Analgesic Drugs Overview
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Questions and Answers

What is the main therapeutic action of the drug that influences ionic channels in nerve membranes?

  • Increasing conduction through nerve pathways
  • Decreasing excitability and hyperexcitability (correct)
  • Increasing excitability to stimulation
  • Suppressing overall CNS activity
  • Which of the following drugs is known to increase plasma levels of phenytoin?

  • Isoniazid (correct)
  • Warfarin
  • Phenobarbital
  • Carbamazepine
  • What is the therapeutic level range for phenytoin in mcg/mL?

  • 5 to 15
  • 10 to 20 (correct)
  • 15 to 25
  • 20 to 30
  • What is the action of ketorolac in pain management?

    <p>It inhibits prostaglandin synthesis.</p> Signup and view all the answers

    CNS depressant effects of which substances are known to add to those of phenytoin?

    <p>Alcohol and barbiturates</p> Signup and view all the answers

    Which condition is phenytoin primarily used to treat?

    <p>Seizures and digoxin-induced dysrhythmias</p> Signup and view all the answers

    What is the recommended frequency for administering ketorolac intramuscularly to adults?

    <p>Every 6 hours</p> Signup and view all the answers

    What is a common adverse effect of NSAIDs when taken without food?

    <p>Gastric irritation</p> Signup and view all the answers

    How often should CBC and calcium levels be monitored in patients under this treatment?

    <p>Every 6 months</p> Signup and view all the answers

    What timeframe does analgesia from parenteral ketorolac typically begin?

    <p>Within 30 minutes</p> Signup and view all the answers

    Which of the following drugs is a known inducer that decreases plasma levels of phenytoin?

    <p>Carbamazepine</p> Signup and view all the answers

    Which of the following assessments is essential for patients on phenytoin?

    <p>Monitor serum drug levels and hepatic function</p> Signup and view all the answers

    How is ketorolac available for administration?

    <p>Orally, intravenously, and intranasally</p> Signup and view all the answers

    What differentiates benzodiazepines from other medications in terms of pharmacokinetics?

    <p>They are highly protein-bound in the bloodstream.</p> Signup and view all the answers

    Which patient population may experience prolonged half-life of benzodiazepines?

    <p>Older adults and those with renal impairment</p> Signup and view all the answers

    What should be encouraged in postoperative patients to prevent atelectasis?

    <p>Turning, coughing, and deep breathing every 2 hours</p> Signup and view all the answers

    What is the protein binding percentage of phenytoin?

    <p>90% to 95%</p> Signup and view all the answers

    What is the half-life range of phenytoin?

    <p>7 to 42 hours</p> Signup and view all the answers

    What should be done to prevent phenytoin absorption interference during tube feeding?

    <p>Stop tube feedings for 2 hours before and after</p> Signup and view all the answers

    Which intravenous solution should not be mixed with phenytoin?

    <p>Dextrose 5% in water (D5W)</p> Signup and view all the answers

    During intravenous administration of phenytoin, what vital signs must be monitored?

    <p>Vital signs, blood pressure, and electrocardiography</p> Signup and view all the answers

    How long should any unused drug be discarded after preparation for IV administration?

    <p>4 hours</p> Signup and view all the answers

    What is the effect of a decrease in serum protein or albumin levels on phenytoin?

    <p>It increases the free phenytoin serum level.</p> Signup and view all the answers

    Which type of tumor cells are generally more sensitive to chemotherapy?

    <p>Rapidly dividing cells</p> Signup and view all the answers

    What is the primary mechanism of action of cetuximab?

    <p>It acts as a competitive antagonist at EGFRs.</p> Signup and view all the answers

    Which adverse effect is commonly associated with cetuximab therapy?

    <p>Infusion reactions</p> Signup and view all the answers

    In what condition is cetuximab primarily used?

    <p>Metastatic EGFR-positive colorectal cancer</p> Signup and view all the answers

    What percentage of patients developed severe hypomagnesemia while on cetuximab in clinical trials?

    <p>6% to 17%</p> Signup and view all the answers

    How is cetuximab administered to patients?

    <p>Slow IV infusion</p> Signup and view all the answers

    What is the initial loading dose of cetuximab for treatment?

    <p>400 mg/m2 over 2 hours</p> Signup and view all the answers

    Cetuximab therapy may lead to which gastrointestinal toxicity?

    <p>Diarrhea</p> Signup and view all the answers

    Which type of cancer is not indicated for cetuximab therapy?

    <p>Pancreatic cancer</p> Signup and view all the answers

    What is the primary mechanism of action of leuprolide therapy in breast cancer prevention?

    <p>Mimics the effects of orchiectomy</p> Signup and view all the answers

    Which of the following is an indication for toremifene therapy?

    <p>ER-positive tumors in postmenopausal women</p> Signup and view all the answers

    What is a common adverse effect associated with leuprolide treatment?

    <p>Hot flashes</p> Signup and view all the answers

    What is a key pharmacokinetic characteristic of toremifene?

    <p>Plasma levels peak in 3 hours after oral administration</p> Signup and view all the answers

    What potential risk is associated with reduced testosterone levels due to leuprolide therapy?

    <p>New-onset diabetes</p> Signup and view all the answers

    How can bone loss associated with leuprolide therapy be mitigated?

    <p>By adequate calcium and vitamin D intake</p> Signup and view all the answers

    What is the recommended daily dosage for the short-acting leuprolide injection?

    <p>1 mg</p> Signup and view all the answers

    What class of drug is fulvestrant, and what is its primary action?

    <p>An antiestrogen; acts as a pure estrogen receptor antagonist</p> Signup and view all the answers

    Which chemotherapeutic agent is specifically indicated for metastatic breast cancer and colon cancer?

    <p>Capecitabine</p> Signup and view all the answers

    What is the primary route of administration for Cytarabine?

    <p>Injectable</p> Signup and view all the answers

    Which adverse effect is NOT commonly associated with Capecitabine?

    <p>Cytarabine syndrome</p> Signup and view all the answers

    What condition contraindicates the use of Capecitabine?

    <p>Known hypersensitivity to fluorouracil</p> Signup and view all the answers

    What type of tumors are mitotic inhibitors primarily used to treat?

    <p>Solid tumors and some hematologic malignancies</p> Signup and view all the answers

    What is a unique adverse effect associated with Cytarabine?

    <p>Cytarabine syndrome</p> Signup and view all the answers

    Which pyrimidine antagonist is available only in tablet form?

    <p>Capecitabine</p> Signup and view all the answers

    What type of cancer is Cytarabine primarily used for?

    <p>Leukemias</p> Signup and view all the answers

    Signup and view all the answers

    Study Notes

    Analgesic Drugs

    • Analgesic drugs, opium is a Greek word meaning "juice".
    • Three main receptor families: μ (mu, MOR), κ (kappa, KOR), δ (delta, DOR).
    • Opioid agonist: MORPHINE, a prototype opioid from the opium poppy.
    • Mechanism of action: mimics endogenous opioid peptides, mainly at mu receptors.
    • Therapeutic uses: acute pain from AMI and cancer, cough suppression, dyspnea relief from pulmonary edema, preoperative anxiety relief.
    • Adverse effects: orthostatic hypotension, miosis, urinary retention, constipation, emesis, respiratory depression, drowsiness, dysphoria, neurotoxicity, tolerance and physical dependence, withdrawal syndrome.
    • Contraindications and cautions: allergy to narcotic agonists, toxic poisons, respiratory dysfunction.
    • Drug interactions: CNS depressants, anticholinergic drugs, hypotensive drugs, monoamine oxidase inhibitors.
    • Agonist-antagonist Opioids: lower potential for abuse, less respiratory depression.
    • Nalbuphine: agonist at kappa receptors and antagonist at mu receptors, with dosage-dependent ceiling effect.

    Fentanyl

    • A potent opioid analgesic (100x morphine potency).
    • Formulations: parenteral, transdermal, transmucosal, intranasal.
    • Transdermal fentanyl patches: reservoir in skin, delayed onset, prolonged offset, for chronic severe pain management, requires prior daily opioid use.
    • Transmucosal fentanyl: lozenges, buccal tablets, sublingual spray, sublingual tablets, for breakthrough cancer pain in opioid-tolerant patients.
    • Ionsys: patient-activated system for on-demand delivery of fentanyl (iontophoresis-based), for acute postoperative pain.
    • Contraindications: heat application over a patch, history of respiratory depression, and shock.

    Butorphanol

    • Agonist at kappa receptors and antagonist at mu receptors.
    • Analgesic effects are less potent than morphine.
    • Used for moderate to moderately severe pain.

    Naloxone

    • Opioid antagonist (antidote).
    • Blocks opioid receptors, reversing respiratory depression, sedation, and psychotomimetic effects.
    • Indications: opioid overdose and postoperative opioid depression.

    Non-steroidal anti-inflammatory drugs (NSAIDs)

    • Ketorolac: short-term pain management, often equal or superior to opioids in analgesic efficacy.

    Benzodiazepines

    • Common sedative-hypnotics and anxiolytics.
    • Indications: anxiety, insomnia, seizure disorders, muscle spasms, alcohol withdrawal.
    • Adverse effects: CNS depression, anterograde amnesia, sleep-driving/related behaviors, paradoxical effects, respiratory depression.
    • Interactions with CNS depressants.

    Hydantoins (Phenytoin)

    • Anticonvulsant, effective in treating tonic-clonic and partial seizures.
    • Adverse effects include gingival hyperplasia, dermatologic effects, pregnancy effects, cardiovascular effects, and potential drug interactions.

    Chemotherapy

    • Aims to eliminate cancerous cells.
    • Principles: target DNA/metabolism, affect replication of all proliferating cells.
    • Treatment strategies: curative goals, control of disease, symptomatic relief, use as adjuvant or neoadjuvant/maintenance therapy.
    • Tumor susceptibility: rapidly dividing cells are more susceptible to treatment.
    • Combination chemotherapy: higher response rates, overlapping host toxicities, improved cell-killing effectiveness.
    • Resistance: intrinsic or acquired, multidrug resistance, step-wise selection of amplification of drug efflux genes (e.g., P-glycoprotein).
    • Toxicity: bone marrow suppression (myelosuppression), extravasation (leakage into surrounding tissues), fertility reduction, related to killing rapidly dividing cells in other tissues.

    Anti-metabolites

    • Structurally similar to normal compounds that exist within cells.
    • Interfere with synthesis of purine or pyrimidine nucleotides, inhibiting synthesis or competing in DNA/RNA synthesis.
    • Methotrexate (MTX), pemetrexed, and pralatrexate.
    • Purine antagonists: cladribine, fludarabine, mercaptopurine, pentostatin, and thioguanine.
    • Pyrimidine antagonists: capecitabine, cytarabine, floxuridine, fluorouracil, and gemcitabine.
    • Adverse effects: varied and potential for serious complications.

    Mitotic Inhibitors

    • Natural products or semisynthetic drugs from plants.
    • Bind to tubulin, preventing assembly of microtubules critical to mitosis, inhibiting cell division.
    • Vinca alkaloids (vinblastine, vincristine, and vinorelbine).
    • Taxanes (paclitaxel).

    Topoisomerase Inhibitors

    • Topotecan and irinotecan.
    • Inhibit DNA-topoisomerase I actions, resulting in DNA strand breaks.
    • Treatment for ovarian and colorectal cancer and small cell lung cancer.
    • Important interactions exist between different agents.

    Hormonal Agents

    • Used in breast and prostate cancer treatment.
    • Breast cancer: antiestrogens (tamoxifen, toremifene), aromatase inhibitors (anastrozole).
    • Prostate cancer: androgen deprivation therapy (ADT) agents like leuprolide, goserelin, and histrelin.
    • Mechanism: blocking or suppressing endogenous hormones impacting tumor growth.
    • Potential adverse effects: diverse, reflecting hormone disruption.

    Targeted Anticancer Drugs

    • Designed to bind specific targets within or on cancer cells, suppressing tumor growth, with reduced impact on healthy cells.
    • EGFR tyrosine kinase inhibitors (e.g., cetuximab): block EGFR receptors, used in colorectal, head, and neck cancers.
    • Side effects can be severe if not managed properly.

    Eye Medications

    • Miotics: contract pupils, increasing aqueous outflow for glaucoma.
    • Mydriatics: dilate pupils for eye exams, procedures.
    • Anti-infectives/anti-microbials: treat eye infections.
    • Lubricants: relieve dry eye symptoms.
    • Osmotics: manage elevated intraocular pressure.

    Ear Medications

    • Antibiotics for ear infections.
    • Analgesics for pain relief.
    • Anti-inflammatory drugs.
    • Anti-viral drugs.
    • Ceruminolytics to aid in impaction removal.

    Vestibular Disorders

    • Symptoms: dizziness, unsteadiness, vertigo, nausea.
    • Underlying causes: Meniere's disease, labyrinthitis, inner ear infections.

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    Description

    This quiz explores the fundamentals of analgesic drugs, focusing on opioid mechanisms, therapeutic uses, and adverse effects. Learn about the different receptor families, drug interactions, and contraindications related to these powerful pain-relieving medications. Understand the implications of using agonist-antagonist opioids in clinical practice.

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