quinupristin and dalfopristin

quinupristin and dalfopristin

Synercid

Pharmacologic class: Streptogramin

Therapeutic class: Anti-infective

Pregnancy risk category B

Action

Synergistic effects of drug combination interfere with bacterial cell-wall synthesis by disrupting DNA and RNA transcription

Availability

Injection: 500 mg/10 ml (150 mg quinupristin, 350 mg dalfopristin), 600 mg/10 ml (180 mg quinupristin, 420 mg dalfopristin)

Indications and dosages

Serious or life-threatening infections caused by vancomycin-resistant Enterococcus faecium

Adults and adolescents ages 16 and older: 7.5 mg/kg by I.V. infusion over 1 hour q 8 hours

Complicated skin and skin-structure infections caused by Staphylococcus aureus (methicillin-susceptible) or Streptococcus pyogenes

Adults and adolescents ages 16 and older: 7.5 mg/kg by I.V. infusion over 1 hour q 12 hours for at least 7 days

Dosage adjustment

• Hepatic impairment

Contraindications

• Hypersensitivity to drug or other streptogramins

Precautions

Use cautiously in:
• hepatic impairment
• breastfeeding patients
• children younger than age 16 (safety and efficacy not established).

Administration

Don't mix with other drugs or saline solution.
• For intermittent infusion through a common I.V. line, flush line with dextrose 5% in water (D5W) before and after giving drug.
• Add 5 ml of sterile water or D5W to powdered drug in vial, and swirl gently by hand until powder dissolves; don't shake vial. Solution should be clear.
• Within 30 minutes of first dilution, draw up prescribed dosage and dilute further in D5W to a final concentration of 2 mg/ml or less.
• Know that if patient has a central venous catheter and is fluid-restricted, drug may be given in 100 ml of D5W.
• Administer by infusion pump over 60 minutes.
• If significant peripheral vein irritation occurs, dilute in 500 to 750 ml of D5W.
• Be aware that duration of therapy depends on infection site and severity.

Adverse reactions

CNS: headache

CV: thrombophlebitis

GI: nausea, vomiting, diarrhea

Musculoskeletal: joint pain, myalgia

Skin: rash, pruritus

Other: inflammation, pain, or edema at infusion site

Interactions

Drug-drug.Drugs metabolized by CYP450-3A4 (antiretrovirals; antineoplastics, such as vinca alkaloids, docetaxel, and paclitaxel; astemizole; benzodiazepines; calcium channel blockers; carbamazepine; cisapride; corticosteroids; disopyramide; HMG-CoA reductase inhibitors; immunosuppressants such as cyclosporine and tacrolimus; lidocaine; quinidine; terfenadine): increased therapeutic and adverse effects of these drugs

Drug-diagnostic tests.Alanine aminotransferase, aspartate aminotransferase, bilirubin: increased levels

Patient monitoring

• Monitor closely for infusion site reactions and thrombophlebitis. If these problems occur, consider increasing infusion volume, changing infusion site, or infusing through peripherally inserted central catheter or central venous catheter.
• Assess weight and fluid intake and output to help detect edema.
• Monitor bilirubin level.

Patient teaching

Instruct patient to immediately report pain or redness at infusion site.
• Tell patient to report muscle aches and pains.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

References in periodicals archive ?
We tested the following: penicillin, amoxicillin, piperacillin, piperacillin and tazobactam, cefotaxime, ceftazidime, ertapenem, imipenem, meropenem, doripenem, gentamicin, tobramycin, amikacin, levofloxacin, ciprofloxacin, moxifloxacin, minocycline, tygecycline, cotrimoxazole, fosfomycin, quinupristin and dalfopristin, rifampin, daptomycin, linezolid, clindamycin, and fucidic acid.
Although all of these linezolid-resistant isolates were still sensitive to the drug combination of quinupristin and dalfopristin (Synercid), the relatively high prevalence of linezolid resistance is "a cause for concern," said Paul C.
The novel synergistic effect of quinupristin and dalfopristin occurs through a two-pronged attack on protein synthesis in bacterial cells.
Synercid, the first injectable streptogramin, is comprised of two molecules, quinupristin and dalfopristin, which when combined create a synergistic agent that has the power to kill susceptible bacteria by inhibiting protein synthesis.
Synercid (quinupristin/dalfopristin), an investigational compound under development by Rhone-Poulenc Rorer, is an injectable streptogramin antibiotic made of two molecules, quinupristin and dalfopristin.
Synercid, which is water-soluble and thus injectable, is made of two individually active molecules, quinupristin and dalfopristin, each of which alone mildly halts reproduction of the bacteria.