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D1 Pharmaceutical products
Assessment statement D.1.1 List the effects of medicines and drugs on the functioning of the body.
D.1.2 Outline the stages involved in the research, development and testing of new pharmaceutical products.
D.1.3 Describe the different methods of administering drugs.
D.1.4 Discuss the terms therapeutic window, tolerance and sideeffects.
Obj Answer 1 A medicine or drug is a chemical that: Alters the physiological state (consciousness, activity level or coordination), alters incoming sensory sensation and or alters mood and emotions. Although drugs and medicines can be helpful in aiding the body against invaders, the first line of defense and the most important is the human body’s natural system of defense. The first line of defense is barriers to prevent entry. These include the skin, mucous membranes, and closures and secretions of natural openings such as lips, eyelids and ear wax. Healing can also be achieved without the use of medicines or drugs. This can be done by the power of suggestion; this is called the placebo effect. The placebo effect occurs when a patient receives therapeutic and healing effects from medicines that are pharmacologically inert, when they believe they are taking an effective drug. 2 The stages involved in the research, development and testing of new pharmaceutical products are first discovery research. Discovery research usually takes up to 3 years and involves the identification of lead compounds, synthesis of analogues ( testing many chemically related compounds) and biological testing done on animals. The next step in developing a pharmaceutical product is developmental research. This step can take up to 6 years and involves human tests and is usually split up into three phases. Phase one involves 50-100 healthy volunteers. Phase 2 involved 200-400 patients. And phase 3 involves 300+ patients in which half are given the drug and the other half a placebo. In phase 3 neither the patient nor the doctor knows which preparation is being given. Sometimes all of these steps fail to detect an adverse side effect. An example of this is the thalidomide case which involved the drug thalidomide which causes birth defects. 2 The different methods of administering drugs are: Oral, which is taken by mouth. Examples of this are tablets, capsules, pills and liquids; Inhalation which is taken by vapor breathed in or by smoking. Examples of this are medications for respiratory conditions such as asthma and some drugs such as nicotine and cocaine; Skin patches, which are absorbed from the skin into the blood. Examples of this are hormone treatments; Suppositories, which are inserted into the rectum. Examples of this are treatments of digestive illnesses; Eye or ear drops, which are delivered directly into the opening. Examples of this are treatments of infections of the eye or ear; parenteral, which are taken by injection. Examples of this are vaccines, anesthetics and dental injections. Injections may be intravenous (the drug is injected directly into the blood stream), intramuscular (the drug is injected into a muscle) or subcutaneous (the drug is injected directly under the surface of the skin). 3 The ED50 of a drug is the dose required to produce the desired effect in 50% of test animals or patients. The ratio of LD50 (lethal dose) to ED50 (therapeutic dose) is known as the therapeutic window. For example a therapeutic window of 10 indicates an LD50 : ED50 ratio of 10 to 1. This
Later on this was found to alleviate the symptoms of arthritis.1 State and explain how excess acidity in the stomach can be reduced by the use of different bases. Acute tolerance occurs within a single exposure to the drug and chronic tolerance occurs when the drug is taken repeatedly. A steady consummation of alcohol will build up tolerance. Mild analgesics act by preventing stimulation of the nerve endings at the site of pain.means that a ten-fold increase in the dose would result in a 50% death rate. stress and some anti-inflammatory drugs. Side effects are any effects other than the intended effects. Examples of these reactions are Aluminum hydroxide Al(OH)3: Al(OH)3 (s) + 3HCl(aq)AlCl3(aq) + 2H2O(l). Reye’s syndrome is a D.3.1 Describe and explain the different ways that analgesics prevent pain. Some of the advantages of using aspirin are that it has been found to be useful in preventing the recurrence of heart attacks and strokes. D2 Antacids Assessment statement D. Antacids react with the acid to produce salt and water. heartburn and ulcers. allergic reactions and Reye’s syndrome in children. There are two different timeframes of tolerance. can cause excess production of gastric juice. Another example of such reaction is Magnesium hydroxide Mg (OH)2: Mg(OH)2(s) + 2HCl(aq) MgCl2(aq) + 2H2O(l). Obj Answer 3 There are many ways that analgesics prevent pain. Antacids are often combines with alginates (which produce a neutralizing layer.2. Side effects can vary from negative to positive. This is where antacids come in. and compare the advantages and disadvantages of using aspirin and paracetamol . preventing acid in the stomach from rising into the esophagus and causing heartburn). smoking. Mild analgesics include aspirin and non-steroidal anti-inflammatory drugs such as ibuprofen. This can lead to acid indigestion. Obj Answer 3 Factors such as alcohol. Option D: Medicines and drugs D3 Analgesics Assessment statement D. Mild analgesics promote the release of prostaglandins from the site of pain and relieve inflammation and fever.3. Strong analgesics are the most effective painkillers for severe pain but come with potential problems like independence. known as the opioids work by binding to the opioid receptors in the brain which blocks the transmission of pain signals between brain cells and alters the perception of pain in the brain. Antacids work by neutralizing the hydrochloric acid and relieving the symptoms. An example of Tolerance is alcohol. 2 IN 1860 the German Chemist Hermann Kolbe synthesized salicylic acid by reacting sodium phenoxide (C6H5O-Na) and carbon dioxide. Acute tolerance and chronic tolerance. Antacids are weak bases which neutralize excess acid.2 Describe the use of derivatives of salicylic acid as mild analgesics. Tolerance is when a higher dose of a drug is required to achieve the same effect that a lower dose initially had. Some side effects of strong analgesics can be drowsiness and possible change in behavior and mood. Strong analgesics such as the drugs related to morphine. Some of the disadvantages of using aspirin include the development of ulcers and stomach bleeding.
This test is not very accurate and most likely leads to more . suicide rates and all cancers. D. Morphine is obtained from raw opium ( 10%). D. alcohol and tertiary amine. In extreme cases paracetamol can cause blood disorders and kidney damage. 3 There are many different techniques used for the detection of ethanol in the breath. The modification of morphine that results in the semisynthetic drug diamorphine is the added ester-ethanoate. the blood and urine. D. Obj Answer 2 The effects of depressants depend on the dosage. A longterm effect of alcohol is that large quantities can lead to brain damage due to the alcohols dehydrating properties. A road side breathalyzer contains crystals of potassium dichromate which are orange. This is cause by the sharing of unsterilized needles. At moderate doses the depressant can induce sedation (soothing. It also relieves stress and discomfort by creating a detachment from pain. alkene. Overdose on paracetamol can lead to serious liver damage.1 Describe the effects of depressants. Some long-term effects causes by ethanol abuse include: alcoholism. ether. The extent of this change can then be measured by a photocell and this can be used to determine the ethanol concentration. D4 Depressants Assessment statement D. The structure of diamorphine consists of a benzene ring.4.3 Compare the structures 3 of morphine. These effects last only for about a week. high blood pressure. especially stomach cancers. At extremely high doses it may cause death. warm and contented. alcohol.3. codeine and diamorphine (heroin. Some short-term effects of ethanol abuse include: Loss of self-restraint. the blood and urine. The structure of codeine consists of a benzene ring. fetal alcohol syndrome and permanent brain damage. reduction of anxiety). cirrhosis of the liver. One of the disadvantages is that users quickly become physically dependent and tolerant to the drug. ester-ethanoate and tertiary amine.4 Discuss the advantages and disadvantages of using morphine and its derivatives as strong analgesics. ether. violent behavior which can cause family brake down.3. 3 The effects of alcohol on society are considerable.(acetaminophen). dangerous risk taking.4. loss of balance and judgment. There is a strong correlation between heavy drinking and diseases like: strokes.3 Describe and explain the techniques used for the detection of ethanol in the breath. dehydration and at high doses vomiting. liver disease. a semi-synthetic opiate). At higher doses the depressant may induce unconsciousness (sleep). The advantages of paracetamol are that paracetamol is very safe especially in children. Long term effects can be the spread of diseases such as tetanus AIDS and Hepatitis. and tertiary amine. At low doses a depressant may show little to no effect. One of the simpler techniques used for the detection of ethanol is a roadside breathalyzer. 3 potentially fatal liver and brain disorder. these crystals are changes to green chromium (lll) in the presence of ethanol as they oxidize the ethanol into ethanol. Heroin is also one of the best painkillers. The structure of morphine consists of a benzene ring. This means that larger does must be taken to achieve the same state of euphoria. alkene. alkene. Withdrawal from high doses of heroin produces a variety of short term effects like symptoms similar to the flu. Dependency of the drug can lead to financial problems which can lead to crime.2 Discuss the social and physiological effects of the use and abuse of ethanol. ether. brain damage and death.4. coronary heart disease. In pregnant woman alcohol can lead to the baby being born with fetal alcohol syndrome where the baby is born underweight with brain damage. Heroin causes the user to feel drowsy. The use and abuse of ethanol can also cause changes in behavior. D.
With depressants ethanol can cause heavy sedations and even lead to comas. 3 Short-term effects of nicotine consumption include: Increased concentration. chocolate and colas. increases risk of heart disease. Nicotine is a habit forming drug which quickly leads to dependence or addiction. increase air flow. Option D: Medicines and drugs D5 Stimulants Assessment statement D.5 Identify other commonly used depressants and describe their structures. increased heart disease risk. decrease in urine output.1 List the physiological effects of stimulants. Another technique that is used for the detection in ethanol is what is called gas-liquid chromatography. Caffeine is a D. helps counter fatigue. D. One of the risks associated with smoking tobacco is the risk of lung cancer due to the chemicals released when a cigarette is burned.4. coronary thrombosis. Long term side effects such as that of nicotine can cause high blood pressure. Obj Answer 1 The physiological effects of stimulants are: increase heart rate and blood pressure.5. increased levels of fatty acids in the blood which can lead to stroke and increased risk of peptic ulcers. increased level of fatty acids which can cause stroke and increased risk of peptic ulcers. This works by injecting vaporized blood or urine into a stream of inter gas and then measuring the retention time.5. 2 accurate tests. ethanol can cause increase risk of bleeding in the stomach and stomach ulcers.4.5. Caffeine reduces physical fatigue and restores mental alertness.and long-term effects of nicotine consumption. increased heart rate and blood pressure. tea. as a result ethanol has a distinct band. ethanol can increase the chances for cancer especially in the liver and intestines. Other commonly used depressants include diazepam marketed as Valium®. Some examples of how ethanol increases the effects of other drugs are: With aspirin.D.4 Describe the effects of caffeine and compare its .4 Describe the synergistic effects of ethanol with other drugs. D. These molecules have high lipid solubility and can cross the brain-blood barrier easily. The size of the peak can then show the ethanol concentration present when compared to the air stream. 3 Caffeine is present in many substances like coffee. relieves tension and boredom. With tobacco.2 Compare amphetamines and epinephrine (adrenaline). this technique has to be carried out in a laboratory. nitrazepam marketed as Mogadon® and fluoxetine hydrochloride marketed as Prozac®. With other drugs alcohol can cause effects that the drug is not meant to do. Ethanol has the potential to increase the activity of other drugs when taken at the same time. This effect is known as synergy. Both diazepam and nitrazepam contain both benzene rings and the diazepine structure. A different version of an intoximeter uses a fuel cell. increase blood flow. increase mental awareness. coronary thrombosis. Amphetamines mimic the effects of adrenaline. which are a seven-membered heterocyclic ring containing carbon and two nitrogen atoms. 2 D. An intoximeter works behind the idea that different molecules cause different absorption bands in the infrared part of the spectrum.3 Discuss the short. 3 Amphetamines and adrenaline are chemically similar they are both derived from the phenylethylamine structure.5. Another more accurate technique used for the detection of ethanol is the use of infrared spectroscopy in an apparatus called an intoximeter. Some long term effects of nicotine include: high blood pressure.
1 State how viruses differ from bacteria.6. D6 Antibacterials Assessment statement D.structure with that of nicotine. Obj Answer 1 Viruses differ from bacteria because they are such small and simple structures.6. irritability and insomnia. When consumed in small amounts caffeine enhances mental energy but when consumed in large amounts caffeine can cause anxiety. Changing the side-chain results in penicillins that are more resistant to the penicillinase enzyme which is created by bacteria that have developed bacterial resistance.3 Discuss the difficulties associated with solving the AIDS problem. which are the cells that should be defending the body from the disease itself. respiratory stimulant. 3 Penicillins work by interfering with the chemicals that bacteria need to form normal cell walls. . The effect of penicillin over prescription is that the bacteria develop resistance to penicillin.7. The first way they work is by altering the cell’s genetic material so that the virus cannot use it to multiply.2 Describe the different ways in which antiviral drugs work.1 Outline the historical development of penicillins. Bacteria have a more complex cellular structure and have the ability to survive and reproduce independently from other living cells. Obj Answer 2 Penicillins were first discovered in 1928 by Alexander Fleming who noticed that a fungus known as penicillium notatum had contaminated some of his cultures.3 Discuss and explain the importance of patient compliance and the effect of penicillin overprescription. In addition. 3 Patient compliance insures that the drug is effective in what it’s treating. Later work was done by Australian bacteriologist Howard Florey and Germany born biochemist Ernst Chain to successfully isolate penicillin. D. 2 There are two ways that an antiviral drug works. Another difficulty associated with solving the AIDS problem is that the virus tends to mutate a lot. The second way they work is that they may prevent the viruses from multiplying by blocking enzyme activity within the host cell. Penicillins inhibit the development of cross-links in bacterial walls therefore weakening the wall. Patient compliance also lowers the drug exposure to the bacteria which lowers the chances for the bacteria to develop resistance to the drug. have no cellular structure and are only capable of reproducing inside another living cell. D.7. Fleming then noticed that where the penicillium notatum had contaminated there were no cultures. The virus also lays dormant which means that the immune system has nothing to respond to. 3 Some of the difficulties associated with solving the AIDS problem and developing a cure is that the virus destroys T helper cells.7. Both the structure of nicotine and caffeine contain heterocyclic rings and a tertiary amine group. they contain two components. D. All of these factors coupled with the high cost of antiretroviral agents and sociocultural issues make the Aids problem a tough problem to solve. Option D: Medicines and drugs D7 Antivirals Assessment statement D.2 Explain how penicillins work and discuss the effects of modifying the side-chain.6. caffeine contains two amide groups. D. The use of penicillin in animal feedstock also contributes to the resistance problem.
3 The increased potency of diamorphine is due to a polar alcohol group (-OH) has been converted to a less polar ethanoyl group. pharmacological and physical properties was obtained to make paclitaxel and docetaxel. 3 Combinatorial chemistry is the process by which a large number of new chemical structures are synthesized on a small scale using solid phase D.1 Describe the importance of geometrical isomerism in drug action. An example of a drug with two possible enantiomers is thalidomide.D8 Drug Action Assessment statement D. For example the cis isomer of [Pt(NH3)2Cl2] is used medically as an anti-cancer drug known as Cisplatin. This group conversion results in an increased potency. D. The ring opens up so that the penicillin becomes bonded to the enzyme thus blocking the synthesis of bacterial cell walls and inhibiting the enzyme from catalyzing any further reactions.1 Discuss the use of a compound library in drug design.2 Discuss the importance of chirality in drug action D.2 Explain the use of combinatorial and . This is when ammonia molecules are adjacent to one another. This also makes it easier to transport into the non-polar part of the central nervous system. These receptors are usually only capable of binding with the enantiomer that has a complementary structure. D.4 Explain the increased potency of diamorphine (heroin) compared to morphine D9 Drug Design Assessment statement D. But the trans isomer does not show any anti-cancer properties 3 Enantiomers that act as a drug have different biological properties because they bind with receptor molecules. Obj Answer 2 There are two different ways in arranging four ligands. The other way of arranging is ‘trans’ arrangement. they can now work from a library of analogues.8. One enantiomer relieves morning sickness while the other causes deformities in the limbs of the fetus. Here the analogues will share common structural features but will have one or more different functional groups. This is when two ammonia molecules are opposite from one another. 3 The importance of the betalactam ring action of penicillin is that this four membered ring is what is responsible for the antibacterial activity of penicillin. The chemical analogues constitute a compound library. This approach is time consuming and costly.8. Obj Answer 3 In traditional drug design collection of related compounds are synthesized one at a time and evaluated. This is better than the traditional method because now the makers of the drug don’t have to go out there and find new analogues.3 Explain the importance of the betalactam ring action of penicillin.9. Two different isomer arrangements can have different pharmacological effects.8.8.9. The first way is the ‘cis’ arrangement. These types of arrangements can occur in inorganic complexes. For example various chemical analogues were retested until a suitable molecule with the best chemical.
Changing the polarity of the drug can improve its medical properties. An example of this is the synthesis of Taxol. LSD users may also experience depression.10. The difference is the various functional groups attached to the indole skeleton which affects their solubility in fats and increase their potency.9. It works by attaching itself to the non-chiral molecule and forces the reaction to follow a pre-determined path. tremors and sleeplessness.4 Discuss how the polarity 3 of a molecule can be modified to increase its aqueous solubility and how this facilitates its distribution around the body. 3 LSD. Once the aspirin reaches the acidic environment in the stomach it changes back to the un-ionized form. The effects of mescaline are the same as LSD but mescaline is considerably less potent. increase in heart rate and blood pressure. sweating.9.3 Describe how computers 2 are used in drug design. The physical effects are dilated pupils.parallel chemistry to synthesize new drugs. . An example of this is soluble aspirin which is the calcium or sodium salt of aspirin. Like arthritis. Parallel chemistry is used to synthesized smaller number of new chemical analogues but turns out more focused libraries. Once the molecule has been formed the auxiliary can be taken off. D. Computers aide in drug design by creating three-dimensional models which can be used for the virtual development and evaluation of the drug. mescaline and psilocybin all contain the common structural feature that is an indole ring structure. Although mescaline does not have an indole ring it has a very similar structure. cancer and HIV. D. A large dosage of LSD produces hallucinations. this avoids the need to separate enantiomers from a mixture. psilocybin and tetrahydrocannabinol (THC). 3 One of the arguments for legalization of cannabis includes the ability of cannabis to relive and help patients with certain diseases. Obj Answer 2 The effects of LSD depend on the dosage.10. mescaline and psilocybin. This is known as de novo drug design. D. Psilocybin and tetrahydrocannabinol have similar effects as LSD including hallucinations but are less potent. D10 Mind-Altering Drugs Assessment statement D. chemistry.9.1 Describe the effects of lysergic acid diethylamide (LSD). Combinatorial chemistry screens for biological activity.10. mescaline.5 Describe the use of 2 chiral auxiliaries to form the desired enantiomer. Computers can also show if the drug is stable or not by performing energy minimization. For example a drug that contains a carboxylic acid functional group can be made more polar by converting them to a salt. D. mood of user and where it is being taken. Computers also offer the hope to developing drugs that will better attack the target sight. Non polar groups like (-CH3) enhance this effect. personality. D. increased body temperature. The solubility of a drug in a polar and non-polar environment determines its abortion. A chiral auxiliaries is used to convert a non-chiral molecule into the desired enantiomer. distribution and excretion. Many hallucinogens are indole-amines and contain the indole ring.3 Discuss the arguments for and against the legalization of cannabis.2 Discuss the structural similarities and differences between LSD. One of the arguments against legalization includes the possible harmful effects and the fear of cannabis users to start using harder drugs.
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