Inhalation/Respiratory Prophylaxis of Pneumocystis (carinii) jirovecii pneumonia
Adult: In HIV-positive patients: 300 mg every 4 weeks or 150 mg every 2 weeks.
Parenteral Leishmaniasis
Adult: For cutaneous leishmaniasis: 3-4 mg/kg via IM inj or IV infusion once or twice weekly until the condition resolves.
Parenteral African trypanosomiasis
Adult: For the treatment of Trypanosoma brucei gambiense infection: 4 mg/kg daily or on alternate days to a total of 7-10 injections, given via IM inj or IV infusion over 60-120 minutes.
In life threatening cases: 4 mg/kg once daily for 7-10 days then on alternate days for the remaining 14-dose course. In less severe cases: 4 mg/kg on alternate days for 14 doses.
Reconstitution
IM: Reconstitute with 3 mL of sterile water for injection. IV: Initially, reconstitute with 3-5 mL of sterile water for injection or 5% dextrose in water. Further dilute with 50-250 mL of 5% dextrose in water or 0.9% NaCl. Inhalation: Reconstitute with 6 mL of sterile water for injection.
Incompatibility
Incompatible with foscarnet.
Contraindications
Hypersensitivity.
Special Precautions
Patient with CV disease, long QT syndrome, history of ventricular arrhythmias, bradycardia, hypotension, hypertension, haematologic disorders (e.g. anaemia, leucopenia, thrombocytopenia), diabetes mellitus, hypoglycaemia, hyperglycaemia, hypocalcaemia, hypokalaemia, hypomagnesaemia, pancreatic disease, elevated amylase or lipase levels, asthma. Renal and hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Extravasation, ulcerations, tissue necrosis, hyperkalaemia, hypocalcaemia, hypomagnesaemia, hypertension, hypotension, ventricular tachycardia, QT prolongation, torsades de pointes, hyperglycaemia, pancreatic islet cell necrosis with hyperinsulinaemia, anaemia, leucopenia, thrombocytopenia; bronchospasm, cough, extrapulmonary infection with P. jirovecii. Gastrointestinal disorders: Nausea, vomiting, anorexia, dysgeusia. General disorders and administration site conditions: Discomfort and pain to indurations, abcess formation, muscle necrosis. Metabolism and nutrition disorders: Anorexia. Nervous system disorders: Dizziness, syncope. Renal and urinary disorders: Renal insufficiency, azotaemia. Reproductive system and breast disorders: Shortness of breath, wheezing. Skin and subcutaneous tissue disorders: Rash. Vascular disorders: Flushing. Potentially Fatal: Severe hypotension, hypoglycaemia, acute pancreatitis, cardiac arrhythmia.
Monitor ECG, blood pressure, LFTs, BUN, serum bilirubin, transaminases, renal function, blood glucose, serum electrolytes (e.g. K, Ca, Mg), haematologic status (e.g. CBC and platelets).
Drug Interactions
Increased risk of arrhythmias with medicines that prolong QT interval (e.g. erythromycin, amiodarone, terfenadine, fluoroquinolones, phenothiazines, TCAs). Increased risk of hypocalcaemia with foscarnet. Increased risk of pancreatitis with didanosine, stavudine, zalcitabine. Increased risk of hyperkalaemia with K sparing diuretics.
Action
Description: Mechanism of Action: Pentamidine, an aromatic diamidine derivative, antiprotozoal agent that acts by inhibition of oxidative phospohorylation and/or interference with the incorporation of nucleotides and nucleic acid into RNA and DNA. Pharmacokinetics: Absorption: Well absorbed (IM); Limited systemic absorption (inhalation). Distribution: Widely distributed in the body with high concentrations specifically in liver, kidney, adrenals, spleen, lungs, and pancreas. Excretion: Via urine (as unchanged drug). Elimination half-life: 5-8 hours (IV); 7-11 hours (IM).
Chemical Structure
Pentamidine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4735, Pentamidine. https://pubchem.ncbi.nlm.nih.gov/compound/Pentamidine. Accessed Jan. 27, 2021.
P01CX01 - pentamidine isethionate ; Belongs to the class of other agents used in the treatment of leishmaniasis and trypanosomiasis.
References
Anon. Pentamidine (Oral Inhalation). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/10/2020.Anon. Pentamidine (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/10/2020.Anon. Pentamidine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 06/10/2020.Buckingham R (ed). Pentamidine Isetionate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/10/2020.DBL Pentamidine Isethionate for Injection (Hospira Australia). MIMS Malaysia. http://www.mims.com/malaysia. Accessed 06/10/2020.Joint Formulary Committee. Pentamidine Isetionate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/10/2020.Nebupent (Fresenius Kabi USA, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 06/10/2020.Pentacarinat 300 mg Powder for Solution for Injection/Infusion (Aventis Pharma Limited). MHRA. https://products.mhra.gov.uk/. Accessed 06/10/2020.Pentam 300 (Fresenius Kabi USA, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 06/10/2020.
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