Drug Interaction:
In vitro studies have shown that crofelemer has the potential to inhibit
cytochrome P450 isoenzyme 3A and transporters MRP2 and OATP1A2 at
concentrations expected in the gut. Due to the minimal absorption of
crofelemer, it is unlikely to inhibit cytochrome P450 isoenzymes
1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1 and CYP3A4
Nelfinavir, Zidovudine, and Lamivudine
FULYZAQ administration did not have a clinically relevant interaction with nelfinavir,
zidovudine, or lamivudine in a drug-drug interaction trial.
Indication:
FULYZAQ (crofelemer) delayed-release tablets, for oral use
Initial U.S. Approval: 2012
Drug Name- Fulyzaq
Active Ingredient - Crofelemer
To treat HIV/AIDS patients whose diarrhea is not an infection from virus,
bacteria, or parasite
Indication-
HIV patients whose diarrhea not caused by infection from a virus,bacteria or
parasite
Approved by FDA on 31-12--2012 (Ref- FDA approved List- 2012)
Adverse Reaction:
Most common adverse reactions (incidence . 3%) are upper respiratory
tract infection, bronchitis, cough, flatulence and increased bilirubin.
Contra-Indications:
CONTRAINDICATIONS
None.
WARNINGS AND PRECAUTIONS
Rule out infectious etiologies of diarrhea before starting crofelemer.
If infectious etiologies are not considered, there is a risk that patients with
infectious etiologies will not receive the appropriate therapy and their
disease may worsen.
Dosages/ Overdosage Etc:
INDICATIONS AND USAGE
FULYZAQ is an anti-diarrheal indicated for the symptomatic relief of
non-infectious diarrhea in adult patients with HIV/AIDS on anti-retroviral therapy
DOSAGE AND ADMINISTRATION
One 125 mg delayed-release tablet taken orally twice a day, with or without food
DOSAGE FORMS AND STRENGTHS
Delayed-Release Tablets: 125 mg
Patient Information:
PATIENT COUNSELING INFORMATION
Instruct patients that FULYZAQ tablets may be taken with or without food.
Instruct patients that FULYZAQ tablets should not be crushed or chewed. Tablets
should be swallowed whole.
The botanical drug substance of FULYZAQ is extracted from Croton lechleri (the botanical raw material) that is harvested from the wild in South America
Pharmacology/ Pharmacokinetics:
CLINICAL PHARMACOLOGY
1. Mechanism of Action
Crofelemer is an inhibitor of both the cyclic adenosine monophosphate
(cAMP)-stimulated cystic fibrosis transmembrane conductance regulator
(CFTR) chloride ion (Cl-) channel, and the
calcium-activated Clchannels (CaCC) at the luminal membrane of enterocytes.
Crofelemer acts by blocking Clsecretion and accompanying high volume water loss
in diarrhea, normalizing the flow of Cland water in the GI tract.
2. Pharmacokinetics
Absorption
The absorption of crofelemer is minimal following oral dosing in healthy adults and
HIV-positive patients and concentrations of crofelemer in plasma are below the level of
quantitation (50 ng/mL). Therefore, standard pharmacokinetic parameters such
as area under the curve, maximum concentration, and half-life cannot be estimated
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
1. Pregnancy
Pregnancy Category C
There are, no adequate, well-controlled studies in pregnant women. Because
animal reproduction studies are not always predictive of human response, this
drug should be used during pregnancy only if clearly needed.
2. Nursing Mothers
It is not known whether crofelemer is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for adverse reactions in nursing infants from FULYZAQ, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
3. Pediatric Use
The safety and effectiveness of FULYZAQ have not been established in pediatric patients less than 18 years of age.
4. Geriatric Use
Clinical studies with crofelemer did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently than younger patients.
Manufacturer Details