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Pharmacodynamics Flashcards

1
Q

Study of the biochemical and physiological effects of drugs and their mechanisms of action

A

Pharmacodynamics

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2
Q

A receptor may exist in what two states

A

Active (Ra) and Inactive (Ri)

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3
Q

Any molecule that attaches selectively to particular receptors

A

Ligand

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4
Q

The strength of the reversible interaction between a drug and its receptor, as measured by the dissociation constant

A

Affinity

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5
Q

Capacity to induce a functional change in the receptor

A

Intrinsic activity

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6
Q

Drugs that bind to the physiological receptors and mimic the regulatory effects of the endogenous signaling compounds

A

Agonists

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7
Q

Drug binds to the same recognition site as the endogenous agonist (ORTHOSTERIC SITE)

A

Primary agonist

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8
Q

Binds to allosteric site

A

Allosteric agonists

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9
Q

Block or reduce the action of an agonist

A

Antagonist

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10
Q

Types of Antagonists

A

Physical, Chemical, Physiological

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11
Q

Types of agonists

A

Partial, Inverse

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12
Q

A maximal effect (Emax) an agonist can produce

A

Efficacy

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13
Q

Efficacy can only be measured with

A

A graded dose-response curve

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14
Q

The amount of drug needed to produce a given effect

A

Potency

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15
Q

Repeated administration of a drug results in

A

Tolerance

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16
Q

A type of tolerance which occurs very rapidly

A

Tachyphylaxis

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17
Q

decreased response to the agonist after its repeated injection in small doses

A

Desensitization

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18
Q

Tolerance may be due to

A
  1. Masking or internalization of receptors
  2. Down regulation (loss of receptors)
  3. Exhaustion of mediators (depletion of catecholamine)
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19
Q

Examples of competitive antagonism

A

ACh - Atropine
Morphine - Naloxone

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20
Q

Example of non competitive antagonism

A

Diazepam - Bicuculline

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21
Q

Aspirin + Paracetamol

A

Additive - Anelgesic/Antipyretic

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22
Q

Nitrous oxide + Halothane

A

Additive - General anaesthetic

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23
Q

Amlodipine + Atenolol

A

Additive - Antihypertensive

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24
Q

Glibenclamide + Metformin

A

Additive - Hypoglycaemic

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25
Ephedrine + Theophylline
Additive - Bronchodilator
26
Acetylcholine + Physostigmine
Supraadditive - Inhibition of breakdown
27
Levodopa + Carbidopa/Benserazide
Supraadditive - Inhibition of peripheral metabolism
28
Adrenaline + Cocaine/Desipramine
Supraadditive- Inhibition of neuronal uptake
29
Sulfamethoxazole + trimethroprim
Supraadditive- Sequential blockade
30
Antihypertensives (enalapril + hydrochlorothiazide)
Supraadditive - Tackling two contributory factors
31
Tyramine + MAO inhibitors
Supraadditive- Increasing releasable CA store
32
Physiological receptors have two functional domains
-ligand-binding domain -effector domain
33
Physiological ligands of *ligand-gated ion channels*
ACh(M2), GABA, 5-HT
34
Examples of drugs that use *ligand-gated ion channels*
Nicotine, Gabapentin
35
Voltage gated ion channels are activated by
Membrane Depolarization
36
Drugs that use voltage gated ion channels
Lidocaine, Verapamil
37
Receptors with intrinsic ion channel
GABAa, 5HT3, NMDA
38
Blockers of L Voltage Sensitive Calcium channels
1. Verapamil 2. Dihydropyridine group of CCBs, Cd2+
39
Blockers of T Voltage-Sensitive calcium channels
1. Flunarizine 2. Ethosuximide, Ni2+
40
Blockers of N voltage sensitive calcium channels
Gabapentin, Cd2+
41
Blockers of voltage sensitive P,Q & R calcium channels
Toxin from funnel web spider
42
Structure of Nicotinic ACh receptor ion channel
5 receptor subunits (2 alpha, gamma, beta and delta) form a cluster surrounding a central transmembrane pore
43
Each subunit of the ligand-gated nicotinic ach receptor pore has
1. A large extra cellular domain 2. Four transmembrane helices
44
Functions families of gcprs
1. Beta Adrenergic 2. Muscarinic cholinergic 3. Eicosanoid receptors
45
Effectors of eicosanoid receptors
Gs, Gi and Gq proteins
46
Example of Beta adrenergic receptor drugs
Dobutamine
47
Examples of muscarinic cholinergic receptor drugs
Atropine
48
Examples of Eicosanoid receptor drugs
Misoprostol, Montelukast
49
GPCRs are heterotrimeric T/F
T
50
G protein regulated effectors include enzymes such as
1. Adenyl Cyclase 2. Phospholipase C 3. cyclic GMP phosphodiesterase (PDE6) 4. membrane ion channels selective for Ca2+ and K+
51
GPCRs span the plasma membrane as a bundle of
7 alpha helices
52
Active alpha GTP returns to basal state by
RGS proteins
53
What enzymes bind agonist activated GPCRs and phosphorylate and regulate them?
1. GRKs 2. Arrestin
54
What alpha subunit activates AC
Gs
55
What alpha subunit inhibits AC
Gi
56
What alpha subunit activates all forms of PLC
Gq
57
G12/13 alpha subunits couple to
Guanine nucleotide exchange factors (GEFs)
58
Increased cAMP leads to PKA phosphorylation which leads to
1. Increased heart contraction 2. Smooth muscle relaxation 3. Glycogenolysis 4. Lipolysis
59
PLC: IP3-DAG pathway leads to the activation of
CCPK, MLCK, PKC -contraction -neuronal excitation -cell proliferation
60
Types of enzyme linked receptors
1. With intrinsic enzymatic activity 2. Without intrinsic enzymatic activity (but bind a JAK-STAT kinase on activation)
61
Example of enzyme linked receptors with intrinsic enzymatic activity
Receptor tyrosine kinase and a cytokine receptor
62
Functional family and effectors of transmembrane, non enzymes
Cytokine receptors; JAK/STAT
63
What proteins inhibit the JAK STat pathway
SOCs
64
JAKs transphorylate and lead to the phosphorylation of
STATs
65
Meaning of JAKs
Janus Kinases
66
Meaning of STATs
Signal Transducers and Activators of Transcription

Pharmacology (11 decks)

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