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Description of Individual Course UnitsCourse Unit Code | Course Unit Title | Type of Course Unit | Year of Study | Semester | Number of ECTS Credits | 300004582008 | PHARMACEUTICAL CHEMISTRY-IV | Compulsory | 4 | 8 | 6 |
| Level of Course Unit | First Cycle and Second Cycle | Objectives of the Course | The purpose of the course is to introduce the chemical structures, chemical and physicochemical properties of the drug groups in this course content; to interrelate this properties with pharmaceutic, pharmacokinetic and pharmacodynamic process and structure-activity relations; to teach the synthetic routes used in industry and approaches in synthetic methodology. The aim of the practical course is to introduce the identification of the drug active compounds by spectroscopic methods and to gain application skills. | Name of Lecturer(s) | Assist. Prof. Dr. Zeynep SOYER | Learning Outcomes | 1 | 1. Being able to understand and interpret the chemical properties causing the pharmaceutical actvity and their relations with biological process. | 2 | 2. Being able to understand the relations between the chemical structures of pharmaceutically active synthetic and semi-synthetic compounds with therapotic and adverse effects and to predict possible biological responses. | 3 | 3. Capable of giving examples about drug design methodology and approaches. | 4 | 4. Being able to understand the chemical structures, chemical and physicochemical properties of the synthetic and semi-synthetic (drug) active compounds. | 5 | 5. Being able to name the synthetic and semisynthetic molecules’ structure according to the nomenclature rules. | 6 | 6. Being able to understand the relations between pharmacokinetic properties with chemical structures of the synthetic and semisynthetic molecules used as drug active compound and use this knowledge during the treatment. | 7 | 7. Being able to understand the relations between pharmacodynamic properties with chemical structures of the synthetic and semisynthetic molecules used as drug active compound and use this knowledge during the treatment. | 8 | 8. Being able to evaluate the potentials of biological response of the molecules in terms of chemical structure and reactivity. | 9 | 9. To be able to understand the general chemical structure leading to a pharmacological response and predict the structure activity relationship. | 10 | 10. Being able to understand and predict the drug-drug interactions by interrelating pharmacodynamic and pharmakokinetic concept with drugs’ chemical and physicochemical properties in biological systems. | 11 | 11. Being able to predict the chemical structures and the possible incompatibilities of activemolecules and excipients and use this knowledge in formulatin and treatment process. | 12 | 12. Capable of understanding the basic approaches regarding to the methods of obtaining pharmaceutical active molecules and excipiants and solving possible problems suring synthesis. | 13 | 13. Being able to understand and interpret the principles of working with spectral analysis methods. | 14 | 14. Being able to recognize the pharmaceutical active compounds by spectroscopic analysis methods and to apply these methods |
| Mode of Delivery | Face to Face | Prerequisites and co-requisities | None | Recommended Optional Programme Components | Being successful in organic chemistry course is recommended. | Course Contents | Chemotherapotics (Anticeptic and disinfectants, Uriner Anticeptics, Tuberculostatics, Leprostatics, Antibacterial Sülfonamides), Antibiotics, Antifungal drugs, Antiviral drugs, Antiprotozoal drugs, Anthelmintics, Anticancer drugs (alkylating agent, antimetabolites, Anticancer hormones and antibiotics), Hormones (Steroidal and nonsteroidal sex hormones, Thyroid hormones), Vitamins. Demonstration courses in spectroscopic methods are given before practical studies. Then methods of spectroscopic analysis are practically applied on the given samples. | Weekly Detailed Course Contents | |
1 | Chemotherapotics 1. Introduction 2. Classification 2.I. Synthetic Antibacterials 2.1.1. Topically used Synthetic Antibacterials 2.1.1.1. Anticeptic and Disinfectants 2.1.1.1.1. Introduction 2.1.1.1.2. General concepts 2.1.1.1.3. Classification of Anticeptic and disinfectants 2.1.1.1.3.1. Halogens and Halophors 2.1.1.1.3.2. Alcohols 2.1.1.1.3.3. phenols 2.1.1.1.3.4.Epoxide and Aldehydes 2.1.1.1.3.5. Acids 2.1.1.1.3.6. Oxidant Agents 2.1.1.1.3.7 Heavy metals 2.1.1.1.3.8.Dye compounds 2.1.1.1.3.9.Diarylureas, Amidines and biguanides 2.1.1.1.3.10. Surface active compounds 2.1.1.1.3.11. Aminoacridines 2.1.1.1.3.12. Nitrofuran derivatives2.1.1.2. Conservatives 2.1.1.2.2.1.Parahydroxybenzoic Acid derivatives 2.1.1.2.2.2. Other compounds used as conservatives
Chemotherapotics 2.1.2. Systemic Synthetic antibacterials 2.1.2.1. Urinary Antiinfectives 2.1.2.1.1. Classification due to chemical structures 2.1.2.1.1.1. 4-Quinolons 2.1.2.1.1.2. Nitrofuran derivatives 2.1.2.1.1.3. Methenamine 2.1.2.1.1.4. Trimethoprim 2.1.2.2. Antimicobacterial drugs
| | Practical spectroscopic analysis | 2 | 2.1.2.2.1. Antituberculosis drugs 2.1.2.2.1.1. Primary drugs used for tuberculosis treatment 2.1.2.2.1.1.1. synthetic drugs 2.1.2.2.1.1.2. antibiotics 2.1.2.2.1.2. Secondary drugs used for tuberculosis treatment 2.1.2.2.1.3. Other drugs used for tuberculosis treatment 2.1.2.2. Antimicobacterial drugs
2.1.2.2.2.1. Drugs used for Lepra Treatment 2.1.2.2.2.2. Sulphones and structure-activity relationships 2.1.2.2.2.3. Clofazimine 2.1.2.2.2.4. thalidomide 2.1.2.3. Antibacterial sulfonamides 2.1.2.3.3.1. Current status of therapeutic effects of antibacterial sulfonamides 2.1.2.3.2. Contributions of Sulfa drugs to drug chemistry 2.1.2.3.3 Classification of Antibacterial sulfonamides 2.1.2.3.3.1. Systemic Antibacterial sulfonamides 2.1.2.3.3.4. Topically used Antibacterial sulfonamides 2.1.2.3.4. General synthesis method of Antibacterial sulfonamides 2.1.2.3.5. Structure activity relatonship of Antibacterial sulfonamides 2.1.2.3.6. Mechanism of action of Antibacterial sulfonamides 2.1.2.3.7. Metabolism of 2.1.2.3.8. Antibacterial sulfonamides Prodrugs facilitate drug intake
| | Practical spectroscopic analysis | 3 | Antibiotics
1. Introduction
2. Classification of antibiotics
I. β –Lactams
1. Penisillins
a) Structure oriented complications of penicillins
b) Brief history of penicillin
c) Transition to semi-synthetic penicillins
d) Methods of obtaining semi-synthetic penicillins
e) β-Lactamase Resistant Penicillins
f) Acid Resistant Penicillins
g) Antipseudomonal Penicillins
h) Geniş Spektrumlu Üreidopenisilinler
i) Penicillins’ mechanism of action
j) Structure-activity relationship of penicillins
k) Metabolism of penicillins
| | Ultraviolet(UV) demonstration | 4 | Antibiotics
1. Cephalosporins
a) Complications of cephalosporins due to structure
b) Classification of cephalosporins
First generation cephalosporins
Second generation cephalosporins
Third generation cephalosporins
Forth generation cephalosporins
c) Structure-activity relationship of cephalosporins
2. Monocyclic β-Lactams
Nocardicins
Monobactams
• Structure-activity relationship of Monobactams
3. Penems and Carbapenems
Penems
Carbapenemler
• Mechanism of action of Carbapenems
5. β-Lactamase Inhibitors
| | Infrared(IR) demonstration | 5 | Antibiotics
I. Tetracycline
1. Introduction
2. Chemical structure and nomenclature of Tetracyclines
3. Structure-activity relationship of Tetracyclines
4. Mechanism of action of Tetracyclines
II. Amphenicols
1. Chloramphenicol
a) Structure-activity relationships
b) Synthesis of Chloramphenicol
c) Prodrugs of Chloramphenicol
Antifungal Drugs
A. Introduction
B. Classification of Antifungal Drugs
I. Topically used drugs in dermatophytosis
1. Synthetic drugs
a) Structurally non-specific drugs (Undecylenic acid, tolnaftate, Ciclopirox)
b) Alylamines (naftifine, terbinafine)
c) Benzylamines (butenafine)
d) Azoles (clotrimazole, miconazole, econazole, izoconazole, sulconazole, thioconazole, oxyconazole, ketoconazole, terconazole)
2. Natural drugs (nistatine, pimaricine)
| | 1H NMR demonstration | 6 | Antifungal drugs
I. Systemic Drugs used for Micosis treatment
1. Synthetic drugs
a) Alylamines (terbinafine)
b) Azoles
İmidazoles (ketoconazole)
Triazoles(fluconazole,voriconazole,itraconazole)
Nukleoside analogs (flucitocine)
2. Natural drugs (griseofulvin, amphfotericin B, nistatin)
Antiviral Drugs
A. Introduction
B. Classification of Antiviral Drugs
I. Drugs used for prophylaxis
1. Drugs preventing viruses entering the host
2. İmmunostimulants and vaccines
| | 1H NMR demonstration | 7 | Antiviral Drugs
I. Antiviral drugs used fort he treatment
1. Antimetabolites
a) Derivatives obtained by preserving the sugar of natural purines and pirimidines while making some structural changes in basic part (idoxuridine, triflouridine)
b) Derivatives synthesized by attaching natural purine and pirimidine nukleosides to pentoses which are not found in natural nucleosides (vidarabin, cytarabine)
c) Compounds obtained by attaching non-sugar substituents which to natural nucleosides.
Purine nucleoside compounds and analogs (acyclovir, 6-deoxyacyclovir, valacyclovir, pencyclovir, famcyclovir)
Pirimidine nucleoside compounds and analogs (zidovudin, sidofovir)
Derivatives bearing heterocyclic rings other than purin and pirimidine (ribavirin)
| | 13C demonstration | 8 | Antiprotozoal Drugs
A. introduction
B. classification
I. Amebicides and tricomoniasis
1. Chemotherapeutics used for Amibiasis
a) Drugs used at Asymptomatic phase
5-Nitroimidazoller
8-Hydroxyquinolines
Haloacetamides
b) Drugs used at symptomatic phase
Drugs used for intestinal Amibiasis
• 5-Nitroimidazoles
• 8- Hydroxyquinolines
• Ipecac Alcoloids
Drugs used for Extraintestinal Amibiasis
• 5-Nitroimidazoles
• ipecac Alcoloids
• Some antibiotics(paromomicine)
• Some 4-aminoquinolines
| | Mass spectroscopy | 9 | Antiprotozoal Drugs
I. Leishmaniasis
1. Pentavalan Antimon compounds
2. Aromatic Amidines
3. natural antibiotics like Amphotericine B and Paromomicine
4. Promising new drugs
II. trypanosomiasis
1. Nifurtimox
2. Amidines: Pentamidine
3. Suramin
4. Organic arsenic drugs: Tryparsamide, Melarsoprol
5. 2-Nitroimidazoles: Benznidazole
6. some 5-Nitrofuran derivatives
7. someı 8-Aminoquinolines
8. Some antibiotics
| | Multicomponent demonstration | 10 | Midterm exam | | | 11 | Antiprotozoal Drugs
I. Drugs used for Toxoplasmosis
II. Antimalarial drugs
1. introduction
2. Antimalarial chemotherapeutics
4-Aminoquinolins: chloroquine, Hydroxy chloroquine
Quinolinomethanol derivatives: Mefloquine
1,4-Naftoquinon derivatives: Atovaquone
Biguanides: Proguanil
1,2-dihydrotriazines: cycloguanil
2,4-Diaminopirimidines: Primethamine
Sulphones: Dapson
Sulphonamides: Sulfadiazine, Sulfadoxin, Sulfisoxazole, Sulfametoxypiridazine
Antibiotics: Doxycyclin
8-aminoquinolines: Primaquine, Pamaquine
9-aminoacridines: quinacrine
phenantren derivatives: Halophantrin
3. developing Antimalarial drugs
4. mechanism of action of Antimalarial drugs
| | Quantitative analysis of multicomponent | 12 | Antihelmintic drugs
A. Introduction
B. Classification
1. Chematherapeutics used for helminthiasis caused by Nematodes
Benzimidazoles
İmidazothiaazoles
Vinylpirimidines
Piperazine and its analogs
Cyanide dyes
Other Antinematode Molecules
2. Chematherapeutics used for helminthiasis caused by Sestodes
Halogenated Bisphenol derivatives
Halogenated Salisilanilide derivatives
Other Antisestode compounds
3. Chematherapeutics used for helminthiasis caused by Trematodes
Antimon Compounds
Thioxsantenones
Nitro Compounds
Tetrahydroquinolines
Hexahydropirazinoquinolines
Pirazinoisoquinolines
| | Quantitative analysis of multicomponent | 13 | Drugs against Ectoparasites
A. Scabies and Pediculocides
I. Hydrocarbons with chlor atom
II. Pyrethroids
III. Comğpounds with sulfur atom
IV. Othet drugs
Anticancer Drugs
A. Introduction
B. Classification of Anticancer drugs
I. Alkylating agents (Radiomimetics)
Mustards with nitrogen atom
Etylenimines (aziridines)
Methansulphonic aside esthers
Nitrosoureas
Metylhidrazine and triazenoimidazole derivatives
Platinum coordination complexes
| | Practical spectroscopic analysis | 14 | Anticancer drugs
I. Antimetabolides
Folic acid antagonists
Purine Antagonists
Pirimidine Antagonists
II. Carcinolytic antibiotics
III. Mitosis inhibitors
IV. Hormones
V. Other derivatives
| | Practical spectroscopic analysis | 15 | Vitamins A. Introduction B. Classification I. Fat-soluable vitamins (Vitamin A, D, E, K)
Water-soluable vitamins (Vitamin B1 (Thiamine), Vitamin B2 (Riboflavin), Vitamin B3 (Niasin), Vitamin B5 (Pantothenic Acid), Vitamin B6 (Pyridoxal, Pyridoxine), Vitamin B9 (Folic Acid), Vitamin B12 (Cobalamin), Vitamin H (Biotin), Vitamin C (Askorbic Acid)
| | Compensation | 16 | Final | | |
| Recommended or Required Reading | 1.İlaçların Tanınması ve Kantitatif Tayini, Prof. Dr. Nedime Ergenç, Prof. Dr. Aysel Gürsoy, Prof. Dr. Öznur Ateş, İstanbul Üniversitesi Yayınları, İstanbul, 1966.
2.Türkiyede Üretilen İlaç Etken Maddeleri, Prof. Dr. Nedime Ergenç, Prof. Dr. Serpil Salman, Prof. Dr. Aydın Salman, İstanbul Üniversitesi Yayınları, İstanbul, 1992.
3.İlaçların Metabolizması (Biyotransformasyon), Prof. Dr. Sevim Rollas, Marmara Üniversitesi Yayınları, İstanbul, 1992.
4.Farmasötik Kimya Ders Kitabı Cilt I (Medisinal Kimya), Prof. Dr. Nedime Ergenç, Prof. Dr. Aysel Gürsoy, Prof. Dr. Öznur Ateş, İstanbul Üniversitesi Yayınları, İstanbul, 1997.
5.Farmasötik Kimya Cilt I, Prof.Dr.Hakkı Erdoğan ve arkadaşları, Irmak Matbaası, Ankara, 2000.
6.Farmasötik Kimya Cilt II, Prof.Dr.Hakkı Erdoğan ve arkadaşları,Irmak Matbaası, Ankara, 2000.
7.Farmasötik Kimya Prof.Dr.Hakkı Erdoğan ve arkadaşları, Hacettepe Üniversitesi Yayınları, Ankara, 2004.
| Planned Learning Activities and Teaching Methods | | Assessment Methods and Criteria | | Language of Instruction | Turkish | Work Placement(s) | None |
| Workload Calculation | |
Midterm Examination | 1 | 1 | 1 | Final Examination | 1 | 2 | 2 | Attending Lectures | 14 | 3 | 42 | Laboratory | 14 | 3 | 42 | Self Study | 14 | 2 | 28 | Individual Study for Mid term Examination | 1 | 25 | 25 | Individual Study for Final Examination | 1 | 30 | 30 | |
Contribution of Learning Outcomes to Programme Outcomes | LO1 | | | | | | | 5 | | | | | | | 4 | | | | | | | | LO2 | | 5 | | | | | | | | | | | 4 | 4 | | 3 | | 2 | | | | LO3 | | 3 | | | | | | 3 | 5 | | | | | | | | | | | 4 | 3 | LO4 | | 4 | | | | | 5 | | | | | | | 3 | | 2 | | | | | | LO5 | | 2 | | | | | 4 | | | | | | | | | | | | | | 4 | LO6 | | 3 | | | | | | | | | | | 5 | 5 | | | | | | | | LO7 | | 3 | | | | | | | | | | | 5 | 5 | | | | | | | | LO8 | | | | | | | 5 | 5 | | | | | | | | | | | | | | LO9 | | | | | | | 5 | 5 | 5 | | | | | | | | | | | | | LO10 | | | | | | | | | | | | | 5 | 5 | | 2 | | | | | | LO11 | | | | | | | | | | | | | 5 | 5 | | 2 | | 2 | | | | LO12 | | | | | | | | | 5 | | 4 | | | | | | | | 4 | | | LO13 | | | | | | | | | | | 5 | | | | | | | | 5 | | 4 | LO14 | | | | | | | | | | | 5 | | | | | | | | 5 | | 4 |
| * Contribution Level : 1 Very low 2 Low 3 Medium 4 High 5 Very High |
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Ege University, Bornova - İzmir / TURKEY • Phone: +90 232 311 10 10 • e-mail: intrec@mail.ege.edu.tr |
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