Tuesday, September 13, 2016

Penicillin V



Class: Natural Penicillins
VA Class: AM110
CAS Number: 87-08-1
Brands: Pen-Vee K, Veetids

Introduction

Antibacterial; β-lactam antibiotic; natural penicillin.3


Uses for Penicillin V


Pharyngitis and Tonsillitis


Treatment of pharyngitis and tonsillitis caused by Streptococcus pyogenes (group A β-hemolytic streptococci).5 8 30 42 57


AAP, IDSA, AHA, and others recommend oral penicillin V or IM penicillin G benzathine as treatments of choice;5 8 30 42 57 oral cephalosporins and oral macrolides are considered alternatives.5 30 42 57 Amoxicillin sometimes used instead of penicillin V, especially for young children.5 57


A second episode can be retreated with the same or other treatment of choice;5 57 other regimens (amoxicillin and clavulanate, clindamycin, penicillin G benzathine with or without rifampin) recommended for symptomatic patients with multiple, recurrent episodes.5 30 57


Consider that multiple, recurrent episodes of symptomatic pharyngitis within several months to years may be repeated episodes of nonstreptococcal (e.g., viral) pharyngitis in a streptococcal carrier;30 57 treatment not usually recommended for streptococcal pharyngeal carriers.5 30 57


Other Streptococcal Infections


Treatment of mild to moderately severe infections (without bacteremia) caused by susceptible streptococci, including upper respiratory tract infections and scarlet fever.1 2 6 8 21 Usually active against streptococci groups A, C, G, H, L, and M.1 2 8 21


Treatment of mild to moderate respiratory tract infections caused by susceptible S. pneumoniae (MIC <0.1 mcg/mL);1 2 3 6 8 however, other penicillins (penicillin G, amoxicillin, amoxicillin and clavulanate, ampicillin and sulbactam) usually recommended when a penicillin used for treatment of these infections.5 63 64


Skin or Skin Structure Infections


Treatment of mild skin or skin structure infections caused by susceptible nonpenicillinase-producing staphylococci or susceptible streptococci (e.g., erysipelas).1 2 8


Not considered a drug of choice;6 susceptibility needs to be confirmed with in vitro testing because of high incidence of penicillinase-producing staphylococci.1 2


Prevention of Rheumatic Fever Recurrence


Prevention of recurrence of rheumatic fever (secondary prophylaxis).1 2 8 30 Continuous prophylaxis recommended following treatment of documented rheumatic fever (even if manifested solely by Sydenham chorea) and in those with evidence of rheumatic heart disease.8 30


AHA recommends IM penicillin G benzathine, oral penicillin V, or oral sulfadiazine for such prophylaxis.30


Prevention of Bacterial Endocarditis


Prevention of bacterial endocarditis in patients with congenital heart disease or rheumatic or other acquired valvular heart disease undergoing certain dental or upper respiratory tract procedures.1


Not a drug of choice; AHA recommends amoxicillin for prevention of bacterial endocarditis in high- or moderate-risk patients undergoing certain dental, oral, respiratory tract, or esophageal procedures.65


Consult most recent AHA recommendations for specific information on which cardiac conditions are associated with high or moderate risk of endocarditis and which procedures require prophylaxis.65


Prevention of S. pneumoniae Infections in Asplenic Individuals


Prevention of S. pneumoniae infections in children with anatomic or functional asplenia (e.g., congenital, as the result of sickle cell disease or splenectomy),4 5 8 58 59 62 children with malignant neoplasms or thalassemia,5 8 and asplenic adults (e.g., after splenectomy for trauma).24 62


Usually drug of choice for prophylaxis in asplenic children;5 60 62 some experts recommend amoxicillin.5


Children at increased risk for pneumococcal infections should receive pneumococcal 7-valent conjugate vaccine and pneumococcal 23-valent polysaccharide vaccine.5 60 61 62 Long-term anti-infective prophylaxis recommended for children with anatomic or functional asplenia regardless of vaccination status.5 60 61 62


Necrotizing Ulcerative Gingivitis


Treatment of mild to moderate acute necrotizing ulcerative gingivitis and pharyngitis (Vincent’s infection, trench mouth, Fusobacterium gingivitis or pharyngitis).1 2


Anthrax


An alternative for postexposure prophylaxis of anthrax following exposure to Bacillus anthracis spores (inhalational anthrax).33 Ciprofloxacin or doxycycline are initial drugs of choice for postexposure prophylaxis following suspected or confirmed bioterrorism-related anthrax exposure.33 36 37 38 39 41 If penicillin susceptibility is confirmed, consideration can be given to changing prophylaxis to a penicillin in infants and children and in pregnant or lactating women;33 36 amoxicillin usually is recommended.36 37 39


Treatment of mild, uncomplicated cutaneous anthrax caused by susceptible B. anthracis that occurs as the result of naturally occurring or endemic exposure to anthrax.34 36 If cutaneous anthrax occurs in the context of biologic warfare or bioterrorism, initial drugs of choice are ciprofloxacin or doxycycline.36 38 41 If penicillin susceptibility is confirmed, consideration can be given to changing to a penicillin in infants and children or in pregnant or lactating women; amoxicillin usually is recommended.36 38


Actinomycosis


Follow-up treatment of actinomycosis after initial treatment with parenteral penicillin G or ampicillin.5 8 20 22 32


Treatment of mild cervicofacial actinomycosis.32


Rat-bite Fever


Follow-up treatment of rat-bite fever caused by Streptobacillus moniliformis in afebrile patients who respond to initial treatment with parenteral penicillin G.5


Whipple’s Disease


Follow-up treatment of Whipple’s disease after initial therapy with parenteral penicillin G.3 8


Penicillin V Dosage and Administration


Administration


Oral Administration


Administer orally.1 2


May be given with meals, but maximum absorption achieved when given at least 1 hour before or 2 hours after meals.13 14


Should not be used for initial treatment of severe infections1 2 5 and should not be relied on in patients with nausea, vomiting, gastric dilatation, cardiospasm, or intestinal hypermotility.1 2


Reconstitution

Reconstitute powder for oral solution at the time of dispensing by adding the amount of water specified on the bottle to provide a solution containing 125 or 250 mg of penicillin V per 5 mL.1 2 Shake bottle to loosen powder and then add water in 2 portions;1 2 shake well after each addition.1 2


Dosage


Available as the potassium salt.1 2 Dosage usually expressed as mg of penicillin V,1 2 but may be expressed in terms of USP penicillin V units.1 2


Potency of penicillin V potassium preparations containing 125, 250, or 500 mg of penicillin V is approximately equivalent to 200,000, 400,000, or 800,000 USP penicillin V units, respectively.1 2


Pediatric Patients


Pharyngitis and Tonsillitis

Oral

Children: 250 mg 2 or 3 times daily for 10 days.5 7 30 57


Adolescents ≥12 years of age: 500 mg 2 or 3 times daily for 10 days5 57 or 250 mg 3 or 4 times daily for 10 days.57


Follow-up throat cultures not indicated in asymptomatic patients,5 30 57 but recommended 2–7 days after treatment in those who remain symptomatic, develop recurring symptoms, or have a history of rheumatic fever and are at unusually high risk for recurrence.30 57


Other Streptococcal Infections

Oral

Adolescents ≥12 years of age: 125–250 mg every 6 to 8 hours for 10 days for mild to moderate infections.1 2


Adolescents ≥12 years of age: 250–500 mg every 6 hours for mild to moderate infections caused by susceptible S. pneumoniae;1 2 continue until afebrile for at least 2 days.1 2


Skin and Skin Structure Infections

Oral

Adolescents ≥12 years of age: 250–500 mg every 6–8 hours.1 2 8


Prevention of Rheumatic Fever Recurrence

Oral

125–250 mg twice daily.1 2 30 AHA recommends 250 mg twice daily.30


Long-term, continuous prophylaxis for ≥ 5 years or into adulthood required.2 5 8 30 (See Prevention of Rheumatic Fever Recurrence under Dosage and Administration.)


Prevention of Bacterial Endocarditis

Patients Undergoing Certain Dental or Upper Respiratory Tract Procedures

Oral

Children weighing <27 kg: 1 g given 1 hour prior to the procedure and 500 mg 6 hours later.1


Children weighing ≥27 kg: 2 g given 1 hour prior to the procedure and 1 g 6 hours later.1


Prevention of S. pneumonia Infections in Asplenic Individuals

Oral

Children <5 years of age: 125 mg twice daily.5 62


Children ≥5 years of age: 250 mg twice daily.5


In infants with sickle cell anemia, initiate penicillin V prophylaxis as soon as diagnosis is established (preferably by 2 months of age);5 60 continue until approximately 5 years of age.5 60 Appropriate duration in children with asplenia from other causes unknown;5 some experts recommend that asplenic children at high risk receive prophylaxis throughout childhood and into adulthood.5


Necrotizing Ulcerative Gingivitis

Oral

Adolescents ≥12 years of age: 250–500 mg every 6–8 hours for mild to moderate infections.1 2


Anthrax

Postexposure Prophylaxis

Oral

50 mg/kg daily given in 4 divided doses for 60 days for postexposure prophylaxis following exposure to B. anthracis spores (inhalational anthrax); use only if penicillin susceptibility confirmed.33


Cutaneous Anthrax

Oral

25–50 mg/kg daily given in 2 or 4 divided doses for treatment of uncomplicated cutaneous anthrax resulting from naturally occurring or endemic exposure to anthrax.34


7–10 days of treatment may be adequate if cutaneous anthrax occurred as the result of natural or endemic exposures; 60 days of treatment necessary if it occurred as the result of exposure to aerosolized anthrax spores (e.g., in context of biologic warfare or bioterrorism).36 38


Adults


Pharyngitis and Tonsillitis

Oral

500 mg 2 or 3 times daily for 10 days5 30 42 57 or 250 mg 3 or 4 times daily for 10 days.57


Other Streptococcal Infections

Oral

125–250 mg every 6 to 8 hours for 10 days for mild to moderate infections.1 2


250–500 mg every 6 hours for mild to moderate infections caused by susceptible S. pneumoniae;1 continue until afebrile for at least 2 days.1 2


Skin and Skin Structure Infections

Oral

250–500 mg every 6–8 hours.1 2 8


Prevention of Rheumatic Fever Recurrence

Oral

125–250 mg twice daily.1 2 30 AHA recommends 250 mg twice daily.30


Long-term, continuous prophylaxis required.2 5 8 30











Recommended Duration of Prophylaxis for Prevention of Rheumatic Fever Recurrence

Patient Category



Duration



Rheumatic fever without carditis



5 years or until 21 years of age, whichever is longer30



Rheumatic fever with carditis but no residual heart disease (no valvular disease)



10 years or well into adulthood, whichever is longer30



Rheumatic fever with carditis and residual heart disease (persistent valvular disease)



At least 10 years since last episode and at least until 40 years of age; sometimes for life30


Prevention of Bacterial Endocarditis

Patients Undergoing Certain Dental or Upper Respiratory Tract Procedures

Oral

2 g given 1 hour prior to the procedure and 1 g 6 hours later.1


Necrotizing Ulcerative Gingivitis

Oral

250–500 mg every 6–8 hours for mild to moderate infections.1 2


Anthrax

Postexposure Prophylaxis

Oral

7.5 mg/kg 4 times daily for 60 days for postexposure prophylaxis following suspected or confirmed exposure to B. anthracis spores (inhalational anthrax); use only if penicillin susceptibility confirmed.33


Cutaneous Anthrax

Oral

200–500 mg 4 times daily for treatment of uncomplicated cutaneous anthrax resulting from naturally occurring or endemic exposure to anthrax.34


7–10 days of treatment may be adequate if cutaneous anthrax occurred as the result of natural or endemic exposures; 60 days of treatment necessary if it occurred as the result of exposure to aerosolized anthrax spores (e.g., in context of biologic warfare or bioterrorism).36 38


Actinomycosis

Oral

2–4 g daily given in divided doses every 6 hours for 6–12 months for follow-up treatment of actinomycosis after initial 4–6 weeks of parenteral treatment.32


For mild cervicofacial actinomycosis, use a 2-month regimen of penicillin V.32


Whipple’ Disease

Oral

1–1.5 g daily.8


Cautions for Penicillin V


Contraindications



  • Known hypersensitivity to any penicillin.1 2



Warnings/Precautions


Warnings


Superinfection/Clostridium difficile-associated Colitis

Possible emergence and overgrowth of nonsusceptible bacteria or fungi.1 2 Discontinue and institute appropriate therapy if superinfection occurs.1 2


Consider Clostridium difficile-associated diarrhea and colitis (antibiotic-associated pseudomembranous colitis) if diarrhea develops and manage accordingly.1 2 25 26 27 28 29


Some mild cases of C. difficile-asssociated diarrhea and colitis may respond to discontinuance alone.2 25 26 27 28 29 Manage moderate to severe cases with fluid, electrolyte, and protein supplementation; appropriate anti-infective therapy (e.g., oral metronidazole or vancomycin) recommended if colitis is severe.2 25 26 27 28 29


Sensitivity Reactions


Hypersensitivity Reactions

Serious and occasionally fatal hypersensitivity reactions, including anaphylaxis, reported with penicillins.1 2 16


Prior to initiation of therapy, make careful inquiry concerning previous hypersensitivity reactions to penicillins, cephalosporins, or other drugs.1 2 Partial cross-allergenicity occurs among penicillins and other β-lactam antibiotics including cephalosporins and cephamycins.1 2 17 18 19


If hypersensitivity reaction occurs, discontinue immediately and institute appropriate therapy as indicated (e.g., epinephrine, corticosteroids, maintenance of an adequate airway and oxygen).1 2


General Precautions


Severe Infections

Use only for mild to moderately severe infections caused by susceptible bacteria.1 2


Do not use to treat acute stage of severe infections such as pneumonia, empyema, bacteremia, pericarditis, meningitis, or arthritis.1 2


Phenylketonuria

Some oral solutions contain aspartame (NutraSweet), which is metabolized in the GI tract to phenylalanine (125 and 250 mg/5 mL solutions from Teva provide 4.5 mg of phenylalanine/5 mL).1


The aspartame content should be considered in individuals with phenylketonuria (i.e., homozygous genetic deficiency of phenylalanine hydroxylase) and others who must restrict their intake of phenylalanine.43 44 45


Specific Populations


Pregnancy

Category B.2


Lactation

Distributed into milk;2 15 use with caution.2


Pediatric Use

Renal clearance of penicillin V delayed in neonates and young infants.1 2 8


Geriatric Use

No differences in safety and/or efficacy compared with younger adults.


Renal Impairment

Substantially eliminated by kidneys; renal clearance decreased in renal impairment.8


Use for longer than 2 weeks in impaired renal function may be associated with increased incidence of serum sickness-like reactions.


Assess renal function periodically during prolonged therapy, especially if high dosage used.


Common Adverse Effects


Adverse GI effects (e.g., nausea, vomiting, epigastric distress, diarrhea, black hairy tongue), hypersensitivity reactions (e.g., fever, eosinophilia, rash, urticaria, serum sickness-like reactions).1 2


Interactions for Penicillin V


Specific Drugs







Drug



Interaction



Hormonal contraceptives



Possible decreased efficacy of estrogen-containing oral contraceptives and increased incidence of breakthrough bleeding46


Penicillin V Pharmacokinetics


Absorption


Bioavailability


Approximately 25–73% of an oral dose of penicillin V absorbed from the GI tract in healthy, fasting adults;1 2 12 47 occasional patients will not absorb therapeutic concentrations of oral penicillin.1 2


Peak serum concentrations attained within 30–60 minutes.3 11 47 48 49 50


Food


Variable results obtained in studies evaluating effect of food on GI absorption of penicillin V potassium.3 12 13 14 Food may result in lower and delayed peak serum concentrations,3 11 13 14 although the total amount of drug absorbed is unaffected.3 47 48


Distribution


Extent


Widely distributed into body tissues.1 2 Highest concentrations in kidneys;1 2 lower concentrations in liver,1 2 skin,1 2 intestines,1 2 bile,3 tonsils,51 maxillary sinus secretions,3 52 saliva,8 13 and ascitic,3 synovial,3 pleural,3 and pericardial fluids.3


Only minimal amounts in CSF.1 2 3 8


Crosses the human placenta3 and is distributed into human milk.2 15


Plasma Protein Binding


Approximately 75–89%.1 2 10 12 50 53 54


Elimination


Metabolism


Metabolized in the liver.56


Approximately 35–70% of an oral dose is metabolized to penicilloic acid which is microbiologically inactive.12 49 50 56


Elimination Route


Penicillin V and metabolites principally excreted in urine by tubular secretion.11 49


Approximately 26–65% of an oral dose excreted in urine as unchanged drug and metabolites within 6–8 hours;11 49 50 approximately 32% of the dose excreted in feces.49


Half-life


Serum half-life is 0.5 hours in adults with normal renal function.55


Special Populations


Renal clearance delayed in neonates, young infants, and individuals with renal impairment.1 2 8


Stability


Storage


Oral


Tablets

15–30°C.1


For Solution

15–30°C.1 Following reconstitution, refrigerate and discard after 14 days.1 2


Actions and SpectrumActions



  • A β-lactam antibacterial classified as a natural penicillin.3 The phenoxymethyl analog of penicillin G.1 3




  • Usually bactericidal.1 2




  • Gram-positive aerobes: active in vitro and in clinical infections against Staphylococcus (nonpenicillinase-producing strains only),1 2 S. pneumoniae,1 2 S. pyogenes (group A β-hemolytic streptococci),1 2 and other streptococci (groups C, G, H, L, M).1 2




  • Also active in vitro against Bacillus anthracis,1 2 Corynebacterium diphtheriae,1 2 and Listeria monocytogenes.1 2




  • Other organisms: active in vitro against some Actinomyces bovis,1 2 Clostridium,1 2 and Streptobacillus moniliformis.1 2




  • Penicillinase-producing bacteria, including penicillinase-producing S. aureus1 2 8 and S. epidermidis are resistant.1 2 Enterococci are resistant.1 2



Advice to Patients



  • Advise individuals with phenylketonuria and other individuals who must restrict their intake of phenylalanine that some oral solutions contain aspartame (NutraSweet), which is metabolized in the GI tract to phenylalanine.43 44 45




  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.




  • Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed.




  • Importance of advising patients of other important precautionary information.1 2 (See Cautions.)



Preparations


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.


* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name






































Penicillin V Potassium

Routes



Dosage Forms



Strengths



Brand Names



Manufacturer



Oral



For solution



125 mg (of penicillin V) per 5 mL*



Penicillin V Potassium for Oral Solution (with aspartame)



Teva



250 mg (of penicillin V) per 5 mL*



Penicillin V Potassium for Oral Solution (with aspartame)



Teva



Tablets



250 mg (of penicillin V)*



Penicillin V Potassium Tablets



Sandoz, Teva



500 mg (of penicillin V)*



Penicillin V Potassium Tablets



Sandoz, Teva



Tablets, film-coated



250 mg (of penicillin V)*



Penicillin V Potassium Tablets



Sandoz



500 mg (of penicillin V)*



Penicillin V Potassium Tablets



Sandoz


Comparative Pricing


This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.


Penicillin V Potassium 250MG/5ML Solution (TEVA PHARMACEUTICALS USA): 100/$14.99 or 200/$19.97


Penicillin V Potassium 250MG Tablets (SANDOZ): 30/$13.99 or 60/$16.98


Penicillin V Potassium 500MG Tablets (TEVA PHARMACEUTICALS USA): 30/$25.99 or 90/$55.97



Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.


The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions June 2006. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.


† Use is not currently included in the labeling approved by the US Food and Drug Administration.




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