D1. Pharmaceutical Products
D2. Aspirin and Penicillin
D3. Opioids
D4. pH regulation
D5. Viruses / D6. Environmental Impact
100
Therapeutic window
What is the range of dosage over which a drug provides the desired effect without causing adverse or toxic effects?
100
Identify and name the site that deactivates the targeted enzyme in bacterium
B: Beta lactam ring
100
Why are opiates considered strong analgesics?
Kill pain by preventing the transmission of pain impulses on the brain, rather than the source
100
Which chemical transmitter that stimulates stomach acid production by binding at H2 receptors?
Histamine
100
Explain the development of resistant virus strains in the presence of antiviral drugs.
Viruses undergo rapid mutation and so the drug cannot bind to the viral protein to inhibit its function.
200
Bioavailability
What is the fraction of an administered dosage that enters the blood?
200
What are three modes that lead to bacterial resistance?
Overuse
Bacterial adaptation
Underuse
200
Why is heroine more potent than morphine?
It is able to cross the blood brain barrier more easily because it is less polar than morphine.
200
Describe a buffer solution:
Solutions that resist the change in pH of a solution upon the addition of small amounts of acid or base
200
What is one way in which antiviral medications work?
Alter the cells DNA
Blocking enzyme activity within the host cell
Changes to the cell membrane to prevent entry of a virus into the host cell
300
Therapeutic Index (TI)
What is the ratio of the dose that produces toxicity to the dose that produces a clinically effective response in a population?
300
Why is aspirin described as a mild analgesic?
Intercepts pain stimulus at the source and does not interfere with the brain.
300
How can morphine be synthesized to produce heroin (diamorphine)
Eterification
300
Differentiate between proton pump inhibitors and antacids.
PPI: Stop the pathway that releases HCl into the stomach.
Antacids: The alkali substance increases the pH of the stomach.
300
Tamiflu and Relenza are both antivirals but are administered by different methods. Relenza must be taken by inhalation, not orally. Deduce what this suggests about the bioavailability of Relenza if taken orally.
Oral bioavailability is low
Unable to be absorbed from gut.
Only a small proportion of the drug reaches the target.
400
What determines the action of a drug?
Activity is determined by the availability to bind to specific receptors due to IMF’s and bonds!
400
Draw out the synthesis of aspirin
400
What is the prescribed sequence of events that are called for in the three step analgesic ladder
Apirin --> codeine --> morphine
400
Formulate an equation that shows the action of an antacid that can neutralize three moles of Hydrogen (H+) per mole of antacid.
Al(OH)3 + 3H+ --> Al3+ + 3 H2O
Or
Al(OH)3 + 3HCl --> AlCl3 + 3 H2O
400
How can penicillins be modified to increase their effectiveness?
Modify side chains.
500
How are new drugs developed?
Target a molecule
Find a lead compound
Effectiveness is optimized by synthesizing and testing many analogues (chemically related compounds)
500
Why is aspirin used to treat patients with heart issues?
Aspirin is an anticoagulant / blood thinner. Allows blood to move through clogged arteries.
500
Why is codeine available without prescription in some countries whilst morphine is administered under strict medical supervision.
Morphine has a smaller therapeutic window and highly addictive.
500
Calculate the pH of a buffer solution of 0.0200 mol dm-3 carbonic acid H2CO3 and 0.400 mol dm-3 sodium hydrogen carbonate, NaHCO3. The pKa of carbonic acid is 6.35
pH = pKa + log ([Salt]/[Acid])
pH = 7.64500
What is the atom economy?
Synthetic methods should be designed to maximize the incorporation of all materials used in the process into the final product