quinupristin/dalfopristin

Absorption: IV administration results in complete bioavailability.

Distribution: Unknown.

Protein Binding: Moderate.

Metabolism/Excretion: Both are converted to compounds with additional anti-infective activity; parent drugs and metabolites are mostly excreted in feces (75–77%); 15% of quinupristin and 17% of dalfopristin excreted in urine.

Half-life: Quinupristin — 0.85 hr; dalfopristin — 0.7 hr.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity.

Use Cautiously in:

Concurrent use of other drugs metabolized by the cytochrome P450 3A4 enzyme system (serious interactions may occur)
Hepatic impairment (dose adjustment may be necessary)
Patients with a history of GI disease, especially colitis
OB: Lactation: Pedi: Pregnancy, lactation, or children <12 yr (safety not established).

Adv. Reactions/Side Effects ⬆ ⬇

CNS: headache.

CV: thrombophlebitis.

GI: CLOSTRIDIUM DIFFICILE-ASSOCIATED DIARRHEA (CDAD), diarrhea, nausea, vomiting.

Derm: pruritus, rash.

Local: edema/inflammation/pain at infusion site, infusion site reactions.

Misc: ALLERGIC REACTIONS INCLUDING ANAPHYLAXIS, pain.

Interactions ⬆ ⬇

Drug-Drug:

Inhibits the cytochrome P450 3A4 drug metabolizing enzyme system; inhibits metabolism of cyclosporine, midazolam, and nifedipine and ↑ risk of toxicity (careful monitoring required).
Similar effects may be expected with concurrent use of delavirdine, nevirapine, indinavir, ritonavir, vinca alkaloids, docetaxel, paclitaxel, diazepam, verapamil, diltiazem, HMG CoA reductase inhibitors, tacrolimus, methylprednisolone, carbamazepine, quinidine, lidocaine, and disopyramide.

Route/Dosage ⬆ ⬇

IV (Adults and Children 12–17 yr): 7.5 mg/kg q 12 hr for at least 7 days.

Implementation ⬆ ⬇

IV Administration:

Intermittent Infusion: Reconstitute the 500-mg vial with 5 mL and the 600-mg vial with 6 mL of D5W or sterile water for injection, respectively, for a concentration of 100 mg/mL. Avoid shaking to prevent foam formation. Allow solution to sit until all foam has disappeared.
Rate: Infuse over 60 min. Flush line before and after infusion with D5W.
Y-Site Compatibility:
- alemtuzumab
- alfentanil
- amikacin
- amiodarone
- anidulafungin
- argatroban
- aztreonam
- bleomycin
- buprenorphine
- busulfan
- butorphanol
- carboplatin
- carmustine
- caspofungin
- chlorpromazine
- ciprofloxacin
- cisatracurium
- cisplatin
- cyclophosphamide
- cyclosporine
- cytarabine
- dacarbazine
- daptomycin
- daunorubicin
- dexmedetomidine
- dexrazoxane
- diltiazem
- diphenhydramine
- docetaxel
- dolasetron
- doxacurium
- doxarubicin
- doxycycline
- droperidol
- enalaprilat
- ephedrine
- epinephrine
- epirubicin
- esmolol
- etoposide
- etoposide phosphate
- fenoldopam
- fentanyl
- fluconazole
- gemcitabine
- granisetron
- haloperidol
- hydromorphone
- idarubicin
- ifosfamide
- isoproterenol
- labetalol
- levofloxacin
- levorphanol
- lidocaine
- linezolid
- lorazepam
- magnesium sulfate
- mannitol
- mechlorethamine
- meperidine
- metoclopramide
- metoprolol
- midazolam
- milrinone
- mitomycin
- mitoxantrone
- morphine
- mycophenolate
- nalbuphine
- naloxone
- nesiritide
- nicardipine
- nitroglycerin
- octreotide
- ondansetron
- oxaliplatin
- oxytocin
- paclitaxel
- palonosetron
- pamidronate
- pancuronium
- pentamidine
- phenylephrine
- potassium chloride
- procainamide
- prochlorperazine
- promethazine
- propranolol
- rocuronium
- sodium phosphates
- succinylcholine
- sufentanil
- tacrolimus
- teniposide
- theophylline
- thiotepa
- tirofiban
- tobramycin
- vasopressin
- vecuronium
- verapamil
- vinblastine
- vincristine
- vinorelbine
- voriconazole
- zidovudine
- zoledronic acid
Y-Site Incompatibility:
- acyclovir
- amifostine
- aminophylline
- amphotericin B colloidal
- amphotericin B lipid complex
- amphotericin B liposome
- ampicillin
- ampicillin/sulbactam
- azithromycin
- bivalirudin
- bumetanide
- calcium chloride
- calcium gluconate
- cefazolin
- cefepime
- cefotaxime
- cefotetan
- cefoxitin
- ceftazidime
- ceftriaxone
- cefuroxime
- clindamycin
- dexamethasone sodium phosphate
- diazepam
- digoxin
- ertapenem
- fludarabine
- fluorouracil
- fosphenytoin
- furosemide
- ganciclovir
- heparin
- hydrocortisone
- imipenem/cilastatin
- insulin
- ketorolac
- leucovorin
- meropenem
- mesna
- methotrexate
- methylprednisolone sodium succinate
- metronidazole
- nitroprusside
- pantoprazole
- pemetrexed
- pentobarbital
- phenobarbital
- phenytoin
- piperacillin/tazobactam
- potassium acetate
- potassium phosphates
- ranitidine
- rituximab
- sodium acetate
- sodium bicarbonate
- thiopental
- tigecycline
- trimethoprim/sulfamethoxazole
Solution Incompatibility: 0.9% NaCl.

US Brand Names ⬆ ⬇

Classifications ⬆ ⬇

Therapeutic Classification: anti-infectives

Pharmacologic Classification: streptogramins

Availability ⬆ ⬇

Powder for injection: 500 mg/vial (150 mg quinupristin and 350 mg dalfopristin); 600 /vial (180 mg quinupristin and 420 mg dalfopristin);

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
IV	rapid	end of infusion	8–12 hr

Assessment ⬆ ⬇

Assess patient for infection (vital signs; appearance of wound, sputum, urine, and stool; WBC) at beginning of and throughout therapy.
Obtain specimens for culture and sensitivity before initiating therapy. First dose may be given before receiving results.
Monitor patient for pain or inflammation at the infusion site frequently throughout infusion. Increasing the volume of diluent from 250 mL to 500 mL or 750 mL or infusing via a peripherally inserted central catheter or central venous catheter may be required.
Observe patient for signs and symptoms of anaphylaxis (rash, pruritus, laryngeal edema, wheezing). Discontinue drug and notify physician or other health care professional immediately if these problems occur. Keep epinephrine, an antihistamine, and resuscitation equipment close by in case of an anaphylactic reaction.
Assess patient for myalgia and arthralgia after infusion. May be severe. Reducing dose frequency to every 12 hr may decrease pain. Symptoms usually resolve upon discontinuation of medication.

Lab Test Considerations:

May cause ↑ serum total bilirubin concentrations.

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Pronunciation ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇