Drug/Small Molecule:
pentamidine

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

Links to Unannotated Labels

These links are to labels associated with pentamidine that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105217

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • 1,3-bis(4-amidinophenoxy)pentane
  • 4, 4'-Diamidinodiphenoxypentane
  • PNT
  • Pentamide
  • Pentamidine Isethionate
Trade Names
  • NebuPent
  • Pentacarinat
  • Pentam
  • Pentam 300
  • Pneumopent
Brand Mixture Names

PharmGKB Accession Id:
PA450850

Description

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.

Source: Drug Bank

Indication

For the treatment of pneumonia due to Pneumocystis carinii.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

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.

Source: Drug Bank

Pharmacology

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. Little is known about the drug's pharmacokinetics. The medication is also useful in Leishmaniasis and in prophylaxis against sleeping sickness caused by Trypanosoma brucei gambiense. Hydration before treatment lessens the incidence and severity of side effects, which include liver or kidney dysfunction, hypertension, hypotension, hypoglycemia, hypocalemia, leukopenia, thrombcytopenia, anemia, and allergic reaction. It is generally well-tolerated.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic.

Source: Drug Bank

Protein Binding

69%

Source: Drug Bank

Absorption

Absorbed poorly through the gastrointestinal tract and is usually administered parenterally.

Source: Drug Bank

Half-Life

9.1-13.2 hours

Source: Drug Bank

Toxicity

Symptoms of overdose include pain, nausea, anorexia, hypotension, fever, rash, bad taste in mouth, confusion/hallucinations, dizziness, and diarrhea.

Source: Drug Bank

Chemical Properties

Chemical Formula

C19H24N4O2

Source: Drug Bank

Isomeric SMILES

c1cc(ccc1C(=N)N)OCCCCCOc2ccc(cc2)C(=N)N

Source: OpenEye

Canonical SMILES

NC(=N)C1=CC=C(OCCCCCOC2=CC=C(C=C2)C(N)=N)C=C1

Source: Drug Bank

Average Molecular Weight

340.4195

Source: Drug Bank

Monoisotopic Molecular Weight

340.189926032

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Antiarrhythmic Pathway, Pharmacodynamics
    Pharmacodynamic pathway of antiarrhythmic drugs in a stylized cardiac myocyte.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

EvidenceGene
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
KCNH2

Drug Targets

Gene Description
TRDMT1 (source: Drug Bank)

Drug Interactions

Drug Description
pentamidine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
pentamidine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
mesoridazine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
mesoridazine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
quinupristin This combination presents an increased risk of toxicity (source: Drug Bank)
thioridazine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
thioridazine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
ziprasidone Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
ziprasidone Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
pentamidine This combination presents an increased risk of toxicity (source: Drug Bank)
pentamidine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
pentamidine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
pentamidine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
pentamidine May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank)
pentamidine May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank)
pentamidine Ticlopidine may decrease the metabolism and clearance of Pentamidine. Consider alternate therapy or monitor for adverse/toxic effects of Pentamidine if Ticlopidine is initiated, discontinued or dose changed. (source: Drug Bank)
pentamidine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank)
pentamidine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
pentamidine Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank)
pentamidine Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank)
pentamidine Additive risk of pancreatitis. Concomitant therapy should be avoided. (source: Drug Bank)
pentamidine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated. (source: Drug Bank)
pentamidine Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank)

Curated Information ?

EvidenceDisease
No Dosing Guideline available DL No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Torsades de Pointes

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
May Prevent
Contraindicated With

Publications related to pentamidine: 7

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The genetics of pro-arrhythmic adverse drug reactions. British journal of clinical pharmacology. 2014. Petropoulou Evmorfia, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. Journal of medicinal chemistry. 2011. Kido Yasuto, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
KCNH2 pharmacogenomics summary. Pharmacogenetics and genomics. 2010. Oshiro Connie, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Drug-induced long QT syndrome. Pharmacological reviews. 2010. Kannankeril Prince, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Comparative evaluation of HERG currents and QT intervals following challenge with suspected torsadogenic and nontorsadogenic drugs. The Journal of pharmacology and experimental therapeutics. 2006. Katchman Alexander N, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pentamidine reduces hERG expression to prolong the QT interval. British journal of pharmacology. 2005. Cordes Jason S, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Options in the management of pneumonia caused by Pneumocystis carinii in patients with acquired immune deficiency syndrome and intolerance to trimethoprim/sulfamethoxazole. Southern medical journal. 1996. Korraa H, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00738
PDB:
PNT
ChEBI:
45081
KEGG Compound:
C07420
PubChem Compound:
4735
PubChem Substance:
150570
46508562
Drugs Product Database (DPD):
2183080
ChemSpider:
4573
HET:
PNT
Therapeutic Targets Database:
DAP000764

Clinical Trials

These are trials that mention pentamidine and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.