Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Unit 2 Pharm III > MOAs > Flashcards

MOAs Flashcards

1
Q

1st generation antihistmines

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

2nd generation antihistamines

A

Compete with histamine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Cromolyn

A

inhibits histamine release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Azelastine

A

decreases histamine release and also blocks receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Cetirizine

A

2nd generation antihistamine which also inhibits histamine release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Beta 2 agonists

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Theophylline

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Zileuton

A

Leukotriene inhibitor:

Inhibits 5-lipoxygenase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Zafirlukast, Monteleukast

A

Leukotriene receptor antagonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Cromolyn sodium, Nedocromil

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Sodium bicarbonate
Calcium carbonate
Magnesium hydroxide
Aluminum hydroxide

A

Inorganic bases, often divalent cations

Neutralize acid by directly binding to HCl

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Sodium bicarbonate

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Calcium carbonate

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

H2 antagonists

A

Decrease GI acid formation

through H2 receptor blockade

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Misoprostol

A

Prostaglandin E1 analogue

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Erythromycin (macrolide) as a prokinetic

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Metoclopramide

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Neostigmine

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Bethanechol

A

Muscarinic agonist M2 receptor→ increased GI tone + motility

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Muscarinic antagonists as antispasmodics

Glycopyrrolate, dicyclomine

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Amitriptyline as an antispasmodic
Muscarinic block→ decreases Spasms Increased NE release→ stimulates α2 receptors in spinal cord→ decrease pain
26
Eluxadoline
Antispasmodic, opioid agonist (IBS-D)
27
Prochlorperazine, promethazine (anti-nausea)
Block DA, muscarinic, histamine receptors
28
Aprepitant
NK1 antagonist
29
Lactulose method of decreasing ammonia
decreases blood ammonia levels (preventing hepatic encephalopathy) by: Conversion to lactic acid in gut lumen decreases pH → NH3 freely enters GI lumen→ converted to
30
Mucosal agents
Stimulate peristalsis | Enhance secretion/ inhibit absorption H2O
31
Lubricants/stool softeners
Increase bulk, Soften and lubricate stool. Not very effective.
32
Docusate
Emulsifies, increases water penetration→ softens. May increase water absorption (oral)
33
Glycerin suppository
lubricates distal end of bowel
34
Lubiprostone
Non-laxative drug for constipation | Prostaglandin E1 analogue→ Activates ClC-2 Cl- channels in luminal cells to increase fluid secretion
35
Linaclotide
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
36
Bismuth subsalicylate
Absorbs water + pathogens→ “Traveller’s diarrhea”
37
Loperamide (Imodium)
Opioid for diarrhea | does not enter CNS, low abuse potential
38
Diphenoxylate/atropine (Lomotil)
Opioid for diarrhea | opioid with atropine reduces abuse potential, increases effectiveness
39
Simethicone
Coats gas, dissipates it→ decreases bloating, flatulence
40
Sulfasalazine (GI)
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
41
TNF-alpha blockers (GI)
Anti-inflammatory for IBD
42
COX-1
Promotes inflammation Protects against gastric irritation (by mucus secretion) Promotes platelet aggregation (TXA2) Vasoconstriction (TXA2)
43
COX-2
Promotes inflammation Protects against gastric irritation Inhibits platelet aggregation (PGI2) Vasodilation (PGI2 )
44
Thromboxane (TXA2)
Produced from Arachidonic acid by COX Leukocyte modulation and inflammation, potent vasoconstriction
45
Prostacyclin
Produced from Arachidonic acid by COX Vasodilation
46
Prostaglandins (PGI2)
Produced from Arachidonic acid by COX Inhibit platelet aggregation Vasodilation
47
Shared effects of Leukotrienes, PGs, TXA
Alteration of vascular permeability, bronchial constriction, increased secretion→ bronchospasm, congestion, mucosal plugging
48
Leukotrienes
Not produced by COX enzymes, not affected by NSAIDs.
49
Mechanism of Aspirin Asthma
Leukotriene is able to bronchoconstrict without opposition due to inhibition of COX enzymes production of PGs
50
Aspirin
Irreversible inhibitor of COX-1 and 2
51
NSAIDS
Reversible inhibitors of COX-1 and 2
52
Celecoxib
Reversible inhibitor of COX 2 (specific)
53
Acetaminophen
Not technically an NSAID? Antipyretic action Analgesic action **No anti-inflammatory action or platelet effects**
54
Low dose ASA + Uric acid
decrease uric acid excretion and elevates plasma urate concentration, worsening gout
55
High dose ASA + Uric acid
enhances uric acid excretion (uricosuria) and lowers the plasma urate levels, alleviating gout symptoms
56
Platelet effects of ASA
Irreversible inhibition of COX enzymes takes 8-10 day to replace. (specifically COX-2 production of PGI2)
57
Other effects of indomethacin
Reduce PMN migration | Inhibit phospholipase A
58
Other effects of Diclofenac
Decreases arachidonic acid bioavailability
59
Other effects of Piroxicam and Meloxicam
Inhibit PMN migration and lymphocyte function | Decrease oxygen radical production
60
What causes dose dependent fatal hepatic necrosis in acetaminophen toxicity?
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
H1 receptor
Gq coupled Allergic response Smooth muscle→ Endothelium→Activates NO→Vasodilation Brain (neurotransmitter) Wakefulness Appetite control
62
H2 Receptor
Gs coupled→ increases cAMP Gastric acid secretion Heart, brain, mast cells +/- Vasodilation (beta2)
63
H3 receptor
Presynaptic in brain | Inhibits release of neurotransmitters, histamine/- promote sleep
64
H4 receptor
Leukocytes, eosinophils, neutrophils | +/- Stimulate chemotaxis in inflammation, allergic reactions
65
H3 and H4 receptors are coupled to
Gi→ decrease cAMP
66
How do 1st generation antihistamines counter motion sickness?
They have anticholinergic effects, and cross blood brain barrier
67
Gold salts
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
Penicillamine
Chelating agent | Resembles gold compounds
69
Hydroxychloroquine
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
Infliximab
Chimeric IgG1k monoclonal antibody targeted against tumor | necrosis factor-alpha (TNF-alpha).
71
Adalimumab
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
Certolizumab pegol
humanized antibody, potent neutralizer of TNF-alpha
73
Golimumab
human-derived monoclonal antibody with human-derived variable and constant regions TNF alpha
74
Etanercept
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
Rituximab
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
Leflunomide
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
Abatacept
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
Mycophenolate mofetil
Prodrug for the immunosuppressive agent mycophenolic acid (MPA) Inhibits lymphocyte purine synthesis by reversibly and noncompetitively inhibiting the enzyme inosine monophosphate dehydrogenase (IMPDH)
79
Anakira
Recombinant, non glycosylated form of the human interleukin-1 receptor antagonist (IL-1Ra)
80
Toclizumab
humanized interleukin-6 (IL-6) receptor-inhibiting monoclonal antibody→ competes with IL-6 for binding to the IL-6 receptor
81
Tofacitinib
Inhibits JAK1 and JAK3 > JAK2
82
Baricitinib
JAK kinase inhibitor 1 + 2 >3
83
All the TNF alpha drugs:
``` Infliximab Adalimumab Certolizumab pegol Golimumab Etanercept ```
84
p75 of TNF receptor
Etanercept
85
Binds CD20 antigen on B cells, preventing differentiation and proliferation
RItuximab
86
Compete with CD23 for CD80 and CD86 binding on APCs
Abatacept
87
Inhibits dihydroorate dehydrogenase and COX2
Leflunomide
88
Inhibits monophosphate dehydrogenase, inhibiting lymphocyte purine synthesis
Mycophenolate mofetil
89
Blocks IL-1
Anakira
90
Blocks IL-6
Tocilizumab
91
"Triptans"
5-HT1D agonist on small peripheral nerves Suppresses release of sensory neuropeptides Less vasoconstriction than ergotamine
92
Ergotamine
Acts on 5-HT receptors | Partial agonist on alpha 1 receptors→ vasoconstriction (more than triptans)
93
Caffeine increases its absorption and potentiates its effects
Ergotamine
94
Erenumab | Galcanezumab
IgG2 monoclonal antibody binds calcitonin gene-related peptide (CGRP) Migraine prophylaxis
95
Colchicine
Binds to tubulin→ inhibits assembly of microtubules Anti-inflammatory by inhibiting leukocyte migration and phagocytosis Inhibits formation of leukotriene B4
96
Probenecid
Blocks active reabsorption of uric acid in proximal tubule→ increase the urinary excretion of uric acid
97
Lesinurad
Urate transporter (URAT1) inhibitor
98
Allopurinol | Febuxostat
Inhibit xanthine oxidase→ inhibit synthesis of uric acid→ effective in primary and secondary gout
99
Rasburicase
Recombinant form of urate oxidase (not endogenous in humans) → catalyzes oxidation of uric acid to allantoin→ readily excreted metabolite
100
Pegloticase
Pegylated, recominbant, mammalian urate oxidase enzyme→ uric acid to allantoin

Unit 2 Pharm III (8 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions