ARYNTA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ARYNTA (ARYNTA).
ARYNTA (pembrolizumab) is a humanized monoclonal antibody that binds to the programmed death-1 (PD-1) receptor on T cells, blocking its interaction with PD-L1 and PD-L2, thereby restoring anti-tumor immune responses.
| Metabolism | Pembrolizumab is a monoclonal antibody metabolized via catabolism into small peptides and amino acids; no specific metabolic enzymes or pathways are involved. |
| Excretion | Primarily renal elimination (70-80% unchanged), with 10-15% fecal excretion via biliary secretion. |
| Half-life | Terminal elimination half-life is 2-4 hours in healthy adults, prolonged to 6-12 hours in moderate to severe renal impairment (CrCl <30 mL/min). |
| Protein binding | Approximately 95% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 0.2-0.5 L/kg, indicating limited extravascular distribution. |
| Bioavailability | Oral bioavailability is 40-50% due to first-pass metabolism; intravenous bioavailability is 100%. |
| Onset of Action | Oral: 30-60 minutes; intravenous: within 5 minutes. |
| Duration of Action | Duration is 4-6 hours for analgesic effect; may extend to 8 hours in renal impairment. |
400 mg orally once daily
| Dosage form | SOLUTION |
| Renal impairment | eGFR 30-89 mL/min: no adjustment; eGFR <30 mL/min: 200 mg once daily; hemodialysis: 200 mg after dialysis |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 200 mg once daily; Child-Pugh C: not recommended |
| Pediatric use | Not established for patients under 18 years |
| Geriatric use | No specific adjustment; monitor renal function and adjust per renal criteria |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ARYNTA (ARYNTA).
| Breastfeeding | It is not known whether ARYNTA is excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants (including renal impairment and electrolyte disturbances), breastfeeding is not recommended during treatment and for at least 2 weeks after the last dose. M/P ratio is unknown. |
| Teratogenic Risk | ARYNTA is contraindicated in pregnancy. In the first trimester, there is a high risk of major congenital malformations, including neural tube defects, cardiovascular anomalies, and orofacial clefts. In the second and third trimesters, fetal growth restriction, oligohydramnios, and fetal renal impairment may occur. Late pregnancy exposure may cause neonatal hypotension, hyperkalemia, and renal dysfunction. |
■ FDA Black Box Warning
None. Pembrolizumab carries no FDA-required boxed warning.
| Serious Effects |
["None known based on prescribing information. Not recommended in patients with severe hypersensitivity to pembrolizumab or any excipients."]
| Precautions | ["Immune-mediated pneumonitis (including fatal cases)","Immune-mediated colitis (including severe diarrhea)","Immune-mediated hepatitis (including fatal cases)","Immune-mediated endocrinopathies (hypophysitis, thyroid disorders, type 1 diabetes, adrenal insufficiency)","Immune-mediated nephritis and renal dysfunction","Immune-mediated skin adverse reactions (including Stevens-Johnson syndrome)","Infusion-related reactions (severe or life-threatening)","Embryo-fetal toxicity (can cause fetal harm when administered to pregnant women)"] |
| Food/Dietary | No specific food interactions. Alcohol may increase risk of ketoacidosis. Avoid excessive alcohol intake. |
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| Fetal Monitoring | Monitor maternal blood pressure, serum electrolytes (especially potassium), renal function (creatinine, BUN), and uric acid levels periodically. Fetal monitoring includes serial ultrasound for growth, amniotic fluid volume, and fetal anatomy (if exposed inadvertently). In neonates, monitor blood pressure, renal function, and electrolytes for at least 48 hours post-delivery if exposure occurred near term. |
| Fertility Effects | Based on animal studies, ARYNTA may impair male and female fertility. In males, decreased spermatogenesis and testicular atrophy have been observed. In females, disrupted estrous cycles and reduced conception rates occurred. Reversibility after discontinuation is unknown. Men should seek advice on sperm preservation before treatment. |
| Clinical Pearls | ARYNTA (empagliflozin) is an SGLT2 inhibitor indicated for type 2 diabetes, heart failure with reduced ejection fraction, and chronic kidney disease. Monitor for euglycemic diabetic ketoacidosis (euDKA), especially in patients with reduced caloric intake or insulin dose reduction. Assess renal function before initiation; avoid if eGFR <30 mL/min/1.73 m² for diabetes, but can be used down to eGFR 20 mL/min/1.73 m² for heart failure or CKD. Check for volume depletion in elderly or those on diuretics. Genitourinary infections are common; counsel on hygiene. Rare but serious: necrotizing fasciitis of the perineum (Fournier gangrene). |
| Patient Advice | Take once daily in the morning with or without food. · Drink adequate fluids to prevent dehydration and low blood pressure. · Report symptoms of genital yeast infections or urinary tract infections promptly. · Seek immediate medical attention for pain, tenderness, redness, or swelling in the genital or perineal area. · Monitor blood glucose regularly; do not skip meals while on this medication. · Stop taking the drug and contact your doctor if you experience nausea, vomiting, abdominal pain, or difficulty breathing (signs of ketoacidosis). |