Year 2 Flashcards
(122 cards)
Azathioprine
- Disease: Used in autoimmune diseases like rheumatoid arthritis, inflammatory bowel disease, and in transplant medicine.
- Mechanism: Suppresses the immune system by inhibiting purine synthesis, leading to decreased proliferation of lymphocytes.
- Side Effects: Bone marrow suppression, increased risk of infections, gastrointestinal disturbances, hepatotoxicity.
- Contraindications: Hypersensitivity, severe bone marrow suppression.
- Pertinent Info: Requires monitoring of blood cell counts and liver function.
Sulfasalazine
- Disease: Primarily used in inflammatory bowel disease (Crohn’s disease, ulcerative colitis), and also in rheumatoid arthritis.
- Mechanism: Combination of 5-aminosalicylic acid (anti-inflammatory) and sulfapyridine (antibacterial). Exact mechanism in IBD is not fully understood.
- Side Effects: Gastrointestinal upset, headache, rash, reversible oligospermia.
- Contraindications: Hypersensitivity to sulfonamides, porphyria.
- Pertinent Info: Requires monitoring for blood cell counts, liver function, and kidney function.
Docetaxel
- Disease: Used in the treatment of various cancers, including breast cancer, non-small cell lung cancer, prostate cancer, gastric cancer, and head and neck cancer.
- Mechanism: Taxane class chemotherapeutic agent that promotes and stabilizes microtubule assembly, inhibiting their disassembly, which disrupts mitotic cell division and leads to cell death.
- Side Effects: Bone marrow suppression (neutropenia, anemia, thrombocytopenia), hypersensitivity reactions, fluid retention, peripheral neuropathy, alopecia, gastrointestinal disturbances (nausea, vomiting, diarrhea), mucositis, fatigue.
- Contraindications: Severe hypersensitivity to docetaxel or polysorbate 80, severe liver impairment, baseline neutrophil count < 1500 cells/mm³.
Cyclophosphamide
- Disease: Used in the treatment of various cancers, including lymphomas, leukemias, breast cancer, ovarian cancer, and as an immunosuppressant in autoimmune diseases like lupus and vasculitis.
- Mechanism: Alkylating agent that cross-links DNA, leading to DNA damage and cell death, particularly in rapidly dividing cells.
- Side Effects: Bone marrow suppression (leading to anemia, leukopenia, thrombocytopenia), gastrointestinal disturbances (nausea, vomiting), hemorrhagic cystitis, alopecia, increased risk of infections, secondary malignancies.
- Contraindications: Hypersensitivity to cyclophosphamide, severe bone marrow suppression, active infections.
- Pertinent Info: Adequate hydration and mesna (a uroprotective agent) are used to prevent hemorrhagic cystitis. Regular monitoring of blood counts and renal function is necessary.
Vincristine
- Disease: Used in the treatment of various cancers, including leukemia, lymphoma, and some solid tumors like neuroblastoma and Wilms’ tumor.
- Mechanism: Vinca alkaloid that inhibits microtubule formation, disrupting mitosis and leading to cell death.
- Side Effects: Neurotoxicity (peripheral neuropathy, constipation, neurogenic bladder), myelosuppression (less common compared to other chemotherapeutic agents), alopecia, gastrointestinal disturbances.
- Contraindications: Hypersensitivity to vincristine, Charcot-Marie-Tooth disease, intrathecal administration (which is fatal).
- Pertinent Info: Dosing is typically capped to minimize neurotoxic effects. Requires careful handling and administration.
Nivolumab
- Disease: Used in the treatment of various cancers, including melanoma, non-small cell lung cancer, renal cell carcinoma, Hodgkin lymphoma, head and neck squamous cell carcinoma, and others.
- Mechanism: Immune checkpoint inhibitor that blocks PD-1 (programmed death-1) receptor, enhancing T-cell responses against cancer cells.
- Side Effects: Immune-related adverse events including colitis, hepatitis, pneumonitis, endocrinopathies (e.g., hypothyroidism, adrenal insufficiency), rash, and fatigue.
- Contraindications: Severe hypersensitivity to nivolumab.
- Pertinent Info: Requires close monitoring for signs of immune-related adverse events, which can often be severe and may require corticosteroids or other immunosuppressive therapies. Regular blood tests and assessments of liver, renal, and thyroid function are typically performed during treatment.
Rituximab
- Disease: Used in the treatment of** non-Hodgkin’s lymphoma, chronic lymphocytic leukemia**, rheumatoid arthritis, and certain autoimmune diseases like granulomatosis with polyangiitis and microscopic polyangiitis.
- Mechanism: Monoclonal antibody that targets CD20, a protein expressed on the surface of B cells, leading to B cell lysis through antibody-dependent cellular cytotoxicity (ADCC), complement-dependent cytotoxicity (CDC), and direct apoptosis.
- Side Effects: Infusion-related reactions (fever, chills, hypotension), infections, cytopenias, progressive multifocal leukoencephalopathy (PML), cardiovascular events.
- Contraindications: Hypersensitivity to rituximab or any component of the formulation, active severe infections.
- Pertinent Info: Requires premedication with antihistamines and antipyretics to reduce the risk of infusion reactions. Monitoring for infections and regular blood counts is essential.
Cytarabine
- Disease: Used primarily in the treatment of acute myeloid leukemia (AML), acute lymphocytic leukemia (ALL), and non-Hodgkin’s lymphoma. It is also used intrathecally for the treatment and prophylaxis of meningeal leukemia and lymphoma.
- Mechanism: Cytarabine is a pyrimidine nucleoside analogue that inhibits DNA synthesis. It is converted into its active form, cytarabine triphosphate (ara-CTP), which incorporates into DNA and inhibits DNA polymerase, leading to impaired DNA replication and repair, resulting in cell death, particularly in rapidly dividing cells.
- Side Effects: Bone marrow suppression (leading to anemia, leukopenia, thrombocytopenia), gastrointestinal disturbances (nausea, vomiting, diarrhea, mucositis), hepatotoxicity, neurotoxicity (cerebellar toxicity, seizures), ocular toxicity (conjunctivitis, keratitis), and pulmonary toxicity. Other side effects include rash, fever, and flu-like symptoms.
- Contraindications: Hypersensitivity to cytarabine, severe bone marrow suppression (except when used in controlled conditions for treatment of leukemia), active infections.
Methotrexate
- Disease: Used in the treatment of various conditions, including rheumatoid arthritis, psoriasis, and certain cancers such as acute lymphoblastic leukemia, non-Hodgkin’s lymphoma, and osteosarcoma.
- Mechanism: Antimetabolite and antifolate agent that inhibits dihydrofolate reductase, leading to inhibition of DNA, RNA, and protein synthesis. This results in reduced cell proliferation and induces apoptosis, particularly in rapidly dividing cells.
- Side Effects: Bone marrow suppression (leading to anemia, leukopenia, thrombocytopenia), gastrointestinal disturbances (nausea, vomiting, mucositis), hepatotoxicity, nephrotoxicity, pulmonary toxicity, and risk of serious infections. Other side effects include alopecia, fatigue, and stomatitis.
- Contraindications: Severe renal or hepatic impairment, bone marrow suppression, active infections, known hypersensitivity to methotrexate, and pregnancy (due to teratogenic effects).
Ipilimumab
- Disease: Used in the treatment of melanoma, renal cell carcinoma, and other cancers.
- Mechanism: Monoclonal antibody that blocks cytotoxic T-lymphocyte-associated protein 4 (CTLA-4). This inhibition enhances T-cell activation and proliferation, boosting the immune system’s response against cancer cells.
- Side Effects: Immune-related adverse events including colitis, hepatitis, dermatitis, endocrinopathies (such as hypothyroidism or hypophysitis), and pneumonitis. Other common side effects include fatigue, diarrhea, rash, and pruritus.
- Contraindications: Severe hypersensitivity to ipilimumab or any component of the formulation.
Trastuzumab and Pertuzumab:
- Disease: Used in the treatment of HER2-positive breast cancer.
- Mechanism: Monoclonal antibodies that** target the HER2 receptor**, inhibiting cancer cell growth and survival.
- Side Effects: Infusion reactions, cardiotoxicity, diarrhea.
- Contraindications: Hypersensitivity, pre-existing heart failure.
Timolol
- Disease: Used in the treatment of glaucoma and ocular hypertension.
- Mechanism: Non-selective beta-blocker that reduces intraocular pressure by decreasing aqueous humor production.
- Side Effects: Eye irritation, bradycardia, hypotension, bronchospasm.
- Contraindications: Asthma, severe COPD, bradycardia, heart block.
Name some drugs that act on the M-phase of the cell cycle.
Colchicine ( prevents microtubule polymerization, leading to the arrest of cells in mitosis.)
Vinca alkaloids (inhibit microtubule polymerization by binding to tubulin subunits, leading to the formation of abnormal microtubules.)
Paclitaxel (microtubule polymerization and prevents depolymerization.)
Colchicine
- Disease: Used primarily in the treatment of gout and familial Mediterranean fever (FMF).
- Mechanism: Inhibits microtubule polymerization, leading to disruption of cell division, migration of inflammatory cells, and phagocytosis.
- Side Effects: Gastrointestinal upset (nausea, vomiting, diarrhea), myopathy, peripheral neuropathy.
- Contraindications: Severe renal or hepatic impairment, gastrointestinal disorders.
Vinca Alkaloids
- Disease: Used in various cancers, including leukemia, lymphoma, breast cancer, and lung cancer.
- Mechanism: Inhibit microtubule assembly, leading to disruption of mitotic spindle formation and cell division.
- Side Effects: Bone marrow suppression, peripheral neuropathy, gastrointestinal disturbances
- Contraindications: Hypersensitivity, severe bone marrow suppression, neuropathy.
Paclitaxel
- Disease: Used in various cancers, including breast cancer, ovarian cancer, and lung cancer.
- Mechanism: Stabilizes microtubules, leading to inhibition of mitotic spindle function and cell division.
- Side Effects: Bone marrow suppression, peripheral neuropathy, hypersensitivity reactions.
- Contraindications: Hypersensitivity, severe bone marrow suppression.
- Pertinent Info: Requires premedication to prevent hypersensitivity reactions.
Hydroxychloroquine
- Disease: Used in autoimmune diseases like rheumatoid arthritis, lupus erythematosus, and malaria.
- Mechanism: Exact mechanism in autoimmune diseases is not fully understood. May modulate immune response and interfere with lysosomal activity.
- Side Effects: Retinopathy, gastrointestinal disturbances, skin reactions.
- Contraindications: Pre-existing retinopathy, hypersensitivity to 4-aminoquinolines.
- Pertinent Info: Requires regular eye examinations due to risk of retinopathy.
Certolizumab-pegol
- Disease: Used in autoimmune diseases like rheumatoid arthritis, psoriatic arthritis, Crohn’s disease.
- Mechanism: Monoclonal antibody against tumor necrosis factor-alpha (TNF-α), inhibiting its inflammatory effects.
- Side Effects: Increased risk of infections, injection site reactions, infusion reactions, increased risk of malignancies.
- Contraindications: Active infections, hypersensitivity.
- Pertinent Info: Increased risk of reactivation of latent tuberculosis (TB).
- Pegylation increases the retention time, reduces the immunogenicity and increases the stability of the drug to be metabolized by enzymes.
MAOI (Monoamine Oxidase Inhibitors)
- Diseases: Depression, particularly atypical depression and treatment-resistant depression.
- Mechanism: Inhibit monoamine oxidase enzyme, increasing levels of neurotransmitters (serotonin, norepinephrine, dopamine)
- Side Effects: Hypertensive crisis (with tyramine-rich foods), weight gain, insomnia, dizziness.
- Contraindications: Concurrent use with SSRIs, TCAs, certain pain medications, and other serotonergic drugs.
SSRI (Selective Serotonin Reuptake Inhibitors)
-
Diseases: Depression, anxiety disorders, PTSD, OCD
. - Mechanism: Inhibit reuptake of serotonin, increasing its availability in the synaptic cleft.
- Side Effects: Nausea, sexual dysfunction, insomnia, weight gain, serotonin syndrome (rare but serious).
- Contraindications: Concurrent use with MAOIs, certain other serotonergic drugs.
TCA (Tricyclic Antidepressants)
- Diseases: Depression, neuropathic pain, migraine prophylaxis.
- Mechanism: Inhibit reuptake of norepinephrine and serotonin, also block acetylcholine and histamine receptors.
- Side Effects: Anticholinergic effects (dry mouth, constipation), sedation, weight gain, cardiotoxicity (in overdose).
- Contraindications: Recent myocardial infarction, concurrent use with MAOIs.
Bupropion
- Diseases: Depression, smoking cessation.
- Mechanism: Inhibits reuptake of norepinephrine and dopamine.
- Side Effects: Insomnia, dry mouth, seizure risk (dose-dependent).
- Contraindications: Seizure disorders, eating disorders, concurrent use with MAOIs.
Mianserin
- Diseases: Depression (primarily used in some countries).
- Mechanism: Noradrenergic and specific serotonergic antidepressant (NaSSA); blocks alpha-2 adrenergic receptors and serotonin receptors.
- Side Effects: Sedation, weight gain, agranulocytosis (rare but serious).
- Contraindications: Severe liver impairment, mania.
Oestrogen
- Diseases: Hormone replacement therapy (HRT), certain cancers, contraceptive.
- Mechanism: Modulates gene expression by binding to estrogen receptors, influencing reproductive and other systems.
- Side Effects: Thromboembolic events, breast tenderness, headache, nausea.
- Contraindications: History of thromboembolic disorders, certain cancers, liver disease.