Description of Individual Course Units
Course Unit CodeCourse Unit TitleType of Course UnitYear of StudySemesterNumber of ECTS Credits
300003442007PHARMACEUTICAL CHEMISTRY IICompulsory366
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 perform qualitative analysis of drugs by classic organic analysis methods and to teach the principles and application of pharmacopoeia analysis.
Name of Lecturer(s)
Prof. Dr. Vildan ALPTÜZÜN
Learning Outcomes
11. Being able to understand and interpret 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.
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. To be able to identify the (unknown) sample by using -classic -organic analysis methods.
1515. Having a basic knowledge and skills about pharmacopeia analysis
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
Autonomic central nervous system drugs (drugs affecting parasympathetic nervous system, drugs affecting sympathetic nervous system, antiparkinson drugs), Antiparkinson drugs, Cardiovascular system drugs (Cardiotonics), Antihypertensives (Calcium channel blockers, Angiotensin-converting enzyme inhibitors and receptor blockers), Peripheric vasodilators, Antianginals antiarrhytmics, Antiarrhytmics, Anticoagulants, Antitrombotics, Diuretics, Antihyperlipidemics, Local Anesthesics, Antihistaminics, Gastrointestinal System Drugs (Peptic ulcer , Laxatives, Purgatives, Emetics, Antiemetics), Oral antidiabetic drugs. Before laboratory studies, 3 demonstrative courses (2 for qualitative analysis, 1 for pharmacopoeia analysis are given. Qualitative analysis of unknown samples are performed during the rest of the laboratory courses. A pharmacopoeia analysis application is performed on the last laboratory day.
Weekly Detailed Course Contents
WeekTheoreticalPracticeLaboratory
1Introduction to autonomic nervous system drugs. 1. Functional Regulation of autonomic nervous system 2. Autonomic nervous system Drugs affecting parasympathetic system 1. parasympathomimetic drugs 1.1. Directly-acting Parasympathomimetic Drug 1.1.1. Choline esters -The relationship between chemical structure of the active compounds and their effects 1.1.2. Some alkaloids and their analogs 1.2. Indirect acting parasympathomimetic drugs 1.2.1. Reversible Anticholinesterases 1.2.2. İrreversible Anticholinesterases 2. Parasympatholytic drugs -The structure-activity relationship in this group of compounds - Stereochemical features of this type of compounds 2.1. Amino alcohol esters 2.1.1. Belladone alkaloids 2.1.2. Semi-synthetic analogs 2.1.3. Synthetic analogs 2.2. Amino alcohols 2.3. Aminoamits 2.4. Various compounds Demonstration of basic principles of qualitative analysis laboratory
2 Drugs affecting sympathetic system 1. Sempatomimetic drugs -Structure activity relationship in Phenethylamine derivatives 1.1. Catecholamine derivatives 1.2. Other sempatomimetic drugs 1.2.1. Directly acting drugs 1.2.1.1. Directly acting drugs on α-receptors a) Anti-hypotensive drugs b) Nasal decongestion 1.2.1.2. Directly acting drugs on β -receptors a) Drugs affecting bronchial β2 -receptors b) Drugs affecting vessel β2 -receptors 1.2.2.Indirect acting drugs 1.2.3.Drugs having both effects 2. Symphatolytic drugs 2.1. Adrenarjik receptor blockers 2.1.1. α-Blockers 2.1.1.1. β- halo-alkylamine 2.1.1.2. Imidazolins 2.1.1.3. Dibenzazepinler 2.1.1.4. Benzodioxanes 2.1.1.5. Ergo alkaloids 2.1.1.6. Yohimbine derivatives 2.1.1.7. Other derivatives 2.1.2. β-Blockers 2.1.2.1. Nonselective β-blockers 2.1.2.2. Cardioselective β-blockers 2.2. Adrenerjic Neuron blockers Demonstration of basic principles of qualitative analysis laboratory
3 Antiparkinson drugs 1. General Information about Parkinson’s disease. 2.Mechanism of action of drugs used in Parkinson’s disease treatment. 3.Drugs used in treatment of the disease. 3.1. Dopa Precursor 3.2.Dopamin agonists 3.3.Dopa decarboxylase inhibitors 3.4.MAO inhibitors 3.5.KOMT inhibitors 3.6.Antimuscarinic drugs 3.7.The others Drugs used in treatment of congestive heart failure 1. Drugs directly affecting blood-vessel system 1.1. Cardiotonic Drugs Demonstration of basic principles of pharmacopoeia analysis
4 1.2. Antihypertensive drugs 1.2.1.Antihypertansive drugs affecting the central nervous system 1.2.2. Drugs affecting the peripheral system 1.2.2.1. α1-receptor blockers 1.2.2.2. β-receptor blockers 1.2.2.3.Adrenerjik neuron blockers 1.2.2.4. ganglionic blocker drugs 1.2.2.5.MAO inhibitors 1.2.3. Drugs acting on vascular smooth muscle 1.2.3.1. Drugs having vasodilator effects on Arteries 1.2.3.2. Drugs having vazodilator effects on both arteries and veins 1.2.4. Calcium channel blockers 1.2.4.1.1,4- dihydropyridine derivatives 1.2.4.2.Verapamil group “arylakylamine derivatives”, 1.2.4.3.Diltiazem group “benzodiazepine derivatives”, 1.2.4.4. Compounds having diphenylalkylamine group Application of melting point determination
5 1.2.5. Angiotensin-converting enzyme inhibitors (ADE) 1.2.5.1. Renin-angiotensin system 1.2.5.2. Structure activity relationship of ADE ınhibitors 1.2.6. Angiotensin receptor blockers Qualitative analysis of the known sample
6 1.3. Peripheral vasodilators 1.3.1. Drugs affecting directly 1.3.2. β-adrenergic receptor activators 1.3.3. Calcium channel blockers 1.3.4. α-adrenergic receptor blockers 1.3.5. Adrenergic neuron blockers 1.3.6. The other drugs Qualitative analysis of the known sample
7 1.4. Antianginal drugs 1.4.1. Organic nitrate and nitrils 1.4.2. Calcium channel blockers 1.4.3. β-adrenergic receptor blockers 1.4.4. The other drugs 1.5. Antiarrhythmic drugs 1.5.1. Sodium channel blockers 1.5.1.1. Drugs prolong action potential duration 1.5.1.2. Drugs shorthen action potential duration 1.5.1.3. Drugs does not affect Action potential duration and prolonged repolarization time 1.5.2. β blockers 1.5.3. Potassium channel blockers 1.5.4. Calsium channel blockers Qualitative analysis of the known sample
8Midterm Exam
9 2. Drugs used in the treatment of heart diseases though having no effect on cardiovasculer system. 2.1. Antihyperlipidemic 2.1.1. Drugs that reduce the synthesis of lipoprotein 2.1.1.1. Hydroxymethylglutaryl-coenzyme A inhibitors 2.1.1.2. Fibrates 2.1.1.3. Nicotinic acid derivatives 2.1.2. Drugs enchancing Lipoprotein catabolism 2.1.3. The others Qualitative analysis of the sample
10 2.2. Antithrombotic 2.2.1. Anticoagulant Drugs 2.2.1.1.Directly affecting drugs 2.2.1.2. Indirectly affecting drugs (Oral Anticoagulants) 2.2.1.2.1. Cumarine derivatives 2.2.1.2.2. Indondion derivatives 2.2.2. Thrombotic and antiplatelet drugs Qualitative analysis of the sample
11 2.3. Diuretics 2.3.1. Drugs affecting Proximal tubules 2.3.1.1. Carbonic anhydrase inhibitors 2.3.1.2. Xanthine derivatives 2.3.1.3. Osmotic diuretics 2.3.2. Drugs affecting Henle handle 2.3.2.1. Mercurial diuretics 2.3.2.2. Loop diuretics Qualitative analysis of the sample
12 2.3.3. Drugs affecting Distal tübüle 2.3.3.1. Tiazit derivatives 2.3.3.2. Potassium-sparing diuretics Qualitative analysis of the sample
13 Local anestesics 1. Structure-activity relationships in local anesthesics 2. Mechanism of local anesthesic drug action 3. Metabolism of Local anesthesics 4. Classification of local anesthesic 4.1. Esther derivatives 4.1.1. Coca alcaloids 4.1.2. Benzoic acid derivatives 4.2. Amide and amidine derivatives 4.3. The other derivatives Antihistaminics 1. Classification of antihistaminics 1.1. Derivatives having dialkylamine structure 4.1.1.1.ethylendiamine derivatives 1.1.2. Ethanolamine derivatives 1.1.3. Propylamine and aklene derivatives Qualitative analysis of the sample
14 1.2. Cyclic amines having basic structure 1.2.1. Piperidine derivatives 1.2.2. Piperazine derivatives 1.3. Tricyclic alkyl amine derivatives 1.4. The other derivatives 1.1.1. Ethylenediamine derivatives 1.1.2. Ethanolamine derivatives 1.1.3. Propylamine and alkene derivatives Gastrointestional system drugs 1. Drugs affecting peptic ulcers 1.1. Drugs reducing Acid secretion 1.1.1. H2 receptor blockers 1.1.2. Proton pomp inhibitors 1.2. Antacids Qualitative analysis of the sample
152. Laxative and purgative drugs 2.1. Osmotic laxative and purgative drugs 2.2. Stimulative laxative and purgative drugs 2.3. Surface active laxatives 3. Emetic drugs 3.1. Peripheral emetics 3.2. Central-acting emetics 4. Antiemetic drugs Oral Antidiabetics 1. Sulphonylurea compounds 1.1. First generation Sulphonylurea compounds 1.2. Second generation Sulphonylurea compounds 2. Third generation Sulphonylurea compounds 3. Biguanides 4. Thiazolidinediones Compensation
16Final
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 Cilt I, Prof.Dr.Hakkı Erdoğan ve arkadaşları, Irmak Matbaası, Ankara, 2000. 5.Farmasötik Kimya Cilt II, Prof.Dr.Hakkı Erdoğan ve arkadaşları,Irmak Matbaası, Ankara, 2000. 6.Farmasötik Kimya Prof.Dr.Hakkı Erdoğan ve arkadaşları, Hacettepe Üniversitesi Yayınları, Ankara, 2004.
Planned Learning Activities and Teaching Methods
Activities are given in detail in the section of "Assessment Methods and Criteria" and "Workload Calculation"
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          44 3 2   
LO2 3     35          43
LO3 4    5      3 2     
LO4 2    4             4
LO5 3          55       
LO6 3          55       
LO7      55             
LO8       55            
LO9            55 2     
LO10            55 2 2   
LO11        5 4       4  
LO12          5       5 4
LO13          5       5 4
LO14          5       5 4
LO15                     
* Contribution Level : 1 Very low 2 Low 3 Medium 4 High 5 Very High
 
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