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All about: Posaconazole

Big Image Pronouncation: (POE-sa-KON-a-zole)
Class: Antifungal

Trade Names:
Noxafil
- Suspension, oral 40 mg/mL

Mechanism of Action

Pharmacology

Blocks the synthesis of ergosterol, a key component of fungal cell membranes.

Pharmacokinetics

Absorption

T max is approximately 3 to 5 h. Steady-state plasma concentrations are reached in 7 to 10 days.

Distribution

Vd is 1,774 L, suggesting extensive extravascular distribution and penetration into body tissues. Posaconazole is over 98% protein bound, primarily to albumin.

Metabolism

Metabolism mainly involves glucuronide conjugation via uridine diphosphate glucuronidation.

Elimination

Elimination is approximately 71% in feces and 13% in urine in up to 120 h. The mean t ½ is 35 h.

Indications and Usage

Prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections because of severe immunocompromise; treatment of oropharyngeal candidiasis refractory to itraconazole and/or fluconazole.

Contraindications

Coadministration of ergot derivatives; coadministration with CYP3A4 substrates, including cisapride, halofantrine, pimozide, or quinidine; hypersensitivity to any component of the product.

Dosage and Administration

Prophylaxis of Invasive Fungal Infections
Adults and children 13 yr of age and older

PO 200 mg tid. The duration is based on recovery from neutropenia or immunosuppression.

Oropharyngeal Candidiasis
Adults and children 13 yr of age and older

PO Start with a loading dose of 100 mg bid on the first day, then 100 mg once daily for 13 days.

Oropharyngeal Candidiasis Refractory to Itraconazole and/or Fluconazole
Adults and children 13 yr of age and older

PO 400 mg bid. Duration based on severity of the underlying disease and clinical response.

General Advice

  • Shake oral suspension well before using.
  • Administer with a full meal or liquid nutritional supplement.
  • A measured dosing spoon marked for 2.5 and 5 mL doses is provided.

Storage/Stability

Store at 59° to 86°F. Do not freeze.

Drug Interactions

Calcium channel blockers metabolized through CYP3A4

Posaconazole may elevate plasma levels of these agents, increasing the risk of toxicity.

Cimetidine, phenytoin, rifabutin

Posaconazole plasma levels may be decreased; if possible, avoid coadministration.

Cyclosporine, sirolimus, tacrolimus

Plasma levels of these drugs may be elevated by posaconazole, increasing the risk of serious adverse reactions, including nephrotoxicity.

CYP3A4 substrates astemizole, cisapride, halofantrine, pimozide, quinidine, or terfenadine

Plasma levels of these agents may be elevated by posaconazole, leading to QTc prolongation and increasing the risk of life-threatening cardiac arrhythmias, including torsades de pointes. Coadministration with posaconazole is contraindicated.

Ergot derivatives

Plasma levels may be elevated by posaconazole, increasing the risk of ergotism. Coadministration with posaconazole is contraindicated.

HMG-CoA reductase inhibitors (statins) metabolized through CYP3A4

Posaconazole may elevate plasma levels of these agents, increasing the risk of adverse reactions (eg, rhabdomyolysis). Statin dose reduction is recommended.

Midazolam, phenytoin, rifabutin

Plasma concentrations of these drugs may be elevated by posaconazole.

Vinca alkaloids

Plasma concentrations may be elevated by posaconazole, increasing the risk of neurotoxicity.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension (18%); hypotension (14%); tachycardia (12%); QT/QTc prolongation (4%).

CNS

Headache (28%); fatigue, insomnia (17%); dizziness (11%); anxiety (9%); weakness (8%); asthenia (2%); somnolence, tremor (1%).

Dermatologic

Rash (19%); pruritus (11%); increased sweating (2%).

EENT

Pharyngitis (12%); blurred vision, taste perversion (1%).

GI

Diarrhea (42%); nausea (38%); vomiting (29%); abdominal pain (27%); constipation (21%); mucositis (17%); anorexia (15%); dyspepsia (10%); dry mouth, flatulence (1%).

Genitourinary

Vaginal hemorrhage (10%); increased blood creatinine (2%).

Hepatic

Bilirubinemia (10%); increased ALT, AST, or gamma-glutamyl transferase (3%); hepatitis (1%).

Hematologic-Lymphatic

Thrombocytopenia (29%); anemia (25%); neutropenia (23%); febrile neutropenia (20%); petechiae (11%).

Metabolic-Nutritional

Hypokalemia (30%); hypomagnesemia (18%); hyperglycemia (11%); increased alkaline phosphatase (2%); decreased weight, dehydration (1%).

Musculoskeletal

Rigors (20%); musculoskeletal pain (16%); arthralgia (11%); back pain (10%).

Respiratory

Coughing (24%); dyspnea (20%); epistaxis (14%); upper respiratory tract infection (7%); pneumonia (3%).

Miscellaneous

Fever (45%); bacteremia (18%); herpes simplex, leg edema (15%); cytomegalovirus infection (14%); edema (9%); oral candidiasis (1%).

Precautions

Monitor

Monitor patients who have severe renal function impairment, severe diarrhea, or vomiting for breakthrough fungal infections. Monitor patients who develop abnormal LFTs during therapy for development of more severe hepatic injury.


Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 13 yr of age.

Hypersensitivity

Because there is no information regarding cross-sensitivity with other azole antifungal agents, use with caution in patients with hypersensitivity to other azoles.

Overdosage

Symptoms

No adverse reactions were noted with doses up to 1,600 mg/day.

Patient Information

  • Advise patient to read the patient information leaflet before using product the first time and with each refill.
  • Explain name, dose, action, possible drug interactions, and potential adverse reactions of the drug.
  • Obtain patient history, including drug history and any known allergies.
  • Instruct patient to take exactly as prescribed and not to change the dose or discontinue therapy unless advised by health care provider.
  • Instruct patient to take this medication with a full meal or liquid nutritional supplement.
  • Advise patient to inform health care provider if severe diarrhea or vomiting develops because these conditions may change blood levels of the drug.
  • Caution patient to not take any prescription or OTC medications, herbal preparations, or dietary supplements unless advised by health care provider.
  • Advise women to notify health care provider if pregnant, planning to become pregnant, or breast-feeding.
  • Advise patient that follow-up visits may be necessary and to keep appointments.

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