Sirolimus

A to Z Drug Facts

Sirolimus

 Actions
 Indications
 Contraindications
 Route/Dosage
 Interactions
 Lab Test Interferences
 Adverse Reactions
 Precautions
Patient Care Considerations
 Administration/Storage
 Assessment/Interventions
 Patient/Family Education


(SER-oh-lih-muss)
Rapamune
Solution, oral: 1 mg/mL
Class: Immunosuppressive

 Actions Inhibits T-lymphocyte activation and proliferation that occurs in response to antigenic and cytokine stimulation; inhibits antibody production.

 Indications Prophylaxis of organ rejection in patients receiving renal transplants.

Treatment of psoriasis.

 Contraindications Standard considerations.

 Route/Dosage

Only physicians experienced in immunosuppressive therapy and management of renal transplant patients should use sirolimus.

ADULTS: PO Recommended loading dose of 6 mg with a daily maintenance dose of 2 mg (ie, loading dose 3 times the maintenance dose) in a regimen with cyclosporine and corticosteroids.

ADULTS AND CHILDREN at least 13 yr who weigh less than 40 kg: PO Adjust dose to 1 mg/m2/day based on body surface area. The loading dose should be 3 mg/m2.

Hepatic Impairment: PO Reduce maintenance dose by approximately 33%; do not modify loading dose.

 Interactions

Cyclosporine: Sirolimus plasma concentrations may be increased; administer sirolimus 4 hr after cyclosporine. Cytochrome P450 3A4 inhibitors (eg, erythromycin, protease inhibitors [eg, ritonavir], verapamil): Sirolimus plasma levels may be elevated, increasing the pharmacologic and adverse effects. Cytochrome P450 3A4 inducers (eg, carbamazepine, phenytoin, St. John's wort): Sirolimus plasma levels may be reduced, decreasing the pharmacologic effects. Diltiazem, ketoconazole: Sirolimus plasma concentrations may be increased. Rifampin: Sirolimus plasma concentrations may be decreased. Vaccination: Response to vaccination may be less effective.

 Lab Test Interferences None well documented.

 Adverse Reactions

CARDIOVASCULAR: Hypertension; hypotension; atrial fibrillation; CHF; hemorrhage; hypervolemia; palpitations; peripheral vascular disorder; postural hypotension; syncope; tachycardia; thrombophlebitis; thrombosis; vasodilation. CNS: Insomnia; tremor; headache; anxiety; confusion; depression; dizziness; emotional lability; hypertonia; hyperesthesia; hypotonia; neuropathy; paresthesia; somnolence. DERMATOLOGIC: Acne; rash; skin ulcer; fungal dermatitis; hirsutism; pruritus; skin hypertrophy; sweating. EENT: Abnormal vision; cataract; conjunctivitis; deafness; ear pain; otitis media; tinnitus. GI: Constipation; diarrhea; dyspepsia; nausea; vomiting; anorexia; dysphagia; eructation; esophagitis; flatulence; gastritis; gastroenteritis; gingivitis; gum hyperplasia; ileus; mouth ulceration; oral moniliasis; stomatitis. GU: UTI; albuminuria; bladder pain; dysuria; hematuria; hydronephrosis; impotence; kidney pain; kidney tubular necrosis; nocturia; oliguria; pyuria; scrotal edema; testis disorder; toxic nephropathy; increased urinary frequency; urinary incontinence; urinary retention. HEMATOLOGIC: Anemia; leukopenia; thrombocytopenia; ecchymosis; leukocytosis; lymphadenopathy; polycythemia. HEPATIC: Abnormal LFTs. METABOLIC: Increased serum creatinine; hypercholesterolemia; hyperkalemia; hyperlipemia; hypokalemia; increased LDH; hypophosphatemia; weight gain/loss; diabetes mellitus; glucosuria; acidosis; increased alkaline phosphatase; increased BUN; increased creatine phosphokinase; dehydration; abnormal healing; hypercalcemia; hypoglycemia; hypomagnesemia; hyponatremia. RESPIRATORY: Dyspnea; pharyngitis; upper respiratory tract infection; asthma; atelectasis; bronchitis; increased cough; epistaxis; hypoxia; lung edema; pleural effusion; pneumonia; rhinitis; sinusitis. OTHER: Edema; peripheral edema; abdominal pain; asthenia; back pain; chest pain; fever; pain; arthralgia; lymphocele; facial edema; Cushing syndrome; arthrosis; bone necrosis; leg cramps; myalgia; osteoporosis; tetany; abdominal enlargement; abscess; ascites; cellulitis; chills; flu syndrome; hernia; infection; malaise; pelvic pain; peritonitis; sepsis.

 Precautions

Pregnancy: Category C. Lactation: Undetermined. Children younger than 13 yr: Safety and efficacy not established. Infection: Increased susceptibility to infection, including Pneumocystis carinii may occur. Lipids: Increased serum cholesterol and triglycerides, requiring treatment, may occur. Lymphoma: Increased possibility of developing lymphoma. Renal function: Decreased renal function may occur; monitor closely.


PATIENT CARE CONSIDERATIONS


 Administration/Storage

 Assessment/Interventions

OVERDOSAGE: SIGNS & SYMPTOMS
  Atrial fibrillation

 Patient/Family Education

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© 2003 Facts and Comparisons
David S. Tatro
A to Z Drug Facts