Introduction Flashcards
What are opiates used for?
Pain relief
What does repeated use of opioids lead to?
Addiction
What is a)Morphine b)Heroin?
a) The active ingredient in opioids
b) Stronger version of morphine synthesised in the lab
How many types of opioid receptors are there?
3
What opioid receptor has very high affinity for morphine?
Mu receptors
What are 2 endogenous opioids?
Endorphins and Enkephalins
What is a drug?
A chemical of known structure which when administrated to a living organism produces a biological effect
What are 3 examples of types of drugs?
1) Synthetic chemicals
2) Plant chemicals
3)Biopharmaceuticals (made from DNA like proteins or just oligonucleotides)
What is a medicine?
A chemical preparation including a drug or many administrated to produce a therapeutic effect
What compounds do medicines often contain as well as drugs?
Excipients, stabilizers, solvents.
What are 2 examples of biopharmaceuticals?
1) Proteins
>Copies of endogenous proteins
>Engineered proteins
>Antibodies
2)Oligonucleotides
>Injected mRNA to lead to production of antibodies.
What is gene therapy?
Addition of genetic material to cells to prevent or alleviate or cure disease.
What is regenerative medicine?
Engineered stem cells to replace irreparably damaged organs.
What are the 2 types stages of development of biologics?
1) 1st generation
>Copies of endogenous proteins produced by recombinant DNA technology.
2) 2nd generation
>Engineered proteins to improve the performance.
What is the most important step in engineering monoclonal antibodies?
Humanization
What does it mean if a drug name ends with “mab”?
It contains monoclonal antibodies.
What 4 proteins do drugs interact with?
Receptors, enzymes, transporters, ion channels.
Why do drugs have side effects?
As no drug is completely specific, increasing the dose will effect other targets.
What are 3 types of drugs acting through receptors and their effects and an example?
1)Agonists
>When bound to receptor causes receptor to switch on as it would if a natural ligand bound to it, brings about change in the cell.
2)Inverse agonists
>When bound to receptor it reduces signalling by the receptor.
3)Antagonists
>Block receptor so no effect occurs, would block effect of agonists and inverse agonists.
>Morphine and Humira
What are the two classes of dugs targeting channels and their effect and an example?
1)Blockers
>Enter pore and prevent ion flow through
>E.g. Lidocaine
2)Modulators
>Don’t block the channel, modify how the channel behaves, either open it more or open it less.
>E.g. Valium
What are the 3 drug types effecting enzymes and how?
1) Inhibitor
>Binds to enzyme and stops it’s function
>E>g. aspirin
2)False substrate
>Molecules enter enzyme and is catalysed into something inactive
3)Prodrug
>Enters enzyme and active drug is produced.
What are 2 drugs which target transporters and how and examples?
1) Inhibitors
>Block transporters from working
>E.g. Prozac and Digoxin
2)False substrate
>Compete with natural substrate creating abnormal accumulation
>E.g. cocaine
What are 2 examples of drugs which target the cytoskeleton and what do they treat and how?
1) Colchicine
>Treats gout by preventing assembly of microtubules at sites of inflammation
2)Paclitaxel
> In chemotherapy, prevents microtubule dissemble and interferes with cell division
What protein category is most targeted by drugs?
Receptors
