CTL week 9 Flashcards
sources of drugs?
sources of drugs?
- microorganism
- plants
- animals
- minerals
- synthesised in laboratories.
what is the difference between the Approved and Proprietary name of a drug?
what is the difference between the Approved and Proprietary name of a drug?
Answer:
Approved -> generic name (non-capital letters)
Proprietary -> brand/trade name
what is the molecular target of drugs?
what is the molecular target of drugs?
Answer:
- Proteins (R.I.C.E) [Receptors, Ion-channels, Carriers, Enzymes]
- nucleic acids
- miscellaneous targets.
an Agonist drug possess ?
an Agonist drug that possess ?
Answer: high Affinity and Efficacy for the receptor
an antagonist drug possess ?
an antagonist drug that possess ?
Answer: high affinity but no efficacy. It blocks the receptor
what is an Allosteric Modulators?
what is an Allosteric Modulators?
Answer: binds to modulatory site on receptor and either increases or inhibits the response.
what is the name for a drug that inhibits ion flow in ion-channels?
what is the name for a drug that inhibits ion flow in ion-channels?
Answer: Blockers
GABA is what kind of transmitter?
GABA is what kind of transmitter?
Answer: an antagonists that opens Chlorine channels to cause the membrane to hyperpolarize, thus relaxing.
3 kinds of drugs used by enzymes?
3 kinds of drugs used by enzymes?
- Inhibitor
- False substrate, converted to something else.
- Pro-drug, is converted by enzyme into active form.
2 kinds of drugs for Carrier molecules (transporters)
2 kinds of drugs for Carrier molecules (transporters)
Answer:
- drugs that inhibit transport
- drugs that act as false substrates
molecular targets for drugs (extended version)?
hint: LCDMSG
molecular targets for drugs (extended version)?
Lipid components of cell membrane (genral anaesthetics) Cell surface proteins DNA nuclei acids (chemotherapy) Metal ions Structural proteins (like tubulin) Gastrointestinal contents (antacids)
what are the 4 classes of receptors?
what kind of molecules (neurotransmitter/hormones) bind to which receptors?
what are the 4 classes of receptors?
- Ligand-gated ion channels (exp: nicotinic, GABA, Glutamate, 5-HT3)
- G-protein coupled receptors (exp: muscarinic, adrenoceptors, dopamine, opioid, 5-HT)
- Kinase-linked receptors (exp: cytokines, insulin, leptin, GH, IGF-1)
- nuclear receptors (exp: Oestrogen, steroids, Thyroid hormones)
what are the receptors for Epinephrine and Norepinephrine?
Epinephrine and Norepinephrine receptors are?
α1, α2, β1, β2
what are the receptors for Acetylcholine?
what are the receptors for Acetylcholine?
Answer: Muscarinic and nicotinic
_________ is the study of the interaction between a drug and its molecular target and the pharmacological response.
___Pharmacodynamics______ is the study of the interaction between a drug and its molecular target and the pharmacological response.
_____ measure of the ability of drug to bind to a receptor?
___Affinity___ measure of the ability of drug to bind to a receptor?
_____ ability of a drug, once bound to a receptor, to activate the receptor and produce a pharmacological response.
___Efficacy___ ability of a drug, once bound to a receptor, to activate the receptor and produce a pharmacological response.
are Efficacy and Affinity related?
are Efficacy and Affinity related?
Answer: no
the concentration that produces a certain pharmacological response is?
the concentration that produces a certain pharmacological response is?
Answer: potency (and it is determined by both Efficacy and Affinity).
The more potent the drug, the lower the concentration required to produce a big impact.
what is EC50?
what is EC50?
Effective concentration: the concentration of agonist which produces 50% of the maximal response. The lower the EC50, the more potent the drug
what is the difference between full and partial agonist?
what is the difference between full and partial agonist?
Answer:
full agonist has high efficacy
low agonist has low efficacy (will never reach max response even at high concentrations)
(note: full and partial agonist can have same affinity)
does an antagonist have an effect on the constitutive activity?
does an antagonist have an effect on the constitutive activity?
Answer: No, but it inhibits the effect of an agonist.
what is constitutive activity?
what is constitutive activity?
Answer: the continuous activity of receptors even in the absence of ligand.
what is an inverse agonist?
what is an inverse agonist?
Answer: it decreases constitutive activity.
Reversible competitive antagonism are?
Reversible competitive antagonism are?
Answer:
- Compete with agonist to bind to receptor.
- Increasing the concentration of the agonist will overcome the antagonist effect.
- Result, the log curve is pushed to the right
Irreversible competitive antagonism are?
Irreversible competitive antagonism are?
answer:
- Forms a strong chemical bond with receptor.
- Cannot be broken (increasing agonist concentration will not overcome antagonist).
- Result, reduces the response of the receptor.
non-competitive agonist are?
non-competitive agonist are?
Answer:
Bind to allosteric site
Inhibit agonist from producing effect
Are not surmountable
is Drug specificity concentration-dependent?
is Drug specificity concentration-dependent?
answer: Yes
At low concentration it will act on specific receptors.
At high concentrations it will act on other receptors or other cells.
Effects of a drug will often lessen if given continuously because?
(hint: ChIA PIE)
Effects of a drug will often lessen if given continuously because?
Answer: Change in receptors Internalization of receptors Active extrusion of drug from cells Physiological adaptation Increased drug breakdown Exhaustion of mediators
