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Synercid
Overview
What is Synercid?
Synercid
Quinupristin is a white to very slightly yellow, hygroscopic powder. It is a combination of three peptide macrolactones. The main component of quinupristin (> 88.0%) has the following chemical name: N-[(6,9,10,13,15,18,22,24 )-22-[-(dimethylamino)benzyl]-6-ethyldocosahydro-10,23-dimethyl-5,8,12,15,17,21,24-heptaoxo-13-phenyl-18-[[(3 )-3-quinuclidinylthio] methyl]-12-pyrido[2,1- ]pyrrolo-[2,1- ][1,4,7,10,13,16] oxapentaazacyclononadecin-9-yl]-3-hydroxypicolinamide.
The main component of quinupristin has an empirical formula of CHNOS, a molecular weight of 1022.24 and the following structural formula:
Dalfopristin is a slightly yellow to yellow, hygroscopic, powder. The chemical name for dalfopristin is: (3,4,5,10,12,14,26,26a)-26-[[2-(diethylamino)ethyl]sulfonyl]-8,9,14,15,24,25,26,26a-octahydro-14-hydroxy-3-isopropyl-4,12-dimethyl-3-21,18-nitrilo-1,22-pyrrolo[2,1- ][1,8,4,19]-dioxadiazacyclotetracosine-1,7,16,22(4,17)-tetrone.
Dalfopristin has an empirical formula of CHNOS, a molecular weight of 690.85 and the following structural formula:
What does Synercid look like?
What are the available doses of Synercid?
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What should I talk to my health care provider before I take Synercid?
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How should I use Synercid?
To reduce the development of drug-resistant bacteria and maintain the effectiveness of and other antibacterial drugs, should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.
Synercid
susceptible
Complicated skin and skin structure infections
Staphylococcus aureus
susceptible
Streptococcus pyogenes
.
Synercid
.
e.g
Synercid
WARNINGS
What interacts with Synercid?
Synercid
Synercid
e.g.
What are the warnings of Synercid?
Drug Interactions
In vitro
Synercid
Synercid
Therapeutic level monitoring of cyclosporine should be performed when cyclosporine must be used concomitantly with Synercid
It is reasonable to expect that the concomitant administration of Synercid and other drugs primarily metabolized by the cytochrome P450 3A4 enzyme system may likely result in increased plasma concentrations of these drugs that could increase or prolong their therapeutic effect and/or increase adverse reactions. (See below.) Therefore, coadministration of Synercid with drugs which are cytochrome P450 3A4 substrates and possess a narrow therapeutic window requires caution and monitoring of these drugs (, cyclosporine), whenever possible. Concomitant medications metabolized by the cytochrome P450 3A4 enzyme system that may prolong the QTc interval should be avoided.
Concomitant administration of and nifedipine (repeated oral doses) and midazolam (intravenous bolus dose) in healthy volunteers led to elevated plasma concentrations of these drugs. The C increased by 18% and 14% (median values) and the AUC increased by 44% and 33% for nifedipine and midazolam, respectively.
Clostridium difficile
Synercid
C. difficile
C. difficile
C. difficile
If CDAD is suspected or confirmed, ongoing antibiotic use not directed against may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of , and surgical evaluation should be instituted as clinically indicated.
| Antihistamines: | Anti-HIV (NNRTIs and Protease inhibitors): | Benzodiazepines: | GI motility agents: | Immunosuppressive agents: | Steroids: | Other: |
What are the precautions of Synercid?
General
Prescribing in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
Venous Irritation
Prescribing in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
Rate of Infusion
In animal studies toxicity was higher when was administered as a bolus compared to slow infusion. However, the safety of an intravenous bolus of has not been studied in humans. Clinical trial experience has been exclusively with an intravenous duration of 60 minutes and, thus, other infusion rates cannot be recommended.
Arthralgias/Myalgias
Episodes of arthralgia and myalgia, some severe, have been reported in patients treated with . In some patients, improvement has been noted with a reduction in dose frequency to q12h. In those patients available for follow-up, treatment discontinuation has been followed by resolution of symptoms. The etiology of these myalgias and arthralgias is under investigation.
Superinfections
The use of antibiotics may promote the overgrowth of nonsusceptible organisms. Should superinfection occur during therapy, appropriate measures should be taken.
Hyperbilirubinemia
Elevations of total bilirubin greater than 5 times the upper limit of normal were noted in approximately 25% of patients in the non-comparative studies. (See
) In some patients, isolated hyperbilirubinemia (primarily conjugated) can occur during treatment, possibly resulting from competition between and bilirubin for excretion. Of note, in the comparative trials, elevations in ALT and AST occurred at a similar frequency in both the and comparator groups.
Information for Patients
Diarrhea is a common problem caused by antibiotics which usually ends when the antibiotic is discontinued. Sometimes after starting treatment with antibiotics, patients can develop watery and bloody stools (with or without stomach cramps and fever) even as late as two or more months after having taken the last dose of the antibiotic. If this occurs, patients should contact their physician as soon as possible.
Patients should be counseled that antibacterial drugs including should only be used to treat bacterial infections. They do not treat viral infections ( the common cold). When is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by or other antibacterial drugs in the future.
Drug Interactions
Array
Synercid
A drug interaction between and digoxin cannot be excluded but is unlikely to occur via CYP3A4 enzyme inhibition. has shown activity (MICs of 0.25 mcg/mL when tested on two strains) against Digoxin is metabolized in part by bacteria in the gut and as such, a drug interaction based on 's inhibition of digoxin's gut metabolism (by ) may be possible.
Array
Array
Carcinogenesis, Mutagenesis, Impairment of Fertility
Long-term carcinogenicity studies in animals have not been conducted with . Five genetic toxicity tests were performed. , dalfopristin, and quinupristin were tested in the bacterial reverse mutation assay, the Chinese hamster ovary cell HGPRT gene mutation assay, the unscheduled DNA synthesis assay in rat hepatocytes, the Chinese hamster ovary cell chromosome aberration assay, and the mouse micronucleus assay in bone marrow. Dalfopristin was associated with the production of structural chromosome aberrations when tested in the Chinese hamster ovary cell chromosome aberration assay. and quinupristin were negative in this assay. , dalfopristin, and quinupristin were all negative in the other four genetic toxicity assays.
No impairment of fertility or perinatal/postnatal development was observed in rats at doses up to 12 to 18 mg/kg (approximately 0.3 to 0.4 times the human dose based on body-surface area).
Pregnancy
Reproductive studies have been performed in mice at doses up to 40 mg/kg/day (approximately half the human dose based on body-surface area), in rats at doses up to 120 mg/kg/day (approximately 2.5 times the human dose based on body-surface area), and in rabbits at doses up to 12 mg/kg/day (approximately half the human dose based on body-surface area) and have revealed no evidence of impaired fertility or harm to the fetus due to .
There are, however, no adequate and well-controlled studies with in pregnant women. Because animal reproduction studies are not always predictive of the human response, this drug should be used during pregnancy only if clearly needed.
Nursing Mothers
In lactating rats, was excreted in milk. It is not known whether is excreted in human breast milk. Because many drugs are excreted in human milk, caution should be exercised when is administered to a nursing woman.
Hepatic Insufficiency
Following a single 1-hour infusion of (7.5 mg/kg) to patients with hepatic insufficiency, plasma concentrations were significantly increased. (See
) However, the effect of dose reduction or increase in dosing interval on the pharmacokinetics of in these patients has not been studied. Therefore, no recommendations can be made at this time regarding the appropriate dose modification.
Pediatric Use
Synercid
Synercid
Geriatric Use
In phase 3 comparative trials of , 37% of patients (n=404) were ≥65 years of age, of which 145 were ≥75 years of age. In the phase 3 non-comparative trials, 29% of patients (n=346) were ≥65 years of age, of which 112 were ≥75 years of age. There were no apparent differences in the frequency, type, or severity of related adverse reactions including cardiovascular events between elderly and younger individuals.
What are the side effects of Synercid?
The safety of was evaluated in 1099 patients enrolled in 5 comparative clinical trials. Additionally, 4 non-comparative clinical trials (3 prospective and 1 retrospective in design) were conducted in which 1199 patients received for infections due to Gram-positive pathogens for which no other treatment option was available. In non-comparative trials, the patients were severely ill, often with multiple co-morbidities or physiological impairments, and may have been intolerant to or failed other antibacterial therapies.
COMPARATIVE TRIALS
ADVERSE REACTION SUMMARY – ALL COMPARATIVE STUDIES
Safety data are available from five comparative clinical studies (n= 1099 ; n= 1095 comparator). One of the deaths in the comparative studies was assessed as possibly related to . The most frequent reasons for discontinuation due to drug-related adverse reactions were as follows:
| Type | Synercid | Comparator |
|---|---|---|
| Venous | 9.2 | 2.0 |
| Non-venous | 9.6 | 4.3 |
| -Rash | 1.0 | 0.5 |
| -Nausea | 0.9 | 0.6 |
| -Vomiting | 0.5 | 0.5 |
| -Pain | 0.5 | 0.0 |
| -Pruritus | 0.5 | 0.3 |
CLINICAL REACTIONS – ALL COMPARATIVE STUDIES
| Adverse Reactions | % of patients with adverse reactions | ||
|---|---|---|---|
| Synercid | Comparator | ||
| Inflammation at infusion site | 42.0 | 25.0 | |
| Pain at infusion site | 40.0 | 23.7 | |
| Edema at infusion site | 17.3 | 9.5 | |
| Infusion site reaction | 13.4 | 10.1 | |
| Nausea | 4.6 | 7.2 | |
| Thrombophlebitis | 2.4 | 0.3 | |
| Diarrhea | 2.7 | 3.2 | |
| Vomiting | 2.7 | 3.8 | |
| Rash | 2.5 | 1.4 | |
| Headache | 1.6 | 0.9 | |
| Pruritus | 1.5 | 1.1 | |
| Pain | 1.5 | 0.1 |
CLINICAL REACTIONS – SKIN AND SKIN STRUCTURE STUDIES
| % of patients discontinuing therapy by reaction type | ||
|---|---|---|
| Type | Synercid | Comparator |
| Venous | 12.0 | 2.0 |
| Non-venous | 11.8 | 4.0 |
| -Rash | 2.0 | 0.9 |
| -Nausea | 1.1 | 0.0 |
| -Vomiting | 0.9 | 0.0 |
| -Pain | 0.9 | 0.0 |
| -Pruritus | 0.9 | 0.5 |
| % of patients with adverse reactions | ||
| Synercid | Comparator | |
| Venous | 68.0 | 32.7 |
| -Pain at infusion site | 44.7 | 17.8 |
| -Inflammation at infusion site | 38.2 | 14.7 |
| -Edema at infusion site | 18.0 | 7.2 |
| -Infusion site reaction | 11.6 | 3.6 |
| Non-venous | 24.7 | 13.1 |
| -Nausea | 4.0 | 2.0 |
| -Vomiting | 3.7 | 1.0 |
| -Rash | 3.1 | 1.3 |
| -Pain | 3.1 | 0.2 |
LABORATORY EVENTS-ALL COMPARATIVE STUDIES
Table 9 shows the number (%) of patients exhibiting laboratory values above or below the clinically relevant "critical" values during treatment phase (with an incidence of 0.1% or greater in either treatment group).
| Parameter | Critically High or Low Value | Synercid Critically High or Low | Comparator Critically High or Low |
|---|---|---|---|
| AST | > 10 × ULN | 9 (0.9) | 2 (0.2) |
| ALT | > 10 × ULN | 4 (0.4) | 4 (0.4) |
| Total Bilirubin | > 5 × ULN | 9 (0.9) | 2 (0.2) |
| Conjugated Bilirubin | > 5 × ULN | 29 (3.1) | 12 (1.3) |
| LDH | > 5 × ULN | 10 (2.6) | 8 (2.1) |
| Alk Phosphatase | > 5 × ULN | 3 (0.3) | 7 (0.7) |
| Gamma-GT | > 10 × ULN | 19 (1.9) | 10 (1.0) |
| CPK | > 10 × ULN | 6 (1.6) | 5 (1.4) |
| Creatinine | ≥ 440 μmoL/L | 1 (0.1) | 1 (0.1) |
| BUN | ≥ 35.5 mmoL/L | 2 (0.3) | 9 (1.2) |
| Blood Glucose | > 22.2 mmoL/L | 11 (1.3) | 11 (1.3) |
| < 2.2 mmoL/L | 1 (0.1) | 1 (0.1) | |
| Bicarbonates | > 40 mmoL/L | 2 (0.3) | 3 (0.5) |
| < 10 mmoL/L | 3 (0.5) | 3 (0.5) | |
| CO | > 50 mmoL/L | 0 (0.0) | 0 (0.0) |
| < 15 mmoL/L | 1 (0.2) | 0 (0.0) | |
| Sodium | > 160 mmoL/L | 0 (0.0) | 0 (0.0) |
| < 120 mmoL/L | 5 (0.5) | 3 (0.3) | |
| Potassium | > 6.0 mmoL/L | 3 (0.3) | 6 (0.6) |
| < 2.0 mmoL/L | 0 (0.0) | 1 (0.1) | |
| Hemoglobin | < 8 g/dL | 25 (2.6) | 16 (1.6) |
| Hematocrit | > 60% | 2 (0.2) | 0 (0.0) |
| Platelets | > 1,000,000/mm | 2 (0.2) | 2 (0.2) |
| < 50,000/mm | 6 (0.6) | 7 (0.7) |
NON-COMPARATIVE TRIALS
CLINICAL ADVERSE REACTIONS
| Adverse Reactions | % of patients with adverse reaction | ||
|---|---|---|---|
| Study 301 | Study 398A | Study 398B | |
| Arthralgia | 7.8 | 5.2 | 4.3 |
| Myalgia | 5.1 | 0.95 | 3.1 |
| Arthralgia and Myalgia | 7.4 | 3.3 | 6.8 |
| Nausea | 3.8 | 2.8 | 4.9 |
LABORATORY EVENTS
The most frequently observed abnormalities in laboratory studies were in total and conjugated bilirubin, with increases greater than 5 times upper limit of normal, irrespective of relationship to , reported in 25.0% and 34.6% of patients, respectively. The percentage of patients who discontinued treatment due to increased total and conjugated bilirubin was 2.7% and 2.3%, respectively. Of note, 46.5% and 59.0% of patients had high baseline total and conjugated bilirubin levels before study entry.
OTHER
Serious adverse reactions in clinical trials, including non-comparative studies, considered possibly or probably related to administration with an incidence < 0.1% include: acidosis, anaphylactoid reaction, apnea, arrhythmia, bone pain, cerebral hemorrhage, cerebrovascular accident, coagulation disorder, convulsion, dysautonomia, encephalopathy, grand mal convulsion, hemolysis, hemolytic anemia, heart arrest, hepatitis, hypoglycemia, hyponatremia, hypoplastic anemia, hypoventilation, hypovolemia, hypoxia, jaundice, mesenteric arterial occlusion, neck rigidity, neuropathy, pancytopenia, paraplegia, pericardial effusion, pericarditis, respiratory distress syndrome, shock, skin ulcer, supraventricular tachycardia, syncope, tremor, ventricular extrasystoles and ventricular fibrillation. Cases of hypotension and gastrointestinal hemorrhage were reported in less than 0.2% of patients.
Post-marketing Experiences
In addition to adverse events reported from clinical trials, reports of angioedema and anaphylactic shock have been identified during post approval use of .
What should I look out for while using Synercid?
Synercid
Synercid
e.g.
What might happen if I take too much Synercid?
There are four reports of patients receiving doses at up to three times that recommended (7.5 mg/kg). No adverse events were considered possibly or probably related to overdose. Signs of acute overdosage may include dyspnea, emesis, tremors, and ataxia as seen in animals given extremely high doses (50 mg/kg) of . Patients who receive an overdose should be carefully observed and given supportive treatment. is not removed by peritoneal dialysis or by hemodialysis.
How should I store and handle Synercid?
Store at 20° to 25° C (68° to 77° F); excursions permitted to 15° to 30° C (59° to 86° F) [see USP Controlled Room Temperature]. Keep this drug and all drugs out of the reach of children. Store at 20° to 25° C (68° to 77° F); excursions permitted to 15° to 30° C (59° to 86° F) [see USP Controlled Room Temperature]. Keep this drug and all drugs out of the reach of children. Store at 20° to 25° C (68° to 77° F); excursions permitted to 15° to 30° C (59° to 86° F) [see USP Controlled Room Temperature]. Keep this drug and all drugs out of the reach of children. Synercid
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Quinupristin and dalfopristin are the main active components circulating in plasma in human subjects. Quinupristin and dalfopristin are converted to several active major metabolites: two conjugated metabolites for quinupristin (one with glutathione and one with cysteine) and one non-conjugated metabolite for dalfopristin (formed by drug hydrolysis).
Pharmacokinetic profiles of quinupristin and dalfopristin in combination with their metabolites were determined using a bioassay following multiple 60-minute infusions of in two groups of healthy young adult male volunteers. Each group received 7.5 mg/kg of intravenously q12h or q8h for a total of 9 or 10 doses, respectively. The pharmacokinetic parameters were proportional with q12h and q8h dosing; those of the q8h regimen are shown in Table 1:
The clearances of unchanged quinupristin and dalfopristin are similar (0.72 L/h/kg), and the steady-state volume of distribution for quinupristin is 0.45 L/kg and for dalfopristin is 0.24 L/kg. The elimination half-life of quinupristin and dalfopristin is approximately 0.85 and 0.70 hours, respectively.
The total protein binding of quinupristin is higher than that of dalfopristin. does not alter the binding of warfarin to proteins in human serum.
Penetration of unchanged quinupristin and dalfopristin in noninflammatory blister fluid corresponds to about 19% and 11% of that estimated in plasma, respectively. The penetration into blister fluid of quinupristin and dalfopristin in combination with their major metabolites was in total approximately 40% compared to that in plasma.
In vitro
Synercid
in vitro
Synercid
.
Synercid
Synercid
.
Fecal excretion constitutes the main elimination route for both parent drugs and their metabolites (75 to 77% of dose). Urinary excretion accounts for approximately 15% of the quinupristin and 19% of the dalfopristin dose. Preclinical data in rats have demonstrated that approximately 80% of the dose is excreted in the bile and suggest that in man, biliary excretion is probably the principal route for fecal elimination.
Non-Clinical Toxicology
SynercidSynercid
e.g.
Synercid
A drug interaction between and digoxin cannot be excluded but is unlikely to occur via CYP3A4 enzyme inhibition. has shown activity (MICs of 0.25 mcg/mL when tested on two strains) against Digoxin is metabolized in part by bacteria in the gut and as such, a drug interaction based on 's inhibition of digoxin's gut metabolism (by ) may be possible.
Prescribing in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
The safety of was evaluated in 1099 patients enrolled in 5 comparative clinical trials. Additionally, 4 non-comparative clinical trials (3 prospective and 1 retrospective in design) were conducted in which 1199 patients received for infections due to Gram-positive pathogens for which no other treatment option was available. In non-comparative trials, the patients were severely ill, often with multiple co-morbidities or physiological impairments, and may have been intolerant to or failed other antibacterial therapies.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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