pentamidine isethionate

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Related to pentamidine isethionate: NebuPent

pentamidine isethionate

NebuPent, Pentacarinat (UK), Pentam 300

Pharmacologic class: Antiprotozoal

Therapeutic class: Anti-infective

Pregnancy risk category C


Unknown. May interfere with nuclear metabolism and synthesis of DNA, RNA, and proteins.


Aerosol: 300 mg

Injection: 300 mg/vial

Indications and dosages

Pneumocystis jiroveci pneumonia

Adults and children ages 5 and older: 4 mg/kg I.V. or deep I.M. daily for 14 days

To prevent P. jiroveci pneumonia in high-risk patients with human immunodeficiency virus

Adults: 300 mg by inhalation once q 4 weeks using Respigard II nebulizer

Off-label uses

• Trypanosomiasis
• Visceral leishmaniasis


• History of anaphylaxis from pentamidine or diamidine compounds (inhalation only)

(Note: No absolute contraindications exist for patients with P. jiroveci.)


Use cautiously in:
• anemia, blood dyscrasias, hepatic or renal disease, hypoglycemia, diabetes mellitus, ventricular tachycardia, hypocalcemia, hypertension, hypotension
• pregnant or breastfeeding patients
• children (safety and efficacy of inhalation solution not established).


• For I.V. infusion, dilute 300 mg-vial with sterile water for injection. Withdraw prescribed dosage, then dilute further in 50 to 250 ml of dextrose 5% in water; infuse over 60 to

120 minutes.
• For I.M. use, dilute 300 mg-vial with 3 ml of sterile water for injection. Withdraw prescribed dosage; administer deep I.M. using Z-track method.
• Keep patient supine during I.M. or I.V. administration to minimize hypotension.
• For inhalation, dilute in 6 ml of sterile water and administer through nebulizer at a flow rate of 6 L/minute from 50-psi compressed air source. Don't mix inhalation solution with other drugs.

Adverse reactions

CNS: headache, disorientation, hallucinations, dizziness, confusion, fatigue, neuralgia

CV: chest pain, ECG abnormalities, syncope, vasodilation, vasculitis, phlebitis, hypertension, palpitations, arrhythmias, severe hypotension

EENT: pharyngitis

GI: nausea, vomiting, diarrhea, abdominal pain, anorexia, acute pancreatitis

Hematologic: anemia, leukopenia, thrombocytopenia

Metabolic: hypocalcemia, hypergly-cemia, hypoglycemia, hyperkalemia Musculoskeletal: myalgia

Respiratory: cough, dyspnea, congestion, pneumothorax, bronchospasm

Skin: rash, night sweats, urticaria, sterile abscess or induration at injection site

Other: metallic or bad taste, fever, chills, pain at injection site or elsewhere, edema, allergic reactions


Drug-diagnostic tests.Blood urea

nitrogen, creatinine, liver function tests,

potassium: increased values

Calcium, hemoglobin, hematocrit,

platelets, white blood cells: decreased levels

ECG: alterations

Glucose: increased or decreased level

Patient monitoring

Closely monitor blood pressure and blood glucose. Watch for arrhythmias and evidence of pulmonary infection, blood dyscrasias, and pancreatitis during and after I.M. or I.V. administration, until patient is stable. (Severe, life-threatening reactions may occur.)
• Assess I.V. site closely during and after I.V. administration. Know that sterile abscess, pain, or induration may occur at injection site.
• Evaluate neurologic status.
• Monitor CBC (including platelet count), calcium and potassium levels, and kidney and liver function tests.

Patient teaching

• Explain purpose of therapy. Stress importance of completing entire course of treatment.

Teach patient to recognize and immediately report serious cardiovascular and neurologic reactions, abdominal pain, and easy bruising or bleeding.
• Teach patient how to use aerosol.
• Tell patient to notify prescriber if infection worsens.
• Advise patient to minimize GI upset by eating small, frequent servings of food and drinking plenty of fluids.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the tests mentioned above.

pen·tam·i·dine i·se·thi·o·nate

(pen-tam'i-dēn īs'ĕ-thī'ō-nāt),
A toxic but effective drug for prophylaxis and treatment of early stages of both types of African sleeping sickness. It does not cross the blood-brain barrier and is not effective in the treatment of the neurologic stage of the disease. Also used to treat resistant leishmaniasis and Pneumocystis pneumonia.

pentamidine isethionate

a parenteral antiprotozoal drug.
indications It is prescribed in the treatment and prevention of pneumonia caused by Pneumocystis jiroveci, particularly in patients who have human immunodeficiency syndrome. It can also be used to treat trypanosomiasis and visceral leishmaniasis.
contraindications To reduce the risk of toxicity, the following tests must be carried out before, during, and after therapy: blood urea nitrogen, serum creatinine, blood glucose, complete blood and platelet counts, liver function, serum calcium, and electrocardiogram.
adverse effects Among adverse reactions to the injectable form of pentamidine are hypotension, hypoglycemia, leukopenia, thrombocytopenia, cardiac arrhythmias, acute renal failure, hypocalcemia, Stevens-Johnson syndrome, elevated serum creatinine level, elevated liver function results, pain or induration at the injection site, nausea, anorexia, fever, and rash. Some of these side effects are reduced by an aerosol formulation of pentamidine, but the aerosol causes other adverse effects, including fatigue, dizziness, and dyspnea.

pentamidine isethionate

a diamidine derivative effective against protozoa. Used in the treatment of Babesia, Leishmania and Pneumocystis spp.
References in periodicals archive ?
Reference drugs included sodium stibogluconate (Pentostam; Sigma), amphotericin B (Fungizone; Squib), pentamidine isethionate (Sigma), trifluralin (Sigma) and acriflavine (Sigma).
Parenteral therapy (pentavalent antimonials, pentamidine isethionate, or amphotericin B) was not used because of adverse effects of these drugs.
That division housed the Parasitic Diseases Drug Service and requests for pentamidine isethionate to treat PCP in other similar patients in New York had been called to the attention of these scientists by the CDC employee who administered the distribution of this drug (which was not yet licensed and was available in the United States only from CDC).
Other drugs commonly used for HIV infection that have caused cutaneous reactions are dapsone, ketoconazole, pyrimethamine (Daraprim), amphotericin B (Fungizone), and pentamidine isethionate (NebuPent, Pentam 300).
Three test groups were established: i) positive control containing 1% DMSO in RPMI-1640 with pentamidine isethionate (Pentacarinat[R], Aventis Pharma S.
Embryofetal effects of pentamidine isethionate administered to pregnant Sprague-Dawley rats.
These patients were treated with 1 or 2 courses of either 3 intravenous or 2 intramuscular injections of pentamidine isethionate (4 mg/kg on alternate days).
Patients were treated with 4 intravenous injections of pentamidine isethionate (4 mg/kg every other day) and were cured without recurrence within 2 years.
Although pentavalent antimony is the recommended treatment for American CL, pentamidine isethionate is widely used in French Guiana.
Management of American cutaneous leishmaniasis: outcome of high-dose pentamidine isethionate treatment of 326 cases.
All tests were performed in triplicate and pentamidine isethionate (Eurofarma) was used as the reference drug (Leon et al.