Protease Inhibitors

5 Drugs classified under this drug class

Protease Inhibitors. Lopinavir 100 mg, 200 mg, 80 mg/ml, Ritonavir 25 mg, 50 mg, 20 mg/ml.
F.C. TABS: 120 x 200 / 50 mg; 60 x 100 / 25 mg.
ORAL SOL.: 60 ml x 80 / 20 mg/ml.
Adult: 400 mg/100 mg (2 tabs of 200/50) 2 x dly with/out food; or 5 ml soln. 2 x dly with food.
Child: 6 mths-18 yrs: Calc. acc. to weight: <15 kg: 12/3 mg/kg; >15-40 kg: 10/2.5 mg/kg, both 2 x dly. Calc. acc. to BSA: See lit. Should not exceed recommend. adult dose. Dosage adjustment according to presc. info.
In comb. with other antiretroviral agents for HIV-1 infect.
C/I: Pts. with prev. demonstrat. clinical.  signific. hypersens. (e.g., toxic epiderm. necrolysis, Stevens-Johnson syndr., erythema multiforme, urticaria, angioedema) to any of its ingred., includ. ritonavir. Concom. use with drugs that are highly dependent on CYP3A for clear. and for which elevated plasma conc. are assoc. with serious and/or life-threat. react. (e.g. alfuzosin, ranolazine, dronedarone, colchicine, lurasidone, pimozide dihydroergotamine, ergotamine, methylergonovine, cisapride, elbasvir/grazoprevir, lovastatin, simvastatin, lomitapide, sildenafil -when used for the tmt. of pulm. arterial hyperten., triazolam, oral. admin. midazolam).
Concom. use with drugs that are potent CYP3A induc. where signific. reduced lopinavir plasma conc. may be assoc. with the potential for loss of virologic response and possible resistance and cross-resist. (e.g. Rifampin, St. John's Wort -hypericum perfor.) See lit.

Protease Inhibitors. Glecaprevir 100 mg, Pibrentasvir 40 mg.
F.C. TABS.:84.  The recomm. dose is 300 mg/120 mg (3tabs.) ×1/d, with food. The recom.  tmt. durat. for HCV genotype 1, 2, 3, 4, 5, or 6 infec. pts. with compens. liver dis. (with/ without cirrhos.): Recomm.  tmt. durat. for pts. without prior HCV therap: All HCV genotyp. with NO cirrhos. – 8 wks., pts. with all  HCV genotyp. WITH  cirrhos. -12 wks. Recomm. tmt. durat. for pts. who failed prior ther.with peg-IFN + ribavirin +/- sofosbuvir, or sofosbuvir + ribavirin:  Genotype 1, 2, 4-6 – with NO cirrhos. -8 wks., pts. WITH  cirrhos.- 12 wks. Genotype GT 3- with/without cirrhos.-16 wks. See lit.
Tmt. of chron. hepat.C virus (HCV) infect. in adults.
C/I: Hypersens. Pts.  with sev. hep. impair. (Child-Pugh C). Concom. use with atazanavir contain. product., atorvastatin, simvastatin, dabigatran etexilate, ethinyl oestradiol-contain. product. , strong P-gp and CYP3A induc.(e.g., rifampicin, carbamazepine, St. John’s wort (Hypericum perforatum), phenobarbital, phenytoin, and primidone). Special precautions, Drug interactions, Side effects: See prescribing information for full details.

Protease Inhibitors. Ritonavir 100 mg.
F.C. TABS: 30, 60 x 100 mg.
Monother., adults: 600 mg 2 x dly
with food. Child. over 2 yrs: 350
mg/m² x dly, max 600 mg 2 x dly. Combined with other PIs as
pharmacokinet. enhanc. See lit.
Alone/in comb. with other antiretroviral agents for tmt. HIV infect.
C/I: Hypesens., pts. with decompens.
liver dis. Meds. that metabol. by CYP3A,CYP2D6. See lit.

Antivirals, Protease Inhibitors. nirmatrelvir 150 mg, Ritonavir 100 mg.
20 X FC pink tabs contain.150 mg of nirmatrelvir.
10 XFC white to off white tabs contain.100 mg of ritonavir.
Recomm. dosage is 300 mg nirmatrelvir (two 150 mg tablets) with 100 mg ritonavir (one 100 mg tablet) all taken together orally every 12 hours for 5 days. This drug should be admin. as soon as possible after a diagnosis of COVID-19 has been made and within 5 days of symptom onset.
Tmt. of confirmed coronavirus dis. 2019 (COVID-19) in adults
who do not require suppl. oxygen and who are at incr. risk for progressing to sev. COVID-19
C/I:  Hypersens.
Medic. prod. listed below are a guide and not considered a comprehensive list of all possible medic. prod. that are contraind. with this drug.
Medic. prod. that are highly dependent on CYP3A for clearance and for which elevated plasma concentr. are associated with serious and/or life-threatening reactions.
 Alpha1-adrenoreceptor antagonist: alfuzosin
 Antianginal: ranolazine
 Antiarrhythmic: dronedarone, propafenone, quinidine
 Anticancer drugs: neratinib, venetoclax
 Anti-gout: colchicine
 Antihistamines: terfenadine
 Antipsychotics/neuroleptics: lurasidone, pimozide, quetiapine
 Benign prostatic hyperplasia medicinal products: silodosin
 Cardiovascular medicinal products: eplerenone, ivabradine
 Ergot derivatives: dihydroergotamine, ergonovine, ergotamine, methylergonovine
 GI motility agents: cisapride
 Immunosuppressants: voclosporin
 Lipid-modifying agents:
o HMG Co-A reductase inhibitors: lovastatin, simvastatin
o Microsomal triglyceride transfer protein (MTTP) inhibitor: lomitapide
 Migraine medicinal products: eletriptan
 Mineralocorticoid receptor antagonists: finerenone
 Neuropsychiatric agents: cariprazine
 Opioid antagonists: naloxegol
 PDE5 inhibitor: avanafil, sildenafil, tadalafil, vardenafil
 Sedative/hypnotics: clorazepate, diazepam, estazolam, flurazepam, oral midazolam and triazolam
 Vasopressin receptor antagonists: tolvaptan
Medic. prod. that are potent CYP3A inducers where significant. reduced nirmatrelvir/ritonavir plasma concentr. may be associated with the potential for loss of virologic response and possible resistance.
 Antibiotics: rifampicin, rifapentine
 Anticancer drugs: apalutamide, enzalutamide
 Anticonvulsants: carbamazepine, phenobarbital, phenytoin, primidone
 Cystic fibrosis transmembrane conductance regulator potentiators: lumacaftor/ivacaftor
 Herbal products: St. John's wort (Hypericum perforatum)
This drug cannot be started immediately after discontinuation of CYP3A4 inducers due to the delayed offset of the recently discontinued CYP3A4 inducer.

Protease Inhibitors. Darunavir 75, 150, 400, 600, 800 mg.
TABS: 480 x 75 mg ; 240 x 150 mg.
Tmt. HIV-1 infect. co-admin. with ritonavir
and with other antiretroviral agents in
adult pts and in tmt-experienc. pediatric
pts 6 yrs of age and older. See lit.
TABS: 60 x 400 mg, 60 x 600 mg, 30 x 800
mg.
Tmt. HIV-1 infect. in adult pts co-admin.
with ritonavir and with other antiretroviral
agents. See lit.
Tmt-naïve adults: 800 mg with 100 mg
ritonavir 1 x dly, with food. See lit.
Tmt-experience. adults: (With no
darunavir resist. assoc. subst.) 800 mg
with 100 mg ritonavir 1 x dly, with
food. See lit.
Tmt-experience. adults: (With at least 1
darunavir resist. assoc. substit.)
600 mg with 100 mg ritonavir 2 x dly,
with food. See lit.
C/I: Hypersens.; severe (Child-Pugh Class
C) hepatic impair.; Co-admin. with
ritonavir is C/I with drugs that are highly
dependent on CYP3A and drugs with
narrow therap. index.
Refer to ritonavir C/I. See lit.