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Pharmacology - Final - Part 1

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davidwurbel7's version from 2016-08-05 12:48

GI 1

Question Answer
Gastrin, Histamine and Ach do this in the stomachAcid Production
Prostaglandins do this in the stomachMucus Production
Side effects of Magnesium hydroxideDiarrhea
Side effects of Aluminum hydroxideConstipation
Side effects of Calcium Carbonate and Sodium bicarbonateBelching, Metabolic alkalosis, Milk Alkali Syndrome
Reduce only the basal acid secretion. Doesn’t reduce the meal stimulated acid secretionH2 Receptor Blockers
This H2 blocker is least potent. Adverse effects include antiandrogenic effects, gynaecomastia, galactorrhea and CYP-450 inhibitionCimetidine
The mechanism of action is irreversible, suicide inhibition of H+/K+-ATPase and thus blocks the final common pathway of acid secretionProton Pump Inhibitors
DOC for both prevention and treatment of NSAID induced ulcers.Proton Pump Inhibitors
DOC for Zollinger Ellison SyndromeProton Pump Inhibitors
Mechanism of action stimulates the EP-3 on parietal cells and increases the mucus and bicarbonate secretion and mucosal blood flowMisoprostol
Mechanism of action reduces the acid secretionMisoprostol
A salt of sucrose complexed to sulfated aluminum hydroxideSucralfate
In water or acidic solutions it forms a viscous, tenacious paste, that binds selectively to base of ulcers or erosions, forms a physical barrier and coats the ulcersSucralfate
Prevention of traveler's diarrhea. Black discoloration of the stool and tongueBismuth
PPI +Clarithromycin+ Amoxicillin or Metronidazole or TinidazoleTriple Regiment
PPIs+ Bismuth+ Metronidazole+ TetracyclineQuadruple Regiment
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GI 2

Question Answer
Antidiarrheal agents that are opioid derivativesLoperamide, diphenoxylate
Actions include increases tone of anal sphincter, decreases propulsive movements and decreases intestinal secretion & enhancing absorptionLoperamide, diphenoxylate
Increase in fiber will add bulk to the stoolsBulk Forming Laxatives
Anionic surfactants that enable additional water and fats to be incorporated in the stoolStool Softeners
Retain water in colon and exert osmotic effectOsmotic Laxatives
Magnesium hydroxide, polyethylene glycol, lactulose, magnesium citrateOsmotic Laxatives
Chloride channel activator for IBS with predominant constipationLubiprostone
Disorder associated with episodes of abdominal discomfort (pain, bloating, distention, or cramps) + diarrhea or constipationIBS
5-HT3 antagonist for IBS with diarrheaAlosetron
First line drugs in mild or moderate ulcerative colitis and also in Crohn’s disease. They are more effective in maintaining than in achieving clinical remissionSulfasalazine and Mesalamine
Mechanism of action inhibition of PGs and leukotriene biosynthesisSulfasalazine and Mesalamine
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(Insert 15-17)
Question Answer
Acts on the CTZ to stimulate the opioid receptors to induce vomitingApomorphine
D2 selective dopamine antagonist. Crosses the blood brain barrier. Hyperprolactenemia, extrapyramidal effects are side effects. Anti-emetic effectMetoclopramide
D2 selective dopamine antagonist. Does not cross blood brain barrier and no extra pyramidal effects. Causes hyperprolactenemia (dopamine inhibits prolactin release)Domperidone
Causes ventricular arrhythmia by torsade's de pointes (when combined with CYP450 inhibitors-ketoconazole, macrolides)Cisapride
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Chemotherapy Drugs

Question Answer
The ratio of proliferating cells to cells in G0Growth Fraction
Antimetabolites, Bleomycin, Podophyllin Alkaloids and Plant AlkaloidsCell Cycle Specific Agents
Alkylating Agents, Antibiotics, Cisplatin and NitrosoureasCell Cycle Non-Specific Agents
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(Insert 6)
Question Answer
Advantages include suppression of drug resistance, increased cancer cell kill and reduced injury to normal cellsCombination Therapy
Increased expression of this gene for a cell surface p-glycoprotein will increase resistance to cytotoxic drugsMDR-1
MDR-1 gene is involved with thisDrug Efflux
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(Insert 11)
Question Answer
G-CSF and GM-CSF are used as adjuncts to chemotherapy for thisLeukopenia
Leukopenia due to chemotherapy can be treated with thisG-CSF and GM-CSF
EPO is used as an adjunct to chemotherapy for thisAnemia
Anemia due to chemotherapy can be treated with thisEPO
Bleomycin, Cisplatin and Vincristine collectively has this effect on the bone marrowMarrow Sparing
This drug is used to treat hemorrhagic cystitis due to cyclophosphamideMercaptoethane Sulfonate (MESNA)
Cyclphosphamide, Chlorambucil, Thiotepa, Busulfan, Carmustine and Lomustine are example of this class of anticancer drugsAlkylating Agents
Cyclphosphamide and Chlorambucil are this type of alkylating agentsNitrogen Mustards
Alkylation of the DNA occurs at this site in the DNA by Alkylating agents by forming either an ethyleneimonium or a carboniumN7 Position of Guanine
Mechlorethamine is used in the regime for treatment of this cancerHogkin's Lymphoma
This non-enzymatic metabolite of cyclophosphamide causes Hemorrhagic CystitisAcrolein
This is the active form metabolite of cyclophosphamideHydroxycyclophosphamide
Carmustine, Lomustine and Semustine are examples of this class of alkylating agentsNitrosoureas
All drugs in this class of drugs can cross the blood brain barrier and are used in brain tumorsNitrosoureas
Cisplatin, Carboplatin and Oxaliplatin are example of this class of alkylating agentsPlatinum Alkylating Agent
This drug can be used to counteract the nephrotoxicity of cisplatinMannitol or Amifostine
Nephrotoxicity and ototoxicity are unique toxicities of this drugCisplatin
Leukemogenic toxicity is unique of this drugProcarbazine
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(Insert 25)
Question Answer
Methotrexate, Mercaptopurine, Fluorouracil are examples of this class of anticancer drugsAntimetabolites
The mechanism of action is the inhibition of dihydrofolate reductaseMethotrexate
The toxic effects of methotrexate can be reduced by administration of this drug as an adjunctLeucovorin
The mechanism of resistance to this drug is alteration of dihydrofolate reductaseMethotrexate
Uses for this drug are Acute leukemia, choriocarcinoma, osteosarcoma, Burkitt’s and non-Hodgkin’s lymphomas, Ca breast. Psoriasis, rheumatoid arthritis (as a immunosuppressant) and as an abortifacientMethotrexate
S phase specific purine antagonistMercaptopurine(6-MP)
The prodrug mercaptopurine is activated by this enzymeHypoxanthine Guanine Phosphoribosyl Transferase (HGPRT)
Mercaptopurine will have an increased toxicity with this drug because mercaptopurine is metabolized by xanthine oxidaseAllopurinol
Acute leukemia (ALL, AML) can be treated with this drugMercaptopurine
The mechanism of action is the inhibition of thymidylate synthetase5-Flurouracil
The drug is part of the regime for colorectal cancer5-Flurouracil
5-Flurouracil with oxaliplatin and leucovorin are used to treat this cancerColorectal Cancer
Acute myelogenous leukemiaCytarabine
Pancreatic cencer and small cell lung cancerGemcitabine
Vinca alkaloids and taxanes act in this phase of the cell cycleM Phase
This drug terminates the formation of microtubules by forming a complex with tubulinVinca Alkaloids
Toxicity is bone marrow suppression and alopecia. Uses in ABVD regime for Hodgkin's disease, breast cancer and testicular cancerVinblastine
Toxicity is peripheral neuritis. It has a marrow sparing effect. Used as part of MOPP regime for Hodgkin's disease, childhood tumors (Wilms' tumor), choriocarcinoma and childhood leukemiasVincristine
Peripheral neuritis is the toxicity of this drugVincristine
Vincristine has this toxicityPeripheral Neuritis
This drug prevents microtubule disassembly by enhancing tubulin polymerizationTaxanes
Mechanism of Action of this drug is as a mitotic “spindle poison” through the enhancement of tubulin polymerization. They prevent micotubule disassembly into tubulin monomersTaxanes
Taxanes have this toxicityNeurotoxicity
Neurotoxicity is the toxicity seen with this class ofTaxanes
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(Insert 46)
Question Answer
The mechanism of action of this class of drugs interfere with the activity of Topoisomerase I- breaks and reseals single-stranded DNA..Resulting in DNA damageCamptothecins
The toxicity of this Camptothecin is severe diarrhea Irinotecan
The use for this drug is for treatment with metastatic ovarian cancer (cisplatin-resistant)Topotecan
The use for this drug is for treatment with colon and rectal cancerIrinotecan
The mechanism of Action is intercalation between DNA, resulting in blockade of DNA and RNA synthesis. Inhibits Topoisomerase II and generation of the oxygen radicalsDoxorubicin
Toxicity includes Bone marrow depression, Total alopecia and Cardiac toxicity- dilated cardiomyopathy can cause arrhythmias and heart failure due to generation of oxygen free radicalsAnthracyclines
An iron chelating agent – prevents formation of free radicals – protect against cardiotoxicity. Used as an adjunct to AnthracyclinesDexrazoxane
Part of the ABVD regimen for Hodgkin’s disease ,carcinomas of the breast, endometrium, ovary, testicle, thyroid, and lung, and osteosarcomaDoxorubicin
Anthracyclines used for acute leukemiaDaunorubicin
The mechanism of action is binds to double stranded DNA through intercalation between adjacent guanine-cytosine base pairsDactinomycin
Therapeutic Uses include Wilms’ tumors and MelanomaDactinomycin
The mechanism of action is it acts in G2 phase intercalation between DNA and complexes with Fe and O2 which leads to DNA strand scissionBleomycin
Toxicity of this drug is pulmonary fibrosisBelomycin
Selective estrogen receptor modulator (SERM) that has antiestrogenic effects on breast tissue. Binds to estrogen receptors (ER) and induces conformational changes in the receptor. Resulting in decreased estrogen responseTamoxifen
Used as primary therapy for metastatic breast cancer. Patients with estrogen-receptor (ER) positive tumorsTamoxifen
The mechanism of action is androgen(testosterone) receptor blockerFlutamide
Used in Carcinoma prostate with GnRH agonist (leuprolide)Flutamide
MOA: act as GnRH agonist- inhibits the release of FSH and LH. Resulting in reduced testicular androgen synthesisLeuprolide
Inhibitor of adrenal steroid synthesis at the first step, conversion of cholesterol to pregnenoloneAminogluthethimide
Inhibits the enzyme aromatase that converts androstenedione to estroneAnastrozole, Letrozole
Use: Advanced Ca breast that is no longer responsive to tamoxifenAminogluthethimide, Anastrozole, Letrozole
Widely used Glucocorticoid in cancer chemotherapy. Used as part of the MOPP. Used for leukemias and lymphomasPrednisone
An enzyme isolated from bacteria. Catalyzes the deamination of asparagine to aspartic acid and ammonia. The mechanism of action neoplastic cells require an external source of asparagine because of their limited capacity to synthesize sufficient amounts of that amino acid to support growth and functionAsparaginase
Used childhood acute leukemiaAsparaginase
Toxicity effects include anaphylactic shock and acute pancreatitisAsparaginase
Inhibits the enzyme ribonucleotide reductase. Resulting in the depletion of deoxynucleoside triphosphate pools. Thereby inhibiting DNA synthesis. S-phase specific agent. Use: Chronic myelogenous leukemiaHydroxyurea
This can be used in hairy cell leukemia and T cell lymphomaInteferon Alpha
Monoclonal antibody against CD20 antigen. Used in non-Hodgkins lymphomaRituximab
Monoclonal antibody against HER-2 antigen. Used in HER2 +ve Breast cancerTrastuzumab
Inhibits the tyrosine kinase activity of protein product of Bcr-Abl oncogene commonly expressed in CML and is used Ph+ Chronic myeloid leukemiaImatinib
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Specific Treatment
Question Answer
ABVD regimen (Adriamycin,bleomycin,vinblastine,dacarbazine) or MOPP regimen (mechlorethamine,vincristine(oncovin),procarbazine,prednisone)Hodgkin’s disease
R-CHOP regimen (Rituximab, cyclophosphamide, doxorubicin, vincristine, prednisone)Non-Hodgkin’s Lymphoma
MP protocol (melphalan and prednisone)Multiple Myeloma
Tamoxifen or CAF regimen (Cyclophosphamide+adriamycin+ fluorouracil) or CMF protocol (cyclophosphamide+methotrexate+fluorouracil) or Anastrozole, letrozoleCa Breast
Cisplatin+Etoposide/IrinotecanSmall cell lung cancer
BEP (Bleomycin, etoposide, cisplatin) or PVB (Cisplatin, vinblastine, bleomycin )Testicular cancer
Leuprolide (LH Releasing Hormone agonist)+ Flutamide (antiandrogen)Prostate Ca
M-VAC (Mtx, vinblastine, adriamycin, cisplatin)Ca Bladder
FOLFOX (fluorouracil + oxaliplatin+leucovorin)Colorectal cancer
Methotrexate+leucovorinChoriocarcinoma
Carmustine/ lomustine/semustineBrain cancer
Imatinib / Hydroxyurea/busulfan/Bone marrow transplantationCML
Cytarabine+ idarubicinAML
For induction:Vincristine+prednisone, Maintainance: methotrexate, MercaptopurineALL
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Management Chemotherapy Induced Toxicity
Question Answer
Nausea and vomiting5-HT3 antagonist (ondansetron)
Bone marrow suppressionFilgrastim, Sargromastim (colony stimulating factors)
Methotrexate toxicityLeucovorin
Cyclophosphamide induced toxicityMESNA
Cisplatin induced nephrotoxicityMannitol/Amifostine
Anthracycline incuced cardiotoxicityDexrazoxane
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