Penicillins By: Corey Bradley and Christine Barlow

My rough outline for my project. Have yet to find a "fun fact"

Extended Spectrum Penicillins

·         Also known as Antipseudomonal Penicillins

·         Broad-Spectrum

·         Well absorbed in the GI tract

·         Affective against Pseudomonas Aeruginosa (a gram negative bacillus that if difficult to eradicate)

·         Can also be used to eradicate other gram-negative organisms such as Proteus spp., Serratia Spp. Klebsibelle Pneumoniae, Enterobacter spp. And Acinetobacter spp.

·         Can be given IM, IV, or oral

·         Medications:

o   Carbenicillin Indanyl (Geocilin): Given in po form in a range of 382-764mg Q6H to adults only. This medication is used to treat infections caused by Proteus spp. And Pseudomonas Aeruginosa. Should be used with caution in clients with hypertension or heart failure because this medication contains large amounts of sodium

o   Piperacillin-tazobactam (Zosyn): Given in IV form 3.375g, Q6H over 30 minutes for a duration of 7-10 days to adults only.  Has many uses such as severe appendicitis, skin infections, pneumonia, and beta-lactamase-producing bacteria (tazobactam is a beta-lactamase inhibitor) Monitor hepatic and renal function, electrolytes as well. One of the most common electrolyte imbalances to occur is hypokalemia. Can cause complications in cystic fibrosis patients.

o   Ticarcillin-clavulanate (timentin): can be given IV to adults 3.1 grams Q6H, or children older than 3 months based on weight 200-300 mg/kg/day in 4-6 divided doses. Indicated in the treatment of septicemia, and lower respiratory tract infections, urinary tract infections, skin infections, bone infections, and joint infections. Clavukanic acid protects ticarcillin from degradation by beta-lactamase enzymes. Monitor hepatic and renal function, electrolytes as well. One of the most common electrolyte imbalances to occur is hypokalemia. Make sure that patient is aware that diarrhea can occur as late as 2+ months after last dose of medication and make sure that patient knows to report diarrhea to MD.

 

Beta-Lactamase Inhibitors

·         Combined with broad spectrum antibiotics

·         When combined the beta-lactamase inhibitor inhibits the bacterial beta-lactamases making the antibiotic more effective and extends the antibiotics antimicrobial effect

·         Three beta-lactamase inhibitor: clavulanic acid, sulbactam, and tazobactam.

·         The above beta-lactamase inhibitors are not given alone, they are combined with a penicillinase-sensitive penicillin (examples incude amoxicillin, ampicillin, piperacillin, or tiracillin)

·         Combined drugs currently on the market

o   Piperacillin-tazobactam (Zosyn): Given in IV form 3.375g, Q6H over 30 minutes for a duration of 7-10 days to adults only.  Has many uses such as severe appendicitis, skin infections, pneumonia, and beta-lactamase-producing bacteria (tazobactam is a beta-lactamase inhibitor) Monitor hepatic and renal function, electrolytes as well. One of the most common electrolyte imbalances to occur is hypokalemia. Can cause complications in cystic fibrosis patients

o   Ampicillin-Sulbactam (unasyn): given IV- dosing in adults 1.5-3g Q6H, dosing in children 100-300mg/kg/day divided Q6H.  Effective against gram negative and gram positive bacteria, people who have allergies penicillin may be allergic to ampicillin. Monitor for GI changes, hematological changes –most common agranulocytosis, monitor hepatic and renal function, monitor estrogen levels in pregnant women because this medication can cause a false positive for glucose with the clinitest, bemedicts solution, or fehlings solution.

o   Amoxicillin-Clavulanic acid (augmentin): given in PO doses- Adult dosing 250-500 mg Q8-12h, Childrens dosing – if the child weighs less than 40 kg than dosing is 20-40 mg/kg/day. This medication is used to treat lower respiratory infections, otitis media, sinusitis, skin infections and UTI’s. Monitor renal function, hepatic function and electrolytes. Monitor for cholestatic jaundice. Make sure that patient is aware that diarrhea can occur as late as 2+ months after last dose of medication and make sure that patient knows to report diarrhea to MD.

 

o   Ticarcillin-clavulante (Timentin): given IV. In adults 3.1g  Q6H and in children who are >3 months in age dosing in 200-300mg/kg/day in 4-6 divided doses. Indicated in the treatment of septicemia, and lower respiratory tract infections, urinary tract infections, skin infections, bone infections, and joint infections. Clavukanic acid protects ticarcillin from degradation by beta-lactamase enzymes . Monitor hepatic and renal function, electrolytes as well. One of the most common electrolyte imbalances to occur is hypokalemia. Make sure that patient is aware that diarrhea can occur as late as 2+ months after last dose of medication and make sure that patient knows to report diarrhea to MD.

 

 

Considerations:

·         Common side effects: hypersensitivity and superinfection (occurance of a secondary infection when the flora of the body is disturbed. GI disturbances  (nausea, vomiting, and diarrhea) Rash = mild to moderate allergic reaction, Signs of a severe anaphylactic reaction include laryngeal edema, severe bronchoconstriction with stridor and hypotension.

    *** Always finish full dose of all antibiotics

By: Corey Bradley

 

Mechanism of action:

Penicillin works by interfering with bacterial cell wall synthesis.  Penicillin has a beta-lactam ring structure, which interferes with from four to eight (depending on the bacteria) related enzymes responsible for bacterial cell division and bacterial wall synthesis.  (Calderwood, S. B., 2014)  Penicillin can be bactericidal and bacteriostatic.  Bacteria can combat penicillin and other antibiotics by producing beta-lactamases.  In the case of penicillin, these beta-lactamases are called penicillinases.  (Kee, Hayes & McCuistion, 2012)

Broad Spectrum Penicillins:

Indications/Dosage: 

Amoxicillin (Amoxil):  Treatment of gram positive and gram negative bacterial infections such as skin infections, lower respiratory tract infection, otitis media, skin infection, and gonorrhea.  Adult:  PO250-500 mg q8-12 hours; Child: PO  20-40 mg/kg/d in 3 divided doses. 

Amoxicillin-clavulanate (Augmentin):  Treatment of sinusitis, lower respiratory tract infections, pneumonia, skin infection.  Adult:  PO:250-500 mg q8-12 hours; Child: PO: <40 kg: 20-40 mg/kg/d

Ampicillin (Principen)- treatment of gram positive/gram negative cocci; gram positive bacilli; respiratory, GI and GU infections; meningitis; septicemia; endocarditis.  Adult: PO/IM/IV: 250-500 mg q6h; Child: PO/IM/IV: 25-50 mg/kg/d in 4 doses

Ampicillin-sulbactam (Unasyn)- skin infections; intra-abdominal infections; pneumonia; gynecologic infections; meningitis; septicemia.  Adult: IV: 1.5 to 3 g q6 hours; Child: IV: 100-300 mg/kg/d in 4 doses. 

(Skidmore-Roth, 2012)

Penicillinase-Resistant Penicillins:

Indications/Dosages:

Dicloxacillin sodium (Dynapen):  treatment of staphylococcus aureus infection.  Adult: PO: 1250500 mg q6 hours; Child: PO: 12.5-25 mg/kg/d in 3 divided doses. 

Nafcillin (Nallpen):  treatment of penicillin G-resistant Staphylococcus aureus.  Adult: IM/IV: 500 mg- 1g q4-6 hours, max 12 g/day.  Child: IM: 25 mg/kg b.i.d.   IV: 50-200 mg/kg/d in 4-6 doses, max 12 g/day

Oxacillin sodium (Bactocill):  For penicillin-resistant staphylococci.  Adult: PO: 500mg -1 g, q 4-6 hours.  IM/IV: 250mg to 1 g, q4-6 hours.  Child: PO/IM/IV: 50-100 mg/kg/d in divided doses 

Pharmacokinetics:

                Amoxicillin- greater than 80% absorbed in the GI tract, it is 20% protein bound, with 60-70% excreted in the urine.  Its half-life is 1-1.5 hours.  Clavulanate is 30-40% excreted in urine.  Fifty percent of Ampicillin is absorbed in the GI tract, it is 15-28% protein bound, with a half-life of 1-2 hours.  Sulbactam has the same absorption, is 28-38% protein bound, with a half-life of 1-2 hours.  Dynapen is absorbed 35-76% in the GI tract, it is 95% protein bound, it’s half-life is 0.5-1 hour.  It is 90% protein bound, and its half-life is 1 hour.  Bactocill is 95% protein bound, with a half-life of 0.5-1 hour. 

Pharmacodynamics:

Amoxicillin interferes with cell-wall synthesis, causing cell destruction.  Clavulanic acid added in Augmentin increases the effect of amoxicillin by decreasing resistance to the drug.   Onset is 0.5 hour, peak 1 hour, duration 4-6 hours. 

(Kee, Hayes & McCuistion, 2012)

Side Effects:  Amoxicillin; Ampicillin; Augmenten:  Nausea, vomiting, diarrhea, rash, edema, stomatitis; Dicloaxdillin: abdominal pain, flatulence; Nafcillin; Oxacillin: Nausea, vomiting, diarrhea, rash.

Adverse reactions:  Superinfections;  Severe: respiratory distress, anaphylaxis, hypotension, blood dyscrasias, hemolytic anemia, bone marrow depression. 

                By: Christine Barlow