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King Abdul-Aziz University College of Health Sciences Department of PHARMACY Final Examination Pharmaceutical Chemistry (HCHM 211) Academic Year 1429-1430 (2009) DATE: … February 14th, 2009…………………. STUDENT NAME: …………………………………………………. INFORMATION TO CANDIDATES 1. NO OF PAGES: …7…… Time: 120 minutes 2. TOTAL NUMBER OF QUESTIONS: …28… QUESTIONS 3. TOTAL NUMBER OF MARKS: …40.. MARKS (This constitutes 30 course marks) % of your final PLEASE READ THE QUESTIONS CAREFULLY & & ANSWER THE FOLLOWING QUESTIONS IN THE ENCLOSED BOOKLET PROVIDED THIS DOCUMENT CONSISTS OF …6… PRINTED PAGES EXCLUDING THIS PAGE SECTION A B C D TOTAL MARKS SIGN. REVIEWED SECTION A: (10 questions, each question 1 mark), please read the question carefully and tick T (True) or F (False) as appropriate. 1. Aminoglycosides are very polar cross BBB in meninges only 2. T( ) F( ) Vitamin D deficiency results in rickets in infants and children as result of inadequate calcification of bones. T( ) F( ) PGE has a C=O at C-9 and -hydroxyl group at C-11 while PGF has two -hydroxyl group at 3. C-9 and C-11. T( ) F( ) 4. Vitamin D3 must be hydroxylated in the liver by vitamin to perform its action. T ( ) F ( ) 5. Vitamin B1 is very effective in cases of neuritis and in combination with vitamin C in treatment of rheumatic conditions. 6. T( ) F( ) Proinsulin is activated by an endopeptidase and carboxypeptidase to liberate equimolar quantities of insulin and connecting C-peptide. T( ) F( ) 7. Vitamin A is present mainly in fish liver, herbivorous liver, carrot and butter fat. T ( ) F ( ) 8. Ascorbic acid is involved in metabolic hydroxylation and drug metabolism. T ( ) F ( ) 9. Lypressin (8-Lys vasopressin) is more stable and more rapidly absorbed than vasopressin. T( ) F( ) Misoprostol prevents gastric ulceration used orally but Dinoprost (PGF2) used parenterally 10. for induction of labor or abortion within 1st trimester. T( ) F( ) SECTION B: MCQs (9 questions, each question 1 mark) The prodrug is prepared to ………………… 11. a. Decrease the drug duration of action ( ) b. Increase the drug potency ( ) c. Increase the drug stability and bioavailability ( ) d. Inactivate the drug at the desired target site of action ( ) Vitamin D accomplishes its biological role through ………………….. 12. a. Enhancing the absorption of calcium and phosphate from small intestine ( ) b. Promoting their mobilization from bone ( ) c. Decreasing their excretion by the kidney ( ) d. All of the above ( ) 13. The following are natural hormones except a. Prostaglandins ( ) b. Insulin ( ) c. Mestranol ( ) d. Estradiol ( ) Page 2 of 7 14. Lispro insulin is… a. Natural human insulin ( ) b. Natural human insulin produced by r-DNA technique ( ) c. More antigenic than porcine insulin ( ) d. Less antigenic than other insulin products ( ) Vitamin K1 is the drug of choice as anti-hemorrhagic because …… 15. a. It can be activated in the body to more active metabolite ( ) b. Rapid onset ( ) c. Short duration of action ( ) d. Vitamin K can be used to diagnosis kidney function accurately ( ) 16. The following statements about antiseptics are true except: a. The antibacterial potencies of primary alcohol increase with molecular weight up to C8, where cutoff is reach ( ) b. Branching decrease antibacterial potency, hence primary > 2ry > 3ry alcohol. ( ) c. Substituted phenols are less potent, less irritant than unsubstituted one. ( ) d. Cationic surfactants are inactivated by soap and not active against spore ( ) 17. Regarding to biological activity of folic acid, the following is true except: a. Reduced metabolically to tetrahydrofolic acid (THF). ( ) b. Participate in the biosynthesis of nucleic acid ( ) c. Its antagonists depends on N10 or N5 hydroxylation. ( ) d. Biologically active as one carbon transfer. ( ) 18. Prostaglandins possess: a. Trans double bond at C13. ( ) b. The hydroxy-bearing chain termed chain and carboxy-bearing chain is -chain. ( ) c. Two side chains are of the trans stereochemistry. ( ) d. All of the above. ( ) Antifungal drugs …… 19. a. The more potent antifungal azoles possess two or three aromatic rings b. The nonpolar functionality give a high degree of lipophilicity to antifungal azoles. ( ) c. all azoles are insoluble in water except fluconazole. ( ) d. All of the above ( ) Page 3 of 7 ( ) SECTION C: Complete the missed information in the following questions: (8 questions, each question 2 marks) Streptomycin belongs to group of antibiotics named as ………………………………. 20. Show on the structure the enzymatic inactivation (resistance) H2N NH2 HO O H2N HO HO O O CH2NH2 HOH2C O HO NH2 OH 21. R 1 H 3C Explain the SAR of tetracyclines a. …………………………………………………..…..… b. ……………………………………………….…..…..… OH OH O N R2 OH OH OH O CONH2 c. …………………………………………………..…..… d. ……………………………………………………..…………………..…..… e. …………………………………………………..…………………………..…..… f. …………………………………………………..…………………………..…..… 22. Regarding macrolid antibiotics, complete the following: a. Erythromycin is acid labile when R = ……… N O R1 = ……………………………… b. Erythromycin prodrug: R = ………… R1 = ……………………………… c. RO O HO R1O HO Acid-stable clarithromycin: R = ………… R1 = ……………………………… OCH3 O OH O O Page 4 of 7 O O O 23. Discuss why acyclovir is antimetabolite drug? N HN ……………………………………....……………………… ………..…………………………….……..………..…..… H2 N HO N N O ………………………………………..………………………… Acyclovir ……..……………………………………………………………………………………………… ……………………………………………………………………………..………………..…..… 24. Moxalactam is a third generation cephalosporin. COOH OCH3 H N O CH3 O N HO S N O Moxalactam a. N COOH N N Illustate the role of the assigned groups on the pharmacological effect of moxalactam: (OH) ………………………………………………………………………..……………… (COOH) ………………………………….…………………………………..……………… (OCH3) …………………………………..…………………………………..……………… (O) ……………………………………………………………………………..……………… b. Using structural formula, explain how moxalactam can be given orally (prodrug)? Page 5 of 7 25. Examine the structure of the following compounds then complete the spaces HO H H HO H3C S N O NH2 N H H H3C S NH NH N H O S O O COOH H2N H NH N O COOH N SO3Na Thienamycin COOH Imipenem a. Aztreonam sodium Imipenem belongs to a group of antibiotic named as ………………………………, ehile aztreonam belongs to ………………………………………group. b. Imipenem is structurally modified derivative of thienamycin, explain the reason of this modification………………………………………………………………………. …………………………………………………………………………………………. c. In treatment of urinary tract infections, imipenem should coadminstred with cilastatin in order to ……………………………………….……………………….. 26. Danazol is oral androgen. CH3 OH C CH CH3 N Danazol O a. It considered as androgen because ……………………… in its structure, orally due to ……………………………………………. b. The increase in anabolic properties over androgenic is due to ……………………… ………………………………………………….. 27. Cyclophosphamide is anticancer prodrug, discuss the mechanism of action? H N Cl O P N O Cl Page 6 of 7 SECTION D: 28. Fill the spaces in the table by the corresponding compound name (5 marks) OCH3 O OCOCH3 CH3 H 3CO OH C CH H Cl O CH3 H3CO O Medroxyprogesterone acetate Norethindrone Chlorotrianisine C2H5 OCH2CH2N C2H 5 H 3C N NH2 H 2N CH3 OH N 2 Cl HOH2C CH3 Tamoxefen OH Vitamin B1 Ascorbic acid CH 2OH OH CH3 O HO C CH CH3 CH3 F N O O Mestranol OH CH3 O O H3CO Triamicinolone acetonide Biological activity Danazol Compound name Semisynthetic anabolic androgen Progesterone prodrug Orally active non-steroidal estrogen Nor-testosterone with progesterone activity Anti-estrogen Anti- scurvy drug Anti-inflammatory steroidal prodrug Orally active steroidal estrogen anti-beriberi factor BEST WISHES Dr. M. Sheha Page 7 of 7 O O C CH