FOLLISTIM AQ
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FOLLISTIM AQ (FOLLISTIM AQ).
Recombinant human follicle-stimulating hormone (FSH) that binds to FSH receptors on granulosa cells in the ovary, stimulating follicular growth and maturation via activation of adenylyl cyclase and increased cAMP production.
| Metabolism | Metabolized via hepatic and renal pathways; exact enzymes not specified. |
| Excretion | Primarily renal (90%), with intact follitropin alfa/beta and metabolites excreted in urine; biliary/fecal excretion minimal (<10%). |
| Half-life | Terminal elimination half-life approximately 24-36 hours (subcutaneous route); clinical context supports daily dosing due to sustained follicular stimulation. |
| Protein binding | Approximately 60-70% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Approximately 0.5-1.0 L/kg, indicating distribution primarily into extracellular fluid; limited tissue binding. |
| Bioavailability | Subcutaneous injection: approximately 70% (relative to IV); intramuscular injection: approximately 60-70%. |
| Onset of Action | Subcutaneous: follicular recruitment begins within 24-48 hours; peak serum estradiol rise by day 5-7 of treatment. |
| Duration of Action | Subcutaneous: therapeutic effect lasts 24-48 hours after last dose, supporting daily administration for follicular development. |
75 to 300 IU subcutaneously once daily for 8 to 14 days, adjusted based on follicular response; maximum daily dose 450 IU and total duration not exceeding 14 days per cycle.
| Dosage form | INJECTABLE |
| Renal impairment | No formal guidelines; use with caution in moderate to severe renal impairment (eGFR <30 mL/min/1.73 m²) due to limited data; consider lower starting doses based on clinical response. |
| Liver impairment | No formal guidelines; use with caution in Child-Pugh class B or C cirrhosis due to potential altered metabolism; monitor response and consider dose reduction. |
| Pediatric use | Not FDA-approved for pediatric use; limited off-label data for anovulatory disorders: start at 75 IU subcutaneously once daily, adjusted per response, based on body weight (1.5-3 IU/kg/day) with careful monitoring. |
| Geriatric use | Not indicated for geriatric use in fertility; no specific dosing recommendations; consider increased risk of adverse events if used off-label; monitor closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FOLLISTIM AQ (FOLLISTIM AQ).
| Breastfeeding | Excretion into human milk is unknown. Due to the potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during treatment. M/P ratio is not available. |
| Teratogenic Risk | Follistim Aq (follitropin beta) is classified as Pregnancy Category X. It is contraindicated in pregnant women due to the risk of ovarian hyperstimulation syndrome and potential fetal harm. First trimester: No adequate human data, but animal studies show embryotoxicity. Second and third trimesters: Not indicated for use; may cause fetal harm if inadvertently administered during early pregnancy. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to FSH or excipients","Primary ovarian failure","Ovarian cyst or enlargement of unknown origin","Gynecological cancers (ovarian, breast, uterine)","Pregnancy","Uncontrolled thyroid or adrenal dysfunction","Presence of non-gonadal endocrine disorders (e.g., pituitary tumor)"]
| Precautions | ["Ovarian hyperstimulation syndrome (OHSS)","Ovarian torsion","Multiple pregnancies","Pulmonary embolism","Ovarian enlargement","Ectopic pregnancy","Congenital malformations"] |
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| Fetal Monitoring | Monitor for signs of ovarian hyperstimulation syndrome (OHSS), including pelvic pain, distension, nausea, vomiting, and weight gain. Perform serial ultrasounds to assess ovarian size and follicle development. Monitor estradiol levels to reduce risk of OHSS. Fetal monitoring includes ultrasonography for multiple gestation and ectopic pregnancy. |
| Fertility Effects | Follitropin beta stimulates multiple follicular development, used for ovulation induction and controlled ovarian stimulation. It increases the risk of multiple gestation (twins, triplets) and OHSS. No evidence of long-term impairment of fertility, but ovarian hyperstimulation may temporarily affect reproductive function. |