Exam 2 Flashcards
Examples of primary lipids
Fixed oils, fats, phospholipids, waxes, mineral oils, paraffin
What are waxes?
esters of fatty acids and alcohols
What are the different triglycerides?
fixed oils and fats
Examples of secondary lipids
Polyketides (aromatics, etc), terpenoids and steroids, phenylpropanoids
secondary lipids property
not soluble in water, soluble in ehter, chloroform, lipid, fat solvents
Examples of volatile oils
essential oils, essences
Properties of volatile oils
small aliphatics, aromatics, potent odors, flavors
Examples of resins
- Oleoresins: turpentine, capsicum
- Balsams: contain benzoic and/or cinnamic acids (benzoin)
Properties of resins
solid, amorphous, complex lipid mixtures; when you injure a plant, liquid comes out and turns to solid when dried
Examples of latex
rubber latex and opium latex
Properties of latex
aqueous suspensions of lipids; when you injure a plant, white liquid comes out and turns black when dried
Examples of fixed oils
Castor oil, Olive oil, Peanut oil, Soybean, Sesame oil. Cottonseed oil, Corn oil, Safflower oil, Coconut Oil
Examples of fatty acids
Stearic, Oleic, Linoleic, Linolenic acids
Examples of waxes
Beeswax, Carnauba wax
What do oil base paints contain?
Linolenic acid
What are the different classes of steroidal drugs?
- Plant Steroids/Sterols
- Steroid Hormones
- Semi- and Synthetic Steroid Drugs
Examples of plant steroids/sterols
Cardiac Steroids, Sitosterol
Examples of steroid hormones
Sex hormones, adrenocorticoid hormones (cholesterol as a derivative)
Examples of semi- and synthetic steroid drugs
Corticosteroids, Anabolic steroids
What are antibiotics derived from acetate metabolism?
These are all BIOsysnthesized:
- Tetracyclines
- Antineoplastic Anthracycline Derivatives
- Macrolide Antibiotics
- Polyenes
Examples of Polyene/Polyketide Drugs
- Lovastatin
- Simvastatin
- Rifampin
- Nystatin
(apparently tetraclycines and erythromycin are under this category?)
Examples of Antineoplastic Anthracycline Derivatives
- Doxorubicin
- Plicamycin
- Mitomycin
Examples of Macrolide Antibiotics
- Erythromycin
- Oleandomycin
- Vancomycin
Structure of macrolide antibiotics
characterized by a macrolactone ring that is glycosidically linked to one or more sugars
Structure of polyenes
Amphoteric actinomycete metabolites characterized by a series of conjugated double bonds.
What is an example of a fatty acid that is a SECONDARY metabolite?
Arachidonic Acid
Where can you find Arachidonic Acid?
- peanuts, animals, coral
- precursor to Prostaglandins
Where can you find Prostaglandins?
animals, coral
What are Terpenoids?
derivatives from Arachidonic Acid with 5 carbon units; derived from acetate
Numbering and naming system for Terpenoids
- C5 —Hemiterpenes
- C15 — Sesquiterpenes
- C20 —Diterpenes
- C10 —Monoterpenes
- C30—Triterpenes
- C40—Tetraterpene
Volatile oils composition
Consist largely of terpenes (isoprene units)
Examples of Phenylpropanoids
Methyl Salicylate, Eugenol, Cinnamaldehyde (these are NOT derived from acetate)
What plant species is used in the treatment of infections, diabetes, and hepatitis B? And what does it consists of?
- Phyllantus species
- Consists of Triterpenoid
T/F; Alkaloids are ubiquitous in nature.
TRUE :)
Define alkaloids
Naturally occurring, organic nitrogenous compounds that are usually basic and derived from amino acids
What are the different types of alkaloids?
- True Alkaloids
- Proto-alkaloids
- Pseudo-alkaloids
Where are proto-alkaloids found?
mammals
Properties of alkaloids
- Solids; basic in nature
- Bitter
- Base and salt forms
How can you purify alkaloids from plant matter?
Reversible reactions going back and forth from base to salt
What can you use to precipitate alkaloids?
Alkaloidal reagents:
- Mayer’s Reagent
- Dragendorff’s reagent
Will only react with true alkaloids
What are the classes of alkaloids?
- Pyridine
- Piperidine
- Pyrrolidine
- Imidazole
- Quinoline
- Isoquinoline
- Indole
- Purine
- Tropane
What is the structure for true alkaloids?
when the N is in a ring structure
What are the precursors for true alkaloids?
- Phenylalanine
- Tyrosine
- Tryptophan
- Histidine
What is the structure for proto-alkaloids?
when the N is outside the ring; may or may not react with alkaloidal reagent
How do pseudoalkaloids differ from true alkaloids?
- are not derived from amino acids
- do not react with alkaloidal reagent
How can you tell if morphine / opium is in a compound or solution?
React it with FeCl3. Meconic acid is present only in opium and will react with FeCl3 to give a red color
Which amino acid are isoquinoline alkaloids derived from?
tyrosine
Which amino acid are indole alkaloids derived from?
tryptophan
Why does pseudo-alkaloids not react with alkaloidal reagents?
because their N can be ionized
Define pharmacology
study of chemical substances that can come into the body and change the physiological function of one of our organs or physiological processes
Define toxicology
the branch of pharmacology that deals with the undesirable side effects of chemicals on living systems, from individual cells to humans to complex ecosystems
Define pharmacophore
the portion of a drug that is responsible for its biological action
Define prototype
a representative agent for a drug class
Define agonist
Drug that binds receptor and produces biologic response
Define antagonist
Drugs that decrease or oppose action of another drug or endogenous ligand
What are the different branches of toxicology?
- Environmental
- Economic
- Forensic
What is pharmacokinetics?
study of what our body will do to the drug; ADME
What does chemotherapeutic agents attack?
anything that is nonhuman + cancer cells; ex. bacteria, fungi, parasite, virus
What are bacteriostatic agents?
stop the growth of bacteria
What are bacteriocidal agents?
eradicate bacteria
What specific targets in bacteria does chemotherapeutic agents attack?
- cell wall synthesis
- ribosomes; transcription and translation
- DNA synthesis and integrity
- folic acid metabolism
What specific targets in fungi does chemotherapeutic agents attack?
- cell membrane ergosterol
- synthesis of specific cell wall glycan
- DNA synthesis
What specific targets in virus does chemotherapeutic agents attack?
- attachment and entry onto the cell
- Polymerase and protease
- Reverse transcriptase
- Reverse transcriptase
- Modulation of viral genes
What specific targets in cancer cells does chemotherapeutic agents attack?
- DNA synthesis
- signal transduction
Properties of pharmacotherapeutic agents
- act on specific sites on the cells
- ↑ or ↓ organ function
- selective for organs but may results in adverse effects in organs that have same receptors
- toxicity is often extension of drug’s therapeutic action
What are the different types of receptors?
- Ligand-gated ion channels
- G protein coupled receptors
- Enzyme linked receptors
- Intracellular receptors
Differentiate between transmembrane receptors and intracellular receptors.
Intracellular are inside the cell. The rest are transmembrane. Transmembrane agonists are hydrophillic. Intracellular agonists are hydrophobic (lipophillic) and can cross the membrane easily to bind to the receptor on the inside.
What (rights) do you have to have in order to have a positive therapeutic effect?
Right drug, right place in the right amount for the right duration of time.
What are the ways in which the action of a drug can be described?
- Symptomatic
- Physiological
- Cellular
- Molecular
What is the difference between agonist antagonist drugs?
- Agonist: binds to receptor to produce response similar to natural ligand
- Antagonist: binds to receptor to block a response; no effect on it’s own; effective in presence of agonist
What is the difference between specific and non-specific drugs?
- Specific targets the cause of the disease
- Non-specific relieves symptoms
Define membrane transporters
binding sites for drugs which do not mediate drug action but are involved with determining plasma concentrations of drugs
What are the types of membrane transporters?
- ATP binding cassettes (ABC)
- Solute carrier transporters (SLC)
Properties of ABC
- primary active transport
- pumps drugs out of cells
Properties of SLC
- facilitated transporters
- ion-coupled secondary active transporters
- reuptake of neurotransmitters
What are SNPs?
proteins that are polymorphs that are genetically determined
What are the types of bond in drug-receptor binding?
- Covalent bonds
- Ionic bonds
- Cation-π interactions
- Hydrogen bonds
- Van der Waals forces
- Hydrophobic interactions
Describe cation-π interactions
happens between electronic cloud of aromatic compounds and positive ions; common in neurotransmitter binding
How are hydrophobic interactions important in drug-receptor binding?
↑ binding to each other & ↓ binding to aqueous environment via hydrogen bonding
Define orthosteric site
the site on the receptor where the agonist binds to
Hippocrates (according to the notes)
first to think of therapeutics without concept of evil spirits/religious rituals
Which century did methods start to develop to do physiological and pharmacological experiments?
18th century
When did the modern pharmaceutical industry start to develop? (chemicals are synthesized instead of solely made from plants)
1920’s
Who discovered aspirin?
Felix Hoffmann
Who discovered penicillin?
Alexander Fleming
Who was John Langley?
- first to postulate receptor theory calling it “receptive substance”
- studied muscle contraction via nicotine, curare, pilocarpine, atropine
- this is where we have our first indications for Pharmacotherapeutic mechanisms
Who was Paul Ehrlich?
- Treated bacterial infections with dyes and heavy metals
- developed chemotherapy further using rabbits
- this is where we have our first indication for Chemotherapeutic mechanisms
Whose research lead to what we now called receptors?
Ehrlich and Langley’s research at the end of the 19th century
What is Vagusstuff?
acetylcholine
Who discovered that neurotransmitters are chemical compositions?
Dale & Loewi
Who is Sir James Black?
Discovered the first agent to block beta adrenergic receptors, Propranolol, a life-saving drug for heart disease.
Define Xenobiotic
A drug or chemical which is foreign to the body.
Define Chemotherapy
Application of drugs for treatment of diseases caused by invading organisms
Define Antibiotic
part of a living organism used to treat to kill another organism
Define Idiosyncracy
Unusual or exaggerated side effect, e.g., barbiturate causing pain and excitement; morphine.
What are Additive Drug Effects?
when two drugs used in combination produce the sum effect of what they would act separately
What is Potentiation?
when two drugs used in combination produces a greater effect than what they would normally produce separately and added together
Explain the types of tolerances
- Drug disposition tolerance - enzyme induction, metabolized faster
- Pharmacodynamic tolerance - CNS adaptation, body adapts to drug
Define Tachyphylaxis
Acute tolerance - tolerance within 1 -2 doses
What are the mechanisms for drug antagonism?
- Receptor (pharmacologic): when both bind to the same receptor
- Physiologic: acting on different receptors but do opposite effect that they nullify each other
- Chemical: chemical bind to drug and inhibit it
What is passive filtration?
passive diffusion (moving along concentration gradient) but through a pore or channel
What is facilitated diffusion?
moves down concentration gradient but requires a carrier
What is transcytosis?
- carries molecules via vesicles
- invovles endo and exo cytosis
- slow
What is the difference between passive filtration and diffusion?
- diffusion: passes through membrane; has to be non-ionized
- filtration: passes through pores or channels; doesn’t matter if ionized or not as long as it can fit through pore
What are the absorption factors?
- Solubility of drug
- Dissolution rate (solid dose)
- Concentration at the site
- Circulation to the site
- Absorbing surface area
What are limitations in oral route?
- Many drugs are poorly absorbed
- GI destruction
- Drug passes through liver
What are (dis)advantages of oral mucosa route?
- Limited absorption
- Avoids first-pass metabolism
What are (dis)advantages of rectal route?
- Used in pediatrics
- No nausea and vomiting
- Avoids portal circulation by 50%
- Absorption is irregular and often incomplete
What is responsible for binding of acidic drugs?
serum albumin
What is responsible for binding of basics drugs?
α1-glycoproteins
Where are ions and heavy metals stored?
in the bone
What are two mechanisms of the kidney?
- Glomerular filtration
- Tubular secretion
How can drugs be excreted?
- Feces
- Lungs
- Milk
- Sweat, saliva, tears
- Hair, skin
What is polypharmacy?
when you’re taking more than 4 tablets at a given time
What is polypharmacology?
refer to drugs that act on more than one target
What is elastase’s function?
to chew up damaged elastin tissues in the lung
What keeps elastase in check?
alpha-1-antitrypsin
What happens if you lack by alpha-1-antitrypsin?
you have a higher chance of getting emphysema
In DNA, how many base pairs are there for each 360 degree turn?
10 nucleotide base pairs
Where are the preferred sites for DNA alkulation?
- N7 of guanine
- N3 of adenine
What is the function of topoisomerase?
remove knots and separate links in tangled DNA
What happens if you block the action of topoisomerase?
cell death
