Aluvia drug 200mg/50mg Abbott supports HIV-1 infection treatment (120 tablets)

Dosage form Box of 120 tablets
Specifications Lopinavir, ritonavir
Ingredient Abbvie

Ingredient

Composition information	Content
Lopinavir	200mg
Ritonavir	50mg

Uses

Indications

Aluvia drugs are indicated in the following cases:

Indications for coordination with other antiviral drugs to treat patients infected with viruses that cause immunodeficiency in humans (HIV-1) on adults, adolescents and children of 2 or more. Humanity

Pharmacokology

The mechanism of action: Aluvia's antiviral active ingredient is Lopinavir. Lopinavir is an enzyme inhibitor of HIV-1 and HIV-2 virus. The protease inhibitor of HIV prevents hydrolysis of polyprotein Gag-polyprotein leads to the formation of incomplete and non-communicable viruses.

Dynamic pharmacy

Lopinavir pharmacokinetic properties in collaboration with Ritonavir are evaluated on healthy volunteers and on HIV -infected patients, there is no significant difference recorded between these two groups.

Lopinavir is fully metabolized through CYP3A. Ritonavir inhibits the metabolism of Lopinavir, thus increasing the concentration of Lopinavir in plasma.

Studies show that the treatment with Aluvia 400/100 mg x 2 times daily creates Lopinavir concentration in a stable state in plasma 15 to 20 times higher than the concentration of Ritonavir in HIV -infected patients.

Ritonavir concentration is 7% less than the concentration obtained after using Ritonavir at a dose of 600 mg 2 daily. The antiviral study on In vitro shows that the EC50 value of Lopinavir is nearly 10 times lower than that of Ritonavir. Therefore, the antiviral activity of Aluvia is caused by Lopinavir.

absorption

Use multi -dose 400/100 mg Lopinavir/ritonavir 2 times a day for 2 weeks with unlimited conditions of diet shows that the top concentration of Lopinavir in plasma (cmax) (average value + sd) is 12.3 ± 5.4 µg/ml that appears about 4 hours after the drug.

The bottom concentration of stable state obtained before using the morning dose is 8.L ± 5.7 µg/ mi. The AUC value of Lopinavir with minerals is 12 hours from the average of 113.2 ± 60.5 µg.h/Mi. Lopinavir's absolute bioavailability when coordinated with Ritonavir has not been established on humans.

Effects of food on oral absorption: Use Aluvia 300/100 mg single tablets with a diet here enough (rich in fat 872 kcal, 56% of calories are supplied from fat) compared to when using drugs when hungry shows that there is no significant change of value of CMAX and AUC.

Therefore, Aluvia tablets can be used with or not with food. Aluvia tablets are less likely to have pharmacokinetic transformation due to more eating conditions, with Aluvia soft capsules.

distribution

In a stable state, the ratio of Lopinavir is attached to plasma proteins about 98-99%, Lopinavir is attached to both alpha-1-acid glycoprotein (AAG) and albumin, but Lopinavir has a higher affinity with AAG.

In a stable state, Lopinavir links with proteins are still constant in the concentration range recorded after the aluvia porcelain dose of 400/100 mg x 2 times daily and this ratio is similar to a healthy volunteer group and HIV -infected patients group.

transformation

In vitro tests conducted on human liver microsom shows that Lopinavir is mainly metabolized by redox.

Lopinavir metabolizes mainly swimming Cytochrom P450 system in the liver, largely due to the ISOZYM CYP3A group. Ritonavir is a strong CYP3A inhibitor, inhibiting the metabolism of Lopinavir thus increasing the concentration of Lopinavir in plasma. A study using Lopinavir with 14C-Lopiravir radio isotope conducted on humans showed that 89% of radioactive activity, plasma after taking 1 dose of Aluvia 400/100 mg was due to mother substance.

There are at least 13 derivative oxidant metabolites from Lopinavir found on humans. Epime isomers of specialized chemicals at 4-oxo and 4-hydrogen are the main metabolites with antiviral activity but the radioactive activity in plasma is very low.

Ritonavir has an enzyme induction effect that leads to its own transformation and can touch the transformation of Lopinavir. Lopinavir concentration from the front dose decreases during multi -dose use and this concentration is stable after about 10 days to 2 weeks.

Elimination

After using 14C-Lopinavir/Ritonavir 400/100 mg, about 10.4 ± 2.3% and 82.6 ± 2.5% of the dose of 14C-Lopinavir are detected in urine and feces. The amount of Lopinavir does not turn hills accounting for about 2.2% and 19.8% of the dosage appears in the urine and feces.

After using multi -dose, less than 3% of Lopinavir excreted in the urine in the form of not being changed by the sea. Lopinavir waste time with a gap of 12 hours is about 5-6 hours on average, the expense of oral clearance (Cl/F) of Lopinavir is 6 to 7 l/h.

DAY DAY MODE: Lopilavir/ritonavir dosage 1 time daily is evaluated in HIV -infected patients who have never treated with antacids. Lopinavir/ritonavir dose of 800/200 mg is used in combination with Emtricitabin 200mg and Tenofovir DF 300mg into a 1 -time dose mode per day.

Use multi -dose Lopinavir/Ritonavir 800/200 mg 1 time per day for 2 weeks in the condition of restrictive diet for the concentration of Lopinavir in, plasma (cmax) (average value ± sd) is 14.8 ± 3.5 µg/ml, exporting about 6 hours after the beginning of treatment.

The bottom concentration is stable before using the morning dose of 5.5 ± 5.4 µg/ml. The AUC value of Lopinavir with an average 24 -hour dose is 206.5 ± 89.7 µg.h/ml.

Compared to the dosage mode 2 times daily, the one -time dose per day reduces the CMIN/CTROY value, approximately 50%.

Special subject group

Pediatric patients

Dynamic data of aluvia tablets in children under 2 years of age is limited.

Dynamic pharmacokinetics of Lopinavir/Ritonavir oral solution dose of 300/75 mg/mg2 2 times daily and 230/57.5 mg/m2 2 times daily are studied on 53 pediatric patients, aged ranging from 6 months to 12 years old.

In a state of stabilization of the value of AUC parameters. Lopinavir's cmax and cmin are 72.6 ± 31.1 µg.h/ml; 8.2 ± 29 µg/ml and 3.4 ± 2.1 µg/ml after taking Lopinavir/Ritonavir solution dose 230/57.5 mg/m2 2 times daily without coordinating Nevirapin (n = 12); The value of the parameters corresponding to 85.8 ± 36.9 µg.h/ml, 10.0 ± 3.3 µg/ml and 3.6 ± 3.5 µg/ml after taking Lopinavir/Ritonavir dose 300/75 mg/mg2 2 times daily with Nevirapin (N = 12).

Dosage mode 230/57.5 mg/m2 2 times daily without coordination Nevirapin and a dose mode of 300/75 mg/m2 2 times daily with Nevirapin combination evenly for Lopinavir concentration in plasma similar to the value obtained in adult adult patients using the dose of 400/100 mg 2 times a day without Nevirapin.

Lopinavir/ritonavir dose 1 time daily has not been evaluated in pediatric patients.

Sex, race and age

The pharmacokinetics of Aluvia have not been studied in the elderly. There is no relationship between age and gender and pharmacokinetic differences recorded in patients. Do not accept the difference in pharmacokinetics due to race.

Renal function impairment

Aluvia's pharmacokinetics have not been studied in patients with renal function. However, due to the negligible lopinavir kidney clearance, the body's total clearance is reduced in patients with renal impairment.

Liver function impairment

Dynamic parameters in the stable state of Lopinavir in HIV -infected patients with mild to moderate liver function impaired are compared to patients with HIV infected with normal liver function in, a multi -dose study using Lopinavir/Ritonavir 400 mg, 2 times daily. Lopinavir's blood concentration increased by about 30% has been received but this increase is not considered clinical significance.

Before taking Aluvia drug 200mg/50mg Abbott supports HIV-1 infection treatment (120 tablets)

How to use

Aluvia drugs are used orally and must be swallowed directly, not chewed, broken or crushed.

Aluvia can be used or not with food.

Dosage

Should use Aluvia according to the doctor's expense already have HIV infection experience.

Used for adults and adolescents

Aluvia is indicated with a standard dose of 400/100 mg (2 tablets 200/50 mg) 2 times daily use or not with food. In adult patients, in the necessary cases of 1 -time dosage daily.

Aluvia may be specified at a dose of 800/200 mg (4 tablets 200/50 mg) once daily use or not with food. It is necessary to limit the use of 1 -time daily for patients with very little mutations related to protease inhibitors (meaning less than 3 mutations related to protease inhibitors described in the results of clinical trials) and should pay attention to the risk of reducing the ability to maintain antivirus effect and high risk of diarrhea compared to the standard regimen recommended by 2 times daily.

Used for pediatric patients (children from 2 years old)

The dosage of Aluvia is indicated for adults (400/100 mg 2 times daily) can be applied to children weighing 40 kg or more or the body surface area is larger than I, 4 m2 (BSA).

Cases of children weighing less than 40 kg or surface area from 0.5 to 1.4 m2 and can be taken in tablet form.

Lopinavir/ritonavir regimen 1 time daily has not been evaluated on pediatric patients.

Children under 2 years old

The safety and effectiveness of Aluvia tablets have not been set for children under 2 years old. The existing data is presented in the pharmacokinetic section but there is no recommendation about the dosage that can be given.

combined therapy: Efavirenz or nevirapin.

The switching guidelines of Aluvia tablets are based on the surface area of the body when used in combination with Efavirenz or Nevirapin for children.

Instructions for use in combination with Efavirenz or Nevirapin for children

Dosage recommended by Lopinavir/Rifonavir (mg) 2 times daily.

The corresponding dose can be achieved with two existing content of Aluvia 100/25 mg and 200/50 mg.

≥ 0.5 to

200/50 mg.

≥ 0.8 to

300/75 mg.

400/100 mg.

≥ 1.4

500/125 mg.

In patients with HIV infected with mild and medium -severe liver failure, Lopinavir concentration increased by about 30% but this increase does not bring any clinical change (see pharmacokinetic part). There is no data on patients with severe liver failure. Aluvia should not be used for patients with severe liver failure.

Patients with renal failure

Lopinavir and ritonavir's clearance in the kidneys is negligible, so it is less likely to have an increased serum concentration in patients with renal impairment. Because Lopinavir and Ritonavir are strongly attached to proteins, it is less likely to be significantly removed by hemorrhage or peritoneal fertilizer.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.

What to do when using overdose?

Clinical symptoms recorded on dogs include increased salivation, vomiting and abnormal diarrhea/stool. The signs of poisoning have been recorded in mice, rats and dogs including reduced activity, loss of air conditioning, thin, dehydration and tremor.

There is no specific antidote for the case of Aluvia overdose. Aluvia overdose should be handled by general support measures including monitoring of survival signs and patient clinical status. When indicated, the amount of drugs should be removed from the intestinal mucosa by causing vomiting or gastric wash.

Using activated carbon can also help eliminate unprocessed drugs. Aluvia is strongly associated with protein, so the separation is ineffective in eliminating the active ingredient.

What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.

Side Effects

When using Aluvia, you may experience unwanted effects (ADR).

The most common harmful reactions related to Lopinavir/Ritonavir therapy in clinical trials are diarrhea, nausea, vomiting, hyperliglycerides and hypercholesterol.

The risk of diarrhea is higher when using Aluxia 1 time daily. Diarrhea, nausea, vomiting can grind at the beginning of the treatment, while hyperglyceride blood and hyperchemical hypercholesterol may occur later. 7% of patients had to stop participating in the term of phase studies II-IV due to adverse neck variables that need treatment.

It should be noted that some cases of pancreatic inflammation have been reported in patients using Lopinavir/Ritonavir, including progressive triglyceride patients. Moreover, prolonging PR interval is also reported while treatment with Lopinavir/ Riritonavir.

Unwanted effects in adults are recorded in clinical trials and after -sales monitoring.

common, ADR ≥ 1/10

Infections and parasites: Sugar infections are steamed.

Infection and parasitic infection: Lower respiratory infections, skin infections include cellulitis, folliculitis and boils. sex. Eye: Reduction of vision. AST, ALT and GGT. Production and mammary gland: erectile dysfunction in men. Menstrual disorders, menstrual loss, menstrual periods in women.

immune system disorders: immune regeneration syndrome. Heart, atrial block, three -leaf valve failure. Vascular, vasculitis.

Liver disorders: Jaundice.

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

Contraindicated

Aluvia drugs are contraindicated in the following cases:

Patients with a history of sensitivity to Lopinavir, Ritonavir or any ingredient of the drug.

Patients with severe liver failure.

Do not use Aluvia combination with rifampicin because of reducing Lopinavir's concentration, leading to a significant reduction in the treatment effect of Lopinavir. Aluvia should not be coordinated with drugs with high dependent clearance on CYP3A because of the high plasma drug concentration related to serious or life -threatening events.

Precautions for use

Patients with diseases with

Hepatic failure

The safety and effectiveness of Aluvia has not been established in patients with significant disorders of liver function. Aluvia is contraindicated to patients with severe liver failure. Patients with chronic hepatitis B or hepatitis C treated with high risk of anti -Retrovirus anti -Retrovirus drugs that have a serious life -threatening response to the liver. When using combined antiviral drugs to treat hepatitis B, C should refer to the relevant information of these preparations.

Patients with a history of liver dysfunction including chronic hepatitis have abnormalities in increased liver function during the treatment process with a combination of Retrovirus anti -Retrovirus medications and need to monitor standard treatment guidelines. If signs of liver disease become more serious, it is necessary to consider suspending or stopping the drug.

kidney failure

Due to the negligible clearance of the kidneys in Lopinavir and Ritonavir, the serum concentration in patients with renal impairment. Because Lopinavir and Ritonavir are strongly attached to proteins, it is less likely, the drug is significantly removed by blood viagers or peritoneal fertilizer.

Difficult hematoma

There have been reports on the increase in bleeding, including the hematoma under the skin spontaneously hematoma in patients with difficulty blood disease A and tube B using protease inhibitors. Some patients have been supplemented with factor VIII. Therefore, patients with difficulty in blood can be cautious with the ability to increase bleeding.

Increase lipid

Treatment with aluvia may significantly increase the level of total cholesterol and triglycerides. It is necessary to check the concentration of triglycerides and cholesterol before starting to use aluvia and periodically checking during treatment. Precautions need to be careful when taking medication for patients with high testing values at the beginning of treatment and a history of blood lipid disorders.

pancreatitis

Pancreatic inflammation has been received in patients treated with aluvia including patients with hyperliglycerides.

Hyperglycemia

Patients with newly started diabetes, hyperglycemia or severe diabetes that have been recorded in patients using protease inhibitors.

Fat redistribution and metabolic disorders

Treatment of combination of antiviral drugs is associated with body fat redistribution (fat disorder) in HIV patients. The long -term consequences of this situation are still unclear. The mechanism has not been fully known.

The immune system reconstruction syndrome

Patients with HIV infected with severe immunodeficiency at the beginning of a combination of antiviral drugs (Cart) may be increased with inflammatory reactions to asymptomatic opportunistic infection agents or left opportunity infections and cause serious clinical condition or worsen symptoms.

Bone necrosis

extends the PR range. Lopinavir/ritonavir is recorded, which lasts a medium PR range without symptoms in healthy volunteers.

Interaction with other drugs

Other notes: Aluvia is not a medicine to treat HIV virus infection or AIDS. Therefore, there is still a risk of HIV infection to others through sex or blood route when using aluvia. Therefore, it is advisable to have appropriate careful measures. Patients who use Aluvia still have an infection or other HIV and AIDS diseases.

The ability to drive and operate machinery

There has been no research on the effect of driving and operating machinery. Patients should be notified of unwanted effects of nausea have been reported when using Aluvia.

Pregnancy

in principle, when deciding to use antacidic drugs to treat HIV infection in pregnant women and to limit the risk of HIV infection directly to infants, data on use on animal as well as clinical experience in pregnant women need to be put in to describe safety for fetal safety.

There is currently no full -controlled research that is designed and reasonably in the use of Aluvia drugs in pregnant women. Following the post -maketing via registration data using antiviral drugs in pregnant women was established in January 1989, there is no report on increased risk of birth defects in more than 600 women using Aluvia in the first three months of pregnancy.

The rate of birth defects after using Lopinavir at any stage of pregnancy is equal to the rate of bruising defects observed in the general population. There is no case of birth defects suggesting the cause of the drug. Animal research shows that there is toxicity on reproduction. Based on the limited data described above, the risk of malformations uncertainty occurs in humans.

Breastfeeding period

Rat research shows that Lopinavir is excreted in milk. It is not clear whether the drug is excreted through breast milk or not. In principle, an HIV -infected mother should be recommended not to breastfeed in any way to avoid HIV transmission. Influence on fertility.

Animal research shows that the drug does not affect fertility. There is currently no data on the influence of Lopinavir/Ritonavir on human fertility.

Medicinal interaction

Aluvia contains Lopinavir and Ritonavir, which both inhibit CYP3A of the enzyme system metabolizing CYP450 on in vitro.

Concomitant use of Aluvia with major metabolic drugs through CYP3A may increase the concentration of these drugs in plasma, leading to increased treatment and reaction effects. Aluvia does not inhibit CYP2D6, CYP2C9, CYP2C19, CYP2E1, CYP2B6 or CYP1A at clinically recorded concentrations.

In Vivo research shows that Aluvia touches its own metabolism and increases the biological metabolism of some metabolism through the cytochrom P450 enzyme (including CYP2C9 and CYP2C19) and through the reaction with glucuronic acid. This reduces plasma concentrations and reduces the effectiveness of medications used simultaneously.

Storage

The aluvia film tablet covers at a temperature not exceeding 30 ° C.

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