Drug profile
Sofovir Daclahep tablets are anti-viral medication, Sofovir Daclahep containing two most predominant ingredients such as Sofosbuvir and Daclatasvir
Sofovir Daclahep tablets are single dose Sofovir Daclahep therapy, it is a prescription medicine used by the patients only under the knowledge of medical practitioner who are well practiced
Daclahep tablet is not used alone, for better action it should be combined with Sofovir tablet.
In some condition Sofovir Daclahep is combined with ribavirin, an anti-viral medicine used in decompensated (Child Pugh B or C) cirrhosis
Brand name: Sofovir Daclahep
Active components: Sofovir-Sofosbuvir, Daclahep-Daclatasvir
Strength of the components: 400mg & 60mg respectively
Mfg: Hetero healthcare
Package: 28 tablets in a container
Category: Anti-viral drug
Prescribing information for Sofovir Daclahep
The main indication of Sofovir Daclahep is;
This combination tablets are used to treat the chronic hepatitis C viral infection caused by genotype I or III
The major limitation occurred while using Sofovir Daclahep tablets are reduction of constant virological response rate in hepatitis C genotype I or III infected patients.
Mechanism of Sofovir Daclahep
The activity of Sofovir Daclahep tablets are occurred by involving in some mechanism;
Sofovir:
Sofovir containing sofosbuvir has anti-hepaciviral activity, which is directly acting drug exhibits its action by prohibiting NS5B RNA reliant RNA polymerase enzyme; essential for hepatitis viral multiplication.
Sofosbuvir is metabolized to form uridine triphosphate, an essential active metabolite which exposes an anti-viral activity.
The infusion of this active metabolite into hepatitis viral RNA with the help of NS5B polymerase and causes viral chain discontinuation
Daclahep:
Daclahep containing Daclatasvir expels anti-viral activity by prohibiting NS5A protein which is needful in viral production and virion accumulation
Absorption
The peak plasma concentration of Daclahep tablets occurs within the range of 2 hours
The absolute bioavailability of Daclahep is 67%
The peak plasma concentration of Sofovir tablets occurs within the range of 0.5 to 2 hours approximately.
The food will not creates any variation in absorption of Sofovir Daclahep tablets, may be taken with or without food
Distribution
The volume of distribution in Daclahep tablet is 47L
The human plasma protein bound with Daclahep tablet is nearly 99%
The blood to plasma ratio of Sofovir is relatively 0.7
The human plasma protein bound with Sofovir occurs nearly 61 to 65%
Metabolism
Sofovir is metabolized hepatically and formed as pharmacologically active metabolite uridine triphosphate, metabolism undergone with the help of cathepsin A or carboxylesterase 1
Daclahep metabolism occurred with the help of CYP3A4
Elimination
88% of Daclatasvir is excreted through feces 53% as an unchanged form, 6.6% excreted through urine.
The terminal half life period of Daclatasvir is occurred at 12 to 15 hours
Sofosbuvir metabolites are excreted through 80% in urine, 14% in feces & 2.5% in exhaled air
The terminal half life period of sofosbuvir is nearly 0.51 hours
How to take the Tablet Sofovir Daclahep
Sofovir Daclahep tablets are administered with or without food, in the condition of hepatitis C viral infection originated by genotype I or III
Sofovir Daclahep is single dose regimen
Dosage regimens
Generally Daclatasvir is not used alone, it is combined with sofosbuvir
The recommended dosage of Sofovir Daclahep is one tablet should be taken as a single dose
If sofosbuvir is discontinued, Daclatasvir also get stopped
Genotype I:
Patient suffered without cirrhosis or with compensated cirrhosis:
The recommended dosage of Sofovir Daclahep is one tablet should be taken as a single dose with or without food
In decompensated cirrhosis patients:
Sofovir Daclahep should be combined with ribavirin as a single dose
Genotype III:
Patient suffered without cirrhosis or with compensated cirrhosis:
The recommended dosage of Sofovir Daclahep is one tablet should be taken as a single dose with or without food
In decompensated cirrhosis patients:
Sofovir Daclahep should be combined with ribavirin as a single dose
The dosage of ribavirin;
On basis of body weight & hemoglobin level of patients, dose can be calculated.
Less than 75kg: 1000mg of ribavirin; in genotype I or III 600mg of ribavirin as an initial dose and followed as 1000mg/per
At least 75 kg: in decompensated cirrhosis 1200mg of ribavirin given as twice daily
The safety and efficacy of Daclahep has not been established <18 years
Sofovir used in ≥12 years or weight of ≥35kg
Dosage adjustment in drug interaction;
If concurrent use with strong CYP3A inhibitors, the dosage of Daclahep is reduced to 30mg while co administration
Concurrent use with moderate CYP3A inducers, the dosage of Daclahep increased to 90mg
Concomitant use of Daclahep with CYP3A strong inducers should be avoided, it is contraindicated
Sofovir Daclahep caused side effects
The most common side effects occurred during the therapy;
Headache
Fatigue
Nausea
Diarrhea
Elevation of lipase
Cardiac problems like symptomatic bradycardia
Insomnia
Pruritus
Asthenia
Rashes
Loss of appetite
Irritability
Neutropenia
Anemia
Chills
Influenza like symptoms
Pyrexia
Myalgia
Pancytopenia
Drug interaction
While combining Sofovir Daclahep with strong CYP3A inducers causes loss of virological reaction rate of both products
Sofovir Daclahep tablets concomitant with amiodarone causes serious symptomatic bradycardia
Sofovir Daclahep tablets concomitant with anti-convulsants, anti-mycobacterials or herbal products like st Johns wort causes decrease in effect of concentration of Sofovir Daclahep
Sofovir Daclahep with HMG CoA reductase inhibitors, this combination leads to cause increasing the exposure of these drugs (statins)
CYP3A strong inducers like st Johns wort, rifampin, phenytoin or carbamazepine
If Sofovir combines with P-gp or BCRP inhibitors leads to cause elevation of sofosbuvir plasma concentration
Food drug interaction
No food drug interaction occurs
While using Sofovir Daclahep tablets, caution should be taken
Diet should be discussed with consultant
Sofovir Daclahep with herbal product like st. Johns wort causes decreasing the therapeutic effect of Sofovir Daclahep
Possible contraindications
Some anaphylactic reaction occurs if patients are contraindicated to the components present in Sofovir Daclahep
Some contraindications occurs while using Sofovir Daclahep tablets
In decompensated cirrhosis, combines with ribavirin contraindicated in pregnancy condition
Safety measures
Using Sofovir Daclahep with ribavirin, should not be recommended in pregnancy condition because of producing fetal damage due to ribavirin
While taking Sofovir Daclahep tablets, with CYP3A strong inducers causes loss of therapeutic response of Sofovir Daclahep tablets. Avoid this concomitant to reduce the adverse effects
Sofovir Daclahep causes serious bradycardia while concurrent use with amiodarone, to prevent this condition some alternative medicine is given or discontinue the amiodarone if possible. Counsel the patients about the exposure of bradycardia during the treatment.
Pregnancy and lactation
Sofovir Daclahep use in pregnancy, safe to use. The pregnancy category is B1
While combining with ribavirin, not recommended for pregnancy
Pregnancy category: X, causes fetal death
Breast feeding should not be recommended
Storage and handling
The storage condition of Sofovir Daclahep should be stored at room temperature below 30oC (86oF) & 20oC and 25oC (68oF and 77oF) respectively
Missed dose
Both Sofovir Daclahep tablets are single dose Sofovir Daclahep therapy, if patient fails to take the dose of these tablets, must consult the physician and take the dose within the time as per the instruction given by medical practitioner
Over dosage
The over dosage of Sofovir Daclahep tablets are occurred due to missed dose , if once over dosage occurs the patients must be Sofovir Daclahep monitored frequently for endorsement of toxicity and provide safety measures
Hemodialysis is a procedure used to eliminate the component from body, sofosbuvir removes with separation coefficient of 54% whereas Daclatasvir is problematic because nearly 99% of drug bounded to human plasma protein
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