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Tivicay(Dolutegravir Tablets,テビケイ錠)

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Tivicay Tablets ( Dolutegravir )
テビケイ錠
Trade name
Tivicay Tablets
Generic name
Te Gras Dollar Bill sodium
(Dolutegravir Sodium)
Chemical Name
Monosodium (4R, 12aS) -9 - {[(2,4-difluorophenyl) methyl] carbamoyl}-4-methyl-6 ,8-dioxo-3, 4,6,8,12,12 a-hexahydro-2H-pyrido [1 ', 2': 4,5] pyrazino [2,1-b] [1,3] oxazin-7-olate
Molecular formula
C20H18F2N3NaO5
Molecular weight
441.36
Structural formula
Behavior
Pale yellow powder white to pale . Slightly soluble in water , and practically insoluble in ethanol ( 99.5 ) .
Melting point
Type 1 crystals decompose at the same time as the melt at about 350 ℃.
Partition coefficient
2.16 ± 0.01 (23 ℃)
The conditions of approval
When using one . This agent , so as to fully explain that or the like which is a collection of continuing the data of efficacy and safety further in relation to this drug for a patient , to obtain informed consent , and requests a doctor thing .
For clinical trials planned or ongoing in 2 . Overseas, shall be submitted analysis results and test results as soon as possible after the end .
Between 3 . Reexamination period until the end , we conduct a post-marketing survey of all patients treated in Japan as a general rule , information about the actual use of this drug (patient background , efficacy and safety (the other agent that it is possible to report on a regular basis by collecting data , etc.) and drug interactions . ) including the efficacy and safety of the combination at the time , should be submitted as application form attached documents to re-examination at the time of application the results of the investigation .
Dose effect and / or usage efficacy
HIV infection
Precautions related to the effect or efficacy

Upon treatment with this drug , it should be referring to ( phenotyping or genotyping ) drug resistance testing (where available) and treatment history of the patient .
Dosage and usage
I usually administered orally in a dosage regimen of less than or equal to adults . This drug can be administered with or without meals . Upon administration , it can be used in combination with other anti-HIV medicines means.
Patients with ( 1) untreated patients , treatment-experienced with anti- HIV drugs integrase inhibitors other than
I will be administered orally once a day 50mg as Dorutegurabiru .
Patients with resistance to ( 2 ) integrase inhibitors
I will orally twice a day 50mg as Dorutegurabiru .
It should be noted that the pediatric patients with untreated weight of 40kg and more than 12 years of age or older , and treatment experience with anti- HIV drugs integrase inhibitors other than , I can be administered orally once a day 50mg as Dorutegurabiru .
Usage Notes that are related to the dose and usage
Treatment with this drug may be initiated under the physician with substantial experience in anti- HIV therapy .
PRECAUTIONS
Careful administration
( It should be administered with caution in the following patients. )
There is a risk of ( exacerbation or increased transaminase ) deterioration of the liver function of hepatitis C virus -infected patients or B-type . (See "Important Precautions" ) ]
Important Precautions
In use one . This agent , after the appropriate person to replace it or patient consent was obtained and well explained for the following items , to be used .
Since this is not a radical treatment agents for HIV infection , there is a possibility to continue to develop a disease associated with the development of HIV infections including opportunistic infections ( 1 ) of this drug , changes in the physical state of this drug after the start for , be reported to the attending physician all .
Because it can cause interactions with the combination drug , ( 2 ) the agent shall be reported to the physician all drugs taking . Also see section " interaction" , in the case of taking the other drugs new treatment in the present agent , shall be reported to the physician in advance.
The effect of long-term administration of ( 3 ) this drug , and that it is currently unknown .
It has not been proven (4 ) this drug , whether to lower the risk of infection to others by blood contamination or sexual contact .
May want to change the dose without the instructions of ( 5 ) attending physician , you do not or stop taking the drug . [ See section "interaction" ]
In patients subjected to multidrug therapy of anti-HIV drugs , including the two . This agent , immune reconstitution inflammatory response syndrome have been reported . Sometimes after the start of the administration , immune function is restored and the inflammatory response to such (as Mycobacterium avium complex , cytomegalovirus , by Pneumocystis , etc.) asymptomatic opportunistic infections is expressed not only symptomatic . In addition , because there is a report ( hyperthyroidism , polymyositis , Guillain -Barre syndrome , uveitis , etc.) autoimmune disease is to express With the recovery of immune function , and to assess these symptoms , it is appropriate when needed taking into account the treatment Na .
In hepatitis C virus -coinfected patients and 3. B -type , since the incidence of exacerbations was higher than non- coinfected patients or transaminase increase , when administered to these patients , performing the liver function tests periodic be sufficiently like observed.
Interaction
This drug is a substrate of UGT1A1 mainly , CYP3A4 also is metabolized slightly . In addition , this drug inhibits (MATE1) organic cation transporter 2 Multidrug and Toxin Extrusion 1 and (OCT2). [ See section and "Usage Notes " and " pharmacokinetics " ]
Note combination
(Note the combination )
1 . Drug name, etc.
Pirushikainido
Clinical symptoms and Treatment
There is a possibility to increase the plasma concentrations of Pirushikainido . The combination , there is a risk that serious of expression and ventricular tachycardia which has been reported as a serious side effect in Pirushikainido , ventricular fibrillation , and the like sinus arrest may occur , observing carefully the combination of .
Mechanism and Risk Factors
There is a possibility that the inhibitory effect of MATE1 and OCT2 of this drug , is inhibited emissions Pirushikainido .
2 . Drug name, etc.
Etravirine
Clinical symptoms and Treatment
1 there is a reported 52% in Cmax, and decreased 88% in Cτ plasma concentrations of this drug ) . When used in combination with this drug , it can be co-administered either atazanavir / ritonavir , darunavir / ritonavir , lopinavir / ritonavir .
Mechanism and Risk Factors
By these agents induce UGT1A1 and CYP3A4, the metabolism of the drug is promoted .
3 . Drug name, etc.
Efavirenz
Clinical symptoms and Treatment
2 there is a reported 39% in Cmax, and decreased 75% in Cτ plasma concentrations of this drug ) . In patients with treatment-experienced with anti- HIV drugs HIV integrase inhibitors other than , it should be increased to twice a day this drug 50mg and untreated patients . In the patients with resistance to HIV integrase inhibitors , and that it not be used with this drug .
Mechanism and Risk Factors
By these agents induce UGT1A1 and CYP3A4, the metabolism of the drug is promoted .
4 . Drug name, etc.
Nevirapine
Clinical symptoms and Treatment
There is a possibility of lowering the plasma level of the drug . In patients with treatment-experienced with anti- HIV drugs integrase inhibitors other than , it should be increased to twice a day this drug 50mg and untreated patients . In the patients with resistance to HIV integrase inhibitors , and that it not be used with this drug .
Mechanism and Risk Factors
By these agents induce UGT1A1 and CYP3A4, the metabolism of the drug is promoted .
5 . Drug name, etc.
Fosamprenavir / ritonavir
Clinical symptoms and Treatment
3 ) Since there is a reported 24% in Cmax, and decreased 49% in Cτ the plasma concentration of the drug , in patients with resistance to HIV integrase inhibitors , and that it not be used with this drug .
Mechanism and Risk Factors
By fosamprenavir to induce UGT1A1 and CYP3A4, the metabolism of this drug is promoted .
6 . Drug name, etc.
Phenytoin
Phenobarbital
Carbamazepine
(St. John's Wort, St. John's wort )-containing food , St. John's Wort
Clinical symptoms and Treatment
There is a possibility of lowering the plasma level of the drug .
Mechanism and Risk Factors
By St. John's wort induces CYP3A4 and UGT1A1 and agents of these , the metabolism of this drug is promoted .
7 . Drug name, etc.
Rifampicin
Clinical symptoms and Treatment
4 there is a reported 43% in Cmax, and decreased 72% in Cτ plasma concentrations of this drug ) . In patients with treatment-experienced with anti- HIV drugs integrase inhibitors other than , it should be increased to twice a day this drug 50mg and untreated patients . In the patients with resistance to HIV integrase inhibitors , and that it not be used with this drug .
Mechanism and Risk Factors
By rifampicin induces UGT1A1 and CYP3A4, the metabolism of this drug is promoted .
8 . Drug name, etc.
(Mg, Al , etc. )-containing formulation polyvalent cations
Clinical symptoms and Treatment
5 to 72% decrease in Cmax, 74% C24 in the plasma concentration of the drug ) . Administration after 6 hours or 2 hours before administration of multivalent cation-containing antacid is recommended for this drug .
Mechanism and Risk Factors
By forming complexes with polyvalent cations thereof , absorption of the drug is inhibited .
9 . Drug name, etc.
Iron , calcium -containing preparations ( supplements )
Clinical symptoms and Treatment
5 to 35% decrease in Cmax, 32% C24 in the plasma concentration of the drug ) . With the exception of When taken at the same time as the meal , administration after 6 hours or 2 hours before administration iron , calcium-containing formulation is recommended for this drug .
Mechanism and Risk Factors
By forming iron complexes with calcium , the absorption of the drug is inhibited .
10 . Drug name, etc.
Metformin
Clinical symptoms and Treatment
Which may increase the plasma concentrations of metformin . The start of the combination therapy and at the end , it should be carefully observed , particularly .
Mechanism and Risk Factors
There is a possibility that the inhibitory effect of MATE1 and OCT2 of this drug , is inhibited discharge of metformin .
Side effect
Overview of side effects such as expression situation
< Test of the examination of the once -daily dosing of this drug >
Clinical trials overseas in (ING111762, ING112276, ING112961, ING113086, ING114467), side effect of that as patients who have experience treating patients with no treatment experience with anti-HIV drugs , was administered once a day this drug 50mg is the observed ( 452 cases of 1,364 patients ) 33% , nausea ( 8%) , diarrhea (6%) and headache major side effect was ( 4%) . ( Approval )
< Test of the examination of the twice-daily administration of this drug >
Clinical trials overseas in (ING112574, ING112961), side effect of that as patients having resistance to HIV integrase inhibitor therapy experience with anti-HIV drugs and , there , was administered twice a day this drug 50mg 27 percent observed in ( 56 cases in 207 cases ) , nausea ( 5% ) , diarrhea (5%) and headache major side effect was ( 5%) . ( Approval )
Clinically significant adverse reactions
Drug-induced hypersensitivity syndrome
( Less than 1% ) Note 1)
Rash as the initial symptoms , fever was observed , because it may hypersensitivity serious symptoms of late-onset associated with liver dysfunction , lymphadenopathy , etc. eosinophilia further appears , should be carefully observed , this If such symptoms are observed, it should be discontinued and administration , and appropriate measures should be taken . In addition, it is important to note because it may be rash symptoms after discontinuation , fever , liver dysfunction , etc. are prolonged or relapse .
Other side effects
1 . The immune system
Note 1: less than 1% )
Immune reconstitution inflammatory response syndrome
2 . Psychiatric and nervous system
Note 1 2% or more )
Headache , insomnia , dizziness , abnormal dreams
3 . Digestive
Note 1 2% or more )
Nausea , diarrhea , vomiting
4 . Digestive
Note 1: 1-2% or less)
Upper abdominal pain , flatulence
5 . Digestive
Note 1: less than 1% )
Abdominal discomfort , abdominal pain
6 . Liver
Note 1: less than 1% )
Hepatitis
7 . Skin
Note 1: 1-2% or less)
Rash , itching
8 . Systemic symptoms
Note 1 2% or more )
Fatigue
9 . Clinical examination
Note 1: less than 1% )
Bilirubin , creatinine rise
10 . Clinical examination
Incidence unknown Note 2 )
CPK rise
For frequency Note 1) side effects , I was described on the basis of the foreign clinical study results that target adult HIV-infected patients .
Side effects reported Note 2 ) Overseas clinical trials from (ING111762, ING112276, ING112961, ING113086, ING114467) than was the frequency unknown .
Administration to elderly
Pharmacokinetics in the elderly of this drug has not been studied . ( Liver function , renal function , cardiac function , etc.) has decreased physiological functions in the elderly in general , if you are a combination of other drugs because there are many or have complications , observe the condition of the patient be administered with caution while .
Administration pregnant women , maternal , to Lactation
Be administered only when it is determined that women suspected of being pregnant or 1 . Pregnant , therapeutic benefit may outweigh the risk . The safety of this drug of the pregnant women has not been established . 6 placental transfer has been observed in animal studies ( rat ) ) . ]
And that it stops the breast-feeding 2 . This agent during the administration . It is not known whether or not to migrate in the milk of the person . Based on ( rat) animal studies , 6 it proceeds to milk in humans is expected ) . Further , in order to prevent HIV infection of infants generally women infected with HIV in all situations should not be lactating . ]
Administration to children , etc.
( Insufficient clinical ) has not been established. Safety for children weighing 40kg or less than 12 years of age in low birth weight infants , newborn , infant , or toddler .
Overdose
Signs and symptoms
Data by overdose is limited . Once the drug to 250mg administered to healthy adults in clinical trials , side effects can not be predicted has not been reported .
Treatment
There is no specific treatment for overdose of this drug . In the case of overdosage , and be closely monitored , and appropriate supportive care according to need . Because of its high protein -binding rate , likely to be removed by hemodialysis is low this drug .
Packing
Tebikei Tablets 50mg: 30 tablets ( bottle )
Production sales agency
ViiV Healthcare Co., Ltd.

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