caspofungin acetate


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caspofungin acetate

Cancidas

Pharmacologic class: Echinocandin

Therapeutic class: Antifungal

Pregnancy risk category C

Action

Inhibits synthesis of beta (1, 3)-D-glucan, an important component of cell wall in Aspergillus and other fungal cells. This inhibition leads to cell rupture and death.

Availability

Lyophilized powder for injection: 50 mg and 70 mg in single-use vials

Indications and dosages

Invasive aspergillosis in patients-refractory to or intolerant of other therapies

Adults ages 18 and older: 70 mg I.V. as a single loading dose on first day, followed by 50 mg/day thereafter

Children ages 3 months to 17 years: 70 mg/m2 I.V. as a single loading dose on first day, followed by 50 mg/m2/day thereafter. Maximum loading dosage and daily maintenance dosage shouldn't exceed 70 mg, regardless of calculated dosage.

Esophageal candidiasis

Adults ages 18 and older: 50 mg I.V. daily

Children ages 3 months to 17 years: 70 mg/m2 I.V. as a single loading dose on first day, followed by 50 mg/m2/day thereafter. Maximum loading dosage and daily maintenance dosage shouldn't exceed 70 mg, regardless of calculated dosage.

Candidemia and other Candida infections (intra-abdominal abscesses, peritonitis, and pleural-space infections)

Adults ages 18 and older: 70 mg I.V. as a single loading dose on first day, followed by 50 mg/day thereafter. Continue therapy for at least 14 days after last positive culture. Consistently neutropenic patient may require longer course of therapy.

Children ages 3 months to 17 years: 70 mg/m2 I.V. as a single loading dose on first day, followed by 50 mg/m2/day thereafter. Maximum loading dosage and daily maintenance dosage shouldn't exceed 70 mg, regardless of calculated dosage.

Empirical therapy for presumed fungal infections in febrile neutropenic patients

Adults ages 18 and older: 70 mg I.V. as a single loading dose on first day, followed by 50 mg/day thereafter. Continue therapy until neutropenia resolves, for at least 14 days in patients with fungal infections, or for at least 7 days after both neutropenia and symptoms resolve. If patient tolerates 50-mg dosage well but doesn't obtain adequate response, increase daily dosage to 70 mg.

Children ages 3 months to 17 years: 70 mg/m2 I.V. as a single loading dose on first day, followed by 50 mg/m2/day thereafter. Maximum loading dosage and daily maintenance dosage shouldn't exceed 70 mg, regardless of calculated dosage.

Dosage adjustment

• Moderate hepatic insufficiency (adults)

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:
• hepatic impairment
• renal insufficiency
• concurrent cyclosporine use
• pregnant or breastfeeding patients.

Administration

Don't mix with other drugs or with diluents containing dextrose.
• Reconstitute powder using 10.8 ml of normal saline solution for injection, sterile water for injection, or bacteriostatic water for injection. Mix gently until solution is clear. Add to I.V. bag or bottle containing 250 ml of normal, half-normal, or quarter-normal saline solution for injection or lactated Ringer's solution. Don't exceed concentration of 0.5 mg/ml.

Don't give by I.V. bolus.
• Administer by slow I.V. infusion over 1 hour.
• Know that in patients with human immunodeficiency virus, oral therapy may be given to help prevent oropharyngeal candidiasis relapse.
• Be aware that adults taking rifampin concurrently should receive 70-mg daily dosage.
• Know that dosage may need to be increased in patients receiving nevirapine, efavirenz, carbamazepine, dexamethasone, or phenytoin.

Adverse reactions

CNS: headache

CV: tachycardia, phlebitis, hypotension, hypertension (children)

GI: nausea, vomiting, diarrhea, abdominal pain

GU: nephrotoxicity

Hematologic: anemia

Metabolic: hypokalemia, hyperkalemia

Musculoskeletal: pain, myalgia, back pain

Respiratory: tachypnea, cough, dyspnea, crackles, pneumonia, respiratory distress (children), pleural effusion, respiratory failure

Skin: erythema, pruritus (children), rash

Other: graft-versus-host disease, central line infection (children), chills, mucosal inflammation, peripheral edema, pyrexia, infusion-related reactions, septic shock

Interactions

Drug-drug.Carbamazepine, dexamethasone, efavirenz, nelfinavir, nevirapine, phenytoin, rifampin: reduced caspofungin blood level

Cyclosporine: markedly increased caspofungin blood level, transient ALT and AST increases

Tacrolimus: possible change in tacrolimus blood level

Drug-diagnostic tests.Albumin, hematocrit, hemoglobin, magnesium, potassium, total protein (children), white blood cells: decreased levels ALP, ALT, AST, bilirubin, calcium, conjugated bilirubin, creatinine, eosinophils, glucose, urea: increased levels

Potassium: decreased or increased level (children)

Urinary red blood cells: positive

Patient monitoring

Monitor closely for signs and symptoms of infusion-related reactions (pyrexia, chills, flushing, hypotension, hypertension, tachycardia, dyspnea, tachypnea, anaphylaxis). Be prepared to provide supportive care as needed.
• Monitor I.V. site carefully for phlebitis and other complications.
• Monitor complete blood count and serum electrolyte levels. Stay alert for signs and symptoms of hypokalemia.
• Monitor vital signs, especially for tachycardia and tachypnea.
• Closely monitor liver function tests; watch for evidence of worsening hepatic function.

Patient teaching

Instruct patient to immediately report signs or symptoms of infusion-related reaction, such as fever, chills, flushing, rapid heart beat, difficult or rapid breathing, or rash.

Tell patient drug may cause problems in vein used for infusion. Tell him to immediately report pain, swelling, or other symptoms.
• Instruct patient to report headache, nausea, or other unusual or troublesome symptoms.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

References in periodicals archive ?
Caspofungin acetate (CAS) was provided by Merck & Co.
Caspofungin acetate (Cancidas, MK-0991, L-743,872) is a parenteral antifungal agent indicated in the treatment of invasive aspergillosis in patients who are intolerant of or whose infection is refractory to other antifungal therapies.
Mass balance results showed that approximately 92% of the administered radioactivity was distributed to tissues by 36 to 48 hours after a single 70-mg dose of (3H) caspofungin acetate.
3% of administered dose) of covalent binding of radiolabel in plasma following single-dose administration of (3H) caspofungin acetate, which may be due to two reactive intermediates formed during the chemical degradation of caspofungin to L-747969.
After single intravenous administration of (3H) caspofungin acetate, excretion of caspofungin and its metabolites in humans was 35% of dose in feces and 41% of dose in urine.
The overall safety of caspofungin was assessed in 631 individuals who received single or multiple doses of caspofungin acetate.