Monograph
P01CX01 - Pentamidine Isethionate |
Propably not porphyrinogenic |
PNP |
Rationale
Pentamidine does not inhibit or induce CYP 2C9 or 3A4.
Close monitoring of carbohydrate intake and blood glucose levels is recommended as pentamidine may cause hypoglycemia or nausea.
Chemical description
Aromatic diamidine
Therapeutic characteristics
Pentamidine is used in the treatment and prevention of Pneumocystis carinii (Pneumocystis jiruveci)- pneumonia in immunocompromised patients.
It is also used against Leishmaniasis and early phase African sleeping sickness.
It is administered intravenously, intramuscularly or by inhalation of aerosol.
Nausea is a common side effect of pentamidine.
Use of pentamidine is reported to induce hypoglycemia associated with inappropriately high plasma insulin concentrations. Development of hyperglycemia and insulin dependent diabetes mellitus may follow. It is suggested that this is due to β-cell destruction caused by pentamidine (Manjula 1993).
Metabolism and pharmacokinetics
When administered parentally, pentamidine is widely distributed in the body. Half-life is given to be about 6 hours (SPC), but is prolonged following repeated dosing (Conte 1991).
Pentamidin is a substrate of CYP 2C19 (Afrin 2011) and 2D6 and 1A1 (Li 2003).
In an in vitro study no or only minor inhibition of CYP 1A2, 2A6, 2C9, 2C19, 2E1 or 3A4 was observed (Bürenheide 2008). The drug is not listed as an inducer of CYP3A4 or other major CYP enzymes (FDA, Hisaka 2010, Isoherranen 2008, Pelkonen 2008).
Published experience
Uneventful use by one patient with acute porphyria is described in a case report by Barone (2001).
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Value of preemptive CYP2C19 genotyping in allogeneic stem cell transplant patients considered for pentamidine administration.
Afrin LB, Afrin JB. Clin Transplant. 2011 May-Jun;25(3):E271-5. |
21299635 |
| 2. | The tolerability of newer immunosuppressive medications in a patient with acute intermittent porphyria.
Barone GW, Gurley BJ, et al. J Clin Pharmacol. 2001 Jan;41(1):113-5. |
|
| 3. | Inhibitory effects on cytochrome p450 enzymes of pentamidine and its amidoxime pro-drug.
Bürenheide A, Kunze T et al. Basic Clin Pharmacol Toxicol. 2008 Jul;103(1):61-5. |
18346045 |
| 4. | Pharmacokinetics of intravenous pentamidine in patients with normal renal function or receiving hemodialysis.
Conte JE Jr. J Infect Dis. 1991 Jan;163(1):169-75. |
3680992 |
| 5. | Prediction of pharmacokinetic drug-drug interaction caused by changes in cytochrome P450 activity using in vivo information.
Hisaka A, Ohno Y, et al. Pharmacol Ther. 2010 Feb;125(2):230-48. |
|
| 6. | Qualitative analysis of the role of metabolites in inhibitory drug-drug interactions: literature evaluation based on the metabolism and transport drug interaction database.
Isoherranen N, Hachad H, et al. Chem Res Toxicol. 2009 Feb;22(2):294-8 |
|
| 7. | Identification of human cytochrome P(450)s that metabolise anti-parasitic drugs and predictions of in vivo drug hepatic clearance from in vitro data.
Li XQ, Björkman A et al. Eur J Clin Pharmacol. 2003 Sep;59(5-6):429-42. |
12920490 |
| 8. | Pandit, MD et al. Drug-Induced Disorders of Glucose Tolerance.
Manjula K. Ann Intern Med. 1993;118(7):529-539993;118(7):529-539. |
|
| 9. | Inhibition and induction of human cytochrome P450 enzymes: current status.
Pelkonen O, Turpeinen M, et al. Arch Toxicol. 2008 Oct;82(10):667-715. |
18618097 |
| * | Government bodies | |
| 10. | U.S Food and Drug Administration (FDA)
|
|
| * | Summary of Product Characteristics | |
| 11. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Pentacarinat.
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