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Questions and Answers
What is the main therapeutic action of the drug that influences ionic channels in nerve membranes?
What is the main therapeutic action of the drug that influences ionic channels in nerve membranes?
Which of the following drugs is known to increase plasma levels of phenytoin?
Which of the following drugs is known to increase plasma levels of phenytoin?
What is the therapeutic level range for phenytoin in mcg/mL?
What is the therapeutic level range for phenytoin in mcg/mL?
What is the action of ketorolac in pain management?
What is the action of ketorolac in pain management?
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CNS depressant effects of which substances are known to add to those of phenytoin?
CNS depressant effects of which substances are known to add to those of phenytoin?
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Which condition is phenytoin primarily used to treat?
Which condition is phenytoin primarily used to treat?
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What is the recommended frequency for administering ketorolac intramuscularly to adults?
What is the recommended frequency for administering ketorolac intramuscularly to adults?
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What is a common adverse effect of NSAIDs when taken without food?
What is a common adverse effect of NSAIDs when taken without food?
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How often should CBC and calcium levels be monitored in patients under this treatment?
How often should CBC and calcium levels be monitored in patients under this treatment?
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What timeframe does analgesia from parenteral ketorolac typically begin?
What timeframe does analgesia from parenteral ketorolac typically begin?
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Which of the following drugs is a known inducer that decreases plasma levels of phenytoin?
Which of the following drugs is a known inducer that decreases plasma levels of phenytoin?
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Which of the following assessments is essential for patients on phenytoin?
Which of the following assessments is essential for patients on phenytoin?
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How is ketorolac available for administration?
How is ketorolac available for administration?
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What differentiates benzodiazepines from other medications in terms of pharmacokinetics?
What differentiates benzodiazepines from other medications in terms of pharmacokinetics?
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Which patient population may experience prolonged half-life of benzodiazepines?
Which patient population may experience prolonged half-life of benzodiazepines?
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What should be encouraged in postoperative patients to prevent atelectasis?
What should be encouraged in postoperative patients to prevent atelectasis?
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What is the protein binding percentage of phenytoin?
What is the protein binding percentage of phenytoin?
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What is the half-life range of phenytoin?
What is the half-life range of phenytoin?
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What should be done to prevent phenytoin absorption interference during tube feeding?
What should be done to prevent phenytoin absorption interference during tube feeding?
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Which intravenous solution should not be mixed with phenytoin?
Which intravenous solution should not be mixed with phenytoin?
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During intravenous administration of phenytoin, what vital signs must be monitored?
During intravenous administration of phenytoin, what vital signs must be monitored?
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How long should any unused drug be discarded after preparation for IV administration?
How long should any unused drug be discarded after preparation for IV administration?
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What is the effect of a decrease in serum protein or albumin levels on phenytoin?
What is the effect of a decrease in serum protein or albumin levels on phenytoin?
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Which type of tumor cells are generally more sensitive to chemotherapy?
Which type of tumor cells are generally more sensitive to chemotherapy?
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What is the primary mechanism of action of cetuximab?
What is the primary mechanism of action of cetuximab?
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Which adverse effect is commonly associated with cetuximab therapy?
Which adverse effect is commonly associated with cetuximab therapy?
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In what condition is cetuximab primarily used?
In what condition is cetuximab primarily used?
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What percentage of patients developed severe hypomagnesemia while on cetuximab in clinical trials?
What percentage of patients developed severe hypomagnesemia while on cetuximab in clinical trials?
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How is cetuximab administered to patients?
How is cetuximab administered to patients?
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What is the initial loading dose of cetuximab for treatment?
What is the initial loading dose of cetuximab for treatment?
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Cetuximab therapy may lead to which gastrointestinal toxicity?
Cetuximab therapy may lead to which gastrointestinal toxicity?
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Which type of cancer is not indicated for cetuximab therapy?
Which type of cancer is not indicated for cetuximab therapy?
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What is the primary mechanism of action of leuprolide therapy in breast cancer prevention?
What is the primary mechanism of action of leuprolide therapy in breast cancer prevention?
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Which of the following is an indication for toremifene therapy?
Which of the following is an indication for toremifene therapy?
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What is a common adverse effect associated with leuprolide treatment?
What is a common adverse effect associated with leuprolide treatment?
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What is a key pharmacokinetic characteristic of toremifene?
What is a key pharmacokinetic characteristic of toremifene?
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What potential risk is associated with reduced testosterone levels due to leuprolide therapy?
What potential risk is associated with reduced testosterone levels due to leuprolide therapy?
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How can bone loss associated with leuprolide therapy be mitigated?
How can bone loss associated with leuprolide therapy be mitigated?
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What is the recommended daily dosage for the short-acting leuprolide injection?
What is the recommended daily dosage for the short-acting leuprolide injection?
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What class of drug is fulvestrant, and what is its primary action?
What class of drug is fulvestrant, and what is its primary action?
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Which chemotherapeutic agent is specifically indicated for metastatic breast cancer and colon cancer?
Which chemotherapeutic agent is specifically indicated for metastatic breast cancer and colon cancer?
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What is the primary route of administration for Cytarabine?
What is the primary route of administration for Cytarabine?
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Which adverse effect is NOT commonly associated with Capecitabine?
Which adverse effect is NOT commonly associated with Capecitabine?
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What condition contraindicates the use of Capecitabine?
What condition contraindicates the use of Capecitabine?
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What type of tumors are mitotic inhibitors primarily used to treat?
What type of tumors are mitotic inhibitors primarily used to treat?
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What is a unique adverse effect associated with Cytarabine?
What is a unique adverse effect associated with Cytarabine?
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Which pyrimidine antagonist is available only in tablet form?
Which pyrimidine antagonist is available only in tablet form?
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What type of cancer is Cytarabine primarily used for?
What type of cancer is Cytarabine primarily used for?
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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.