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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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215
Anti-neoplastic
Agents
death. It is useful in the treatment of advanced ovarian cancer in women with deleterious germline
or somatic BRCA mutation.
Imfinzi (Durvalumab)
Mechanism of action: It is an immune checkpoint inhibitor that blocks the interaction of
PD-L1 with PD-1. It is useful in the treatment of advanced or metastatic urothelial carcinoma and
Stage III non-small cell lung cancer.
Ocrevus (Ocrelizumab)
Mechanism of action: It selectively targets the CD20 positive B-cells by binding to the
surface proteins of the cells. It is useful for the treatment of multiple sclerosis.
Xpovio (Selinexor)
Mechanism of action: It has a unique mechanism of action that offers a new pathway for
treating RRMM by selectively inhibiting XPO1, reactivating tumor-suppressing proteins, and
inducing tumor cell apoptosis. It is useful in the treatment of multiple myeloma.
Zirabev (Bevacizumab-bvzr)
Mechanism of action: It inhibits the formation of new blood cells (angiogenesis) by
specifically recognizing and binding to vascular endothelial growth factor (VEGF) protein.
It is used in the treatment of colorectal cancer, non-small cell lung cancer.
Kanjinti (Trastuzumab-anns)
Mechanism of action: It binds to the extracellular ligand-binding domain and blocks the
cleavage of the extracellular domain of HER-2 to induce its antibody-induced receptor
downmodulation.
It is used in the treatment of breast cancer and gastric cancer.
Polivy (Polatuzumab vedotin-piiq)
Mechanism of action: It target B-cell antigen receptor complex-associated protein beta
chain (CD79b). It is useful in the treatment of diffuse large B-cell lymphoma.
Piqray (Alpelisib)
Mechanism of action: It selectively inhibits PIK3 in the PI3K/AKT kinase (or protein
kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. It is
mainly useful in the treatment of breast cancer.
Balversa (Erdafitinib)
Mechanism of action: It inhibits fibroblast growth factor receptor (FGFR) kinase inhibitor
that binds to and inhibits the enzymatic activity of FGFR1, FGFR2, FGFR3, and FGFR4. It is
useful in the treatment of urothelial carcinoma.
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A Textbook of Pharmaceutical
Chemistry
Gemcitabine-cisplatin
Mechanism of action: It exhibits its cytotoxic action by binding to DNA and producing
DNA-DNA crosslinks. It provides a synergism effect. It is used in the treatment of biliary tract
cancer, bladder cancer, cervical cancer, etc.
Immunosuppressant Agents
Imbruvica (Ibrutinib)
Mechanism of action: It is a small molecule that acts as an irreversible potent inhibitor of
Burton's tyrosine kinase (BTK). It is used in the treatment of chronic graft-versus-host disease.
General Information
217
Bibliography
(1) Swallow, S. Fluorine in Medicinal Chemistry. Progress in Medicinal Chemistry 2015, 54, 65-133.
(2) Patrick, G.L. An Introduction to Medicinal Chemistry. UCL lecture notes 2009, 40, 752.
(3) Alessio, E. Bioinorganic Medicinal Chemistry 2011.
(4) Hagmann, W.K., The Many Roles for Fluorine in Medicinal Chemistry. Journal of Medicinal
Chemistry 2008, 4359-4369.
(5) Böhm, H.J.; Banner, D.; Bendels, S.; Kansy, M.; Kuhn, B.; Müller, K.; Obst-Sander, U.; Stahl, M.
Fluorine in Medicinal Chemistry. Chembiochem : a European Journal of Chemical Biology
2004, 5 (5), 637-643.
(6) Wermuth, C.G. The Practice of Medicinal Chemistry 2008.
(7) Lowe, D.B. Nowhere to Go But Up: The Return of Medicinal Chemistry. ACS Medicinal
Chemistry Letters 2012, 3-4.
(8) Stahl, M.; Bajorath, J. Computational Medicinal Chemistry. Journal of Medicinal Chemistry 2011,
1–2.
(9) Gooch, E. Medicinal Chemistry – An Introduction; Fundamentals of Medicinal Chemistry (Gareth
Thomas) 2004; Vol. 81.
(10) Maggiora, G.M.; Vogt, M.; Stumpfe, D.; Bajorath, J.J. Molecular Similarity in Medicinal
Chemistry. Journal of Medicinal Chemistry 2013, 57 (8), 3186-3204.
(11) Thomas, G. Fundamentals of Medicinal Chemistry 2004.
(12) Nicola, G.; Liu, T.; Gilson, M.K. Public Domain Databases for Medicinal Chemistry. Journal of
Medicinal Chemistry 2012, 6987-7002.
(13) Boström, J.; Hogner, A.; Llinàs, A.; Wellner, E.; Plowright, A.T. Oxadiazoles in Medicinal
Chemistry. Journal of Medicinal Chemistry 2012, 55 (5), 1817-1830.
(14) Carloni, P.; Alber, F. Quantum Medicinal Chemistry; 2003; Vol. 1.
(15) Burn, J.H. Medicinal Chemistry. British Medical Journal 1961, 2, 689-690.
(16) Valliant, J.F.; Guenther, K.J.; King, A.S.; Morel, P.; Schaffer, P.; Sogbein, O.O.; Stephenson, K. A.
The Medicinal Chemistry of Carboranes. Coordination Chemistry Reviews 2002, 232 (1-2), 173-
230.
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Chemistry
(17) Bryan, M.C.; Dillon, B.; Hamann, L.G.; Hughes, G.J.; Kopach, M.E.; Peterson, E.A.; Pourashraf,
M.; Raheem, I.; Richardson, P.; Richter, D.; Sustainable Practices in Medicinal Chemistry:
Current State and Future Directions. Journal of Medicinal Chemistry 2013, 6007-6021.
(18) Kappe, C.O.; Stadler, A.; Dallinger, D. Microwaves in Organic and Medicinal Chemistry 2012.
(19) Satyanarayanajois, S.D.; Hill, R. A. Medicinal Chemistry for 2020. Future Medicinal Chemistry
2011, 3 (14), 1765-1786.
(20) Copeland, R.A. Epigenetic Medicinal Chemistry. ACS Medicinal Chemistry Letters 2016, 124-127.
(21) Moorhouse, A.D.; Moses, J.E. Click Chemistry and Medicinal Chemistry: A Case of “Cyclo-
Addiction.” ChemMedChem 2008, 715-723.
(22) Koppitz, M.; Eis, K. Automated Medicinal Chemistry. Drug Discovery Today 2006, 561-568.
(23) Kuhn, B.; Mohr, P.; Stahl, M. Intramolecular Hydrogen Bonding in Medicinal Chemistry. Journal
of Medicinal Chemistry 2010, 53 (6), 2601-2611.
(24) Vogel, A.I. Vogel’s Textbook of Practical Organic Chemistry. 5th Edn 1990, Vol. 14.
(25) Harvey, D. Modern Analytical Chemistry 2000.
(26) Cheng, L.; Stopkowicz, S.; Gauss, J. Analytic Energy Derivatives in Relativistic Quantum
Chemistry. International Journal of Quantum Chemistry 2014, 1108-1127.
(27) Skoog, D. a; West, D.M.; Holler, F.J.; Crouch, S.R. Fundamentals of Analytical Chemistry. Anal.
Chem 2004, 398, 27-28.
(28) Burns, M. A. Analytic Chemistry. Everyone’s a (Future) Chemist. Science (New York, N.Y.) 2002,
296 (5574), 1818–1819.
(29) Etchegoin, P.G.; Le Ru, E.C.; Meyer, M. An Analytic Model for the Optical Properties of Gold.
The Journal of Chemical Physics 2006, 125 (16), 164705.
(30) Haynes, W.M. CRC Handbook of Chemistry and Physics, 95th Edition, 2014-2015, 2014; Vol. 54.
(31) Slater, J.C. Analytic Atomic Wave Functions. Physical Review 1932, 42 (1), 33-43.
General Information
219
Question Bank
A.1 QUESTION BANK
02 Mark Questions
Define limit test as per I.P. and give its importance.
Enlist heavy metals and their permitted limit.
What is ppm?
Define titre and titrant.
Define indicator with examples.
Define end point.
Define equivalence point.
How will you prepare 0.1M NaOH solution?
Enlist the role of sodium thioglycollate in iron limit test.
How will you prepare 1M HCl solution?
Draw neat and well labeled diagram for Gutzeit’s apparatus.
What is qualitative and quantitative analysis? Explain with examples.
Give the principle behind chloride limit test.
Define equivalent weight and calculate equivalent weight of:
Sulfuric acid
Sodium hydroxide
Define normality and molarity.
Enlist acid-base indicators.
Enlist adsorption indicators.
What is stoichiometry?
Give the preparation of crystal violet indicator.
Define primary standard with examples.
Write ideal properties of primary standard.
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A Textbook of Pharmaceutical
Chemistry
‘NaOH is secondary standard’- Justify.
Define buffer capacity.
‘Precipitation titration is also called as argentometric titration’- Justify.
What is silver mirror?
What is solubility product?
Give the chemical composition of Dettol.
Give the significance of non-aqueous titration.
What is leveling effect?
Acetic anhydride is banned, why?
What is oxidation number?
Define and give the examples of:
Oxidation
Reduction
Redox
Give the difference between Iodimetry and Iodometry.
Why potassium iodide is added in iodine solution?
Give the preparation of starch indicator as per IP.
‘KMnO
4
act as a self indicator’- Justify.
Define sequestering agent with examples.
Describe the role of Osmium tetraoxide.
Define ligand and classify it with examples.
Define masking and demasking agents with examples.
Write note on back titration with examples.
Give account on Metallochrome indicators with examples.
Define digestion in gravimetry.
Write note on co-precipitation.
Enlist factors affecting on precipitation.
Define hematinics with examples and give its any two marketed preparations.
Define antacids and give its role with examples.
Write note on bleaching powder.
Give the account on anticaries agents.
What is pyorrhea?
Write IUPAC names and structures for:
Halothane
Thiopental sodium
Define sedatives and hypnotics with examples.
Write note on calcium channel blockers.
221
Question Bank
Give the structure, brand name and uses for sodium nitropruside.
What are loop diuretics? Give its structure and uses.
Give the structure for EDTA.
Give the uses and brand names of ferrous gluconate.
What is milk of magnesia?
Give the uses and formulations of hydrogen peroxide.
Give the uses and formulations of sodium fluoride.
Define analgesic and antipyretic agents with examples.
What is tooth decay?
Give the color code for oxygen and carbon dioxide gas cylinders.
Define antimicrobial agents with examples.
Give the IUPAC name for:
Aziridine
Acetaldehyde
Write a note on insulin and give its two brand names.
Define hematinics and give its any two examples.
Define antibiotics with examples.
Write note on stereochemistry of penicillin.
INH is always given with pyridoxine? Justify.
Enlist the uses for morphine.
Enlist with structure morphine selective antagonist.
Write note on epimers in tetracycline.
What is Grey baby syndrome?
What is Steven Johnson Syndrome?
Give the brand names and uses for Co-trimoxazole.
Give the chemical name and uses for:
Chloroquine
Quinine
Halofantrine
What is HAART therapy?
What is first line therapy in Tuberculosis?
Draw the structure and IUPAC name for INH.
Enlist the brand names and uses for PAS.
Give chemical name and structure for dapsone.
What is rescue agent? Give its example.
Give the structure and class for Spironolactone.
Give the uses and brand names for boric acid.
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A Textbook of Pharmaceutical
Chemistry
Write uses for:
Norephinephrine
Ephedrine
Salbutamol
What are ergot alkaloids?
Give the structures and uses for:
Malathion
Parathion
Write note on myasthenia gravis and give its treatment.
What is chemotherapy?
Give the drug of choice for swine flu.
Give the drug of choice for prevention of malaria.
Write note on alopecia.
Give the chemical name, structure and uses of Chloramphenicol.
Sulfonamides are contraindicated childrens below age 12 years? Justify.
Tetracyclines are contraindicated in pregnant women? Justify.
Give IUPAC nomenclature for alcohols.
DOTS?
MDT?
What is AZT?
04 Mark Questions
Write short note on sources of impurities in pharmaceuticals.
Write short note on limit test of arsenic.
Give account on principle, reaction and theory behind sulfate limit test.
Write short note on strong acid vs weak base titration.
Explain in detail Fajan’s method.
Write short note on solvents used in non-aqueous titration.
Give the preparation, reaction, principle and procedure for 0.1M HClO
4
.
Write note on Cerimetry.
Write note on Permanganometry.
Give the merits of Cerimetry over the Permanganometry.
Write note on IUPAC nomenclature.
Explain in short gravimetry.
Write note on medicated nitrous oxide.
Draw the structure and IUPAC name for followings:
Imidazole
Indole
223
Question Bank
Furan
Quinoxaline
Anthracene
Give the IUPAC names for
N
N
N
N
Write note on ultra short acting anesthetics with examples.
Give the IUPAC names, structures and uses for:
Diazepam
Phenobarbitone
Chlorpromazine
Haloperidol
Clozapine
Phenytoin
Ethosuximide
Valproic acid
Give the structure, IUPAC name, Brand name and uses of followings:
Piroxicam
Diclofenac
Paracetamol
Naloxane
Aspirin
Give the structure and chemical names for:
Mafenide
Sulfacetamide
Pyrazinamide
Sulfamethoxazole
Verapamil
Explain in detail Diazepam drug profile.
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A Textbook of Pharmaceutical
Chemistry
Give the numbering system to given structures:
N
N
N
Write note on third generation cephalosporins.
Classify general anesthetic agents.
Write note on solubility profile of sulfonamides.
Add short note on nitrates with examples.
Write short note on UTI agents.
Define diuretics and add note on osmotic diuretic with examples.
Explain Volhard’s method.
Define and classify antineoplastic agents.
Give the brand names and uses for followings:
Methotrexate
Thiotepa
Cisplatin
5-Flurouracil
Carmustine
Write the brand names and uses for followings:
Metformin
Tolbutamide
Co-trimoxazole
Furosemide
Ethacrynic acid
Explain drug profile for ciprofloxacin.
Classify Sympathomimetic drugs with examples.
Explain the drug profile for:
Epinephrine
Dopamine
Give the structure, chemical name, uses and brand names for:
Propranolol
Atenolol
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