Chemotherapy drugs

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Questions and Answers

Drug metabolism in humans usually results in a product that is:

  • More likely to distribute intracellularly
  • Less lipid soluble than the original drug (correct)
  • More lipid soluble than the original drug
  • More likely to be reabsorbed by kidney tubules

Which of the following cytochrome isoforms is responsible for metabolizing the largest number of drugs?

  • CYP3A4 (correct)
  • CYP2C19
  • CYP1A2
  • CYP2C9

Your 37-year-old patient has been diagnosed with a rare metastatic carcinoid tumor. This neoplasm is releasing serotonin, bradykinin, and several unknown peptides. The effects of serotonin in this patient are most likely to include:

  • Episodes of bronchospasm
  • Constipation
  • Hypersecretion of gastric acid (correct)
  • Hypotension

Which drug does not activate opioid receptors, has been proposed as a maintenance drug in treatment programs for opioid addicts, and with a single oral dose, will block the effects of injected heroin for up to 48 h?

<p>Naltrexone (C)</p> Signup and view all the answers

Which drug is a full agonist at opioid receptors with analgesic activity equivalent to morphine, a longer duration of action, and fewer withdrawal signs on abrupt discontinuance than morphine?

<p>Methadone (B)</p> Signup and view all the answers

Total intravenous anesthesia with fentanyl has been selected for a frail elderly woman about to undergo cardiac surgery. Which statement about this anesthesia protocol is accurate?

<p>Patient awareness may occur during surgery, with recall after recovery (B)</p> Signup and view all the answers

A 32-year-old woman underwent segmental mastectomy for a breast tumor of 3 cm diameter. Lymph node sampling revealed 2 involved nodes. Because chemotherapy is of established value in her situation, she underwent postoperative treatment with antineoplastic drugs. The regimen consisted of doxorubicin followed by cyclophosphamide/methotrexate/fluorouracil. Adjunctive drugs included tamoxifen because the tumor cells were hormone receptor-positive. The chemotherapy undertaken by this patient caused acute hemorrhagic cystitis. Which drug was most likely to be responsible for this toxicity?

<p>Cyclophosphamide (D)</p> Signup and view all the answers

A 32-year-old woman underwent segmental mastectomy for a breast tumor of 3 cm diameter. Lymph node sampling revealed 2 involved nodes. Because chemotherapy is of established value in her situation, she underwent postoperative treatment with antineoplastic drugs. The regimen consisted of doxorubicin followed by cyclophosphamide/methotrexate/fluorouracil. Adjunctive drugs included tamoxifen because the tumor cells were hormone receptor-positive. After several cycles of chemotherapy, the patient was found to have a high resting pulse rate. A noninvasive radionuclide scan revealed evidence of cardiomyopathy. The drug that is most likely responsible for the cardiac toxicity is:

<p>Doxorubicin (B)</p> Signup and view all the answers

A patient with multiple myeloma was started on bortezomib after 2 rounds of other combination chemotherapy did not have any effect. What is the mechanism of action of bortezomib?

<p>Inhibition of the 26S proteasome (B)</p> Signup and view all the answers

An adult patient is being treated for acute leukemia with a combination of anticancer drugs that includes cyclophosphamide, mercaptopurine, methotrexate, vincristine, and prednisone. He is also using ondansetron for emesis, a chlorhexidine mouthwash to reduce mucositis, and laxatives. The patient complains of “pins and needle" sensations in the extremities and muscle weakness. He is not able to execute a deep knee bend or get up out of a chair without using his arm muscles. He is also very constipated. If these problems are related to the chemotherapy, which of the following is the most likely causative agent?

<p>Vincristine (A)</p> Signup and view all the answers

A cancer cell that is resistant to the effects of both vincristine and methotrexate probably has developed the resistance as a result of which of the following mechanisms?

<p>Increased expression of a P-glycoprotein transporter (A)</p> Signup and view all the answers

All the following agents have been used in drug regimens for the treatment of breast carcinoma. Which one has specific activity in a subset of female breast cancers?

<p>Trastuzumab (D)</p> Signup and view all the answers

Cyclosporine is effective in organ transplantation. Which of the following most accurately describes the immunosuppressant action of cyclosporine?

<p>Inhibition of the gene transcription of interleukins (D)</p> Signup and view all the answers

Which of the following is a widely used drug that suppresses cellular immunity, inhibits prostaglandin and leukotriene synthesis, and increases the catabolism of IgG antibodies?

<p>Prednisone (D)</p> Signup and view all the answers

A 36-year-old man presents with swollen, painful heels, nail changes, and left lower back pain that wakes him from sleep. The back pain gets better with exercise. He reports 1-2 h of morning stiffness. He has a history of psoriasis and psoriatic arthritis since age 12 years. You decide to change his current regimen of indomethacin to a biologic that targets TNF-α. Which of the following is a chimeric monoclonal antibody that binds to TNF-a and inhibits its action?

<p>Infliximab (B)</p> Signup and view all the answers

A 24-year-old woman underwent kidney transplantation. A week later, she developed alloantibody-mediated acute rejection (acute humoral rejection [AHR]). She was successfully treated with tacrolimus and a second drug that targets both B and T lymphocytes. Which of the following is an immunosuppressant that suppresses both B and T lymphocytes via inhibition of de novo synthesis of purines?

<p>Mycophenolate mofetil (B)</p> Signup and view all the answers

Which of the following is an immune modulator that increases phagocytosis by macrophages in patients with chronic granulomatous disease?

<p>Interferon-y (D)</p> Signup and view all the answers

A 30-year-old woman undergoes abdominal surgery. In spite of minimal tissue damage, complete ileus (absence of bowel motility) follows, and she complains of severe bloating. She also finds it difficult to urinate. Mild cholinomimetic stimulation with bethanechol or neostigmine is often effective in relieving these complications of surgery. Neostigmine and bethanechol in moderate doses have significantly different effects on which one of the following?

<p>Salivary glands (B)</p> Signup and view all the answers

Ms Brown has been treated for myasthenia gravis for several years. She reports to the emergency department complaining of recent onset of weakness of her hands, diplopia, and difficulty swallowing. She may be suffering from a change in response to her myasthenia therapy, that is, a cholinergic or a myasthenic crisis. Which of the following is the best drug for distinguishing between myasthenic crisis (insufficient therapy) and cholinergic crisis (excessive therapy)?

<p>Edrophonium (D)</p> Signup and view all the answers

The primary mechanism of antibacterial action of the penicillins involves inhibition of?

<p>Peptidoglycan cross-linking (C)</p> Signup and view all the answers

A patient needs antibiotic treatment for native valve, culture-positive infective enterococcal endocarditis. His medical history includes a severe anaphylactic reaction to penicillin G during the last year. The best approach would be treatment with?

<p>Vancomycin (D)</p> Signup and view all the answers

The mechanism of antibacterial action of tetracycline involves:

<p>Interference with binding of aminoacyl-tRNA to bacterial ribosomes (C)</p> Signup and view all the answers

The primary mechanism of resistance of gram-positive organisms to macrolide antibiotics including erythromycin is:

<p>Methylation of binding sites on the 50S ribosomal subunit (C)</p> Signup and view all the answers

A 26-year-old woman was treated for a suspected chlamydial infection at a neighborhood clinic. She was given a prescription for oral doxycycline to be taken for 14 d. Three weeks later, she returned to the clinic with a mucopurulent cervicitis. On questioning she admitted not having the prescription filled. The best course of action at this point would be to:

<p>Treat her in the clinic with a single oral dose of azithromycin (B)</p> Signup and view all the answers

Regarding the mechanism of action of aminoglycosides, the drugs:

<p>Cause misreading of the code on the mRNA template (C)</p> Signup and view all the answers

Which statement is accurate regarding the antibacterial action of the aminoglycoside amikacin?

<p>Efficacy is directly proportional to the duration of time that the plasma level is greater than the minimal inhibitory concentration (A)</p> Signup and view all the answers

Regarding the toxicity of aminoglycosides, which statement is accurate?

<p>Ototoxicity due to amikacin and gentamicin includes vestibular dysfunction, which is often irreversible (A)</p> Signup and view all the answers

Trimethoprim-sulfamethoxazole is established to be effective against which of the following opportunistic infections in the AIDS patient?

<p>Toxoplasmosis (A)</p> Signup and view all the answers

Which statement about the fluoroquinolones is accurate?

<p>Gonococcal resistance to fluoroquinolones may involve changes in DNA gyrase (A)</p> Signup and view all the answers

Which statement about ciprofloxacin is accurate?

<p>Tendinitis may occur during treatment (C)</p> Signup and view all the answers

Which statement about fluconazole is accurate?

<p>Does not penetrate the blood-brain barrier (A)</p> Signup and view all the answers

A 37-year-old woman with leukemia was undergoing chemotherapy with intravenous antineoplastic drugs. During treatment, she developed a systemic infection from an opportunistic pathogen. There was no erythema or edema at the catheter insertion site. A white vaginal discharge was observed. After appropriate specimens were obtained for culture, empiric antibiotic therapy was started with gentamicin, nafcillin, and ticarcillin intravenously. This regimen was maintained for 72 h, during which time the patient's condition did not improve significantly. Her throat was sore, and white plaques had appeared in her pharynx. On day 4, none of the cultures had shown any bacterial growth, but both the blood and urine cultures grew out Candida albicans. At this point, the best course of action is to:

<p>Stop current antibiotics and start amphotericin B (A)</p> Signup and view all the answers

A 27-year-old nursing mother is diagnosed as suffering from genital herpes. She has a history of this viral infection. Previously, she responded to a drug used topically. Apart from her current problem, she is in good health. Which drug to be used orally is most likely to be prescribed at this time?

<p>Valacyclovir (D)</p> Signup and view all the answers

More than 90% of this drug is excreted in the urine in intact form. Because its urinary solubility is low, patients should be well hydrated to prevent nephrotoxicity. Which drug is described?

<p>Acyclovir (D)</p> Signup and view all the answers

Among NSAIDs, aspirin is unique because it:

<p>Irreversibly inhibits its target enzyme-cyclooxygenase (B)</p> Signup and view all the answers

Which of the following is an analgesic and antipyretic drug that lacks an anti-inflammatory action?

<p>Acetaminophen (A)</p> Signup and view all the answers

A 16-year-old girl comes to the emergency department suffering from the effects of an aspirin overdose. Which of the following syndromes is this patient most likely to exhibit as a result of this drug overdose?

<p>Hyperthermia, metabolic acidosis, and coma (A)</p> Signup and view all the answers

Which of the following drugs is most likely to increase serum concentrations of conventional doses of methotrexate, a weak acid that is primarily cleared in the urine?

<p>Probenecid (B)</p> Signup and view all the answers

The main advantage of ketorolac over aspirin is that ketorolac:

<p>Is available in a parenteral formulation that can be injected intramuscularly or intravenously (A)</p> Signup and view all the answers

An 18-month-old boy dies from an accidental overdose of acetaminophen. Which of the following is the most likely cause of this patient's death?

<p>Liver failure (D)</p> Signup and view all the answers

Which antifungal agent is MOST likely to cause renal insufficiency?

<p>Amphotericin B (A)</p> Signup and view all the answers

Which drug is relatively free of drug-drug interactions?

<p>Micafungin (C)</p> Signup and view all the answers

Which drug works by creating pores/channels in the fungal cell membrane?

<p>Amphotericin B (C)</p> Signup and view all the answers

A 32-year-old man presents to an outpatient clinic with a 5-day history of productive cough, purulent sputum, and shortness of breath. He is diagnosed with community-acquired pneumonia (CAP). It is noted that this patient has a severe ampicillin allergy (anaphylaxis). Which would be an acceptable treatment for this patient?

<p>Levofloxacin (C)</p> Signup and view all the answers

Which is a common adverse effect of cotrimoxazole?

<p>Hyperkalemia (C)</p> Signup and view all the answers

The pharmacokinetics of a new drug are under study in a phase 1 clinical trial. Which statement about the distribution of drugs to specific tissues is most correct?

<p>Distribution into a tissue depends on the unbound drug concentration gradient between blood and the tissue (B)</p> Signup and view all the answers

Flashcards

Drug Metabolism Outcome

Drug metabolism usually results in a product that is less lipid soluble than the original drug, facilitating excretion.

Most Common CYP450 Isoform

CYP3A4 is the cytochrome P450 isoform responsible for metabolizing the largest number of drugs.

Serotonin Effects

Serotonin effects include episodes of bronchospasm.

Opioid Addiction Treatment Drug

Naltrexone is an opioid receptor blocker used for opioid addiction treatment.

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Opioid Agonist with Long Action

Methadone is a full opioid agonist with a long duration of action and milder withdrawal.

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Fentanyl Anesthesia Consideration

Patient awareness may occur during surgery with fentanyl.

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Cyclophosphamide Toxicity

Cyclophosphamide can cause acute hemorrhagic cystitis.

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Doxorubicin Cardiotoxicity

Doxorubicin is cardiotoxic and can cause cardiomyopathy.

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Bortezomib Mechanism

Bortezomib inhibits the 26S proteasome.

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Vincristine Toxicity

Vincristine's toxicity is "pins and needles."

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Drug Resistance Mechanism

Increased P-glycoprotein transporter expression leads to resistance to vincristine and methotrexate.

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Breast Cancer Treatment

Trastuzumab is for breast cancers.

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Cyclosporine Action

Cyclosporine inhibits gene transcription of interleukins.

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Prednisone Effects

Prednisone suppresses cellular immunity, inhibits prostaglandin and leukotriene synthesis, and increases IgG catabolism.

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Infliximab Action

Infliximab is a chimeric monoclonal antibody that binds to and inhibits TNF-alpha.

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Mycophenolate Mofetil

Mycophenolate mofetil suppresses B and T lymphocytes via inhibition of de novo synthesis of purines.

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Immune modulator

Interferon-gamma increases phagocytosis.

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Neostigmine vs Bethanechol

Neostigmine and bethanechol have different effects on vascular endothelium.

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Crisis Differentiation

Edrophonium distinguishes between myasthenic crisis and cholinergic crisis.

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Penicillin Mechanism

Penicillins inhibit peptidoglycan cross-linking, preventing bacterial cell wall synthesis.

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Patient allergy w/ endocarditis

Treat with Vancomycin following reaction to penicillin

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Tetracycline Action

Tetracycline impairs binding of aminoacyl-tRNA to bacterial ribosomes, halting protein synthesis.

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Macrolide Resistance

Methylation of binding sites on the 50S ribosomal subunit is the primary macrolide resistance mechanism.

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Cervicitis Treatment

Treat cervicitis with single-dose oral azithromycin

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Aminoglycoside Mechanism

Aminoglycosides cause misreading of the code on the mRNA template.

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Aminoglycoside Action

Aminoglycosides have concentration-dependent antibacterial action and continue to exert effects after plasma levels decrease.

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Aminoglycoside Toxicity

Aminoglycoside ototoxicity includes vestibular dysfunction, which is often irreversible.

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Opportunistic Infection Treatment

Trimethoprim-sulfamethoxazole is effective against toxoplasmosis.

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Fluoroquinolone Resistance

Gonococcal resistance to fluoroquinolones may involve changes in DNA gyrase.

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Ciprofloxacin Toxicity

Tendinitis may occur during ciprofloxacin treatment.

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Study Notes

  • Drug metabolism usually results in a product less lipid soluble than the original drug.
  • CYP3A4 metabolizes the largest number of drugs.
  • Serotonin effects in a patient with a metastatic carcinoid tumor are most likely to include hypotension.
  • Naltrexone does not activate opioid receptors and blocks the effects of injected heroin for up to 48 hours with a single oral dose, and is proposed as a maintenance drug
  • Methadone is a full agonist at opioid receptors with analgesic activity equivalent to morphine, a longer duration of action, and fewer withdrawal signs.
  • It is inaccurate to specify that Fentanyl will control the hypertensive response to surgical stimulation
  • Cyclophosphamide caused acute hemorrhagic cystitis as a toxicity
  • Doxorubicin is most likely responsible for cardiac toxicity
  • Bortezomib inhibits the 26S proteasome
  • Vincristine is the likely cause of "pins and needles" sensations, muscle weakness, and constipation
  • A cancer cell resistant to vincristine and methotrexate has likely developed resistance through increased expression of a P-glycoprotein transporter.
  • Trastuzumab has specific activity in a subset of female breast cancers.
  • Cyclosporine's immunosuppressant action inhibits the gene transcription of interleukins.
  • Prednisone suppresses cellular immunity, inhibits prostaglandin and leukotriene synthesis, and increases the catabolism of IgG antibodies.
  • Infliximab is a chimeric monoclonal antibody that binds to TNF-α and inhibits its action
  • Mycophenolate mofetil suppresses both B and T lymphocytes
  • Interferon-y is an immune modulator that increases phagocytosis
  • Neostigmine and bethanechol have different effects on gastric secretory cells.
  • Edrophonium is the best drug for distinguishing between myasthenic crisis (insufficient therapy) and cholinergic crisis (excessive therapy).
  • Penicillins inhibit peptidoglycan cross-linking
  • Vancomycin is the best approach treating a patient needing antibiotic treatment for native valve
  • Tetracycline interferes with binding of aminoacyl-tRNA
  • Gram-positive organisms achieve resistance to macrolide antibiotics through methylation of binding sites on the 50S ribosomal subunit.
  • The best course of action is to treat her with a single dose of azithromycin
  • Aminoglycosides cause misreading of the code on the mRNA template.
  • Efficacy of amikacin is directly proportional to the duration of time
  • Ototoxicity due to amikacin and gentamicin includes vestibular dysfunction, which is often irreversible
  • Trimethoprim-sulfamethoxazole is effective against Toxoplasmosis.

Fluoroquinolones

  • Gonococcal resistance to fluoroquinolones may involve changes in DNA gyrase
  • Tendinitis may occur during Ciprofloxacin treatment
  • Fluconazole does not penetrate the blood-brain barrier
  • Stop current antibiotics and start amphotericin B since Cultures grew out Candida albicans
  • Itraconazole is the best medication for the condition presented
  • Valacyclovir is the most suitable prescription.
  • Acyclovir needs more than 90% of drug excretion
  • Hemorrhagic stroke is most likely due to a 55-year-old lawyer
  • Aspirin uniquely and irreversibly inhibits its target enzyme-cyclooxygenase among NSAIDs.
  • Acetaminophen lacks anti-inflammatory action
  • Hyperthermia, metabolic acidosis, and coma is common syndrome of aspirin overdose
  • Probenecid increases serum concentrations
  • Ketorolac is available and can be injected intramuscularly or intravenously
  • Liver failure is most likely the cause of death
  • Allopurinol may be most effective
  • Amphotericin B is MOST likely to cause renal insufficiency.
  • The answer is Terbinafine
  • Micafungin is relatively free of drug-drug interactions.
  • Amphotericin B is the dug affecting the fungal cell membrane
  • Levofloxacin may be acceptable for this patient since he has a severe ampicillin allergy
  • Nitrofurantoin should be avoided in the treatment of her UTI
  • Hyperkalemia is a common adverse effect of cotrimoxazole
  • Distribution into a tissue depends on the unbound drug concentration gradient between blood and the tissue
  • Animal tests cannot be used to predict the types of clinical toxicities that may occur because there is no correlation with human toxicity

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