The Navigation Model of Therapy: Why Awareness Changes Everything
November 16, 2025
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Brand Name :
Sandimmune, Neoral, Gengraf
Synonyms :
cyclosporine
Class :
DMARDs, Immunomodulators; Calcineurin Inhibitors; ImmunosuppressantsÂ
Brand Name :
Sandimmune, Neoral, Gengraf
Synonyms :
cyclosporine
Class :
DMARDs, Immunomodulators; Calcineurin Inhibitors; ImmunosuppressantsÂ
Dosage Forms & Strengths Â
Capsule Â
100mg  Â
50mg Â
25mg Â
Injectable solution Â
50mg/mLÂ Â Â
Oral solution Â
100mg/mLÂ Â Â
Oral
4 to 12 hours of pre-transplant: Administer 15 mg/kg orally for 1 dose
1 to 2 weeks post-transplant: Administer 15 mg/kg/day orally divided twice a day
until 5% reduction per week: Administer 5 to 10 mg/kg/day orally divided twice a day
Intravenous
4-to-12-hour pre-transplant intravenous: Administer 5 to 6 mg/kg intravenously for 1 dose for 2 to 6 hours
Post-transplant, until oral therapy can be tolerated: Administer 5 to 6 mg/kg intravenously every day
Neoral or Gengraf: Administer 1.25 mg/kg orally twice a day
can increase the dose by 0.5 to 0.75 mg/kg/day after 8 weeks, and if needed again after 12 weeks, Do not exceed 4 mg/kg in a day
If no improvement is shown after 16 weeks, discontinue.
Neoral or Gengraf: Administer 1.25 mg/kg orally twice a day
doses of 0.5 mg/kg/day may be increased after 4 weeks and every 2 weeks if necessary.
Do not exceed 4 mg/kg in a day.
Treatment should be stopped if no improvement is shown after six weeks at the highest recommended dosage of 4 mg/kg daily.
Dosage Forms & Strengths Â
Capsule Â
25mg  Â
50mg  Â
100mg  Â
Injectable solution Â
50mg/mLÂ Â Â
Oral solution Â
100mg/mLÂ Â Â
Indicated for Solid Organ Transplantation (Off label):
To avoid solid organ transplant rejection, cyclosporine has been administered to infants as early as six months old.
Oral
4 to 12 hours of pre-transplant: Administer 15 mg/kg orally for 1 dose
1 to 2 weeks post-transplant: 15 mg/kg/day orally divided twice a day
Reduce until 5% per week: Administer 5 to 10 mg/kg/day orally divided twice a day
Intravenous
4-to-12-hour pre-transplant intravenous: Administer 5 to 6 mg/kg intravenously for 1 dose for 2 to 6 hours
Post-transplant, until oral therapy can be tolerated: Administer 5 to 6 mg/kg intravenously every day
Refer adult dosing Â
may increase the nephrotoxic effect of nonsteroidal anti-inflammatory agents
may increase the nephrotoxic effect of nonsteroidal anti-inflammatory agents
may increase the nephrotoxic effect of nonsteroidal anti-inflammatory agents
may increase the nephrotoxic effect of nonsteroidal anti-inflammatory agents
may increase the nephrotoxic effect of nonsteroidal anti-inflammatory agents
may have an increased adverse effect when combined with caspofungin
cyclosporin: they may diminish the serum concentration of CYP3A4 Inducers
cyclosporin: they may diminish the serum concentration of CYP3A4 Inducers
cyclosporin: they may diminish the serum concentration of CYP3A4 Inducers
cyclosporin: they may diminish the serum concentration of CYP3A4 Inducers
cyclosporin: they may diminish the serum concentration of CYP3A4 Inducers
may enhance the serum concentration of P-glycoprotein/ABCB1 Inhibitors
may enhance the serum concentration of cyclosporine
relugolix/​estradiol/​norethindrone
may increase the hepatotoxic effect of cyclosporine
relugolix/estradiol/norethindrone
may increase the hepatotoxic effect of cyclosporine
may increase the hepatotoxic effect of cyclosporine
may increase the hepatotoxic effect of cyclosporine
may increase the hepatotoxic effect of cyclosporine
may diminish the metabolism of cyclosporine
triamcinolone acetonide/nystatin
may diminish the metabolism of cyclosporine
may diminish the metabolism of cyclosporine
methenamine/sodium salicylate/benzoic acid
may diminish the metabolism of cyclosporine
may diminish the metabolism of cyclosporine
may increase the nephrotoxic effect of cyclosporine
may increase the nephrotoxic effect of cyclosporine
may increase the nephrotoxic effect of cyclosporine
may increase the nephrotoxic effect of cyclosporine
may increase the nephrotoxic effect of cyclosporine
respiratory syncytial virus vaccine, adjuvanted
may diminish the therapeutic effect of immunosuppressants
respiratory syncytial virus (RSV) vaccine
may diminish the therapeutic effect of immunosuppressants
may diminish the therapeutic effect of immunosuppressants
when both drugs are combined, there may be an increased risk of adverse effects 
may increase the toxicity of each other
may increase the toxicity of each other
may increase the myelosuppressive effect
may increase the nephrotoxic effect of fibric acid derivatives
may increase the nephrotoxic effect of tacrolimus
may increase the nephrotoxic effect of tacrolimus
may increase the nephrotoxic effect of nonsteroidal anti-inflammatory agents
estrogens esterified/methyltestosterone            Â
may increase the hepatotoxic effect of androgens
may have an increased risk of renal failure and hypertension when combined with cyclosporine
The severity of the increase in blood pressure may be increased when cyclosporine is coadministered with peginesatide
may increase the toxic effect of Immunosuppressants
testolactone decreases the metabolism and increases the effect of cyclosporine
cyclosporine can impact the hepatic/intestinal enzyme CYP3A4 metabolism, leading to an elevation in the level or potency of intranasal midazolam
It may diminish the effect when combined with efavirenz affecting CYP3A4 metabolism
methytestosterone decreases the metabolism and increases the effect of cyclosporine
when cyclosporine is used in combination with diphtheria & tetanus toxoids, this leads to a reduction in the effects of diphtheria & tetanus toxoids through pharmacodynamic antagonism
dengue vaccine efficacy will be reduced by pharmacodynamic antagonism of cyclosporine
cyclosporine: it may enhance the serum concentration of simvastatin
when both drugs are combined, there may be an increased level of serum concentration of alpelisib   
oxymetholone decreases the metabolism and increases the effect of cyclosporine
danazol decreases metabolism and increases the effect of cyclosporine
methytestosterone decreases the metabolism and increases the effect of cyclosporine
methytestosterone decreases the metabolism and increases the effect of cyclosporine
May enhance the toxic effects of the other by pharmacodynamic synergism
may increase the level of effectiveness through P-glycoprotein MDR1 efflux transporter
may increase the levels of serum concentration of elagolix
may diminish the serum concentration
may enhance the serum concentration when combined
the toxicity of either of the drugs is increased by immunosuppressive activity
it decreases the concentration of eltrombopag in the serum
it increases the effect of neuromuscular blockage of neuromuscular-blocking agents
it increases the effect of neuromuscular blockage of neuromuscular-blocking agents
it increases the effect of neuromuscular blockage of neuromuscular-blocking agents
it increases the effect of neuromuscular blockage of neuromuscular-blocking agents
it increases the effect of neuromuscular blockage of neuromuscular-blocking agents
may enhance the serum concentration when combined with cyclosporine
may enhance the serum concentration when combined with cyclosporine
may enhance the serum concentration when combined with cyclosporine
may enhance the serum concentration when combined with cyclosporine
may enhance the serum concentration when combined with cyclosporine
CYP3A4 inhibitors increase the concentration of iloperidone in the serum
CYP3A4 inhibitors increase the concentration of iloperidone in the serum
CYP3A4 inhibitors increase the concentration of iloperidone in the serum
CYP3A4 inhibitors increase the concentration of iloperidone in the serum
CYP3A4 inhibitors increase the concentration of iloperidone in the serum
may have an increased neuromuscular-blocking effect when combined with neuromuscular-blocking agents
may have an increased neuromuscular-blocking effect when combined with neuromuscular-blocking agents
may have an increased neuromuscular-blocking effect when combined with neuromuscular-blocking agents
may have an increased neuromuscular-blocking effect when combined with neuromuscular-blocking agents
may have an increased neuromuscular-blocking effect when combined with neuromuscular-blocking agents
may enhance the concentration of serum when combined with cyclosporine
may enhance the concentration of serum when combined with cyclosporine
may enhance the concentration of serum when combined with cyclosporine
may enhance the concentration of serum when combined with cyclosporine
may enhance the concentration of serum when combined with cyclosporine
may increase the nephrotoxic effect of cyclosporine
neomycin/polymyxin B/bacitracin topical
may increase the nephrotoxic effect of cyclosporine
may increase the nephrotoxic effect of cyclosporine
may increase the nephrotoxic effect of cyclosporine
may increase the nephrotoxic effect of cyclosporine
may enhance the serum concentration of cyclosporine
may enhance the serum concentration of cyclosporine
may enhance the serum concentration of cyclosporine
may enhance the serum concentration of cyclosporine
may enhance the serum concentration of cyclosporine
It may enhance toxicity when combined with cholic acid by diminishing the elimination
cyclosporine: they may enhance the serum concentration of CYP3A4 Inhibitors
cyclosporine: they may enhance the serum concentration of CYP3A4 Inhibitors
Combining tegafur with cyclosporine can reduce tegafur’s metabolism
When loracarbef is used together with cyclosporine, the risk or seriousness of nephrotoxicity is enhanced
When alprazolam and cyclosporine is used together, this leads to reduction in the alprazolam’s metabolism
When encainide is used together with cyclosporine, this leads to a reduction in the encainide’s metabolism
When cefmenoxime is used together with cyclosporine, this leads to enhanced risk or seriousness of nephrotoxicity
When cyclosporine is used in combination with rabies vaccine, this leads to a reduction in the rabies vaccine effects through the process of pharmacodynamic antagonism
poliovirus vaccine inactivatedÂ
cyclosporine reduces the poliovirus vaccine's inactivating effects through pharmacodynamic antagonistic interactions
cyclosporine leads to a reduction in the rate of excretion of nitric oxide, which leads to an increased level of serum
the potential or intensity of adverse effects can be heightened when flurandrenolide is combined with cyclosporine
nafcillin will decrease the effect of action of cyclosporin by affecting enzyme CYP3A4 metabolism.
when cyclosporine and melphalan combine the immunosuppressive effects of both the drugs are enhanced and lead to increased risk of infection
may increase the hepatotoxic adverse effects of methotrexate by enhancing the serum concentration
may increase the hepatotoxic adverse effects of trimetrexate by enhancing the serum concentration
increase the therapeutic effect of daunorubicin by P-glycoprotein efflux transporter
both the drugs increase the effect of immunosuppression risk of infection increases on administering both the drugs simultaneously
increases serum level of cabazitaxel by affecting the enzyme CYP3A4
may enhance the serum level of docetaxel
increase the therapeutic effect of idarubicin by P-glycoprotein efflux transporter
may alter the level by affecting CYP450 enzyme metabolism
may alter the level by affecting CYP450 enzyme metabolism
may enhance the serum concentration of CYP3A4 inhibitors
may increase the neurotoxic effects of imipenem
imipenem/cilastatin/relebactamÂ
may increase the neurotoxic effects of imipenem
may increase the risk or severity of hypertension when combined
may increase the nephrotoxic effect when combined with cyclosporine
may increase the nephrotoxic effect when combined with cyclosporine
may have an increased nephrotoxic effect when combined with cyclosporine
may diminish the amount of P-glycoprotein (MDR1) efflux transporter
may enhance the serum concentration of CYP3A4 Inhibitors
omeprazole: they may enhance the serum concentration of cyclosporine
may diminish the concentration of serum when combined with cyclosporine
melphalan flufenamide: they may increase the nephrotoxic effect of cyclosporin
may have an increased risk of rhabdomyolysis & myoglobinuria when combined with cyclosporine
the serum levels of potassium may be increased
pneumococcal vaccine 13-valentÂ
cyclosporine diminishes the efficacy of the 13-valent pneumococcal vaccine through pharmacodynamic antagonism
may have a decrease in excretion when combined with cyclosporine
the rate of metabolism of cyclosporine may be reduced
the risk of adverse effects may be increased
When cyclosporine is used together with oliceridine, this leads to enhanced concentration serum of oliceridine
cyclosporine might lead to a reduction in the rate of excretion of telavancin, potentially leading to elevated levels of serum
androgens increase the effect of hepatotoxicity of cyclosporine
Actions and Spectrum:Â Â
The mechanism of action of cyclosporine is the ability to inhibit the response of the immune system; it is particularly known to influence T lymphocytes (T cells), which are responsible for immune reactions.Â
Cyclosporine primarily acts on calcineurin which is a protein phosphatase involved in the T cells. During T cell activation, calcineurin gets involved in activation pathways that synthesizes and secretes cytokine molecules in immune response. cyclosporine forms a complex with a protein known as cyclophilin and competes with activated calcium for binding to calcineurin to render the enzyme inactive. This inhibits the activation of transcription factors referred to as nuclear factor of activated T cells (NFAT) that are required to synthesize the cytokines such as interleukin-2 (IL-2).Â
The activity of cyclosporine is selective on T cells, although other immune cells are influenced to a lesser degree. Due to its action on inhibiting T cell activation and cytokine, cyclosporine reduces the body’s ability to reject transplanted organs by moderating the immune system’s reaction to the foreign organ.Â
Frequency defined Â
>10%Â Â
Nephrotoxicity (32%)Â Â
Infection (3-25%)Â Â
Nausea (23%)Â Â
Hypertrichosis (5-19%)Â Â
Gum hyperplasia (2-16%)Â Â
Hypertension (26%)Â Â
Headache (2-25%)Â Â
Hirsutism (21%)Â Â
Female reproductive disorder (5-19%)Â Â
Tremor (12-55%)Â Â
1-10%Â Â
Convulsions Â
Hyperkalemia, hypomagnesemia Â
Hepatotoxicity Â
Acne Â
Pruritus Â
Pancreatitis Â
Flu-like syndrome Â
Frequency Not Defined Â
Thrombocytopenia Â
Glomerular capillary thrombosis Â
Migraine Â
Hyponatremia Â
Anaphylaxis Â
Hypomagnesemia Â
Leukopenia Â
Post-marketing reports Â
Pain in lower extremities Â
Black box warningÂ
Concurrent use of other immunosuppressive agents has been found to increase the risk of infection and neoplasia in kidney, liver, and heart transplant patients.Â
Risk of developing new lymphomas and other skin cancers elevated; reduce exposure to excessive amounts of UV radiation.Â
Contraindications/caution:Â Â
Contraindications:Â Â
CautionÂ
Pregnancy/Lactation Â
Pregnancy consideration: CÂ Â
Lactation: Excretion of the drug in human breast milk is known Â
Pregnancy category:Â Â
Pharmacology Â
cyclosporine is an immunosuppressive drug with combination of effecting mechanisms on body. It mainly works through the suppression of activation and proliferation of the T lymphocyte cells otherwise known as the T cells which are a form of white blood cells that participate in immune responses.Â
The major action of cyclosporine is that interferes with function and activation of T lymphocytes and prevents them from multiplying. It inhibits the production and release of interleukin-2 (IL-2) which is needed for the T-cells activation and replication. Â
PharmacodynamicsÂ
Cyclosporine possesses an anti-inflammatory activity and regulates the immune response as well. Cyclosporine acts selectively on T lymphocytes but also exerts an indirect influence on other components of the immune system; it suppresses B lymphocyte functions and inhibits the cytotoxicity of natural killer cells, which plays a role in cell-mediated immune reactions.Â
Pharmacokinetics:Â Â
AbsorptionÂ
Neoral has higher level of bioavailability compared to Sandimmune. Â
The peak plasma time for Neoral is 1.5 to 2 hours and for Sandimmune it is 3. 5 hours.Â
DistributionÂ
90% of the drug is protein boundedÂ
The volume of distribution-13 L/Kg.Â
MetabolismÂ
It undergoes hepatic metabolism through CYP3A4 and active metabolites AM1, AM9, and AM4N are formed. Â
Elimination/ExcretionÂ
Half-life ranges from 8.4 to 27 hours and clearance is 5 to 7 mL/min/kg. The elimination is mainly through bile and feces with 6% through urine.Â
Administration Â
It is administered orally in the form of capsules. It is also given intravenously Â
Patient information leaflet Â
Generic Name: cyclosporine Â
Why do we use cyclosporine? Â
It is an immunosuppressive drug used in the treatment of organ transplantation, autoimmune disorders and psoriasis. Â
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