Chemical Property of Pentamidine
Chemical Property:
- Appearance/Colour:Crystalline Solid
- Vapor Pressure:1.06E-11mmHg at 25°C
- Melting Point:186 °C (dec.)
- Refractive Index:1.6620 (estimate)
- Boiling Point:539.4 °C at 760 mmHg
- PKA:pKa 11.4 (Uncertain)
- Flash Point:280 °C
- PSA：118.20000
- Density:1.2 g/cm3
- LogP:4.48290
- Storage Temp.:-20°C Freezer, Under Inert Atmosphere
- Solubility.:DMSO, Methanol (Sparingly)
- XLogP3:2.6
- Hydrogen Bond Donor Count:4
- Hydrogen Bond Acceptor Count:4
- Rotatable Bond Count:10
- Exact Mass:340.18992602
- Heavy Atom Count:25
- Complexity:376
- Purity/Quality:
-
97% *data from raw suppliers
Pentamidine *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
-
SDS file from LookChem
Useful:
- Drug Classes:Antifungal/Anthelmintic Agents
- Canonical SMILES:C1=CC(=CC=C1C(=N)N)OCCCCCOC2=CC=C(C=C2)C(=N)N
- Recent ClinicalTrials:Pentamidine + Salvage Chemo for Relapsed/Refractory Classical Hodgkin Lymphoma
- Recent EU Clinical Trials:A Phase IIa Exploratory Study of OCZ103-OS in Combination with Platinum-Gemcitabine based Doublet First Line Therapy in Stage IV Non-Small Cell Lung Cancer (NSCLC) Patients
-
Indications
Trypanosomiasis
In the treatment of early-stage Trypanosoma brucei gambiense.
Leishmaniasis
In the treatment of patients with visceral, diffuse cutaneous, or mucocutaneous leishmaniasis due to L. aethiopica and L. guyanensis who are unresponsive or intolerant to antimony preparations.
Pneumocystis carinii pneumonia
Pentamidine is also used in the prophylaxis and treatment of Pneumocystis carinii pneumonia as a second choice. Pentamidine (Pentam 300) binds to DNA and may inhibit
kinetoplast DNA replication and function. It also
may act by inhibiting dihydrofolate reductase and interfering
with polyamine metabolism. An effect on organism
respiration, especially at high doses, also may play a
role.
-
Description
Pentamidine is an aromatic diamine that is effective against protozoal diseases, such as amoebic dysentery, malaria, trypanosomiasis, and leishmaniasis. In clinical studies, it has also been shown to be an effective prophylaxis against pneumocystis pneumonia.
-
Uses
antiprotozoal, inhibits nucleic acid & protein synthesis Has been widely used as a drug to treat protozoal diseases, such as malaria, amoebic dysentery and trypanosomiasis. It has also been shown to be effective for both prophylaxis of pneumocystic carinii pneumonia (PCC) Has been widely used as a drug to treat protozoal diseases, such as malaria, amoebic dysentery and trypanosomiasis. It has also been shown to be effective for both prophylaxis of pneumocystic carinii pneumonia (PCC).
-
Therapeutic Function
Antiprotozoal
-
Clinical Use
Pentamidine is active against Pneumocystis carinii,
trypanosomes, and leishmaniasis unresponsive to pentavalent
antimonials. It is an alternative agent for the
treatment of P. carinii pneumonia. Although it is more
toxic than trimethoprim–sulfamethoxazole, it has been
widely used in patients with acquired immunodeficiency
syndrome (AIDS), in whom P. carinii infection is
common.
Pentamidine is an alternative drug for visceral leishmaniasis,
especially when sodium stibogluconate has
failed or is contraindicated. Pentamidine is also a reserve
agent for the treatment of trypanosomiasis before
the CNS is invaded. This characteristic largely restricts
its use to Gambian trypanosomiasis. Human African trypanosomiasis (early stages before CNS involvement)
Prophylaxis and therapy of Pn. jirovecii pneumonia
Visceral leishmaniasis unresponsive to pentavalent antimonials and
cutaneous leishmaniasis caused by L. guyanensis
There is limited evidence for its use in the treatment of
babesiosis.
