单词 | efavirenz |
释义 | efavirenze·fa·vir·enzE0047750 (ə-fä′vîr-ĕnz′)efavirenzefavirenz[ef´ah-vi″renz]efavirenzPharmacologic class: Nonnucleoside reverse transcriptase inhibitor Therapeutic class: Antiretroviral Pregnancy risk category D ActionInhibits human immunodeficiency virus (HIV) reverse transcriptase (required for transcription of HIV-1 RNA to DNA), leading to viral cell death AvailabilityCapsules: 50 mg, 200 mg Tablets: 600 mg Indications and dosages➣ HIV infection (given with one or more additional antiretrovirals) Adults and children older than age 3 and weighing more than 40 kg (88 lb): 600 mg P.O. once daily Children weighing 32.5 to 40 kg (71.5 to 88 lb): 400 mg P.O. once daily Children weighing 25 to 32.5 kg (55 to 71.5 lb): 350 mg P.O. once daily Children weighing 20 to 25 kg (44 to 55 lb): 300 mg P.O. once daily Children weighing 15 to 20 kg (33 to 44 lb): 250 mg P.O. once daily Children weighing 10 to 15 kg (22 to 33 lb): 200 mg P.O. once daily Dosage adjustment• Concurrent use of rifampin or voriconazole Contraindications• Hypersensitivity to drug • Concurrent use of astemizole, cisapride, midazolam, triazolam, ergot derivatives, voriconazole, or bepridil PrecautionsUse cautiously in: • hypercholesterolemia, hepatic impairment, concurrent use of hepatotoxic drugs, mental illness, or substance abuse • concurrent use of St. John's wort (use not recommended) • pregnant or breastfeeding patients • children. Administration• Give on empty stomach. • Know that drug is given with other antiretrovirals. ![]() Adverse reactionsCNS: dizziness, drowsiness, fatigue, insomnia, abnormal dreams, hypoesthesia, depression, headache, poor concentration, nervousness, anxiety, CNS depression, suicidal ideation CV: arrhythmias GI: nausea, diarrhea, flatulence, abdominal pain, dyspepsia GU: hematuria, renal calculi Hepatic: hepatotoxicity Respiratory: respiratory depression Skin: rash, diaphoresis, pruritus,erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome Other: increased appetite InteractionsDrug-drug. Azole antifungals (ketoconazole, voriconazole): decreased antifungal plasma concentration, increased efavirenz plasma concentration Calcium channel blockers: possible decreased calcium channel blocker concentration Clarithromycin, indinavir: reduced blood levels of these drugs CNS depressants (including antidepressants, antihistamines, opioids): increased CNS depression CYP450 inducers (including phenobarbital, rifabutin, rifampin): increased clearance and decreased blood level of efavirenz CYP450 inhibitors, ergot alkaloids, estrogen, midazolam, ritonavir, triazolam: increased blood levels of these drugs, greater risk of serious adverse reactions (including arrhythmias, CNS and respiratory depression, and hepatotoxicity) HMG-CoA reductase inhibitors: decreased plasma concentration of atorvastatin, pravastatin, and simvastatin Hormonal contraceptives: increased ethinyl estradiol blood level Protease inhibitors: decreased plasma level and efficacy of these drugs Saquinavir: decreased saquinavir blood level Warfarin: increased or decreased warfarin effects Drug-diagnostic tests. Alanine aminotransferase, aspartate aminotransferase, gamma-glutamyltransferase, total cholesterol, triglycerides: increased levels Urine cannabinoid test: false-positive result Drug-food. High-fat meal: increased drug absorption Drug-herbs. St. John's wort: decreased efavirenz blood level and efficacy, drug resistance Drug-behaviors. Alcohol use: increased CNS depression Patient monitoring• Monitor dietary intake and hepatic and lipid profile. • Closely monitor patients with hepatic failure. See Record mood changes and stay alert for suicidal ideation or behavior. • Be aware that drug may cause hypercholesterolemia. • Know that amount of HIV in blood may increase if patient stops drug therapy even briefly. Patient teaching• Instruct patient to take with full glass of water, preferably at bedtime to improve tolerance of CNS effects. Also tell him to avoid taking drug with high-fat meals. • Inform patient that drug must be taken in combination with other antiretrovirals. • Tell patient that drug doesn't cure HIV or AIDS and that he can still transmit virus to others. See Advise patient to report suicidal thoughts and other psychiatric symptoms. • Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness. See Tell female patient to immediately inform prescriber if she becomes pregnant. • Advise female patient to use adequate contraceptive measures for 12 weeks after discontinuing drug. • As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above. efavirenz(ə-fä′vîr-ĕnz′)efavirenzSustiva™ AIDS A reverse transcriptase inhibitor used with other antivirals–eg, zidovudine, lamivudine for HIV-1 infection Adverse effects N&V, maculopapular rash, fatigue, headache, dizziness. See Non-nucleoside reverse transcriptase inhibitor.efavirenzA non-nucleoside reverse transcriptase inhibitor used, in combination with other antiretroviral drugs, to treat HIV infections. The drug is on the WHO official list. A brand name is Sustiva. |
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