Tacrolimus Extended-Release Capsules

Name: Tacrolimus Extended-Release Capsules

Description

ASTAGRAF XL, a calcineurin-inhibitor immunosuppressant, is available for oral administration as hard gelatin capsules (tacrolimus extended-release capsules) containing the equivalent of 0.5 mg, 1 mg or 5 mg of anhydrous tacrolimus USP. Inactive ingredients include ethylcellulose NF, hypromellose USP, magnesium stearate NF and lactose monohydrate NF. The ingredients are directly proportional across all capsule strengths. The capsule shell contains gelatin NF, titanium dioxide USP, ferric oxide NF, and sodium lauryl sulfate.

Tacrolimus is the active ingredient in ASTAGRAF XL. Tacrolimus is a macrolide immunosuppressant produced by Streptomyces tsukubaensis. Chemically, tacrolimus is designated as [3S – [3R*[E(1S*, 3S*, 4S*)], 4S*, 5R*, 8S*, 9E, 12R*, 14R*, 15S*, 16R*, 18S*, 19S*, 26aR*]] – 5, 6, 8, 11, 12, 13, 14, 15, 16, 17, 18, 19, 24, 25, 26, 26a – hexadecahydro – 5, 19 – dihydroxy – 3 – [2 – (4 – hydroxy – 3 – methoxycyclo – hexyl) – 1 – methylethenyl] – 14, 16 – dimethoxy – 4, 10, 12, 18 – tetramethyl – 8 – (2 – propenyl) – 15, 19 – epoxy – 3H – pyrido[2, 1 – c][1, 4]oxaazacyclotricosine – 1, 7, 20, 21(4H, 23H) – tetrone, monohydrate.

The chemical structure of tacrolimus is:

Tacrolimus has an empirical formula of C44H69NO12•H2O and a formula weight of 822.03. Tacrolimus appears as white crystals or crystalline powder. It is practically insoluble in water, freely soluble in ethanol, and very soluble in methanol and chloroform.

Warnings

Included as part of the PRECAUTIONS section.

Overdose

Postmarketing cases of overdose with tacrolimus have been reported. Overdosage adverse reactions included:

  • nervous system disorders (tremor, headache, confusional state, balance disorders, encephalopathy, lethargy and somnolence)
  • gastrointestinal disturbances (nausea, vomiting, and diarrhea)
  • abnormal renal function (increased blood urea nitrogen and elevated serum creatinine)
  • urticarial
  • hypertension
  • peripheral edema, and
  • infections [one fatal postmarketing case of bilateral pneumopathy and CMV infection was attributed to tacrolimus (extended-release) overdose].

Based on the poor aqueous solubility and extensive erythrocyte and plasma protein binding, it is anticipated that tacrolimus is not dialyzable to any significant extent; there is no experience with charcoal hemoperfusion. The oral use of activated charcoal has been reported in treating acute overdoses, but experience has not been sufficient to warrant recommending its use. General supportive measures and treatment of specific symptoms should be followed in all cases of overdosage.

How is this medicine (Tacrolimus Extended-Release Capsules) best taken?

Use this medicine (tacrolimus extended-release capsules) as ordered by your doctor. Read all information given to you. Follow all instructions closely.

  • Keep taking this medicine as you have been told by your doctor or other health care provider, even if you feel well.
  • To gain the most benefit, do not miss doses.
  • Take this medicine (tacrolimus extended-release capsules) at the same time of day.
  • Take in the morning on an empty stomach. Take at least 1 hour before or at least 2 hours after breakfast.
  • Swallow whole with a drink of water.
  • Do not chew, break, or crush.
  • If you have trouble swallowing, talk with your doctor.

What do I do if I miss a dose?

  • Take a missed dose as soon as you think about it.
  • If it has been 14 hours or more since the missed dose, skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.

If OVERDOSE is suspected

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out Tacrolimus Extended-Release Capsules?

  • Store at room temperature.
  • Store in a dry place. Do not store in a bathroom.
  • Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
  • Check with your pharmacist about how to throw out unused drugs.
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