Anti-cancer & Biological Agents

Question 1

Dinoprost

Answer 1

A= synthetic PGF2alpha
B= stimulates contraction of the uterus in myometrium (via its interaction with pg receptors) and directly affects collagenases in the uterus as well as increases proteoglycan content resulting in softening of the cervix
C= induces abortion during 2nd trimester, for missed abortion, for benign hydatidiform mole and is also used for ripening of the cervix for induction of labor in patients at or near term

Question 2

Latanoprost

Answer 2

A= long acting prostanoid analog, PGF2alpha
B= decreases intraocular pressure by increasing the outflow of aqueous fluid through selective agonism at FP receptors located in the eye
C= open-angle glaucoma, ocular hypertension

Question 3

Travoprost

Answer 3

A=prostanoid analog, PGF2alpha
B= decreases intraocular pressure by increasing the outflow of aqueous fluid through selective agonism at FP receptors located in the eye
C= open-angle glaucoma, ocular hypertension

Question 4

Misoprostol

Answer 4

A= oxytocic methyl-synthetic PGE1 analog, cytoprotective agent
B= stimulates mucosal production and bicarbonate secretion + enhances mucosal blood flow. Also binds a prostaglandin receptor on parietal cells that reduces histamine-stimulated cAMP production causing modest acid inhibition. Oxytocic properties that increases frequency of uterine contraction during preg
C= NSAID induced ulcers in high risk patients. In combination with mifepristone for terminating pregnancies

Question 5

Interferon Alpha

Answer 5

A= antiviral, immunomodulating agent, antiproliferative, 2nd generation interferon 
B= inhibits viral penetration, translation, transcription, protein processing, maturation and release + increases phagocytic activities of mphs and augmentation of proliferation and survival of cytotoxic Tcells and NK cells
C= neoplasms treatment; hairy cell leukemia, chronich myelogenous leukemia, malignant melanoma, Kaposi's sarcoma, HBV, HCV, renal cell carcinoma, carcinoid syndrome, Tcell leukemia, condylomata acuminata

Question 6

Interferon Betas

Answer 6

A= antiviral, immunomodulating agent, antiproliferative, 2nd generation interferons  
B= inhibits viral penetration, translation, transcription, protein processing, maturation and release + increases phagocytic activities of mphs and augmentation of proliferation and survival of cytotoxic Tcells and NK cells
C= neoplasms treatment; hairy cell leukemia, chronich myelogenous leukemia, malignant melanoma, Kaposi's sarcoma, HBV, HCV, renal cell carcinoma, carcinoid syndrome, Tcell leukemia, condylomata acuminata + relapsing type MS!!

Question 7

Glatiramer

Answer 7

A= immunomodulator, peptide containing IM
B= Konstantins: glatiramir is a peptide containing immunomodulator with 4 aa that resembles myelin aa. Because of its resemblance of myelin it binds MHC molecules and subsequently competes with various myelin antigens for their presentation to Tcells and switch certain TCells to "T suppressors" to suppress other T cells. Activation of specific glatiramer cells that expresses anti infl cytokines IL10 and TGFbeta. Also directly inhibits the activity of circulating APCs; dendritic cells and monocytes
C= relapsing type MS

Question 8

Cyclophosphamide

Answer 8

A= synthetic DMARD, alkylating agent, immunosuppressant
B= its major active metabolite is phosphoramide mustard, which cross-links DNA to prevent cell replication and therefore suppresses Tcell and Bcell function (detaljerat: exert their cytotoxic effect by transfering their alkyl groups to the  N7 position of guanine in DNA-->leads to miscoding through abnormal base paring with thymine--> disruption of DNA function and cell death)
C= RA, SLE, vasculitits, wegeners granulomatosis and other severe rheumatic disorders. Lymphoma, leukemia, multiple myeloma, neuroblastoma, retinoblastoma, carcicoma of the breast and other malignancies

Question 9

Anakinra

Answer 9

A=  recombinant competetive interleukin-1 receptor antagonist (IL-1Ra), biological DMARD
B= prevents IL-1 from binding to its receptor, stemming the cascade of cytokines that would otherwise be released
C= adult RA, acute gout

Question 10

Infliximab

Answer 10

A= chimeric IgG1 anti-TNF monoclonal antibody, biological DMARD
B= complexes with TNFalpha and prevents its interaction with p55 and p75 cell surface receptors--> downregulation of mph and Tcell function
C= RA, ankylosing spondylitits, psoriatic arthritis, chrons disease, psoriasis, ulcerative colitis, juvenile chronic arthritis, wegners granulomatosis, giant cell arteritis, sarcoidosis

Question 11

Bevacizumab (Avastin)

Answer 11

A= recombinant monoclonal IgG1 antibody, anticancer drug, antiangiogenic drug
B= inhibits binding of VEGF-A to VEGFR leading to inhibition of VEGF signaling+ inhibits tumor vascular permability and inhibits angiogenesis in tumors
C= colorectal cancer, breast cancer, non-small cell lung cancer, renal cell cancer

Question 12

Fluorouracil

Answer 12

A= pyrimidine analog, antineoplastic antimetabolite
B= inhibits thymidylate synthetase, interfering with the synthesis of DNA and RNA. These effects are most marked in atypical, rapidly proliferating cells
C= topical treatment for multiple actinic keratoses, colorectal cancer, breast cancer, gastroesophageal cancer, head and neck cancer, hepatocellular cancer

Question 13

Vincristine

Answer 13

A= vinca alkaloid, anticancer drug
B= inhibits mitosis by inhibition of tubulin polymerization, which disrupts the assembly of the microtubules and subsequently the cytoskeleton and the mitotic spindle. This inhibtory effect results in mitotic arrest in metaphase, bringing cell division to a halt which then leads to cell death
C= treatment of acute leukaemia, malignant lymphoma, Hodgkin’s disease and non-Hodgkins lymphomas, acute erythraemia, rhabdomyosarcoma, neuroblastoma, Wilms tumor and acute panmyelosis

Question 14

Doxorubicin

Answer 14

A= anthracycline antibiotic, intercalating drug antitumor
B= oxygen free radicals bind to DNA causing single- and double-strand DNA breaks, binds to cellular membranes to alter fluidity and ion transport, inhibits topoisomerase II, binds to DNA through intercalation with consequent blockade of DNA and RNA synthesis, DNA strand scission,
C= Breast cancer, Hodgkins and non-hodgkins lymphoma, soft tissue sarcoma, ovarian cancer, non-small cell and small cell lung cancer, thyroid cancer, wilms tumor, neuroblastoma, cancers of testicles, stomach, bladder, liver

Question 15

Oxaliplatin

Answer 15

A= platinum analog, thrid generation diaminocyclohexane 
B= kill tumor cells in all stages of the cell cycle by forming intrastrand and interstrand DNA cross-links, binds to nuclear and cytoplasmic proteins and therefore leading to inhibition of DNA synthesis and function (primary binding site is N7 guanine)
C= colorectal cancer, gastroesophageal cancer, pancreatic cancer

Question 16

Etoposide

Answer 16

A=semisynthetic derivative of podophyllotoxin, antitumor
B= inhibits DNA synthesis by forming a complex with topoisomerase II and DNA. This complex induces breaks in double stranded DNA and prevents repair by topoisomerase II binding. Accumulated breaks in DNA prevent entry into the mitotic phase of cell division, and lead to cell death. Etoposide acts primarily in the G2 and S phases of the cell cycle
C= non-small cell and small cell lung cancer, gastric cancer, non-hodgkins lymphoma, germ cell cancer

Question 17

Paclitaxel

Answer 17

A= alkaloid ester of taxanes
B= inhibits mitosis by functioning as a mitotic spindle poison through high-affinity binding to microtubules with enhancement of tubulin polymerization. This promotion of microtubule assembly occurs in the absence of normally requred microtubule-associated proteins and GTP and therefore results in inhibition of mitosis and cell division
C= breast cancer, nonsmall cell and small cell lung cancer, ovarian cancer, gastroesophageal cancer, prostate cancer, bladder cancer, head and neck cancer, AIDS related Kaposis sarcoma