Axlovir Tablet
Nirmatrelvir + Ritonavir
150mg + 100mg
Square Pharmaceuticals Ltd.
| Pack size | 3's Combipack |
|---|---|
| Unite Price | 1600.00 BDT |
Indications
Axlovir Tablet is used for:
Treatment of mild-to-moderate coronavirus disease (COVID-19) (EUA)
Adult Dose
Oral
Emergency use authorization issued for treatment of mild-to-moderate coronavirus disease 2019 (COVID-19) in adults and pediatric patients (aged >12 years and weight >40 kg) testing positive for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus, and who are at high risk for progression to severe COVID-19, including hospitalization or death
300 mg nirmatrelvir plus 100 mg ritonavir PO BID for 5 days
Initiate as soon as possible after COVID-19 diagnosis and within 5 days of symptom onset.
Hepatic impairment
Mild or moderate (Child-Pugh Class A or B): No dosage adjustment required
Severe (Child-Pugh Class C): Not recommended; data are unavailable
Child Dose
Oral
Emergency use authorization issued for treatment of mild-to-moderate coronavirus disease 2019 (COVID-19) in pediatric patients (aged >12 years and weight >40 kg) testing positive for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus, and who are at high risk for progression to severe COVID-19, including hospitalization or death
300 mg nirmatrelvir plus 100 mg ritonavir PO BID for 5 days
Initiate as soon as possible after COVID-19 diagnosis and within 5 days of symptom onset
Renal Dose
Renal impairment
Mild (eGFR >60 to <90 mL/min): No dosage adjustment required
Moderate (eGFR >30 to <60 mL/min): Decrease to 150 mg nirmatrelvir plus 100 mg ritonavir BID x 5 days
Severe (eGFR <30 mL/min): Not recommended; data are unavailable
Administration
May take with or without food
Contra Indications
Nirmatrelvir + Ritonavir are contraindicated in patients with a history of clinically significant hypersensitivity reactions to its active ingredients (nirmatrelvir or ritonavir) or any other components of the product.
It is contraindicated with drugs that are highly dependent on CYP3A for clearance and for which elevated concentrations are associated with serious and/or life-threatening reactions:
Drug highly dependent on CYP3A for clearance
Alpha1-adrenoreceptor antagonist: Alfuzosin
Analgesics: Pethidine, piroxicam, propoxyphene
Antianginal: Ranolazine
Antiarrhythmic: Amiodarone, dronedarone, flecainide, propafenone, quinidine
Antigout: Colchicine
Antipsychotics: Lurasidone, pimozide, clozapine
Ergot derivatives: Dihydroergotamine, ergotamine, methylergonovine
HMG-CoA reductase inhibitors: Lovastatin, simvastatin
PDE5 inhibitor: Sildenafil (Revatio) when used for pulmonary arterial hypertension (PAH)
Sedative/hypnotics: Triazolam, oral midazolam
Drugs that are potent CYP3A inducers
Anticancer drugs: Apalutamide
Anticonvulsant: Carbamazepine, phenobarbital, phenytoin
Antimycobacterials: Rifampin
Herbal products: St. John’s Wort (hypericum perforatum)
Precautions
Hepatic transaminase elevations, clinical hepatitis, and jaundice reported with ritonavir; caution when administering to patients with preexisting liver diseases, liver enzyme abnormalities, or hepatitis.
Because nirmatrelvir is coadministered with ritonavir, possible risk of developing resistance to HIV protease inhibitors in individuals with uncontrolled or undiagnosed HIV-1 infection.
Pregnancy-Lactation
Nirmatrelvir
No human data are available on use of nirmatrelvir during pregnancy to evaluate for drug-associated risks of major birth defects, miscarriage, or adverse maternal or fetal outcomes
Ritonavir
Observational studies on ritonavir use in pregnant females have not identified an increase in the risk of major birth defects
Studies with ritonavir are insufficient to identify a drug-associated risk of miscarriage
Clinical considerations
There are maternal and fetal risks (eg, preeclampsia, eclampsia, preterm birth, premature rupture of membranes, venous thromboembolic disease, fetal death) associated with untreated COVID-19 in pregnancy
Contraception
Use of ritonavir may reduce efficacy of combined hormonal contraceptives
Advise patients using combined hormonal contraceptives to use an effective alternative contraceptive method or an additional barrier method of contraception
Animal data
Nirmatrelvir: Reduced fetal body weights following oral administration to pregnant rabbits were observed at systemic exposures (AUC) ~10x higher than clinical exposure at the authorized human dose
Ritonavir: No evidence of teratogenicity for rats and rabbits at systemic exposures of ~4x higher than authorized human dose exposure
Lactation
Breastfeeding individuals with COVID-19 should follow practices according to clinical guidelines to avoid exposing the infant to COVID-19
Nirmatrelvir
There are no available data on presence of nirmatrelvir in human or animal milk, effects on breastfed infants, or effects on milk production
Transient decrease in body weight observed in nursing offspring of rats administered nirmatrelvir
Ritonavir
Limited published data reports that ritonavir is present in human milk
There is no information on effects of ritonavir on breastfed infants or its effects on milk production
Interactions
Drug interaction overview
Potential for nirmatrelvir and ritonavir to affect other drugs
Nirmatrelvir and ritonavir is an inhibitor of CYP3A and may increase drugs primarily metabolized by CYP3A.
Coadministration with drugs highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events is contraindicated.
Potential for other drugs to affect nirmatrelvir and ritonavir
Nirmatrelvir and ritonavir are CYP3A substrates; therefore, drugs that induce CYP3A may decrease nirmatrelvir and ritonavir plasma concentrations and reduce therapeutic effect.
The healthcare provider should consult appropriate references for comprehensive information.
Side Effects
Side effects of Nirmatrelvir + Ritonavir :
1-10%
Dysgeusia (6%)
Diarrhea (3%)
Hypertension (1%)
Myalgia (1%)
Mode of Action
Nirmatrelvir is a peptidomimetic inhibitor of SARS-CoV-2 main protease (Mpro), also referred to as 3C-like protease (3CLpro) or nsp5 protease
Inhibition of SARS-CoV-2 Mpro renders it incapable of processing polyprotein precursors, preventing viral replication
Nirmatrelvir is boosted with low-dose ritonavir that slows nirmatrelvir metabolism via inhibition of CYP3A4, and thereby provides higher systemic exposure
Note
Axlovir 150mg + 100mg Tablet generic name is Nirmatrelvir + Ritonavir. Axlovir 150mg + 100mg Tablet is manufactured by Square Pharmaceuticals Ltd.Axlovir is availble in all over Bangladesh.
Mes BD drug index information on Axlovir Tablet is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.