Drug
Something that causes a physiological change in the body
Medicine
Something used to treat or prevent diseases
Medicine and Drugs must do one of the following…
alter incoming sensory sensations
alter a person’s mood or emotions
alter the physiological state of the body, including consciousness and coordination
Therapeutic effect
beneficial effect of a medicine
What are the 3 parenteral methods of administration?
intramuscular - into muscle
subcutaneous - directly under the skin
intravenous - bloodstream(most rapid effect)
bioavailability
fraction of administered dosage of a drug that enters the bloodstream and have an active effect
What factors affect bioavailability?
method of drug administration
polarity of drug
type of function groups in drug
True or False? Intravenous administration has a bioavailability of 100%
True
True or False? Oral doses need to be 3 times stronger than an intravenous dose
False. They must be 4 times stronger
What are the best type of molecules to be administered, in terms of solubility
One that is largely hydrophobic but still has some solubility
Which functional groups are able to form hydrogen bonds easily?
carboxyl
hydroxyl
amine
Which functional groups enhance lipid solubility(non-polar)?
Ones that lack the ability to ionize or form hydrogen bonds
phenyl group(benzene ring)
hydrocarbon chain
How is the solubility of aspirin increased?
It reacts with NaOH
True or False? Ionic salts increase solubility
True
Therapeutic window
Measure of safety of a drug. A wide window means a wide margin between toxic and safe doses
Therapeutic Index(TI) for humans
TI = TD(50)/ED(50)
TD(50) - median toxic dose
ED(50) - median effective dose
What are the main stages of drug development?
drug is synthesized
Drug is tested on animals to find lethal dose
Drug is tested on humans in a double blind experiment
Unwanted side effects and tolerance must be determined
How can you test the purity of aspirin?
Can be determined by melting points and IR spectrum
True or False? More impurities means higher a melting point
False. More impurities means a lower melting point
Analgesic
painkiller
aspirin
ibuprofen
paracetamol
morphine
codeine
dimorphine
How does aspirin block the sensation of pain?
It blocks the action of enzymes that produce prostaglandins, which are involved in the transmission of pain impulses to the brain
Anticogulant
prevents blood from clotting
What are 5 common methods of drug administration?
oral
polar, water-soluble
intravenous
unstable or poorly soluble
transdermal(skin patch or ointment)
non-polar, lipid-soluble
rectal
unstable in gastric acid
inhalation
volatile
Antibiotics
Drugs that kill or inhibit the growth of bacteria
penicillin
What is a beta-lactam ring?
A box shaped structure found in penicillin consists of three carbons and a nitrogen to make the base. One of the carbons in double bonded to an oxygen
What doe beta-lactam antibiotics do?
They interfere with cell wall formation in bacteria by inhibiting the enzymes responsible for creating cross-links in the cell wall
Antibiotic resistance
Bacteria that resists the effects of an antibiotic
What are the causes of antibiotic resistance?
overprescription of antibiotics for basic illnesses
patients don’t complete their course of antibiotics
How are antibiotics released into the environment?
antibiotics are given to healthy farm animals
Improper disposal by hospitals or companies
excreted by human urine
pharmaceutical waste
Opiates
Natural analgesics derived from opium. Bind to opioid receptors in the brain and block transmissions of pain impulses.
morphine
codine
dimorphine
What are the advantages and disadvantages of strong analgesics/opiates?
Advantages:
provide relief for pain
wide therapeutic window
improve quality of life
reduce anxiety
Disadvantages:
euphoria and lack of self-control
regular usage can lead to addiction, dependence, and withdraw
Blood-brain barrier
Tightly packed cell restricting passage of substances from bloodstream to brain that is largely composed of lipids
How is dimorphine created from morphine?
morphine + ethanoic acid →dimorphine + water
algmates
type of antacids that prevents acid from rising in the esophagus
Proton pump inhibitor
inhibits the secretion of H+ ions into gastric juice. Stomach acid inhibitor that can last up to three days.
omeprazole
H2 Receptor antagonists(H2 blockers)
stomach acid inhibitor that blocks histamine receptors in acid-producing cells in the stomach
ranitidine
Virus
submicroscopic organism that replicates inside living cells of other organisms. Consist of a protein coat and nucleic acid
Bacteria
small single cell microorganisms that are self reproducing, living, and contain various cell organelles. They are larger than viruses
Why are viruses harder to target with drugs than bacteria?
they lack a cell structure
they lack subunits that can be targeted by antivirals
they mutate quicker
they must be targeted at a genetic level
True or False? Antibiotics are effective against bacteria but ineffective against viruses
True
How do antiviral drugs work?
alter a cell’s genetic material
block enzyme activity
bind to cellular receptors targeted by viruses
prevent release of viruses
What are some examples of antiviral drugs for the common flu?
oseltamivir(oral)
zanamivir(inhalation)
Why is HIV hard to treat?
mutates rapidly
has host cells to replicate
drugs that treat HIV may harm the host cell
high price of anti-viral drugs
What are Socio-Cultural factors that affect AIDS?
condom use
ignorance and misinformation
stigmas
prostitution
What are the three levels that nuclear waste is classified into?
Low-Level waste(LLW)
produces weak radiation for a short time
Intermediate-Level Waste(ILW)
produces strong radiation for a short time
High-Level Waste(HLW)
produces strong radiation for a long time
What levels of radiation are typically found in medical settings?
Low-Level and Intermediate-Level
What are examples of low-level waste?
gowns
protective clothing
shoe covers
tissues
needles
mops
How do you dispose Low-level waste?
Store in shielded containers until the isotopes have decayed, then dispose of as non-radioactive waste
What are some examples of Intermediate-level waste?
sources for radiotherapy
Co-60
Cs-137
How do you dispose of Intermediate-level waste?
long term storage in shielding containers or concrete chambers, then buried underground
In green chemistry, what are the preferred solvents in synthesizing drugs?
water
methanol
ethanol
In green chemistry, what are the undesired solvents in synthesizing drugs?
pentane
dichloromethane
dichloroethane
True or False? Many undesirable solvents are VOC(volatile organic compounds)
True
Why are VOCs used as solvents?
They have high volatility
Chlorinated vs non-chlorinated solvent types
Chlorinated:
ozone-depleting
accumulates in ground water
forms toxins if burned
toxic, irritant, and forms greenhouse gases
Non-chlorinated:
flammable
toxic, irritant, and forms greenhouse gases
What are some of the Green Chemistry principles?
prevent waste
design less hazardous chemical synthesis
design safer chemicals and products
use safer solvents
How are some bacteria inactivating penicillin?
They produce penicillinase/enzyme that deactivates penicillin
How has the structure of penicillin been modified to overcome this resistance?
the side chain has been changed to preserve the beta-lactam ring
How do antacids neutralize stomach acid
weak base + stomach acid(HCl) →XCl + water
CaCO3 + 2HCl →CaCl2 + H2O + CO2
MgO + 2HCl → MgCl2 + H2O
What are the advantages of taking ranitidine instead of antacid?
ranitidine can treat stomach ulcers
ranitidine prevents long term damage
ranitidine lasts longer
ranitidine doesn’t cause bloating