Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/2384
Predicate | Object |
---|---|
rdf:type | |
rdfs:label |
Capastat sulfate (Injection, Powder, For Solution)
|
dailymed-instance:dosage |
Capastat Sulfate may
be administered intramuscularly or intravenously following reconstitution.
Reconstitution is achieved by dissolving the vial contents (1 g)
in 2 mL of 0.9% Sodium Chloride Injection
or Sterile Water for Injection. Two to 3 minutes should be
allowed for complete dissolution. Intravenously���For intravenous infusion, reconstituted Capastat Sulfate should
be diluted in 100 mL of 0.9% Sodium Chloride
Injection and administered over 60 minutes. Intramuscularly���Reconstituted Capastat Sulfate should
be given by deep intramuscular injection into a large muscle mass, since superficial
injection may be associated with increased pain and the development of sterile
abscesses. For administration of a 1���g dose, the
entire contents of the vial should be given. For doses lower than 1 g,
the following dilution table may be used. The solution may acquire a pale straw color and darken with
time, but this is not associated with loss of potency or the development of
toxicity. After reconstitution, all solutions of Capastat Sulfate may
be stored for up to 24 hours under refrigeration. Capreomycin is
always administered in combination with at least 1 other
antituberculosis agent to which the patient's strain of tubercle bacilli
is susceptible. The usual dose is 1 g daily (not to exceed
20 mg/kg/day) given intramuscularly or intravenously for
60 to 120 days, followed by 1 g
by either route 2 or 3 times weekly. (Note���Therapy for tuberculosis should be maintained for 12 to 24 months.
If facilities for administering injectable medication are not available, a
change to appropriate oral therapy is indicated on the patient's release
from the hospital.) Patients with reduced renal function should have dosage reduction
based on creatinine clearance using the guidelines included in Table 1.
These dosages are designed to achieve a mean steady���state capreomycin level
of 10��g/mL. Parenteral drug products should be inspected visually for particulate
matter and discoloration prior to administration, whenever solution and container
permit.
|
dailymed-instance:descripti... |
Capastat Sulfate is
a polypeptide antibiotic isolated from Streptomyces capreolus. It is a complex of 4 microbiologically
active components which have been characterized in part; however, complete
structural determination of all the components has not been established. Capreomycin is supplied as the disulfate salt and is soluble in water. In complete solution,
it is almost colorless. Each vial contains the equivalent of 1 g capreomycin activity. The structural formula is as follows:
|
dailymed-instance:clinicalP... |
Human
Pharmacology: Capreomycin is
not absorbed in significant quantities from the gastrointestinal tract and
must be administered parenterally. In 2 studies of 10 patients
each, peak serum concentrations following 1 g of capreomycin given
intramuscularly were achieved 1 to 2 hours
after administration, and average peak levels reached were 28 and
32��g/mL respectively (range, 20 to
47��g/mL). Low serum concentrations were present at 24 hours.
However, 1 g of capreomycin daily for 30 days or more produced no significant accumulation
in subjects with normal renal function. Two patients with marked reduction
of renal function had high serum concentrations 24 hours
after administration of the drug. When a 1���g dose of capreomycin was
given intramuscularly to normal volunteers, 52% was excreted
in the urine within 12 hours. Lehmann, et al,
examined the pharmacokinetics of single dose capreomycin (1.0 g)
administered intramuscularly and by intravenous infusion (1 hour)
in 6 healthy volunteers. The area under the serum concentration
versus time curve was similar for the two routes of administration. Capreomycin peak
concentrations after intravenous infusion were 30��47%
higher than after intramuscular administration. Paper chromatographic
studies indicated that capreomycin is excreted essentially unaltered. Urine concentrations averaged 1.68 mg/mL
(average urine volume, 228 mL) during the 6 hours
following a 1���g dose.<br/>Microbiology: Capreomycin is active against strains of Mycobacterium
tuberculosis found in humans.<br/>Susceptibility
Tests: The in vitro susceptibility of strains of M. tuberculosis to capreomycin varies
with the media and techniques employed. In general, the minimum inhibitory
concentrations for M. tuberculosis are
lowest in liquid media that are free of egg protein (7H10 or
Dubos) and range from 1 to 5��g/mL
when the indirect method is used. Comparable inhibitory concentrations are
obtained when 7H10 agar is used for direct susceptibility
testing. When indirect susceptibility tests are performed on standard tube
slants with 7H10 media, susceptible strains are inhibited
by 10 to 25��g/mL capreomycin.
Egg-containing media, such as L��wenstein-Jensen or ATS,
require concentrations of 25 to 50��g/mL
to inhibit susceptible strains.<br/>Cross���Resistance: Frequent cross-resistance occurs between capreomycin and
viomycin. Varying degrees of cross-resistance between capreomycin and
kanamycin and neomycin have been reported. No cross-resistance has been observed
between capreomycin and
isoniazid, aminosalicylic acid, cycloserine, streptomycin, ethionamide, or
ethambutol.
|
dailymed-instance:activeIng... | |
dailymed-instance:supply |
Capastat Sulfate, Capreomycin for
Injection, USP, is available in: Vials: 1 g,
10 mL size (No. 718) (1s) NDC 0002-1485-01 _________ Store at controlled room temperature 15��to 30��C
(59��to 86��F) prior to reconstitution.
|
dailymed-instance:boxedWarn... |
WARNINGS: The use of Capastat Sulfate (Capreomycin for
Injection, USP) in patients with renal insufficiency or preexisting
auditory impairment must be undertaken with great caution, and the risk of
additional cranial nerve VIII impairment or renal injury
should be weighed against the benefits to be derived from therapy. Refer to ANIMAL PHARMACOLOGY for additional information. Since other parenteral antituberculosis agents (streptomycin, viomycin)
also have similar and sometimes irreversible toxic effects, particularly on
cranial nerve VIII and renal function, simultaneous administration
of these agents with Capastat Sulfate is
not recommended. Use with nonantituberculosis drugs (polymyxin A
sulfate, colistin sulfate, amikacin, gentamicin, tobramycin, vancomycin, kanamycin,
and neomycin) having ototoxic or nephrotoxic potential should be undertaken
only with great caution. Usage in Pregnancy: The
safety of the use of Capastat Sulfate in
pregnancy has not been determined. Pediatric Usage: Safety
and effectiveness in pediatric patients have not been established.
|
dailymed-instance:activeMoi... | |
dailymed-instance:precautio... |
General: Audiometric measurements and assessment of vestibular function should
be performed prior to initiation of therapy with Capastat Sulfate and
at regular intervals during treatment. Renal injury, with tubular necrosis, elevation of the blood urea nitrogen (BUN)
or serum creatinine, and abnormal urinary sediment, has been noted. Slight
elevation of the BUN and serum creatinine has been observed in a significant
number of patients receiving prolonged therapy. The appearance of casts, red
cells, and white cells in the urine has been noted in a high percentage of
these cases. Elevation of the BUN above 30 mg/100 mL
or any other evidence of decreasing renal function with or without a rise
in BUN levels calls for careful evaluation of the patient, and the dosage
should be reduced or the drug completely withdrawn. The clinical significance
of abnormal urine sediment and slight elevation in the BUN (or serum creatinine)
observed during long-term therapy with Capastat Sulfate has
not been established. The peripheral neuromuscular blocking action that has been attributed
to other polypeptide antibiotics (colistin sulfate, polymyxin A
sulfate, paromomycin, and viomycin) and to aminoglycoside antibiotics (streptomycin,
dihydrostreptomycin, neomycin, and kanamycin) has been studied with Capastat Sulfate. A
partial neuromuscular blockade was demonstrated after large intravenous doses
of Capastat Sulfate. This
action was enhanced by ether anesthesia(as has been reported for neomycin)
and was antagonized by neostigmine. Caution should be exercised in the administration of antibiotics, including Capastat Sulfate, to
any patient who has demonstrated some form of allergy, particularly to drugs.<br/>Laboratory
Tests: Regular tests of renal function should be made throughout the period
of treatment, and reduced dosage should be employed in patients with known
or suspected renal impairment. Renal function studies should be made both before therapy with Capastat Sulfate is
started and on a weekly basis during treatment. Since hypokalemia, hypomagnesemia and hypocalcemia may occur during therapy, these serum electrolyte levels should be determined frequently.<br/>Drug
Interactions: For neuromuscular blocking action of this drug, see PRECAUTIONS,
GENERAL.<br/>Carcinogenesis,
Mutagenesis, Impairment of Fertility: Studies have not been performed to determine potential for carcinogenicity,
mutagenicity, or impairment of fertility.<br/>Usage
in Pregnancy���Pregnancy Category C: Capastat Sulfate has
been shown to be teratogenic in rats when given in doses 3 1/2 times
the human dose. There are no adequate and well-controlled studies in pregnant
women. Capastat Sulfate should
be used during pregnancy only if the potential benefit justifies the potential
risk to the fetus (see
boxed WARNINGS and ANIMAL PHARMACOLOGY).<br/>Nursing
Mothers: It is not known whether this drug is excreted in human milk. Because
many drugs are excreted in human milk, caution should be exercised when Capastat Sulfate is
administered to a nursing woman.<br/>Pediatric
Use: Safety and effectiveness in pediatric patients have not been established
.<br/>Geriatric
Use: Clinical studies of Capastat Sulfate did
not analyze the safety and efficacy of patients aged 65 and over to determine
whether they respond differently from younger patients. Other reported clinical
experience has not identified differences in responses between the elderly
and younger patients. In general, dose selection for an elderly patient should
be cautious, usually starting at the low end of the dosing range, reflecting
the greater frequency of decreased hepatic, renal, or cardiac function, and
of concomitant disease or other drug therapy. Capastat Sulfate is
known to be substantially excreted by the kidney (see CLINICAL
PHARMACOLOGY), and the risk of toxic reactions to this drug
may be greater in patients with impaired renal function. Because elderly patients
are more likely to have decreased renal function, care should be taken in
dose selection, and it may be useful to monitor renal function .
Patients with reduced renal function should have dosage reduction based on
creatinine clearance using the guidelines included in Table 1 (see DOSAGE
AND ADMINISTRATION). The geriatric population is also more likely to have impaired hearing
at baseline. Audiometric measurements and assessment of vestibular function
should be performed prior to initiation of therapy with Capastat Sulfate and
at regular intervals during treatment (see PRECAUTIONS,
General).
|
dailymed-instance:overdosag... |
Signs
and Symptoms: Nephrotoxicity
following the parenteral administration of Capastat Sulfate is
most closely related to the area under the curve of the serum concentration
versus time graph. The elderly patient, patients with abnormal renal function
or dehydration, and patients receiving other nephrotoxic drugs are at much
greater risk for developing acute tubular necrosis. Damage
to the auditory and vestibular divisions of cranial nerve VIII
has been associated with Capastat Sulfate given
to patients with abnormal renal function or dehydration and in those receiving
medications with additive auditory toxicities. These patients often experience
dizziness, tinnitus, vertigo, and a loss of high���tone acuity. Neuromuscular
blockage or respiratory paralysis may occur following rapid intravenous infusion. If capreomycin is
ingested, toxicity would be unlikely because it is poorly absorbed (less than 1%)
from an intact gastrointestinal system. Hypokalemia,
hypocalcemia, hypomagnesemia, and an electrolyte disturbance resembling Bartter's
syndrome have been reported to occur in patients with capreomycin toxicity. The
subcutaneous median lethal dose in mice was 514 mg/kg.<br/>Treatment: To
obtain up-to-date information about the treatment of overdose, a good resource
is your certified Regional Poison Control Center. Telephone numbers of certified
poison control centers are listed in the Physicians' Desk Reference (PDR). In managing
overdosage, consider the possibility of multiple drug overdoses, interaction
among drugs, and unusual drug kinetics in your patient. Protect
the patient's airway and support ventilation and perfusion. Meticulously
monitor and maintain, within acceptable limits, the patient's vital
signs, blood gases, serum electrolytes, etc. Absorption of drugs from the
gastrointestinal tract may be decreased by giving activated charcoal, which,
in many cases, is more effective than emesis or lavage; consider charcoal
instead of or in addition to gastric emptying. Repeated doses of charcoal
over time may hasten elimination of some drugs that have been absorbed. Safeguard
the patient's airway when employing gastric emptying or charcoal. Patients
who have received an overdose of capreomycin and have normal renal function should be carefully hydrated to maintain
a urine output of 3 to 5 mL/kg/h. Fluid
balance, electrolytes, and creatinine clearance should be carefully monitored. Hemodialysis
may be effectively used to remove capreomycin in patients with significant renal disease.
|
dailymed-instance:genericMe... |
Capreomycin sulfate
|
dailymed-instance:fullName |
Capastat sulfate (Injection, Powder, For Solution)
|
dailymed-instance:adverseRe... |
Nephrotoxicity: In
36% of 722 patients treated with Capastat Sulfate,
elevation of the BUN above 20 mg/100 mL
has been observed. In many instances, there was also depression of PSP excretion
and abnormal urine sediment. In 10% of this series, the BUN
elevation exceeded 30 mg/100 mL. Toxic nephritis was reported in 1 patient
with tuberculosis and portal cirrhosis who was treated with Capastat Sulfate (1 g)
and aminosalicylic acid daily for 1 month. This patient developed
renal insufficiency and oliguria and died. Autopsy showed subsiding acute
tubular necrosis. Electrolyte disturbances including hypokalemia, hypomagnesemia and hypocalcemia, sometimes serious in nature, have been reported. Ototoxicity: Subclinical
auditory loss was noted in approximately 11% of 722 patients
undergoing treatment with Capastat Sulfate. This
was a 5���to 10���decibel loss in the 4000���to 8000���CPS
range. Clinically apparent hearing loss occurred in 3% of the 722 subjects.
Some audiometric changes were reversible. Other cases with permanent loss
were not progressive following withdrawal of Capastat Sulfate. Tinnitus and vertigo have occurred. Liver: Serial
tests of liver function have demonstrated a decrease in BSP excretion without
change in AST (SGOT) or ALT (SGPT) in the
presence of preexisting liver disease. Abnormal results in liver function
tests have occurred in many persons receiving Capastat Sulfate in
combination with other antituberculosis agents that also are known to cause
changes in hepatic function. The role of Capastat Sulfate in
producing these abnormalities is not clear; however, periodic determinations
of liver function are recommended. Blood: Leukocytosis
and leukopenia have been observed. The majority of patients treated have had
eosinophilia exceeding 5% while receiving daily injections
of Capastat Sulfate. This
has subsided with reduction of the Capastat Sulfate dosage
to 2 or 3 g weekly. Pain and induration at the injection site
have been observed. Excessive bleeding at the injection site has been reported.
Sterile abscesses have been noted. Rare cases of thrombocytopenia have been
reported. Hypersensitivity: Urticaria
and maculopapular skin rashes associated in some cases with febrile reactions
have been reported when Capastat Sulfate and
other antituberculosis drugs were given concomitantly.
|
dailymed-instance:warning |
The use of Capastat Sulfate (Capreomycin for
Injection, USP) in patients with renal insufficiency or preexisting
auditory impairment must be undertaken with great caution, and the risk of
additional cranial nerve VIII impairment or renal injury
should be weighed against the benefits to be derived from therapy. Refer to ANIMAL PHARMACOLOGY for additional information. Since other parenteral antituberculosis agents (streptomycin, viomycin)
also have similar and sometimes irreversible toxic effects, particularly on
cranial nerve VIII and renal function, simultaneous administration
of these agents with Capastat Sulfate is
not recommended. Use with nonantituberculosis drugs (polymyxin A
sulfate, colistin sulfate, amikacin, gentamicin, tobramycin, vancomycin, kanamycin,
and neomycin) having ototoxic or nephrotoxic potential should be undertaken
only with great caution. Usage in Pregnancy: The
safety of the use of Capastat Sulfate in
pregnancy has not been determined. Pediatric Usage: Safety
and effectiveness in pediatric patients have not been established.
|
dailymed-instance:indicatio... |
Capastat Sulfate, which
is to be used concomitantly with other appropriate antituberculosis agents,
is indicated in pulmonary infections caused by capreomycin���susceptible
strains of M. tuberculosis when
the primary agents (isoniazid, rifampin, ethambutol, aminosalicylic acid,
and streptomycin) have been ineffective or cannot be used because of toxicity
or the presence of resistant tubercle bacilli. Susceptibility studies should be performed to determine the presence
of a capreomycin���susceptible
strain of M. tuberculosis.
|
dailymed-instance:represent... | |
dailymed-instance:routeOfAd... | |
dailymed-instance:name |
Capastat sulfate
|