Cyclosporine: Difference between revisions
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==Adult Dosing== | ==Adult Dosing== | ||
===Organ transplant rejection prophylaxis=== | ===Organ transplant rejection prophylaxis=== | ||
* Dosing protocols vary | *Dosing protocols vary | ||
* Start: 7- | *Start: 7-9mg/kg/day PO divided BID; give 1st dose 4-12 hr pre-transplant or postop | ||
* For heart, kidney, or liver transplant, adjust dose based on target levels, rejection status, adverse effects | *For heart, kidney, or liver transplant, adjust dose based on target levels, rejection status, adverse effects | ||
===Rheumatoid arthritis, severe=== | ===Rheumatoid arthritis, severe=== | ||
* Start: 2. | *Start: 2.5mg/kg/day PO divided BID, increase 0.5-0.75mg/kg/day after 8 wk and after 12 wk; Max: 4mg/kg/day | ||
* Use alone or with methotrexate; decreased 25-50% PRN adverse effects, discontinue if no benefit by 16 wks | *Use alone or with methotrexate; decreased 25-50% PRN adverse effects, discontinue if no benefit by 16 wks | ||
===Psoriasis, severe recalcitrant plaque=== | ===Psoriasis, severe recalcitrant plaque=== | ||
* Start: 2. | *Start: 2.5mg/kg/day PO divided BID, increase 0.5mg/kg/day q 2 wk after 4 wk; Max: 4mg/kg/day | ||
* Decrease 25-50% PRN adverse effects, discontinue if inadequate response after 6 weeks on max tolerated dose | *Decrease 25-50% PRN adverse effects, discontinue if inadequate response after 6 weeks on max tolerated dose | ||
==Pediatric Dosing== | ==Pediatric Dosing== | ||
===Organ transplant rejection prophylaxis=== | ===Organ transplant rejection prophylaxis=== | ||
* Dosing protocols vary | *Dosing protocols vary | ||
* Start 7- | *Start 7-9mg/kg/day PO divided BID, give 1st dose 4-12 hr pre-transplant or post op | ||
* For heart, kidney, or liver transplant, adjust dose based on target levels, rejection status, adverse effects | *For heart, kidney, or liver transplant, adjust dose based on target levels, rejection status, adverse effects | ||
==Special Populations== | ==Special Populations== | ||
*[[Drug Ratings in Pregnancy|Pregnancy Rating]]: | *[[Drug Ratings in Pregnancy|Pregnancy Rating]]: Pregnancy Category C | ||
*[[Lactation risk categories|Lactation risk]]: | *[[Lactation risk categories|Lactation risk]]: safety unknown | ||
===Renal Dosing=== | ===Renal Dosing=== | ||
*Adult: | *Adult: | ||
**transplant: no adjustment | |||
**rheumatoid arthritis or psoriasis: contraindicated in renal impairment | |||
*Pediatric: | *Pediatric: | ||
**transplant: no adjustment | |||
===Hepatic Dosing=== | ===Hepatic Dosing=== | ||
*Adult: | *Adult: not defined, caution advised | ||
*Pediatric: | *Pediatric: not defined, caution advised | ||
==Contraindications== | ==Contraindications== | ||
*Allergy to class/drug | *Allergy to class/drug | ||
*uncontrolled hypertension (RA or psoriasis use) | |||
*renal impairment (RA or psoriasis use) | |||
*malignancy (RA or psoriasis use) | |||
*PUVA/UVB treatment (psoriasis use) | |||
*concurrent immunosuppressants (psoriasis use) | |||
*coal tar treatment (psoriasis use) | |||
*concomitant XRT (psoriasis use) | |||
==Adverse Reactions== | ==Adverse Reactions== | ||
===Serious=== | ===Serious=== | ||
*hypertension, severe | |||
*immunosuppression | |||
*infection, severe | |||
*opportunistic infection | |||
*BK virus-associated nephropathy | |||
*hyperkalemia, severe | |||
*nephrotoxicity | |||
*hepatotoxicity | |||
*glomerular capillary thrombosis | |||
*diabetes mellitus | |||
*leukopenia | |||
*thrombocytopenia | |||
*hemolytic anemia | |||
*malignancy | |||
*malignancy | |||
*seizures | |||
*encephalopathy | |||
*posterior reversible encephalopathy syndrome | |||
*neurotoxicity | |||
*intracranial hypertension | |||
*optic disc edema | |||
*MI | |||
*depression | |||
*pancreatitis | |||
*GI bleeding | |||
===Common=== | ===Common=== | ||
*BUN, creatinine elevated | |||
*hypertension | |||
*hirsutism | |||
*infection | |||
*tremor | |||
*gingival overgrowth | |||
*headache | |||
*hypertriglyceridemia | |||
*nausea/vomiting | |||
*diarrhea | |||
*leg cramps | |||
*paresthesia | |||
*influenza-like symptoms | |||
*edema | |||
*dizziness | |||
*rash | |||
*acne | |||
*chest pain | |||
*stomatitis | |||
*hypomagnesemia | |||
*arthralgia | |||
*flushing | |||
*bronchospasm | |||
*hyperkalemia | |||
*hyperglycemia | |||
*hyperuricemia | |||
==Pharmacology== | ==Pharmacology== | ||
*Half-life: | *Half-life: 8.4h | ||
*Metabolism: | *Metabolism: liver extensively, GI tract, kidney; CYP450 | ||
*Excretion: | *Excretion: bile primarily, urine 6% | ||
==Mechanism of Action== | ==Mechanism of Action== | ||
exact mechanism of action unknown; inhibits T-lymphocytes | |||
==Comments== | ==Comments== | ||
| Line 56: | Line 118: | ||
==References== | ==References== | ||
<references/> | <references/> | ||
[[Category: | [[Category:Pharmacology]] | ||
epocrates | |||
Latest revision as of 07:21, 11 August 2016
Administration
- Type: immunosuppressant
- Dosage Forms: 25,100; 100/mL
- Routes of Administration: PO, injection
- Common Trade Names: Sandimmune
Adult Dosing
Organ transplant rejection prophylaxis
- Dosing protocols vary
- Start: 7-9mg/kg/day PO divided BID; give 1st dose 4-12 hr pre-transplant or postop
- For heart, kidney, or liver transplant, adjust dose based on target levels, rejection status, adverse effects
Rheumatoid arthritis, severe
- Start: 2.5mg/kg/day PO divided BID, increase 0.5-0.75mg/kg/day after 8 wk and after 12 wk; Max: 4mg/kg/day
- Use alone or with methotrexate; decreased 25-50% PRN adverse effects, discontinue if no benefit by 16 wks
Psoriasis, severe recalcitrant plaque
- Start: 2.5mg/kg/day PO divided BID, increase 0.5mg/kg/day q 2 wk after 4 wk; Max: 4mg/kg/day
- Decrease 25-50% PRN adverse effects, discontinue if inadequate response after 6 weeks on max tolerated dose
Pediatric Dosing
Organ transplant rejection prophylaxis
- Dosing protocols vary
- Start 7-9mg/kg/day PO divided BID, give 1st dose 4-12 hr pre-transplant or post op
- For heart, kidney, or liver transplant, adjust dose based on target levels, rejection status, adverse effects
Special Populations
- Pregnancy Rating: Pregnancy Category C
- Lactation risk: safety unknown
Renal Dosing
- Adult:
- transplant: no adjustment
- rheumatoid arthritis or psoriasis: contraindicated in renal impairment
- Pediatric:
- transplant: no adjustment
Hepatic Dosing
- Adult: not defined, caution advised
- Pediatric: not defined, caution advised
Contraindications
- Allergy to class/drug
- uncontrolled hypertension (RA or psoriasis use)
- renal impairment (RA or psoriasis use)
- malignancy (RA or psoriasis use)
- PUVA/UVB treatment (psoriasis use)
- concurrent immunosuppressants (psoriasis use)
- coal tar treatment (psoriasis use)
- concomitant XRT (psoriasis use)
Adverse Reactions
Serious
- hypertension, severe
- immunosuppression
- infection, severe
- opportunistic infection
- BK virus-associated nephropathy
- hyperkalemia, severe
- nephrotoxicity
- hepatotoxicity
- glomerular capillary thrombosis
- diabetes mellitus
- leukopenia
- thrombocytopenia
- hemolytic anemia
- malignancy
- malignancy
- seizures
- encephalopathy
- posterior reversible encephalopathy syndrome
- neurotoxicity
- intracranial hypertension
- optic disc edema
- MI
- depression
- pancreatitis
- GI bleeding
Common
- BUN, creatinine elevated
- hypertension
- hirsutism
- infection
- tremor
- gingival overgrowth
- headache
- hypertriglyceridemia
- nausea/vomiting
- diarrhea
- leg cramps
- paresthesia
- influenza-like symptoms
- edema
- dizziness
- rash
- acne
- chest pain
- stomatitis
- hypomagnesemia
- arthralgia
- flushing
- bronchospasm
- hyperkalemia
- hyperglycemia
- hyperuricemia
Pharmacology
- Half-life: 8.4h
- Metabolism: liver extensively, GI tract, kidney; CYP450
- Excretion: bile primarily, urine 6%
Mechanism of Action
exact mechanism of action unknown; inhibits T-lymphocytes
Comments
See Also
References
epocrates
