Description of Individual Course Units
Course Unit CodeCourse Unit TitleType of Course UnitYear of StudySemesterNumber of ECTS Credits
300004532008PHARMACEUTICAL CHEMISTRY-IIICompulsory476
Level of Course Unit
First Cycle and Second Cycle
Objectives of the Course
The purpose of the course is being able 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. Also, the aim of the practical course is to be able to introduce the spectrophotometric and volumetric methods used in quantitative analysis and to gain application skills.
Name of Lecturer(s)
Prof. Dr. Varol PABUÇÇUOĞLU
Learning Outcomes
11. Being able to understand and anterpret the chemical properties causing the pharmaceutical actvity and their relations with biological process.
22. Being able to understand the relations between the chemical structures of pharmaceutically active synthetic and semi-synthetic compounds with therapotic and adverse effects and predict the possible biological responses.
33. Capable of giving examples about drug design methodology and approaches.
44. Being able to understand the chemical structures, chemical and physicochemical properties of the synthetic and semi-synthetic (drug) active compounds.
55. Being able to name the synthetic and semisynthetic molecules’ structure according to the nomenclature rules.
66. 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.
77. 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.
88. Being able to evaluate the potentials of biological response of the molecules in terms of chemical structure and reactivity.
99. To be able to understand the general chemical structure leading to a pharmacological response and predict the structure activity relationship.
1010. 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.
1111. Being able to predict the chemical structures and the possible incompatibilities of activemolecules and excipients and use this knowledge in formulatin and treatment process.
1212. Capable of understanding the basic approaches regarding to the methods of obtaining pharmaceutical active molecules and excipiants and solving possible problems suring synthesis.
1313. Capable of understanding and applying the principles, techniques and instrumentation of chemistry lab for qualitative and quantitative analysis.
1414. Capable of doing quantitative analysis of drug active molecules having specific functional group by spectrophotometric method.
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
Central nervous system drugs (Sedatives/Hypnotics, General Anesthesics, Anxiolitic drugs, centrally acting muscle relaxants, Antipsychotic (Neuroleptic) drugs, Antiepileptics, Non-steroidal Antiinflammatory drugs, Antigout drugs, Narcotic analgesic drugs, Analeptics and psychostimulants, Antidepresants), Gastrointestinal system medications, Antidiabetic drugs, hormones. Three demonstration courses are given before practical studies. Then quantitative analysis by spectrophotometric and volumetric methods are applied to the samples.
Weekly Detailed Course Contents
WeekTheoreticalPracticeLaboratory
1Sedative/Hypnotic Drugs A. Introduction B. Classification due to chemical structures I. Drugs bearing heterocyclic ring a) Barbituric Acid Derivatives Structure-Activity Relationship in Barbituric acid derivatives Metabolism of Barbituric acid derivatives General Synthesis Method for Barbituric acid derivatives Introduction to Spectral Analysis Methods
2Sedative/Hyipnotic Drugs a) Benzodiazepine Derivatives b) Quinazoline Derivatives c) Piperidinedione Derivatives d) Cyclopyrrolone Derivatives e) Imidazopyridine Derivatives f) Pyrazolopyrimidine Derivatives II. Non-heterocyclic drugs a) Alcohol Derivatives b) Aldehyde Derivatives General Anesthetic drugs A. Inhalation anesthetics I. Mechanisms of action II. Non-halogenated General Anesthetics III. Halogenated General Anesthetics IV. Anorganic Derivatives B. Intraventricular Anesthetics Single Component Analysis by UV Spectroscopy
3Anxiolytic Drugs A. Introduction B. Classification due to chemical structures I. 1,4-Benzodiazepine Derivatives II. Diphenylmethane Derivatives III. Propandiole dicarbamate Derivatives IV. Azaspirodecanedione Derivatives Introduction to quantitative volumetric analysis
4Centrally-acting muscle relaxants A. Introduction B. Classification due to chemical structures I. Glycerole monoether Derivatives II. Propandiole Derivatives III. Oxazolidinone Derivatives IV. Benzoxazole Derivatives V. Benzodiazepine Derivatives VI. GABA Derivatives VII. Imidazoline and Imidazolidindione Derivatives VIII. Derivatives withe different chemical structures Antipsychotic (Neuroleptic) drugs A. Introduction B. Classification due to chemical structures I. Phenotiyazine Derivatives Loanin the equipments and ıntroduction of the instruments
5Antipsychotic (Neuroleptic) drugs I. Thioxanthene Derivatives II. Butirophenon Derivatives III. Diphenylbutylpiperidine Derivatives IV. Dibenzoxazepine Derivatives V. Dibenzodiazepine Derivatives VI. Benzamide Derivatives VII. Reduced Indol Derivatives VIII. Pyridopyrimidine Derivatives C. Mechanism of action of Antipsychotic drugs and structural similarities to dopamin Vitamin B2 (Lactoflavin) Preparing solutions, reactives and reagents; drawing the calibration graph.
6Antiepileptic Drugs A. Introduction B. Mechanism of action of Antiepileptic Drugs C. Classification of antiepileptic drugs currently used in treatment I. Barbituric Acide Derivatives and compounds with similar structure II. Propandiole dicarbamate Derivatives III. Hydantoin Derivatives IV. 1,2,4-Triazine Derivatives V. Oxazolidinedione Derivatives VI. Acetic acid Derivatives VII. Süccinimide Derivatives VIII. Benzodiazepine Derivatives IX. Dibenzazepine Derivatives X. Sulfonamide Derivatives XI. Acylurea Derivatives XII. Nipecotic acid Derivatives Studying quantitative analysis of B2 vitamin sample
7Non-steroidal Antiinflammatory drugs A. Introduction B. Classification due to chemical structures I. Acetanilide Derivatives II. Salisilic Acide Derivatives III. Pyrazolinone and Pyrazolidinedione Derivatives IV. Aryl / Heteroarylalkanoic Acides V. N-Arylantranilic Acides VI. Enolic Acides VII. Quinazolinone Derivatives Vitamin B6 Preparing solutions, reactives and reagents; drawing the calibration graph
8Midterm exam
9Non-steroidal Antiinflammatory drugs I. Sulfonamide and Bioizosteric Derivatives (Selektive COX-2 Inbitors) B. Interactions of Antiinflammatory drugs with cyclooxygenase enzyme C. Inhibition of Cyclooxygenase enzyme with 5-Lypooxygenase enzyme Antigout drugs Studying quantitative analysis of the vitamin B6 sample
10Narcotic analgesic drugs A. Introduction B. Classification due to chemical structures I. Morphine and its derivatives II. Oripavine derivatives III. Morphinane derivatives IV. 2,6-methano-3-benzazocine(6,7- benzomorphan) derivatives V. Phenylpiperidine derivatives VI. Anilidopiperidine derivatives VII. Diphenylenylpropylamine derivatives Preparation of the Iodine solution and quantitative analysis of Novalgine by volumetric methods
11Analeptics and psychostimulant Drugs A. Analeptic Drugs B. Psychostimulant Drugs I. Amphetamine and its similars (Adrenergic Stimulants) Preparation of the sodiumthiosulphate solution and quantitative analysis of Vitamin C by volumetric methods
12Antidepressant Drugs A. Introduction B. Classification due to chemical structures I. Monoamine oxidases (MAO) Inhibitors II. Tricyclic Antidepressants (TCA) III. Serotonine (5-HT) re-uptake inhibitors IV. Norepinefrin (NE) and serotonine (5-HT) re-uptake inhibitors C. Anorganic compounds Preparation of KMnO4 solution and quantitative analysis of oxalic acid by volumetric methods
13Gastrointestinal Medications 1. Drugs used in Acid-peptic disorders (Antacids, H2 blockers, proton pump inhibitors, drugs that increase gastrointestinal mucosal resistance ), prokinetics, laxatives, antidiarrheal drugs, antiemetic drugs, miscellaneous drugs.Preparation of HCl and NaOH solutions and determination of factors
14Antidiabetic drugs: Oral hypoglycemic drugs (sulfonylureas, glinide derivatives, Thiazolidinedione derivatives, GLP-1 agonists/DPP-4 inhibitors, biguanide derivatives, Alpha-glucosidase inhibitors, SGLT-2 inhibitors), amylin agonistsQuantitative analysis of lactic acid by volumetric methods
15Hormones A. Introduction B. Classification due to chemical structure I. Hormones as amine structure II. Hormones as aminoacid structure 1. Thyroid Hormones 2. Antithyroid drugs a) Organic Antithyroid drugs b) Inorganic Antithyroid drugs c) Hormones as peptides Steroid Hormones 1. Adrenal gland hormones, Glucocorticoids, Mineralocorticoits 2. Sex hormones, Androgen ve Anabolisants, Estrogen (Steroid ve Nonsteroid estrogens, estrogen antagonists), Lutheal hormones ve contraceptives. Compensation
16Final
Recommended or Required Reading
1. Farmasötik Kimya I ve II (A. Akgün, A. Balkan, A. A. Bilgin, U. Çalış, S. Dalkara, H. Erdoğan, D. D. Erol, M. Ertan, F. Özkanlı, E. Palaska, S. Saraç, C. Şafak, Irmak Matbaası, Ankara, 2000) 2. Farmasötik Kimya Ders Kitabı. I. Medisinal Kimya (N. Ergenç, A. Gürsoy, O. Ateş, İstanbul Üniversitesi Basım ve Film Merkezi, İstanbul, 1997) 3. İlacların Metabolizması (Biyotransformasyon) (S. Rollas, Marmara Üniversitesi MatbaasI, İstanbul, 1992) 4. Burger’s Medicinal Chemistry and Drug Discovery , Volumes 1-6 (M. Wolff, editor, John Wiley and Sons, Inc., New York) 5. İlaçların Metabolizması (Biyotransformasyon), Prof. Dr. Sevim Rollas, Marmara Üniversitesi Yayınları, İstanbul, 1992. 6. 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. 7. Farmasötik Kimya Cilt I, Prof.Dr.Hakkı Erdoğan ve arkadaşları, Irmak Matbaası, Ankara, 2000. 8. Farmasötik Kimya Cilt II, Prof.Dr.Hakkı Erdoğan ve arkadaşları,Irmak Matbaası, Ankara, 2000. 9. Farmasötik Kimya Prof.Dr.Hakkı Erdoğan ve arkadaşları, Hacettepe Üniversitesi Yayınları, Ankara, 2004.
Planned Learning Activities and Teaching Methods
Assessment Methods and Criteria
Term (or Year) Learning ActivitiesQuantityWeight
Midterm Examination1100
SUM100
End Of Term (or Year) Learning ActivitiesQuantityWeight
Final Sınavı1100
SUM100
Term (or Year) Learning Activities40
End Of Term (or Year) Learning Activities60
SUM100
Language of Instruction
Turkish
Work Placement(s)
None
Workload Calculation
ActivitiesNumberTime (hours)Total Work Load (hours)
Midterm Examination111
Final Examination122
Attending Lectures14342
Laboratory14342
Self Study14228
Individual Study for Mid term Examination12525
Individual Study for Final Examination13030
TOTAL WORKLOAD (hours)170
Contribution of Learning Outcomes to Programme Outcomes
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LO1      5      4       
LO2 5          44 3 2   
LO3 3     35          43
LO4 4    5      3 2     
LO5 2    4             4
LO6 3          55       
LO7 3          55       
LO8      55             
LO9       55            
LO10           55 2      
LO11           55 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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