Fezotan Tablet
Fezolinetant
45 MG
Acme Laboratories Ltd.
| Pack size | 10's Pack |
|---|---|
| Dispensing mode | |
| Source | |
| Agent | |
| Retail Price | 95.00 AED |
Indications
Fezotan Tablet is used for:
Menopausal Vasomotor Symptoms
Adult Dose
Adult
Tablet
Menopausal Vasomotor Symptoms
Indicated for the treatment of moderate-to-severe vasomotor symptoms (VMS) caused by menopause
45 mg PO daily
Child Dose
Renal Dose
Renal impairment
Mild or moderate (eGFR 30-89 mL/min/1.73 m2): No dose adjustment required
Severe (eGFR 15-29 mL/min/1.73 m2 or end-stage renal disease [ESRD]): Contraindicated
Administration
May take with or without food
Administer at approximately the same time each day
Swallow tablet whole with liquids; do not cut, crush, or chew
Contra Indications
Known cirrhosis
Severe renal impairment or ESRD
Coadministration with CYP1A2 inhibitors
Precautions
Hepatotoxicity
Elevated transaminases reported in clinical trials; most patients were asymptomatic
Patients with cirrhosis were not studied
Cases of serious drug-induced liver injury (i.e., increased AST/ALT [≤50x ULN], alkaline phosphatase [≤4x ULN], and bilirubin [≤5x ULN] at peak elevation) occurring within 40 days of starting therapy reported in postmarketing surveillance; signs and symptoms resolved after therapy discontinuation
Exclude alternative causes of abnormal LFTs
Monitoring Parameters
Before initiating
Obtain liver function tests (LFTs), including ALT/AST, alkaline phosphatase, and total and direct bilirubin
Do not begin therapy if ALT/AST >2x ULN or TB >2x ULN
During treatment
Monitor LFTs monthly for the first 3 months, at 6 months, and 9 months after starting therapy
Perform more frequent LFT monitoring (until resolution) if ALT/AST >3x ULN develops
Pregnancy-Lactation
Pregnancy
There are no data on use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes
Animal studies
In a pre- and post-natal development animal study, delayed parturition and embryo-lethality occurred at high doses above the human therapeutic dose in rats
Additionally, in male offspring, delayed male reproductive maturation was observed, characterized by incomplete preputial separation, which affected male fertility at doses above the human therapeutic dose in rats
Lactation
Data are not available on presence in human milk, effects on breastfed children, or effects on milk production
Unknown if present in human milk
Animal studies
Following administration of radiolabeled fezolinetant to lactating rats, concentration in milk was higher than that in plasma at all time points
This indicated that fezolinetant-derived components transferred to tissues in infant rats via breast milk
Interactions
CYP1A2 substrate
CYP1A2 inhibitors
Contraindicated
Peak plasma concentration and AUC of fezolinetant are increased if coadministered with drugs that are weak, moderate, or strong CYP1A2 inhibitors
Contraindicated (27)
caffeine
cannabidiol
cimetidine
ciprofloxacin
conjugated estrogens
diazoxide choline
disulfiram
enasidenib
estradiol
estrogens conjugated synthetic
ethinylestradiol
fexinidazole
fluvoxamine
givosiran
interferon alfa 2b
mestranol
methoxsalen
mexiletine
peginterferon alfa 2a
peginterferon alfa 2b
propafenone
propranolol
rucaparib
stiripentol
verapamil
viloxazine
zileuton
Adverse Effects
Side effects of Fezolinetant :
1-10%
Abdominal pain (4.3%)
Diarrhea (3.9%)
Insomnia (3.9%)
Back pain (3%)
Hot flush (2.5%)
AST/ALT >3x ULN (2.3%)
Mechanism of Action
Nonhormonal selective neurokinin 3 (NK3) receptor antagonist
Blocks neurokinin B (NKB) binding on the kisspeptin/neurokinin/dynorphin (KNDy) neuron to modulate neuronal activity in the hypothalamus, and thereby reduces frequency and severity of vasomotor symptoms
Note
Fezotan 45 MG Tablet manufactured by Acme Laboratories Ltd.. Its generic name is Fezolinetant. Fezotan is availble in Bangladesh.
Farmaco BD drug index information on Fezotan Tablet is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.