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Pharmacology 2 > Exam 3 Drugs > Flashcards

Exam 3 Drugs Flashcards

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1
Q

Donepezil

A

Aricept

Cholinesterase inhibitor
Treats Alzheimer’s

ADRs: muscarinic effects (↑ urination, ↑ salivation, bradycardia, etc.) and Insomnia in the brain

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2
Q

Rivastigmine

A

Exelon

Cholinesterase inhibitor
Treats Alzheimer’s

ADRs: muscarinic effects (↑ urination, ↑ salivation, bradycardia, etc.) and Insomnia in the brain

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3
Q

Galantamine

A

Razadyne

Cholinesterase inhibitor
Treats Alzheimer’s

ADRs: muscarinic effects (↑ urination, ↑ salivation, bradycardia, etc.) and Insomnia in the brain

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4
Q

Memantine

A

Namenda XR

NMDA receptor antagonist
Treats Alzheimer’s

  • Reduced glutamatergic signaling
  • Preserves cholinergic neurons
  • Short-term and used in combination with AChE inhibitors
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5
Q

Donanemab

A

Kisunla

Anti-amyloid monoclonal antibody
- Enter the brain → targets and clears amyloid plaques and fibrils
- Improve neuronal signaling and reduce neurodegeneration
- Taken intermittently for 1-1.5 years then PRN as symptoms return

ADRs: intracranial bleeding

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6
Q

Lecanembab

A

Leqembi

Anti-amyloid monoclonal antibody
- Enters the brain → targets and clears amyloid plaques and fibrils
- Improve neuronal signaling and reduce neurodegeneration
- Taken intermittently for 1-1.5 years then PRN as symptoms return

ADR: intracranial bleeding

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7
Q

Riluzole

A

Rilutek

ALS drug
- Extends life by 60 days

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8
Q

Edaravone

A

Radicava

Antioxidant - ALS drug
- Free radical scavenger reducing their ability to attack cells and nerves
- Similar to Vit. E and CoQ10

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9
Q

High-dose corticosteroids

A

Treat relapsing-remitting multiple sclerosis (RRMS)

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10
Q

Avonex (no generic)

A

Interferon-β-1a to treat MS
- Disease modifying agent
- Reduces activity of T-cells → fewer T-cell movement into bloodstream
- Very powerful immunosuppression

ADRs: ↑ risk of infection, ↓ wound healing, flu-like symptoms (muscle/joint aches, fever), ↓ WBC (some ↓RBC), hepatotoxic
Characteristic: depression, suicidal thoughts and actions

Limitation: renders INF less effective

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11
Q

Rebif (no generic)

A

Interferon-β-1a to treat MS
- Disease modifying agent
- Reduces activity of T-cells → fewer T-cell movement into bloodstream
- Very powerful immunosuppression

ADRs: ↑ risk of infection, ↓ wound healing, flu-like symptoms (muscle/joint aches, fever), ↓ WBC (some ↓RBC), hepatotoxic
Characteristic: depression, suicidal thoughts and actions

Limitation: renders INF less effective

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12
Q

Betaseron (no generic)

A

Interferon-β-1b to treat MS
- Disease modifying agent
- Reduces activity of T-cells → fewer T-cell movement into bloodstream
- Very powerful immunosuppression

ADRs: ↑ risk of infection, ↓ wound healing, flu-like symptoms (muscle/joint aches, fever), ↓ WBC (some ↓RBC), hepatotoxic
Characteristic: depression, suicidal thoughts and actions

Limitation: renders INF less effective

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13
Q

Extavia (no generic)

A

Interferon-β-1b to treat MS
- Disease modifying agent
- Reduces activity of T-cells → fewer T-cell movement into bloodstream
- Very powerful immunosuppression

ADRs: ↑ risk of infection, ↓ wound healing, flu-like symptoms (muscle/joint aches, fever), ↓ WBC (some ↓RBC), hepatotoxic
Characteristic: depression, suicidal thoughts and actions

Limitation: renders INF less effective

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14
Q

Capaxone

A

Glatiramer acetate

Treats MS - Disease modifying agent
- Reduces T-cell activity by mimicking myelin basic protein
- Immunosuppressant

ADRs: Mimics MI (SOB, chest pain, flushing) → No CV CI, immunosuppression

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15
Q

Tysabri

A

Natalizumab

Monoclonal antibody - disease modifying agent
- Immunosuppressant directed against ɑ4β1 integrin on activated T-cells
- Reduces movement of T cells into CNS

Severe ADR: Progressive Multifocal Leukoencephalopathy (PML) → severe brain infection (prion disease) - first signs are visual/speech defects

CI with use of INF - too much immunosuppression

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16
Q

Lemtrada

A

Alemtuzumab

Monoclonal antibody - disease modifying agent
- Immunosuppressant directed against CD52 on B-cells and T-cells
- Causes antibody-dependent cell mediated toxicity → death to B and T lymphocytes

ADR: ↑ risk of hemorrhagic stroke

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17
Q

Ocrevus

A

Ocrelizumab

Monoclonal antibody - RRMS
- Bind to CD20 → antibody-dependent cell mediated toxicity
- Immunosuppressant

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18
Q

Briumvi

A

Ublituxumab

Monoclonal antibody - RMSS
- Binds to CD20 → antibody-dependent cell mediated toxicity
- Immunosuppressant

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19
Q

Kesumpti

A

Ofetumumab

Monoclonal antibody - RMSS
- Binds to CD20 → antibody dependent cell mediated toxicity
- Immunosuppressant

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20
Q

Novantrone

A

Mitoxantrone

Injectable anti-cancer drug - secondary/ progressive MS
- Inhibits topoisomerase → reduces DNA replication
- Immunosuppressant

ADRs: Significant cardiotoxicity (HF-like effect), chemotherapy-like effects, teratogenic

Limited to a certain life-time cumulative dose

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21
Q

Gilenya

A

Fingolimod

Agonist at S1P1 GPCR - Disease modifying agent
- Immunosuppressant
- Mimics sphingosene-1-phosphate and signals for T-cells to move into the bloodstream
- Rise in T-cells causes desensitization of S1P1 receptors
- Reduction of T-cells in circulation

Significant ADRs: edema (cardiac, pulmonary, macular), HTN, bronchitis, hepatotoxicity, first-dose bradycardia

Taper dose to prevent worsening of symptoms if stopped abruptly

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22
Q

Mayzent

A

Siponimod

Agonist at S1P1 GPCR - Disease modifying agent
- Immunosuppressant
- Mimics sphingosine-1-phosphate and signals for T-cells to move into the bloodstream
- Rise in T-cells causes desensitization of the S1P1 receptors
- Reduction of T-cells in circulation

Significant ADRs: edema (cardiac, pulmonary, macular), HTN, bronchitis, hepatotoxicity, first-dose bradycardia

Taper dose to prevent worsening of symptoms if stopped abruptly

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23
Q

Zeposia

A

Ozanimod

Agonist at S1P1 GPCR - Disease modifying agent
- Immunosuppressant
- Mimics sphingosine-1-phosphate and signals for T-cells to move into the bloodstream
- Rise in T-cells causes desensitization of the S1P1 receptors
- Reduction of T-cells in circulation

Significant ADRs: edema (cardiac, pulmonary, macular), HTN, bronchitis, hepatotoxicity, first-dose bradycardia

Taper dose to prevent worsening of symptoms if stopped abruptly

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24
Q

Ponvory

A

Ponesimod

Agonist at S1P1 GPCR - Disease modifying agent
- Immunosuppressant
- Mimics sphingosine-1-phosphate and signals for T-cells to move into the bloodstream
- Rise in T-cells causes desensitization
- Reduction of T-cells in circulation

Significant ADRs: edema (cardiac, pulmonary, macular), HTN, bronchitis, hepatotoxicity, first-dose bradycardia

Taper dose to prevent worsening of symptoms if stopped abruptly

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25
Aubagio
Teriflunamide Inhibits dihydroorotate dehydrogenase - Interferes with de novo synthesis of pyrimidine - Slows DNA replication → immunosuppression ADRs: chemotherapy-like effects → sloughing of GIT (D/V), agranulocytosis (↓ WBC), alopecia, anemia, ↓ wound healing, teratogenic Cholestyramine washout to eliminate the drug rapidly
26
Tecfidera
Dimethyl fumarate Fumaric acid derivative - Immunosuppressants - Suspected: oxidative damage toward T-cells
27
Vumerity
Diroximel fumarate Fumaric acid derivative - Immunosuppressant - Suspected: oxidative damage toward T-cells
28
Bafiertam
monomethyl fumarate Fumaric acid derivative - Immunosuppressant - Suspected: oxidative damage toward T-cells
29
Mavenclad
Cladribine - NOT a monoclonal antibody - Unclear mechanism: causes apoptosis of B and T cells - Immunosuppressant
30
Amprya
Dalfampridine K+ channel blocker - NOT AN IMMUNOSUPPRESSANT - Stops K+ leaving the neuron through exposed stretches of myelin - Reduction in hyperpolarization decreases neuronal deficit ADRs: ↑ risk of seizures, UTIs
31
Cyclosporine
Sandimmune; Neoral (microemulsion ↑ oral availability - Not interchangeable Immunosuppressant - Calcineurin inhibitor Indicated for successful organ transplantation - Take on empty stomach - Binds to cyclophilin and forms a drug-protein complex to inhibit calcineurin - ↓ dephosphorylation of NFAT → ↓ IL-2 - Decreases proliferation of T-cells ADRs: **HTN**, **nephrotoxicity** (pts. with transplanted kidneys must be stable before , taking this drug - Muscle tremors, hirsutism, gingival hyperplasia, DM (destruction of β-cells) Substrate for 3A4
32
Tacrolimus
Program; Protopic (topical) Immunosuppressant - Calcineurin inhibitor Indicated for successful organ transplantation - Take on empty stomach - Binds to FKBP and forms a drug-protein complex to inhibit calcineurin - ↓ dephosphorylation of NFAT → ↓ IL-2 - Decreases proliferation of T-cells ADRs: **HTN**, **nephrotoxicity** (pts. with transplanted kidneys must be stable before , taking this drug - Muscle tremors, hirsutism, gingival hyperplasia, DM (destruction of β-cells) Substrate for 3A4
33
Pimecrolimus
Elidel (topical) Topical Immunosuppressant - less systemic ADRs - Calcineurin inhibitor Indicated for psoriasis (skin conditions) - Binds to FKBP and forms a drug-protein complex to inhibit calcineurin - ↓ dephosphorylation of NFAT → ↓ IL-2 - Decreases proliferation of T-cells Substrate for 3A4
34
Sirolimus
Rapamune (AKA Rapamycin) Indicated to prevent organ transplant rejection and also used coat stents for CAD (↓ restenosis over time = ↓ hyperplasia of endothelial and smooth muscle cells from metal irritation) - Binds to FKBP (drug-protein complex) complexes with mTOR (mammalian target of Rapamycin) - Complex inhibits CDK-2 → ↓ T-cell proliferation ADRs: ↑ cholesterol and TGs, ↓ WBCs DDIs: substrate for 3A4 - Take on empty stomach bc. it's a large molecule
35
Everolimus
Zortress, Afinitor Indication: cancer - Binds to FKBP (drug-protein complex) complexes with mTOR (mammalian target of Rapamycin) - Complex inhibits CDK-2 → ↓ T-cell proliferation ADRs: ↑ cholesterol and TGs, ↓ WBCs DDIs: substrate for 3A4 - Take on empty stomach bc. it's a large molecule
36
Azathioprine
Imuran Prodrug → 6-mp → 6-thioguanine - Replaces guanine in DNA and stops DNA Replicase enzyme → ↓ DNA replication - Reduces T-cell proliferation ADRs: chemotherapy-like effects + teratogenic DDI: - 6-mp is a substrate for XO → interact with XOi → ↑ conc. → toxic to WBCs (agranulocytosis) - Substrate for TPMT: deficiency of TPMT ↑ 6-mp toxicity → can cause fatal agranulocytosis (pharmacogenomic testing required)
37
Mycophenolate mofetil
Cellcept, Myfortic Inhibits inosine monophosphate dehydrogenase (IMD) - ↓ pyrimidine synthesis → ↓ DNA replication - ↓ T-cell activity ADRs: chemotherapy-like effects + teratogenic CI: Cannot give with azathioprine - Too much immunosuppression
38
Simulect
Basilximab Indication: induction phase of organ transplantation mAB directed against IL-2 - Inhibit IL-2 receptors → ↓ CDK-2 activation → ↓ T-cell proliferation Small risk of anaphylaxis
39
Muromonab-CD3
OKT3 Indication: for pts. actively rejecting organ transplantation (to buy time) mAB directed against CDK-3 - CDK-3 is located on B and T cells → cell dependent toxicity → rapid drop in T-cells
40
Cyclosporin (dry eye disease)
Restasis - Eye drops Calcineurin inhibitor - Inhibits T-cell activity in the eye
41
Xiidra
Lifitegrast - Eye drops Inhibits LFA-1 cell adhesion molecule - Reduced movement of T-cells from bloodstream into the eye
42
Methotrexate (no brand)
DMARD - oral - Most common DMARD - once a week Inhibits dihydrofolate reductase - ↓ purine synthesis → ↓ DNA replication ADRs: ***Pulmonary toxicity*** chemotherapy like effects + teratogenic, ↓ WBC count (leukopenia) - May take folic acid to combat leukopenia (controversial) Other indication: cancer
43
Leflunamide
Arava - half-life of 2 weeks DMARD - oral - Prodrug to teriflunamide Inhibits dihydroorotate reductase - ↓ pyridine synthesis → ↓ DNA replication → ↓ T-cell activity ADRs: chemotherapy-like effects, teratogenic DDI w/ bile acid sequestrants - Cholestyramine washout to flush out of system
44
Sulfasalizine
Azulfidine DMARD - oral Prodrug to 5-ASA and **sulphapyridine** - Azo-linkage provides orange colour to the tablets required to metabolize sulfasalizine into metabolites ADRs: orange tint to skin/bodily fluids, skin rashes, ↓ WBC count (co-administer with folic acid), anemia, photosensitivity
45
Hydroxychloroquine
Plaquenil DMARD - oral - ↓ release of IL-1 from T-cells → ↓ cytokine release - Takes ~6mo to see progress ADRs: retinopathy with chronic use
46
Azathioprine (no brand)
DMARD - oral Prodrug → 6-mp → 6-thioguanine - Replaces guanine in DNA and stops DNA Replicase enzyme → ↓ DNA replication - Reduces T-cell proliferation - Immunosuppressant ADRs: chemotherapy-like effects + teratogenic DDI: - 6-mp is a substrate for XO → interact with XOi → ↑ conc. → toxic to WBCs (agranulocytosis) - Substrate for TPMT: deficiency of TPMT ↑ 6-mp toxicity → can cause fatal agranulocytosis (pharmacogenomic testing required)
47
Cyclosporine (no brand)
DMARD - oral Immunosuppressant - Calcineurin inhibitor Indicated for successful organ transplantation - Take on empty stomach - Binds to cyclophilin and forms a drug-protein complex to inhibit calcineurin - ↓ dephosphorylation of NFAT → ↓ IL-2 - Decreases proliferation of T-cells ADRs: **HTN**, **nephrotoxicity** (pts. with transplanted kidneys must be stable before , taking this drug - Muscle tremors, hirsutism, gingival hyperplasia, DM (destruction of β-cells) Substrate for 3A4
48
Penicillamine
Old DMARD - oral Rarely used anymore
49
Gold salts
Old DMARD - available as 2 formulations - Oral capsule - Injection into joints
50
SERCH
TNF-ɑ inhibitors - Bind to TNF-ɑ and prevents it from binding to its receptor - Helps excrete TNF-ɑ Simponi (golimumab) Enbrel (etanercept) Remicade (infliximab) Cimzia (certolizumab) Humira (adalimumab)
51
Simponi
Golimumab TNF-ɑ antagonist - mAB - Binds to TNF-ɑ in circulation to prevent it binding to its receptor - Neutralization → excretion ADRs: Injection site reactions, susceptible to severe infections/ malignancies (fungal, sepsis, TB, etc.), ↓ wound healing Cautions: live-vaccines CI: other biological DMARDs
52
Enbrel
Etanercept TNF-ɑ antagonist - NOT a mAB - Uses recombinant DNA to form the extracellular and transmembrane portion of the TNF-ɑ receptor - Binds to circulating TNF-ɑ and helps excrete it ADRs: injection site reactions, susceptible to severe infections and malignancies (e.g., fungal, sepsis, TB, etc.), ↓ wound healing Caution: live-vaccines CI: other biological DMARDs
53
Remicade
Infliximab TNF-ɑ antagonist - mAB - Binds to TNF-ɑ in circulation to prevent it binding to its receptor - Neutralization → excretion ADRs: injection site reactions, susceptible to severe infection and malignancies (e.g., fungal, sepsis, TB, etc.), ↓ wound healing Caution: live-vaccines CI: ***HF***, other biological DMARDs
54
Cimzia
Certolizumab TNF-ɑ antagonist - Binds to TNF-ɑ in circulation to prevent it binding to its receptor - Neutralization → excretion ADRs: injection site reactions, susceptible to severe infections and malignancies (e.g., fungal, sepsis, TB, etc.), ↓ wound healing Caution: live-vaccines CI: other biological DMARDs
55
Humira
Adalimumab TNF-ɑ antagonist - Binds to TNF-ɑ in circulation to prevent it binding to its receptor - Neutralization → excretion ADRs: injection site reaction, susceptible to severe infections and malignancies (e.g., fungal, sepsis, TB, etc.), ↓ wound healing Caution: live-vaccines CI: other biological DMARDS
56
KI-IL-1
IL-1 inhibitors Prevents binding of IL-1 to its receptor - No inflammatory process → ↓ immune system activity ADRs: injection site reactions, susceptible to severe infections and malignancies (e.g., fungal, sepsis, TB, etc.), ↓ wound healing Caution: live-vaccines CI: other biological DMARDs
57
Kineret
Anakinra IL-1 receptor inhibitor - Binds to the IL-1 receptor protein → preventing IL-1β from binding - ↓ Immune system activity ADRs: injection site reactions, susceptible to sever infections and malignancies (e.g., fungal, sepsis, TB, etc.), ↓ wound healing Caution: live-vaccines CI: other biological DMARDs
58
Ilaris
Canakinumab IL-1β inhibitor - Binds to IL-1β → ↓ ability of IL-1β to bind to its receptor - ↓ immune system activity ADRs: injection site reaction, susceptible to severe infections and malignancies (e.g., fungal, sepsis, TB, etc.), ↓ wound healing Caution: live-vaccines CI: other biological DMARDS
59
ACT-KEV-IL-6
IL-6 antagonists - mAB against the IL-6 receptor - ↓ ability of IL-6 to bind to its receptor ADRs: GI perforations, hepatotoxicity, ↓ WBC/RBCs, ↑ cholesterol and TGs, cause neuronal demylenation CIs: other biological DMARDs
60
Actemra
Tocilizumab IL-6 inhibitor - mAB against the IL-6 receptor - ↓ ability of IL-6 to bind to its receptor ADRs: GI perforations, hepatotoxicity, ↓ WBC/RBC, ↑ cholesterol and TGs, causes neuronal demylenation CI: other biological DMARDs
61
Kevzara
Sarilumab IL-6 inhibitor - mAB against the IL-6 receptor - ↓ ability of IL-6 to bind to its receptor ADRs: GI perforations, hepatotoxicity, ↓ WBC/RBC, ↑ cholesterol and TGs, causes neuronal demylenation CI: other biological DMARDs
62
ABAT-RIT-B/T
B and T cell inhibitors
63
Abatacept
Orencia T-cell inhibitor - Binds to CD8086 on T cells during antigen presentation - Interferes with ability of T-cell to be stimulation by antigen presenting cell Caution: associated with more malignancies than other drugs CI: patients with prior cancer/malignancies
64
Rituxan
Rituxumab B-cell inhibitor - Targets CD-20 on B-cells and produces antibody-dependent cell toxicity - Loss of B-cells in response to cell toxicity - Infused q6mo bc. it takes time for B cells to regenerate ADRs: significant skin rashes
65
CROX-O
JAK inhibitors - Janus Kinases are activated following the stimulation of any/all cytokines - JAK phosphorylates STAT → 2 STATs form a homodimer - STAT dimer enters the nucleus and acts as a transcription factor for inflammatory genes - Inhibiting JAK → ↓ inflammatory signaling pathway ADRs: CV risks (MI, strokes, etc.) CI: unstable angina, history of MI
66
Cibinqo
Abrocitinib JAK inhibitor - ↓ Phosphorylation of STAT → ↓ dimerization of STAT → ↓ transcription of inflammatory genes - Inhibition of JAK → ↓ inflammatory signaling ADRs: CV risks (MI, strokes, etc.) CI: unstable angina, history of MI
67
Rinvoq
Upadacitinib JAK inhibitor - ↓ phosphorylation of STAT → ↓ dimerization of STAT → ↓ transcription of inflammatory genes - Inhibition of JAK → ↓ inflammatory signaling ADRs: CV risks (MI, stroke, etc.) CI: unstable angina, history of MI
68
Olumiant
Baricitinib JAK inhibitor - ↓ phosphorylation of STAT → ↓ dimerization of STAT → ↓ transcription of inflammatory genes - Inhibition of JAK → ↓ inflammatory signaling ADRs: CV risks (MI, stokes, etc.) CI: unstable angina, history of MI
69
Xeljanz
Tofacitinib JAK inhibitor - ↓ phosphorylation of STAT→ ↓ dimerization of STAT → ↓ transcription of inflammatory genes - Inhibition of JAK → ↓ inflammatory signaling ADRs: CV risks (MI, stroke, etc.) CI: unstable angina, history of MI
70
Opzelura
Ruxolitinib JAK inhibitor - Topical - ↓ phosphorylation of STAT → ↓ dimerization of STAT → ↓ transcription of inflammatory genes - Inhibition of JAK → ↓ inflammatory signaling ADRs are ↓ bc. of local application - CV risks
71
Otezla
Apremilast PDE-4 Inhibitor - oral/systemic - ↑ cAMP and PKA in skin cells (epidermis) → inhibits various transcription factors → inhibits cytokine formation SE: bronchodilation (like Roflumilast) ADRs: weight loss, depression
72
Eucrisa
Crisaborole PDE-4 inhibitor - Topical - ↑ cAMP and PKA in skin cells (epidermis) → inhibits various transcription factors → inhibits cytokine formation SE: bronchodilation ADRs: depression
73
Taltz
Ixekizumab Inhibitor of IL-17 signaling - Against the ***ligand*** - mAB against the IL-17 protein
74
Cosentyx
Secukinumab Inhibition of IL-17 signaling - Against the ***ligand*** - mAB against the IL-17 protein
75
Bimzelx
Bimekizumab Inhibition of IL-17 signaling - Against the ***ligand*** - mAB against the IL-17 protein
76
Siliq
Brodalumab Inhibition of IL-17 signaling - Against the ***receptor*** - mAB against the IL-17 receptor → prevents the binding of IL-17 to its receptor ADRs: severe depression - counselling on suicidality, ideation, and actions
77
Nucala
Mepolizumab Inhibition of IL-5 signaling - Involved in eosinophilic asthma - Against the ***ligand*** - mAB against the IL-5 protein
78
Cinqair
Reslizumab Inhibition of IL-5 signaling - Involved in eosinophilic asthma - Against the ***ligand*** - mAB against the IL-5 protein
79
Fasenra
Benralizumab Inhibition of IL-5 signaling - Involved in eosinophilic signaling - Against the ***receptor*** - mAB against the IL-5 receptor
80
Adbry
Tralokinumab IL-13 antagonist - Bind to IL-13 protein and prevent it from binding to its receptor
81
Ebglyss
Lebrikizumab IL-13 antagonists - Bind to the IL-13 protein and prevent it from binding to its receptor
82
Dupixent
Dupilumab IL-4 receptor antagonists - mAB directed against the IL-4 receptor - Note: IL-4 receptor is also part of the IL-4/IL-13 receptor - Prevents signalling between both receptors
83
Relation between IL-23 and IL-12
IL-23 is composed of P19 and P40 subunits IL-12 is composed of P40 and P35 subunit Drugs that act on IL-23 alone target only the P19 subunit Drugs directed against the P40 subunit can target both IL-23 AND IL-12
84
Tremfya
Guselkumab IL-23 antagonist - mAB directing against the P19 subunit of IL-23
85
Skyrizi
Risankizumab IL-23 antagonist - mAB directed against the P19 subunit of IL-23
86
Ilumya
Tildrakizumab IL-23 antagonist - mAB directed against the P19 subunit of IL-23
87
Omvoh
Mirikizumab IL-23 antagonist - mAB directed against the P19 subunit of IL-23
88
Stalera
Ustekinumab IL-12 and IL-12 antagonist - mAB directed against the P40 subunit present in BOTH IL-12 and IL-23
89
Spevigo
Spesolimab IL-36 receptor antagonist - mAB directed against the IL-36 receptor - Preventing IL-36 from binding to its receptor
90
Sulfasalazine (IBD)
Azulfidine Indications: Ulcerative colitis, colon inflammation Prodrug for 5-ASA (mesalamine) - Azo-linkage is broken into 5-ASA and sulfapyridine ***in the colon*** - 5-ASA is useful in IBD → unknown mechanism - Poor absorption in GIT → local effect ADRs: ↓ WBC/RBC, orange tint to skin/body fluids, rashes, photosensitivity
91
Balsalazide
Colazal Indications: Ulcerative colitis, colon inflammation - Azo linkage is broken ***in the colon*** to release 5-ASA - MOA unknown - Poor absorption in GIT → local effect - no ADRs associated with sulfapyridine
92
Olsalazine
Dipentum Indications: Ulcerative colitis, colon inflammation - Azo linkage is broken ***in the colon*** to release 5-ASA - MOA unknown - Poor absorption in GIT → local effect - No ADRs associated with sulfapyridine
93
Pentasa
Mesalamine (5-aminosalisylic acid) Indication: IBD - Enteric coating/Extended release formulation → inflammation of the ileum and jejunum - Unknown MOA - Poor absorption in GIT → local effect
94
Rowasa and Canasa
Mesalamine (5-aminosalicylic acid) Indication : IBD - Enemas/Suppositories → distal inflammation of the intestines - ***rectum***, colon - Unknown MOA - Poor absorption in GIT → local effects
95
Asacol and Lialda
Mesalamine (5-aminosalicylic acid) Indication : IBD - pH sensitive coating → inflammation in the ileum and past it - Unknown MOA - Poor absorption in GIT → local effects
96
Apprise and Delzicol
Mesalamine (5-aminosalicylic acid) Indication: IBD - Unknown MOA - Poor absorption in GIT → local effects
97
Budesonide
Entocort EC Glucocorticoid - oral - Given chronically but high 1st pass metabolism → ↓ ADRs associated with other systemic glucocorticoids - Local effect → activates glucocorticoid receptors in the GIT and ↓ inflammation
98
Hydrocortisone
Cortenema Glucocorticoid - enema - Given for ***relapse*** of IBD symptoms - Bc. it can be absorbed systemically and cause severe ADRs if used chronically
99
Vedolizumab (IBD)
Entyvio
100
Post menopausal effects
Huge ↓ in estrogen levels which cause complications... 1) Vasomotor symptoms - Lack of estrogen causes vasodilation in the skin (face, neck, and chest) - Hot flashes → ↓ QoL - Subside after ~1-2yrs - Treated systemically 2) Risk of osteoporosis - chronic - ↓ estrogen = ↓ bone mineral density - Treated systemically 3) Vaginal dryness - Treated topically/locally
101
MOA and indication for estrogen/progestin receptor agonists
Estrogen receptors are nuclear hormone receptors - Agonist crosses the membrane into the nucleus - Cause detachment of heat-shock protein from estrogen receptor - Bind to estrogen receptor → complex - Complex dimerizes with another - Binds to ***coactivator*** protein → activates estrogen/progestin response element on the promoter region → ↑ transcription factors for various genes ɑ and β subtypes that are not clinically relevant Indications: Contraceptives and Hormone Replacement Therapy
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Beneficial effects of estrogen agonists
1) ↓ vaginal dryness 2) ↓ cholesterol; ↑ HDL
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Harmful effects of estrogen agonists
1) ↑ synthesis of clotting factors - ↑ risk of MI, stroke, clots, etc. 2) ↑ growth of estrogen-dependent cells (e.g., breast tissue, endometrial cell tissues, etc.) - ↑ risk of breast cancer - ↑ risk of endometrial/uterine cancer - CI in pts. with histories of cancers associated with estrogen-dependent tissues
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Estradiol
Estrace, Estring, Femring, Climara, Vivelle Agonists at the estrogen receptor
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Vezoah
Fezolinetant Indication: Hot flashes MOA: 1) Blocks NKB binding on the hypothalamic KNDy neuron a) Under normal conditions... - Endogenous estrogen and neurokinin B stimulate receptors on the KNDy neurons → balance each other out - No effects on the neurons b) Post-menopausal conditions... - Balance tipped toward neurokinin B, causing vasomotor symptoms (Hot Flashes In short.. - Neurokinin 3 receptor antagonist → Neither estrogen nor NKB receptors are stimulated
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MOA for estrogen receptor antagonists
Estrogen receptors are nuclear hormone receptors - Antagonist crosses the membrane into the nucleus - Cause detachment of heat-shock protein from estrogen receptor - Bind to estrogen receptor → complex - Complex dimerizes with another - Binds to ***corepressor*** protein - This complex prevents binding to estrogen response elements - ↓ transcription of various genes
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Medroxyprogesterone Acetate
Provera Progestin receptor agonist Indications: 1) HRT - Used to nullify the risk of endometrial cancer → ↓ risk of endometrial growth - NO EFFECT on breast cancer 2) Endometriosis - condition of overgrowth of endometrial tissue - ↓ endometrial growth 3) To support pregnancy - Progestins have beneficial effects on endometrial lining → helps the egg attach to uterine lining - Prevents blastocysts from detaching → ↓ risk of miscarriage
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Progesterone
Progestin receptor agonist Indications: 1) HRT - Used to nullify the risk of endometrial cancer → ↓ risk of endometrial growth - NO EFFECT on breast cancer 2) Endometriosis - condition of overgrowth of endometrial tissue - ↓ endometrial growth 3) To support pregnancy - Progestins have beneficial effects on endometrial lining → helps the egg attach to uterine lining - Prevents blastocysts from detaching → ↓ risk of miscarriage
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Norethindrone
Aygestin Progestin receptor agonist Indications: 1) HRT - Used to nullify the risk of endometrial cancer → ↓ risk of endometrial growth - NO EFFECT on breast cancer 2) Endometriosis - condition of overgrowth of endometrial tissue - ↓ endometrial growth 3) To support pregnancy - Progestins have beneficial effects on endometrial lining → helps the egg attach to uterine lining - Prevents blastocysts from detaching → ↓ risk of miscarriage
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Prempro, Femhrt
Combination of estrogen and progestin Receptor agonist Indications: 1) HRT - Used to nullify the risk of endometrial cancer → ↓ risk of endometrial growth - NO EFFECT on breast cancer 2) Endometriosis - condition of overgrowth of endometrial tissue - ↓ endometrial growth 3) To support pregnancy - Progestins have beneficial effects on endometrial lining → helps the egg attach to uterine lining - Prevents blastocysts from detaching → ↓ risk of miscarriage
111
Climara Pro, Combipatch
Combination of estrogen and progestin Receptor agonist Indications: 1) HRT - Used to nullify the risk of endometrial cancer → ↓ risk of endometrial growth - NO EFFECT on breast cancer 2) Endometriosis - condition of overgrowth of endometrial tissue - ↓ endometrial growth 3) To support pregnancy - Progestins have beneficial effects on endometrial lining → helps the egg attach to uterine lining - Prevents blastocysts from detaching → ↓ risk of miscarriage
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Raloxifene
Evista SERM Indications: breast cancer - Only acts on breast tissue with no effects on uterine cancer Beneficial effects : ↓ growth in breast tissue, ↓ risk of uterine tissue growth, ↑ bone mineral density (↓ risk of osteoporosis), ↑ HDL and ↓ cholesterol, ↓ vaginal dryness Harmful effects: ↑ vasomotor symptoms, ↑ clotting factors
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Tamoxifen
Nolvadex SERM Indications: breast cancer Beneficial effects: ↓ growth of breast tissue, ↓ risk of osteoporosis, ↓ LDL and cholesterol, ↑ HDL, ↓ vaginal dryness Harmful effects: ↑ risk of uterine cancer, ↑ clotting factors, ↑ vasomotor symptoms
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Toremifene
Fareston SERM Indications: breast cancer Beneficial effects: ↓ growth of breast tissue, ↓ risk of osteoporosis, ↓ LDL and cholesterol, ↑ HDL, ↓ vaginal dryness Harmful effects: ↑ risk of uterine cancer, ↑ clotting factors
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Ospemifene
Osphena Indication: dyspareunia Beneficial effects: ↓ vaginal dryness, ↓ risk of osteoporosis, ↓ cholesterol and LDL, ↑ HDL Harmful effects: ↑ clotting factors, ↑ vasomotor symptoms, ↑ risk of uterine/breast tissue growth
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Duavee
Bazedoxefine + conjugated estrogens Indications: hot flashes - Estrogen is given to reduce vasomotor symptoms - Bazedoxefine is given as an antagonist at the breast and uterine tissue to ↓ risk of breast/uterine cancer Harmful effects: ↑ clotting factors
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Fluvestrant
Faslodex SERD - only bind to estrogen receptor ɑ - Causes conformational change of the estrogen receptor to expose proteolytic sites → proteolytic enzymes attack and break apart the receptor - less estrogen can bind Effect: ↓ risk of breast cancer - Given q6-9months
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Elacestrant
Orserdu SERD - only bind to estrogen receptor ɑ - Causes conformational change of the estrogen receptor to expose proteolytic sites → proteolytic enzymes attack and break apart the receptor - less estrogen can bind Effect: ↓ risk of breast cancer - Given q6-9months - Less estrogenic effects

Pharmacology 2 (4 decks)

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