XYOSTED (AUTOINJECTOR)
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XYOSTED (AUTOINJECTOR) (XYOSTED (AUTOINJECTOR)).
XYOSTED is a progestin-only contraceptive that suppresses gonadotropins, inhibiting ovulation and altering cervical mucus and endometrial receptivity.
| Metabolism | Hepatic via CYP3A4 |
| Excretion | Renal: ~90% as unchanged drug; fecal: <10%. |
| Half-life | Terminal elimination half-life is approximately 2.5–3.6 hours. In patients with renal impairment, half-life may be prolonged; in end-stage renal disease, half-life can exceed 5 hours. |
| Protein binding | ~37% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | Approximately 0.6 L/kg (range 0.4–0.9 L/kg), indicating distribution into total body water. |
| Bioavailability | Subcutaneous: ~100% (complete absorption via autoinjector). |
| Onset of Action | Subcutaneous: Detectable serum concentrations within minutes; peak effect on blood pressure typically occurs within 1–2 hours. |
| Duration of Action | Blood pressure reduction persists for 8–12 hours following a single subcutaneous dose, supporting twice-daily dosing. |
0.5 mL of 40 mg/mL solution (20 mg) subcutaneously once daily; self-administered via autoinjector.
| Dosage form | SOLUTION |
| Renal impairment | No dosage adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (CrCl <30 mL/min) or ESRD; use with caution. |
| Liver impairment | Not studied in hepatic impairment. Use with caution in severe hepatic impairment (Child-Pugh C) due to potential for increased exposure. |
| Pediatric use | Safety and efficacy not established in pediatric patients (<18 years). |
| Geriatric use | No specific dosage adjustment; limited data in patients ≥65 years. No overall differences in safety observed, but greater sensitivity cannot be ruled out. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XYOSTED (AUTOINJECTOR) (XYOSTED (AUTOINJECTOR)).
| Breastfeeding | No human data on excretion in breast milk; based on molecular size (succinylated gelatin and small peptides), potential for transfer is low but unknown. Use during breastfeeding is not recommended; consider alternative therapies. |
| Teratogenic Risk | Pregnancy Category X. Risk of fetal harm in all trimesters due to androgenic effects; can cause virilization of female fetus (clitoral enlargement, labial fusion) and potential developmental toxicity. Contraindicated in pregnancy. |
■ FDA Black Box Warning
There is an increased risk of thromboembolic disorders in women who use progestin-only contraceptives, especially in those with predisposing conditions.
| Serious Effects |
Known or suspected pregnancy, current or past thromboembolic disorders, known or suspected breast cancer, hypersensitivity to hydroxyprogesterone caproate.
| Precautions | Increased risk of thromboembolic disorders, ectopic pregnancy, bone mineral density loss, and hepatic enzyme abnormalities. |
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| Fetal Monitoring |
| Monitor maternal blood pressure, electrolytes, and signs of fluid overload; fetal assessment via ultrasound for growth and anatomy if accidental exposure occurs. |
| Fertility Effects | May impair spermatogenesis in males due to anti-androgenic effects; no specific data on female fertility, but hormonal disruption possible. Reversible upon discontinuation. |