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Pharmacology > Block 4 > Flashcards

Block 4 Flashcards

1
Q

Methotrexate

A

Antimetabolite (Chemotherapy)

  • folate analog, binds to dihydrofolate reductase (DHFR) resulting in inhibition of tetrahydrofolate (THF)
  • converted to a series of polyglutamates for therapeutic action
  • NEPHROTOXICITY
  • treats breast cancer, RA, psoriasis
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2
Q

Leucovorin

A

Methotrexate rescue

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3
Q

Cyclophosphamide

A

Alkylating Agent (Chemotherapy)

  • alkylates N7 position of guanine twice, creating a cross link, inhibits DNA synth
  • must be activated by cytochrome P450
  • metabolite acrolein causes severe cystitis
  • treats breast cancer, RA, MS
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4
Q

Mesna

A

Cyclophosphamide rescue

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5
Q

Cisplatin

A

Alkylating Agent (Chemotherapy)

  • alkylates N7 position of guanine twice, creating a cross link, inhibits DNA synth
  • kills tumor cells at all stages
  • PT MUST BE GIVEN SALINE SOLUTION BEFORE, DURING, AND AFTER ADMIN TO AVOID NEPHROTOXICITY
  • treats solid tumors
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6
Q

Doxorubicin (Hydroxydaunorubicin)

A

Cytotoxic Antibiotic (Chemotherapy)

  1. Inhibit Topoisomerase II
  2. High affinity DNA binding through INTERCALATION, blocks DNA/RNA synth
  3. Free radical generation
  4. Bind cellular membranes to alter fluidity and ion transport
    - urine may turn bright red
    - can cause cardiotoxicity
    - treats breast cancer
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7
Q

Vincristine (Oncovin)

A

Microtubule Inhibitor (Chemotherapy)

  • disrupts microtubule assembly and causes mitotic arrest in M phase –> cell death
  • metabolized by cytochrome P450
  • Nephrotoxicity with neuropathy
  • BLISTERS (vesicant)
  • treats acute lymphoblastic leukemia
  • derived from periwinkle plant
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8
Q

Paclitaxel

A

Microtubule Inhibitor (Chemotherapy)

  • binds microtubules with enhanced tubular polymerization causing mitotic arrest
  • metabolized by cytochrome P450
  • peripheral neuropathy, hypersensitivity, myalgia, arthralgia, HAND-FOOT SYNDROME
  • treats solid tumors and breast cancer
  • derived from yew plant
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9
Q

Imatinib

A

Protein Kinase Inhibitor (Chemotherapy)

  • TARGETED THERAPY
  • inhibits Bcr-Abl Tyrosine Kinase and other receptor kinases, prevents kinase phosphorylation
  • CYP3A4 metabolism
  • fluid retention with ankle and periorbital edema
  • treats Philadelphia chromosome, chronic leukemia, GI stromal tumor
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10
Q

Trastuzumab

A

HER2/neu Receptor Antibodies (Chemotherapy)

  • IMMUNOTHERAPY/TARGETED THERAPY
  • monoclonal antibody interfering with HER2/neu receptor which inhibits epidermal growth factor (HER2 expressed 100x more in cancer cells)
  • binds to domain IV of extracellular segment of HER2 and arrests cells in G1 phase
  • causes cardiac dysfunction
  • treats HER2-positive breast cancer
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11
Q

Prednisone

A

Glucocorticoid Receptor Agonist (Chemotherapy)

  • inhibit leukocyte infiltration
  • interfere with inflammatory response mediators
  • suppresses immune response
  • reduce edema and scar tissue
  • must be converted to prednisolone in liver to become activated
  • causes Cushing like symptoms
  • treats acute lymphoblastic leukemia, UC, Crohns
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12
Q

CHOP Therapy

A
  1. Cyclophosphamide
  2. Doxorubicin (Hydroxydaunorubicin)
  3. Vincristine (Oncovin)
  4. Prednisone

treats non-Hodgkin lymphoma

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13
Q

Misoprostol

A

Gastric Acid Suppressant / Mucosal Lining Protectant

  • Prostaglandin analog
  • binds to EP3 receptors on parietal cells to inhibit cAMP and H-K ATPase acid secretion
  • binds to EP3 to increase mucin and bicarbonate secretion from epithelial cells
  • extensive first pass metabolism to principle metabolite misoprostol acid
  • high incidence of adverse effects: diarrhea, IBD exacerbation, INDUCES ABORTION
  • can protect from NSAID mucosal injury
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14
Q

Omeprazole

A

PPI

  • Inhibits H-K ATPase, prevents acid production
  • promotes healing for gastric ulcer, GERD
  • require multiple doses for full effect
  • subject to CYP3A4 metabolism, inhibits CYP2C19
  • inhibits Cytochrome P450 and increases other drugs half lives
  • can cause acid rebound if discontinued
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15
Q

Pantoprazole

A

PPI

  • Inhibits H-K ATPase, prevents acid production
  • promotes healing for gastric ulcer, GERD
  • require multiple doses for full effect
  • subject to CYP3A4 and CYP2C19 metabolism
  • inhibits Cytochrome P450 and increases other drugs half lives
  • can cause acid rebound if discontinued
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16
Q

Cimetidine

A

H2 Antagonist

  • reversibly binds H2 receptors, inhibits H2 activation of cAMP and the activation of H-K ATPase
  • most effective against nocturnal secretion
  • cause gynecomastia and impotence in males
  • CAN DEVELOP TOLERANCE
  • displaces dihydrotestosterone from binding sites and inhibits P450 metabolism of estrogen, other drugs
  • can cause acid rebound if discontinued
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17
Q

Famotidine

A

H2 Antagonist

  • reversibly binds H2 receptors, inhibits H2 activation of cAMP and the activation of H-K ATPase
  • most effective against nocturnal secretion
  • cause gynecomastia and impotence in males
  • CAN DEVELOP TOLERANCE
  • virtually no drug interactions
  • can cause acid rebound if discontinued
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18
Q

Sucralfate

A

Mucosal Lining Protectant

  • made of aluminum hydroxide
  • cross links in pH <4 to create a viscous, sticky polymer to coat the stomach lining
  • causes constipation
  • used when limited response to PPI or with ulcers
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19
Q

Sodium Bicarbonate

A

Antacid

  • neutralize acid, don’t block secretion
  • increases pH from 1 to 3.5, short action
  • decreases absorption of other drugs
  • causes alkalosis with excessive use
  • PRODUCES CO2 GAS
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20
Q

Calcium Carbonate

A

Antacid

  • neutralize acid, don’t block secretion
  • increases pH from 1 to 3.5, short action
  • decreases absorption of other drugs
  • causes systemic alkalosis with excessive use
  • PRODUCES CO2 GAS, causes constipation, acid rebound
  • LONG ACTING
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21
Q

Magnesium Hydroxide

A

Antacid

  • neutralize acid, don’t block secretion
  • increases pH from 1 to 3.5, short action
  • decreases absorption of other drugs
  • causes diarrhea
  • increases plasma magnesium and can lead to CNS toxicity
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22
Q

Aluminum Hydroxide

A

Antacid

  • neutralize acid, don’t block secretion
  • increases pH from 1 to 3.5, short action
  • decreases absorption of other drugs
  • causes constipation, nephrotoxicity, myopathy
  • REDUCES PHOSPHATE REABSORPTION –> removes calcium from bone and weakens it
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23
Q

Magnesium-Aluminum Combo

A

Antacid

  • neutralize acid, don’t block secretion
  • increases pH from 1 to 3.5, short action
  • decreases absorption of other drugs
  • DOES NOT CAUSE CONSTIPATION OR DIARRHEA
  • exposed to 2 cations, problem if renal function is decreased
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24
Q

H. Pylori treatment options

A

A: x 7 days
1. PPI or H2 antagonist
2. Amoxicillin
3. Clarithromycin or Metronidazole

B: x 7 days
1. PPI
2. Tetracycline
3. Bismuth
4. Metronidazole

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25
Q

Domperidone

A

Prokinetic - enhance GI motility

  • Dopamine antagonist, enhances Ach release
  • inhibit emesis via CTZ (chemoreceptor trigger zone)
  • no extrapyramidal effects, but can increase prolactin release
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26
Q

Metoclopramide

A

Prokinetic AND Antiemetic

  • Dopamine antagonist
  • doesn’t affect lower GI motility
  • also a 5-HT3 antagonist/5-HT4 agonist (increase ACh)
  • extrapyramidal effects –> tardive dyskinesia
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27
Q

Dicyclomine

A

Antispasmodic - enhance GI motility

  • block M2 cholinergic receptor in enteric plexus to inhibit motility
  • limited side effects at low dose
  • high doses cause dry mouth, visual disturbance, constipation, urinary retention
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28
Q

Hycosamine

A

Antispasmodic - inhibit GI motility

  • block M2 cholinergic receptor in enteric plexus to inhibit motility
  • limited side effects at low dose
  • high doses cause dry mouth, visual disturbance, constipation, urinary retention
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29
Q

Meclizine

A

Antiemetic - Antihistamine (H1R Antagonist)

  • depress labyrinth excitability in ear
  • can cause CNS depression
  • good for motion sickness
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30
Q

Doxylamine (+ pyridoxine)

A

Antiemetic - Antihistamine (H1R Antagonist)

  • depress labyrinth excitability in ear
  • can cause CNS depression
  • good for motion sickness
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31
Q

Diphenhydramine

A

Antiemetic - Antihistamine (H1R Antagonist)

  • depress labyrinth excitability in ear
  • can cause CNS depression
  • good for motion sickness
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32
Q

Promethazine

A

Antiemetic - Antihistamine (H1R Antagonist)

  • ALSO BLOCKS D2 RECEPTORS
  • depress labyrinth excitability in ear
  • can cause CNS depression
  • good for motion sickness
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33
Q

Scopolamine

A

Antimuscarinic Antiemetic

  • block M2 receptors in CTZ
  • anti-muscarinic side effects (dry mouth, constipation, hallucination, fever)
34
Q

Prochlorperazine

A

Antimuscarinic Antiemetic

  • block M2 receptors in CTZ
  • anti-muscarinic side effects (dry mouth, constipation, hallucination, fever)
35
Q

Ondansetron

A

5-HT Receptor Antagonist Antiemetic

  • treats N/V post-op or in chemo
  • selective 5-HT3 antagonist
  • itch, rash, constipation, fever
36
Q

Bismuth

A

Antidiarrheal

  • forms salicylic acid and a bismuth clay in stomach acid to absorb water and protect stomach
  • treats Traveler’s diarrhea
  • blackens stool and may darken tongue
37
Q

Loperamide

A

Antidiarrheal

  • Mu opioid receptor agonist (decrease intestinal motility and increase absorption)
  • low abuse potential, low CNS penetration
  • use for less than 48 hrs, can cause CNS depression
  • don’t use with inflammatory bowel disease
38
Q

Anthraquinone

A

Laxative

  • causes cramping and inflammation
  • can get into breast milk
  • can cause “Lazy Bowel Syndrome” with abuse
39
Q

Diphenylmethane

A

Laxative

  • can cause bowel inflammation
40
Q

Aspirin

A

NSAID (Anti-inflammatory)

  • irreversible COX1 and COX2 inhibitor
  • inhibits COX1 at low dose, both at high dose
  • platelet inhibition and vasodilation at low doses
  • causes gastric ulcers, bleeding, Reyes syndrome, hepatotoxicity
  • no for kids with viral infections (Reyes / CNS)
  • no in pregnancy (decrease placental volume) or gout
  • no tolerance
41
Q

Ibuprofen

A

NSAID (Anti-inflammatory)

  • nonselective COX1 and COX2 reversible inhibitor
  • causes gastric ulcers, MI, stroke, HF, bleeding, renal impairment
  • no in pregnancy or gout
  • no tolerance
42
Q

Naproxen

A

NSAID (Anti-inflammatory)

  • nonselective COX1 and COX2 reversible inhibitor
  • longer duration of action
  • causes gastric ulcers, MI, stroke, HF, bleeding, renal impairment
  • no in pregnancy or gout
  • no tolerance
43
Q

Diclofenac

A

NSAID (Anti-inflammatory)

  • nonselective COX1 and COX2 reversible inhibitor
  • causes gastric ulcers, MI, stroke, HF, bleeding, renal impairment
  • no in pregnancy or gout
  • no tolerance
44
Q

Meloxicam

A

NSAID (Anti-inflammatory)

  • predominant COX2 reversible inhibitor
  • causes gastric ulcers, MI, stroke, HF, bleeding, renal impairment
  • no in pregnancy or gout
  • no tolerance
45
Q

Celecoxib

A

NSAID (Anti-inflammatory)

  • selective COX2 reversible inhibitor
  • more CV risks due to platelet aggregation and vasoconstriction via TXA2
  • little GI or renal effects
  • no in pregnancy or gout
  • no tolerance
46
Q

Acetaminophen

A

Anti-inflammatory

  • treats pain and fever but NOT inflammation
  • little platelet effects, little GI effects
  • overdose causes fatal hepatic necrosis
47
Q

N-Acetylcysteine

A

antidote to acetaminophen poisoning

48
Q

Azathioprine

A

Antimetabolite (Anti-Inflammatory and Immunosuppressant)

  • purine analog inhibits gene translation of immune cells
  • bone marrow suppression, increased infection risk
  • contraindicated in pregnancy
  • targets inflammation and its destructive process
49
Q

Methotrexate

A

Antimetabolite (Anti-Inflammatory and Immunosuppressant)

  • folate analog inhibits gene translation of immune cells via dihydrofolate reductase inhibition
  • cytotoxic
  • contraindicated in pregnancy
  • targets inflammation and its destructive process
50
Q

Infliximab

A

DMARD - TNF-alpha Inhibitor

  • can cause anaphylaxis or lupus like syndrome
  • increased risk for malignancies and infection
  • used for RA or Crohns
51
Q

Etanercept

A

DMARD - TNF-alpha Inhibitor

  • increased risk for malignancies and infection
52
Q

Abatacept

A

DMARD - T-Cell Modulation

  • increased risk for malignancies and infection
53
Q

Rituximab

A

DMARD - B-Cell Cytotoxic Agent

  • increased risk for malignancies and infection
54
Q

Colchicine

A

Gout (Anti-Inflammatory)

  • mitotic inhibitor
  • used when NSAIDs ineffective
  • not uricosuric
  • GI distress, myopathy, neuropathy
55
Q

Anakinra

A

DMARD - IL-1 Inhibition

  • increased risk for malignancies and infection
56
Q

Probenecid

A

Gout (Anti-Inflammatory)

  • uricosuric
  • precipitate uric acid crystals in renal tubules
  • GI irritation with peptic ulcers, hypersensitivity
57
Q

Allopurinol

A

Gout (Anti-Inflammatory)

  • inhibit xanthine oxidase
  • decrease uric acid production
  • fever, malaise, muscle aches
58
Q

Sumatriptan

A

Migraine - 5HT1 Agonist

  • acute migraine treatment
  • direct vasoconstriction intracranially, inhibits sensory neurons presynaptically
  • serious CV complications
  • contraindicated in heart disease, MAOi, or SSRI/SNRI
59
Q

Rimegepant

A

Migraine - CGRP Antagonist

  • inhibit the CGRP receptor
  • acute migraine treatment

(CGRP are small molecules tied directly to migraine activity)

60
Q

Fremanezumab

A

Migraine - CGRP Antibody

  • monoclonal Ab to the CGRP receptor
  • MIGRAINE PROPHYLAXIS
  • no current contraindications
  • causes URIs and injection site reactions
61
Q

Cortisone

A

Glucocorticoid (Immunosuppressant)

  • must be activated by IIB-hydroxysteroid dehydrogenase I
  • toxic in long term use
  • reduce cytokine release, decrease inflammation
  • increase blood glucose, increase muscle catabolism (amino acids in blood), increase lipolysis (Trigs in blood)
  • major side effect profile: Cushing disease, osteoporosis/bone growth suppression, myopathy
62
Q

Prednisone

A

Glucocorticoid (Immunosuppressant)

  • must be activated by IIB-hydroxysteroid dehydrogenase I
  • toxic in long term use
  • reduce cytokine release, decrease inflammation
  • increase blood glucose, increase muscle catabolism (amino acids in blood), increase lipolysis (Trigs in blood)
  • major side effect profile: Cushing disease, osteoporosis/bone growth suppression, myopathy
63
Q

Dexamethasone

A

Glucocorticoid (Immunosuppressant)

  • no mineralocorticoid activity, about 18x more potent than cortisol
  • toxic in long term use
  • reduce cytokine release, decrease inflammation
  • increase blood glucose, increase muscle catabolism (amino acids in blood), increase lipolysis (Trigs in blood)
  • major side effect profile: Cushing disease, osteoporosis/bone growth suppression, myopathy
64
Q

Cyclosporine A

A

IL-2 Synthesis Inhibition (Immunosuppressant)

  • binds to cyclophilin and then to calcineurin to inhibit IL-2 production via NFAT inactivation
  • metabolized by CYP3A
  • NEPHROTOXIC, hepatotoxic, neurotoxic
  • for severe RA or organ transplants
65
Q

Tacrolimus

A

IL-2 Synthesis Inhibition (Immunosuppressant)

  • binds FK Binding Protein (FKBP) and then to calcineurin to inhibit IL-2 production via NFAT inactivation
  • metabolized by CYP3A
  • NEPHROTOXIC, neurotoxic
  • for sever RA or organ transplants
66
Q

Sirolimus (Rapamycin)

A

IL-2 Signaling Inhibition (Immunosuppressant)

  • binds FK Binding Protein (FKBP) and then blocks IL-2 receptor signaling by blocking mTOR
  • metabolized by CYP3A
  • USED FOR PT AT RISK FOR NEPHROTOXICITY
  • leukopenia, thrombocytopenia
67
Q

Mycophenolic Acid

A

Antimetabolite (Immunosuppressant)

  • inhibits IMPDH, the rate limiting enzyme for guanosine formation
  • preferentially affects lymphocytes because of their high IMPDH expression
  • can’t use with Azathioprine
  • causes vomiting, diarrhea, leukopenia
68
Q

Anti-Thymocyte Globulin (ATG)

A

Antibodies (Immunosuppressant)

  • polyclonal Ab from rabbits injected with thymocytes
  • Ab to T-cell antigens (CDs), depletes circulating lymphocytes
  • causes cytokine release syndrome (fever, HA, tremor, N/V, weakness)
  • used for renal rejection and transplants
69
Q

Muronomab-CD3 (OKT3)

A

Antibodies (Immunosuppressant)

  • mouse monoclonal Ab against human CD3
  • depletes available T cells
  • causes cytokine release syndrome (fever, HA, tremor, N/V, weakness)
  • potentially fatal pulmonary edema, CV collapse, or arrhythmias
  • used for organ rejection
70
Q

Basiliximab

A

Antibodies (Immunosuppressant)

  • humanized anti-CD25 mouse monoclonal Ab
  • bind to IL-2 on activated T cells
  • causes anaphylaxis
  • PROPHYLAXIS FOR RENAL TRANSPLANT
71
Q

Albuterol

A

Beta 2 Agonist (COPD / Asthma)

  • short acting
  • activated cAMP in bronchial smooth muscle to cause bronchodilation
  • contraindicated in pt with CV disease or taking MAOi
  • 1st line with inhaled glucocorticoid
72
Q

Salmeterol

A

Beta 2 Agonist (COPD / Asthma)

  • long acting
  • activated cAMP in bronchial smooth muscle to cause bronchodilation
  • contraindicated in pt with CV disease or taking MAOi
  • 1st line with inhaled glucocorticoid
73
Q

Theophylline

A

Methylxanthine (COPD / Asthma)

  • maintenance therapy for asthma/COPD
  • increases cAMP, blocks Adenosine A2 receptors and phosphodiesterase PDE-4 receptors
  • side effects similar to caffeine
  • for moderate to severe asthma
74
Q

Ipratropium

A

Antimuscarinic (COPD / Asthma)

  • M3 antagonist
  • used in pt who can’t take B2 agonists
  • quaternary derivative of atropine, which limits the CNS side effects
75
Q

Zafirlukast

A

Leukotriene Receptor Antagonist (COPD / Asthma)

  • prevents action at CysLT1 receptors
  • PROPHYLACTIC TREATMENT FOR MILD ASTHMA
  • minimal side effects, but can cause inflammatory condition involving pulmonary infiltrates, neuropathy, and vasculitis
76
Q

Zileuton

A

5-Lipoxygenase Inhibitor (COPD / Asthma)

  • inhibits formation of 5-Lipoxygenase products like leukotrienes
  • PROPHYLACTIC FOR MILD ASTHMA
  • minimal side effects, can cause elevated liver enzymes
77
Q

Beclomethasone

A

Glucocorticoid (COPD / Asthma)

  • reduces cytokine release and production of eicosanoids (prostaglandins and leukotrienes)
  • NOT for chronic daily use due to side effects
  • hoarse voice, oral candidiasis, typical glucocorticoid effects
  • 1st line asthma tx with B2 agonist
78
Q

Cromolyn

A

Mast Cell Stabilizer (COPD / Asthma)

  • prevents release of histamine and leukotrienes
  • prevent mild to moderate asthma attacks by reducing airway reactivity
  • DOES NOT RELIEVE ACUTE SYMPTOMS
  • use with glucocorticoids
  • bad taste, respiratory side effects
79
Q

Omalizumab

A

Anti-IgE Antibody (COPD / Asthma)
- binds to Fc domain of IgE and blocks antigen presentation
- “humanized” Ab via mouse Ab
- reduces airway responsiveness
- concern for infections

80
Q

Methacholine

A

Muscarinic receptor agonist used as a provocative test for hyperactive airways

81
Q

Asthma vs COPD

A

Asthma: bronchial narrowing, lymphocytic and eosinophilic inflmmation
COPD: smaller airway narrowing, neutrophilic inflammation

Pharmacology (3 decks)

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