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Capreomycin sulfate for injection
Generic name and construction:
Capreomycin sulfate for injection
The main content of this drug was capreomycin sulfate. Its contains four active contents----ⅠA,ⅠB,ⅡA and ⅡB. The essential action of contents were ⅠA and ⅠB.
The construction as follows.
Character:
White or almost white powder, odourless and tasteless, to produce moisture, easy to dissolved in water, do not dissolved in methanol, alcohol, acetone, ether and chloroform etc. PH4-8 in water.It was more stabilize; but it was less stabilize in strong acid and strong base. The character, color, transparency, PH and sterility of ampoule preparation were accord with quality standard after three years. In door temperature , the total content and content of capreomycin 1 were not decreased. No degration production.
Pharmacology:
The antibiotics mechanism of capreomycin unknown yet, but its construction was similar viomycin and between them had cross resistance; so that it had been estimated the antibiotics mechanism of capreomycin as same as aminoglycoside. Capreomycin may be combined with ribosome of tubercle bacillus that may be influence the synthesia of bacterial proteins. It could be introduced the inhibit and eliminate effect.
Antibiotics experiment in vitro: The MIC for H37RV was 3.1-4.0mg/L. The most lowest MIC was 1.6mg/L. According to the resistant limit was over 10mg/L, the resistance of capreomycin was lower, about 0.8-2.4 % in China. Resistant streptomycin bacilli was sensitive for capreomycin yet. Capraeomycin was the slow resisrant drug.. However, when capraeomycin was use as single, it was easy to produce resistance.
Inhibit experiment In vitro shows that the inhibit effect was better for partial Grams positive coccus as streptococcus pneumonia, B-streptococcus and partial Grams negative bacilli. As bacilli pneumonia. However, the inhibit effect was more strong for coccus.
The LD50 of capreomycin by intravenous drip was 172.9mg/L, by hypoderma was 1189.6mg/L It was as same as British sample. Capreomycin was no influence for fertility, no malformation had happenings.
Pharmacokinetics:
The absorption by gastro-intestinal tract of capreomycin was very few. So it must be injection.
The serum drug concentration can become peak value with muscular injection in health person after 1-2 hours. The mean level was 28-32mg/L.Half-life was 3-6 hours. The MIC was continued at 8 hours yet.
The excretion of capreomycin mainly by urine, closing 12 hours there were 50-60% excretion by urine in perform.
The drug concentration was 2mg/L in urine after three hours by muscular injection. After 12 hours was 0.32mg/L. The t1/2 was elongated in patients with renal function disturbance, capreomycin may be accumulated in serum.
Capreomycin 1.0gm ad normal saline 250ml by intravenous drip, 60 droplet per minute, 70 minutes end all. Two hours after drip end, the serum drug concentration was 124-302mg/L. It was more three times than muscular injection ; however , the serum drug concentration was decreased to zero after 4 hours by intravenous drip.
The serum drug concentration sustained time by intravenous drip more shorter the muscular injection.
Indication:
Adopt to therapy pulmonary tuberculosis that antituberculosis routine therapy had failure by first line antituberculous drugs , toxic effect or resistance by first line antituberculous drugs.
Capreomycin was use single may be produced resistance rapidly. So it must be combined with other antituberculous drugs when it use to therapy tuberculosis.
Method and dosage:
Initial 2-4 months by QD, sequence by BIW.
Muscular injection: 0..75-1.0gm ad sterile dist water 2-4ml to dissolved it. Once a day by muscular deeper injection.
Intravenous drip: 1.0gm [If body weight <55 Kg, use 0.75gm once a day] ad normal saline 250ml by intravenous drip ,60 droplet per minute, once a day. The total dose do not over 20mg/L per day.
Side effect:
1, Local pain or nodule by muscular injection, so it must be muscular deeper injection.
2, During intravenous drip may be appeared local phlebitis, hypokalcemia, blood pressure transient decreased, hypocalcemia, hypomagnesemia, so that must be examined serum electrolytes.
3,Renal function damage: Slight increased of BUN, when large high dose was use may be injured renal tissue that the signs as hematurea, urine volume decreased, anorexia, very thirsty etc. were appeared. These side effects were severe and must be concerned.
4, Hearing disturbance: Tinnitus,hypocusis, staggering gait, vertigo. If capreomycin combined Gentamycin will be aggravated hypocusis. These two drugs combined use will not allowed.
5, Electrolytes disturbance: The reabsorption of K and Mg will be decreased by renal tubule damaged that may be introduced hypokalcemia and hypomagnesemia. Its sign as asthenia, somnolentia, pulse weakness, cardiac arrhythemia, dyspnea, abdominal distended, nausea, vomiting etc. Hypocalcemia may be appeared convulsion and/or spasm of musculars.
6, Rash and fever by drug may be appeared in a few patients.
7, Cardiac arrhythemia, psychic disturbance and headache etc. symptoms may be appeared occasionally.
Contraindication: Patients with hypersensitivity for capreomycin.
Special precaution:
1, Capreomycin combined with drugs as toxic for renal, muscular block and toxic for ear as aminoglycoside antibiotics, polymyxin B, amphotericin B, vancomycin, cisplatin, furosemide and carmustine etc.
2, Capreomycin combined with analgerics drugs as opium could be aggravated the inhibition for respiratory center. It must be observed and supervised.
3, Capreomycin must be precaution in patients with renal function disturbance,dehydration, hypoacusis, myasthenia gravis and Parkinson disease.
4, It's necessary to full consider the benefit and trouble in pregnancy.
5, When therapy course of capreomycin must be examined on time----audition, vestibule function, renal function, hepatic function and serum calcium concentration. If hypoacusis or renal function damage were appeared, capreomycin must be stopped on time.
6, The dosage must be decreased in olds.
Contraindication: To interdict to use capreomycin for injection to the anaphylactic patient.
Specification:
1, 0.5gm [500 thousand units].
2, 0.75gm[750 thousand unites].
3, 1g[1000 thousand unites].
Packing: 20 ampoules per box.
Store: close, preserved in cold and dry place.
Effective time: Three years [temporary].
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