Option D - Medicinal Chemistry Flashcards
(149 cards)
List the possible ways of administration of drugs and examples of medicines for each.
- oral - mouth - tablets
- inhalation - breathed in - asthma medications (bronchodilators).
- skin patches - absorbed from skin into the blood - hormone treatments.
- suppositories - inserted into the rectum - digestive illnesses treatments
- eye/ear drops - come on - eye/ear infections (who would’ve expected).
List the types of injections with the corresponding level of tissue the substance is injected into.
- intramuscular - muscle (wow)
- subcutaneous - subcutaneous tissue
- intravenous - veins
- intradermal - epidermis
Define bioavailability of a drug and state its significance.
Amount of a drug that reaches the bloodstream.
(higher in intravenous)
Important to consider in choosing dosage.
Define the first-pass effect.
Initial metabolism/alteration of a (orally ingested usually) drug that occurs in the liver after it is absorbed from the gastrointestinal tract and before it enters the systemic circulation.
(reduction in the amount of active drug entering the bloodstream)
State the advantages for drug solubility of both water and lipid solubility.
- water solubility: crucial for circulation in the aqueous solution in the blood.
- lipid solubility: helps in the passage of drug through membrane.
Define and thus distinguish tolerance and addiction.
Tolerance - a person given a repeated dose of a drug responds with a reduced response to the drug of the same dose.
Addiction - occurs when a patient requires a drug to feel normal and suffers from withdrawal symptoms if the drug is not taken.
Define the therapeutic index (TI) of a drug and list its formula.
Ratio comparing the dose of a drug required to produce a therapeutic response (ED50) to the dose that causes toxicity (TD50)
TI = TD50 / ED50
State the correlation between the TI of a drug and its safety.
Higher TI -> safer drug.
Define the ED50.
Effective dose 50%
Dose of a drug required to produce a therapeutic effect in 50% of the population/experimental subjects.
Define LD50.
Lethal dose 50%
Dose of a drug lethal/ causing death in 50% of the population/experimental subjects.
Define TD50.
Toxic dose 50%
Dose of a drug required to produce a toxic effect in 50% of the population/experimental subjects.
Distinguish the TI testing in animals vs in human subjects.
TI (animals) = LD50/ED50
TI (humans) =TD50/ED50
List the stages of drug development.
- Identify target molecule within the body.
- Find lead compound with desired pharmaceutical activity.
- Optimize the lead compound by synthesizing and testing chemically related analogues.
- Combinatorial chemistry to produce and test candidate medicines.
- Laboratory testing
- Animal testing
- Determine TI
- Human trials (three phases)
- Evaluate drug effectiveness based on real medication vs placebo in phase III.
- Post-marketing surveillance programs.
- Adverse reaction monitoring.
Define the prostaglandins.
Chemical stimulating the pain receptors, released from damaged cells, which mediate the inflammatory response.
State the principle of functioning of prostaglandins.
Causing blood vessel dilatation near the injury site, leading to swelling and increased pain
impact body temperature regulation potentially causing fever.
Define the major principle of painkiller action mechanism.
Interception or blockage of the pathway between the source of pain and the receptors in the brain, disrupting the transmission of pain signals.
State the category of drugs aspirin belongs.
non-steroidal anti-inflammatory drugs (NSAIDs)
mild analgesics
State the bulk of aspirin mechanism of action.
Prevention of the stimulation of the nerve endings at the site of pain and inhibition of the release of prostaglandins from the site of injury.
Gives relief to inflammation and fever as well as pain.
State why mild analgesics are known as non-narcotics.
Because they do not interfere with the functioning of the brain
(as strong analgesics do).
State the historical predecessor of aspirin and the active ingredient in it.
chewing willow bark
active: salicin
State the current active ingredient in aspirin and what changed.
Ester derivative of salicylic acid
(by Bayer).
Changed alcohol group into an ether which made it more palatable and less irritating substance.
State the name of the property of a drug reducing fever.
Antipyretic
State the process of synthesis of aspirin.
Salicylic acid (2-hydroxybenzoic acid) esterificated in a condensation reaction with usually ethanoic anhydride to form aspirin.
State the current use of aspirin.
anticoagulant - heart
attacks/strokes
antipyretic - mild analgesic