Bula do remedy Rescriptor

the package insert of the medicine Rescriptor.

what For?

Use in combination with anti-retroviral agents suitable in the treatment of infection by HIV-1, when the treatment is justified.


When should I not use?

clinically significant Hypersensitivity demonstrated previously to any of the components of the formulation. – Warnings: coadministration of Rescriptor with certain antihistamines non-sedative, hypnotic sedatives, antiarrhythmics, calcium channel blockers, preparations of the alkaloids of ergot, amphetamines, and cisapride, may result in adverse reactions potentially serious and/or that offer life-threatening because of the possible effects of Rescriptor on the hepatic metabolism of certain drugs.


How to use?

The recommended dose of Rescriptor is 400 mg (4 tablets of 100 mg), 3 times per day. Rescriptor should be used in combination with other antiretroviral treatments appropriate. The prescribing information for the complete other antiretroviral agents should be consulted for information on dosage and administration. Care in the administration: the tablets of Rescriptor may be dispersed in water prior to consumption. To prepare a dispersion, add 4 tablets of Rescriptor to at least 85 ml of water. After a few minutes, mix the solution, to obtain a uniform dispersion. The solution should be used immediately. The glass should be rinsed with water and this water should be ingested, to ensure that the entire dose has been consumed. Rescriptor can be administered with or without food. Patients with achlorhydria should take the tablets of Rescriptor with a drink the acid (for example, orange juice). However, the effect of a drink the acid in the absorption of delavirdine in patients with achlorhydria has not been investigated. The patients in treatment with Rescriptor and antacids should take your medications at least one hour of range. Overdosage: there are no reports of overdosage with Rescriptor in humans. The treatment of overdose of Rescriptor should consist of measures of general support, including monitoring of vital signs and observation of the clinical status of the patient. There is no specific antidote to the overdose of Rescriptor. If indicated, elimination of the drug is not absorbed must be made by êmese or gastric lavage. Such as delavirdine is metabolized extensively by the liver and provides a link to protein high, it is unlikely that the dialysis is beneficial, to remove significantly the drug. Elderly patients: the pharmacokinetics of delavirdine has not been investigated specifically in patients over 65 years of age.

Side Effects

What are the evils that can cause me?

Headache; fatigue; nausea; diarrhea; vomiting; ALT increased (SGPT); AST increased (SGOT); rash; rash maculopapular; rash. General symptoms: colic abdominal, abdominal distension, abdominal pain (generalized or localized), allergic reaction, asthenia, pain in back, chest pain, chills, edema (generalized or localized), cyst, epidermoid, fever, back pain, flu syndrome, lethargy, swelling, sores, malaise, stiff neck, pain (generalized or localized), sebaceous cyst, trauma, and infection respiratory upper. Cardiovascular system: bradycardia, migraine, pallor, palpitation, postural hypotension, syncope, tachycardia, and vasodilation. Digestive system: anorexia, stomatitis mouth, melena, colitis, constipation, reduced appetite, diarrhea (Clostridium difficile), diverticulitis, duodenite, dry mouth, dyspepsia, dysphagia, enteritis, esophagitis, fecal incontinence, flatulence, nausea, gastritis, gastroesophageal reflux, bleeding gastrointestinal disorder gastrointestinal, gingivitis, bleeding, gingival, increased appetite, increased salivation, increased thirst, ulcers of the mouth, hepatitis nonspecific, pancreatitis, disorder rectal, sialadenite, stomatitis, and edema or ulceration on the tongue. System haematological and lymphatic systems: anemia, hematoma, bruising, eosinophilia, granulocitose, neutropenia, pancytopenia, petechia, time of thromboplastin partial, prolonged, purple, and disorder in the spleen and thrombocytopenia. Metabolic and nutritional disorders: alcohol intolerance, bilirrubinemia, hyperkalemia, hyperuricemia, hypocalcemia, hyponatremia, hipofosfatemia, increased gamma-glutamiltranspeptidase, lipase increased, alkaline phosphatase serum increased, amylase serum increased, creatine fosfoquinase serum increased, blood creatinine increased, peripheral edema, and increase or weight reduction. Musculoskeletal system: arthralgia or arthritis of the joints isolated or multiple, bone disorders, bone pain, leg cramps, muscle weakness, myalgia, disorders of the tendon, tenosynovitis and tetania. Nervous system: coordination abnormal, agitation, amnesia, anxiety, disorders of dreams, cognitive impairment, confusion, reduced libido, depressive symptoms, disorientation, dizziness, emotional lability, hallucination, hiperestesia, hyper-reflexia, hypoesthesia, impaired concentration, insomnia, manic symptoms, muscle cramp, nervousness, neuropathy, nightmares, nystagmus, paralysis, symptoms paranoid, paresthesia, restlessness, somnolence, tingling, tremor, vertigo, weakness. Respiratory system: bronchitis, congestion of the chest, cough, dyspnea, epistaxis, laringismo, pharyngitis, rhinitis, and sinusitis. Skin and appendages: angioedema, leukocytoclastic vasculitis dermal, peeling, dermatitis, diaforese, dry skin, erythema, erythema multiforme, folliculitis, dermatitis fungal, hair loss, onicopatias, rash petechial, seborrhea, skin disorder, skin nodule, Stevens-Johnson syndrome, urticaria, and rash vesiculobolhoso. Senses: special: blepharitis, conjunctivitis, diplopia, dry eyes, otalgia, photophobia, perversion of taste and tinnitus. Urogenital system: breast enlargement, kidney stones, epididymitis, hematuria, hemospermia, impotence, pain, renal, metrorragia, noctúria, polyuria, proteinuria and f-vaginal.

Warnings and Precautions

what should I know before using?

General: delavirdine is metabolized primarily by the liver. For this reason, you should be careful, when the administration of Rescriptor in patients with liver failure. Resistance/cross-resistance: non-nucleosídios reverse transcriptase inhibitors, when used alone or in combination, may confer cross-resistance to other non-nucleosídios reverse transcriptase inhibitors. Skin rash: the rash was typically diffuse, maculopapular, lupus erythematosus, and often pruriginoso. The skin rash was more common in patients with counts, smaller CD4 cells and generally occurred within 1 to 3 weeks (median = 11 days) of treatment. In most cases, the duration of the rash was less than 2 weeks and have not been required dose reductions or interruption of treatment with Rescriptor. The majority of patients could resume treatment after provocation with Rescriptor, after a treatment interruption due to rash. The distribution of the rash was mainly in the upper part of the body and the region proximal of the arms, with an intensity decreasing of the lesions in the neck and face that was progressively less on the rest of the trunk and limbs. The erythema multiforme and the Stevens-Johnson syndrome have been observed rarely, and have resolved themselves after discontinuation of Rescriptor. Every patient present a rash-severe or a rash accompanied by symptoms such as fever, blistering, oral lesions, conjunctivitis, swelling, muscle or joint pain, you should suspend the Rescriptor and consult a doctor. The occurrence of an exanthema related with the delavirdine after a month of treatment is unusual, unless there is a prolonged interruption of treatment with Rescriptor. Has been obtained symptomatic relief with the hydrochloride of diphenhydramine, hydrochloride hydroxyzine and/or topical corticosteroids. Patients should be informed that Rescriptor does not cure the infection by HIV-1 and that they may continue to develop illnesses associated with infection by HIV-1, including opportunistic infections. Has not been demonstrated that the treatment with Rescriptor reduces the incidence or frequency of such illnesses, and patients should be advised to remain under medical supervision during treatment with Rescriptor. Warn patients as to the fact that the effects in the long-term treatment with mesilato of delavirdine are not yet known. They should be warned that it has not been demonstrated that the use of Rescriptor reduces the risk of transmission of HIV-1. Patients should be informed that the main toxic effect of Rescriptor is rash and should inform your doctor immediately if you are experiencing this adverse effect. Most of the exantemas associated with the mesilato de delavirdine occurs within 1 to 3 weeks after initiating treatment with Rescriptor. The rash normally resolves in 3 to 14 days and can be treated symptomatically during the treatment with Rescriptor. Every patient present a rash-severe or a rash accompanied by symptoms such as fever, blistering, oral lesions, conjunctivitis, swelling, muscle or joint pain, you should discontinue the medicine and consult a doctor. Patients should be instructed to take Rescriptor every day as the prescription. Patients should not modify the dose of Rescriptor without consulting your doctor. If a dose is not taken, patients should take the dose of subseqüente, as soon as possible. However, if a dose is not taken, the patient should not double the next dose. As mesilato of delavirdine can interact with certain drugs, patients should be instructed to inform your doctor about any drugs used under prescription or as self-medication. Pregnancy: no studies have been conducted, adequate and well-controlled of delavirdine in pregnant women. Rescriptor should be used during pregnancy only if the potential benefit justify the potential risk to the fetus. Lactating women: it should be recommended that HIV-infected mothers not breastfeed their infants to avoid the risk of postnatal transmission of HIV to a child who may not be infected yet. Paediatric use: the safety and effectiveness of delavirdine in combination with other antiretroviral agents have not been established in individuals infected by HIV-1 with less than 16 years of age. Drug interactions: general: coadministration of Rescriptor with certain antihistamines non-sedative, hypnotic sedatives, antiarrhythmics, calcium channel blockers, preparations of the alkaloids of ergot, amphetamines, and cisapride, may result in adverse reactions potentially serious and/or life-threatening. In virtue of the inhibitory effect of delavirdine on CYP3A and CYP2C9, coadministration of Rescriptor with drugs that are metabolized primarily by these hepatic enzymes may result in decreased plasma concentrations increased. Plasma concentrations the highest of these drugs may enhance or prolong the therapeutic effects and adverse effects: HIV protease inhibitors: indinavir, saquinavir. Antihistamines: terfenadine**, astemizole**. Antimicrobial agents: clarithromycin, dapsone, rifabutin. Agents against migraine headache: ergot derivatives. Benzodiazepines: alprazolam,**, midazolam**, triazolam**. Calcium channel blockers: diidropiridinas, for example, nifedipine. Agents that act on motility gastrointestinal: cisapride**. Other: quinidine, warfarin. (*Not included for all drugs) (** See Warnings). For this reason, it may be necessary adjustments posológicos proper of these drugs. Drugs that induce CYP3A may also reduce plasma concentrations of delavirdine: anticonvulsants: carbamazepine, phenobarbital, phenytoin. Agents antimicobacterianos: rifabutin, rifampin. (* Are not inclusive of all drugs. (** Rescriptor may not be effective, when administered concomitantly with these drugs). Physicians should consider the use of alternative drugs for the drugs that induce CYP3A while a patient is taking Rescriptor. Antacids: the doses of an antacid and Rescriptor should be separated by at least an hour, because the absorption of delavirdine is reduced when it is administered concomitantly with antacids. Agents anticonvulsants: phenobarbital, phenytoin, carbamazepine: it is not recommended the concomitant administration of delavirdine with these agents, because of the limited data on the pharmacokinetics in the population indicate that there may occur a substantial reduction in the plasma concentrations of delavirdine. Agents antimicobacterianos: rifabutin: coadministration of delavirdine and rifabutin is not recommended, because rifabutin substantially reduces the plasma concentrations of delavirdine, and delavirdine increases the plasma concentrations of rifabutin. Rifampin: the delavirdine should not be administered concomitantly with rifampin, because rifampin reduces exposure systemic to delavirdine (AUC) by almost 100%. Receptor antagonists antihistamines H2: cimetidine, famotidine, nizatidine, and ranitidine: these agents increase the pH of gastric and may reduce the absorption of delavirdine. Although the effect of these drugs on the absorption of delavirdine has not been evaluated, is not recommended for chronic use of these drugs with delavirdine. Analógos of nucleosídios reverse transcriptase inhibitors: didanosine: administration of didanosine and delavirdine should be separated by at least one hour, because coadministration of didanosine and delavirdine resulted in the exposure systemic reduced to both drugs by approximately 20%. Protease inhibitors: indinavir: due to an increase in the plasma concentrations of indinavir (preliminary results), one should consider a reduction in the dose of indinavir to 600 mg 3 times per day, when delavirdine and indinavir are administered concomitantly. Currently, there are no data on safety and efficacy of this combination. Ritonavir: no studies have been conducted with the combination therapy of delavirdine and ritonavir at the recommended doses. The preliminary results indicate that there is no evidence of an interaction with doses of 400 mg to 600 mg of delavirdine, 2 times per day, and 300 mg of ritonavir, 2 times a day. Currently, there are no data on safety and efficacy of this combination. Saquinavir: the AUC of saquinavir increased by 5 times, when delavirdine (400 mg, 3 times per day) and saquinavir (600 mg, 3 times per day) were administered in combination. Currently, there are no data on safety and efficacy of this combination. In a small preliminary study, there were elevations of the enzymes monitored in 13% of individuals during the first few weeks of treatment with the combination of delavirdine and saquinavir (6%, grade 3 or 4). Enzymes, hepatocellular (ALT/AST) should be monitored frequently if this combination is prescribed.