Intro to pharm. receptors Flashcards
(50 cards)
What is a receptor?
macromolecular component that binds the drug and initiates its effect. (most are proteins that have undergone post-translational modifications)
What are the key concepts for: drugs that antagonize cell surface receptors?
- cell surface receptors send chem. signals from outside to inside of cell
- drug binds receptor- preventing agonist from binding= preventing response (antagonize/block endogenous/normal chem.)
What is the important example of: a Cell surface receptor antagonist?
Propranolol (Inderal)
What is Propranolol used for, and how does it work?
- for angina, myocardial infarction, heart failure, high BP, and performance anxiety
- B-Adrenoceptor blocker (cell surface receptor antagonist)- decreasing force of heart contraction= heart doesn’t have to work so hard.
What is a nuclear receptor?
in intracell. compartment; binds to DNA regulator regions and modulated gene expression when activated
What are the key concepts for: drugs that antagonize nuclear receptors?
- nuclear receptors mediate effects of intracell. endogenous chems. on gene expression
- these drugs bind to nuclear receptors= prevent receptor translocation to nucleus= prevents binding to DNA and altering of gene expression.
What is the important example of: a Nuclear receptor antagonist?
Tamoxifen (Nolvadex)
What is Tamoxifen used for, and how does it work?
- to prevent and treat breast cancer
2. Estrogen receptor antagonist (nuclear receptor antagonist)
What are the key concepts for: drugs that inhibit enzymes?
- bind enzymes to inhibit enzymatic activity= lose product
What is the important example of: an enzyme inhibitor?
Aspirin and Ibuprofen (motrin)
What are Aspirin and Ibuprofen used for, and how do they work?
- pain relief (arthritis)
2. inhibit cyclooxygenase (prevent prostaglandin and thromboxane production)
What are the key concepts for: drugs that block ion channels?
- bind ion channels preventing flow of ions through pore/down electrochem. gradient
- can physically block pore or cause closure of pore (allosterically)
- changes in intracell. ion conc. causes drugs’ effects
What is the important example of: an ion channel blocker?
Diltiazim (Cardizem)
What is Diltiazim used for, and how does it work?
- Angina and high BP
2. blocks calcium channels (ion channel blocker)
What are the key concepts for: drugs that inhibit transporters?
- transporters bind and shuttle mem. impermeable solutes across mem.
- drugs bind transporters= allosteric change= non functional transporters
- intracell. solute conc. changes (of specific solutes) cause drugs’ effects
What is the important example of: a transporter inhibitor?
Fluoxetine (Prozac)
What is Fluoxetine used for, and how does it work?
- depression
2. selective serotonin reuptake inhibitors (transporter inhibitor)
What are the key concepts for: drugs that inhibit signal transduction proteins?
- signal transduction proteins send chem. signal from receptor to final target
- can block/ augment signal transduction pathway= what mediates drugs’ effects.
What is the important example of: a signal transduction inhibitor?
Sildenafil (Viagra)
What is Sildenafil used for, and how does it work?
- erectile dysfunction
2. inhibits type 5 phosphodiesterase (signal transduction inhibitor)
What are the key concepts for: drugs that activate cell surface receptors? (Agonists)
- binding triggers a response (activates receptor)
2. can be: the actual endogenous chem. signal or something that mimics the endogenous chem. signal
What is the important example of: a Cell surface receptor agonist?
Phenylephrine (neosynephrine)
What is phenylephrine used for, and how does it work?
- nasal congestion
2. Alpha 1- Adrenoceptor Agonist (cell surface receptor agonist)
What are the key concepts for: drugs that activate nuclear receptors? (agonists)
- trigger response by binding to nuclear receptors- alter gene expression
- some are actual endogenous chem. signal and some just mimic endogenous chem. signal
