Name of the Mitotic inhibitors Drugs
- Vinblastine
- Vincristine
- Vinorelbine
- Docetaxel
- Paclitaxel
1.Vinblastine
| VINBLASTINE |
| Availability: Injection Solution: 1 mg/mL |
| Administration/handling: May be carcinogenic, mutagenic, teratogenic. Handle with extreme care during preparation and administration. Give by IV injection. Leakage from IV site into surrounding tissue may produce extreme irritation. Avoid eye contact with solution (severe eye irritation, possible corneal ulceration may result). If eye contact occurs, immediately irrigate eye with water |
| IV: Note: In order to prevent inadvertent intrathecal administration, dispense as a piggyback (not a syringe). Reconstitution: Using 1 mg/mL solution, further dilute in 25–50 mL D5W or 0.9% NaCl. Rate of administration • Infuse over 5–15 min. Prolonged administration time and/or increased volume may increase risk of vein irritation and extravasation. Storage: Refrigerate unopened vials. • Solution appears clear, colorless. • Following dilution, solution is stable for up to 21 days if protected from light (consult manufacturer prescribing information). • Discard if solution is discolored or precipitate forms. |
| Dosage individualized based on clinical response, tolerance to adverse effects. When used in combination therapy, consult specific protocols for optimum dosage, sequence of drug administration. |
| Usual Dosage: IV: Adults, elderly: Initially, 3.7 mg/m2 (adjust dose q7days based on WBC response) up to 5.5 mg/m2 (second wk), 7.4 mg/m2 (third wk), 9.25 mg/m2 (fourth wk), and 11.1 mg/m2 (fifth wk). Maximum: 18.5 mg/m2. CHILDREN: 3–6 mg/m2 q7–14days. Maximum: 12.5 mg/m2/wk. |
| Hodgkin’s disease; advanced testicular cancer; lymphoma; AIDS-related Kaposi’s sarcoma; bladder cancer; renal cancer; non-small-cell lung cancer; melanoma; breast cancer; choriocarcinoma; histiocytosis X; mycosis fungoides Adults: 3.7 mg/m2 I.V. weekly; may increase to a maximum of 18.5 mg/m2 I.V. weekly, based on response. Withhold weekly dose if white blood cell (WBC) count is less than 4,000 cells/ mm3.May increase dosage in increments of 1.8mg/m2 if needed, but not after WBC count drops to approximately 3,000 cells/mm3. |
| Dosage in Hepatic Impairment: Direct serum bilirubin concentration 1.5–3 mg/dL: Reduce dose by 50%. Greater than 3 mg/dL: Avoid use. |
Mechanism of Action:
Binds to tubulin, inhibiting microtubule formation; may interfere with nucleic acid, protein synthesis.
Therapeutic Effect: Inhibits cell division by disrupting mitotic spindle.
Indications:
- Treatment of hodgkin’s lymphoma
- Non- Hodgkin’s lymphoma
- Langerhans cell histiocytosis
- Advanced testicular carcinoma
- Kaposi’s sarcoma
- Letterer-siwe disease
- Breast carcinoma
- Resistant choriocarcinoma.
OFF-LABEL:
Treatment of bladder ovarian cancer
- Non–small-cell lung cancer
- Soft tissue sarcoma
- Melanoma.
Cautions & Contraindications:
- Hypersensitivity to vinblastine.
- Bacterial infection
- Significant granulocytopenia (unless as a result of condition being treated).
Cautions:
Hepatic impairment, severe leukopenia, neurotoxicity, recent exposure to radiation therapy, chemotherapy, ischemic heart disease, preexisting pulmonary disease.
Metabolism and Half- Life:
- Does not cross blood-brain barrier.
- Protein binding: 99%. Metabolized in liver.
- Primarily excreted in feces.
- Half-life: 24.8 hrs
Drug interactions:
- May decrease concentration/anticonvulsant effects of phenytoin.
- Strong CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole) may increase level/toxicity.
- Strong CYP3A4 inducers (e.g., carbamazepine, phenytoin, rifampin) may decrease concentration/effect.
- Bone marrow depressant cladribine) may increase myelosuppression.
- Live virus vaccines may potentiate virus replication, increase vaccine side effects, decrease pt’s antibody response to vaccine.
- May increase serum uric acid.
Side – Effects:
Frequent:
- Nausea, vomiting, alopecia.
Occasional:
- Constipation, diarrhea, rectal bleeding, headache, paresthesia (occur 4–6 hrs after administration, persist for 2–10 hrs), malaise, asthenia, dizziness, pain at tumor site, jaw/face pain, depression, dry mouth.
Rare:
- Dermatitis, stomatitis, phototoxicity, hyperuricemia.
Nursing Considerations
Baseline assessment
- Nausea, vomiting easily controlled by antiemetics.
- Discontinue therapy if WBC, platelet counts fall abruptly (unless drug is clearly destroying tumor cells in bone marrow).
- Obtain CBC weekly or before each dosing.
- Offer emotional support.
Intervention/evaluation
- If neutrophils fall below 2,000 cells/ mm3, assess diligently for signs of infection.
- Assess for stomatitis; maintain strict oral hygiene.
- Monitor for hematologic toxicity: infection (fever, sore throat, signs of local infection), unusual bruising/bleeding from any site, symptoms of anemia (excessive fatigue, weakness).
- Monitor daily pattern of bowel activity, stool consistency. Avoid constipation.
- Extravasation may result in cellulitis, phlebitis.
- Large amount of extravasation may result in tissue sloughing. If extravasation occurs, give local injection of hyaluronidase, apply warm compresses.
Patient/family teaching
- Immediately report any pain/burning at injection site during administration.
- Pain at tumor site may occur during or shortly after injection.
- Do not have immunizations without physician approval (drug lowers resistance).
- Avoid crowds, those with infection.
- Promptly report fever, sore throat, signs of local infection, unusual bruising/bleeding from any site.
- Hair loss is reversible, but new hair growth may have different color, texture.
- Report persistent nausea/vomiting.
- Avoid constipation by increasing fluids, bulk in diet, exercise as tolerated.
2.Vincristine
| VINCRISTINE |
| Availability: Injection Solution: 1 mg/mL. Injection; Suspension: (Marqibo): 5 mg/31 mL. |
| Administration/handling: Note: In order to prevent inadvertent intrathecal administration, dispense as a piggyback. (not a syringe). IV: May be carcinogenic, mutagenic, teratogenic. Handle with extreme care during preparation and administration. Use extreme caution in calculating administering vincristine. Overdose may result in serious or fatal outcome. Injection Solution: Reconstitution • Dilute in 25–50 mL D5W or 0.9% NaCl. Rate of administration: Administer as 5–10 min infusion (preferred). • Do not inject into extremity with impaired, potentially impaired circulation caused by compression or invading neoplasm, phlebitis, varicosity. Storage: Refrigerate unopened vials. • Solution appears clear, colorless. • Discard if solution is discolored or precipitate forms. • Diluted solutions are stable for 7 days refrigerated or 2 days at room temperature. |
| Injection Suspension: Calculate dose of vincristine and remove volume equal to volume of intended solution from 100 mL 0.9% NaCl or D5W infusion bag. Inject vincristine into infusion bag (total volume: 100 mL). Rate of administration • Administer over 60 min. Storage : Solution must be administered within 12 hrs of preparation |
| Usual Dosage Injection Solution: IV: Adults, elderly: 1.4 mg/m2, frequency may vary based on protocol. CHildren Weighing more than 10 kg: 1.5–2 mg/m2, frequency may vary based on protocol. Children weighing less than 10 kg: 0.05 mg/kg once wkly. Maximum: 2 mg. |
| ALL Injection Suspension: IV: Adults, elderly: 2.25 mg/m2 q7days. Infuse over 1 hr |
| Acute leukemia: Adults: 0.4 to 1.4 mg/m2 I.V. weekly, not to exceed 2 mg/dose. (Dosages higher than 2 mg may be used depending on patient, physician, protocol, and facility.) Children weighing more than 10 kg (22 lb): 2 mg/m2 I.V. weekly Children weighing 10 kg (22 lb) or less: 0.05 mg/kg I.V. weekly |
Mechanism of Action:
Binds to tubulin, inhibiting microtubule formation; may interfere with nucleic acid/protein synthesis.
Therapeutic Effect: Inhibits cell division by disrupting mitotic spindle.
Indications:
- Treatment of acute lymphocytic leukemia (ALL)
- Hodgkin’s lymphoma
- advanced non-Hodgkin’s lymphomas
- Neuroblastoma
- Rhabdomyosarcoma
- Wilms tumor.
- Relapsed Philadelphia chromosome negative (Ph−) ALL in adults whose disease has progressed after 2 or more anti-leukemic therapies.
OFFLABEL:
Treatment of multiple myeloma, chronic lymphocytic leukemia (CLL), brain tumors, small cell lung cancer, ovarian germ cell tumors, Ewing’s sarcoma, gestational trophoblastic tumors, retinoblastoma
Cautions & Contraindications:
- Hypersensitivity to vincristine.
- Demyelinating form of Charcot-Marie-Tooth syndrome.
- Intrathecal administration.
Cautions:
Hepatic impairment, pts receiving radiation therapy through ports (including liver), neurotoxicity, preexisting neuromuscular disease, hepatobiliary dysfunction, elderly.
Metabolism and half- life :
- Does not cross blood-brain barrier.
- Protein binding: 75%. Metabolized in liver.
- Primarily excreted in feces by biliary system.
- Half-life: 24 hrs. Marqibo: 45 hrs
Drug Interactions:
- May decrease concentration/anticonvulsant effects of phenytoin.
- Itraconazole may increase severity of neuromuscular side effects.
- Strong CYP3A4 inducers (e.g., carbamazepine, phenytoin, rifAMPin) may decrease concentration/effect.
- Strong CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole) may increase concentration/effect.
- Live virus vaccines may potentiate virus replication, increase vaccine side effects, decrease pt’s antibody response to vaccine.
- May increase serum uric acid.
Side- Effects:
Expected:
- Peripheral neuropathy (occurs in nearly every pt; first clinical sign is depression of Achilles tendon reflex).
Frequent:
- Peripheral paresthesia, alopecia, constipation/obstipation (upper colon impaction with empty rectum), abdominal cramps, headache, jaw pain, hoarseness, diplopia, ptosis/drooping of eyelid, urinary tract disturbances.
Occasional:
- Nausea, vomiting, diarrhea, abdominal distention, stomatitis, fever.
Rare:
- Mild leukopenia, mild anemia, thrombocytopenia.
Nursing Considerations
Baseline assessment
- Obtain baseline CBC, LFT.
- Offer emotional support.
- Question history of hepatic impairment, neuromuscular disease.
Intervention/evaluation
- Monitor serum uric acid levels, renal/hepatic function studies, CBC.
- Assess Achilles tendon reflex.
- Monitor daily pattern of bowel activity, stool consistency.
- Monitor for ptosis, diplopia, blurred vision.
- Question pt regarding urinary changes.
- Extravasation produces stinging, burning, edema at injection site. Terminate injection immediately, locally inject hyaluronidase, apply heat (disperses drug, minimizes discomfort, cellulitis).
Patient/family teaching
- Immediately report any pain/burning at injection site during administration.
- Hair loss is reversible, but new hair growth may have different color/texture.
- Report persistent nausea/vomiting.
- Report signs of peripheral neuropathy (burning/numbness of bottom of feet, palms of hands).
- Report fever, sore throat, unusual bleeding/bruising, shortness of breath
- Explain drug therapy to patient. Emphasize importance of follow-up laboratory tests.
- Advise patient to promptly report signs and symptoms of infection and to take his temperature daily.
- Urge patient to practice good oral hygiene, to help prevent infected mouth sores.
- Instruct female of childbearing age to avoid pregnancy. Caution her not to breastfeed during therapy.
3.Vinorelbine
| VINORELBINE |
| Availability: Injection Solution: 10 mg/mL (1-mL, 5-mL vials) |
| ADMINISTRATION/HANDLING: IV: IV needle, catheter must be correctly positioned before administration. Leakage into surrounding tissue produces extreme irritation, local tissue necrosis, thrombophlebitis. Handle drug with extreme care during administration; wear protective clothing per protocol. If solution comes in contact with skin/mucosa, immediately wash thoroughly with soap, water. |
| Reconstitution • Must be diluted and administered via syringe or IV bag. Syringe Dilution: Dilute calculated vinorelbine dose with D5W or 0.9% NaCl to concentration of 1.5–3 mg/mL. I V Bag Dilution : Dilute calculated vinorelbine dose with D5W, 0.45% or 0.9% NaCl, 5% dextrose and 0.45% NaCl, Ringer’s or lactated Ringer’s to concentration of 0. |
| Rate of administration • Administer diluted vinorelbine over 6–10 min into side port of free-flowing IV closest to IV bag followed by flushing with 75–125 mL of one of the solutions. • If extravasation occurs, stop injection immediately; give remaining portion of dose into another vein |
| Storage: Refrigerate unopened vials. • Protect from light. • Unopened vials are stable at room temperature for 72 hrs. • Do not administer if particulate has formed. • Diluted vinorelbine may be used for up to 24 hrs under normal room light when stored in polypropylene syringes or polyvinyl chloride bags at room temperature. |
| Dosage adjustments should be based on granulocyte count obtained on the day of treatment, as follows: Granulocyte Count (cells/mm3) on Day of Treatment Dosage 1)1,500 or higher 100% of starting dose 2)1,000–1,499 50% of starting dose 3) Less than 1,000 Do not administer |
| NSCLC Monotherapy IV injection: ADULTS, ELDERLY: 30 mg/m2 q7 days. |
| NSCLC Combination Therapy with Cisplatin IV injection: Adults, elderly: 25–30 mg/m2 q7 days. |
| Inoperable non-small-cell lung cancer : Adults: As monotherapy, 30 mg/m2 I.V. weekly given over 6 to 10 minutes. In combination therapy, 25mg/m2 weekly given with cisplatin q 4 weeks. Alternatively, in combination therapy, 30 mg/m2 I.V. given with cisplatin on days 1 and 29, then q 6 weeks |
Mechanism Of Action:
Binds to tubulin, inhibiting microtubule formation; may interfere with nucleic acid protein synthesis.
Therapeutic Effect: Prevents cellular division by disrupting formation of mitotic spindle.
Indications:
Single agent or in combination with Cisplatin for treatment of unresectable, advanced or metastatic, non–small-cell
lung cancer (NSCLC).
OFF-LABEL:
Treatment of metastatic breast cancer, cervical carcinoma, ovarian carcinoma, malignant pleural mesothelioma, soft tissue sarcoma, small-cell lung cancer.
Cautions & Contraindications:
- Hypersensitivity to vinorelbine.
Cautions:
- Compromised marrow reserve due to prior chemotherapy/radiation therapy
- Hepatic impairment
- Neurotoxicity, neuropathy
- Pulmonary impairment.
Metabolism and Half- Life:
- Widely distributed after IV administration.
- Protein binding: 80%–90%. Metabolized in liver.
- Primarily excreted in feces by biliary system.
- Half-life: 28–43 hrs.
Drug Interactions:
- Cisplatin may increase risk of granulocytopenia.
- Live virus vaccines may potentiate virus replication, increase vaccine side effects, decrease pt’s antibody response to vaccine.
- Strong CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole) may increase concentration/effects.
- May increase serum bilirubin, alkaline phosphatase, ALT, AST.
Side- Effects:
Frequent:
- Asthenia, nausea, constipation, erythema, pain, vein discoloration at injection site, fatigue,
- peripheral neuropathy manifested as paresthesia, hyperesthesia, diarrhea, alopecia.
Occasional:
- Phlebitis, dyspnea, loss of deep tendon reflexes.
Rare:
- Chest pain, jaw pain, myalgia, arthralgia, rash.
Nursing Considerations
Baseline assessment
- Review medication history.
- Obtain CBC prior to each dose. Granulocyte count should be at least 1,000 cells/mm3 before vinorelbine administration. Granulocyte nadirs occur 7–10 days following dosing.
- Do not give hematologic growth factors within 24 hrs before administration of chemotherapy or earlier than 24 hrs following cytotoxic chemotherapy.
- Advise women of childbearing potential to avoid pregnancy during drug therapy.
- Offer emotional support.
Intervention/evaluation
- Diligently monitor injection site for swelling, redness, pain.
- Frequently monitor for myelosuppression during and following therapy (infection [fever, sore throat, signs of local infection], unusual bleeding/bruising, anemia [excessive fatigue, weakness]).
- Monitor pts developing severe granulocytopenia for evidence of infection, fever. Crackers, dry toast, sips of cola may help relieve nausea.
- Monitor daily pattern of bowel activity, stool consistency.
- Question for tingling, burning, numbness of hands/feet (peripheral neuropathy). Pt complaint of “walking on glass” is sign of hyperesthesia
Patient/family teaching
- Immediately report redness, swelling, pain at injection site.
- Avoid crowds, those with infection.
- Do not have immunizations without physician’s approval.
- Promptly report fever, signs of infection, unusual bruising/bleeding from any site, difficulty breathing.
- Avoid pregnancy.
- Hair loss is reversible, but new hair growth may have different color, texture.
- Urge patient to practice good oral hygiene, to help prevent infected mouth sores.
4.Docetaxel
| DOCETAXEL |
| Availability : Injection, Powder for Reconstitution: 20 mg, 80 mg. Injection Solution: 10 mg/mL, 20 mg/mL |
| Administration/handling: IV: Reconstitution (solution) • Withdraw dose and add to 250–500 mL 0.9% NaCl or D5W in glass or polyolefin container to provide a final concentration of 0.3–0.74 mg/mL. (Powder) • Add 1 mL diluent provided to 20-mg vial to provide a concentration of 20 mg/0.8 mL (4 mL to 80-mg vial to provide a concentration of 24 mg/mL). Shake well. Further dilute in 250 mL NaCl or D5W to a final concentration of 0.3–0.74 mg/mL. Rate of administration: Administer as a 1-hr infusion. • Monitor closely for hypersensitivity reaction (flushing, localized skin reaction, bronchospasm [may occur within a few min after beginning infusion]). |
| Storage • Store vials between 36°F–77°F. • Protect from bright light. • If refrigerated, stand vial at room temperature for 5 min before administering (do not store in PVC bags). • Diluted solution should be used within 4 hrs (including infusion time). |
| Pt should be premedicated with oral corticosteroids (e.g., dexamethasone 16 mg/day for 5 days beginning day 1 before Docetaxel therapy); reduces severity of fluid retention, hypersensitivity reaction |
| Breast Carcinoma: IV: Adults: Locally advanced or metastatic: 60–100 mg/m2 given over 1 hr q3wks as a single agent. Operable, node positive: 75 mg/m2 q3wks for 6 courses (in combination with Doxorubicin and cyclophosphamide). |
| Non–Small-Cell Lung Carcinoma: IV: Adults: 75 mg/m2 q3wks (as monotherapy or in combination with Cisplatin) |
| Prostate Cancer: IV: Adults, elderly: 75 mg/m2 q3wks with concurrent administration of prednisone. |
| Head/Neck Cancer: IV: Adults, elderly: 75 mg/m2 q3wks (in combination with Cisplatin and fluorouracil) for 3–4 cycles, followed by radiation therapy |
| Gastric Adenocarcinoma: IV: Adults, elderly: 75 mg/m2 q3wks (in combination with Cisplatin and fluorouracil). |
| Dose Modification for Gastric or Head/Neck Cancer: •ALT, AST 2.5 to 5 times ULN and alkaline phosphatase less than or equal to 2.5 times ULN : 80% of dose •ALT, AST 1.5 to 5 times ULN and alkaline phosphatase 2.5 to 5 times ULN : 80% of dose •ALT, AST greater than 5 times ULN and/or alkaline phosphatase greater than 5 times ULN : Discontinue Docetaxel |
| Toxicity includes febrile neutropenia, neutrophils less than 500 cells/mm3 for longer than 1 wk, severe cutaneous reactions. Also, for NSCLC, platelet nadir less than 25,000 cells/mm3, any CTCAE Grade 3 or 4 nonhematologic toxicity |
| Breast Cancer: Reduce dose to 75 mg/m2; if toxicity persists, reduce to 55 mg/m2 |
| Breast Cancer Adjuvant: Administer when neutrophils are less than 1,500 cells/mm3. If toxicity persists, or Grade 3 or 4 stomatitis, reduce dose to 60 mg/m2. |
| Non–Small-Cell Lung Cancer: Monotherapy Hold dose until toxicity resolves, then reduce dose to 55 mg/m2. Discontinue if Grade 3 or 4 neuropathy occurs. Combination Therapy: Reduce dose to 65 mg/m2; may further reduce to 50 mg/m2 if needed. |
| Prostate Cancer: Reduce dose to 60 mg/m2; discontinue if toxicity persists. |
| Gastric or Head and Neck Cancer: Reduce dose to 60 mg/m2; if neutropenic toxicity persists, further reduce to 45 mg/m2. For Grade 3 or 4 thrombocytopenia, reduce dose from 75 mg/m2 to 60 mg/m2; discontinue if toxicity persists. |
| Dosage in Hepatic Impairment: Total bilirubin more than ULN, or ALT, AST more than 1.5 times ULN with alkaline phosphatase more than 2.5 times ULN: Use not recommended |
Mechanism of Acton:
Promotes assembly of microtubules and inhibits depolymerization of tubulin, which stabilizes microtubules. Therapeutic Effect: Inhibits DNA, RNA, protein synthesis.
Indications:
- Treatment of locally advanced or metastatic breast carcinoma after failure of prior chemotherapy.
- Treatment of metastatic non–small-cell lung cancer (NSCLC).
- Treatment of metastatic prostate cancer, head and neck cancer (with prednisone).
- Treatment of advanced gastric adenocarcinoma.
OFF-LABEL:
- Bladder, esophageal, ovarian, small-cell lung carcinoma
- Soft tissue carcinoma,
- Cervical cancer
- Wing’s sarcoma
- Osteosarcoma.
Cautions & Contraindications:
- Hypersensitivity to docetaxel.
- History of severe hypersensitivity to drugs formulated with polysorbate 80
- Neutrophil count less than 1,500 cells/mm3.
Cautions:
- Hepatic impairment
- Myelosuppression
- Concomitant CYP3A4 inhibitors/inducers
- Fluid retention
- Pulmonary disease
- HF
- Active infection
Metabolism and Half- Life:
- Widely distributed.
- Protein binding: 94%.
- Extensively metabolized in liver.
- Excreted in feces (75%), urine (6%).
- Half-life: 11.1 hr
Drug interactions:
- Strong CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole, ritonavir) may increase concentration/effect.
- Strong CYP3A4 inducers (e.g., carbamazepine, phenytoin, rifampin) may decrease concentration/effect.
- Live virus vaccines may potentiate replication, increase vaccine side effects, decrease pt’s antibody response to vaccine.
- May increase serum alkaline phosphatase, bilirubin, ALT, AST. Reduces neutrophil, platelet count, Hgb, Hct.
Side- Effects:
Frequent:
- Alopecia, asthenia, hypersensitivity reaction (e.g., dermatitis), which is decreased in pts pretreated with oral corticosteroids; fluid retention, stomatitis, nausea, diarrhea, fever, nail changes, vomiting, myalgia.
Occasional:
- Hypotension, edema, anorexia, headache, weight gain, infection (urinary tract, injection site, indwelling catheter tip), dizziness.
Rare:
- Dry skin, sensory disorders (vision, speech, taste), arthralgia, weight loss, conjunctivitis, hematuria, proteinuria.
Nursing Considerations
Baseline assessment
- •Obtain baseline ANC, CBC, serum chemistries.
- •Offer emotional support to pt, family.
- •Antiemetics may be effective in preventing, treating nausea/vomiting.
- •Pt should be pretreated with corticosteroids to reduce fluid retention, hypersensitivity reaction.
Intervention/evaluation
- Frequently monitor blood counts, particularly ANC count (less than 1,500 cells/mm3 requires discontinuation of therapy).
- Monitor LFT, serum uric acid levels.
- Observe for cutaneous reactions (rash with eruptions, mainly on hands, feet).
- Assess for extravascular fluid accumulation: rales in lungs, dependent edema, dyspnea at rest, pronounced abdominal distention (due to ascites)
Patient/family teaching
- Hair loss is reversible, but new hair growth may have different color or texture.
- New hair growth resumes 2–3 mos after last therapy dose.
- Maintain strict oral hygiene.
- Do not have immunizations without physician’s approval (drug lowers resistance).
- Avoid those who have recently taken any live virus vaccine.
- Report persistent nausea, diarrhea, respiratory difficulty, chest pain, fever, chills, unusual bleeding, bruising
5.Paclitaxel
| PACLITAXEL |
| Availability : Injection, Powder for Reconstitution (Abraxane): 100-mg vial. Injection Solution: 6 mg/mL (5-mL, 16.7-mL, 25-mL, 50-mL vials). |
| Administration/handling: IV: Wear gloves during handling; if contact with skin occurs, wash hands thoroughly with soap, water. If contact with mucous membranes occurs, flush with water. |
| PACLitaxel: Reconstitution • Dilute with 250–1,000 mL 0.9% NaCl, D5W to final concentration of 0.3–1.2 mg/mL. Rate of administration • Administer at rate per protocol (range: 1–96 hrs) through in-line filter not greater than 0.22 microns. • Monitor vital signs during infusion, esp. during first hour. • Discontinue administration if severe hypersensitivity reaction occurs. Storage • Store unopened vials at room temperature. • Reconstituted solution is stable at room temperature for 72 hrs. • Store diluted solutions in bottles or plastic bags. Administer through polyethylene-lined administration sets (avoid plasticized PVC equipment or devices). |
| Abraxane (Paclitaxel—Protein Bound): Reconstitution • Reconstitute each vial with 20 mL 0.9% NaCl to provide concentration of 5 mg/mL. • Slowly inject onto inside wall of vial; gently swirl over 2 min to avoid foaming. • Inject appropriate amount into empty PVC-type bag. Rate of administration • Infuse over 30 min. Do not use in-line filter. Storage: Store unopened vials at room temperature. • Once reconstituted, use immediately but may refrigerate for up to 8 hrs |
| Follow facility protocol for handling chemotherapeutic drugs and preparing solutions. Dilute in dextrose 5% in water, normal saline solution, or dextrose 5% in lactated Ringer’s solution per manufacturer’s Guidelines. Inspect solution for particles. Administer through polyethylene-lined administration set attached to 0.22- micron in-line filter. To prevent severe hypersensitivity reaction, premedicate with dexamethasone20 mg 12 and 6 hours before infusion, as prescribed. Also give diphenhydramine 50 mg I.V., plus either cimetidine 300 mg or ranitidine 50 mg I.V. 30 to 60 minutes before paclitaxel. |
| Keep epinephrine available. If severe hypersensitivity reaction occurs, stop infusion immediately and give epinephrine, I.V. fluids, and additional antihistamine and corticosteroid doses, as indicated and prescribed. |
| Advanced ovarian cancer : Adults: As first-line therapy, 175 mg/m2 I.V. over 3 hours q 3 weeks, or 135mg/m2 I.V. over 24 hours q 3 weeks, followed by cisplatin. After failure of first-line therapy, 135 mg/m2 I.V. or 175 mg/m2 I.V. over 3 hours q 3 weeks |
| Breast cancer after failure of combination chemotherapy: Adults: As adjuvant treatment for node-positive breast cancer, 175 mg/m2 I.V. over 3 hours q 3 weeks for four courses given sequentially with doxorubicin combination chemotherapy. After chemotherapy failure for metastatic disease or relapse within 6 months of adjuvant therapy, 175 mg/m2 I.V. over 3 hours q 3 weeks |
| Non-small-cell lung cancer: Adults: 135 mg/m2 I.V. over 24 hours q3 weeks, followed by cisplatin |
| AIDS-related Kaposi’s sarcoma: Adults: 135 mg/m2 I.V. over 3 hours q3 weeks, or 100 mg/m2 I.V. over 3 hours q 2 weeks |
Mechanism of Action:
Increases action of tubulin dimers; stabilizes existing microtubules; inhibits their disassembly; interferes with late G2 mitotic phase.
Therapeutic Effect: Inhibits cellular mitosis, replication.
Indications:
- Conventional: Treatment of node-positive breast cancer
- Metastatic breast cancer after failure of combination therapy or relapse within 6 months of adjuvant therapy
- Subsequent therapy for advanced ovarian cancer or as first-line therapy (in combination with Cisplatin).
- Treatment of AIDS related Kaposi’s sarcoma
- Non–small-cell lung cancer (NSCLC) as first-line therapy (in combination with Cisplatin).
- Abraxane: Treatment of breast cancer after failure of combination chemotherapy or relapse within 6 months of adjuvant chemotherapy.
- First-line treatment of metastatic adenocarcinoma of pancreas.
- Treatment of locally advanced or metastatic NSCLC.
OFF-LABEL:
- Bladder, cervical, small-cell lung, head and neck cancers.
- Treatment of adenocarcinoma.
- Abraxane: Recurrent/persistent ovarian, fallopian tube, primary peritoneal cancers.
Cautions & Contraindications:
- Hypersensitivity to Paclitaxel.
- Hypersensitivity to drugs developed with Cremophor EL (polyoxyethylated castor oil).
- Treatment of solid tumors with baseline neutrophil count less than 1,500 cells/mm3;
- Treatment of Kaposi’s sarcoma with baseline neutrophil count less than 1,000 cells/mm3
Cautions: Hepatic impairment, severe neutropenia, peripheral neuropathy
Metabolism & half- life:
- Does not readily cross blood-brain barrier.
- Protein binding: 89%–98%.
- Metabolized in liver.
- Excreted in bile/feces (71%), urine (14%). Not removed by hemodialysis.
- Half-life: 3-hr infusion: 13.1–20.2 hrs; 24-hr infusion: 15.7–52.7 hrs
Drug Interactions:
- Strong CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole, ritonavir) may increase concentration/effect.
- Strong CYP3A4 inducers (e.g., carBAMazepine, phenytoin, rifAMPin) may decrease effect.
- Bone marrow depressants (e.g., cladribine) may increase myelosuppression.
- Strong CYP2C8 inhibitors (e.g., gemfibrozil) may increase concentration/effect.
- Live virus vaccines may potentiate virus replication, increase vaccine side effects, decrease pt’s antibody response to vaccine.
- May elevate serum alkaline phosphatase, bilirubin, ALT, AST, triglycerides.
Side- Effects:
- Expected: Diarrhoea, alopecia, nausea, vomiting.
- Frequent: Myalgia, arthralgia, peripheral neuropathy.
- Occasional: Mucositis, hypotension during infusion, pain/redness at injection site.
- Rare: Bradycardia
Nursing Considerations
Baseline assessment
- Obtain CBC (note neutrophil count), BMP, LFT prior to each course.
- Receive full medication history and screen for interactions.
- Offer emotional support.
Intervention/evaluation
- Monitor CBC, LFT, vital signs.
- Monitor for hematologic toxicity (fever, sore throat, signs of local infections, unusual bleeding/bruising), symptoms of anemia (excessive fatigue, weakness).
- Monitor daily pattern of bowel activity, stool consistency; report diarrhea.
- Avoid IM injections, rectal temperatures, other traumas that may induce bleeding.
- Hold pressure to injection sites for full 5 min.
Patient/family teaching
- Hair loss is reversible, but new hair may have different color, texture.
- Do not have immunizations without physician’s approval (drug lowers resistance).
- Avoid crowds, persons with known infections. Report signs of infection at once (fever, flu-like symptoms).
- Report persistent nausea/vomiting.
- Be alert for signs of peripheral neuropathy.
- Avoid pregnancy.
- Avoid tasks that may require alertness, motor skills until response to drug is established.
REFERENCES
- Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
- McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
- April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
- Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
- Nursebro.com, Search – Nursebro
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