Select a medication above to begin.
Orladeyo
berotralstat
Adult Dosing .
Dosage forms: CAP: 110 mg, 150 mg
hereditary angioedema prophylaxis, routine
- [150 mg PO qd]
- Info: may decr. dose to 110 mg PO qd if not tolerated; give with food
renal dosing
- [see below]
- CrCl >15: no adjustment; CrCl <15: not defined
- HD/PD: not defined
hepatic dosing
- [adjust dose amount]
- Child-Pugh Class B or C: 110 mg qd
Peds Dosing .
- Dosage forms: CAP: 110 mg, 150 mg; PELLET: 72 mg per pkt, 96 mg per pkt, 108 mg per pkt, 132 mg per pkt
hereditary angioedema prophylaxis, routine
- [2-11 yo, 12-23 kg]
- Dose: 72 mg PO qd; Info: give with food; do not chew/crush pellet
- [2-11 yo, 24-31 kg]
- Dose: 96 mg PO qd; Info: give with food; do not chew/crush pellet
- [2-11 yo, 32-39 kg]
- Dose: 108 mg PO qd; Info: give with food; do not chew/crush pellet
- [2-11 yo, >40 kg]
- Dose: 132 mg PO qd; Info: give with food; do not chew/crush pellet
- [12 yo and older]
- Dose: 150 mg PO qd; Info: may decr. dose to 110 mg PO qd if not tolerated; give with food
renal dosing
- [2-11 yo]
- CrCl 15-30: avoid use; CrCl <15: not defined
- HD/PD: not defined
- [12 yo and older]
- CrCl >15: no adjustment; CrCl <15: not defined
- HD/PD: not defined
hepatic dosing
- [2-11 yo]
- Child-Pugh Class B or C: avoid use
- [12 yo and older]
- Child-Pugh Class B or C: 110 mg qd
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- CrCl <30 (patients 2-11 yo)
- hepatic impairment, Child-Pugh Class B-C (patients 2-11 yo)
- caution: hepatic impairment, Child-Pugh Class B-C (patients 12 yo and older)
- caution: electrolyte abnormalities
- caution: long QT syndrome, congenital
- caution: QT prolongation
- caution: QT prolongation family history
- caution: torsades de pointes history
- caution: ventricular arrhythmia
- caution: bradycardia
- caution: MI, recent
- caution: CHF
Drug Interactions .
Overview
berotralstat
kallikrein inhibitor
- P-gp substrate
- CYP2C9 inhibitor, weak
- CYP2D6 inhibitor, moderate
- CYP3A4 inhibitor, moderate
- P-gp inhibitor, weak
- prolongs QT interval (conditional)
Contraindicated
- cisapride
- colchicine
- eliglustat
- flibanserin
- lomitapide
- pimozide
- thioridazine
Avoid/Use Alternative
- alfentanil
- alprazolam
- amiodarone
- amphetamine
- apalutamide
- aprepitant
- arsenic trioxide
- avapritinib
- bedaquiline
- bosentan
- bosutinib
- brigatinib
- buspirone
- carbamazepine
- cariprazine
- cobimetinib
- codeine
- conivaptan
- crizotinib
- dabigatran
- danshen
- defactinib
- desogestrel (contraceptive)
- dextroamphetamine
- dicloxacillin
- dihydrocodeine
- dihydroergotamine
- disopyramide
- domperidone
- dordaviprone
- doxorubicin
- dronedarone
- efavirenz
- elacestrant
- encorafenib
- ensartinib
- entrectinib
- ephedra
- ergotamine
- etrasimod
- fentanyl
- fexinidazole
- fosaprepitant
- fosfomycin injection
- fosphenytoin
- gepotidacin
- hydrocodone
- hydroxychloroquine
- ivabradine
- ivacaftor
- ivosidenib
- ixabepilone
- lefamulin
- lemborexant
- levoketoconazole
- lisdexamfetamine
- lonafarnib
- lorlatinib
- lovastatin
- lumacaftor/ivacaftor
- lurbinectedin
- macitentan
- meperidine
- methadone
- methylergonovine
- midazolam
- mitapivat
- mobocertinib
- naloxegol
- neratinib
- nirogacestat
- nisoldipine
- olaparib
- oliceridine
- omaveloxolone
- oxycodone
- palovarotene
- pemigatinib
- pexidartinib
- phenobarbital
- phenytoin
- pirfenidone
- pralsetinib
- primidone
- propafenone
- quizartinib
- relugolix
- remibrutinib
- repotrectinib
- rifabutin
- rifampin
- rifapentine
- rilzabrutinib
- rivaroxaban
- selpercatinib
- selumetinib
- simvastatin
- siponimod
- sirolimus albumin-bound
- sonidegib
- sotalol
- St. John's wort
- sufentanil
- taletrectinib
- tazemetostat
- tipranavir
- tolvaptan
- topotecan
- toremifene
- tramadol
- turmeric
- vandetanib
- vardenafil
- venetoclax
- ziprasidone
Monitor/Modify Tx
- abemaciclib
- acalabrutinib
- adagrasib
- afatinib
- aficamten
- alfuzosin
- anagrelide
- apixaban
- apomorphine
- aripiprazole oral
- artemether/lumefantrine
- asenapine
- atorvastatin
- avanafil
- avatrombopag
- axitinib
- azithromycin
- brexpiprazole
- bromocriptine
- budesonide
- butorphanol
- cabozantinib
- capivasertib
- celecoxib
- ceritinib
- chloroquine
- cilostazol
- citalopram
- clarithromycin
- clofazimine
- clonazepam
- clozapine
- copanlisib
- cyclosporine
- daridorexant
- dasatinib
- deflazacort
- degarelix
- desflurane
- desipramine
- deuruxolitinib
- deutetrabenazine
- dexmedetomidine
- dexmedetomidine injection
- diclofenac
- digoxin
- docetaxel
- dofetilide
- donepezil
- droperidol
- edoxaban
- elexacaftor/tezacaftor/ivacaftor
- elinzanetant
- enfortumab vedotin
- epirubicin
- eplerenone
- erdafitinib
- eribulin
- erythromycin
- estazolam
- estradiol (contraceptive)
- eszopiclone
- ethinyl estradiol (contraceptive)
- everolimus
- fedratinib
- felodipine
- finerenone
- flecainide
- fluorouracil
- fluvastatin
- futibatinib
- gepirone
- gilteritinib
- glasdegib
- glimepiride
- goserelin
- guanfacine
- haloperidol
- histrelin
- hydrocortisone
- hydroxyzine
- ibrutinib
- ibutilide
- iloperidone
- imipramine
- inotuzumab ozogamicin
- irinotecan
- isoflurane
- itraconazole
- lapatinib
- leuprolide
- levofloxacin
- lidocaine
- lofexidine
- lumateperone
- lurasidone
- macimorelin
- mavacamten
- mavorixafor
- mefloquine
- metoprolol
- midostaurin
- morphine
- moxifloxacin
- nebivolol
- nifedipine
- nilotinib
- nimodipine
- nortriptyline
- ondansetron
- osimertinib
- pacritinib
- palbociclib
- paliperidone
- palonosetron
- pasireotide
- pazopanib
- pentamidine
- perphenazine
- pimavanserin
- pirtobrutinib
- pitolisant
- ponatinib
- procainamide
- propranolol
- quetiapine
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- quinine
- ranolazine
- red yeast rice
- repaglinide
- revumenib
- ribociclib
- rimegepant
- riociguat
- romidepsin
- rucaparib
- ruxolitinib
- ruxolitinib topical
- saxagliptin
- sebetralstat
- sertraline
- sevoflurane
- sildenafil
- sirolimus
- sparsentan
- sunitinib
- suvorexant
- suzetrigine
- tacrolimus
- tadalafil
- talazoparib
- tamsulosin
- telavancin
- temsirolimus
- tenofovir alafenamide
- tenofovir disoproxil
- tetrabenazine
- tezacaftor/ivacaftor
- tofacitinib
- torsemide
- trabectedin
- trazodone
- triazolam
- triclabendazole
- trifluridine
- triptorelin
- ubrogepant
- vanzacaftor/tezacaftor/deutivacaftor
- vemurafenib
- vinblastine
- vincristine
- vinorelbine
- voclosporin
- warfarin
- yohimbe
- zanubrutinib
- ziftomenib
Caution Advised
- aliskiren
- avacopan
- budesonide rectal
- cyclophosphamide
- darifenacin
- darolutamide
- dexamethasone
- duvelisib
- eletriptan
- erlotinib
- glecaprevir
- grazoprevir
- ifosfamide
- imlunestrant
- isavuconazonium
- istradefylline
- larotrectinib
- maraviroc
- meropenem
- methylprednisolone
- mifepristone
- naldemedine
- ospemifene
- oxcarbazepine
- pibrentasvir
- roflumilast
- roflumilast topical
- seladelpar
- sevabertinib
- silodosin
- sirolimus topical
- tamoxifen
- ticagrelor
- tretinoin
- upadacitinib
- vaborbactam
- verapamil
- vilazodone
- vortioxetine
Adverse Reactions .
Serious Reactions
may occur but none reported
Common Reactions
- abdominal pain
- vomiting
- diarrhea
- headache
- fatigue
- flatulence
- back pain
- GERD
Safety/Monitoring .
Monitoring Parameters
no routine tests recommended
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; inadequate human data available; no known risk of fetal harm based on animal data at 2x and 10x MRHD
Lactation
Clinical Summary
weigh risk/benefit while breastfeeding; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: for berotralstat: liver; CYP450: 2D6, 3A4 substrate
Excretion: for berotralstat: feces 79%, urine 9% (3.4% unchanged); Half-life: 93h
Subclass: Hereditary Angioedema
Mechanism of Action
for berotralstat: binds plasma kallikrein, inhibiting bradykinin generation
Formulary .
No Formulary Selected
Join Now to View Patient Handouts!
Create a FREE epocrates Online account to access patient medication instructions. Your patients and caregivers will appreciate you printing these friendly handouts, available in English and Spanish. Each handout addresses common concerns such as how to take the medication, and possible side effects.
Current Members: Sign In.
Pill Pictures
Join Now to View Pill Pictures!
Create a FREE epocrates Online account to access full-color images of medications within the drug monograph.
Current Members: Sign In.