Paromomycin

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Paromomycin
Paromomycin structure.svg
Paromomycin ball-and-stick.png
Clinical data
Trade names Catenulin, Aminosidine, others[2]
AHFS/Drugs.com Monograph
MedlinePlus a601098
Pregnancy
category
  • US: N (Not classified yet)
  • C
Routes of
administration
By mouth, intramuscular, topical[1]
ATC code A07AA06 (WHO)
Legal status
Legal status
Pharmacokinetic data
Bioavailability Poorly absorbed in the GI tract
Metabolism Not Available
Biological half-life ?
Excretion Fecal
Identifiers
Synonyms monomycin, aminosidine[3]
CAS Number 1263-89-4 YesY
PubChem (CID) 441375
DrugBank DB01421 YesY
ChemSpider 390117 YesY
ChEBI CHEBI:7934 YesY
ChEMBL CHEMBL370143 N
ECHA InfoCard 100.028.567
Chemical and physical data
Formula C23H47N5O18S
Molar mass 615.629 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

Paromomycin is an antibiotic used to treat a number of infections including amebiasis, giardiasis, leishmaniasis, and tapeworm infection. It is a first line treatment for amebiasis or giardiasis during pregnancy. Otherwise it is generally a second line treatment option. It is used by mouth, applied to the skin, or by injection into a muscle.[1]

Common side effects when taken by mouth include loss of appetite, vomiting, abdominal pain, and diarrhea. When applied to the skin side effects include itchiness, redness, and blisters. When given by injection there may be fever, liver problems, or hearing loss.[1] Use during breastfeeding appears to be safe.[4] Paromomycin is in the aminoglycoside family of medications and causes bacterial death by stopping the making of protein.[1]

Paromomycin was discovered from Streptomyces krestomuceticus in the 1950s and came into medical use in 1960.[2][4] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[5] Paromomycin is available as a generic medication.[6] In India the injectable form is about 4.19 to 8.38 pounds for a course of treatment as of 2007.[4] In the United States a typical course of treatment is more than 200 USD as of 2015.[6]

Medical uses[edit]

It is an antibiotic used to treat intestinal infections such as cryptosporidiosis[7] and amoebiasis,[8] and other diseases such as leishmaniasis.[9] Paromomycin was demonstrated to be effective against cutaneous leishmaniasis in clinical studies in the USSR in the 1960s, and in trials with visceral leishmaniasis in the early 1990s.[3]

The route of administration is intramuscular injection and capsule. Paromomycin topical cream with or without gentamicin is an effective treatment for ulcerative cutaneous leishmaniasis, according to the results of a phase-3, randomized, double-blind, parallel group–controlled trial.[10]

Pregnancy and breastfeeding[edit]

The medication is poorly absorbed.[11] The effect it may have on the baby is still unknown.[12]

There is limited data regarding the safety of taking paromomycin while breastfeeding but because the drug is poorly absorbed minimal amounts of drug will be secreted in breastmilk.[13]

HIV/AIDS[edit]

There is limited evidence that paromomycin can be used in persons coinfected with HIV and Cryptosporidium. A few small trials have showed a reduction in oocyst shedding after treatment with paromomycin.[14]

Adverse effects[edit]

The most common adverse effects associated with paromomycin sulfate are abdominal cramps, diarrhea, heartburn, nausea, and vomiting. Long-term use of paromomycin increases the risk for bacterial or fungal infection. Signs of overgrowth include white patches in the oral cavities. Other less common adverse events include myasthenia gravis, kidney damage, enterocolitis, malabsorption syndrome, eosinophilia, headache, hearing loss, ringing in the ear, itching, severe dizziness, and pancreatitis.[15]

Interactions[edit]

Paromomycin belongs to the aminoglycoside drug class and therefore are toxic to the kidneys and to ears. These toxicities are additive and are more likely to occur when used with other drugs that cause ear and kidney toxicity.[16] Concurrent use of foscarnet increases the risk of kidney toxicity.[17] Concurrent use of colistimethate and paromomycin can cause a dangerous slowing of breathing known as respiratory depression, and should be done with extreme caution if necessary.[17] When used with systemic antibiotics such as paromomycin, the cholera vaccine can cause an immune response.[17] Use with strong diuretics, which can also harm hearing, should be avoided.[18] Paromomycin may have dangerous reactions when used with succinylcholine by increasing the neuromuscular effects.[19]

There are no known food or drink interactions with paromomycin.[17]

Mechanism[edit]

Paromomycin is a protein synthesis inhibitor in nonresistant cells by binding to 16S ribosomal RNA.[20] This broad-spectrum antibiotic soluble in water, is very similar in action to neomycin. Antimicrobial activity of paromomycin against Escherichia coli and Staphylococcus aureus has been shown.[21]

Pharmacokinetics[edit]

Absorption[edit]

GI absorption is poor. For IM injection, the absorption is rapid. Paromomycin will reach peak plasma concentration within one hour following an IM injection.[1] The invitro and invivo activities parallel those of neomycin.[22] Anything that impairs GI motility or any obstructions may increase the absorption of the drug. In addition structural damage such as lesions or ulcerations will tend to increase drug absorption.[23]

Distribution[edit]

Information not available.[22]

Elimination[edit]

Almost 100% of the oral dose is eliminated unchanged via feces; and if there is any absorbed drug, it is will be excreted in urine.[24]

References[edit]

  1. ^ a b c d e "Paromomycin Sulfate". The American Society of Health-System Pharmacists. Retrieved 3 December 2016. 
  2. ^ a b Publishing, William Andrew (2013). Pharmaceutical Manufacturing Encyclopedia, 3rd Edition (3 ed.). Elsevier. p. 21p. ISBN 9780815518563. 
  3. ^ a b Neal RA, Murphy AG, Olliaro P, Croft SL (1994). "Aminosidine ointments for the treatment of experimental cutaneous leishmaniasis". Transactions of the Royal Society of Tropical Medicine and Hygiene. 88 (2): 223–5. doi:10.1016/0035-9203(94)90307-7. PMID 8036682. 
  4. ^ a b c Davidson RN, den Boer M, Ritmeijer K (2008). "Paromomycin". Transactions of the Royal Society of Tropical Medicine and Hygiene. 103 (7): 653–60. doi:10.1016/j.trstmh.2008.09.008. PMID 18947845. 
  5. ^ "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Retrieved 8 December 2016. 
  6. ^ a b Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 54. ISBN 9781284057560. 
  7. ^ Sweetman S, ed. (2002). Martindale: The Complete Drug Reference (33rd ed.). London: Pharmaceutical Press. ISBN 978-0-85369-499-1. 
  8. ^ "paromomycin" at Dorland's Medical Dictionary
  9. ^ Sundar S, Jha TK, Thakur CP, Sinha PK, Bhattacharya SK (2007). "Injectable paromomycin for visceral leishmaniasis in India". N. Engl. J. Med. 356 (25): 2571–81. doi:10.1056/NEJMoa066536. PMID 17582067. 
  10. ^ Ben Salah A, Ben Messaoud N, Guedri E, Zaatour A, Ben Alaya N, Bettaieb J, Gharbi A, Belhadj Hamida N, et al. (2013). "Topical Paromomycin with or without Gentamicin for Cutaneous Leishmaniasis". N. Engl. J. Med. 368 (6): 524–32. doi:10.1056/NEJMoa1202657. PMID 23388004. 
  11. ^ Sweet, Richard L.; Gibbs, Ronald S. (2009). Infectious Diseases of the Female Genital Tract. Lippincott Williams & Wilkins. p. 364. ISBN 9780781778152. 
  12. ^ Handbook of Antimicrobial Therapy. New Rochelle, New York: The Medical Letter Inc. 2015. p. 468. ISBN 978-0-9815278-8-8. 
  13. ^ "Paromomycin Use During Pregnancy". Drugs.com. Retrieved 2016-11-10. 
  14. ^ Mandell, Douglas, and Bennett (2015). Principles and Practice of Infectious Diseases. Philadelphia, PA: Elsevier Saunders. p. 3181. ISBN 978-1-4557-4801-3. 
  15. ^ "paromomycin oral : Uses, Side Effects, Interactions, Pictures, Warnings & Dosing - WebMD". WebMD. Retrieved 2016-11-10. 
  16. ^ Principles and Practice of Infectious Diseases: Edition 8. ISBN 978-1455748013. 
  17. ^ a b c d "Micromedex". www.micromedexsolutions.com. 
  18. ^ Grayson, M. Lindsay, ed. (2012). Kucers' the use of antibiotics a clinical review of antibacterial, antifungal, antiparasitic and antiviral drugs (6th ed.). Boca Raton, FL: CRC Press. p. 2144. ISBN 9781444147520. 
  19. ^ Drug Therapy in Nursing. Lippincott Williams & Wilkins. 2009. ISBN 978-1605472706. 
  20. ^ Vicens Q, Westhof E (2001). "Crystal Structure of Paromomycin Docked into the Eubacterial Ribosomal Decoding A Site". Structure. 9 (8): 647–58. doi:10.1016/S0969-2126(01)00629-3. PMID 11587639. 
  21. ^ "Paromomycin" (pdf). Toku-E. 2010-01-12. Retrieved 2012-06-11. 
  22. ^ a b DrugBank, ed. (2016-08-17). "Paromomycin". DrugBank. 
  23. ^ Caraco Pharmaceutical Laboratories. Paromomycin sulfate capsules, USP prescribing information. Detroit, MI; 1997 Mar.
  24. ^ Product Information: Humatin(R), paromomycin sulfate capsules. Parke-Davis, Division of Warner-Lambert Company, Morris Plains, NJ, 1999