Pharmacology - General
Card Set Information
Pharmacology - General
Class of drugs that bind directly to DNA (CA)
Inhibit microtubule function
Mechanism of resistance=gene amplification
Methotrexate (meth heads have to amp their dose to get high)
Most widely used drug for Breast CA
MOA: inhibit thymidylate synthetase
Used to describe the maximal response obtainable from a drug
Lung toxicity (single drug)
MOA: inhibits dihydrofolate reductase
Mechanism of resistance=DNA repair enzymes
Site of action of most therapeutic agents
Group of drugs that target S phase
MOA: inhibit lymphocyte proliferation
Non-natural product drug that targets s-phase
(meth heads like to have sex)
Target M-phase of cell cycle
Largest family of receptors
Prodrug Alkylating agent
Increased GI toxicity
How are steroid transported in the blood?
Bound to CBG (capillary blood glucose)
Inhibits purine anabolism
6-mercaptopurine (6 letters in purine)
What is the Kd of a drug?
The concentration of drug that occupies 50% of receptors
Turns urine red
What is the overall objective of drug therapy?
Use of proper dose of drug to achieve the desired therapeutic action with minimal amount of side effects
Causes uterine hyperplasia
Heart toxicity (single drug)
Adriamycin (Adrian Peterson has my heart racing ;) )
Lipid-soluble alkylating agent
Plotting drug dose on x-axis and amount of response on y-axis describes what type of curve
Log-dose response curve
Toxicity: sodium retention, osteoporosis
MOA: Intercalates DNA (2 drugs)
Neurological toxicity (single drug name)
A strong drug-receptor interaction when only small amount of the drug is present is said to have high or low affinity?
Drug-receptor interaction results in a response of the cell/tissue
Drug binds to the receptor and does not stimulate a response
Competitive antagonist is an example of what type of receptor
Ligand-gated ion channels
Can an allosteric modulator have its own effect?
No-it only enhances/inhibits an effect
Fractional occupancy is synonymous to…
% receptors occupied
Which type of receptor is activated by phosphorylation?
What do tyrosine kinase receptors do?
Turn on other signaling molecules such as JAK and STAT
What is special about the steroid hormone receptors?
They bind inside the nucleus
When do we use Kd values?
To compare drugs
What is Kd
Equilibrium dissociation constant
Occupancy equation=(actual equation)
D/(D + Kd)
EC50 vs LD50
EC50-“test tube” experimental value of the effective conc, LD50-effective dose in a clinical/physiological setting
On an LDR curve, how do you determine which drug is the most potent?
The one furthest left is the most potent
Maximal level of response produced by the drug
Amount of drug that produces a give level of response
Potency vs. efficacy
Potency refers to the amount of drug, efficacy refers to the amount of response
What does it mean if drug A is more potent than drug B?
To achieve any level of response, less of drug A is needed than of drug B
How do you determine the maximal response
Testing increasing levels of a drug until the response reaches a constant value (top of the LDR curve) and it plateaus
An unusual effect of the drug that occurs in a small percentage of people
Loss of responsiveness to a drug treatment over time
Pharmacokinetic vs pharmacodynamics
Rate and extent of absorption of a drug