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Lecture 4

BPS1101 Lecture 4: Drugs 101

16 Pages
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Department
Biopharmaceutical sciences
Course Code
BPS1101
Professor
William Ogilvie

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Description
Drugs 101 – Notes from Lecture Two: Pain Medication Prescription Drugs:  $300 billion per year (U.S.)  Requires doctor’s prescription Over the Counter: OTC  $25 Billion per year (U.S.)  No prescription required  Some are “behind the counter” Top OTC drugs in North America  On the chart, cough and cold meds are “#1 making up 4.1 billion dollars” and pain reliever drugs are #2 making 2.7 billion dollars … but we need to remember that cough and cold costs more money and therefor o Pain reliever is the one we use most often o Cough and cold costs more but use them less often Important Considerations when Buying  Safety o Dose makes the drugs … We take more than one pill due to us wanting it to go away – but dose is based on body size (ex. Julia takes one pill because she’s 13, if she takes 10 it will not make her headache go away any faster and The Rock would probably take 4 due to his body composition) o Dose makes the Poison … look at the side effects on the box – all drugs will have side effects warnings but we also need to ask ourselves how much these side effects happen (difficult to find)  Indications o What is this used for? Ex; taking Tylenol for inflammation even though it reduces pain but not inflammation – people also take drugs when not needed  Counter-indications o When you should NOT use  Conditions  Drug combinations: sometimes Advil or other drugs may interfere with the effect of the prescription drug  Foods  “Natural” remedies: can evoke an unwanted response even if you don’t think it will – must be careful and ask doctor if your natural remedies will cause side effects Pain relievers are the most common OTC Drug  $2.7 billion per year (North America)  50 billion tablets (North America)  16,000 tonnes/year  500 dump trucks The world’s most popular Drugs  Aspirin is the most popular but not as popular in Canada anymore  Caffeine  Alcohol  Aspirin  Nicotine? Aspirin  Salix is the genus – about 400 species of Salix o Willow o Poplar o Beech o Wintergreen  Salicylates: chemicals that occur naturally in plants, kind of natural pesticide to protect plant against insects and diseases o Sumerians used willow for pain back in ancient times and o Egyptians used it for inflammation  The knowledge of herbs were lost in the dark ages due to the strict control the church had on what was to be used and what was not – if the church demanded a specific herb be used for something it must be used for that purpose and not for anything else. As well if a person found a drug and the church didn’t know about the drug they got in serious trouble: known as Dark Hearts … all this went on in the Dark Ages  Reverend Edward Stone 1702 – 1768 … o Rector in Church of England o Described treatment for ague (argue meaning: malaria or some other illness involving fever and shivering) in 1763 o Was suffering from a fever and he discovered that willow could be used – tasted bark of willow tree, the tree tasting was similar to quinine due to this bitter taste he believed that willow bark would cure fever (grows in this area and taste) o Doctrine of Signatures - Association between disease and cure – their analysis is stated bellow  People who live near swamps get malaria  People with malaria have fever  Treat malaria with quinine  Quinine is bitter  Willow bark is bitter  Willows grow in swamps  Therefore … Willow bark will cure fever!!! Willow Tree Bark  Dried bark  Ground to a powder  Given for fever  Active ingredient in willow is salicin Not many people lived near water and swampy areas so they didn’t have access to these willow trees. Had to pay a lot of money to get the willow bark – but sometimes the bark wouldn’t produce the same effects due to it being a natural substance Salicin Evolution  Salicin was converted to salicylic acid in 1838  Better drug than salicin (lower dosages) – because it was more available in higher quantities; needed a lot of bark to give dose to a person – 30 g of bark to cure one person’s headache; coal tar manufacturing could happen in big quantities and was a lot cheaper  Occurs in meadowsweet flowers (very small amounts) o Salicylic Acid was an  Analgesic: reduce pain  Antipyretic: reduce fever  Ant inflammatory: reduce swelling  Cold Tar was a waste product … it comes from coal, convert coal into coal gas – which was used to light street lights and was effective to light the city o Coal was a waste – it was just dumped until people found Natural Vs Synthetic Natural – using willow tree bark for benefits of the Salicin, Natural doesn’t mean there are no downsides Artificial – designed by humans Synthetic – made from oil (ex. Using coal tar to create  Natural needed 100 million trees just create pills for one year (58 billion tablets)  Synthetic needed a few minutes of production to get the oil for the synthetic drugs – shows that source isn’t a big deal and in these case artificial was better but it varies which one is better natural or synthetic Dye Companies – experts in coal tar Chemistry  Specialized in Coal Tar and became the first pharmaceutical companies  Salicylic acid made and sold by dye companies o 2 major side effects for this drug were the stomach pains and the bitter taste o Felix Hoffmann 1868 – 1946 came along, after his father having arthritis and dealing with this pain for so long he came up with a different way for the drug to be effective – better version and artificial o First try – the drug didn’t have any side effects that were existent before but mainly due to the fact the drug didn’t solve anything at all  August 10, 1897 – the creation ofAcetasalicylic acid o First artificial drug that was made a difference: he made thousands of little changes until finally it worked o Not only that he was the first person to start testing on animals  He used a fish gill as a surrogate for what happened in a human stomach Aspirin was originally sold as a powder but once put into tablets they were a lot more popular due to how easy they were to take – not as brutal of a taste  Aspirin and ASA are the same thing… Aspirin is the trade name of the company and ASA is the scientific/generic name o Benefits of ASA: Pain and fever relief, helps with inflammation, and reduces rise of heart attack o Side Effects of ASA: Tinnitus (Ring in the Ear), Stomach irritation, and Blood clotting o Not effective for pain of an organ, but is effective for muscle pain Mechanical Breakdown: The ASA interferes with the prostaglandins - Problems with prostaglandins production can occur, leading to unwanted inflammation in the body. The prostaglandins are part of a natural response to stresses, but excessive prostaglandins production can cause chronic problems with pain. Painful menstruation, arthritis, heavy menstrual bleeding and some types of cancer are all connected to excessive prostaglandins levels. Some anti-inflammatory medications work by blocking the enzymes that cause these hormones’ production, thus reducing inflammation and preventing a blood clot from forming Aspirin blocks the Cyclooxygenase … the body doesn’t use prostaglandins for pain in the organs  One aspirin, every 2 days for 5 years – done under doctor’s prescription; aspirin harms the stomach so not worth taking unless severely needed Myocardial Aspirin Placebo infarction Fatal 10 26 Non-fatal 129 213 Aspirin and the Heart – early ads claim that aspirin does nothing for your heart: aspirin is now advertised for heart protection – but then it was believed that aspirin had a link to cancer Aspirin (ASA) was featured in the news due to its explosive properties: Anders Breivik is a Norwegian far-right terrorist who committed the 2011 Norway attacks he killed 8 people with his explosive made with ASA Issues and Health Risks with ASA  If you take more than 60 capsules at once can have harmful effects on your body and even death  Tinnitus (ringing in the ears) can happen if one consumes more than 10 tablets  Stomach irritation – excess HCl  ASA decreases mucous production and increase acid production whereas Prostaglandins do the opposite they increase mucous production which lines and protects the stomach o Sometimes if one takes too many aspirin the prostaglandins cannot bind and create the mucous so the pill will get stuck in the lining of your stomach wall and create a “hole” almost … an Ulcer Bufferin consumes the hydrochloric Acid – contains an anti-acid as well the pills now have a plastic coating around them so they dissolve faster – taking a big gulp of water with it too will help to neutralize the acid Reye Syndrome: people believed that giving children aspirin was causing Reye Syndrome. Reye's (Ryes) syndrome is a rare but serious condition that causes swelling in the liver and brain… association was that there was a correlation but one did not cause the other, there were other medications to give children so we though that we should just stay away from aspirin What does the Box Say?  Gel Caps VS Tablets – gel and tabs only have 5 minutes difference (15-20 vs 20-25), and tablets have a longer shelf life  Caffeine for headaches: only a small amount in them, better to just swig down a cup of coffee to get an effect (Anacin) Drugs: Generic vs Name Brands  Same stuff in same amount – just a chemical substance o 325 mg in both sets of drugs, and the big name drugs have to show that there is another cheaper option with just the same amount of the product in it o Must have equivalent bioavailability  Same amount of drug enters the body o Salt is Salt no matter what kind of drug it is o Always read the bad of the box – people mistake quality for the name of the generic drug  Extra Strength – a lot more substance in it  Anacin – contains caffeine Summary of ASA Benefit Side effect Pain yes Reduced blood yes
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