ADHD Treatments Under the Spotlight: Weighing Benefits and Harms
November 28, 2025
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Brand Name :
Rapamune
Synonyms :
sirolimus
Class :
Selective Immunosuppressants
Brand Name :
Rapamune
Synonyms :
sirolimus
Class :
Selective Immunosuppressants
Dosage forms and strengths Â
oral solutionÂ
(1mg/mL)Â
tabletÂ
2mgÂ
1mgÂ
0.5mgÂ
Indicated for Rejection Prophylaxis of Organ Transplantat
The initial dose administered on the first day is 3 mg/m²
followed by a daily maintenance dose of 1 mg/ m²
weight of 40 kg or greater-
Initial dose- 6 mg orally to be taken on the first day
Maintenance-2 mg to be taken orally once daily
Individuals undergoing sirolimus treatment in combination with cyclosporine-
The recommended loading dose for sirolimus on the first day after transplantation is up to 15 mg
From day 2 onwards, an initial maintenance dose of 5 mg/day is recommended
It is important to obtain a trough level between days 5 and 7 and adjust the daily dose of sirolimus accordingly
Maintenance therapy after discontinuation of cyclosporine-
It is recommended to gradually discontinue the use of cyclosporine over a period of 4 to 8 weeks
The range for dose adjusted are typically between 16 and 24 ng/mL during the first year after transplantation
Subsequently, the target range is usually between 12 and 20 ng/mL
Dosage forms and strengthsÂ
oral solutionÂ
(1mg/mL)Â
tabletÂ
2mgÂ
1mgÂ
0.5mgÂ
indicated for Rejection Prophylaxis of Organ Transplantion For individuals with a low to modest immune system risk-
Age more than or equal to 13 years
Weight <40 kg
An initial dose of 3 mg/m²should be given on the first day
followed by a daily maintenance dose of 1 mg/m²
weight more than or equal 40 kg
loading dose is 6 mg taken orally on the first day
maintenance dose of 2 mg taken orally once daily
Refer adult dosingÂ
sirolimus: they may enhance the serum concentration of CYP3A4 Inhibitors
sirolimus: they may enhance the serum concentration of CYP3A4 Inhibitors
sirolimus: they may enhance the serum concentration of CYP3A4 Inhibitors
sirolimus: they may enhance the serum concentration of CYP3A4 Inhibitors
sirolimus: they may enhance the serum concentration of CYP3A4 Inhibitors
sirolimus: they may enhance the serum concentration of CYP3A4 Inducers
sirolimus: they may enhance the serum concentration of CYP3A4 Inducers
sirolimus: they may enhance the serum concentration of CYP3A4 Inducers
sirolimus: they may enhance the serum concentration of CYP3A4 Inducers
sirolimus: they may enhance the serum concentration of CYP3A4 Inducers
sirolimus: they may enhance the serum concentration of glycoprotein IIa Inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may decrease the therapeutic effect of drugs affecting gallbladder function
may enhance the serum concentration of P-glycoprotein/ABCB1 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 Inhibitors
It may enhance the effect when combined with grapefruit by CYP3A4 metabolism
It may diminish the effect when combined with griseofulvin by CYP3A4 metabolism
It may enhance the effect when combined with miconazole vaginal by affecting CYP3A4 metabolism
When sirolimus is used in combination with rabies vaccine, this leads to a reduction in the rabies vaccine effects through the process of pharmacodynamic antagonism
when sirolimus is used in combination with diphtheria & tetanus toxoids, this leads to a reduction in the effects of diphtheria & tetanus toxoids through pharmacodynamic antagonism
interaction raises immunosuppressive effects and risk of infection
the effect of sirolimus is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
when both drugs are combined, there may be a decreased effect of sirolimus by affecting hepatic or intestinal enzyme cyp3a4 metabolism  
metronidazole enhances the effect of sirolimus by altering the intestinal or hepatic CYP3A4 enzyme metabolism
pneumococcal vaccine 13-valentÂ
sirolimus diminishes the efficacy of the 13-valent pneumococcal vaccine through pharmacodynamic antagonism
it may decrease the levels of serum concentration of Sirolimus
it may decrease the levels of serum concentration of Sirolimus
it may decrease the levels of serum concentration of Sirolimus
it may decrease the levels of serum concentration of Sirolimus
it may decrease the levels of serum concentration of Sirolimus
may increase the levels of serum concentration
It may enhance and diminish the immunosuppressive effects when combined with maitake
both the drugs increase the effect of immunosuppression risk of infection increases on administering both the drugs simultaneously
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
CYP3A4 inhibitors increase the concentration of sirolimus in serum
prokinetic GI agents decrease the concentration of sirolimus in serum
CYP3A4 inducers decrease the concentration of sirolimus in serum
may enhance the serum concentration of clotrimazole
may enhance the serum concentration of micafungin
CYP3A4 inhibitors increase the concentration of sirolimus in the serum
CYP3A4 inhibitors increase the concentration of sirolimus in the serum
CYP3A4 inhibitors increase the concentration of sirolimus in the serum
CYP3A4 inhibitors increase the concentration of sirolimus in the serum
CYP3A4 inhibitors increase the concentration of sirolimus in the serum
sirolimus serum concentration may be elevated by cannabidiol
Actions and SpectrumÂ
Action:Â
Immunosuppression: The drug suppresses the activity of the immune system, particularly the function of T-cells. It inhibits the activation and proliferation of T-cells, which are involved in immune response and rejection of transplanted organs.Â
Anti-proliferative effect: The drug has an anti-proliferative effect on cells, which means it inhibits their growth and division. It achieves this by blocking the mTOR pathway, a crucial signaling pathway that regulates cell growth, survival, and metabolism. Â
Anti-inflammatory effect: The drug has anti-inflammatory properties and can reduce inflammation in various conditions, such as autoimmune diseases and certain types of skin disorders.Â
Spectrum:Â
Organ transplantation: The drug is used in combination with other immunosuppressant drugs to prevent rejection of transplanted organs, such as kidneys, liver, or heart. Â
Autoimmune diseases: The drug may be used in the treatment of certain autoimmune diseases, including rheumatoid arthritis, systemic lupus erythematosus, and autoimmune hepatitis. Â
Certain types of cancer: The drug may be used in the treatment of certain types of cancer, such as renal cell carcinoma, breast cancer, and lymphoma.Â
Frequency defined Â
>10%Â
Acne (22%)Â
Nausea (25-31%)Â
Constipation (36-38%)Â
Anemia (23-33%)Â
Rash (10-20%)Â
Hypertension (45-49%)Â
Fever (23-34%)Â
Diarrhea (25-35%)Â
Thrombocytopenia (14-30%)Â
Pain (29-33%)Â
Arthralgia (25-31%)Â
Headache (34%)Â
Increased creatinine (39-40%)Â
Urinary tract infection (26-33%)Â
Arthralgia (25-31%)Â
Abdominal pain (29-36%)Â
Black Box Warning:Â Â
Immunosuppression: Immunosuppression can lead to an increased vulnerability to infections and raise the risk of developing lymphoma and other types of malignancies.Â
Contraindication/Caution:Â Â
Hypersensitivity: The drug should not be used in individuals who have a known hypersensitivity or allergy to sirolimus or any of its components. Â
Pregnancy: The use of this drug is contraindicated during pregnancy. If a woman becomes pregnant while taking sirolimus, she should inform her healthcare provider immediately.Â
Breastfeeding: It is generally not recommended to breastfeed while taking sirolimus. A healthcare provider should be consulted to discuss alternative feeding options.Â
Severe hepatic impairment: The use of sirolimus in patients with severe hepatic impairment should be approached with caution or avoided altogether.Â
Active infections: The drug can suppress the immune system, making individuals more susceptible to infections. It is generally recommended to avoid sirolimus in the presence of active, uncontrolled infections.Â
Interactions: The drug can interact with other medications, including certain antibiotics, antifungal agents, and other immunosuppressive drugs.
Pregnancy warnings:    Â
Pregnancy category: CÂ
Lactation: Data not availableÂ
Pregnancy Categories:        Â
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.Â
Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.  Â
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   Â
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.  Â
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.   Â
Category N: There is no data available for the drug under this category
Pharmacology:Â Â
sirolimus, also known as rapamycin, is a medication that belongs to the class of drugs known as mammalian target of rapamycin (mTOR) inhibitors.Â
Pharmacodynamics:Â Â
sirolimus inhibits the mTOR pathway, a key signaling pathway involved in cellular growth, proliferation, and survival. By binding to a protein called FKBP12, drug forms a complex that inhibits mTOR complex 1 (mTORC1), leading to the suppression of downstream signaling cascades. This inhibition ultimately results in reduced T-cell activation, proliferation, and antibody production, thereby suppressing the immune response.  Â
Pharmacokinetics:Â
AbsorptionÂ
The drug is primarily administered orally in the form of tablets or capsules. It is well-absorbed from the gastrointestinal tract, but its absorption can be affected by factors such as food intake and formulation. The oral bioavailability of sirolimus is approximately 14-28%.Â
DistributionÂ
It has a large volume of distribution, suggesting extensive tissue distribution. The drug is known to penetrate into red blood cells and accumulate in various tissues, including the liver, kidney, lung, and spleen.Â
MetabolismÂ
The drug undergoes extensive metabolism in the liver by the cytochrome P450 enzyme system, primarily CYP3A4. The main metabolite formed is 42-O-demethylated sirolimus (active metabolite), which also exhibits immunosuppressive activity. Â
Excretion and EliminationÂ
The drug and its metabolites are primarily eliminated through the feces. Only a small portion is excreted unchanged in the urine (approximately 2%). The elimination half-life of sirolimus is around 57 hours, indicating a slow clearance from the body.Â
Administration: Â
The administration of the drug is typically done orally, in the form of tablets or oral solution. The dose of sirolimus varies depending on various factors, such as the patient’s age, weight, and specific medical condition.Â
Patient information leafletÂ
Generic Name: sirolimusÂ
Why do we use sirolimus? Â
Lymphangioleiomyomatosis (LAM): sirolimus has shown efficacy in slowing down the progression of LAM and improving lung function. It helps stabilize lung function and reduces the risk of pneumothorax (collapsed lung) in individuals with LAM. Â
Drug-Eluting Stents: The drug is used in the development of drug-eluting stents (DES) used in interventional cardiology. DES are tiny tubes placed in narrowed blood vessels to improve blood flow. The drug coating on the stent, which includes sirolimus, helps prevent restenosis (re-narrowing) of the vessel. Â
Certain Cancers: The drug has been studied for its potential anticancer properties. used in certain types of cancers, including advanced renal cell carcinoma (kidney cancer) and subependymal giant cell astrocytomas (SEGAs) associated with TSC.Â
Dermatological Conditions: The drug has been explored for its use in certain dermatological conditions, such as facial angiofibromas (a symptom of TSC), cutaneous T-cell lymphoma, and other rare skin disorders. It can help reduce the size and proliferation of these skin lesions.Â
Organ Transplantation: The drug is commonly used in transplant medicine as an immunosuppressant. It helps prevent rejection of transplanted organs, such as kidney, liver, or heart, by inhibiting the body’s immune response. sirolimus is often used in combination with other immunosuppressive medications to achieve optimal results. Â
Renal angiomyolipomas: The drug is used in the treatment of renal angiomyolipomas, which are non-cancerous tumors that can occur in individuals with a genetic disorder called tuberous sclerosis complex (TSC).
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