E01L02 Mechanisms of Drug Action Flashcards
_______-____-_____ _____ implies that # of receptors may limit max effect of drug
sigmoid-dose-response curve
True about Receptor-mediated drug action except
A. All receptors are protein
B. Specificity is due to shape and electrical charge via structural diversity
C. has 2 major domains - receptor and effector
D. Can be identified by drug binding and gene sequencing
A
[Type of receptor] Neurotransmitters, autocoids, hormones
Regulatory Proteins
[Type of receptor] inhibited by drug binding
Enzymes
[Type of receptor] e.g. Na-K-ATPase
Transport
[Type of receptor] e.g. tubulin - receptor for colchines
Sturctural
IUPHAR stands for
International Union of Pharmacology
Ach, Serotonin, GABA, glutamate act on A. Ligand Gated Ion Channels B. Voltage Gated Ion Channels C. G-Protein coupled receptors D. Enzyme-linked receptors
A
What is common about Phenytoin, Lamotrigine and Valporate?
Inhibit Na+ channels therefore are used as anticonvulsants
What is verapamil for?
Inhibit voltage-gated Ca2+ channels at vascular smooth muscle, decrease BP antiarrhythmic
___________ Receptor - no ion but linked to G-receptor
Metabotropic
Which of the following statements is false?
A. Gαs open ion channels (Ca2+) in myocardium and skeletal muscle
B. Gi open K+ Channel in heart and smooth muscles
C. Gαs close neuronal Ca2+ channel
D. Gi close neuronal Ca2+ channel
C
Physiological ligand for receptor for tyrosine kinase are the following except A. Insulin B. PDGF C. EGF D. VEGF E. Interleukin
E
Effector of Receptors for tyrosine kinase
SH2 domain
Herceptin and Imatinib target
Receptor for tyrosine kinase
Interleukin and other cytokines act on
Cytokine receptors
Effector of cytokine receptor
Jak/STAT
Effetor of guanylylcyclase
cGMP
Physiological ligand of guanylyl cyclase
Natriuretic peptides
Example drug that targets guanylyl cyclase
Nesiritide
Purpose of phsophorylation include the following EXCEPT A. Amplification B. Flexible regulation C. A only D. Both A and B
D
Non-receptor mediated drug action; chelates blood thus used in treating lead poisoning
EDTA
Non-receptor mediated drug action; treat fibrotic skin disorder
PABA
What is the non-receptor mediated action of KMnO4?
antiseptic
What is the non-receptor mediated action of Mannitol?
Osmotic disorder
Describe tachyplaxis
diminution of receptor response due to frequent exposure to agonists
