Drug profile of Lopimune
Lopimune tablets are used as anti-retroviral agent by containing Lopinavir & ritonavir as an active substances.
Both the component present in Lopimune tablets are classified pharmacologically as protease inhibitors.
Lopimune tablets are not used as curing the disease, but it can manage the progression and prevent the spreadness and developing severe stage known as AIDS.
Lopimune is a prescription medicine which is used in adults and pediatric with 14 days of age or older by only under the supervision of physician.
Lopimune is a fixed dose combinational therapy; it is also used with other anti-retroviral medications.
Brand name: Lopimune
Active components: Lopinavir & ritonavir
Strength: 200mg & 50mg respectively
Pack: 60 tablets in a container
Classified as: Anti-retroviral drugs
Prescribing information of Lopimune
Lopimune is mainly indicated for treating HIV-1 infection by combining with other anti-retroviral medications.
The most important point take into consideration like;
The use of other active drugs with Lopimune is related with a better possibility of therapy counters.
Before starting the treatment, genotypic or phenotypic testing should be guided which is helpful for using the Lopimune tablets.
The Lopinavir resistance related substitutions will disturb the virological response to Lopimune.
Mechanism of Lopimune
Lopimune containing protease inhibitor activity component, exhibits an anti-retroviral activity.
Both Lopinavir & ritonavir are undergoes action by inhibiting the protease enzymes which is effective for separation of gag-pol polyproteins which is essential for viral assembly production.
This process is prevent by interfering with protease enzyme activity and finally concludes as termination of production of virus.
The formation of immature non infectious virus occurs.
The peak plasma concentration of Lopinavir occurs after oral administration reaches at 4 hours approximately.
No alteration of pharmacokinetic effect occurs while taking Lopimune with or without food.
Lopinavir & ritonavir are highly bound to human plasma protein with the range of 98 to 99%.
Lopinavir is metabolized hepatically, by using CYP3A isoenzymes.
Ritonavir is present as an unchanged form, in circulation.
The major metabolite of ritonavir is Isopropylthiazole oxidation metabolite which is present as low level attaining anti-retroviral activity.
CYP3A & CYP2D6 isoenzymes are major cytochrome enzyme resposile for metabolism of ritonavir.
The terminal half life period of Lopinavir is occur over 12 hours after dosing with range of 5 to 6 hours
The terminal half life period of ritonavir is 3 to 5 hours.
The unchanged form of Lopinavir is encountered with the ranfge of 2.2% & 19.8% through urine & feces.
The metabolite of ritonavir should be eliminated through feces & urine.
When to take the Lopimune
Lopimune tablets should be administered with food or without food.
Lopimune tablets should not be chewed, crushed or broke.
Dosage regimens of Lopimune
In adults, the prescribed dose of Lopimune is 400mg/100mg that is 2 tablets of Lopimune should be administered orally as two times a day.
Patient with lesser three Lopinavir resistance related substitutions, the prescribed dose of Lopimune tablets is 800mg/200mg 4 Lopimune tablets should be administered orally as single dose.
This 800mg/200mg dose should not be recommended for the patients with 3 or greater Lopinavir resistance related substitutions.
Lopimune should not be used as single dose for combined with carbamazepine, Phenobarbital or phenytoin
Lopimune should not be used as single dose therapy by combining with efavirenz, nevirapine, or Nelfinavir.
During the combination of these drugs, the dose of Lopimune should be 500mg/125mg( 2 tablets of 200mg/50mg Lopimune & one tablet of 100mg/25mg Lopimune) as twice a day
Lopimune tablets as single dose therapy should not be recommended in pediatric patients with the age of <18 years.
Depending up on the body weight or body surface area of pediatric patients, the dose should be calculated to avoid the problems like under dosing or over dosing.
6 months to 18 years:
Without combining with efavirenz, nevirapine or Nelfinavir:
15 to 25kg or ≥ 0.6 to <0.9 m2: The prescribed dose of Lopimune is 2 tablets of 100mg/25mg Lopimune tablets should be administered as two times a day
>25 to 35kg or ≥0.9 to <14 m2: The prescribed dose of Lopimune is 3 tablets of 100mg/25mg Lopimune tablets should be used as two times a day
>35kg or ≥ 1.4 m2: The prescribed dose is 4 tablets of 100mg/25mg of Lopimune tablets or 2 tablets of 200mg/50mg Lopimune tablets should be suggested as two times a day.
By combining with efavirenz, nevirapine or Nelfinavir:
15 to 20kg or ≥0.6 to <0.8m2: 2 tablets of 100mg/25mg Lopimune should be administered as two times a day.
>20 to 30kg or ≥0.8 to <1.2 m2: The prescribed dose is 3 tablets 100mg/25mg of Lopimune should be administered as two times a day.
>30 to 45kg or ≥1.2 to <1.7 m2: The prescribed dose is 4 tablets 100mg/25mg of Lopimune should be administered as two times a day.
>45kg or ≥1.7 m2: The prescribed dose is 5 tablets 100mg/25mg of Lopimune should be administered as two times a day.
Lopimune caused side effects
The major adverse effects;
PR interval extension, QT interval extension
The most common side effects;
Loss of weight
Loss of libido
Increased glucose levels
Increased uric acid level
Increased AST, ALT
Elevation of cholesterol
Elevation of amylase, lipase
Depletion of creatinine clearance
Increased sodium levels
Increased total bilirubin
Increased AST, ALT
Decreased platelets count
Toxic epidermal necrolysis, Stevens Johnson’s syndrome
Drug- drug interaction
Lopimune is an inhibitor of CYP3A, may elevates the plasma concentration of agents that ate formerly metabolized by CYP3A.
Lopimune is a CYP3A substrate, when Lopimune is co administered with CYP3A inducers causes depletion of Lopinavir plasma concentration and leads to loss of effectiveness.
Lopimune combined with NNRTI like efavirenz or nevirapine causes decreasing the effect of concentration of Lopinavir.
Lopimune with delaveridine causes elevation of effect of concentration of Lopinavir.
Lopimune combined with tenofovir, causes increasing effect of concentration of tenofovir.
Lopimune combined with abacavir, leads to decreasing the effect of concentration of abacavir.
Lopimune with other protease inhibitors causes increasing the effect of concentration of these drugs.
Lopimune combined with anti-cancer, anti-arrhythmia drugs causes increasing concentration of these drugs.
Lopimune tablets are combined with anti-convulsants, or anti-depressents causes decreasing the effect of concentration of these drugs.
Lopimune with anti-gout or anti-mycobacterials causes increasing effect of concentration of these drugs.
Lopimune with calcium channel blocker leads to cause elevating the effect of concentration of these drugs.
Lopimune with dexamethasone decreases the concentration of Lopinavir.
Lopimune tablets are combined with lipid lowering drugs or Immuno suppressants leads to cause increasing concentration of these drugs.
Food drug interaction
Moderate food drug interaction is occurs
Intake of food, leads to affect the bioavailability of ritonavir
Food will increase the bioavailability of Lopinavir.
Ritonavir should be administered with meals for elevates the gastrointestinal tolerability.
Lopinavir should be taken by without regard to meals.
Lopimune tablets are produces hypersensitive reactions, due to patient may contraindicated to the components present in Lopimune tablets.
Drugs that are largely vulnerable on CYP3A for clearance & for which increased plasma concentration are related with severe life threatening conditions during concurrent use of Lopimune is contraindicated.
Lopimune is contraindicated by using with strong CYP3A inducers, causes decreasing Lopinavir plasma concentration.
Some drugs are contraindicated;
St John ’s wort
Drug interaction-CYP3A enzyme prohibition, causes increased plasma concentration of concurrent used drugs. Avoid the concomitant use.
Toxicity occurs to neonates, potential risk may occur while using Lopimune in neonates.
Take alcohol & propylene glycol from all the drugs should be given to infants for reducing thwe toxicity associated to the components.
Elevation of triglyceride levels may leads to cause pancreatitis.
Pancreatitis is the major risk factor during the Lopimune treatment.
Lipase and amylase value should be monitored periodically.
Due to elevation of AST, ALT & bilirubin, leads to cause liver injury this may concluds as liver damage or failure.
Monitor liver function test periodically during or after completion of treatment.
Diabetes mellitus: Patients blood glucose level should be maintained by checking the levels frequently.
QT prolongation: Stop the therapy.
Immune reconstitution syndrome: Discontinue the Lopimune treatment
Fat redistribution: Reaccumulation of fat occur which may results as obesity.
In severe condition, discontinue the therapy.
Elevation of lipids:
During the therapy with Lopimune may leads to elevate the lipid levels.
In severe condition, therapy should be discontinue or interrupt.
During therapy with protease inhibitor causes hemophilia, in this condition the therapy should be stopped or postponed.
Pregnancy and lactation
Pregnancy category: C
Lopimune should not be used in both pregnancy and lactating period.
Storage and handling
Lopimune container should be stored at temperature between 20oC to 25oC.
Container should be protecting from heat, moisture & light.
Missed dose of Lopimune should be avoided.
In case of missed dose, patient should be following the instructions provided by medical adviser.
Regular dosing schedule should be maintained.
In case of over dosage, patients must be;
Provided with supportive measures
Activated charcoal should be used for adsorbing the unabsorbed dose of Lopimune
Lopinavir is largely bound with human plasma protein, so it its difficult to remove by hemodialysis.