22 . May , 2019 - Wednesday
Check todays hot topics or new products

Find a Drug: Advanced

Please Sign in or Register

All about: Pentamidine Isethionate

Big Image Pronouncation: (pen-TAM-ih-deen ice-uh-THIGH-uh-nate)
Class: Antiprotozoal

Trade Names:
NebuPent
- Aerosol 300 mg

Trade Names:
Pentacarinat
- Injection 300 mg

Trade Names:
Pentam 300
- Injection 300 mg

Mechanism of Action

Pharmacology

Mechanism of action not fully understood. Interferes with synthesis of DNA, RNA, phospholipids, and proteins.

Pharmacokinetics

Absorption

Well absorbed after IM administration and detectable in the blood briefly due to extensive tissue binding.

C max is 612 ng/mL (single 2-hr IV infusion).

T max is 0.5 to 1 hr (IM), 1 to 2 hr (IV).

Distribution

Rapidly distributed with highest concentrations in liver, kidneys, adrenal glands, and spleen; smaller amount in lungs, and slow uptake into CNS and brain tissue.

Vd is 3 to 32 L/kg (at steady state).

Metabolism

Unknown in humans.

Elimination

Urine (12% as unchanged).

T 1/2 is 6.4 hr (IV), 9.1 to 13.2 hr (IM).

Clearance is 248 L/hr (IV).

Terminal t 1/2 is 2 to 4 wk.

Special Populations

Renal Function Impairment

Pentamidine may accumulate in renal failure.

Indications and Usage

Parenteral form

Treatment of Pneumocystis carinii pneumonia (PCP).

Inhalation

Prevention of PCP in high risk HIV-infected patients.

Unlabeled Uses

Treatment of trypanosomiasis and visceral leishmaniasis.

Contraindications

Parenteral form

Once diagnosis of PCP is made, there are no absolute contraindications.

Inhalation

History of anaphylactic reaction to pentamidine.

Dosage and Administration

Adults and Children

IM / IV 4 mg/kg qd for 14 days.

Adults

Inhalation 300 mg once q 4 wk administered via Respirgard II nebulizer.

General Advice

Injection
  • Dissolve contents of vial in Sterile Water for Injection or D5W as directed.
  • For IV infusion, solution may be diluted further in D5W.
  • Infuse pentamidine IV over 1 hr with patient supine to minimize severe hypotension and arrhythmias.
  • For IM administration, inject deeply and rotate sites.
Inhalation
  • Reconstitute medication for inhalation in Sterile Water for Injection. Do not mix with any other drugs.
  • Deliver aerosol dose until nebulizer chamber is empty (approximately 30 to 45 min).

Storage/Stability

  • Reconstituted aerosol preparation is stable up to 48 hr at room temperature, if protected from light source. Discard unused portion.
  • IV solutions prepared with D5W are stable at room temperature for up to 48 hr. Discard unused portion.
  • Store unopened vial at controlled room temperature (59° to 86°F). Protect from light.

Drug Interactions

Incompatibility

Do not reconstitute with saline solutions. Do not mix with other drugs.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension; ventricular tachycardia; cardiac arrhythmias; chest pain; edema; phlebitis.

CNS

Confusion; hallucinations; dizziness; fatigue; headache.

Dermatologic

Stevens-Johnson syndrome; sterile abscess, pain or induration at IM injection site; rash.

EENT

Bad or metallic taste.

GI

Nausea; anorexia; vomiting; diarrhea; abdominal pain.

Genitourinary

Acute renal failure; elevated serum creatinine.

Hematologic

Leukopenia; thrombocytopenia; anemia; pancytopenia.

Hepatic

Elevated LFT results.

Metabolic

Hypoglycemia; hypocalcemia; hyperkalemia.

Respiratory

Shortness of breath; cough; pharyngitis; chest congestion; bronchospasm; pneumothorax (generally associated with inhalation).

Miscellaneous

Neuralgia; myalgia; night sweats, chills.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy of inhalation solution not established.

Renal Function

Reduction of dosage, longer infusion time, or extension of dosing interval may be required.

Special Risk Patients

Use drug with caution in patients with hypertension, hypotension, hypoglycemia, hyperglycemia, hypocalcemia, leukopenia, thrombocytopenia, anemia, hepatic or renal dysfunction, ventricular tachycardia, pancreatitis, Stevens-Johnson syndrome.

Development of acute PCP

Acute PCP may develop despite pentamidine prophylaxis.

Fatalities

Fatalities from severe hypotension (even after one dose), hypoglycemia and cardiac arrhythmias have been reported with IM and IV routes. Monitor BP continuously throughout infusion, every 30 min for 2 hr thereafter and then q 4 hr until BP stabilizes.

Patient Information

  • Inform the patient that there may be pain at the injection site with IM administration.
  • Caution patient to avoid crowds and persons with known infections.
  • Instruct patient to report the following symptoms to health care provider: nausea, vomiting, anorexia, diarrhea, oliguria, dizziness, chest pain, or edema.
  • Advise patient that drug may cause dizziness, and to use caution while driving or performing other tasks requiring mental alertness.

Recent Drug Updates at DrugIndexOnline:





Aristopak oral and injectable Aristopak oral and injectable
Generic Name: triamcinolone (oral and injectable) (trye am SIH no lone) Brand Names: Acetocot, Aristocort, Aristopak, Aristospan Injection, Clinacort, Clinalog, Cort-K, Kenaject-40, Kenalog-10, Kenalog-40, TAC 3, Tramacort-D, Triam-A, Triam-Forte, Triamcot, Triamonide 40, Trilog, Trilone, more...

cinacalcet cinacalcet
Generic Name: cinacalcet (sin ah CAL set) Brand Names: Sensipar What is cinacalcet? Cinacalcet is an agent that increases the sensitivity of the parathyroid gland to calcium in the body. This causes a decrease in levels of parathyroid hormone (PTH), calcium, and phosphorous in the body. more...

Detrol LA Detrol LA
Some commonly used brand names are: In the U.S.— Detrol Detrol LA Category Antispasmodic (urinary bladder) Description Tolterodine (TOLE-tear-oh-deen) is used to treat bladder problems such as frequent need to urinate or loss of control of urinary function. This medicine is avail more...

Emadine Emadine
Generic Name: emedastine ophthalmic (eh MEH dah steen off THAL mick) Brand Names: Emadine What is Emadine (emedastine ophthalmic)? Emedastine is an anti-allergic medication. It inhibits processes in the body that cause allergic symptoms after exposure to an allergen. Emedastine ophthalm more...

guaifenesin/phenylephrine/phenylpropanolamine guaifenesin/phenylephrine/phenylpropanolamine
Generic Name: guaifenesin/phenylephrine/phenylpropanolamine (gwye FEN e sin/fen ill EFF rin/fen ill proe pa NOLE a meen) Brand Names: Ami-Tex, Banex, Dura-Gest, Duratex, Enomine, Entex, Fentex, Guaifenex, Phenylfenesin, Quintex What is guaifenesin/phenylephrine/phenylpropanolamine? Guaif more...

Metformin hydrochloride Metformin hydrochloride
Generic name: Metformin hydrochloride Brand names: Glucophage Why is Metformin hydrochloride prescribed? Glucophage is an oral antidiabetic medication used to treat type 2 (non-insulin-dependent) diabetes. Diabetes develops when the body proves unable to burn sugar and the unused sugar builds up more...

Neosporin Ophthalmic Ointment Ophthalmic Neosporin Ophthalmic Ointment Ophthalmic
Some commonly used brand names are: In the U.S.— Ak-Spore Ophthalmic Ointment Neocidin Ophthalmic Ointment Neosporin Ophthalmic Ointment Neotal Ocu-Spor-B Ocusporin Ocutricin Ophthalmic Ointment Ophthalmic Spectro-Sporin Triple Antibiotic In Canada— Neosporin Ophthalmic Ointment more...

Pantoprazole Delayed-Release Tablets Pantoprazole Delayed-Release Tablets
Generic Name: Pantoprazole Delayed-Release Tablets (pan-TOE-pra-zole) Brand Name: ProtonixPantoprazole Delayed-Release Tablets is used for:Treating irritation of the esophagus caused by gastroesophageal reflux disease (GERD). It may be used to treat conditions that cause your body to make too mu more...