral cephalosporins
Cefotaxime
Ceftriaxone
Ceftizoxime
(d) Fourth-generation Cephalosporins
(i) Parenteral cephalosporins
Cefepime
Cefpirome
14.5 AMINOGLYCOSIDES
Aminoglycosides inhibit the protein synthesis of bacteria and are mainly used to treat the
infections caused by gram-positive bacteria.
(a) Synthetic Agents
Streptomycin
Tobramycin
Gentamycin
Amikacin
Kanamycin
(b) Topical Agents
Neomycin
Framycetin
199
Antibiotics
Streptomycin Drug Profile
Uses: As an antibiotic use in the treatment of tuberculosis, endocarditis, and brucellosis.
Adverse effects: Ototoxicity and nephrotoxicity.
Formulation: Dry powder vial for injection.
Brand name: Ambistryn.
Neomycin Drug Profile
Uses: As a topical medication such as creams, ointments and eye drops to treat local
infections.
Formulations: Powder, Ointment, Cream and Eye drops.
Brand names: Nebasulf and Neosporin.
14.6 TETRACYCLINES
Tetracyclines are broad spectrum antibiotics produced by Streptomyces species. They are
used to treat a number of bacterial infections.
Note: It is contraindicated in pregnant women and children below age eight years because it
causes browning of teeth.
Tetracycline
OH O OH O O
NH
2
OH
CH
3
H H
N
OH
HO
H
3
C CH
3
Chemical name: (4S,6S,12aS)-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-
3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxonaphthacene-2-carboxamide
Uses: As a broad spectrum antibiotic in the treatment of bacterial infections like pneumonia,
cholera, acne, malaria, syphilis etc. It is a drug of choice for Rocky mountain spotted fever (blue
disease)
Formulations: Ointment and Capsule.
Brand names: Resteclin and Sumycin.
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Chemistry
Doxycycline
Structure:
OH
O
OH O
O
NH
2
OH
H H
N
OH
H
3
C CH
3
OH
Chemical name: (4S, 4aR, 5S, 5aR, 6R, 12aS)-4-(dimethylamino)-3, 5, 10, 12, 12a-
pentahydroxy-6-methyl-1, 11-dioxo-1, 4, 4a, 5, 5a, 6, 11, 12a-octahydrotetracene-2-carboxamide.
Uses: As a broad-spectrum antibiotic in the treatment of bacterial infections like pneumonia,
cholera, Lyme disease (an infectious disease caused by bacteria), syphilis, etc. It is used
in prophylaxis against malaria.
Formulation: Capsule.
Brand names: Tetradox and Doxt.
Minocycline
Structure:
OH O OH O O
NH
2
OH
H H
N
OH
H
3
C CH
3
HN
CH
3
H
3
C
Chemical name: (2E, 4S, 4aR, 5aS, 12aR)-2-(aminohydroxymethylidene)-4, 7-
bis(dimethylamino)-10, 11, 12a-trihydroxy-4a, 5, 5a, 6-tetrahydro-4H-tetracene-1, 3, 12-trione.
Uses: As a broad-spectrum antibiotic is mainly useful in the treatment of acne, anthrax
(infection caused by the bacterium Bacillus anthracis).
Formulation: Capsule.
Brand names: CNN-50 and Cyanomycin.
201
Antibiotics
14.7 CHLORAMPHENICOL
Chloramphenicol is a non-classified antibiotic produced by the bacterium Streptomyces
venezuelae and is now produced synthetically. Mainly used in meningitis, cholera, and typhoid
fever as a drug of choice.
OH
NH
C
l
C
l
O
N
+
O
-
O
OH
Chemical name: 2,2-Dichloro-N-[(1R,2R)-1,3-dihydroxy-1-(4-nitrophenyl)-propan-2-yl]-
acetamide.
Adverse effect: Gray baby syndrome in newborns.
Formulations: Capsule and Eye drops.
Brand names: Ocuchlor, Paraxin palmitate and succinate, Pentamycetin and Chloromycetin.
14.8 MACROLIDE ANTIBIOTICS
Macrolide antibiotics contain a large macrocyclic lactone rings to which one or more deoxy
sugars are attached.
Erythromycin Drug Profile
Uses: As a broad-spectrum antibiotic. In the treatment of bacterial infections like chlamydia
infection and syphilis.
Formulations: Tablet, Lotion, Capsule, Suspension, Eye drops and Ointment.
Brand names: Erysafe, Eromed and Robimycin.
Azithromycin Drug Profile
Uses: As a broad-spectrum antibiotic in the treatment of middle ear infections, sore throat,
pneumonia, traveler's diarrhea.
Formulations: Tablet, Capsule and Injectable.
Brand names: Aziwin, Aziwok, and Zithromax.
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14.9 LINCOSAMIDE ANTIBIOTICS
Lincosamide class of antibacterials originates from a natural product, lincomycin which
includes lincomycin, clindamycin and pirlimycin.
Clindamycin Drug Profile
Uses: As a broad-spectrum antibiotic in the treatment of strep throat, middle ear infection,
pneumonia, acne vulgaris (pimples).
Formulations: Capsule, Gel and Creams.
Brand names: Dalcap, Clicin, Clindac-A and Clinacin.
General Information
203
Chapter
Anti-neoplastic Agents
Neoplasm is an abnormal growth of tissue caused by the rapid division of cells that have
undergone some form of mutation. It may be non-cancerous (benign), precancerous
(premalignant), or cancerous (malignant).
There are more than 100 types of cancer including breast cancer, skin cancer, lung cancer,
colon cancer, prostate cancer and lymphoma. Symptoms vary depending on the type. Cancer
treatment may include chemotherapy, radiation, or surgery.
Classification of Neoplasm
(a) Carcinoma: Cancers are derived from epithelial cells.
(b) Lymphoma and leukemia: These two classes of cancer arise from hematopoietic
(blood-forming) cells.
(c) Sarcoma: Cancers arise from connective tissue (i.e., bone, cartilage, nerve).
(d) Germ cell tumor: Cancers are derived from pluripotent cells are most often present in
the testicle or the ovary.
(e) Blastoma: Cancers derived from immature “precursor” cells or embryonic tissue.
Antineoplastic or anticancer drugs are the drugs that prevent or inhibit the maturation and
proliferation of neoplasms. Antineoplastic agents travel the body, reach the site and destroy the
cancer cells.
Anticancer agents are classified as follows:
(a) Alkylating Agents
(i) Nitrogen mustards
Ifosphamide
Chlorambucil
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Chemistry
Melphalan
Meclorethamine
(ii) Ethylenimine
Thiotepa
(iii) Nitrosoureas
Carmustine
Lomustine
(iv) Triazine
Dacarbazine
(v) Alkylsulfonate
Busulfan
(b) Platinum Compounds
Cisplatin
Carboplatin
Oxaliplatin
(c) Antimetabolites
(i) Folate antagonist
Methotrexate
(ii) Purine antagonist
6-Mercaptopurine
6-Thioguanin
(d) Pyrimidine Antagonists
5-Fluorouracil
Cytarabine
(e) Plant Alkaloids
(i) Vinca alkaloids
Vincristine
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