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CMBM exam 4 > Intro to pharm. receptors > Flashcards

Intro to pharm. receptors Flashcards

1
Q

What is a receptor?

A

macromolecular component that binds the drug and initiates its effect. (most are proteins that have undergone post-translational modifications)

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2
Q

What are the key concepts for: drugs that antagonize cell surface receptors?

A
  1. cell surface receptors send chem. signals from outside to inside of cell
  2. drug binds receptor- preventing agonist from binding= preventing response (antagonize/block endogenous/normal chem.)
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3
Q

What is the important example of: a Cell surface receptor antagonist?

A

Propranolol (Inderal)

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4
Q

What is Propranolol used for, and how does it work?

A
  1. for angina, myocardial infarction, heart failure, high BP, and performance anxiety
  2. B-Adrenoceptor blocker (cell surface receptor antagonist)- decreasing force of heart contraction= heart doesn’t have to work so hard.
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5
Q

What is a nuclear receptor?

A

in intracell. compartment; binds to DNA regulator regions and modulated gene expression when activated

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6
Q

What are the key concepts for: drugs that antagonize nuclear receptors?

A
  1. nuclear receptors mediate effects of intracell. endogenous chems. on gene expression
  2. these drugs bind to nuclear receptors= prevent receptor translocation to nucleus= prevents binding to DNA and altering of gene expression.
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7
Q

What is the important example of: a Nuclear receptor antagonist?

A

Tamoxifen (Nolvadex)

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8
Q

What is Tamoxifen used for, and how does it work?

A
  1. to prevent and treat breast cancer

2. Estrogen receptor antagonist (nuclear receptor antagonist)

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9
Q

What are the key concepts for: drugs that inhibit enzymes?

A
  1. bind enzymes to inhibit enzymatic activity= lose product
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10
Q

What is the important example of: an enzyme inhibitor?

A

Aspirin and Ibuprofen (motrin)

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11
Q

What are Aspirin and Ibuprofen used for, and how do they work?

A
  1. pain relief (arthritis)

2. inhibit cyclooxygenase (prevent prostaglandin and thromboxane production)

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12
Q

What are the key concepts for: drugs that block ion channels?

A
  1. bind ion channels preventing flow of ions through pore/down electrochem. gradient
  2. can physically block pore or cause closure of pore (allosterically)
  3. changes in intracell. ion conc. causes drugs’ effects
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13
Q

What is the important example of: an ion channel blocker?

A

Diltiazim (Cardizem)

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14
Q

What is Diltiazim used for, and how does it work?

A
  1. Angina and high BP

2. blocks calcium channels (ion channel blocker)

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15
Q

What are the key concepts for: drugs that inhibit transporters?

A
  1. transporters bind and shuttle mem. impermeable solutes across mem.
  2. drugs bind transporters= allosteric change= non functional transporters
  3. intracell. solute conc. changes (of specific solutes) cause drugs’ effects
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16
Q

What is the important example of: a transporter inhibitor?

A

Fluoxetine (Prozac)

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17
Q

What is Fluoxetine used for, and how does it work?

A
  1. depression

2. selective serotonin reuptake inhibitors (transporter inhibitor)

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18
Q

What are the key concepts for: drugs that inhibit signal transduction proteins?

A
  1. signal transduction proteins send chem. signal from receptor to final target
  2. can block/ augment signal transduction pathway= what mediates drugs’ effects.
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19
Q

What is the important example of: a signal transduction inhibitor?

A

Sildenafil (Viagra)

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20
Q

What is Sildenafil used for, and how does it work?

A
  1. erectile dysfunction

2. inhibits type 5 phosphodiesterase (signal transduction inhibitor)

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21
Q

What are the key concepts for: drugs that activate cell surface receptors? (Agonists)

A
  1. binding triggers a response (activates receptor)

2. can be: the actual endogenous chem. signal or something that mimics the endogenous chem. signal

22
Q

What is the important example of: a Cell surface receptor agonist?

A

Phenylephrine (neosynephrine)

23
Q

What is phenylephrine used for, and how does it work?

A
  1. nasal congestion

2. Alpha 1- Adrenoceptor Agonist (cell surface receptor agonist)

24
Q

What are the key concepts for: drugs that activate nuclear receptors? (agonists)

A
  1. trigger response by binding to nuclear receptors- alter gene expression
  2. some are actual endogenous chem. signal and some just mimic endogenous chem. signal
25
Q

What is the important example of: a nuclear surface receptor agonist?

A

Conjugated Equine estrogens (Premarin)

26
Q

What is Premarin used for, and how does it work?

A
  1. hormone replacement therapy (post-menopausal women)

2. Estrogen receptor agonist (nuclear receptor agonist)

27
Q

What are the key concepts for: drugs that activate enzymes?

A
  1. bind to enzymes and increase enzymatic activity

2. increased product mediates drugs’ effects

28
Q

What is the important example of: an enzyme activator?

A

Pralidoxime (protopam)

29
Q

What is Pralidoxime used for, and how does it work?

A
  1. used after poisoning with nerve gas/organophosphate pesticide
  2. activates cholinesterase (enzyme activator)
30
Q

What are the key concepts for: drugs that open ion channels?

A
  1. drugs bind and cause allosteric change- can be: opening ion channel or make channel more readily opened by other endogenous chems.
  2. change in intracell. ion conc. mediates drugs’ effects
31
Q

What is the important example of: a ion channel openers?

A

Minoxidil (Rogaine)

32
Q

What is Minoxidil used for, and how does it work?

A
  1. hair regrowth

2. opens potassium channels (ion channel opener)

33
Q

What are the important examples of: a drug that disrupts structural proteins?

A

Vincristine (oncovin) and Vinblastine (Velban)

34
Q

What is Vincristine and Vinblastine used for, and how do they work?

A
  1. cancer

2. Vinca Alkaloids (disrupt structural proteins)

35
Q

What is the important example of: a drug that is an enzyme?

A

Alteplase (Activase)

36
Q

What is Alteplase used for, and how does it work?

A
  1. Acute myocardial Infarction

2. Thrombolytic therapy (drug that’s an enzyme)

37
Q

What is the important example of: a drug that covalently links to macromolecules?

A

Cyclophosphamide (Cytoxan)

38
Q

What is Cyclophosphamide used for, and how does it work?

A
  1. Cancer

2. DNA alkylating agent (drug that covalently links to macromolecules)

39
Q

What is the important example of: a drug that reacts chemically with small molecules?

A

various preparations containing Al(OH)3, Mg(OH)2, or CaCO3

40
Q

What are various preparations containing Al(OH)3, Mg(OH)2, or CaCO3 used for, and how do they work?

A

1/2. Antacids that neutralize gastric acid (drugs that react chemically with small molecules).

41
Q

What is the important example of: a drug that binds free molecules/atoms?

A

Dimercaprol

42
Q

What is Dimercaprol used for, and how does it work?

A
  1. Heavy metal poisoning

2. Chelating agent (binds free molecules/atoms)

43
Q

What are the important examples of: drugs that are nutrients?

A

vitamins, minerals, lipids, carbs., and amino acids

44
Q

What is the important example of: a drug that exert actions due to physical properties?

A

Mannitol

45
Q

What is mannitol used for, and how does it work?

A
  1. Edema

2. Osmotic diuretic (drug that exerts actions due to physical properties)

46
Q

What is the important example of: a drug that work via an antisense action?

A

Fomivirsen (Vitravene)

47
Q

What is Fomivirsen used for, and how does it work?

A
  1. Cytomegalovirus (CMV) retinitis in AIDS patients

2. Antisense Deoxyoligonucleotides (drug that works via an antisense action)

48
Q

What is the important example of: a drug that is an antigen?

A

vaccines

49
Q

What is the important example of: a drug whose mechanism of action is unknown?

A

Isoflurane (Forane)

50
Q

What is Isoflurane used for, and how does it work?

A
  1. Inhalation anesthetic for general anesthesia

2. mechanism of action is unknown

CMBM exam 4 (6 decks)

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