medicinal chemistry
No description yet. This curated deck is ready for daily study.
Card preview (24)
the four types of administration routes are… 1. oral 2. ??? 3. rectal 4. topical
parental
capsules, suspensions, solutions and tablets are all ______ administrated
orally
what are two rectal dosage forms?
suppositories, creams
what are three types of injections
• intravenous • subcutaneous • muscular
why are there different administrative routes? (2 short)
• increase bioavailability of drug • prevents degradation by acidic pH in the stomach environment • incr patient compliance
what is bioavailability?
fraction of of administered dosage that enters the blood stream
which type of administration has 100% bioavailability?
parental
what is pharmocokinetics? (short recap)
what the body does to the drug after it enters the body
the four processes of pharmokinetics are…
• absorption • distribution • metabolism • elimination (All Dogs Make Eggs)
what is one way absorption is negatively affected?
poor solubility in water -> poor uptake
distribution is affected by the _______ity and _____ity of drugs
hydrophilicity, lipophilicity
what affects the hydrophilicity and lipophilicity of drugs?
the functional groups present on compounds
what type of drug administration is usually affected by metabolism?
oral
drugs that become metabolites undergo ______________
first pass metabolism
how does metabolism affect bioavailability? (3)
• drugs experience ‘first-pass metabolism’ by the liver • cannot exert therapeutic affects • this significantly affects F
what is the therapeutic window? (short def.)
the range of acceptable dosage strengths where the drug will exert its therapeutic effect without causing toxic effects
what is the formula for therapeutic index for animals
LD50/ED50
what is the formula for therapeutic index for humans
TD50/ED50
is a high therapeutic index good? why?
• yes • greater safety margin btw effective and toxic/lethal dose • when taken in higher doses than required for it to exert therapeutic effect, the drug will still be safe
how does aspirin work as a mild analgesic?
it binds to COX 2 enzyme and prevents it from releasing prostaglandin
aspirin prevents pain detection at the source by
preventing nerve messages from being sent to the brain
aspirin reduces swelling by
• preventing dilation of blood vessels • decr swelling • reduces inflammatory response
what does prostaglandin do? (2)
• send nerve messages to brain -> pain detection at source • causes inflammatory response -> dilation of blood vessels -> swelling -> incr pain
what reagents and conditions are required for the synthesis of aspirin?
• reagents: salicylic acid, ethanoic anhydride • cond: catalyst H2SO4, warm e mixture