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

Which condition is phenytoin primarily used to treat?

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

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

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

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

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

What timeframe does analgesia from parenteral ketorolac typically begin?

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

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

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

How is ketorolac available for administration?

<p>Orally, intravenously, and intranasally (C)</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. (A)</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 (D)</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 (C)</p> Signup and view all the answers

What is the protein binding percentage of phenytoin?

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

What is the half-life range of phenytoin?

<p>7 to 42 hours (A)</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 (D)</p> Signup and view all the answers

Which intravenous solution should not be mixed with phenytoin?

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

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

<p>4 hours (D)</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. (A)</p> Signup and view all the answers

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

<p>Rapidly dividing cells (D)</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. (A)</p> Signup and view all the answers

Which adverse effect is commonly associated with cetuximab therapy?

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

In what condition is cetuximab primarily used?

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

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

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

How is cetuximab administered to patients?

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

What is the initial loading dose of cetuximab for treatment?

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

Cetuximab therapy may lead to which gastrointestinal toxicity?

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

Which type of cancer is not indicated for cetuximab therapy?

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

Which of the following is an indication for toremifene therapy?

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

What is a common adverse effect associated with leuprolide treatment?

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

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

<p>New-onset diabetes (D)</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 (A)</p> Signup and view all the answers

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

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

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

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

What is the primary route of administration for Cytarabine?

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

Which adverse effect is NOT commonly associated with Capecitabine?

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

What condition contraindicates the use of Capecitabine?

<p>Known hypersensitivity to fluorouracil (C)</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 (B)</p> Signup and view all the answers

What is a unique adverse effect associated with Cytarabine?

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

Which pyrimidine antagonist is available only in tablet form?

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

What type of cancer is Cytarabine primarily used for?

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

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Flashcards

Pyrimidine Antagonists

Drugs that interfere with the synthesis of pyrimidines, essential components of DNA and RNA.

Capecitabine

A pyrimidine antagonist used mainly to treat metastatic breast and colon cancers.

Cytarabine

A pyrimidine antagonist specifically used to treat various leukemias and lymphomas.

Cytarabine Syndrome

A syndrome specific to cytarabine treatment, characterized by adverse side effects.

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Mitotic Inhibitors

Drugs that prevent cells from dividing, disrupting the cell cycle.

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Etoposide

A drug commonly used in chemotherapy regimens to enhance the cytotoxic effects of other medications.

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Extravasation

A serious event occurring when a drug leaks out of the vein, damaging surrounding tissues.

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Specific Antidote

A substance administered to counter the harmful effects of a drug.

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Antiestrogen

A type of drug that blocks the effects of estrogen in the body.

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ER-positive breast cancer

A type of breast cancer that is fueled by estrogen.

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Leuprolide Therapy

A medication used to treat breast cancer by mimicking the effects of removing the testicles.

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Hot flashes

The most common side effect of leuprolide therapy.

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Toremifene (Fareston)

A medication that is an antiestrogen used to treat metastatic ER-positive breast cancer in postmenopausal women.

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Fulvestrant (Faslodex)

A medication that is an antiestrogen indicated for metastatic ER-positive breast cancer in postmenopausal women.

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Reduced testosterone

A common side effect of leuprolide therapy, often leading to sexual dysfunction.

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Osteoporosis

A serious side effect of leuprolide therapy, particularly in postmenopausal women.

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Hirsutism

A condition marked by excessive hair growth, especially in women, often in a male pattern on the face, chest, and abdomen.

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Epilepsy

A neurological disorder characterized by recurrent seizures.

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Phenytoin

A medication used to treat seizures by stabilizing nerve membranes and decreasing excitability.

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Tonic-clonic Seizures (Grand Mal)

A type of seizure involving the entire brain, causing tonic (muscle stiffness) and clonic (jerking) movements.

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Psychomotor Seizures (Temporal Lobe)

A type of seizure originating in the temporal lobe, often characterized by confusion, hallucinations, and repetitive motor activity.

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Osteomalacia

A condition characterized by softening of the bones due to vitamin D deficiency or problems with calcium absorption.

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Rickets

A condition characterized by bone softening in children due to vitamin D deficiency.

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Dysrhythmia

A condition characterized by irregular heartbeat or rhythm.

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What are NSAIDs?

A group of medications that reduce pain by blocking the production of prostaglandins which are chemicals involved in inflammation and pain.

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What is Ketorolac?

A type of NSAID known for its potent pain-relieving properties, commonly used for short-term management of pain.

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How is Ketorolac administered?

It can be given orally, through injection (IV or IM), or as a nasal spray.

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How quickly does Ketorolac work?

When given through injection (IV or IM), pain relief starts within 30 minutes, peaks in 1-2 hours, and lasts for 4-6 hours.

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How is Ketorolac processed by the body?

It's broken down by the liver and excreted in urine.

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What are some common side effects of Ketorolac?

Ketorolac can cause stomach irritation, especially if taken without food.

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How can Ketorolac affect fluid balance?

It can increase fluid retention in the body.

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Why is it important to administer Ketorolac slowly?

Rapid IV injection of Ketorolac can increase the risk of adverse effects.

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Half-life of a drug

The amount of time it takes for the concentration of a drug in the body to decrease by half.

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Therapeutic range of a drug

The range of drug concentrations in the blood that is effective without causing too many side effects.

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Protein binding of phenytoin

Phenytoin is highly bound to proteins in the blood, such as albumin. Changes in protein levels can affect the amount of free phenytoin available in the bloodstream, potentially causing side effects.

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Purple glove syndrome

Phenytoin can cause discoloration of the veins if injected into the back of the hand, leading to a condition called 'purple glove syndrome'.

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Cell growth fraction and chemotherapy sensitivity

Rapidly dividing cells are more sensitive to chemotherapy than slowly dividing cells.

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Tumor susceptibility

The ability of a tumor to respond to chemotherapy treatment.

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Non-dividing cells and chemotherapy

Chemotherapy agents mainly target cells that are actively dividing. Non-dividing cells are generally less impacted by chemotherapy.

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Growth fraction and chemotherapy effectiveness

The effectiveness of chemotherapy is influenced by the proportion of tumor cells that are actively dividing, which can vary based on the type of cancer and its stage.

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What is Cetuximab?

Cetuximab is a monoclonal antibody that targets and blocks epidermal growth factor receptors (EGFRs).

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What are EGFRs?

EGFRs, or epidermal growth factor receptors, play a role in regulating cell growth and are often found in excess in various cancers.

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How does Cetuximab work?

Cetuximab works by attaching to EGFRs, preventing the signaling that promotes uncontrolled cell growth in cancer cells.

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What type of cancer is Cetuximab primarily used for?

Cetuximab is approved for use in metastatic colorectal cancer that is positive for EGFR, meaning the cancer cells have high levels of EGFR.

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How is Cetuximab administered?

Treatment with Cetuximab can involve a loading dose followed by maintenance doses, given either weekly or bi-weekly.

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What are some side effects of Cetuximab?

Combining Cetuximab with the drug irinotecan frequently leads to gastrointestinal (GI) side effects, including diarrhea, nausea, pain, vomiting, and constipation.

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What is a notable side effect of Cetuximab?

Low magnesium levels (hypomagnesemia) are a common side effect of Cetuximab treatment, occurring in a significant portion of patients.

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How can Cetuximab be used in conjunction with other treatments?

Cetuximab can be used in combination with other cancer treatments, such as an irinotecan-based regimen, or alone in cases where patients cannot tolerate irinotecan.

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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.

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