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TRUTH IN PEPTIDES
Peer Reviewed

Rapamycin — Interactions & Safety Profile

4 contraindications2 known interactions⚠ Pregnancy warning

Contraindications

Hypersensitivity to sirolimus or derivatives

Allergic reactions documented.

Active untreated infections

Immunosuppressive at transplant doses; even at low doses, immune function is modulated.

Severe hepatic impairment

Rapamycin is hepatically metabolised via CYP3A4.

Surgery within 2 weeks

Rapamycin impairs wound healing even at low doses.

Drug Interactions

CYP3A4 inhibitors (ketoconazole, erythromycin, grapefruit juice)Seriousmajor interaction

Significantly increase rapamycin blood levels, potentially causing toxicity.

Mechanism: CYP3A4 inhibition reduces rapamycin metabolism.

Avoid grapefruit/grapefruit juice entirely. Monitor levels closely if CYP3A4 inhibitor is necessary.

CYP3A4 inducers (rifampin, St. John's Wort)Seriousmajor interaction

Dramatically decrease rapamycin levels, rendering it ineffective.

Mechanism: CYP3A4 induction accelerates rapamycin metabolism.

Avoid concurrent use of strong CYP3A4 inducers.

Monitoring Required

  • Lipid panel (rapamycin can elevate triglycerides and cholesterol)
  • CBC with differential
  • Fasting glucose / HbA1c
  • Renal function
  • Liver function
  • Rapamycin trough levels (transplant dosing only)

Pregnancy & Nursing

Contraindicated. Teratogenic potential. Effective contraception required during treatment.

Pending physician review — consult your provider before use.

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