Ispenoral may be available in the countries listed below.
Phenoxymethylpenicillin potassium (a derivative of Phenoxymethylpenicillin) is reported as an ingredient of Ispenoral in the following countries:
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Amoxicilina Fmndtria may be available in the countries listed below.
Amoxicillin is reported as an ingredient of Amoxicilina Fmndtria in the following countries:
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Famopril may be available in the countries listed below.
Famotidine is reported as an ingredient of Famopril in the following countries:
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Wet-Comod may be available in the countries listed below.
Povidone is reported as an ingredient of Wet-Comod in the following countries:
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Liotontrauma may be available in the countries listed below.
Diethylamine Salicylate is reported as an ingredient of Liotontrauma in the following countries:
Escin is reported as an ingredient of Liotontrauma in the following countries:
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To reduce the development of drug-resistant bacteria and maintain the effectiveness of Doxycycline capsules and other antibacterial drugs, Doxycycline capsules should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
Doxycycline is a broad-spectrum antibiotic synthetically derived from oxytetracycline. Doxycycline 150 mg, 100 mg and 50 mg capsules contain Doxycycline monohydrate equivalent to 150 mg, 100 mg or 50 mg of Doxycycline for oral administration. Inactive ingredients include colloidal silicon dioxide, gelatin, magnesium stearate, microcrystalline cellulose, sodium starch glycolate and titanium dioxide. In addition, the 50 mg strength contains D&C Yellow #6 and D&C Yellow #10. The 100 mg strength also contains black iron oxide, red iron oxide and yellow iron oxide. The 150 mg strength includes FD&C Red #40 and FD&C Yellow #6. Its molecular weight is 462.46. The chemical designation of the light-yellow crystalline powder is alpha-6-deoxy-5-oxytetracycline.
| C22H24N2O8•H20 |
Doxycycline has a high degree of lipid solubility and a low affinity for calcium binding. It is highly stable in normal human serum. Doxycycline will not degrade into an epianhydro form.
Tetracyclines are readily absorbed and are bound to plasma proteins in varying degrees. They are concentrated by the liver in the bile and excreted in the urine and feces at high concentrations in a biologically active form. Doxycycline is virtually completely absorbed after oral administration.
Following a 200 mg dose of Doxycycline monohydrate, 24 normal adult volunteers averaged the following serum concentration values:
| Time (hr): | 0.5 | 1.0 | 1.5 | 2.0 | 3.0 | 4.0 | 8.0 | 12.0 | 24.0 | 48.0 | 72.0 |
| Conc. (mcg/mL): | 1.02 | 2.26 | 2.67 | 3.01 | 3.16 | 3.03 | 2.03 | 1.62 | 0.95 | 0.37 | 0.15 |
| Average Observed Values | |
| Maximum Concentration | 3.61 mcg/mL (± 0.9 sd) |
| Time of Maximum Concentration | 2.60 hr (± 1.10 sd) |
| Elimination Rate Constant | 0.049 per hr (± 0.030 sd) |
| Half-Life | 16.33 hr (± 4.53 sd) |
Excretion of Doxycycline by the kidney is about 40%/72 hours in individuals with normal function (creatinine clearance about 75 mL/min). This percentage excretion may fall as low as 1 to 5%/72 hours in individuals with severe renal insufficiency (creatinine clearance below 10 mL/ min). Studies have shown no significant difference in serum half-life of Doxycycline (range 18 to 22 hours) in individuals with normal and severely impaired renal function. Hemodialysis does not alter serum half-life.
Microbiology: The tetracyclines are primarily bacteriostatic and are thought to exert their antimicrobial effect by the inhibition of protein synthesis. The tetracyclines, including Doxycycline, have a similar antimicrobial spectrum of activity against a wide range of gram-positive and gram-negative microorganisms. Cross-resistance of these microorganisms to tetracyclines is common.
Doxycycline has been shown to be active against most strains of the following microorganisms, both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section.
Aerobic Gram-Positive Microorganisms:
Because many strains of the following groups of gram-positive microorganisms have been shown to be resistant to tetracyclines, culture and susceptibility testing are recommended:
*Doxycycline is not the drug of choice in the treatment of any type of staphylococcal infection.
Up to 44 percent of strains of Streptococcus pyogenes and 74 percent of Streptococcus faecalis have been found to be resistant to tetracycline drugs. Therefore, tetracyclines should not be used to treat streptococcal infections unless the microorganism has been demonstrated to be susceptible.
Aerobic Gram-Negative Microorganisms:
| Bartonella bacilliformis | Brucella species |
| Calymmatobacterium granulomatis | Campylobacter fetus |
| Francisella tularensis | Haemophilus ducreyi |
| Haemophilus influenzae | Neisseria gonorrhoeae |
| Vibrio cholerae | Yersinia pestis |
Because many strains of the following groups of gram-negative microorganisms have been shown to be resistant to tetracyclines, culture and susceptibility testing are recommended:
| Acinetobacter species | Enterobacter aerogenes |
| Escherichia coli | Klebsiella species |
| Shigella species | |
| Anaerobic Microorganisms: | |
| Actinomyces israelii | Clostridium species |
| Fusobacterium fusiforme | |
| Other Microorganisms: | |
| Borrelia recurrentis | Chlamydia psittaci |
| Chlamydia trachomatis | Mycoplasma pneumoniae |
| Rickettsiae | |
| Treponema pallidum | Treponema pertenue |
Quantitative methods are used to determine antimicrobial minimum inhibitory concentrations (MIC’s). These MIC’s provide estimates of the susceptibility of bacteria to antimicrobial compounds. The MIC’s should be determined using a standardized procedure. Standardized procedures are based on a dilution method 1,3 (broth or agar) or equivalent with standardized inoculum concentrations and standardized concentrations of tetracycline powder. The MIC values should be interpreted according to the following criteria for indicated aerobic microorganisms other than Haemophilus species, Neisseria gonorrhoeae, and Streptococcus pneumoniae:
A report of “Susceptible” indicates that the pathogen is likely to be inhibited if the antimicrobial compound in the blood reaches the concentrations usually achievable. A report of “Intermediate” indicates that the result should be considered equivocal, and, if the microorganism is not fully susceptible to alternative, clinically feasible drugs, the test should be repeated. This category implies possible clinical applicability in body sites where the drug is physiologically concentrated or in situations where high dosage of drug can be used. This category also provides a buffer zone which prevents small uncontrolled technical factors from causing major discrepancies in interpretation. A report of “Resistant” indicates that the pathogen is not likely to be inhibited if the antimicrobial compound in the blood reaches the concentrations usually achievable; other therapy should be selected.
Standardized susceptibility test procedures require the use of laboratory control microorganisms to control the technical aspects of the laboratory procedures. Standard tetracycline powder should provide the following MIC values:
Quantitative methods that require measurement of zone diameters also provide reproducible estimates of the susceptibility of bacteria to antimicrobial compounds. One such standardized procedure 2,3 requires the use of standardized inoculum concentrations. This procedure uses paper disks impregnated with 30 mcg tetracycline or 30 mcg Doxycycline to test the susceptibility of microorganisms to Doxycycline.
Reports from the laboratory providing results of the standard single-disk susceptibility test with 30-µg tetracycline-class disk or the 30 mcg Doxycycline disk should be interpreted according to the following criteria for indicated aerobic microorganisms other than Haemophilus species, Neisseria gonorrhoeae, and Streptococcus pneumoniae:
| Zone Diameter (mm) | Interpretation | ||
| tetracycline | Doxycycline | ||
| ≥19 | ≥16 | Susceptible (S) | |
| 15-18 | 13-15 | Intermediate (I) | |
| ≤14 | ≤12 | Resistant (R) | |
| When testing Haemophilus spp.a | |||
| Zone Diameter (mm) | Interpretation | ||
| tetracycline | |||
| ≥29 | Susceptible (S) | ||
| 26-28 | Intermediate (I) | ||
| ≤25 | Resistant (R) | ||
| When testing Neisseria gonorrhoeaeb | |||
| Zone Diameter (mm) | Interpretation | ||
| tetracycline | |||
| ≥38 | Susceptible (S) | ||
| 31-37 | Intermediate (I) | ||
| ≤30 | Resistant R) | ||
Zone diameters ≤ 19 mm may indicate a plasmid-mediated tetracycline-resistant Neisseria gonorrhoeae (TRNG) isolate. These TRNG strains should be confirmed by the dilution test (MIC ≥16 µg/mL).
Interpretation should be as stated above for results using dilution techniques. Interpretation involves correlation of the diameter obtained in the disk test with the MIC for tetracycline or Doxycycline, respectively.
As with standardized dilution techniques, diffusion methods require the use of laboratory control microorganisms that are used to control the technical aspects of the laboratory procedures. For the diffusion technique, the 30 mcg tetracycline-class disk or the 30 mcg Doxycycline disk should provide the following zone diameters in these laboratory test quality control strains:
For anaerobic bacteria, the susceptibility to tetracycline as MIC’s can be determined by standardized test methods. 4 The MIC values obtained should be interpreted according to the following criteria:
| MIC (mcg/mL) | Interpretation |
| ≤4 | Susceptible (S) |
| 8 | Intermediate (I) |
| ≥16 | Resistant (R) |
Interpretation is identical to that stated above for results using dilution techniques.
As with other susceptibility techniques, the use of laboratory control microorganisms is required to control the technical aspects of the laboratory standardized procedures. Standardized tetracycline powder should provide the following MIC values:
a. Range applicable only to tests performed by the reference agar dilution method. | ||
| Microorganism | MIC (mcg/mL) | |
| Bacteroides fragilisa | ATCC 25285 | 0.12-0.5 |
| Bacteroides thetaiotaomicrona | ATCC 29741 | 8-32 |
To reduce the development of drug-resistant bacteria and maintain the effectiveness of Doxycycline capsules and other antibacterial drugs, Doxycycline capsules should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible 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 empiric selection of therapy.
Doxycycline is indicated for the treatment of the following infections:
Rocky mountain spotted fever, typhus fever and the typhus group, Q fever, rickettsialpox, and tick fevers caused by Rickettsiae.
Respiratory tract infections caused by Mycoplasma pneumoniae.
Lymphogranuloma venereum caused by Chlamydia trachomatis.
Psittacosis (omithosis) caused by Chlamydia psittaci.
Trachoma caused by Chlamydia trachomatis, although the infectious agent is not always eliminated as judged by immunofluorescence.
Inclusion conjunctivitis caused by Chlamydia trachomatis.
Uncomplicated urethral, endocervical or rectal infections in adults caused by Chlamydia trachomatis.
Nongonococcal urethritis caused by Ureaplasma urealyticum.
Relapsing fever due to Borrelia recurrentis.
Doxycycline is also indicated for the treatment of infections caused by the following gram-negative microorganisms:
Chancroid caused by Haemophilus ducreyi.
Plague due to Yersinia pestis (formerly Pasteurella pestis).
Tularemia due to Francisella tularensis (formerly Pasteurella tularensis).
Cholera caused by Vibrio cholerae (formerly Vibrio comma).
Campylobacter fetus infections caused by Campylobacter fetus (formerly Vibrio fetus).
Brucellosis due to Brucella species (in conjunction with streptomycin).
Bartonellosis due to Bartonella bacilliformis.
Granuloma inguinale caused by Calymmatobacterium granulomatis.
Because many strains of the following groups of microorganisms have been shown to be resistant to Doxycycline, culture and susceptibility testing are recommended.
Doxycycline is indicated for treatment of infections caused by the following gram-negative microorganisms, when bacteriologic testing indicates appropriate susceptibility to the drug:
Enterobacter aerogenes (formerly Aerobacter aerogenes )
Acinetobacter species (formerly Mima species and Herellea species)
Respiratory tract infections caused by Haemophilus influenzae.
Respiratory tract and urinary infections caused by Klebsiella species.
Doxycycline is indicated for treatment of infections caused by the following gram-positive microorganisms, when bacteriologic testing indicates appropriate susceptibility to the drug:
Upper respiratory infections caused by Streptococcus pneumoniae (formerly Diplococcus pneumoniae).
Skin and skin structure infections caused by Staphylococcus aureus.
Anthrax due to Bacillus anthracis, including inhalational anthrax (post-exposure): to reduce the incidence or progression of disease following exposure to aerosolized Bacillus anthracis.
Doxycycline is not the drug of choice in the treatment of any type of staphylococcal infections.
When penicillin is contraindicated, Doxycycline is an alternative drug in the treatment of the following infections:
Uncomplicated gonorrhea caused by Neisseria gonorrhoeae.
Syphilis caused by Treponema pallidum.
Yaws caused by Treponema pertenue.
Listeriosis due to Listeria monocytogenes.
Vincent’s infection caused by Fusobacterium fusiforme.
Actinomycosis caused by Actinomyces israelii.
Infections caused by Clostridium species.
In acute intestinal amebiasis, Doxycycline may be a useful adjunct to amebicides.
In severe acne, Doxycycline may be useful adjunctive therapy.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of Doxycycline capsules and other antibacterial drugs, Doxycycline capsules should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible 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 empiric selection of therapy.
Doxycycline is indicated for the treatment of the following infections:
Rocky mountain spotted fever, typhus fever and the typhus group, Q fever, rickettsialpox, and tick fevers caused by Rickettsiae.
Respiratory tract infections caused by Mycoplasma pneumoniae.
Lymphogranuloma venereum caused by Chlamydia trachomatis.
Psittacosis (omithosis) caused by Chlamydia psittaci.
Trachoma caused by Chlamydia trachomatis, although the infectious agent is not always eliminated as judged by immunofluorescence.
Inclusion conjunctivitis caused by Chlamydia trachomatis.
Uncomplicated urethral, endocervical or rectal infections in adults caused by Chlamydia trachomatis.
Nongonococcal urethritis caused by Ureaplasma urealyticum.
Relapsing fever due to Borrelia recurrentis.
Doxycycline is also indicated for the treatment of infections caused by the following gram-negative microorganisms:
Chancroid caused by Haemophilus ducreyi.
Plague due to Yersinia pestis (formerly Pasteurella pestis).
Tularemia due to Francisella tularensis (formerly Pasteurella tularensis).
Cholera caused by Vibrio cholerae (formerly Vibrio comma).
Campylobacter fetus infections caused by Campylobacter fetus (formerly Vibrio fetus).
Brucellosis due to Brucella species (in conjunction with streptomycin).
Bartonellosis due to Bartonella bacilliformis.
Granuloma inguinale caused by Calymmatobacterium granulomatis.
Because many strains of the following groups of microorganisms have been shown to be resistant to Doxycycline, culture and susceptibility testing are recommended.
Doxycycline is indicated for treatment of infections caused by the following gram-negative microorganisms, when bacteriologic testing indicates appropriate susceptibility to the drug:
Enterobacter aerogenes (formerly Aerobacter aerogenes )
Acinetobacter species (formerly Mima species and Herellea species)
Respiratory tract infections caused by Haemophilus influenzae.
Respiratory tract and urinary infections caused by Klebsiella species.
Doxycycline is indicated for treatment of infections caused by the following gram-positive microorganisms, when bacteriologic testing indicates appropriate susceptibility to the drug:
Upper respiratory infections caused by Streptococcus pneumoniae (formerly Diplococcus pneumoniae).
Skin and skin structure infections caused by Staphylococcus aureus.
Anthrax due to Bacillus anthracis, including inhalational anthrax (post-exposure): to reduce the incidence or progression of disease following exposure to aerosolized Bacillus anthracis.
Doxycycline is not the drug of choice in the treatment of any type of staphylococcal infections.
When penicillin is contraindicated, Doxycycline is an alternative drug in the treatment of the following infections:
Uncomplicated gonorrhea caused by Neisseria gonorrhoeae.
Syphilis caused by Treponema pallidum.
Yaws caused by Treponema pertenue.
Listeriosis due to Listeria monocytogenes.
Vincent’s infection caused by Fusobacterium fusiforme.
Actinomycosis caused by Actinomyces israelii.
Infections caused by Clostridium species.
In acute intestinal amebiasis, Doxycycline may be a useful adjunct to amebicides.
In severe acne, Doxycycline may be useful adjunctive therapy.
This drug is contraindicated in persons who have shown hypersensitivity to any of the tetracyclines.
THE USE OF DRUGS OF THE TETRACYCLINE CLASS DURING TOOTH DEVELOPMENT (LAST HALF OF PREGNANCY, INFANCY, AND CHILDHOOD TO THE AGE OF 8 YEARS) MAY CAUSE PERMANENT DISCOLORATION OF THE TEETH (YELLOW-GRAY-BROWN). This adverse reaction is more common during long-term use of the drugs but has been observed following repeated short-term courses. Enamel hypoplasia has also been reported. TETRACYCLINE DRUGS, THEREFORE, SHOULD NOT BE USED IN THIS AGE GROUP, EXCEPT FOR ANTHRAX, INCLUDING INHALATIONAL ANTHRAX (POST-EXPOSURE), UNLESS OTHER DRUGS ARE NOT LIKELY TO BE EFFECTIVE OR ARE CONTRAINDICATED.
Clostridiumdifficile associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including Doxycycline monohydrate capsules, and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile.
C. difficile produces toxins A and B which contribute to the development of CDAD. Hypertoxin producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhea following antibiotic use. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents.
If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C. difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of C. difficile, and surgical evaluation should be instituted as clinically indicated.
All tetracyclines form a stable calcium complex in any bone-forming tissue. A decrease in the fibula growth rate has been observed in prematures given oral tetracycline in doses of 25 mg/kg every six hours. This reaction was shown to be reversible when the drug was discontinued.
Results of animal studies indicate that tetracyclines cross the placenta, are found in fetal tissues, and can have toxic effects on the developing fetus (often related to retardation of skeletal development). Evidence of embryo toxicity has been noted in animals treated early in pregnancy. If any tetracycline is used during pregnancy or if the patient becomes pregnant while taking these drugs, the patient should be apprised of the potential hazard to the fetus.
The antianabolic action of the tetracyclines may cause an increase in BUN. Studies to date indicate that this does not occur with the use of Doxycycline in patients with impaired renal function.
Photosensitivity manifested by an exaggerated sunburn reaction has been observed in some individuals taking tetracyclines. Patients apt to be exposed to direct sunlight or ultraviolet light should be advised that this reaction can occur with tetracycline drugs, and treatment should be discontinued at the first evidence of skin erythema.
General: As with other antibiotic preparations, use of this drug may result in overgrowth of non-susceptible organisms, including fungi. If superinfection occurs, the antibiotic should be discontinued and appropriate therapy instituted.
Bulging fontanels in infants and benign intracranial hypertension in adults have been reported in individuals receiving tetracyclines. These conditions disappeared when the drug was discontinued.
Incision and drainage or other surgical procedures should be performed in conjunction with antibiotic therapy when indicated.
Prescribing Doxycycline monohydrate capsules 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.
Unguentum Acidi Salicylici may be available in the countries listed below.
Salicylic Acid is reported as an ingredient of Unguentum Acidi Salicylici in the following countries:
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Vitacin may be available in the countries listed below.
Ascorbic Acid is reported as an ingredient of Vitacin in the following countries:
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Injection, USP
For Intravenous or Intramuscular
Use Only
Ampul
Rx only
WARNING
Cases of QT prolongation and/or torsade de pointes have been reported in patients receiving Droperidol at doses at or below recommended doses. Some cases have occurred in patients with no known risk factors for QT prolongation and some cases have been fatal.
Due to its potential for serious proarrhythmic effects and death, Droperidol should be reserved for use in the treatment of patients who fail to show an acceptable response to other adequate treatments, either because of insufficient effectiveness or the inability to achieve an effective dose due to intolerable adverse effects from those drugs (see Warnings, Adverse Reactions, Contraindications, and Precautions).
Cases of QT prolongation and serious arrhythmias (e.g., torsade de pointes) have been reported in patients treated with Droperidol. Based on these reports, all patients should undergo a 12-lead ECG prior to administration of Droperidol to determine if a prolonged QT interval (i.e., QTc greater than 440 msec for males or 450 msec for females) is present. If there is a prolonged QT interval, Droperidol should NOT be administered. For patients in whom the potential benefit of Droperidol treatment is felt to outweigh the risks of potentially serious arrhythmias, ECG monitoring should be performed prior to treatment and continued for 2-3 hours after completing treatment to monitor for arrhythmias.
Droperidol is contraindicated in patients with known or suspected QT prolongation, including patients with congenital long QT syndrome.
Droperidol should be administered with extreme caution to patients who may be at risk for development of prolonged QT syndrome (e.g., congestive heart failure, bradycardia, use of a diuretic, cardiac hypertrophy, hypokalemia, hypomagnesemia, or administration of other drugs known to increase the QT interval). Other risk factors may include age over 65 years, alcohol abuse, and use of agents such as benzodiazepines, volatile anesthetics, and I.V. opiates. Droperidol should be initiated at a low dose and adjusted upward, with caution, as needed to achieve the desired effect.
Droperidol Injection, USP is a sterile, nonpyrogenic solution of Droperidol in water for injection for intravenous or intramuscular injection. Each mL contains Droperidol 2.5 mg. Contains lactic acid to adjust pH. pH is 3.4 (3.0 to 3.8).
The solution contains no bacteriostat, antimicrobial agent or added buffer and is intended only for use as a single-dose injection. Discard unused portion.
Droperidol is a neuroleptic (tranquilizer) agent chemically designated as 1-[1-[3-(p-Fluorobenzoyl) propyl]-1,2,3,6-tetrahydro-4-pyridyl]-2-benzimidazolinone with a molecular weight of 379.43.
It has the following structural formula:
Droperidol produces marked tranquilization and sedation. It allays apprehension and provides a state of mental detachment and indifference while maintaining a state of reflex alertness.
Droperidol produces an antiemetic effect as evidenced by the antagonism of apomorphine in dogs. It lowers the incidence of nausea and vomiting during surgical procedures and provides antiemetic protection in the postoperative period.
Droperidol potentiates other CNS depressants. It produces mild alpha-adrenergic blockade, peripheral vascular dilatation and reduction of the pressor effect of epinephrine. It can produce hypotension and decreased peripheral vascular resistance and may decrease pulmonary arterial pressure (particularly if it is abnormally high). It may reduce the incidence of epinephrine-induced arrhythmias but it does not prevent other cardiac arrhythmias.
The onset of action of single intramuscular and intravenous doses is from three to ten minutes following administration, although the peak effect may not be apparent for up to thirty minutes. The duration of the tranquilizing and sedative effects generally is two to four hours, although alteration of alertness may persist for as long as twelve hours.
Droperidol injection is indicated to reduce the incidence of nausea and vomiting associated with surgical and diagnostic procedures.
Droperidol is contraindicated in patients with known or suspected QT prolongation (i.e., QTc interval greater than 440 msec for males or 450 msec for females). This would include patients with congenital long QT syndrome.
Droperidol is contraindicated in patients with known hypersensitivity to the drug.
Droperidol is not recommended for any use other than for the treatment of perioperative nausea and vomiting in patients for whom other treatments are ineffective or inappropriate (see WARNINGS).
Droperidol should be administered with extreme caution in the presence of risk factors for development of prolonged QT syndrome, such as: 1) clinically significant bradycardia (less than 50 bpm), 2) any clinically significant cardiac disease, 3) treatment with Class I and Class III antiarrhythmics, 4) treatment with monoamine oxidase inhibitors (MAOI’s), 5) concomitant treatment with other drug products known to prolong the QT interval (see PRECAUTIONS, Drug Interactions), and 6) electrolyte imbalance, in particular hypokalemia and hypomagnesemia, or concomitant treatment with drugs (e.g., diuretics) that may cause electrolyte imbalance.
Effects on Cardiac Conduction:
A dose-dependent prolongation of the QT interval was observed within 10 minutes of Droperidol administration in a study of 40 patients without known cardiac disease who underwent extracranial head and neck surgery. Significant QT prolongation was observed at all three dose levels evaluated, with 0.1, 0.175, and 0.25 mg/kg associated with prolongation of median QTc by 37, 44, and 59 msec, respectively.
Cases of QT prolongation and serious arrhythmias (e.g., torsade de pointes, ventricular arrhythmias, cardiac arrest, and death) have been observed during post-marketing treatment with Droperidol. Some cases have occurred in patients with no known risk factors and at doses at or below recommended doses. There has been at least one case of nonfatal torsade de pointes confirmed by rechallenge.
Based on these reports, all patients should undergo a 12-lead ECG prior to administration of Droperidol to determine if a prolonged QT interval (i.e., QTc greater than 440 msec for males or 450 msec for females) is present. If there is a prolonged QT interval, Droperidol should NOT be administered. For patients in whom the potential benefit of Droperidol treatment is felt to outweigh the risks of potentially serious arrhythmias, ECG monitoring should be performed prior to treatment and continued for 2-3 hours after completing treatment to monitor for arrhythmias.
FLUIDS AND OTHER COUNTERMEASURES TO MANAGE HYPOTENSION SHOULD BE READILY AVAILABLE.
As with other CNS depressant drugs, patients who have received Droperidol should have appropriate surveillance.
It is recommended that opioids, when required, initially be used in reduced doses.
As with other neuroleptic agents, very rare reports of neuroleptic malignant syndrome (altered consciousness, muscle rigidity and autonomic instability) have occurred in patients who have received Droperidol.
Since it may be difficult to distinguish neuroleptic malignant syndrome from malignant hyperpyrexia in the perioperative period, prompt treatment with dantrolene should be considered if increases in temperature, heart rate or carbon dioxide production occur.
General: The initial dose of Droperidol should be appropriately reduced in elderly, debilitated and other poor-risk patients. The effect of the initial dose should be considered in determining incremental doses.
Certain forms of conduction anesthesia, such as spinal anesthesia and some peridural anesthetics, can alter respiration by blocking intercostal nerves and can cause peripheral vasodilatation and hypotension because of sympathetic blockade. Through other mechanisms (see CLINICAL PHARMACOLOGY), Droperidol can also alter circulation. Therefore, when Droperidol is used to supplement these forms of anesthesia, the anesthetist should be familiar with the physiological alterations involved, and be prepared to manage them in the patients elected for these forms of anesthesia.
If hypotension occurs, the possibility of hypovolemia should be considered and managed with appropriate parenteral fluid therapy. Repositioning the patient to improve venous return to the heart should be considered when operative conditions permit. It should be noted that in spinal and peridural anesthesia, tilting the patient into a head-down position may result in a higher level of anesthesia than is desirable, as well as impair venous return to the heart. Care should be exercised in the moving and positioning of patients because of a possibility of orthostatic hypotension. If volume expansion with fluids plus these other countermeasures do not correct the hypotension, then the administration of pressor agents other than epinephrine should be considered. Epinephrine may paradoxically decrease the blood pressure in patients treated with Droperidol due to the alpha-adrenergic blocking action of Droperidol.
Since Droperidol may decrease pulmonary arterial pressure, this fact should be considered by those who conduct diagnostic or surgical procedures where interpretation of pulmonary arterial pressure measurements might determine final management of the patient.
Vital signs and ECG should be monitored routinely.
When the EEG is used for postoperative monitoring, it may be found that the EEG pattern returns to normal slowly.
Impaired Hepatic or Renal Function: Droperidol should be administered with caution to patients with liver and kidney dysfunction because of the importance of these organs in the metabolism and excretion of drugs.
Pheochromocytoma: In patients with diagnosed/ suspected pheochromocytoma, severe hypertension and tachycardia have been observed after the administration of Droperidol.
Potentially Arrhythmogenic Agents: Any drug known to have the potential to prolong the QT interval should not be used together with Droperidol. Possible pharmacodynamic interactions can occur between Droperidol and potentially arrhythmogenic agents such as class I or III antiarrhythmics, antihistamines that prolong the QT interval, antimalarials, calcium channel blockers, neuroleptics that prolong the QT interval, and antidepressants.
Caution should be used when patients are taking concomitant drugs known to induce hypokalemia or hypomagnesemia as they may precipitate QT prolongation and interact with Droperidol. These would include diuretics, laxatives and supraphysiological use of steroid hormones with mineralocorticoid potential.
CNS Depressant Drugs: Other CNS depressant drugs (e.g., barbiturates, tranquilizers, opioids and general anesthetics) have additive or potentiating effects with Droperidol. Following the administration of Droperidol, the dose of other CNS depressant drugs should be reduced.
Carcinogenesis, Mutagenesis, Impairment of Fertility: No carcinogenicity studies have been carried out with Droperidol. The micronucleus test in female rats revealed no mutagenic effects in single oral doses as high as 160 mg/kg. An oral study in rats (Segment I) revealed no impairment of fertility in either males or females at 0.63, 2.5 and 10 mg/kg doses (approximately 2, 9 and 36 times maximum recommended human I.V./I.M. dosage).
Pregnancy — Category C: Droperidol administered intravenously has been shown to cause a slight increase in mortality of the newborn rat at 4.4 times the upper human dose. At 44 times the upper human dose, mortality rate was comparable to that for control animals. Following intramuscular administration, increased mortality of the offspring at 1.8 times the upper human dose is attributed to CNS depression in the dams who neglected to remove placentae from their offspring. Droperidol has not been shown to be teratogenic in animals. There are no adequate and well-controlled studies in pregnant women. Droperidol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Labor and Delivery: There are insufficient data to support the use of Droperidol in labor and delivery. Therefore, such use is not recommended.
Nursing Mothers: It is not known whether Droperidol is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Droperidol is administered to a nursing mother.
Pediatric Use: The safety of Droperidol in children younger than two years of age has not been established.
QT interval prolongation, torsade de pointes, cardiac arrest, and ventricular tachycardia have been reported in patients treated with Droperidol. Some of these cases were associated with death. Some cases occurred in patients with no known risk factors, and some were associated with Droperidol doses at or below recommended doses.
Physicians should be alert to palpitations, syncope, or other symptoms suggestive of episodes of irregular cardiac rhythm in patients taking Droperidol and promptly evaluate such cases (see WARNINGS, Effects on Cardiac Conduction).
The most common somatic adverse reactions reported to occur with Droperidol are mild to moderate hypotension and tachycardia, but these effects usually subside without treatment. If hypotension occurs and is severe or persists, the possibility of hypovolemia should be considered and managed with appropriate parenteral fluid therapy.
The most common behavioral adverse effects of Droperidol include dysphoria, postoperative drowsiness, restlessness, hyperactivity and anxiety, which can either be the result of an inadequate dosage (lack of adequate treatment effect) or of an adverse drug reaction (part of the symptom complex of akathisia).
Care should be taken to search for extrapyramidal signs and symptoms (dystonia, akathisia, oculogyric crisis) to differentiate these different clinical conditions. When extrapyramidal symptoms are the cause, they can usually be controlled with anticholinergic agents.
Postoperative hallucinatory episodes (sometimes associated with transient periods of mental depression) have also been reported.
Other less common reported adverse reactions include anaphylaxis, dizziness, chills and/or shivering, laryngospasm and bronchospasm.
Elevated blood pressure, with or without pre-existing hypertension, has been reported following administration of Droperidol combined with fentanyl citrate or other parenteral analgesics. This might be due to unexplained alterations in sympathetic activity following large doses; however, it is also frequently attributed to anesthetic or surgical stimulation during light anesthesia.
Manifestations: The manifestations of Droperidol overdosage are an extension of its pharmacologic actions and may include QT prolongation and serious arrhythmias (e.g. torsade de pointes) (see BOX WARNING, WARNINGS, and PRECAUTIONS).
Treatment: In the presence of hypoventilation or apnea, oxygen should be administered and respiration should be assisted or controlled as indicated. A patent airway must be maintained; an oropharyngeal airway or endotracheal tube might be indicated. The patient should be carefully observed for 24 hours; body warmth and adequate fluid intake should be maintained. If hypotension occurs and is severe or persists, the possibility of hypovolemia should be considered and managed with appropriate parenteral fluid therapy. (See PRECAUTIONS).
If significant extrapyramidal reactions occur, in the context of an overdose, an anticholinergic should be administered.
The intravenous Median Lethal Dose is 20 ― 43 mg/kg in mice; 30 mg/kg in rats; and 25 mg/kg in dogs and 11 ― 13 mg/kg in rabbits. The intramuscular Median Lethal Dose of Droperidol is 195 mg/kg in mice; 104 ― 110 mg/kg in rats; 97 mg/kg in rabbits and 200 mg/kg in guinea pigs.
Dosage should be individualized. Some of the factors to be considered in determining dose are age, body weight, physical status, underlying pathological condition, use of other drugs, the type of anesthesia to be used, and the surgical procedure involved.
Vital signs and ECG should be monitored routinely.
Adult Dosage: The maximum recommended initial dose of Droperidol is 2.5 mg I.M. or slow I.V. Additional 1.25 mg doses of Droperidol may be administered to achieve the desired effect. However, additional doses should be administered with caution, and only if the potential benefit outweighs the potential risk.
Pediatric Dosage: For children two to 12 years of age, the maximum recommended initial dose is 0.1 mg/kg, taking into account the patient’s age and other clinical factors. However, additional doses should be administered with caution, and only if the potential benefit outweighs the potential risk.
See WARNINGS and PRECAUTIONS for use of Droperidol with other CNS depressants and in patients with altered response.
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. If such abnormalities are observed, the drug should not be administered.
Droperidol Injection, USP 2.5 mg/mL is supplied in 2 mL (5 mg) single-dose ampuls packaged in cartons of ten (List No. 1187).
Store at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.]
Protect from light.
Saarnivaara L, Klemola UM, Lindgren L, et al. QT interval of the ECG, heart rate and arterial pressure using propofol, methohexital or midazolam for induction of anesthesia. Acta Anaesthesiol Scand 1990: 34: 276-81.
Schmeling WT, Warltier DC, McDonald DJ, et al. Prolongation of the QT interval by enflurane, isoflurane, and halothane in humans. Anesth Analg 1991:72:137-44.
Späth G. Torsade des pointe oder die andere Ursache des plötz-lichen Herztodes. Wien: Ueberreuter, 1998.
Riley DC, Schmeling WT, Al-Wathiqui MH, et al. Prolongation of the QT-interval by volatile anesthetics in chronically instrumented dogs. Anesth Analg 1988: 67: 741-9.
McConachie I, Keaveny JP, Healy TF, et al. Effects of anaesthesia on the QT-interval. Br J Anaesth 1989: 63: 558-60.
Lawrence KR, Nasraway SA. Conduction disturbances associated with administration of butyrophenone antipsychotics in the critically ill: a review of the literature. Pharmacotherapy 1997: 17(3): 531-7.
Lischke V, Behne M, Doelken P, et al. Droperidol causes a dose-dependent prolongation of the QT interval. Anesth Analg 1994: 79: 983-6.
Revised: October, 2004
©Hospira 2004 EN - 0531 Printed in USA
HOSPIRA, INC., LAKE FOREST, IL 60045 USA
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| Marketing Category | Application Number or Monograph Citation | Marketing Start Date | Marketing End Date |
| ANDA | ANDA071981 | 08/11/2011 | |
| Labeler - Hospira, Inc. (141588017) |
In some countries, this medicine may only be approved for veterinary use.
Dichlorophen is reported as an ingredient of Difolin in the following countries:
Toluene is reported as an ingredient of Difolin in the following countries:
International Drug Name Search
In the US, Sirolimus (sirolimus systemic) is a member of the drug class selective immunosuppressants and is used to treat Organ Transplant, Rejection Prophylaxis.
US matches:
Rec.INN
L04AA10
0053123-88-9
C51-H79-N-O13
914
Selective immunosuppressant
(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-Hexadecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dime (WHO)
(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-Hexadecahydro-9,27-dihydroxy-3-{(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl}-10,2 (IUPAC)
Rapamycin (USAN)
International Drug Name Search
Glossary
| BAN | British Approved Name |
| DCF | Dénomination Commune Française |
| IUPAC | International Union of Pure and Applied Chemistry |
| IS | Inofficial Synonym |
| OS | Official Synonym |
| Rec.INN | Recommended International Nonproprietary Name (World Health Organization) |
| USAN | United States Adopted Name |
| WHO | World Health Organization |
Treating overactive bladder with symptoms of urinary frequency, urgency, and leakage. It may also be used for other conditions as determined by your doctor.
Detrol is an antimuscarinic (anticholinergic) agent. It works by blocking a chemical that causes contractions of the bladder.
Contact your doctor or health care provider right away if any of these apply to you.
Some medical conditions may interact with Detrol. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:
Some MEDICINES MAY INTERACT with Detrol. Tell your health care provider if you are taking any other medicines, especially any of the following:
This may not be a complete list of all interactions that may occur. Ask your health care provider if Detrol may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.
Use Detrol as directed by your doctor. Check the label on the medicine for exact dosing instructions.
Ask your health care provider any questions you may have about how to use Detrol.
All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:
Blurred vision; constipation; dizziness; drowsiness; dry eyes; dry mouth; headache; indigestion; stomach pain.
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, throat, or tongue; unusual hoarseness); chest pain; confusion; difficult or painful urination; disorientation; fainting; fast or irregular heartbeat; hallucinations; memory problems; severe dizziness; swelling of the hands, ankles, or feet.
This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.
See also: Detrol side effects (in more detail)
Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include difficulty breathing; difficulty urinating; dilated pupils; dry mouth; excitation; fast heartbeat; hallucinations; seizures.
Store Detrol at room temperature, between 59 and 86 degrees F (15 and 30 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Detrol out of the reach of children and away from pets.
This information is a summary only. It does not contain all information about Detrol. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.
Docmetoclo may be available in the countries listed below.
Metoclopramide hydrochloride (a derivative of Metoclopramide) is reported as an ingredient of Docmetoclo in the following countries:
International Drug Name Search
