very Insoluble - rapid rate of induction/emergence MAC= 1.8%
Analgesia and muscle relaxation, no airway irritation. Sweet smelling, no pungency, potent bronchodilator, excellent for mask induction
Decreases CMR, increases CBF, mild increase in ICP Decreases BP, less tachycardia at higher MACs than other agents Potent bronchodilator, decrease tidal vol, increases resp rate, decreases response to hypoxia and hypercarbia
Use - Anesthesia (& analgesia). replaces halothane for pediatric anesthesia, degradation to compound A - neprotoxic in rates, can form CO during epxosure to dry CO2 absorbents - exothermic rxn - fires
Dissociates thalamus from the limbic cortex
structural analogue of PCP
IV/IM peak levels 10-15 min
more lipid-soluble,less protein-bound
can develop tolerance
Increases HR,BP,CO,myocardial work
Use care in those with CAD,CHF,uncontrolled BP,aneurysms,shock
airway tone remains intact
Emergence delirium and hallucinations
Natural product cancer drug
Paclitaxel and docetaxel interfere with the normal function of the mitotic spindle and are therefore cell cycle specific. They act differently from vinca alkaloids, since they prevent microtubule disassembly into tubulin dimers.
Paclitaxel and docetaxel are given intravenously. The taxanes have activity in a number of solid tumors, including breast, ovarian, lung, gastroesophageal, prostate, bladder, and head and neck cancers.
Paclitaxel causes neutropenia, a high incidence of peripheral neuropathy, and hypersensitivity reactions during infusion.
Breast - estrogen
• Is a selective estrogen-receptor modulator.
• Tamoxifen competitively binds to estrogen receptors on tumor cells and other tissue targets, producing a nuclear complex that inhibits the effects of ligand-receptor binding.
• Tamoxifen causes cells to remain in the G0 and G1 phases of the cell cycle; thus is primarily cytostatic in its mechanism of action.
• In breast, it acts as an ER-antagonist; however it also has agonist activity.
• Mild - bone and tumor pain, hot flashes, venous thrombosis, hypercalcemia, peripheral edema, distaste for food, pruritus vulvae, depression, dizziness, light-headedness, headache, hair thinning and/or partial hair loss, and vaginal dryness.
Since tamoxifen has agonist activity in the endometrium, extended use increases the risk of endometrial hyperplasia and neoplasms.
CML & GIST - BCR-ABL/c-kit
Identified via high-throughput screening against BCR-ABL, chemical modifications of the original parent compound resulted in additional improved activity against Platelet derived growth factor receptor (PDGFR) and c-kit mutant tumors.
Therapeutic Indication -
• FIRST-LINE therapy in chronic CML, in blast crisis,
• SECOND-LINE therapy for patients who have progressed on prior interferon-alpha treatment.
• It is also effective in the treatment of gastrointestinal stromal tumors (GIST) harboring c-Kit mutations. In the case of GIST tumors, doses of 600 mg/day are associated with improved response rates.
• Acute: Infusion reaction.
Delayed: Fluid retention with ankle and peri-orbital edema, diarrhea, nausea, vomiting, myalgias, congestive heart failure, hepatoxicity.
Renal/colon/breast & NSCLC - VEGF
• A recombinant, humanized monoclonal antibody that targets all forms of VEGF-A.
• The most common adverse reactions (> 10%) are epistaxis, headache, hypertension, rhinitis, proteinuria, taste alteration, dry skin, rectal hemorrhage, lacrimation disorder, back pain and exfoliative dermatitis.
• Hypertension and infusion reactions may also occur.
• The most serious complications are gastrointestinal (GI) perforation, surgery and wound healing problems, or severe bleeding, all of which necessitate discontinuation of treatment.