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Pharmacology > Pharmacodynamics > Flashcards

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
Q

Ephedrine + Theophylline

A

Additive - Bronchodilator

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26
Q

Acetylcholine + Physostigmine

A

Supraadditive - Inhibition of breakdown

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27
Q

Levodopa + Carbidopa/Benserazide

A

Supraadditive - Inhibition of peripheral metabolism

28
Q

Adrenaline + Cocaine/Desipramine

A

Supraadditive- Inhibition of neuronal uptake

29
Q

Sulfamethoxazole + trimethroprim

A

Supraadditive- Sequential blockade

30
Q

Antihypertensives (enalapril + hydrochlorothiazide)

A

Supraadditive - Tackling two contributory factors

31
Q

Tyramine + MAO inhibitors

A

Supraadditive- Increasing releasable CA store

32
Q

Physiological receptors have two functional domains

A

-ligand-binding domain
-effector domain

33
Q

Physiological ligands of ligand-gated ion channels

A

ACh(M2), GABA, 5-HT

34
Q

Examples of drugs that use ligand-gated ion channels

A

Nicotine, Gabapentin

35
Q

Voltage gated ion channels are activated by

A

Membrane Depolarization

36
Q

Drugs that use voltage gated ion channels

A

Lidocaine, Verapamil

37
Q

Receptors with intrinsic ion channel

A

GABAa, 5HT3, NMDA

38
Q

Blockers of L Voltage Sensitive Calcium channels

A
  1. Verapamil
  2. Dihydropyridine group of CCBs, Cd2+
39
Q

Blockers of T Voltage-Sensitive calcium channels

A
  1. Flunarizine
  2. Ethosuximide, Ni2+
40
Q

Blockers of N voltage sensitive calcium channels

A

Gabapentin, Cd2+

41
Q

Blockers of voltage sensitive P,Q & R calcium channels

A

Toxin from funnel web spider

42
Q

Structure of Nicotinic ACh receptor ion channel

A

5 receptor subunits (2 alpha, gamma, beta and delta) form a cluster surrounding a central transmembrane pore

43
Q

Each subunit of the ligand-gated nicotinic ach receptor pore has

A
  1. A large extra cellular domain
  2. Four transmembrane helices
44
Q

Functions families of gcprs

A
  1. Beta Adrenergic
  2. Muscarinic cholinergic
  3. Eicosanoid receptors
45
Q

Effectors of eicosanoid receptors

A

Gs, Gi and Gq proteins

46
Q

Example of Beta adrenergic receptor drugs

A

Dobutamine

47
Q

Examples of muscarinic cholinergic receptor drugs

A

Atropine

48
Q

Examples of Eicosanoid receptor drugs

A

Misoprostol, Montelukast

49
Q

GPCRs are heterotrimeric T/F

A

T

50
Q

G protein regulated effectors include enzymes such as

A
  1. Adenyl Cyclase
  2. Phospholipase C
  3. cyclic GMP phosphodiesterase (PDE6)
  4. membrane ion channels selective for Ca2+ and K+
51
Q

GPCRs span the plasma membrane as a bundle of

A

7 alpha helices

52
Q

Active alpha GTP returns to basal state by

A

RGS proteins

53
Q

What enzymes bind agonist activated GPCRs and phosphorylate and regulate them?

A
  1. GRKs
  2. Arrestin
54
Q

What alpha subunit activates AC

A

Gs

55
Q

What alpha subunit inhibits AC

A

Gi

56
Q

What alpha subunit activates all forms of PLC

A

Gq

57
Q

G12/13 alpha subunits couple to

A

Guanine nucleotide exchange factors (GEFs)

58
Q

Increased cAMP leads to PKA phosphorylation which leads to

A
  1. Increased heart contraction
  2. Smooth muscle relaxation
  3. Glycogenolysis
  4. Lipolysis
59
Q

PLC: IP3-DAG pathway leads to the activation of

A

CCPK, MLCK, PKC
-contraction
-neuronal excitation
-cell proliferation

60
Q

Types of enzyme linked receptors

A
  1. With intrinsic enzymatic activity
  2. Without intrinsic enzymatic activity (but bind a JAK-STAT kinase on activation)
61
Q

Example of enzyme linked receptors with intrinsic enzymatic activity

A

Receptor tyrosine kinase and a cytokine receptor

62
Q

Functional family and effectors of transmembrane, non enzymes

A

Cytokine receptors; JAK/STAT

63
Q

What proteins inhibit the JAK STat pathway

A

SOCs

64
Q

JAKs transphorylate and lead to the phosphorylation of

A

STATs

65
Q

Meaning of JAKs

A

Janus Kinases

66
Q

Meaning of STATs

A

Signal Transducers and Activators of Transcription

Pharmacology (11 decks)

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