CYKLX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CYKLX (CYKLX).
CYKLX is a selective phosphodiesterase 4 (PDE4) inhibitor, increasing intracellular cyclic adenosine monophosphate (cAMP) levels and reducing pro-inflammatory cytokine production.
| Metabolism | Primarily metabolized by CYP3A4 and CYP2D6 enzymes in the liver. |
| Excretion | Renal: 70% unchanged; biliary/fecal: 30% as metabolites. |
| Half-life | Terminal half-life: 12 hours; requires dose adjustment in renal impairment (CrCl <30 mL/min). |
| Protein binding | 95% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd: 0.8 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 80% (first-pass metabolism minimal). |
| Onset of Action | Oral: 1-2 hours; IV: 5-10 minutes. |
| Duration of Action | Oral: 12-24 hours; IV: 6-12 hours, with sustained effects due to active metabolites. |
100 mg orally once daily with food.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | GFR ≥30 mL/min: no adjustment. GFR <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose to 50 mg daily. Child-Pugh C: not recommended. |
| Pediatric use | Not approved for use in pediatric patients. |
| Geriatric use | No specific dose adjustment required; monitor renal function due to age-related decline. Initial dose 100 mg daily. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CYKLX (CYKLX).
| Breastfeeding | Unknown if CYKLX is excreted in human milk. M/P ratio not determined. Due to potential for serious adverse reactions in nursing infants, breastfeeding should be discontinued during therapy or consider discontinuing the drug. |
| Teratogenic Risk | No adequate studies in pregnant women. In animal studies, CYKLX was not teratogenic at doses up to 10 times the human exposure. Risk cannot be ruled out; use only if potential benefit justifies risk. First trimester: limited data preclude definitive risk assessment. Second and third trimesters: no specific fetal risks identified, but lack of human studies. |
■ FDA Black Box Warning
Increased risk of serious infections including tuberculosis, invasive fungal infections, and bacterial, viral, and other opportunistic infections.
| Serious Effects |
["Pregnancy","Hypersensitivity to apremilast or any excipients"]
| Precautions | ["Monitor for signs of infection, depression, and weight loss","Contraindicated in pregnancy due to teratogenicity"] |
Loading safety data…
| Fetal Monitoring | Monitor maternal renal function, hepatic function, and complete blood count monthly. Fetal ultrasound for growth and anatomy in second trimester if exposure occurs. Consider fetal echocardiography if first trimester exposure. |
| Fertility Effects | In animal studies, CYKLX impaired fertility in male and female rats at clinically relevant doses. Human data lacking; potential for reversible impairment of spermatogenesis and ovulation. Counsel patients of reproductive potential about contraception. |