Pentamidine

What is Pentamidine?

• Pentamidine is a potent, broad spectrum anti infective agent with activity against several parasitic worms, protozoa and fungi that has been used mainly in the treatment and the prophylaxis of Pneumocystis jirovecii (formerly carinii) infection in immunodeficient persons.

Pentamidine-skeletal

Pentamidine 3D

Pentamidine-3D-balls

What are the uses of this medicine?

• Pentamidine injection (Pentacarinat; Pentam) is used to treat pneumonia caused by a fungus called Pneumocystis carinii.

Pentamidine Oral Inhalation (NebuPent) is used for the prevention of Pneumocystis jiroveci pneumonia (PJP) in high-risk, HIV-infected patients defined by one or both of the following criteria:

• a history of one or more episodes of PJP
• a peripheral CD4+ (T4 helper/inducer) lymphocyte count less than or equal to 200/mm3.

How does this medicine work?

• Pentamidine (pen tam' i deen) is an aromatic diamine that is active against a broad spectrum of infectious agents.
• Its mechanism of action is unknown, but it appears to be taken up and concentrated within microorganisms where it inhibits DNA, RNA and protein synthesis. Pentamidine has a broad spectrum of activity against several cestodes, trematodes and protozoan parasites such as Giardia, Cryptosporidium and Entamoeba.
• Pentamidine is also active against Pneumocystis jiroveci (formerly known as P. carinii), which is now considered a fungal agent.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• with a history of hypersensitivity to pentamidine isethionate.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention the following:

• aminoglycoside antibiotics such as amikacin, gentamicin, or tobramycin; amphotericin B (Abelcet, Ambisome), cisplatin, foscarnet (Foscavir), or vancomycin (Vancocin)

Is this medicine FDA approved?

• Pentamidine was approved for use in the United States in 1984 at which time a major indication was the prophylaxis and therapy of Pneumocystis jiroveci infection.
• In intervening years, pentamidine has been replaced by better tolerated and less toxic agents in treating Pneumocystis such as trimethoprim/sulfamethoxazole or dapsone with atovaquone. Pentamidine is also an alternative, second line therapy for leishmaniasis and trypanosomiasis.

How should this medicine be used?

Recommended dosage: Pentamidine injection:

• The recommended regimen for adults and pediatric patients beyond 4 months of age is 4 mg/kg once a day for 14 to 21 days.
• Therapy for longer than 21 days with pentamidine isethionate has also been used but may be associated with increased toxicity.

Pentamidine Oral Inhalation:

• The recommended adult dosage of NebuPent for the prevention of Pneumocystis jiroveci pneumonia is 300 mg once every four weeks administered via the Respirgard® II nebulizer.

Administration: Pentamidine injection:

• Pentamidine injection comes as powder to be mixed with liquid to be injected intramuscularly (into a muscle) or intravenously (into a vein) by a doctor or nurse in a medical facility.
• If it is given intravenously, then it is usually given as a slow infusion over 60 to 120 minutes.
• The length of treatment depends on the type of infection being treated.
• You should be lying down while you receive the medication.
• You should begin to feel better during the first 2 to 8 days of treatment with pentamidine.
• If your symptoms do not improve or get worse, call your doctor.

Pentamidine Oral Inhalation:

• Pentamidine comes as a solution to be inhaled using a nebulizer.
• It usually is used once every 4 weeks.
• Inhalation of pentamidine delivers the drug directly to your lungs.
• Your doctor, nurse, or pharmacist will show you how to use the nebulizer.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Oral Inhalation
• Pentamidine isethionate injection 300 mg

This medicine is available in fallowing brand namesː

• Pentamidine injection (Pentacarinat; Pentam)
• Pentamidine Oral Inhalation (NebuPent)

What side effects can this medication cause?

The most common side effects of this medicine include:

• loss of appetite
• nausea
• bad taste in the mouth
• fatigue
• cough
• dizziness
• burning sensation in your throat
• lightheadedness or faintness
• itching
• upset stomach
• vomiting
• night sweats or chills

• Pentamidine therapy is highly toxic and the side effects of intravenous therapy are often severe and can be fatal.
• These side effects include nausea, abdominal discomfort, dizziness, hypotension, tachycardia, headache, rash, fever, hypoglycemia, hyponatremia, renal insufficiency and allergic reactions, including Stevens Johnson syndrome.

What special precautions should I follow?

• Fatalities due to severe hypotension, hypoglycemia, acute pancreatitis and cardiac arrhythmias have been reported in patients treated with pentamidine isethionate, both by the IM and IV routes. The administration of the drug should, therefore, be limited to the patients in whom Pneumocystis carinii has been demonstrated. Patients should be closely monitored for the development of serious adverse reactions.
• The intravenous needle or catheter must be properly positioned and closely observed throughout the period of pentamidine isethionate administration. If extravasation occurs, the injection should be discontinued immediately and restarted in another vein. Because there are no known local treatment measures which have proven to be useful, management of the extravasation should be symptomatic.
• Pentamidine isethionate should be used with caution in patients with hypertension, hypotension, ventricular tachycardia, hypoglycemia, hyperglycemia, hypocalcemia, pancreatitis, leukopenia, thrombocytopenia, anemia, hepatic or renal dysfunction and Stevens-Johnson syndrome.
• Patients may develop sudden, severe hypotension after a single dose of pentamidine isethionate, whether given IV or IM. Therefore, patients receiving the drug should be lying down and the blood pressure should be monitored closely during administration of the drug and several times thereafter until the blood pressure is stable.
• Hyperglycemia and diabetes mellitus, with or without preceding hypoglycemia, have also occurred, sometimes several months after therapy with pentamidine isethionate. Therefore, blood glucose levels should be monitored daily during therapy with pentamidine isethionate, and several times thereafter.
• Inhalation of NebuPent may induce bronchospasm or cough. This has been noted particularly in some patients who have a history of smoking or asthma. In patients who experience bronchospasm or cough, administration of an inhaled bronchodilator prior to giving each NebuPent dose may minimize recurrence of the symptoms.
• Pentamidine is relatively toxic and therapy requires careful monitoring. Pentamidine has been associated with transient serum aminotransferase elevations during therapy and with rare instances of clinically apparent liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include: Pentamidine injection:

• hepatic function impairment
• hypotension
• cardiopulmonary arrest

Pentamidine Oral Inhalation:

• Overdosage has not been reported with NebuPent.
• The symptoms and signs of overdosage are not known.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Treatment may include cardiopulmonary resuscitation, epinephrine, atropine and intubation.
• In addition, a four hour course of charcoal hemoperfusion may reduce pentamidine serum concentration and stabilization of the patient’s condition.

Can this medicine be used in pregnancy?

• Pregnancy Category C.
• Pentamidine isethionate should not be given to a pregnant woman unless the potential benefits are judged to outweigh the unknown risks.

Can this medicine be used in children?

Pentamidine injection:

• Intravenous and intramuscular pentamidine has been described as an effective treatment for Pneumocystis carinii pneumonia (PCP) in immunocompromised pediatric patients beyond 4 months of age.

Pentamidine Oral Inhalation:

• The safety and effectiveness of NebuPent in pediatric patients (birth to 16 years of age) have not been established.

What are the active and inactive ingredients in this medicine?

Pentamidine injection: Active ingredient:

• PENTAMIDINE ISETHIONATE

Inactive ingredients:

• none

Pentamidine Oral Inhalation: Active ingredient:

• PENTAMIDINE ISETHIONATE

Inactive ingredients:

• none

Who manufactures and distributes this medicine?

• Fresenius Kabi USA, LLC

What should I know about storage and disposal of this medication?

Pentamidine injection:

• Store dry product at 20° to 25°C (68° to 77°F).
• Protect from light.
• Preservative Free.
• Discard unused portion.

Pentamidine Oral Inhalation:

• Store dry product at 20° to 25°C (68° to 77°F).
• Protect the dry product and the reconstituted solution from light.

• Dailymed label info on Pentamidine
• FDA Pentamidine

Pentamidine Resources
Latest articles Most recent articles Ongoing trials	Wikipedia