SL Chemistry Notes Medicines and Drugs Option

Taken and typed by Emily N.

INTRODUCTORY NOTES
Pharmacology: the study of the interactions of drugs with cells in the body A drug (or medicine) is any chemical, man-made or natural, which may do one of the following: - alters moods or emotions (directly/indirectly) - alters incoming sensory sensations - alters psychological state (consciousness, coordination, activity level) If a disease is treated by using chemicals, it is called chemotherapy Three groups of drugs: antibiotics/antivirals, hormones and vitamins, and analgesics/anesthetics/stimulants/depressants

RESEARCH/DEVELOPMENT OF NEW DRUGS

It takes about 10-12 years to get a drug to market at a cost of over $225 million (US) Most drugs dont make it through the development and testing phases Drugs must first be tested on various animal species, including its LD50, and if found safe, it may go on to clinical trials where volunteers are used to establish safe doses, and placebos are often used The drug then goes to clinical evaluation using statistical analysis to eliminate variables and if all goes well, the drug goes on to full human studies (with continuing evaluation). Testing is not always foolproof; sometimes it takes years for side effects to be known - Examples: Vioxx (increased risks of heart attacks/stroke), Thalidomide (birth defects), DES (increased cancer risk) LD50: the lethal dose required to kill 50% of the population (population = number of subjects taking the drug) Many household products have LD50 values (soap, etc.) LD50 values are used in conjunction with ED50 values (ED50 values are the effective doses for 50% of the population) to determine the therapeutic window for a drug (margin of safety).

DANGERS OF DRUGS
Tolerance of the drug must also be determined. Tolerance is when a patient needs increasing amounts of the drug to get the same physiological effect. The danger is that as the dose increases, so do the risks of dependence and reaching the level of a lethal dose. Other issues are dependence and side effects Dependence is when a person feels they cannot function normally without a drug Physical dependence occurs when a body can only function while using the drug and without the drug experiences withdrawal

Psychological dependence is when a person cannot stop using a drug or stop thinking about the drug Side effects are unwanted effects in addition to the main effects To achieve the main effect the side effects must be able to be tolerated. One example is aspirin: its main effect is a pain killer/fever reducer but its side effects are stomach bleeding and allergies. The seriousness of the side effects will determine the risk-to-benefit ratio. If an effective treatment is found for a life-threatening disease, a high risk from side effects is more acceptable than for a non-life-threatening disease.

ADMINISTERING DRUGS
4 ways to administer drugs Way 1: Injection (parenteral) - Subcutaneously (beneath skin) administered, usually localized effect. Example: dental injections - Intra-muscular (for larger volumes when immediate response is not needed). Example: vaccinations - Intravenous (directly into veins), most practical, instantaneous effect Way 2: Oral - Convenient, but slowly absorbed, might be affected by stomach acid, tablet versus liquid state, food or no food, etc. Way 3: Rectal - Good for avoiding the stomach (usually given as a suppository), absorbed slowly. Example: hemorrhoids Way 4: Inhalation - Systematic effect (whole body), rapidly absorbed by blood supply in the lungs. Example: inhalers, asthma medication

ANALGESICS
Prostaglandins are made by COX-2 molecules, and analgesics block COX-2 molecules from making prostaglandins, and also block COX-1 molecules from protecting the stomach lining (hence bleeding risks in aspirin) Mild analgesics block prostaglandins, which receive/transmit pain signals to the brain Strong analgesics attach to receptors called opoid receptors found in the brain, spinal cord, and gastrointestinal tract. When they bind to the receptors, they block the pain signal being sent

Weak Analgesics Examples: aspirin (acetylsalicylic acid), acetaminophen (paracetamol) Aspirin - Aspirin is taken to reduce substances that cause mild to moderate pain, inflammation, and fever by inhibiting the production of prostaglandins at the site of the pain.

- Advantages of aspirin: it is a good anti-inflammatory, eases arthritis/rheumatism, prevents/treats heart attacks, strokes and angina because it prevents blood clots, and may prevent prostate cancer. - Disadvantages of aspirin: can cause bleeding in the stomach lining where consistent usage can cause ulcers, can worsen asthma, can cause kidney damage in high doses, and can cause Reyes syndrome (a deadly liver disorder) in children under age 12.

Structure of aspirin

Acetaminophen - Acetaminophen blocks the messages signaling pain in the brain rather than at the source of the pain. - It has a similar structure to aspirin - It is mainly metabolized in the liver, but is safe at the right dose - Advantages of acetaminophen: safe for mild pain, does not irritate the stomach, very safe at the correct dose, and preferable for young children because of fewer side effects. - Disadvantages of acetaminophen: not an anti-inflammatory, can cause kidney/liver problems in rare cases, and can cause brain/liver damage in very high doses.

Structure of Acetaminophen

Strong Analgesics Examples: Morphine, codeine, heroin Also known as narcotics or opiates

Morphine and codeine are alkaloids (contains nitrogen) derived from opium, and heroin is synthesized from morphine (is semi-synthetic) All affect the central nervous system, relieving pain, and are also good for treating chronic diarrhea and severe coughing Heroin is the most potent, and codeine is the least potent Strong analgesics are very likely to be tolerated and cause dependency Short-term effects of strong analgesics: relief from pain, reduced tension, reduced coughing, and overdosing Long-term effects of strong analgesics: loss of appetite, constipation, risk of infection from shared needles, crime, loss of job

Structure of heroin

Structure of Morphine

Structure of Codeine

STIMULANTS
Stimulate the brain and central nervous system by increasing a state of mental alertness and wakefulness and can sometimes decrease appetite Sometimes they are used to treat mild depression since a temporary elevation of mood is produced. Examples: amphetamines, nicotine, caffeine Amphetamines - The hormone adrenaline (epinephrine) is a natural stimulant produced by the endocrine gland. It raises heart rate, blood levels, and glucose levels, and is responsible for the fight or flight reaction. - Amphetamines have structures very similar to adrenaline, both containing the phenylethylamine structure - They are sympathomimetic drugs (their effects are similar to the stimulated sympathetic nerves, which means to mimic the effects of adrenaline). - Amphetamines are strong stimulants that affect the central nervous system and brain. - Examples: methamphetamine, ecstasy Nicotine - Nicotine is a mild alkaloid stimulant commonly found in tobacco. - Short-term effects include increased heart rate and blood pressure which puts stress on the heart

- Long-term effects include heart disease and coronary thrombosis (blood clots), lung cancer, emphysema, bronchitis, excess stomach acid which causes ulcers, and yellow-stained fingernails and teeth. - Nicotine causes psychological dependence and tolerance

Caffeine - Caffeine is another alkaloid that works within the central nervous system by working inside nerve cells to increase cellular metabolism, so energy becomes more available. - Caffeine increases alertness, energy, and motivation, and in large amounts, can cause sleeplessness. It is also a diuretic because it stimulates the kidneys. - Tolerance can develop and can lead to psychological addiction.

Methamphetamine Adrenaline

Nicotine

Caffeine

DEPRESSANTS
Depressants include tranquilizers, sedatives, barbiturates, and hypnotics. Depressants calm and relax the central nervous system by interfering with nerve impulse transmission. Examples include Valium (diazepam), Mogadon (nitrazepam), alcohol, and Prozac (fluoexetine hydrochloride) Depressants affect behavior based on dosage, so any depressant can act as a sedative and sometimes can cause coma/death. Tranquilizers (Valium, alcohol) reduce nervous tensions and anxieties, and create a feeling of non-inhibition but do not induce sleep Sedatives are similar to tranquilizers but are stronger, and hypnotics produce sleep.

Long-term effects of alcohol abuse: health complications (cirrhosis, liver cancer, coronary heart disease, high blood pressure, strokes, gastritis, peptic ulcers), physical dependence, tolerance, anxiety, depression, and poor eating habits. Alcohol abuse in pregnant women can cause birth defects and fetal alcohol syndrome.

Basic Effects of Alcohol Blood Alcohol Concentration (BAC) mg/100 mL of blood 10-30

Symptoms Near normal behavior Euphoria, sociability, talkativeness, feelings of relaxation, increased self-confidence, decreased inhibitions, impairment of attention/judgment/control, some loss of sensory-motor efficiency and fine motor skills. Small blood vessels in the skin are dilated causing feelings of warmth, loss of critical judgment, impairment of perception, memory, and comprehension, increased reaction time, drowsiness. Violent/aggressive behavior, increased pain threshold, slurred speech, dizziness, double vision, loss of balance, nausea, vomiting. Loss of motor functions, general inertia, inability to stand or walk, asleep or in a stupor, impaired consciousness Coma, unconsciousness Death from respiratory arrest

30-90

90-200

200-300

300-400 400-450 >450

SYNERGY
Synergy enhances the effects many times over with often devastating results. With tranquilizers, sedatives, and other drugs that affect the central nervous system, coma/death is more likely. With aspirin, there is an increased risk of stomach bleeding due to severe irritation of the stomach lining, and bleeding ulcers can result, causing death. Some drugs are inhibited in their breakdown, so they remain in the body longer with increased effects.

VIRUSES VERSUS BACTERIA

A virus is very small; the largest viruses are only as big as the smallest bacteria. Bacteria are complex compared to viruses. A typical bacterium as a cell wall and membrane surrounding the cytoplasm. Viruses only have a protein viral coat (capsid

coat), a core of genetic material (DNA or RNA), and sometimes an outermost layer called an envelope. The envelopes may be studded by spikes made of carbohydrates and proteins that help the virus particles attach to host cells. Bacteria contain the genetic blueprint and all the tools needed to reproduce themselves. Viruses have to invade the cells of living hosts and hijack their cellular machinery to reproduce. Most viruses land on the surface of a cell and inject its genetic material into the host cell. By taking over the host cells genetic machinery, the viral genes tell the host cell to begin making new virus parts. Eventually so many new viruses are made that the cell bursts open and dies, releasing new viruses to infect more cells.

PENICILLIN
History Discoverer: Alexander Fleming, 1928 Fleming was a bacteriologist who was working with cultures of staphylococcus aureus, which causes boils and other infections. He accidentally left an open Petri dish containing one of the cultures in the lab while he was on vacation. When he returned, a type of mold called penicillium notatum had developed and had inhibited the growth of the bacteria. Fleming inferred that the mold produced a compound called penicillin which inhibited the bacterias growth. Development: Howard Florey, Ernest Chain There were many problems in isolating/purifying penicillin. Florey and Chain managed to overcome the problems and developed a powdered form of penicillin. In 1941 they used penicillin to treat a policeman dying of septicemia (blood poisoning). They noticed significant improvement in his condition, but they ran out of penicillin before he could be cured, and the policeman relapsed and died. In 1945 they performed the required trials and production was scaled up and available to treat Allied soldiers wounded on D-Day. Fleming, Florey, and Chain were awarded the Nobel Peace Prize for medicine in 1945 Penicillin G was the first widely-used penicillin but it was deactivated by stomach acid, so it was required to be injected. Modifications were made to the R-Group (side chain) keeping the main structure intact. As bacteria became resistant to penicillin (by synthesizing an enzyme called penicillinase), the side chain had to be modified. As soon as penicillin/antibiotics became readily available, doctors began prescribing them to treat minor illnesses like strep throat. This caused it to be over prescribed and certain bacteria resistant to antibiotics were able to multiply/survive. Bacteria can become resistant due to mutations or natural selection so it is important to take the entire prescription prescribed (to make sure all of the bacteria are killed). Antibiotics, if used repeatedly, may kill harmless or even beneficial bacteria. Antibiotics are sometimes given to animal feed to prevent disease and help the animals grow faster, but often bacteria become resistant to the antibacterial and are passed on to humans. Therefore, it is important to thoroughly cook foods such as meat.

How Penicillin Works Bacteria have cell wall layers that are supported by 3-D cross-linking, linking each layer to another layer. Penicillin (and most other antibiotics) works by interfering with the cell wall production of bacteria. It weakens the cell as the bacteria attempts to grow, and eventually the cell bursts open and the bacteria die. Most penicillins are a narrow-spectrum antibiotic. Ampicillin is an example of a broadspectrum antibiotic. Narrow-spectrum should be used if possible.

ANTIVIRALS
Antivirals work in one of the following ways: They alter the host cells genetic material so that the virus cannot use it to multiply. They prevent the virus from multiplying by blocking enzyme activity within the host cell. The binding site is altered to prevent attaching. The cell membrane is altered to prevent viruses from entering or leaving the cell. Examples of antivirals: - Acyclovir: applied topically to cold sores caused by herpes. The viral enzymes use it for viral DNA. It prevents successful multiplication. - Tamiflu: inhibits the active site which all flu viruses use to exit a cell, thus preventing new viruses from leaving the cell. - AZT: blocks reverse transcriptase (an enzyme needed to replicate DNA) to prevent the replication of HIV The development of antivirals is difficult because viruses are constantly mutating.

DETECTING ALCOHOL IN THE BREATH, BLOOD, OR URINE

Three techniques: breathalyzer, gas liquid chromatography (GLC), infra-red spectroscopy (intoximeter)

BREATHALYZERS
Breathalyzers use a redox reaction using acidified potassium dichromate (K2Cr2O7) The dichromate oxidizes alcohol in the breath into ethanoic acid. There is an orange to green color change. The redox reaction produced a voltage that is converted into a BAC The BAC is a measure of the grams of ethanol per 100 mL of blood, often listed as a percentage. Breathalyzers are not very accurate and are not admissible in a court of law (USA).

GAS LIQUID CHROMATOGRAPHY (GLC)

Small samples of gas or liquid are injected into a column filled with a stationary phase and a mobile phase.

The sample (breath or urine) separates into its components based on differences in intermolecular forces with the two phases. The components move through the column at different rates and are detected by a recorder. A standard ethanol sample will be run through the GLC so that a comparison can be made to identify the alcohol and the amount present in the sample.

INFRA-RED SPECTROSCOPY/INTOXIMETER
An infra-red spectroscope uses infra-red energy to identify the various functional groups often present in organic compounds. Each bond (OH, CH, C==O, etc.) absorbs and transmits a specific amount of energy which is unique to that bond (called a signal or a stretch). The intoximeter is used to confirm the presence of CH and OH bonds in the breath. The intensity of the signal signifies the BAC.

Note: These notes were taken in a class that was preparing for the SL Chemistry exam. For those not taking the SL exam, this class was the first year for the HL exam. I am one of those students who was in the SL class but did not take the SL exam because I am planning to take the HL exam. Nevertheless I still had to take these notes and found them quite interesting! So for everyone who is studying medicines and drugs as an option for the SL Paper 3, good luck and I hope you use my notes! I dont know if these notes are applicable for HL Chemistry. Enjoy!