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Unit 2 Pharm III > MOAs > Flashcards

MOAs Flashcards

1
Q

1st generation antihistmines

A

Compete with histamine, block muscarinic receptors (anticholinergic), enter brain

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2
Q

2nd generation antihistamines

A

Compete with histamine

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3
Q

Cromolyn

A

inhibits histamine release

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4
Q

Azelastine

A

decreases histamine release and also blocks receptors

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5
Q

Cetirizine

A

2nd generation antihistamine which also inhibits histamine release

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6
Q

Beta 2 agonists

A

Increase cAMP→ relax smooth muscle, inhibit histamine release from cell

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7
Q

Theophylline

A

Phosphodiesterase inhibitor→ increases cAMP
Blocks adenosine receptor
Relaxes smooth muscle, stimulates CNS + heart

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8
Q

Corticosteroids (for asthma)

A

Reverse: infiltration of inflammatory cells in epithelial cells, bronchoconstriction, mucus hypersecretion, epithelial permeability, epithelial destruction, and edema.

Reduced arachidonate metabolites

Increased B adrenergic tone (improved response to B agonists)

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9
Q

Zileuton

A

Leukotriene inhibitor:

Inhibits 5-lipoxygenase

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10
Q

Zafirlukast, Monteleukast

A

Leukotriene receptor antagonists

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11
Q

Omalizumab

A

Biologic

Monoclonal antibody to IgE high affinity Fc receptor→ prevents binding of IgE to cells associated with allergic response
Lowers free serum IgE concentrations

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12
Q

Cromolyn sodium, Nedocromil

A

Inhibit release of histamine from mast cells (degranulation) (not bronchodilators)

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13
Q

Sodium bicarbonate
Calcium carbonate
Magnesium hydroxide
Aluminum hydroxide

A

Inorganic bases, often divalent cations

Neutralize acid by directly binding to HCl

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14
Q

Used together to cancel out their effects, Magnesium hydroxide causes ______ and Aluminum hydroxide causes _____

A

Magnesium: Diarrhea
Aluminum: Constipation

Mg(OH)2 + 2 HCl = MgCl2 + 2 H2O

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15
Q

Sodium bicarbonate

A

Fast acting
NaHCO3 + HCl = CO2 + NaCl + H2O
CO2→ Burping

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16
Q

Calcium carbonate

A

CaCO3 + 2 HCl = CaCl2 + CO2 + H2O (CO2→ burp)

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17
Q

H2 antagonists

A

Decrease GI acid formation

through H2 receptor blockade

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18
Q

PPIs

A

Prodrugs→ activated in the parietal cell to sulfenamide→ Irreversible block of acid formation
Converted to S-OH which can bind the H+K+ ATPase

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19
Q

Misoprostol

A

Prostaglandin E1 analogue

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20
Q

Erythromycin (macrolide) as a prokinetic

A

stimulate motilin receptors→ contraction of GI tract (motilin=gastric stimulatory protein)

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21
Q

Metoclopramide

A

blocks D2 receptor (antagonist)→ blocks decreased motility action of DA on GI tract. Increase ACh release.

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22
Q

Neostigmine

A

AChE inhibitor→ more ACh stimulates M2 receptor→ increased GI tone + motility

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23
Q

Bethanechol

A

Muscarinic agonist M2 receptor→ increased GI tone + motility

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24
Q

Muscarinic antagonists as antispasmodics

Glycopyrrolate, dicyclomine

A

Block muscarinic receptors→ decrease GI spasms/cramping, decrease intestinal overactivity

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25
Q

Amitriptyline as an antispasmodic

A

Muscarinic block→ decreases
Spasms
Increased NE release→ stimulates α2 receptors in spinal cord→ decrease pain

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26
Q

Eluxadoline

A

Antispasmodic, opioid agonist (IBS-D)

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27
Q

Prochlorperazine, promethazine (anti-nausea)

A

Block DA, muscarinic, histamine receptors

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28
Q

Aprepitant

A

NK1 antagonist

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29
Q

Lactulose method of decreasing ammonia

A

decreases blood ammonia levels (preventing hepatic encephalopathy) by:
Conversion to lactic acid in gut lumen decreases pH → NH3 freely enters GI lumen→ converted to

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30
Q

Mucosal agents

A

Stimulate peristalsis

Enhance secretion/ inhibit absorption H2O

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31
Q

Lubricants/stool softeners

A

Increase bulk, Soften and lubricate stool. Not very effective.

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32
Q

Docusate

A

Emulsifies, increases water penetration→ softens. May increase water absorption (oral)

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33
Q

Glycerin suppository

A

lubricates distal end of bowel

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34
Q

Lubiprostone

A

Non-laxative drug for constipation

Prostaglandin E1 analogue→ Activates ClC-2 Cl- channels in luminal cells to increase fluid secretion

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35
Q

Linaclotide

A

Non-laxative drug for constipation
Activates guanylate cyclase C in
lumen→ Increased cGM→ activates cystic
fibrosis transmembrane conductor (CFTR) → increases secretion of Cl- and fluid into the lumen

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36
Q

Bismuth subsalicylate

A

Absorbs water + pathogens→ “Traveller’s diarrhea”

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37
Q

Loperamide (Imodium)

A

Opioid for diarrhea

does not enter CNS, low abuse potential

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38
Q

Diphenoxylate/atropine (Lomotil)

A

Opioid for diarrhea

opioid with atropine reduces abuse potential, increases effectiveness

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39
Q

Simethicone

A

Coats gas, dissipates it→ decreases bloating, flatulence

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40
Q

Sulfasalazine (GI)

A

5-Aminosalicylic acid plus sulfapyridine

Decrease inflammation local to the colon in IBD

Bacteria in GI tract activate it by cleaving the linkage to sulfapyridine

Used for Rheumatoid arthritis inflammation

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41
Q

TNF-alpha blockers (GI)

A

Anti-inflammatory for IBD

42
Q

COX-1

A

Promotes inflammation
Protects against gastric irritation (by mucus secretion)
Promotes platelet aggregation (TXA2)
Vasoconstriction (TXA2)

43
Q

COX-2

A

Promotes inflammation
Protects against gastric irritation
Inhibits platelet aggregation (PGI2)
Vasodilation (PGI2 )

44
Q

Thromboxane (TXA2)

A

Produced from Arachidonic acid by COX

Leukocyte modulation and inflammation, potent vasoconstriction

45
Q

Prostacyclin

A

Produced from Arachidonic acid by COX

Vasodilation

46
Q

Prostaglandins (PGI2)

A

Produced from Arachidonic acid by COX

Inhibit platelet aggregation
Vasodilation

47
Q

Shared effects of Leukotrienes, PGs, TXA

A

Alteration of vascular permeability, bronchial constriction, increased secretion→ bronchospasm, congestion, mucosal plugging

48
Q

Leukotrienes

A

Not produced by COX enzymes, not affected by NSAIDs.

49
Q

Mechanism of Aspirin Asthma

A

Leukotriene is able to bronchoconstrict without opposition due to inhibition of COX enzymes production of PGs

50
Q

Aspirin

A

Irreversible inhibitor of COX-1 and 2

51
Q

NSAIDS

A

Reversible inhibitors of COX-1 and 2

52
Q

Celecoxib

A

Reversible inhibitor of COX 2 (specific)

53
Q

Acetaminophen

A

Not technically an NSAID?

Antipyretic action
Analgesic action

No anti-inflammatory action or platelet effects

54
Q

Low dose ASA + Uric acid

A

decrease uric acid excretion and elevates plasma urate concentration, worsening gout

55
Q

High dose ASA + Uric acid

A

enhances uric acid excretion (uricosuria) and lowers the plasma urate levels, alleviating gout symptoms

56
Q

Platelet effects of ASA

A

Irreversible inhibition of COX enzymes takes 8-10 day to replace. (specifically COX-2 production of PGI2)

57
Q

Other effects of indomethacin

A

Reduce PMN migration

Inhibit phospholipase A

58
Q

Other effects of Diclofenac

A

Decreases arachidonic acid bioavailability

59
Q

Other effects of Piroxicam and Meloxicam

A

Inhibit PMN migration and lymphocyte function

Decrease oxygen radical production

60
Q

What causes dose dependent fatal hepatic necrosis in acetaminophen toxicity?

A

Hydroxylated intermediate metabolite causes the damage

When circulating metabolites
exceed the available reduced glutathione in the body→ cannot neutralize toxic metabolite

Worsened with chronic ETOH

61
Q

H1 receptor

A

Gq coupled

Allergic response

Smooth muscle→ Endothelium→Activates NO→Vasodilation

Brain (neurotransmitter)
Wakefulness
Appetite control

62
Q

H2 Receptor

A

Gs coupled→ increases cAMP

Gastric acid secretion
Heart, brain, mast cells
+/- Vasodilation (beta2)

63
Q

H3 receptor

A

Presynaptic in brain

Inhibits release of neurotransmitters, histamine/- promote sleep

64
Q

H4 receptor

A

Leukocytes, eosinophils, neutrophils

+/- Stimulate chemotaxis in inflammation, allergic reactions

65
Q

H3 and H4 receptors are coupled to

A

Gi→ decrease cAMP

66
Q

How do 1st generation antihistamines counter motion sickness?

A

They have anticholinergic effects, and cross blood brain barrier

67
Q

Gold salts

A

Inhibition of phagocytosis.

Uncouple oxidative phosphorylation and inhibit cellular respiration.

Stabilize lysosomal membranes and inhibit actions of lysosomal enzymes.

React with proteins (e.g., sulfahydryl groups).

Inhibit proteolytic enzymes of leukocytes.

Prevent prostaglandin synthesis.

Suppress cellular immunity.

68
Q

Penicillamine

A

Chelating agent

Resembles gold compounds

69
Q

Hydroxychloroquine

A

Antihistaminic, anticholinesterase, and antiprotease properties.

Inhibits prostaglandin synthesis.

Inhibits biosynthesis of mucopolysaccharide.

Inhibits responses to chemotactic stimuli and
phagocytosis.

Stabilizes lysosomes.

Reacts with nucleic acids and tissue proteins.

70
Q

Infliximab

A

Chimeric IgG1k monoclonal antibody targeted against tumor

necrosis factor-alpha (TNF-alpha).

71
Q

Adalimumab

A

Recombinant human IgG1 monoclonal antibody
Human-derived heavy and light chain variable regions and human IgG1:κ constant regions (100% human peptide sequences).
Specific for tumor necrosis factor-alpha (TNF-alpha)

72
Q

Certolizumab pegol

A

humanized antibody, potent neutralizer of TNF-alpha

73
Q

Golimumab

A

human-derived monoclonal antibody with human-derived variable and constant regions TNF alpha

74
Q

Etanercept

A

Recombinant DNA technology→ dimeric fusion protein

Consists of the extracellular ligand-binding portion of the
human 75 kilodalton (p75) tumor necrosis factor (TNF) receptor linked to the Fc portion of human IgG1

Inhibits TNF

75
Q

Rituximab

A

Genetically engineered chimeric murine/human monoclonal antibody
IgG immunoglobulin containing murine light- and heavy-chain
variable regions and human constant regions

Binds specifically to CD20 antigen, a on pre-B and mature B-lymphocytes→ blocks differentiation

Expressed on B-cells in non-Hodgkin’s lymphoma
(Not on hematopoietic stem cells, pro-B cells, normal
plasma cells or other normal tissues)

76
Q

Leflunomide

A

Inhibits dihydroorotate dehydrogenase (DHODH), in cell mitochondria, catalyzes a key step in de novo pyrimidine synthesis

Secondary MOA→ inhibition of cytokine and growth factor receptor associated tyrosine kinase activity
Inhibits the induction of cyclooxygenase-2 (COX-2)

77
Q

Abatacept

A

Fully human recombinant fusion protein, costimulatory or second-signal blocker of T cell activation

Competes with CD28 (on T cell) for CD80 and CD86 (on APC) binding

Disturbs a key mechanisms of inflammation and progressive joint
destruction in rheumatoid arthritis

T cells mediate cellular immune responses→ may affect host defenses against infections and malignancies

78
Q

Mycophenolate mofetil

A

Prodrug for the immunosuppressive agent mycophenolic acid
(MPA)
Inhibits lymphocyte purine synthesis by reversibly and noncompetitively inhibiting the enzyme inosine monophosphate
dehydrogenase (IMPDH)

79
Q

Anakira

A

Recombinant, non glycosylated form of the human interleukin-1 receptor antagonist (IL-1Ra)

80
Q

Toclizumab

A

humanized interleukin-6 (IL-6) receptor-inhibiting monoclonal antibody→ competes with IL-6 for binding to the IL-6 receptor

81
Q

Tofacitinib

A

Inhibits JAK1 and JAK3 > JAK2

82
Q

Baricitinib

A

JAK kinase inhibitor 1 + 2 >3

83
Q

All the TNF alpha drugs:

A 
Infliximab
Adalimumab
Certolizumab pegol
Golimumab
Etanercept
84
Q

p75 of TNF receptor

A

Etanercept

85
Q

Binds CD20 antigen on B cells, preventing differentiation and proliferation

A

RItuximab

86
Q

Compete with CD23 for CD80 and CD86 binding on APCs

A

Abatacept

87
Q

Inhibits dihydroorate dehydrogenase and COX2

A

Leflunomide

88
Q

Inhibits monophosphate dehydrogenase, inhibiting lymphocyte purine synthesis

A

Mycophenolate mofetil

89
Q

Blocks IL-1

A

Anakira

90
Q

Blocks IL-6

A

Tocilizumab

91
Q

“Triptans”

A

5-HT1D agonist on small peripheral nerves
Suppresses release of sensory neuropeptides
Less vasoconstriction than ergotamine

92
Q

Ergotamine

A

Acts on 5-HT receptors

Partial agonist on alpha 1 receptors→ vasoconstriction (more than triptans)

93
Q

Caffeine increases its absorption and potentiates its effects

A

Ergotamine

94
Q

Erenumab

Galcanezumab

A

IgG2 monoclonal antibody binds calcitonin gene-related peptide (CGRP)
Migraine prophylaxis

95
Q

Colchicine

A

Binds to tubulin→ inhibits assembly of microtubules

Anti-inflammatory by inhibiting leukocyte migration and phagocytosis

Inhibits formation of leukotriene B4

96
Q

Probenecid

A

Blocks active reabsorption of uric acid in proximal tubule→ increase the urinary excretion of uric acid

97
Q

Lesinurad

A

Urate transporter (URAT1) inhibitor

98
Q

Allopurinol

Febuxostat

A

Inhibit xanthine oxidase→ inhibit synthesis of uric acid→ effective in primary and secondary gout

99
Q

Rasburicase

A

Recombinant form of urate oxidase (not endogenous in humans) → catalyzes oxidation of uric acid to allantoin→ readily excreted metabolite

100
Q

Pegloticase

A

Pegylated, recominbant, mammalian urate oxidase enzyme→ uric acid to allantoin

Unit 2 Pharm III (8 decks)

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