Musculoskeletal Pharmacology
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Questions and Answers

Which route of administration is specified for alendronate in the provided text?

  • Subcutaneous (SC)
  • Intravenous (IV)
  • Intramuscular (IM)
  • Oral (PO) (correct)
  • A patient is prescribed alendronate for osteoporosis prevention. What is the recommended daily oral dosage according to the text?

  • 5 mg (correct)
  • 10 mg
  • 40 mg
  • 70 mg
  • Alendronate's primary therapeutic action is to:

  • Stimulate osteoblast activity to increase bone formation.
  • Increase calcium absorption in the intestines.
  • Promote vitamin D synthesis for bone health.
  • Inhibit osteoclast activity to reduce bone resorption. (correct)
  • Which of the following conditions is a contraindication for alendronate administration due to the risk of esophageal complications?

    <p>Esophageal strictures causing delayed emptying. (B)</p> Signup and view all the answers

    What is the approximate half-life of alendronate, reflecting its release from the skeleton?

    <p>10 years (B)</p> Signup and view all the answers

    Which of the following patient instructions is MOST critical to enhance the absorption of oral alendronate?

    <p>Ingest on an empty stomach with plain water. (B)</p> Signup and view all the answers

    For which of the following conditions is alendronate indicated according to the provided text?

    <p>Paget's disease of the bone (D)</p> Signup and view all the answers

    A patient reports experiencing persistent nausea and fatigue after starting alendronate. According to the patient teaching guidelines, what is the MOST appropriate action?

    <p>Notify the health care professional as it may require discontinuation of therapy. (A)</p> Signup and view all the answers

    Which of the following is NOT listed as a Y-site incompatibility with alendronate in the provided text?

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

    What is the recommended duration of alendronate therapy for Paget's disease of the bone?

    <p>6 months (B)</p> Signup and view all the answers

    A patient taking alendronate for osteoporosis should be advised to avoid which beverage concurrently to minimize interaction?

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

    What is the primary desired therapeutic outcome of alendronate in musculoskeletal conditions, as stated in the text?

    <p>Relief of muscle spasm (A)</p> Signup and view all the answers

    For patients receiving corticosteroids, alendronate is indicated for osteoporosis treatment when the prednisone dosage is at least:

    <p>7.5 mg/day (A)</p> Signup and view all the answers

    Which of the following instructions should be given to a patient who missed their daily dose of alendronate?

    <p>Take the missed dose if remembered within 1 hour of the scheduled time. (C)</p> Signup and view all the answers

    What is the rationale behind advising patients to remain upright for at least 30 minutes after taking oral alendronate?

    <p>To prevent esophageal irritation and facilitate gastric emptying. (D)</p> Signup and view all the answers

    What is the primary therapeutic classification of cyclobenzaprine?

    <p>Centrally acting skeletal muscle relaxant (B)</p> Signup and view all the answers

    Which condition is cyclobenzaprine indicated for?

    <p>Acute musculoskeletal pain with muscle spasm (B)</p> Signup and view all the answers

    What is the mechanism of action of cyclobenzaprine?

    <p>Reduces tonic somatic muscle activity in the brain stem (C)</p> Signup and view all the answers

    What is the approximate half-life of cyclobenzaprine?

    <p>1-3 days (B)</p> Signup and view all the answers

    Which adverse effect is a significant concern with cyclobenzaprine?

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

    Which drug interaction is specifically cautioned against with cyclobenzaprine?

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

    What is the peak effect time frame for oral cyclobenzaprine?

    <p>3–8 hours (A)</p> Signup and view all the answers

    Which population requires cautious use of cyclobenzaprine due to an increased risk of hepatotoxicity?

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

    What is the maximum daily dose of dantrolene for children over 5 years old?

    <p>400 mg (A)</p> Signup and view all the answers

    What initial dose of dantrolene is recommended for the treatment of malignant hyperthermia in adults?

    <p>1–2.5 mg/kg (D)</p> Signup and view all the answers

    Which form of dantrolene should NOT be used for reconstitution with other solutions?

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

    How should Ryanodex be administered for the prevention of malignant hyperthermia?

    <p>Rapid IV push over 1 minute (D)</p> Signup and view all the answers

    What is the recommended way to address gastric irritation caused by dantrolene?

    <p>Administer with food (D)</p> Signup and view all the answers

    Which lab test should be monitored frequently during dantrolene therapy?

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

    What is the maximum cumulative dose of dantrolene for the treatment of malignant hyperthermia?

    <p>10 mg/kg (D)</p> Signup and view all the answers

    What is the recommended dilution for reconstituting Dantrium for IV administration?

    <p>20 mg in 60 mL of sterile water (C)</p> Signup and view all the answers

    How long is the reconstituted Dantrium solution stable?

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

    What might warrant discontinuation of dantrolene therapy?

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

    What is the primary mechanism of action of celecoxib?

    <p>Selectively inhibits COX-2 enzyme, essential for prostaglandin synthesis. (C)</p> Signup and view all the answers

    Which condition is NOT a listed indication for celecoxib?

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

    What is the recommended duration of tamoxifen treatment for adjuvant therapy of breast cancer?

    <p>5-10 years (A)</p> Signup and view all the answers

    A patient with a history of deep vein thrombosis (DVT) and currently on warfarin therapy is being evaluated for tamoxifen. What is the most important consideration?

    <p>Tamoxifen is contraindicated due to the DVT and warfarin use. (C)</p> Signup and view all the answers

    Which adverse effect is common to both tamoxifen and celecoxib?

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

    Tamoxifen may increase the anticoagulant effect of which drug?

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

    Which lab value should be closely monitored in patients taking tamoxifen, especially those with bone metastases?

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

    What is the primary route of administration for tamoxifen in the treatment of breast cancer?

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

    Which CYP enzyme is primarily involved in the metabolism of celecoxib?

    <p>CYP2C9 (C)</p> Signup and view all the answers

    What advice should be given to a patient experiencing nausea after taking tamoxifen?

    <p>Take the medication with food or fluids. (B)</p> Signup and view all the answers

    Which serious adverse effect of tamoxifen should be reported to a healthcare professional immediately?

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

    A patient on tamoxifen reports experiencing bone pain. What is the appropriate nursing action?

    <p>Assess the pain and consult with the healthcare professional regarding analgesics. (C)</p> Signup and view all the answers

    What type of contraception should women of reproductive potential use while taking tamoxifen?

    <p>Non-hormonal contraceptives (D)</p> Signup and view all the answers

    Genetic polymorphism of which enzyme can significantly affect celecoxib concentrations?

    <p>CYP2C9 (B)</p> Signup and view all the answers

    What is a common side effect of tamoxifen related to the female reproductive system?

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

    What is the recommended dosage of alendronate for postmenopausal women not receiving estrogen?

    <p>10 mg once daily (A)</p> Signup and view all the answers

    How should effervescent alendronate tablets be taken?

    <p>Dissolved in 4 oz of plain room temperature water, stirred and drunk after effervescence stops (C)</p> Signup and view all the answers

    What is the primary route of excretion for tamoxifen?

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

    Which CYP isoenzyme plays a major role in the metabolism of tamoxifen into its active metabolites?

    <p>CYP2D6 (B)</p> Signup and view all the answers

    What is a key patient teaching point regarding alendronate administration?

    <p>Remain upright for at least 30 minutes after taking (B)</p> Signup and view all the answers

    Which condition is alendronate used to treat besides osteoporosis?

    <p>Paget's Disease (D)</p> Signup and view all the answers

    What is the recommended time to wait after taking alendronate before consuming other medications, beverages, or food?

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

    What type of water should be used to dissolve effervescent alendronate tablets?

    <p>Plain room temperature water (D)</p> Signup and view all the answers

    If a weekly dose of alendronate is missed, what should the patient do?

    <p>Take it the morning after remembered and resume the usual schedule the following week (C)</p> Signup and view all the answers

    What advice should be given to patients regarding calcium and vitamin D intake while on alendronate therapy?

    <p>Consult a healthcare professional about the need for supplementation (A)</p> Signup and view all the answers

    What are the two main metabolites of tamoxifen that contribute to its therapeutic effect?

    <p>Endoxifen and 4-hydroxytamoxifen (A)</p> Signup and view all the answers

    What is the potential impact of genetic polymorphism in the CYP2D6 enzyme system on tamoxifen therapy?

    <p>Decreased metabolism and reduced effectiveness (A)</p> Signup and view all the answers

    Besides breast cancer treatment and prevention, what other indication is tamoxifen used for?

    <p>None of the above; it is exclusively indicated for breast cancer-related conditions (D)</p> Signup and view all the answers

    What type of medication is tamoxifen classified as?

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

    How does tamoxifen exert its therapeutic effects in breast cancer?

    <p>By competing with estrogen for binding sites, reducing DNA synthesis and estrogen response (B)</p> Signup and view all the answers

    Flashcards

    Cyclobenzaprine

    A muscle relaxant used to relieve pain from muscle spasms.

    Indications of Cyclobenzaprine

    Used for acute painful musculoskeletal conditions and fibromyalgia.

    Half-life of Cyclobenzaprine

    Ranges from 1 to 3 days, influencing dosing schedule.

    Alendronate dosage for men

    5 mg once daily for men and premenopausal women.

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    Alendronate dosage for postmenopausal women

    10 mg once daily for postmenopausal women not on estrogen.

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    Osteoporosis assessment

    Evaluate patients for low bone mass before and during therapy.

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    Paget’s disease symptoms

    Symptoms include bone pain, headache, and increased skull size.

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    Serum calcium monitoring

    Assess serum calcium before starting alendronate therapy.

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    Administration timing for alendronate

    Take in the morning, 30 min before food or other medications.

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    Effervescent tablet preparation

    Dissolve tablet in half a glass of room temperature water.

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    Patient teaching on missed doses

    Skip missed dose; do not double dose next morning.

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    Post-medication precautions

    Remain upright for 30 min after taking alendronate.

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    Dietary recommendations with alendronate

    Encourage balanced diet and potential calcium, vitamin D supplements.

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    Tamoxifen indication

    Used for estrogen-receptor positive metastatic breast cancer.

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    Mechanism of action for Tamoxifen

    Competes with estrogen for binding sites, reducing tumor growth.

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    CYP2D6 genetic polymorphism

    Affects metabolism of tamoxifen; some may not process effectively.

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    Half-life of Tamoxifen

    Half-life is approximately 7 days.

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    Time/Action Profile of Tamoxifen

    Oral: Onset in 4-10 weeks; peak several months; duration several weeks.

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    Contraindications of Tamoxifen

    Not suitable for hypersensitivity, pregnancy, warfarin with DVT or PE.

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    Adverse Reactions of Tamoxifen

    Can cause DVT, edema, hot flashes, nausea, and confusion.

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    Monitoring during Tamoxifen Therapy

    Monitor CBC, platelets, calcium levels; verify negative pregnancy test.

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    Tamoxifen Patient Teaching

    Instruct patients on missed doses, pain reporting, and weight monitoring.

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    Typical Dosage of Tamoxifen

    20 mg PO daily for metastatic breast cancer and prevention in high-risk women.

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    Celecoxib Classification

    Therapeutic: antirheumatics; Pharmacologic: COX-2 inhibitors.

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    Indications of Celecoxib

    Used for osteoarthritis, rheumatoid arthritis, acute pain, and primary dysmenorrhea.

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    Celecoxib Action

    Inhibits COX-2 enzyme, decreasing prostaglandin synthesis.

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    Adverse Effects of Celecoxib

    Can lead to cardiovascular issues, gastrointestinal problems, and liver enzymes increase.

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    Celecoxib Drug Interactions

    May decrease effects of certain drugs or increase warfarin's anticoagulant effect.

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    Celecoxib Pharmacokinetics

    Extensively distributed, 97% protein binding, metabolized in the liver.

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    Use of Celecoxib in Acute Pain

    Effective for acute pain and can be used in migraine treatment.

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    Celecoxib Absorption

    Bioavailability is unknown; absorption varies significantly.

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    Pregnancy Precautions with Tamoxifen

    May cause fetal harm; nonhormonal contraception recommended for women of reproductive potential.

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    Y-Site Incompatibility

    A condition where certain drugs cannot be mixed in the same IV line.

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    Alemtuzumab

    A monoclonal antibody used for treating certain cancers and multiple sclerosis.

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    Dosing Advice

    Patient guidance to avoid exceeding the prescribed medication amount.

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    Photosensitivity Reactions

    Skin reactions caused by exposure to sunlight while on certain medications.

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    Alendronate

    A medication used to treat and prevent osteoporosis by inhibiting bone resorption.

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    Pharmacokinetics of Alendronate

    Describes how alendronate is absorbed, distributed, metabolized, and excreted.

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    Indications for Alendronate

    Used for treating osteoporosis, Paget’s disease, and corticosteroid-induced osteoporosis.

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    Contradictions/Precautions of Alendronate

    Conditions where alendronate should not be used, like esophageal abnormalities.

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    Route/Dosage for Osteoporosis

    Dosing of alendronate typically involves daily or weekly oral intake.

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    Treatment for Paget's Disease

    Alendronate is administered in higher doses for 6 months to treat Paget’s disease.

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    Side Effects to Monitor

    Potential adverse effects such as dizziness or muscle weakness that require patient observation.

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    Patient Education on CNS depressants

    Patients should avoid concurrent use of alcohol and CNS depressants to reduce risks.

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    Study Notes

    Cyclobenzaprine (Amrix, Fexmid, Flexeril)

    • Classification: Skeletal muscle relaxant (centrally acting)
    • Indications: Acute musculoskeletal pain with muscle spasm; unlabeled use for fibromyalgia
    • Mechanism: Reduces tonic somatic muscle activity in the brain stem; structurally similar to tricyclic antidepressants
    • Pharmacokinetics:
      • Absorption: Well absorbed from the GI tract
      • Distribution: Unknown
      • Protein Binding: 93%
      • Metabolism: Primarily by the liver
      • Half-life: 1-3 days
    • Time/Action Profile (Skeletal Muscle Relaxation):
      • Oral: Onset within 1 hour; Peak 3-8 hours; Duration 12-24 hours
      • Extended-release: Onset and peak unknown; Duration 24 hours
    • Contraindications/Precautions/Use Cautiously in: Hypersensitivity; MAO inhibitor use within 14 days; recent MI; severe/symptomatic cardiovascular disease; cardiac conduction disturbances; hyperthyroidism; cardiovascular disease; pregnancy (potential maternal/fetal risk); breastfeeding (potential maternal/infant risk); children under 35 years (increased risk of hepatotoxicity); older adults (lower dose needed due to increased risk of hepatotoxicity)
    • Adverse Reactions/Side Effects: Many, including cardiovascular (BP changes, heart failure, tachycardia), dermatological (flushing, itching, sweating, hives), eyes/ears/nose/throat (increased tearing, vision changes), gastrointestinal (diarrhea, loss of appetite, cramps, difficulty swallowing, GI bleeding, hepatotoxicity, nausea, vomiting), genitourinary (crystalluria, painful urination, erectile dysfunction, increased urination, incontinence, nighttime urination), hematological (anemia, aplastic anemia, elevated white blood cell count, low white blood cell count, low platelet count), musculoskeletal (muscle pain), neurological (drowsiness, muscle weakness, confusion, dizziness, headache, insomnia, malaise, nervousness), respiratory (shortness of breath, fluid around the lungs, respiratory slowing), and miscellaneous (anaphylaxis, chills, drooling, fever)
    • Interactions:
      • Drug-Drug: Calcium channel blockers may increase risk of cardiovascular collapse; avoid concomitant use with CNS depressants (alcohol, antihistamines, opioids, sedatives/hypnotics, parenteral magnesium sulfate); increased risk of hepatotoxicity with other hepatotoxic agents or estrogens; increased arrhythmia risk with verapamil; increased neuromuscular blocking effects with vecuronium
      • Drug-Natural Products: Increased CNS depression with kava-kava, valerian, chamomile, or hops
    • Dosage: Varies by indication and age
    • Nursing Implications/Lab Test Considerations:
      • Assess bowel function (diarrhea noted = possible discontinuation)
      • Assess muscle spasticity periodically
      • Assess anesthesia history & family history of malignant hyperthermia in surgical patients
      • IV administration: Monitor ECG, vital signs, electrolytes, and urine output continuously for malignant hyperthermia
      • Monitor for difficulty swallowing (oral)
      • Monitor liver function (AST, ALT, alkaline phosphatase, bilirubin, GGT) frequently
      • Monitor renal function and CBC (complete blood count) before and during prolonged therapy.
    • Patient/Family Teaching:
      • Do not exceed prescribed dose
      • Avoid driving/hazardous activities due to potential side effects
      • Use caution when walking stairs & eating post IV dose (surgical)
      • Avoid alcohol and other CNS depressants
      • Report any rash, excessive itching, yellowing of eyes or skin, dark urine, or unusual stools -Wear sunscreen and protective clothing -Notify health care providers if required (Rep, OB)
      • Follow-up exams and blood tests are essential -Malignant hyperthermia patients should carry identification.

    Alendronate (Binosto, Fosamax)

    • Classification: Bone resorption inhibitor (bisphosphonate)
    • Indications: Postmenopausal osteoporosis, osteoporosis in men, Paget's disease, corticosteroid-induced osteoporosis (≥ 7.5 mg prednisone/day)
    • Mechanism: Inhibits osteoclast activity, reversing osteoporosis & slowing Paget's progression.
    • Pharmacokinetics:
      • Absorption: Poor, ~0.6-0.8% orally
      • Distribution: To soft tissues, then bone
      • Metabolism & Excretion: Excreted in urine
      • Half-life: 10 years (reflects skeletal release)
    • Time/Action Profile (Bone Resorption Inhibition):
      • Oral: Onset 1 month; Peak 3-6 months; Duration 3 wk - 7 months post-discontinuation
    • Contraindications/Precautions: Esophageal abnormalities; Inability to remain upright for 30 minutes; Renal impairment
    • Interactions/Use cautiously: -Drug-Food: Food significantly decreases absorption; Caffeine, mineral water, & orange juice also decrease absorption. -NSAIDs (nonsteroidal anti-inflammatory drugs) increase risk of GI adverse effects.
    • Dosage: Varies by indication (osteoporosis, prevention, Paget's, corticosteroid-related)
    • Nursing Implications/Lab Test Considerations:
      • Assess bone mass before and after therapy (osteoporosis)
      • Assess symptoms of Paget's disease
      • Monitor serum calcium before & during therapy (correct hypocalcemia/vitamin D deficiency before starting)
      • Monitor alkaline phosphatase before and periodically (for Paget's disease)
    • Implementation:
      • Oral: First thing in the morning, with 6-8 oz plain water, 30 minutes before other medications/beverages/food. Swallow whole.
    • Effervescent tablets: Dissolve in water at room temperature (not mineral or flavored).
    • Patient/Family Teaching:
      • Take exactly as directed, by mouth, first thing in the morning with plain water
      • Remain upright for 30 minutes after taking
      • Report esophageal pain or difficulty swallowing promptly
      • Avoid crushing, chewing, or dissolving effervescent tablets in the mouth
      • balanced diet including supplemental calcium and vitamin D may be necessary. -Exercise and lifestyle modifications to reduce osteoporosis risk -Important to consult health care professional before starting, stopping, or changing dosage. -Inform health care professional about all other Rx/OTC meds, vitamins, or herbals. -Inform health care professional of alendronate therapy before dental procedures
    • Evaluation/Desired outcomes: -Prevention/reduction of osteoporosis progression -Treatment of osteoporosis in men -Decreased Paget's disease progression -Treatment of corticosteroid-induced osteoporosis

    Tamoxifen (Soltamox)

    • Classification: Antineoplastic (antiestrogen)
    • Indications: Estrogen receptor-positive metastatic breast cancer; adjuvant treatment of early-stage estrogen receptor-positive breast cancer; reducing contralateral breast cancer risk; preventing breast cancer in high-risk individuals; reducing invasive breast cancer risk after ductal carcinoma in situ.
    • Mechanism: Competes with estrogen for binding sites; reduces DNA synthesis.
    • Pharmacokinetics:
      • Absorption: Well absorbed
      • Metabolism: Primarily metabolized by liver enzymes (CYP3A and CYP2D6) into various active metabolites (endoxifen, 4-hydroxytamoxifen) with greater potency than tamoxifen. Genetic polymorphisms in CYP2D6 can affect effectiveness.
      • Excretion: Primarily feces.
      • Half-life: 7 days.
    • Time/Action Profile (Tumor Response):
      • Oral: Onset 4-10 weeks; Peak effect several months; Duration varies
    • Contraindications/Precautions/Use Cautiously in: Hypersensitivity; Concurrent warfarin therapy (in specific breast cancer cases); Pregnancy & breastfeeding; decreased bone marrow reserve; history of thromboembolic events; women of reproductive potential.
    • Adverse Reactions/Side Effects: Many, including cardiovascular (DVT, swelling), dermatological (hot flashes), eyes/ears/nose/throat (blurred vision), fluid and electrolyte (high calcium), gastrointestinal (nausea, vomiting), genitourinary (uterine malignancies, vaginal bleeding), hematological (low white blood cell count, low platelet), musculoskeletal (bone pain), neurological (confusion, depression, headache, stroke, weakness), respiratory (pulmonary embolism), and miscellaneous (tumor flare)
    • Interactions: -Drug-Drug: Estrogens may decrease tamoxifen effectiveness; bromocriptine may increase levels and risks; tamoxifen may increase warfarin's anticoagulant effects. Increased risk of thromboembolic events with other antineoplastics.
    • Dosage: Varies by indication
    • Nursing Implications/Lab Test Considerations:
      • Monitor for increased bone/tumor pain (analgesics may be necessary) -Verify negative pregnancy test before starting -Monitor CBC, platelets and calcium levels -Assess estrogen receptor status before starting -Monitor serum cholesterol and triglycerides (may be elevated) -Monitor liver function tests and thyroxine (T4) -Regular gynecologic exams
    • Patient/Family Teaching:
      • Take as directed; skip missed doses; read Medication Guide
      • Inform health care professional of skin changes -Report bone pain promptly; analgesics may be prescribed -Monitor weight & report concerning changes. -Report hot flashes -Report any pain, swelling, breathing difficulty, weakness, sleepiness, confusion, severe nausea, vomiting, weight changes, dizziness, headaches, vision loss. -Report menstrual changes, vaginal bleeding or pelvic pain. -Reproductive potential: contraception and breastfeeding considerations,
    • Evaluation/Desired Outcomes: Decrease in breast tumor size/spread; effects may be delayed. Reduced breast cancer incidence in high-risk patients

    Celecoxib (CeleBREX, Elyxyb)

    • Classification: Anti-rheumatic (COX-2 inhibitor)
    • Indications: Osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, juvenile rheumatoid arthritis, acute pain, primary dysmenorrhea, acute migraine (oral solution only)
    • Mechanism: Inhibits COX-2 enzyme, decreasing prostaglandin synthesis; analgesic, anti-inflammatory, and antipyretic
    • Pharmacokinetics:
      • Absorption: Bioavailability is unknown
      • Distribution: Widely distributed
      • Protein Binding: 97%
      • Metabolism: Primarily by the liver via CYP2C9 isoenzyme (polymorphic). Poor metabolizers may have increased drug levels and risks.
    • Dosage: Varies by indication/condition.

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    Description

    This quiz focuses on Cyclobenzaprine, a skeletal muscle relaxant used for acute musculoskeletal pain and fibromyalgia. It covers its pharmacokinetics, mechanism of action, and contraindications. Test your knowledge about this medication and its therapeutic use.

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