Lecture 19 Flashcards
(22 cards)
Drugs
A substance of known structure which produces a biological effect. Exogenous administration. Cannot create a new effect in a biological system, they modify the activity of that system. Most are small molecules.
chemical
Derived from plants or animals or synthetic. Isolated natural products/via synthetical chemistry.
Biological
Antibodies, enzymes, growth factors. Usually produced via genetic engineering
Drug nomenclature
Chemical name (sometimes too difficult), CAS registry no., generic name, proprietary name (brand name). Drugs can have more than one generic name.
Drug action
They must be specific to cells/tissues. The drug and the binding site must be complementary. A drug must bind to one or more cell constituents to produce a pharmacological response. Achieved by intra and inter molecular forces.
charges
+ attracted -
Shape and 3D structure
Arrangement of functional groups in both
Size
Drug and binding site must fit exactly.
Bonding types between drugs and their targets
Ionic, ion-dipole/dipole-dipole, induced dipole bonds, covalent, cation-pi interactions
Affinity
ability to bind to target. Increase affinity = decrease conc. drugs. A drug can have affinity for multiple targets but, only those. Drug with increased affinity to its preferred target is called selective.
Receptors
Ligand-gated ion channels, GPCR, kinase-linked and nuclear. Aim to stimulate or block receptors
Ion channels
Ligand ICs or voltage-gates ICs. Can block or modulate ICs
Enzymes
Can inhibit, mimic substrate or activate drug
transporters
inhibits transport ions or substrates of transport
drug affect
- activating
-enhancing - attenuating
-interferring
biologics
- vaccines
-blood/blood components
-recombinant therapeutic proteins
all isolates organisms and may be produced via biotechnologies
biological vs small molecules
biologicals: complex, derived from living cells, injection, IV, sensitive to storing and handling.
Nucleic acid therapeutics
Use of DNA/RNA to alter cells. Nucleic acids are too large and - to enter cell on their own. To overcome challenge, they are injected to site of origin or are transported via lipid nanoparticles.
Antisense oligonucleotides
short, single RNA or DNA that can bind to target-RNA to control how a protein is made. Achieved by recruiting enzymes, inhibit translation and splicing modulation. End in ~rsen
RNAi
Using small interfering RNAs to degrade specific RNA by activating RISC. Double stranded and incorporates it into RISC ~siran ending.
mRNA therapy
Delivering synthetic RNA for the translation of a protein ~meran ending.
Protein-based therapies
Peptides, enzymes, antibodies e.g ozempic binds to GLP1 receptors and end in ~tide.
