Drug information of Pentamidine

Pentamidine

Drug group:

Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of pneumocystis pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.

Mechanism of effect

The mode of action of pentamidine is not fully understood. It is thought that the drug interferes with nuclear metabolism producing inhibition of the synthesis of DNA, RNA, phospholipids, and proteins.

Pharmacodynamic

Pentamidine is an antiprotozoal agent. It is an aromatic diamidine, and is known to have activity against Pneumocystis carinii. The exact nature of its antiprotozoal action is unknown. in vitro studies with mammalian tissues and the protozoan Crithidia oncopelti indicate that the drug interferes with nuclear metabolism producing inhibition of the synthesis of DNA, RNA, phospholipids and proteins.

Pharmacokinetics

Absorbed poorly through the gastrointestinal tract and is usually administered parenterally. Volume of distribution Is not Available. Protein binding is 69%. Metabolism is Hepatic. Route of elimination is not Available. Half life is 9.1-13.2 hours

Dosage

Pneumocystis jirovecii pneumonia (PCP), treatment:

IM, IV: 4 mg/kg once daily for 14 to 21 days

HIV-infected patients (alternative to preferred therapy):

IV: 4 mg/kg/dose once daily for 21 days; may reduce to 3 mg/kg/dose once daily if toxicity occurs .

Trypanosomiasis (off-label use):

IM, IV: 4 mg/kg once daily for 7 to 10 days.

Drug contraindications

hypersensitivity to this drug

Side effects

nausea , skin rush

Alerts

  • Hypotension: Severe hypotension (some fatalities) has been observed, even after a single dose. May occur with either IV or IM administration, although more common with rapid IV administration. Monitor blood pressure during (and after) infusion.
  • QT prolongation: May cause QT prolongation and subsequent torsade de pointes; avoid use in patients with diagnosed or suspected congenital long QT syndrome.
  • Stevens-Johnson syndrome: Has been reported with use.
  • Cardiovascular disease: Use with caution in patients with preexisting cardiovascular disease; hyper-/hypotension and arrhythmia, including ventricular tachycardia (eg, torsade de pointes) have been reported.
  • Diabetes: Use with caution in patients with diabetes mellitus; hyper-/hypoglycemia and pancreatic islet cell necrosis with hyperinsulinemia has been reported. Symptoms may occur months after therapy; monitor blood glucose daily on therapy and periodically thereafter.
  • Extravasation: Intravenous pentamidine is an irritant with vesicant-like properties. Ensure proper needle or catheter placement prior to and during infusion; avoid extravasation. Ulceration, tissue necrosis, and/or sloughing have been reported with extravasation.
  • Hematologic disorders: Use with caution in patients with current evidence and/or prior history of hematologic disorders; anemia, leukopenia and/or thrombocytopenia have been reported. Concurrent use with other bone marrow suppressants may increase the risk for myelotoxicity.
  • Hepatic impairment: Use with caution in patients with hepatic impairment.
  • Hypocalcemia: Use with caution in patients with hypocalcemia.
  • Pancreatitis: Use with caution in patients with a history of pancreatic disease or elevated amylase/lipase levels; acute pancreatitis (with fatality) has been reported. Discontinue pentamidine if signs/symptoms of acute pancreatitis occur.
  • Renal impairment: Use with caution in patients with renal impairment.

Points of recommendation

To make sure this medicine is safe for you, tell your doctor if you have:

  • If you have an allergy to this medicine or any other part of it.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.

Importance of completing full course of therapy.

When used for the prevention of PCP, importance of informing clinicians if symptoms of a pulmonary infection (cough, fever, dyspnea) occur.

Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

Importance of informing patients of other important precautionary information.

Pregnancy level

C


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