12.3C Chemisrty and Materials Design Flashcards
Drug
any chemical that measurably alters the physiological function of an organism qualifies as a drug
- Alterations caused by drugs can include activity level, conciousness, coordination, incoming sensory information, mood, or emotion
- Very commonly, drugs inhibit, block, or (less othen) speed up the action of specific enzymes, receptors, or signalling proteins
Medicine
means a drug that is intended to cure a disease or provide symptomatic relief
Drugs from plants
- drug Digoxin is extracted from foxgloves
- painkiller aspirin originated from a compound found in the bark of willow tree
- Taxol an anticancer drug obtained from a bark of a Pacific yew tree
ASPIRIN
made by acylation of salicylic acid
- Aspirin is almost insoluble in water, so its Bioavaliability is limited
- The solubility and bioavaliability of pharmaceutical drugs can be increased by converting them into ionic salts
- Has analgesic, antipyretic, anti-inflammatory, and anti-clotting effect
- Negative side effects include stomach bleeding, allergies, and Reye’s syndrome
Designing new medicinal drugs
Structural features:
- should fit into the active site of essential enzyme of the pathogen and block it
- bind to the active site using its functional groups. The intermolecular bonds formed between drug and target molecule (hydrogen bonding, ionic attraction, dipole-dipole forces)
Designing new medicinal drugs:
Molecular modelling
- Computers judge the fit of potential drug and target molecule
- The interactions between those molecules can be studied before mass production in lab
What are the benefits of molecular modelling?
- lower the number of trials and errors; With molecular modelling, only potentialy successful medicine made and tested.
Chirality in pharmaceutical synthesis
Most of the drugs have optical isomerism. They exist as two enantiomers with identical physical properties, but differemt “pharmaceutical activity” (effect the drug has on the body)
- Thalidomade +enantiomer was used for treatment of morning sickness during pregnancy. -enatiomer caused deformation of limbs of babies. congential deformities.
- Naproxen used to treat the pain of arthritis, other enantiomer can cause liver damage
Ways to prepare pure enantiomers
- Optical resolution for separation a racemic mixture
- Optically active starting materials
- Chiral catalyst
Methods of administration: ORAL
Drug delivered by mouth and absorbed through gastrointestinal tract
Advantages:
+ convenient
+ non-invasive
Disadvantages:
- low % absorption (wasteful and reduces effectiveness)
- drugs may interact with food & beverages
- may be disabled by stomsch acid
- absoption occurs slowly
Methods of administration: PARENTERAL
Drug delivered by injection
Advantages:
+ fast delivery (subcutaneous<intramuscular<intravenous)
+ amounts can be precisely controlled
Disadvantages:
- drug is irretrievable (mistakes cannot be corrected)
- unpleasant & painful (needles or IV lines)
Methods of administration: INHALED
Drug delivered as aerosol into lungs
Advantages:
+ fast delivery, hits brain & body nearly simultaneously
Disadvantages:
- not possible with many drugs
- irretrievable
Methods of administration: RECTAL
Drug delivered by suppository (dissolves in rectum)
Advantages:
+ can be used with nauseted patients
+ avoids problems with stomach acid
Disadvantages:
- distasteful to many people
- can’t take in public
Delivery of drugs: Liposomes
- liposomes made of phospholipids, have hudrophilic head and hydrophobic tails
- reduce drug toxicity in cancer treatment as only get thru walls of tumour’s blood vessels
- used to carry DNA for gene therapy
- deliver the active ingredients of cosmetic agents, such as antiwrinkle creams, deeper into the skin
Delivery of drugs: Gold Nano-Cages
- coated by a polymer PEG;
PEG stops body’s immune system from attacking the gold particles and ejecting them from the bloodstream - used to carry insoluble cancer-fighting drugs to the tumour;
When laser warms the gold atoms, the cage opens, polymer dissolves, releasing the drug
Nanotechnology
is the synthesis and study of compounds, devices and structures within the 10^-9m to 10^−7m (1-100 nanometers) in size.