Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Pharmacology > Block 4 > Flashcards

Block 4 Flashcards

(81 cards)

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

Leucovorin

A

Methotrexate rescue

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

Mesna

A

Cyclophosphamide rescue

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

CHOP Therapy

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

treats non-Hodgkin lymphoma

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Domperidone
Prokinetic - enhance GI motility - Dopamine antagonist, enhances Ach release - inhibit emesis via CTZ (chemoreceptor trigger zone) - no extrapyramidal effects, but can increase prolactin release
26
Metoclopramide
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
27
Dicyclomine
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
28
Hycosamine
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
29
Meclizine
Antiemetic - Antihistamine (H1R Antagonist) - depress labyrinth excitability in ear - can cause CNS depression - good for motion sickness
30
Doxylamine (+ pyridoxine)
Antiemetic - Antihistamine (H1R Antagonist) - depress labyrinth excitability in ear - can cause CNS depression - good for motion sickness
31
Diphenhydramine
Antiemetic - Antihistamine (H1R Antagonist) - depress labyrinth excitability in ear - can cause CNS depression - good for motion sickness
32
Promethazine
Antiemetic - Antihistamine (H1R Antagonist) - ALSO BLOCKS D2 RECEPTORS - depress labyrinth excitability in ear - can cause CNS depression - good for motion sickness
33
Scopolamine
Antimuscarinic Antiemetic - block M2 receptors in CTZ - anti-muscarinic side effects (dry mouth, constipation, hallucination, fever)
34
Prochlorperazine
Antimuscarinic Antiemetic - block M2 receptors in CTZ - anti-muscarinic side effects (dry mouth, constipation, hallucination, fever)
35
Ondansetron
5-HT Receptor Antagonist Antiemetic - treats N/V post-op or in chemo - selective 5-HT3 antagonist - itch, rash, constipation, fever
36
Bismuth
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
Loperamide
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
Anthraquinone
Laxative - causes cramping and inflammation - can get into breast milk - can cause "Lazy Bowel Syndrome" with abuse
39
Diphenylmethane
Laxative - can cause bowel inflammation
40
Aspirin
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
Ibuprofen
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
Naproxen
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
Diclofenac
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
Meloxicam
NSAID (Anti-inflammatory) - predominant COX2 reversible inhibitor - causes gastric ulcers, MI, stroke, HF, bleeding, renal impairment - no in pregnancy or gout - no tolerance
45
Celecoxib
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
Acetaminophen
Anti-inflammatory - treats pain and fever but NOT inflammation - little platelet effects, little GI effects - overdose causes fatal hepatic necrosis
47
N-Acetylcysteine
antidote to acetaminophen poisoning
48
Azathioprine
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
Methotrexate
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
Infliximab
DMARD - TNF-alpha Inhibitor - can cause anaphylaxis or lupus like syndrome - increased risk for malignancies and infection - used for RA or Crohns
51
Etanercept
DMARD - TNF-alpha Inhibitor - increased risk for malignancies and infection
52
Abatacept
DMARD - T-Cell Modulation - increased risk for malignancies and infection
53
Rituximab
DMARD - B-Cell Cytotoxic Agent - increased risk for malignancies and infection
54
Colchicine
Gout (Anti-Inflammatory) - mitotic inhibitor - used when NSAIDs ineffective - not uricosuric - GI distress, myopathy, neuropathy
55
Anakinra
DMARD - IL-1 Inhibition - increased risk for malignancies and infection
56
Probenecid
Gout (Anti-Inflammatory) - uricosuric - precipitate uric acid crystals in renal tubules - GI irritation with peptic ulcers, hypersensitivity
57
Allopurinol
Gout (Anti-Inflammatory) - inhibit xanthine oxidase - decrease uric acid production - fever, malaise, muscle aches
58
Sumatriptan
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
Rimegepant
Migraine - CGRP Antagonist - inhibit the CGRP receptor - acute migraine treatment (CGRP are small molecules tied directly to migraine activity)
60
Fremanezumab
Migraine - CGRP Antibody - monoclonal Ab to the CGRP receptor - MIGRAINE PROPHYLAXIS - no current contraindications - causes URIs and injection site reactions
61
Cortisone
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
Prednisone
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
Dexamethasone
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
Cyclosporine 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
Tacrolimus
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
Sirolimus (Rapamycin)
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
Mycophenolic Acid
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
Anti-Thymocyte Globulin (ATG)
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
Muronomab-CD3 (OKT3)
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
Basiliximab
Antibodies (Immunosuppressant) - humanized anti-CD25 mouse monoclonal Ab - bind to IL-2 on activated T cells - causes anaphylaxis - PROPHYLAXIS FOR RENAL TRANSPLANT
71
Albuterol
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
Salmeterol
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
Theophylline
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
Ipratropium
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
Zafirlukast
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
Zileuton
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
Beclomethasone
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
Cromolyn
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
Omalizumab
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
Methacholine
Muscarinic receptor agonist used as a provocative test for hyperactive airways
81
Asthma vs COPD
Asthma: bronchial narrowing, lymphocytic and eosinophilic inflmmation COPD: smaller airway narrowing, neutrophilic inflammation

Pharmacology (3 decks)

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