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Pharm S2015 > Lecture 2 to 3: PD > Flashcards

Lecture 2 to 3: PD Flashcards

1
Q

Drugs affecting Ligand-gated Ion Channels

A
  • Local anesthetics: all local anesthetics bind to intracell site
  • Benzodiazepines: hyperpolarize GABAaR
  • Ligand can either be:
    • extracell mediator: ACh, GABA, aspartate or glutamate
    • intracell: Ca2+, cAMP or cGMP
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2
Q

Drugs affecting G Protein-linked Receptors

A
  • Albuterol, a β2-agonist, is used for asthma.
  • Propranolol, a β-antagonist, is used for hypertension.
  • Bethanechol, a muscarinic agonist, is used for atonic bladder.
  • Ipratropium, a muscarinic antagonist, is used for asthma.
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3
Q

cAMP-Mediated Hormonal Responses

A
  • Breakdown of glycogen in liver: β-adrenoceptors & glucagon receptors
  • Breakdown of TAGs in adipose tissue: β-adrenoceptors
  • Increased heart rate and contraction force: β-adrenoceptors
  • Relaxation of smooth muscle: β-adrenoceptors
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4
Q

Ca2+-mediated responses

A
  • Smooth muscle contraction
  • Increased force of contraction of cardiac muscle
  • Secretion from exocrine glands
  • Neurotransmitter release from neurons
  • Hormone release
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5
Q

Ligand-regulated Transmembrane Enzymes

A
  • polypeptides consisting of:
    • an extracellular hormone-binding domain and
    • cytoplasmic enzyme domain.
  • Tyrosine kinase: insulin, EGFR, NGFR, PDGFR
    • Ex. Imantinib,
  • serine/threonine kinase,
  • guanylyl cyclase.
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6
Q

Cytokine Receptors

A
  • Cytokine receptors respond to many peptide ligands, such as growth hormone, prolactin, erythropoietin, and interferons.
  • no intrinsic enzymatic activity
  • bind an intracellular JAK -> STAT/STAT dimers translocate to the nucleus where they regulate transcription of specific genes.
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7
Q

Statins

A
  • HMG CoA reductase inhibitor -> By inhibiting cholesterol synthesis statins deplete intracellular supply of cholesterol.
  • Depletion of intracellular cholesterol leads to up-regulation of LDL receptors in hepatocytes -> increased clearance of LDL from the blood.
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8
Q

Structural Proteins Drug

A

vinca alkaloids bind to tubulin

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9
Q

Actions of Drugs Not Mediated by Binding to Receptors

A
  • Antacids
  • Mesna
  • Mannitol
  • Cholestyramine
  • Dimercaprol
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10
Q

Extracell enzymes

A
  • ACE found in blood
  • ACE inhibitors inhibit formation of AT II to Rx sodium & water retention & lower BP
  • Ex. Captopril
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11
Q

Mesna

A
  • Mesna mops up acroleine
  • Reacts in the bladder with acroleine, a metabolite of the anticancer drug cyclophosphamide, thus preventing hemorrhagic cystitis.
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12
Q

Mannitol

A

increases the osmolarity of various body fluids. This effect can promote diuresis or reduction of cerebral edema.

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13
Q

Cholestyramine, colestipol and colesevelam

A

Bind bile acids in the intestinal lumen and prevent their reabsorption. Used to treat hyperlipidemia.

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14
Q

Dimercaprol

A

chelates heavy metals.

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15
Q

Graded Dose-Response Curves

A

hyperbolic curve according to the following equation:

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16
Q

Receptor Binding of Drugs

A
17
Q

Irreversible Competitive Antagonism drug examples

A
  • Phenoxybenzamine: alpha-adrenoceptor blocker for rx pheochromocytoma
  • Aspirin
  • Omeprazole: PPI
  • Some authors refer to this type of antagonism as noncompetitive.
  • Ex. Ketamine: NMDAR
18
Q

Noncompetitive Antagonism

A
  • aka allosteric antagonism.
  • insurmountable.
  • Emax is decreased.
19
Q

Partial agonist

A

An agonist that has a lower Emax than a full agonist is a partial agonist. (This refers to the question with the graphs showing the dose responses of norepinephrine and Drug X).

20
Q

Nonreceptor antagonists

A
  • Functional: indirect & physiological
  • Chemical
21
Q

Indirect Antagonism

A
  • antagonist binds to a macromolecule in the pathway that links the receptor to the effect.
  • Ex.a drug that inhibits PKA blocks the effects of a β-adrenoceptor agonist.
22
Q

Physiological Antagonism

A

One agonist opposes another agonist, but through different receptors.

Ex. Epi & Histamine

23
Q

Chemical Antagonism

A

protamine, a protein which is positively charged, counteracts the effects of heparin, an anticoagulant that is negatively charged.

24
Q

Drug Selectivity

A

A drug is selective if there is at least a 10-fold difference between its binding affinity for its first target (the target which mediates the therapeutic effects) versus its second target (which mediates adverse effects).

The greater the difference, the more selective the drug is.

25
Q

Inverse agonist

A
  • reverse the constitutive activity of a receptor.
  • famotidine, losartan, metoprolol and risperidone.
26
Q

Quantal Dose-Effect Curves

A
  • based on a graded response (as seen above) or on an all-or-nothing (quantal) response
  • plots fraction of the population

Pharm S2015 (47 decks)

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