Drug Set 1 Flashcards by Amit Zaidman

What are the clinical applications of Dexamethosone?

Management of acute inflammatory conditions, prevention of organ transplant rejection, treatment of autoimmune disorders

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What are some adverse effects of Dexamethosone?

Widespread transcriptional alterations, increased risk of opportunistic infections

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What is the clinical application of Rho(D) Immune Globulin?

Prevention of hemolytic disease of the newborn

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What are the mechanisms of action of Dexamethosone?

Corticosteroid receptor (CR) binding: NF-κB complex stabilization → no nuclear translocation: inhibits transcription of inflammatory cytokines; CR nuclear translocation: promotes transcription of anti-inflammatory cytokines; Reduces expression of adhesion molecules: decreased inflammatory cell recruitment; Inhibits PLA2: inhibits prostaglandin synthesis

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What is the mechanism of action of Rho(D) Immune Globulin?

Binds Rho(D) antigens on fetal RBCs, facilitating their clearance from maternal circulation; prevents anti-Rho(D) antibody formation in the mother

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What is the clinical application of Muromonab-CD3?

Prevention of organ transplant rejection

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What are some adverse effects of Basiliximab?

Increased risk of opportunistic infections

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What is the mechanism of action of Muromonab-CD3?

Binds CD3 on T cells, leading to initial activation followed by complex internalization and deactivation

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What are some adverse effects of Muromonab-CD3?

Cytokine release syndrome, immunogenic reactions

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What is the clinical application of Basiliximab?

Prevention of organ transplant rejection

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What are the mechanisms of action of Basiliximab?

Blocks IL-2 receptor (α subunit) preventing IL-2 binding and T cell maturation; reduces antibody production due to decreasing CD4+ T cells

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What is the mechanism of action of Infliximab, Adalimumab, or Golimumab?

Bind soluble/free TNFα reducing cytokine signalling through TNFα receptors and suppressing inflammatory cytokine production

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What is the clinical application of Infliximab, Adalimumab, or Golimumab?

Management of TNFα-mediated inflammatory conditions

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What are some adverse effects of Infliximab, Adalimumab, or Golimumab?

Increased risk of opportunistic infections

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What is the clinical application of Imiquimod?

Treatment of pre-cancerous tissues/lesions (topical)

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What is the mechanism of action of Imiquimod?

TLR7 agonism; stimulating leukocyte activation and secretion of inflammatory cytokines

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What are some adverse effects of Imiquimod?

Localized inflammation, skin irritation

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What is the mechanism of action of Rituximab?

Binds CD20 on B cells, inducing ADCC

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What is the clinical application of Trastuzumab?

Treatment of HER2+ breast cancer

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What is the mechanism of action of Trastuzumab?

Binds overexpressed HER2 receptors, inducing ADCC

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What is the clinical application of Rituximab?

Treatment of B cell lymphomas and autoimmune conditions

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What are some adverse effects of Rituximab?

Depletion of healthy B cells

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What is the clinical application of Nivolumab or Pembrolizumab?

Cancer immunotherapy

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What is the mechanism of action of Nivolumab or Pembrolizumab?

Bind PD-1 preventing its interaction with PD-L1; reverses T cell exhaustion and restores anti-tumor immune responses

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What is the clinical application of Atezolizumab?

Cancer immunotherapy

What is the mechanism of action of Atezolizumab?

Binds PD-L1 preventing its interaction with PD-1; enhances T cell-mediated anti-tumor immunity

What is the clinical application of Ipilimumab?

Cancer immunotherapy

What is the mechanism of action of Ipilimumab?

Binds CTL4, blocking its inhibitory signalling; enables T cell activation through CD28/CD80 promoting anti-tumor immunity

What is the clinical application of Brentuximab Vedotin (Adcetris)?

Treatment of Hodgkin's Lymphoma

What is the mechanism of action of Trastuzumab-Emtansine (Kadcyla)?

Binds overexpressed HER2, delivering DM1 aka Mertansine (microtubule inhibitor) which kills cells

What is the mechanism of action of Brentuximab Vedotin (Adcetris)?

Binds CD30, delivering MMAE (microtubule inhibitor) which kills cells

What is the mechanism of action of Inotuzumab Ozogamicin (Besponsa)?

Binds CD22, delivering calicheamicin (DNA-damaging agent) which kills cells

What is the clinical application of Inotuzumab Ozogamicin (Besponsa)?

Treatment of relapsed/refractory B cell acute lymphoblastic leukemia

What is the clinical application of Gemtuzumab Ozogamicin (Mylotarg)?

Treatment of relapsed/refractory AML

What is the mechanism of action of Gemtuzumab Ozogamicin (Mylotarg)?

Binds CD22, delivering calicheamicin (DNA-damaging agent), which kills cells

What is the clinical application of Mosunetuzumab?

Treatment of cancer

What is the mechanism of action of Mosunetuzumab?

Bispecific antibody; binds CD3 (on T cells) and CD20 (on tumours) forcing an interaction for T-cell mediated killing; can also initiate ADCC

What is the clinical application of Blinatumomab?

Treatment of cancer

What is the mechanism of action of Blinatumomab?

Bispecific antibody (only antigen-recognition domains); binds CD3 (on T cells) and CD19 (on tumours) forcing an interaction for T-cell mediated killing

What is the clinical application of Abatacept?

Management of rheumatoid arthritis

What is Abatacept?

Recombinant CTLA-4

What is the mechanism of action of Abatacept?

Competes with CD28 for CD80/86 binding, reducing T cell costimulation and activation

What is the clinical application of Etanercept?

Treatment of rheumatoid arthritis and autoimmune conditions

What is the mechanism of action of Etanercept?

Fusion protein; neutralizes soluble/free TNFα, reducing inflammatory cytokine signalling

What is one application of CAR-T Therapy?

Treatment of CD19+ B cell lymphomas and leukemias

What is the mechanism of action of CD19 CAR-T Therapy?

Engineered T cells recognize overexpressed CD19, inducing direct killing of target cells (doesn't require costimulation)

What are some adverse effects of CD19 CAR-T Therapy?

Cytokine release syndrome, severe inflammation, B cell depletion

What is the mechanism of action of Tocilizumab?

Binds IL-6 receptor blocking IL-6 signalling and reducing inflammation

What is the clinical application of Tocilizumab?

Management of cytokine release syndrome and rheumatoid arthritis

What are some adverse effects of Tocilizumab?

Increased risk of opportunistic infections

What is the mechanism of action of Paracetamol/Acetaminophen (Tylenol)?

Acts as a reducing agent at the peroxidase site of COX, reducing prostaglandin synthesis; conjugates with arachidonic acid to form AM404, an endocannabinoid reuptake inhibitor

What is the clinical application of Paracetamol/Acetaminophen (Tylenol)?

Pain relief, fever reduction

What are some adverse effects of Paracetamol/Acetaminophen (Tylenol)?

Hepatotoxicity at high doses

What is the clinical application of Aspirin (Acetylsalicylic acid, ASA)?

Pain, fever, inflammation management

What is the mechanism of action of Aspirin (Acetylsalicylic acid, ASA)?

Irreversibly inhibits COX-1 and COX-2 by acetylating Ser529 and blocking arachidonic acid entry, preventing prostaglandin synthesis

What is the clinical application of NSAIDs (e.g. Ibuprofen, Naproxen)?

Pain, fever, inflammation management

What is the mechanism of action of NSAIDs (e.g. Ibuprofen, Naproxen)?

Inhibits COX-1 and COX-2 through non-covalent interaction (ion pair with Arg120), blocking arachidonic acid entry, preventing prostaglandin synthesis

What are some adverse effects associated with NSAIDs?

GI irritation, risk of ulcers, kidney damage with chronic use

What is the clinical application of Rofecoxib (Vioxx)?

Withdrawn from market (NSAID)

What is the main adverse effect of Rofecoxib (Vioxx)?

Increased cardiovascular event risk

What is the mechanism of action of Rofecoxib (Vioxx)?

Selective COX-2 inhibitor, reduces prostaglandin synthesis

What is the mechanism of action of Dinoprostone (PGE2)?

Mimics endogenous PGE2; stimulating uterine contractions and cervical softening

What is the clinical application of Dinoprostone (PGE2)?

Labor induction, pregnancy, abortion

What is the clinical application of Dinoprost (PGF2α)?

Labor induction, pregnancy, abortion

What is the mechanism of action of Dinoprost (PGF2α)?

Mimics endogenous PGF2α; stimulating uterine contractions

What is the clinical application of Carboprost (Analogue of PGF2α)?

Postpartum hemorrhage, abortion

What is the mechanism of action of Carboprost (Analogue of PGF2α)?

Stimulates uterine contractions and promotes hemostasis, reducing bleeding in the uterus

What is the clinical application of Trastuzumab-Emtansine (Kadcyla)?

Treatment of HER2+ metastatic or resistant breast cancer