Basic Principles Flashcards
Drug Molecule Interacts as what?
1.
2.
What do you call its target?
1.
- Agonist (activator)
- Antagonist (inhibitory)
- Receptor
- Drugs that have almost exclusively harmful effects?
2. Poison of biologic origin?
- Poisons
2. Toxins
How can a drug chemically interact with its receptor? (4)
- Appropriate size
- Electrical charge
- Shape
- Atomic Composition
In most cases, a molecule should be at least how many MW units to achieve selective binding?
100 MW units
In terms of drug sizes, (100-1000)
- The lower limit is set by what?
- The upper limit means?
- If more than the upper limit?
- Requirements for specificity of action
- Determined primarily that the drug must be able to move within the body
- Do not diffuse readily between the compartments of the body
Drug Reactivity and Drug-Receptor Bonds
- Covalent Bonds
- Electrostatic Bonds
- Hydrophobic Bonds
- Very Strong and irreversible under biologic conditions
- Vary from relatively strong linkages between permanently charged ionic molecule to weaker hydrogen bonds and very weak induced dipole interactions such as van der Waals forces and similar phenomena
- Usually quite weak and important in the interactions of highly lipid-soluble drug
What is allosteric inhibition?
Drugs that bind to the same receptor molecule but
A. Do not prevent binding of the agonist
B. May enhance or inhibit the action of the agonist molecule
- When drugs are administered at concentrations sufficient to saturate the receptor pool, will activate their receptor-effector system to maximum extent
- Bind to the same receptors and activate them in the same way but do not evoke as great a response, no matter how high the concentration
- Presence of antagonist at the receptor site will block access of agonist to the receptor and prevent the usual agonist effect
- Full Agonist
- Partial Agonist
- Neutral Antagonism
True or False:
- Dissociation of drug from the receptor automatically terminate its effect.
- In all cases, If the drug dissociates from its receptor the action will be terminated.
- True
- False
- the action may persist after dissociation because some coupling molecule is still present in activated form.
An Inactive precursor chemical that is readily absorbed and distributed must be administered and then converted to active drug by biologic process inside the body?
Prodrug
Pharmacokinetic Principle
Absorption
Distribution
Permeation
Elimination