What is Pharmacology?

1. What is Pharmacology? • Name of faculty member responsible for the course: • Dr.AmiraBadr • Dr.NajlaaAl.Orabi • Dr.NayiraAbdulbaqy

2. Syllbus • Summary of the main learning outcomes for students enrolled in the course. • To be familiar to the scope of pharmacology, common drug uses, their sources and routes of administration. • To understand the basis of drug actions , drug pharmacokinetics and pharmacodynamics, receptor types drug-receptor interaction, and common adverse effects of drugs. • To identify the different classes of drugs affecting the two main divisions of the autonomic nervous system (sympathetic and parasympsathatic).

3. To identify the effectct and therapeutic uses of different class of autonomic drugs. • To discuss side effects and contraindication of commonly used autonomic drugs • To identify the various classes of cardiovascular affecting drugs; antihypertensives and antiarrhythmic drugs • To identify various cardiovascular diseases, and drug classes use in management of each disease. • To explain the major pharmacological actions of different autocoids in the body.

6. LECTURES’ OUTLINE PHL 311

10. EvaluationD/amira: • Midterm: 7marks • Quiz on week 4: 2 marks • File (4 stunts) : 2 marks تنبيهات: • لا يتجاوز الغياب 6 محاضرات على مدار الترم. • الغياب عن الquizz لا بد أن يكو بعزر مسبق. • يتم تسليم النشاط فى الوقت المحدد والا لن يعتد به. • التغيب عن الامتحان الفصلى لا بد أن يرفق بشهادة مرضية مختومة من جهة حكومية.

11. What is Pharmacology? • derived from the Greek word for drug • A science that studies drug effects within a living system, biochemical and physiological aspects • Deals with all drugs used in society today, legal or illegal, including street, prescription, and non-prescription or over –the-counter medications

13. Drug • A drug is defined as any substance; chemical agent; used in the • Diagnosis • Cure • Treatment • prevention of a disease or condition

14. Drug Names • Chemical Name • Generic Name • Trade Name

15. Chemical Name • Describes its molecular structure and distinguishes it from other drugs

16. Generic name • Determined by the pharmaceutical company along with a special organization known as the U.S. Adopted Names Council (USAN)

17. Trade Name • Or brand name- the manufacturer selects alone…can become a registered trademark. • They are the only one who can advertise and market the drug under that name.

18. How is the Trade Name Chosen? • The particular spelling of a brand name drug is proposed by a manufacturer for one of several reasons.

19. 1. To indicate the disease process being treated • Azmacort- treats asthma • Rythmol- treats cardiac arrhythmias

20. 2. To simplify the generic name • Pseudoephedrine to Sudefed • Haloperidol to Haldol • Ciprofloxacin to Cipro

21. 3. To indicate the duration • Slow-K slow release potassium supplement

22. Prescription Drugs • Or legend drugs • Means in order to obtain drug, you must have a legal prescription

23. Non-Prescription Drugs • Or Over-the-Counter (OTC) drugs • Drug that may be purchased without a prescription

24. Sources of Drugs Drugs have been identified or derived from four main sources: • Plants • Animals • Minerals and Mineral Products • Synthetic or Chemical Substances Made in the Laboratory

25. Routes of drug administration

26. Important Info Routes of Drug Administration The route of administration (ROA) that is chosen may have a profound effect upon the speed and efficiency with which the drug acts

28. The main routes of drug entry into the body may be divided into two classes: • Enteral • Parenteral

29. Enteral Routes • Enteral- drug placed directly in the GI tract: • sublingual - placed under the tongue • oral - swallowing (p.o., per os) • rectum - Absorption through the rectum

30. Sublingual/Buccal Some drugs are taken as smaller tablets which are held in the mouth or under the tongue. • Advantages • rapid absorption • drug stability • avoid first-pass effect

31. Sublingual/Buccal • Disadvantages • inconvenient • small doses • unpleasant taste of some drugs

32. Oral • Disadvantages • Sometimes inefficient - only part of the drug may be absorbed • First-pass effect - drugs absorbed orally are initially transported to the liver via the portal vein • irritation to gastric mucosa - nausea and vomiting

33. Oral • Disadvantages • destruction of drugs by gastric acid and digestive juices • effect too slow for emergencies • unpleasant taste of some drugs • unable to use in unconscious patient

34. First-pass Effect • The first-pass effect is the term used for the hepatic metabolism of a pharmacological agent when it is absorbed from the gut and delivered to the liver via the portal circulation. • The greater the first-pass effect, the less the agent will reach the systemic circulation when the agent is administered orally

35. First-pass Effect Magnitude of first pass hepatic effect:Extraction ratio (ER) ER = CL liver * Q ; where Q is hepatic blood flow (usually about 90 L per hour. Systemic drug bioavailability (F) may be determined from the extent of absorption (f) and the extraction ratio (ER): F = f x (1 -ER)

36. First-pass Effect

37. RECTAL ADMINISTRATION: • Absorption across the rectal mucosa occurs by passive diffusion. • This route of administration is useful in children, old people and unconscious patients. • Eg., drugs that administered are: aspirin, acetaminophen, theophylline, indomethacin, promethazine & certain barbiturates. KLECOP, Nipani

38. Rectal Advantages: Suitable for unconscious patients and children 2. suitable if patient is nauseous or vomiting 3. easy to terminate exposure 4. good for drugs affecting the bowel such as laxatives Disadvantages: absorption may be variable irritating drugs contraindicated

39. Parenteral Routes • Intravascular (IV, IA)- placing a drug directly into the blood stream • Intramuscular (IM) - drug injected into skeletal muscle • Subcutaneous- Absorption of drugs from the subcutaneous tissues • Intrathecal : into CSF

41. Intravascular Absorption phase is bypassed (100% bioavailability) 1.precise, accurate and almost immediate onset of action, 2. large quantities can be given, fairly pain free Disadvantages a-. greater risk of adverse effects b-high concentration attained rapidly C- risk of embolism

42. Intramuscular 1. very rapid absorption of drugs in aqueous solution 2. Slow release preparations Disadvantages pain at injection sites for certain drugs

43. Subcutaneous slow and constant absorption 2. absorption is limited by blood flow, affected if circulatory problems exist 3. concurrent administration of vasoconstrictor will slow absorption

44. Inhalation 1. gaseous and volatile agents and aerosols 2. rapid onset of action due to rapid access to circulation a. large surface area b. thin membranes separates alveoli from circulation c. high blood flow

45. Topical • Mucosal membranes (eye drops, antiseptic) • Skin • a. Dermal - rubbing in of oil or ointment (local action, sun screen, an callus removal) • b. Transdermal - absorption of drug through skin (systemic action) • i. stable blood levels • ii. no first pass metabolism • iii. drug must be potent or patch becomes too large

46. Intra nasal administration • Drugs generally administered by intra nasal route for treatment of local condition such as perennial rhinitis, allergic rhinitis and nasal decongestion etc.

47. Route for administration -Time until effect- • intravenous 30-60 seconds • intraosseous 30-60 seconds • endotracheal 2-3 minutes • inhalation 2-3 minutes • sublingual 3-5 minutes • intramuscular 11-30 minutes • subcutaneous 14-30 minutes • rectal 5-30 minutes • ingestion 30-90 minutes • transdermal (topical) variable (minutes to hours)

48. DEFINITION OF PHARMACOKINETICS AND PHARMACODYNAMICS

49. Aspects of Drug Pharmacokinetics (ADME) Drug at site of administration Absorption Drug in plasma Distribution Drug/metabolites in tissues Metabolism Elimination Drug/metabolites in urine, feces, bile