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Binds to reverse transcriptase enzyme, blocking RNA-dependent and DNA-dependent DNA polymerase synthesis
Tablets: 100 mg, 200 mg
Indications and dosages
➣ Human immunodeficiency virus (HIV)-1 infection
Adults: 400 mg P.O. t.i.d.
• Hypersensitivity to drug
• Concurrent use of alprazolam, astemizole, ergot derivatives, midazolam, pimozide, terfenadine, or triazolam
Use cautiously in:
• hepatic impairment
• pregnant or breastfeeding patients
• children younger than age 16 (safety and efficacy not established).
• Know that drug is usually given with at least two other antiretrovirals.
• If patient can't swallow tablets, dissolve 100-mg tablets in water by adding four tablets to at least 3 oz of water; let stand for a few minutes and then stir until completely dissolved. Have patient swallow entire mixture immediately. Then add small amount of water to glass and have him swallow this mixture to ensure that he consumes entire dose.
• Give 200-mg tablets intact; don't dissolve in water.
• If patient has achlorhydria, give drug with acidic beverage, such as orange juice.
Don't give concurrently with alprazolam, astemizole or terfenadine (no longer available in United States), ergot derivatives, midazolam, pimozide, or triazolam.
CNS: confusion, disorientation, dizziness, drowsiness, agitation, amnesia, changes in dreams, hallucinations, hyperesthesia, poor concentration, mania, nervousness, restlessness, paranoia, paresthesia, tremor, migraine, neuropathy, paralysis, seizures
CV: abnormal heart rate and rhythm, peripheral vascular disorder, peripheral edema, hypertension, orthostatic hypotension, cardiac insufficiency, cardiomyopathy
EENT: blurred or double vision, nystagmus, conjunctivitis, dry eyes, scleral yellowing, ear pain, otitis media, tinnitus, epistaxis, rhinitis
GI: nausea, diarrhea, constipation, abdominal pain or cramps, dyspepsia, abdominal distention, bloody stools, colitis, diverticulitis, enteritis, gastroenteritis, gastroesophageal reflux, mouth and tongue irritation and ulcers, increased saliva, difficulty swallowing, GI bleeding, pancreatitis
GU: hematuria, polyuria, chromaturia, proteinuria, nocturia, urinary tract infection, renal calculi, kidney pain, gynecomastia, erectile dysfunction, epididymitis, hemospermia, testicular pain, vaginal candidiasis, amenorrhea, irregular uterine bleeding
Hematologic: purpura, spleen disorders, eosinophilia, granulocytosis, disseminated intravascular coagulation, leukopenia, neutropenia, pancytopenia, hemolytic anemia
Hepatic: hepatotoxicity, hepatic failure, hepatomegaly
Metabolic: hypomagnesemia, hyperglycemia, hyperuricemia, hypocalcemia, hyponatremia, hypoglycemia, hyperkalemia, metabolic acidosis
Musculoskeletal: joint pain, arthritis, bone disorders, myalgia, muscle cramps, muscle weakness, bone pain, bone disorders, tendon disorders, tenosynovitis, neck pain and rigidity, limb pain, tetany, rhabdomyolysis
Respiratory: pulmonary congestion, dyspnea, pneumonia
Skin: pallor, bruising, yellowing of skin, dermal leukocytoblastic vasculitis, dermatitis, skin dryness and discoloration, erythema, folliculitis, herpes zoster or herpes simplex infection, petechiae, petechial or pruritic rash, seborrhea, alopecia, skin nodules, urticaria, sebaceous or epidermal cyst, angioedema, erythema multiforme
Other: tooth abscess, toothache, gingivitis, gum hemorrhage, weight gain or loss, fever, lymphadenopathy, adenopathy, increased thirst, hiccups, facial edema, pain, abscess, bacterial infection, Mycobacterium tuberculosis infection, body fat redistribution, hypersensitivity reaction, sepsis, Stevens-Johnson syndrome
Drug-drug. Alprazolam, astemizole, cisapride, ergot derivatives, midazolam, pimozide, terfenadine: increased risk of serious or life-threatening adverse reactions
Antacids, histamine2-receptor antagonists: reduced delavirdine absorption
Bepridil, clarithromycin, estrogen, hormonal contraceptives, indinavir, lopinavir-ritonavir, saquinavir, sildenafil, warfarin: increased blood levels of these drugs
Carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin: loss of virologic response, resistance to delavirdine
Cholesterol-lowering HMG-CoA reductase inhibitors cleared by the CYP3A4 pathway: increased risk of myopathy and rhabdomyolysis
Dexamethasone: decreased delavirdine blood level
Didanosine: decreased blood levels of both drugs
Fluoxetine, ketoconazole: 50% increase in delavirdine blood level
Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, bilirubin, creatinine, lipase, gamma-glutamyl transpeptidase, triglycerides: increased levels Granulocytes, hemoglobin, neutrophils, platelets, red blood cells, white blood cells: decreased values
Partial thromboplastin time, prothrombin time: increased
Drug-herbs. St. John's wort: loss of virologic response or resistance to delavirdine
• Monitor liver function test results frequently when giving drug concurrently with saquinavir.
• Check electrolyte and uric acid levels regularly.
☞ Monitor patient for serious hepatic, cardiovascular, and CNS problems and hypersensitivity reactions.
• Tell patient he can take drug with or without food.
• If patient can't swallow tablets, teach him how to dissolve 100-mg tablets in water.
☞ Tell patient to discontinue drug and consult prescriber immediately if he develops severe rash accompanied by fever, blistering, oral lesions, conjunctivitis, swelling, or muscle aches.
☞ Tell patient to promptly report unusual fatigue, yellowing of skin or eyes, unusual bruising or bleeding, muscle weakness, or signs and symptoms of infection.
☞ Advise patient that rash is a major adverse effect, usually occurring 1 to 3 weeks after therapy starts and resolving in 3 to 14 days. Instruct him to report rash promptly.
• Inform patient that drug doesn't cure HIV or reduce its transmission.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.