Pharmaceutics Flashcards
Why do we need to formulate cancer drugs?
Existing drugs have a low theraputic window?
Cancer drugs are dosed close to the maximum tolerated dose
biological drugs are degraded if taken orally
Why is it an issue to take Nilotinib with food?
It has a LogP of 4.4 and is therefore lipid soluble so bioavalibility is largely increased and may be to a toxic level
What are the advantages of giving chemo IV?
Accurate, rapid dosing that can be removed instantly if adverse effects are too severe.
It also avoids first pass metabolism and fed or fasting effects on drug don’t apply.
Flexibility of dosing schedule.
Disadvantage of chemo via IV
accurate dosing but increased nausea
What are the stringent requirements for IV formulations?
Sterile production, formulation stability, no preservatives and low excipients as bypassing body’s natural defence barrier
What would we have to consider when formulating a chemo drug for subcutaneous use? (i.e. IM)
Highly vascularised muscles
formulation requirements are less severe
could use implants colloids and suspensions
A high collagen content in the muscle could bind the charged drugs.
Name a topical treatment used for malignant melnoma
Tretonoin
Why would you use etoposide phosphate over etoposide?
Easier to formulate and handle in vitro cytotoxicity is less
Why should alkaline solutions be avoided with doxorubicin?
Promotes hydrolysis
